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PMC11987044 | core_pubmed_pmc | AI‐Driven Applications in Clinical Pharmacology and Translational Science: Insights From the ASCPT 2024 AI Preconference | AI‐Driven Applications in Clinical Pharmacology and Translational Science: Insights From the ASCPT 2024 AI Preconference Abstract ABSTRACT Artificial intelligence (AI) is driving innovation in clinical pharmacology and translational science with tools to advance drug development, clinical trials, and patient care. This... |
PMC8703159 | core_pubmed_pmc | The Pharmacokinetics of Beta-Lactam Antibiotics Using Scavenged Samples in Pediatric Intensive Care Patients: The EXPAT Kids Study Protocol | The Pharmacokinetics of Beta-Lactam Antibiotics Using Scavenged Samples in Pediatric Intensive Care Patients: The EXPAT Kids Study Protocol Abstract Abstract Background: Emerging evidence supports the importance of optimized antibiotic exposure in pediatric intensive care unit (PICU) patients. Traditional antibiotic do... |
PMC9664596 | core_pubmed_pmc | Efficacy and pharmacokinetics of betaine in CBS and cblC deficiencies: a cross-over randomized controlled trial | Efficacy and pharmacokinetics of betaine in CBS and cblC deficiencies: a cross-over randomized controlled trial Abstract Abstract Background Betaine is an “alternate” methyl donor for homocysteine remethylation catalyzed by betaine homocysteine methyltransferase (BHMT), an enzyme mainly expressed in the liver and kidne... |
PMC5522996 | core_pubmed_pmc | Big conductance calcium‐activated potassium channel openers control spasticity without sedation | Big conductance calcium‐activated potassium channel openers control spasticity without sedation Abstract Background and Purpose Our initial aim was to generate cannabinoid agents that control spasticity, occurring as a consequence of multiple sclerosis (MS), whilst avoiding the sedative side effects associated with can... |
PMC8192039 | core_pubmed_pmc | Engineering Quick- and Long-acting Naloxone Delivery Systems for Treating Opioid Overdose | Engineering Quick- and Long-acting Naloxone Delivery Systems for Treating Opioid Overdose Abstract Abstract Purpose Opioids have been the main factor for drug overdose deaths in the United States. Current naloxone delivery systems are effective in mitigating the opioid effects only for hours. Naloxone-loaded poly(lacti... |
PMC9401461 | core_pubmed_pmc | Phase 1 Trial of ALRN-6924, a Dual Inhibitor of MDMX and MDM2, in Patients with Solid Tumors and Lymphomas Bearing Wild-type TP53 | Phase 1 Trial of ALRN-6924, a Dual Inhibitor of MDMX and MDM2, in Patients with Solid Tumors and Lymphomas Bearing Wild-type TP53 Abstract Abstract Purpose: We describe the first-in-human dose-escalation trial for ALRN-6924, a stabilized, cell-permeating peptide that disrupts p53 inhibition by mouse double minute 2 (MD... |
PMC12167921 | core_pubmed_pmc | Effect of Cumulative Exposure on the Efficacy of Paroxetine: A Population Pharmacokinetic‐Pharmacodynamic and Machine Learning Analyses | Effect of Cumulative Exposure on the Efficacy of Paroxetine: A Population Pharmacokinetic‐Pharmacodynamic and Machine Learning Analyses Abstract ABSTRACT Selective serotonin reuptake inhibitors (SSRIs) are widely used in depression treatment. However, the relationship between treatment efficacy and plasma concentration... |
PMC7884051 | core_pubmed_pmc | “Identification of Nafamostat and VR23 as COVID-19 drug candidates by targeting 3CL pro and PL pro " | “Identification of Nafamostat and VR23 as COVID-19 drug candidates by targeting 3CL pro and PL pro " Abstract The sudden increase in the COVID-19 epidemic affected by novel coronavirus 2019 has jeopardized public health worldwide. Hence the necessities of a drug or therapeutic agent that heal SARS-CoV-2 infections are ... |
PMC10835732 | core_pubmed_pmc | Pharmacokinetics of Hydroxytyrosol and Its Sulfate and Glucuronide Metabolites after the Oral Administration of Table Olives to Sprague-Dawley Rats | Pharmacokinetics of Hydroxytyrosol and Its Sulfate and Glucuronide Metabolites after the Oral Administration of Table Olives to Sprague-Dawley Rats Abstract The pharmacokinetics (PK) of hydroxytyrosol and its metabolites were characterized following oral administration to Sprague-Dawley rats of 3.85 and 7.70 g of desto... |
PMC7761673 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics and Drug–Drug Interactions of New Anti-Migraine Drugs—Lasmiditan, Gepants, and Calcitonin-Gene-Related Peptide (CGRP) Receptor Monoclonal Antibodies | Pharmacokinetics, Pharmacodynamics and Drug–Drug Interactions of New Anti-Migraine Drugs—Lasmiditan, Gepants, and Calcitonin-Gene-Related Peptide (CGRP) Receptor Monoclonal Antibodies Abstract Abstract In the last few years, there have been significant advances in migraine management and prevention. Lasmiditan, ubrogep... |
PMC8511786 | core_pubmed_pmc | Toward Predicting Impact of Common Genetic Variants on Schizophrenia Clinical Responses With Antipsychotics: A Quantitative System Pharmacology Study | Toward Predicting Impact of Common Genetic Variants on Schizophrenia Clinical Responses With Antipsychotics: A Quantitative System Pharmacology Study Abstract Abstract CNS disorders are lagging behind other indications in implementing genotype-dependent treatment algorithms for personalized medicine. This report uses a... |
PMC10947261 | core_pubmed_pmc | Pharmacokinetic pharmacodynamic modeling of analgesics and sedatives in children | Pharmacokinetic pharmacodynamic modeling of analgesics and sedatives in children Abstract Abstract Pharmacokinetic pharmacodynamic modeling is an important tool which uses statistical methodology to provide a better understanding of the relationship between concentration and effect of drugs such as analgesics and sedat... |
PMC8121789 | core_pubmed_pmc | Characterization of an engineered live bacterial therapeutic for the treatment of phenylketonuria in a human gut-on-a-chip | Characterization of an engineered live bacterial therapeutic for the treatment of phenylketonuria in a human gut-on-a-chip Abstract Engineered bacteria (synthetic biotics) represent a new class of therapeutics that leverage the tools of synthetic biology. Translational testing strategies are required to predict synthet... |
