brigimadlin + rifampicin

Brigimadlin + rifampicin is a combination of two pharmaceuticals: brigimadlin (BI 907828), a highly potent oral MDM2–p53 antagonist under development for cancer treatment, and rifampicin, a well-established antibiotic primarily used for tuberculosis. Brigimadlin works by inhibiting the interaction between MDM2 and p53, thus restoring p53 tumor suppressor activity; it is orally administered and displays a long half-life, manageable toxicity, and encouraging antitumor efficacy, particularly in MDM2-amplified sarcomas such as dedifferentiated liposarcoma[2][4]. Rifampicin is a potent inducer of metabolic enzymes (notably CYP3A4) and drug transporters (such as OATP1B1/1B3), which can alter the pharmacokinetics of co-administered compounds via induction or inhibition of these pathways[3][5]. Pharmacokinetic studies modeling the coadministration of brigimadlin and rifampicin reveal only minor exposure changes to brigimadlin when given with rifampicin (a decrease of about 6% due to increased metabolism), reflecting brigimadlin's low dependency on CYP3A4 metabolism, and a minor impact of OATP1B induction/inhibition by rifampicin[1]. No significant new safety signals, but drug-drug interaction potential requires monitoring.

Other names

brigimadlinrifampicinrifampin