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PMC12712899 | core_pubmed_pmc | Integration of artificial intelligence and high-content screening enabled identification of drugs for long-term treatment of cerebral cavernous malformation disease | Integration of artificial intelligence and high-content screening enabled identification of drugs for long-term treatment of cerebral cavernous malformation disease Abstract Background. Adults and children with cerebral cavernous malformations (CCMs) are at risk of experiencing lifelong complications such as hemorrhagi... |
PMC10025503 | core_pubmed_pmc | Effects of emamectin benzoate on pharmacokinetic profiles, bioavailability, and serum biochemical indices in crucian carp ( Carassius carassius ) following oral administration with multiple dosage levels | Effects of emamectin benzoate on pharmacokinetic profiles, bioavailability, and serum biochemical indices in crucian carp ( Carassius carassius ) following oral administration with multiple dosage levels Abstract Abstract The aim of this investigation was to explore the effect of three different dose levels of emamecti... |
PMC12608587 | core_pubmed_pmc | Novel Ingredients: Hydroxytyrosol as a Neuroprotective Agent; What Is New on the Horizon? | Novel Ingredients: Hydroxytyrosol as a Neuroprotective Agent; What Is New on the Horizon? Abstract Hydroxytyrosol (HXT), a phenolic compound from olive, shows great potential as a neuroprotective agent and a translational target for claim-ready nutrition and food products. Human studies increasingly report benefits for... |
PMC6110617 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of Dexmedetomidine in Children Undergoing Ambulatory Surgery | Population Pharmacokinetics and Pharmacodynamics of Dexmedetomidine in Children Undergoing Ambulatory Surgery Abstract BACKGROUND: Dexmedetomidine (DEX) is an α-2 adrenergic agonist with sedative and analgesic properties. Although not approved for pediatric use by the Food and Drug Administration, DEX is increasingly u... |
PMC9310908 | core_pubmed_pmc | Mechanistic modelling of enzyme‐restoration effects of new recombinant liver‐targeted proteins in acute intermittent porphyria | Mechanistic modelling of enzyme‐restoration effects of new recombinant liver‐targeted proteins in acute intermittent porphyria Abstract Abstract Background and Purpose Acute intermittent porphyria (AIP) is a rare disease caused by a genetic mutation in the hepatic activity of the porphobilinogen‐deaminase. We aimed to ... |
PMC3467658 | core_pubmed_pmc | Effects of nicotine mouth spray on urges to smoke, a randomised clinical trial | Effects of nicotine mouth spray on urges to smoke, a randomised clinical trial Abstract Objective A new nicotine mouth spray was shown to be an effective stop-smoking treatment. This study was set up to examine the speed with which it relieves urges to smoke, and how it compares with nicotine lozenge in this respect. D... |
PMC4776255 | core_pubmed_pmc | Relative bioavailability, food effect, and safety of the single-dose pharmacokinetics of omecamtiv mecarbil following administration of different modified-release formulations in healthy subjects | Relative bioavailability, food effect, and safety of the single-dose pharmacokinetics of omecamtiv mecarbil following administration of different modified-release formulations in healthy subjects Abstract Abstract Objective: Omecamtiv mecarbil is a novel small molecule that directly activates cardiac myosin and increas... |
PMC9322950 | core_pubmed_pmc | Population Pharmacokinetics of Palbociclib and Its Correlation with Clinical Efficacy and Safety in Patients with Advanced Breast Cancer | Population Pharmacokinetics of Palbociclib and Its Correlation with Clinical Efficacy and Safety in Patients with Advanced Breast Cancer Abstract Abstract Neutropenia is the most frequent dose-limiting toxicity reported in patients with metastatic breast cancer receiving palbociclib. The objective of this study was to ... |
PMC9199876 | core_pubmed_pmc | The pharmacokinetics of oral trazpiroben ( TAK ‐906) after organic anion transporting polypeptide 1B1 / 1B3 inhibition: A phase I, randomized study | The pharmacokinetics of oral trazpiroben ( TAK ‐906) after organic anion transporting polypeptide 1B1 / 1B3 inhibition: A phase I, randomized study Abstract Abstract Trazpiroben is a dopamine D 2 /D 3 receptor antagonist under development for the treatment of gastroparesis. This phase I, open‐label, randomized, two‐way... |
PMC9691842 | core_pubmed_pmc | Review of preclinical data of PF-07304814 and its active metabolite derivatives against SARS-CoV-2 infection | Review of preclinical data of PF-07304814 and its active metabolite derivatives against SARS-CoV-2 infection Abstract Main protease (M pro ) is a superior target for anti-SARS-COV-2 drugs. PF-07304814 is a phosphate ester prodrug of PF-00835231 that is rapidly metabolized into the active metabolite PF-00835231 by alkal... |
PMC10756690 | core_pubmed_pmc | Abacavir Drug Exposures in African Children Under 14 kg Using Pediatric Solid Fixed Dose Combinations According to World Health Organization Weight Bands | Abacavir Drug Exposures in African Children Under 14 kg Using Pediatric Solid Fixed Dose Combinations According to World Health Organization Weight Bands Abstract Abstract Background The pharmacokinetics of abacavir (ABC) in African children living with HIV (CLHIV) weighing <14 kg and receiving pediatric fixed dose com... |
PMC11462461 | core_pubmed_pmc | Novel quinoline-4-carboxamide derivatives potentiates apoptosis by targeting PDK1 to overcome chemo-resistance in colorectal cancer: Theoretical and experimental results | Novel quinoline-4-carboxamide derivatives potentiates apoptosis by targeting PDK1 to overcome chemo-resistance in colorectal cancer: Theoretical and experimental results Abstract A series of novel N,2-diphenyl-6-(aryl/heteroaryl)quinoline-4-carboxamide derivatives were designed and synthesized using the Suzuki coupling... |
