Chemistry:Dagrocorat
From HandWiki
Short description: Chemical compound
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| Other names | PF-00251802; PF-251802 |
| Drug class | Selective glucocorticoid receptor modulator |
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| Formula | C29H29F3N2O2 |
| Molar mass | 494.558 g·mol−1 |
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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]
See also
References
- ↑ 1.0 1.1 "Dagrocorat - AdisInsight". http://adisinsight.springer.com/drugs/800029003.
- ↑ Drug Information World Health Organization
- ↑ 3.0 3.1 "Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold". Bioorg. Med. Chem. 25 (13): 3461–3470. 2017. doi:10.1016/j.bmc.2017.04.032. PMID 28506584.
- ↑ 4.0 4.1 "Glucocorticoid-targeted therapies for the treatment of rheumatoid arthritis". Expert Opin Investig Drugs 26 (2): 187–195. 2017. doi:10.1080/13543784.2017.1276562. PMID 28043173.
- ↑ "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. doi:10.5414/CP202659. PMID 27781421.
- ↑ "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. 2017. doi:10.1111/1756-185X.13053. PMID 28328159.
- ↑ "Fosdagrocorat - AdisInsight". http://adisinsight.springer.com/drugs/800029004.
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