PMC9147171 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Evaluation of a New Purine-2,6-Dione Derivative in Rodents with Experimental Autoimmune Diseases | Pharmacokinetic/Pharmacodynamic Evaluation of a New Purine-2,6-Dione Derivative in Rodents with Experimental Autoimmune Diseases Abstract Current treatment strategies of autoimmune diseases (ADs) display a limited efficacy and cause numerous adverse effects. Phosphodiesterase (PDE)4 and PDE7 inhibitors have been studie... |
PMC5337879 | core_pubmed_pmc | Peritoneal Nebulization of Ropivacaine during Laparoscopic Cholecystectomy: Dose Finding and Pharmacokinetic Study | Peritoneal Nebulization of Ropivacaine during Laparoscopic Cholecystectomy: Dose Finding and Pharmacokinetic Study Abstract Background . Intraperitoneal nebulization of ropivacaine reduces postoperative pain and morphine consumption after laparoscopic surgery. The aim of this multicenter double-blind randomized control... |
PMC8447941 | core_pubmed_pmc | Synthetic Pept-Ins as a Generic Amyloid-Like Aggregation-Based Platform for In Vivo PET Imaging of Intracellular Targets | Synthetic Pept-Ins as a Generic Amyloid-Like Aggregation-Based Platform for In Vivo PET Imaging of Intracellular Targets Abstract Amyloid-like aggregation of proteins is induced by short amyloidogenic sequence segments within a specific protein sequence resulting in self-assembly into β-sheets. We recently validated a ... |
PMC7725875 | core_pubmed_pmc | The Pharmacokinetics, Tissue Distribution, Metabolism, and Excretion of Pinostrobin in Rats: Ultra-High-Performance Liquid Chromatography Coupled With Linear Trap Quadrupole Orbitrap Mass Spectrometry Studies | The Pharmacokinetics, Tissue Distribution, Metabolism, and Excretion of Pinostrobin in Rats: Ultra-High-Performance Liquid Chromatography Coupled With Linear Trap Quadrupole Orbitrap Mass Spectrometry Studies Abstract Pinostrobin is a natural flavonoid found in various plants, well known for its wide range of pharmacol... |
PMC5597703 | core_pubmed_pmc | Evaluation of the Population Pharmacokinetic Properties of Lidocaine and its Metabolites After Long-Term Multiple Applications of a Lidocaine Plaster in Post-Herpetic Neuralgia Patients | Evaluation of the Population Pharmacokinetic Properties of Lidocaine and its Metabolites After Long-Term Multiple Applications of a Lidocaine Plaster in Post-Herpetic Neuralgia Patients Abstract Abstract Background and Objectives Lidocaine 5% medicated plaster is the first lidocaine containing product for chronic use. ... |
PMC11860008 | core_pubmed_pmc | Prediction of Pharmacokinetics for CYP3A4-Metabolized Drugs in Pediatrics and Geriatrics Using Dynamic Age-Dependent Physiologically Based Pharmacokinetic Models | Prediction of Pharmacokinetics for CYP3A4-Metabolized Drugs in Pediatrics and Geriatrics Using Dynamic Age-Dependent Physiologically Based Pharmacokinetic Models Abstract Abstract Background/Objectives : The use of medicines in pediatrics and geriatrics is widespread. However, information on pharmacokinetics of therape... |
PMC12156175 | core_pubmed_pmc | Enhancing Oral Absorption of Quercetin Through Multifactorial Synergies in Crystal Dispersion Systems | Enhancing Oral Absorption of Quercetin Through Multifactorial Synergies in Crystal Dispersion Systems Abstract This study aims to enhance the dissolution rate and oral absorption of quercetin (QUR) by formulating quercetin crystalline solid dispersion (QUR-CSD). Quercetin, as a natural antioxidant, can effectively neut... |
PMC9694406 | core_pubmed_pmc | Prospective Validation and Refinement of a Population Pharmacokinetic Model of Fludarabine in Children and Young Adults Undergoing Hematopoietic Cell Transplantation | Prospective Validation and Refinement of a Population Pharmacokinetic Model of Fludarabine in Children and Young Adults Undergoing Hematopoietic Cell Transplantation Abstract Abstract Fludarabine is a nucleoside analog with antileukemic and immunosuppressive activity commonly used in allogeneic hematopoietic cell trans... |
PMC12067525 | core_pubmed_pmc | Effect of tripterine on the pharmacokinetics of cyclosporine A and its mechanism in rats | Effect of tripterine on the pharmacokinetics of cyclosporine A and its mechanism in rats Abstract Tripterine is a key active component in Tripterygium wilfordii polyglycosides tablets. Cyclosporine A (CsA) is an immunosuppressive drug that is widely used in organ transplantation. The combined use of Tripterygium wilfor... |
PMC12196478 | core_pubmed_pmc | Tissue Distribution and Pharmacokinetic Characteristics of Aztreonam Based on Multi-Species PBPK Model | Tissue Distribution and Pharmacokinetic Characteristics of Aztreonam Based on Multi-Species PBPK Model Abstract Background/Objectives : As a monocyclic β-lactam antibiotic, aztreonam has regained attention recently because combining it with β-lactamase inhibitors helps fight drug-resistant bacteria. This study aimed to... |
PMC9054278 | core_pubmed_pmc | A novel biocompatible, simvastatin-loaded, bone-targeting lipid nanocarrier for treating osteoporosis more effectively † | A novel biocompatible, simvastatin-loaded, bone-targeting lipid nanocarrier for treating osteoporosis more effectively † Abstract An insufficient drug concentration at the target site and drug efflux resulting in poor efficacy are recognized as important obstacles in osteoporosis treatment. Simvastatin (SIM), which can... |
PMC10330959 | core_pubmed_pmc | Population pharmacokinetic analysis of transdermal granisetron in healthy Chinese and Caucasian volunteers | Population pharmacokinetic analysis of transdermal granisetron in healthy Chinese and Caucasian volunteers Abstract Granisetron patches are a prolonged delivery transdermal system that is used to prevent Chemotherapy-induced nausea and vomiting (CINV). To date, no pharmacokinetics comparison between Chinese and Caucasi... |
