Dosing & Uses
Dosage Forms & Strengths
tablet
- 10mg
- 50mg
- 100mg
Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
Indicated for patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)
Dose ramp-up phase
- Administer dose according to a weekly ramp-up schedule over 5 weeks to the recommended daily dose of 400 mg
- Ramp-up dosing schedule designed to gradually reduce tumor burden and decrease risk of tumor lysis syndrome
- Week 1: 20 mg PO qDay
- Week 2: 50 mg PO qDay
- Week 3: 100 mg PO qDay
- Week 4: 200 mg PO qDay
- Week 5 and beyond: 400 mg PO qDay
Monotherapy
- 400 mg PO qDay after completing the 5-week dose ramp-up schedule
- Continue until disease progression or unacceptable toxicity
Combination with obinutuzumab
-
Cycle 1
- Day 1: Obinutuzumab 100 mg IV
- Day 2: Obinutuzumab 900 mg IV
- Days 8 and 15: Obinutuzumab 1000 mg IV
- Day 22: Start venetoclax according to 5-week ramp up schedule
-
Cycle 2
- Day 1: Obinutuzumab 1000 mg IV
- Day 28: After completing the ramp-up phase on Cycle 2 Day 28, continue venetoclax 400 mg qDay from Cycle 3 Day 1 until Cycle 12 Day 28
-
Cycles 3-6
- Day 1: Obinutuzumab 1000 mg IV
- Days 1-28: Continue venetoclax 400 mg PO qDay
-
Cycles 7-12
- Days 1-28: Continue venetoclax 400 mg PO qDay
Combination with rituximab
-
Venetoclax
- Complete 5-week ramp-up dosing to reach 400 mg PO qDay
- Continue venetoclax 400 mg PO qDay for 24 months from Cycle 1 Day 1 of rituximab
-
Rituximab
- Initiate 375 mg/m² IV after patient has received venetoclax 400 mg/day x 7 days (ie, this will be Day 1 of Cycle 1)
- 500 mg/m² IV on Day 1 for Cycles 2-6
Acute Myeloid Leukemia
Indicated in combination with azacitidine or decitabine or low-dose cytarabine for treatment in adults (≥75 years) who are newly-diagnosed acute myeloid leukemia (AML) or who have comorbidities that preclude use of intensive induction chemotherapy
Venetoclax dosing depends on the combination agent
Dose ramp-up phase
- Day 1: 100 mg PO qDay
- Day 2: 200 mg PO qDay
- Day 3: 400 mg PO qDay
- Day 4 and beyond (in combination with decitabine or azacitidine): 400 mg PO qDay
- Day 4 and beyond (in combination with low-dose cytarabine): 600 mg PO qDay
- In combination with decitabine, azacitidine, or low-dose cytarabine: Continue until disease progression or unacceptable toxicity
Refer to prescribing information for azacitidine, decitabine, or cytarabine for additionaldosing information
Dosage Modifications
For a dosing interruption >1 week during the first 5 weeks of ramp-up phase or >2 weeks after completing the ramp-up phase, reassess for risk of tumor lysis syndrome (TLS) to determine if reinitiation with a reduced dose is necessary (eg, all or some levels of the dose ramp-up schedule)
Consider discontinuing treatment for patients who require dose reductions to <100 mg for >2 weeks
Dose reduction schedule (CLL/SLL)
- Dose at interruption 400 mg: Restart at 300 mg
- Dose at interruption 300 mg: Restart at 200 mg
- Dose at interruption 200 mg: Restart at 100 mg
- Dose at interruption 100 mg: Restart at 50 mg
- Dose at interruption 50 mg: Restart at 20 mg
- Dose at interruption 20 mg: Restart at 10 mg
- During the ramp-up phase, continue reduced dose for 1 week before increasing the dose
Tumor lysis syndrome
- Modify for any occurrence of blood chemistry changes or symptoms suggestive of TLS
- Withhold the next day’s dose; if resolved within 24-48 hr of last dose, resume at the same dose
- For any blood chemistry changes requiring >48 hr to resolve, resume at a reduced dose
- For any events of clinical TLS, resume at a reduced dose following resolution
Grade 3 or 4 nonhematologic toxicities
- First occurrence: Interrupt dose; once resolved to grade ≤1, resume at same dose; no dose modification is required
- Second and subsequent occurrences: Interrupt dose; follow dose reduction schedule when resuming treatment after resolution; a larger dose reduction may be used at discretion of physician
Hematologic toxicities (CLL/SLL)
- Grade 3 or 4 neutropenia with infection or fever, or grade 4 hematologic toxicities (except lymphopenia)
- First occurrence: Interrupt dose; reduce infection risks with neutropenia by administering G-CSF with venetoclax if clinically indicated; once toxicity resolves to grade ≤1, resume at the same dose
- Second and subsequent occurrences: Interrupt dose; consider using G-CSF as clinically indicated; follow dose reduction schedule when resuming treatment after resolution; a larger dose reduction may be used at discretion of physician
Hematologic toxicities (AML)
- Grade 4 neutropenia with or without fever or infection; or Grade 4 thrombocytopenia
