Crizotinib (Xalkori) is an oral kinase inhibitor that may be used to treat:
1.Adults with non-small cell lung cancer which has spread to other parts of the body and is caused by a defect in either a gene called ALK (anaplastic lymphoma kinase) or a gene called ROS1. An ROS1 error occurs in about 1 percent of people with NSCLC, while and ALK error occurs in about 5 percent of cases.
2.Children aged 1 year and older and young adults with anaplastic large cell lymphoma (ALCL) that is ALK-positive. It is used when the ALCL has returned or when a treatment has been tried and it did not work or is no longer working.
3.Adults and children aged 1 year of age and older with ALK-positive inflammatory myofibroblastic tumors (IMT). It is used when the IMT cannot be surgically removed or has returned, or when a treatment has been tried and it did not work or is no longer working.
Crizotinib works by blocking the effects of receptor tyrosine kinases (RTKs), such as ALK, hepatocyte growth factor receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d’Origine Nantais (RON). RTKs are essential components of signaling pathways that mediate cell-to-cell communication. Defects in RTKs can result in increased cell proliferation and survival in tumors expressing these proteins. Laboratory research has shown crizotinib-induced cell death and tumor regression in ALCL-derived cell lines that contained nucleophosmin-ALK or c-Met.
Crizotinib was FDA-approved on August 26, 2011. When it was approved, it was the first therapy to be approved for patients with ROS1-positive NSCLC.
