THG was developed completely in secret by Patrick Arnold as a designer drug, on the basis that doping testers would be unlikely to detect a totally new compound.

This was then transferred to the research group of pharmacologist Don Catlin, who identified the drug using mass spectrometry techniques and gave it its present name.

[11] According to Patrick Arnold, due to the drug's potency, he never had to supply significant quantities to BALCO, because "just a couple of drops under the tongue" were a sufficient dose.

[15] THG was developed by Patrick Arnold for the Bay Area Laboratory Co-operative (BALCO), which claimed to be a nutritional supplement company.

[16] The company manufactured the drug through palladium-charcoal catalyzed hydrogenation from gestrinone, a substance used in gynecology for treatment of endometriosis (Australian Medicines handbook 2011).

This helped Don Catlin, MD, the founder and then-director of the UCLA Olympic Analytical Lab, to identify and develop a test for THG, the second reported designer anabolic steroid.