Precision-cut intestinal slices: alternative model for drug transport, metabolism, and toxicology research.

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：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：INTRODUCTION:The blood-brain barrier (BBB) is a selectively permeable micro-vascular unit which prevents many central nervous system (CNS)-targeted compounds from reaching the brain. A significant problem in CNS drug development is the ability to model BBB permeability in a timely, reproducible and cost-effective manne...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Geldenhuys WJ,Allen DD,Bloomquist JR

更新日期：2012-06-01 00:00:00

abstract：:Severe adverse drug reactions (ADRs) are a major problem in drug development and clinical practice and the most common cause of market withdrawals of drugs. Individualised drug safety aims at the prospective identification of single patients who carry genetic predispositions for the development of serious or fatal ADR...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gut J,Bagatto D

更新日期：2005-10-01 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:Enzalutamide is the first approved second-generation androgen receptor (AR) antagonist in the treatment of metastatic castration-resistant prostate cancer (mCRPC) with or without docetaxel-based chemotherapy. Over the past 5 years, a number of attempts were made to determine the efficacy of enzalutamide in...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hong JH

更新日期：2018-03-01 00:00:00

abstract：BACKGROUND:Telmisartan is an orally active angiotensin II receptor antagonist prescribed once daily. OBJECTIVE:To evaluate the efficacy of telmisartan on blood pressure control, and on other end points, when given as monotherapy or in combination. METHODS:Review of published literature. RESULTS:Telmisartan produces ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rosario BH,Hendra TJ

更新日期：2008-04-01 00:00:00

abstract：INTRODUCTION:In vitro genotoxicity assays have a high sensitivity to detect rodent carcinogens, but mammalian cell tests have a propensity for misleading positive results (poor specificity). Recent data show a greater risk of misleading positive results in p53-deficient rodent cell lines than in p53-competent human cel...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Kirkland D

更新日期：2011-12-01 00:00:00

abstract：:Three first-line antituberculosis drugs, isoniazid, rifampicin and pyrazinamide, may induce liver injury, especially isoniazid. This antituberculosis drug-induced liver injury ranges from a mild to severe form, and the associated mortality cases are not rare. The major drug-metabolizing enzyme of isoniazid is N-acetyl...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Huang YS

更新日期：2007-02-01 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:Chronic constipation is a frequent condition often treated pharmacologically. The laxatives available belong to very different pharmacologic groups. AREAS COVERED:This is a short but comprehensive review of the pharmacology, efficacy and safety of currently available laxatives for chronic constipation. Pe...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Müller-Lissner S

更新日期：2013-04-01 00:00:00

abstract：INTRODUCTION:Drug metabolism is one of the most important processes involving a drug after administration. Undesirable pharmacokinetic properties may lead to drug discontinuation. In the past several decades, a number of drugs have been withdrawn from the market due to safety issues caused by metabolites, especially re...

journal_title：Expert opinion on drug metabolism & toxicology

authors： He C,Wan H

更新日期：2018-10-01 00:00:00

abstract：INTRODUCTION:Multiple myeloma (MM) patients who relapse, or become refractory to currently available novel agents, have limited treatment options with poor outcomes. The introductions of the newer proteasome inhibitor carfilzomib and the immunomodulatory agent pomalidomide have provided new treatment strategies within ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gay F,Mina R,Troia R,Bringhen S

更新日期：2013-11-01 00:00:00

abstract：:The pharmaceutical relevance of proton-coupled peptide transporters is currently under intense investigation in many laboratories. Studies have shown that these membrane proteins, expressed in intestine, kidney, choroid plexus and other tissues, accept many peptidomimetic drugs and prodrugs as substrates. The focus of...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Brandsch M

更新日期：2009-08-01 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：:Antithrombotic therapies form the cornerstone of management of acute coronary syndromes (ACS). An ideal antithrombotic agent should reduce ischemic complications while keeping bleeding events to a minimum. Heparins, both unfractionated and low molecular weight, reduce ischemic outcomes but also significantly increase ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Chaturvedi V,Karthikeyan G

更新日期：2009-12-01 00:00:00

abstract：INTRODUCTION:Boceprevir is an NS3/NS4A serine protease inhibitor that was approved for use in Hepatitis C virus (HCV) genotype 1 patients by the US Food and Drug Administration (FDA) in May 2011. The approval of this protease inhibitor marked a major paradigm shift in the treatment of HCV, as it was one of the first of...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Shankar H,Bichoupan K,Dieterich DT

