Rosenberg B
Adv Exp Med Biol. 1977;91:129-50. doi: 10.1007/978-1-4684-0796-9_10.
Platinum coordination complexes form a new class of active anticancer agents in animals and man. Cis-dichlorodiammineplatinum (II), the most widely investigated drug, is now in experimental clinical use against a wide variety of cancers in man. The dose-limiting toxicity in man is renal tubular damage. Hydration of the patient and the use of osmotic diuretics have minimized this effect and allowed higher doses with largely improved responses. Combination chemotherapy with the drug has also produced significant response rates in a variety of cancers. The mode of action of the drug is not yet clear, but most likely involves a primary lesion on nuclear DNA and the stimulation of a host reaction to the cancer. So far, only square planar and octahedral complexes of platinum, with a variety of inorganic and organic ligands, have shown marked activity in animal studies.
铂配位络合物在动物和人类中构成了一类新型的活性抗癌剂。顺二氯二氨铂(II)是研究最广泛的药物,目前正处于针对人类多种癌症的实验性临床应用阶段。人类中的剂量限制性毒性是肾小管损伤。患者水化及使用渗透性利尿剂已使这种效应降至最低,并允许使用更高剂量且反应大幅改善。该药物的联合化疗在多种癌症中也产生了显著的缓解率。该药物的作用方式尚不清楚,但很可能涉及对核DNA的原发性损伤以及对癌症的宿主反应的刺激。到目前为止,在动物研究中,只有铂的平面正方形和八面体络合物与各种无机和有机配体显示出显著活性。