Walz D T, DiMartino M J, Griswold D E, Intoccia A P, Flanagan T L
Am J Med. 1983 Dec 30;75(6A):90-108. doi: 10.1016/0002-9343(83)90481-3.
The preclinical profiles of auranofin (Ridaura), an oral chrysotherapeutic agent, parenteral gold sodium thiomalate, gold thioglucose, and their respective ligands were compared. Auranofin was more effective than gold sodium thiomalate in suppressing inflammation and stimulating cell-mediated immunity. In contrast to gold sodium thiomalate and gold thioglucose, auranofin inhibited cellular release of lysosomal enzymes, antibody-dependent cellular cytotoxicity, production of antibodies in adjuvant arthritic rats, and antibodies involved in cytotoxicity reactions. The respective ligands were without significant biologic activity. In rats, a higher fraction of gold was associated with blood cells after auranofin administration than after gold sodium thiomalate. The absorption, distribution, metabolism, and excretion of auranofin are uniquely different from other gold compounds.
比较了口服金制剂金诺芬（瑞得）、胃肠外给药的硫代苹果酸金钠、硫代葡萄糖金及其各自配体的临床前概况。金诺芬在抑制炎症和刺激细胞介导免疫方面比硫代苹果酸金钠更有效。与硫代苹果酸金钠和硫代葡萄糖金不同，金诺芬可抑制溶酶体酶的细胞释放、抗体依赖性细胞毒性、佐剂性关节炎大鼠体内抗体的产生以及细胞毒性反应中涉及的抗体。各自的配体没有显著的生物学活性。在大鼠中，给予金诺芬后与血细胞结合的金的比例高于给予硫代苹果酸金钠后。金诺芬的吸收、分布、代谢和排泄与其他金化合物有独特的差异。
