Entrectinib

Entrectinib is an inhibitor of TrkA (IC₅₀ = 1.7 nM), TrkB (IC₅₀ = 0.1 nM), and TrkC (IC₅₀ = 0.1 nM), as well as C-ros oncogene 1 (ROS1; IC₅₀ = 0.2 nM) and anaplastic lymphoma kinase (ALK; IC₅₀ = 1.6 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with L1196M or C1156Y resistance mutations, and inhibits ALK‐dependent signaling