Пефицитиниб

Использование

Peficitinib can be used in therapeutic use and biological study of codrug and preparation of bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators.

Имя бренда

Smyraf^TM

Ферментативный ингибитор

This orally bioavailable JAK inhibitor and anti-rheumatoid arthritis drug (FW = 326.39 g/mol; CAS 944118-01-8; Solubility: 200 mM in DMSO), also named ASP015K, JNJ-54781532, and trans-4-[[5-hydroxy-2- adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, targets Janus Kinase JAK1, JAK2, JAK3 and the nonreceptor tyrosine kinase Tyk2 enzyme with IC50 values of 3.9, 5.0, 0.71 and 4.8 nM, respectively. Itsselectively suppress JAK3 or JAK1/2, respectively, may explain the weaker effects on red blood cells and platelets reported to be caused by JAK2 inhibition. Moreover, peficitinib improves symptoms in RA animal models after once-daily oral administration and demonstrates dosedependent improvement in psoriatic disease activities in a 6-week phase IIa study. The terminal mean half-life of peficitinib is 7–13 hours in pharmacological studies with healthy subjects