MALE CONTRACEPTION UPDATE

August 2008
Volume 3, Issue 8

Summaries of new peer-reviewed publications

RISUG
“Contact mode atomic force microscopy (AFM) has been used to analyze quantitatively the micro-structural properties of RISUG and its precipitate in various systems… [RISUG] has a tendency to form a complex with ionic biomolecules present in the seminal plasma. This is supported by the experimental observations using AFM. This RISUG-biomolecule complex possibly acts as an ionic trap for spermatozoa passing through the vas deferens…  Significant alterations in the surface charge distribution of the sperm cell is observed on exposure to RISUG.”
Study of the micro-structural properties of RISUG--a newly developed male contraceptive.
Kumar S, Roy S, Chaudhury K, Sen P, Guha SK.
J Biomed Mater Res B Appl Biomater. 2008 Jul;86(1):154-61.
PMID: 18161821

Endocrinological approaches
Incomplete suppression of spermatogenesis has been an ongoing mystery in the quest for a globally efficacious hormonal male contraceptive.  This is a new epidemiological analysis of the factors associated with incomplete suppression in men participating in the Phase III WHO-sponsored testosterone undecanoate trial in China.  The study was designed as a case control series, comparing 43 “partial suppressors” dropped from the trial’s efficacy phase to 855 “complete suppressors” who entered the efficacy phase after 6 months of monthly depot TU injections (500 mg).  “Baseline serum LH level was higher and serum LH as well as FSH level during the suppression phase was less suppressed in partial suppressors. Additionally, in a logistic regression analysis larger testis volume, higher serum FSH concentrations alone, or interaction of serum LH, FSH, testosterone and sperm concentrations were associated with degree of suppression. The distribution of polymorphisms of AR or FSH receptor genes did not differ between partial and complete suppressors.”  This analysis does not support pharmacogenetics as a possible mechanism of action for non-response within an ethnically homogeneous population.
Predictors for partial suppression of spermatogenesis of hormonal male contraception.
Li JW, Gu YQ.
Asian J Androl. 2008 Sep;10(5):723-30.
PMID: 18645675

Proteomic analysis of testicular biopsies before and 2 weeks after treatment with either testosterone undecanoate or TU + LNG revealed distinct mechanisms of action.  TU only treatment altered protein expression associated with assembly and induced cell death.  TU + LNG treatment resulted in protein expression linked to “‘proliferation/cell survival’ and ‘apoptosis/death’… hnRNP K, PSMF1, SOD2, P4HB, Annexin II, and Pvalb are key proteins that may be early molecular targets responsible for spermatogenesis suppression induced by hormone treatment.”
Proteomic Analysis of Testis Biopsies in Men Treated with Injectable Testosterone Undecanoate Alone or in Combination with Oral Levonorgestrel as Potential Male Contraceptive.
Cui Y, Zhu H, Zhu Y, Guo X, Huo R, Wang X, Tong J, Qian L, Zhou Z, Jia Y, Lue YH, Hikim AS, Wang C, Swerdloff RS, Sha J.
J Proteome Res. 2008 Aug 15. [Epub ahead of print]
PMID: 18702538

Supporting endocrinological research
Combined hormonal treatment and testicular heating in cynomolgus monkey  showed “spatiotemporal expression changes of 16 reported or novel genes in [the] epididymis… It was demonstrated that these region-specific genes, some of which were not regionally fixed, changed greatly with these treatments. The expression levels of these epididymal genes fluctuated, and the expression of most of the genes returned to nearly normal level at the end of treatments.” The spatiotemporal expression changes of 16 epididymis-specific genes induced by testosterone, heat, and combination treatment in cynomolgus monkey.
Li X, Liu Q, Liu S, Zhang X, Liu Y, Zhang Y.
Acta Biochim Biophys Sin (Shanghai). 2008 Aug;40(8):721-8.
PMID: 18685788

Testicular biopsies from 18 infertile men were “assessed by in-situ hybridization and immunohistochemistry” for progesterone receptor (PR) expression. “Semi-quantitative assessment of PR expression and Johnsen scores in the testicular biopsies of infertile men demonstrating different phenotypes indicated a direct relationship between PR expression and extent of spermatogenesis.”
Altered expression of progesterone receptors in testis of infertile men.
Abid S, Gokral J, Maitra A, Meherji P, Kadam S, Pires E, Modi D.
Reprod Biomed Online. 2008 Aug;17(2):175-84.
PMID: 18681990

