abstract：:The development of peptide therapeutics has increased enormously in recent decades. Many of the peptide drugs and antibody fragments that lack Fc backbone have a short half-life in circulation. In general, the half-life supports the design of the dosing regimen and frequency of administration, which are key aspects in...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hijazi Y

更新日期：2021-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:UPARANT has emerged as a novel therapeutic agent with the potential to treat ocular diseases as assessed by studies in animal models. Since limited information is available on the pharmacokinetics of UPARANT, the aim of this study is to evaluate its pharmacokinetics after single and multiple a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Ciccone M,D'Alonzo D,Cangiano AM,De Fenza M,Pavone V,Mancinelli A

更新日期：2021-01-01 00:00:00

abstract：BACKGROUND:Omadacycline is a semisynthetic aminomethylcycline antibacterial derived from the tetracycline class. It is approved in the USA to treat adults with acute bacterial skin and skin-structure infections and community-acquired bacterial pneumonia. OBJECTIVES:This phase I, open-label study evaluated the effect o...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hunt TL,Tzanis E,Bai S,Manley A,Chitra S,McGovern PC

更新日期：2021-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Ginseng is usually consumed as a dietary supplement for health care in the normal state or prescribed as a herbal medicine in pathologic conditions. Although metabolic studies of ginseng are commonly performed on healthy organisms, the metabolic characteristics in pathologic organisms remain un...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Zhu JH,Xu JD,Zhou SS,Zhang XY,Zhou J,Kong M,Mao Q,Zhu H,Li SL

更新日期：2021-01-01 00:00:00

abstract：:Mathematical models that can predict the kinetics of compounds have been increasingly adopted for drug development and risk assessment. Data for these models may be generated from in vitro experimental systems containing enzymes contributing to metabolic clearance, such as subcellular tissue fractions including micros...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Doerksen MJ,Jones RS,Coughtrie MWH,Collier AC

更新日期：2020-12-19 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Sorafenib is an oral, multikinase inhibitor with established single-agent activity in several tumor types. Sorafenib was moderately transported by P-glycoprotein (P-gp) and more efficiently by breast cancer resistance protein. The constitutive androstane receptor (CAR) is a ligand-activated tra...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Karbownik A,Stanisławiak-Rudowicz J,Stachowiak A,Romański M,Grześkowiak E,Szałek E

更新日期：2020-12-01 00:00:00

abstract：BACKGROUND:Experimental determination of a drug's oral bioavailability in humans is cost and time consuming; therefore, is usually performed on preclinical animals. It is believed that animal data are predictive of human data; however, there are some doubts regarding the reliability of this concept. The aim of this stu...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Beheshti S,Shayanfar A

更新日期：2020-12-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:The antitumor activity and toxicity of doxorubicin are potentiated and attenuated by calcitriol, respectively. Potentially, calcitriol can be combined with doxorubicin for clinical benefit in chemotherapy. To gain insight into the interaction between doxorubicin and calcitriol, proposed for com...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Durna Corum D,Uney K

更新日期：2020-10-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Polyethylene glycol-modified canine uricase (PEG-UHC) prepared with a lower-molecular-weight (5 kDa) PEG is used to treat gout. This study investigated the comparative pharmacokinetics of single and multiple doses of PEG-UHC administered intravenously and a single dose of uricase (UHC) administ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Li H,Huo J,Sun D,Jiang L,Hu C,Bai Y,Ma X,Zhang H,Shi X,Zhao Z,Zhou J,Lu Y,Zhang C

更新日期：2020-08-01 00:00:00

abstract：:The original version of this article unfortunately contained a mistake. ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Cui H,Zhao CY,Lv Y,Wei MJ,Zhu Y,Li Y,Xia YH,Liu Y,Tian JH,Zhang P

更新日期：2020-06-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Doxorubicin plays an essential role in the treatment of paediatric cancers. Defining genotypes with a higher risk for developing anthracycline-induced cardiotoxicity could help to reduce cardiotoxicity. METHODS:Data originated from a phase II study assessing the pharmacokinetics of doxorubici...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hellmann F,Völler S,Krischke M,Jamieson D,André N,Bisogno G,Boddy A,Hempel G

