Is There Room for SERMs or SARMs as Alternative Therapies for Adult Male Hypogonadism?

Is There Room for SERMs or SARMs as Alternative Therapies for Adult Male Hypogonadism? / Vito A Giagulli, Andrea Silvestrini, Carmine Bruno, Vincenzo Triggiani, Alvaro Mordente, Antonio Mancini. - (International Journal of Endocrinology (2020) 21 January)

  • PMID: 32411230
  • PMCID: PMC7201459
  • DOI: 10.1155/2020/9649838


Abstract

Hypogonadotropic hypogonadism (HH) can be sustained by organic or functional alterations of the hypothalamic-pituitary-testicular axis. Functional HH is related to systemic alterations, such as obesity or chronic inflammatory diseases, but could contribute to a negative course of the illness. For such situation, according to results obtained in infertile women, the administration of selective estrogen receptor modulators (SERMs) has been proposed in males too, with positive results on both metabolic and sexual function. This class of medications increases gonadotropin levels via antagonism to the estrogenic receptor; similar biological effects are also exerted by aromatase inhibitors (AIs), despite different mechanism of action. After a brief review of trials regarding SERMs and AIs use in male HH, we describe the structure and function of the androgen receptor (AR) as a basis for clinical research about compounds able to bind to AR, in order to obtain specific effects (SARMs). The tissue selectivity and different metabolic fate in comparison to testosterone can potentiate anabolic versus androgenic effects; therefore, they might be a valid alternative to testosterone replacement therapy avoiding the negative effects of testosterone (i.e., on prostate, liver, and hematopoiesis). Trials are still at an early phase of investigation and, at the moment, the application seems to be more useful for chronic disease with catabolic status while the validation as replacement for hypogonadism requires further studies.

Original document

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Science
Research / Study
Date
21 January 2020
People
Bruno, Carmine
Giagulli, Vito A
Mancini, Antonio
Mordente, Alvaro
Silvestrini, Andrea
Triggiani, Vincenzo
Country
Italy
Language
English
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Università Cattolica del Sacro Cuore (UCSC) - Catholic University of the Sacred Heart
Università degli Studi di Bari Aldo Moro - University of Bari Aldo Moro
Doping classes
S1. Anabolic Agents
Substances
Clomifene
Enobosarm (ostarine)
Letrozole
LGD-4033 (ligandrol)
RAD140
Selective androgen receptor modulators (SARMs)
Tamoxifen
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Hormone replacement therapy (HRT)
Hypogonadism
Legitimate Medical Treatment
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28 October 2021
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3 November 2021
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