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Sphingomyelin/cholesterol liposomal vincristine: a new formulation for an old drug.

机译:鞘磷脂/胆固醇脂质体长春新碱:一种用于旧药物的新制剂。

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Sphingomyelin/cholesterol liposomal vincristine (SV) is a novel formulation of vincristine encapsulated in the aqueous interior of liposomes composed of sphingomyelin and cholesterol. Benefits of the liposomal formulation include prolongation of the circulation half-life of total vincristine and an increase in drug delivery to sites of tumour growth resulting in enhanced efficacy. In addition, higher doses of vincristine than ordinarily administered can be prescribed without significant toxicity. Phase II studies have demonstrated that SV is active and well tolerated in relapsed diffuse large B cell lymphoma (DLBCL), including patients who have relapsed following an autologous stem cell transplant. SV has been successfully substituted for free vincristine in the CHOP regimen for those with previously untreated aggressive B cell non-Hodgkin's lymphoma, and is undergoing study in other settings. The achievement of responses in heavily pretreated patients with DLBCL and its low toxicity profile make SV a potential therapy for the palliative treatment of patients with multiply relapsed DLBCL. Ultimately, it is likely to be incorporated into combination chemotherapy regimens for use in untreated or relapsed patients. Its true value both as a single agent in heavily pretreated patients and in combination regimens will need to be established in Phase III trials.
机译:鞘磷脂/胆固醇脂质体长春新碱(SV)是长春新碱的新型制剂,其包裹在由鞘磷脂和胆固醇组成的脂质体的水性内部中。脂质体制剂的益处包括延长了长春新碱的循环半衰期,并增加了向肿瘤生长部位的药物输送,从而提高了疗效。另外,可以开出比常规给药更高剂量的长春新碱,而没有明显的毒性。 II期研究表明,SV在复发性弥漫性大B细胞淋巴瘤(DLBCL)中(包括在自体干细胞移植后复发的患者中)是活跃的且具有良好的耐受性。在先前未经治疗的侵袭性B细胞非霍奇金淋巴瘤的患者中,SV已被CHOP方案成功取代游离长春新碱,并且正在其他环境中进行研究。在高度预处理的DLBCL患者中,其反应的实现及其低毒性使SV成为多发性DLBCL患者姑息治疗的潜在疗法。最终,有可能将其纳入联合化疗方案中,以用于未治疗或复发的患者。在III期临床试验中,必须确定其在经过大量预处理的患者中作为单一药物以及在联合治疗中的真实价值。

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