Ontogeny of hepatic CYP1A2 and CYP2E1 expression in rat

FA Elbarbry, PJ McNamara… - Journal of biochemical …, 2007 - Wiley Online Library
We report a comprehensive examination of rat hepatic CYP1A2 and CYP2E1 ontogeny. We
compare the data to human data to determine the rat's capacity as a model to identify CYP …

Drug metabolism in the paediatric population and in the elderly

MS Benedetti, R Whomsley, M Canning - Drug discovery today, 2007 - Elsevier
This review focuses on one of the key factors accounting for differences in drug/metabolite
exposure in paediatric and elderly subjects compared with that of the adult population, that …

Species differences between mouse, rat, dog, monkey and human CYP-mediated drug metabolism, inhibition and induction

M Martignoni, GMM Groothuis… - Expert opinion on drug …, 2006 - Taylor & Francis
Animal models are commonly used in the preclinical development of new drugs to predict
the metabolic behaviour of new compounds in humans. It is, however, important to realise …

Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance

UM Zanger, K Klein, T Saussele, J Blievernicht… - 2007 - Future Medicine
Polymorphisms in drug-metabolizing enzymes and drug transporters contribute to wide and
inheritable variability in drug pharmacokinetics, response and toxicity. One of the less well …

Incorporating pharmacokinetic differences between children and adults in assessing children's risks to environmental toxicants

G Ginsberg, D Hattis, B Sonawane - Toxicology and applied pharmacology, 2004 - Elsevier
Children's risks from environmental toxicant exposure can be affected by pharmacokinetic
factors that affect the internal dose of parent chemical or active metabolite. There are …

Polymorphism of human cytochrome P450 enzymes and its clinical impact

SF Zhou, JP Liu, B Chowbay - Drug metabolism reviews, 2009 - Taylor & Francis
Pharmacogenetics is the study of how interindividual variations in the DNA sequence of
specific genes affect drug response. This article highlights current pharmacogenetic …

The use of pharmacokinetic and pharmacodynamic data in the assessment of drug safety in early drug development

DK Walker - British journal of clinical pharmacology, 2004 - Wiley Online Library
The pharmaceutical industry continues to look for ways to reduce drug candidate attrition
throughout the drug discovery and development process. A significant cause of attrition is …

Two linked mutations in transcriptional regulatory elements of the CYP3A5 gene constitute the major genetic determinant of polymorphic activity in humans

A Paulussen, K Lavrijsen, H Bohets… - Pharmacogenetics …, 2000 - journals.lww.com
Cytochrome P450 3A subfamily members (CYP3A) are the most abundant liver cytochrome
P450 forms, responsible for the biotransformation of over 50% of all drugs. The expression …

Drug metabolism for the paediatrician

SN de Wildt, D Tibboel, JS Leeder - Archives of disease in childhood, 2014 - adc.bmj.com
Drug metabolism importantly determines drug concentrations. The efficacy and safety of
many drugs prescribed for children are, therefore, dependent on intraindividual and …

Leveraging physiologically based pharmacokinetic modeling and experimental data to guide dosing modification of CYP3A-mediated drug-drug interactions in the …

SN Salerno, FO Carreño, AN Edginton… - Drug Metabolism and …, 2021 - ASPET
Solithromycin is a novel fluoroketolide antibiotic that is both a substrate and time-dependent
inhibitor of CYP3A. Solithromycin has demonstrated efficacy in adults with community …