trastuzumab deruxtecan + itraconazole

Trastuzumab deruxtecan + itraconazole refers to the co-administration of the HER2-targeted antibody-drug conjugate (ADC) trastuzumab deruxtecan and the potent CYP3A4 and P-glycoprotein (P-gp) inhibitor itraconazole. This combination is primarily utilized in clinical pharmacology trials, specifically Drug-Drug Interaction (DDI) studies, to evaluate the impact of metabolic inhibition on the pharmacokinetics of the deruxtecan payload (DXd). Trastuzumab deruxtecan consists of a humanized anti-HER2 IgG1 monoclonal antibody linked via a cathepsin B-cleavable linker to a topoisomerase I inhibitor payload. Itraconazole is a triazole antifungal agent that acts as a strong inhibitor of cytochrome P450 3A4 (CYP3A4), the primary enzyme responsible for the metabolism of DXd. These studies are critical for establishing safety and dosing guidelines for patients receiving trastuzumab deruxtecan who may require concomitant treatment with strong CYP3A4 inhibitors.

Other names

T-DXd + itraconazole