A New Combination of Testosterone and Nestorone Transdermal Gels for Male Hormonal Contraception

Ilani, Niloufar; Roth, Mara Y.; Amory, John K.; Swerdloff, Ronald S.; Dart, Clint; Page, Stephanie T.; Bremner, William J.; Sitruk-Ware, Régine; Kumar, Narender; Blithe, Diana L.; Wang, Christina

doi:10.1210/jc.2012-1384

Cited by 88 publications

(83 citation statements)

References 36 publications

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“…Progestin has anti-gonadotropic activity and supports the action of testosterone. The combination of these two hormones is much more effective in suppressing sperm production in Caucasians than testosterone alone [13]. Several combinations of various progestins and derivatives of testosterone have been tested in clinical trials within the last 30 years achieving different effects.…”

Section: Testosterone With Gonadotropin-suppressing Agentmentioning

confidence: 99%

“…The solution to this problem might be to use testosterone and nestorone transdermal gels. Studies show that this route of administration of hormones is more accepted among patients with the efficacy of 88-89% among different ethnic groups and allows us to effectively achieve the sperm concentration to less than 1 million/mL with minimal side effects [13]. An optimal hormone administration method has not yet been identified.…”

Section: Connection Between Adverse Effects and Ways Of Administrationmentioning

confidence: 99%

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Brdt Bromodomains Inhibitors and Other Modern Means of Male Contraception

Zdrojewicz¹,

Konieczny²,

Papier³

et al. 2015

Adv Clin Exp Med

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Compared to efficient and secure female contraception, a vasectomy and condoms are the only options for men. The choice of male contraceptive methods is limited, so contraception mainly rests on the shoulders of women. Several concepts are considered: testosterone administration -inhibiting pituitary secretion of lutropin (LH) and follicle stimulating hormone (FSH), progestogen -affecting the secretion of gonadotropin and gonadoliberin (GnRH) antagonists. New potential targets for non-hormonal male contraception were discovered: glyceraldehyde-3-phosphate-dehydrogenase (GAPDHS) -specific to male germ cells and voltage-gated cation channel (CatSper). Both are responsible for sperm motility. Drugs such as thioridazine used in schizophrenia treatment and phenoxybenzamine (antihypertensive activity) exhibit a contraceptive effect. Similar action exhibits an analogue of lonidamine -adjudin and an antagonist of retinoic acid receptors (BMS-189453). Researchers are working on a contraceptive vaccine, whose active ingredient is epididymal protease inhibitor (Eppin). Another promising method acts by blocking Bromodomain testis-specific proteins (Brdt) involved in the process of spermatogenesis. JQ1-the Brdt inhibitor causes reversible infertility without affecting the endocrine signaling pathways. A recent discovery of Juno as the binding partner for Izumo1 identifies these proteins as the cell-surface receptor pair, essential for gamete recognition and this interaction can be inhibited by an anti-Juno monoclonal antibody. Our review shows that the situation of men can change and investigators are close to the optimal solution. In the near future men will be able to choose the best contraceptive suited to their needs (Adv Clin Exp Med 2015, 24, 4, 705-714).

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Section: Testosterone With Gonadotropin-suppressing Agentmentioning

confidence: 99%

Section: Connection Between Adverse Effects and Ways Of Administrationmentioning

confidence: 99%

Brdt Bromodomains Inhibitors and Other Modern Means of Male Contraception

Zdrojewicz¹,

Konieczny²,

Papier³

et al. 2015

Adv Clin Exp Med

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show abstract

“…12 In contrast, daily use of testosterone/nestorone gel formulations has been shown to suppress sperm levels to #1 million sperm/mL in 89% of men, with few adverse effects. 16 Nieschlag 12 has comprehensively summarized the advantages and disadvantages of the various testosterone and testosterone combination formulations.…”

