Translational modeling and simulation approaches for molecularly targeted small molecule anticancer agents from bench to bedside.

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：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：: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: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:A major challenge in transplantation is improving long-term organ transplant and patient survival. Immunosuppressants protect the transplant organ from alloimmune reactions, but sometimes also exhibit limiting side effects. The key to improving long-term outcome following transplantation is the selection o...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Christians U,Klawitter J,Klawitter J,Brunner N,Schmitz V

更新日期：2011-02-01 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: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：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:Telaprevir is one of the first direct-acting antiviral drugs approved for the treatment of the hepatitis C virus (HCV) genotype 1. Following its approval in 2011, new data regarding the pharmacokinetics and pharmacodynamics were reported, leading to important clinical applications. AREAS COVERED:This arti...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rivero-Juarez A,Camacho A,Rivero A

更新日期：2015-07-01 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：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:There have been increasing concerns regarding adverse reactions and toxicity incidents caused by traditional Chinese medicines (TCMs), among which the nephrotoxicity is particularly worrying. AREAS COVERED:This review summarizes the ingredients with renal toxicity from some TCMs through searching the rele...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Xu XL,Yang LJ,Jiang JG

更新日期：2016-01-01 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: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：:Rats are an important tool in pharmacology and toxicology. The authors focus on rat P450s in relation to diazepam metabolism. In particular, considerable attention is devoted to the CYP2D subfamily, which is a group of highly polymorphic enzymes. First, the metabolic profiles of diazepam of humans and other animals ar...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sakai N,Ishizuka M

更新日期：2009-11-01 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: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：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: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: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: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：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：INTRODUCTION:Neonatal patients, because of the inability of their immune system to properly respond to microbial challenge, are highly susceptible to viral infections. Immunoglobulins, monoclonal antibody and antiviral drugs are used for prophylaxis and treatment of viral diseases in neonates. Neonates and, especially,...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Enioutina EY,Constance JE,Stockmann C,Linakis MW,Yu T,Rower JE,Balch AH,Sherwin CM

更新日期：2015-01-01 00:00:00

abstract：OBJECTIVE:To investigate the metabolic routes and metabolites of myricitrin, an important active ingredient of traditional herbal medicine, yielded by the isolated human intestinal bacteria, which have not been reported previously. METHODS:Fresh human fecal samples were collected from a healthy female volunteer and ab...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Du LY,Zhao M,Xu J,Qian DW,Jiang S,Shang EX,Guo JM,Liu P,Su SL,Duan JA,Leng XJ

更新日期：2014-07-01 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：: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：: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: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: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: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