4, 6-0-Benzylidene-D-glucopyranose (BG) in the treatment of solid malignant tumours, an extended phase I study

Abstract

Summary 4, 6-0-Benzylidene-D-glucopyranose (BG), a derivative of benzaldehyde (BA), whose anti-tumour action has often been reported, showed responses in 10 out of 24 patients (41.7%). These patients consisted of 11 cases of primary lung cancer, 4 of metastatic lung cancer, 5 of gastric cancer, and one each of cancer of the sigmoid colon, liver, pancreas and prostate. There were two complete responses (one each of ipsilateral lung metastasis from breast cancer and metastatic liver lesions due to gastric cancer). The mean total dose of BG was 392.6 g, given by intravenous infusion of 1.2 g BG in 100 ml saline twice daily. The treatment was discontinued when no response was observed after two months. Careful monitoring showed no toxic action of BG at these large doses. Complete necrotic liquefaction of tumour, without any damage to surrounding tissue, was seen in 2 of 3 cases in which histological examination was feasible. It is apparent that BG, like BA, is not a cytotoxic agent in the ordinary sense, but its mechanism of action is still unknown.

Tumour necrotisation in nude mice xenografts by the reversible protein synthesis inhibitor zilascorb(2H)

“…In the present experiments, no signs of any side-effects were seen in the animals, there was not observed any difference in body weight between drug treated and placebo treated animals (Table I) We know that the drugs tested in clinical studies by Dr Kochi (1980Kochi ( , 1985Kochi ( , 1988, and later by others (Tatsemura et al, 1990), induced some anticancer effect without any observed side-effects and this is given an explanation with the present hypothesis. Warrington (1986) suggested that normal cells, as a response to protein synthesis inhibition, will stop cycling while cancer cells will not.…”

“…In fact, experiments using various benzaldehyde derivatives against tumours grown in mice have often shown little or no effect, although the same derivatives were reported to be effective in patients (Kochi et al, 1980;1985;1988;Tatsemura, 1990). One can wonder whether this seeming difference between the effect as seen in mice and in humans could be due to some metabolic difference between the two species, or perhaps, to differences in administration of the drug, being i.v.…”