| 词条 | Fosdagrocorat |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = [(2R,4aS,10aR)-4a-Benzyl-7-[(2-methylpyridin-3-yl)carbamoyl]-2-(trifluoromethyl)-1,3,4,9,10,10a-hexahydrophenanthren-2-yl] dihydrogen phosphate | image = File:Fosdagrocorat.svg | width = | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 1044535-58-1 | CAS_supplemental = | class = Selective glucocorticoid receptor modulator | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 24872952 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 32699790 | UNII = HPI19004QS | KEGG = D10634 | ChEBI = | ChEMBL = 3137316 | C=29 | H=30 | F=3 | N=2 | O=5 | P=1 | molecular_weight = 574.537 g/mol | 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)OP(=O)(O)O)CC5=CC=CC=C5 | StdInChI_Ref = | StdInChI = 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 | StdInChIKey_Ref = | StdInChIKey = BVXLAHSJXXSWFF-KEKPKEOLSA-N | synonyms = PF-04171327; PF-4171327; Dagrocorat 2-(dihydrogen phosphate); Dagrocorat dihydrogen phosphate }}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] See also
References1. ^1 {{cite web|url=http://adisinsight.springer.com/drugs/800029004|title=Fosdagrocorat - AdisInsight|website=adisinsight.springer.com}} 2. ^International Nonproprietary Names for Pharmaceutical Substances (INN) 3. ^1 {{cite journal | vauthors = Yoshioka H, Yamada A, Nishiyama Y, Kagechika H, Hashimoto Y, Fujii S | title = Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold | journal = Bioorg. Med. Chem. | volume = 25 | issue = 13 | pages = 3461–3470 | year = 2017 | pmid = 28506584 | doi = 10.1016/j.bmc.2017.04.032 | url = }} 4. ^1 {{cite journal | vauthors = Strehl C, van der Goes MC, Bijlsma JW, Jacobs JW, Buttgereit F | title = Glucocorticoid-targeted therapies for the treatment of rheumatoid arthritis | journal = Expert Opin Investig Drugs | volume = 26 | issue = 2 | pages = 187–195 | year = 2017 | pmid = 28043173 | doi = 10.1080/13543784.2017.1276562 | url = }} 5. ^{{cite journal | vauthors = Miyoshi S, Hey-Hadavi J, Nagaoka M, Tammara B | title = Pharmacokinetics and food-effect of fosdagrocorat (PF-04171327), a dissociated agonist of the glucocorticoid receptor, in healthy adult Caucasian and Japanese subjects | journal = Int J Clin Pharmacol Ther | volume = 54 | issue = 12 | pages = 966–976 | year = 2016 | pmid = 27781421 | doi = 10.5414/CP202659 | url = }} 6. ^{{cite journal | vauthors = Stock T, Fleishaker D, Wang X, Mukherjee A, Mebus C | title = Improved disease activity with fosdagrocorat (PF-04171327), a partial agonist of the glucocorticoid receptor, in patients with rheumatoid arthritis: a Phase 2 randomized study | journal = Int J Rheum Dis | volume = | issue = | pages = | year = 2017 | pmid = 28328159 | doi = 10.1111/1756-185X.13053 | url = }} External links
11 : Anti-inflammatory agents|Antirheumatic products|Carboxamides|Glucocorticoids|Organophosphates|Phenanthrenes|Phenyl compounds|Prodrugs|Pyridines|Selective glucocorticoid receptor modulators|Trifluoromethyl compounds |
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