Description
TPX 0005 (Ropotrectinib, Repotrectinib, TPX0005) is a novel ALK/ROS1/TRK inhibitor, effectively inhibits a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants; potently inhibits WT ALK (IC50=1.01nM) and mutant ALKs including ALK G1202R (IC50=1.26nM) and ALK L1196M (IC50=1.08nM); is also a potent SRC inhibitor (IC50=5.3nM); shows low nano-molar activities against CD74-ROS1 G2032R (IC50=8.4nM), LMNA-TRKA G595R (IC50=0.4nM), TEL-TRKB G639R (IC50=1.9nM) and TEL-TRKC G623R (IC50=0.4nM) in Ba/F3 cell proliferation assays; dramatically causes tumor growth inhibition and tumor regression in xenograft tumor model; demonstrates desired druglike properties and good safety profile. Solid Tumors Phase 2 Clinical