Highlights of the XII International Congress on Toxicology, 19 - 23 July 2010, Barcelona, Spain.

abstract：INTRODUCTION:Major depressive disorder (MDD), one of the most common disorders in medical practice and one of the leading causes of disability worldwide, is frequently comorbid with anxiety disorders. Vortioxetine (Lu AA21004) is a new antidepressant that combines a number of neurotransmitter reuptake and receptor effe...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Dubovsky SL

更新日期：2014-05-01 00:00:00

abstract：INTRODUCTION:In preliminary clinical studies, aleglitazar, a new dual PPAR-α-γ agonist, has been demonstrated to improve hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus. This review will provide up-to-date information on the clinical safety and efficacy of aleglitazar, which is currently under ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Younk LM,Uhl L,Davis SN

更新日期：2011-06-01 00:00:00

abstract：INTRODUCTION:Golimumab is a human anti-TNF monoclonal antibody that was derived from human antibody-transgenic mice. Golimumab demonstrated meaningful clinical benefit and tolerable safety in patients with active rheumatoid arthritis (RA) who were methotrexate (MTX)-naïve, or who inadequately responded to MTX or who ha...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Tanaka Y,Senoo A,Fujii H,Baker D

更新日期：2016-01-01 00:00:00

abstract：INTRODUCTION:A more concentrated insulin glargine formulation, containing 300 U/mL (Gla-300) was approved in 2015 in the US and Europe for the treatment of diabetes mellitus in adults. AREAS COVERED:This drug evaluation focuses on the pharmacokinetics (PK) and pharmacodynamics (PD) of Gla-300 from studies published up...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Owens DR

更新日期：2016-08-01 00:00:00

abstract：BACKGROUND:CYP enzymes from the CYP2C and CYP2J subfamilies metabolize arachidonic acid in a regiospecific and stereoselective manner to eight epoxyeicosatrienoic acids (EETs). Various EETs have been detected in the liver, as well as in many extrahepatic tissues, and have been implicated in numerous physiological funct...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Kaspera R,Totah RA

更新日期：2009-07-01 00:00:00

abstract：INTRODUCTION:The goal of pharmacologic therapy with antiepileptic drugs (AEDs) is to reduce the frequency of seizures and achieve a seizure-free state with minimal side effects. However 30% of patients treated with available AEDs continue to experience uncontrolled seizures. There is still need for new AEDs with enhanc...

journal_title：Expert opinion on drug metabolism & toxicology

authors： de Biase S,Valente M,Gigli GL,Merlino G

更新日期：2017-09-01 00:00:00

abstract：INTRODUCTION:Unacceptable failure rates in clinical trials are largely responsible for the high costs of bringing successful drugs to market - costs that are passed on to patients, insurers or healthcare providers. Furthermore, failures in clinical trials deny patients much-needed new drugs and potentially expose them ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Clotworthy M,Archibald K

更新日期：2013-09-01 00:00:00

abstract：OBJECTIVES:A medical need remains for a once-daily insulin with 24-h basal coverage in all patients. We characterize the steady-state (SS) pharmacokinetic/pharmacodynamic properties of insulin degludec (IDeg) versus insulin glargine (IGlar). RESEARCH DESIGN AND METHODS:In this controlled, single-center study, 66 type ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Heise T,Hövelmann U,Nosek L,Hermanski L,Bøttcher SG,Haahr H

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:Donepezil is a highly selective acetylcholinesterase inhibitor and one of the only four drugs currently approved for treatment of Alzheimer's dementia. Providing high bioavailability and a very long half-time, donepezil is regarded as effective and well tolerable in Alzheimer's disease patients, even in di...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Prvulovic D,Schneider B

更新日期：2014-07-01 00:00:00

abstract：:Introduction: Overactive bladder (OAB) has a heterogeneous presentation that varies between individuals and by gender. Treatment with antimuscarinic medications is standard first line pharmacotherapy for most patients with OAB. However, gender specific differences in the pharmacokinetics and pharmacodynamics of antimu...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hartigan SM,Dmochowski RR

