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European Journal of Drug Metabolism and Pharmacokinetics

Joanna Porażka, Edyta Szałek, Wojciech Połom, Mateusz Czajkowski, Tomasz Grabowski, Marcin Matuszewski, Edmund Grześkowiak
BACKGROUND AND OBJECTIVES: The number of overweight, obese and diabetic patients is constantly increasing. Metabolic disorders may affect the pharmacokinetics of drugs, e.g., by altering the activity of cytochrome P450 (CYP) isoenzymes. Tramadol is a commonly used analgesic metabolised mainly via CYP2D6 to its active metabolite, O-desmethyltramadol. The aim of the study was to assess the influence of overweight, obesity and type 2 diabetes mellitus on tramadol and O-desmethyltramadol pharmacokinetics...
February 18, 2019: European Journal of Drug Metabolism and Pharmacokinetics
Vinod S Ipar, Anisha Dsouza, Padma V Devarajan
Curcumin is a promising therapeutic agent that exhibits manifold therapeutic activities. However, it is challenging to study curcumin as it exhibits poor aqueous solubility and low permeability and it is a substrate for P-glycoprotein (P-gp). It is readily metabolized in the body, but many active metabolites of curcumin have been identified that could also be exploited for therapy. Strategies for the oral bioenhancement of curcumin to leverage the potential of curcumin as a therapeutic molecule are discussed here in light of these challenges...
February 15, 2019: European Journal of Drug Metabolism and Pharmacokinetics
Gulsah Kaya Aksoy, Elif Comak, Mustafa Koyun, Halide Akbaş, Bahar Akkaya, Bülent Aydınlı, Fahri Uçar, Sema Akman
BACKGROUND AND OBJECTIVES: The most important determinant of long-term graft survival in renal transplantation is adequate immunosuppression. Inadequate immunosuppression may lead to graft loss due to the presence of anti-HLA antibody. The aim of this study was to investigate the effect of variability in tacrolimus blood concentration on anti-HLA antibody development in pediatric recipients of living-donor renal transplants. METHODS: Pediatric recipients of living-donor renal transplants were retrospectively evaluated...
February 8, 2019: European Journal of Drug Metabolism and Pharmacokinetics
Jennypher Mudunuru, Chen Ren, David R Taft, Manoj Maniar
BACKGROUND AND OBJECTIVES: ON 123300, a small molecule dual inhibitor of the c-MYC activated kinases ARK5 and CDK4/6, is being developed as a novel drug candidate for the treatment of cancer. The objective of this research was to evaluate gender differences in the in vitro metabolism and in vivo systemic exposure of ON 123300 in rats. METHODS: In vitro metabolism experiments (n = 2/group) were performed in rat liver microsomes from male and female donors. ON 123300 bislactate (final concentration 10 µM) was incubated with 0...
January 30, 2019: European Journal of Drug Metabolism and Pharmacokinetics
Hanna Davideit, Susanne Becker, Johannes Müller, Niels-Peter Becker, Peter Göttel, Ayşe Abay, Angela Sinn, Matthias Grossmann, Markus Mallek, Annekathrin Haberland, Hardy Weisshoff
BACKGROUND AND OBJECTIVES: Since there is no clear evidence in the literature to show how non-modified single-stranded DNA (ssDNA) drugs are metabolized in humans, we assessed the metabolism of BC 007, an ssDNA therapeutic, under development as a neutralizer of autoantibodies against G-protein-coupled receptors. In-vitro, investigating its stability in monkey plasma and serum, a successive 3'-exonuclease degradation resulting in several n-x degradation products has been previously reported...
January 23, 2019: European Journal of Drug Metabolism and Pharmacokinetics
Farnaz Deris-Abdolahpour, Lida Abdolalipouran-Sadegh, Siavoush Dastmalchi, Maryam Hamzeh-Mivehroud, Omid Zarei, Gholamreza Dehgan, Mohammad-Reza Rashidi
Unfortunately, the original article was published with error in author names. The author names are corrected here by this correction paper. The original article has been corrected.
January 18, 2019: European Journal of Drug Metabolism and Pharmacokinetics
Suzanne J Dilly, George S Morris, Paul C Taylor, Frederic Parmentier, Coralie Williams, Mohammad Afshar
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 uptake of risperidone, thus enabling anticancer biology to be exhibited in preclinical testing. METHODS: This first human trial of VAL401 measured the concentrations of risperidone and its primary metabolite, 9-hydroxyrisperidone, in the blood of patients after treatment with a single 2-mg dose of VAL401...
