Muvalaplin


Muvalaplin is an investigational new drug that is being evaluated in clinical trials for the treatment of cardiovascular disease associated with elevated lipoprotein(a) levels. It is an orally bioavailable small molecule drug that blocks the initial interaction between apolipoprotein and apoB100, thereby preventing the assembly of new lipoprotein particles without interfering with plasminogen function. Large-scale studies are underway to assess muvalaplin’s safety and efficacy for reducing cardiovascular risk in people with high levels of lipoprotein.

Chemistry

Muvalaplin is a synthetic trivalent small molecule built around a central tribenzylamine scaffold. Attached to this core are three identical arms, each consisting of a -2-propanoic acid moiety. The molecule’s tripodal configuration enables simultaneous engagement of multiple lysine-binding sites on the apo kringle domains, which is essential for potent inhibition of lipoprotein assembly.