MALE CONTRACEPTION UPDATE

December 2006
Volume 1, Issue 9

Summaries of new peer-reviewed publications

Review

A survey of all contraceptive methods available to men, ranging from condoms and vasectomy to emerging methods. “Male contraception research has yielded a number of promising leads over the past 50 years. Yet little is known by the public due to lack of institutional support and funding. This in unfortunate since, apart from condom and vasectomy, there are many male methods which may be safer, more effective and easier to use.”
Male contraception: Past, present and future.
Herdiman J, Nakash A, Beedham T.
J Obstet Gynaecol. 2006 Nov;26(8):721-7.
PMID: 17130015

Cell adhesion targets

Exploration of the molecular causes of infertility in male symplastic spermatid (sys) mice. The authors identify the deletion of a gene on chromosome 14, Fndc3a, as the primary cause of the sys phenotype, in which male mice are infertile due to the “loss of adhesion between spermatids and Sertoli cells occur[ing] at step 8.” They locate the gene product in step 2-10 spermatid acrosomes and in Leydig cells, concluding that the mechanism through which FNDC3A “mediate[s] adhesion between Sertoli cells and round spermatids” is as yet unknown.
FNDC3A is required for adhesion between spermatids and Sertoli cells.
Obholz KL, Akopyan A, Waymire KG, MacGregor GR.
Dev Biol. 2006 Oct 15;298(2):498-513. Epub 2006 Jul 8.
PMID: 16904100

Immunological approaches

A review of the status of the peptide vaccines being developed against conception, including 8 sperm peptide targets, LDH-C4 among them.
Peptide vaccines against cancer, infectious diseases, and conception.
Naz RK, Dabir P.
Front Biosci. 2007 Jan 1;12:1833-44.
PMID: 17127424

Motility targets

“Ion channel blockers remain attractive model contraceptive drugs because of their ability to modulate cholesterol levels [in sperm membranes]. However, the large number of sperm ion channel variants shared with other cell types make ion channels less attractive targets… than a few years ago. In this review, the genetics, structure and function of voltage-dependent calcium channels and related CatSper molecules will be discussed…”
Voltage-dependent calcium channels in mammalian spermatozoa revisited.
Benoff S, Chu CC, Marmar JL, Sokol RZ, Goodwin LO, Hurley IR.
Front Biosci. 2007 Jan 1;12:1420-49.
PMID: 17127392

Supporting motility research

Sperm tail protein NYD-SP28 “is expressed in cytoplasm of spermatogenic cells… [and] NYD-SP28 immunoreactivity was detected in [the] entire sperm tail.” The protein, which contains “a cluster of phosphorylation sites, N-glycosylation sites and N-myristoylation sites… [is] post-translationally modified during sperm capacitation.”
Cloning and characterization of a novel sperm tail protein, NYD-SP28.
Zheng Y, Zhang J, Wang L, Zhou Z, Xu M, Li J, Sha JH.
Int J Mol Med. 2006 Dec;18(6):1119-25.
PMID: 17089017

High mitochondrial membrane potential in sperm is correlated with “normal morphology, high motility values, and calcium ionophore-induced acrosome reaction, suggesting the importance of mitochondrial functionality for fertilizing capacity of human spermatozoa.”
The functionality of mitochondria differentiates human spermatozoa with high and low fertilizing capability.
Gallon F, Marchetti C, Jouy N, Marchetti P.
Fertil Steril. 2006 Nov;86(5):1526-30. Epub 2006 Sep 25.
PMID: 16996512

Supporting endocrinological research

“… [T]he predominance of FSH isoforms bearing fully processed oligosaccharides in circulation may contribute to the development and maintenance of seminiferous epithelium function in men… Although the physiological significance of a hormone existing as glycosylation variants has not been clarified yet, it has been postulated that signal transduction systems can be differentially activated by specific carbohydrate structures present in the hormone.”
Carbohydrate complexity and proportions of serum FSH isoforms in the male: Lectin-based studies.
Campo S, Ambao V, Creus S, Gottlieb S, Fernandez Vera G, Benencia H, Bergada C.
Mol Cell Endocrinol. 2007 Jan 2;260-262:197-204. Epub 2006 Nov 2.
PMID: 17084021

