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Current Molecular Medicine

Editor-in-Chief

ISSN (Print): 1566-5240
ISSN (Online): 1875-5666

Review Article

Human Recombinant Relaxin (Serelaxin) as Anti-fibrotic Agent: Pharmacology, Limitations and Actual Perspectives

(E-pub Ahead of Print)
Author(s): Chiara Sassoli, Silvia Nistri, Flaminia Chellini and Daniele Bani*

DOI: 10.2174/1566524021666210309113650

open access plus

Abstract

Relaxin (recombinant human relaxin-2 hormone; RLX-2; serelaxin) had raised expectations as a new medication for fibrotic diseases. A plethora of in vitro and in vivo studies have offered convincing demonstrations that relaxin promotes remodelling of connective tissue extracellular matrix mediated by inhibition of multiple fibrogenic pathways, especially the downstream signalling of transforming growth factor (TGF)-β1, a major pro-fibrotic cytokine, and the recruitment and activation of myofibroblast, the main fibrosis-generating cells. However, all clinical trials with relaxin in patients with fibrotic diseases gave inconclusive results. In this review, we have summarized the molecular mechanisms of fibrosis, highlighting those which can be effectively targeted by relaxin. Then, we have performed a critical reappraisal of the clinical trials performed to-date with relaxin as anti-fibrotic drug, in order to highlight their key points of strength and weakness and to identify some future opportunities for the therapeutic use of relaxin, or its analogues, in fibrotic diseases and pathologic scarring which, in our opinion, deserve to be investigated.

Keywords: Connective tissue, extracellular matrix (ECM), fibrosis, myofibroblasts, relaxin (RLX), RXFP1, sereleaxin, TGF-β


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