entrectinib (Rx)

Non-small Cell Lung Cancer

Indicated for metastatic non-small cell lung cancer (NSCLC) in adults whose tumors are ROS1-positive

600 mg PO qDay

Continue until disease progression or unacceptable toxicity

Neurotrophic Tyrosine Receptor Kinase Gene Fusion Solid Tumors

Indicated for patients with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and progressed following treatment or have no satisfactory alternative therapy

600 mg PO qDay

Continue until disease progression or unacceptable toxicity

Dosage Modifications

Dosage modifications for adverse reactions

• First dose reduction: 400 mg qDay
• Second dose reduction: 200 mg qDay
• Permanently discontinue if toxicities persist or recur following 2 dose reductions

Congestive heart failure

• Grade 2 or 3: Withhold until recovered to Grade ≤1; resume at reduced dose
• Grade 4: Permanently discontinue

Central nervous system effects

• Intolerable Grade 2: Withhold until recovered to Grade ≤1; resume at reduced dose, as clinically appropriate
• Grade 3: Withhold until recovered to Grade ≤1; resume at reduced dose
• Grade 4: Permanently discontinue

Hepatoxicity

• Grade 3
  • Withhold until recovered to Grade ≤1; resume at reduced dose;
  • If resolution occurs within 4 weeks, resume at same dose
  • If adverse reaction persists after 4 weeks, permanently discontinue
  • For recurrent Grade 3 events that resolve within 4 weeks, resume at a reduced dose

• Grade 4

  • Withhold until recovered to Grade ≤1; resume at reduce dose;
  • If adverse reaction does not resolve within 4 weeks or Grade 4 events recurs, permanently discontinue

• Elevated ALT or AST

  • ALT or AST >3x ULN with concurrent total bilirubin >1.5x ULN (in the absence of cholestasis or hemolysis): Permanently discontinue

Hyperuricemia

• Symptomatic or Grade 4: Initiate urate-lowering therapy; withhold until improvement of signs or symptoms; resume at same or reduced dose

QTc prolongation

• QTc >500 ms

  • Withhold until QTc interval recovers to baseline
  • Resume at same dose if causes of QT prolongation are identified and corrected
  • Resume at reduced dose if other causes of QT prolongation are not identified

• Life-threatening arrhythmia

  • Torsade de pointes; polymorphic ventricular tachycardia; signs/symptoms of serious arrhythmia: Permanently discontinue

Vision disorders

• Grade ≥2: Withhold until improvement or stabilization; resume at same dose or reduced dose, as clinically appropriate

Anemia or neutropenia

• Grade 3 or 4: Withhold until recovery to Grade≤2; resume at same or reduced dose, as clinically appropriate

Other clinically relevant adverse reactions

• Grade 3 or 4

  • Withhold until adverse reaction resolves to Grade 1 or baseline
  • Resume at same or reduced dose if resolved within 4 weeks
  • Permanently discontinue if adverse reaction does not resolve within 4 weeks or Grade 4 events recurs

Coadministration of moderate and strong CYP3A inhibitors

• Avoid coadministration

• If coadministration is unavoidable, reduce entrectinib dose as follows:

  • Moderate CYP3A Inhibitors: 200 mg PO qDay
  • Strong CYP3A Inhibitors: 100 mg PO qDay
  • After discontinuation of strong or moderate CYP3A inhibitor for 3-5 elimination half-lives, resume entrectinib dose taken prior to initiating the CYP3A inhibitor

Renal impairment

• Mild-to-moderate (CrCl 30 to <90 mL/min): No dosage adjustment necessary
• Severe (CrCl <30 mL/min): Not studied

Hepatic impairment

• Mild (total bilirubin ≤1.5x ULN): No dosage adjustment necessary
• Moderate-to-severe (total bilirubin >1.5x ULN): Not studied

Dosing Considerations

Patient selection

• Select patients for treatment based on the following:

  • NSCLC: Presence of ROS1 rearrangement
  • Locally advanced or metastatic solid tumors: Presence of a NTRK gene fusion
  • FDA-approved tests for detecting ROS1 rearrangement for NSCLC and NTRK gene fusion in solid tumors are not available

Neurotrophic Tyrosine Receptor Kinase Gene Fusion Solid Tumors

Indicated for adult and pediatric patients (≥12 years) with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and progressed following treatment or have no satisfactory alternative therapy

<12 years: Safety and efficacy not established

≥12 years

• Recommended dosage is based on body surface area (BSA)

  • 0.91-1.1 m²: 400 mg PO qDay
  • 1.11-1.5 m²: 500 mg PO qDay
  • >1.5 m²: 600 mg PO qDay

Continue until disease progression or unacceptable toxicity

Dosage Modifications

Dosage modifications of adverse reactions

• BSA 0.91-1.1 m2

  • First dose reduction: 300 mg qDay
  • Second dose reduction: 200 mg qDay

• BSA >1.11 m2

  • First dose reduction: 400 mg qDay
  • Second dose reduction: 200 mg qDay
• If toxicities persist or recur following 2 dose reductions, permanently discontinue

Congestive heart failure

• Grade 2 or 3: Withhold until recovered to Grade ≤1; resume at reduced dose
• Grade 4: Permanently discontinue

Central nervous system effects

• Intolerable Grade 2: Withhold until recovered to Grade ≤1; resume at reduced dose, as clinically appropriate
• Grade 3: Withhold until recovered to Grade ≤1; resume at reduced dose
• Grade 4: Permanently discontinue

Hepatoxicity

• Grade 3

  • Withhold until recovered to Grade ≤1
  • If resolution occurs within 4 weeks, resume at same dose
  • If adverse reaction persists after 4 weeks, permanently discontinue
  • For recurrent Grade 3 events that resolve within 4 weeks, resume at reduced dose

