Product
Plevitrexed (BGC 9331)

Description
BGC 9331 (plevitrexed) is a novel targeted thymidylate synthase inhibitor for the treatment of ovarian and gastrointestinal tumours. BTG has completed a Phase IIa trial in advanced gastric cancer patients with results presented at ASCO GI Symposium in January 2007.

Further Information
Plevitrexed is a novel, direct-acting, potent and specific inhibitor of thymidylate synthase (TS), a key enzyme involved in DNA synthesis and the regulation of proliferation. TS is a well studied and validated target for anti-cancer therapeutics.

Unlike other TS inhibitors, plevitrexed does not require intracellular polyglutamation by the enzyme folylpolyglutamate synthetase (FPGS) to become active. Down-regulation of FPGS is one mechanism by which resistance develops in cancer cells. Since plevitrexed is not a substrate for FPGS, repeat dosing should not cause development of such resistance.

Plevitrexed’s action is independent of dihydropyrimidine dehydrogenase (DPD), and is not subject to resistance caused by modulation of DPD expression, as occurs with 5-FU.

Plevitrexed has been evaluated in Phase I and Phase II clinical trials in over 1,000 patients with solid tumours. Plevitrexed has demonstrated competitive efficacy as a single agent in gastric, pancreatic and ovarian cancer patients and has been developed as both ready-to-use intravenous and oral tablet formulations.

Clinical data generated to date supports the further evaluation of plevitrexed in gastric, pancreatic and ovarian cancers. Each of these cancers presents a significant unmet medical need and a corresponding commercial opportunity. Orphan drug status has been granted in the US for both ovarian and gastric cancer.

According to the American Cancer Society, in 2008 an estimated 21,500 gastric, 37,700 pancreatic and 21,650 ovarian cancer patients will be diagnosed in the US, indicating a significant unmet medical need for potential therapeutics, such as plevitrexed.

BTG is currently seeking a licensing partner for Plevitrexed. For more information, please contact us.

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