Epididymal targets
 Additional information about the role of Eppin, a possible male contraceptive target.  “Human semenogelin (Sg) cDNA (nucleotides 82-849) and Eppin cDNA (nucleotides 70-723) were generated by polymerase chain reaction (PCR) and cloned… In vitro the digestion of recombinant Sg by PSA in the presence or absence of recombinant Eppin was studied… Eppin binds Sg on the surface of human spermatozoa with the C-terminal of Eppin (amino acids 75-133). rSg was digested with PSA and many low molecular weight fragments were produced. When rEppin is bound to rSg, then digested by PSA, incomplete digestion and a 15-kDa fragment results”
Molecular mechanism of epididymal protease inhibitor modulating the liquefaction of human semen.
Wang ZJ, Zhang W, Feng NH, Song NH, Wu HF, Sui YG.
Asian J Androl. 2008 Sep;10(5):770-5.
PMID: 18645681

Supporting motility research
Spindlin 1 (Spin 1) isoform2 was identified in mouse testis by RT-PCR and immunoblot.  “[The] isoform was more highly expressed in adult testes compared with newborn testes. Interestingly, Spin1 isoform2 did not show up in the cytoplasm of primary spermatocytes until day 14… Spin1 isoform2 is a protein expressed highly in adult testis, which might be involved in spermatogenesis and could be necessary for normal sperm motility.”
Characterization of Spindlin1 isoform2 in mouse testis.
Zhang KM, Wang YF, Huo R, Bi Y, Lin M, Sha JH, Zhou ZM.
Asian J Androl. 2008 Sep;10(5):741-8.
PMID: 18645677

Cell adhesion targets
“Somatic, targeted, inactivation of Rxrb in Sertoli cells (yielding RxrbSer-/- mutants) leads to failure of spermatid release, accumulation of cholesterol esters and, subsequently, testis degeneration… The failure of spermiation was also reported in mice lacking the retinoic acid (RA) receptor alpha in Sertoli cells (RaraSer-/- mutants) and represents, in addition, a feature of vitamin A deficiency that can be readily induced in mice lacking the lecithin:retinol acyl transferase (Lrat-/- mutants). Altogether, these findings support the conclusion that RXRbeta heterodimerized with a RA-liganded RARalpha transduces signals required in Sertoli cells for spermatid release.”
RXR beta expression in Sertoli cells controls cholesterol homeostasis and spermiation.
Vernet N, Dennefeld C, Kloppfenstein M, Ruiz A, Bok D, Ghyselinck N, Mark M.
Reproduction. 2008 Aug 19. [Epub ahead of print]
PMID: 18713813

Gamete binding / fusion targets
“Sperm-egg interactions have been studied for many years using biochemical approaches such as the employment of antibodies and ligands that interact with sperm or with eggs and their vestments. As a result, various factors that participate in fertilization have emerged. However, when animals were genetically manipulated to examine the roles of those factors, most of them were found, to our surprise, to be "not essential"… In this review, information about sperm-egg interactions obtained from genetically manipulated animals is mainly revisited in order to propose a new vision.”
Mechanisms of sperm-egg interactions emerging from gene-manipulated animals.
Ikawa M, Inoue N, Okabe M.
Int J Dev Biol. 2008;52(5-6):657-64.
PMID: 18649279

 “A combination of biochemical and proteomic membrane protein techniques have enabled us to dissect and highly purify the apical sperm plasma membrane area from control and capacitated sperm cells. The actual ZP-binding proteins identified predominantly belonged to the sperm membrane-associated family members of spermadhesins (AQN-3) and were present in the aggregating lipid ordered membrane microdomains (lipid rafts) that emerged during in vitro capacitation in the apical ridge area of the sperm head plasma membrane… We inferred that the capacitation-dependent formation of an aggregated lipid ordered apical ridge surface area in the sperm head plasma membrane was not only relevant for ZP-binding, but also for the ZP-induced acrosome reaction.
Capacitation-dependent reorganization of microdomains in the apical sperm head plasma membrane: Functional relationship with zona binding and the zona-induced acrosome reaction.
Boerke A, Tsai PS, Garcia-Gil N, Brewis IA, Gadella BM.
Theriogenology. 2008 Jul 18. [Epub ahead of print]
PMID: 18640708

