Repotrectinib (Augtyro)

General information

Class/mechanism from the NCI Drug Dictionary: An orally available inhibitor of multiple kinases, including the receptor tyrosine kinase anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), the neurotrophic tyrosine receptor kinase (NTRK) types 1, 2 and 3, the proto-oncogene SRC, and focal adhesion kinase (FAK), with potential antineoplastic activity. Upon oral administration, repotrectinib binds to and inhibits wild-type, point mutants and fusion proteins of ALK, ROS1, NTRK1-3, SRC, FAK and, to a lesser extent, other kinases. Inhibition of these kinases leads to the disruption of downstream signaling pathways and the inhibition of cell growth of tumors in which these kinases are overexpressed, rearranged or mutated.
Route: PO
Extravasation: n/a

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Diseases for which it is established

• ROS1+ NSCLC

History of changes in FDA indication

• 2023-11-15: Approved for locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC). (Based on TRIDENT-1)
• 2024-06-13: Granted accelerated approval for adult and pediatric patients 12 years and older with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion, are locally advanced or metastatic or where surgical resection is likely to result in severe morbidity, and that have progressed following treatment or have no satisfactory alternative therapy. (Based on TRIDENT-1)

Also known as

• Code name: TPX-0005
• Brand name: Augtyro