open access

Vol 4, No 2 (2019)
REVIEW ARTICLES
Published online: 2019-08-06
Get Citation

Duality nature of Selective Androgen Receptor Modulators and Specific Steroids Substance

Damian Gorczyca, Dorota Kwiatkowska
DOI: 10.5603/DEMJ.2019.0012
·
Disaster Emerg Med J 2019;4(2):60-62.

open access

Vol 4, No 2 (2019)
REVIEW ARTICLES
Published online: 2019-08-06

Abstract

Selective Androgen Receptor Modulators (SARMs) are the novel class of the androgen receptors (AR), often called tissue-selective AR ligands. Discovery of SARMs will give a possibility to the alternative therapy for androgens therapy (osteoporosis, prostate cancer, muscle wasting). SARMs should have high specificity for the AR, tissue-selective pharmacokinetic activities, improved oral bioavailability and pharmacokinetic profile which allows once-a-day administration [1].

Example of SARMs is flutamide (flutamidum, Eulexin, imid 2-methyl-N-{4-nitro-(3-trifluoromethyl)-phenyl]- propionic acid), a synthetic nonsteroidal drug that is a competitive antagonist of the androgen receptor. SARMs were recognized as forbidden substances by the World Anti-Doping Agency (WADA) and since 2004 they are on the Prohibited List. To point on the Prohibited List 2019 “Substance and methods prohibited at all time (in- and out-of-competition)” SARMs belong to group S1. 2. Other Anabolic Agents, and to group S4. Hormone Antagonist and Modulators [2].

The main role of an anti-doping laboratory is to analyse and to determine whether a given substance should be prohibited in sport. The principal analyses of SARMs and Specific Steroid Substance are a different variant of chromatography (LC — liquid or GC — gas) with many detection techniques (MS — mainly mass spectrometer, MS/MS — tandem mass spectrometer).

Abstract

Selective Androgen Receptor Modulators (SARMs) are the novel class of the androgen receptors (AR), often called tissue-selective AR ligands. Discovery of SARMs will give a possibility to the alternative therapy for androgens therapy (osteoporosis, prostate cancer, muscle wasting). SARMs should have high specificity for the AR, tissue-selective pharmacokinetic activities, improved oral bioavailability and pharmacokinetic profile which allows once-a-day administration [1].

Example of SARMs is flutamide (flutamidum, Eulexin, imid 2-methyl-N-{4-nitro-(3-trifluoromethyl)-phenyl]- propionic acid), a synthetic nonsteroidal drug that is a competitive antagonist of the androgen receptor. SARMs were recognized as forbidden substances by the World Anti-Doping Agency (WADA) and since 2004 they are on the Prohibited List. To point on the Prohibited List 2019 “Substance and methods prohibited at all time (in- and out-of-competition)” SARMs belong to group S1. 2. Other Anabolic Agents, and to group S4. Hormone Antagonist and Modulators [2].

The main role of an anti-doping laboratory is to analyse and to determine whether a given substance should be prohibited in sport. The principal analyses of SARMs and Specific Steroid Substance are a different variant of chromatography (LC — liquid or GC — gas) with many detection techniques (MS — mainly mass spectrometer, MS/MS — tandem mass spectrometer).

Get Citation

Keywords

SARMs; SERMs; antiandrogens; antiestrogens; doping analysis

About this article
Title

Duality nature of Selective Androgen Receptor Modulators and Specific Steroids Substance

Journal

Disaster and Emergency Medicine Journal

Issue

Vol 4, No 2 (2019)

Pages

60-62

Published online

2019-08-06

DOI

10.5603/DEMJ.2019.0012

Bibliographic record

Disaster Emerg Med J 2019;4(2):60-62.

Keywords

SARMs
SERMs
antiandrogens
antiestrogens
doping analysis

Authors

Damian Gorczyca
Dorota Kwiatkowska

References (6)
  1. Wenqing G, Dalton JT. Drug Discovery Today. 2007; 12: 241.
  2. World Anti-Doping Agency: The 2019 prohibited list, World Anti-Doping Agency, Montreal (2019). http://www.wada-ama.org/rtecontent/document/2019_List_En.pdf (14.07.2019).
  3. Macgregor JI, Jordana C. Pharmacological Reviews. 1998; 50: 151.
  4. Gjerde J, et al. Chromatogr A. 2005; 1082: 6.
  5. Thevis M., Kamber M., Schänzer W. Proceeding of the 5th Workshop on Dope analysis. Cologne, 2000.
  6. World Anti-Doping Agency: WADA annually publishes statistical reports as reported by the WADA-accredited laboratories in ADAMS, 2017 Anti-Doping Testing Figures Report - Executive Summary (online 14.07.2019).

Important: This website uses cookies. More >>

The cookies allow us to identify your computer and find out details about your last visit. They remembering whether you've visited the site before, so that you remain logged in - or to help us work out how many new website visitors we get each month. Most internet browsers accept cookies automatically, but you can change the settings of your browser to erase cookies or prevent automatic acceptance if you prefer.

By "Via Medica sp. z o.o." sp.k., ul. Świętokrzyska 73, 80–180 Gdańsk, Poland
tel.:+48 58 320 94 94, fax:+48 58 320 94 60, e-mail: viamedica@viamedica.pl