Fosdagrocorat Explained

Fosdagrocorat (developmental code names PF-04171327 and PF-4171327; also known as dagrocorat 2-(dihydrogen phosphate)) 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 the C2 dihydrogen phosphate ester of dagrocorat, and acts as a prodrug of dagrocorat with improved pharmacokinetics.^[5] ^[6] The drug reached phase II clinical trials prior to the discontinuation of its development.

External links

Web site: Fosdagrocorat - AdisInsight. adisinsight.springer.com.
https://www.who.int/medicines/publications/druginformation/innlists/PL111.pdf International Nonproprietary Names for Pharmaceutical Substances (INN)
Yoshioka H, Yamada A, Nishiyama Y, Kagechika H, Hashimoto Y, Fujii S . Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold . Bioorg. Med. Chem. . 25 . 13 . 3461–3470 . 2017 . 28506584 . 10.1016/j.bmc.2017.04.032 .
Strehl C, van der Goes MC, Bijlsma JW, Jacobs JW, Buttgereit F . Glucocorticoid-targeted therapies for the treatment of rheumatoid arthritis . Expert Opin Investig Drugs . 26 . 2 . 187–195 . 2017 . 28043173 . 10.1080/13543784.2017.1276562 . 2306241 .
Miyoshi S, Hey-Hadavi J, Nagaoka M, Tammara B . 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 . 2016 . 27781421 . 10.5414/CP202659 .
Stock T, Fleishaker D, Wang X, Mukherjee A, Mebus C . 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 . 2017 . 20 . 8 . 960–970 . 28328159 . 10.1111/1756-185X.13053 . 6084298 .