Dosing & Uses
Dosage Forms & Strengths
tablet
- 40mg
- 80mg
Non-Small Cell Lung Cancer
Adjuvant therapy
- Indicated as adjuvant therapy after tumor resection for non-small cell lung cancer (NSCLC) in patients whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations
- 80 mg PO qDay
- Continue until disease recurrence, or unacceptable toxicity, or for up to 3 years
First-line treatment for metastatic NSCLC
- Indicated for first-line treatment of patients with metastatic NSCLC whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations
- 80 mg PO qDay
- Continue until disease progression or unacceptable toxicity, or for up to 3 years
Previously treated metastatic NSCLC
- Indicated for metastatic EGFR T790M mutation-positive NSCLC in patients whose disease has progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy
- 80 mg PO qDay
- Continue until disease progression or unacceptable toxicity, or for up to 3 years
Dosage Modifications
Pulmonary adverse effects
- Interstitial lung disease/pneumonitis: Permanently discontinue
Cardiac adverse effects
QTc interval >500 msec on at least 2 separate ECGs: Withhold until QTc interval <481 msec or recovery to baseline if baseline QTc is ≥481 msec, then resume at 40 mg dose
Permanently discontinue
- QTc interval prolongation with signs/symptoms of life-threatening arrhythmia
- Symptomatic congestive heart failure
Other adverse effects
- Grade ≥3: Withhold for up to 3 weeks
- If improvement to Grade ≤2 within 3 weeks: Resume at 80 mg or 40 mg qDay
- If no improvement within 3 weeks: Permanently discontinue
Cutaneous adverse effects
- Stevens Johnson syndrome (SJS), erythema multiforme major (EMM): Withhold if suspected and permanently discontinue if confirmed
CYP3A4 inducers
- Moderate and/or weak CYP3A inducers: No dose adjustments required
-
Strong CYP3A4 inducers
- Avoid coadministration
- If coadministration is unavoidable, increase osimertinib to 160 mg/day when used with a strong CYP3A inducer
- Resume osimertinib at 80 mg 3 weeks after discontinuing the strong CYP3A4 inducer
Renal impairment
- Mild-to-moderate (CrCl 15-89 mL/min): No dosage adjustment necessary
- End-stage renal disease (CrCl <15 mL/min): No recommended dose
Hepatic impairment
- Mild-to-moderate (Child-Pugh A and B or total bilirubin ≤3x ULN and any AST): No dose adjustment necessary
- Severe (total bilirubin 3-10x ULN and any AST): No recommended dose
Dosing Considerations
Patient selection
First-line treatment of metastatic EGFR-positive NSCLC: Confirm presence of EGFR exon 19 deletions or exon 21 L858R mutations in tumor or plasma specimens
Metastatic EGFR T790M mutation-positive NSCLC: Confirm presence of T790M mutation in tumor specimens prior to initiating treatment
Information on FDA-approved tests is available at http://www.fda.gov/companiondiagnostics
Safety and efficacy not established
No overall differences in effectiveness were observed based on age
Exploratory analysis suggests a higher incidence of Grade 3 and 4 adverse reactions (13.4% versus 9.3%) and more frequent dose modifications for adverse reactions (13.4% versus 7.6%) in patients ≥65 years as compared to those <65 year
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- lefamulin
lefamulin will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lefamulin is contraindicated with CYP3A substrates know to prolong the QT interval.
Serious - Use Alternative (79)
- abametapir
abametapir will increase the level or effect of osimertinib 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.
- alfuzosin
alfuzosin and osimertinib both increase QTc interval. Avoid or Use Alternate Drug.
- alpelisib
osimertinib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.
- apalutamide
apalutamide will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
- aripiprazole
aripiprazole and osimertinib both increase QTc interval. Avoid or Use Alternate Drug.
- artemether
artemether and osimertinib both increase QTc interval. Avoid or Use Alternate Drug.
- atazanavir
atazanavir will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- atomoxetine
atomoxetine and osimertinib both increase QTc interval. Avoid or Use Alternate Drug.
- bosentan
bosentan will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- carbamazepine
carbamazepine will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- ceritinib
ceritinib and osimertinib both increase QTc interval. Avoid or Use Alternate Drug.
