Drug intelligence / Profile preview

enzalutamide + rifampin

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

**Enzalutamide + rifampin** is a combination of two pharmaceutical drugs, **enzalutamide** (an oral androgen receptor inhibitor) and **rifampin** (a rifamycin class antibiotic, and strong cytochrome P450 inducer). Enzalutamide is indicated for the treatment of advanced prostate cancer, specifically metastatic castration-resistant prostate cancer. It inhibits androgen receptor signaling at multiple steps, thereby blocking testosterone-driven prostate cancer growth. Rifampin is used to treat tuberculosis and other bacterial infections, and is a well-known strong inducer of CYP3A4 and a moderate inducer of CYP2C8. When used together, rifampin induces the metabolism of enzalutamide via CYP3A4 and CYP2C8, lowering enzalutamide plasma concentration and possibly undermining its efficacy. Enzalutamide is developed primarily by Medivation (now part of Pfizer). Rifampin is an older generic antibiotic originally developed by Ciba-Geigy (now Novartis). This combination is not a marketed product, but rather describes pharmacological co-administration relevant for drug-drug interaction studies.

Brand names
XtandiRifadinRimactane
Other names
enzalutamide plus rifampinenzalutamide combination with rifampin
02

Targets

AR (Adrenergic receptors)

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