Effects of ketoconazole and carbamazepine on lapatinib pharmacokinetics in healthy subjects

British Journal of Clinical Pharmacology

Volumn 67, Issue 4, 2009, Pages 421-426

  Smith, Deborah A ^a   Koch, Kevin M ^a   Arya, Nikita ^a   Bowen, Carolyn J ^a   Herendeen, Jill M ^a   Beelen, Andrew ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

Carbamazepine; Drug interaction; Ketoconazole; Lapatinib; Pharmacokinetics

Indexed keywords

CARBAMAZEPINE; CYTOCHROME P450 3A4; KETOCONAZOLE; LAPATINIB; MULTIDRUG RESISTANCE PROTEIN 1;

ABDOMINAL PAIN; ADULT; ANTICONVULSANT ACTIVITY; ANTIFUNGAL ACTIVITY; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE TIME EFFECT RELATION; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG CROSS REACTIVITY; DRUG DOSE TITRATION; DRUG HALF LIFE; DRUG INHIBITION; DRUG METABOLISM; DRUG POTENTIATION; ENZYME ACTIVITY; FEMALE; HEADACHE; HUMAN; HUMAN EXPERIMENT; LOOSE FECES; MALE; NAUSEA; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; SOMNOLENCE;

ADOLESCENT; ADULT; ANALGESICS, NON-NARCOTIC; ANTIFUNGAL AGENTS; ANTINEOPLASTIC AGENTS; AREA UNDER CURVE; CARBAMAZEPINE; CROSS-OVER STUDIES; DRUG INTERACTIONS; FEMALE; HALF-LIFE; HUMANS; KETOCONAZOLE; MALE; MIDDLE AGED; PROTEIN KINASE INHIBITORS; QUINAZOLINES; TREATMENT OUTCOME; YOUNG ADULT;

EID: 63849243041     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2009.03370.x     Document Type: Article

References (14)

1. Bence AK, Anderson EB, Halepota MA, Doukas MA, DeSimone PA, Davis GA, Smith DA, Koch KM, Stead AG, Mangum S, Bowen CJ, Spector NL, Hsieh S, Adams VR. Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW572016, a dual EGFR-erbb2 inhibitor, in healthy subjects. Invest New Drugs 2005 23 : 39 49.
2. Reddy N, Cohen R, Whitehead B, Koch KM, Stead A, Beelen AP, Lewis LD. A phase I, open-label, three-period, randomized crossover study to evaluate the effect of food on the pharmacokinetics of lapatinib in cancer patients. Clin Pharmacol Ther 2007 81 : S16 7.
3. Polli JW, Humphreys JE, Harmon KA, Castellino S, O'Mara MJ, Olson KL, St John-Williams L, Koch KM, Serabjit-Singh CJ. The role of efflux and uptake transporters in N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2- (methylsulfonyl) ethyl]amino}methyl)-2-furyl]-4-quinazolinamine) (GW572016, Lapatinib) disposition and drug interactions. Drug Metab Dispos 2008 36 : 1 7.
4. Hsieh S, Tobien T, Koch K, Dunn J. Increasing throughput of parallel on-line extraction liquid chromatography/ electrospray ionization tandem mass spectrometry system for GLP quantitative bioanalysis in drug development. Rapid Commun Mass Spectrom 2004 18 : 285 92.
5. Gibbs MA, Thummel KE, Shen DD, Kunze KL. Inhibition of cytochrome P-450 3A (CYP3A) in human intestinal and liver microsomes: comparison of Ki values and impact of CYP3A5 expression. Drug Metab Dispos 1999 27 : 180 7.
6. Lapple F, von Richter O, Fromm MF, Richter T, Thon KP, Wisser H, Griese EU, Eichelbaum M, Kivisto KT. Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics 2003 13 : 565 75.
7. Schuetz EG, Schuetz JD, Strom SC, Thompson MT, Fisher RA, Molowa DT, Li D, Guzelian PS. Regulation of human liver cytochromes P-450 in family 3A in primary and continuous culture of human hepatocytes. Hepatology 1993 18 : 1254 62.
8. Magnusson MO, Dahl M-L, Cederberg J, Karlsson MO, Sandstrom R. Pharmacodynamics of carbamazepine-mediated induction of CYP3A4, CYP1A2, and Pgp as assessed by probe substrates midazolam, caffeine, and digoxin. Clin Pharmacol Ther 2007 84 : 52 62.
9. Fagiolino P, Vazquez M, Olano I, Delfino A. Systemic and presystemic conversion of carbamazepine to carbamazepine-10,11-epoxide during long term treatment. J Epilepsy Clin Neurophysiol 2006 12 : 13 6.
10. Lucas RA, Gilfillan DJ, Bergstrom RF. A pharmacokinetic interaction between carbamazepine and olanzapine: observations on possible mechanism. Eur J Clin Pharmacol 1998 54 : 639 43.
11. Han P, Brichant JF, Pieron F, Pieyns P, Born JD, Lamy M. Elevated plasma alpha 1-acid glycoprotein levels: lack of connection to resistance to vecuronium blockade induced by anticonvulsant therapy. J Neurosurg Anesthesiol 1997 9 : 3 7.
12. Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR. Interrelationship between substrates and inhibitors of human CYP3A4 and P-glycoprotein. Pharm Res 1999 16 : 408 14.
13. Rautio J, Humphreys JE, Webster LO, Balakrishnan A, Keogh JP, Kunta JR, Serabjit-Singh CJ, Polli JW. In vitro p-glycoprotein inhibition assays for assessment of clinical drug interaction potential of new drug candidates: a recommendation for probe substrates. Drug Metab Dispos 2006 34 : 786 92.
14. Giessmann T, May K, Modess C, Wegner D, Hecker U, Zschiesche M, Dazert P, Grube M, Schroeder E, Warzok R, Cascorbi I, Kroemer HK, Siegmund W. Carbamazepine regulates intestinal P-glycoprotein and multidrug resistance protein MRP2 and influences disposition of tolamolol in humans. Clin Pharmacol Ther 2004 76 : 192 200.