“Using a Cre-loxP conditional knockout strategy, we generated a tissue-selective knockout mouse with the AR gene deleted in testis peritubular myoid cells (PM-AR(-/y)).” With the exception of smaller testes, these mice were phenotypically identical to wild type; they have comparable serum T concentrations and normal fertility. However, PM-AR(-/y) mice had oligozoospermia in the epididymis and decreased total germ cell number. These mice had “defects in the expression of Sertoli cells’ functional marker genes.”
Oligozoospermia with normal fertility in male mice lacking the androgen receptor in testis peritubular myoid cells.
Zhang C, Yeh S, Chen YT, Wu CC, Chuang KH, Lin HY, Wang RS, Chang YJ, Mendis-Handagama C, Hu L, Lardy H, Chang C.
Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17718-23. Epub 2006 Nov 9.
PMID: 17095600

“hCG and hCG-derived molecules of non-placental origin have recently been substantiated in… the human testis and the human prostate… hCGα is not derived from heterodimeric GPH suggesting hCG-independent functions of hCGα and hCGβ in male and female fertility.”
Human chorionic gonadotropin (hCG) in the male reproductive tract.
Berger P, Gruschwitz M, Spoettl G, Dirnhofer S, Madersbacher S, Gerth R, Merz WE, Plas E, Sampson N.
Mol Cell Endocrinol. 2007 Jan 2;260-262:190-6. Epub 2006 Nov 9.
PMID: 17097221

“A specific haplotype (AGATA) in the estrogen receptor alpha (ER1) gene was recently described as a new risk factor for cryptorchidism in the Japanese population… We confirm that SNP12 is the tag SNP for the AGATA haplotype also in Caucasians. However,… we found a protective effect for ESR1 SNP12 on cryptorchidism in the Italian population. No association between SNP12 and severe spermatogenic disturbances was observed.”
Molecular analysis of estrogen receptor alpha gene AGATA haplotype and SNP12 in European populations: potential protective effect for cryptorchidism and lack of association with male infertility.
Galan JJ, Guarducci E, Nuti F, Gonzalez A, Ruiz M, Ruiz A, Krausz C.
Hum Reprod. 2006 Nov 10; [Epub ahead of print]
PMID: 17099213

Proteomic/genomic supporting research

Identification and functional categorization of the 381 proteins of the Drosophila melanogaster sperm proteome. Gene ontology functional groups included proteolysis (3%), DNA/RNA binding (6%), cytoskeletal and central metabolism (9% each), energetics (12%), miscellaneous functions (13%) and catalysis (13%). The remaining 31% of the proteins have, as yet, no molecular function predictions.
Genomic and functional evolution of the Drosophila melanogaster sperm proteome.
Dorus S, Busby SA, Gerike U, Shabanowitz J, Hunt DF, Karr TL.
Nat Genet. 2006 Dec;38(12):1440-5. Epub 2006 Nov 12.
PMID: 17099714

Primarily a methodological report of the search for “specific genes related to the meiosis of germ cells during spermatogenesis in the rat testis.”
Meiosis related gene expression in rat spermatogenesis. [Chinese]
Liu DY, Wu YW.
Zhonghua Nan Ke Xue. 2006 Oct;12(10):883-7.
PMID: 17121015

“In humans, all three [BOULE] isoforms are exclusively expressed in the testes in a relative proportion of 80:220:1 for B1, B2 and B3, respectively… Alteration of the B1/B2 and B1/B3 transcript ratios was correlated with reduced meiotic capacity of spermatocytes to produce round spermatids as assessed by flow cytometry.”
Association of three isoforms of the meiotic BOULE gene with spermatogenic failure in infertile men.
Kostova E, Yeung CH, Luetjens CM, Brune M, Nieschlag E, Gromoll J.
Mol Hum Reprod. 2006 Nov 17; [Epub ahead of print]
PMID: 17114206

“By analysis of a large number of subjects…, we showed the first genetic evidence that [single nucleotide polymorphism mutations in three of the typical folate metabolism enzymes] MTHFR C677T, MS A2756G and MTRR A66G genotypes were independently associated with male infertility.”
Mutations in the testis-specific NALP14 gene in men suffering from spermatogenic failure.
Westerveld GH, Korver CM, van Pelt AM, Leschot NJ, van der Veen F, Repping S, Lombardi MP.
Hum Reprod. 2006 Dec;21(12):3178-84. Epub 2006 Aug 24.
PMID: 16931801

NALP14 was, as are the three other genes in 11p15, exclusively expressed in the testis. Within the testis, the NALP14 protein was mainly expressed in A dark spermatogonia, mid and late spermatocytes and spermatids… Our data suggest that NALP14 has a function in spermatogenesis and that mutation in this gene might cause spermatogenic failure.”
Association study of four polymorphisms in three folate-related enzyme genes with non-obstructive male infertility.
Lee HC, Jeong YM, Lee SH, Cha KY, Song SH, Kim NK, Lee KW, Lee S.
Hum Reprod. 2006 Dec;21(12):3162-70. Epub 2006 Jul 22.
PMID: 16861746

