GTx presents preclinical studies of GTx-758 and GTx-230 for treatment of cancer

Nov 15 2010

GTx, Inc. (Nasdaq: GTXI) announced the presentation of preclinical studies evaluating GTx-758, a selective estrogen receptor alpha agonist being developed for first line treatment of advanced prostate cancer, and GTx-230, a novel microtubule polymerization inhibitor.

“Improved bone quality and suppression of testosterone levels by a novel selective estrogen receptor alpha agonist.”

The study results were presented this past weekend in Atlanta at the annual meeting of the Society of Basic Urologic Research (SBUR).

GTx-758: An oral selective estrogen receptor alpha agonist, GTx-758 is being developed for first line treatment in men with advanced prostate cancer. In a Phase II open label pharmacokinetic/pharmacodynamic (PK/PD) clinical trial in 60 healthy young male volunteers, treatment with 1000 mg and 1500 mg doses of GTx-758 demonstrated the ability to achieve medical castration (serum total testosterone < 50 ng/dL). In the first half of 2011, GTx is planning to initiate a Phase II clinical trial evaluating GTx-758 compared to Lupron® (leuprolide acetate) for first line treatment of advanced prostate cancer.

GTx presented results of three preclinical GTx-758 studies at the SBUR:

• "Improved bone quality and suppression of testosterone levels by a novel selective estrogen receptor alpha agonist."
  Lead author: Kearbey, Jeffrey

• "Oral administration of GTx-758 reduces serum testosterone but does not increase whole blood platelet aggregation in mature male cynomolgus monkeys."
  Lead author: Veverka, Karen

• "Anti-prostate effects of a selective estrogen receptor-α agonist, GTx-758, in vitro and in aged male cynomolgus monkeys."
  Lead author: Narayanan, Ramesh

GTx-230: An orally available tubulin antagonist discovered by GTx researchers, GTx-230 has the potential to treat cancer and cancer refractory to taxane and vinca alkaloid therapy. Unlike currently approved therapies, GTx-230 binds to tubulin at the colchicine site and circumvents multidrug resistance transporters resulting in potent suppression of cancer and taxane-resistant tumor xenografts. Importantly, in animal models GTx-230 also has less neurotoxicity than currently approved therapies.

GTx presented results of a preclinical GTx-230 study at the SBUR:

• "Potent antitumor activity and pharamcokinetics of a novel microtubule polymerization inhibitor in xenograft models of multidrug resistant tumors."
  Lead author: Ahn, Sunjoo