Drug intelligence / Profile preview

crizotinib

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Crizotinib is a small molecule tyrosine kinase inhibitor used as an antineoplastic agent. It is primarily indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) with genetic alterations in anaplastic lymphoma kinase (ALK) or ROS1, relapsed or refractory systemic anaplastic large cell lymphoma (ALCL) that is ALK-positive, and unresectable, recurrent, or refractory inflammatory myofibroblastic tumor (IMT) that is ALK-positive. Crizotinib works by competitively inhibiting the ATP-binding site of several receptor tyrosine kinases including ALK, ROS1, hepatocyte growth factor receptor (HGFR/c-MET), and Recepteur d’Origine Nantais (RON). This inhibition blocks downstream signaling pathways involved in cell proliferation and survival. Crizotinib was developed by Pfizer and was first approved by the FDA in 2011 as the first-in-class therapy for ALK-positive NSCLC[1][3][4][5][6].

Brand names
Xalkori
Other names
crizotinib
02

Targets

MET (Mesenchymal-epithelial transition factor receptor)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)MST1R (Recepteur d'origine nantais)

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