• Grade 4

  • Withhold until recovered to Grade ≤1If resolution occurs within 4 weeks, resume at reduced dose
  • If adverse reaction does not resolve within 4 weeks or Grade 4 events recurs, permanently discontinue

• Elevated ALT or AST

  • ALT or AST >3x ULN with concurrent total bilirubin >1.5x ULN (in the absence of cholestasis or hemolysis): Permanently discontinue

Hyperuricemia

• Symptomatic or Grade 4: Initiate urate-lowering therapy; withhold until improvement of signs or symptoms; resume at same or reduced dose

QTc prolongation

• QTc >500 ms

  • Withhold until QTc interval recovers to baseline
  • Resume at same dose if causes of QT prolongation are identified and corrected
  • Resume at reduced dose if other causes of QT prolongation are not identified

• Life-threatening arrhythmia

  • Torsade de pointes; polymorphic ventricular tachycardia; signs/symptoms of serious arrhythmia: Permanently discontinue

Vision disorders

• Grade ≥2: Withhold until improvement or stabilization; resume at same dose or reduced dose, as clinically appropriate

Anemia or neutropenia

• Grade 3 or 4: Withhold until recovery to Grade ≤2; resume at same or reduced dose, as clinically appropriate

Other clinically relevant adverse reactions

• Grade 3 or 4

  • Withhold until adverse reaction resolves to Grade 1 or baseline
  • Resume at same or reduced dose if resolved within 4 weeks
  • Permanently discontinue if adverse reaction does not resolve within 4 weeks or Grade 4 events recurs

Coadministration of moderate and strong CYP3A inhibitors

• Avoid coadministration

• If coadministration is unavoidable, reduce entrectinib dose as follows:

  • Moderate CYP3A Inhibitors: 200 mg PO qDay
  • Strong CYP3A Inhibitors: 100 mg PO qDay
  • After discontinuation of strong or moderate CYP3A inhibitor for 3-5 elimination half-lives, resume entrectinib dose taken prior to initiating the CYP3A inhibitor

Renal impairment

• Mild-to-moderate (CrCl 30 to <90 mL/min): No dosage adjustment necessary
• Severe (CrCl <30 mL/min): Not studied

Hepatic impairment

• Mild (total bilirubin ≤1.5x ULN): No dosage adjustment necessary
• Moderate-to-severe (total bilirubin >1.5x ULN): Not studied

Dosing Considerations

Patient selection

• Select patients for treatment based on the following:

  • NSCLC: Presence of ROS1 rearrangement
  • Locally advanced or metastatic solid tumors: Presence of a NTRK gene fusion
  • FDA-approved tests for detecting ROS1 rearrangement for NSCLC and NTRK gene fusion in solid tumors are not available

Contraindicated (1)

• lefamulin

  lefamulin will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lefamulin is contraindicated with CYP3A substrates know to prolong the QT interval.

Serious - Use Alternative (203)

• abametapir

  abametapir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

• adagrasib

  adagrasib, entrectinib. Either increases effects of the other by QTc interval. Avoid or Use Alternate Drug. Each drug prolongs the QTc interval, which may increased the risk of Torsade de pointes, other serious arryhthmias, and sudden death. If coadministration unavoidable, more frequent monitoring is recommended for such patients.

• alfuzosin

  alfuzosin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• amiodarone

  amiodarone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  amiodarone will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• amisulpride

  entrectinib and amisulpride both increase QTc interval. Avoid or Use Alternate Drug. ECG monitoring is recommended if coadministered.

• anagrelide

  anagrelide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• apalutamide

  apalutamide will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• apomorphine

  apomorphine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• aprepitant

  aprepitant will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• aripiprazole

  aripiprazole and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• armodafinil

  armodafinil will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• arsenic trioxide

  arsenic trioxide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• artemether

  artemether and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• asenapine

  asenapine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• asenapine transdermal

  asenapine transdermal and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• atazanavir

  atazanavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• atomoxetine

  atomoxetine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• bedaquiline

  entrectinib and bedaquiline both increase QTc interval. Avoid or Use Alternate Drug.

• bexarotene

  bexarotene will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• bicalutamide

  bicalutamide will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• bosentan

  bosentan will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• brigatinib

  brigatinib will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• buprenorphine

  entrectinib and buprenorphine both increase QTc interval. Avoid or Use Alternate Drug.

• buprenorphine buccal

  buprenorphine buccal and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• buprenorphine subdermal implant

  buprenorphine subdermal implant and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• buprenorphine transdermal

  buprenorphine transdermal and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• buprenorphine, long-acting injection

  buprenorphine, long-acting injection and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• carbamazepine

  carbamazepine will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• ceritinib

  ceritinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.
  
  ceritinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• chloramphenicol

  chloramphenicol will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• chloroquine

  chloroquine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• chlorpromazine

  chlorpromazine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• ciprofloxacin

  ciprofloxacin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• citalopram

  citalopram and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• clarithromycin

  clarithromycin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  clarithromycin will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• clobazam

  clobazam will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• clofazimine

  clofazimine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• clotrimazole

  clotrimazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• clozapine

  clozapine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• cobicistat

  cobicistat will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• conivaptan

  conivaptan will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• crizotinib

  crizotinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  crizotinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• cyclosporine

  cyclosporine will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• dabrafenib

  dabrafenib will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• darunavir

  darunavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• dasatinib

  dasatinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• degarelix

  degarelix and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• desflurane

  desflurane and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• desipramine

  desipramine will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• diltiazem

  diltiazem will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• disopyramide

  disopyramide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• dofetilide

  dofetilide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• dolasetron

  dolasetron and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• donepezil

  donepezil and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• doxycycline

  doxycycline will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• dronedarone

  dronedarone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  dronedarone will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• droperidol

  droperidol and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• efavirenz

  efavirenz and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  efavirenz will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• eliglustat

  eliglustat and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• encorafenib

  encorafenib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  encorafenib will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• enzalutamide

  enzalutamide will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• eribulin

  eribulin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• erythromycin base

  erythromycin base and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  erythromycin base will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• erythromycin ethylsuccinate

  erythromycin ethylsuccinate and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  erythromycin ethylsuccinate will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• erythromycin lactobionate

  erythromycin lactobionate and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  erythromycin lactobionate will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• erythromycin stearate

  erythromycin stearate and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  erythromycin stearate will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• escitalopram

  escitalopram and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• eslicarbazepine acetate

  eslicarbazepine acetate will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• etravirine

  etravirine will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• ezogabine

  ezogabine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• fexinidazole

  fexinidazole and entrectinib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels or prolong QT interval.
  
  fexinidazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

• fingolimod

  fingolimod and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• flecainide

  flecainide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• fluconazole

  fluconazole and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  fluconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• fluoxetine

  fluoxetine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• fluvoxamine

  fluvoxamine will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidabole, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.5m2. Resume previous entrectinib dose after discontinuing moderate CYP3A4 inhibitor for 3-5 elimination half-lives.
  
  entrectinib and fluvoxamine both increase QTc interval. Avoid or Use Alternate Drug.

• formoterol

  formoterol and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• fosamprenavir

  fosamprenavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• fosaprepitant

  fosaprepitant will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• foscarnet

  entrectinib and foscarnet both increase QTc interval. Avoid or Use Alternate Drug.

• fosphenytoin

  fosphenytoin will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• fostamatinib

  fostamatinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• gemifloxacin

  gemifloxacin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• gemtuzumab

  gemtuzumab and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• gilteritinib

  entrectinib and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

• glasdegib

  glasdegib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• goserelin

  goserelin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• granisetron

  granisetron and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• grapefruit

  grapefruit will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid grapefruit products with entrectinib, a CYP3A4 substrate.

• haloperidol

  haloperidol and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  haloperidol will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• histrelin

  histrelin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• hydroxychloroquine sulfate

  hydroxychloroquine sulfate and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• hydroxyzine

  entrectinib and hydroxyzine both increase QTc interval. Avoid or Use Alternate Drug.

• ibutilide

  ibutilide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• idelalisib

  idelalisib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• iloperidone

  iloperidone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  iloperidone will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• imatinib

  imatinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• indacaterol, inhaled

  indacaterol, inhaled and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• indinavir

  indinavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• inotuzumab

  inotuzumab and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• isoflurane

  entrectinib and isoflurane both increase QTc interval. Avoid or Use Alternate Drug.

• isoniazid

  isoniazid will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• itraconazole

  itraconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.
  
  entrectinib and itraconazole both increase QTc interval. Avoid or Use Alternate Drug.

• ivosidenib

  entrectinib and ivosidenib both decrease QTc interval. Avoid or Use Alternate Drug.

• ketoconazole

  ketoconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• lapatinib

  lapatinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.
  
  lapatinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• lefamulin

  entrectinib and lefamulin both increase QTc interval. Avoid or Use Alternate Drug.

• lenvatinib

  lenvatinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• letermovir

  letermovir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• leuprolide

  leuprolide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• levofloxacin

  levofloxacin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• levoketoconazole

  levoketoconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• lithium

  entrectinib and lithium both increase QTc interval. Avoid or Use Alternate Drug.

• lofexidine

  lofexidine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• loperamide

  entrectinib and loperamide both increase QTc interval. Avoid or Use Alternate Drug.

• lopinavir

  lopinavir and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  lopinavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• lorlatinib

  lorlatinib will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• lumefantrine

  lumefantrine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• macimorelin

  entrectinib and macimorelin both increase QTc interval. Avoid or Use Alternate Drug.

• maprotiline

  entrectinib and maprotiline both increase QTc interval. Avoid or Use Alternate Drug.

• mefloquine

  entrectinib and mefloquine both increase QTc interval. Avoid or Use Alternate Drug.

• methadone

  methadone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• metronidazole

  metronidazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• midostaurin

  entrectinib and midostaurin both increase QTc interval. Avoid or Use Alternate Drug.

• mifepristone

  mifepristone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  mifepristone will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• mirtazapine

  entrectinib and mirtazapine both increase QTc interval. Avoid or Use Alternate Drug.

• mitotane

  mitotane will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• mobocertinib

  mobocertinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.

• moxifloxacin

  moxifloxacin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• nafcillin

  nafcillin will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• nefazodone

  nefazodone will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• nelfinavir

  nelfinavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• netupitant/palonosetron

  netupitant/palonosetron will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• nilotinib

  nilotinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• octreotide

  entrectinib and octreotide both increase QTc interval. Avoid or Use Alternate Drug.

• ofloxacin

  ofloxacin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• olanzapine

  olanzapine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• ondansetron

  entrectinib and ondansetron both increase QTc interval. Avoid or Use Alternate Drug.

• osimertinib

  osimertinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• oxaliplatin

  entrectinib and oxaliplatin both increase QTc interval. Avoid or Use Alternate Drug.

• paliperidone

  paliperidone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• panobinostat

  panobinostat and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• pasireotide

  pasireotide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• pazopanib

  pazopanib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• pentamidine

  pentamidine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• phenobarbital

  phenobarbital will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• phenytoin

  phenytoin will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• pimavanserin

  pimavanserin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• pimozide

  pimozide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• pitolisant

  pitolisant and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• ponesimod

  entrectinib and ponesimod both increase QTc interval. Avoid or Use Alternate Drug.

• posaconazole

  posaconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.
  
  entrectinib and posaconazole both increase QTc interval. Avoid or Use Alternate Drug.

• primaquine

  primaquine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• primidone

  primidone will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• procainamide

  procainamide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• promethazine

  entrectinib and promethazine both decrease QTc interval. Avoid or Use Alternate Drug.

