| Cas number | 2565656-70-2 |
|---|---|
| Pubchem | 155369486 |
| Iuphar ligand | 12939 |
| Chemspiderid | 129341115 |
| Unii | HSU2KY4EFK |
| Kegg | D12460 |
| Chembl | 4802585 |
| Pdb ligand | A1AAK |
| Synonyms | LY3473329 |
| Iupac name | (2S)-3-[3-[[bis[[3-[(2S)-2-carboxy-2-[(3R)-pyrrolidin-3-yl]ethyl]phenyl]methyl]amino]methyl]phenyl]-2-[(3R)-pyrrolidin-3-yl]propanoic acid |
| C | 42 |
| H | 54 |
| N | 4 |
| O | 6 |
| Smiles | C1CNC[C@H]1[C@H](CC2=CC(=CC=C2)CN(CC3=CC=CC(=C3)C[C@@H]([C@H]4CCNC4)C(=O)O)CC5=CC=CC(=C5)C[C@@H]([C@H]6CCNC6)C(=O)O)C(=O)O |
| Stdinchi | InChI=1S/C42H54N4O6/c47-40(48)37(34-10-13-43-22-34)19-28-4-1-7-31(16-28)25-46(26-32-8-2-5-29(17-32)20-38(41(49)50)35-11-14-44-23-35)27-33-9-3-6-30(18-33)21-39(42(51)52)36-12-15-45-24-36/h1-9,16-18,34-39,43-45H,10-15,19-27H2,(H,47,48)(H,49,50)(H,51,52)/t34-,35-,36-,37-,38-,39-/m0/s1 |
| Stdinchikey | BRLGERLDHZRETI-BGBFCPIGSA-N |
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 small molecule built around a central tribenzylamine core. 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
- ^ De Los Reyes C, Rikhi RR, Doherty S, Hernandez S, Mirzai S, Shapiro MD, Christof M, McIntosh S, Wong ND, Block RC (December 2025). "Current Clinical Trials for Treating Elevated Lipoprotein(a)". Current Cardiovascular Risk Reports. 19 (1). doi:10.1007/s12170-025-00759-8. PMC 12282488. PMID 40703143
- ^ Hooper AJ, Fernando PM, Burnett JR (January 2024). "Potential of muvalaplin as a lipoprotein(a) inhibitor". Expert Opinion on Investigational Drugs. 33 (1): 5–7. doi:10.1080/13543784.2024.2302592. PMID 38186354
- ^ Diaz N, Perez C, Escribano AM, Sanz G, Priego J, Lafuente C, Barberis M, Calle L, Espinosa JF, Priest BT, Zhang HY, Nosie AK, Haas JV, Cannady E, Borel A, Schultze AE, Sauder JM, Hendle J, Weichert K, Nicholls SJ, Michael LF (May 2024). "Discovery of potent small-molecule inhibitors of lipoprotein(a) formation". Nature. 629 (8013): 945–950. Bibcode:2024Natur.629..945D. doi:10.1038/s41586-024-07387-z. PMC 11111404. PMID 38720069