Search Results - "Drug metabolism and disposition"

Indole and Tryptophan Metabolism: Endogenous and Dietary Routes to Ah Receptor Activation by Hubbard, Troy D, Murray, Iain A, Perdew, Gary H

“…The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor recognized for its role in xenobiotic metabolism. The physiologic function of…”
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Physiologically Based Pharmacokinetic (PBPK) Modeling and Simulation Approaches: A Systematic Review of Published Models, Applications, and Model Verification by Sager, Jennifer E, Yu, Jingjing, Ragueneau-Majlessi, Isabelle, Isoherranen, Nina

“…Modeling and simulation of drug disposition has emerged as an important tool in drug development, clinical study design and regulatory review, and the number…”
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Trimethylamine and Trimethylamine N-Oxide, a Flavin-Containing Monooxygenase 3 (FMO3)-Mediated Host-Microbiome Metabolic Axis Implicated in Health and Disease by Fennema, Diede, Phillips, Ian R, Shephard, Elizabeth A

“…Flavin-containing monooxygenase 3 (FMO3) is known primarily as an enzyme involved in the metabolism of therapeutic drugs. On a daily basis, however, we are…”
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Disposition of Nirmatrelvir, an Orally Bioavailable Inhibitor of SARS-CoV-2 3C-Like Protease, across Animals and Humans by Eng, Heather, Dantonio, Alyssa L, Kadar, Eugene P, Obach, R Scott, Di, Li, Lin, Jian, Patel, Nandini C, Boras, Britton, Walker, Gregory S, Novak, Jonathan J, Kimoto, Emi, Singh, Ravi Shankar P, Kalgutkar, Amit S

“…The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3C-like protease inhibitor PF-07321332 (nirmatrelvir), in combination with ritonavir…”
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Simultaneous absolute protein quantification of transporters, cytochromes P450, and UDP-glucuronosyltransferases as a novel approach for the characterization of individual human liver: comparison with mRNA levels and activities by Ohtsuki, Sumio, Schaefer, Olaf, Kawakami, Hirotaka, Inoue, Tae, Liehner, Stephanie, Saito, Asami, Ishiguro, Naoki, Kishimoto, Wataru, Ludwig-Schwellinger, Eva, Ebner, Thomas, Terasaki, Tetsuya

“…The purpose of the present study was to determine the absolute protein expression levels of multiple drug-metabolizing enzymes and transporters in 17 human…”
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Identification of the Human Cytochrome P450 Enzymes Involved in the Two Oxidative Steps in the Bioactivation of Clopidogrel to Its Pharmacologically Active Metabolite by KAZUI, Miho, NISHIYA, Yumi, ISHIZUKA, Tomoko, HAGIHARA, Katsunobu, FARID, Nagy A, OKAZAKI, Osamu, IKEDA, Toshihiko, KURIHARA, Atsushi

“…The aim of the current study is to identify the human cytochrome P450 (P450) isoforms involved in the two oxidative steps in the bioactivation of clopidogrel…”
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Cannabinoid Metabolites as Inhibitors of Major Hepatic CYP450 Enzymes, with Implications for Cannabis-Drug Interactions by Nasrin, Shamema, Watson, Christy J W, Perez-Paramo, Yadira X, Lazarus, Philip

“…The legalization of cannabis in many parts of the United States and other countries has led to a need for a more comprehensive understanding of cannabis…”
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Emerging Roles of the Human Solute Carrier 22 Family by Yee, Sook Wah, Giacomini, Kathleen M

“…The human Solute Carrier 22 family (SLC22), also termed the organic ion transporter family, consists of 28 distinct multi-membrane spanning proteins, which…”
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Expression of hepatic drug-metabolizing cytochrome p450 enzymes and their intercorrelations: a meta-analysis by Achour, Brahim, Barber, Jill, Rostami-Hodjegan, Amin

“…Cytochrome P450 is a family of enzymes that catalyze reactions involved in the metabolism of drugs and other xenobiotics. These enzymes are therefore important…”
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Gestational Age-Dependent Abundance of Human Placental Transporters as Determined by Quantitative Targeted Proteomics by Anoshchenko, Olena, Prasad, Bhagwat, Neradugomma, Naveen K, Wang, Joanne, Mao, Qingcheng, Unadkat, Jashvant D

“…Some women take medication during pregnancy to address a variety of clinical conditions. Because of ethical and logistical concerns, it is impossible to…”
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Inhibition of the multidrug resistance P-glycoprotein: time for a change of strategy? by Callaghan, Richard, Luk, Frederick, Bebawy, Mary

