Tu Yuxuan, Gong Jianbao, Mou Jing, Jiang Hongfei, Zhao Haibo, Gao Jiake
The Afffliated Hospital of Qingdao University, Qingdao University, Qingdao, China.
Qingdao Hospital, University of Health and Rehabilitation Sciences, Qingdao Municipal Hospital, Qingdao, China.
Front Pharmacol. 2024 Jul 31;15:1434137. doi: 10.3389/fphar.2024.1434137. eCollection 2024.
Approved anticancer drugs typically face challenges due to their narrow therapeutic window, primarily because of high systemic toxicity and limited selectivity for tumors. Prodrugs are initially inactive drug molecules designed to undergo specific chemical modifications. These modifications render the drugs inactive until they encounter specific conditions or biomarkers , at which point they are converted into active drug molecules. This thoughtful design significantly improves the efficacy of anticancer drug delivery by enhancing tumor specificity and minimizing off-target effects. Recent advancements in prodrug design have focused on integrating these strategies with delivery systems like liposomes, micelles, and polymerosomes to further improve targeting and reduce side effects. This review outlines strategies for designing stimuli-responsive small molecule prodrugs focused on cancer treatment, emphasizing their chemical structures and the mechanisms controlling drug release. By providing a comprehensive overview, we aim to highlight the potential of these innovative approaches to revolutionize cancer therapy.
获批的抗癌药物通常因其治疗窗口狭窄而面临挑战，主要原因是全身毒性高且对肿瘤的选择性有限。前药最初是无活性的药物分子，旨在进行特定的化学修饰。这些修饰使药物在遇到特定条件或生物标志物之前保持无活性，此时它们会转化为活性药物分子。这种精心设计通过提高肿瘤特异性和最小化脱靶效应，显著提高了抗癌药物递送的疗效。前药设计的最新进展集中在将这些策略与脂质体、胶束和聚合物囊泡等递送系统相结合，以进一步改善靶向性并减少副作用。本综述概述了用于癌症治疗的刺激响应性小分子前药的设计策略，强调了它们的化学结构和控制药物释放的机制。通过提供全面的概述，我们旨在突出这些创新方法在彻底改变癌症治疗方面的潜力。
