brentuximab vedotin + ketoconazole

**Brentuximab vedotin + ketoconazole** is a pharmacological combination used for clinical drug-drug interaction studies rather than as a marketed co-formulation or therapeutic regimen. Brentuximab vedotin is an antibody-drug conjugate (ADC) consisting of an anti-CD30 monoclonal antibody linked to the microtubule-disrupting agent monomethyl auristatin E (MMAE). It selectively targets and delivers MMAE into CD30-expressing tumor cells, leading to cell cycle arrest and apoptosis. Ketoconazole is a potent oral inhibitor of the cytochrome P450 3A (CYP3A) enzyme, often used in pharmacokinetic studies to assess the impact of CYP3A inhibition on the metabolism of investigational drugs. When administered together, ketoconazole increases the exposure of MMAE (the cytotoxic payload of brentuximab vedotin), though exposures of the conjugated ADC itself are unaffected. This combination is important in oncology clinical pharmacology for defining dose adjustment and safety guidance when CYP3A-modifying agents are present.

Other names

brentuximab vedotinmonomethyl auristatin E antibody-drug conjugateketoconazole