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Male Sex Hormones, Analogs, and Antagonists

Pulmonary, Bone, Vitamins and Autocoid Therapeutic Agents

  1. Robert W. Brueggemeier

Published Online: 15 JAN 2003

DOI: 10.1002/0471266949.bmc055

Burger's Medicinal Chemistry and Drug Discovery

Burger's Medicinal Chemistry and Drug Discovery

How to Cite

Brueggemeier, R. W. 2003. Male Sex Hormones, Analogs, and Antagonists. Burger's Medicinal Chemistry and Drug Discovery. 153–218.

Author Information

  1. The Ohio State University, College of Pharmacy, Columbus, OH

Publication History

  1. Published Online: 15 JAN 2003


The steroid testosterone is the major circulating sex hormone of the male and serves as the prototype for the androgens, the anabolic agents, and androgen antagonists. The endogenous androgens are biosynthesized from cholesterol in various tissues in the body; the majority of the circulating androgens are made in the testes under the stimulation of the gonadotropin luteinizing hormone (LH). The reduction of testosterone to dihydrotestosterone is necessary for the androgenic actions of testosterone in many androgen target tissues such as the prostate; the oxidation of testosterone by the enzyme aromatase produces estrogens. The androgenic actions of testosterone and dihydrotestosterone are due to their binding to the androgen receptor, followed by nuclear localization, dimerization of the receptor complex, and binding to a specific DNA sequence. This binding of the homodimer to the androgen response element leads to gene expression, stimulation or repression of the synthesis of new mRNA, and subsequent protein biosynthesis. The synthetic androgens and anabolics were prepared to impart oral activity to the androgen molecule, to separate the androgenic effects of testosterone from its anabolic effects, and to improve upon its biological activities. Novel nonsteroidal androgens, termed selective androgen receptor modulators, were developed to impart agonist activity in selective tissues. Drug preparations are used for the treatment of various androgen-deficient diseases, for the therapy of diseases characterized by muscle wasting and protein catabolism, for postoperative adjuvant therapy, and for the treatment of certain hormone-dependent cancers. The two major categories of androgen antagonists are the antiandrogens, which block interactions of androgens with the androgen receptor, and the inhibitors of androgen biosynthesis and metabolism. Such compounds have therapeutic potential in the treatment of acne, virilization in women, hyperplasia and neoplasia of the prostate, and baldness and male contraception.


  • anabolics;
  • androgens;
  • antiandrogens;
  • dihydrotestosterone;
  • 5α-reductase inhibitors;
  • selective androgen receptor modulators;
  • testosterone