Department of Oncology, Istituto di Ricerche Farmacologiche Mario Negri, Via La Masa 19, Milan, Italy.
Cancer Chemother Pharmacol. 2010 Sep;66(4):635-41. doi: 10.1007/s00280-009-1201-8. Epub 2009 Dec 20.
This study compared the antitumor activity and the pharmacological profile of gimatecan given orally and irinotecan (CPT-11) on pediatric tumor xenografts.
Gimatecan was tested in two neuroblastoma cell lines (SK-N-DZ and SK-N-(BE)2c) and on TE-671 rhabdomyosarcoma cells using two different schedules. We characterized its pharmacokinetic profile in nude mice bearing human SK-N-DZ and TE-671 cell lines.
Gimatecan appears to have high plasma disposition. The drug was present in plasma almost completely as the intact lactone form and showed substantial activity in all tumor models. Prolonged daily treatment with low doses of gimatecan produced significant tumor regression in all tumor xenografts.
The antitumor activity and the promising pharmacological profile indicate gimatecan as an excellent candidate for clinical treatment of pediatric tumors.
本研究比较了吉西他滨口服和伊立替康（CPT-11）在儿科肿瘤异种移植中的抗肿瘤活性和药理学特征。
吉西他滨在两种神经母细胞瘤细胞系（SK-N-DZ 和 SK-N-（BE）2c）和 TE-671 横纹肌肉瘤细胞上使用两种不同的方案进行了测试。我们在携带人 SK-N-DZ 和 TE-671 细胞系的裸鼠中对其药代动力学特征进行了表征。
吉西他滨似乎具有较高的血浆分布。该药物几乎完全以完整内酯形式存在于血浆中，并在所有肿瘤模型中均显示出显著的活性。延长的每日低剂量治疗可使所有肿瘤异种移植产生明显的肿瘤消退。
抗肿瘤活性和有前途的药理学特征表明吉西他滨是治疗儿科肿瘤的临床治疗的优秀候选药物。
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