Experimental models for predicting drug absorption and metabolism.

abstract：INTRODUCTION:Pemphigus is an autoimmune blistering disease of the skin and mucous membranes characterized by the development of autoantibodies against the desmosomal proteins, desmoglein-1 and -3. Before the advent of corticosteroids, therapy was almost fatal. The introduction of high-dose corticosteroid therapy has re...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Doukaki S,Pistone G,Aricò M,Bongiorno MR

更新日期：2011-02-01 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：: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:In preliminary clinical studies, aleglitazar, a new dual PPAR-α-γ agonist, has been demonstrated to improve hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus. This review will provide up-to-date information on the clinical safety and efficacy of aleglitazar, which is currently under ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Younk LM,Uhl L,Davis SN

更新日期：2011-06-01 00:00:00

abstract：INTRODUCTION:Type 2 diabetes often involves derangements in lipid levels in addition to insulin resistance and diminishing insulin secretion. Colesevelam hydrochloride, a bile acid sequestrant (BAS), is approved for adjunctive therapy to diet and exercise for glycemic control in type 2 diabetes. In clinical studies in ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Younk LM,Davis SN

更新日期：2012-04-01 00:00:00

abstract：INTRODUCTION:Pregabalin is an alternative compound to SSRIs and SNRIs for the first-line treatment of generalized anxiety disorder (GAD). Areas covered: We describe the pharmacokinetic properties of pregabalin and their implications for the treatment of GAD. A search in the main database sources (Medline, ISI, Web of K...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Buoli M,Caldiroli A,Serati M

更新日期：2017-03-01 00:00:00

abstract：INTRODUCTION:Patients with gout often have comorbid conditions such as renal failure, cardiovascular disease and metabolic syndrome. The presence and required treatment of these conditions can make the treatment of gout challenging. Knowledge of the pharmacokinetics of the available drugs for the management of gout is ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Richette P,Frazier A,Bardin T

更新日期：2014-07-01 00:00:00

abstract：BACKGROUND:Testosterone replacement therapy in hypogonadal men has been used for > 60 years. The use of testosterone substitution is continuously growing and is given to aging men to improve the quality of life. Because testosterone use is associated with muscle strength enhancing effects, it has become a popular drug ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Schulze JJ,Rane A,Ekström L

更新日期：2009-07-01 00:00:00

abstract：BACKGROUND:The aim of the study was to evaluate the bioequivalence of two itraconazole 100 mg capsule formulations. RESEARCH DESIGN AND METHODS:The single-center, open-label, randomized, three-period, three-sequence, reference-replicated, cross-over study included 38 healthy subjects under fed conditions. In each stud...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Dragojević-Simić V,Kovačević A,Jaćević V,Rančić N,Djordjević S,Kilibarda V,Mikov M,Bokonjić D

更新日期：2018-09-01 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：: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:Drug-disease interactions include the impact of a drug and a particular disease condition on each other. However, the current practice in addressing drug-disease interaction is unbalanced and mostly limited to how the drug worsens the disease or health condition. AREAS COVERED:Aspirin and gastric ulcer in...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Nwose EU,Yee KC

更新日期：2016-09-01 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: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: 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

abstract：:In adapting to the challenge to make more informed selection of compounds for development, the pharmaceutical industry is increasingly embracing the application of mechanism-based models and prediction tools for prediction of pharmacokinetic parameters. This review first outlines the concepts and application of the ma...

journal_title：Expert opinion on drug metabolism & toxicology

authors： De Buck SS,Mackie CE

更新日期：2007-12-01 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:Drug metabolism is one of the most important processes involving a drug after administration. Undesirable pharmacokinetic properties may lead to drug discontinuation. In the past several decades, a number of drugs have been withdrawn from the market due to safety issues caused by metabolites, especially re...

journal_title：Expert opinion on drug metabolism & toxicology

authors： He C,Wan H

更新日期：2018-10-01 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: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：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:Despite initial patient benefit, drug resistance to first-generation EGFR tyrosine kinase inhibitors (TKIs) is inevitable. One of the key mechanisms responsible for the development of acquired drug resistance is the secondary T790M missense mutation in exon 20 of the EGFR kinase domain. Afatinib is an ATP-...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Yap TA,Popat S

更新日期：2013-11-01 00:00:00

abstract：INTRODUCTION:Bioaccessibility is a growing area of research in the field of risk assessment. As polycyclic aromatic hydrocarbons (PAHs) are ubiquitous environmental pollutants, they are the toxicants of focus to establish cancer risks in humans. Orally ingested PAHs also cause toxicity and even affect the pharmacokinet...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Harris KL,Banks LD,Mantey JA,Huderson AC,Ramesh A

更新日期：2013-11-01 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：: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: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: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: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:The absorption, distribution, metabolism, excretion and toxicity (ADME-tox) processes of drugs are of importance and require preclinical investigation intestine in addition to the liver. Various models have been developed for prediction of ADME-tox in the intestine. In this review, precision-cut intestinal...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Li M,de Graaf IA,Groothuis GM

更新日期：2016-01-01 00:00:00