Abstract | PURPOSE: METHODS: Including this patient, we administered 150 mg erlotinib daily to nine NSCLC patients with CNS metastases and measured the plasma and CSF concentrations just before administration on day 8. The concentrations were determined using high-performance liquid chromatography with ultraviolet detection. RESULTS: The plasma and CSF concentrations of erlotinib at a dose of 75 mg were 433 and 14 nM, respectively. The plasma and CSF concentrations of erlotinib at a dose of 150 mg were increased to 1,117 and 44 nM, respectively. The mean ± standard deviation of CSF concentrations and penetration rates were 106 ± 59 nM and 4.5 ± 1.5%, respectively. There was a good correlation (R(2) = 0.84) between plasma and CSF concentrations (P = 0.0005). CONCLUSIONS: This study indicates that CSF concentrations of erlotinib depend on its plasma concentration. As seen in this patient, high CSF concentrations of erlotinib can be achieved by high-dose administration, and this finding suggests the efficacy of high-dose administration, especially to refractory CNS metastases of NSCLC patients.
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Authors | Yosuke Togashi, Katsuhiro Masago, Masahide Fukudo, Yasuhiro Tsuchido, Chiyuki Okuda, Young Hak Kim, Yasuaki Ikemi, Yuichi Sakamori, Tadashi Mio, Toshiya Katsura, Michiaki Mishima |
Journal | Cancer chemotherapy and pharmacology
(Cancer Chemother Pharmacol)
Vol. 68
Issue 4
Pg. 1089-92
(Oct 2011)
ISSN: 1432-0843 [Electronic] Germany |
PMID | 21681573
(Publication Type: Case Reports, Journal Article)
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Chemical References |
- Protein Kinase Inhibitors
- Quinazolines
- Erlotinib Hydrochloride
- ErbB Receptors
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Topics |
- Aged
- Carcinoma, Non-Small-Cell Lung
(drug therapy, pathology)
- Central Nervous System Neoplasms
(drug therapy, secondary)
- Chromatography, High Pressure Liquid
- Dose-Response Relationship, Drug
- ErbB Receptors
(genetics)
- Erlotinib Hydrochloride
- Female
- Humans
- Lung Neoplasms
(drug therapy, pathology)
- Mutation
- Protein Kinase Inhibitors
(administration & dosage, pharmacokinetics, therapeutic use)
- Quinazolines
(administration & dosage, pharmacokinetics, therapeutic use)
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