- Occurrence prior to achieving remission: Transfuse blood products, administer prophylactic and treatment anti-infectives as clinically indicated
- First occurrence after remission (last ≥7 days): Delay subsequent treatment cycle of venetoclax and azacitidine, decitabine, or low-dose cytarabine; monitor blood counts; once resolved to Grade 1 or 2, resume all therapy at same dose
- Subsequent occurrence after remission (last ≥7 days): Delay subsequent treatment cycle of venetoclax and azacitidine, decitabine, or low-dose cytarabine; monitor blood counts; once resolved to Grade 1 or 2, resume all therapy at same dose and reduce duration by 7 days for each subsequent cycle
Coadministration with strong CYP3A4 inhibitors
-
CLL/SLL
- Dose ramp-up phase: Contraindicated
- After ramp-up phase, consider alternative medications or reduce dose to 70 mg (coadministered with posaconazole) and 100 mg (coadministered with other strong CYP3A4 inhibitors)
-
AML
- Day 1: Reduce to 10 mg
- Day 2: Reduce to 20 mg
- Day 3: Reduce to 50 mg
- Day 4: Reduce to 70 mg (coadministered with posaconazole) OR 100 mg (coadministered with other strong CYP3A4 inhibitors
- Steady daily dose (after ramp-up phase): Reduce dose to 70 mg (coadministered with posaconazole) and 100 mg (coadministered with other strong CYP3A4 inhibitors)
- Resume venetoclax dose used prior to initiating the CYP3A inhibitor or P-gp inhibitor 2-3 days after discontinuation of inhibitor
Coadministration with moderate CYP3A inhibitor or P-gp inhibitor
- Reduce venetoclax dose by at least 50%
- Resume venetoclax dose used prior to initiating the CYP3A inhibitor or P-gp inhibitor 2-3 days after discontinuation of the inhibitor
Renal impairment
- Mild or moderate (CrCl ≥15 mL/min): No dosage adjustment necessary
- Severe (CrCl <15 mL/min) or patients on dialysis: Recommended dose has not been determined
Hepatic impairment
- Mild or moderate (Child-Pugh A or B): No dosage adjustment; monitor more frequently for signs of toxicity or adverse reactions during initiation and ramp-up phases
- Severe (Child-Pugh C): Reduce venetoclax dose by 50%; monitor
Dosing Considerations
Patients without 17p deletion at diagnosis should be retested at relapse because acquisition of 17p deletion can occur
TLS risk
- Consider all patient comorbidities before final determination of prophylaxis and monitoring schedule
- Assess patient-specific factors for level of risk of TLS and provide prophylactic hydration and antihyperuricemics prior to first dose to reduce risk of TLS
- Perform tumor burden assessments, including radiographic evaluation (eg, CT scan)
- Assess blood chemistry (potassium, uric acid, phosphorus, calcium, and creatinine) in all patients and correct preexisting abnormalities prior to initiation; monitor blood chemistries for TLS
- Reassess risk of TLS when reinitiating therapy after a dosage interruption lasting more than 1 week during the ramp-up phase, or more than 2 weeks after completion of ramp-up
- Institute prophylaxis and monitoring as needed
-
AML
- All patients should have WBC<25 x 109/L before to initiation
- Consider reducing venetoclax starting dose and closely monitor patients with risk factors for TLS (eg, circulating blasts, high burden of leukemia involvement in bone marrow, elevated pretreatment LDH levels, reduced renal function
TLS prophylaxis (CLL/SLL)
-
Low tumor burden (all lymph nodes (LNs) <5 cm AND absolute lymphocyte count (ALC) <25 x109/L)
- Hydration: Oral (1.5-2 L)
- Give allopurinol or xanthine oxidase inhibitor 2-3 days prior to initiation
- Administer IV hydration for patients unable to tolerate oral hydration
- Outpatient monitoring (20-mg or 50-mg dose): Blood chemistry predose, at 6-8 hr, and 24 hr after first dose and predose for subsequent ramp-up doses
-
Medium tumor burden (any LN 5 to <10 cm OR ALC ≥25 x109/L)
- Hydration: Oral (1.5-2 L, also consider additional IV hydration)
- Give allopurinol or xanthine oxidase inhibitor (2-3 days prior to initiation)
- Administer IV hydration for patients unable to tolerate oral hydration
- Outpatient monitoring (20-mg or 50-mg dose): Blood chemistry predose, at 6-8 hr, and 24 hr after first dose and predose for subsequent ramp-up doses; consider hospitalization for patients with CrCl <80 mL/min at first dose
-
High tumor burden (any LN ≥10 cm OR, ALC ≥25 x109/L AND any LN ≥5 cm)
- Hydration: Oral (1.5-2 L) and IV (150-200 mL/hr as tolerated)
- Give allopurinol 2-3 days before initiating venetoclax; consider rasburicase if baseline uric acid is elevated
