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

Demei Chemical Technology Co., Ltd. is a modern high-tech enterprise integrating R&D, production, and sales. The company's founder, Dr. Arron, born in April 1975, graduated from the School of Mechanical Engineering at Yanshan University and has been engaged in research in the fields of mechanical engineering and chemical synthesis for many years. The company's products focus on the chemical industry, primarily dealing in chemical raw materials and chemical production machinery and equipment. With its strong technical capabilities, advanced production equipment, and strict quality management system, the company has earned the trust of customers worldwide.

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