Notice2025-16416
Government Owned Inventions Available for Licensing or Collaboration: RFXP1 AGONISTS
Primary source
Metadata and text below are from the Federal Register, a public-domain U.S. government work. Always verify the official published version before relying on it for any legal matter.
Published
August 27, 2025
Issuing agencies
Health and Human Services DepartmentNational Institutes of Health
Abstract
The National Center for Advancing Translational Sciences (NCATS), an institute of the National Institutes of Health (NIH), Department of Health and Human Services (HHS), is giving notice of the licensing opportunities for the inventions listed below, which are owned by an agency of the U.S. Government, Florida International University (FIU), and University of South Florida (USF). The NCATS has taken the lead in both patenting and licensing via consolidation of rights under an Inter Institutional Agreement (IIA). The inventions are available for licensing and collaboration to achieve expeditious commercialization results of federally funded research and development.
Full Text
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<title>Federal Register, Volume 90 Issue 164 (Wednesday, August 27, 2025)</title>
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[Federal Register Volume 90, Number 164 (Wednesday, August 27, 2025)]
[Notices]
[Pages 41834-41835]
From the Federal Register Online via the Government Publishing Office [<a href="http://www.gpo.gov">www.gpo.gov</a>]
[FR Doc No: 2025-16416]
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DEPARTMENT OF HEALTH AND HUMAN SERVICES
National Institutes of Health
Government Owned Inventions Available for Licensing or
Collaboration: RFXP1 AGONISTS
AGENCY: National Institutes of Health, HHS.
ACTION: Notice.
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SUMMARY: The National Center for Advancing Translational Sciences
(NCATS), an institute of the National Institutes of Health (NIH),
Department of Health and Human Services (HHS), is giving notice of the
licensing opportunities for the inventions listed below, which are
owned by an agency of the U.S. Government, Florida International
University (FIU), and University of South Florida (USF). The NCATS has
taken the lead in both patenting and licensing via consolidation of
rights under an Inter Institutional Agreement (IIA). The inventions are
available for licensing and collaboration to achieve expeditious
commercialization results of federally funded research and development.
FOR FURTHER INFORMATION CONTACT: Inquiries related to these licensing
or collaboration opportunities should be directed to: Jasmine Kalsi,
M.S., Licensing and Patenting Manager, Office of Strategic Alliances
(OSA), NCATS, Email: <a href="/cdn-cgi/l/email-protection#b7ddd6c4daded9d299dcd6dbc4def7d9dedf99d0d8c1"><span class="__cf_email__" data-cfemail="b9d3d8cad4d0d7dc97d2d8d5cad0f9d7d0d197ded6cf">[email protected]</span></a> or Phone: 301-435-0129.
Respondents will be required to submit an ``Application for License to
Public Health Service Inventions.'' An executed CDA will be required to
receive copies of the patent applications.
SUPPLEMENTARY INFORMATION: NIH seeks to ensure that technologies
developed by NIH and its partners are expeditiously commercialized and
brought to practical use. NCATS is actively seeking a licensing partner
to facilitate the development and commercialization of a technology or
small molecule compounds that are in an early phase of development for
therapeutic interventions for cancers, fibrotic and vascular disease
including but not limited to breast cancer, solid tumors,
atherosclerosis, and liver fibrosis.
NCATS in collaboration with Florida International University (FIU)
and University of South Florida (USF) has identified low molecular
weight, highly potent, and efficient full RXFP1 agonists with low
cytotoxicity. The identification and characterization of these
compounds may lead to the development of a new class of cost-effective
drugs for the treatment of numerous cancers, fibrotic, and vascular
disorders.
It is well documented in literature that activation of RXFP1 by
relaxin induces: (1) up-regulation of the endothelin system which leads
to vasodilation; (2) extracellular matrix remodeling through regulation
of collagen deposition, cell invasiveness, proliferation, and overall
tissue homeostasis; (3) a moderation of inflammation by reducing levels
of inflammatory cytokines, such as TNF-a and TGF-b; and (4)
angiogenesis by activating transcription of VEGF.
The present invention is directed to novel relaxin receptor (RFXP1
receptor) small molecule agonists useful for treating relaxin-related
disorders including fibrosis, certain cancers, vascular calcifications,
including atherosclerosis, and heart failure. The RFXP1 agonists of
this invention possess a number of advantages not found in earlier
RFXP1 agonists. These properties include, for example, improved
bioavailability, low toxicity, and better activity in RXFP1-dependent
biological functional assays.
The development of small-molecule agonists of RXFP1 would have
numerous benefits and will allow investigating additional therapeutic
applications where chronic administration is required. NCATS has
identified a series of small-molecule agonists of RXFP1 which are
potent, highly selective, easy to synthesize, and with reasonable
metabolic and physical properties. Our molecules display similar
efficacy as the natural hormone in several functional assays.
