Tumor Biology Center, Breisacher Strasse 117, D-79106 Freiburg, Germany.
J Control Release. 2014 Sep 28;190:331-6. doi: 10.1016/j.jconrel.2014.03.013. Epub 2014 Mar 15.
Human serum albumin (HSA) has emerged as a versatile carrier for therapeutic agents, primarily for treating diabetes and cancer, improving the pharmacokinetic profile of the drug or delivering the drug to the pathogenic site addressing diseases with unmet medical needs. Market approved products include fatty acid derivatives of human insulin or the glucagon-like-1 peptide (Levemir, Tresiba, and Victoza) which bind physically to the respective binding sites of HSA thus extending their half-life. For cancer treatment, the paclitaxel albumin nanoparticle Abraxane has been approved for treating metastatic breast cancer, non-small cell lung cancer, and advanced pancreatic cancer. Finally, the albumin-binding prodrug of doxorubicin, Aldoxorubicin, which binds covalently to the cysteine-34 position of circulating albumin, is in advanced clinical trials with a registration phase 3 trial for soft tissue sarcoma initiated in Q1 2014.
人血清白蛋白（HSA）已成为治疗剂的多功能载体，主要用于治疗糖尿病和癌症，改善药物的药代动力学特征或将药物递送至治疗具有未满足医疗需求的疾病的致病部位。市场批准的产品包括人胰岛素或胰高血糖素样肽（Levemir、Tresiba 和 Victoza）的脂肪酸衍生物，它们与 HSA 的相应结合位点物理结合，从而延长其半衰期。对于癌症治疗，紫杉醇白蛋白纳米颗粒 Abraxane 已被批准用于治疗转移性乳腺癌、非小细胞肺癌和晚期胰腺癌。最后，阿霉素的白蛋白结合前药 Aldoxorubicin，与循环白蛋白的半胱氨酸-34 位置共价结合，正在进行晚期临床试验，软组织肉瘤的注册阶段 3 试验于 2014 年第一季度启动。