Based on the genotyping of 167 idiopathically infertile men, data indicate that a single nucleotide polymorphism at the KIT tyrosine kinase receptor “may be involved in a low sperm count trait in humans.”
Association of genetic markers within the KIT and KITLG genes with human male infertility.
Galan JJ, De Felici M, Buch B, Rivero MC, Segura A, Royo JL, Cruz N, Real LM, Ruiz A.
Hum Reprod. 2006 Dec;21(12):3185-92. Epub 2006 Aug 11.
PMID: 16905672

“Haspin is a unique protein kinase expressed predominately in haploid male germ cells… The transcript unit of Gsg2 contains features of germ cell-specific genes, including the lack of introns and a GC-rich DNA sequence. Further studies on the regulation of Gsg2 will help detail the transcriptional control of germ cells and their evolutionary history, such as the diversification of the genes by retrotransposons.”
The 193-Base Pair Gsg2 (Haspin) Promoter Region Regulates Germ Cell-Specific Expression Bidirectionally and Synchronously.
Tokuhiro K, Miyagawa Y, Yamada S, Hirose M, Ohta H, Nishimune Y, Tanaka H.
Biol Reprod. 2006 Nov 22; [Epub ahead of print]
PMID: 17123944

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Progress on drugs to inhibit vasa deferentia contractions

The work of Drs. Amobi and Smith of King’s College London was in the spotlight this week in media across the globe. They have been working since 1995 to elucidate the male contraceptive mechanism of action of phenoxybenzamine, a hypertension medication, and thioridazine, a schizophrenia medication. They were approached by a UK freelance reporter interested in a scoop, and the story ricocheted from there.

Drs. Amobi and Smith found that these two medications act in similar ways to disrupt the longitudinal smooth muscle contractions of the vas deferens which usually accompany ejaculation. The circular smooth muscles still function and they effectively squeeze the vas closed, resulting in an ejaculation that feels normal. However, the resulting ejaculate lacks sperm.

Having identified which receptors on the muscles are being blockaded by these drugs, the researchers are working to identify other compounds which will have a similar contraceptive effect, but a reduced side-effect profile. The duration of action of proposed formulations would be less than 24 hours, and would take effect within 2 hours of ingestion. So a man could take the pill only as needed. The researchers are now talking with a pharmaceutical company about bringing such a product to market. Based on the media’s fascinated reception thus far, men and women are ready for it!

Read some of the popular press articles:

• BBC News’ “Sperm-blocking contraceptive hope
• CBS News’ “Male contraceptive pill in the works
• The Guardian’s “But will men take it?
• The Telegraph’s “British scientists invent male pill

Read some of the most recent research articles from this group:

Attenuation of contractility in rat epididymal vas deferens by Rho kinase inhibitors.
Amobi NI, Chung IP, Smith IC.
Auton Autacoid Pharmacol. 2006 Apr;26(2):169-81.
PMID: 16553645

Contractile actions of imidazoline alpha-adrenoceptor agonists and effects of noncompetitive alpha1-adrenoceptor antagonists in human vas deferens.
Amobi N, Guillebaud J, Kaisary A, Lloyd-Davies RW, Turner E, Smith IC.
Eur J Pharmacol. 2003 Feb 21;462(1-3):169-77. Erratum in: Eur J Pharmacol. 2003 Mar 19;464(2-3):241.
PMID: 12591110

Discrimination by SZL49 between contractions evoked by noradrenaline in longitudinal and circular muscle of human vas deferens.
Amobi NI, Guillebaud J, Kaisary AV, Turner E, Smith IC.
Br J Pharmacol. 2002 May;136(1):127-35.
PMID: 11976277

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Press: New York Times, ABC News, JAMA and Geraldo!

Adjudin, Zavesca, and the IVD in the New York Times on November 7: “Contraception as an option for the man” by Michael Mason.

The entire November 15 issue (Volume 296, Number 19) of JAMA features articles on men’s health, including a review of Drs. Schill, Comhaire and Hargreave’s new text, Andrology for the Clinician.

Adjudin and men’s attitudes in the New York Observer on November 27: “Obsessed scientist finally throttles ’em: Non-paternity potion” by Lizzy Ratner.

Mapping of the full Drosophila melanogaster sperm proteome in Seed magazine on November 29: “Researchers map the sperm proteome, laying the groundwork for a wave of new research into the sex cell” by Jeanene Swanson.

