Definition

An orally bioavailable, selective inhibitor of Bruton’s tyrosine kinase (BTK), with potential antineoplastic activity. Upon oral administration, BTK inhibitor TL-895 targets and covalently binds to BTK, thereby preventing its activity. This leads to an inhibition of B cell receptor (BCR) signaling and inhibits cell proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.