安全、药物动力学和影响乐金显示器- 4033,一种新的非甾体类口服,选择性雄激素受体调节剂,在健康的年轻人。
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柯林斯Basaria年代,L,狄龙EL, Orwoll K,仓库保管员TW, Miciek R, Ulloor J,张,埃德尔R, Zientek H, Gordon G,伤势严重,Sheffield-Moore M,哈
安全、药物动力学和影响乐金显示器- 4033,一种新的非甾体类口服,选择性雄激素受体调节剂,在健康的年轻人。
J Gerontol Sci地中海Sci杂志。2013年1月,68 (1):87 - 95。doi: 10.1093 /赫罗那/ gls078。Epub 2012年3月28日。
- PubMed ID
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22459616 (在PubMed]
- 文摘
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背景:担忧的潜在不利影响睾丸素在前列腺动机beplayapp选择性雄激素受体调节剂的发展显示tissue-selective激活的雄激素信号。乐金显示器- 4033,一种新的非甾体类,口服选择性雄激素受体调节剂,结合雄激素受体具有高亲和力和选择性。目标。评估安全、耐受性、药物动力学和影响提升剂乐金显示器- 4033管理每日21天瘦体重,肌肉力量,踩步力量,性激素。方法:在这个安慰剂对照研究中,76名健康男性(21-50年)随机安慰剂或0.1,0.3或1.0毫克,每日乐金显示器- 4033 21天。血液计数、化学反应、脂质,前列腺特异性抗原,心电图,激素、瘦肉和脂肪,肌肉力量测量期间和5周后干预。结果:乐金显示器- 4033是耐受性良好。没有与毒品有关的严重不良事件。不良事件的发生频率之间类似的活跃和安慰剂组。血红蛋白,前列腺特异性抗原,天冬氨酸转氨酶,丙氨酸转氨酶,或在任何剂量QT间隔没有显著变化。 LGD-4033 had a long elimination half-life and dose-proportional accumulation upon multiple dosing. LGD-4033 administration was associated with dose-dependent suppression of total testosterone, sex hormone-binding globulin, high density lipoprotein cholesterol, and triglyceride levels. follicle-stimulating hormone and free testosterone showed significant suppression at 1.0-mg dose only. Lean body mass increased dose dependently, but fat mass did not change significantly. Hormone levels and lipids returned to baseline after treatment discontinuation. CONCLUSIONS: LGD-4033 was safe, had favorable pharmacokinetic profile, and increased lean body mass even during this short period without change in prostate-specific antigen. Longer randomized trials should evaluate its efficacy in improving physical function and health outcomes in select populations.