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Drug interaction between erlotinib and phenytoin for brain metastases in a patient with nonsmall cell lung cancer.

Abstract
Erlotinib, a substrate drug metabolized by the CYP3A4 enzyme, is an epidermal growth factor receptor tyrosine kinase inhibitor used to treat nonsmall cell lung cancer (NSCLC). Concomitant use of erlotinib and the antiepileptic drug phenytoin, an inducer of CYP3A4, may result in a drug-drug interaction accompanied by changes in the blood concentrations of both drugs. We determined the blood concentration of each drug to confirm the interaction between phenytoin and erlotinib in a case of NSCLC with brain metastases. The phenytoin blood concentration (8.2-10.0μg/mL) gradually increased 3-fold (to 24.2μg/mL) 7 months after the start of erlotinib (150mg/d) co-administration. The erlotinib blood concentration which was maintained at 0.15-0.37μg/mL under phenytoin co-administration, increased 12-fold (to 1.77μg/mL) after the stoppage of phenytoin co-administration. The present case revealed that blood phenytoin increased and blood erlotinib decreased subsequent to the interaction of the 2 drugs in the CYP3A4 metabolic enzyme system.
AuthorsMasahiro Ohgami, Takayuki Kaburagi, Atsuhiko Kurosawa, Masato Homma
JournalLung cancer (Amsterdam, Netherlands) (Lung Cancer) Vol. 101 Pg. 9-10 (11 2016) ISSN: 1872-8332 [Electronic] Ireland
PMID27794414 (Publication Type: Case Reports, Journal Article)
CopyrightCopyright © 2016 Elsevier Ireland Ltd. All rights reserved.
Chemical References
  • Cytochrome P-450 CYP1A2 Inducers
  • Protein Kinase Inhibitors
  • Phenytoin
  • Erlotinib Hydrochloride
  • Cytochrome P-450 CYP3A
  • ErbB Receptors
Topics
  • Brain (pathology)
  • Brain Neoplasms (complications, drug therapy, secondary)
  • Carcinoma, Non-Small-Cell Lung (complications, drug therapy, pathology, surgery)
  • Cytochrome P-450 CYP1A2 Inducers (blood, therapeutic use)
  • Cytochrome P-450 CYP3A (metabolism)
  • Drug Interactions
  • ErbB Receptors (antagonists & inhibitors)
  • Erlotinib Hydrochloride (blood, therapeutic use)
  • Female
  • Humans
  • Lung Neoplasms (pathology)
  • Middle Aged
  • Phenytoin (adverse effects, blood, therapeutic use)
  • Protein Kinase Inhibitors (adverse effects, therapeutic use)
  • Seizures (drug therapy, etiology)
  • Treatment Outcome

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