Motohiro Ohkoshi

Clinical experience with a protease inhibitor [N,N-dimethylcarbamoylmethyl 4-(4-guanidinobenzoyloxy)-phenylacetate] methanesulfate for prevention of recurrence of carcinoma of the mouth and in treatment of terminal carcinoma

A protease inhibitor, (N,N-dimethylcarbamoylmethyl 4-(4-guanidinobenzoyloxy)-phenylacetate) methanesulfate was administered orally 3 times daily to 9 patients with squamous cell carcinoma of the oral cavity, at doses ranging from 0.6 g. to 7.2 g. Seven of 9 patients who had undergone all kinds of therapies were observed to see whether recurrence was prevented and in no case did the tumour recur. Also, in 2 terminal secondary cases tumour remission resulted. Histologically, after this therapy, carcinomatous lesions showed marked hyperkeratosis in 2 cases and the survival time in 1 case was markedly prolonged. Haematological and gastrointestinal toxicity was almost never observed at these doses.

EFFECT OF A PROTEASE INHIBITOR [N,N-DIMETHYL-CARBAMOYLMETHYL 4-(4-GUANIDINOBENZOYLOXY)-PHENYLACETATE] METHANESULFATE OF THE GROWTH OF MOUSE SKIN CARCINOMA IN THE RAPID GROWING STAGE

The oral administration of synthetic broad spectrum protease inhibitor, [N,N‐dimethylcarbamoylmethyl 4‐(4‐guanidinobenzoyloxy)‐phenylacetate] methanesulfate, was used to challenge 3‐methylcholanthrene‐induced skin carcinoma in the rapid growing stage.

AGE-RELATED CHANGES IN DRUG CONCENTRATION IN SKIN AND LUNGS OF MICE

How drug concentration in skin and lung due to vascular action changed with aging was examined quantitatively by a bioassay using bacteria. The concentration of the drug (anticancerous agent, Bleomycin) did not decrease in the skin of older mice as compared with that in younger mice, but showed a decrease in the lungs.