Assays and applications in warfarin metabolism: what we know, how we know it and what we need to know.

abstract：INTRODUCTION:The pharmacokinetic properties of anti-infective drugs are a determinant part of treatment success. Pathogen replication is inhibited if adequate drug levels are achieved in target sites, whereas excessive drug concentrations linked to toxicity are to be avoided. Anti-infective distribution can be predicte...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Moss DM,Marzolini C,Rajoli RK,Siccardi M

更新日期：2015-01-01 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：: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：INTRODUCTION:Membrane transport proteins play a central role in regulating the disposition of endobiotics, dietary nutrients and environmental toxins. The inhibition of transporters by drugs has potential physiologic consequences. The full extent of the effect of drugs on the function of transporters is poorly understo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lepist EI,Ray AS

更新日期：2017-10-01 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：INTRODUCTION:This meeting report presents a brief summary on the 4th Annual Predictive Toxicology Summit 2012, which was held on 15 - 16 February 2012 in London. AREAS COVERED:The majority of presentations came from global pharmaceutical companies, although small and medium enterprise (SME) and academic researchers we...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Cui Z

更新日期：2013-08-01 00:00:00

abstract：BACKGROUND:Anticancer drugs are characterized by a narrow therapeutic window and significant inter-patient variability in therapeutic and toxic effects. Current body surface area (BSA)-based dosing fails to standardize systemic anticancer drug exposure and other alternative dosing strategies also have their limitations...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gao B,Klumpen HJ,Gurney H

更新日期：2008-10-01 00:00:00

abstract：:Rats are an important tool in pharmacology and toxicology. The authors focus on rat P450s in relation to diazepam metabolism. In particular, considerable attention is devoted to the CYP2D subfamily, which is a group of highly polymorphic enzymes. First, the metabolic profiles of diazepam of humans and other animals ar...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sakai N,Ishizuka M

更新日期：2009-11-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Cytochrome (CYP) P450 is a collective name for a very large group of heme enzymes, which catalyze largely oxidative reactions, including those of pharmacological and toxicological importance. Their efficient operation requires coupling of specific electron donor and O(2) consumption and substrat...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Shakunthala N

更新日期：2010-01-01 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：BACKGROUND:Sertindole is a second-generation antipsychotic recently reintroduced in the market for the treatment of schizophrenia after a reevaluation of its risks and benefits. OBJECTIVE:This article provides an overview of the pharmacological properties of sertindole as well as of its efficacy, tolerability and safe...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Spina E,Zoccali R

更新日期：2008-05-01 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：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: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:Mepolizumab is a humanized monoclonal antibody that binds to and inactivates IL-5. It is available as a subcutaneous preparation. The practical application of mepolizumab is as an add-on therapy in the treatment of severe eosinophilic asthma. Areas covered: This article was created from a comprehensive lit...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Kallur L,Gonzalez-Estrada A,Eidelman F,Dimov V

更新日期：2017-12-01 00:00:00

abstract：INTRODUCTION:Picoplatin was developed as platinum coordination complex to overcome development of resistance, through conjugation to thioles, by the introduction of a methyl-pyridine moiety into the cisplatin parent structure. Pharmacokinetic parameters of the drug, after intravenous and oral application, were studied ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hamilton G

更新日期：2013-10-01 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：:Hyperphosphatemia is recognized as a principal mineral disorder in chronic kidney disease (CKD) that leads to the development of secondary hyperparathyroidism. Recent data indicate that hyperphosphatemia is associated with accelerated cardiac calcification and increased mortality in patients with CKD. Control of serum...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Barton Pai A,Conner TA,McQuade CR

更新日期：2009-01-01 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：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:Catechins of green tea extract (GTE) have been associated with the rare risk of hepatotoxicity in a few individuals. As GTE were coadministered with synthetic drugs in some hepatotoxicity cases, uncertainty emerged whether GTE are a risk factor of drug-induced liver injury (DILI). AREAS COVERED:Case repor...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Teschke R,Zhang L,Melzer L,Schulze J,Eickhoff A

更新日期：2014-12-01 00:00:00

abstract：INTRODUCTION:Sumatriptan was developed more than 20 years ago as a 5-HT1B/1D receptor agonist, the first drug in a new class of specific anti-migraine drugs, the triptans. A large amount of information and experience has been gained from the clinical trials undertaken as well the various formulations of sumatriptan use...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Tfelt-Hansen P,Hougaard A

更新日期：2013-01-01 00:00:00

abstract：INTRODUCTION:The elucidation of the toxicological mechanisms of herbal medicines is becoming more and more important with the increasing application of herbal medicines, for treatment of various diseases and the promotion of health. Furthermore, it is widely recognized that as herbal components undergo bioactivation, t...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Fang ZZ,Zhang YY,Wang XL,Cao YF,Huo H,Yang L

更新日期：2011-08-01 00:00:00

abstract：INTRODUCTION:Recent advances in molecular biology have enabled personalized cancer therapies with molecularly targeted agents (MTAs), which offer a promising future for cancer therapy. Dynamic modeling and simulation (M&S) is a powerful mathematical approach linking drug exposures to pharmacological responses, providin...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Yamazaki S,Spilker ME,Vicini P

更新日期：2016-01-01 00:00:00

abstract：INTRODUCTION:The fixed-dose combination of three direct-acting antivirals (DAA), namely sofosbuvir, velpatasvir and voxilaprevir is the first pangenotypic, single tablet regimen developed for the treatment of HCV infection. Areas covered: The pharmacokinetics, pharmacodynamics, efficacy and safety of the co-formulation...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Soriano V,Benítez-Gutiérrez L,Arias A,Carrasco I,Barreiro P,Peña JM,de Mendoza C

更新日期：2017-09-01 00:00:00

abstract：INTRODUCTION:For orally administered drugs, their intestinal absorption and hepatic metabolism are key players for determining a drug's systemic bioavailability and thus therapeutic effect. Drug absorption and metabolism are both complicated processes, with many physicochemical and physiological factors involved. Under...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Alqahtani S,Mohamed LA,Kaddoumi A

更新日期：2013-10-01 00:00:00

abstract：INTRODUCTION:Iron overload is an inevitable consequence of transfusion therapy for a variety of underlying anemias. Iron overload, without effective chelation, will lead to significant morbidity and mortality. Deferasirox (Exjade®) is an oral tridentate iron chelator used for reducing iron overload. AREAS COVERED:In a...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Galanello R,Campus S,Origa R

更新日期：2012-01-01 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：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 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