Entrectinib (Rxdx-101): Selectivity & Specificity

Entrectinib (Rxdx-101) is a potent inhibitor of TRKB (0.1 nM), TRKC (0.1 nM), ROS1 (0.2 nM), ALK (1.6 nM), TRKA (1.7 nM), TRKA/B/C fusions (0.3–1.3 nM), CYP3A4/5 (2000 nM), DENV2 (2430 nM), JAK2, TNK2, ACK1, NEK7, NLRP3. Entrectinib (Rxdx-101) exhibits the greatest inhibitory potency toward TRKB and TRKC (IC50 = 0.1 nM).