Arnold A M
Cancer Chemother Pharmacol. 1979;3(2):71-80. doi: 10.1007/BF00254976.
VP 16-213, a derivative of podophyllotoxin, is currently entering phase-III studies. Its mode of action is incompletely understood, but differs markedly from that of its parent compound. The greatest lethal damage is experienced by cells in the late S and G2 phases. In the L 1210 system the drug shows marked schedule dependency: prolonged administration may be more effective than single bolus administration. As a single agent, VP 16-213 is the most active compound yet tested against small-cell bronchial carcinoma. It may also prove to be a useful agent in patients with other types of lung tumour, testicular teratomas, and some types of leukaemia. No long-term or cumulative toxicity has been reported. Most side effects are predictable and reproducible.
VP 16 - 213是鬼臼毒素的衍生物,目前正进入三期研究。其作用方式尚未完全明确,但与母体化合物的作用方式有显著差异。处于S期后期和G2期的细胞受到的致死性损伤最大。在L 1210系统中,该药物显示出明显的给药方案依赖性:长期给药可能比单次大剂量给药更有效。作为单一药物,VP 16 - 213是目前针对小细胞支气管癌测试的最具活性的化合物。它也可能被证明是治疗其他类型肺肿瘤、睾丸畸胎瘤和某些类型白血病患者的有效药物。尚未报告有长期或累积毒性。大多数副作用是可预测和可重复的。