January 9, 2019: European Journal of Drug Metabolism and Pharmacokinetics
Pierre Mugabo, Mwila Mulubwa
BACKGROUND AND OBJECTIVES: Pyrazinamide, a drug used in the regimen for the treatment of drug-sensitive tuberculosis, is also used for the treatment of multidrug-resistant tuberculosis (MDR-TB). We aimed to describe the population pharmacokinetics of pyrazinamide and its major metabolite, pyrazinoic acid, in patients with MDR-TB and characterise the effects of demographic variables. METHODS: This was a non-randomised clinical study involving 51 adult patients admitted for the intensive phase of MDR-TB treatment...
January 8, 2019: European Journal of Drug Metabolism and Pharmacokinetics
Muhammad Nadeem Ashraf, Muhammad Waheed Asghar, Yan Rong, Michael R Doschak, Tony K L Kiang
Several HepaRG three-dimensional (3D) in vitro model systems have been developed to improve the predictability of xenobiotic metabolism and toxicity. In this review, we present a detailed summary and critique of the performance of various HepaRG 3D models compared to the conventional 2D monolayer culture. HepaRG 3D models can be broadly categorized into (1) scaffold-free, (2) scaffold-based, and (3) bioartificial liver (BAL) models. With respect to the scaffold-free configurations, the hanging drop model closely mimics the normal physiological function and metabolic profile of the liver...
December 10, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Daichi Yamaguchi, Yasuhiro Tsuji, Miki Sonoda, Kenji Shin, Hiroko Kito, Chika Ogami, Hidefumi Kasai, Hideto To, Hidetoshi Kamimura
BACKGROUND AND OBJECTIVE: Lithium, which is used to treat bipolar disorder, has a narrow therapeutic blood concentration range and quickly reaches clinically toxic levels. We performed a population pharmacokinetic analysis with a lithium tubular reabsorption model including urinary pH and investigated the relationship between blood lithium concentration and tremor as a side effect. METHODS: Routine clinical data, including 389 serum concentrations, were collected from 214 patients orally administered an adjusted amount of lithium carbonate...
December 7, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Fan Zhang, Yan Li, Jingqiu Hu, Jinhua Zhong, Huafang Li
BACKGROUND AND OBJECTIVE: Bupropion is used for the treatment of major depressive disorder. We determined the pharmacokinetics, safety, and tolerability of extended-release bupropion XL in healthy Chinese volunteers. METHODS: This open-label, single-center pharmacokinetic study was conducted between May 2016 and June 2016. Eligible volunteers received bupropion XL 150 mg once daily for 5 days, then 300 mg once daily from days 6 to 14. Pharmacokinetic parameters were evaluated after first and repeated doses by non-compartmental and population pharmacokinetic analyses...
December 5, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Qian Zhang, Jianming Guo, Guoliang Dai, Jianping Li, Lijing Zhu, Shufen He, Yang Zong, Zhishu Tang, Buchang Zhao, Wenzheng Ju, Jinao Duan
BACKGROUND AND OBJECTIVES: Danhong injection is the most commonly prescribed adjuvant drug applied for the treatment of cardiovascular and cerebrovascular diseases in China. Ceftriaxone is usually prescribed along with Danhong injection to elderly patients with complications. However, the pharmacokinetic interactions between these two medications have not been investigated. The aim of this study was to investigate whether Danhong injection influences the pharmacokinetic profile of ceftriaxone in old rats when these two medications are used in combination...
December 3, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Ying Zhou, Feifei Gao, Chaoyang Chen, Lingyun Ma, Ting Yang, Xiao Liu, Yaou Liu, Xiaoqing Wang, Xia Zhao, Chengli Que, Shuangling Li, JiCheng Lv, Yimin Cui, Li Yang
BACKGROUND: The optimal use of vancomycin in the elderly requires information about the drug's pharmacokinetics and the influence of various factors on the drug's disposition. However, because of sampling restrictions, it is often difficult to perform traditional pharmacokinetic studies in elderly patients. OBJECTIVE: This study was conducted to estimate the population pharmacokinetics of vancomycin in Chinese geriatric patients (age ≥ 65 years) with pulmonary infections and to explore the clinical application of this information for vancomycin dose individualization...
