Dagrocorat

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]

Dagrocorat
Clinical data
Other namesPF-00251802; PF-251802
Drug classSelective glucocorticoid receptor modulator
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC29H29F3N2O2
Molar mass494.558 g/mol g·mol−1
3D model (JSmol)

See also

References

  1. http://adisinsight.springer.com/drugs/800029003
  2. http://www.who.int/medicines/publications/druginformation/innlists/PL111.pdf
  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.
  7. http://adisinsight.springer.com/drugs/800029004



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