更新日期：2020-06-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Effective management of immunosuppressants is extemely important to improve prognosis of heart transplant recipients. We aim to investigate the effects of cytochrome P450 (CYP) 3A5 (rs776746) single nucleotide polymorphisms (SNPs) on serum tacrolimus concentrations/doses (C/Ds, ng/mL per mg/kg...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Liu BY,Chen WQ,Chen ZG,Huang J,Liao ZK,Liu Q,Zheng Z,Song YH,Wang W,Hu SS

更新日期：2019-12-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:A clinical trial was conducted to measure and analyse the pharmacokinetic parameters of a lipid formulation of risperidone, VAL401. The VAL401 formulation is designed to repurpose risperidone from an antipsychotic to an adenocarcinoma treatment, with the lipid formulation altering the cellular...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Dilly SJ,Morris GS,Taylor PC,Parmentier F,Williams C,Afshar M

更新日期：2019-08-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Mast cell-mediated allergic diseases are a significant global health problem. Nitric oxide (NO) produced by acute type 1 allergies greatly suppresses hepatic cytochrome P450 (CYP) metabolism. A recent in vitro study demonstrated that repeated FcεRI-mediated activation intrinsically modulates m...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Tanino T,Bando T,Okada Y,Nojiri Y,Hashimoto K,Ueda Y,Sakurai E

更新日期：2019-06-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:The disposition of azithromycin in the human eye following topical administration has not been fully explored. Population pharmacokinetic (PopPK) modeling can allow useful conclusions to be drawn based on limited tear sampling data. The aim of this study was therefore to develop and evaluate a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Wu F,Zhao X,Li X,Cui Y

更新日期：2019-06-01 00:00:00

abstract：:BACKGROUND AND OBJECTIVE: Efavirenz is commonly used in Africa and is frequently associated with neurocognitive toxicity, which may compromise clinical outcomes. Older individuals are at increased risk for drug toxicity and clinical outcomes may be worse in older age, particularly among those individuals with cytochro...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Torgersen J,Bellamy SL,Ratshaa B,Han X,Mosepele M,Zuppa AF,Vujkovic M,Steenhoff AP,Bisson GP,Gross R

更新日期：2019-04-01 00:00:00

abstract：BACKGROUND:Aldehyde oxidase (AOX) is an important molybdenum-containing enzyme with high similarity with xanthine oxidase (XO). AOX involved in the metabolism of a large array of aldehydes and N-heterocyclic compounds and its activity is highly substrate-dependent. OBJECTIVES:The aim of this work was to study the effe...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Deris-Abdolahpour F,Abdolalipouran-Sadegh L,Dastmalchi S,Hamzeh-Mivehroud M,Zarei O,Dehgan G,Rashidi MR

更新日期：2019-04-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Methyl 3,4-dihydroxybenzoate (MDHB) has the potential to prevent neurodegenerative diseases (NDDs). The present work aims to reveal the pharmacokinetics and tissue distribution characteristics of MDHB. METHODS:The pharmacokinetics and tissue distribution of MDHB were analyzed using LC-MS/MS a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Wang JH,Hu SH,Su JY,Pan JP,Mi XN,Geng HJ,Zhang W,Cai L,Su CF,Hong AH,Luo HM

更新日期：2019-04-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Drug-drug interactions (DDIs) can occur when one drug alters the metabolism of another drug. Drug metabolism mediated by cytochrome P450 enzymes (CYPs) is responsible for the majority of metabolism of known drugs and inhibition of CYP enzymes is a well-known cause of DDIs. In the current study...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Reinen J,Smit M,Wenker M

更新日期：2018-12-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Protein-calorie malnutrition (PCM) is one of the most suffered complications in cancer patients. Polyphyllin I (PPI), a saponin isolated from rhizome of Paris polyphylla, is a potential candidate in cancer therapy. In this study, the influence of nutritional status on the absorption of PPI in ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Yu FL,Gong WL,Xu FJ,Wu JW,Shakya S,Zhu H