- Inpatient monitoring (20-mg or 50-mg dose): Blood chemistry predose, 4, 8, 12, and 24 hr
- Outpatient monitoring (subsequent ramp-up doses): Blood chemistry at predose, at 6-8 hr, and 24 hr after dose
Orphan Designations
Multiple myeloma
Mantle cell lymphoma
Myelodysplastic syndromes
Sponsor
- AbbVie Inc; 1 Waukegan Road, Dept PA77, Bldg. AP30; North Chicago, Illinois 60044
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (24)
- atazanavir
atazanavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- ceritinib
ceritinib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- clarithromycin
clarithromycin will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- cobicistat
cobicistat will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- conivaptan
conivaptan will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- darunavir
darunavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- fosamprenavir
fosamprenavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- grapefruit
grapefruit will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. Avoid grapefruit products, Seville oranges, and starfruit during treatment with venetoclax as they contain inhibitors of CYP3A.
- idelalisib
idelalisib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- imatinib
imatinib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- indinavir
indinavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- isoniazid
isoniazid will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- itraconazole
itraconazole will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- ketoconazole
ketoconazole will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- levoketoconazole
levoketoconazole will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- lopinavir
lopinavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- nefazodone
nefazodone will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- nelfinavir
nelfinavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- nicardipine
nicardipine will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- posaconazole
posaconazole will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- ritonavir
ritonavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- saquinavir
saquinavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- tipranavir
tipranavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
- voriconazole
voriconazole will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Use of strong CYP3A4 inhibitors is contraindicated with venetoclax during the initial ramp-up dosing phase. If a strong CYP3A inhibitor must be used after the ramp-up phase, reduce the venetoclax dose by at least 75%.
Serious - Use Alternative (108)
- abametapir
abametapir will increase the level or effect of venetoclax 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.
- abiraterone
abiraterone will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- afatinib
afatinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- amiodarone
amiodarone will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
amiodarone will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities. - apalutamide
apalutamide will decrease the level or effect of venetoclax 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.
- aprepitant
aprepitant will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- armodafinil
armodafinil will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- atorvastatin
atorvastatin will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- azithromycin
azithromycin will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- bicalutamide
bicalutamide will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- bosentan
bosentan will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- captopril
captopril will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- carbamazepine
carbamazepine will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- carvedilol
carvedilol will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- chloramphenicol
chloramphenicol will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with a strong CYP3A inhibitor at initiation and during the ramp-up phase in patients with CLL/SLL is contraindicated. In CLL/SLL patients taking a steady daily dosage (after ramp-up phase), consider an alternant or adjust venetoclax dosage and closely monitor for adverse reactions. In AML patients, adjust venetoclax dosage and closely monitor for adverse reactions. Resume venetoclax dosage that was used before initiating the strong CYP3A inhibitor 2-3 days after discontinuing of the inhibitor.
