65277-42-1 | Ketoconazole

Chemical type

• Steroidogenesis inhibitor

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• Synthetic imidazole antifungal drug
• Weakly basic Active Pharmaceutical Ingredient (API)
• BCS Class II drug (low solubility, high permeability)

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Key properties

• Blocks multiple enzymes in adrenal steroidogenesis pathway, including CYP11B1 and CYP11B2
• Inhibits CYP7A (associated with hepatotoxicity)
• Strong inhibition of CYP3A4 (leads to drug-drug interactions, decreased testosterone, QTc prolongation)
• Less selective compared to osilodrostat

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• Poor aqueous solubility
• pKa values: 2.9 (piperazine ring), 6.5 (imidazole ring)
• Strongly pH-dependent solubility
• High permeability
• Melting point: ~155 °C
• Forms crystalline, salt, and co-amorphous systems
• Capable of hydrogen bonding interactions
• Undergoes Acid–Base Supersolubilization (ABS) with weak acids

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• Medical therapy for Cushing syndrome
• Alternative to osilodrostat when surgery is not possible

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• Broad-spectrum antifungal agent
• Oral, topical, and vaginal pharmaceutical formulations
• Model drug for crystal engineering studies
• Used in solubility enhancement research

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Classification by use

• Medications for Cushing syndrome
• Steroidogenesis inhibitors

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• Chemicals used as antifungal drugs
• Chemicals used as active pharmaceutical ingredients (APIs)
• Chemicals used in pharmaceutical formulation development

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A trustworthy factory and manufacturer

1. [Cite:1] Osilodrostat for Cyclic Cushing Disease, AACE Endocrinology and Diabetes, Volume 13, Issue 1, January–February 2026, Pages 17-21
2. [Cite:2] Crystal engineering to improve the physicochemical properties of ketoconazole in the presence of saccharin, Results in Chemistry, Volume 19, January 2026, 102919