Taletrectinib in Previously Treated Metastatic CDH1-mutated Invasive Lobular Cancer (ILC)

Taletrectinib (AB-106/DS-6051b) is a potent, highly selective, orally bioavailable ROS1 and TRK family inhibitor, which has activity against mutations conferring resistance to crizotinib including in vitro and in vivo against the acquired ROS1 G2032R solvent front mutation. Taletrectinib has been shown to have anti-tumor activity against recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in an ATP dependent manner, in addition to completely inhibiting ACK, ALK, DDR1 and LTK at micromolar concentrations. Anti-tumor activity of taletrectinib was observed in two ROS1 rearranged lung cancer cell lines, glioblastoma cell line, and in NTRK-rearranged colorectal cancer cell lines.