Presnov M A, Konovalova A L, Kozlov A M, Brovtsyn V K, Romanova L F
Neoplasma. 1985;32(1):73-83.
A coordination complex cis-dichlorodiamminedihydroxoplatinum (IV) (oxoplatinum) was first synthesized in the USSR by Chugaev and Khlopin in 1927 [3]. Its marked antitumor properties were revealed by one of the authors of this article at the All-Union Cancer Research Center of the Academy of Medical Sciences of the USSR. The paper gives data on the antiblastic and side effects of oxoplatinum and also on the results of pharmacokinetic studies of the drug. Particular attention was paid to the similarity and differences of biological properties of oxoplatinum and cis-dichlorodiammineplatinum(II) (DDP) which has found wide use in oncological practice. It has been established that, on principle, oxoplatinum differs from DDP in action on the body and tumors. The new drug is 10 times less toxic than DDP. Oxoplatinum has a wide spectrum of antineoplastic action resulting in marked inhibition of growth of solid and ascitic forms of transplantable tumors. The drug has a longer duration of antitumor effect after the end of the therapeutic course. An important property of oxoplatinum is its high therapeutic index. The new drug manifests high antitumor activity with different ways of its administration into the body. Oxoplatinum in therapeutic doses does not produce necrotic lesions in the kidneys. The new drug exerted no cross-resistance with DDP and the alkylating antitumor agent sarcolysin. At the present time oxoplatinum is undergoing preclinical investigation.
一种配位化合物顺二氯二氨二羟基铂(IV)(氧铂)于1927年由丘加耶夫和赫洛平在苏联首次合成[3]。本文的一位作者在苏联医学科学院全苏癌症研究中心发现了它显著的抗肿瘤特性。该论文给出了氧铂的抗瘤作用和副作用的数据,以及该药物的药代动力学研究结果。特别关注了氧铂和顺二氯二氨铂(II)(顺铂)生物学特性的异同,顺铂已在肿瘤学实践中广泛应用。已经确定,原则上,氧铂在对身体和肿瘤的作用方面与顺铂不同。这种新药的毒性比顺铂低10倍。氧铂具有广泛的抗肿瘤作用谱,能显著抑制可移植肿瘤实体瘤和腹水瘤的生长。在治疗疗程结束后,该药物的抗肿瘤作用持续时间更长。氧铂的一个重要特性是其高治疗指数。这种新药通过不同的给药方式进入体内均表现出高抗肿瘤活性。治疗剂量的氧铂不会在肾脏产生坏死性病变。这种新药与顺铂和烷化抗肿瘤剂溶肉瘤素不存在交叉耐药性。目前氧铂正在进行临床前研究。