“CRISP1 (cysteine-rich secretory protein 1) is an epididymal protein thought to participate in gamete fusion through its binding to egg-complementary sites. Structure-function studies using recombinant fragments of CRISP1 as well as synthetic peptides reveal that its egg-binding ability resides in a 12 amino acid region corresponding to an evolutionary conserved motif of the CRISP family, named Signature 2 (S2)… [Our] results suggest a functional cooperation between CRISP1 and CRISP2 to ensure the success of fertilization.”
Participation of cysteine-rich secretory proteins (CRISP) in mammalian sperm-egg interaction.
Cohen DJ, Busso D, Da Ros V, Ellerman DA, Maldera JA, Goldweic N, Cuasnicu PS.
Int J Dev Biol. 2008;52(5-6):737-42.
PMID: 18649285

“[We] demonstrate that [rat epididymal epithelium CRISP1’s] Protein D associates transiently with the sperm surface in a concentration dependent manner, exhibiting saturable binding to both caput and cauda sperm in a concentration range that is consistent with its capacitation inhibiting activity. In contrast, Protein E persists on the sperm surface after all exogenous Protein D has been dissociated… These studies also confirm a tightly bound population of Protein E that could act in the female tract.”
Association of the Protein D and Protein E Forms of Rat CRISP1 with Epididymal Sperm.
Roberts KP, Ensrud-Bowlin KM, Piehl LB, Parent KR, Bernhardt ML, Hamilton DW.
Biol Reprod. 2008 Aug 13. [Epub ahead of print]
PMID: 18703418

“Crisp proteins appear to play multiple roles in the life history of sperm. One of these roles is to act as a sperm chemoattractant. Allurin, a 21 kDa Crisp protein rapidly released from the egg jelly of at least two frogs, X. laevis and X. tropicalis, elicits directed motility in both homospecific and heterospecific sperm… [The] observation that allurin can also elicit chemotaxis in mouse sperm raises the question of whether allurin-like proteins might act as sperm chemoattractants in mammals.”
Crisp proteins and sperm chemotaxis: discovery in amphibians and explorations in mammals.
Burnett LA, Xiang X, Bieber AL, Chandler DE.
Int J Dev Biol. 2008;52(5-6):489-501.
PMID: 18649262

Gossypol
An in vitro study identifies a possible mechanism of action for gossypol.  “The present study was designed to investigate the effects of gossypol on the gap junctional intercellular communication (GJIC) and the expression of connexin43 (Cx43) in the cultured cells… The scrape loading and dye transfer (SLDT) assay showed gossypol significantly decreased GJIC between adjacent cells. RT-PCR, immunofluorescence and Western blot analyses demonstrated the expression of Cx43 in TM4 cells. The expression of Cx43 was gradually decreased with the increasing concentrations of gossypol, and the effect occurred as early as 6h after the treatment and continued until 48h. These results suggested that gossypol impaired GJIC by decrease of Cx43 expression in the cells, which is important for Sertoli cells to regulate spermatogenesis.”
Gossypol repressed the gap junctional intercellular communication between Sertoli cells by decreasing the expression of Connexin43.
Zhou DR, Zhou YC, Cui GH, Guo X, Qin J, Gui YT, Cai ZM.
Toxicol In Vitro. 2008 Jul 29. [Epub ahead of print]
PMID: 18706992

“In this study, we compared the toxicity and efficacy in mice of natural product gossypol and its semisynthetic derivative apo-gossypol, compounds that bind and inhibit antiapoptotic Bcl-2 family proteins. Daily oral dosing studies showed that mice tolerate doses of apogossypol 2- to 4-times higher than gossypol. Hepatotoxicity and gastrointestinal toxicity represented the major adverse activities of gossypol, with apogossypol far less toxic.”
Bcl-2 antagonist apogossypol (NSC736630) displays single-agent activity in Bcl-2-transgenic mice and has superior efficacy with less toxicity compared with gossypol (NSC19048).
Kitada S, Kress CL, Krajewska M, Jia L, Pellecchia M, Reed JC.
Blood. 2008 Mar 15;111(6):3211-9.
PMID: 18202226

