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https://www.readbyqxmd.com/read/29137842/comparison-of-pharmacokinetics-of-newly-discovered-aromatase-inhibitors-by-a-cassette-microdosing-approach-in-healthy-japanese-subjects
#1
Hiroyuki Kusuhara, Tadayuki Takashima, Hisako Fujii, Tsutomu Takashima, Masaaki Tanaka, Akira Ishii, Shusaku Tazawa, Kazuhiro Takahashi, Kayo Takahashi, Hidekichi Tokai, Tsuneo Yano, Makoto Kataoka, Akihiro Inano, Suguru Yoshida, Takamitsu Hosoya, Yuichi Sugiyama, Shinji Yamashita, Taisuke Hojo, Yasuyoshi Watanabe
The aim of the present study is to investigate the pharmacokinetics of our newly developed aromatase inhibitors (cetrozole and TMD-322) in healthy subjects by a cassette microdose strategy. A cocktail of cetrozole and TMD-322 was administered intravenously or orally (1.98 μg for each drug) to six healthy volunteers in a crossover fashion. Anastrozole (1.98 μg) was also included in the oral cocktail. Total body clearance and bioavailability were 12.1 ± 7.1 mL/min/kg and 34.9 ± 32.3% for cetrozole, and 16...
September 21, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29136336/effect-of-polymorphisms-on-the-pharmacokinetics-pharmacodynamics-and-safety-of-sertraline-in-healthy-volunteers
#2
Miriam Saiz-Rodríguez, Carmen Belmonte, Manuel Román, Dolores Ochoa, Dora Koller, María Talegón, María C Ovejero-Benito, Rosario López-Rodríguez, Teresa Cabaleiro, Francisco Abad-Santos
Sertraline is a selective serotonin reuptake inhibitor (SSRI) widely metabolized in the liver by cytochrome P450 (CYP) enzymes. Besides, it is a P-glycoprotein substrate. Moreover, serotonin transporters and serotonin receptors are involved in its efficacy and safety. The aim of the present study was to evaluate the role of polymorphisms of metabolizing enzymes, transporters and receptors on the pharmacokinetics, pharmacodynamics and tolerability of sertraline in healthy volunteers. Forty-six healthy volunteers (24 men and 22 women) receiving a 100-mg single oral dose of sertraline were genotyped for 17 genetic variants of CYP enzymes (CYP2B6, CYP2C9, CYP2C19, CYP2D6), ATP binding cassette subfamily B member 1 (ABCB1), Solute carrier family 6 member 4 (SLC6A4), 5-Hydroxytryptamine receptor 2A (HTR2A) and 5-Hydroxytryptamine receptor 2C (HTR2C) genes...
November 14, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29127901/cerium-dioxide-doped-carboxyl-fullerene-as-novel-nanoprobe-and-catalyst-in-electrochemical-biosensor-for-amperometric-detection-of-the-cyp2c19-2-allele-in-human-serum
#3
Chengli Zhang, Junlin He, Yuchan Zhang, Jun Chen, Yilin Zhao, Yazhen Niu, Chao Yu
The disposition dose of clopidogrel is different in CYP2C19*2 gene carriers and non-carriers. High-dose clopidogrel has been recommended to overcome a low-responsiveness to clopidogrel in patients with the CYP2C19*2 gene. To guide the choice of clopidogrel dosage and catalyse a development in the field of personalized therapy, we developed an ultrasensitive electrochemical biosensor to detect CYP2C19*2 gene. We constructed a novel assay based on cerium dioxide (CeO2)-functionalized carboxyl fullerene (c-C60) supported by Pt nanoparticles (c-C60/CeO2/PtNPs) for signal amplification...
November 8, 2017: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/29123929/palpitations-and-asthenia-associated-with-venlafaxine-in-a-cyp2d6-poor-metabolizer-and-cyp2c19-intermediate-metabolizer
#4
Sofia Garcia, Michael Schuh, Anvir Cheema, Herjot Atwal, Paldeep S Atwal
Cardiotoxicity has been extensively reported in venlafaxine (VEN) overdoses. Asthenia is also among the common side effects described for this antidepressant. VEN is metabolized mainly by CYP2D6 and to a minor extent by CYP2C19 to the major active metabolite O-desmethylvenlafaxine (ODV). Altered pharmacokinetic parameters in patients with polymorphisms in the CYP2D6 and CYP2C19 genes that result in decreased enzymatic activity have been documented. Here we describe a patient case of VEN associated palpitations and asthenia...
