Pharmaceutical Research

, Volume 23, Issue 8, pp 1641–1658

Pharmacokinetics and Pharmacodynamics of Nonsteroidal Androgen Receptor Ligands

Expert Review


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.

Key Words

androgen receptor antiandrogen pharmacokinetics prostate cancer selective androgen receptor modulator testosterone 

Copyright information

© Springer Science+Business Media, Inc. 2006

Authors and Affiliations

  1. 1.Division of Pharmaceutics, College of PharmacyThe Ohio State UniversityColumbusUSA
  2. 2.ColumbusUSA
  3. 3.GTx, Inc.MemphisUSA

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