alisertib + rifampin

Alisertib + rifampin refers to the combination of two drugs: **alisertib**, a selective small molecule inhibitor of Aurora A kinase, and **rifampin**, a broad-spectrum antibiotic known as a strong inducer of CYP3A4 and other metabolic enzymes. Alisertib is under development primarily for the treatment of advanced malignancies, including various solid tumors and hematologic cancers. Rifampin, while not indicated for oncology, is studied here as a metabolic interactant to understand drug-drug interactions. Coadministration of rifampin with alisertib dramatically reduces the systemic exposure (AUC) of alisertib by approximately 50%, likely due to induction of metabolizing enzymes, ultimately shortening alisertib’s half-life and potentially compromising its therapeutic efficacy. Due to this interaction, strong inducers like rifampin are recommended to be avoided during alisertib treatment.