| RET inhibitor | |
|---|---|
| Drug class | |
 Selpercatinib inhibitor (magenta spheres) complexed with RET kinase (rainbow colored) | |
| Class identifiers | |
| ATC code | L01EX |
| Biological target | RET proto-oncogene |
| Clinical data | |
| WebMD | RxList |
| External links | |
| MeSH | D051096 |
| Legal status | |
| In Wikidata | |
RET kinase inhibitors are a type of targeted cancer treatment that block abnormally activated RET proto-oncogene, a protein involved in cell growth. These inhibitors are used to treat cancers like non-small cell lung cancer, medullary thyroid carcinoma, and some types of colorectal and pancreatic cancer.
RET inhibitors 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 a low frequency across a broad range of tumors, the three main indications for RET inhibitors today are non-small cell lung cancer (NSCLC, which harbors RET fusions in 1-2% of cases), medullary thyroid cancer (MTC, with activating RET mutations in 25% of cases), and papillary thyroid cancer (PTC, where RET fusions are present in up to 80% of cases, depending on the region). As of 2020, up to 48 fusion partners have been cataloged 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 their clinical impact remains unclear as of 2018.[2]