ALK (Anaplastic Lymphoma Kinase) Inhibitors
Small molecule inhibitors of EGFR (epidermal growth factor receptor) have been widely used in lung cancer therapy. A small subset (3–13 %) of non-small cell lung cancer (NSCLC) has been shown to have rearrangements in the ALK (anaplastic lymphoma kinase) gene. Over the last few years, ALK inhibitors have shown significant benefits in the management of ALK-positive NSCLC as compared to conventional chemotherapy. The treatment of patients with advanced NSCLC harboring chromosomal rearrangements of ALK has been revolutionized by the development of Crizotinib, a small molecule inhibitor of the tyrosine kinases ALK, ROS1, and MET. However, the limited progression-free survival (PFS) and the rate of progression in the CNS using Crizotinib for the treatment of NSCLC have led to the development of second-generation ALK-inhibitors such as Ceritinib (Zykadia) and Alectinib (Alecensa) that can inhibit most of the clinically observed ALK mutations that drive resistance to Crizotinib. Several new Tyrosine Kinase Inhibitors (TKIs) are in the various stages of clinical development for ALK-positive cancers. Many of these agents have activity both in the CNS and in cancers that have become resistant to Crizotinib. BioVision is proud to offer a wide variety of ALK inhibitors for research.