更新日期：2013-12-01 00:00:00

abstract：BACKGROUND:Carboxylesterases (CEs) are ubiquitous enzymes responsible for the hydrolysis of numerous clinically useful drugs. As ester moieties are frequently included in molecules to improve their water solubility and bioavailability, de facto they become substrates for CEs. OBJECTIVE:In this review, we describe the ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hatfield JM,Wierdl M,Wadkins RM,Potter PM

更新日期：2008-09-01 00:00:00

abstract：:Several first-line antihypertensive drugs, including calcium channel blockers, beta-adrenergic blockers and angiotensin receptor blockers, undergo metabolism through different CYP isoforms. As a consequence of CYP-dependent metabolism, wide interindividual variability of plasma concentrations of antihypertensive drugs...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Höcht C,Bertera FM,Mayer MA,Taira CA

更新日期：2010-02-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:many promising targeted agents and combination therapies are being investigated for brain cancer. However, the results from recent clinical trials have been disappointing. A better understanding of the disposition of drug in the brain early in drug development would facilitate appropriate channe...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Blakeley J,Portnow J

更新日期：2010-12-01 00:00:00

abstract：:Introduction: Although the hepatotoxicity of acetaminophen is a well-known problem, the search for reliable biomarker of toxicity is still a current issue as clinical tools are missing to assess patients intoxicated following chronic use, sequential ingestion, use of modified release formulations or in case of delayed...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gloor Y,Schvartz D,F Samer C

更新日期：2019-08-01 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：BACKGROUND:Aerosol administration of therapeutics to the respiratory system represents a significant opportunity for many classes of drugs, both small molecules and macromolecules, including recently engineered peptide and protein therapeutics. However, minimally invasive assessment of drug absorption mechanisms in viv...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sporty JL,Horálková L,Ehrhardt C

更新日期：2008-04-01 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：INTRODUCTION:Various trials have attempted to develop gene expression profiles (GEPs) that may provide a better predictor of clinical outcome over traditional clinicopathological criteria. AREAS COVERED:The review focuses on two main areas: trials examining chemotherapy-induced GEP changes pre- and post-treatment, and...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Tan SH,Lee SC

更新日期：2012-09-01 00:00:00

abstract：INTRODUCTION:Type IV drug hypersensitivity remains an important clinical problem and an obstacle to the development of new drugs. Several forms of drug hypersensitivity are associated with expression of specific HLA alleles. Furthermore, drug-specific T-lymphocytes have been isolated from patients with reactions. Despi...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sullivan A,Watkinson J,Waddington J,Park BK,Naisbitt DJ

更新日期：2018-03-01 00:00:00

abstract：INTRODUCTION:Variations in the human genome sequence sometimes play an important role in pharmacokinetics and/or pharmacodynamics. Previous studies have demonstrated a high degree of variation both between and within different ethnic populations. Areas covered: This review sought to summarize key SNPs in CYP2B6, CYP3A ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Neary M,Owen A

更新日期：2017-11-01 00:00:00

abstract：INTRODUCTION:The association between pregnancy and altered drug pharmacokinetic (PK) properties is acknowledged, as is its impact on drug plasma concentrations and thus therapeutic efficacy. However, there have been few robust PK studies of antimalarial use in pregnancy. Given that inadequate dosing for prevention or t...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Moore BR,Davis TM

更新日期：2020-09-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:The use of the first generation non-nucleoside reverse transcriptase inhibitor efavirenz (EFV) as a component of first-line antiretroviral therapy has been accepted worldwide. EFV is the only antiretroviral agent currently on the market that has been combined with emtricitabine and tenofovir dis...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rakhmanina NY,van den Anker JN

更新日期：2010-01-01 00:00:00

abstract：INTRODUCTION:Luteinizing hormone-releasing hormone agonists such as leuprolide acetate (LA) are the most frequently utilized treatment of advanced prostate cancer as the regimen for achieving androgen deprivation therapy (ADT). The efficacy of LA is determined by extent of testosterone (T) suppression in prostate cance...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Crawford ED,Moul JW,Sartor O,Shore ND

更新日期：2015-01-01 00:00:00