Role of membrane transporters in the safety profile of drugs.

abstract：:Luminogenic cytochrome P450 (CYP) assays couple CYP enzyme activity to firefly luciferase luminescence in a technology called P450-Glo(TM) (Promega). Luminogenic substrates are used in assays of human CYP1A1, -1A2, -1B1, -2C8, -2C9, -2C19, -2D6, -2J2, -3A4, -3A7, -4A11, -4F3B, -4F12 and -19. The assays detect dose-dep...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Cali JJ,Ma D,Sobol M,Simpson DJ,Frackman S,Good TD,Daily WJ,Liu D

更新日期：2006-08-01 00:00:00

abstract：INTRODUCTION:Adverse drug reactions with an immune pathogenesis are a problem in the clinic and an impediment to drug development. T lymphocytes are believed to play a role in the pathogenesis; however, the nature of the drug interaction with immune receptors remains an area of debate. AREAS COVERED:This article revie...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sullivan A,Gibson A,Park BK,Naisbitt DJ

更新日期：2015-03-01 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:Lenalidomide is an oral immunomodulatory drug, which was recently introduced for the treatment of multiple myeloma (MM). It has been used for the treatment of newly diagnosed and relapsed MM patients, as both maintenance and preventive therapy. Available data show a progression-free survival and overall su...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Bringhen S,Gay F,Pautasso C,Cerrato C,Boccadoro M,Palumbo A

更新日期：2012-09-01 00:00:00

abstract：INTRODUCTION:Extensive within-population variability is the essence of neonatal pharmacology. Despite this, infants remain one of the last therapeutic orphans. Together with additional legal initiatives, tailoring of already available tools (modeling, covariates, pharmacovigilance) may significantly improve pharmacothe...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Allegaert K

更新日期：2014-08-01 00:00:00

abstract：INTRODUCTION:Type 2 diabetes often involves derangements in lipid levels in addition to insulin resistance and diminishing insulin secretion. Colesevelam hydrochloride, a bile acid sequestrant (BAS), is approved for adjunctive therapy to diet and exercise for glycemic control in type 2 diabetes. In clinical studies in ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Younk LM,Davis SN

更新日期：2012-04-01 00:00:00

abstract：BACKGROUND:Testosterone replacement therapy in hypogonadal men has been used for > 60 years. The use of testosterone substitution is continuously growing and is given to aging men to improve the quality of life. Because testosterone use is associated with muscle strength enhancing effects, it has become a popular drug ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Schulze JJ,Rane A,Ekström L

更新日期：2009-07-01 00:00:00

abstract：INTRODUCTION:Whereas in the past, (Q)SAR methods have been largely used to support the design of new drugs, in the last few decades, there has been a new interest in its applications for the assessment of drug safety. In particular, the ICH M7 guideline has introduced the concept that (Q)SAR predictions for the Ames mu...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Benigni R,Bassan A,Pavan M

更新日期：2020-08-01 00:00:00

abstract：INTRODUCTION:Gut microbiota plays critical roles in drug metabolism. The variation of gut microbiota contributes to the interindividual differences toward drug therapy including drug-induced toxicity and efficacy. Accordingly, the investigation and elucidation of gut microbial impacts on drug metabolism and toxicity wi...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Li H,He J,Jia W

更新日期：2016-01-01 00:00:00

abstract：INTRODUCTION:Pemphigus is an autoimmune blistering disease of the skin and mucous membranes characterized by the development of autoantibodies against the desmosomal proteins, desmoglein-1 and -3. Before the advent of corticosteroids, therapy was almost fatal. The introduction of high-dose corticosteroid therapy has re...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Doukaki S,Pistone G,Aricò M,Bongiorno MR

更新日期：2011-02-01 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：: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：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：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:Idiosyncratic drug-induced agranulocytosis (IDIAG) is a life-threatening adverse reaction characterized by an absolute neutrophil count < 500 cells/μl of blood. It shares many of the characteristics of other idiosyncratic drug reactions (IDRs), and this presumably reflects mechanistic similarities. AREAS ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Johnston A,Uetrecht J

更新日期：2015-02-01 00:00:00

abstract：BACKGROUND:The intestinal epithelial membrane expresses ATP-binding cassette (ABC) transporters such as P-glycoprotein (P-gp), multi-drug resistance-associated proteins (MRPs) and breast cancer resistance protein (BCRP), in addition to various solute carrier (SLC) transporters. These ABC transporters affect the oral bi...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Murakami T,Takano M

