Chemistry:Fenclozic acid
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Short description: Chemical compound
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| Trade names | Myalex |
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| Formula | C11H8ClNO2S |
| Molar mass | 253.70 g·mol−1 |
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Fenclozic acid (proposed brand name Myalex) is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, and anti-inflammatory properties developed in 1960s by ICI Pharmaceuticals.[1][2] It failed to pass Phase III clinical trial and was withdrawn from clinical development in 1971 due to severe dose-related hepatotoxicity and jaundice in human, despite showing excellent preclinical safety profile and promising clinical efficacy in animal testings.[3][4] It is considered a classic example of human-specific drug induced liver injury linked to unique metabolic activation in humans.[4][5]
References
- ↑ "The pharmacology of fenclozic acid (2-(4-chlorophenyl)-thiazol-4-ylacetic acid; I.C.I. 54,450; 'Myalex'); a new compound with anti-inflammatory, analgesic and antipyretic activityl". British Journal of Pharmacology 35 (3): 487–497. March 1969. doi:10.1111/j.1476-5381.1969.tb08290.x. PMID 5809740.
- ↑ Hepworth W, Stacey GJ, "Aryl-thiazolyl-acetic acid derivatives", US patent 3538107, issued 1970, assigned to Imperial Chemical Industries Ltd
- ↑ "Hepatic effects of fenzlozic acid". Annals of the Rheumatic Diseases 29 (6): 684. November 1970. doi:10.1136/ard.29.6.684. PMID 5496073.
- ↑ 4.0 4.1 "In vitro exploration of potential mechanisms of toxicity of the human hepatotoxic drug fenclozic acid". Archives of Toxicology 87 (8): 1569–1579. August 2013. doi:10.1007/s00204-013-1056-y. PMID 23609606.
- ↑ "Acute liver effects, disposition and metabolic fate of [14C-fenclozic acid following oral administration to normal and bile-cannulated male C57BL/6J mice"]. Archives of Toxicology 91 (7): 2643–2653. July 2017. doi:10.1007/s00204-016-1894-5. PMID 27896398.
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