nistration of multiple doses of a strong CYP3A4 inducer.
Rifampin: Avoid the concomitant use of venetoclax and rifampin; venetoclax levels may be altered. Consider alternative agents. Venetoclax is a substrate of CYP3A4 and P-glycoprotein (P-gp) and rifampin is a strong inducer of CYP3A4 and an inhibitor of P-gp. In a drug interaction study in healthy subjects (n = 10), the venetoclax Cmax and AUC values were decreased by 42% and 71%, respectively, following the co-administration of rifampin 600 mg/day for 13 days. In another drug interaction study (n = 11), the venetoclax Cmax and AUC values were increased by 106% and 78%, respectively, when a single 600-mg dose of rifampin was co-administered in healthy subjects.
Rifapentine: Avoid the concomitant use of venetoclax and rifapentine; venetoclax levels may be significantly decreased and its efficacy reduced. Venetoclax is a CYP3A4 substrate and rifapentine is a strong CYP3A4 inducer. Consider alternative agents. In a drug interaction study in healthy subjects (n = 10), the venetoclax Cmax and AUC values were decreased by 42% and 71%, respectively, following the co-administration of multiple doses of a strong CYP3A4 inducer.
Ritonavir: Avoid the concomitant use of venetoclax and lopinavir; ritonavir or ritonavir; venetoclax is a substrate of CYP3A4 and P-glycoprotein (P-gp) and ritonavir is a strong CYP3A4 and P-gp inhibitor. The concomitant use of these agents together is contraindicated during the initial and dose titration phase of venetoclax. If concomitant use of these drugs is required when the patient is on a steady venetoclax dose (after the titration phase), reduce the venetoclax dosage by at least 75% (maximum dose of 100 mg/day). If the strong CYP3A4 inhibitor is discontinued, wait 2 to 3 days and then resume the recommended venetoclax dosage (or prior dosage if less). Monitor patients for signs and symptoms of venetoclax toxicity such as hematologic toxicity, GI toxicity, and tumor lysis syndrome. In a drug interaction study, the venetoclax Cmax and AUC values were increased by 2.3-fold and 6.4-fold, respectively, when a strong CYP3A4 inhibitor was co-administered in NHL patients.
Rolapitant: Avoid the concomitant use of venetoclax and rolapitant. Venetoclax is a substrate of P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP); rolapitant is an inhibitor of P-gp and BCRP. Consider alternative agents. If concomitant use of these drugs is required, reduce the venetoclax dosage by at least 50% (maximum dose of 200 mg/day). If rolapitant is discontinued, wait 2 to 3 days and then resume the recommended venetoclax dosage (or prior dosage if less). Monitor patients for signs and symptoms of venetoclax toxicity such as hematologic toxicity, GI toxicity, and tumor lysis syndrome. In a drug interaction study (n = 11), the venetoclax Cmax and AUC values were increased by 106% and 78%, respectively, when a P-gp inhibitor was co-administered in healthy subjects.
Saquinavir: Avoid the concomitant use of venetoclax and saquinavir; venetoclax is a substrate of CYP3A4 and P-glycoprotein (P-gp) and saquinavir is a strong CYP3A4 and P-gp inhibitor. The concomitant use of these agents together is contraindicated during the initial and dose titration phase of venetoclax. If concomitant use of these drugs is required when the patient is on a steady venetoclax dose (after the titration phase), reduce the venetoclax dosage by at least 75% (maximum dose of 100 mg/day). If saquinavir is discontinued, wait 2 to 3 days and then r |
