RET Inhibitors

The RET (REarranged during Transfection) proto-oncogene codes for a receptor tyrosine kinase (RTK). The RET protein initiates signalling pathways such as Ras/MAP kinase, PI3 kinase/AKT and phospholipase C-γ. It plays an important role in the development of kidney and nervous system. It becomes oncogenic due to RET gene fusions, mutations and aberrant overexpression. Oncogenic RET causes papillary and medullary thyroid carcinoma, multiple endocrine neoplasias type 2A and 2B. RET gene alterations and overexpression also occurs in multiple cancer types such as breast carcinoma, pancreatic adenocarcinoma, non-small cell lung cancer (NSCLC), etc. Small molecule inhibitors of RET tyrosine kinase act by competing with ATP and suppressing downstream signaling pathways. Several RET inhibitors such as Pralsetininb, Vandetanib, Ponatinib, Carbozantinib, Lenvatinib, Sunitinib, which are also multiple tyrosine kinase inhibitors, are in clinical trials for different types of cancer. The first RET inhibitor Selpercatinib (Retevmo) has been approved by the U.S. FDA for use in NSCLC and thyroid cancer in 2020. BioVision offers a broad range of RET inhibitors for cancer research. BioVision also provides ready-to-use, EZSolutions of RET inhibitors for convenience and flexibility.