Mutagenesis studies have mapped the specific regions responsible for
relaxin receptor activation by these compounds to an allosteric site on
the receptor. Finally, these compounds display good in vivo
pharmacokinetic properties and are currently being evaluated in vivo.
This Notice is in accordance with 35 U.S.C. 209 and 37 CFR part
404.
NIH Reference Number: E-145-2024-0.
Product Type: Therapeutics.
Therapeutic Area(s): Reproductive Health, Pulmonology, Oncology,
Geriatrics, Dermatology, Cardiology.
Potential Commercial Applications:
<bullet> Vascular health
<bullet> Fibrotic diseases
<bullet> Cancers
<bullet> Human reproductive health
Competitive Advantages:
<bullet> Potent and highly selective
<bullet> Bioavailable with excellent exposure
<bullet> Easy to synthesize and scale-up
Publication:
``Anti-apoptotic and Matrix Remodeling Actions of a Small Molecule
Agonist of the Human Relaxin Receptor, ML290 in Mice With Unilateral
Ureteral Obstruction.'' Ng HH, Soula M, Rivas B, Wilson KJ, Marugan JJ,
Agoulnik AI. Front Physiol. 2021 Jul 7.
Therapeutic effects of a small molecule agonist of the relaxin
receptor ML290 in liver fibrosis. Kaftanovskaya EM, Ng HH, Soula M,
Rivas B, Myhr C, Ho BA, Cervantes BA, Shupe TD, Devarasetty M, Hu X, Xu
X, Patnaik S, Wilson KJ, Barnaeva E, Ferrer M, Southall NT, Marugan JJ,
Bishop CE, Agoulnik IU, Agoulnik AI. FASEB J. 2019 Nov.
Optimization of the first small-molecule relaxin/insulin-like
family peptide receptor (RXFP1) agonists: Activation results in an
antifibrotic gene expression profile. Wilson KJ, Xiao J, Chen CZ, Huang
Z, Agoulnik IU, Ferrer
[[Page 41835]]
M, Southall N, Hu X, Zheng W, Xu X, Wang A, Myhr C, Barnaeva E, George
ER, Agoulnik AI, Marugan JJ. Eur J Med Chem. 2018 Aug 5.
ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.
Kocan M, Sarwar M, Ang SY, Xiao J, Marugan JJ, Hossain MA, Wang C,
Hutchinson DS, Samuel CS, Agoulnik AI, Bathgate RAD, Summers RJ. Sci
Rep. 2017 Jun 7.
Structural Insights into the Activation of Human Relaxin Family
Peptide Receptor 1 by Small-Molecule Agonists. Hu X, Myhr C, Huang Z,
Xiao J, Barnaeva E, Ho BA, Agoulnik IU, Ferrer M, Marugan JJ, Southall
N, Agoulnik AI. Biochemistry. 2016 Mar 29.
Activation of Relaxin Family Receptor 1 from Different Mammalian
Species by Relaxin Peptide and Small-Molecule Agonist ML290. Huang Z,
Myhr C, Bathgate RA, Ho BA, Bueno A, Hu X, Xiao J, Southall N, Barnaeva
E, Agoulnik IU, Marugan JJ, Ferrer M, Agoulnik AI. Front Endocrinol
(Lausanne). 2015 Aug 17.
Identification and optimization of small-molecule agonists of the
human relaxin hormone receptor RXFP1. Xiao J, Huang Z, Chen CZ,
Agoulnik IU, Southall N, Hu X, Jones RE, Ferrer M, Zheng W, Agoulnik
AI, Marugan JJ. Nat Commun. 2013.
Discovery, optimization, and biological activity of the first
potent and selective small-molecule agonist series of human relaxin
receptor 1 (RXFP1). Xiao J, Chen CZ, Huang Z, Agoulnik IU, Ferrer M,
Southall N, Hu X, Zheng W, Agoulnik AI, Marugan JJ. 2012 Mar 10
[updated 2013 May 8].
Identification of small-molecule agonists of human relaxin family
receptor 1 (RXFP1) by using a homogenous cell-based cAMP assay. Chen
CZ, Southall N, Xiao J, Marugan JJ, Ferrer M, Hu X, Jones RE, Feng S,
Agoulnik IU, Zheng W, Agoulnik AI. J Biomol Screen. 2013 Jul.
Patent Status: RFXP1 AGONISTS,'' U.S. Provisional Application No.
63/780,976 and NIH Reference No.: E-145-2024-0-US-02 filed 31 March
2025.
Development Stage: Preclinical (in vitro).
Date: August 20, 2025.
Joni L. Rutter,
Director, Office of the Director, National Center for Advancing
Translational Sciences.
[FR Doc. 2025-16416 Filed 8-26-25; 8:45 am]
BILLING CODE 4140-01-P
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