Eli Lilly Initiates Phase 3 Trial of Oral Small-Molecule Lp(a) Inhibitor Muvalaplin

▎Armstrong

September 2025On the 5th day of the month, Eli Lilly registered the small molecule Lpa inhibitor Muvalaplin on the Clinicaltrials.gov website for the purpose of reducingRisk of MACE in Patients with Elevated Lp(a) LevelsPhase III clinical trial.

This Phase III clinical trial plans to enroll 10,450 subjects with elevated Lp(a) and is expected to be completed by 2031.

Eli Lilly published the phase II clinical data of Muvalaplin in the JAMA journal in November 2024.

MuvalaplinAt 12 weeks of treatment, compared with placebo,Muvalaplin 10 mg, 60 mg group, 240 mg dose groupThe respective reductions in Lpa from baseline were47.6%、81.7%、85.8%。

Eli Lilly has made a deep strategic layout around Lpa. The Lpa siRNA new drug Lepodisiran entered phase III clinical trials last year, and its phase II clinical data was published in the New England Journal of Medicine this May.

Lepodisiran 400mg dose group, administered once every six months, can reduce Lpa by 93.9%, with a significantly greater inhibitory effect compared to small molecules.

Summary

As chronic disease drugs, both small molecules and small nucleic acids have their application scenarios. siRNA can be administered once every 3 to 6 months, while small molecules can be delivered orally. Amgen and Novartis have invested in small nucleic acid drugs, Eli Lilly and Company has invested in both small nucleic acids and siRNA drugs, Merck has introduced a small molecule Lpa inhibitor from Hengrui Medicine, and AstraZeneca has introduced a small molecule Lpa inhibitor from CSPC Pharmaceutical Group.