PMC10706259 | core_pubmed_pmc | Pharmacokinetic Profiling of Ginsenosides, Rb1, Rd, and Rg3, in Mice with Antibiotic-Induced Gut Microbiota Alterations: Implications for Variability in the Therapeutic Efficacy of Red Ginseng Extracts | Pharmacokinetic Profiling of Ginsenosides, Rb1, Rd, and Rg3, in Mice with Antibiotic-Induced Gut Microbiota Alterations: Implications for Variability in the Therapeutic Efficacy of Red Ginseng Extracts Abstract Ginsenoside Rg3 is reported to contribute to the traditionally known diverse effects of red ginseng extracts.... |
PMC8468656 | core_pubmed_pmc | PBPK Modeling as a Tool for Predicting and Understanding Intestinal Metabolism of Uridine 5′-Diphospho-glucuronosyltransferase Substrates | PBPK Modeling as a Tool for Predicting and Understanding Intestinal Metabolism of Uridine 5′-Diphospho-glucuronosyltransferase Substrates Abstract Uridine 5′-diphospho-glucuronosyltransferases (UGTs) are expressed in the small intestines, but prediction of first-pass extraction from the related metabolism is not well s... |
PMC4869751 | core_pubmed_pmc | The effect of dipyridamole on the pharmacokinetics of metformin: a randomized crossover study in healthy volunteers | The effect of dipyridamole on the pharmacokinetics of metformin: a randomized crossover study in healthy volunteers Abstract Abstract Purpose Concomitant treatment with the glucose-lowering drug metformin and the platelet aggregation inhibitor dipyridamole often occurs in patients with type 2 diabetes mellitus who have... |
PMC12410251 | core_pubmed_pmc | Optimizing Early Ophthalmology Clinical Trials: Home OCT and Modeling Can Reduce Sample Size by 20% to 40% | Optimizing Early Ophthalmology Clinical Trials: Home OCT and Modeling Can Reduce Sample Size by 20% to 40% Abstract Abstract Purpose Early-stage clinical trials for major retinal diseases face challenges due to substantial interpatient variability, end points with high intrapatient variability, and prolonged follow-up ... |
PMC5809517 | core_pubmed_pmc | Risk factors contributing to a low darunavir plasma concentration | Risk factors contributing to a low darunavir plasma concentration Abstract Abstract Darunavir is an efficacious drug; however, pharmacokinetic variability has been reported. The objective of this study was to find predisposing factors for low darunavir plasma concentrations in patients starting the once‐ or twice‐daily... |
PMC11044803 | core_pubmed_pmc | Improving olaparib exposure to optimize adverse effects management | Improving olaparib exposure to optimize adverse effects management Abstract Background: Olaparib is an inhibitor of the human poly-(ADP-ribose)-polymerase enzymes (PARP1/2) needed to repair single-strand DNA breaks. It is used in breast, ovarian, prostate and pancreatic cancer. Objectives: This work aimed to describe t... |
PMC6536720 | core_pubmed_pmc | Target identification, screening and in vivo evaluation of pyrrolone-fused benzosuberene compounds against human epilepsy using Zebrafish model of pentylenetetrazol-induced seizures | Target identification, screening and in vivo evaluation of pyrrolone-fused benzosuberene compounds against human epilepsy using Zebrafish model of pentylenetetrazol-induced seizures Abstract Pyrrolone-fused benzosuberene (PBS) compounds were semi-synthesized from α,β,γ -Himachalenes extracted from the essential oil of ... |
PMC11043318 | core_pubmed_pmc | Quantification of biochemical PSA dynamics after radioligand therapy with [ 177 Lu]Lu-PSMA-I&T using a population pharmacokinetic/pharmacodynamic model | Quantification of biochemical PSA dynamics after radioligand therapy with [ 177 Lu]Lu-PSMA-I&T using a population pharmacokinetic/pharmacodynamic model Abstract Abstract Background There is an unmet need for prediction of treatment outcome or patient selection for [ 177 Lu]Lu-PSMA therapy in patients with metastatic ca... |
PMC7125369 | core_pubmed_pmc | Safety and pharmacokinetics of Withaferin-A in advanced stage high grade osteosarcoma: A phase I trial | Safety and pharmacokinetics of Withaferin-A in advanced stage high grade osteosarcoma: A phase I trial Abstract Background Withaferin-A (WA), an active principle obtained from a traditional Indian herb known as Ashwagandha or the Indian ginseng, has been shown to prevent and cure urethane-induced lung tumors in mice, a... |
PMC6263666 | core_pubmed_pmc | Pharmacokinetic‐Pharmacodynamic Model of Neutropenia in Patients With Myeloma Receiving High‐Dose Melphalan for Autologous Stem Cell Transplant | Pharmacokinetic‐Pharmacodynamic Model of Neutropenia in Patients With Myeloma Receiving High‐Dose Melphalan for Autologous Stem Cell Transplant Abstract Abstract High‐dose melphalan (HDM) is part of the conditioning regimen in patients with multiple myeloma (MM) receiving autologous stem cell transplantation (ASCT). Ho... |
PMC4997947 | core_pubmed_pmc | Preclinical Pharmacokinetics, Pharmacodynamics and Safety of Sucroferric Oxyhydroxide | Preclinical Pharmacokinetics, Pharmacodynamics and Safety of Sucroferric Oxyhydroxide Abstract Sucroferric oxyhydroxide (VELPHORO ® ) is a polynuclear iron-based phosphate binder recently approved for the treatment of hyperphosphataemia in patients with chronic kidney disease (CKD). As a number of the available phospha... |
PMC7540325 | core_pubmed_pmc | The Effects of Weak and Strong CYP3A Induction by Rifampicin on the Pharmacokinetics of Five Progestins and Ethinylestradiol Compared to Midazolam | The Effects of Weak and Strong CYP3A Induction by Rifampicin on the Pharmacokinetics of Five Progestins and Ethinylestradiol Compared to Midazolam Abstract Abstract It is known that co‐administration of CYP3A inducers may decrease the effectiveness of oral contraceptives containing progestins as mono‐preparations or co... |
PMC8389024 | core_pubmed_pmc | Determination of Susceptibility Breakpoint for Cefquinome against Streptococcus suis in Pigs | Determination of Susceptibility Breakpoint for Cefquinome against Streptococcus suis in Pigs Abstract Streptococcus suis ( S. suis ), a zoonotic pathogen, causes severe diseases in both pigs and human beings. Cefquinome can display excellent antibacterial activity against gram-negative and gram-positive bacteria. The a... |
