Barton B E, Levy D A
J Immunopharmacol. 1985;7(3):343-71. doi: 10.3109/08923978509026481.
A potent antischistosomal drug, Amoscanate, was found to be immunogenic to mice and Cebus apella monkeys. The drug was readily haptenated to proteins under relatively mild conditions. The Amoscanate-protein conjugates were observed to be immunogenic when injected into the footpads of several strains of mice. However, such protein conjugates were not found to raise IgE antibody to the drug in high-responder strains using several procedures. When the formulated drug (dissolved in oil) was fed to CD 1 mice, a rise in serum antibody against the drug was noted 1 week following the primary dose. This is preliminary evidence that the drug, or a cross-reactive metabolite, becomes covalently bound to proteins in vivo. Cebus apella monkeys fed the drug exhibited a rise in anti-Amoscanate antibody one month after a second oral dose. These data suggest that the immunogenicity of Amoscanate is readily detected; furthermore, since there is no lasting immunity to schistosomiasis, thus necessitating multiple administration of the drug, the possibility that serum antibody titers to Amoscanate may interfere with its therapeutic efficacy cannot be overlooked.
一种强效抗血吸虫药物——硝硫氰胺，被发现对小鼠和卷尾猴具有免疫原性。该药物在相对温和的条件下很容易与蛋白质形成半抗原。当将硝硫氰胺 - 蛋白质偶联物注射到几种品系小鼠的足垫中时，观察到其具有免疫原性。然而，使用多种方法在高反应性品系中未发现此类蛋白质偶联物能产生针对该药物的IgE抗体。当将配方药物（溶解在油中）喂给CD1小鼠时，在初次给药1周后，血清中针对该药物的抗体出现升高。这是该药物或交叉反应性代谢物在体内与蛋白质共价结合的初步证据。喂食该药物的卷尾猴在第二次口服给药1个月后，抗硝硫氰胺抗体出现升高。这些数据表明，硝硫氰胺的免疫原性很容易被检测到；此外，由于对血吸虫病不存在持久免疫力，因此需要多次给药，所以不能忽视血清中针对硝硫氰胺的抗体滴度可能会干扰其治疗效果的可能性。
