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PMC9299591 | core_pubmed_pmc | Edoxaban Exposure in Patients With Atrial Fibrillation and Estimated Creatinine Clearance Exceeding 100 mL/min | Edoxaban Exposure in Patients With Atrial Fibrillation and Estimated Creatinine Clearance Exceeding 100 mL/min Abstract Abstract Edoxaban 60 mg is approved for stroke prevention in patients with atrial fibrillation (AF) not fulfilling any dose‐reduction criteria. As edoxaban is partially renally cleared (≈50%), this st... |
PMC10299927 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of Single-Dose Orally Administered Venglustat in Healthy Chinese Volunteers | Pharmacokinetics, Safety, and Tolerability of Single-Dose Orally Administered Venglustat in Healthy Chinese Volunteers Abstract Background and Objective Deficiencies of enzymes acting downstream of glucosylceramide synthase (GCS) can cause severe substrate accumulation. Venglustat is a small-molecule, brain-penetrant G... |
PMC9615618 | core_pubmed_pmc | Clinical pharmacologist from the eyes of a clinical pharmacologist: a questionnaire-based survey | Clinical pharmacologist from the eyes of a clinical pharmacologist: a questionnaire-based survey Abstract Introduction Management of a clinical condition is patient centric. Interdisciplinary coordination plays an influential role in patient management. Pharmacology deals with the study of drugs. Clinical pharmacology ... |
PMC11343942 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of Nebulized GB05-Human IFNα1b Inhalation Solution: A Randomized, Placebo-Controlled, Dose-Escalation Phase I Study in Healthy Chinese Adult Volunteers | Safety, Tolerability, and Pharmacokinetics of Nebulized GB05-Human IFNα1b Inhalation Solution: A Randomized, Placebo-Controlled, Dose-Escalation Phase I Study in Healthy Chinese Adult Volunteers Abstract Introduction Human respiratory syncytial virus (RSV) is the leading cause of lower respiratory tract infection, espe... |
PMC7983936 | core_pubmed_pmc | Tolerance to Opioid‐Induced Respiratory Depression in Chronic High‐Dose Opioid Users: A Model‐Based Comparison With Opioid‐Naïve Individuals | Tolerance to Opioid‐Induced Respiratory Depression in Chronic High‐Dose Opioid Users: A Model‐Based Comparison With Opioid‐Naïve Individuals Abstract Chronic opioid consumption is associated with addiction, physical dependence, and tolerance. Tolerance results in dose escalation to maintain the desired opioid effect. I... |
PMC5805208 | core_pubmed_pmc | Administration of rocuronium based on real body weight versus fat-free mass in patients with lymphedema | Administration of rocuronium based on real body weight versus fat-free mass in patients with lymphedema Abstract Abstract Objective To compare the clinical pharmacokinetics of rocuronium when applied according to fat-free mass versus real body weight during anesthetic induction of patients with lymphedema. Methods Sixt... |
PMC4558629 | core_pubmed_pmc | Pharmacokinetic study of metformin to compare a voglibose/metformin fixed-dose combination with coadministered voglibose and metformin | Pharmacokinetic study of metformin to compare a voglibose/metformin fixed-dose combination with coadministered voglibose and metformin Abstract The aim of this study was to compare the pharmacokinetic characteristics of metformin between a fixed-dose combination (FDC) of voglibose/metformin and co-administered individu... |
PMC10226670 | core_pubmed_pmc | Pharmacogenomic-guided dosing of fluoropyrimidines beyond DPYD : time for a polygenic algorithm? | Pharmacogenomic-guided dosing of fluoropyrimidines beyond DPYD : time for a polygenic algorithm? Abstract Fluoropyrimidines are chemotherapeutic agents widely used for the treatment of various solid tumors. Commonly prescribed FPs include 5-fluorouracil (5-FU) and its oral prodrugs capecitabine (CAP) and tegafur. Bioco... |
