Drug intelligence / Profile preview

enzalutamide + itraconazole

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

Overview

This is a combination of **enzalutamide**, an androgen receptor inhibitor used primarily in the treatment of metastatic castration-resistant prostate cancer (mCRPC), and **itraconazole**, a triazole antifungal agent and strong inhibitor of cytochrome P450 3A4 (CYP3A4). Enzalutamide acts by inhibiting androgen receptor signaling, while itraconazole is included for its pharmacokinetic interaction, as it can increase enzalutamide exposure by inhibiting its CYP3A4-mediated metabolism. The combination does not have a unique clinical indication and is primarily referenced in the context of drug-drug interaction studies rather than as a formal fixed-dose pharmaceutical combination.[1][2][3]

02

Targets

CYP3A4 (Cytochrome P450 3A4)CYP51A1 (Sterol 14α-demethylase)AR (Adrenergic receptors)

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