November 30, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Malek Okour, Richard C Brundage
BACKGROUND AND OBJECTIVES: Strategies for modeling the enterohepatic circulation (EHC) process reported in the literature vary; however, gallbladder-based models currently provide the best physiological representation of the process. Regardless, the addition of a gallbladder to the model does not fully depict the physiology of EHC. A more physiological gallbladder-based EHC model is needed. This model should take into account a physiological representation of the bile secretion, gallbladder filling and emptying, the duration of gallbladder emptying, and irregular mealtimes...
November 28, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Aiko Iida, Shohei Ouchi, Toshio Oda, Jun Aketagawa, Yasuhiko Ito, Yusuke Takizawa, Mikio Tomita, Masahiro Hayashi
The Editor-in-Chief has retracted this article [1] based on an investigation by the Ministry of Education, Culture, Sports, Science and Technology, Japan, which found that the article contained overlap with a previously published article by Kalitsky-Szirtes J, et al. [2].
December 2018: European Journal of Drug Metabolism and Pharmacokinetics
Kyle John Wilby, Nesma Ahmed Eissa
Doravirine is a new HIV-1 non-nucleoside reverse transcriptase inhibitor that has demonstrated a good efficacy and safety profile in clinical trials. It has a therapeutic profile that makes it an attractive option for treatment of HIV-1 infection. As such, there has been an increase in the published literature regarding the pharmacokinetics of doravirine and potential for drug-drug interactions. This review aimed to identify pharmacokinetic literature pertaining to doravirine, used findings from the literature to summarize its pharmacokinetic profile, and finally evaluated literature describing actual and potential drug interactions...
December 2018: European Journal of Drug Metabolism and Pharmacokinetics
Lilian W Kibathi, SoHyun Bae, Scott R Penzak, Parag Kumar
Complementary and alternative medications (CAM) with known or suspected pharmacologic activity in the central nervous system (CNS) are common. These herbal preparations may cause clinically significant drug-drug interactions (DDIs) when coadministered with medications that act in the CNS. This can result in negative outcomes such as toxicity or loss of efficacy. Most drug interaction reports with CAM focus on cytochrome P450 (CYP) modulation. However, drug interactions between CAM and conventional medications may occur via mechanisms other than CYP inhibition or induction; in particular, modulation of drug transport proteins represents an important mechanism by which such interactions may occur...
December 2018: European Journal of Drug Metabolism and Pharmacokinetics
Jelle Reinen, Martijn Smit, Mira Wenker
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, the use of various human liver microsomes (HLM)-based methods to determine occurrence of CYP-mediated metabolism-dependent inhibition (MDI) and possible follow-up studies were evaluated...
December 2018: European Journal of Drug Metabolism and Pharmacokinetics
Waroonrat Sukarnjanaset, Thitima Wattanavijitkul, Sutep Jarurattanasirikul
BACKGROUND AND OBJECTIVES: First-order conditional estimation with interaction (FOCEI) is one of the most commonly used estimation methods in nonlinear mixed effects modeling, while the stochastic approximation expectation maximization (SAEM) is the newer estimation algorithm. This work aimed to compare the performance of FOCEI and SAEM methods when using NONMEM® with the classical one- and two-compartment models across rich, medium, and sparse data. METHODS: One- and two-compartment models of the previous studies were used to simulate data in three scenarios: rich, medium, and sparse data...
December 2018: European Journal of Drug Metabolism and Pharmacokinetics
Roland Heinig, Michael Gerisch, Anna Engelen, Johannes Nagelschmitz, Stephanie Loewen
BACKGROUND AND OBJECTIVES: Finerenone is a selective, non-steroidal mineralocorticoid receptor antagonist. In vivo and in vitro studies were performed to assess absolute bioavailability of finerenone, the effect of metabolic enzyme inhibitors on the pharmacokinetics of finerenone and its metabolites, the quantitative contribution of the involved enzymes cytochrome P450 (CYP) 3A4 and CYP2C8 and the relevance of gut wall versus liver metabolism. METHODS: The pharmacokinetics, safety and tolerability of finerenone (1...
December 2018: European Journal of Drug Metabolism and Pharmacokinetics
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