Vascular effects of serelaxin in patients with stable coronary artery disease: a randomized placebo-controlled trial

Cardiovasc Res. 2021 Jan 1;117(1):320-329. doi: 10.1093/cvr/cvz345.

Abstract

Aims: The effects of serelaxin, a recombinant form of human relaxin-2 peptide, on vascular function in the coronary microvascular and systemic macrovascular circulation remain largely unknown. This mechanistic, clinical study assessed the effects of serelaxin on myocardial perfusion, aortic stiffness, and safety in patients with stable coronary artery disease (CAD).

Methods and results: In this multicentre, double-blind, parallel-group, placebo-controlled study, 58 patients were randomized 1:1 to 48 h intravenous infusion of serelaxin (30 µg/kg/day) or matching placebo. The primary endpoints were change from baseline to 47 h post-initiation of the infusion in global myocardial perfusion reserve (MPR) assessed using adenosine stress perfusion cardiac magnetic resonance imaging, and applanation tonometry-derived augmentation index (AIx). Secondary endpoints were: change from baseline in AIx and pulse wave velocity, assessed at 47 h, Day 30, and Day 180; aortic distensibility at 47 h; pharmacokinetics and safety. Exploratory endpoints were the effect on cardiorenal biomarkers [N-terminal pro-brain natriuretic peptide (NT-proBNP), high-sensitivity troponin T (hsTnT), endothelin-1, and cystatin C]. Of 58 patients, 51 were included in the primary analysis (serelaxin, n = 25; placebo, n = 26). After 2 and 6 h of serelaxin infusion, mean placebo-corrected blood pressure reductions of -9.6 mmHg (P = 0.01) and -13.5 mmHg (P = 0.0003) for systolic blood pressure and -5.2 mmHg (P = 0.02) and -8.4 mmHg (P = 0.001) for diastolic blood pressure occurred. There were no between-group differences from baseline to 47 h in global MPR (-0.24 vs. -0.13, P = 0.44) or AIx (3.49% vs. 0.04%, P = 0.21) with serelaxin compared with placebo. Endothelin-1 and cystatin C levels decreased from baseline in the serelaxin group, and there were no clinically relevant changes observed with serelaxin for NT-proBNP or hsTnT. Similar numbers of serious adverse events were observed in both groups (serelaxin, n = 5; placebo, n = 7) to 180-day follow-up.

Conclusion: In patients with stable CAD, 48 h intravenous serelaxin reduced blood pressure but did not alter myocardial perfusion.

Keywords: Aortic stiffness; Coronary artery disease; Myocardial perfusion; Serelaxin.

Publication types

  • Clinical Trial, Phase II
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Arterial Pressure / drug effects*
  • Biomarkers / blood
  • Coronary Artery Disease / diagnostic imaging
  • Coronary Artery Disease / drug therapy*
  • Coronary Artery Disease / physiopathology
  • Coronary Circulation / drug effects*
  • Double-Blind Method
  • Female
  • Humans
  • Magnetic Resonance Imaging, Cine
  • Male
  • Manometry
  • Middle Aged
  • Myocardial Perfusion Imaging
  • Prospective Studies
  • Pulse Wave Analysis
  • Recombinant Proteins / adverse effects
  • Recombinant Proteins / pharmacokinetics
  • Recombinant Proteins / therapeutic use
  • Relaxin / adverse effects
  • Relaxin / pharmacokinetics
  • Relaxin / therapeutic use*
  • Treatment Outcome
  • United Kingdom
  • Vascular Stiffness / drug effects*
  • Vasodilation / drug effects*
  • Vasodilator Agents / adverse effects
  • Vasodilator Agents / pharmacokinetics
  • Vasodilator Agents / therapeutic use*

Substances

  • Biomarkers
  • Recombinant Proteins
  • Vasodilator Agents
  • serelaxin protein, human
  • Relaxin