Use of Cocktail Probe Drugs for Indexing Cytochrome P450 Enzymes in Clinical Pharmacology Studies – Review of Case Studies
Conclusion: The review provides a comprehensive list of various types of cocktail approaches and discusses some key considerations including the evolution of the cocktail approaches over time, perspectives and futuristic views for the use of probe drugs to aid the execution of clinical pharmacology studies and data interpretation. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - April 30, 2019 Category: Drugs & Pharmacology Source Type: research
Preface
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - April 30, 2019 Category: Drugs & Pharmacology Source Type: research
Meet Our Editorial Board Member
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - April 30, 2019 Category: Drugs & Pharmacology Source Type: research
Alam K et al. (2018) Drug Metabolism Letters; 12, 24-32.
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 23, 2018 Category: Drugs & Pharmacology Source Type: research
Quantitative Proteomics Reveals Changes in Transporter Protein Abundance in Liver, Kidney and Brain of Mice by Pregnancy
Conclusion: Protein abundance of drug transporters can be significantly changed particularly in the liver by pregnancy. These results will be helpful to understand pregnancy-induced changes in drug/xenobiotic disposition in the mouse model. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 23, 2018 Category: Drugs & Pharmacology Source Type: research
Genistein Affects Expression of Cytochrome P450 (CYP450) Genes in Hepatocellular Carcinoma (HEPG2/C3A) Cell Line
Conclusion: Our results suggest that treatment with genistein in non-toxic concentrations may impact the expression level of CYPs involved in the biotransformation of xenobiotics and drug metabolizing enzymes. Moreover, the downregulation of ATRA metabolism-related genes opens a new research path for the study of genistein as retinoic acid metabolism blocking agent for treating cancer and other pathologies. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 23, 2018 Category: Drugs & Pharmacology Source Type: research
A Novel In vitro Experimental System for the Evaluation of Enteric Drug Metabolism: Cofactor-Supplemented Permeabilized Cryopreserved Human Enterocytes (MetMax™ Cryopreserved Human Enterocytes)
Conclusion: Our results suggest that the MMHE system represents a convenient and robust in vitro experimental system for the evaluation of enteric drug metabolism. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 23, 2018 Category: Drugs & Pharmacology Source Type: research
Hepatic Flavin-containing Monooxygenase and Aldehyde Oxidase Activities in Male Domestic Pigs at Different Ages
Conclusion: Age impact on hepatic activities of both FMO and AO is obvious in domestic male pigs although age patterns of both enzymes are different. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 23, 2018 Category: Drugs & Pharmacology Source Type: research
Effects of Tobacco Nicotine-Derived Nitrosamine Ketone (NNK) Exposures on Brain Alcohol Metabolizing Enzyme Activities
Conclusion: Dual exposures to ethanol and NNK increase brain ethanol metabolism and inhibit the expression of CYP450s that regulate xenobiotic metabolism. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 23, 2018 Category: Drugs & Pharmacology Source Type: research
Acknowledgements to Reviewers
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 22, 2018 Category: Drugs & Pharmacology Source Type: research
In Vitro Drug-Drug Interaction Potential of Sulfoxide and/or Sulfone Metabolites of Albendazole, Triclabendazole , Aldicarb, Methiocarb, Montelukast and Ziprasidone
Conclusion: Based on the findings, a proper risk assessment strategy needs to be factored (i.e., perpetrator and/or victim drug) to overcome any imminent risk of potential clinical drug-drug interaction when sulfoxide/sulfone metabolite(s) generating drugs are coadministered in therapy. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 22, 2018 Category: Drugs & Pharmacology Source Type: research
Using LC Retention Times in Organic Structure Determination: Drug Metabolite Identification
Conclusion: In our experience, this simple methodology allows complementing the discovery efforts that saves resources for in-depth characterization using NMR. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 22, 2018 Category: Drugs & Pharmacology Source Type: research
New Perspectives on Acyl Glucuronide Risk Assessment in Drug Discovery: Investigation of In vitro Stability, In situ Reactivity, and Bioactivation
Conclusion: While the compounds tested from “withdrawn” and “warning category” all formed the glutathione adduct in buffer, none from “safe” category formed the glutathione adduct. In contrast, none of the compounds tested from any category formed methoxylamine conjugate, a reaction with putative aldehyde moiety formed via acyl migration. These results, highly favor the nucleophilic displacement as a cause of the reactivity rather than the acyl migration via aldehyde formation. The workflow presented could also be applied in the discovery setting to triage new chemical entities of interest. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 22, 2018 Category: Drugs & Pharmacology Source Type: research
Meet Our Editorial Board Member
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 22, 2018 Category: Drugs & Pharmacology Source Type: research
Evaluation of the Effect of Uremic Serum on Hepatic Reductase Functional Expression
Conclusion: Although uremic serum can upregulate mRNA expression of several reductases, this effect was not observed at the activity level. Future studies are necessary to improve our understanding of the mechanistic effects of impaired kidney function on drug reduction. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - August 28, 2018 Category: Drugs & Pharmacology Source Type: research
