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Clinical Pharmacokinetics of Docetaxel

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Abstract

Docetaxel belongs to the class of taxane antineoplastic agents that act by inducing microtubular stability and disrupting the dynamics of the microtubular network. The drug has shown a broad spectrum of antitumour activity in preclinical models as well as clinically, with responses observed in various disease types, including advanced breast cancer and non-small cell lung cancer. The pharmacokinetics and metabolism of docetaxel are extremely complex and have been the subject of intensive investigation in recent years. Docetaxel is subject to extensive metabolic conversion by the cytochrome P450 (CYP) 3A isoenzymes, which results in several pharmacologically inactive oxidation products. Elimination routes of docetaxel are also dependent on the presence of drug-transporting proteins, notably P-glycoprotein, present on the bile canalicular membrane. The various processes mediating drug elimination, either through metabolic breakdown or excretion, impact substantially on interindividual variability in drug handling. Strategies to individualise docetaxel administration schedules based on phenotypic or genotype-dependent differences in CYP3A expression are underway and may ultimately lead to more selective chemotherapeutic use of this agent.

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  1. The use of trade names is for product identification purposes only and does not imply endorsement.

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Acknowledgements

Dr Baker receives research funding from Sanofi Aventis and the terms of this arrangement are being managed by the Johns Hopkins University in accordance with its conflict of interest policies. All other authors do not have any conflicts of interest directly relevant to the contents of this manuscript.

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Authors and Affiliations

  1. The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Bunting-Blaustein Cancer Research Building, 1650 Orleans Street, Room 1M87, Baltimore, Maryland, 21231-1000, USA

    Sharyn D. Baker

  2. National Cancer Institute, Bethesda, Maryland, USA

    Alex Sparreboom

  3. Erasmus University Medical Center, Rotterdam, The Netherlands

    Jaap Verweij

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  1. Sharyn D. Baker
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  2. Alex Sparreboom
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  3. Jaap Verweij
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Correspondence to Sharyn D. Baker.

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Baker, S.D., Sparreboom, A. & Verweij, J. Clinical Pharmacokinetics of Docetaxel. Clin Pharmacokinet 45, 235–252 (2006). https://doi.org/10.2165/00003088-200645030-00002

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