Recombinant human H2 relaxin (serelaxin) as a cardiovascular drug: aiming at the right target

Drug Discov Today. 2020 Jul;25(7):1239-1244. doi: 10.1016/j.drudis.2020.04.014. Epub 2020 Apr 29.

Abstract

Serelaxin (recombinant human relaxin-2 hormone; RLX-2) had raised expectations as a new medication for cardiovascular diseases. Evidence from preclinical studies indicated that serelaxin has chronotropic, inotropic, and anti-arrhythmic actions on the myocardium and cardioprotective effects mediated by vasodilation, angiogenesis, and inhibition of inflammation and fibrosis. However, clinical trials with serelaxin in patients with acute heart failure (AHF) gave inconclusive results. A critical reappraisal of the comprehensive cardiovascular actions of serelaxin clearly delineates acute myocardial infarction (AMI) as a feasible therapeutic target. Serelaxin acts at multiple levels on the pathogenic mechanisms of AMI and previous in vivo studies suggest that its administration at reperfusion affords myocardial salvage. Thus, serelaxin could be an effective adjunctive medical therapy to coronary angioplasty.

Publication types

  • Review

MeSH terms

  • Animals
  • Cardiovascular Agents / pharmacology*
  • Cardiovascular Agents / therapeutic use*
  • Humans
  • Myocardium / metabolism
  • Recombinant Proteins / therapeutic use*
  • Relaxin / therapeutic use*

Substances

  • Cardiovascular Agents
  • RLN2 protein, human
  • Recombinant Proteins
  • serelaxin protein, human
  • Relaxin