Which medications in the drug class Antineoplastics, Anaplastic Lymphoma 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, Anaplastic Lymphoma Kinase Inhibitor

Testing for ALK rearrangement is recommended in patients with metastatic NSCLC adenocarcinoma to determine if a therapy targeted toward ALK would be beneficial.

Crizotinib (Xalkori)

Inhibitor of receptor tyrosine kinases including, anaplastic lymphoma kinase (ALK), hepatocyte growth factor receptor (HGFR, c-Met), and recepteur d'origine nantais (RON). The gene's expression and signaling that contribute to increased cell proliferation and survival of the tumors becomes activated following the expression of ALK oncogenic fusion proteins. Indicated for locally advanced or metastatic non-small cell lung cancer (NSCLC) that is ALK positive as detected by an FDA-approved test. It is also indicated for NSCLC tumors positive for the ROS-1 gene mutation.

Ceritinib (Zykadia)

Ceritinib is a tyrosine kinase inhibitor that targets anaplastic lymphoma kinase (ALK), insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. It is indicated for ALK-positive, metastatic NSCLC.

Alectinib (Alecensa)

Tyrosine kinase inhibitor that targets ALK and RET. The major active metabolite of alectinib, M4, showed similar in vitro potency and activity. In nonclinical studies, alectinib inhibited ALK phosphorylation and ALK-mediated activation of the downstream signaling proteins STAT3 and AKT, and decreased tumor cell viability in multiple cell lines harboring ALK fusions, amplifications, or activating mutations.. It is indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive, metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test.

Brigatinib (Alunbrig)

Brigatinib inhibits autophosphorylation of ALK and ALK-mediated phosphorylation of the downstream signaling proteins STAT3, AKT, ERK1/2, and S6 in in vitro and in vivo assays. It is indicated for ALK-positive metastatic NSCLC in patients who have progressed on or are intolerant to crizotinib.

Lorlatinib (Lorbrena)

ALK/ROS1 tyrosine kinase inhibitor indicated for patients with ALK-positive metastatic NSCLC who have progressed on crizotinib and at least 1 other ALK inhibitor, or, alectinib or ceritinib as first ALK inhibitor therapy.

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