Stella V J, Charman W N, Naringrekar V H
Drugs. 1985 May;29(5):455-73. doi: 10.2165/00003495-198529050-00002.
Prodrugs are pharmacologically inactive chemical derivatives of a drug molecule that require a transformation within the body in order to release the active drug. They are designed to overcome pharmaceutical and/or pharmacokinetically based problems associated with the parent drug molecule that would otherwise limit the clinical usefulness of the drug. The scientific rationale, based on clinical, pharmaceutical and chemical experience, for the design of various currently used prodrugs is presented in this review. The examples presented are by no means comprehensive, but are representative of the different ways in which the prodrug approach has been used to enhance the clinical efficacy of various drug molecules.
前体药物是药物分子的药理惰性化学衍生物,需要在体内进行转化才能释放出活性药物。它们旨在克服与母体药物分子相关的基于药学和/或药代动力学的问题,否则这些问题会限制药物的临床应用。本文综述了基于临床、药学和化学经验设计各种当前使用的前体药物的科学原理。所举的例子绝非全面,但代表了前体药物方法用于提高各种药物分子临床疗效的不同方式。