Which medications in the drug class Antineoplastics, Tyrosine 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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Antineoplastics, Tyrosine Kinase Inhibitors

Entrectinib (Rozlytrek)

Entrectinib and its major metabolite inhibit tropomyosin receptor tyrosine kinases (TRKs), proto-oncogene tyrosine-protein kinase ROS1 (ROS1), and anaplastic lymphoma kinase (ALK). It is indicated for metastatic NSCLC in adults whose tumors are ROS1-positive. Entrectinib is also indicated for NTRK genetic fusion solid tumors in pediatric and adult patients for whom there are no effective treatments.

Larotrectinib (Vitrakvi)

Larotrectinib is an oral tyrosine kinase inhibitor that binds to tropomyosin receptor kinase (TrK), preventing TrK activation. Thus, this induces cellular apoptosis and inhibition of cell growth in tumors. It is currently indicated for solid tumors that have a NTRK gene fusion in adults and pediatric patients without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have no satisfactory alternative treatments or that have progressed following treatment.

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