Section: Male Hormonal Contraceptivesmentioning

confidence: 99%

An update on the potential for male contraception: emerging options

Garside¹,

Gebril²,

Alsaadi³

et al. 2013

OAJC

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The human population continues to grow and is estimated to rise to 10.1 billion by the end of the century. Therefore, there is still an unmet need for safe and highly effective contraceptive options for both men and women. Current options available to men include withdrawal, condoms, and vasectomy. Methods in development fall into two categories: hormonal and nonhormonal. This review will provide an overview of the testosterone combinations and immunocontraception of hormonal targets. Nonhormonal immunocontraception of sperm proteins will also be examined, together with the use of agents to disrupt other sperm-associated targets and pathways. The categories focused on include epididymal proteins, testicular kinases, epigenetic reader proteins, opioids, lonidamine derivatives, retinoic acid, microRNAs associated with spermatogenesis, and plant extracts. Considering these developments, the number of options available to men is likely to increase in the near future.

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“…In this study, to circumvent the known pulsatility of gonadotropin release from the pituitary in normal men (Baker et al ., 1975; Matsumoto & Bremner, 1984; Plymate et al ., 1989), we performed multiple measurements of gonadotropins at each time point to determine if multiple gonadotropin measurements in sequence (within a 60-min time period) would add to the model for identifying response, or failure to suppress sperm concentration to <1 million/mL. We analysed data from a recently completed male hormonal contraceptive trial using a novel transdermal combination regimen of testosterone gel and Nestorone gel to examine these relationships (Ilani et al ., 2012). …”

Section: Introductionmentioning

confidence: 99%

Characteristics associated with suppression of spermatogenesis in a male hormonal contraceptive trial using testosterone and Nestorone^®gels

et al. 2013

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SUMMARY Development of a male hormonal contraceptive has been challenging ascribable to the failure to adequately suppress spermatogenesis in 5–10% of men. Methods to identify incomplete suppressors early in treatment might identify men most responsive to male hormonal contraceptives. We hypothesized that serum hormone and gonadotropin concentrations after 4 weeks of transdermal treatment with testosterone and Nestorone in a contraceptive trial would be associated with suppression of sperm concentrations to <1 million/mL after 24 weeks. Indeed, luteinizing hormone or follicle-stimulating hormone concentrations greater than 1 IU/L after 4 weeks of transdermal testosterone/nestorone treatment were 97% sensitive for predicting failure to suppress spermatogenesis after 24 weeks of treatment. Serum nestorone concentrations were significantly associated with suppression, but serum testosterone concentrations were not. Early suppression of gonadotropins is associated with, but does not ensure, adequate suppression of spermatogenesis. This information may allow for rapid identification of non-responders in male hormonal contraceptive trials.

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A New Combination of Testosterone and Nestorone Transdermal Gels for Male Hormonal Contraception

Abstract: A combination of daily NES+T gels suppressed sperm concentration to 1 million/ml or less in 88.5% of men, with minimal adverse effects, and may be further studied as a male transdermal hormonal contraceptive.

Cited by 88 publications

References 36 publications

Brdt Bromodomains Inhibitors and Other Modern Means of Male Contraception

Brdt Bromodomains Inhibitors and Other Modern Means of Male Contraception

An update on the potential for male contraception: emerging options

Characteristics associated with suppression of spermatogenesis in a male hormonal contraceptive trial using testosterone and Nestorone^®gels

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A New Combination of Testosterone and Nestorone Transdermal Gels for Male Hormonal Contraception

Abstract: A combination of daily NES+T gels suppressed sperm concentration to 1 million/ml or less in 88.5% of men, with minimal adverse effects, and may be further studied as a male transdermal hormonal contraceptive.

Cited by 88 publications

References 36 publications

Brdt Bromodomains Inhibitors and Other Modern Means of Male Contraception

Brdt Bromodomains Inhibitors and Other Modern Means of Male Contraception

An update on the potential for male contraception: emerging options

Characteristics associated with suppression of spermatogenesis in a male hormonal contraceptive trial using testosterone and Nestorone®gels

Contact Info

Product

Resources

About

Characteristics associated with suppression of spermatogenesis in a male hormonal contraceptive trial using testosterone and Nestorone^®gels