sembragiline + ketoconazole

The combination of **sembragiline** (RO4602522) and **ketoconazole** has been primarily utilized in clinical pharmacology studies to evaluate drug-drug interactions. Sembragiline is a potent, selective, and reversible inhibitor of **monoamine oxidase B (MAO-B)**, which was originally developed by Roche for the treatment of Alzheimer's disease. Ketoconazole is a broad-spectrum antifungal agent that also serves as a potent inhibitor of the **cytochrome P450 3A4 (CYP3A4)** enzyme. Because sembragiline is partially metabolized via the CYP3A4 pathway, clinical trials (such as NCT01422915) were conducted to assess the impact of strong CYP3A4 inhibition on the pharmacokinetics, safety, and tolerability of sembragiline. While sembragiline reached Phase 2 clinical development, its development for Alzheimer's disease was ultimately discontinued by Roche in 2015.

Brand names

Nizoral

Other names

RO4602522 + ketoconazolesembragiline + ketoconazoleRO-4602522 + ketoconazole