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21.12.2020

GLPG0492 | The SARM that disappeared

The Belgian-Dutch research company Galapagos conducted trials in the 2010s with a SARM that is available orally. Galalagos even conducted phase-1 trials, but after that GLPG0492 disappeared from the scene. Whether that also means we'll never hear from GLPG0492 again?

Only animal studies
You will not find studies in which real humans have received GLPG0492 in the biomedical scientific literature, but there are some animal studies. [BMC Musculoskelet Disord. 2014 Sep 3;15:291.] [Pharmacol Res. 2013 Jun;72:9-24.]

The first animal study appeared in 2012. In this paper Galapagos introduced GLPG0492 as an orally available SARM that approximated the muscle-enhancing effect of testosterone propionate administered by injection, with only a fraction of the androgenic effect of testosterone propionate. [J Med Chem. 2012 Oct 11;55(19):8236-47.]

Human studies
The first publication from 2012 already states that "GLPG0492 is now undergoing phase-1 clinical trials". According to a press release issued by Galapagos on 12/2/2010, the first pharmacokinetic experiments, in which subjects received single doses of 0.5 to 120 milligrams, had positive results. Galapagos experimented with solid and liquid oral formulations.

On clinicaltrials.gov [clinicaltrials.gov] we see that in 2010-2012 Galapagos had already completed 3 clinical phase-1 trials with oral applications of GLPG0492. The results have not been published in peer reviewed papers, as far as we know.

Tests
You might suspect that the results of those trials have been disappointing. Yet researchers outside of Galapagos are taking GLPG0492 seriously.

The European Union recently commissioned chemists from Queen's University Belfast to develop a test for detecting the use of GLPG0492 in cattle and racehorses. [Drug Test Anal. 2020 Sep;12(9):1373-9.] Brussels apparently does not rule out that the hormone mafia will ever start using GLPG0492 in the future. Two years earlier, in 2018, German biochemists published a doping test commissioned by WADA. [Mol Cell Endocrinol. 2018 Mar 15;464:34-45.]

Developing tests takes time and money. It only happens when scientists have indications that a drug has potential. So it is possible that we will come across GLPG0492 again as a gray supplement...

Source:
J Med Chem. 2012 Oct 11;55(19):8236-47.

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