PEP-0012Investigational

B7-33

Also known as

Single-chain relaxin-3/RXFP1 peptide agonist studied for metabolic and cardiorenal conditions. Preliminary evidence — early investigational stage with preclinical data.


Evidence

Preliminary· 2.8

Animal or in-vitro only

Risk band

Moderate

Known AEs, monitoring advised

Research goals

Summary

B7-33 is a single-chain functionally selective agonist of the relaxin family peptide receptor 1 (RXFP1), designed as a mimetic of human relaxin-2 (serelaxin) [1,4]. In preclinical models it replicated the vasoprotective effects of serelaxin, preventing trophoblast-induced endothelial dysfunction in mouse and rat mesenteric arteries [1], and in mice it attenuated adverse cardiac remodeling after myocardial infarction while improving cardiomyocyte survival and reducing endoplasmic-reticulum stress markers in vitro [2]. In a rodent cardiomyopathy model it reduced left ventricular fibrosis more rapidly than perindopril while retaining relaxin's cardioprotective effects [3], and PLGA coatings releasing B7-33 reduced fibrotic encapsulation around implants in mice [4]. All available evidence is preclinical (ex vivo, animal, and in-vitro); there are no human interventional trials, so its therapeutic value in people remains unproven.

Sources

  1. 1. B7-33 replicates the vasoprotective functions of human relaxin-2 (serelaxin) European journal of pharmacology, 2017.
  2. 2. B7-33, a Functionally Selective Relaxin Receptor 1 Agonist, Attenuates Myocardial Infarction-Related Adverse Cardiac Remodeling in Mice Journal of the American Heart Association, 2020.
  3. 3. The single-chain relaxin mimetic, B7-33, maintains the cardioprotective effects of relaxin and more rapidly reduces left ventricular fibrosis compared to perindopril in an experimental model of cardiomyopathy Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 2023.
  4. 4. Coatings Releasing the Relaxin Peptide Analogue B7-33 Reduce Fibrotic Encapsulation ACS applied materials & interfaces, 2019.

For educational purposes only.