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Ketoconazole 2%

University of California, Davis · FDA-approved active Small molecule

Ketoconazole inhibits fungal cytochrome P450 enzymes, disrupting ergosterol synthesis in the fungal cell membrane and causing cell death.

Ketoconazole inhibits fungal cytochrome P450 enzymes, disrupting ergosterol synthesis in the fungal cell membrane and causing cell death. Used for Tinea corporis (ringworm), Tinea cruris (jock itch), Tinea pedis (athlete's foot).

At a glance

Generic nameKetoconazole 2%
SponsorUniversity of California, Davis
Drug classImidazole antifungal
TargetFungal cytochrome P450 (CYP51 / lanosterol 14α-demethylase)
ModalitySmall molecule
Therapeutic areaInfectious Disease / Dermatology
PhaseFDA-approved

Mechanism of action

Ketoconazole is an imidazole antifungal that blocks the fungal enzyme lanosterol 14α-demethylase (CYP51), a key step in ergosterol biosynthesis. Without ergosterol, the fungal cell membrane becomes unstable and permeable, leading to leakage of cellular contents and fungal cell death. The 2% formulation is typically used for topical application to treat superficial fungal infections.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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