Novel compounds
A study comparing the “antifertility effects of 50% ethanolic extract of the root bark of Cananga odorata with gossypol” after oral dosing for 60 days. “Differences were not observed in the sperm count and fertility index of the gossypol group in comparison with the C. odorata group. But statistically significant alterations were noted in the sperm morphology as well as in the activity of HMG CoA reductase, 3beta-hydroxy steroid dehydrogenase, glucose-6-phosphate dehydrogenase, cholesterol, and protein of the testis and in serum testosterone. On withdrawal of the drugs, sperms in C. odorata group became completely motile but not in the gossypol group. The active component is a 52 kd protein.”
Spermatotoxic effects of Cananga odorata (Lam): a comparison with gossypol.
Pankajakshy A, Madambath I.
Fertil Steril. 2008 Aug 8. [Epub ahead of print]
PMID: 18692834

Proteomic / genomic supporting research
“Despite the importance of [gametogenesis], progress in elucidating the molecular mechanisms underpinning mammalian germ cell development has been retarded by the lack of an efficient and reproducible system of in vitro culture for the expansion and trans-meiotic differentiation of germline cells. The dearth of such a culture system has rendered the study of germ cell biology refractory to the application of new high-throughput technologies such as RNA interference (RNAi), leaving in vivo gene-targeting approaches as the only option to determine the function of genes believed to be involved in gametogenesis… This review considers the developments made in modelling germ cell development using stem cells, and some of the challenges that need to be overcome to make this a useful tool for studying gametogenesis and to realise any future clinical application.
New research horizons: modelling germ cell development in vitro.
Childs AJ, Saunders PT, Anderson RA.
Mol Hum Reprod. 2008 Aug 1. [Epub ahead of print]
PMID: 18676971

“A significant proportion of [vasectomized men who undergo vasovasostomy] remain infertile, despite the reestablishment of patent ducts, possibly due to epididymal damage caused by vasectomy… To complete the list of epididymal genes affected by vasectomy, we analyzed the epididymal gene expression pattern of three vasectomized donors using the Affymetrix human GeneChip U133 Plus 2. These results were compared with the gene expression pattern of three "normal" donors… Quantitative (Qt)-PCR and Western blot analysis of six selected genes known to be expressed in specific epididymal segments were performed… These results contribute to an understanding of the reasons why fertility is not recovered in vasovasostomized men.”
Effects of vasectomy on gene expression profiling along the human epididymis.
Thimon V, Calvo E, Koukoui O, Légaré C, Sullivan R.
Biol Reprod. 2008 Aug;79(2):262-73. Epub 2008 Apr 23.
PMID: 18434627

“We investigated eight proteins encoded by novel spermatogenic cell-specific genes previously identified from the mouse round spermatid UniGene library… The authenticity of the eight novel proteins and their specificity to spermatogenic cells were confirmed… [Four] proteins [were] only in testicular germ cells, a single protein [was] in testicular germ cells and testicular sperm, and three proteins [were] in the testicular stages and mature sperm from the epididymis.”  Of the three present in sperm, “one is located at the surface of the acrosomal region and the other two are associated with cytoskeletal structures in the sperm flagellum. We name the genes for these sperm proteins Shsp1 (Sperm head surface protein 1), Sfap1 (Sperm flagellum associated protein 1) and Sfap2 (Sperm flagellum associated protein 2).”
 Characterization of eight novel proteins with male germ cell-specific expression in mouse.
Baek N, Woo JM, Han C, Choi E, Park I, Kim do H, Eddy EM, Cho C.
Reprod Biol Endocrinol. 2008 Jul 24;6:32.
PMID: 18652659

A report of a putative mechanism for the transformation of “guinea pig heterodimeric membrane protein ADAM1/ADAM2 (fertilin)… from a stationary state to one of rapid diffusion within the lipid bilayer… [These] data suggest that the release of ADAM1/ADAM2 from its diffusion constraints results from a cAMP-induced signaling pathway that, like others of capacitation, is established during epididymal sperm maturation.”
Cyclic 3', 5'-AMP Causes ADAM1/ADAM2 to Rapidly Diffuse Within the Plasma Membrane of Guinea Pig Sperm.
Hunnicutt GR, Koppel DE, Kwitny S, Cowan AE.
Biol Reprod. 2008 Jul 30. [Epub ahead of print]
PMID: 18667756

“Here we report the identification and characterization of a novel homeobox gene of the paired-like class on the X chromosome distal to the reproductive homeobox (Rhox) cluster in mice. Transcripts are found in the testis and ovary as early as 13.5 days post coitum (dpc). Transcription ceases in the ovary by 3 days post partum (dpp), but continues in the testis through adulthood. The Rhox13 gene encodes a 25.3 kDa protein expressed in the adult testis in germ cells at the basal aspect of the seminiferous epithelium.”
Identification and characterization of Rhox13, a novel X-linked mouse homeobox gene.
Geyer CB, Eddy EM.
Gene. 2008 Jul 15. [Epub ahead of print]
PMID: 18675325

