Chemistry: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.[1][2] It is an orally bioavailable small molecule drug that blocks the initial interaction between apolipoprotein(a) and apoB100, thereby preventing the assembly of new lipoprotein(a) 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(a).[1]
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 (S)-2-[(3R)-pyrrolidin-3-yl]propanoic acid moiety. The molecule’s tripodal configuration enables simultaneous engagement of multiple lysine-binding sites on the apo(a) kringle domains, which is essential for potent inhibition of lipoprotein(a) assembly.[3]
References
- ↑ 1.0 1.1 "Current Clinical Trials for Treating Elevated Lipoprotein(a)". Current Cardiovascular Risk Reports 19 (1). December 2025. doi:10.1007/s12170-025-00759-8. PMID 40703143.
- ↑ "Potential of muvalaplin as a lipoprotein(a) inhibitor". Expert Opinion on Investigational Drugs 33 (1): 5–7. January 2024. doi:10.1080/13543784.2024.2302592. PMID 38186354.
- ↑ "Discovery of potent small-molecule inhibitors of lipoprotein(a) formation". Nature 629 (8013): 945–950. May 2024. doi:10.1038/s41586-024-07387-z. PMID 38720069. Bibcode: 2024Natur.629..945D.
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