- ciprofloxacin
ciprofloxacin will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- clarithromycin
clarithromycin will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- clobazam
clobazam will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- crizotinib
crizotinib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
crizotinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities. - cyclosporine
cyclosporine will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
cyclosporine will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
venetoclax will increase the level or effect of cyclosporine by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. In vitro data suggest venetoclax may inhibit P-gp substrates at therapeutic dose levels in the gut. Avoid coadministration of narrow therapeutic index P-gp substrates with venetoclax. If a narrow therapeutic index P-gp substrate must be used, it should be taken at least 6 hr before venetoclax. - dabrafenib
dabrafenib will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- darunavir
darunavir will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- dexamethasone
dexamethasone will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- digoxin
venetoclax will increase the level or effect of digoxin by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. In vitro data suggest venetoclax may inhibit P-gp substrates at therapeutic dose levels in the gut. Avoid coadministration of narrow therapeutic index P-gp substrates with venetoclax. If a narrow therapeutic index P-gp substrate must be used, it should be taken at least 6 hr before venetoclax.
- diltiazem
diltiazem will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- dipyridamole
dipyridamole will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- doxycycline
doxycycline will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- dronedarone
dronedarone will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
dronedarone will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities. - efavirenz
efavirenz will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- eliglustat
eliglustat will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- enzalutamide
enzalutamide will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- erdafitinib
erdafitinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If coadministration unavoidable, separate administration by at least 6 hr before or after administration of P-gp substrates with narrow therapeutic index.
- erythromycin base
erythromycin base will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
erythromycin base will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities. - erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
erythromycin ethylsuccinate will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities. - erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
erythromycin lactobionate will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities. - erythromycin stearate
erythromycin stearate will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
erythromycin stearate will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities. - eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- etravirine
etravirine will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
etravirine will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction. - everolimus
venetoclax will increase the level or effect of everolimus by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. In vitro data suggest venetoclax may inhibit P-gp substrates at therapeutic dose levels in the gut. Avoid coadministration of narrow therapeutic index P-gp substrates with venetoclax. If a narrow therapeutic index P-gp substrate must be used, it should be taken at least 6 hr before venetoclax.
- felodipine
felodipine will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- fexinidazole
fexinidazole will increase the level or effect of venetoclax 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.
- flibanserin
flibanserin will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- fluconazole
fluconazole will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- fosaprepitant
fosaprepitant will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- fosphenytoin
fosphenytoin will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- haloperidol
haloperidol will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- ibrutinib
ibrutinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- iloperidone
iloperidone will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- isavuconazonium sulfate
isavuconazonium sulfate will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- ivosidenib
ivosidenib will decrease the level or effect of venetoclax 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.
- lapatinib
lapatinib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
lapatinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities. - lasmiditan
lasmiditan increases levels of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- ledipasvir/sofosbuvir
ledipasvir/sofosbuvir will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- lomitapide
lomitapide will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- lonafarnib
lonafarnib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.
- lorlatinib
lorlatinib will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- mefloquine
mefloquine will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- metronidazole
metronidazole will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- mifepristone
mifepristone will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mitotane
mitotane will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- nafcillin
nafcillin will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- nelfinavir
nelfinavir will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- netupitant/palonosetron
netupitant/palonosetron will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- nevirapine
nevirapine will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- nicardipine
nicardipine will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- nifedipine
nifedipine will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- nilotinib
nilotinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- nirmatrelvir
nirmatrelvir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nirmatrelvir/ritonavir
nirmatrelvir/ritonavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- oxcarbazepine
oxcarbazepine will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- palifermin
palifermin increases toxicity of venetoclax 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.
- paliperidone
paliperidone will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- pentobarbital
pentobarbital will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- phenobarbital
phenobarbital will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- phenytoin
phenytoin will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- ponatinib
ponatinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- primidone
primidone will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- progesterone micronized
progesterone micronized will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- propafenone
propafenone will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- propranolol
propranolol will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- quinidine
quinidine will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- quinine
quinine will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- ranolazine
ranolazine will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- ribociclib
ribociclib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifabutin
rifabutin will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- rifampin
rifampin will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- rifapentine
rifapentine will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- rimegepant
venetoclax will increase the level or effect of rimegepant by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- schisandra
schisandra will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- sertraline
sertraline will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- sirolimus
venetoclax will increase the level or effect of sirolimus by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. In vitro data suggest venetoclax may inhibit P-gp substrates at therapeutic dose levels in the gut. Avoid coadministration of narrow therapeutic index P-gp substrates with venetoclax. If a narrow therapeutic index P-gp substrate must be used, it should be taken at least 6 hr before venetoclax.
