linustedastat

Linustedastat (FOR-6219, OG-6219) is an oral small molecule inhibitor of 17β-hydroxysteroid dehydrogenase 1 (HSD17B1), an enzyme that catalyzes the final step in estradiol biosynthesis. By inhibiting HSD17B1, linustedastat reduces the local conversion of estrone to the more potent estrogen estradiol within endometriotic lesions. This targeted approach aims to decrease estrogen-driven growth of endometriosis tissue while minimizing systemic estrogen deficiency and its associated side effects. Linustedastat is being developed primarily for the treatment of endometriosis and has completed Phase I trials demonstrating safety and tolerability in healthy premenopausal and postmenopausal women. It is currently in Phase II clinical development for endometriosis[2][3][4][7].

Other names

linustedastat3-[(17E)-4-Fluoro-17-(hydroxyimino)estra-1,3,5(10)-trien-15β-yl]-N-(5-fluoropyridin-2-yl)propanamide