Which medications in the drug class RET Kinase Inhibitors are used in the treatment of Non-Small Cell Lung Cancer (NSCLC)?

Updated: Jul 15, 2021
  • Author: Winston W Tan, MD, FACP; Chief Editor: Nagla Abdel Karim, MD, PhD  more...
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Answer

RET Kinase Inhibitors

Genomic alterations in rearranged during transfection (RET) kinase, which include fusions and activating point mutations, lead to overactive RET signaling and uncontrolled cell growth.

Selpercatinib (Retevmo)

Selpercatinib is a kinase inhibitor of wild-type rearranged during transfection (RET) and multiple mutated RET isoforms, as well as vascular endothelial growth factor receptors (VEGFR1, VEGFR3). It is indicated for metastatic RET fusion-positive NSCLC. 

Pralsetinib (Gavreto)

Pralsetinib is a selective inhibitor of RET alterations and resistant mutations; specifically designed to spare VEGFR2 and other kinases with the potential to drive off-target toxicity. This RET inhibitor exhibited antitumor activity in cultured cells and animal tumor implantation models harboring oncogenic RET fusions or mutations. It is Indicated for metastatic rearranged during transfection (RET) gene-positive NSCLC.


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