Emre M Isin
Affiliation: AstraZeneca R and D
- Substrate binding to cytochromes P450Emre M Isin
Biotransformation Section, Department of Discovery DMPK and Bioanalytical Chemistry, AstraZeneca R and D Molndal, 431 83, Molndal, Sweden
Anal Bioanal Chem 392:1019-30. 2008..Some of the substrate binding studies extending over a period of more than 40 years of dedicated work have been summarized in this review and categorized by the techniques employed in the binding studies...
- Use of radiolabeled compounds in drug metabolism and pharmacokinetic studiesEmre M Isin
CVGI iMED DMPK, ADME Section, Centre of Excellence, AstraZeneca R and D, Molndal, SE 431 83 Sweden
Chem Res Toxicol 25:532-42. 2012..Finally, we outline strategic changes to our use of radiolabeled compounds in drug metabolism and pharmacokinetic studies, with an emphasis on delaying of in vivo studies employing radiolabeled drug molecules...
- In vitro approach to assess the potential for risk of idiosyncratic adverse reactions caused by candidate drugsRichard A Thompson
DMPK Innovative Medicine, AstraZeneca, Molndal, 431 83, Sweden
Chem Res Toxicol 25:1616-32. 2012....
- Database Extraction of Metabolite Information of Drug Candidates: Analysis of 27 AstraZeneca Compounds with Human Absorption, Distribution, Metabolism, and Excretion DataJessica Iegre
Cardiovascular and Metabolic Diseases, Innovative Medicines and Early Development Biotech Unit J I, M A H, L W, E M I and Respiratory, Inflammation and Autoimmunity, Innovative Medicines and Early Development Biotech Unit R A T, AstraZeneca, Molndal, Sweden
Drug Metab Dispos 44:732-40. 2016..This retrospective analysis assesses the predictive value of Met-ID experiments and improves our ability to discriminate between metabolites expected to circulate in humans and irrelevant metabolites seen in preclinical studies. ..
- Model electrochemical-mass spectrometric studies of the cytochrome P450-catalyzed oxidations of cyclic tertiary allylaminesUlrik Jurva
Department of DMPK and Bioanalytical Chemistry, AstraZeneca R and D Molndal, S 431 83 Molndal, Sweden
J Am Chem Soc 127:12368-77. 2005....
- Risk assessment and mitigation strategies for reactive metabolites in drug discovery and developmentRichard A Thompson
Discovery DMPK, AstraZeneca R and D Molndal, SE 413 83 Mölndal, Sweden
Chem Biol Interact 192:65-71. 2011..We exemplify the potential value of this approach by consideration of the thiazolidinedione class of drugs...
- Reactive Metabolites: Current and Emerging Risk and Hazard AssessmentsRichard A Thompson
DMPK, Respiratory, Inflammation and Autoimmunity iMed, AstraZeneca R and D, 431 83 Mölndal, Sweden
Chem Res Toxicol 29:505-33. 2016..Finally, the potential impact of systems pharmacology approaches in reactive metabolite risk assessments is highlighted. ..
- Use of electrochemical oxidation and model peptides to study nucleophilic biological targets of reactive metabolites: the case of rimonabantAnnika Thorsell
DMPK Design and Biotransformation, CVMD iMed DMPK, AstraZeneca R and D Molndal, Sweden, Pepparedsleden 1, SE 431 83, Molndal, Sweden
Chem Res Toxicol 27:1808-20. 2014....
- Bioactivation pathways of the cannabinoid receptor 1 antagonist rimonabantMoa Andresen Bergström
CVGI iMED DMPK, AstraZeneca R and D Molndal, SE 43183 Mölndal, Sweden
Drug Metab Dispos 39:1823-32. 2011..In view of these findings, it is noteworthy that, to date, no toxicity findings related to the formation of reactive metabolites from rimonabant have been reported...