Tejada-Berges T, Granai C O, Gordinier M, Gajewski W
Department of Obstetrics & Gynecology, Women and Infants' Hospital, Providence, RI 02905-2499, USA.
Expert Rev Anticancer Ther. 2002 Apr;2(2):143-50. doi: 10.1586/14737140.2.2.143.
Caelyx/Doxil is a novel pegylated liposomal formulation of the first-generation anthracycline, doxorubicin. The pharmacokinetics of this polyethylene-glycol-coated liposome are characterized by a reduced volume of distribution, a long intravascular circulating half-life and slow plasma clearance compared with free doxorubicin. This, coupled with a small vesicular size, uniquely promotes the localization of Caelyx/Doxil at tumor sites and explains its altered toxicity profile. The FDA and EMEA have approved its use for the treatment of AIDS-related Kaposi's sarcoma and, more recently, for recurrent epithelial ovarian cancer (EOC). Numerous investigations have focused on its use in the treatment of metastatic breast cancer, as well as recurrent squamous cell cervical carcinoma, soft tissue sarcoma, squamous head and neck cancers, prostate cancers and malignant gliomas. Ongoing clinical studies of combination regimens incorporating Caelyx/Doxil will further clarify its role in the treatment of advanced solid tumors.
凯素/多柔比星脂质体是第一代蒽环类药物多柔比星的一种新型聚乙二醇化脂质体制剂。与游离多柔比星相比，这种聚乙二醇包被脂质体的药代动力学特征为分布容积减小、血管内循环半衰期延长以及血浆清除缓慢。这一点，再加上小泡尺寸小，独特地促进了凯素/多柔比星脂质体在肿瘤部位的定位，并解释了其改变的毒性特征。美国食品药品监督管理局（FDA）和欧洲药品管理局（EMEA）已批准其用于治疗艾滋病相关的卡波西肉瘤，最近还批准用于复发性上皮性卵巢癌（EOC）。众多研究集中在其用于治疗转移性乳腺癌，以及复发性宫颈鳞状细胞癌、软组织肉瘤、头颈部鳞状癌、前列腺癌和恶性胶质瘤。正在进行的关于包含凯素/多柔比星脂质体的联合方案的临床研究将进一步阐明其在治疗晚期实体瘤中的作用。
