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


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.

Potential Commercial Applications: Competitive Advantages:
  • Cardiovascular diseases
  • Ischemia
  • Fibrosis
  • Inflammation
  • Acute heart failure
  • Human and animal reproductive health
 
  • First and only small molecule agonists of RXFP1
  • Potent and highly selective
  • Bioavailable with excellent exposure
  • Easy to synthesize and scale-up


Development Stage:
  • Early-stage
  • In vitro data available
  • In vivo data available (animal)


Inventors:

Juan Marugan (NCATS)  ➽ more inventions...

Wei Zheng (NCATS)  ➽ more inventions...

Marc Ferrer-Alegre (NCATS)  ➽ more inventions...

Catherine Chen (NCATS)  ➽ more inventions...

Alexander Agoulnik

Noel Southall (NCATS)  ➽ more inventions...

Jingbo Xiao (NCATS)  ➽ more inventions...


Intellectual Property:
US Pat: 10,125,112 issued 2018-11-13
PCT Pat: 9,452,973 issued 2016-09-27
US Application No. 15/247,438 filed on 2016-08-25
US Application No. 14/398,830 filed on 2014-11-04

Publications:
Xiao J, et al. PMID 23764525
Chen CZ, et al. PMID 23212924

Collaboration Opportunity:

The National Center for Advancing Translational Sciences is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize small molecule agonists of RXFP1. For collaboration opportunities, please contact Krishna (Balki) Balakrishnan, Ph.D. at 301-217-2336 or balki@nih.gov.


Licensing Contact:
Ami Gadhia,
Email: ami.gadhia@nih.gov
Phone: 301-827-7159

OTT Reference No: E-072-2012-0
Updated: Nov 18, 2015