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Radiolabel Uncovers Nonintuitive Metabolites of BIIB104: Novel Release of [14C]Cyanide from 2-Cyanothiophene and Subsequent Formation of [14C]Thiocyanate [Articles]
Radiolabel Uncovers Nonintuitive Metabolites of BIIB104: Novel Release of [14C]Cyanide from 2-Cyanothiophene and Subsequent Formation of [14C]Thiocyanate [Articles]
AbstractBIIB104 (formerly PF-04958242), N-((3S,4S)-4-(4-(5-cyanothiophen-2-yl)phenoxy)tetrahydrofuran-3-yl)propane-2-sulfo...
Enzymatic Defluorination of a Terminally Monofluorinated Pentyl Moiety: Oxidative or Hydrolytic Mechanism? [Articles]
Enzymatic Defluorination of a Terminally Monofluorinated Pentyl Moiety: Oxidative or Hydrolytic Mechanism? [Articles]
AbstractFluorination of organic compounds plays an important role in the chemical and pharmaceutical industry and is often...
Improving In Vitro-In Vivo Extrapolation of Clearance Using Rat Liver Microsomes for Highly Plasma Protein-Bound Molecules [Articles]
Improving In Vitro-In Vivo Extrapolation of Clearance Using Rat Liver Microsomes for Highly Plasma Protein-Bound Molecules [Articles]
AbstractIt is common practice in drug discovery and development to predict in vivo hepatic clearance from in vitro incubat...
Pharmacokinetic Effects of Different Models of Nonalcoholic Fatty Liver Disease in Transgenic Humanized OATP1B Mice [Articles]
Pharmacokinetic Effects of Different Models of Nonalcoholic Fatty Liver Disease in Transgenic Humanized OATP1B Mice [Articles]
AbstractOrganic anion transporting polypeptide (OATP) 1B1 and OATP1B3 (collectively, OATP1B) transporters encoded by the s...
Identification and Biosynthesis of an N-Glucuronide Metabolite of Camonsertib [Articles]
Identification and Biosynthesis of an N-Glucuronide Metabolite of Camonsertib [Articles]
AbstractCamonsertib is a novel ATR kinase inhibitor in clinical development for advanced cancers targeting sensitizing mut...
In Vitro to In Vivo Scalars for Drug Clearance in Nonalcoholic Fatty Liver and Steatohepatitis [Articles]
In Vitro to In Vivo Scalars for Drug Clearance in Nonalcoholic Fatty Liver and Steatohepatitis [Articles]
AbstractIn vitro–in vivo extrapolation (IVIVE) allows prediction of clinical outcomes across populations from in vitro dat...
An Integrated Hepatocyte Stability Assay for Simultaneous Metabolic Stability Assessment and Metabolite Profiling [Articles]
An Integrated Hepatocyte Stability Assay for Simultaneous Metabolic Stability Assessment and Metabolite Profiling [Articles]
AbstractThe determination of metabolic stability is critical for drug discovery programs, allowing for the optimization of...
Activation of the YY1-UGT2B7 Axis Promotes Mammary Estrogen Homeostasis Dysregulation and Exacerbates Breast Tumor Metastasis [Articles]
Activation of the YY1-UGT2B7 Axis Promotes Mammary Estrogen Homeostasis Dysregulation and Exacerbates Breast Tumor Metastasis [Articles]
AbstractMetastasis is the most common pathway of cancer death. The lack of effective predictors of breast cancer metastasi...
Low Molecular Weight Acids and Organic Anion Transporting Polypeptide (OATP1B)-Mediated Hepatic Clearance: In Vitro and In Vivo Evaluation Using Novel Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (Dustats) [Articles]
Low Molecular Weight Acids and Organic Anion Transporting Polypeptide (OATP1B)-Mediated Hepatic Clearance: In Vitro and In Vivo Evaluation Using Novel Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (Dustats) [Articles]
AbstractOrganic anion transporting polypeptide (OATP1B) plays a key role in the hepatic clearance of a majority of high mo...
CYP7A1 Gene Induction via SHP-Dependent or Independent Mechanisms can Increase the Risk of Drug-Induced Liver Injury Independently or in Synergy with BSEP Inhibition [Articles]
CYP7A1 Gene Induction via SHP-Dependent or Independent Mechanisms can Increase the Risk of Drug-Induced Liver Injury Independently or in Synergy with BSEP Inhibition [Articles]
AbstractDrug-induced liver injury (DILI) is a frequent cause of clinical trial failures during drug development. While inh...
