甲氨蝶呤与甲氨蝶呤单克隆抗体复合物在小鼠体内的比较生物分布
Comparative biodistribution of methotrexate and monoclonal antibody-methotrexate complexes in mice.
作者信息
Pimm M V, Caten J E, Clegg J A, Jacobs E, Baldwin R W
机构信息
Cancer Research Campaign Laboratories, University of Nottingham, UK.
出版信息
J Pharm Pharmacol. 1987 Sep;39(9):764-7. doi: 10.1111/j.2042-7158.1987.tb06990.x.
The biodistribution of radiolabelled methotrexate and immune complexes of methotrexate and a murine monoclonal anti-methotrexate antibody has been compared in mice. Complexes formed in-vitro with the antibody, but not with control immunoglobulin. The complexes were, characteristically, acid labile. In-vivo, blood levels, organ distribution and whole body catabolism of methotrexate in immune complexes were similar to those of free antibody, and markedly different from those of free drug. These findings suggest the feasibility of prolonging the survival of drugs and altering in-vivo distribution using complexes with monoclonal antibodies.
已在小鼠中比较了放射性标记的甲氨蝶呤以及甲氨蝶呤与鼠抗甲氨蝶呤单克隆抗体的免疫复合物的生物分布。该复合物是在体外与抗体而非对照免疫球蛋白形成的。这些复合物的特点是对酸不稳定。在体内，免疫复合物中甲氨蝶呤的血药浓度、器官分布及全身分解代谢与游离抗体相似，与游离药物明显不同。这些发现提示利用单克隆抗体复合物延长药物存留时间并改变体内分布的可行性。
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