TG-1701 (BTK Inhibitor)

TG-1701 is a novel, orally available and covalently-bound BTK inhibitor that exhibits superior selectivity to BTK compared to ibrutinib in in vitro kinase screening. Bruton's tyrosine kinase (BTK) is an essential component of the B-cell receptor signaling pathways and a critical nod that activates several transcription factors including NFKB and NFAT. Those nuclear factors regulate the survival, activation, proliferation, and differentiation of B lymphocytes. Targeting BTK with small molecule inhibitors has been demonstrated to be an effective treatment option for B-cell lymphomas and autoimmune diseases.

TG-1701 is currently in a Phase I clinical trial in China.