Li A P.
In Vitro Technologies, 1450 S. Rolling Rd, 21227, Baltimore, MD, USA
Drug Discov Today. 2001 Apr 1;6(7):357-366. doi: 10.1016/s1359-6446(01)01712-3.
There is no doubt that ADME/Tox drug properties, absorption, distribution, metabolism, elimination and toxicity, are properties crucial to the final clinical success of a drug candidate. It has been estimated that nearly 50% of drugs fail because of unacceptable efficacy, which includes poor bioavailability as a result of ineffective intestinal absorption and undesirable metabolic stability(1). It has also been estimated that up to 40% of drug candidates have failed in the past because of safety issues(2). In this review, the methodologies that are available for use in drug development as in vitro human-based screens for ADME/Tox drug properties are discussed.
毫无疑问,药物的ADME/Tox性质,即吸收、分布、代谢、排泄和毒性,是候选药物最终临床成功的关键性质。据估计,近50%的药物因疗效不佳而失败,这包括肠道吸收无效导致的生物利用度差以及不理想的代谢稳定性(1)。据估计,过去高达40%的候选药物因安全问题而失败(2)。在本综述中,将讨论可用于药物开发的、作为基于体外人体的ADME/Tox药物性质筛选方法。