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
Lead IC
NCATS
Co-Inventors
Zheng, Wei
Ferrer-Alegre, Marc
Chen, Catherine
Agoulnik, Alexander
Southall, Noel
Xiao, Jingbo
ICs
NCATS
FDA
Applications
Vaccines
Therapeutics
Research Materials
Diagnostics
Therapeutic Areas
Reproductive Health
Immunology
Cardiology
Development Stages
Pre-clinical (in vivo)
Development Status
- Early-stage
- In vitro data available
- In vivo data available (animal)
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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