LGD-4033是一种新型非甾体口服选择性雄激素受体调节剂，在健康年轻男性中的安全性、药代动力学和效果
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Basaria S, Collins L, Dillon EL, Orwoll K, Storer TW, Miciek R, Ulloor J, Zhang A, Eder R, Zientek H, Gordon G, Kazmi S, sheffard - moore M, Bhasin S
LGD-4033是一种新型非甾体口服选择性雄激素受体调节剂，在健康年轻男性中的安全性、药代动力学和效果
中华老年医学杂志。2013年1月;68(1):87-95。doi: 10.1093 /赫罗那/ gls078。Epub 2012 3月28日。
- PubMed ID
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22459616 (PubMed视图］
- 摘要
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背景:对睾酮对前列腺潜在不良影响的担忧促使选择性雄激素受体调节剂的发展，这些调节剂显示雄激素信号的组织选择性激活。LGD-4033是一种新型非甾体口服选择性雄激素受体调节剂，具有高亲和力和选择性结合雄激素受体。目标。评估安全性、耐受性、药代动力学，以及每天增加剂量的LGD-4033对瘦体重、肌肉力量、爬楼梯力量和性激素的影响，持续21天。方法:在这项安慰剂对照研究中，76名健康男性(21-50岁)被随机分为安慰剂组、0.1 mg、0.3 mg或1.0 mg LGD-4033组，持续21天。在干预期间和干预后的5周内测量血液计数、化学物质、血脂、前列腺特异性抗原、心电图、激素、瘦脂肪量和肌肉力量。结果:LGD-4033耐受性良好。未发生与药物相关的严重不良事件。积极组和安慰剂组不良事件发生率相似。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QT间期在任何剂量下均无显著变化。 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.