2565656-70-2

Muvalaplin (LY3473329) is an orally active, selective small molecule inhibitor of lipoprotein (a) (Lp (a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, preventing the disulphide bond and Lp(a) formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys[1][2][3][4][5].

[1] Bhatia HS, et al. Lipoprotein(a): Evidence for Role as a Causal Risk Factor in Cardiovascular Disease and Emerging Therapies. J Clin Med. 2022 Oct 13;11(20):6040. DOI:10.3390/jcm11206040
[2] Nicholls SJ, et al. Muvalaplin, an Oral Small Molecule Inhibitor of Lipoprotein(a) Formation: A Randomized Clinical Trial. JAMA. 2023 Sep 19;330(11):1042-1053. DOI:10.1001/jama.2023.16503
[3] Diaz N, et al. Discovery of potent small-molecule inhibitors of lipoprotein(a) formation. Nature. 2024 May;629(8013):945-950. DOI:10.1038/s41586-024-07387-z
[4] Hooper AJ, et al. Potential of muvalaplin as a lipoprotein(a) inhibitor. Expert Opin Investig Drugs. 2024 Jan;33(1):5-7. DOI:10.1080/13543784.2024.2302592
[5] Norata GD, et al. Oral strategies to target proprotein convertase subtilisin/kexin type 9 and lipoprotein(a): the new frontier of lipid lowering. Eur Heart J. 2023 Dec 21;44(48):5018-5020. DOI:10.1093/eurheartj/ehad682