Meet Our Editorial Board Member
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - June 30, 2020 Category: Drugs & Pharmacology Source Type: research
Acknowledgements to reviewers
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - January 15, 2020 Category: Drugs & Pharmacology Source Type: research
Oral Bioavailability Enhancement of Amisulpride: Complexation and its Pharmacokinetics and Pharmacodynamics Evaluations
Conclusion: Pharmacodynamic studies in mice showed improved effectiveness of drug compared to pure drug. The oral bioavailability of AMS was improved from 48% to 78%. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - January 15, 2020 Category: Drugs & Pharmacology Source Type: research
Assessment of Inhibition of Bovine Hepatic Cytochrome P450 by 43 Commercial Bovine Medicines Using a Combination of In Vitro Assays and Pharmacokinetic Data from the Literature
Conclusion: This combination of in vitro assay and in vivo Cmax data provides a good approach to assess the inhibition of bovine medicines on bovine hepatic CYP450. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - January 15, 2020 Category: Drugs & Pharmacology Source Type: research
The Effects of Special Patient Population Plasma on Pharmacokinetic Quantifications Using LC-MS/MS
Conclusion: Special population plasma did not affect quantitation of drugs with a wide range of plasma protein binding levels in human plasma. With the confirmation that there is no impact on quantification from the matrix, the bioanalytical method can be used to support the pharmacokinetic evaluations for clinical studies in special populations. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - January 15, 2020 Category: Drugs & Pharmacology Source Type: research
Imatinib Uptake into Cells is Not Mediated by Organic Cation Transporters OCT1, OCT2, or OCT3, But is Influenced by Extracellular pH
Conclusion: Imatinib is not a substrate of OCTs 1-3 while the environmental pH modulates cellular disposition of imatinib. The observation that a slightly acidic extracellular pH influences imatinib cellular accumulation is important, considering the low extracellular pH reported in the hematopoietic leukemia/ cancer cell microenvironment. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - January 15, 2020 Category: Drugs & Pharmacology Source Type: research
Prominence of Oxidative Stress in the Management of Anti-tuberculosis Drugs Related Hepatotoxicity
Advanced medical services and treatments are available for treating Tuberculosis. Related prevalence has increased in recent times. Unfortunately, the continuous consumption of related drugs is also known for inducing hepatotoxicity which is a critical condition and cannot be overlooked. The present review article has focused on the pathways causing these toxicities and also the role of enzyme CYP2E1, hepatic glutathione, Nrf2-ARE signaling pathway, and Membrane Permeability Transition as possible targets which may help in preventing the hepatotoxicity induced by the drugs used in the treatment of tuberculosis. (Source: Dr...
Source: Drug Metabolism Letters - January 15, 2020 Category: Drugs & Pharmacology Source Type: research
A Practical Perspective on the Evaluation of Small Molecule CNS Penetration in Drug Discovery
The separation of the brain from blood by the blood-brain barrier and the bloodcerebrospinal fluid (CSF) barrier poses unique challenges for the discovery and development of drugs targeting the central nervous system (CNS). This review will describe the role of transporters in CNS penetration and examine the relationship between unbound brain (Cu-brain) and unbound plasma (Cu-plasma) or CSF (CCSF) concentration. Published data demonstrate that the relationship between Cu-brain and Cu-plasma or CCSF can be affected by transporter status and passive permeability of a drug and CCSF may not be a reliable surrogate for CNS pene...
Source: Drug Metabolism Letters - January 15, 2020 Category: Drugs & Pharmacology Source Type: research
Meet Our Editorial Board Member
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - January 15, 2020 Category: Drugs & Pharmacology Source Type: research
Formation of a Toxic Quinoneimine Metabolite from Diclofenac: A Quantum Chemical Study
Conclusion: The results demonstrate the possibility of formation of quinoneimine metabolite due to various factors that are involved in the metabolism of diclofenac. The present study may provide the structural in-sights during the drug development processes to avoid the metabolism directed idiosyncratic toxicity. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - April 30, 2019 Category: Drugs & Pharmacology Source Type: research
Comparison of Rat and Human Pulmonary Metabolism Using Precision-cut Lung Slices (PCLS)
Conclusion: PCLS is a promising tool for the investigation of pulmonary drug metabolism. The data indicates that pulmonary CYP activity is relatively low and that there are significant differences in enzyme activity between rat and human lung. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - April 30, 2019 Category: Drugs & Pharmacology Source Type: research
“Branched Tail” Oxyquinoline Inhibitors of HIF Prolyl Hydroxylase: Early Evaluation of Toxicity and Metabolism Using Liver-on-a-chip
Conclusion: The optimized adaptaquin analogs are suitable for further preclinical trials. Activation of CYP2B6 with adaptaquin and its variants points to a potential increase in Tylenol toxicity if administered together. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - April 30, 2019 Category: Drugs & Pharmacology Source Type: research
Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study
Conclusion: Assuming that the radiotracer was proportional to total drug throughout a radiolabeled study was not valid in a 14C study in beagle dogs. This presumably resulted from unequal absorption of the radiotracer and nonradiolabeled test articles from the oral dose due to inequivalent solid forms. We were able to provide a more accurate description of the AME of GDC-0276 in dogs by characterizing the differential absorption of the radiotracer. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - April 30, 2019 Category: Drugs & Pharmacology Source Type: research
Transport of Bupropion and its Metabolites by the Model CHO and HEK293 Cell Lines
Conclusion: BUP and metabolites are not substrates of the major hepatic transporters tested and thus these hepatic transporters likely do not play a role in the overall disposition of the drug. Our results also suggest that caution should be taken when using the model CHO and HEK293 cell lines to evaluate potential roles of transporters in drug disposition. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - April 30, 2019 Category: Drugs & Pharmacology Source Type: research
Effect of Aqueous Extract of Azadirachta indica Leaves on Pharmacokineics and Pharmacodynamics of Glipizide
Conclusion: This indicated that the pharmacokinetics and pharmacodynamics of GZ altered by AZI might be due to the induction of CYP3A activity. In conclusion, AZI can decrease the bioavailability of GZ, and hence, it should be cautiously used. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - April 30, 2019 Category: Drugs & Pharmacology Source Type: research
