Pharmacokinetics, efficacy and safety of aleglitazar for the treatment of type 2 diabetes with high cardiovascular risk.

abstract：INTRODUCTION:Assessments of the pharmacokinetic/pharmacodynamic (PK/PD) characteristics are an integral part in the development of novel therapeutic agents. Compared with traditional small molecule drugs, therapeutic proteins possess many distinct PK/PD features that necessitate the application of modified or separate ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Diao L,Meibohm B

更新日期：2015-07-01 00:00:00

abstract：INTRODUCTION:Emtricitabine/tenofovir disoproxil fumarate fixed-dose combination (FTC/TDF FDC) is the co-formulation of a nucleoside and a nucleotide, respectively. After oral administration, both drugs exhibit plasma and intracellular half-lives suitable for once-daily dosing. Within the host cells, active metabolites ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Uglietti A,Zanaboni D,Gnarini M,Maserati R

更新日期：2012-10-01 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：:The past decade has seen an increase in therapeutic options for Alzheimer's disease (AD) that target neurotransmitters, such as acetylcholine, and research continues to target abnormal proteins in the AD brain. Recently, glutamate excitotoxicity has also become a target for AD treatment with the advent of memantine. C...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Schmitt F,Ryan M,Cooper G

更新日期：2007-02-01 00:00:00

abstract：INTRODUCTION:Lenalidomide is an oral immunomodulatory drug, which was recently introduced for the treatment of multiple myeloma (MM). It has been used for the treatment of newly diagnosed and relapsed MM patients, as both maintenance and preventive therapy. Available data show a progression-free survival and overall su...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Bringhen S,Gay F,Pautasso C,Cerrato C,Boccadoro M,Palumbo A

更新日期：2012-09-01 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：INTRODUCTION:Selective serotonin reuptake inhibitors (SSRIs) are commonly used to manage antenatal depression. Hence, the aim of this systematic review is to assess the prevalence of birth defects associated with pregnancy exposure to such agents and summarize the hypothesized teratogenic mechanisms. AREAS COVERED:Med...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Gentile S

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:The second-line treatment of endometriosis-related pain symptoms includes injectable depot formulations of gonadotropin-releasing hormone analogs (GnRH-as). These drugs improve the symptomatology by inducing a hypoestrogenic status and a consequent regression of endometriotic implants. However, GnRH-a may ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Della Corte L,Barra F,Mercorio A,Evangelisti G,Rapisarda AMC,Ferrero S,Bifulco G,Giampaolino P

更新日期：2020-09-01 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: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：: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: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：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:The goal of pharmacologic therapy with antiepileptic drugs (AEDs) is to reduce the frequency of seizures and achieve a seizure-free state with minimal side effects. However 30% of patients treated with available AEDs continue to experience uncontrolled seizures. There is still need for new AEDs with enhanc...

journal_title：Expert opinion on drug metabolism & toxicology

authors： de Biase S,Valente M,Gigli GL,Merlino G

更新日期：2017-09-01 00:00:00

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：: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: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: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

abstract：INTRODUCTION:Various trials have attempted to develop gene expression profiles (GEPs) that may provide a better predictor of clinical outcome over traditional clinicopathological criteria. AREAS COVERED:The review focuses on two main areas: trials examining chemotherapy-induced GEP changes pre- and post-treatment, and...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Tan SH,Lee SC

更新日期：2012-09-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Iloperidone is a newly commercialized second-generation (atypical) antipsychotic approved for the acute treatment of schizophrenia in adults. AREAS COVERED IN THIS REVIEW:the purpose of this review is to describe the pharmacokinetic profile of iloperidone and its clinical implications in the tr...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Citrome L

更新日期：2010-12-01 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：IMPORTANCE OF THE FIELD:Cytochrome (CYP) P450 is a collective name for a very large group of heme enzymes, which catalyze largely oxidative reactions, including those of pharmacological and toxicological importance. Their efficient operation requires coupling of specific electron donor and O(2) consumption and substrat...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Shakunthala N

更新日期：2010-01-01 00:00:00

abstract：:The onset, intensity and duration of therapeutic response to a compound depend on the intrinsic pharmacological activity of the drug and pharmacokinetic factors related to its absorption, distribution, metabolism and elimination that are inherent to the biological system. The process of drug transfer from the site of ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hurst S,Loi CM,Brodfuehrer J,El-Kattan A

更新日期：2007-08-01 00:00:00

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：INTRODUCTION:. Membrane transporters are integral to the maintenance of cellular integrity of all tissue and cell types. While transporters play an established role in the systemic pharmacokinetics of therapeutic drugs, tissue specific expression of uptake transporters can serve as an initiating mechanism that governs ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Huang KM,Uddin ME,DiGiacomo D,Lustberg MB,Hu S,Sparreboom A

更新日期：2020-06-01 00:00:00

abstract：BACKGROUND:CYP enzymes from the CYP2C and CYP2J subfamilies metabolize arachidonic acid in a regiospecific and stereoselective manner to eight epoxyeicosatrienoic acids (EETs). Various EETs have been detected in the liver, as well as in many extrahepatic tissues, and have been implicated in numerous physiological funct...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Kaspera R,Totah RA

更新日期：2009-07-01 00:00:00

abstract：INTRODUCTION:DNA damaging drugs are widely used for the chemotherapeutic treatment of high-grade osteosarcoma (HGOS). In HGOS patients, several germline polymorphisms have been reported to impact on the development of adverse toxic events related to DNA damaging drugs treatment. Some of these polymorphisms, when presen...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hattinger CM,Patrizio MP,Luppi S,Magagnoli F,Picci P,Serra M

更新日期：2019-04-01 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：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：INTRODUCTION:Sepsis remains a leading cause of death worldwide. Despite years of extensive research, effective drugs that inhibit the pro-inflammatory effects of lipopolysaccharide (LPS) and improve outcome when added to conventional sepsis treatments are lacking. Eritoran tetrasodium (E5564) is a promising candidate t...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Barochia A,Solomon S,Cui X,Natanson C,Eichacker PQ

更新日期：2011-04-01 00:00:00