Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol

Clinical Pharmacokinetics

Volumn 44, Issue 10, 2005, Pages 1067-1081

  Swaisland, Helen C ^a   Ranson, Malcolm ^b   Smith, Robert P ^a   Leadbetter, Joanna ^a   Laight, Alison ^a   McKillop, David ^a   Wild, Martin J ^a  

^a ASTRAZENECA   (United Kingdom)

^b CHRISTIE HOSPITAL   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CLARITHROMYCIN; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; CYTOCHROME P450 INHIBITOR; FURAFYLLINE; GEFITINIB; ITRACONAZOLE; KETOCONAZOLE; LIVER PROTEIN; METOPROLOL; OMEPRAZOLE; QUINIDINE; RIFAMPICIN; SULFAPHENAZOLE;

ABNORMALLY HIGH SUBSTRATE CONCENTRATION IN BLOOD; ADULT; ADVANCED CANCER; AGED; ALANINE AMINOTRANSFERASE BLOOD LEVEL; AREA UNDER THE CURVE; ARTICLE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; CANCER CHEMOTHERAPY; CANCER PREVENTION; CARCINOID; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIARRHEA; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG EFFECT; DRUG EXPOSURE; DRUG METABOLISM; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; DRUG TOLERABILITY; DRY SKIN; ENZYME ACTIVITY; ENZYME SUBSTRATE; FEMALE; GEOMETRY; HEADACHE; HUMAN; INCUBATION TIME; INTESTINE TUMOR; ISOTOPE LABELING; LIVER METASTASIS; LIVER MICROSOME; LIVER TOXICITY; LYMPH NODE METASTASIS; MALE; NORMAL HUMAN; PHARYNGITIS; PHASE 1 CLINICAL TRIAL; PRIORITY JOURNAL; PROTEIN EXPRESSION; PRURITUS; QUANTITATIVE ANALYSIS; RANDOMIZED CONTROLLED TRIAL; RASH; SIDE EFFECT; SOLID TUMOR; STATISTICAL SIGNIFICANCE; TITRIMETRY; ULTRASOUND; UNIVERSITY HOSPITAL;

ADOLESCENT; ADULT; ANTINEOPLASTIC AGENTS; CROSS-OVER STUDIES; CYTOCHROME P-450 CYP2D6; CYTOCHROME P-450 ENZYME SYSTEM; DRUG COMBINATIONS; DRUG INTERACTIONS; ENZYME INDUCTION; ENZYME INHIBITORS; FEMALE; HUMANS; ITRACONAZOLE; MALE; METOPROLOL; MICROSOMES, LIVER; MIDDLE AGED; NEOPLASMS; QUINAZOLINES; RIFAMPIN;

EID: 25144436285     PISSN: 03125963     EISSN: 03125963     Source Type: Journal    
DOI: 10.2165/00003088-200544100-00005     Document Type: Article

References (23)

1. Traxler P. Tyrosine kinases as targets in cancer therapies: successes and failures. Expert Opin Ther Targets 2003; 7: 215-34
2. Mendelsohn J, Baselga J. The EGF receptor family as targets for cancer therapy. Oncogene 2000; 19: 6550-65
3. Wakeling AE, Barker AJ, Davies DH, et al. Specific inhibition of epidermal growth factor receptor tyrosine kinase by 4-anilinoquinazolines. Breast Cancer Res Treat 1996; 38: 67-73
4. Hammond LA. Pharmacokinetic evaluation of gefitinib when administered with chemotherapy. Clin Lung Cancer 2003; 5 Suppl. 1: S18-21
5. Bertz RJ, Granneman GR. Use of in vitro and in vivo data to estimate the likelihood of metabolic pharmacokinetic interactions. Clin Pharmacokinet 1997; 32: 210-58
6. Rodrigues AD. Use of in vitro human metabolism studies in drug development. Biochem Pharmacol 1994; 48: 2147-56
7. McKillop D, Wild MJ, Butters CJ, et al. Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica 1998; 28: 845-53
8. Jones HK, Stafford LE, Swaisland HC, et al. A sensitive assay for ZD1839 (Iressa) in human plasma by liquid-liquid extraction and high performance liquid chromatography with mass spectrometric detection: validation and use in phase I clinical trials. J Pharm Biomed Anal 2002; 29: 221-8
9. Swart KJ, Papgis M. Automated high-performance liquid chromatographic method for the determination of rifampicin in plasma. J Chromatog A 1992; 593: 21-4
10. Cooper KJ, Martin PD, Dane AL, et al. Effect of itraconazole on the pharmacokinetics of rosuvastatin. Clin Pharmacol Ther 2003; 73: 322-9
11. Rau T, Heide R, Bergmann K, et al. Effect of CYP2D6 genotype on metoprolol metabolism persists during long-term treatment. Pharmacogenetics 2002; 12: 465-72
12. Ranson M, Hammond LA, Ferry D, et al. ZD1839, a selective oral epidermal growth factor receptor-tyrosine kinase inhibitor, is well tolerated and active in patients with solid, malignant tumors: results of a phase I trial. J Clin Oncol 2002; 20: 2240-50
13. Ohnhaus EE, Breckenridge AM, Park BK. Urinary excretion of 6β-hydroxycortisol and the time course measurement of enzyme induction in man. Eur J Clin Pharmacol 1989; 36: 39-46
14. Park BK, Ohnhaus EE. Urinary 6β-hydroxycortisol: a simple, non-invasive index of enzyme induction in man. Das Artzliche Laboratorium 1983; 29: 53-8
15. Williamson KM, Patterson JH, McQueen RH, et al. Effects of erythromycin or rifampicin on losartan pharmacokinetics in healthy volunteers. Clin Pharmacol Ther 1998; 63: 316-23
16. Data on file, AstraZeneca, 2002
17. Venkatakrishnan K, von Moltke LL, Greenblatt DJ. Effects of the antifungal agents on oxidative drug metabolism: clinical relevance. Clin Pharmacokinet 2000; 38: 111-80
18. Haria M, Bryson HM, Goa KL. Itraconazole: a reappraisal of its pharmacological properties and therapeutic use in the management of superficial fungal infections. Drugs 1996; 51: 585-620
19. Varhe A, Olkkola KT, Neuvonen PJ. Oral triazolam is potentially hazardous to patients receiving systemic antimycotics ketoconazole or itraconazole. Clin Pharmacol Ther 1994; 56: 601-7
20. Kivisto KT, Lamberg TS, Kantola T, et al. Plasma buspirone concentrations are greatly increased by erythromycin and itraconazole. Clin Pharmacol Ther 1997; 62: 348-54
21. Kaukonen KM, Olkkola KT, Neuvonen PJ. Itraconazole increases plasma concentrations of quinidine. Clin Pharmacol Ther 1997; 62: 510-7
22. Backman JT, Kivisto KT, Olkkola KT, et al. The area under the plasma concentration-time curve for oral midazolam is 400-fold larger during treatment with itraconazole than with rifampicin. Eur J Clin Pharmacol 1998; 54: 53-8
23. Hardman JG, Limbird LE, Gilman AG, editors. Goodman and Gilman's the pharmacological basis of therapeutics. 10th ed. New York: McGraw-Hill, 2001: 255-6