LOXO-292 – (2152628-33-4)

Selpercatinib, also known as LOXO-292, is a highly selective and potent RET kinase inhibitor designed to target cancers with RET gene alterations. This includes RET fusions and mutations, which are prevalent in various tumor types such as non-small cell lung cancer (NSCLC), medullary thyroid cancer (MTC), and other solid tumors. Selpercatinib has demonstrated significant efficacy in clinical trials, showing robust objective response rates (ORR) and sustained durability in heavily pretreated patients.

Selpercatinib’s mechanism of action involves direct inhibition of RET kinase. This specificity for RET over other tyrosine kinases contributes to its improved safety profile compared to multi-kinase inhibitors.

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Sources:

https://pubchem.ncbi.nlm.nih.gov/compound/134436906
https://www.medchemexpress.com/RET_kinase_inhibitor_1.html
https://www.medkoo.com/products/32309
https://investor.lilly.com/news-releases/news-release-details/lilly-announces-positive-results-selpercatinib-loxo-292
https://pmc.ncbi.nlm.nih.gov/articles/PMC7450975/
https://www.sciencedirect.com/science/article/pii/S0923753419604539