The Effects of Statin Therapy on the Human Airway
Conclusion: Statins may have beneficial pleiotropic effects in addition to their actions as potent lipid-lowering agents particularly in patients with chronic obstructive pulmonary disease and post lung transplantation. Further human studies are required to substantiate their possible potential as many of the clinical trials performed to date have not demonstrated the translation of results of these promising scientific and observational studies into positive outcomes in well-designed, randomized, placebo-controlled human trials. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - June 14, 2016 Category: Drugs & Pharmacology Source Type: research
Commentary: A Myriad Aberrations on Information of Ontogeny of Drug Metabolizing Enzymes in the Pediatric Population: An Obstacle for Personalizing Drug Therapy in the Pediatric Population
Major lacunae exist in our understanding of how developmental changes in drug biotransformation influence drug’s exposure and thus its efficacy and toxicity in children. It is not just about smaller weight in children, which modifies the pattern of the drug's exposure. There are developmental, functional changes in organ systems, liver to body mass ratios, and changes in metabolism. Understanding these changes and conducting studies to obtain data on ontogeny of drug metabolizing enzymes is essential for implementation of personalized dosing schedules in the pediatric population. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - June 14, 2016 Category: Drugs & Pharmacology Source Type: research
Meet Our Editorial Board Member
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - June 14, 2016 Category: Drugs & Pharmacology Source Type: research
Impact of Cytochrome P450 2C19*2 and *3 on Clopidogrel Loading Dose in Saudi Patients with Acute Coronary Syndrome
Conclusion: Genotype differences may not explain variations in the PRU of patients during short-term in-hospital stays. Although it is difficult to confirm, 117–267 units may be a safe PRU range for such patients, with emphasis on attaining higher PRU values in females. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - February 13, 2016 Category: Drugs & Pharmacology Source Type: research
Common and Distinct Interactions of Chemical Inhibitors with Cytochrome P450 CYP1A2, CYP2A6 and CYP2B6 Enzymes
Conclusion: This in silico approach will provide a means for very rapid and high throughput prediction of cross-inhibition of these three CYP enzymes. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - February 13, 2016 Category: Drugs & Pharmacology Source Type: research
Induction of Haemolysis and DNA Fragmentation in a Normal and Malarial-Infected Blood by Commonly - used Antimalarial Drugs in the North-Western Region of Nigeria
Conclusion: Commonly-used antimalarial drugs induced haemolysis and altered haemoglobin status which may spontaneously increases the cellular iron levels; a substrate for Fenton and Haber Weiss reactions, and eventually induces DNA fragmentation. Hence, adequate care should be taken during prescription with total avoidance for self medications and/or drugs abuse as a result of their adverse effects within the red blood cells and its immediate microenvironment. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - February 13, 2016 Category: Drugs & Pharmacology Source Type: research
Clinical Confirmation that the Selective JAK1 Inhibitor Filgotinib (GLPG0634) has a Low Liability for Drug-drug Interactions
Conclusion: the collective in vivo and in vitro data on drug-metabolizing enzymes and on key drug transporters, support co-administration of filgotinib with commonly used RA drugs to patients without the need for dose adjustments. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - February 13, 2016 Category: Drugs & Pharmacology Source Type: research
Metabolism, Excretion and Pharmacokinetics of MLN3897, a CCR1 Antagonist, in Humans
MLN3897 is a small molecule antagonist of the C-C chemokine receptor-1. Since preclinical studies showed that the molecule was metabolized into two halves, the metabolism, excretion, and pharmacokinetics of MLN3897 were investigated in humans using MLN3897 14C-radiolabeled either on the chlorophenyl (CP) or the tricyclic (TC) half of MLN3897 after an oral dose. Objective: To evaluate the mass balance, metabolism and pharmacokinetics of MLN3897 in two cohorts of six randomized healthy subjects. Method: After receiving informed consent, subjects were dosed after an overnight fast of 10-hours followed by at least 4- hours...
Source: Drug Metabolism Letters - February 13, 2016 Category: Drugs & Pharmacology Source Type: research
Inactivation of CYP3A4 by Benzbromarone in Human Liver Microsomes
Conclusion: Modification of the P450 enzyme by the reactive metabolite is a common trait of drugs that induce idiosyncratic hepatotoxicity, and might provide a speculative, mechanistic model for the rare occurrences of this type of drug toxicity. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - February 13, 2016 Category: Drugs & Pharmacology Source Type: research
A Novel Plated Hepatocyte Relay Assay (PHRA) for In Vitro Evaluation of Hepatic Metabolic Clearance of Slowly Metabolized Compounds
Conclusion: PHRA represents a useful experimental system for the evaluation of the metabolic fates of low clearance compounds in drug development.. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - February 13, 2016 Category: Drugs & Pharmacology Source Type: research
Preface
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - February 13, 2016 Category: Drugs & Pharmacology Source Type: research
Meet Our Co-Editor
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - February 13, 2016 Category: Drugs & Pharmacology Source Type: research
Acknowledgements to Reviewers:
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 18, 2015 Category: Drugs & Pharmacology Source Type: research
The Detection of Anti-adalimumab Antibodies in a Series of Inflammatory Polyarthritis: three ELISA Methods Compared
Conclusions: The three bridging ELISA methods under study showed a good agreement and were able to identify uniquely the presence of high positive AAA, even after a long time since ADL discontinuation. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 18, 2015 Category: Drugs & Pharmacology Source Type: research
Non-Clinical Disposition and Metabolism of DM1, a Component of Trastuzumab Emtansine (T-DM1), in Sprague Dawley Rats
DM1, a derivative of maytansine, is the cytotoxic component of the antibody–drug conjugate trastuzumab emtansine (T-DM1). Understanding the disposition and metabolism of DM1 would help to assess (1) any tissue-specific distribution and risk for potential drug–drug interactions and (2) the need for special patient population studies. To this end, the current study determined the disposition and metabolism of DM1 following single intravenous administration of [3H]-DM1 in Sprague Dawley rats. Blood, tissues, urine, bile, and feces were collected up to 5 days after dose administration and analyzed for total radioactivity a...
Source: Drug Metabolism Letters - November 18, 2015 Category: Drugs & Pharmacology Source Type: research