“…P-glycoprotein (P-gp) is a key player in the multidrug-resistant phenotype in cancer. The protein confers resistance by mediating the ATP-dependent efflux of…”
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Brain Exposure of Two Selective Dual CDK4 and CDK6 Inhibitors and the Antitumor Activity of CDK4 and CDK6 Inhibition in Combination with Temozolomide in an Intracranial Glioblastoma Xenograft by Raub, Thomas J, Wishart, Graham N, Kulanthaivel, Palaniappan, Staton, Brian A, Ajamie, Rose T, Sawada, Geri A, Gelbert, Lawrence M, Shannon, Harlan E, Sanchez-Martinez, Concepcion, De Dios, Alfonso

“…Effective treatments for primary brain tumors and brain metastases represent a major unmet medical need. Targeting the CDK4/CDK6-cyclin D1-Rb-p16/ink4a pathway…”
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Commensal Gut Bacteria Convert the Immunosuppressant Tacrolimus to Less Potent Metabolites by Guo, Yukuang, Crnkovic, Camila Manoel, Won, Kyoung-Jae, Yang, Xiaotong, Lee, John Richard, Orjala, Jimmy, Lee, Hyunwoo, Jeong, Hyunyoung

“…Tacrolimus exhibits low and variable drug exposure after oral dosing, but the contributing factors remain unclear. Based on our recent report showing a…”
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The pharmacokinetics, metabolism, and clearance mechanisms of tofacitinib, a janus kinase inhibitor, in humans by Dowty, Martin E, Lin, Jinyan, Ryder, Tim F, Wang, Weiwei, Walker, Gregory S, Vaz, Alfin, Chan, Gary L, Krishnaswami, Sriram, Prakash, Chandra

“…Tofacitinib is a novel, oral Janus kinase inhibitor. The objectives of this study were to summarize the pharmacokinetics and metabolism of tofacitinib in…”
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Drug Concentration Asymmetry in Tissues and Plasma for Small Molecule-Related Therapeutic Modalities by Zhang, Donglu, Hop, Cornelis E C A, Patilea-Vrana, Gabriela, Gampa, Gautham, Seneviratne, Herana Kamal, Unadkat, Jashvant D, Kenny, Jane R, Nagapudi, Karthik, Di, Li, Zhou, Lian, Zak, Mark, Wright, Matthew R, Bumpus, Namandjé N, Zang, Richard, Liu, Xingrong, Lai, Yurong, Khojasteh, S Cyrus

“…The well accepted "free drug hypothesis" for small-molecule drugs assumes that only the free (unbound) drug concentration at the therapeutic target can elicit…”
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Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds by Lombardo, Franco, Berellini, Giuliano, Obach, R Scott

“…We report a trend analysis of human intravenous pharmacokinetic data on a data set of 1352 drugs. The aim in building this data set and its detailed analysis…”
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Transcriptional, Functional, and Mechanistic Comparisons of Stem Cell-Derived Hepatocytes, HepaRG Cells, and Three-Dimensional Human Hepatocyte Spheroids as Predictive In Vitro Systems for Drug-Induced Liver Injury by Bell, Catherine C, Lauschke, Volker M, Vorrink, Sabine U, Palmgren, Henrik, Duffin, Rodger, Andersson, Tommy B, Ingelman-Sundberg, Magnus

“…Reliable and versatile hepatic in vitro systems for the prediction of drug pharmacokinetics and toxicity are essential constituents of preclinical safety…”
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In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans by Dawson, Sarah, Stahl, Simone, Paul, Nikki, Barber, Jane, Kenna, J Gerald

“…Inhibition of the activity of the human bile salt export pump (BSEP: ABCB11) has been proposed to play a role in drug-induced liver injury (DILI). To enhance…”
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Absorption, Distribution, Metabolism, and Excretion of US Food and Drug Administration-Approved Antisense Oligonucleotide Drugs by Migliorati, Julia M, Liu, Sunna, Liu, Anna, Gogate, Anagha, Nair, Sreenidhi, Bahal, Raman, Rasmussen, Theodore P, Manautou, José E, Zhong, Xiao-Bo

“…Absorption, distribution, metabolism, and excretion (ADME) are the key biologic processes for determination of a drug's pharmacokinetic parameters, which have…”
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Berberine Directly Affects the Gut Microbiota to Promote Intestinal Farnesoid X Receptor Activation by Tian, Yuan, Cai, Jingwei, Gui, Wei, Nichols, Robert G, Koo, Imhoi, Zhang, Jingtao, Anitha, Mallappa, Patterson, Andrew D

“…Intestinal bacteria play an important role in bile acid metabolism and in the regulation of multiple host metabolic pathways (e.g., lipid and glucose…”
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