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Cyclic Peptides as Non-Hormonal Male Contraceptive Agents and Methods of Use Thereof

Summary
The National Institute of Child Health and Human Development (NICHD) seeks licensees and/or research co-development partners for the development of cyclic peptides or peptidomimetic molecules as potential non-hormonal contraceptives for males. The cyclic peptides disrupt spermatogenesis by inhibiting the phosphorylation of GRTH/DDX25 (gonadotropin-regulated testicular helicase).
NIH Reference Number
E-185-2021
Product Type
Keywords
  • Gonadotropin Regulated Testicular Helicase, GRTH/DDX25, GRTH, DDX25, Male Contraceptive, Peptide, Cyclic Peptide, Peptidomimetic, National Institute of Child Health and Human Development, NICHD, Dufau
Collaboration Opportunity
This invention is available for licensing and co-development.
Contact
Description of Technology

The available options for male contraceptives are limited. Current research is focused mainly on hormonal male contraceptives. This technology is a potential non-hormonal contraceptive using cyclic peptides to prevent spermatogenesis or the process of generating sperm within the male reproductive organs.  Specifically, this technology describes the development of a class of cyclic peptides inhibiting phosphorylation of gonadotropin-regulated testicular helicase (GRTH/DDX25). Images of the structures of the cyclic peptides currently designed and tested are included in a Journal of Medicinal Chemistry article published October 2, 2021, see PMID 34601876. These peptides have not exhibited toxicity in vitro. 

GRTH is expressed in the male gonad. Phosphorylation of GRTH is required for the successful completion of spermatogenesis. This invention from the National Institute of Child Health and Human Development (NICHD) demonstrates effective delivery into Cos-1 mammalian and germ cells and dose-dependent inhibition of GRTH phosphorylation.  The peptides inhibit GRTH phosphorylation by interfering with the kinase efficacy at the GRTH/PKA binding interface.

The NICHD seeks licensees and/or research co-development partners for the development of cyclic peptides or peptidomimetic molecules as potential non-hormonal contraceptives for males.

Potential Commercial Applications
  • Contraceptive for human males
  • Contraceptive for domestic animals (e.g., dogs and cats)
  • Contraceptive for livestock animals (e.g., cows and pigs)

 

Competitive Advantages

Non-hormonal
Does not reduce sex drive or physical enjoyment
Significant, unmet medical need given limited male contraceptive options (condoms, vasectomy, and withdrawal)
Novel approach could attract interest from pharmaceutical partners, whose involvement is needed for commercialization

 

Inventor(s)

Maria L Dufau MD PhD (NICHD), Murugananth Kumar Raju PhD (NICHD), Raghuveer Kavarthapu PhD (NICHD), Sergio A Hassan Ph.D (CIT)

Development Stage
Publications

Raju M, et al. Blockade of GRTH/DDX25 Phosphorylation by Cyclic Peptides Provides an Avenue for Developing a Nonhormonal Male Contraceptive.  [PMID 34601876]

Patent Status
  • U.S. Provisional: U.S. Provisional Patent Application Number 63/250,665, Filed 30 Sep 2021
Therapeutic Area
Posted
Wednesday, January 5, 2022