• propafenone

  propafenone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• quetiapine

  quetiapine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• quinidine

  quinidine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• quinine

  quinine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• quinupristin/dalfopristin

  quinupristin/dalfopristin will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• ranolazine

  ranolazine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• ribociclib

  ribociclib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  ribociclib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• rifabutin

  rifabutin will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• rifampin

  rifampin will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• rifapentine

  rifapentine will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• rilpivirine

  entrectinib and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.

• risperidone

  risperidone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• ritonavir

  ritonavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• romidepsin

  romidepsin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• saquinavir

  saquinavir and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  saquinavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• schisandra

  schisandra will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• secobarbital

  secobarbital will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• sertraline

  sertraline will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.
  
  entrectinib and sertraline both increase QTc interval. Avoid or Use Alternate Drug.

• sevoflurane

  entrectinib and sevoflurane both increase QTc interval. Avoid or Use Alternate Drug.

• siponimod

  entrectinib and siponimod both increase QTc interval. Avoid or Use Alternate Drug.

• solifenacin

  entrectinib and solifenacin both increase QTc interval. Avoid or Use Alternate Drug.

• sorafenib

  sorafenib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• sotalol

  sotalol and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• stiripentol

  stiripentol will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• sunitinib

  sunitinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• tacrolimus

  entrectinib and tacrolimus both increase QTc interval. Avoid or Use Alternate Drug.

• telavancin

  telavancin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• telotristat ethyl

  telotristat ethyl will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• tetrabenazine

  tetrabenazine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• tetracycline

  tetracycline will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• thioridazine

  thioridazine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• tipranavir

  tipranavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• toremifene

  toremifene and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• trazodone

  trazodone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• triclabendazole

  triclabendazole and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• triptorelin

  triptorelin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• tucatinib

  tucatinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

• umeclidinium bromide/vilanterol inhaled

  entrectinib and umeclidinium bromide/vilanterol inhaled both decrease QTc interval. Avoid or Use Alternate Drug.

• vandetanib

  vandetanib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• vardenafil

  entrectinib and vardenafil both increase QTc interval. Avoid or Use Alternate Drug.

• vemurafenib

  vemurafenib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• venlafaxine

  entrectinib and venlafaxine both decrease QTc interval. Avoid or Use Alternate Drug.

• verapamil

  verapamil will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• voriconazole

  voriconazole and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  voriconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• vorinostat

  entrectinib and vorinostat both increase QTc interval. Avoid or Use Alternate Drug.

• voxelotor

  voxelotor will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

• ziprasidone

  ziprasidone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

Monitor Closely (38)

• albuterol

  albuterol and entrectinib both increase QTc interval. Use Caution/Monitor.

• amitriptyline

  entrectinib and amitriptyline both increase QTc interval. Use Caution/Monitor.

• arformoterol

  arformoterol and entrectinib both increase QTc interval. Use Caution/Monitor.

• azithromycin

  azithromycin increases toxicity of entrectinib by QTc interval. Use Caution/Monitor.

• belzutifan

  belzutifan will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.

• cenobamate

  cenobamate will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

• clomipramine

  entrectinib and clomipramine both increase QTc interval. Use Caution/Monitor.

• desipramine

  entrectinib and desipramine both increase QTc interval. Use Caution/Monitor.

• deutetrabenazine

  deutetrabenazine and entrectinib both increase QTc interval. Use Caution/Monitor. At the maximum recommended dose, deutetrabenazine does not prolong QT interval to a clinically relevant extent. Certain circumstances may increase risk of torsade de pointes and/or sudden death in association with drugs that prolong the QTc interval (eg, bradycardia, hypokalemia or hypomagnesemia, coadministration with other drugs that prolong QTc interval, presence of congenital QT prolongation).

• doxepin

  doxepin and entrectinib both increase QTc interval. Use Caution/Monitor.

• elagolix

  elagolix will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

• fedratinib

  fedratinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

• fluphenazine

  entrectinib and fluphenazine both increase QTc interval. Use Caution/Monitor.

• fostemsavir

  entrectinib and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.

• gadobenate

  gadobenate and entrectinib both increase QTc interval. Use Caution/Monitor.

• imipramine

  entrectinib and imipramine both increase QTc interval. Use Caution/Monitor.

• istradefylline

  istradefylline will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

• ivacaftor

  ivacaftor will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• lenacapavir

  lenacapavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir (a moderate CYP3A4 inhibitor) may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.

• levalbuterol

  entrectinib and levalbuterol both increase QTc interval. Use Caution/Monitor.

• nortriptyline

  entrectinib and nortriptyline both increase QTc interval. Use Caution/Monitor.

• olodaterol inhaled

  entrectinib and olodaterol inhaled both increase QTc interval. Use Caution/Monitor.

• osilodrostat

  osilodrostat and entrectinib both increase QTc interval. Use Caution/Monitor.

• ozanimod

  ozanimod and entrectinib both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.

• perphenazine

  entrectinib and perphenazine both increase QTc interval. Use Caution/Monitor.

• ponesimod

  ponesimod and entrectinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

• prochlorperazine

  entrectinib and prochlorperazine both decrease QTc interval. Use Caution/Monitor.

• protriptyline

  entrectinib and protriptyline both increase QTc interval. Use Caution/Monitor.

• rucaparib

  rucaparib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

• salmeterol

  entrectinib and salmeterol both increase QTc interval. Use Caution/Monitor.

• selpercatinib

  selpercatinib increases toxicity of entrectinib by QTc interval. Use Caution/Monitor.

• siponimod

  siponimod and entrectinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

• tazemetostat

  tazemetostat will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

• trifluoperazine

  entrectinib and trifluoperazine both decrease QTc interval. Use Caution/Monitor.

• trimipramine

  entrectinib and trimipramine both increase QTc interval. Use Caution/Monitor.

• valbenazine

  valbenazine and entrectinib both increase QTc interval. Use Caution/Monitor.

