06May 2023
In vitro profiling reveals JAK isoform selectivity differences among rheumatic-disease-evaluated JAK inhibitors

In vitro profiling reveals JAK isoform selectivity differences among rheumatic-disease-evaluated JAK inhibitors

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.

  • #rheumatology

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