2017: Case Reports in Genetics
https://www.readbyqxmd.com/read/29118712/comparative-long-term-effect-of-three-anti-p2y12-drugs-after-percutaneous-angioplasty-an-observational-study-based-on-electronic-drug-adherence-monitoring
#5
Valentina Forni Ogna, Isabelle Bassi, Isabelle Menetrey, Olivier Muller, Eric Tousset, Pierre Fontana, Eric Eeckhout, Chin B Eap, Bernard Vrijens, Michel Burnier, Grégoire Wuerzner
Aims: Dual platelet inhibition using anti-P2Y12 drugs and aspirin is the standard of care in patients after percutaneous coronary interventions (PCI). Prasugrel and ticagrelor have been shown to be more potent than clopidogrel with less high on-treatment platelet reactivity. Whether differences in long-term adherence to these drugs can partly explain different antiplatelet efficacy has not been studied so far. The objective was to compare the long-term P2Y12 receptor inhibition and drug adherence to different anti-P2Y12 drugs, and to assess the impact of adherence on the pharmacodynamic effect...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29115994/exploring-venlafaxine-pharmacokinetic-variability-with-a-phenotyping-approach-a-multicentric-french-swiss-study-marvel-study
#6
Célia Lloret-Linares, Youssef Daali, Sylvie Chevret, Isabelle Nieto, Fanny Molière, Philippe Courtet, Florence Galtier, Raphaëlle-Marie Richieri, Sophie Morange, Pierre-Michel Llorca, Wissam El-Hage, Thomas Desmidt, Frédéric Haesebaert, Philippe Vignaud, Jerôme Holtzmann, Jean-Luc Cracowski, Marion Leboyer, Antoine Yrondi, Fabienne Calvas, Liova Yon, Philippe Le Corvoisier, Olivier Doumy, Kyle Heron, Damien Montange, Siamak Davani, Julien Déglon, Marie Besson, Jules Desmeules, Emmanuel Haffen, Frank Bellivier
BACKGROUND: It is well known that the standard doses of a given drug may not have equivalent effects in all patients. To date, the management of depression remains mainly empirical and often poorly evaluated. The development of a personalized medicine in psychiatry may reduce treatment failure, intolerance or resistance, and hence the burden and costs of mood depressive disorders. The Geneva Cocktail Phenotypic approach presents several advantages including the "in vivo" measure of different cytochromes and transporter P-gp activities, their simultaneous determination in a single test, avoiding the influence of variability over time on phenotyping results, the administration of low dose substrates, a limited sampling strategy with an analytical method developed on DBS analysis...
November 7, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29105855/dicloxacillin-induces-cyp2c19-cyp2c9-and-cyp3a4-in-vivo-and-in-vitro
#7
Tore Bjerregaard Stage, Magnus Graff, Susan Wong, Louise Ladebo Rasmussen, Flemming Nielsen, Anton Pottegård, Kim Brøsen, Deanna L Kroetz, S Cyrus Khojasteh, Per Damkier
AIM: The aim of this study was to study potential cytochrome P450 induction by dicloxacillin. METHODS: We performed an open-label randomized two-phase 5-drug clinical pharmacokinetic cocktail crossover study in 12 healthy men with and without pretreatment with 1g dicloxacillin three times daily for 10 days. Plasma and urine was collected over 24 hours and the concentration of all five drugs and their primary metabolites was determined using a LC-MS/MS method. Cryopreserved primary human hepatocytes were exposed to dicloxacillin for 48h and changes in gene expression and enzyme activity of CYP3A4, CYP2C9, CYP2B6 and CYP1A2 was investigated...
