Abstract
Aims:
We analyzed the association of ABCB1 polymorphisms with erlotinib-induced toxicity and the pharmacokinetics in patients with non-small-cell lung cancer.
Materials & methods:
After erlotinib 150 mg was administered to 50 patients, ABCB1 polymorphisms were analyzed via either TaqMan(®) assays or direct nucleotide sequencing. Plasma concentrations were measured by HPLC.
Results:
The trough concentration at steady state in patients with the ABCB1 1236TT-2677TT-3435TT genotype was higher compared with others groups (p = 0.021) and patients carrying this genotype had a higher risk of developing higher grade 2 toxicity (p = 0.012).
Conclusion:
The present study suggested that the ABCB1 1236TT-2677TT-3435TT genotype was associated with higher plasma concentration and the risk of developing higher toxicity in patients treated with erlotinib.
Publication types
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Clinical Trial
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics*
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Administration, Oral
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Aged
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Aged, 80 and over
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Carcinoma, Non-Small-Cell Lung / drug therapy*
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Carcinoma, Non-Small-Cell Lung / genetics
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ErbB Receptors / antagonists & inhibitors
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Erlotinib Hydrochloride
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Female
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Humans
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Japan
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Lung Neoplasms / drug therapy*
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Lung Neoplasms / genetics
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Male
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Middle Aged
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Neoplasm Staging
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Polymorphism, Single Nucleotide*
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Prospective Studies
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Protein Kinase Inhibitors* / adverse effects
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Protein Kinase Inhibitors* / pharmacokinetics
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Protein Kinase Inhibitors* / therapeutic use
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Quinazolines* / adverse effects
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Quinazolines* / pharmacokinetics
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Quinazolines* / therapeutic use
Substances
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ABCB1 protein, human
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ATP Binding Cassette Transporter, Subfamily B
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Protein Kinase Inhibitors
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Quinazolines
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Erlotinib Hydrochloride
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ErbB Receptors