Abstract
KUMANO, N., NAKAI, Y., ISHIKAWA, T., KOINUMARU, S., SUZUKI, S., OIZUMI, K. and KONNO, K. Changes in the Immunological Parameters after a Single Dose of Forphenicinol, a New Small Molecular Immunomodifier. Tohoku J. exp. Med., 1985, 146 (4), 419-427 - Forphenicinol [L-2-(3-hydroxy-4-hydroxymethylphenyl) glycine, M.W. 197.19] is a derivative of forphenicine, an inhibitor of alkaline phosphatase discovered by Umezawa. In order to find an optimal dose, a single dose of the drug ranging from 10 to 600mg per body was orally administered to a total of 55 patients (36 cancer, 13 tuberculosis, and 6 others). The possible changes in the percentages of the peripheral T and B lymphocytes, natural killer (NK) activity, and the proliferative response to phytohemaglutinin (PHA) were studied as immunological parameters. A significant effect of forphenicinol was demonstrated in restoring the normal proportion of T and B cells, especially in those who had 'low'-T and/or 'high'-B before administration of the drug. No difference was found between cancer and tuberculosis. The mean percentage of T cells increased from the low initial level of 68.0 to 75.6 in cancer (n=12, p<0.05) or from 63.1 to 78.5 in tuberculosis (n=7, p<0.05), while that of B cells decreased from the high initial level of 34.6 to 26.9 in cancer (n=7) or from 34.9 to 14.3 in tuberculosis (n=6, p<0.025). The effect of a single dose of the drug tended to disappear by day 8, a peak response being found on day 3 in most cases. With respect to this parameter, an optimal dose was found in a range from 60 to 100mg. Forphenicinol was rather inhibitory on the NK activity, while it exerted diverse effect on the lymphocyte proliferation. No evidence of adverse effect was observed. - forphenicinol; small molecular BRM; T and B cells; NK activity
