title: Comparison of the pharmacokinetics of erlotinib administered in complete fasting and 2 h after a meal in patients with lung cancer.
abstract: BACKGROUND
  The recommended dose of erlotinib is 150 mg daily either 1 h before a meal (complete fasting) or 2 h after a meal (2 h post-meal), because of the food effect.
  
  
  METHODS
  We conducted a cross-over pharmacokinetic study to compare the fed bioequivalence in the two conditions.
  
  
  RESULTS
  Twenty-three patients with non-small cell lung cancer were included in the analysis. AUC0-24 and C max in the 2-h post-meal status were significantly higher than in the complete fasting status (GMR = 1.33, P < 0.001; GMR = 1.44, P < 0.001, respectively). However, because the concentration of erlotinib did not reach the steady state within 7 days in the complete fasting state, we conducted analyses only on day 14, which showed no significant difference in AUC0-24 or C max between the two conditions. The more rapid increase in AUC0-24 and C min did not produce any earlier and more severe toxic events.
  
  
  CONCLUSIONS
  The AUC0-24 increased significantly faster (48-53 % greater) in the 2-h post-meal status than in complete fasting status, which suggested that the two gastric emptying states might differ in their absorption. However, there was no clinically significant difference in bioavailability or toxicity between the two clinically used fed conditions at least in 14 days.
authors.affiliation: Department of Thoracic Oncology, National Cancer Center Hospital, Tsukiji 5-1-1, Chuo-ku, Tokyo, 104-0045, Japan, katsuya-tky@umin.ac.jp.
authors.forename: Yuki
authors.initials: Y
authors.lastname: Katsuya
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Fujiwara
authors.forename: Kuniko
authors.initials: K
authors.lastname: Sunami
authors.forename: Hirofumi
authors.initials: H
authors.lastname: Utsumi
authors.forename: Yasushi
authors.initials: Y
authors.lastname: Goto
authors.forename: Shintaro
authors.initials: S
authors.lastname: Kanda
authors.forename: Hidehito
authors.initials: H
authors.lastname: Horinouchi
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Nokihara
authors.forename: Noboru
authors.initials: N
authors.lastname: Yamamoto
authors.forename: Yuki
authors.initials: Y
authors.lastname: Takashima
authors.forename: Satoko
authors.initials: S
authors.lastname: Osawa
authors.forename: Yuichiro
authors.initials: Y
authors.lastname: Ohe
authors.forename: Tomohide
authors.initials: T
authors.lastname: Tamura
authors.forename: Akinobu
authors.initials: A
authors.lastname: Hamada
mesh_terms: D000328:Adult; D000368:Aged; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy / Q000378:metabolism*; D015331:Cohort Studies; D018592:Cross-Over Studies; D000069347:Erlotinib Hydrochloride; D005215:Fasting / Q000378:metabolism; D005260:Female; D018565:Food-Drug Interactions; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D019518:Postprandial Period; D047428:Protein Kinase Inhibitors / Q000493:pharmacokinetics*; D011799:Quinazolines / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D000069347:Erlotinib Hydrochloride