 “To gain insight into the physiological function of nephrocystin, Nphp1-targeted mutant mice were generated by homologous recombination. Interestingly, homozygous Nphp1 mutant mice were viable without renal manifestations of nephronophthisis. They appeared normal, but males were infertile… Electron microscopic analysis revealed detachment of early elongating spermatids from Sertoli cells, and a failure of sperm head and tail morphogenesis… These novel findings indicate that nephrocystin is critically required for the differentiation of early elongating spermatids into spermatozoa in mice. The possible roles of nephrocystin in the formation and maintenance of Sertoli-spermatid junctions are still under investigation.
Targeted disruption of Nphp1 causes male infertility due to defects in the later steps of sperm morphogenesis in mice.
Jiang ST, Chiou YY, Wang E, Lin HK, Lee SP, Lu HY, Wang CK, Tang MJ, Li H.
Hum Mol Genet. 2008 Aug 5. [Epub ahead of print]
PMID: 18684731

“We set out to test the hypothesis that HSP27 protein is expressed in the human testes and its expression varies with the state of spermatogenesis. HSP27 expression was examined in 30 human testicular biopsy specimens (normal spermatogenesis, maturation arrest and Sertoli cell only syndrome, 10 cases each) using immunofluorescent methods… We report for the first time the expression patterns of HSP27 in the human testes and show differential expression during normal spermatogenesis, indicating a possible role in this process. The altered expression of this protein in testes showing abnormal spermatogenesis may be related to the pathogenesis of male infertility.”
Heat shock protein 27 expression in the human testis showing normal and abnormal spermatogenesis.
Adly MA, Assaf HA, Hussein MR.
Cell Biol Int. 2008 Jul 23. [Epub ahead of print]
PMID: 18692580

“To study the behavior of Sertoli cells as a first approach to the molecular and functional characterization of the vitamin C transporters in [the blood-testis] barrier, we used the 42GPA9 cell line immortalized from mouse Sertoli cells… This work describe[s] the molecular identity of the transporters involved in vitamin C transport in these cells, which we hope will improve our understanding of how germ cells obtain vitamin C, transported from the plasma into the adluminal compartment of the seminiferous tubules.”
Molecular identification and functional characterization of the vitamin C transporters expressed by Sertoli cells.
Angulo C, Castro MA, Rivas CI, Segretain D, Maldonado R, Yañez AJ, Slebe JC, Vera JC, Concha II.
J Cell Physiol. 2008 Jul 30. [Epub ahead of print]
PMID: 18668520

The “epididymis is responsible for the sperm maturation and storage, and its gene expression is highly region-specific, so it maybe an ideal model for proteomics, especially for differential proteomics study. This paper gives a brief introduction [to] the application of proteomics in the epididymis and the differential proteins expressed in different epididymal regions. These epididymis-specific/selective proteins identified by proteomics technology may prove to be targets for contraception or may provide insight to the unique responsibilities of the epididymis in supporting male fertility.”
The application of proteomics in epididymis research [Chinese]
Zou M, Wang HF, Hu JM.
Sheng Li Ke Xue Jin Zhan. 2008 Apr;39(2):139-44.
PMID: 18664178

Blood-testis barrier elucidation
 “The objective of the current study was to examine the immunoprotective properties of a mouse Sertoli cell line (MSC-1) in order to identify a Sertoli cell line that could be used to aid in investigation of the immunoprotective abilities of Sertoli cells… MSC-1 cells were found to express known Sertoli cell-expressed, immunoprotective factors, clusterin, Fas ligand, and transforming growth factor-beta1, suggesting additional factors may be involved in Sertoli cell immune privilege. These data indicate the MSC-1 cell line lacks the immunoprotective properties associated with primary Sertoli cells. Further study of this cell line could be useful in examining the mechanisms that enable Sertoli cells to provide immune privilege.”
Sertoli cell line lacks the immunoprotective properties associated with primary Sertoli cells.
Dufour JM, Dass B, Halley KR, Korbutt GS, Dixon DE, Rajotte RV.
Cell Transplant. 2008;17(5):525-34.
PMID: 18714671