PMC9254459 | core_pubmed_pmc | A validated LC-MS/MS method for determination of antiviral prodrug molnupiravir in human plasma and its application for a pharmacokinetic modeling study in healthy Egyptian volunteers | A validated LC-MS/MS method for determination of antiviral prodrug molnupiravir in human plasma and its application for a pharmacokinetic modeling study in healthy Egyptian volunteers Abstract Abstract A fully validated, simple, rapid and reproducible liquid chromatography-tandem mass spectrometry method was developed ... |
PMC4600912 | core_pubmed_pmc | Comparison of Folate Receptor Targeted Optical Contrast Agents for Intraoperative Molecular Imaging | Comparison of Folate Receptor Targeted Optical Contrast Agents for Intraoperative Molecular Imaging Abstract Abstract Background . Intraoperative imaging can identify cancer cells in order to improve resection; thus fluorescent contrast agents have emerged. Our objective was to do a preclinical comparison of two fluore... |
PMC4223725 | core_pubmed_pmc | Evaluation of the transporter-mediated herb-drug interaction potential of DA-9801, a standardized dioscorea extract for diabetic neuropathy, in human in vitro and rat in vivo | Evaluation of the transporter-mediated herb-drug interaction potential of DA-9801, a standardized dioscorea extract for diabetic neuropathy, in human in vitro and rat in vivo Abstract Background Drug transporters play important roles in the absorption, distribution, and elimination of drugs and thereby, modulate drug e... |
PMC4621644 | core_pubmed_pmc | Pharmacokinetics, intestinal absorption and microbial metabolism of single platycodin D in comparison to Platycodi radix extract | Pharmacokinetics, intestinal absorption and microbial metabolism of single platycodin D in comparison to Platycodi radix extract Abstract Background: Platycodi radix , the dried root of Platycodon grandiflorum A. DC, has been widely used as food and herb medicine for treating cough, cold and other respiratory ailments,... |
PMC6217653 | core_pubmed_pmc | Analysis of the Binding of Aripiprazole to Human Serum Albumin: The Importance of a Chloro-Group in the Chemical Structure | Analysis of the Binding of Aripiprazole to Human Serum Albumin: The Importance of a Chloro-Group in the Chemical Structure Abstract Aripiprazole (ARP), a quinolinone derivative, is an atypical antipsychotic drug that is used in the treatment of schizophrenia. ARP has an extensive distribution and more than 99% of the A... |
PMC8072969 | core_pubmed_pmc | Screening of Benzimidazole-Based Anthelmintics and Their Enantiomers as Repurposed Drug Candidates in Cancer Therapy | Screening of Benzimidazole-Based Anthelmintics and Their Enantiomers as Repurposed Drug Candidates in Cancer Therapy Abstract Abstract Repurposing of approved non-antitumor drugs represents a promising and affordable strategy that may help to increase the repertoire of effective anticancer drugs. Benzimidazole-based an... |
PMC11297101 | core_pubmed_pmc | The many dimensions of combination therapy: How to combine antibiotics to limit resistance evolution | The many dimensions of combination therapy: How to combine antibiotics to limit resistance evolution Abstract Abstract In combination therapy, bacteria are challenged with two or more antibiotics simultaneously. Ideally, separate mutations are required to adapt to each of them, which is a priori expected to hinder the ... |
PMC10976115 | core_pubmed_pmc | Using an In Vivo Mouse Model to Determine the Exclusion Criteria of Preexisting Anti-AAV9 Neutralizing Antibody Titer of Pompe Disease Patients in Clinical Trials | Using an In Vivo Mouse Model to Determine the Exclusion Criteria of Preexisting Anti-AAV9 Neutralizing Antibody Titer of Pompe Disease Patients in Clinical Trials Abstract The efficacy of adeno-associated virus (AAV)-based gene therapy is dependent on effective viral transduction, which might be inhibited by preexistin... |
PMC6954144 | core_pubmed_pmc | Pharmacodynamic assessment of prasugrel and clopidogrel in patients with non-cardioembolic stroke: a multicenter, randomized, active-control clinical trial | Pharmacodynamic assessment of prasugrel and clopidogrel in patients with non-cardioembolic stroke: a multicenter, randomized, active-control clinical trial Abstract Prasugrel, a novel P2Y 12 receptor antagonist, has been shown to be more effective than clopidogrel for preventing cardiovascular events in patients with a... |
PMC11133961 | core_pubmed_pmc | Impact of P‐gp inhibition on systemic exposure of pralsetinib and dosing considerations | Impact of P‐gp inhibition on systemic exposure of pralsetinib and dosing considerations Abstract Abstract A study to determine the impact of cyclosporine (Neoral), an inhibitor of P‐gp, on the pharmacokinetics of pralsetinib (trade name GAVRETO ® ) was conducted in 15 healthy adult volunteers. A single 200 mg dose of p... |
PMC7685239 | core_pubmed_pmc | Pharmacokinetics of solifenacin in pediatric populations with overactive bladder or neurogenic detrusor overactivity | Pharmacokinetics of solifenacin in pediatric populations with overactive bladder or neurogenic detrusor overactivity Abstract Abstract The aim of this investigation was to characterize and compare the pharmacokinetics (PK) of the antimuscarinic drug solifenacin in pediatric patients with overactive bladder (OAB) or neu... |
PMC11381611 | core_pubmed_pmc | Study on the mechanisms and Pharmacodynamic substances of Lian-Gui-Ning-Xin-Tang on Arrhythmia Therapy based on Pharmacodynamic–Pharmacokinetic associations | Study on the mechanisms and Pharmacodynamic substances of Lian-Gui-Ning-Xin-Tang on Arrhythmia Therapy based on Pharmacodynamic–Pharmacokinetic associations Abstract Background The Chinese herbal compound Lian-Gui-Ning-Xin-Tang (LGNXT), composed of 9 herbs, has a significant antiarrhythmic effect. Previous studies have... |
