Technology Bundle ID
TAB-2498

Novel Small Molecule Agonists of the Relaxin Receptor as Potential Therapy for Heart Failure and Fibrosis

Applications
Vaccines­­­
Therapeutics
Linked ID
E-072-2012-0
Lead Inventors
Juan Marugan (NCATS)
Co-Inventors
Alexander Agoulnik (Florida International University)
Catherine Chen (NCATS)
Jingbo Xiao (NCATS)
Marc Ferrer-Alegre (NCATS)
Noel Southall (NCATS)
Wei Zheng (NCATS)
Development Status
  • Early-stage
  • In vitro data available
  • In vivo data available (animal)
Therapeutic Areas
Reproductive Health
ICs
NCATS
The present invention is directed to novel small molecule agonists of the mammalian relaxin family receptor 1 (RXFP1), including human RXFP1. Activation of RXFP1 induces: 1) vasodilation due to up-regulation of the endothelin system; 2) extracellular matrix remodeling; 3) moderation of inflammation by reducing levels of inflammatory cytokines; and 4) angiogenesis. Small molecule agonists of RXFP1 may be useful in treating acute heart failure (AHF), scleroderma, fibrosis, other conditions associated with the biology of relaxin, and in improving reproductive health and wound healing. These compounds are the first and only small molecule agonists of RXFP1.
Commercial Applications
  • Cardiovascular diseases
  • Ischemia
  • Fibrosis
  • Inflammation
  • Acute heart failure
  • Human and animal reproductive health
Competitive Advantages
  • First and only small molecule agonists of RXFP1
  • Potent and highly selective
  • Bioavailable with excellent exposure
  • Easy to synthesize and scale-up

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