Detecting reactive drug metabolites for reducing the potential for drug toxicity

Reactive Metabolite Trapping Screens and Potential Pitfalls: Bioactivation of a Homomorpholine and Formation of an Unstable Thiazolidine Adduct

(2014) Eva. M. Lenz et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Recent advances in 2D and 3D in vitro systems using primary hepatocytes, alternative hepatocyte sources and non-parenchymal liver cells and their use in investigating mechanisms of hepatotoxicity, cell signaling and ADME

(2013) Patricio Godoy et al.   ARCHIVES OF TOXICOLOGY

N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Strategies to eliminate reactive metabolites

(2013) Sajiv K. Nair et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Bioinformatic Analysis of 302 Reactive Metabolite Target Proteins. Which Ones Are Important for Cell Death?

(2013) Robert P. Hanzlik et al.   TOXICOLOGICAL SCIENCES

In Vitro Bioactivation of a Selective Estrogen Receptor Modulator (2S,3R)-(+)-3-(3-Hydroxyphenyl)-2-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-2,3-dihydro-1,4-benzoxathiin-6-ol (I) in Liver Microsomes: Formation of Adenine Adducts

(2012) Ying Li et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Preclinical Strategy to Reduce Clinical Hepatotoxicity Using in Vitro Bioactivation Data for >200 Compounds

(2012) Melanie Z. Sakatis et al.   CHEMICAL RESEARCH IN TOXICOLOGY

In Vitro Approach to Assess the Potential for Risk of Idiosyncratic Adverse Reactions Caused by Candidate Drugs

(2012) Richard A. Thompson et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Use of Micropatterned Cocultures to Detect Compounds That Cause Drug-Induced Liver Injury in Humans

(2012) Salman R. Khetani et al.   TOXICOLOGICAL SCIENCES

Overcoming the Genotoxicity of a Pyrrolidine Substituted Arylindenopyrimidine As a Potent Dual Adenosine A2A/A1Antagonist by Minimizing Bioactivation to an Iminium Ion Reactive Intermediate

(2011) Heng-Keang Lim et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Application of the Hard and Soft, Acids and Bases (HSAB) Theory to Toxicant–Target Interactions

(2011) Richard M. LoPachin et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Drug-S-Acyl-Glutathione Thioesters: Synthesis, Bioanalytical Properties, Chemical Reactivity, Biological Formation and Degradation

(2011) Mark P. Grillo   CURRENT DRUG METABOLISM

Managing the challenge of chemically reactive metabolites in drug development

(2011) B. Kevin Park et al.   NATURE REVIEWS DRUG DISCOVERY

Formation of a Quinoneimine Intermediate of 4-Fluoro-N-methylaniline by FMO1: Carbon Oxidation Plus Defluorination

(2010) James P. Driscoll et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Can In Vitro Metabolism-Dependent Covalent Binding Data Distinguish Hepatotoxic from Nonhepatotoxic Drugs? An Analysis Using Human Hepatocytes and Liver S-9 Fraction

(2009) Jonathon N. Bauman et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Simultaneous Determination of Six Mercapturic Acid Metabolites of Volatile Organic Compounds in Human Urine

(2009) Yan S. Ding et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Rapid Detection and Characterization of in Vitro and UrinaryN-Acetyl-l-cysteine Conjugates Using Quadrupole-Linear Ion Trap Mass Spectrometry and Polarity Switching

(2009) Wenying Jian et al.   CHEMICAL RESEARCH IN TOXICOLOGY

A Zone Classification System for Risk Assessment of Idiosyncratic Drug Toxicity Using Daily Dose and Covalent Binding

(2009) S. Nakayama et al.   DRUG METABOLISM AND DISPOSITION

Evaluation of the Potential for Drug-Induced Liver Injury Based on in Vitro Covalent Binding to Human Liver Proteins

(2009) T. Usui et al.   DRUG METABOLISM AND DISPOSITION

Quantitative Assessment of Reactive Metabolite Formation using 35S-labeled Glutathione

(2009) Hideo Takakusa et al.   Drug Metabolism and Pharmacokinetics

The Nrf2-Keap1-ARE Toxicity Pathway as a Cellular Sensor for Skin Sensitizers—Functional Relevance and a Hypothesis on Innate Reactions to Skin Sensitizers

(2009) Andreas Natsch   TOXICOLOGICAL SCIENCES

Activation of the Nrf2/ARE pathway via S-alkylation of cysteine 151 in the chemopreventive agent-sensor Keap1 protein by falcarindiol, a conjugated diacetylene compound

(2009) Tomokazu Ohnuma et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

High-Throughput Screening and Characterization of Reactive Metabolites Using Polarity Switching of Hybrid Triple Quadrupole Linear Ion Trap Mass Spectrometry

(2008) Bo Wen et al.   ANALYTICAL CHEMISTRY

Unbiased High-Throughput Screening of Reactive Metabolites on the Linear Ion Trap Mass Spectrometer Using Polarity Switch and Mass Tag Triggered Data-Dependent Acquisition

(2008) Zhengyin Yan et al.   ANALYTICAL CHEMISTRY

In VitroMetabolism and Covalent Binding of Enol-Carboxamide Derivatives and Anti-Inflammatory Agents Sudoxicam and Meloxicam: Insights into the Hepatotoxicity of Sudoxicam

(2008) R. Scott Obach et al.   CHEMICAL RESEARCH IN TOXICOLOGY

γ-Glutamyltranspeptidase-Mediated Degradation of Diclofenac-S-acyl-glutathione in Vitro and in Vivo in Rat

(2008) Mark P. Grillo et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Chemical Reactivity of Methoxy 4-O-Aryl Quinolines: Identification of Glutathione Displacement Products in Vitro and in Vivo

(2008) Yohannes Teffera et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Effect of Intestinal Glucuronidation in Limiting Hepatic Exposure and Bioactivation of Raloxifene in Humans and Rats

(2008) Deepak Dalvie et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Novel Metabolites of Amodiaquine Formed by CYP1A1 and CYP1B1: Structure Elucidation Using Electrochemistry, Mass Spectrometry, and NMR

(2008) T. Johansson et al.   DRUG METABOLISM AND DISPOSITION

A generic method to detect electrophilic intermediates using isotopic pattern triggered data-dependent high-resolution accurate mass spectrometry

(2008) Heng-Keang Lim et al.   RAPID COMMUNICATIONS IN MASS SPECTROMETRY

Metabolism and Toxicity of Drugs. Two Decades of Progress in Industrial Drug Metabolism

(2007) Thomas A. Baillie   CHEMICAL RESEARCH IN TOXICOLOGY

Protein Damage by Reactive Electrophiles: Targets and Consequences

(2007) Daniel C. Liebler   CHEMICAL RESEARCH IN TOXICOLOGY

Modulation of 11β-Hydroxysteroid Dehydrogenase (11βHSD) Activity Biomarkers and Pharmacokinetics of PF-00915275, a Selective 11βHSD1 Inhibitor

(2007) Rachel Courtney et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Prediction of drug-induced liver injury in humans by using in vitro methods: The case of ximelagatran

(2007) Kerstin Kenne et al.   TOXICOLOGY IN VITRO