CYP51 inhibitor
Lanosterol 14-alpha-demethylase (CYP51) inhibitor
- ↓ fungal ergosterol synthesis
- Defective fungal membranes → fungistatic-to-fungicidal effect
- Potent CYP3A4 inhibition drives major interactions
- Hepatotoxicity and QT prolongation
Drugs with this mechanism (3)
- Fluconazole — Azole antifungal with good CNS penetration; a CYP2C9/3A inhibitor.
- Miconazole — Topical imidazole for skin, vaginal and oral candidiasis; can still boost warfarin.
- Posaconazole — Broad triazole antifungal for prophylaxis in immunocompromised patients.
Self-check
- Which fungal membrane component is reduced by CYP51 inhibition?
Ergosterol. - Which CYP inhibition drives the major drug interactions described here?
CYP3A4.
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