The work of Drs. Amobi and Smith on a "male pill" was featured on the December 1st "Geraldo at Large" show, with commentary from MCIP's director.  Of course there was only brief mention that the pill is very early research. But no matter: people across the country got to hear that there are exciting leads and check out the attitudes of men and women on the street. You can watch a clip at MCIP's In the News section.

Hormonal methods, the IVD and RISUG on ABC News on December 4: “Despite hype, male pill still years away” by Dr. Jasmine Karalakulasingam. Includes a call for full funding of the World Health Organization’s Male Task Force.

Finally, this week's issue of JAMA (Volume 296, Number 21) features a Medical News & Perspectives piece on emerging male contraceptives: "Male Contraceptives on the Horizon". Author Bridget Kuehn touches on male hormonal contraceptive advances, the recent Adjudin developments and the ongoing Intra Vas Device clinical trial.

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Over 450 signatories of a letter supporting your work

Since September, MaleContraceptives.org has been collecting survey responses from men and women around the world. The survey is designed to characterize the market for new and emerging male contraceptives, and learn why contraceptive consumers support the development of these products. Survey respondents may also sign a letter of support for the work of the male contraceptive research community – over 450 men and women have done so.

The Male Contraception Coalition will prepare a report summarizing the survey findings and the personalized letters of support. This report will go to key funders and policymakers in January. The report will be available for distribution to your organization’s decisionmakers, and to your current and potential funding sources. More next month…

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Ultrasound as a form of external heat for contraception

It has been acknowledged for over half a century that hot sitz baths or special underwear can provide effective, low-tech male contraception. However, not everybody is aware of the more convenient heat method: ultrasound. When applied to the testes, a few minutes of sound waves – the same kind used by physical therapists to help heal injuries – can provide six months of contraception.

In the orginal studies, the method was painless and effective in murine and primate models. Ultrasound as a male contraceptive was studied in surprising detail in the 1970s. Researchers monitored Leydig and Sertoli cell health, and watched for genetic abnormalities in three generations of progeny.

Today, ultrasound machines are widely available and not particularly expensive. But this research has not been pursued in almost 30 years. Perhaps this is because this approach is so low-tech that it has not garnered much industry or policymaker support.

The Male Contraception Information Project is in contact with a foundation interested in funding confirmatory ultrasound studies. Are the orginal results reproducible in another lab? Stay tuned. To read about ultrasound’s background and what’s already known, see the review in MCIP’s heat methods section.

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Calendar of events

December 2-3
1st conference of the Ageing, Gender, Andrology & Sexual Sciences Society of India; Mumbai, India
December 3-6
9th Congress of the European Society for Sexual Medicine; Vienna, Austria
December 3-8
3o Encuentro iberoamericano de andrología; La Habana, Cuba
December 4-7
4th International Workshop on the Epididymis; Chatel-Guyon, France
December 8-10
4th European Congress of Andrology; Toulouse, France
2007
January 1st
Deadline for 2nd World Congress on Gender-specific medicine abstract submission
January 10
Deadline for ENDO 07 abstract submission
January 12
Deadline for Frontiers in Reproduction participant application
January 12
Deadline for World Congress on Fertility and Sterility abstract submission
March 5-8
Society for Endocrinology Annual BES Meeting; Birmingham, UK
March 8-11
2nd World Congress on Gender-specific medicine and aging: the endocrine impact; Rome, Italy
March 21-24
22nd Annual European Association of Urology Meeting; Berlin, Germany
April 15-19
1st World Congress for Sexual Health; Sydney, Australia
April 18-21
North American Testis Workshop; Tampa, FL, USA
April 21-24
American Society of Andrology 32nd Annual Conference; Tampa, FL, USA
April 25-27
20a Reunión de la Asociación Latinoamericana de Investigadores en Reprodución Humana; Buenos Aires, Argentina
April 28 - May 2
9th European Congress of Endocrinology; Budapest, Hungary
April 30 - May 5
IFFS 19th World Congress on Fertility and Sterility; Durban, South Africa
May 6 - June 17
Frontiers in Reproduction lab and lecture course for research careers in reproductive biology; Woods Hole, MA, USA
June 2-5
89th Annual Meeting of The Endocrine Society, ENDO 07; Toronto, Canada
July 15-20
Gordon Research Conferences Fertilization and Activation of Development; Plymouth, NH, USA

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Editors

Kirsten Thompson, Director of the Male Contraceptive Coalition (MCC)
Email: Kirsten@MaleContraceptives.org
Phone: +1 (510) 292-1186

Elaine Lissner, Director of the Male Contraception Information Project (MCIP)
Email: Lissner@NewMaleContraception.org
Phone: +1 (415) 863-1859 x107