Cardiovascular effects of relaxin-2: therapeutic potential and future perspectives

Abstract

The hormone relaxin-2 has emerged as a promising player in regulating the physiology of the cardiovascular system. Through binding to the relaxin family peptide receptor 1 (RXFP1), this hormone elicits multiple physiological responses including vasodilation induction, reduction of inflammation and oxidative stress, and angiogenesis stimulation. The role of relaxin-2, or its recombinant human form known as serelaxin, has been investigated in preclinical and clinical studies as a potential therapy for cardiovascular diseases, especially heart failure, whose current therapy is still unoptimized. However, evidence from past clinical trials has been inconsistent and further research is needed to fully understand the potential applications of relaxin-2. This review provides an overview of serelaxin use in clinical trials and discusses future directions in the development of relaxin-2 mimetics, which may offer new therapeutic options for patients with heart failure.

Seleno-relaxin analogues: effect of internal and external diselenide bonds on the foldability and a fibrosis-related factor of endometriotic stromal cells

“…5,6 Consequently, H2 relaxin shows diverse physiological functions, including anti-inflammatory, anti-fibrotic, and vasodilatory, and is currently undergoing clinical trials for treatment of variety of diseases in several countries. [7][8][9][10][11][12][13] Although a recent clinical trial (Novartis; second phase III) 14 found no significant effect of H2 relaxin on the treatment of acute heart failure, there is still a great deal of interest in H2 relaxin's pharmacological applications. Several research institutions, including pharmaceutical companies, have developed a variety of H2 relaxin-related formulation candidates, such as long-acting relaxins 15,16 , single-chain relaxin mimics [17][18][19] , and small molecular RXFP1 agonists 20,21 , and some of which are undergoing clinical trials.…”