PMC8916538 | core_pubmed_pmc | Intensified Antituberculosis Therapy Regimen Containing Higher Dose Rifampin for Tuberculous Meningitis: A Systematic Review and Meta-Analysis | Intensified Antituberculosis Therapy Regimen Containing Higher Dose Rifampin for Tuberculous Meningitis: A Systematic Review and Meta-Analysis Abstract Abstract Background Tuberculous meningitis is difficult to diagnose and is associated with high mortality. Recently, several studies evaluated the intensified regimen c... |
PMC6118295 | core_pubmed_pmc | Pharmacometabolomics Informs About Pharmacokinetic Profile of Methylphenidate | Pharmacometabolomics Informs About Pharmacokinetic Profile of Methylphenidate Abstract Abstract Carboxylesterase 1 (CES1) metabolizes methylphenidate and other drugs. CES1 gene variation only partially explains pharmacokinetic (PK) variability. Biomarkers predicting the PKs of drugs metabolized by CES1 are needed. We i... |
PMC7209288 | core_pubmed_pmc | Inhibition of complement pathway activation with Pozelimab, a fully human antibody to complement component C5 | Inhibition of complement pathway activation with Pozelimab, a fully human antibody to complement component C5 Abstract Abstract Complement is a key component of the innate immune system. Inappropriate complement activation underlies the pathophysiology of a variety of diseases. Complement component 5 (C5) is a validate... |
PMC11983545 | core_pubmed_pmc | High vs. low vancomycin therapeutic concentrations in periprosthetic joint infection: A retrospective cohort analysis | High vs. low vancomycin therapeutic concentrations in periprosthetic joint infection: A retrospective cohort analysis Abstract Objective Current guidelines recommend vancomycin concentrations of 10–20 μg/mL for most infections, with higher levels (15–20 μg/mL) suggested for severe cases. However, evidence supporting th... |
PMC4277280 | core_pubmed_pmc | Controlled Release of Dutasteride from Biodegradable Microspheres: In Vitro and In Vivo Studies | Controlled Release of Dutasteride from Biodegradable Microspheres: In Vitro and In Vivo Studies Abstract Abstract The aim of the present work was to study the in vitro/in vivo characteristics of dutasteride loaded biodegradable microspheres designed for sustained release of dutasteride over four weeks. An O/W emulsion-... |
PMC11540137 | core_pubmed_pmc | Implementation of a Pharmacist-Driven Vancomycin Area Under the Concentration-Time Curve Monitoring Program Using Bayesian Modeling in Outpatient Parenteral Antimicrobial Therapy | Implementation of a Pharmacist-Driven Vancomycin Area Under the Concentration-Time Curve Monitoring Program Using Bayesian Modeling in Outpatient Parenteral Antimicrobial Therapy Abstract Abstract Background Current vancomycin monitoring guidelines recommend monitoring 24-hour area under the concentration-time curve (A... |
PMC6609541 | core_pubmed_pmc | Enterohepatic circulation of glucuronide metabolites of drugs in dog | Enterohepatic circulation of glucuronide metabolites of drugs in dog Abstract Abstract The enterohepatic circulation (EHC) of drugs is often the result of the direct glucuronidation, excretion of the metabolite into bile, followed by hydrolysis to the aglycone by the gut microbiome and finally reabsorption of drug into... |
PMC5457398 | core_pubmed_pmc | A simple and rapid LC-MS/MS method for therapeutic drug monitoring of cetuximab: a GPCO-UNICANCER proof of concept study in head-and-neck cancer patients | A simple and rapid LC-MS/MS method for therapeutic drug monitoring of cetuximab: a GPCO-UNICANCER proof of concept study in head-and-neck cancer patients Abstract Abstract Administration of first-in-class anti-EGFR monoclonal antibody cetuximab is contingent upon extensive pharmacogenomic testing. However in addition t... |
PMC12415973 | core_pubmed_pmc | Preclinical studies of an AAV8-CYP4V2 gene therapy VGR-R01 for the treatment of Bietti crystalline dystrophy | Preclinical studies of an AAV8-CYP4V2 gene therapy VGR-R01 for the treatment of Bietti crystalline dystrophy Abstract Bietti crystalline dystrophy (BCD) is an autosomal recessive disorder caused by loss-of-function mutations in the CYP4V2 gene, characterized by crystal-like lipid deposits in the retina, progressive pho... |
PMC5678913 | core_pubmed_pmc | Concomitant proton pump inhibitor use does not reduce the efficacy of elbasvir/grazoprevir: A pooled analysis of 1,322 patients with hepatitis C infection | Concomitant proton pump inhibitor use does not reduce the efficacy of elbasvir/grazoprevir: A pooled analysis of 1,322 patients with hepatitis C infection Abstract Concomitant proton pump inhibitor (PPI) use reduces plasma concentrations of certain nonstructural protein 5A inhibitors, which are key components of modern... |
PMC5799957 | core_pubmed_pmc | Study of drug–Drug interactions among the hypertensive patients in a tertiary care teaching hospital | Study of drug–Drug interactions among the hypertensive patients in a tertiary care teaching hospital Abstract Aim: Drug–drug interactions (DDIs) are one of the major but preventable cause of adverse drug reaction. Study of prevalence and prediction of DDIs will make the physician easier to provide better patient care a... |
PMC4783652 | core_pubmed_pmc | Physiological, pharmacokinetic and liver metabolism comparisons between 3-, 6-, 12- and 18-month-old male Sprague Dawley rats under ketamine-xylazine anesthesia | Physiological, pharmacokinetic and liver metabolism comparisons between 3-, 6-, 12- and 18-month-old male Sprague Dawley rats under ketamine-xylazine anesthesia Abstract Abstract The main objective of this study was to compare the physiological changes (withdrawal and corneal reflexes, respiratory and cardiac frequency... |
PMC12649378 | core_pubmed_pmc | Comparative Pharmacokinetics and Safety of a Micellar Chrysin–Quercetin–Rutin Formulation: A Randomized Crossover Trial | Comparative Pharmacokinetics and Safety of a Micellar Chrysin–Quercetin–Rutin Formulation: A Randomized Crossover Trial Abstract Chrysin is a dietary flavonoid with antioxidant and anti-inflammatory activity, but its clinical potential is limited by poor oral bioavailability. This randomized double-blind three period c... |
