Transport of drugs by proton-coupled peptide transporters: pearls and pitfalls.

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：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：: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：INTRODUCTION:Arterial and venous thrombotic states, including myocardial infarction (MI), stroke and deep vein thrombosis with subsequent pulmonary embolism, are a significant cause of cardiovascular mortality and morbidity. Factor Xa (FXa) plays a pivotal role in thrombus formation. Its inhibition following acute coro...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gopalakrishnan L,Kumar V,Kohli P,Singh P,Rastogi U,Gibson CM

更新日期：2012-07-01 00:00:00

abstract：INTRODUCTION:Capecitabine , an oral prodrug of 5-fluorouracil (5-FU), is adsorbed in its intact form through the intestine and metabolized to 5-FU in tumour cells. In metastatic breast cancer (MBC), capecitabine is an effective and well-tolerated therapeutic option both in monotherapy and in combination with chemothera...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Daniele G,Gallo M,Piccirillo MC,Giordano P,D'Alessio A,Del Giudice A,La Porta ML,Perrone F,Normanno N,De Luca A

更新日期：2013-02-01 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：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:Telaprevir is one of the first direct-acting antiviral drugs approved for the treatment of the hepatitis C virus (HCV) genotype 1. Following its approval in 2011, new data regarding the pharmacokinetics and pharmacodynamics were reported, leading to important clinical applications. AREAS COVERED:This arti...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rivero-Juarez A,Camacho A,Rivero A

更新日期：2015-07-01 00:00:00

abstract：INTRODUCTION:DNA damaging drugs are widely used for the chemotherapeutic treatment of high-grade osteosarcoma (HGOS). In HGOS patients, several germline polymorphisms have been reported to impact on the development of adverse toxic events related to DNA damaging drugs treatment. Some of these polymorphisms, when presen...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hattinger CM,Patrizio MP,Luppi S,Magagnoli F,Picci P,Serra M

更新日期：2019-04-01 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：: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:Medullary thyroid carcinoma (MTC) is a rare endocrine malignancy accounting for a significant percentage of thyroid cancer-related fatal events. Traditional treatment modalities used in the other types of thyroid carcinomas have been proved largely ineffective in advanced MTC. Better understanding of the m...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Karras S,Anagnostis P,Krassas GE

更新日期：2014-03-01 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: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

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：BACKGROUND:Cytochrome P450 2E1 (CYP2E1) plays a central role in the metabolism and metabolic activation of a large number of small, mostly xenobiotic compounds. These qualities distinguish CYP2E1 from traditional enzymes and pose significant challenges to understanding the role and consequences of CYP2E1-mediated metab...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Miller GP

更新日期：2008-08-01 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:Treatments for hepatitis C virus (HCV) infection have advanced rapidly in the last decade. Pegylated interferon alpha 2a (PEG-IFN alpha 2a) alone, in combination with ribavirin and with or without direct acting antivirals (DAAs) is modestly effective in the treatment of chronic HCV infection. Areas covered...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Maughan A,Ogbuagu O

更新日期：2018-02-01 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:. Membrane transporters are integral to the maintenance of cellular integrity of all tissue and cell types. While transporters play an established role in the systemic pharmacokinetics of therapeutic drugs, tissue specific expression of uptake transporters can serve as an initiating mechanism that governs ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Huang KM,Uddin ME,DiGiacomo D,Lustberg MB,Hu S,Sparreboom A

更新日期：2020-06-01 00:00:00

abstract：:Changes in mammalian diets alter the hepatic expression of CYP drug-metabolising enzymes and endobiotic oxidases. Thus, dietary constituents may significantly influence the duration of action of chemicals in tissues. Recent improvements in the mechanistic information on the regulation of constitutive and inducible exp...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Murray M

更新日期：2007-04-01 00:00:00

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:Sesamin is a major lignan found in sesame and is known to have various biological effects. Some of these biological effects occur following its metabolic conversion to corresponding catechols and, therefore, the study of sesamin metabolism is quite important. There is currently a need to identify the enzym...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Yasuda K,Sakaki T

更新日期：2012-01-01 00:00:00

abstract：INTRODUCTION:First- and second-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), such as gefitinib, erlotinib, icotinib, and afatinib are the standard-of-care for first-line therapy of non-small-cell lung cancer (NSCLC) harboring activating EGFR mutations. Unfortunately, after initial ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rossi A,Muscarella LA,Di Micco C,Carbonelli C,D'alessandro V,Notarangelo S,Palomba G,Sanpaolo G,Taurchini M,Graziano P,Maiello E

更新日期：2017-12-01 00:00:00

abstract：INTRODUCTION:The key feature of the newborn is its fast age-dependent maturation, resulting in extensive variability in pharmacokinetics and -dynamics, further aggravated by newly emerging covariates like treatment modalities, environmental issues or pharmacogenetics. This makes clinical research in neonates relevant a...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Samardzic J,Turner MA,Bax R,Allegaert K

更新日期：2015-07-01 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：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:Emtricitabine/tenofovir disoproxil fumarate fixed-dose combination (FTC/TDF FDC) is the co-formulation of a nucleoside and a nucleotide, respectively. After oral administration, both drugs exhibit plasma and intracellular half-lives suitable for once-daily dosing. Within the host cells, active metabolites ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Uglietti A,Zanaboni D,Gnarini M,Maserati R

更新日期：2012-10-01 00:00:00

abstract：:Introduction: The target concentration strategy uses PKPD information for dose determination. Models have also quantified exposure-response relationships, improved understanding of developmental pharmacokinetics, rationalized dose prescription, provided insight into the importance of covariate information, explained d...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Anderson BJ,Morse JD,Hannam JA,Cortinez LI

更新日期：2020-04-01 00:00:00

abstract：INTRODUCTION:Over the past decade, zebrafish have been tasked to play important roles from modeling human diseases to finding cures for them. Inadvertently, these fish now find themselves swimming along the drug development pipeline. A number of studies have been conducted to see if these small fish are up to the task ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sukardi H,Chng HT,Chan EC,Gong Z,Lam SH

更新日期：2011-05-01 00:00:00