早期临床研究与cis-diammine-1 1-cyclobutane dicarboxylate铂二世。

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卡尔弗特啊,哈兰SJ,纽厄尔博士,Siddik,琼斯AC, McElwain TJ, Raju年代,Wiltshaw E,史密斯即贝克JM, Peckham MJ, Harrap出版社KR

早期临床研究与cis-diammine-1 1-cyclobutane dicarboxylate铂二世。

癌症Chemother杂志。1982;9 (3):140 - 7。doi: 10.1007 / BF00257742。

PubMed ID

6761010 (在PubMed

]

文摘

cis-Diammine-1, 1-cyclobutane dicarboxylate铂二世(CBDCA JM8)、顺铂的模拟显示减少毒性在临床前研究中,在60个病人评估。每3周剂量有最初从20到520 mg / m2和升级。这后,每4周剂量有和从300升级到500毫克/平方米。thrombocytopoenia dose-limiting毒性,发生在4/5的患者在520 mg / m2,最低点在治疗后3周发生。Leucopoenia和贫血也发生,但不太严重。呕吐发生在所有患者接受超过120 mg / m2但很少持续超过24小时。连续测量51 cr-edta许可,尿N-acetylglucosaminidase,尿亮氨酸氨基肽酶,和β2-microglobulin没有揭示肾毒性的重要证据。损害听力图尚未见过的第一个13个病人进行了研究。药理研究表明,大部分的剂量的白金在尿液中排出,,肾功能的损伤可能与药物有关保留和myelosuppression的风险增加。之前的治疗和患者的年龄也会影响药物的耐受性。临床反应被认为卵巢癌患者接受大于120 mg / m2。 A further dose escalation was performed on a 4-week schedule in patients under 65 with good renal function. The maximum dose it was possible to administer repeatedly without incurring myelosuppression was in the range 400-500 mg/m2. JM8 is not significantly nephrotoxic and is less emetic than cisplatin. It has antitumour activity in man and deserves wider evaluation, along with the other analogues under study in various centres, as an alternative to cisplatin.

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药物

卡铂