Intestinal efflux transporters and drug absorption.

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: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: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:Oral mucositis, one of the major side effects of chemotherapy and irradiation, is still a burden of modern oncology. The keratinocyte growth factor (KGF) palifermin has been approved as a new, targeted therapy for the prevention of severe oral mucositis. AREAS COVERED:The authors review the literature on ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Weigelt C,Haas R,Kobbe G

更新日期：2011-04-01 00:00:00

abstract：INTRODUCTION:Due to their multiple effects, glucocorticoids (GCs) have versatile medical uses. They can regulate many xenobiotic-metabolizing enzymes of the cytochrome P450 (CYP) superfamily, and thus, influence pharmacotherapy. AREAS COVERED:The aim of this paper is to summarize the molecular effects of GCs on CYP as...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Matoulková P,Pávek P,Malý J,Vlček J

更新日期：2014-03-01 00:00:00

abstract：:Acute kidney injury is a common condition and is associated with a high mortality rate. It has been recognised that routinely used measures of renal function, such as levels of blood urea nitrogen and serum creatinine, increase significantly only after substantial kidney injury occurs and then with a time delay. Insen...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Vaidya VS,Bonventre JV

更新日期：2006-10-01 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: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：INTRODUCTION:Drug-induced cholestasis, intrahepatic cholestasis of pregnancy and viral hepatitis are acquired forms of liver disease. Cholestasis is a pathophysiologic state with impaired bile formation and subsequent accumulation of bile salts in hepatocytes. The bile salt export pump (BSEP) (ABCB11) is the key export...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Stieger B,Geier A

更新日期：2011-04-01 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:Multiple myeloma (MM) patients who relapse, or become refractory to currently available novel agents, have limited treatment options with poor outcomes. The introductions of the newer proteasome inhibitor carfilzomib and the immunomodulatory agent pomalidomide have provided new treatment strategies within ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gay F,Mina R,Troia R,Bringhen S

更新日期：2013-11-01 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: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:Mortality from invasive fungal disease involving the central nervous system (CNS) is excessive. Achieving therapeutic drug concentrations at the site of infection within the CNS is always difficult and its evaluation is complex due to anatomical barriers and variable pathophysiological lesions. Areas cover...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Stott KE,Hope W

更新日期：2018-08-01 00:00:00

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:Peripheral T-cell lymphomas (PTCLs) are a heterogeneous group of T-cell neoplasms. Most patients with PTCL have a poor outcome with conventional therapies and are not cured without stem-cell transplantation. Pralatrexate, a novel antifolate chemotherapeutic agent, was rationally designed to impede folate m...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Foss FM

更新日期：2011-09-01 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: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：:Antithrombotic therapy is a crucial component of interventional cardiology and currently involves the administration of both anticoagulant and antiplatelet agents. The implementation of standard dual or triple antiplatelet therapies has allowed percutaneous coronary intervention (PCI) with stent implantation to become...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Ahrens I,Smith BK,Bode C,Peter K

更新日期：2007-08-01 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：: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:It is widely accepted that current practice of polypharmacy inevitably increases the incidence of drug-drug interactions (DDIs). Serious DDIs are a major liability for new molecular entities entering the pharmaceutical market. Various strategies are employed to avoid problematic compounds for clinical deve...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Riley RJ,Wilson CE

更新日期：2015-04-01 00:00:00

abstract：BACKGROUND:5-Aminosalicylate (5-ASA) agents are the mainstay of oral therapy for ulcerative colitis (UC). Balsalazide, a prodrug of 5-ASA, has recently been approved for the treatment of UC. OBJECTIVE:To summarize current data on balsalazide and to discuss its impact on management of UC. METHODS:A systematic review o...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Wiggins JB,Rajapakse R

更新日期：2009-10-01 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:If a drug is found to be an inducer of hepatic drug metabolizing enzymes via activation of nuclear receptors such as pregnane X receptor (PXR) or constitutive androstane receptor (CAR), it is likely that drug transporters regulated through these same receptors will be induced as well. This review highlight...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Amacher DE

更新日期：2016-12-01 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：: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: Overactive bladder (OAB) has a heterogeneous presentation that varies between individuals and by gender. Treatment with antimuscarinic medications is standard first line pharmacotherapy for most patients with OAB. However, gender specific differences in the pharmacokinetics and pharmacodynamics of antimu...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hartigan SM,Dmochowski RR

更新日期：2020-02-01 00:00:00

abstract：INTRODUCTION:Cardiovascular disease is still the leading cause of death worldwide. There are many environmental and genetic factors that play a role in the development of cardiovascular disease. The treatment of cardiovascular disease is beginning to move in the direction of personalized medicine by using biomarkers fr...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Berinstein E,Levy A

更新日期：2017-09-01 00:00:00

abstract：INTRODUCTION:Cervical cancer is the second-most common malignancy in women worldwide. Cisplatin was introduced as a radiosensitizer in 1999 to improve chances of survival. Tumor cell hypoxia, however, remains a major limiting factor in the treatment of solid tumors with chemotherapy and radiation. There has since been ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Ghatage P,Sabagh H

更新日期：2012-12-01 00:00:00