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Prostate-sparing effects in primates of the potent androgen 7alpha-methyl-19-nortestosterone: a potential alternative to testosterone for androgen replacement and male contraception

机译:强效雄激素7alpha-methyl-19-nortestosterone的灵长类动物的前列腺保留作用:替代睾丸激素替代雄激素和男性避孕的潜在替代方法

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摘要

7alpha-Methyl-19-nortestosterone (MENT) is a potent synthetic androgen that cannot be converted to dihydrotestosterone. In this study we determined the relative androgenic, antigonadotropic, and anabolic potencies of testosterone vs. MENT in the nonhuman primate M. fascicularis. In castrated monkeys, dose-response relationships were generated for the effects of testosterone and MENT on gonadotropin levels, prostate growth, body weight, and lipid metabolism. In a pilot study, four monkeys were castrated, and magnetic resonance imaging (MRI) was used to document a 50% loss of prostate volume within 8 weeks, verifying that MRI is a reliable means to measure prostate size in this species. Two additional groups of six monkeys each were then castrated and serially administered four graded dosages of testosterone or MENT via osmotic minipumps over 20 weeks. Complete suppression of LH was achieved with a minimum of 0.3 mg/day MENT, compared to 3.0 mg/day testosterone. MENT supported body weight 10 times more potently than did testosterone. Baseline prostate volumes were maintained with 0.1-0.2 mg/day MENT vs. 0.3 mg/day testosterone. Thus, in monkeys, MENT is 10 times more potent than testosterone with regard to the clinically desirable end points of gonadotropin suppression and anabolism, but only twice as potent at stimulating prostate growth. These results suggest that MENT may have a wider therapeutic index than testosterone for human androgen replacement and male contraception.
机译:7alpha-Methyl-19-nortestosterone(MENT)是有效的合成雄激素,无法转化为二氢睾丸激素。在这项研究中,我们确定了非人类灵长类动物M. fascicularis中睾丸激素相对于MENT的相对雄激素,促性腺激素和合成代谢能力。在cast割的猴子中,产生了睾丸激素和MENT对促性腺激素水平,前列腺生长,体重和脂质代谢的影响的剂量反应关系。在一项先导研究中,将四只猴子去势,并使用磁共振成像(MRI)记录了8周内前列腺体积减少50%的情况,证明MRI是测量该物种前列腺大小的可靠方法。然后将另外两组每只六只猴子were割,并在20周内通过渗透性微型泵连续给药四级剂量的睾丸激素或MENT。相对于3.0毫克/天的睾丸激素,使用最低0.3毫克/天的MENT可以完全抑制LH。 MENT支持体重的效力比睾丸激素高10倍。基线前列腺体积维持在0.1-0.2 mg /天MENT与0.3 mg /天的睾丸激素水平之间。因此,在猴子中,就促性腺激素抑制和合成代谢的临床理想终点而言,MENT的功效是睾丸激素的10倍,但在刺激前列腺生长方面的功效仅是其两倍。这些结果表明,对于人类雄激素替代和男性避孕,MENT可能具有比睾丸激素更广泛的治疗指数。

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