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首页> 外文期刊>Journal of pharmaceutical sciences. >Pharmacokinetics of SN2310, an Injectable Emulsion That Incorporates a New Derivative of SN-38 in Patients with Advanced Solid Tumors
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Pharmacokinetics of SN2310, an Injectable Emulsion That Incorporates a New Derivative of SN-38 in Patients with Advanced Solid Tumors

机译：SN2310（一种新的SN-38衍生物）在晚期实体瘤患者中的注射乳剂的药代动力学

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摘要

SN2310 is an injectable emulsion composed of vitamin E, a succinate derivative, as well as 7-ethyl-10-hydroxycamptothecin (SN-38), the active metabolite of irinotecan. Single intravenous doses of 15, 20, 25, and 30mg/m~2 of SN2310 emulsion were administered in a total of 26 patients with advanced solid malignancies. Serial blood samples were collected and concentrations of SN2310, SN-38, and SN-38 glucuronide were assayed. Mean systemic clearance of SN2310 ranged between 1.91 and 2.02L/h/m~2. Peak concentrations of SN-38 were observed at the end of infusion, suggesting a fast metabolic conversion of SN2310 to its active form, SN-38. Mean t_(1/2) values of SN-38 across the 20-30 mg/m~2 dose levels (131-199 h) were 33-55-fold longer than those observed for SN2310. The systemic exposure of SN-38 increased in a proportional manner over the dose range studied. SN2310 emulsion displayed an improved safety profile as compared with irinotecan. The most significant safety risk was neutropenia. Considering the rapid formation of SN-38, the proportional increase in exposure levels, and its longer elimination half-life, less frequent dosing of SN2310 emulsion may be considered for the treatment of patients with advanced solid malignancies.
机译：SN2310是由维生素E（一种琥珀酸酯衍生物）和7-乙基-10-羟基喜树碱（SN-38）（伊立替康的活性代谢物）组成的可注射乳剂。 SN2310乳剂的单次静脉注射剂量分别为15、20、25和30mg / m〜2，共26例患有晚期实体恶性肿瘤的患者。收集一系列血液样品，并测定SN2310，SN-38和SN-38葡糖醛酸的浓度。 SN2310的平均全身清除率介于1.91和2.02L / h / m〜2之间。输注结束时观察到SN-38的峰值浓度，表明SN2310快速代谢转化为其活性形式SN-38。在20-30 mg / m〜2剂量水平（131-199小时）内，SN-38的平均t_（1/2）值比SN2310的平均t_（1/2）值长33-55倍。在研究的剂量范围内，SN-38的全身暴露呈比例增加。与伊立替康相比，SN2310乳液显示出更高的安全性。最重大的安全风险是中性粒细胞减少。考虑到SN-38的快速形成，暴露水平的成比例增加及其消除半衰期的延长，SN2310乳剂的低剂量给药可考虑用于晚期实体恶性肿瘤的治疗。

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