更新日期：2018-10-01 00:00:00

abstract：:Angiogenesis is integral to tumour growth and invasion, and is a key target for cancer therapeutics. However, for many of the licensed indications, only a modest clinical benefit has been observed for both monoclonal antibody and small-molecule tyrosine kinase inhibitor anti-angiogenic therapy. Pre-clinical and clinic...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Morotti M,Dass PH,Harris AL,Lord S

更新日期：2018-04-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Fufang Danshen formula, a famous Chinese patent medicine containing Salvia miltiorrhiza, Panax notoginseng and borneol, has been widely used in the treatment of coronary heart disease. The application is restricted by low bioavailability partly due to Panax notoginseng saponins (PNS) instabilit...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Chen XN,Li DQ,Zhao MD,Yu GY,Du SY,Lu Y,Bai J,Li PY,Wu YL,Tian ZH,Zeng YY

更新日期：2018-04-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Maximum plasma concentration of biopharmaceuticals sometimes occurs long after completion of intravenous infusion. The objective of this research was to study the hypothetical adsorption of biopharmaceuticals to endothelium and infusion material, which may theoretically explain this phenomenon...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Reijers JAA,Dane MJC,van Zonneveld AJ,Burggraaf J,Moerland M

更新日期：2018-02-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Even though lithium has been used for the treatment of bipolar disorder for several decades, its toxicities are still being reported. The major limitation in the use of lithium is its narrow therapeutic window. Several methods have been proposed to predict lithium doses essential to attain the...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Methaneethorn J

更新日期：2018-02-01 00:00:00

abstract：:The evaluation of new intranasal medications requires the development of in vitro cell model suitable for high-throughput screening studies. The aim of a pharmacological model is to closely mimic the barrier properties of human nasal mucosa that will influence drug pharmacokinetics. In this context, the human nasal ce...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Mercier C,Perek N,Delavenne X

更新日期：2018-02-01 00:00:00

abstract：:Although the application of medical marijuana and cannabinoid drugs is controversial, it is a part of modern-day medicine. The list of diseases in which cannabinoids are promoted as a treatment is constantly expanding. Cases of significant improvement in patients with a very poor prognosis of glioma or epilepsy have a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hryhorowicz S,Walczak M,Zakerska-Banaszak O,Słomski R,Skrzypczak-Zielińska M

更新日期：2018-02-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Previous studies reported that tapentadol-sulfate represented one of the major metabolites of tapentadol excreted in urine. The current study aimed to identify the human cytosolic sulfotransferases (SULTs) that is(are) capable of sulfating tapentadol and to examine whether human cells and huma...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Bairam AF,Rasool MI,Kurogi K,Liu MC

更新日期：2017-10-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Lidocaine 5% medicated plaster is the first lidocaine containing product for chronic use. As no previous investigations have been conducted to evaluate the population pharmacokinetics of long-term exposure to lidocaine 5% medicated plasters, further insights into the evaluation of the pharmaco...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Bursi R,Piana C,Grevel J,Huntjens D,Boesl I

更新日期：2017-10-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Gadobenate dimeglumine (Gd-BOPTA) is a commercialised hepatobiliary contrast agent used during liver magnetic resonance imaging (MRI) to detect liver diseases. It enters into human hepatocytes through organic anion transporting polypeptides (OATP1B1/B3) and crosses the canalicular transporter ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Daire JL,Leporq B,Vilgrain V,Van Beers BE,Schmidt S,Pastor CM

更新日期：2017-08-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:In the present work, pharmacological and pharmacokinetic properties of the supramolecular complex of non-steroid anti-inflammatory drug ibuprofen (IBU) with natural polysaccharide arabinogalactan (AG) were studied. The main goals of such complexation were the increase of ibuprofen's bioavailab...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Khvostov MV,Borisov SA,Tolstikova TG,Dushkin AV,Tsyrenova BD,Chistyachenko YS,Polyakov NE,Dultseva GG,Onischuk AA,An'kov SV

