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Clinical Pharmacokinetics of Tyrosine Kinase Inhibitors
Pyrimidine (imatinib, dasatinib, nilotinib and pazopanib), pyridine (sorafenib) and pyrrole (sunitinib) tyrosine kinase inhibitors (TKIs) are multi-targeted TKIs with high activity towards severalExpand
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Toxicokinetics of Acrylamide in Humans after Ingestion of a Defined Dose in a Test Meal to Improve Risk Assessment for Acrylamide Carcinogenicity
High amounts of acrylamide in some foods result in an estimated daily mean intake of 50 μg for a western style diet. Animal studies have shown the carcinogenicity of acrylamide upon oral exposure.Expand
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Assessment of CYP1A2 activity in clinical practice: why, how, and when?
The cytochrome P450 enzyme CYP1A2 mediates the rate-limiting step in the metabolism of many drugs including theophylline, clozapine, and tacrine as well as in the bioactivation of procarcinogens.Expand
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Estimation of cytochrome P-450 CYP1A2 activity in 863 healthy Caucasians using a saliva-based caffeine test.
A pronounced variability limits the usefulness of CYP1A2 phenotyping for drug therapy, for evaluating liver function, and for assessing the role of this enzyme in carcinogenesis. To identify andExpand
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Inhibitory effects of silibinin on cytochrome P-450 enzymes in human liver microsomes.
Silibinin, the main constituent of silymarin, a flavonoid drug from silybum marianum used in liver disease, was tested for inhibition of human cytochrome P-450 enzymes. Metabolic activities wereExpand
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Clinical Pharmacokinetics of Tyrosine Kinase Inhibitors
The 4-anilinoquinazolines (gefitinib, erlotinib and lapatinib) are members of a class of potent and selective inhibitors of the human epidermal growth factor receptor (HER) family of tyrosine kinasesExpand
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Induction of Drug Metabolising Enzymes
  • U. Fuhr
  • Chemistry, Medicine
  • Clinical pharmacokinetics
  • 1 June 2000
Currently, 5 different main mechanisms of induction are distinguished for drug-metabolising enzymes. The ethanol type of induction is mediated by ligand stabilisation of the enzyme, but the othersExpand
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Evaluation of probe drugs and pharmacokinetic metrics for CYP2D6 phenotyping
IntroductionCytochrome P450 2D6 (CYP2D6) is one of the most important enzymes catalyzing biotransformation of xenobiotics in the human liver. This enzyme’s activity shows a high degree ofExpand
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Pharmacokinetics and pharmacodynamics of rosiglitazone in relation to CYP2C8 genotype
Rosiglitazone is metabolically inactivated predominantly via the cytochrome P450 (CYP) enzyme CYP2C8. The functional impact of the CYP2C8*3 allele coding for the Arg139Lys and Lys399Arg amino acidExpand
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Appropriate Phenotyping Procedures for Drug Metabolizing Enzymes and Transporters in Humans and Their Simultaneous Use in the “Cocktail” Approach
Phenotyping for drug metabolizing enzymes and transporters is used to assess quantitatively the effect of an intervention (e.g., drug therapy, diet) or a condition (e.g., genetic polymorphism,Expand
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