Turning Point Therapeutics, Inc discovered novel repotrectinib, a leading drug candidate for the treatment of patients with advanced solid tumors having an NTRK gene fusion.
Repotrectinib is a therapeutic option for patients who have shown progress with 1 or 2 prior TRK TKIs after treatment, with or without prior chemotherapy and for patients who remain with no other options.
Repotrectinib consists of a small macrocyclic TKI of ROS1, TRK, and ALK. It is bind with the active kinase conformation and avoids steric interference from several clinically-resistant mutations.
Repotrectinib has also been granted an Orphan Drug designation in 2017. U.S. Food and Drug Administration (FDA) grants Breakthrough Therapy Designation to lead drug candidate, repotrectinib for the treatment of TKI-pretreated advanced solid tumors.