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Pharmacokinetics and Pharmacodynamics of Nonsteroidal Androgen Receptor Ligands

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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.

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  1. Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, Ohio, 43210, USA

    Wenqing Gao, Juhyun Kim & James T. Dalton

  2. 500 West 12th Avenue, L.M. Parks Hall, Room 242, Columbus, Ohio, 43210, USA

    James T. Dalton

  3. GTx, Inc., 3 North Dunlap Street, Memphis, TN, 38163, USA

    James T. Dalton

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Gao, W., Kim, J. & Dalton, J.T. Pharmacokinetics and Pharmacodynamics of Nonsteroidal Androgen Receptor Ligands. Pharm Res 23, 1641–1658 (2006). https://doi.org/10.1007/s11095-006-9024-3

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