Changes in the immunological parameters after a single dose of forphenicinol, a new small molecular immunomodifier.
Forphenicinol [L-2-(3-hydroxy-4-hydroxymethyl-phenyl) 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 600 mg 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 less than 0.05) or from 63.1 to 78.5 in tuberculosis (n = 7, p less than 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 less than 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 100 mg. Forphenicinol was rather inhibitory on the NK activity, while it exerted diverse effect on the lymphocyte proliferation. No evidence of adverse effect was observed.
D000276:Adjuvants, Immunologic / Q000008:administration & dosage / Q000494:pharmacology*; D000328:Adult; D000368:Aged; D004305:Dose-Response Relationship, Drug; D005260:Female; D005998:Glycine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D007694:Killer Cells, Natural / Q000187:drug effects; D007958:Leukocyte Count; D008213:Lymphocyte Activation / Q000187:drug effects; D008214:Lymphocytes / Q000187:drug effects*; D008297:Male; D008875:Middle Aged
D000276:Adjuvants, Immunologic; C035946:forphenicinol; D005998:Glycine