Drug Interaction Report

Consumer information for this interaction is not currently available.

MONITOR: Coadministration with inhibitors of CYP450 3A4 may increase the plasma concentrations of mobocertinib, which is primarily metabolized by the isoenzyme. 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. 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%. No data are available for other, less potent CYP450 3A4 inhibitors.

MANAGEMENT: Caution is advised when mobocertinib is used concomitantly with CYP450 3A4 inhibitors. Patients should be advised to seek medical attention if they experience symptoms that could indicate the occurrence of torsade de pointes such as dizziness, lightheadedness, fainting, palpitations, irregular heartbeat, shortness of breath, or syncope.

You should avoid consumption of grapefruit and grapefruit juice during treatment with mobocertinib. Grapefruit juice can increase the blood levels of mobocertinib. This may increase the risk of side effects such as diarrhea, nausea, vomiting, rash, fatigue, musculoskeletal pain, mouth sores and inflammation, heart failure, and rare but potentially serious and life-threatening irregular heart rhythm disorders. Talk to your doctor if you have any questions or concerns. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.