Repotrectinib (1 brand name, 1 dosage form, 1 route)
Available dosage forms: CAPSULE.
Routes of administration: ORAL.
Brand Names
- AUGTYRO
Contraindications
None.
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: •Central Nervous System Adverse Reactions [see Warnings and Precautions (5.1)] •Interstitial Lung Disease (ILD)/Pneumonitis [see Warnings and Precautions (5.2)] •Hepatotoxicity [see Warnings and Precautions (5.3)] •Myalgia with Creatine Phosphokinase Elevation [see Warnings and Precautions (5.4)] •Hyperuricemia [see Warnings and Precautions (5.5)] •Skeletal Fractures [see Warnings and Precautions (5.6)] •Embryo-Fetal Toxicity [see Warnings and Precautions (5.7)]
Mechanism of Action
Repotrectinib is an inhibitor of proto-oncogene tyrosine-protein kinase ROS1 (ROS1) and of the tropomyosin receptor tyrosine kinases (TRKs) TRKA, TRKB, and TRKC. Fusion proteins that include ROS1 or TRK domains can drive tumorigenic potential through hyperactivation of downstream signaling pathways leading to unconstrained cell proliferation. Repotrectinib exhibited anti-tumor activity in cultured cells expressing ROS1 fusions and mutations including SDC4-ROS1, SDC4-ROS1 G2032R , CD74-ROS1, CD74-ROS1 G2032R , CD74-ROS1 D2033N , and CD74-ROS1 L2026M . Repotrectinib also inhibited cell proliferation in cultured cells expressing NTRK fusions and mutations including LMNA-TRKA, LMNA-TRKAG595R, EVT6-TRKBG639R, and ETV6-TRKCG623R.