Abstract | BACKGROUND: METHOD: We administered 150 mg erlotinib daily to four patients with NSCLC who had CNS metastases, and we investigated plasma pharmacokinetics of erlotinib and OSI-420 on days 1 and 8. In addition, we measured the concentrations of erlotinib and OSI-420 in CSF just before administration of erlotinib on day 8. RESULTS: In all cases except for one case, plasma pharmacokinetics data on day 8 were similar to those previously reported. The mean +/- SD CSF concentrations of erlotinib and OSI-420 were 54 +/- 30 ng/ml and 10.8 +/- 8.2 ng/ml, respectively. The mean +/- SD CSF penetration rates of erlotinib and OSI-420 were 5.1% +/- 1.9% and 5.8% +/- 3.6%, respectively. CSF concentrations of erlotinib exceeded median inhibitory concentration (IC50) of erlotinib in intact tumor cells with wild-type epidermal growth factor receptor gene. CONCLUSION: The CSF penetrations of erlotinib and OSI-420 in patients with NSCLC who had CNS metastases were approximately 5.1% and 5.8%, respectively. This indicates that erlotinib can become a treatment option for CNS metastases of NSCLC.
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Authors | Yosuke Togashi, Katsuhiro Masago, Masahide Fukudo, Tomohiro Terada, Shiro Fujita, Kaoru Irisa, Yuichi Sakamori, Young Hak Kim, Tadashi Mio, Ken-ichi Inui, Michiaki Mishima |
Journal | Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer
(J Thorac Oncol)
Vol. 5
Issue 7
Pg. 950-5
(Jul 2010)
ISSN: 1556-1380 [Electronic] United States |
PMID | 20479691
(Publication Type: Case Reports, Journal Article)
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Chemical References |
- OSI-420
- Protein Kinase Inhibitors
- Quinazolines
- Erlotinib Hydrochloride
- ErbB Receptors
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Topics |
- Adenocarcinoma
(cerebrospinal fluid, drug therapy, pathology)
- Aged
- Aged, 80 and over
- Carcinoma, Non-Small-Cell Lung
(cerebrospinal fluid, drug therapy, pathology)
- Central Nervous System Neoplasms
(cerebrospinal fluid, drug therapy, secondary)
- ErbB Receptors
(antagonists & inhibitors, genetics)
- Erlotinib Hydrochloride
- Female
- Humans
- Lung Neoplasms
(cerebrospinal fluid, drug therapy, pathology)
- Middle Aged
- Mutation
(genetics)
- Protein Kinase Inhibitors
(cerebrospinal fluid, pharmacokinetics, pharmacology)
- Quinazolines
(cerebrospinal fluid, pharmacokinetics, pharmacology)
- Survival Rate
- Tissue Distribution
- Treatment Outcome
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