非甾体雄激素受体配体的药代动力学和药效学
Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands.
作者信息
Gao Wenqing, Kim Juhyun, Dalton James T
机构信息
Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA.
出版信息
Pharm Res. 2006 Aug;23(8):1641-58. doi: 10.1007/s11095-006-9024-3.
Abstract
Testosterone and structurally related anabolic steroids have been used to treat hypogonadism, muscle wasting, osteoporosis, male contraception, cancer cachexia, anemia, and hormone replacement therapy in aging men or age-related frailty; while antiandrogens may be useful for treatment of conditions like acne, alopecia (male-pattern baldness), hirsutism, benign prostatic hyperplasia (BPH) and prostate cancer. However, the undesirable physicochemical and pharmacokinetic properties of steroidal androgen receptor (AR) ligands limited their clinical use. Nonsteroidal AR ligands with improved pharmacological and pharmacokinetic properties have been developed to overcome these problems. This review focuses on the pharmacokinetics, metabolism, and pharmacology of clinically used and emerging nonsteroidal AR ligands, including antagonists, agonists, and selective androgen receptor modulators.
摘要
睾酮及结构相关的合成代谢类固醇已被用于治疗性腺功能减退、肌肉萎缩、骨质疏松症、男性避孕、癌症恶病质、贫血以及老年男性的激素替代疗法或与年龄相关的身体虚弱；而抗雄激素药物可能有助于治疗痤疮、脱发（男性型秃发）、多毛症、良性前列腺增生（BPH）和前列腺癌等病症。然而，甾体雄激素受体（AR）配体不理想的物理化学和药代动力学特性限制了它们的临床应用。为克服这些问题，已开发出具有改善的药理学和药代动力学特性的非甾体AR配体。本综述重点关注临床使用的和新兴的非甾体AR配体的药代动力学、代谢和药理学，包括拮抗剂、激动剂和选择性雄激素受体调节剂。
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