PMC9323915 | core_pubmed_pmc | CYP3A5*3 and SLCO1B1 c.521T>C Polymorphisms Influence the Pharmacokinetics of Atorvastatin and 2-Hydroxy Atorvastatin | CYP3A5*3 and SLCO1B1 c.521T>C Polymorphisms Influence the Pharmacokinetics of Atorvastatin and 2-Hydroxy Atorvastatin Abstract Abstract There is a large variability in individual responses to atorvastatin administration. This study assessed the pharmacogenetic effects of solute carrier organic anion transporter family ... |
PMC12898445 | core_pubmed_pmc | Orforglipron: A Comprehensive Review of an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity and Type 2 Diabetes | Orforglipron: A Comprehensive Review of an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity and Type 2 Diabetes Abstract Abstract Orforglipron (LY3502970) is a novel, orally available, nonpeptide glucagon-like peptide-1 receptor agonist (GLP-1 RA) designed to replicate the efficacy of injectable GLP-1 RAs for gly... |
PMC4538754 | core_pubmed_pmc | Hepatotoxicity and pharmacokinetics of cisplatin in combination therapy with a traditional Chinese medicine compound of Zengmian Yiliu granules in ICR mice and SKOV-3-bearing nude mice | Hepatotoxicity and pharmacokinetics of cisplatin in combination therapy with a traditional Chinese medicine compound of Zengmian Yiliu granules in ICR mice and SKOV-3-bearing nude mice Abstract Abstract Background Cisplatin (CDDP) is a highly effective chemotherapeutic agent used for therapy of many tumors and has been... |
PMC8813842 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Modelling of Allopurinol, its Active Metabolite Oxypurinol, and Biomarkers Hypoxanthine, Xanthine and Uric Acid in Hypoxic-Ischemic Encephalopathy Neonates | Pharmacokinetic/Pharmacodynamic Modelling of Allopurinol, its Active Metabolite Oxypurinol, and Biomarkers Hypoxanthine, Xanthine and Uric Acid in Hypoxic-Ischemic Encephalopathy Neonates Abstract Background Allopurinol, an xanthine oxidase (XO) inhibitor, is a promising intervention that may provide neuroprotection fo... |
PMC11743193 | core_pubmed_pmc | Utilising paired measurements of phosphatidylethanol to monitor early success in alcohol abstinence | Utilising paired measurements of phosphatidylethanol to monitor early success in alcohol abstinence Abstract Abstract Introduction Phosphatidylethanol (PEth) is a specific and persisting marker of ethanol (alcohol) consumption. Early success of medically necessary abstinence can be assessed by monitoring PEth disappear... |
PMC7540496 | core_pubmed_pmc | A Phase 2, Double‐Blind, Placebo‐Controlled Trial to Investigate Potential Drug‐Drug Interactions Between Cannabidiol and Clobazam | A Phase 2, Double‐Blind, Placebo‐Controlled Trial to Investigate Potential Drug‐Drug Interactions Between Cannabidiol and Clobazam Abstract Abstract We investigated the effects of cannabidiol (CBD; 21‐day maintenance dose) on the pharmacokinetics (PK) of clobazam (CLB) and monitored the safety of CBD (or placebo) plus ... |
PMC9144093 | core_pubmed_pmc | Application of Machine Learning Classification to Improve the Performance of Vancomycin Therapeutic Drug Monitoring | Application of Machine Learning Classification to Improve the Performance of Vancomycin Therapeutic Drug Monitoring Abstract Bayesian therapeutic drug monitoring (TDM) software uses a reported pharmacokinetic (PK) model as prior information. Since its estimation is based on the Bayesian method, the estimation performan... |
PMC12715538 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Caffeine in Preterm Neonates: Influence of Renal Function and Impairment on Dosing | Physiologically Based Pharmacokinetic Modeling of Caffeine in Preterm Neonates: Influence of Renal Function and Impairment on Dosing Abstract Abstract Currently, the same weight‐based caffeine citrate dosing regimen is applied to all neonates. However, due to differences in growth trajectories by gestational age (GA) a... |
PMC11876956 | core_pubmed_pmc | First Results of Migoprotafib, a Potent and Highly Selective Src Homology-2 Domain–Containing Phosphatase 2 Inhibitor in Patients with Advanced Solid Tumors | First Results of Migoprotafib, a Potent and Highly Selective Src Homology-2 Domain–Containing Phosphatase 2 Inhibitor in Patients with Advanced Solid Tumors Abstract Abstract Src homology-2 domain–containing phosphatase 2 promotes rat sarcoma viral oncogene homolog–MAPK signaling and tumorigenesis and is a promising th... |
PMC4788427 | core_pubmed_pmc | Distinguishing Antimicrobial Models with Different Resistance Mechanisms via Population Pharmacodynamic Modeling | Distinguishing Antimicrobial Models with Different Resistance Mechanisms via Population Pharmacodynamic Modeling Abstract Abstract Semi-mechanistic pharmacokinetic-pharmacodynamic (PK-PD) modeling is increasingly used for antimicrobial drug development and optimization of dosage regimens, but systematic simulation-esti... |
PMC3262315 | core_pubmed_pmc | Antiplatelet therapy in acute coronary syndromes: focus on ticagrelor | Antiplatelet therapy in acute coronary syndromes: focus on ticagrelor Abstract The use of antiplatelet agents, specifically the thienopyridines, has become a standard of care in the approach to the patient presenting with an acute coronary syndrome. These drugs irreversibly inhibit the platelet by permanently binding t... |
PMC7511311 | core_pubmed_pmc | Visualization of the distribution of nanoparticle-formulated AZD2811 in mouse tumor model using matrix-assisted laser desorption ionization mass spectrometry imaging | Visualization of the distribution of nanoparticle-formulated AZD2811 in mouse tumor model using matrix-assisted laser desorption ionization mass spectrometry imaging Abstract Abstract Penetration of nanoparticles into viable tumor regions is essential for an effective response. Mass spectrometry imaging (MSI) is a nove... |
PMC9985189 | core_pubmed_pmc | Pharmacokinetics and safety of two Voriconazole formulations after intravenous infusion in two doses in healthy Chinese subjects | Pharmacokinetics and safety of two Voriconazole formulations after intravenous infusion in two doses in healthy Chinese subjects Abstract Abstract Background Voriconazole is a second-generation triazole that is used to prevent and treat invasive fungal infections. The purpose of this study was to evaluate the pharmacok... |