- clarithromycin
clarithromycin will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- cobicistat
cobicistat will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- conivaptan
conivaptan will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- dabrafenib
dabrafenib will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- darolutamide
darolutamide will increase the level or effect of osimertinib by Other (see comment). Avoid or Use Alternate Drug. Darolutamide is a BCRP inhibitor. Avoid coadministration with BCRP inhibitors. If use is unavoidable, closely monitor for adverse reactions and consider dose reduction of BCRP substrate drug (refer BCRP substrate prescribing information).
- darunavir
darunavir will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- deferiprone
deferiprone, osimertinib. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.
- dexamethasone
dexamethasone will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- dofetilide
dofetilide increases toxicity of osimertinib by QTc interval. Avoid or Use Alternate Drug.
- efavirenz
efavirenz will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- entrectinib
osimertinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
- enzalutamide
enzalutamide will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- erythromycin base
erythromycin base will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- erythromycin stearate
erythromycin stearate will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- escitalopram
escitalopram increases toxicity of osimertinib by QTc interval. Avoid or Use Alternate Drug.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- etravirine
etravirine will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- fexinidazole
fexinidazole and osimertinib 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 osimertinib 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. - fosamprenavir
fosamprenavir will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- fosphenytoin
fosphenytoin will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- glasdegib
osimertinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- grapefruit
grapefruit will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- hydroxychloroquine sulfate
hydroxychloroquine sulfate and osimertinib both increase QTc interval. Avoid or Use Alternate Drug.
- idelalisib
idelalisib will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- imatinib
imatinib will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- indinavir
indinavir will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- inotuzumab
inotuzumab and osimertinib both increase QTc interval. Avoid or Use Alternate Drug. If unable to avoid concomitant use, obtain ECGs and electrolytes before and after initiation of any drug known to prolong QTc, and periodically monitor as clinically indicated during treatment.
- isoniazid
isoniazid will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- ivosidenib
ivosidenib and osimertinib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of QTc prolonging drugs with ivosidenib or replace with alternate therapies. If coadministration of a QTc prolonging drug is unavoidable, monitor for increased risk of QTc interval prolongation.
ivosidenib will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs. - ketoconazole
ketoconazole will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- lasmiditan
lasmiditan increases levels of osimertinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
lasmiditan increases levels of osimertinib by Other (see comment). Avoid or Use Alternate Drug. Comment: Lasmiditan inhibits BCRP in vitro. Avoid coadministration of lasmiditan with BCRP substrates. - lopinavir
lopinavir will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- macimorelin
macimorelin and osimertinib both increase QTc interval. Avoid or Use Alternate Drug. Macimorelin causes an increase of ~11 msec in the corrected QT interval. Avoid coadministration with drugs that prolong QT interval, which could increase risk for developing torsade de pointes-type ventricular tachycardia. Allow sufficient washout time of drugs that are known to prolong the QT interval before administering macimorelin.
- mifepristone
mifepristone will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mitotane
mitotane will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- mobocertinib
mobocertinib and osimertinib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- nafcillin
nafcillin will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- nefazodone
nefazodone will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- nelfinavir
nelfinavir will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- nevirapine
nevirapine will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- nicardipine
nicardipine will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- oxcarbazepine
oxcarbazepine will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- ozanimod
osimertinib increases toxicity of ozanimod by Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of ozanimod (a BCRP substrate) with BCRP inhibitors increases the exposure of the minor (RP101988, RP101075) and major active metabolites (CC112273, CC1084037) of ozanimod, which may increase the risk of ozanimod adverse reactions. .
- palifermin
palifermin increases toxicity of osimertinib by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- pentobarbital
pentobarbital will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- phenobarbital
phenobarbital will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- phenytoin
phenytoin will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- pitolisant
osimertinib and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.
- posaconazole
posaconazole will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- primidone
primidone will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- ribociclib
ribociclib increases toxicity of osimertinib by QTc interval. Avoid or Use Alternate Drug.
- rifabutin
rifabutin will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- rifampin
rifampin will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- rifapentine
rifapentine will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- ritonavir
ritonavir will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- saquinavir
saquinavir will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- sotorasib
sotorasib will decrease the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.
- St John's Wort
St John's Wort will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of osimertinib with strong CYP3A inducers.
