RET inhibitors are targeted therapies that act on tumors with activating alterations in the RET proto-oncogene, such as point mutations or fusions. They fall under the category of the tyrosine kinase inhibitors, which work by inhibiting proteins involved in the abnormal growth of cancer cells. Existing molecules fall in two main categories: the older multikinase inhibitors and the more recent selective inhibitors. Although RET alterations are found at low frequency in a broad range of tumors, the three main indications for RET inhibitors today are non-small cell lung cancer (which harbor RET fusions at a frequency of 1-2%), medullary thyroid cancer (MTC, with activating RET mutations in 25% of cases) and papillary thyroid cancer (PTC, with up to 80% prevalence of fusions depending on the region). As of 2020, up to 48 fusion partners have been catalogued in NSCLC rearrangements, with KIF5B and CCDC6 being the most prevalent. [1] At least 10 different fusion variants have been described for KIF5B-RET, each with different breakpoints within the partner gene, but unclear clinical impact as of 2018. [2]
^Cite error: The named reference nsclc-partners was invoked but never defined (see the help page).
^Cite error: The named reference FerraraAuger2018 was invoked but never defined (see the help page).
RETinhibitors are targeted therapies that act on tumors with activating alterations in the RET proto-oncogene, such as point mutations or fusions. They...
is an experimental anticancer medication which acts as a RETinhibitor, as well as an inhibitor of SRC kinase. Pralsetinib Rebecsinib Resigratinib Selpercatinib...
acts as a RETinhibitor. Enbezotinib Pralsetinib Rebecsinib Resigratinib Selpercatinib Vodopivec DM, Hu MI (2022). "RET kinase inhibitors for RET-altered...
trial number NCT03037385 for "Phase 1/2 Study of the Highly-selective RETInhibitor, Pralsetinib (BLU-667), in Patients With Thyroid Cancer, Non-Small Cell...
Vandetanib is an inhibitor of vascular endothelial growth factor receptor-2, epidermal growth factor receptor, and RET tyrosine kinases. RET tyrosine kinases;...
A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation...
received at least four prior lines of therapy, including a proteasome inhibitor, an immunomodulatory agent, and an anti-CD38 monoclonal antibody. The...
whose tumors have an alteration (mutation or fusion) in a specific gene (RET which is short for "rearranged during transfection"). It is taken by mouth...
A protein kinase inhibitor (PKI) is a type of enzyme inhibitor that blocks the action of one or more protein kinases. Protein kinases are enzymes that...
another inhibitor to the malfunction enzyme that causes the leukemia. This inhibitor is a highly selective Bcr-Abl tyrosine kinase inhibitor. Sunitinib...
(RYK receptor family) RTK class XIII (DDR receptor family) RTK class XIV (RET receptor family) RTK class XV (ROS receptor family) RTK class XVI (LTK receptor...
carcinoma. It is a small molecule inhibitor of the tyrosine kinases c-Met and VEGFR2, and also inhibits AXL and RET. It was discovered and developed by...
as well. It was developed by Eisai Co. and acts as a multiple kinase inhibitor against the VEGFR1, VEGFR2 and VEGFR3 kinases. Lenvatinib is approved...
receptors exhibiting tyrosine kinase activity, such as Ret and Kit, play indispensable roles. Ret, for instance, plays a critical role in the formation...
normal cells to repopulate the bone marrow. A recent study showed that ATRA inhibits and degrades active PIN1. For its use in acne, tretinoin (along with other...
The P-glycoprotein inhibitor ketoconazole is known to increase blood plasma levels of nintedanib by a factor of 1.8; other inhibitors such as erythromycin...
by the U.S. FDA for this indication. Cabozantinib which is a potent inhibitor of RET, MET and VEGF was evaluated in a double-blind placebo controlled trial...
therapy medication used to treat cancer. Imatinib is a small molecule inhibitor targeting multiple tyrosine kinases such as CSF1R, ABL, c-KIT, FLT3, and...
kinase inhibitor. Many therapeutic approaches are aimed at the EGFR. Cetuximab and panitumumab are examples of monoclonal antibody inhibitors. However...
clinically significant interaction with potent CYP2D6 inhibitor terbinafine has been reported. A potent inhibitor of CYP2C19 and other cytochromes fluvoxamine...
Global Information