November 4, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29102810/role-of-cytochrome-p450-2c19-polymorphisms-and-body-mass-index-in-endometriosis-a-case-control-study
#8
Jéssica Vilarinho Cardoso, Maurício Simões Abrão, Plínio Tostes Berardo, Renato Ferrari, Luiz Eurico Nasciutti, Daniel Escorsim Machado, Jamila Alessandra Perini
OBJECTIVE: To investigate the contribution of CYP2C19 polymorphisms and body mass index (BMI) in the development of endometriosis. STUDY DESIGN: This is a case-control study that includes 356 women (187 cases and 169 controls) recruited from two hospitals in the Brazilian public health system. The genotyping analyses of the CYP2C19*2 and CYP2C19*17 polymorphisms were performed using TaqMan allelic discrimination assays, and the association of the studied polymorphisms with endometriosis was evaluated by multivariate logistic regression...
October 31, 2017: European Journal of Obstetrics, Gynecology, and Reproductive Biology
https://www.readbyqxmd.com/read/29102584/cyp2c19-genotyping-in-percutaneous-coronary-intervention-treated%C3%A2-patients-ready-for-prime-time
#9
EDITORIAL
Dirk Sibbing, Lisa Gross
No abstract text is available yet for this article.
October 25, 2017: JACC. Cardiovascular Interventions
https://www.readbyqxmd.com/read/29102571/multisite-investigation-of-outcomes-with%C3%A2-implementation-of-cyp2c19-genotype-guided-antiplatelet-therapy-after-percutaneous-coronary-intervention
#10
Larisa H Cavallari, Craig R Lee, Amber L Beitelshees, Rhonda M Cooper-DeHoff, Julio D Duarte, Deepak Voora, Stephen E Kimmel, Caitrin W McDonough, Yan Gong, Chintan V Dave, Victoria M Pratt, Tameka D Alestock, R David Anderson, Jorge Alsip, Amer K Ardati, Brigitta C Brott, Lawrence Brown, Supatat Chumnumwat, Michael J Clare-Salzler, James C Coons, Joshua C Denny, Chrisly Dillon, Amanda R Elsey, Issam S Hamadeh, Shuko Harada, William B Hillegass, Lindsay Hines, Richard B Horenstein, Lucius A Howell, Linda J B Jeng, Mark D Kelemen, Y M Lee, Oyunbileg Magvanjav, May Montasser, David R Nelson, Edith A Nutescu, Devon C Nwaba, Ruth E Pakyz, Kathleen Palmer, Josh F Peterson, Toni I Pollin, Alison H Quinn, Shawn W Robinson, Jamie Schub, Todd C Skaar, D Max Smith, Vindhya B Sriramoju, Petr Starostik, Tomasz P Stys, James M Stevenson, Nicholas Varunok, Mark R Vesely, Dyson T Wake, Karen E Weck, Kristin W Weitzel, Russell A Wilke, James Willig, Richard Y Zhao, Rolf P Kreutz, George A Stouffer, Philip E Empey, Nita A Limdi, Alan R Shuldiner, Almut G Winterstein, Julie A Johnson
OBJECTIVES: This multicenter pragmatic investigation assessed outcomes following clinical implementation of CYP2C19 genotype-guided antiplatelet therapy after percutaneous coronary intervention (PCI). BACKGROUND: CYP2C19 loss-of-function alleles impair clopidogrel effectiveness after PCI. METHODS: After clinical genotyping, each institution recommended alternative antiplatelet therapy (prasugrel, ticagrelor) in PCI patients with a loss-of-function allele...
October 25, 2017: JACC. Cardiovascular Interventions
https://www.readbyqxmd.com/read/29099769/influence-of-amlodipine-enantiomers-on-human-microsomal-cytochromes-p450-stereoselective-time-dependent-inhibition-of-cyp3a-enzyme-activity
#11
Kristyna Krasulova, Ondrej Holas, Pavel Anzenbacher
Amlodipine (AML) is available as a racemate, i.e., a mixture of R- and S-enantiomers. Its inhibitory potency towards nine cytochromes P450 (CYP) was studied to evaluate the drug-drug interactions between the enantiomers. Enzyme inhibition was evaluated using specific CYP substrates in human liver microsomes. With CYP3A, both enantiomers exhibited reversible and time-dependent inhibition. S-AML was a stronger reversible inhibitor of midazolam hydroxylation: the Ki values of S- and R-AML were 8.95 µM, 14.85 µM, respectively...
