Which medications in the drug class Antineoplastics, Tyrosine Kinase Inhibitor are used in the treatment of Non-Small Cell Lung Cancer (NSCLC)?

Updated: Jun 05, 2020
  • Author: Winston W Tan, MD, FACP; Chief Editor: Nagla Abdel Karim, MD, PhD  more...
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Antineoplastics, Tyrosine Kinase Inhibitor

Entrectinib and its major metabolite inhibit tropomyosin receptor tyrosine kinases (TRKs), proto-oncogene tyrosine-protein kinase ROS1 (ROS1), and anaplastic lymphoma kinase (ALK).Approval of entrectinib for NSCLC was based on pooled analysis of 3 multicenter, single-arm, open-label trials (ALKA, STARTRK-1, STARTRK-2). Of the 51 patients with ROS1-positive confirmed NSCLC who were assessed, ORR was 78% and 55% had a DOR that lasted for at least 12 months. Favorable results were also shown in patients with CNS metastases. [142, 143]

Entrectinib (Rozlytrek)

Entrectinib is indicated for metastatic NSCLC in adults whose tumors are ROS1-positive.

Capmatinib (Tabrecta)

Capmatinib is a kinase inhibitor that targets mesenchymal-epithelial transition (MET) , including the exon 14 skipping mutation. MET tyrosine kinase stimulates cell scattering, invasion, protection from apoptosis, and angiogenesis. A variety of cancers (eg, lung, gastric) are associated with dysregulation of MET, owing to MET amplifications and exon 14 skipping mutations. Capmatinib is indicated for metastatic NSCLC in adults whose tumors have a mutation that leads to exon 14 skipping.

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