Title: Teriflunomide
CAS Registry Number: 163451-81-8; 108605-62-5 (unspecified stereo)
CAS Name: (2Z)-2-Cyano-3-hydroxy-N--2-butenamide
Manufacturers' Codes: A-771726
Molecular Formula: C12H9F3N2O2
Molecular Weight: 270.21
Percent Composition: C 53.34%, H 3.36%, F 21.09%, N 10.37%, O 11.84%
Literature References: Disease modifying antirheumatic drug (DMARD); active metabolite of leflunomide, q.v. Prepn: R. R. Bartlett, F.-J. Kämmerer, WO 9117748; eidem, US 5494911 (1991, 1996 both to Hoechst). Identification as active metabolite: J. W. Patterson et al., J. Med. Chem. 35, 507 (1992). Phamacokinetics: J. Lucien et al., Ther. Drug Monit. 17, 454 (1995). Inhibits dihydroorotate dehydrogenase: J. P. Davis et al., Biochemistry 35, 1270 (1996). Configurational study: G. Bertolini et al., J. Med. Chem. 40, 2011 (1997); and crystal structure: C. Papageorgiou et al., Bioorg. Chem. 25, 233 (1997). HPLC determn in plasma: V. Chan et al., J. Chromatogr. B 803, 331 (2004).
Therap-Cat: Immunomodulator; in treatment of multiple sclerosis.
Keywords: Immunomodulator.
