Drug Metabolism in Drug Design and Development Basic Concepts and Practice

Renwick et al., 2000); (10) Interindividual variability of enzymes in human; (11) potential complication due to renal or hepatic ...

Bjornsson TD, Callaghan JT, Einolf HJ, Fischer V, Gan L, Grimm S, Kao J, King SP, Miwa G, Ni L, Kumar G, McLeod J, Obach RS, Rob ...

Draper AJ, Madan A, Smith K, Parkinson A. Development of a non-high pressure liquid chromatography assay to determine testostero ...

Honig PK, Wortham DC, Hull R, Zamani K, Smith JE, Cantilena LR. Itraconazole affects single-dose terfenadine pharmacokinetics an ...

Kenworthy KE, Bloomer JC, Clarke SE, Houston JB. CYP3A4 drug interactions: correlation of 10in vitroprobe substrates. Br J Clin ...

Renwick AB, Watts PS, Edwards RJ, Barton PT, Guyonnet I, Price RJ, Tredger JM, Pelkonen O, Boobis AR, Lake BG. Differential main ...

Yao C, Levy RH. Inhibition-based metabolic drug–drug interactions: predictions from in vitrodata. J Pharm Sci 2002;91:1923–1935. ...

17 Testing Drug Candidates for CYP3A4 Induction GANGLUO,LIANG-SHANGGAN,ANDTHOMASM. GUENTHNER 17.1 INTRODUCTION The primary objec ...

type of drug–drug interaction is the increased incidence of failure of oral contraceptives occurring in women who were concurren ...

isoform that plays an important role in the metabolism of drugs and xenobiotics in humans. In addition to the noninducible isofo ...

human subjects, and induction can be assessed by measuring the metabolism or clearance of model substrates for the drug metaboli ...

only be useful if the signaling mechanisms responsible for inducing the specific drug metabolizing enzymes targeted by the scree ...

It is evident, therefore, that while animal studies may offer valuable information regarding the potential of compounds for indu ...

oral route of administration is preferred for preclinical studies, either by gavage or as an admixture in the animal diet, to pr ...

0.125 M sucrose), and can be stored at  80 oC if they cannot be used immediately. The total protein concentration is determined ...

proximity assay)-based binding assay is prone to false positive results, while the PXR reporter gene assay only represents the P ...

The most common techniques for isolating human hepatocytes from donor livers involve a two-step collagenase perfusion and digest ...

medium is then collected, and the concentration of 6b-hydroxytestosterone, a metabolite generated specifically by CYP3A4 is dete ...

The source of hepatocytes, whether via autopsy from accident victims or via biopsy from diseased livers, may affect the inductio ...

(Chan and Delucchi, 2000; Desai et al., 2002; Goodwin et al., 1999; He et al., 1999; Ledirac et al., 2000; Luo et al., 2002, 200 ...