更新日期：2008-07-01 00:00:00

abstract：:Introduction: Graft-versus-host disease (GVHD) is the most common complication of hematopoietic stem cell transplantation (HSCT); therefore, the prevention of GVHD is important for a successful treatment. Tacrolimus (Tac), a calcineurin inhibitor, has been widely used for the prophylaxis of GVHD in HSCT recipients. Ar...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gao Y,Ma J

更新日期：2019-10-01 00:00:00

abstract：:The human ether-a-go-go-related gene (hERG) encodes the pore-forming alpha-subunit of a voltage-gated potassium (K(+)) channel. A variety of unrelated compounds reduce K(+ )current in the heart by blocking the pore or disrupting trafficking of the hERG channel to the membrane surface. This induces a syndrome known as ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Stansfeld PJ,Sutcliffe MJ,Mitcheson JS

更新日期：2006-02-01 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：:Introduction: In quantitative modeling, the resolving of underpredictions and overpredictions of hepatic clearance (CLh) makes a top priority for pharmacokinetic modelers. Clearly, the 'protein-mediated hepatic uptake' is a violation of 'the free drug hypothesis', but the lack of its consideration in CLh-predictive ap...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Bteich M,Poulin P,Haddad S

更新日期：2019-08-01 00:00:00

abstract：INTRODUCTION:Patients with gout often have comorbid conditions such as renal failure, cardiovascular disease and metabolic syndrome. The presence and required treatment of these conditions can make the treatment of gout challenging. Knowledge of the pharmacokinetics of the available drugs for the management of gout is ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Richette P,Frazier A,Bardin T

更新日期：2014-07-01 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:Epilepsy is a chronic neurological disease manifesting as recurrent seizures. Despite the availability of numerous antiepileptic drugs (AEDs), one-third of the patients are not responsive to treatment. Such inter-individual variability in the response to AEDs may be partly explained by genetic differences....

journal_title：Expert opinion on drug metabolism & toxicology

authors： Piana C,Antunes Nde J,Della Pasqua O

更新日期：2014-03-01 00:00:00

abstract：INTRODUCTION:Neonatal patients, because of the inability of their immune system to properly respond to microbial challenge, are highly susceptible to viral infections. Immunoglobulins, monoclonal antibody and antiviral drugs are used for prophylaxis and treatment of viral diseases in neonates. Neonates and, especially,...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Enioutina EY,Constance JE,Stockmann C,Linakis MW,Yu T,Rower JE,Balch AH,Sherwin CM

更新日期：2015-01-01 00:00:00

abstract：:The past decade has seen an increase in therapeutic options for Alzheimer's disease (AD) that target neurotransmitters, such as acetylcholine, and research continues to target abnormal proteins in the AD brain. Recently, glutamate excitotoxicity has also become a target for AD treatment with the advent of memantine. C...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Schmitt F,Ryan M,Cooper G

更新日期：2007-02-01 00:00:00

abstract：:Acetaminophen (APAP) hepatotoxicity is currently the single most important cause of acute liver failure in the US, and is associated with a significant number of deaths. The toxic response to APAP is triggered by a highly reactive metabolite N-acetyl-p-benzoquinone-imine. Following the hepatocellular initiation events...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Liu ZX,Kaplowitz N

更新日期：2006-08-01 00:00:00

abstract：BACKGROUND:The aim of the study was to evaluate the bioequivalence of two itraconazole 100 mg capsule formulations. RESEARCH DESIGN AND METHODS:The single-center, open-label, randomized, three-period, three-sequence, reference-replicated, cross-over study included 38 healthy subjects under fed conditions. In each stud...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Dragojević-Simić V,Kovačević A,Jaćević V,Rančić N,Djordjević S,Kilibarda V,Mikov M,Bokonjić D

更新日期：2018-09-01 00:00:00

abstract：:Pathologists play a central role in the recognition and prevention of drug-induced toxicity. Pathologists engaged in clinical practice must identify a pattern of histological lesions that are interpreted in concert with a variety of clinical data to determine the probability of drug-induced toxicity versus background ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Cullen JM,Miller RT

更新日期：2006-04-01 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：INTRODUCTION:Small molecule tyrosine and serine-threonine kinase inhibitors (TKIs and STKIs) are emerging drugs that interfere with downstream signaling pathways involved in cancer proliferation, invasion, metastasis and angiogenesis. The understanding of their pharmacokinetics, the identification of their transporters...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Da Silva CG,Honeywell RJ,Dekker H,Peters GJ

更新日期：2015-05-01 00:00:00