PMC7697022 | core_pubmed_pmc | Echinacea angustifolia DC. Lipophilic Extract Patch for Skin Application: Preparation, In Vitro and In Vivo Studies | Echinacea angustifolia DC. Lipophilic Extract Patch for Skin Application: Preparation, In Vitro and In Vivo Studies Abstract Dodeca-2 E ,4 E ,8 Z ,10 E / Z -tetraenoic isobutylamide (tetraene) is the main component of Echinacea angustifolia DC. lipophilic extract, the bioavailability and immunomodulatory effect after o... |
PMC9543418 | core_pubmed_pmc | Assessment of ethanol exposure from hand sanitizer use and potential for developmental toxicity in nursing infants | Assessment of ethanol exposure from hand sanitizer use and potential for developmental toxicity in nursing infants Abstract Abstract Ingestion of ethanol during pregnancy is known to have detrimental effects on the fetus. Although the potential developmental effects of maternal ethanol intake during lactation are less ... |
PMC5554475 | core_pubmed_pmc | A Multicentre Study on the Efficacy, Safety and Pharmacokinetics of IqYmune®, a Highly Purified 10% Liquid Intravenous Immunoglobulin, in Patients with Primary Immune Deficiency | A Multicentre Study on the Efficacy, Safety and Pharmacokinetics of IqYmune®, a Highly Purified 10% Liquid Intravenous Immunoglobulin, in Patients with Primary Immune Deficiency Abstract This multicentre, open-label, prospective, single-arm study was designed to evaluate the efficacy, pharmacokinetics, and safety of Iq... |
PMC4604629 | core_pubmed_pmc | NKTR-102 Efficacy versus irinotecan in a mouse model of brain metastases of breast cancer | NKTR-102 Efficacy versus irinotecan in a mouse model of brain metastases of breast cancer Abstract Abstract Background Brain metastases are an increasing problem in women with invasive breast cancer. Strategies designed to treat brain metastases of breast cancer, particularly chemotherapeutics such as irinotecan, demon... |
PMC4159916 | core_pubmed_pmc | LC-MS/MS determination and pharmacokinetics study of puerarin and daidzein in rat plasma after oral administration of Gegenqinlian decoction and Radix Puerariae extract | LC-MS/MS determination and pharmacokinetics study of puerarin and daidzein in rat plasma after oral administration of Gegenqinlian decoction and Radix Puerariae extract Abstract Background: Gegenqinlian decoction (GQD) is a famous traditional medicine recipe. It is composed of four herbs including Radix Puerariae (GG),... |
PMC4112772 | core_pubmed_pmc | Absorption and Peak Blood Alcohol Concentration After Drinking Beer, Wine, or Spirits | Absorption and Peak Blood Alcohol Concentration After Drinking Beer, Wine, or Spirits Abstract Background Both the amount and the rate of absorption of ethanol ( EtOH ) from alcoholic beverages are key determinants of the peak blood alcohol concentration ( BAC ) and exposure of organs other than gut and liver. Previous... |
PMC12114325 | core_pubmed_pmc | Exploring Ginseng Bioactive Compound’s Role in Hypertension Remedy: An In Silico Approach | Exploring Ginseng Bioactive Compound’s Role in Hypertension Remedy: An In Silico Approach Abstract Abstract Background/Objectives : Ginseng has been a traditional remedy for centuries, known for its diverse benefits such as anti-inflammation, antioxidant, bactericidal, fungicidal antidiabetic, and anticancer effects. T... |
PMC6972521 | core_pubmed_pmc | Effects of Maribavir on P‐Glycoprotein and CYP2D6 in Healthy Volunteers | Effects of Maribavir on P‐Glycoprotein and CYP2D6 in Healthy Volunteers Abstract Abstract Maribavir is an investigational drug being evaluated in transplant recipients with cytomegalovirus infection. To understand potential drug‐drug interactions, we examined the effects of multiple doses of maribavir on cytochrome P45... |