PMC8452293 | core_pubmed_pmc | Application of a dual mechanistic approach to support bilastine dose selection for older adults | Application of a dual mechanistic approach to support bilastine dose selection for older adults Abstract Abstract The objective of this study was to evaluate bilastine dosing recommendations in older adults and overcome the limitation of insufficient data from phase I studies in this underrepresented population. This w... |
PMC6127415 | core_pubmed_pmc | Extracorporeal Stromal Cell Therapy for Subjects With Dialysis-Dependent Acute Kidney Injury | Extracorporeal Stromal Cell Therapy for Subjects With Dialysis-Dependent Acute Kidney Injury Abstract Introduction The pathophysiology of acute kidney injury (AKI) involves damage to renal epithelial cells, podocytes, and vascular beds that manifests into a deranged, self-perpetuating immune response and peripheral org... |
PMC12796782 | core_pubmed_pmc | Pharmacokinetics of Ilunocitinib, a New Janus Kinase Inhibitor, in Dogs | Pharmacokinetics of Ilunocitinib, a New Janus Kinase Inhibitor, in Dogs Abstract ABSTRACT Ilunocitinib, a novel Janus kinase inhibitor, is indicated for managing pruritus and skin lesions associated with canine allergic and atopic dermatitis. Pharmacokinetics of ilunocitinib were investigated following single intraveno... |
PMC8574943 | core_pubmed_pmc | Pharmacokinetics of Vancomycin in Critically Ill Children: A Systematic Review | Pharmacokinetics of Vancomycin in Critically Ill Children: A Systematic Review Abstract Background and Objective Vancomycin is often used in the ICU for the treatment of Gram-positive bacterial infection. In critically ill children, there are pathophysiologic changes that affect the pharmacokinetics of vancomycin. A sy... |
PMC6008565 | core_pubmed_pmc | 6′-Hydroxy Justicidin B Triggers a Critical Imbalance in Ca 2+ Homeostasis and Mitochondrion-Dependent Cell Death in Human Leukemia K562 Cells | 6′-Hydroxy Justicidin B Triggers a Critical Imbalance in Ca 2+ Homeostasis and Mitochondrion-Dependent Cell Death in Human Leukemia K562 Cells Abstract Justicia procumbens ( J. procumbens ) is a traditional Chinese herbal medicine which was used for the treatment of fever, pain, and cancer. A compound 6′-hydroxy justic... |
PMC11629297 | core_pubmed_pmc | Effect of rabbit ATG PK on outcomes after TCR-αβ/CD19–depleted pediatric haploidentical HCT for hematologic malignancy | Effect of rabbit ATG PK on outcomes after TCR-αβ/CD19–depleted pediatric haploidentical HCT for hematologic malignancy Abstract Key Points • Nonoptimal rATG exposure increases nonrelapse mortality, relapse, and chronic GVHD and worsens DFS in pediatric AB-TCD haploidentical HCT. • Targeting rATG dosing to a predicted e... |
PMC7821292 | core_pubmed_pmc | Population Pharmacokinetic Analysis for Plasma and Epithelial Lining Fluid Ceftolozane/Tazobactam Concentrations in Patients With Ventilated Nosocomial Pneumonia | Population Pharmacokinetic Analysis for Plasma and Epithelial Lining Fluid Ceftolozane/Tazobactam Concentrations in Patients With Ventilated Nosocomial Pneumonia Abstract Abstract Ceftolozane/tazobactam (C/T) is a combination of a novel cephalosporin with tazobactam, recently approved for the treatment of hospital‐acqu... |
PMC11272598 | core_pubmed_pmc | RG7774 (Vicasinabin), an orally bioavailable cannabinoid receptor 2 (CB2R) agonist, decreases retinal vascular permeability, leukocyte adhesion, and ocular inflammation in animal models | RG7774 (Vicasinabin), an orally bioavailable cannabinoid receptor 2 (CB2R) agonist, decreases retinal vascular permeability, leukocyte adhesion, and ocular inflammation in animal models Abstract Introduction Preclinical studies suggest that cannabinoid receptor type 2 (CB2R) activation has a therapeutic effect in anima... |
PMC5522985 | core_pubmed_pmc | A Bayesian Approach for Population Pharmacokinetic Modeling of Alcohol in Japanese Individuals | A Bayesian Approach for Population Pharmacokinetic Modeling of Alcohol in Japanese Individuals Abstract Abstract Background Blood alcohol concentration data that were previously obtained from 34 healthy Japanese subjects with limited sampling times were reanalyzed. Characteristics of the data were that the concentratio... |
PMC11236728 | core_pubmed_pmc | Naoxintong capsule for treating cardiovascular and cerebrovascular diseases: from bench to bedside | Naoxintong capsule for treating cardiovascular and cerebrovascular diseases: from bench to bedside Abstract Naoxintong Capsule (NXT), a renowned traditional Chinese medicine (TCM) formulation, has been broadly applied in China for more than 30 years. Over decades, accumulating evidences have proven satisfactory efficac... |
PMC9916073 | core_pubmed_pmc | Behavioral and Pharmacokinetics Studies of N -Methyl-2-Aminoindane (NM2AI) in Mice: An Aminoindane Briefly Used in the Illicit Drug Market | Behavioral and Pharmacokinetics Studies of N -Methyl-2-Aminoindane (NM2AI) in Mice: An Aminoindane Briefly Used in the Illicit Drug Market Abstract Abstract Drug forums are considered as the main platform sources that have contributed to the increase in NPS popularity, especially for those not yet known to law enforcem... |
PMC11002211 | core_pubmed_pmc | Lung microdialysis and in vivo PK/PD integration of cefquinome against Actinobacillus pleuropneumoniae in a porcine experimental lung infection model | Lung microdialysis and in vivo PK/PD integration of cefquinome against Actinobacillus pleuropneumoniae in a porcine experimental lung infection model Abstract This study aim to explore the application of microdialysis in pharmacokinetic (PK) and pharmacodynamic (PD) integration of cefquinome against Actinobacillus pleu... |