- talazoparib
osimertinib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- tepotinib
tepotinib will increase the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
- tipranavir
tipranavir will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- tucatinib
tucatinib will increase the level or effect of osimertinib 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.
- voriconazole
voriconazole will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of osimertinib with strong CYP3A4 inhibitors. If no other alternative treatment exists, monitor patient more closely for adverse effects.
- voxelotor
voxelotor will increase the level or effect of osimertinib 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.
Monitor Closely (144)
- acalabrutinib
acalabrutinib increases levels of osimertinib by Other (see comment). Use Caution/Monitor. Comment: Acalabrutinib may increase exposure to coadministered BCRP substrates by inhibition of intestinal BCRP.
- albuterol
albuterol and osimertinib both increase QTc interval. Use Caution/Monitor.
- alfuzosin
osimertinib and alfuzosin both increase QTc interval. Use Caution/Monitor.
- amiodarone
osimertinib and amiodarone both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- amitriptyline
osimertinib and amitriptyline both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- amoxapine
osimertinib and amoxapine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- apalutamide
apalutamide will decrease the level or effect of osimertinib by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces BCRP and may decrease systemic exposure of drugs that are BCRP substrates.
- apomorphine
osimertinib and apomorphine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- arformoterol
osimertinib and arformoterol both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- arsenic trioxide
osimertinib and arsenic trioxide both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- artemether/lumefantrine
osimertinib and artemether/lumefantrine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- asenapine
osimertinib and asenapine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- azithromycin
osimertinib and azithromycin both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- bedaquiline
osimertinib and bedaquiline both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- berotralstat
osimertinib increases levels of berotralstat by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduced berotralstat dose to 110 mg/day when coadministered with P-gp inhibitors.
osimertinib increases levels of berotralstat by Other (see comment). Modify Therapy/Monitor Closely. Comment: Reduced dose of berotralstat (a BCRP substrate) to 110 mg/day when coadministered with BCRP inhibitors.
berotralstat will increase the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered. - cenobamate
cenobamate will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- chloroquine
chloroquine increases toxicity of osimertinib by QTc interval. Use Caution/Monitor.
- chlorpromazine
osimertinib and chlorpromazine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- cholera vaccine
osimertinib decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Immunosuppressive therapies, including irradiation, antimetabolites, alkylating agents, cytotoxic drugs and corticosteroids (used in greater than physiologic doses), may reduce the immune response to cholera vaccine.
- ciprofloxacin
osimertinib and ciprofloxacin both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- citalopram
osimertinib and citalopram both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- clarithromycin
osimertinib and clarithromycin both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- clomipramine
osimertinib and clomipramine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- clozapine
osimertinib and clozapine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- crizotinib
osimertinib and crizotinib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- dasatinib
osimertinib and dasatinib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- daunorubicin
osimertinib will increase the level or effect of daunorubicin by Other (see comment). Modify Therapy/Monitor Closely. Osimertinib is an inhibitor of BCRP transport. Caution if coadministered with sensitive BCRP substrates.
- degarelix
osimertinib and degarelix both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- dengue vaccine
osimertinib decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine.
- desipramine
osimertinib and desipramine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- diazepam intranasal
osimertinib, diazepam intranasal. Other (see comment). Use Caution/Monitor. Comment: Coadministration may either increase or decrease diazepam elimination.
- disopyramide
osimertinib and disopyramide both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- dofetilide
osimertinib and dofetilide both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- dolasetron
osimertinib and dolasetron both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- dronedarone
osimertinib and dronedarone both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- droperidol
osimertinib and droperidol both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- duvelisib
osimertinib will increase the level or effect of duvelisib by Other (see comment). Use Caution/Monitor. Coadministration of duvelisib (a BCRP substrate) with a BCRP transport inhibitor may increase levels or effects of duvelisib.
- elagolix
elagolix will increase the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
elagolix decreases levels of osimertinib 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. - encorafenib
encorafenib, osimertinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
- eribulin
osimertinib and eribulin both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- erythromycin base
osimertinib and erythromycin base both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- erythromycin ethylsuccinate
osimertinib and erythromycin ethylsuccinate both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- erythromycin lactobionate
osimertinib and erythromycin lactobionate both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- erythromycin stearate
osimertinib and erythromycin stearate both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- escitalopram
osimertinib and escitalopram both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- ezogabine
osimertinib and ezogabine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- fedratinib
fedratinib will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- fentanyl iontophoretic transdermal system
osimertinib, fentanyl iontophoretic transdermal system. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Osimertinib is a competitive inhibitor and inducer of CYP3A. Monitor sensitive CYP3A substrates for alterations in serum levels or efficacy/toxicity.