- sotorasib
sotorasib will decrease the level or effect of venetoclax 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 venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of venetoclax with strong or moderate CYP3A inducers. Consider alternative treatment with agents that have less CYP3A induction.
- sunitinib
sunitinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- suvorexant
suvorexant will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- tacrolimus
tacrolimus will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
venetoclax will increase the level or effect of tacrolimus by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. In vitro data suggest venetoclax may inhibit P-gp substrates at therapeutic dose levels in the gut. Avoid coadministration of narrow therapeutic index P-gp substrates with venetoclax. If a narrow therapeutic index P-gp substrate must be used, it should be taken at least 6 hr before venetoclax. - tamoxifen
tamoxifen will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- temsirolimus
venetoclax will increase the level or effect of temsirolimus by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. In vitro data suggest venetoclax may inhibit P-gp substrates at therapeutic dose levels in the gut. Avoid coadministration of narrow therapeutic index P-gp substrates with venetoclax. If a narrow therapeutic index P-gp substrate must be used, it should be taken at least 6 hr before venetoclax.
- tepotinib
tepotinib will increase the level or effect of venetoclax 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.
- tetracycline
tetracycline will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- ticagrelor
ticagrelor will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- tucatinib
tucatinib will increase the level or effect of venetoclax 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.
- ulipristal
ulipristal will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- vandetanib
vandetanib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- vemurafenib
vemurafenib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- verapamil
verapamil will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
verapamil will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities. - voxelotor
voxelotor will increase the level or effect of venetoclax 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 (21)
- berotralstat
berotralstat will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered.
- betrixaban
venetoclax increases levels of betrixaban by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Decrease betrixaban dose to 80 mg PO once, then 40 mg PO qDay if coadministered with a P-gp inhibitor.
- cholera vaccine
venetoclax 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.
- duvelisib
duvelisib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.
- elagolix
elagolix will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
elagolix decreases levels of venetoclax 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, venetoclax. 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.
- fedratinib
fedratinib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- glecaprevir/pibrentasvir
venetoclax will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - haemophilus influenzae type b vaccine
venetoclax decreases effects of haemophilus influenzae type b vaccine by pharmacodynamic antagonism. Use Caution/Monitor.
- istradefylline
istradefylline will increase the level or effect of venetoclax 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 venetoclax 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. - ivacaftor
ivacaftor increases levels of venetoclax by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Ivacaftor and its M1 metabolite has the potential to inhibit P-gp; may significantly increase systemic exposure to sensitive P-gp substrates with a narrow therapeutic index.
- lenacapavir
lenacapavir will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir 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.
- naldemedine
venetoclax increases levels of naldemedine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor naldemedine for potential adverse effects if coadministered with P-gp inhibitors.
- poliovirus vaccine inactivated
venetoclax decreases effects of poliovirus vaccine inactivated by pharmacodynamic antagonism. Use Caution/Monitor. Vaccines administered during venetoclax therapy may be less effective.
- ponesimod
ponesimod and venetoclax 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.
- sarecycline
sarecycline will increase the level or effect of venetoclax 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.
- siponimod
siponimod and venetoclax 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.
- stiripentol
stiripentol, venetoclax. 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 venetoclax 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. - tazemetostat
tazemetostat will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- tucatinib
tucatinib will increase the level or effect of venetoclax 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.
