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Review
. 2016 Jan;157:105-11.
doi: 10.1016/j.pharmthera.2015.11.004. Epub 2015 Nov 22.

Non-hormonal Male Contraception: A Review and Development of an Eppin Based Contraceptive

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Free PMC article
Review

Non-hormonal Male Contraception: A Review and Development of an Eppin Based Contraceptive

Michael G O'Rand et al. Pharmacol Ther. .
Free PMC article

Abstract

Developing a non-hormonal male contraceptive requires identifying and characterizing an appropriate target and demonstrating its essential role in reproduction. Here we review the development of male contraceptive targets and the current therapeutic agents under consideration. In addition, the development of EPPIN as a target for contraception is reviewed. EPPIN is a well characterized surface protein on human spermatozoa that has an essential function in primate reproduction. EPPIN is discussed as an example of target development, testing in non-human primates, and the search for small organic compounds that mimic contraceptive antibodies; binding EPPIN and blocking sperm motility. Although many hurdles remain before the success of a non-hormonal male contraceptive, continued persistence should yield a marketable product.

Keywords: EPPIN; Male contraception; Reproductive pharmacology; Semenogelin; Sperm.

Conflict of interest statement

Conflict of interest statement:

Dr. Silva has no conflicts of interest to declare. Drs. O’Rand and Hamil have affiliations with Eppin Pharma Inc.

Figures

Figure 1
Figure 1
(A) 3D model of the EPPIN C-terminal with the SEMG1 binding sequence shown in blue. Three of EPPIN’s key amino acids within the binding site are indicated by the arrows: Y107, Q118 and N116. (B) The SEMG1 peptide E2Q (red) binding to the EPPIN C-terminal. Green lines indicate H-bonds. Not all the EPPIN-E2Q H-bonds are visible in this view. Q7 and H2 are E2Q amino acids, see Table 1 (C) The SEMG1 peptide E2Q (red) binding to the EPPIN C-terminal shown in surface view with the docking pocket indicated in blue.
Figure 2
Figure 2. Potential Contraceptive Compounds
Four compounds which have been evaluated for their contraceptive potential to bind EPPIN and inhibit sperm motility utilizing the assays described in the text. The data are given in Table 2.

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