a400

A400 (also known as EP0031 or KL590586) is a next-generation, highly selective RET inhibitor developed for the treatment of cancers driven by RET gene alterations. It is a small molecule designed to inhibit key RET kinases with broad activity against common RET fusions and mutations. Preclinical studies have demonstrated potent in vitro and in vivo inhibition of RET kinases and improved blood-brain barrier penetration compared to first-generation selective RET inhibitors (SRIs). Clinical trials have shown promising efficacy in patients with advanced non-small cell lung cancer (NSCLC), thyroid cancer, and other solid tumors harboring RET alterations—including those previously treated with first-generation SRIs or presenting with brain metastases. The drug has received Fast Track Designation and Orphan Drug Designation from the FDA for the treatment of RET fusion-positive NSCLC and solid tumors[1][2][3][4][7].

Brand names

Ningtailai宁泰莱

Other names

EP0031EP-0031EP 0031KL590586KL-590586KL 590586