Technology ID
TAB-2498

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

E-Numbers
E-072-2012-0
Lead Inventor
Marugan, Juan (NHGRI)
Co-Inventors
Zheng, Wei (NHGRI)
Ferrer-Alegre, Marc (NCATS)
Chen, Catherine (NHGRI)
Agoulnik, Alexander (Florida International University (FIU))
Southall, Noel (NHGRI)
Xiao, Jingbo (NHGRI)
Applications
Vaccines­­­
Therapeutics
Research Materials
Diagnostics
Therapeutic Areas
Reproductive Health
Immunology
Cardiology
Development Status
  • Early-stage
  • In vitro data available
  • In vivo data available (animal)
Lead IC
NCATS
ICs
NHGRI
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

Request More Info

Licensing Contact:
Kalsi, Jasmine
jasmine.kalsi@nih.gov

Patents

  • US
    Provisional (PRV) 61/642,986
    Filed on 2012-05-04
    Status: Abandoned
  • Patent Cooperation Treaty
    (PCT) PCT/US13/32231
    Filed on 2013-03-15
    Status: Expired
  • US Patent 10,125,112
    Filed on 2016-08-25
    Status: Issued
  • US Patent 9,452,973
    Filed on 2014-11-04
    Status: Issued

Publications

Collaborations

  • Collaboration

Collaboration Description

  • 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.
Date Published