- flecainide
osimertinib and flecainide both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- fluconazole
osimertinib and fluconazole both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- fluoxetine
osimertinib and fluoxetine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- fluphenazine
osimertinib and fluphenazine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- formoterol
osimertinib and formoterol both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- foscarnet
osimertinib and foscarnet both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- fostamatinib
fostamatinib will increase the level or effect of osimertinib by decreasing metabolism. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of BCRP substrate drugs. Monitor for toxicities of BCRP substrate drug that may require dosage reduction when given concurrently with fostamatinib.
fostamatinib will increase the level or effect of osimertinib by Other (see comment). Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of P-gp/BCRP substrate drugs. Monitor for toxicities of P-gp/BCRP substrate drug that may require dosage reduction when given concurrently with fostamatinib. - fostemsavir
fostemsavir will increase the level or effect of osimertinib by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits BCRP transporters. If possible, avoid coadministration or modify dose of BCRP substrate coadministered with fostemsavir.
osimertinib and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir. - gemifloxacin
osimertinib and gemifloxacin both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- gemtuzumab
osimertinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.
- glecaprevir/pibrentasvir
osimertinib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with BCRP inhibitors.
glecaprevir/pibrentasvir will increase the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of osimertinib by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates. - glyburide
osimertinib will increase the level or effect of glyburide by Other (see comment). Modify Therapy/Monitor Closely. Osimertinib is an inhibitor of BCRP transport. Caution if coadministered with sensitive BCRP substrates.
- goserelin
goserelin increases toxicity of osimertinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- haloperidol
osimertinib and haloperidol both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- histrelin
histrelin increases toxicity of osimertinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- ibutilide
osimertinib and ibutilide both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- iloperidone
osimertinib and iloperidone both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- indacaterol, inhaled
osimertinib and indacaterol, inhaled both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- indapamide
osimertinib and indapamide both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- irinotecan
osimertinib will increase the level or effect of irinotecan by Other (see comment). Modify Therapy/Monitor Closely. Osimertinib is an inhibitor of BCRP transport. Caution if coadministered with sensitive BCRP substrates.
- irinotecan liposomal
osimertinib will increase the level or effect of irinotecan liposomal by Other (see comment). Modify Therapy/Monitor Closely. Osimertinib is an inhibitor of BCRP transport. Caution if coadministered with sensitive BCRP substrates.
- isradipine
osimertinib and isradipine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- istradefylline
istradefylline will increase the level or effect of osimertinib 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.
istradefylline will increase the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates. - itraconazole
itraconazole will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- lapatinib
osimertinib and lapatinib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- leuprolide
leuprolide increases toxicity of osimertinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- levofloxacin
osimertinib and levofloxacin both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- lonafarnib
lonafarnib will increase the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Lonafarnib is a weak P-gp inhibitor. Monitor for adverse reactions if coadministered with P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicities. Reduce P-gp substrate dose if needed.
- lopinavir
osimertinib and lopinavir both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- lorlatinib
lorlatinib will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- maprotiline
osimertinib and maprotiline both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- mefloquine
osimertinib and mefloquine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- methadone
osimertinib and methadone both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- methotrexate
osimertinib will increase the level or effect of methotrexate by Other (see comment). Modify Therapy/Monitor Closely. Osimertinib is an inhibitor of BCRP transport. Caution if coadministered with sensitive BCRP substrates.
- mifepristone
osimertinib and mifepristone both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- moxifloxacin
osimertinib and moxifloxacin both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- nilotinib
osimertinib and nilotinib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- nortriptyline
osimertinib and nortriptyline both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- octreotide
osimertinib and octreotide both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- ofloxacin
osimertinib and ofloxacin both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- olanzapine
osimertinib and olanzapine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- ondansetron
osimertinib and ondansetron both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- osilodrostat
osilodrostat and osimertinib both increase QTc interval. Use Caution/Monitor.
