getretinib

Getretinib is a highly selective and specific small molecule inhibitor of the RET (REarranged during Transfection) tyrosine kinase. Developed by the University of California San Diego, it utilizes novel chiral chemistry leveraging atropisomerism to achieve an atropisomerically stable analog. This design provides similar potency and improved selectivity compared to other next-generation RET inhibitors, with a lower molecular weight and enhanced ligand efficiencies towards RET. Getretinib is being investigated for its potential in treating neuroblastoma, a condition where increased RET expression is linked to poor prognosis. Its mechanism of action involves reducing the phosphorylation of RET, thereby inhibiting its downstream signaling pathways.

Other names

(R)-getretinib