Muvalaplin

Pharmaceutical compound From Wikipedia, the free encyclopedia

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]

Other namesLY3473329
CAS Number
Quick facts Clinical data, Other names ...
Muvalaplin
Clinical data
Other namesLY3473329
Identifiers
  • (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
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
PDB ligand
Chemical and physical data
FormulaC42H54N4O6
Molar mass710.916 g·mol−1
3D model (JSmol)
  • 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
  • InChI=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
  • Key:BRLGERLDHZRETI-BGBFCPIGSA-N
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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

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