更新日期：2020-02-01 00:00:00

abstract：INTRODUCTION:The review aims to discuss effects of vitrectomy on pharmacokinetics of anti-vascular endothelial growth factor (anti-VEGF) agents, and attempt to provide treatment guidance. Areas covered: An Embase search was conducted using the terms 'anti-VEGF', 'pegaptanib', 'ranibizumab', 'bevacizumab', 'aflibercept'...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Edington M,Connolly J,Chong NV

更新日期：2017-12-01 00:00:00

abstract：:The onset, intensity and duration of therapeutic response to a compound depend on the intrinsic pharmacological activity of the drug and pharmacokinetic factors related to its absorption, distribution, metabolism and elimination that are inherent to the biological system. The process of drug transfer from the site of ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hurst S,Loi CM,Brodfuehrer J,El-Kattan A

更新日期：2007-08-01 00:00:00

abstract：INTRODUCTION:multiple myeloma (MM) is a plasma cell disorder that represents the second most frequent hematologic cancer. Although MM is still an incurable disease, prognosis has improved in the last decades thanks to the introduction of novel agents such as proteasome inhibitors (PIs), immunomodulatory drugs, monoclon...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Salvini M,Troia R,Giudice D,Pautasso C,Boccadoro M,Larocca A

更新日期：2018-01-01 00:00:00

abstract：:The calcium sensing receptor (CaSR) is expressed in cells secreting calcium-regulating hormones, in cells involved in calcium transport and in many other tissues, with an as yet not completely defined role. In parathyroid cells, the CaSR stimulation inhibits parathyroid hormone (PTH) secretion, synthesis and parathyro...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Messa P,Alfieri C,Brezzi B

更新日期：2008-12-01 00:00:00

abstract：INTRODUCTION:Many different drugs and xenobiotics (chemical compounds foreign to an organism) can injure the bile duct epithelium and cause inflammatory bile duct diseases (cholangiopathies) ranging from transient cholestasis to vanishing bile duct syndrome, sclerosing cholangitis with development of biliary fibrosis a...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Österreicher CH,Trauner M

更新日期：2012-05-01 00:00:00

abstract：:Background: The liver plays a central role in human drug metabolism. To model drug metabolism, the major cell type of the liver, the hepatocyte, is commonly used. Hepatocytes can be derived from human and animal sources, including pluripotent stem cells. Cell-based models have shown promise in modeling human drug expo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Zhou W,Graham K,Lucendo-Villarin B,Flint O,Hay DC,Bagnaninchi P

更新日期：2019-01-01 00:00:00

abstract：OBJECTIVE:Oral bioavailability is one of the most important properties in drug design and development. A poor oral bioavailability can result in low efficacy and unpredictable response to a drug. Several dosages of melatonin have been used for various investigations to clarify its bioavailability in humans. Aiming to s...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Proietti S,Carlomagno G,Dinicola S,Bizzarri M

更新日期：2014-09-01 00:00:00

abstract：:The expression of drug-metabolising enzymes is affected by many endogenous and exogenous factors, including sex, age, diet and exposure to xenobiotics and drugs. To understand fully how the organism metabolises a drug, these alterations in gene expression must be taken into account. The central process, the definition...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Podvinec M,Meyer UA

更新日期：2006-06-01 00:00:00

abstract：INTRODUCTION:Short- and long-acting β agonists (SABA and LABA) are bronchodilators for treating asthma. Bronchodilator response (BDR) is quantified by measuring air expired in the first second during a forced expiratory maneuver, prior to and following inhalation of SABA. BDR has been associated with a significant degr...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lima JJ

更新日期：2014-09-01 00:00:00

abstract：:It has increasingly been recognized that few molecules move across the cell membrane without the assistance of transporter proteins. Large superfamilies of transporter proteins have been identified in every living cell, including microorganisms and mitochondria. This report reviews the role of transporters in physiolo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lee EJ,Lean CB,Limenta LM

