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Other names | PF-00251802; PF-251802 |
Drug class | Selective glucocorticoid receptor modulator |
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Formula | C29H29F3N2O2 |
Molar mass | 494.558 g·mol−1 |
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Dagrocorat (developmental code names PF-00251802, PF-251802) is a nonsteroidal but steroid-like selective glucocorticoid receptor modulator (SGRM) which was under development for the treatment of rheumatoid arthritis but was never marketed.[1][2][3][4] It is described as a partial agonist and "dissociable" agonist of the glucocorticoid receptor.[5][6] The drug reached phase I clinical trials prior to the discontinuation of its development.[1][3][4] The C2α dihydrogen phosphate ester of dagrocorat, fosdagrocorat, was also under investigation, but its development was terminated as well.[7]
See also
[edit]References
[edit]- ^ a b "Dagrocorat - AdisInsight".
- ^ Drug Information World Health Organization Archived 2020-08-15 at the Wayback Machine
- ^ a b Yoshioka H, Yamada A, Nishiyama Y, Kagechika H, Hashimoto Y, Fujii S (2017). "Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold". Bioorg. Med. Chem. 25 (13): 3461–3470. doi:10.1016/j.bmc.2017.04.032. PMID 28506584.
- ^ a b Strehl C, van der Goes MC, Bijlsma JW, Jacobs JW, Buttgereit F (2017). "Glucocorticoid-targeted therapies for the treatment of rheumatoid arthritis". Expert Opin Investig Drugs. 26 (2): 187–195. doi:10.1080/13543784.2017.1276562. PMID 28043173. S2CID 2306241.
- ^ Miyoshi S, Hey-Hadavi J, Nagaoka M, Tammara B (2016). "Pharmacokinetics and food-effect of fosdagrocorat (PF-04171327), a dissociated agonist of the glucocorticoid receptor, in healthy adult Caucasian and Japanese subjects". Int J Clin Pharmacol Ther. 54 (12): 966–976. doi:10.5414/CP202659. PMID 27781421.
- ^ Stock T, Fleishaker D, Wang X, Mukherjee A, Mebus C (2017). "Improved disease activity with fosdagrocorat (PF-04171327), a partial agonist of the glucocorticoid receptor, in patients with rheumatoid arthritis: a Phase 2 randomized study". Int J Rheum Dis. 20 (8): 960–970. doi:10.1111/1756-185X.13053. PMC 6084298. PMID 28328159.
- ^ "Fosdagrocorat - AdisInsight".
External links
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