The utility of microdosing over the past 5 years

Lappin, Graham and Garner, R. Colin (2008) The utility of microdosing over the past 5 years. Expert Opinion on Drug Metabolism and Toxicology, 4 (12). pp. 1499-1506. ISSN 1742-5255

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Background: Microdosing studies (human Phase 0) are used to select drug candidates for Phase I clinical trials on the basis of their pharmacokinetic properties, using subpharmacologic doses (maximum 100 μg). There are questions as to whether pharmacokinetic data obtained at these low doses will predict those at the clinically relevant dose. Objective: To review the current literature on microclosing and assess how well microdose data have predicted the pharmacokinetics obtained at a therapeutic dose. Methods: All data published in the peer reviewed literature comparing pharmacokinetics at a microdose with a therapeutic dose were reviewed, excluding those studies aimed at imaging. Conclusions: Of the 18 drugs reported, 15 demonstrated linear pharmacokinetics within a factor of 2 between a microdose and a therapeutic dose. Therefore, data that support the utility of microdosing are beginning to emerge. © 2008 Informa UK Ltd.

Keywords:alpha 1 adrenergic receptor blocking agent, alpha 1A adrenergic receptor, antiestrogen, atenolol, carbamazepine, clarithromycin, diazepam, digoxin, diphenhydramine, erythromycin, fexofenadine, fluconazole, metoprolol, midazolam, paracetamol, phenazone, phenobarbital, propafenone, sumatriptan, tolbutamide, unclassified drug, warfarin, zidovudine, zk 253, area under the curve, clinical trial, computer model, distribution volume, drug bioavailability, drug clearance, drug dose comparison, drug dose regimen, drug half life, human, in vitro study, liquid chromatography, mass spectrometry, maximum plasma concentration, microdosing, nonhuman, peer review, pharmacodynamics, positron emission tomography, prediction, review, Animals, Clinical Trials, Phase I as Topic, Humans, Pharmaceutical Preparations, Time Factors
Divisions:College of Science > School of Pharmacy
ID Code:8223
Deposited On:24 Mar 2013 16:15

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