Dagrocorat Explained

Iupac Name:(4bS,7R,8aR)-4b-Benzyl-7-hydroxy-N-(2-methylpyridin-3-yl)-7-(trifluoromethyl)-5,6,8,8a,9,10-hexahydrophenanthrene-2-carboxamide
Width:250px
Cas Number:1044535-52-5
Class:Selective glucocorticoid receptor modulator
Pubchem:24873449
Chemspiderid:32700623
Unii:OPM23UN90U
Kegg:D10617
Chembl:3137304
C:29
H:29
F:3
N:2
O:2
Smiles:CC1=C(C=CC=N1)NC(=O)C2=CC3=C(C=C2)[C@@]4(CC[C@@](C[C@H]4CC3)(C(F)(F)F)O)CC5=CC=CC=C5
Stdinchi: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
Stdinchikey:QJJBNCHSWFGXML-KEKPKEOLSA-N
Synonyms:PF-00251802; PF-251802

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. The C2α dihydrogen phosphate ester of dagrocorat, fosdagrocorat, was also under investigation, but its development was terminated as well.[7]

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Notes and References

  1. Web site: Dagrocorat - AdisInsight.
  2. https://www.who.int/medicines/publications/druginformation/innlists/PL111.pdf Drug Information
  3. 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 .
  4. 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 .
  5. 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 .
  6. 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 .
  7. Web site: Fosdagrocorat - AdisInsight.

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