更新日期：2009-11-01 00:00:00

abstract：INTRODUCTION:Co-medication, gene polymorphisms and co-morbidity are main causes for high variability in expression and function of the CYP3A isoenzymes. Pharmacokinetic variability is a major source of interindividual variability of drug effect and response of CYP3A substrates. While CYP3A genotyping is of limited use,...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hohmann N,Haefeli WE,Mikus G

更新日期：2016-05-01 00:00:00

abstract：:There is an increasing recognition within the pharmaceutical industry of the importance of the ADME studies in drug registration. Consequently, there has been a drive in recent times to conduct the ADME studies as early as possible in the development programme. There are, however, regulatory barriers, particularly in ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lappin G,Garner RC

更新日期：2005-06-01 00:00:00

abstract：INTRODUCTION:Due to their multiple effects, glucocorticoids (GCs) have versatile medical uses. They can regulate many xenobiotic-metabolizing enzymes of the cytochrome P450 (CYP) superfamily, and thus, influence pharmacotherapy. AREAS COVERED:The aim of this paper is to summarize the molecular effects of GCs on CYP as...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Matoulková P,Pávek P,Malý J,Vlček J

更新日期：2014-03-01 00:00:00

abstract：INTRODUCTION:Drug ototoxicity represents one of the main preventable causes of deafness. Ototoxicity is a trait shared by aminoglycoside and macrolide antibiotics, antimalarial medications, loop diuretics, platinum-based chemotherapeutic agents, some NSAIDs and most recently described, acetaminophen when abused with na...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Yorgason JG,Luxford W,Kalinec F

更新日期：2011-12-01 00:00:00

abstract：INTRODUCTION:Invasive fungal infections remain a leading cause of infectious morbidity and mortality in immunocompromised patients. There are relatively few effective antifungal agents, and currently available agents all have significant limitations. Isavuconazole is a novel second-generation triazole with broad-spectr...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Livermore J,Hope W

更新日期：2012-06-01 00:00:00

abstract：INTRODUCTION:Cytochromes P450 (P450) and associated monooxygenases are a family of heme proteins involved in metabolism of endogenous compounds (arachidonic acid, eicosanoids and prostaglandins) as also xenobiotics including drugs and environmental chemicals. Liver is the major organ involved in P450-mediated metabolis...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Ravindranath V,Strobel HW

更新日期：2013-05-01 00:00:00

abstract：:Toxicogenomics is the application of gene expression profiling technology to toxicology. This results in the generation of very large and complex gene expression data sets associated with the development of toxicities. It is widely assumed that this data can be deconvoluted to reveal novel insights into toxicological ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Huby R,Tugwood JD

更新日期：2005-08-01 00:00:00

abstract：:In adapting to the challenge to make more informed selection of compounds for development, the pharmaceutical industry is increasingly embracing the application of mechanism-based models and prediction tools for prediction of pharmacokinetic parameters. This review first outlines the concepts and application of the ma...

journal_title：Expert opinion on drug metabolism & toxicology

authors： De Buck SS,Mackie CE

更新日期：2007-12-01 00:00:00

abstract：INTRODUCTION:Coumadin (R/S-warfarin) is the most widely prescribed oral anticoagulant in the world; nevertheless, its clinical use is complicated by unpredictability in dose requirements to achieve and maintain optimal anticoagulation. Variations in warfarin metabolism among patients contribute to unpredictability in t...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Jones DR,Miller GP

更新日期：2011-07-01 00:00:00

abstract：:Antithrombotic therapy is a crucial component of interventional cardiology and currently involves the administration of both anticoagulant and antiplatelet agents. The implementation of standard dual or triple antiplatelet therapies has allowed percutaneous coronary intervention (PCI) with stent implantation to become...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Ahrens I,Smith BK,Bode C,Peter K

更新日期：2007-08-01 00:00:00