Drug intelligence / Profile preview

apalutamide + itraconazole

Development stage
Unknown
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral
01

Overview

**Apalutamide** is an orally administered, nonsteroidal antiandrogen that acts as a potent and selective antagonist of the androgen receptor, thereby blocking androgen-induced signaling crucial for prostate cancer progression. It is primarily indicated for non-metastatic, castration-resistant prostate cancer (NM-CRPC) and metastatic castration-sensitive prostate cancer. **Itraconazole** is an oral triazole antifungal agent that inhibits the fungal cytochrome P450 enzyme 14α-demethylase, affecting ergosterol synthesis and thus cell membrane integrity in fungi. In clinical pharmacology, **itraconazole** is notable as a strong inhibitor of CYP3A4 and P-glycoprotein, and is commonly studied or used to assess drug-drug interaction potential. The combination "apalutamide + itraconazole" is not a fixed-dose or approved combination product, but may be explored in drug interaction studies since itraconazole can markedly increase the exposure of apalutamide by inhibiting its metabolic clearance, posing potential risks of enhanced toxicity or adverse events. No branded coformulation exists for this combination.

Other names
apalutamide + itraconazoleJNJ-56021927 + itraconazoleARN-509 + itraconazole
02

Targets

CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)AR (Adrenergic receptors)

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