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Relaxin

A two-chain insulin-family hormone studied for vasodilatory and antifibrotic actions; recombinant serelaxin reached heart-failure trials.

Overview

Relaxin is a two-chain peptide hormone of the insulin/relaxin family, best known for pregnancy-related remodeling of the reproductive tract. Beyond reproduction it is studied for vasodilatory, matrix-remodeling, and antifibrotic actions in the cardiovascular, renal, and other systems. A recombinant form of human relaxin-2, serelaxin, has been evaluated in clinical trials for acute heart failure.

Mechanism

Relaxin signals mainly through the G-protein-coupled receptor RXFP1, activating pathways that relax smooth muscle, stimulate nitric oxide production, and induce matrix metalloproteinases. These actions can reduce collagen deposition and myofibroblast activity, providing the basis for the proposed antifibrotic effects, and they increase cardiac output and renal perfusion in heart-failure models.

Dosing

In research settings relaxin is administered systemically in animal models of fibrosis and heart failure; serelaxin clinical trials used continuous intravenous infusion. There is no approved oral or outpatient peptide formulation, and doses are protocol-defined.

  • Animal protocols typically use systemic injection or infusion over days to weeks
  • Clinical heart-failure trials used intravenous infusion in hospitalized patients
  • Dose-response relationships are context-specific and not transferable to other uses

Expected Effects

  • Antifibrotic effects in rodent models of cardiac, renal, and pulmonary fibrosis
  • Vasodilation and increased arterial compliance in cardiovascular studies
  • Reduced markers of organ fibrosis in several disease models
  • Large clinical trials of serelaxin in acute heart failure reported mixed results on primary endpoints

Side Effects & Tolerability

Serelaxin infusion was generally well tolerated in trials, with hypotension as the main dose-limiting effect. Peptide-level adverse events were otherwise uncommon. Long-term safety data relate mainly to the completed heart-failure program.

Storage

Lyophilized peptide should be stored cold and desiccated, protected from light. Reconstituted solutions are typically aliquoted and refrigerated or frozen, avoiding repeated freeze-thaw cycles.

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