November 3, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29098786/functional-characterization-of-cyp2c19-variants-in-nebivolol-4-hydroxlation-in-vitro
#12
Xiao-Yang Zhou, Xiao-Xia Hu, Meng-Fang Li, Hao Wang, Li-Qun Zhang, Guo-Xin Hu, Jian-Ping Cai
Cytochrome P450 2C19 (CYP2C19) allelic variants are thought to play an important part in inter-individual variability in drug metabolism. We evaluated the in vitro hydroxylation of nebivolol by 31 CYP2C19 alleles identified in a Chinese Han population recently. Wild-type CYP2C19*1B and 30 isoforms were highly expressed in insect cells, and the enzymatic activities of CYP2C19 variants towards nebivolol hydroxylation were characterized. Among the 30 CYP2C19 alleles, most of the recombinant CYP2C19 variants exhibited no or significantly low activity compared with CYP2C19*1B...
November 3, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29081699/optimization-of-antidepressant-use-with-pharmacogenetic-strategies
#13
Clara Torrellas, Juan Carlos Carril, Ramón Cacabelos
BACKGROUND: The response rate in the pharmacological treatment of depression has been estimated to be around 50%, achieving a remission in symptomatology in only one third of the patients. Suboptimal prescription of antidepressants has been proposed as a significant explanatory factor for this therapeutic inefficacy. The use of pharmacogenetic testing might favor the optimization of pharmacotherapy in emotional disorders. However, its implementation in the clinical routine requires studies which prove its efficacy...
October 2017: Current Genomics
https://www.readbyqxmd.com/read/29075133/do-cyp2c19-and-abcb1-gene-polymorphisms-and-low-cyp3a4-isoenzyme-activity-have-an-impact-on-stent-implantation-complications-in-acute-coronary-syndrome-patients
#14
Eric Rytkin, Karin B Mirzaev, Elena A Grishina, Valeriy V Smirnov, Kristina A Ryzhikova, Zhannet A Sozaeva, Michael Iu Giliarov, Denis A Andreev, Dmitriy A Sychev
AIM: The aim of this study was to determine the impact of CYP2C19 and ABCB1 gene polymorphisms and CYP3A4 isoenzyme activity on stent implantation complications among patients with an acute coronary syndrome (ACS) who underwent percutaneous coronary intervention (PCI). PATIENTS AND METHODS: Seventy-six patients (median age 63, range 37-91 years) with an ACS who underwent PCI were screened for CYP2C19 and ABCB1 gene polymorphisms with real-time polymerase chain reaction: CYP2C19*2, CYP2C19*17, and ABCB1 3435...
2017: Pharmacogenomics and Personalized Medicine
https://www.readbyqxmd.com/read/29072432/effectiveness-of-7-day-and-14-day-moxifloxacin-dexlansoprazole-based-triple-therapy-and-probiotic-supplement-for-helicobacter-pylori-eradication-in-thai-patients-with-non-ulcer-dyspepsia-a-double-blind-randomized-placebo-controlled-study
#15
Peranart Chotivitayatarakorn, Varocha Mahachai, Ratha-Korn Vilaichone
Background: Helicobacter pylori (H. pylori) is important cause of peptic ulcer and gastric cancer. Moxifloxacin is effective antibiotic for treatment for H. pylori. However, there were limited studies as first line therapy. Probiotics had been shown to decrease therapy-related side-effect and increase eradication rate. Aim of this study was to evaluate the efficacy of moxifloxacin-dexlansoprazole based triple therapy with probiotic for H. pylori treatment in Thailand. Methods: Patients with H. pylori infected gastritis were randomized to receive 7- or 14-day moxifloxacin-dexlansoprazole based triple therapy with probiotic or placebo...