- oxaliplatin
oxaliplatin and osimertinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Use of oxaliplatin with concomitant immunosuppressants or with impaired immune systems may increased risk for serious infections.
oxaliplatin will increase the level or effect of osimertinib by Other (see comment). Use Caution/Monitor. Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT interval. - ozanimod
ozanimod and osimertinib 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
osimertinib and paliperidone both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- panobinostat
osimertinib and panobinostat both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- pasireotide
osimertinib and pasireotide both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- pazopanib
osimertinib and pazopanib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- pentamidine
osimertinib and pentamidine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- perphenazine
osimertinib and perphenazine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- pimozide
osimertinib and pimozide both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- posaconazole
osimertinib and posaconazole both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- procainamide
osimertinib and procainamide both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- propafenone
osimertinib and propafenone both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- protriptyline
osimertinib and protriptyline both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- quetiapine
osimertinib and quetiapine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- quinidine
osimertinib and quinidine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- regorafenib
regorafenib will increase the level or effect of osimertinib by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.
- rucaparib
rucaparib will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- safinamide
safinamide will increase the level or effect of osimertinib by Other (see comment). Use Caution/Monitor. Safinamide and its major metabolite may inhibit intestinal BCRP. Monitor BCRP substrates for increased pharmacologic or adverse effects.
- saquinavir
osimertinib and saquinavir both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- sarecycline
sarecycline will increase the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor for toxicities of P-gp substrates that may require dosage reduction when coadministered with P-gp inhibitors.
- selexipag
osimertinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- selpercatinib
selpercatinib increases toxicity of osimertinib by QTc interval. Use Caution/Monitor.
- sertraline
osimertinib and sertraline both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- siponimod
siponimod and osimertinib 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.
- solifenacin
osimertinib and solifenacin both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- sorafenib
osimertinib and sorafenib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- sotalol
osimertinib and sotalol both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- stiripentol
stiripentol, osimertinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
stiripentol will increase the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing the dose of P-glycoprotein (P-gp) substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.
stiripentol will increase the level or effect of osimertinib by Other (see comment). Modify Therapy/Monitor Closely. Stiripentol is a BCRP transport inhibitor. Consider dosage reduction for BCRP substrates if adverse effects are experienced when coadministered. - sunitinib
osimertinib and sunitinib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- tacrolimus
osimertinib and tacrolimus both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- tafamidis
tafamidis will increase the level or effect of osimertinib by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.
- tafamidis meglumine
tafamidis meglumine will increase the level or effect of osimertinib by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.
- tazemetostat
tazemetostat will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- telavancin
osimertinib and telavancin both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- thioridazine
osimertinib and thioridazine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- thiothixene
osimertinib and thiothixene both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- topotecan
osimertinib will increase the level or effect of topotecan by Other (see comment). Modify Therapy/Monitor Closely. Osimertinib is an inhibitor of BCRP transport. Caution if coadministered with sensitive BCRP substrates.
- toremifene
osimertinib and toremifene both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- trastuzumab
trastuzumab, osimertinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- trastuzumab deruxtecan
trastuzumab deruxtecan, osimertinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- triclabendazole
triclabendazole and osimertinib both increase QTc interval. Use Caution/Monitor.
- trimipramine
osimertinib and trimipramine both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- triptorelin
triptorelin increases toxicity of osimertinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- tucatinib
tucatinib will increase the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.
- vandetanib
osimertinib and vandetanib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- vardenafil
osimertinib and vardenafil both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- vemurafenib
osimertinib and vemurafenib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- vilanterol/fluticasone furoate inhaled
osimertinib and vilanterol/fluticasone furoate inhaled both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- voclosporin
voclosporin, osimertinib. Either increases effects of the other by QTc interval. Use Caution/Monitor.
