CYP51 inhibitor
Lanosterol 14-alpha-demethylase (CYP51) inhibitor
CYP51 inhibitor — mechanism card
- ↓ fungal ergosterol synthesis
- Defective fungal membranes → fungistatic-to-fungicidal effect
- Blocks fungal ergosterol synthesis — the azoles
- 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 azole antifungal.
- Posaconazole — Broad triazole antifungal for prophylaxis in immunocompromised patients.
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