PMC4674186 | core_pubmed_pmc | Pharmacokinetic and Genomic Effects of Arsenite in Drinking Water on Mouse Lung in a 30-Day Exposure | Pharmacokinetic and Genomic Effects of Arsenite in Drinking Water on Mouse Lung in a 30-Day Exposure Abstract Abstract The 2 objectives of this subchronic study were to determine the arsenite drinking water exposure dependent increases in female C3H mouse liver and lung tissue arsenicals and to characterize the dose re... |
PMC6617853 | core_pubmed_pmc | Time‐Varying Clearance and Impact of Disease State on the Pharmacokinetics of Avelumab in Merkel Cell Carcinoma and Urothelial Carcinoma | Time‐Varying Clearance and Impact of Disease State on the Pharmacokinetics of Avelumab in Merkel Cell Carcinoma and Urothelial Carcinoma Abstract Avelumab, a human anti–programmed death ligand 1 immunoglobulin G1 antibody, has shown efficacy and manageable safety in multiple tumors. A two‐compartment population pharmac... |
PMC10135334 | core_pubmed_pmc | Predicting the Area under the Plasma Concentration-Time Curve (AUC) for First Dose Vancomycin Using First-Order Pharmacokinetic Equations | Predicting the Area under the Plasma Concentration-Time Curve (AUC) for First Dose Vancomycin Using First-Order Pharmacokinetic Equations Abstract Abstract To treat critically ill patients, early achievement of the target area under the plasma concentration-time curve/minimum inhibitory concentration (AUC/MIC) in the f... |
PMC6600563 | core_pubmed_pmc | Quantitative Structure–Activity Relationships for Structurally Diverse Chemotypes Having Anti- Trypanosoma cruzi Activity | Quantitative Structure–Activity Relationships for Structurally Diverse Chemotypes Having Anti- Trypanosoma cruzi Activity Abstract Abstract Small-molecule compounds that have promising activity against macromolecular targets from Trypanosoma cruzi occasionally fail when tested in whole-cell phenotypic assays. This outc... |
PMC12937474 | core_pubmed_pmc | Artificial Intelligence and the Discovery of Antibiotics: Reinventing with Opportunities, Challenges, and Clinical Translation | Artificial Intelligence and the Discovery of Antibiotics: Reinventing with Opportunities, Challenges, and Clinical Translation Abstract Abstract Background: The outbreak and spreading of antimicrobial resistance (AMR) in a very short time has made most of the old-fashioned antibiotics ineffective, and thus new therapeu... |
PMC11672834 | core_pubmed_pmc | Dynamic In Vitro PK/PD Infection Models for the Development and Optimisation of Antimicrobial Regimens: A Narrative Review | Dynamic In Vitro PK/PD Infection Models for the Development and Optimisation of Antimicrobial Regimens: A Narrative Review Abstract The antimicrobial concentration–time profile in humans affects antimicrobial activity, and as such, it is critical for preclinical infection models to simulate human-like dynamic concentra... |
PMC8496728 | core_pubmed_pmc | Chloroquine combined with concurrent radiotherapy and temozolomide for newly diagnosed glioblastoma: a phase IB trial | Chloroquine combined with concurrent radiotherapy and temozolomide for newly diagnosed glioblastoma: a phase IB trial Abstract ABSTRACT Treatment of glioblastoma xenografts with chloroquine results in macroautophagy/autophagy inhibition, resulting in a reduction of tumor hypoxia and sensitization to radiation. Preclini... |
PMC12387202 | core_pubmed_pmc | Real-World Evidence on Low-Dose Olanzapine (≤1.25 mg) for Personalized Antipsychotic Dosing | Real-World Evidence on Low-Dose Olanzapine (≤1.25 mg) for Personalized Antipsychotic Dosing Abstract Abstract Background/Objectives : This cohort study aimed to elucidate the real-world treatment course of patients receiving low-dose olanzapine (<2.5 mg), to assess its efficacy, and to examine its metabolic side effect... |
PMC9415367 | core_pubmed_pmc | Inhibition of Hepatitis E Virus Replication by Novel Inhibitor Targeting Methyltransferase | Inhibition of Hepatitis E Virus Replication by Novel Inhibitor Targeting Methyltransferase Abstract Abstract Hepatitis E Virus (HEV) is a quasi-enveloped virus having a single-stranded, positive-sense RNA genome (~7.2 kb), flanked with a 5′ methylated cap and a 3′ polyadenylated tail. The HEV open reading frame 1 (ORF1... |
PMC7323312 | core_pubmed_pmc | Impact of Disease on Plasma and Lung Exposure of Chloroquine, Hydroxychloroquine and Azithromycin: Application of PBPK Modeling | Impact of Disease on Plasma and Lung Exposure of Chloroquine, Hydroxychloroquine and Azithromycin: Application of PBPK Modeling Abstract We use a mechanistic lung model to demonstrate that accumulation of chloroquine (CQ), hydroxychloroquine (HCQ), and azithromycin (AZ) in the lungs is sensitive to changes in lung pH, ... |
PMC7567642 | core_pubmed_pmc | A Fully Integrated Assay Panel for Early Drug Metabolism and Pharmacokinetics Profiling | A Fully Integrated Assay Panel for Early Drug Metabolism and Pharmacokinetics Profiling Abstract Abstract Evaluation and optimization of physicochemical and metabolic properties of compounds are a crucial component of the drug development process. Continuous access to this information during the design-make-test-analys... |
PMC10301809 | core_pubmed_pmc | Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid Nanocarriers | Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid Nanocarriers Abstract The feasibility of using lipid–polymer hybrid (LPH) nanocarriers as a potential platform for the intranasal delivery of ziprasidone (ZP), a second-generation antipsychotic, was explor... |
PMC11310985 | core_pubmed_pmc | Clinical Effects and Pharmacokinetic Profile of Intramuscular Dexmedetomidine (10 μg/kg) in Cats | Clinical Effects and Pharmacokinetic Profile of Intramuscular Dexmedetomidine (10 μg/kg) in Cats Abstract Simple Summary This study investigated how dexmedetomidine, a sedative, works when given to healthy cats via intramuscular injection at a dose of 10 μg/kg. Nine adult cats were observed before and after receiving t... |