Minor (4)
- acetazolamide
acetazolamide will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- larotrectinib
larotrectinib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
All grades of severity listed unless otherwise indicated
>10% (Combination with rituximab)
Leukopenia (89%)
Lymphopenia (87%)
Neutropenia (65-86%)
Neutropenia, Grade 3 or 4 (62-64%)
Hypocalcemia (62%)
Hypophosphatemia (57%)
Lymphopenia, Grade 3 or 4 (56%)
Leukopenia, Grade 3 or 4 (46%)
Diarrhea (43%)
Increased AST/SGOT (46%)
Diarrhea (40%)
Upper respiratory tract infection (39%)
Hyperuricemia (36%)
Increased alkaline phosphatase (35%)
Hyperbilirubinemia (33%)
Hyponatremia (30%)
Hypokalemia (29%)
Hyperkalemia (24%)
Hypernatremia (24%)
Nausea (21%)
Musculoskeletal pain (19%)
Lower respiratory tract infection (18%)
Anemia (16%)
Thrombocytopenia (15%)
Constipation (14%)
Hypophosphatemia, Grade 3 or 4 (14%)
Abdominal pain (13%)
Rash (13%)
Headache (11%)
Insomnia (11%)
>10% (Monotherapy)
Neutropenia (50%)
Neutropenia, Grade 3 or 4 (45%)
Nausea (42%)
Upper respiratory tract infection (36%)
Anemia (33%)
Fatigue (32%)
Thrombocytopenia (29%)
Edema (22%)
Thrombocytopenia, Grade 3 or 4 (20%)
Anemia, Grade 3 or 4 (18%)
Abdominal pain (18%)
Pyrexia (18%)
Vomiting (16%)
Constipation (16%)
Mucositis (13%)
Lymphopenia (11%)
1-10% (Combination with rituximab)
Mucositis (10%)
Pneumonia (10%)
Vomiting (8%)
Lymphopenia, Grade 3 or 4 (7%)
Hyponatremia, Grade 3 or 4 (6%)
Hypokalemia, Grade 3 or 4 (6%)
Hypocalcemia, Grade 3 or 4 (5%)
Febrile neutropenia (4%)
Hyperbilirubinemia, Grade 3 or 4 (4%)
Diarrhea, Grade 3 or 4 (3%)
TLS, Grade 3 or 4 (3%)
Hyperkalemia, Grade 3 or 4 (3%)
Upper respiratory tract infection, Grade 3 or 4 (2%)
Lower respiratory tract infection, Grade 3 or 4 (2%)
Increased AST/SGOT (2%)
Hypernatremia, Grade 3 or 4 (1%)
Musculoskeletal pain, Grade 3 or 4 (1%)
Increased alkaline phosphatase, Grade 3 or 4 (1%)
1-10% (Monotherapy)
Febrile neutropenia (6%)
Fatigue, Grade 3 or 4 (4%)
Abdominal pain, Grade 3 or 4 (3%)
Diarrhea, Grade 3 or 4 (3%)
Edema, Grade 3 or 4 (2%)
Nausea, Grade 3 or 4 (1%)
Vomiting, Grade 3 or 4 (1%)
Upper respiratory tract infection, Grade 3 or 4 (1%)
<1%
Monotherapy
- Constipation, Grade 3 or 4
- Mucositis, Grade 3 or 4
- Pyrexia, Grade 3 or 4
Posmarketing Reports
Sepsis
Warnings
Contraindications
Strong CYP3A inhibitors at initiation and during ramp-up phase
Cautions
Tumor lysis syndrome (TLS), including fatal events and renal failure requiring dialysis, has occurred in previously treated CLL patients with high tumor burden when treated with venetoclax
The risk of TLS is a continuum based on multiple factors, particularly reduced renal function, tumor burden, and type of malignancy; splenomegaly may also increase risk of TLS in patients with CLL/SLL
Therapy can cause rapid reduction in tumor and thus poses a risk for TLS at initiation and during ramp-up phase in all patients, and during reinitiation after dosage interruption in patients with CLL/SLL; changes in blood chemistries consistent with TLS that require prompt management can occur as early as 6 to 8 hours following first dose and at each dose increase; TLS, including fatal cases, has been reported after a single 20 mg dose
Neutropenia frequently reported; monitor complete blood cell counts throughout treatment period
Fatal and serious infections such as pneumonia and sepsis have occurred; monitor patients closely for signs and symptoms of infection and treat promptly; withhold therapy for Grade 3 and higher infection
Do not administer live attenuated vaccines prior to, during, or after treatment until B-cell recovery occurs; safety and efficacy of immunization with live attenuated vaccines during or following therapy have not been studied; advise patients that vaccinations may be less effective
Based on its mechanism of action and findings in animals, may cause embryofetal harm when administered to a pregnant woman
In a randomized trial in patients with relapsed or refractory multiple myeloma, the addition of venetoclax to bortezomib plus dexamethasone, resulted in increased mortality; treatment of patients with multiple myeloma with venetoclax in combination with bortezomib plus dexamethasone is not recommended outside of controlled clinical trials
Drug interaction overview