“To investigate the correlation of exogenous estrogens with the expression of FasL in Sertoli cells and the blood-testis barrier, … super-physiological doses of exogenous estrogenic compounds (diethylstilbestrol and estradiol) were administered to pubertal Sprague-Dawley rats in vitro and in vivo… FasL expression was markedly up-regulated in the immature Sertoli cells (P < 0.05) as well as in the Sertoli cell membrane and the blood-testis barrier of the epithelium. The tracer lanthanum passed through the blood-testis barrier and reached the whole layer of the epithelium at 18 days.”
Estrogens affect Sertoli cells and the blood-testis barrier in pubertal rats. [Article in Chinese]
Pan YQ, Guo QS, Wang RY, Xu C.
Zhonghua Nan Ke Xue. 2008 Jul;14(7):590-6.
PMID: 18686377

“Adult male BALB/c mice were exposed to EMP at 200 kV/m for 200 pulses with 2 seconds interval… The permeability of the blood-testis barrier (BTB) in mice was observed by using Evans Blue tracer and lanthanum nitrate tracer.  After exposure, cloudy Evans Blue was found in the testicle convoluted seminiferous tubule of mice. Lanthanum nitrate was observed not only between testicle spermatogonia near seminiferous tubule wall and Sertoli cells, but also between Sertoli cells and primary spermatocyte or secondary spermatocyte.”
Effect of electromagnetic pulse exposure on permeability of blood-testicle barrier in mice.
Wang XW, Ding GR, Shi CH, Zhao T, Zhang J, Zeng LH, Guo GZ.
Biomed Environ Sci. 2008 Jun;21(3):218-21.
PMID: 18714819

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Start-ups in male contraception: A status report

Every few years, academic and major pharma researchers have come together at the NIH's "Future of Male Contraception" conference to compare notes.  The common hurdles faced during the transition from a contraceptive target, to an effective drug or device, to a marketable product are often part of the discussion.  Sometimes stepping outside the worlds of academia and large pharma seems like the best way forward.  More than half a dozen start-up companies are thus working to bring a drug or device to the male contraception market—some of them spinoffs from academia, and some of them founded by non-academics with a vision.  Most of these companies are struggling, and it’s possible that with the current economic and venture capital retrenchment, few will make it through the next couple years if there isn't a fresh infusion of public-sector funding.

In a 2006 external review of the government contraceptive research program at USAID, Dr. Gordon Duncan posits that “these types of companies would need additional expertise in cGMP manufacturing, registration, distribution, and marketing to complete the product development process of an acceptable drug candidate… While their size and access to venture capital allows them to undertake more risky projects, they lack the staying power to overcome long delays or setbacks in developing a product candidate.”  This creates an opening for savvy public-sector and foundation funders, who can provide an investment in companies’ products in exchange for legally-guaranteed future public-sector pricing.  This win-win arrangement would keep the companies alive long enough to reach market, while making sure their products benefit more than a select few.

Here’s a roster of today’s male contraceptive start-ups:

Product: CatSper ion channel blockers
Company: Massachusetts-based Hydra Biosciences
Status: Continuing to search for larger partners interested in helping the company use high-throughput screening to look for a drug to block sperm-specific CatSper ion channels.  The CatSpers are crucial players in sperm hyperactivation, discovered by company co-founder and Harvard researcher Dr. David Clapham and his team.

Product: Intra Vas Device (IVD)
Company: Minnesota-based Shepherd Medical Company
Status: Presented promising Phase I clinical trial 6-month interim results at last year's Future of Male Contraception conference.  The company learned several lessons from the initial study, and planned to run a new study with a refined insertion procedure and inserter to increase the 92% success rate.  However, the company did not garner a second NIH grant, despite a high score on its application.  A company representative now says there is “nothing to report” clinically or structurally.  Is it possible that the company has not found sufficient funding to continue operations and conduct further studies in the U.S. and Canada as planned?

Product: Vassonic device
Company: California-based Vassonic
Status: This company has taken advantage of advances in miniaturized energy storage and delivery to design an implantable ring-shaped device intended to kill sperm passing through the vas deferens.  The device, which encircles the vas, is intended to render sperm permanently immotile without obstructing sperm flow, thus avoiding many of the potential side effects of occlusive devices.  The device is designed to be non-invasively activated or deactivated by a healthcare professional, much like a pacemaker is adjusted.  The company is being tight-lipped about the technological details until hearing back on its patent applications.  In this era of shrinking government science budgets, a first NIH grant submission did not result in funding, so the company will be looking for private funding sources as well as other grant submissions to finish feasibility studies on the device.