- voriconazole
osimertinib and voriconazole both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- vorinostat
osimertinib and vorinostat both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- ziprasidone
osimertinib and ziprasidone both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
Minor (1)
- ribociclib
ribociclib will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
Adverse drug reactions listed are all grades of severity unless listed otherwise
>10%
Lymphopenia (63%)
Thrombocytopenia (46%)
Anemia (43%)
Diarrhea (41%)
Rash (34%)
Neutropenia (27%)
Hypermagnesemia (27%)
Hyponatremia (26%)
Dry skin (23%)
Nail toxicity (22%)
Fatigue (22%)
Hypoglycemia (20%)
Eye disorders (18%)
Decreased appetite (18%)
Cough (17%)
Nausea (16%)
Stomatitis (15%)
Constipation (14%)
Pruritus (14%)
Vomiting (11%)
1-10%
Back pain (10%)
Headache (10%)
Hypokalemia (9%)
Lymphopenia, Grade 3 or 4 (8.2%)
Venous thromboembolism (7%)
Pneumonia (4%)
Interstitial lung disease/pneumonitis (3.3%)
QTc increased from baseline >60 msec (2.7%)
Neutropenia, Grade 3 or 4 (2.2%)
Hyponatremia, Grade 3 or 4 (1.8%)
Hypomagnesemia, Grade 3 or 4 (1.8%)
Hypokalemia, Grade 3 or 4 (1.8%)
Fatigue, Grade 3 or 4 (1.8%)
Cardiomyopathy (1.4%)
Diarrhea, Grade 3 or 4 (1.1%)
Decreased appetite, Grade 3 or 4 (1.1%)
<1%
Keratitis
Nausea
Vomiting
Rash
Back pain
Thrombocytopenia
Postmarketing Reports
Erythema multiforme and Stevens-Johnson syndrome, cutaneous vasculitis
Warnings
Contraindications
None
Cautions
Interstitial lung disease (ILD)/pneumonitis reported; permanently discontinue if diagnosed with ILD/pneumonitis
May prolong QTc interval; monitor ECG and electrolytes in patients with a history or predisposition for QTc prolongation or in those who are taking medications that are known to prolong the QTc interval
Cardiomyopathy (defined as cardiac failure, chronic cardiac failure, congestive heart failure, pulmonary edema or decreased ejection fraction) occurred, some fatal; assess LVEF before treatment and then every 3 months thereafter
Keratitis reported; promptly refer patients with signs and symptoms suggestive of keratitis (eg, eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain, red eye) to an ophthalmologist
May cause fetal harm
Postmarketing cases consistent with SJS and EMM reported
Postmarketing cases of cutaneous vasculitis including leukocytoclastic vasculitis, urticarial vasculitis, and IgA vasculitis have been reported
Drug interaction overview
- Osimertinib is a CYP3A4 substrate; a P-gp and BCRP inhibitor
-
CYP3A4 inducers
- Avoid use; if concurrent use is unavoidable, increase osimertinib dose
- Coadministration with a strong CYP3A4 inducer decreased osimertinib systemic exposure
-
BCRP and P-gp substrates
- Monitor for adverse effects of BCRP and P-gp substrates
- Coadministration with a BCRP or P-gp substrate increased exposure and risk of toxicities of BCRP or P-gp substrate
-
Drugs that prolong QTC interval
- Avoid use; if unavoidable, monitor ECG periodically
- Effects of coadministration with QT prolonging drugs is unknown
Pregnancy & Lactation
Pregnancy
Based on data from animal studies and its mechanism of action, fetal harm may occur when administered to pregnant females
No data available in humans
Animal data
- Administration to pregnant rats was associated with embryolethality and reduced fetal growth at plasma exposures 1.5x the exposure at the recommended human dose
Infertility
- Based on animal studies, may impair fertility in females and males of reproductive potential
Contraception
- Females of reproductive potential: Use effective contraception during treatment and for 6 weeks after final dose
- Males with female partners of reproductive potential: Use effective contraception during and for 4 months following final dose
Lactation
Unknown if distributed in human breast milk
Administration to rats during gestation and early lactation was associated with adverse effects, including reduced growth rates and neonatal death
Advise lactating women not to breastfeed during treatment and for 2 weeks after final dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) at ~9-fold lower concentrations than wild-type
Absorption
Peak plasma time: 6 hr
Distribution
Protein bound: 95%
Vd, steady-state: 918 L
Metabolism
Main metabolic pathways of osimertinib were oxidation (predominantly CYP3A) and dealkylation in vitro
Metabolites: Two pharmacologically-active metabolites (AZ7550 and AZ5104 circulating at approximately 10% of the parent) with similar inhibitory profiles to osimertinib have been identified
Elimination
Half-life: 48 hr
Clearance: 14.3 L/hr
Excretion: 68% (feces); 14% (urine); ~2% (unchanged osimertinib)
Administration
Oral Administration
Administer with or without food
Missed dose: Do not make up the missed dose and take the next dose as scheduled
Administration to patients with swallowing difficulty
- Disperse tablet in 4 tablespoons of noncarbonated water only
- Stir until tablet is completely dispersed and swallow or administer through nasogastric tube immediately
