Early clinical and toxicological results of a combi nation of natural glycolysis inhibitors (METABLOC™) on cancer patients.

The metabolism of tumor cells plays an important role in cancer development. Although aerobic glycolysis is inefficient from the standpoi nt of ATP production, it provides cancer cells with biomolecules implicated in the synthesis of lipids and nucleotides required for cellular proliferation. Thus, targeting aerobic glycolys is has clearly been recognized as a potentially fruitful approach for the treatment of cance r. The inhibition of aerobic glycolysis by a combination of alpha lipoic acid and hydroxycitrate (METABLOC) is efficient to inhibit tumor development in several mouse models. In association with chemotherapy, it seems to improve survival of patients with tumors difficult to treat when compared to a single chemotherapy regimen. We herein report our preliminary cases on both the clinical efficacy and side effects of METABLOC. Eleven patients with advanced metastatic cancer from were treated with per os 0.4 to 1.8 g of lipoic acid and 1.2 to 3 g of hydroxycitrate during 2 to 21 months inaddition to their normal chemotherapeutic regimen. Side effects occurred in half of the patients but were mild (grade 1-3) and limited to gastrointestinal disorders that disappeared on using proton pump inhibitors or decreasing the doses. Five patients were characterized by a partial regression, 3 by a stable dise ase, and 3 by disease progression. In conclusion the results from these preliminary treatments support that METABLOC can be used safely with various common standard chemotherapeutic regimens. It also suggests that its use may slow down tumor growth, an observation that needs to be confirmed by a randomized controlled trial .