Dagrocorat

In this article, we will explore Dagrocorat from different approaches, analyzing its many facets and addressing various questions related to this topic. _Var1 is a topic of great relevance in today's society, and along these lines, we will delve into its importance, its implications and its impact in different areas. Through a detailed analysis, we will seek to further understand Dagrocorat and offer a comprehensive perspective that allows the reader to delve into this exciting topic.

Dagrocorat
Clinical data
Other namesPF-00251802; PF-251802
Drug classSelective glucocorticoid receptor modulator
Identifiers
  • (4bS,7R,8aR)-4b-Benzyl-7-hydroxy-N-(2-methylpyridin-3-yl)-7-(trifluoromethyl)-5,6,8,8a,9,10-hexahydrophenanthrene-2-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC29H29F3N2O2
Molar mass494.558 g·mol−1
3D model (JSmol)
  • CC1=C(C=CC=N1)NC(=O)C2=CC3=C(C=C2)4(CC(C4CC3)(C(F)(F)F)O)CC5=CC=CC=C5
  • InChI=1S/C29H29F3N2O2/c1-19-25(8-5-15-33-19)34-26(35)22-10-12-24-21(16-22)9-11-23-18-28(36,29(30,31)32)14-13-27(23,24)17-20-6-3-2-4-7-20/h2-8,10,12,15-16,23,36H,9,11,13-14,17-18H2,1H3,(H,34,35)/t23-,27+,28-/m1/s1
  • Key:QJJBNCHSWFGXML-KEKPKEOLSA-N

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. It is described as a partial agonist and "dissociable" agonist of the glucocorticoid receptor. The drug reached phase I clinical trials prior to the discontinuation of its development. The C2α dihydrogen phosphate ester of dagrocorat, fosdagrocorat, was also under investigation, but its development was terminated as well.

See also

References

  1. ^ a b "Dagrocorat - AdisInsight".
  2. ^ Drug Information World Health Organization Archived 2020-08-15 at the Wayback Machine
  3. ^ 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.
  4. ^ 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.
  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. 20 (8): 960–970. doi:10.1111/1756-185X.13053. PMC 6084298. PMID 28328159.
  7. ^ "Fosdagrocorat - AdisInsight".

External links


Stub icon

This hormonal preparation article is a stub. You can help Wikipedia by expanding it.

Wikious
Boobota
Sagapedia