PMC3935934 | core_pubmed_pmc | Inhibition of Baicalin on Metabolism of Phenacetin, a Probe of CYP1A2, in Human Liver Microsomes and in Rats | Inhibition of Baicalin on Metabolism of Phenacetin, a Probe of CYP1A2, in Human Liver Microsomes and in Rats Abstract Baicalin has been used as mainly bioactive constituent of about 100 kinds of traditional Chinese medicines in Chinese pharmacopoeia. The effect of baicalin on cytochrome P450 should be paid more attenti... |
PMC11369615 | core_pubmed_pmc | Safety, Efficacy, and Biological Data of T-Cell–Enabling Oncolytic Adenovirus TILT-123 in Advanced Solid Cancers from the TUNIMO Monotherapy Phase I Trial | Safety, Efficacy, and Biological Data of T-Cell–Enabling Oncolytic Adenovirus TILT-123 in Advanced Solid Cancers from the TUNIMO Monotherapy Phase I Trial Abstract Abstract Purpose: TILT-123 (igrelimogene litadenorepvec) is an oncolytic adenovirus armed with TNFa and IL2, designed to induce T-cell infiltration and cyto... |
PMC12040625 | core_pubmed_pmc | Structure-guided virtual screening reveals phytoconstituents as potent cathepsin B inhibitors: Implications for cancer, traumatic brain injury, and Alzheimer’s disease | Structure-guided virtual screening reveals phytoconstituents as potent cathepsin B inhibitors: Implications for cancer, traumatic brain injury, and Alzheimer’s disease Abstract Abstract Cathepsin B (CathB) is a lysosomal cysteine protease involved in various pathological and physiological processes and is becoming an a... |
PMC11096781 | core_pubmed_pmc | Population pharmacokinetics of intravenous daptomycin in critically ill patients: implications for selection of dosage regimens | Population pharmacokinetics of intravenous daptomycin in critically ill patients: implications for selection of dosage regimens Abstract Daptomycin is gaining prominence for the treatment of methicillin-resistant Staphylococcus aureus infections. However, the dosage selection for daptomycin in critically ill patients r... |
PMC4283056 | core_pubmed_pmc | Tafenoquine at therapeutic concentrations does not prolong fridericia-corrected QT interval in healthy subjects | Tafenoquine at therapeutic concentrations does not prolong fridericia-corrected QT interval in healthy subjects Abstract Tafenoquine is being developed for relapse prevention in Plasmodium vivax malaria. This Phase I, single-blind, randomized, placebo- and active-controlled parallel group study investigated whether taf... |
PMC7766900 | core_pubmed_pmc | Multi-Therapeutic Potential of Naringenin (4′,5,7-Trihydroxyflavonone): Experimental Evidence and Mechanisms | Multi-Therapeutic Potential of Naringenin (4′,5,7-Trihydroxyflavonone): Experimental Evidence and Mechanisms Abstract Extensive research has been carried out during the last few decades, providing a detailed account of thousands of discovered phytochemicals and their biological activities that have the potential to be ... |
PMC12387821 | core_pubmed_pmc | Genetic Modulation of Silodosin Exposure and Efficacy: The Role of CYP3A4, CYP3A5, and UGT2B7 Polymorphisms in Benign Prostatic Hyperplasia Management | Genetic Modulation of Silodosin Exposure and Efficacy: The Role of CYP3A4, CYP3A5, and UGT2B7 Polymorphisms in Benign Prostatic Hyperplasia Management Abstract Abstract Objectives : Silodosin, a selective α1A-adrenoceptor antagonist, is used to treat lower urinary tract symptoms (LUTS) associated with benign prostatic ... |
PMC5142133 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic characterization of a novel formulation containing co-formulated interferons alpha-2b and gamma in healthy male volunteers | Pharmacokinetic and pharmacodynamic characterization of a novel formulation containing co-formulated interferons alpha-2b and gamma in healthy male volunteers Abstract Background More potent antitumor activity is desired in Interferon (IFN)-treated cancer patients. This could be achieved by combining IFN alpha and IFN ... |
PMC12944280 | core_pubmed_pmc | Ocular and Systemic Pharmacokinetics of Baicalein and Baicalin After Intravitreal Injection and Oral Administration in Mice | Ocular and Systemic Pharmacokinetics of Baicalein and Baicalin After Intravitreal Injection and Oral Administration in Mice Abstract Abstract Background: Glaucoma requires therapies that extend beyond intraocular pressure (IOP)-lowering strategies, and baicalein (BA) offers dual IOP-lowering and neuroprotective potenti... |
PMC7822507 | core_pubmed_pmc | Early prognostic performance of miR155-5p monitoring for the risk of rejection: Logistic regression with a population pharmacokinetic approach in adult kidney transplant patients | Early prognostic performance of miR155-5p monitoring for the risk of rejection: Logistic regression with a population pharmacokinetic approach in adult kidney transplant patients Abstract Abstract Previous results from our group and others have shown that urinary pellet expression of miR155-5p and urinary CXCL-10 produ... |
PMC8396372 | core_pubmed_pmc | Multivariate Assessment for Bioequivalence Based on the Correlation of Random Effect | Multivariate Assessment for Bioequivalence Based on the Correlation of Random Effect Abstract Abstract Background and Objective Bioequivalence tests are fundamental step in assessing the equivalence in bioavailability between a test and reference product. In practice, two separate linear mixed models (LMMs) with random... |
PMC5395281 | core_pubmed_pmc | Bioequivalence study of a new sildenafil 100 mg orodispersible film compared to the conventional film-coated 100 mg tablet administered to healthy male volunteers | Bioequivalence study of a new sildenafil 100 mg orodispersible film compared to the conventional film-coated 100 mg tablet administered to healthy male volunteers Abstract A new orodispersible film formulation of the phosphodiesterase type 5 inhibitor, sildenafil, has been developed to examine the advantages of an oral... |
