[1] The company licensed toremifene from Orion Corporation, and licensed andarine, enobosarm and prostarine from the University of Tennessee Research Foundation; the SARM compounds from Tennessee had been invented by Duane D Miller and James T Dalton, who later joined the company and served as Chief Scientific Officer.

[2][3] In 2006 GTx signed a partnership with Ipsen to develop toremifene, a selective estrogen receptor modulator to prevent prostate cancer and to prevent bone loss in men with prostate cancer; the FDA rejected the application to market the drug for this use in 2009, and Ipsen terminated the arrangement in 2011.

[4][5] In 2012 GTx sold its rights to toremifene to ProStrakan, a subsidiary of Kyowa Hakko Kirin, for around $19 million, and terminated its agreement with Orion.

[8] In August 2013 GTx announced that enobosarm had failed in two Phase III clinical trials to treat wasting in people with lung cancer.

[12] In 2016 GTx began Phase II trials, to see if enosobarm might be effective to treat stress urinary incontinence in women.