Time over plasma concentrations >IC50 and percentage daily inhibition were compared between drugs for each pathway. The Kis of zasocitinib and deucravacitinib for the JAK1 JH2 domain were >15 000 and 1 nM, respectively. The Kis of zasocitinib and deucravacitinib for the TYK2 JH2 domain ...
Specifically, TAK-279 had an IC50 value of 0.002 μM for TYK2 inhibition, while its IC50 values for JAK1, JAK2, and JAK3 inhibition were all greater than 10 μM. This indicates that TAK-279 is highly selective for inhibition over JAK1, JAK2, and JAK3 inhibition. The in vivo eff...
Sigmoidal Emax models were fitted to the concentration鈥搃nhibition data from healthy donors to estimate IC50, Emax and Hill slope for each assay and compound. The obtained relationships were subsequently coupled to the clinical pharmacokinetic (PK) profiles of the compounds (population PK model for...