Projections of Drug-Drug Interactions Caused by Time-Dependent Inhibitors of Cytochrome P450 1A2, 2B6, 2C8, 2C9, 2C19, and 2D6 Using In Vitro Data in Static and Dynamic Models [Articles]
Projections of Drug-Drug Interactions Caused by Time-Dependent Inhibitors of Cytochrome P450 1A2, 2B6, 2C8, 2C9, 2C19, and 2D6 Using In Vitro Data in Static and Dynamic Models [Articles]
AbstractIn vitro time-dependent inhibition (TDI) kinetic parameters for cytochrome P450 (P450) 1A2, 2B6, 2C8, 2C9, 2C19, a...
Pharmacogenetic Influence on Stereoselective Steady-State Disposition of Bupropion [Articles]
Pharmacogenetic Influence on Stereoselective Steady-State Disposition of Bupropion [Articles]
AbstractBupropion is used for treating depression, obesity, and seasonal affective disorder, and for smoking cessation. Bu...
LX-2 Stellate Cells Are a Model System for Investigating the Regulation of Hepatic Vitamin A Metabolism and Respond to Tumor Necrosis Factor {alpha} and Interleukin 1{beta} [Articles]
LX-2 Stellate Cells Are a Model System for Investigating the Regulation of Hepatic Vitamin A Metabolism and Respond to Tumor Necrosis Factor {alpha} and Interleukin 1{beta} [Articles]
AbstractHepatic stellate cells (HSCs) are the major site of vitamin A (retinol) esterification and subsequent storage as r...
Gut Microbiome Integration in Drug Discovery and Development of Small Molecules [Minireview]
Gut Microbiome Integration in Drug Discovery and Development of Small Molecules [Minireview]
AbstractHuman microbiomes, particularly in the gut, could have a major impact on the efficacy and toxicity of drugs. Howev...
Cytosolic 5'-Nucleotidase III and Nucleoside Triphosphate Diphosphohydrolase 1 Dephosphorylate the Pharmacologically Active Metabolites of Gemcitabine and Emtricitabine [Articles]
Cytosolic 5'-Nucleotidase III and Nucleoside Triphosphate Diphosphohydrolase 1 Dephosphorylate the Pharmacologically Active Metabolites of Gemcitabine and Emtricitabine [Articles]
AbstractGemcitabine (dFdC) and emtricitabine (FTC) are first-line drugs that are used for the treatment of pancreatic canc...
Use of a Double-Transfected System to Predict hOCT2/hMATE1-Mediated Renal Drug-Drug Interactions [Articles]
Use of a Double-Transfected System to Predict hOCT2/hMATE1-Mediated Renal Drug-Drug Interactions [Articles]
AbstractAccurate predictions of renal drug–drug interactions (DDIs) mediated by the human organic cation transporter 2 (hO...
Novel Tree Shrew Cytochrome P450 2Ds (CYP2D8a and CYP2D8b) Are Functional Drug-Metabolizing Enzymes that Metabolize Bufuralol and Dextromethorphan [Articles]
Novel Tree Shrew Cytochrome P450 2Ds (CYP2D8a and CYP2D8b) Are Functional Drug-Metabolizing Enzymes that Metabolize Bufuralol and Dextromethorphan [Articles]
AbstractTree shrews are a nonprimate species used in a range of biomedical studies. Recent genome analysis of tree shrews ...
Interaction and Transport of Benzalkonium Chlorides by the Organic Cation and Multidrug and Toxin Extrusion Transporters [Articles]
Interaction and Transport of Benzalkonium Chlorides by the Organic Cation and Multidrug and Toxin Extrusion Transporters [Articles]
AbstractHumans are chronically exposed to benzalkonium chlorides (BACs) from environmental sources. The U.S. Food and Drug...
Correction to "Dissecting Parameters Contributing to the Underprediction of Aldehyde Oxidase-Mediated Metabolic Clearance of Drugs" [Erratum]
Correction to "Dissecting Parameters Contributing to the Underprediction of Aldehyde Oxidase-Mediated Metabolic Clearance of Drugs" [Erratum]
The above article [Subash S, Singh DK, Ahire DS, Khojasteh SC, Murray BP, Zientek MA, Jones RS, Kulkarni P, Smith BJ, Heyw...
Recommendations on the Use of Multiple Labels in Human Mass Balance Studies [Minireview]
Recommendations on the Use of Multiple Labels in Human Mass Balance Studies [Minireview]
AbstractThe administration of radiolabeled drug candidates is considered the gold standard in absorption, distribution, me...
Leveraging in Vitro Models for Clinically Relevant Rare CYP2D6 Variants in Pharmacogenomics [Minireview]
Leveraging in Vitro Models for Clinically Relevant Rare CYP2D6 Variants in Pharmacogenomics [Minireview]
AbstractCytochrome P450 2D6 (CYP2D6) is responsible for the metabolism of up to 20% of small-molecule drugs and therefore,...
