Clinical Pharmacokinetics

, Volume 43, Issue 15, pp 1127–1156 | Cite as

Effects of Food on the Clinical Pharmacokinetics of Anticancer Agents

Underlying Mechanisms and Implications for Oral Chemotherapy
  • Brahma N. SinghEmail author
  • Bimal K. Malhotra
Review Article


Pharmacokinetic interactions between food and orally administered drugs involve changes mainly in the absorption and metabolism of a drug, and may have clinical implications. Such interactions, in particular, may be of major clinical significance for cancer chemotherapy since the majority of anticancer agents are toxic, have a low therapeutic index and are administered long term, most often in combination with other cytotoxic agents. The purpose of this review is to compare the pharmacokinetic profiles of various anticancer drugs, including chemopreventive agents that have been examined previously in fasted and fed conditions, and to discuss the underlying basis/mechanisms of food effect in light of a drug’s physicochemical and pharmacokinetic properties. Clinical pharmacokinetic parameters such as maximum concentration, area under the concentration-time curve, time to maximum concentration and half-life for each drug are compared in fasted and fed states, and specific dietary recommendations are summarised accordingly. In addition, the effects of food on the metabolite kinetics and pharmacodynamic responses, and the potential role of food effect in the modulation of oral biovariability and multidrug resistance have been extensively discussed. Overall, this comprehensive pharmacokinetic analysis indicates that a broad spectrum of food effects is seen among anticancer agents because of diverse factors regulating each drug’s oral bioavailability and its interactions with food. The consideration of such effects is important, as it could lead to more rational pharmacological monitoring and possibly improve the oral chemotherapy of cancer in children, adults and the elderly.


Oral Bioavailability Vinorelbine Finasteride Tamsulosin Grapefruit Juice 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



This work was presented in part at the Annual Scientific Meeting of the International Society of Preventive Oncology, 28–31 October 2000, Geneva, Switzerland. Brahma Singh gratefully acknowledges the financial support of the College of Pharmacy, St John’s University, Jamaica, New York, USA, in the form of a doctoral fellowship.

The authors have no current or potential conflicts of interest that are directly relevant to the contents of this manuscript.


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Copyright information

© Adis Data Information BV 2004

Authors and Affiliations

  1. 1.Department of Pharmacy and Administrative Sciences, College of Pharmacy and Allied Health ProfessionsSt John’s UniversityJamaicaUSA
  2. 2.Department of Clinical SciencesPfizer Inc.New YorkUSA

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