Eppin
Alternative Name: Epididymal Protease Inhibitor
Description: The Eppin protein is specific to male reproductive tissue (secreted by Sertoli cells and epididymal epithelial cells) and covers the surface of spermatozoa. Eppin binds semenogelin and is critical for the protection of sperm from the enzymatic degradation of the semen coagulum, which frees the spermatozoa for motility and capacitation. Eppin is the contraceptive target for a small organic compound that binds Eppin and inhibits sperm motility. Blocking Eppin has been shown to inhibit the motility required for fertilization by decreasing the sperm pH and reducing calcium levels.
Target
Product Details
User: Male
Hormonal: No
Delivery Method: Oral
Duration Type: Short-acting
Role in reproduction: Sperm Function
Multipurpose Preventive Technology (MPT): No
Reference target/product: EP055
Status Details
Developer: Eppin Pharma, Inc.
Project Phase: Discovery and Early Development
Development Stage: Pre-clinical
Began discovery in: 2009
Active Development: Yes
Status Details: - Contraceptive efficacy has been shown in a non-human primate model. Anti-Eppin antibodies from male monkeys have been shown to inhibit human sperm motility (in vitro).
- High throughput screening has been conducted to identify compounds that bind to Eppin and cause inhibition of sperm motility, similar to the effects of anti-Eppin antibodies. Lead compounds are currently being tested for PK and toxicology.
- Results from successful trial in male macaques published in April 2018.
- Contraceptive efficacy has been shown in a non-human primate model. Anti-Eppin antibodies from male monkeys have been shown to inhibit human sperm motility (in vitro).
- High throughput screening has been conducted to identify compounds that bind to Eppin and cause inhibition of sperm motility, similar to the effects of anti-Eppin antibodies. Lead compounds are currently being tested for PK and toxicology.
- Results from successful trial in male macaques published in April 2018.
Additional Information
References: Eppin Pharma website: https://eppinpharmainc.com/
Silva EJR, Hamil KG, et al. (2012) Characterization of EPPIN's semenogelin I binding site: A contraceptive drug target. Biol Repro 87(3):56, 1-8.
O'Rand MG, Widgren EE, et al. (2006) Eppin: an effective target for male contraception. Mol Cell Endocrinol 250:157-162.
O'Rand MG, Hamil K, Adevai T, Zelinski M. (2018). Inhibition of sperm motility in male macaques with EP055, a potential non-hormonal male contraceptive. PLoS ONE 13(4): e0195953.
Eppin Pharma website: https://eppinpharmainc.com/
Silva EJR, Hamil KG, et al. (2012) Characterization of EPPIN's semenogelin I binding site: A contraceptive drug target. Biol Repro 87(3):56, 1-8.
O'Rand MG, Widgren EE, et al. (2006) Eppin: an effective target for male contraception. Mol Cell Endocrinol 250:157-162.
O'Rand MG, Hamil K, Adevai T, Zelinski M. (2018). Inhibition of sperm motility in male macaques with EP055, a potential non-hormonal male contraceptive. PLoS ONE 13(4): e0195953.