PMC5826112 | core_pubmed_pmc | Intrapulmonary Pharmacokinetics of Relebactam, a Novel β-Lactamase Inhibitor, Dosed in Combination with Imipenem-Cilastatin in Healthy Subjects | Intrapulmonary Pharmacokinetics of Relebactam, a Novel β-Lactamase Inhibitor, Dosed in Combination with Imipenem-Cilastatin in Healthy Subjects Abstract ABSTRACT This phase I study assessed the intrapulmonary pharmacokinetic profiles of relebactam (MK-7655), a novel β-lactamase inhibitor, and imipenem. Sixteen healthy ... |
PMC8381248 | core_pubmed_pmc | Comparison of Pinoresinol and its Diglucoside on their ADME Properties and Vasorelaxant Effects on Phenylephrine-Induced Model | Comparison of Pinoresinol and its Diglucoside on their ADME Properties and Vasorelaxant Effects on Phenylephrine-Induced Model Abstract Abstract Pinoresinol (PINL) and pinoresinol diglucoside (PDG), two natural lignans found in Eucommia ulmoides Oliv. (Duzhong), have several pharmacological activities. However, there i... |
PMC5110652 | core_pubmed_pmc | Pharmacokinetic study of furosemide incorporated PLGA microspheres after oral administration to rat | Pharmacokinetic study of furosemide incorporated PLGA microspheres after oral administration to rat Abstract Objective(s): The purpose of the current study was to assess the feasibility of microspheres from biocompatible polymer for oral bioavailability (BA) enhancement of potent sulfonamide- type loop diuretic- Furose... |
PMC12757290 | core_pubmed_pmc | Potassium-competitive acid blockers and advances in the management of patients with acid-related diseases: a narrative review | Potassium-competitive acid blockers and advances in the management of patients with acid-related diseases: a narrative review Abstract Traditional management of acid-related diseases, including gastroesophageal reflux disease, Helicobacter pylori infection, and peptic ulcer disease, primarily relies on proton pump inhi... |
PMC11399464 | core_pubmed_pmc | Pharmacokinetic characteristics of mesenchymal stem cells in translational challenges | Pharmacokinetic characteristics of mesenchymal stem cells in translational challenges Abstract Abstract Over the past two decades, mesenchymal stem/stromal cell (MSC) therapy has made substantial strides, transitioning from experimental clinical applications to commercial products. MSC therapies hold considerable promi... |
PMC6588954 | core_pubmed_pmc | Molidustat for the treatment of renal anaemia in patients with dialysis-dependent chronic kidney disease: design and rationale of three phase III studies | Molidustat for the treatment of renal anaemia in patients with dialysis-dependent chronic kidney disease: design and rationale of three phase III studies Abstract Abstract Introduction New medications for anaemia associated with chronic kidney disease (CKD) are desirable, owing to the limitations of erythropoiesis-stim... |
PMC12605969 | core_pubmed_pmc | Single Center, Open‐Label, Randomized Crossover Trial on Drug–Drug Interactions of Levothyroxine/Magnesium‐Citrate and Levothyroxine/Magnesium‐Aspartate in Healthy Subjects—The ThyroMag Trial | Single Center, Open‐Label, Randomized Crossover Trial on Drug–Drug Interactions of Levothyroxine/Magnesium‐Citrate and Levothyroxine/Magnesium‐Aspartate in Healthy Subjects—The ThyroMag Trial Abstract ABSTRACT Divalent cations such as calcium and ferrous sulfate interfere with the absorption of levothyroxine due to com... |
PMC12085125 | core_pubmed_pmc | Computational and Experimental Investigation of Antidiabetic Drugs on Tofacitinib Metabolism: Molecular Docking, in vitro, and in vivo Studies | Computational and Experimental Investigation of Antidiabetic Drugs on Tofacitinib Metabolism: Molecular Docking, in vitro, and in vivo Studies Abstract Abstract Background Tofacitinib is an orally administered Janus kinase (JAK) inhibitor that has demonstrated significant efficacy in the treatment of rheumatoid arthrit... |
PMC10568095 | core_pubmed_pmc | Eight Zhes Decoction ameliorates the lipid dysfunction of nonalcoholic fatty liver disease using integrated lipidomics, network pharmacology and pharmacokinetics | Eight Zhes Decoction ameliorates the lipid dysfunction of nonalcoholic fatty liver disease using integrated lipidomics, network pharmacology and pharmacokinetics Abstract Nonalcoholic fatty liver disease (NAFLD) has developed into the most common chronic liver disease and can lead to liver cancer. Our laboratory previo... |
PMC9050193 | core_pubmed_pmc | Population Pharmacokinetics of Intravenous Acyclovir in Oncologic Pediatric Patients | Population Pharmacokinetics of Intravenous Acyclovir in Oncologic Pediatric Patients Abstract Background: Acyclovir represents the first-line prophylaxis and therapy for herpes virus infections. However, its pharmacokinetics in children exposes them to the risk of ineffective or toxic concentrations. The study was aime... |
PMC5217889 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic evaluation of linagliptin for the treatment of type 2 diabetes mellitus, with consideration of Asian patient populations | Pharmacokinetic and pharmacodynamic evaluation of linagliptin for the treatment of type 2 diabetes mellitus, with consideration of Asian patient populations Abstract Abstract Our aims were to summarize the clinical pharmacokinetics and pharmacodynamics of the dipeptidyl‐peptidase‐4 inhibitor, linagliptin, and to consid... |
PMC7518612 | core_pubmed_pmc | Drug metabolism and pharmacokinetics of praziquantel: A review of variable drug exposure during schistosomiasis treatment in human hosts and experimental models | Drug metabolism and pharmacokinetics of praziquantel: A review of variable drug exposure during schistosomiasis treatment in human hosts and experimental models Abstract Abstract Schistosomiasis control is heavily reliant on the drug praziquantel (PZQ), which is used as preventive chemotherapy as part of national helmi... |
PMC6009248 | core_pubmed_pmc | A review of pharmacokinetic and pharmacodynamic interactions with antipsychotics | A review of pharmacokinetic and pharmacodynamic interactions with antipsychotics Abstract Introduction: Antipsychotics are widely used and often in combination with other drugs, thereby frequently subjected to drug-drug interactions. This review will provide a summary of potential pharmacokinetic (PK) and pharmacodynam... |