• vilanterol/fluticasone furoate inhaled

  entrectinib and vilanterol/fluticasone furoate inhaled both increase QTc interval. Use Caution/Monitor.

• voclosporin

  voclosporin, entrectinib. Either increases effects of the other by QTc interval. Use Caution/Monitor.

Minor (4)

• acetazolamide

  acetazolamide will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

• anastrozole

  anastrozole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

• cyclophosphamide

  cyclophosphamide will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

• larotrectinib

  larotrectinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

• abametapir

  Serious - Use Alternative (1)abametapir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

• acetazolamide

  Minor (1)acetazolamide will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

• adagrasib

  Serious - Use Alternative (1)adagrasib, entrectinib. Either increases effects of the other by QTc interval. Avoid or Use Alternate Drug. Each drug prolongs the QTc interval, which may increased the risk of Torsade de pointes, other serious arryhthmias, and sudden death. If coadministration unavoidable, more frequent monitoring is recommended for such patients.

• albuterol

  Monitor Closely (1)albuterol and entrectinib both increase QTc interval. Use Caution/Monitor.

• alfuzosin

  Serious - Use Alternative (1)alfuzosin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• amiodarone

  Serious - Use Alternative (2)amiodarone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  amiodarone will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• amisulpride

  Serious - Use Alternative (1)entrectinib and amisulpride both increase QTc interval. Avoid or Use Alternate Drug. ECG monitoring is recommended if coadministered.

• amitriptyline

  Monitor Closely (1)entrectinib and amitriptyline both increase QTc interval. Use Caution/Monitor.

• anagrelide

  Serious - Use Alternative (1)anagrelide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• anastrozole

  Minor (1)anastrozole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

• apalutamide

  Serious - Use Alternative (1)apalutamide will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• apomorphine

  Serious - Use Alternative (1)apomorphine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• aprepitant

  Serious - Use Alternative (1)aprepitant will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• arformoterol

  Monitor Closely (1)arformoterol and entrectinib both increase QTc interval. Use Caution/Monitor.

• aripiprazole

  Serious - Use Alternative (1)aripiprazole and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• armodafinil

  Serious - Use Alternative (1)armodafinil will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• arsenic trioxide

  Serious - Use Alternative (1)arsenic trioxide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• artemether

  Serious - Use Alternative (1)artemether and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• asenapine

  Serious - Use Alternative (1)asenapine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• asenapine transdermal

  Serious - Use Alternative (1)asenapine transdermal and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• atazanavir

  Serious - Use Alternative (1)atazanavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• atomoxetine

  Serious - Use Alternative (1)atomoxetine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• azithromycin

  Monitor Closely (1)azithromycin increases toxicity of entrectinib by QTc interval. Use Caution/Monitor.

• bedaquiline

  Serious - Use Alternative (1)entrectinib and bedaquiline both increase QTc interval. Avoid or Use Alternate Drug.

• belzutifan

  Monitor Closely (1)belzutifan will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.

• bexarotene

  Serious - Use Alternative (1)bexarotene will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• bicalutamide

  Serious - Use Alternative (1)bicalutamide will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• bosentan

  Serious - Use Alternative (1)bosentan will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• brigatinib

  Serious - Use Alternative (1)brigatinib will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• buprenorphine

  Serious - Use Alternative (1)entrectinib and buprenorphine both increase QTc interval. Avoid or Use Alternate Drug.

• buprenorphine buccal

  Serious - Use Alternative (1)buprenorphine buccal and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• buprenorphine subdermal implant

  Serious - Use Alternative (1)buprenorphine subdermal implant and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• buprenorphine transdermal

  Serious - Use Alternative (1)buprenorphine transdermal and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• buprenorphine, long-acting injection

  Serious - Use Alternative (1)buprenorphine, long-acting injection and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• carbamazepine

  Serious - Use Alternative (1)carbamazepine will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• cenobamate

  Monitor Closely (1)cenobamate will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

• ceritinib

  Serious - Use Alternative (2)ceritinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.
  
  ceritinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• chloramphenicol

  Serious - Use Alternative (1)chloramphenicol will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• chloroquine

  Serious - Use Alternative (1)chloroquine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• chlorpromazine

  Serious - Use Alternative (1)chlorpromazine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• ciprofloxacin

  Serious - Use Alternative (1)ciprofloxacin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• citalopram

  Serious - Use Alternative (1)citalopram and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• clarithromycin

  Serious - Use Alternative (2)clarithromycin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  clarithromycin will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• clobazam

  Serious - Use Alternative (1)clobazam will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• clofazimine

  Serious - Use Alternative (1)clofazimine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• clomipramine

  Monitor Closely (1)entrectinib and clomipramine both increase QTc interval. Use Caution/Monitor.

• clotrimazole

  Serious - Use Alternative (1)clotrimazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• clozapine

  Serious - Use Alternative (1)clozapine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• cobicistat

  Serious - Use Alternative (1)cobicistat will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• conivaptan

  Serious - Use Alternative (1)conivaptan will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• crizotinib

  Serious - Use Alternative (2)crizotinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  crizotinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• cyclophosphamide

  Minor (1)cyclophosphamide will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

• cyclosporine

  Serious - Use Alternative (1)cyclosporine will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• dabrafenib

  Serious - Use Alternative (1)dabrafenib will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• darunavir

  Serious - Use Alternative (1)darunavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• dasatinib

  Serious - Use Alternative (1)dasatinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• degarelix

  Serious - Use Alternative (1)degarelix and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• desflurane

  Serious - Use Alternative (1)desflurane and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• desipramine

  Monitor Closely (1)entrectinib and desipramine both increase QTc interval. Use Caution/Monitor.Serious - Use Alternative (1)desipramine will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• deutetrabenazine

  Monitor Closely (1)deutetrabenazine and entrectinib both increase QTc interval. Use Caution/Monitor. At the maximum recommended dose, deutetrabenazine does not prolong QT interval to a clinically relevant extent. Certain circumstances may increase risk of torsade de pointes and/or sudden death in association with drugs that prolong the QTc interval (eg, bradycardia, hypokalemia or hypomagnesemia, coadministration with other drugs that prolong QTc interval, presence of congenital QT prolongation).

