Pyrazoles are organic compounds of the general formula C3H3N2H. It is a five-membered heterocycle consisting of three carbon atoms and two adjacent nitrogen atoms. As an H-bond-donating heterocycle, pyrazole has been used as a more lipophilic and metabolically more stable bioisomer of phenol. Pyrazoles have attracted more and more attention due to their broad spectrum of action and strong efficacy.
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Repotrectinib receives approval for the treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC) from the U.S. FDA on November 15, 2023. ROS1 gene is altered in about 1-2% of patients with NSCLC. ROS1-positive lung cancer tends to be aggressive and can spread to the brain and the bones.
Repotrectinib is a highly potent and differentiated small molecule TKI that binds inside the ATP pocket, and is active against both wild-type and resistant mutations, including solvent front and gatekeeper mutations. Repotrectinib is expected to enter the U.S. market in mid-December 2023.