Description
Entrectinib (NMS-E628, RXDX-101,nMS-01191372) is a potent, ATP-competitive, orally available pan-TRK, ROS1 and ALK inhibitor with IC50 of 1/3/5/12/7nM for TRKA/TRKB/TRKC/ALK/ROS1, respectively; exhibits high antiproliferative activity against colorectal carcinoma cell line KM12 with IC50 of 17nM, abolishes autophosphorylation of TPM3-TRKA, concomitant with complete inhibition of the phosphorylation of PLCgamma1, AKT, and MAPK; induces regression in relevant human xenograft tumors, including the TRKA-dependent colorectal carcinoma KM12, ROS1-driven tumors, and several ALK-dependent models. Lung Cancer Phase 2 Clinical