Celsion Corporation, 997 Lenox Drive, Lawrenceville, PA, USA.
Duke University School of Medicine, Research Drive, Durham, NC, USA.
Adv Drug Deliv Rev. 2021 Nov;178:113985. doi: 10.1016/j.addr.2021.113985. Epub 2021 Sep 30.
We review the drug development of lyso-thermosensitive liposomal doxorubicin (LTLD) which is the first heat-activated formulation of a liposomal drug carrier to be utilized in human clinical trials. This class of compounds is designed to carry a payload of a cytotoxic agent and adequately circulate in order to accumulate at a tumor that is being heated. At the target the carrier is activated by heat and releases its contents at high concentrations. We summarize the preclinical and clinical experience of LTLD including its successes and challenges in the development process.
我们回顾了溶致热敏脂质体阿霉素（LTLD）的药物研发历程，它是第一种用于人体临床试验的热激活型脂质体药物载体。这类化合物旨在携带细胞毒性药物，并在适当的循环中充分积累到正在加热的肿瘤部位。在目标部位，载体通过热激活，并以高浓度释放其内容物。我们总结了 LTLD 的临床前和临床经验，包括其在开发过程中的成功和挑战。
