Cerebrospinal fluid concentration of gefitinib and erlotinib in patients with non-small cell lung cancer.

DOI 機関リポジトリ (HANDLE) HANDLE PDF Web Site ほか2件をすべて表示 一部だけ表示 被引用文献19件 参考文献36件 オープンアクセス

書誌事項

公開日
2012-09
資源種別
journal article
権利情報
  • The final publication is available at www.springerlink.com
  • This is not the published version. Please cite only the published version.
  • この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。
DOI
  • 10.1007/s00280-012-1929-4
公開者
Springer-Verlag

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説明

[Purpose]: Several cases have been reported in which central nervous system (CNS) metastases of non-small cell lung cancer (NSCLC) resistant to gefitinib were improved by erlotinib. However, there has been no study in which cerebrospinal fluid (CSF) concentrations of gefitinib and erlotinib are directly compared. Thus, we aimed to compare them. [Methods]: We examined 15 Japanese patients with NSCLC and CNS metastases with epidermal growth factor receptor gene mutations who received CSF examinations during epidermal growth factor receptor-tyrosine kinase inhibitors treatment (250 mg daily gefitinib or 150 mg daily erlotinib). Plasma and CSF concentrations were determined using high-performance liquid chromatography with tandem mass spectrometry. [Results]: The concentration and penetration rate of gefitinib (mean ± standard deviation) in the CSF were 3.7 ± 1.9 ng/mL (8.2 ± 4.3 nM) and 1.13 ± 0.36 %, respectively. The concentration and penetration rate of erlotinib in the CSF were 28.7 ± 16.8 ng/mL (66.9 ± 39.0 nM) and 2.77 ± 0.45 %, respectively. The CSF concentration and penetration rate of erlotinib were significantly higher than those of gefitinib (P = 0.0008 and <0.0001, respectively). The CNS response rates of patients with erlotinib treatment were preferentially (but not significantly) higher than those with gefitinib treatment. (1/3 vs. 4/7, respectively). Leptomeningeal metastases in one patient, which were refractory to gefitinib, dramatically responded to erlotinib. [Conclusions]: This study suggested that higher CSF concentration could be achieved with erlotinib and that erlotinib could be more effective for the treatment for CNS metastases, especially leptomeningeal metastases, than gefitinib.

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