entrectinib

Entrectinib (RXDX-101) is a Trk, ROS1, and ALK inhibitor that inhibits TrkA, TrkB, TrkC, ROS1, and ALK (IC50=1/3/5/12/7 nM) with oral activity and blood-brain-barrier penetration. Entrectinib exhibits both antitumor and CNS activity.

Entrectinib-d4 is the deuterium-labeled isotope of Paquinimod. Entrectinib is an orally active inhibitor of TrkA/B/C, ROS1, and ALK, capable of crossing the blood-brain barrier and possessing central nervous system activity, with IC50 values of 1, 3, 5, 12, and 7 nM, respectively. It induces apoptosis and cell cycle arrest in cancer cells, exhibits antitumor efficacy, and mitigates bleomycin-induced pulmonary fibrosis in mice.

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is the deuterated form of Entrectinib. Entrectinib (NMS-E628) is an orally bioavailable inhibitor that effectively crosses the blood-brain barrier and exhibits central nervous system activity. It targets TrkA/B/C, ROS1, and ALK with IC50 values of 1, 3, 5, 12, and 7 nM, respectively. Entrectinib induces apoptosis and cell cycle arrest in cancer cells, demonstrates antitumor properties, and alleviates bleomycin-induced pulmonary fibrosis in mice.