PMC10941566 | core_pubmed_pmc | Evaluation of the potential impact on pharmacokinetics of various cytochrome P450 substrates of increasing IL‐6 levels following administration of the T‐cell bispecific engager glofitamab | Evaluation of the potential impact on pharmacokinetics of various cytochrome P450 substrates of increasing IL‐6 levels following administration of the T‐cell bispecific engager glofitamab Abstract Abstract Glofitamab is a novel T cell bispecific antibody developed for treatment of relapsed‐refractory diffuse large B ce... |
PMC7686313 | core_pubmed_pmc | Phase 1 study of mTORC1/2 inhibitor sapanisertib (TAK-228) in advanced solid tumours, with an expansion phase in renal, endometrial or bladder cancer | Phase 1 study of mTORC1/2 inhibitor sapanisertib (TAK-228) in advanced solid tumours, with an expansion phase in renal, endometrial or bladder cancer Abstract Abstract Background This Phase 1 dose-escalation/expansion study assessed safety/tolerability of sapanisertib, an oral, highly selective inhibitor of mTORC1/mTOR... |
PMC5572576 | core_pubmed_pmc | Selective Inhibition of FLT3 by Gilteritinib in Relapsed/Refractory Acute Myeloid Leukemia: a Multicenter, First-in-human, Open-label, Phase 1/2 Study | Selective Inhibition of FLT3 by Gilteritinib in Relapsed/Refractory Acute Myeloid Leukemia: a Multicenter, First-in-human, Open-label, Phase 1/2 Study Abstract Abstract Background Fms -like tyrosine kinase 3-internal tandem duplication (FLT3-ITD) mutations are common in acute myeloid leukemia (AML) and are associated w... |
PMC9785299 | core_pubmed_pmc | Applications of In Silico Models to Predict Drug-Induced Liver Injury | Applications of In Silico Models to Predict Drug-Induced Liver Injury Abstract Abstract Drug-induced liver injury (DILI) is a major cause of the withdrawal of pre-marketed drugs, typically attributed to oxidative stress, mitochondrial damage, disrupted bile acid homeostasis, and innate immune-related inflammation. DILI... |
PMC12503347 | core_pubmed_pmc | SNP genotypes in CYP2C9 and VKORC1 genes do not affect prostate cancer or cancer mortality among warfarin users in Finnish prostate cancer patients | SNP genotypes in CYP2C9 and VKORC1 genes do not affect prostate cancer or cancer mortality among warfarin users in Finnish prostate cancer patients Abstract Abstract The coagulation cascade is thought to contribute to cancer progression. Although in vitro studies suggest that anticoagulants, such as warfarin, might red... |
PMC10135263 | core_pubmed_pmc | Comparison of Intravenous Microdialysis and Standard Plasma Sampling for Monitoring of Vancomycin and Meropenem Plasma Concentrations—An Experimental Porcine Study | Comparison of Intravenous Microdialysis and Standard Plasma Sampling for Monitoring of Vancomycin and Meropenem Plasma Concentrations—An Experimental Porcine Study Abstract Abstract Microdialysis is a catheter-based method suitable for dynamic sampling of unbound antibiotic concentrations. Intravenous antibiotic concen... |
PMC11871726 | core_pubmed_pmc | In vitro activity of rifampicin, rifapentine and rifabutin in combination with their 25-deacetyl-metabolites against various Mycobacterium tuberculosis lineages | In vitro activity of rifampicin, rifapentine and rifabutin in combination with their 25-deacetyl-metabolites against various Mycobacterium tuberculosis lineages Abstract Objectives Rifamycin agents (rifampicin (RIF), rifapentine (RFP), rifabutin (RFB)) are the cornerstone of tuberculosis (TB) therapy. Rifamycins are me... |
PMC10833183 | core_pubmed_pmc | Relevance of pharmacogenetic analyses and therapeutic drug monitoring of antidepressants for an individualized treatment of peripartum psychopathology | Relevance of pharmacogenetic analyses and therapeutic drug monitoring of antidepressants for an individualized treatment of peripartum psychopathology Abstract Objective Psychiatric disorders burden the peripartum period, often requiring psychopharmacological treatment, including antidepressants. Efficacy and tolerabil... |
PMC12240381 | core_pubmed_pmc | Computational insights into flavonoids inhibition of dengue virus envelope protein: ADMET profiling, molecular docking, dynamics, PCA, and end-state free energy calculations | Computational insights into flavonoids inhibition of dengue virus envelope protein: ADMET profiling, molecular docking, dynamics, PCA, and end-state free energy calculations Abstract Abstract Dengue virus is a critical worldwide health concern, and efforts to identify useful antiviral drugs remain imperative. This stud... |
PMC10363032 | core_pubmed_pmc | Phase I study to assess the effect of adavosertib (AZD1775) on the pharmacokinetics of substrates of CYP1A2, CYP2C19, and CYP3A in patients with advanced solid tumors | Phase I study to assess the effect of adavosertib (AZD1775) on the pharmacokinetics of substrates of CYP1A2, CYP2C19, and CYP3A in patients with advanced solid tumors Abstract Abstract Purpose Adavosertib may alter exposure to substrates of the cytochrome P450 (CYP) family of enzymes. This study assessed its effect on ... |
PMC3570572 | core_pubmed_pmc | Chemistry, Metabolism, and Toxicology of Cannabis: Clinical Implications | Chemistry, Metabolism, and Toxicology of Cannabis: Clinical Implications Abstract Abstract Cannabis is one of the most widely abused substances throughout the world. The primary psychoactive constituent of cannabis, delta 9-tetrahydrocannabinol (▵ 9_ THC), produces a myriad of pharmacological effects in animals and hum... |
PMC3137796 | core_pubmed_pmc | Cassia auriculata : Aspects of Safety Pharmacology and Drug Interaction | Cassia auriculata : Aspects of Safety Pharmacology and Drug Interaction Abstract Abstract Safety pharmacology studies help in identifying preclinical adverse drug reactions. We carried out routine safety pharmacology with focus on cardiovascular variables and pharmacokinetic herb-drug interaction studies on rats fed wi... |
PMC4314250 | core_pubmed_pmc | Evaluating Health Risks from Inhaled Polychlorinated Biphenyls: Research Needs for Addressing Uncertainty | Evaluating Health Risks from Inhaled Polychlorinated Biphenyls: Research Needs for Addressing Uncertainty Abstract Background: Indoor air concentrations of polychlorinated biphenyls (PCBs) in some buildings are one or more orders of magnitude higher than background levels. In response to this, efforts have been made to... |
