EPPIN Inhibitors
EP055
- User: Male
- Hormonal: Non-Hormonal
-
Delivery type:
- Oral
- Injectable
- Subdermal
-
Intended Duration:
- Pericoital
- Development Stage: Pre-Clinical
- Developer(s)/researcher(s): Eppin Pharma, Inc., University of North Carolina, São Paulo State University, Washington University, Queensland University
Details
- API: EP055
- Target: EPPIN
-
Mechanism of Action:
- Inhibition of Sperm Motility
- Inactive Materials: Not Yet Determined
- Regimen: Not Yet Determined
- MPT: Not Potential MPT
- Promising Attributes: Developers are seeking to create a product that is orally administered or injectable, non-hormonal, and potentially reversible.
Product Status
Active/Recent Pre-Clinical Development
History
2004: Animal studies conducted by UNC Chapel Hill conclude that EPPIN, a protein essential to the formation, viability, and motility of sperm, is an effective target for male contraception. This concept would continue to be evaluated in vivo and in vitro.
2010: Developers began evalutation of molecules that could inhibit EPPIN function. In 2014, Eppin Pharma was founded to further development of an oral male contraceptive using an EPPIN inhibitor and patent viable compounds.
2018: EP055 is synthesized and proven to inhibit EPPIN and contribute to significant reduction in sperm motility in a macaque model
2022: The Benhabbour Lab at UNC Chapel Hill presents animal study findings that suggest the viability of EP055 as a reversible, non-hormonal, long-acting male contraceptive delivered through injection.
2025: EP055's development team, inclusive of Eppin Pharma, the UNC Eshelman School of Pharmacy, the UNC School of Medicine, and the Joint Department of Biomedical Engineering at NC State and UNC Chapel Hill, publish findings documenting EP055's reformulation as an in-situ forming implant, noting that an optimized formulation elicited sustained release, appeared to produce a reversible effect in mice, and was well-tolerated.
Eppin Pharma has been confirmed to be inactive as a development group, but development of EP055 continues through collaborative network.
São Paulo State University has led identification of new compounds to selectively inhibit mouse sperm motility through EPPIN binding, with focus on targeting the SEMG1-binding pocket of EPPIN, to address deficiencies in original EP055 compound. São Paulo State University is actively conducting in vivo mouse experiments on EP055 as well, in collaboration with Queensland University, largely to further define the inhibitor's mechanism of action. However, they confirm they do not currently have capacity or intention to pursue clinical evaluation.
Publications
doi: 10.1016/j.mce.2005.12.039
doi: 10.1371/journal.pone.0195953
doi: 10.1038/s41598-023-41365-1
doi: 10.1093/molehr/gaab066
doi: 10.1016/j.pharmthera.2015.11.004
doi: 10.1095/biolreprod.112.101832
doi: 10.1095/biolreprod.111.094227
doi: 10.2164/jandrol.110.012781
doi: 10.1095/biolreprod.108.072942
PMID: 17644992
PMID: 17566290
doi: 10.1126/science.1099743