Results 51 to 60 of about 44,899 (264)

Transgenic HepaRG cells expressing CYP2D6 as an improved model of primary human hepatocytes

Pharmacology Research & Perspectives, 2022
CYP2D6 and CYP3A4, which are members of the cytochrome P450 superfamily of metabolic enzymes, play major roles in the metabolism of commonly available drugs.
Shota Okuyama, Akari Mine, Teppei Nakamura, Yusuke Ohasi, Mayuko Seto, Masako Tada   +5 more
doaj   +1 more source

Differential quantification of CYP2D6 gene copy number by four different quantitative real-time PCR assays [PDF]

, 2010
Copy number variations (CNVs) in the CYP2D6 gene contribute to interindividual variation in drug metabolism. As the most common duplicated allele in Asian populations is the nonfunctional CYP2D6*36 allele, the goal of this study was to identify CNV ...
Flockhart, David A., Hosono, Naoya, Kubo, Michiaki, Nakamura, Yusuke, Ramamoorthy, Anuradha, Skaar, Todd C.   +5 more
core   +1 more source

Multi-site investigation of strategies for the clinical implementation of CYP2D6 genotyping to guide drug prescribing [PDF]

, 2019
PURPOSE: A number of institutions have clinically implemented CYP2D6 genotyping to guide drug prescribing. We compared implementation strategies of early adopters of CYP2D6 testing, barriers faced by both early adopters and institutions in the process
Beitelshees, Amber L., Bell, Gillian C., Bishop, Jeffrey R., Blake, Kathryn, Cavallari, Larisa H., Crona, Daniel J., Dressler, Lynn, Duong, Benjamin Q., Empey, Philip E., Gregg, Ryan A., Hicks, J. Kevin, Hines, Lindsay J., Johnson, Julie A., Lee, James C., Limdi, Nita A., Obeng, Aniwaa Owusu, Peterson, Josh F., Pratt, Victoria M., Prows, Cynthia A., Ramsey, Laura B., Scott, Stuart A., Shelton, Richard C., Skaar, Todd C., Smith, D. Max, Tuteja, Sony, Van Driest, Sara L., Weitzel, Kristin Wiisanen   +26 more
core   +1 more source

Real‐World Longitudinal Data on the Impact of Hydroxychloroquine Blood Level Monitoring on Lupus Outcomes: Results of a Prospective Longitudinal Cohort Study

Arthritis Care &Research, EarlyView.
Objective Hydroxychloroquine (HCQ) is a cornerstone therapy in systemic lupus erythematosus (SLE), but the weight‐based dosing does not account for clinical factors that can introduce individual variability in drug metabolism and clearance. We leveraged longitudinal data from a prospective SLE cohort to identify clinical factors that predict ...
Jay J. Patel, Fauzia Hollangel, Caroline Packee, Amita Kapoor, Brad Rovin, Nathalie Costedoat‐Chalumeau, Shivani Garg   +6 more
wiley   +1 more source

Clinical pharmacogenetics implementation consortium guideline (CPIC) for CYP2D6 and CYP2C19 genotypes and dosing of tricyclic antidepressants: 2016 update [PDF]

, 2017
CYP2D6 and CYP2C19 polymorphisms affect the exposure, efficacy and safety of tricyclic antidepressants (TCAs), with some drugs being affected by CYP2D6 only (e.g., nortriptyline and desipramine) and others by both polymorphic enzymes (e.g., amitriptyline,
Bishop, Jeffrey R., Caudle, Kelly E., Dunnenberger, Henry M., Ellingrod, Vicki L., Gaedigk, Andrea, Hicks, J. Kevin, Kharasch, Evan D., Klein, Teri E., Müller, Daniel J., Sangkuhl, Katrin, Shimoda, Kazutaka, Skaar, Todd C., Stingl, Julia C., Swen, Jesse J.   +13 more
core   +1 more source

Rolapitant Is a Reversible Inhibitor of CYP2D6 [PDF]

Drug Metabolism and Disposition, 2019
Rolapitant [(Varubi), 5S,8S)-8-[[(1R)-1-[3,5 bis(trifluoromethyl phenyl]ethoxy]methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one] is a high-affinity NK1 receptor antagonist that was approved in September 2015 as a treatment for nausea and vomiting caused by chemotherapy.
Sarah M, Glass, Sabrina M, Leddy, Michael C, Orwin, Garret P, Miller, Kyle A, Furge, Laura Lowe, Furge   +5 more
openaire   +2 more sources

Multimodal Multiorgan‐on‐a‐Chip Platform for Probing Liver‐Tumor Interactions and Advancing Prodrug Screening

Advanced Science, EarlyView.
This work introduces a multimodal multi‐OoC platform that overcomes current limitations in liver‐tumor interaction studies and prodrug screening. By integrating dynamic microfluidic circuits, electrochemical sensing, and mass analysis, this platform enables non‐invasive, longitudinal monitoring of drug metabolism and hepatotoxicity, offering a ...
Dan Wang, Yisong Huang, Weijian Zhao, Tian Chen, Siyu Bai, Denghui Guo, Mengying Wang, Yaoyao Zhao, Liang Zhao, Guangsheng Guo, Xiayan Wang   +10 more
wiley   +1 more source

An increase in urinary primaquine and a reduction in urinary primaquine-5,6-orthoquinone in the Thai population with CYP2D6 reduced enzyme function

Heliyon
Objectives: Primaquine is metabolized by the cytochrome P450-2D6 enzyme (CYP2D6) to an active primaquine-5,6-orthoquinone (POQ). No relationships of CYP2D6 polymorphisms with the pharmacokinetics of primaquine and POQ were reported in the Thai population.
Waritda Pookmanee, Siriwan Thongthip, Mathirut Mungthin, Chonlaphat Sukasem, Jeeranut Tankanitlert, Pajaree Chariyavilaskul, Supeecha Wittayalertpanya   +6 more
doaj   +1 more source

Tamoxifen and CYP2D6: A Contradiction of Data [PDF]

The Oncologist, 2012
Abstract Learning Objectives: After completing this course, the reader will be able to: Describe the significant heterogeneity among the published studies on the link between CYP2D6 genotype and tamoxifen treatment efficacy.Explain the role of CYP2D6 metabolism in the conversion of tamoxifen to its ...
Daniel L, Hertz, Howard L, McLeod, William J, Irvin   +2 more
openaire   +2 more sources

Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors

Advanced Science, EarlyView.
This study presents the first ubiquitin‐specific protease 1 (USP1) allosteric fluoroprobe and fluorescence polarization assay, enabling the differentiation of allosteric and catalytic site inhibitors. Further, a novel class of tetrahydroisoquinoline‐based USP1 inhibitors is designed, with compound 14a (USP1 IC50 = 29.9 nM) showing strong selectivity ...
Jiawei Cheng, Peipei Wang, Pengfei Wang, Jiamin Wang, Baiyang Li, Daqing Fang, Jian He, Xiaobei Hu, Weijuan Kan, Yubo Zhou, Chunpu Li, Jia Li, Hong Liu   +12 more
wiley   +1 more source