Cytochrome P450 time-dependent inhibition and induction: advances in assays, risk analysis and modelling.

abstract：INTRODUCTION:Although naturally occurring peptides have been widely used as drugs, their rapid in vivo degradation by proteolysis and their interactions at multiple receptors are part of the reason for the limitation of their clinical applications. AREAS COVERED:This paper reviews peptide-metabolizing enzymes in the b...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Pernot M,Vanderesse R,Frochot C,Guillemin F,Barberi-Heyob M

更新日期：2011-07-01 00:00:00

abstract：INTRODUCTION:Nucleosidic analogs such as pyrimidine and purine derivatives are mainstay in the field of treating cancers, both in adults and in children. All these drugs act as antimetabolite compounds, that is, they interfere with the ability of cancer cells to synthesize the nucleosides or the nucleotides necessary f...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Serdjebi C,Milano G,Ciccolini J

更新日期：2015-05-01 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：:With the progressive ageing of the population, an increasing number of elderly patients are being exposed to multiple drugs because of co-existing morbidity states requiring pharmacological management. However, the knowledge of the effects of ageing on the pharmacokinetics and pharmacodynamics of individual drugs is f...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Mangoni AA

更新日期：2007-06-01 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: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: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: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

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: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: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：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:Epigenetics is a rapidly growing field describing heritable alterations in gene expression that do not involve DNA sequence variations. Advances in epigenetics and epigenomics have influenced pharmacology, leading to the development of a new specialty, pharmacoepigenetics, the study of the epigenetic basis...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Majchrzak-Celińska A,Baer-Dubowska W

更新日期：2017-04-01 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：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：IMPORTANCE OF THE FIELD:The prevalence of acute renal allograft rejection has decreased substantially in past decades due to new and more specific immunosuppressive compounds but improvements in long-term graft function have not been achieved. There is a large need for new immunosuppressive agents that lack toxicity of...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Matz M,Naik M,Mashreghi MF,Glander P,Neumayer HH,Budde K

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:The importance of transporters in drug disposition and response has led to increasing interest in genetic variations and expression differences of their genes. OBJECTIVE:This review summarizes: i) genetic variations in transporters and associated drug response; and ii) a pharmacogenomic approach to correlat...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Huang Y,Penchala S,Pham AN,Wang J

更新日期：2008-03-01 00:00:00

abstract：BACKGROUND:Obesity, hypertension and Type 2 diabetes are major contributing factors to the increase in the number of patients that have chronic kidney disease. The clustering of visceral obesity and cardiovascular risk factors has been designated metabolic syndrome or cardiometabolic syndrome. Cardiometabolic syndrome ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Imig JD

更新日期：2008-02-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:genetic and pharmacologically-driven variations in common mechanisms involved in the disposition of antidepressant medications may contribute to variable interpatient response. This review describes the pharmacological properties underlying the safety and efficacy of desvenlafaxine, a second-gen...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Nichols AI,Tourian KA,Tse SY,Paul J

更新日期：2010-12-01 00:00:00

abstract：:Introduction: Chemokine receptors are important therapeutic targets for the treatment of many human diseases. This study will provide an overview of approved chemokine receptor antagonists and promising candidates in advanced clinical trials.Areas covered: We will describe clinical aspects of chemokine receptor antago...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Miao M,De Clercq E,Li G

更新日期：2020-01-01 00:00:00

abstract：:Valproate (2-propylpentanoate) is available as valproic acid, sodium valproate and semisodium valproate. It has actions on dopamine, GABA and glutamate neurotransmission and intracellular signaling. Its main psychiatric use is to treat bipolar disorder. It has been used in other psychiatric disorders, including schizo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Haddad PM,Das A,Ashfaq M,Wieck A

更新日期：2009-05-01 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：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: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：BACKGROUND:The number of patients eligible for cardiovascular therapies in general is forecast to increase substantially in the coming decades. However, the current list of potential future cardiovascular blockbuster drugs is alarmingly short. There is thus a clear need for innovative strategies to increase the efficie...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Jänis MT,Laaksonen R,Oresic M

更新日期：2008-06-01 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：: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：: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：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: 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