PMC9019721 | core_pubmed_pmc | Pharmacological Properties of Ginsenoside Re | Pharmacological Properties of Ginsenoside Re Abstract Abstract Ginsenoside Re is a protopanaxatriol-type saponin extracted from the berry, leaf, stem, flower bud, and root of Panax ginseng . In recent years, ginsenoside Re (Re) has been attracting attention as a dietary phytochemical. In this review, studies on Re were... |
PMC7493425 | core_pubmed_pmc | Quantitative systems pharmacology and the personalized drug–microbiota–diet axis | Quantitative systems pharmacology and the personalized drug–microbiota–diet axis Abstract Abstract Precision medicine is an emerging paradigm that aims at maximizing the benefits and minimizing the adverse effects of drugs. Realistic mechanistic models are needed to understand and limit heterogeneity in drug responses.... |
PMC3895035 | core_pubmed_pmc | Population Pharmacodynamic Modeling and Simulation of the Respiratory Effect of Acetazolamide in Decompensated COPD Patients | Population Pharmacodynamic Modeling and Simulation of the Respiratory Effect of Acetazolamide in Decompensated COPD Patients Abstract Background Chronic obstructive pulmonary disease (COPD) patients may develop metabolic alkalosis during weaning from mechanical ventilation. Acetazolamide is one of the treatments used t... |
PMC6221082 | core_pubmed_pmc | Extended dosing with CC‐486 (oral azacitidine) in patients with myeloid malignancies | Extended dosing with CC‐486 (oral azacitidine) in patients with myeloid malignancies Abstract Abstract CC‐486 (oral azacitidine) is an epigenetic modifier in clinical development for treatment of hematological cancers. This study of extended CC‐486 dosing included patients with myelodysplastic syndromes (MDSs), chronic... |
PMC11947583 | core_pubmed_pmc | Evaluation of the need for dosing adaptations in obese patients for surgical antibiotic prophylaxis: a model-based analysis of cefazolin pharmacokinetics | Evaluation of the need for dosing adaptations in obese patients for surgical antibiotic prophylaxis: a model-based analysis of cefazolin pharmacokinetics Abstract Abstract Background Cefazolin is used as a prophylactic antibiotic to reduce surgical site infections (SSIs). Obesity has been identified as a risk factor fo... |
PMC10589434 | core_pubmed_pmc | Perinatal Azithromycin Provides Limited Neuroprotection in an Ovine Model of Neonatal Hypoxic-Ischemic Encephalopathy | Perinatal Azithromycin Provides Limited Neuroprotection in an Ovine Model of Neonatal Hypoxic-Ischemic Encephalopathy Abstract Abstract BACKGROUND: Hypoxic-ischemic brain injury/encephalopathy affects about 1.15 million neonates per year, 96% of whom are born in low- and middle-income countries. Therapeutic hypothermia... |
PMC4753534 | core_pubmed_pmc | Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection | Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection Abstract Abstract Recently, we reported that chlorcyclizine (CCZ, Rac-2 ), an over-the-counter antihistamine piperazine drug, possesses in vitro and in vivo activity against hepatitis C vir... |
PMC5529777 | core_pubmed_pmc | Dissociated Agonist of Glucocorticoid Receptor or Prednisone for Active Rheumatoid Arthritis: Effects on P1NP and Osteocalcin Pharmacodynamics | Dissociated Agonist of Glucocorticoid Receptor or Prednisone for Active Rheumatoid Arthritis: Effects on P1NP and Osteocalcin Pharmacodynamics Abstract Abstract Fosdagrocorat (PF‐04171327), a dissociated agonist of the glucocorticoid receptor, has potent anti‐inflammatory activity in patients with rheumatoid arthritis ... |
PMC6510840 | core_pubmed_pmc | A phase 1b study of transforming growth factor-beta receptor I inhibitor galunisertib in combination with sorafenib in Japanese patients with unresectable hepatocellular carcinoma | A phase 1b study of transforming growth factor-beta receptor I inhibitor galunisertib in combination with sorafenib in Japanese patients with unresectable hepatocellular carcinoma Abstract Summary Background Galunisertib inhibits type I transforming growth factor-beta receptor serine/threonine kinase. The primary objec... |
PMC7927872 | core_pubmed_pmc | Cumulative Fraction of Response for Once- and Twice-Daily Delamanid in Patients with Pulmonary Multidrug-Resistant Tuberculosis | Cumulative Fraction of Response for Once- and Twice-Daily Delamanid in Patients with Pulmonary Multidrug-Resistant Tuberculosis Abstract Pharmacokinetic (PK) and pharmacodynamic (PD) analyses were conducted to determine the cumulative fraction of response (CFR) for 100 mg twice-daily (BID) and 200 mg once-daily (QD) de... |
PMC10011319 | core_pubmed_pmc | A Single- and Multiple-Dose Pharmacokinetic Study of Oral Perampanel in Healthy Chinese Subjects | A Single- and Multiple-Dose Pharmacokinetic Study of Oral Perampanel in Healthy Chinese Subjects Abstract Abstract Background and Objective Perampanel is a once-daily oral anti-seizure medication indicated for focal-onset seizures and generalized tonic-clonic seizures. This study investigated the single- and multiple-d... |
PMC6175223 | core_pubmed_pmc | In Vivo Assessment of the Effect of CYP1A2 Inhibition and Induction on Pomalidomide Pharmacokinetics in Healthy Subjects | In Vivo Assessment of the Effect of CYP1A2 Inhibition and Induction on Pomalidomide Pharmacokinetics in Healthy Subjects Abstract Abstract Pomalidomide is an immunomodulatory drug, and the dosage of 4 mg per day taken orally on days 1‐21 of repeated 28‐day cycles has been approved in the European Union and the United S... |
PMC4612403 | core_pubmed_pmc | Re-engineering a neuroprotective, clinical drug as a procognitive agent with high in vivo potency and with GABA A potentiating activity for use in dementia | Re-engineering a neuroprotective, clinical drug as a procognitive agent with high in vivo potency and with GABA A potentiating activity for use in dementia Abstract Abstract Background Synaptic dysfunction is a key event in pathogenesis of neurodegenerative diseases such as Alzheimer’s disease (AD) where synapse loss p... |
