Fosdagrocorat

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.[1][3][4]

Fosdagrocorat
Clinical data
Other namesPF-04171327; PF-4171327; Dagrocorat 2-(dihydrogen phosphate); Dagrocorat dihydrogen phosphate
Drug classSelective glucocorticoid receptor modulator
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC29H30F3N2O5P
Molar mass574.537 g/mol g·mol−1
3D model (JSmol)

See also

References
  1. "Fosdagrocorat - AdisInsight". adisinsight.springer.com.
  2. International Nonproprietary Names for Pharmaceutical Substances (INN)
  3. 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.
  4. 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.
  5. 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.
  6. 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. doi:10.1111/1756-185X.13053. PMC 6084298. PMID 28328159.



This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.