- Do not crush, heat, or ultrasonicate during preparation
- Rinse the container with 4-8 ounces of water and immediately drink
Nasogastric tube administration
- Disperse tablet as above in 15 mL of noncarbonated water, then use an additional 15 mL of water to transfer any residues to the syringe; administer resulting 30 mL liquid as per the nasogastric tube instructions with appropriate water flushes (~30 mL)
Storage
Tablets: Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Tagrisso oral - | 80 mg tablet |  | |
| Tagrisso oral - | 40 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
osimertinib oral
OSIMERTINIB - ORAL
(OH-sim-ER-ti-nib)
COMMON BRAND NAME(S): Tagrisso
USES: This medication is used to treat lung cancer. Osimertinib belongs to a class of drugs known as kinase inhibitors. It works by slowing or stopping the growth of cancer cells. It binds to a certain protein (epidermal growth factor receptor-EGFR) in some tumors.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking osimertinib and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once daily.If you have trouble swallowing the tablet whole, place the tablet into a container with a small amount of non-carbonated water (2 ounces/60 milliliters). Stir well until the tablet breaks into small pieces. The tablet will not completely dissolve. Do not crush the tablet or heat the mixture. Drink all of the mixture right away. Add at least another half a glass of water (4 ounces/120 milliliters) to the container and drink all of the mixture to make sure you are getting all of the drug. Use only non-carbonated water for mixing, and do not prepare a supply in advance. The mixture may also be given through a tube into the stomach (nasogastric tube). If you are giving this medication through a nasogastric tube, ask your health care professional for detailed instructions on how to give it.The dosage is based on your medical condition and response to treatment.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.
SIDE EFFECTS: Diarrhea, nausea, mouth sores, dry/itchy skin, tiredness, back pain, headache, or loss of appetite may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, such as: easy bruising/bleeding, changes in your nails (such as nail tenderness/irritation/redness, change in nail color), signs of eye disease (such as vision changes, eye redness/pain, light sensitivity, eye discharge), signs of low level of sodium in the blood (such as nausea, extreme drowsiness, mental/mood changes, seizures).Get medical help right away if you have any very serious side effects, such as: slow/fast/irregular heartbeat, severe dizziness, fainting, slow/shallow breathing, symptoms of heart failure (such as shortness of breath, swelling ankles/feet, unusual tiredness, unusual/sudden weight gain), new or worsening symptoms of lung disease (such as trouble breathing, chest pain, cough, fever), signs of blood clots (such as pain/swelling/warmth in the groin/calf).This medication may lower your ability to fight infections. This may make you more likely to get a serious (rarely fatal) infection or make any infection you have worse. Tell your doctor right away if you have any signs of infections (such as sore throat that doesn't go away, fever, chills).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, such as: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking osimertinib, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history.Osimertinib may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using osimertinib, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using osimertinib safely.This drug may cause blurred vision. Do not drive, use machinery, or do any activity that requires clear vision until you are sure you can perform such activities safely. Limit alcoholic beverages.Osimertinib can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this drug, especially QT prolongation (see above).This medication is not recommended for use during pregnancy. It may harm an unborn baby. It is important to prevent pregnancy while taking this medication and after treatment. Females should use reliable forms of birth control (such as condoms, birth control pills) during treatment and for 6 weeks after the end of treatment. Males with female partners should use reliable forms of birth control (such as condoms) during treatment and for 4 months after the end of treatment. If you become pregnant or think you may be pregnant or may have caused pregnancy, tell your doctor right away.It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding is not recommended while using this drug and for 2 weeks after the end of treatment. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Certain lab tests should be done before you start treatment to check for the EGFR protein in your tumor.Lab and/or medical tests (such as heart imaging) should be done before you start taking this medication and while you are taking it. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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