Physicochemical properties of novel protein kinase inhibitors in relation to their substrate specificity for drug transporters.

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：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: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:First- and second-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), such as gefitinib, erlotinib, icotinib, and afatinib are the standard-of-care for first-line therapy of non-small-cell lung cancer (NSCLC) harboring activating EGFR mutations. Unfortunately, after initial ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rossi A,Muscarella LA,Di Micco C,Carbonelli C,D'alessandro V,Notarangelo S,Palomba G,Sanpaolo G,Taurchini M,Graziano P,Maiello E

更新日期：2017-12-01 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: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：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：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：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:Medication of pregnant women is increasingly common in developed countries. Several placental drug transporters have been shown to transfer their substrates from the trophoblast back to the maternal circulation, thus hindering the transplacental passage of xenobiotics and protecting the fetus. However, the...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Staud F,Ceckova M

更新日期：2015-04-01 00:00:00

abstract：INTRODUCTION:Organic anion transporting polypeptide (OATP) uptake transporters are important for the disposition of many drugs and perturbed OATP activity can contribute to adverse drug reactions (ADRs). It is well documented that both genetic and environmental factors can alter OATP expression and activity. Genetic fa...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Clarke JD,Cherrington NJ

更新日期：2012-03-01 00:00:00

abstract：:The interaction between drug-metabolising enzymes and active transporters is an emerging concept in pharmacokinetics. In the gut mucosa, P-glycoprotein and cytochrome P450 (CYP)3A functionally interact in three ways: i) drugs are repeatedly taken up and pumped out of the enterocytes by P-glycoprotein, thus increasing ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Christians U,Schmitz V,Haschke M

更新日期：2005-12-01 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:Adverse drug reactions with an immune pathogenesis are a problem in the clinic and an impediment to drug development. T lymphocytes are believed to play a role in the pathogenesis; however, the nature of the drug interaction with immune receptors remains an area of debate. AREAS COVERED:This article revie...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sullivan A,Gibson A,Park BK,Naisbitt DJ

更新日期：2015-03-01 00:00:00

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：INTRODUCTION:Unacceptable failure rates in clinical trials are largely responsible for the high costs of bringing successful drugs to market - costs that are passed on to patients, insurers or healthcare providers. Furthermore, failures in clinical trials deny patients much-needed new drugs and potentially expose them ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Clotworthy M,Archibald K

更新日期：2013-09-01 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：: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 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:Golimumab is a human anti-TNF monoclonal antibody that was derived from human antibody-transgenic mice. Golimumab demonstrated meaningful clinical benefit and tolerable safety in patients with active rheumatoid arthritis (RA) who were methotrexate (MTX)-naïve, or who inadequately responded to MTX or who ha...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Tanaka Y,Senoo A,Fujii H,Baker D

更新日期：2016-01-01 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：: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: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:multiple myeloma (MM) is a plasma cell disorder that represents the second most frequent hematologic cancer. Although MM is still an incurable disease, prognosis has improved in the last decades thanks to the introduction of novel agents such as proteasome inhibitors (PIs), immunomodulatory drugs, monoclon...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Salvini M,Troia R,Giudice D,Pautasso C,Boccadoro M,Larocca A

更新日期：2018-01-01 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: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：INTRODUCTION:Obesity is an epidemic associated with significant morbidity. Lorcaserin , a novel serotonin 2C receptor antagonist, was recently approved as an adjunct to lifestyle modification for long-term weight loss and maintenance. Clinical studies in patients without diabetes demonstrated 5.8% mean weight loss from...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Berlie HD,Hurren KM

更新日期：2013-08-01 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:Chronic low back pain (CLBP) is a common and difficult illness to manage. Some individuals with CLBP have pain processing disorders and are also at risk for opioid abuse, misuse; addiction and diversion. Guidelines have been published to guide management; neuromodulation, exercise, mindfulness-based stress...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Davis MP

更新日期：2016-07-01 00:00:00

abstract：INTRODUCTION:Mathematical models of dermal transport offer the advantages of being much faster and less expensive than in vitro or in vivo studies. The number of methods used to create such models has been increasing rapidly, probably due to the steady rise in computational power. Although each of the various approache...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Selzer D,Neumann D,Schaefer UF

更新日期：2015-01-01 00:00:00