October 26, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/29065189/establishment-of-a-novel-hepatocyte-model-that-expresses-four-cytochrome-p450-genes-stably-via-mammalian-derived-artificial-chromosome-for-pharmacokinetics-and-toxicity-studies
#16
Daisuke Satoh, Satoru Iwado, Satoshi Abe, Kanako Kazuki, Shinobu Wakuri, Mitsuo Oshimura, Yasuhiro Kazuki
The utility of HepG2 cells to assess drug metabolism and toxicity induced by chemical compounds is hampered by their low cytochrome P450 (CYP) activities. To overcome this limitation, we established HepG2 cell lines expressing major CYP enzymes involved in drug metabolism (CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and CYP oxidoreductase (POR) using the mammalian-derived artificial chromosome vector. Transchromosomic HepG2 (TC-HepG2) cells expressing four CYPs and POR were used to determine time- and concentration-dependent inhibition and toxicity of several compounds by luminescence detection of CYP-specific substrates and cell viability assays...
2017: PloS One
https://www.readbyqxmd.com/read/29063606/harnessing-meta-analysis-to-refine-an-oncology-patient-population-for-physiology-based-pharmacokinetic-modeling-of-drugs
#17
Emily Schwenger, Venkatesh Pilla Reddy, Ganesh Moorthy, Pradeep Sharma, Helen Tomkinson, Eric Masson, Karthick Vishwanathan
Certain oncology compounds exhibit fundamental PK disparities between healthy and malignant conditions. Given the effects of tumor-associated inflammation on enzyme and transporter expression, we performed a meta-analysis of CYP- and transporter-sensitive substrate clinical PK to quantitatively compare enzyme and transporter abundances between healthy volunteers (HV) and cancer patients (CP). Hepatic and intestinal CYP1A2, CYP2C19, and CYP3A4 abundance were subsequently adjusted via Simcyp®'s sensitivity analysis tool...
October 24, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29060457/a-pharmacokinetic-model-of-drug-drug-interaction-between-clopidogrel-and-omeprazole-at-cyp2c19-in-humans
#18
Wimonchat Tangamornsuksan, Pongpak Thiansupornpong, Thirawut Morasuk, Ornrat Lohitnavy, Manupat Lohitnavy
BACKGROUND: Clopidogrel is a thienopryridine antiplatelet agent commonly used in the management of cardiovascular diseases. Clopidogrel is metabolized by hepatic CYP2C19 and CYP2B6, therefore, co-administration of clopidogrel and CYP2C19 inhibitors can alter pharmacokinetics of clopidogrel. Omeprazole is a proton pump inhibitor used for decreasing gastric acid production. Omeprazole is known to be a potent inhibitor of CYP2C19. Thus when the drugs are simultaneously administered, clopidogrel plasma concentration levels can be increased...
July 2017: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/29054193/polymorphisms-of-cytochrome-p450-are-potential-candidates-that-could-potentially-help-clinicians-on-the-treatment-of-cardiovascular-diseases-among-asian-populations
#19
López-Hernández Daniel
There are significant ethnic differences in the metabolism of some drugs that can be explained by cytochrome P450 polymorphisms and, in particular, the CYP2D6 isozyme. In addition, among patients who are not carriers of the CYP2C19 loss-of-function alleles, there is a reduced risk of stroke when clopidogrel is taken with aspirin compared to aspirin alone. These findings demonstrate that there is inter-ethnic variability in the metabolism of some drugs, which results in different responses to cardiovascular drugs in Asian versus non-Asian populations...
September 2017: Indian Heart Journal
https://www.readbyqxmd.com/read/29050321/interaction-among-cyp2c8-gpiiia-and-p2y12-variants-increase-susceptibility-to-ischemic-stroke-in-chinese-population
#20
Xingyang Yi, Jing Lin, Yanfen Wang, Ju Zhou, Qiang Zhou
PURPOSE: Genetic variants in cytochrome P450 (CYP), platelet membrane receptor (P2Y12, P2Y1), and glycoprotein IIIa (GPIIIa) genes are associated with the efficacy of clopidogrel and adverse clinical events on ischemic stroke (IS) patients. However, few studies have assessed whether gene-gene interactions among these genes influence the risk of IS. The aim of the present study was to investigate the association of fifteen variants with IS and to determine whether these gene-gene interactions increase the risk of IS...
September 19, 2017: Oncotarget
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