• diltiazem

  Serious - Use Alternative (1)diltiazem will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• disopyramide

  Serious - Use Alternative (1)disopyramide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• dofetilide

  Serious - Use Alternative (1)dofetilide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• dolasetron

  Serious - Use Alternative (1)dolasetron and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• donepezil

  Serious - Use Alternative (1)donepezil and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• doxepin

  Monitor Closely (1)doxepin and entrectinib both increase QTc interval. Use Caution/Monitor.

• doxycycline

  Serious - Use Alternative (1)doxycycline will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• dronedarone

  Serious - Use Alternative (2)dronedarone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  dronedarone will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• droperidol

  Serious - Use Alternative (1)droperidol and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• efavirenz

  Serious - Use Alternative (2)efavirenz will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
  
  efavirenz and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• elagolix

  Monitor Closely (1)elagolix will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

• eliglustat

  Serious - Use Alternative (1)eliglustat and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• encorafenib

  Serious - Use Alternative (2)encorafenib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  encorafenib will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• enzalutamide

  Serious - Use Alternative (1)enzalutamide will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• eribulin

  Serious - Use Alternative (1)eribulin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• erythromycin base

  Serious - Use Alternative (2)erythromycin base and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  erythromycin base will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• erythromycin ethylsuccinate

  Serious - Use Alternative (2)erythromycin ethylsuccinate and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  erythromycin ethylsuccinate will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• erythromycin lactobionate

  Serious - Use Alternative (2)erythromycin lactobionate and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  erythromycin lactobionate will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• erythromycin stearate

  Serious - Use Alternative (2)erythromycin stearate and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  erythromycin stearate will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• escitalopram

  Serious - Use Alternative (1)escitalopram and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• eslicarbazepine acetate

  Serious - Use Alternative (1)eslicarbazepine acetate will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• etravirine

  Serious - Use Alternative (1)etravirine will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• ezogabine

  Serious - Use Alternative (1)ezogabine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• fedratinib

  Monitor Closely (1)fedratinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

• fexinidazole

  Serious - Use Alternative (2)fexinidazole and entrectinib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels or prolong QT interval.
  
  fexinidazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

• fingolimod

  Serious - Use Alternative (1)fingolimod and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• flecainide

  Serious - Use Alternative (1)flecainide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• fluconazole

  Serious - Use Alternative (2)fluconazole and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  fluconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• fluoxetine

  Serious - Use Alternative (1)fluoxetine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• fluphenazine

  Monitor Closely (1)entrectinib and fluphenazine both increase QTc interval. Use Caution/Monitor.

• fluvoxamine

  Serious - Use Alternative (2)fluvoxamine will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidabole, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.5m2. Resume previous entrectinib dose after discontinuing moderate CYP3A4 inhibitor for 3-5 elimination half-lives.
  
  entrectinib and fluvoxamine both increase QTc interval. Avoid or Use Alternate Drug.

• formoterol

  Serious - Use Alternative (1)formoterol and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• fosamprenavir

  Serious - Use Alternative (1)fosamprenavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• fosaprepitant

  Serious - Use Alternative (1)fosaprepitant will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• foscarnet

  Serious - Use Alternative (1)entrectinib and foscarnet both increase QTc interval. Avoid or Use Alternate Drug.

• fosphenytoin

  Serious - Use Alternative (1)fosphenytoin will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• fostamatinib

  Serious - Use Alternative (1)fostamatinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• fostemsavir

  Monitor Closely (1)entrectinib and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.

• gadobenate

  Monitor Closely (1)gadobenate and entrectinib both increase QTc interval. Use Caution/Monitor.

• gemifloxacin

  Serious - Use Alternative (1)gemifloxacin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• gemtuzumab

  Serious - Use Alternative (1)gemtuzumab and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• gilteritinib

  Serious - Use Alternative (1)entrectinib and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.

• glasdegib

  Serious - Use Alternative (1)glasdegib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• goserelin

  Serious - Use Alternative (1)goserelin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• granisetron

  Serious - Use Alternative (1)granisetron and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• grapefruit

  Serious - Use Alternative (1)grapefruit will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid grapefruit products with entrectinib, a CYP3A4 substrate.

• haloperidol

  Serious - Use Alternative (2)haloperidol and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  haloperidol will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• histrelin

  Serious - Use Alternative (1)histrelin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• hydroxychloroquine sulfate

  Serious - Use Alternative (1)hydroxychloroquine sulfate and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• hydroxyzine

  Serious - Use Alternative (1)entrectinib and hydroxyzine both increase QTc interval. Avoid or Use Alternate Drug.

• ibutilide

  Serious - Use Alternative (1)ibutilide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• idelalisib

  Serious - Use Alternative (1)idelalisib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• iloperidone

  Serious - Use Alternative (2)iloperidone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  iloperidone will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• imatinib

  Serious - Use Alternative (1)imatinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• imipramine

  Monitor Closely (1)entrectinib and imipramine both increase QTc interval. Use Caution/Monitor.

• indacaterol, inhaled

  Serious - Use Alternative (1)indacaterol, inhaled and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• indinavir

  Serious - Use Alternative (1)indinavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• inotuzumab

  Serious - Use Alternative (1)inotuzumab and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• isoflurane

  Serious - Use Alternative (1)entrectinib and isoflurane both increase QTc interval. Avoid or Use Alternate Drug.

• isoniazid

  Serious - Use Alternative (1)isoniazid will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• istradefylline

  Monitor Closely (1)istradefylline will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

• itraconazole

  Serious - Use Alternative (2)itraconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.
  
  entrectinib and itraconazole both increase QTc interval. Avoid or Use Alternate Drug.

