Drug intelligence / Profile preview

volenrelaxin

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Small Molecules, Fc-Fusion Proteins → Carrier/Scaffold Proteins → Recombinant Proteins and Enzymes
Administration
Subcutaneous, Intravenous
01

Overview

Volenrelaxin (LY3540378) is a long-acting recombinant human relaxin protein developed by Eli Lilly and Company for the treatment of chronic heart failure with preserved ejection fraction (HFpEF). It is engineered as a fusion protein consisting of an immunoglobulin G (IgG) domain against serum albumin, fused to human relaxin-2 chains. This design extends its half-life in circulation via high-affinity binding to serum albumin. Volenrelaxin acts as a potent agonist of the relaxin family peptide receptor 1 (RXFP1), mimicking the effects of endogenous relaxin hormone, which regulates cardiovascular, renal, and pulmonary adaptations. Preclinical studies demonstrated that volenrelaxin increases renal plasma flow, reduces cardiac hypertrophy, improves diastolic function, lowers blood pressure, and enhances kidney perfusion without significant adverse effects. The drug was administered subcutaneously in clinical trials but development for HFpEF was terminated after interim analysis due to lack of efficacy on heart failure events[2][4][5][6].

Brand names
Relaxin-LA
Other names
IGG against serum albumin fused with relaxin 2, chain B (2-29) and relaxin 2 (chain A)
02

Targets

RXFP1 (Relaxin family peptide receptor 1)

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