PMC8157244 | core_pubmed_pmc | Computational Treatment Simulations to Assess the Need for Personalized Tamoxifen Dosing in Breast Cancer Patients of Different Biogeographical Groups | Computational Treatment Simulations to Assess the Need for Personalized Tamoxifen Dosing in Breast Cancer Patients of Different Biogeographical Groups Abstract Simple Summary Tamoxifen is a drug often used to treat the most common type of breast cancer. Its metabolite endoxifen is formed by the liver enzyme CYP2D6, who... |
PMC12816223 | core_pubmed_pmc | Fibroblast growth factor receptor inhibitors in glioma: a narrative review of recent advances | Fibroblast growth factor receptor inhibitors in glioma: a narrative review of recent advances Abstract Gliomas are devastating CNS malignancies characterized by extreme molecular heterogeneity and poor prognosis; the fibroblast growth factor receptor (FGFR) signaling axis, which drives proliferation, stemness, and meta... |
PMC9544171 | core_pubmed_pmc | Glucose‐dependent insulinotropic polypeptide receptor antagonist treatment causes a reduction in weight gain in ovariectomised high fat diet‐fed mice | Glucose‐dependent insulinotropic polypeptide receptor antagonist treatment causes a reduction in weight gain in ovariectomised high fat diet‐fed mice Abstract Abstract Background and purpose The incretin hormone, gastric inhibitory peptide/glucose‐dependent insulinotropic polypeptide (GIP), secreted by the enteroendocr... |
PMC6858924 | core_pubmed_pmc | Bioavailability and Pharmacokinetics of Once-Daily Amantadine Extended-Release Tablets in Healthy Volunteers: Results from Three Randomized, Crossover, Open-Label, Phase 1 Studies | Bioavailability and Pharmacokinetics of Once-Daily Amantadine Extended-Release Tablets in Healthy Volunteers: Results from Three Randomized, Crossover, Open-Label, Phase 1 Studies Abstract Introduction In February 2018, OS320—an amantadine extended-release (ER) tablet formulation with once-daily morning administration—... |
PMC6042594 | core_pubmed_pmc | Oral propranolol for prevention of threshold retinopathy of prematurity (ROPROP): protocol of a randomised controlled trial | Oral propranolol for prevention of threshold retinopathy of prematurity (ROPROP): protocol of a randomised controlled trial Abstract Introduction Retinopathy of prematurity (ROP) is a disease observed in extremely premature infants characterised by visioning-threatening retinal vessel proliferation. Propranolol, a drug... |
PMC10302681 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Perampanel in Portuguese Patients Diagnosed with Refractory Epilepsy | Population Pharmacokinetic Analysis of Perampanel in Portuguese Patients Diagnosed with Refractory Epilepsy Abstract Perampanel is a promising antiepileptic drug (AED) for refractory epilepsy treatment due to its innovative mechanism of action. This study aimed to develop a population pharmacokinetic (PopPK) model to b... |
PMC12205928 | core_pubmed_pmc | Leveraging machine learning models in evaluating ADMET properties for drug discovery and development | Leveraging machine learning models in evaluating ADMET properties for drug discovery and development Abstract Abstract Background and purpose The evaluation of ADMET properties remains a critical bottleneck in drug discovery and development, contributing significantly to the high attrition rate of drug candidates. Trad... |
PMC11787889 | core_pubmed_pmc | Insights into interspecies protein binding variability using clindamycin as an example | Insights into interspecies protein binding variability using clindamycin as an example Abstract Abstract Background In the preclinical development of new drugs, animal models are often employed to predict their efficacy in humans, relying on translational pharmacokinetic/pharmacodynamic (PK/PD) studies. We performed in... |