Product: HIFU non-surgical vasectomy
Company: California-based Vitality Medical Products, LLC
Status: High-intensity focused ultrasound (HIFU) has been tested as a way to nonsurgically close the vas deferens for permanent contraception.  For HIFU sterilization, a small ultrasound transducer is clamped around the vas deferens and the scrotal skin.  Proof-of-concept studies carried out at the Johns Hopkins Medical Institute with dogs have established the proper power level and length of time needed to permanently occlude the vas (about 40-60 seconds), using equipment supplied by a company that sells HIFU equipment for treating heart defects.  The developer of the technology founded the start-up company a few years ago to test and commercialize the sterilization method. Funding was not forthcoming, however, and the project has been dropped barring new investment.

Product: Pro-Vas implantable clip
Company: Florida-based MenRx Surgical
Status: This company is well on its way to market with a vasectomy alternative, the Pro-Vas implantable vas-occlusive clip.  The clip would be used in conjunction with no-scalpel vasectomy to occlude the vas slightly more quickly and, it is hoped, with less tissue damage than standard ligation. Like the Vasclip before it, Pro-Vas has been approved under theFDA's 510(k) rule as equivalent to a device already on the market for another use in terms of safety and biocompatibility.  However, under this program, there is little reporting of efficacy required.  The Vasclip, for example, no longer appears to be on the market, after substantial failure rates were reported by physicians, users, and in the medical literature. The Pro-Vas incorporates design improvements that may make it more effective than the Vasclip – the key change is that the device has a spring clip that should allow varying vas diameters to be effectively ligated while not damaging the underlying tissue’s blood flow. Product release is scheduled for November, at which time the company will solicit physicians to participate in an efficacy trial.

Product: Non-occlusive vas device
Company: Canadian-based, but not yet named
Status: A team including Ron Weiss, a Canadian vasectomy expert who also participated in the WHO evaluation of RISUG facilities in 2002, is working on a non-occlusive, reversible vas-based device that is still under secrecy but is reportedly “redefining the field without re-inventing the wheel.”   Rodent tests are scheduled to begin this calendar year, and the startup is looking for funding.

Product: Sperm-specific flagellar motility blockers
Company: Norwegian biotech Spermatech
Status: The company is looking for a drug to directly target a sperm protein discovered by University of Massachusetts Medical School researcher Dr. George Witman.  The company has gathered all the intellectual property related to this sperm-specific protein under one roof, avoiding protracted patent fights and giving this approach its best chance at success.  Spermatech recently partnered to move forward with high-throughput screening (HTS) for compounds that affect “sperm motility in general,” and in vitro tests of synthesized peptides for their target protein.  They will seek additional funding, both grants and equity investments, early next year to cover the costs of reaching the clinical Phase I milestone.

Product: SpermCheck home sperm count kit
Company: Virginia-based ContraVac
Status: The company’s SpermCheck Vasectomy is an over-the-counter test with a much lower threshold than the commonly-available sperm count tests.  It gained FDA approval last March, and the kit was to be available by the end of this summer but apears to be delayed.  In addition to allowing at-home confirmation of vasectomy success, the test will be useful for men using DIY heat-based methods of contraception. ContraVac is seeking additional financing in order to begin a sales and marketing campaign for the device.

Product: Selective Androgen Receptor Modulators (SARMs)
Company:  Tennessee-based GTx 
Status: The company is conducting a Phase IIb clinical trial evaluating Ostarine™, its lead SARM, for the treatment of cancer cachexia, the severe muscle loss associated with many cancers. The Phase IIb cancer cachexia trial is a randomized, double blind, placebo controlled study of muscle wasting in 150 patients with non-small cell lung cancer, colorectal cancer, non-Hodgkin's lymphoma, or breast cancer. GTx anticipates results from the trial in the third quarter of 2008.  GTx and Merck have formed a global strategic collaboration for SARMS. Though GTx is concentrating on the profitable (and less politically fraught) cancer market, this SARM could potentially be used as an oral male contraceptive, possibly with an improved side effect profile compared to other currently available forms of testosterone.

