Department of Chemistry, University at Albany, 1400 Washington Ave., Albany, NY 12222, USA.
Genes (Basel). 2022 Mar 5;13(3):466. doi: 10.3390/genes13030466.
Gemcitabine is a nucleoside analog that has been used widely as an anticancer drug for the treatment of a variety of conditions, including ovarian, bladder, non-small-cell lung, pancreatic, and breast cancer. However, enzymatic deamination, fast systemic clearance, and the emergence of chemoresistance have limited its efficacy. Different prodrug strategies have been explored in recent years, seeking to obtain better pharmacokinetic properties, efficacy, and safety. Different drug delivery strategies have also been employed, seeking to transform gemcitabine into a targeted medicine. This review will provide an overview of the recent developments in gemcitabine prodrugs and their effectiveness in treating cancerous tumors.
吉西他滨是一种核苷类似物，已被广泛用作抗癌药物，用于治疗多种疾病，包括卵巢癌、膀胱癌、非小细胞肺癌、胰腺癌和乳腺癌。然而，酶脱氨作用、快速全身清除和化疗耐药性的出现限制了其疗效。近年来，人们探索了不同的前药策略，旨在获得更好的药代动力学特性、疗效和安全性。还采用了不同的药物传递策略，试图将吉西他滨转化为靶向药物。本综述将概述吉西他滨前药的最新进展及其在治疗癌性肿瘤方面的效果。
