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Review
. 2018 Oct 5;549(1-2):133-149.
doi: 10.1016/j.ijpharm.2018.07.046. Epub 2018 Jul 21.

Drug metabolites and their effects on the development of adverse reactions: Revisiting Lipinski's Rule of Five

Caroline Manto Chagas  1 , Sara Moss  1 , Laleh Alisaraie  2
Affiliations
Review

Drug metabolites and their effects on the development of adverse reactions: Revisiting Lipinski's Rule of Five

Caroline Manto Chagas et al. Int J Pharm. .

Abstract

Many studies have shown that toxicities of anticancer drugs and their adverse effects are related to their chemical structure and high molecular weight that may result in a number of metabolites interacting with drug off-target networks. These factors require further attention for advancing cancer treatment and decreasing toxicities caused by the molecular complexity of antineoplastic agents. Providing more target-selective and tolerable cancer therapy with fewer side effects would not only improve patients' compliance, but also would decrease cancer-remission rates. This review presents several antineoplastic agents and their metabolites with molecular weights greater than 500 g/mol, which reportedly cause more than fifteen types of adverse reactions during breast cancer therapy.

Keywords: ADME; Adverse drug reactions; Anticancer drug; Metabolites; Toxicity.

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