PMC9197535 | core_pubmed_pmc | Use of physiologically‐based pharmacokinetic modeling to inform dosing of the opioid analgesics fentanyl and methadone in children with obesity | Use of physiologically‐based pharmacokinetic modeling to inform dosing of the opioid analgesics fentanyl and methadone in children with obesity Abstract Abstract Obesity is an increasingly alarming public health threat, with nearly 20% of children classified as obese in the United States today. Children with obesity ar... |
PMC7262232 | core_pubmed_pmc | Hydroxychloroquine for Treatment of SARS‐CoV‐2 Infection? Improving Our Confidence in a Model‐Based Approach to Dose Selection | Hydroxychloroquine for Treatment of SARS‐CoV‐2 Infection? Improving Our Confidence in a Model‐Based Approach to Dose Selection Conclusion CONCLUSIONS When simulated tissue drug concentrations are used to support dosing recommendations, the quality of the data used to inform the time‐dependent drug distribution to tissu... |
PMC11916277 | core_pubmed_pmc | Immune modulation in solid tumors: a phase 1b study of RO6870810 (BET inhibitor) and atezolizumab (PD-L1 inhibitor) | Immune modulation in solid tumors: a phase 1b study of RO6870810 (BET inhibitor) and atezolizumab (PD-L1 inhibitor) Abstract Abstract Purpose Bromodomain and extra-terminal domain (BET) inhibitors (BETi) have demonstrated epigenetic modulation capabilities, specifically in transcriptional repression of oncogenic pathwa... |
PMC6287197 | core_pubmed_pmc | Eukaryotic Cell Toxicity and HSA Binding of [Ru(Me 4 phen)(bb 7 )] 2+ and the Effect of Encapsulation in Cucurbit[10]uril | Eukaryotic Cell Toxicity and HSA Binding of [Ru(Me 4 phen)(bb 7 )] 2+ and the Effect of Encapsulation in Cucurbit[10]uril Abstract The toxicity (IC 50 ) of a series of mononuclear ruthenium complexes containing bis[4(4′-methyl-2,2′-bipyridyl)]-1, n -alkane (bb n ) as a tetradentate ligand against three eukaryotic cell ... |
PMC10649612 | core_pubmed_pmc | Investigating the ability to adhere to cardiometabolic medications with different properties: a retrospective cohort study of >500 000 patients in the USA | Investigating the ability to adhere to cardiometabolic medications with different properties: a retrospective cohort study of >500 000 patients in the USA Abstract Abstract Objective Poor medication adherence remains highly prevalent and adversely affects health outcomes. Patients frequently describe properties of the ... |
PMC12211128 | core_pubmed_pmc | Safety, tolerability, pharmacokinetic and pharmacodynamic effects of the muscarinic M 1 positive allosteric modulator VU0467319 for Alzheimer’s disease: a single ascending-dose study in healthy participants | Safety, tolerability, pharmacokinetic and pharmacodynamic effects of the muscarinic M 1 positive allosteric modulator VU0467319 for Alzheimer’s disease: a single ascending-dose study in healthy participants Abstract The development of cholinergic neurotransmitter based cognitive enhancers for Alzheimer’s disease and ot... |
PMC10634346 | core_pubmed_pmc | Enitociclib, a Selective CDK9 Inhibitor, Induces Complete Regression of MYC+ Lymphoma by Downregulation of RNA Polymerase II Mediated Transcription | Enitociclib, a Selective CDK9 Inhibitor, Induces Complete Regression of MYC+ Lymphoma by Downregulation of RNA Polymerase II Mediated Transcription Abstract Abstract Double-hit diffuse large B-cell lymphoma (DH-DLBCL) is an aggressive, and often refractory, type of B-cell non–Hodgkin lymphoma (NHL) characterized by rea... |
PMC6826385 | core_pubmed_pmc | The Odyssey of Bioactive Compounds in Avocado ( Persea americana ) and Their Health Benefits | The Odyssey of Bioactive Compounds in Avocado ( Persea americana ) and Their Health Benefits Abstract Abstract Persea americana , commonly known as avocado, has recently gained substantial popularity and is often marketed as a “superfood” because of its unique nutritional composition, antioxidant content, and biochemic... |