• ivacaftor

  Monitor Closely (1)ivacaftor will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• ivosidenib

  Serious - Use Alternative (1)entrectinib and ivosidenib both decrease QTc interval. Avoid or Use Alternate Drug.

• ketoconazole

  Serious - Use Alternative (1)ketoconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• lapatinib

  Serious - Use Alternative (2)lapatinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.
  
  lapatinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• larotrectinib

  Minor (1)larotrectinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

• lefamulin

  Contraindicated (1)lefamulin will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lefamulin is contraindicated with CYP3A substrates know to prolong the QT interval.Serious - Use Alternative (1)entrectinib and lefamulin both increase QTc interval. Avoid or Use Alternate Drug.

• lenacapavir

  Monitor Closely (1)lenacapavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir (a moderate CYP3A4 inhibitor) may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.

• lenvatinib

  Serious - Use Alternative (1)lenvatinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• letermovir

  Serious - Use Alternative (1)letermovir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• leuprolide

  Serious - Use Alternative (1)leuprolide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• levalbuterol

  Monitor Closely (1)entrectinib and levalbuterol both increase QTc interval. Use Caution/Monitor.

• levofloxacin

  Serious - Use Alternative (1)levofloxacin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• levoketoconazole

  Serious - Use Alternative (1)levoketoconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• lithium

  Serious - Use Alternative (1)entrectinib and lithium both increase QTc interval. Avoid or Use Alternate Drug.

• lofexidine

  Serious - Use Alternative (1)lofexidine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• loperamide

  Serious - Use Alternative (1)entrectinib and loperamide both increase QTc interval. Avoid or Use Alternate Drug.

• lopinavir

  Serious - Use Alternative (2)lopinavir and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  lopinavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• lorlatinib

  Serious - Use Alternative (1)lorlatinib will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• lumefantrine

  Serious - Use Alternative (1)lumefantrine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• macimorelin

  Serious - Use Alternative (1)entrectinib and macimorelin both increase QTc interval. Avoid or Use Alternate Drug.

• maprotiline

  Serious - Use Alternative (1)entrectinib and maprotiline both increase QTc interval. Avoid or Use Alternate Drug.

• mefloquine

  Serious - Use Alternative (1)entrectinib and mefloquine both increase QTc interval. Avoid or Use Alternate Drug.

• methadone

  Serious - Use Alternative (1)methadone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• metronidazole

  Serious - Use Alternative (1)metronidazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• midostaurin

  Serious - Use Alternative (1)entrectinib and midostaurin both increase QTc interval. Avoid or Use Alternate Drug.

• mifepristone

  Serious - Use Alternative (2)mifepristone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  mifepristone will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• mirtazapine

  Serious - Use Alternative (1)entrectinib and mirtazapine both increase QTc interval. Avoid or Use Alternate Drug.

• mitotane

  Serious - Use Alternative (1)mitotane will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• mobocertinib

  Serious - Use Alternative (1)mobocertinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.

• moxifloxacin

  Serious - Use Alternative (1)moxifloxacin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• nafcillin

  Serious - Use Alternative (1)nafcillin will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• nefazodone

  Serious - Use Alternative (1)nefazodone will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• nelfinavir

  Serious - Use Alternative (1)nelfinavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• netupitant/palonosetron

  Serious - Use Alternative (1)netupitant/palonosetron will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• nilotinib

  Serious - Use Alternative (1)nilotinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• nortriptyline

  Monitor Closely (1)entrectinib and nortriptyline both increase QTc interval. Use Caution/Monitor.

• octreotide

  Serious - Use Alternative (1)entrectinib and octreotide both increase QTc interval. Avoid or Use Alternate Drug.

• ofloxacin

  Serious - Use Alternative (1)ofloxacin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• olanzapine

  Serious - Use Alternative (1)olanzapine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• olodaterol inhaled

  Monitor Closely (1)entrectinib and olodaterol inhaled both increase QTc interval. Use Caution/Monitor.

• ondansetron

  Serious - Use Alternative (1)entrectinib and ondansetron both increase QTc interval. Avoid or Use Alternate Drug.

• osilodrostat

  Monitor Closely (1)osilodrostat and entrectinib both increase QTc interval. Use Caution/Monitor.

• osimertinib

  Serious - Use Alternative (1)osimertinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• oxaliplatin

  Serious - Use Alternative (1)entrectinib and oxaliplatin both increase QTc interval. Avoid or Use Alternate Drug.

• ozanimod

  Monitor Closely (1)ozanimod and entrectinib both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.

• paliperidone

  Serious - Use Alternative (1)paliperidone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• panobinostat

  Serious - Use Alternative (1)panobinostat and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• pasireotide

  Serious - Use Alternative (1)pasireotide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• pazopanib

  Serious - Use Alternative (1)pazopanib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• pentamidine

  Serious - Use Alternative (1)pentamidine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• perphenazine

  Monitor Closely (1)entrectinib and perphenazine both increase QTc interval. Use Caution/Monitor.

• phenobarbital

  Serious - Use Alternative (1)phenobarbital will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• phenytoin

  Serious - Use Alternative (1)phenytoin will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• pimavanserin

  Serious - Use Alternative (1)pimavanserin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• pimozide

  Serious - Use Alternative (1)pimozide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• pitolisant

  Serious - Use Alternative (1)pitolisant and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• ponesimod

  Monitor Closely (1)ponesimod and entrectinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.Serious - Use Alternative (1)entrectinib and ponesimod both increase QTc interval. Avoid or Use Alternate Drug.

• posaconazole

  Serious - Use Alternative (2)posaconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.
  
  entrectinib and posaconazole both increase QTc interval. Avoid or Use Alternate Drug.