PMC9197540 | core_pubmed_pmc | Population PBPK modeling using parametric and nonparametric methods of the Simcyp Simulator, and Bayesian samplers | Population PBPK modeling using parametric and nonparametric methods of the Simcyp Simulator, and Bayesian samplers Abstract Abstract Physiologically‐based pharmacokinetic (PBPK) models usually include a large number of parameters whose values are obtained using in vitro to in vivo extrapolation. However, such extrapola... |
PMC11258086 | core_pubmed_pmc | Predictive performance of population pharmacokinetic models of imatinib in chronic myeloid leukemia patients | Predictive performance of population pharmacokinetic models of imatinib in chronic myeloid leukemia patients Abstract Abstract Background and aim Chronic myeloid leukemia is a myeloproliferative neoplasm associated with the specific chromosomal translocation known as the Philadelphia chromosome. Imatinib is a potent BC... |
PMC3065744 | core_pubmed_pmc | The Impact of Dosing Interval in a Novel Tandem Oral Dosing Strategy: Enhancing the Exposure of Low Solubility Drug Candidates in a Preclinical Setting | The Impact of Dosing Interval in a Novel Tandem Oral Dosing Strategy: Enhancing the Exposure of Low Solubility Drug Candidates in a Preclinical Setting Abstract Abstract In drug discovery, time and resource constraints necessitate increasingly early decision making to accelerate or stop preclinical programs. Early disc... |
PMC12485330 | core_pubmed_pmc | Forecasting in vivo pharmacokinetics of metformin HCl floating beads using Gastroplus® PBPK | Forecasting in vivo pharmacokinetics of metformin HCl floating beads using Gastroplus® PBPK Abstract Abstract Background Diabetes mellitus type II is expected to impact a large population worldwide. Among the available therapeutic options, Metformin hydrochloride is a key medication, particularly for those who cannot e... |
PMC12960935 | core_pubmed_pmc | Personalized pharmacokinetic–pharmacodynamic guided therapy via an induced pluripotent stem cell–derived multi-organoid platform in NF1-mutant breast cancer | Personalized pharmacokinetic–pharmacodynamic guided therapy via an induced pluripotent stem cell–derived multi-organoid platform in NF1-mutant breast cancer Abstract Effective precision oncology demands integration of pharmacokinetics/pharmacodynamics (PK/PD) profiling with tumor-specific genomic features. Here, we pre... |
PMC10955596 | core_pubmed_pmc | Average Electron Density: A Quantitative Tool for Evaluating Non-Classical Bioisosteres of Amides | Average Electron Density: A Quantitative Tool for Evaluating Non-Classical Bioisosteres of Amides Abstract Abstract Bioisosterism is strategically used in drug design to enhance the pharmacokinetic and pharmacodynamic properties of therapeutic molecules. The average electron density (AED) tool has been used in several ... |
PMC5428297 | core_pubmed_pmc | Short-Course, High-Dose Rifampicin Achieves Wolbachia Depletion Predictive of Curative Outcomes in Preclinical Models of Lymphatic Filariasis and Onchocerciasis | Short-Course, High-Dose Rifampicin Achieves Wolbachia Depletion Predictive of Curative Outcomes in Preclinical Models of Lymphatic Filariasis and Onchocerciasis Abstract Abstract Lymphatic filariasis (LF) and onchocerciasis are priority neglected tropical diseases targeted for elimination. The only safe drug treatment ... |
PMC10386913 | core_pubmed_pmc | A Joint Pharmacokinetic Model for the Simultaneous Description of Plasma and Whole Blood Tacrolimus Concentrations in Kidney and Lung Transplant Recipients | A Joint Pharmacokinetic Model for the Simultaneous Description of Plasma and Whole Blood Tacrolimus Concentrations in Kidney and Lung Transplant Recipients Abstract Abstract Background and Objective Historically, dosing of tacrolimus is guided by therapeutic drug monitoring (TDM) of the whole blood concentration, which... |
PMC6593619 | core_pubmed_pmc | Influence of the Proton Pump Inhibitor Esomeprazole on the Bioavailability of Regorafenib: A Randomized Crossover Pharmacokinetic Study | Influence of the Proton Pump Inhibitor Esomeprazole on the Bioavailability of Regorafenib: A Randomized Crossover Pharmacokinetic Study Abstract Abstract Regorafenib exposure could potentially be influenced by an interaction with acid‐reducing drugs. In this crossover trial, patients were randomized into two sequence g... |
PMC9054077 | core_pubmed_pmc | Oxidative radical coupling of hydroquinones and thiols using chromic acid: one-pot synthesis of quinonyl alkyl/aryl thioethers † | Oxidative radical coupling of hydroquinones and thiols using chromic acid: one-pot synthesis of quinonyl alkyl/aryl thioethers † Abstract An efficient, simple and practical protocol for one-pot sequential oxidative radical C–H/S–H cross-coupling of thiols with hydroquinones (HQs) and oxidation leading to the formation ... |
PMC9574852 | core_pubmed_pmc | Discovery and Optimization of the First Highly Effective and Orally Available Galectin-3 Inhibitors for Treatment of Fibrotic Disease | Discovery and Optimization of the First Highly Effective and Orally Available Galectin-3 Inhibitors for Treatment of Fibrotic Disease Abstract Galectin-3 is a carbohydrate-binding protein central to regulating mechanisms of diseases such as fibrosis, cancer, metabolic, inflammatory, and heart disease. We recently found... |
PMC4546427 | core_pubmed_pmc | Stereoselective Regulation of P-gp Activity by Clausenamide Enantiomers in Caco-2, KB/KBv and Brain Microvessel Endothelial Cells | Stereoselective Regulation of P-gp Activity by Clausenamide Enantiomers in Caco-2, KB/KBv and Brain Microvessel Endothelial Cells Abstract The (−)- and (+)-clausenamide (CLA) enantiomers have different pharmacokinetic effects in animals, but their association with putative stereoselective regulation of P-glycoprotein (... |
