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Fosdagrocorat

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Fosdagrocorat
Clinical data
Other namesPF-04171327; PF-4171327; Dagrocorat 2-(dihydrogen phosphate); Dagrocorat dihydrogen phosphate
Drug classSelective glucocorticoid receptor modulator
Identifiers
  • [(2R,4aS,10aR)-4a-Benzyl-7-[(2-methylpyridin-3-yl)carbamoyl]-2-(trifluoromethyl)-1,3,4,9,10,10a-hexahydrophenanthren-2-yl] dihydrogen phosphate
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC29H30F3N2O5P
Molar mass574.537 g·mol−1
3D model (JSmol)
  • CC1=C(C=CC=N1)NC(=O)C2=CC3=C(C=C2)[C@@]4(CC[C@@](C[C@H]4CC3)(C(F)(F)F)OP(=O)(O)O)CC5=CC=CC=C5
  • InChI=1S/C29H30F3N2O5P/c1-19-25(8-5-15-33-19)34-26(35)22-10-12-24-21(16-22)9-11-23-18-28(29(30,31)32,39-40(36,37)38)14-13-27(23,24)17-20-6-3-2-4-7-20/h2-8,10,12,15-16,23H,9,11,13-14,17-18H2,1H3,(H,34,35)(H2,36,37,38)/t23-,27+,28-/m1/s1
  • Key:BVXLAHSJXXSWFF-KEKPKEOLSA-N

Fosdagrocorat (developmental code namesPF-04171327 andPF-4171327; also known asdagrocorat 2-(dihydrogen phosphate)) is anonsteroidal butsteroid-likeselective glucocorticoid receptor modulator (SGRM) which was under development for the treatment ofrheumatoid arthritis but was never marketed.[1][2][3][4] It is the C2dihydrogenphosphateester ofdagrocorat, and acts as aprodrug of dagrocorat with improvedpharmacokinetics.[5][6] The drug reachedphase IIclinical trials prior to the discontinuation of its development.[1][3][4]

See also

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References

[edit]
  1. ^ab"Fosdagrocorat - AdisInsight".adisinsight.springer.com.
  2. ^International Nonproprietary Names for Pharmaceutical Substances (INN)
  3. ^abYoshioka 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. ^abStrehl 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.

External links

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GRTooltip Glucocorticoid receptor
Agonists
Mixed
(SEGRMsTooltip Selective glucocorticoid receptor agonists)
Antagonists
Others


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