
The study analyzed the selectivity of JAK inhibitors (JAKinibs) indicated or evaluated for rheumatic diseases for their JAK and cytokine selectivity in vitro. Ten JAKinibs were analyzed for JAK-isoform selectivity using various assays. The results showed that the inhibition of JAK kinase activity did not directly translate into cellular inhibition of JAK-STAT signaling. While the currently approved JAKinibs showed similar cytokine inhibition profiles with a preference for JAK1-mediated cytokines, novel types of JAKinibs showed a narrow cytokine inhibition profile specific for JAK3- or TYK2-mediated signaling.
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