Chronic Exposure to E-Cigarettes Elevates CYP2A5 Activity, Protein Expression, and Cotinine-Induced Production of Reactive Oxygen Species in Mice [Articles]
Chronic Exposure to E-Cigarettes Elevates CYP2A5 Activity, Protein Expression, and Cotinine-Induced Production of Reactive Oxygen Species in Mice [Articles]
AbstractCoumarin 7’-hydroxylase activity, a specific marker of CYP2A5 activity, and the protein level were measured in liv...
Effects of Strong Inhibition of Cytochrome P450 3A and UDP glucuronosyltransferase 1A9 and Strong Induction of Cytochrome P450 3A on the Pharmacokinetics, Safety, and Tolerability of Soticlestat: Two Drug-Drug Interaction Studies in Healthy Volunteers [Articles]
Effects of Strong Inhibition of Cytochrome P450 3A and UDP glucuronosyltransferase 1A9 and Strong Induction of Cytochrome P450 3A on the Pharmacokinetics, Safety, and Tolerability of Soticlestat: Two Drug-Drug Interaction Studies in Healthy Volunteers [Articles]
AbstractTwo open-label, phase 1 studies (NCT05064449, NCT05098041) investigated the effects of cytochrome P450 (CYP) 3A i...
Dihydrotanshinone I-Induced CYP1 Enzyme Inhibition and Alteration of Estradiol Metabolism [Articles]
Dihydrotanshinone I-Induced CYP1 Enzyme Inhibition and Alteration of Estradiol Metabolism [Articles]
State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics...
Association of Valproic Acid and Its Main Metabolites Plasma Concentrations with Clinical Outcomes among Epilepsy Patients: A 10-Year Retrospective Study Based on Therapeutic Drug Monitoring [Articles]
Association of Valproic Acid and Its Main Metabolites Plasma Concentrations with Clinical Outcomes among Epilepsy Patients: A 10-Year Retrospective Study Based on Therapeutic Drug Monitoring [Articles]
Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China (R.L., S.T...
The Current Status and Use of Microphysiological Systems by the Pharmaceutical Industry: The International Consortium for Innovation and Quality Microphysiological Systems Affiliate Survey and Commentary [Articles]
The Current Status and Use of Microphysiological Systems by the Pharmaceutical Industry: The International Consortium for Innovation and Quality Microphysiological Systems Affiliate Survey and Commentary [Articles]
AbstractMicrophysiological systems (MPS) are comprised of one or multiple cell types of human or animal origins that mimic...
Correlation of In Vitro Kinetic Stability to Preclinical In Vivo Pharmacokinetics for a Panel of Anti-PD-1 Monoclonal Antibody Interleukin 21 Mutein Immunocytokines [Articles]
Correlation of In Vitro Kinetic Stability to Preclinical In Vivo Pharmacokinetics for a Panel of Anti-PD-1 Monoclonal Antibody Interleukin 21 Mutein Immunocytokines [Articles]
AbstractThe development of therapeutic fusion protein drugs is often impeded by the unintended consequences that occur fro...
Identification and Functional Assessment of Eight CYP3A4 Allelic Variants *39-*46 Detected in the Chinese Han Population [Articles]
Identification and Functional Assessment of Eight CYP3A4 Allelic Variants *39-*46 Detected in the Chinese Han Population [Articles]
AbstractCytochrome P450 3A4 (CYP3A4), a key enzyme, is pivotal in metabolizing approximately half of the drugs used clinic...
Biocatalysis using Thermostable Cytochrome P450 Enzymes in Bacterial Membranes - Comparison of Metabolic Pathways with Human Liver Microsomes and Recombinant Human Enzymes [Articles]
Biocatalysis using Thermostable Cytochrome P450 Enzymes in Bacterial Membranes - Comparison of Metabolic Pathways with Human Liver Microsomes and Recombinant Human Enzymes [Articles]
AbstractDetailed structural characterization of small molecule metabolites is desirable during all stages of drug developm...
Assessing Pleiotropic Effects of a Mixed-Mode Perpetrator Drug, Rifampicin, by Multiple Endogenous Biomarkers in Dogs [Articles]
Assessing Pleiotropic Effects of a Mixed-Mode Perpetrator Drug, Rifampicin, by Multiple Endogenous Biomarkers in Dogs [Articles]
AbstractRifampicin (RIF) is a mixed-mode perpetrator that produces pleiotropic effects on liver cytochrome P450 enzymes an...
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