更新日期：2017-06-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:LCZ696 (sacubitril/valsartan), a novel angiotensin receptor neprilysin inhibitor has been recently approved for the treatment of patients with heart failure (HF) and reduced ejection fraction. As several HF patients are likely to use statins as co-medications, the potential for a pharmacokineti...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Ayalasomayajula S,Pan W,Han Y,Yang F,Langenickel T,Pal P,Zhou W,Yuan Y,Rajman I,Sunkara G

更新日期：2017-04-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Acetaminophen (APAP, paracetamol) is currently the principal cause of acute liver failure in both the USA and the UK. However, relatively little is known about the influence of genes and race/ethnicity on the disposition of APAP and the extent to which genetic variation and ethnicity may predi...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Zurlinden TJ,Reisfeld B

更新日期：2017-02-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Hydronidone is a novel pyridine derivative with therapeutic potential for hepatic fibrosis. The aim of this study was to investigate the safety, tolerability, and pharmacokinetics of hydronidone in healthy subjects. Effects of sex and food on hydronidone pharmacokinetics were also evaluated. ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Liu Y,Wu J,Li Z,Luo Y,Zeng F,Shi S

更新日期：2017-02-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Beraprost sodium (BPS) is a chemically stable and orally active prostacyclin analog that is used in the treatment of chronic arterial occlusive disease since 1992 and primary pulmonary hypertension since 1999 in Japan. Multiple-drug therapy is common in clinical practice, and BPS is co-administ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Oshida K,Shimamura M,Seya K,Ando A,Miyamoto Y

更新日期：2017-02-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Chalcone constitutes one of the most used molecular frameworks in medicinal chemistry and its derivatives exhibit a broad spectrum of biological activities. Low absolute bioavailability, poor distribution, intensive metabolism and elimination of chalcones are the main problems in designing new...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Okoniewska K,Konieczny MT,Lemke K,Grabowski T

更新日期：2017-02-01 00:00:00

abstract：BACKGROUND:MTBH, a novel hesperetin derivative, possesses in vivo hepatoprotective effects against carbon tetrachloride (CCl4)-induced acute liver injury in Institute of Cancer Research (ICR) mice. OBJECTIVES:This study investigated the pharmacokinetics and tissue distribution of MTBH and its conjugated metabolites in...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Shen C,Qian Z,Chen R,Meng X,Hu T,Chen Z,Li Y,Huang C,Hu C,Li J

更新日期：2016-12-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Clopidogrel is an antiplatelet and antithrombotic prodrug. It has poor oral bioavailability due to poor dissolution and possible premature degradation in the intestine. Accordingly, the objective of this study was to enhance clopidogrel dissolution rate and to reduce its premature degradation ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Bali DE,Osman MA,El Maghraby GM

更新日期：2016-12-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Ketoprofen, a potent nonsteroidal anti-inflammatory drug, is clinically administered as a racemic mixture. One of the possible metabolism routes of ketoprofen is the inversion of the R- to S-enantiomer in the gastrointestinal tract. Ketoprofen, as a weak acid drug, might undergo recirculation ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Lorier M,Magallanes L,Ibarra M,Guevara N,Vázquez M,Fagiolino P

更新日期：2016-12-01 00:00:00

abstract：:Currently, macromolecular drugs such as proteins are mainly administered by means of injections due to their low intestinal epithelial permeability and poor stability in the gastrointestinal tract. This study investigated binary combinations of chemical drug absorption enhancers to determine if synergistic drug absorp...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： du Toit T,Malan MM,Lemmer HJ,Gouws C,Aucamp ME,Breytenbach WJ,Hamman JH

更新日期：2016-10-01 00:00:00

abstract：:Lisofylline (LSF), is the R-(-) enantiomer of the metabolite M1 of pentoxifylline, and is currently under development for the treatment of type 1 diabetes. The aim of the study was to develop a physiologically based pharmacokinetic (PBPK) model of LSF in mice and to perform simulations in order to predict LSF concentr...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Wyska E,Świerczek A,Pociecha K,Przejczowska-Pomierny K

更新日期：2016-08-01 00:00:00