PMC7993273 | core_pubmed_pmc | Population Pharmacokinetic Analysis of the BTK Inhibitor Zanubrutinib in Healthy Volunteers and Patients With B‐Cell Malignancies | Population Pharmacokinetic Analysis of the BTK Inhibitor Zanubrutinib in Healthy Volunteers and Patients With B‐Cell Malignancies Abstract Abstract Zanubrutinib is a potent, second‐generation Bruton’s tyrosine kinase inhibitor that is currently being investigated in patients with B‐cell malignancies and recently receiv... |
PMC12761356 | core_pubmed_pmc | Anti‐Inflammatory, Antioxidant, Molecular Docking and Pharmacokinetics Properties of Cycloeucalenone Isolated From Musa × paradisiaca L. Fruit Peels | Anti‐Inflammatory, Antioxidant, Molecular Docking and Pharmacokinetics Properties of Cycloeucalenone Isolated From Musa × paradisiaca L. Fruit Peels Abstract ABSTRACT This study isolated a compound with anti‐inflammatory properties from Musa × paradisiaca fruit peels. The methanol extract was partitioned, and the hexan... |
PMC5970530 | core_pubmed_pmc | Absolute oral bioavailability and disposition kinetics of puerarin in female rats | Absolute oral bioavailability and disposition kinetics of puerarin in female rats Abstract Background Pueraria candollei var . mirifica is a medicinal plant that is promoted as a “Champion Product” by the Government of Thailand. This plant has been reported to relieve postmenopausal symptoms, prevent and reverse bone l... |
PMC8328391 | core_pubmed_pmc | Bioequivalence and Pharmacokinetic Evaluation of Two Oral Formulations of Regorafenib: An Open-Label, Randomised, Single-Dose, Two-Period, Two-Way Crossover Clinical Trial in Healthy Chinese Volunteers Under Fasting and Fed Conditions | Bioequivalence and Pharmacokinetic Evaluation of Two Oral Formulations of Regorafenib: An Open-Label, Randomised, Single-Dose, Two-Period, Two-Way Crossover Clinical Trial in Healthy Chinese Volunteers Under Fasting and Fed Conditions Abstract Abstract Background Regorafenib is an oral multi-kinase inhibitor approved f... |
PMC4727972 | core_pubmed_pmc | Chronic unpredicted mild stress-induced depression alter saxagliptin pharmacokinetics and CYP450 activity in GK rats | Chronic unpredicted mild stress-induced depression alter saxagliptin pharmacokinetics and CYP450 activity in GK rats Abstract Abstract Background. This study was to explore the pharmacokinetics of saxagliptin (Sax) in Goto–Kakizaki (GK) rats complicated with depression induced by chronic unpredicted mild stress (CUMS).... |
PMC3233417 | core_pubmed_pmc | Development of a Human Physiologically Based Pharmacokinetic (PBPK) Toolkit for Environmental Pollutants | Development of a Human Physiologically Based Pharmacokinetic (PBPK) Toolkit for Environmental Pollutants Abstract Abstract Physiologically Based Pharmacokinetic (PBPK) models can be used to determine the internal dose and strengthen exposure assessment. Many PBPK models are available, but they are not easily accessible... |
PMC11688075 | core_pubmed_pmc | Prescription regularity and pharmacodynamics mechanism of traditional Chinese medicine in autoimmune hepatitis: A data mining and network pharmacology study | Prescription regularity and pharmacodynamics mechanism of traditional Chinese medicine in autoimmune hepatitis: A data mining and network pharmacology study Abstract This study aims to provide a basis and reference for traditional Chinese medicine (TCM) in treating autoimmune hepatitis (AIH) by exploring the prescripti... |
PMC11134614 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics, and pharmacodynamics of TG103 injection in participants who are overweight or obese: a randomized, double-blind, placebo-controlled, multiple-dose phase 1b study | Safety, tolerability, pharmacokinetics, and pharmacodynamics of TG103 injection in participants who are overweight or obese: a randomized, double-blind, placebo-controlled, multiple-dose phase 1b study Abstract Background TG103, a glucagon-like peptide-1 analog, is being investigated as an option for weight management.... |
PMC8075933 | core_pubmed_pmc | Using physiologically-based pharmacokinetic modeling to assess the efficacy of glove materials in reducing internal doses and potential hazards of N-methylpyrrolidone during paint stripping | Using physiologically-based pharmacokinetic modeling to assess the efficacy of glove materials in reducing internal doses and potential hazards of N-methylpyrrolidone during paint stripping Abstract A refined risk assessment was conducted to evaluate the efficacy of different glove materials in reducing the potential h... |
PMC2997321 | core_pubmed_pmc | Influence of hepatic impairment on pharmacokinetics of the human GLP-1 analogue, liraglutide | Influence of hepatic impairment on pharmacokinetics of the human GLP-1 analogue, liraglutide Abstract AIMS To compare the pharmacokinetics (PK) of a single-dose of liraglutide in subjects with hepatic impairment. METHODS This parallel group, open label trial involved four groups of six subjects with healthy, mild, mode... |
PMC3315066 | core_pubmed_pmc | Relative Pesticide and Exposure Route Contribution to Aggregate and Cumulative Dose in Young Farmworker Children | Relative Pesticide and Exposure Route Contribution to Aggregate and Cumulative Dose in Young Farmworker Children Abstract Abstract The Child-Specific Aggregate Cumulative Human Exposure and Dose (CACHED) framework integrates micro-level activity time series with mechanistic exposure equations, environmental concentrati... |
PMC4678974 | core_pubmed_pmc | Effect of piperine on pharmacokinetics of sodium valproate in plasma samples of rats using gas chromatography-mass spectrometry method | Effect of piperine on pharmacokinetics of sodium valproate in plasma samples of rats using gas chromatography-mass spectrometry method Abstract Abstract Piperine (PIP) is used as anticonvulsant in traditional Chinese medicine. Co-administration of low-dose sodium valproate with PIP has been regarded to have potential a... |
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