• primaquine

  Serious - Use Alternative (1)primaquine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• primidone

  Serious - Use Alternative (1)primidone will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• procainamide

  Serious - Use Alternative (1)procainamide and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• prochlorperazine

  Monitor Closely (1)entrectinib and prochlorperazine both decrease QTc interval. Use Caution/Monitor.

• promethazine

  Serious - Use Alternative (1)entrectinib and promethazine both decrease QTc interval. Avoid or Use Alternate Drug.

• propafenone

  Serious - Use Alternative (1)propafenone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• protriptyline

  Monitor Closely (1)entrectinib and protriptyline both increase QTc interval. Use Caution/Monitor.

• quetiapine

  Serious - Use Alternative (1)quetiapine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• quinidine

  Serious - Use Alternative (1)quinidine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• quinine

  Serious - Use Alternative (1)quinine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• quinupristin/dalfopristin

  Serious - Use Alternative (1)quinupristin/dalfopristin will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• ranolazine

  Serious - Use Alternative (1)ranolazine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• ribociclib

  Serious - Use Alternative (2)ribociclib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  ribociclib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• rifabutin

  Serious - Use Alternative (1)rifabutin will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• rifampin

  Serious - Use Alternative (1)rifampin will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• rifapentine

  Serious - Use Alternative (1)rifapentine will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• rilpivirine

  Serious - Use Alternative (1)entrectinib and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.

• risperidone

  Serious - Use Alternative (1)risperidone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• ritonavir

  Serious - Use Alternative (1)ritonavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• romidepsin

  Serious - Use Alternative (1)romidepsin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• rucaparib

  Monitor Closely (1)rucaparib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

• salmeterol

  Monitor Closely (1)entrectinib and salmeterol both increase QTc interval. Use Caution/Monitor.

• saquinavir

  Serious - Use Alternative (2)saquinavir and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  saquinavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• schisandra

  Serious - Use Alternative (1)schisandra will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• secobarbital

  Serious - Use Alternative (1)secobarbital will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• selpercatinib

  Monitor Closely (1)selpercatinib increases toxicity of entrectinib by QTc interval. Use Caution/Monitor.

• sertraline

  Serious - Use Alternative (2)sertraline will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.
  
  entrectinib and sertraline both increase QTc interval. Avoid or Use Alternate Drug.

• sevoflurane

  Serious - Use Alternative (1)entrectinib and sevoflurane both increase QTc interval. Avoid or Use Alternate Drug.

• siponimod

  Monitor Closely (1)siponimod and entrectinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.Serious - Use Alternative (1)entrectinib and siponimod both increase QTc interval. Avoid or Use Alternate Drug.

• solifenacin

  Serious - Use Alternative (1)entrectinib and solifenacin both increase QTc interval. Avoid or Use Alternate Drug.

• sorafenib

  Serious - Use Alternative (1)sorafenib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• sotalol

  Serious - Use Alternative (1)sotalol and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• stiripentol

  Serious - Use Alternative (1)stiripentol will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• sunitinib

  Serious - Use Alternative (1)sunitinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• tacrolimus

  Serious - Use Alternative (1)entrectinib and tacrolimus both increase QTc interval. Avoid or Use Alternate Drug.

• tazemetostat

  Monitor Closely (1)tazemetostat will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

• telavancin

  Serious - Use Alternative (1)telavancin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• telotristat ethyl

  Serious - Use Alternative (1)telotristat ethyl will decrease the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

• tetrabenazine

  Serious - Use Alternative (1)tetrabenazine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• tetracycline

  Serious - Use Alternative (1)tetracycline will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• thioridazine

  Serious - Use Alternative (1)thioridazine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• tipranavir

  Serious - Use Alternative (1)tipranavir will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• toremifene

  Serious - Use Alternative (1)toremifene and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• trazodone

  Serious - Use Alternative (1)trazodone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• triclabendazole

  Serious - Use Alternative (1)triclabendazole and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• trifluoperazine

  Monitor Closely (1)entrectinib and trifluoperazine both decrease QTc interval. Use Caution/Monitor.

• trimipramine

  Monitor Closely (1)entrectinib and trimipramine both increase QTc interval. Use Caution/Monitor.

• triptorelin

  Serious - Use Alternative (1)triptorelin and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• tucatinib

  Serious - Use Alternative (1)tucatinib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

• umeclidinium bromide/vilanterol inhaled

  Serious - Use Alternative (1)entrectinib and umeclidinium bromide/vilanterol inhaled both decrease QTc interval. Avoid or Use Alternate Drug.

• valbenazine

  Monitor Closely (1)valbenazine and entrectinib both increase QTc interval. Use Caution/Monitor.

• vandetanib

  Serious - Use Alternative (1)vandetanib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• vardenafil

  Serious - Use Alternative (1)entrectinib and vardenafil both increase QTc interval. Avoid or Use Alternate Drug.

• vemurafenib

  Serious - Use Alternative (1)vemurafenib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

• venlafaxine

  Serious - Use Alternative (1)entrectinib and venlafaxine both decrease QTc interval. Avoid or Use Alternate Drug.

• verapamil

  Serious - Use Alternative (1)verapamil will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives.

• vilanterol/fluticasone furoate inhaled

  Monitor Closely (1)entrectinib and vilanterol/fluticasone furoate inhaled both increase QTc interval. Use Caution/Monitor.

• voclosporin

  Monitor Closely (1)voclosporin, entrectinib. Either increases effects of the other by QTc interval. Use Caution/Monitor.

• voriconazole

  Serious - Use Alternative (2)voriconazole and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
  
  voriconazole will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of strong CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce entrectinib dose to 100 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing strong CYP3A inhibitor for 3-5 elimination half-lives.

• vorinostat

  Serious - Use Alternative (1)entrectinib and vorinostat both increase QTc interval. Avoid or Use Alternate Drug.

• voxelotor

  Serious - Use Alternative (1)voxelotor will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

• ziprasidone

  Serious - Use Alternative (1)ziprasidone and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.