PMC6353801 | core_pubmed_pmc | Enhanced Anti-diabetic Effect of Berberine Combined With Timosaponin B2 in Goto-Kakizaki Rats, Associated With Increased Variety and Exposure of Effective Substances Through Intestinal Absorption | Enhanced Anti-diabetic Effect of Berberine Combined With Timosaponin B2 in Goto-Kakizaki Rats, Associated With Increased Variety and Exposure of Effective Substances Through Intestinal Absorption Abstract Objective: Inspired by the traditionally clinical application of herb pair Zhimu - Huangbo to treat diabetes, a com... |
PMC8449932 | core_pubmed_pmc | Immunogenicity to biological drugs in psoriasis and psoriatic arthritis | Immunogenicity to biological drugs in psoriasis and psoriatic arthritis Abstract Monoclonal antibodies or fusion proteins, defined as biological drugs, have modified the natural history of numerous immune-mediated disorders, allowing the development of therapies aimed at blocking the pathophysiological pathways of the ... |
PMC9921301 | core_pubmed_pmc | Design, Synthesis, and Antiproliferative Activity of New 5-Chloro-indole-2-carboxylate and Pyrrolo[3,4- b ]indol-3-one Derivatives as Potent Inhibitors of EGFR T790M /BRAF V600E Pathways | Design, Synthesis, and Antiproliferative Activity of New 5-Chloro-indole-2-carboxylate and Pyrrolo[3,4- b ]indol-3-one Derivatives as Potent Inhibitors of EGFR T790M /BRAF V600E Pathways Abstract Abstract Mutant EGFR/BRAF pathways are thought to be crucial targets for the development of anticancer drugs since they are ... |
PMC6973126 | core_pubmed_pmc | Preferential Inhibition of JAK1 Relative to JAK3 by Upadacitinib: Exposure‐Response Analyses of Ex Vivo Data From 2 Phase 1 Clinical Trials and Comparison to Tofacitinib | Preferential Inhibition of JAK1 Relative to JAK3 by Upadacitinib: Exposure‐Response Analyses of Ex Vivo Data From 2 Phase 1 Clinical Trials and Comparison to Tofacitinib Abstract Abstract Upadacitinib is a selective Janus kinase (JAK) 1 inhibitor being developed for treatment of rheumatoid arthritis. This study charact... |
PMC3684141 | core_pubmed_pmc | Differential effects of dosing regimen on the safety and efficacy of dasatinib: retrospective exposure–response analysis of a Phase III study | Differential effects of dosing regimen on the safety and efficacy of dasatinib: retrospective exposure–response analysis of a Phase III study Abstract Abstract Purpose Dasatinib is a prototypic short half-life BCR-ABL1 tyrosine kinase inhibitor. The recommended dose of dasatinib for chronic myeloid leukemia in chronic ... |
PMC4342742 | core_pubmed_pmc | Prediction of Pharmacokinetics and Penetration of Moxifloxacin in Human with Intra-Abdominal Infection Based on Extrapolated PBPK Model | Prediction of Pharmacokinetics and Penetration of Moxifloxacin in Human with Intra-Abdominal Infection Based on Extrapolated PBPK Model Abstract Abstract The aim of this study is to develop a physiologically based pharmacokinetic (PBPK) model in intra-abdominal infected rats, and extrapolate it to human to predict moxi... |
PMC11342882 | core_pubmed_pmc | Modulation of the pharmacokinetics of soluble ACE2 decoy receptors through glycosylation | Modulation of the pharmacokinetics of soluble ACE2 decoy receptors through glycosylation Abstract The Spike of SARS-CoV-2 recognizes a transmembrane protease, angiotensin-converting enzyme 2 (ACE2), on host cells to initiate infection. Soluble derivatives of ACE2, in which Spike affinity is enhanced and the protein is ... |
PMC12908643 | core_pubmed_pmc | Efficacy and Safety of Aficamten in Children and Adolescents With Obstructive Hypertrophic Cardiomyopathy: Study Design and Rationale of CEDAR-HCM | Efficacy and Safety of Aficamten in Children and Adolescents With Obstructive Hypertrophic Cardiomyopathy: Study Design and Rationale of CEDAR-HCM Abstract BACKGROUND: Hypertrophic cardiomyopathy (HCM) is an important cause of morbidity and mortality in children, but treatment options are limited. Aficamten, a next-in-... |
PMC10676574 | core_pubmed_pmc | In-silico and in-vitro screening of Asiatic acid and Asiaticoside A against Cathepsin S enzyme | In-silico and in-vitro screening of Asiatic acid and Asiaticoside A against Cathepsin S enzyme Abstract Abstract Background Atherosclerosis is a form of cardiovascular disease that affects the endothelium of the blood vessel. Series of events are involved in the pathophysiology of this disease which includes the breaki... |
PMC9959474 | core_pubmed_pmc | Nanosystems for Brain Targeting of Antipsychotic Drugs: An Update on the Most Promising Nanocarriers for Increased Bioavailability and Therapeutic Efficacy | Nanosystems for Brain Targeting of Antipsychotic Drugs: An Update on the Most Promising Nanocarriers for Increased Bioavailability and Therapeutic Efficacy Abstract Abstract Orally administered antipsychotic drugs are the first-line treatment for psychotic disorders, such as schizophrenia and bipolar disorder. Neverthe... |
PMC8012855 | core_pubmed_pmc | Design and High Expression of Non-glycosylated Lysostaphins in Pichia pastoris and Their Pharmacodynamic Study | Design and High Expression of Non-glycosylated Lysostaphins in Pichia pastoris and Their Pharmacodynamic Study Abstract Abstract Lysostaphin is an effective antimicrobial agent to Staphylococcus , especially for the methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Staphylococcus aureus (MDRSA)... |
PMC5024067 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of SMT C1100, a 2‐arylbenzoxazole utrophin modulator, following single‐ and multiple‐dose administration to healthy male adult volunteers | Safety, tolerability, and pharmacokinetics of SMT C1100, a 2‐arylbenzoxazole utrophin modulator, following single‐ and multiple‐dose administration to healthy male adult volunteers Abstract Abstract SMT C1100 is a small molecule utrophin modulator in development to treat Duchenne muscular dystrophy. This study evaluate... |
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