Drug Interactions between efavirenz and mobocertinib
This report displays the potential drug interactions for the following 2 drugs:
- efavirenz
- mobocertinib
Interactions between your drugs
efavirenz mobocertinib
Applies to: efavirenz and mobocertinib
GENERALLY AVOID: Coadministration with strong or moderate inducers of CYP450 3A4 may significantly decrease the plasma concentrations and anti-cancer activity of mobocertinib, which is primarily metabolized by the isoenzyme. Based on drug interaction studies using model-informed approaches, coadministration of mobocertinib with multiple doses of rifampin (a strong CYP450 3A4 inducer) is predicted to decrease the steady-state combined molar AUC (systemic exposure) of mobocertinib and its active metabolites by 92%, while coadministration with multiple doses of efavirenz (a moderate CYP450 3A4 inducer) is predicted to decrease this value by 58%.
MANAGEMENT: Coadministration of mobocertinib with strong or moderate CYP450 3A4 inducers should be avoided.
References
- (2021) "Product Information. Exkivity (mobocertinib)." Takeda Pharmaceuticals America
- (2022) "Product Information. Exkivity (mobocertinib)." Takeda UK Ltd
- (2022) "Product Information. Exkivity (mobocertinib)." Takeda Pharmaceuticals Australia Pty Ltd, EXKIVITY PI V1.0 (CC
Drug and food interactions
mobocertinib food
Applies to: mobocertinib
GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of mobocertinib. The mechanism may involve inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Inhibition of hepatic CYP450 3A4 may also contribute. The interaction has not been studied with grapefruit juice. Based on drug interaction studies using model-informed approaches, coadministration of mobocertinib with multiple doses of itraconazole or ketoconazole (strong CYP450 3A4 inhibitors) is predicted to increase the steady-state combined molar AUC (systemic exposure) of mobocertinib and its active metabolites by 374% to 419%, while coadministration with multiple doses of a moderate CYP450 3A4 inhibitor is predicted to increase this value by approximately 100% to 200%. In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands. Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition. Elevated plasma concentrations of mobocertinib may increase the risk for adverse effects such as QT prolongation, heart failure or reduced ejection fraction, cardiomyopathy, heart block, diarrhea, rash, stomatitis, fatigue, and musculoskeletal pain.
MANAGEMENT: Patients should avoid consumption of grapefruit and grapefruit juice during treatment with mobocertinib.
References
- (2021) "Product Information. Exkivity (mobocertinib)." Takeda Pharmaceuticals America
- (2022) "Product Information. Exkivity (mobocertinib)." Takeda UK Ltd
efavirenz food
Applies to: efavirenz
ADJUST DOSING INTERVAL: Administration with food increases the plasma concentrations of efavirenz and may increase the frequency of adverse reactions. According to the product labeling, administration of efavirenz capsules (600 mg single dose) with a high-fat/high-caloric meal (894 kcal, 54 g fat, 54% calories from fat) or a reduced-fat/normal-caloric meal (440 kcal, 2 g fat, 4% calories from fat) was associated with mean increases of 39% and 51% in efavirenz peak plasma concentration (Cmax) and 22% and 17% in systemic exposure (AUC), respectively, compared to administration under fasted conditions. For efavirenz tablets, administration of a single 600 mg dose with a high-fat/high-caloric meal (approximately 1000 kcal, 500-600 kcal from fat) resulted in a 79% increase in mean Cmax and a 28% increase in mean AUC of efavirenz relative to administration under fasted conditions.
MANAGEMENT: Efavirenz should be taken on an empty stomach, preferably at bedtime. Dosing at bedtime may improve the tolerability of nervous system symptoms such as dizziness, insomnia, impaired concentration, somnolence, abnormal dreams and hallucinations, although they often resolve on their own after the first 2 to 4 weeks of therapy . Patients should be advised of the potential for additive central nervous system effects when efavirenz is used concomitantly with alcohol or psychoactive drugs, and to avoid driving or operating hazardous machinery until they know how the medication affects them.
References
- (2001) "Product Information. Sustiva (efavirenz)." DuPont Pharmaceuticals
Therapeutic duplication warnings
No warnings were found for your selected drugs.
Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.
See also
Drug Interaction Classification
Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit. | |
Moderately clinically significant. Usually avoid combinations; use it only under special circumstances. | |
Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan. | |
No interaction information available. |
Further information
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
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