LSK9985: a selective and potent BTK/JAK3 dual kinase inhibitor

Bruton’s tyrosine kinase (BTK) and Janus kinase 3 (JAK3) dual targeting presents a unique opportunity for the effective treatment of both hematologic and autoimmune disorders. BTK targeting has been clinically validated for the treatment of hematologic malignances such as chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL), and for the treatment of autoimmune disorders such as rheumatoid arthritis. Similar to BTK, JAK3 is primarily expressed in lymphoid hematopoietic cells and has also been validated as a clinical target in autoimmune diseases and has been implicated in a number of blood cancers. Dual targeting of both BTK and JAK3 has the potential to show synergistic effects in the treatment of both of these diseases.

LSK9985 was developed in the Center for Investigational Therapeutics of the Huntsman Cancer Institute where it was discovered through a fragment-based screening approach. LSK9985 was selected from a family of candidate compounds based on its desirable drug-like properties and its ability to both selectively and potently inhibit both BTK and JAK3. Further in vitro testing has shown that LSK-9985 displays impressive activity in a number of hematologic cancer cell lines compared to other BTK- and JAK3-targeting compounds.

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