-
Effects of other drugs on venetoclax
- Venetoclax is a CYP3A substrate
- Concomitant use with a strong or moderate CYP3A inhibitor or a P-gp inhibitor increases venetoclax plasma concentrations and toxicities, including the risk of TLS
- Reduce dose when coadministered with P-gp or moderate CYP3A4 inhibitors
- Avoid grapefruit products, Seville oranges, and starfruit during treatment, as they contain inhibitors of CYP3A
- Concomitant use with a strong CYP3A inducer decreases venetoclax plasma concentrations and efficacy
-
Venetoclax effects on other drugs
- Venetoclax has inhibition potential on P-gp substrates at therapeutic dose levels in the gut; therefore, avoid coadministration with narrow-therapeutic index P-gp substrates
- Coadministration with warfarin increases warfarin peak plasma concentrations and AUC, which may increase the risk of bleeding; closely monitor INR; monitor international normalized ratio (INR) more frequently in patients using warfarin concomitantly
Pregnancy
Pregnancy
There are no available human data on use in pregnant women; based on its mechanism of action and findings in animals, may cause embryofetal harm when administered to a pregnant woman
Females of reproductive potential should undergo pregnancy testing before initiation
Animal studies
- In mice, venetoclax was fetotoxic at exposures 1.2 times the human clinical exposure based on AUC at the recommended human dose of 400 mg daily
Fertility and contraception
- Advise females of reproductive potential to use effective contraception during treatment and for at least 30 days after the last dose
- Male fertility may be compromised by treatment
Lactation
Unknown if distributed in human breast milk; advise nursing women to discontinue breastfeeding during treatment and for at least one week after last 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
Selective inhibitor of the B-cell lymphoma 2 (Bcl-2) regulator protein, an antiapoptotic protein
Overexpression of Bcl-2 has been demonstrated in CLL cells where it mediates tumor cell survival and has been associated with resistance to chemotherapeutic agents
Venetoclax helps restore the process of apoptosis by binding directly to the Bcl-2 protein, displacing proapoptotic proteins like BIM (a novel member of the Bcl-2 family), triggering mitochondrial outer membrane permeabilization, and activating caspases
Absorption
Peak plasma time: 5-8 hr
Peak plasma concentration at steady-state: 2.1 mcg/mL (400 mcg/day)
AUC at steady-state: 32.8 mcg·hr/mL (400 mcg//day)
Food effects
- Administration with a low-fat meal increased venetoclax exposure by ~3.4-fold and administration with a high-fat meal increased venetoclax exposure by 5.1- to 5.3-fold compared withto fasting conditions
- Venetoclax should be administered with a meal
Distribution
Protein bound: >99.9%
Vd: 256-321 L
Metabolism
Metabolized by CYP3A4/5
M27 was identified as a major metabolite in plasma with an inhibitory activity against Bcl-2 that is at least 58-fold lower than venetoclax in vitro
Elimination
Half-life: 26 hr
Excretion: >99.9% in feces; <0.1% in urine
Administration
Oral Administration
Administer 1 time a day with a meal and water at about the same time each day
Swallow whole; do not chew, crush, or break tablets
Missed dose
- If dose is missed within 8 hr of scheduled dose, take as soon as possible
- If a patient misses a dose by >8 hr, skip dose and resume usual dosing schedule the next day
- If patient vomits following dosing, do not take an extra dose; take the next prescribed dose at the usual time
Storage
Tablets: Store at ≥86°F (30°C); keep tablets in the original package during the first 4 weeks of treatment; do not transfer tablets to a different container
Images
BRAND | FORM. | UNIT PRICE | PILL IMAGE |
---|---|---|---|
Venclexta Starting Pack oral - | 10 mg-50 mg- 100 mg tablet | ![]() | |
Venclexta oral - | 100 mg tablet | ![]() | |
Venclexta oral - | 100 mg tablet | ![]() | |
Venclexta oral - | 100 mg tablet | ![]() | |
Venclexta oral - | 50 mg tablet | ![]() | |
Venclexta oral - | 50 mg tablet | ![]() | |
Venclexta oral - | 10 mg tablet | ![]() | |
Venclexta oral - | 10 mg tablet | ![]() |
Copyright © 2010 First DataBank, Inc.
Formulary
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