Ezetimibe: an update on the mechanism of action, pharmacokinetics and recent clinical trials.

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：: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:Within recent years, glucagon-like peptide 1 receptor agonists (GLP-1-RA) have emerged as a new treatment option for type 2 diabetes. The GLP-1-RA are administered subcutaneously and differ substantially in pharmacokinetic profiles. AREAS COVERED:This review describes the pharmacokinetics and safety aspec...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Jespersen MJ,Knop FK,Christensen M

更新日期：2013-01-01 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：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: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: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：INTRODUCTION:Integration of targeted therapy and additional chemotherapy options has improved median overall survival (OS) in patients with unresectable metastatic colorectal cancer (mCRC). Cetuximab and panitumumab are examples of targeted therapies, specifically against the epidermal growth factor receptor (EGFR). Th...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lo L,Patel D,Townsend AR,Price TJ

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：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: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：: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: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:Approaches aiming to model the time course of tumor growth and tumor growth inhibition following a therapeutic intervention have recently been proposed for supporting decision making in oncology drug development. When considered in a comprehensive model-based approach, tumor growth can be included in the c...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Bernard A,Kimko H,Mital D,Poggesi I

更新日期：2012-09-01 00:00:00

abstract：:Psychiatric disorders are a leading cause of disability worldwide and despite significant pharmacologic advances, often remain difficult to diagnose correctly and treat fully. Factors which contribute to these difficulties include imprecise understanding of etiology, syndromal nature of many disorders and overlap in d...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lombard J,Doraiswamy PM

更新日期：2013-01-01 00:00:00

abstract：INTRODUCTION:The availability of non-vitamin K antagonist oral anti-coagulants alongside vitamin K antagonists has offered a variety of options for anti-coagulation, but has also necessitated a good understanding of the pharmacological properties of each of these drugs prior to their use, to maximise the therapeutic be...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Fawzy AM,Lip GYH

更新日期：2019-05-01 00:00:00

abstract：INTRODUCTION:Immunosuppressive drugs have a narrow therapeutic range and large inter-individual response variability. This has prompted pharmacogenetic studies, mostly with regard to their dose-concentration relationships, but also about proteins involved in their pharmacodynamics. Some polymorphisms of genes involved ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Picard N,Marquet P

更新日期：2011-06-01 00:00:00

abstract：:There is an increasing recognition within the pharmaceutical industry of the importance of the ADME studies in drug registration. Consequently, there has been a drive in recent times to conduct the ADME studies as early as possible in the development programme. There are, however, regulatory barriers, particularly in ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lappin G,Garner RC

更新日期：2005-06-01 00:00:00

abstract：INTRODUCTION:There are profound changes that take place in drug metabolism enzymes during fetal and postnatal development. These changes may significantly impact drug therapy in children. AREAS COVERED:A combination of focused and comprehensive literature searches using PubMed and reference lists (from inception to 7 ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： de Wildt SN

更新日期：2011-08-01 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: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:Pharmacokinetic and pharmacodynamic drug interactions (DIs) can occur between antiepileptics (AEDs) and second-generation antipsychotics (SGAPs). Some AED and SGAP pharmacodynamic mechanisms are poorly understood. AED-SGAP combinations are used for treating comorbid illnesses or increasing efficacy, partic...

journal_title：Expert opinion on drug metabolism & toxicology

authors： de Leon J,Santoro V,D'Arrigo C,Spina E

更新日期：2012-03-01 00:00:00

abstract：OBJECTIVE:The objectives of this study are to characterize capsaicin glucuronidation using liver microsomes and to determine the contribution of individual UDP-glucuronosyltransferase (UGT) enzymes to hepatic glucuronidation of capsaicin. METHODS:The rates of glucuronidation were determined by incubating capsaicin wit...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sun H,Wang H,Liu H,Zhang X,Wu B

更新日期：2014-10-01 00:00:00

abstract：INTRODUCTION:Topotecan was initially approved for the treatment of recurrent ovarian cancer. In cervical cancer, it has been investigated for its potential as part of systemic therapy for advanced and/or recurrent disease and in combination with cisplatin and radiation as a first-line treatment for advanced disease. As...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Musa F,Blank S,Muggia F

更新日期：2013-02-01 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：INTRODUCTION:A more concentrated insulin glargine formulation, containing 300 U/mL (Gla-300) was approved in 2015 in the US and Europe for the treatment of diabetes mellitus in adults. AREAS COVERED:This drug evaluation focuses on the pharmacokinetics (PK) and pharmacodynamics (PD) of Gla-300 from studies published up...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Owens DR

更新日期：2016-08-01 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：:It has increasingly been recognized that few molecules move across the cell membrane without the assistance of transporter proteins. Large superfamilies of transporter proteins have been identified in every living cell, including microorganisms and mitochondria. This report reviews the role of transporters in physiolo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lee EJ,Lean CB,Limenta LM

更新日期：2009-11-01 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