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A personal note from MCIP

From Elaine Lissner, director of MCIP

Kirsten Thompson, the International Male Contraception Coalition's director and co-author of this newsletter, is back from an intensive Masters of Public Health program at Johns Hopkins, the nation's top-ranked public health school, where she completed two years of coursework crammed into 11 months. She's now back in the San Francisco Bay Area, where she has been sorely missed. In addition to co-producing this newsletter and maintaining MaleContraceptives.org, she now wears a new hat. She is the project coordinator for U.C. San Francisco Bixby Center for Global Reproductive Health’s Long-Acting Reversible Contraception project, which seeks to identify and overcome barriers to greater US use of highly effective “forgettable” contraceptives such as IUDs and Implanon. Kudos to Kirsten for keeping us up on male contraceptive research during all these transitions, and welcome back!

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Press coverage: Time Magazine

Time Magazine focuses on hormonal research: what happened to Big Pharma’s  participation? Are men ready for a new contraceptive? “Just a few years ago, the new male contraceptive seemed like an inevitable reality. Major pharmaceutical companies like Wyeth, Schering and Organon were pumping millions into hormonal birth-control development programs for men, and researchers were breathlessly promising imminent production...”  IMCC director Kirsten Thompson and researcher Dr. David Handelsman are quoted attesting to the demand and the progress that could be made; but “the lack of definitive results is a major problem, says Dr. John Amory, who has spearheaded much of the male contraceptive research at the University of Washington. He says the science needs to progress before researchers can blame Big Pharma for dragging its heels. Amory's most recent treatment, a daily testosterone gel combined with a quarterly injection, showed a 90% success rate in trials, but, he says, ‘if we had a compound that was 99% effective, then the drug companies would be on board, the FDA would be on board, and consumers would embrace it.’”
The Long Wait for Male Birth Control
Time Magazine, 3 August

Finding Dulcinea, “the Internet's librarian,” summarizes the Time story and adds context, links, analysis, and resources.  “Scientifically speaking, birth control for men is an imminent possibility, but researchers and doctors involved in developing male contraceptive medications and devices say we’re a long way off from seeing these products on the market. Pharmaceutical companies aren’t making the necessary investments because of a widespread belief that men simply won’t take responsibility for birth control. ‘You can lead a horse to water, but you can't make it drink,’ researcher Dr. David Handelsman said, referring to the drug companies’ continued disinterest, and accusing the companies of being out of touch with what people actually want.”
Men’s Birth Control Faces Many Obstacles
findingDulcinea.com, 5 August

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Calendar of events

Planning to attend a male contraception or andrology-related event that's not listed here? Let us know so we can post it and alert your colleagues to interesting upcoming events.

September 15
Deadline for Asia-Pacific Council on Contraception abstract submission
September 26
World Contraception Day
October 1-3
Androgens 2008, 5th Biennial Meeting on Androgen Receptor Function; Rotterdam, The Netherlands
October 15-17
14th International Workshop on the Development and Function of the Reproductive Organs; Villa Mondragone, Italy
October 15
Deadline for International Congress of Andrology abstract submission
October 22-25
30th Annual British Adrology Society Meeting; Gijon, Spain
October 25-28
2008 American Public Health Association Annual Meeting & Exposition; San Diego, CA, USA
November 8-12
American Society for Reproductive Medicine 64th Annual Meeting; San Francisco, CA, USA
November 24
Deadline for European Congress of Endocrinology abstract submission
November 26-28
5th European Congress of Andrology; Rome, Italy
December 1
Deadline for North American Testis Workshop abstract submission
December 4-6
Second Congress of the Asia-Pacific Council on Contraception (APCOC); Macao, China
December 15
Deadline for World Congress on Reproduction abstract submission
2009
March 5-8 
13th World Congress on Human Reproduction; Venice, Italy
March 7-10
9th International Congress on Andrology; Barcelona, Spain
 April 1-4
20th North American Testis Workshop; Philadelphia, PA, USA
April 4-7 
34th American Society of Andrology meeting; Philadelphia, PA, USA
April 25-29 
11th European Congress of Endocinology; Istanbul, Turkey
May 31 
Deadline for Asia-Pacific Forum on Andrology abstract submission
October 10-13 
Third Asia-Pacific Forum on Andrology; Nanjing, China

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Editors

Kirsten Thompson, Director of the Male Contraception Coalition (MCC)
Email: Kirsten@MaleContraceptives.org
Phone: +1 (443) 858-1183

Elaine Lissner, Director of the Male Contraception Information Project (MCIP)
Email: Lissner@NewMaleContraception.org
Phone: +1 (415) 839-6304