PMC12655431 | core_pubmed_pmc | Evaluation of the Activity of Amino Chalcone Against Staphylococcus Strains Harboring Efflux Pumps | Evaluation of the Activity of Amino Chalcone Against Staphylococcus Strains Harboring Efflux Pumps Abstract Background/Objectives: The increasing prevalence of multidrug-resistant Staphylococcus aureus represents a major clinical challenge, primarily driven by the acquisition of multiple resistance mechanisms. Among th... |
PMC8710486 | core_pubmed_pmc | Kill Rate and Evaluation of Ex Vivo PK/PD Integration of Cefquinome Against Actinobacillus pleuropneumoniae | Kill Rate and Evaluation of Ex Vivo PK/PD Integration of Cefquinome Against Actinobacillus pleuropneumoniae Abstract Abstract We wished to study the detailed and precise antibacterial activity of cefquinome against Actinobacillus pleuropneumoniae (APP) in vitro and ex vivo . We analyzed the relationships between kill r... |
PMC3670493 | core_pubmed_pmc | Combination neratinib (HKI-272) and paclitaxel therapy in patients with HER2-positive metastatic breast cancer | Combination neratinib (HKI-272) and paclitaxel therapy in patients with HER2-positive metastatic breast cancer Abstract Abstract Introduction: Neratinib is a potent irreversible pan-ErbB tyrosine kinase inhibitor that has demonstrated antitumour activity and an acceptable safety profile in patients with human epidermal... |
PMC12185263 | core_pubmed_pmc | Limited Sampling Strategies to Predict Mycophenolic Acid and Tacrolimus Area Under the Concentration–Time Curve in Steroid‐Free Kidney Transplant Patients | Limited Sampling Strategies to Predict Mycophenolic Acid and Tacrolimus Area Under the Concentration–Time Curve in Steroid‐Free Kidney Transplant Patients Abstract ABSTRACT This study aimed to develop limited sampling strategies to predict oral mycophenolic acid (MPA) exposure from one to three blood samples in stable ... |
PMC10675695 | core_pubmed_pmc | Ornidazole Transfer into Colostrum and Assessment of Exposure Risk for Breastfeeding Infant: A Population Pharmacokinetic Analysis | Ornidazole Transfer into Colostrum and Assessment of Exposure Risk for Breastfeeding Infant: A Population Pharmacokinetic Analysis Abstract Ornidazole is frequently used for the prevention and treatment of anaerobic infections after caesarean section. There is still a lack of data on the excretion of ornidazole in brea... |
PMC3611076 | core_pubmed_pmc | False selection of syringe-brand compatibility and the method of correction during target-controlled infusion of propofol | False selection of syringe-brand compatibility and the method of correction during target-controlled infusion of propofol Abstract Background We evaluated volumetric differences of syringe brand compatibilities, and investigated the impact of false brand settings on target-controlled infusion (TCI) and their methods of... |
PMC11961695 | core_pubmed_pmc | FIGHT-101, a first-in-human study of potent and selective FGFR 1–3 inhibitor pemigatinib in pan-cancer patients with FGF / FGFR alterations and advanced malignancies | FIGHT-101, a first-in-human study of potent and selective FGFR 1–3 inhibitor pemigatinib in pan-cancer patients with FGF / FGFR alterations and advanced malignancies Abstract Background: The phase I/II FIGHT-101 study ( NCT02393248 ) evaluated safety, pharmacokinetics, pharmacodynamics, and preliminary efficacy of pemi... |
PMC4265270 | core_pubmed_pmc | Pharmacokinetics of marbofloxacin in pigs after intravenous and intramuscular administration of a single dose of 8 mg/kg: dose proportionality, influence of the age of the animals and urinary elimination | Pharmacokinetics of marbofloxacin in pigs after intravenous and intramuscular administration of a single dose of 8 mg/kg: dose proportionality, influence of the age of the animals and urinary elimination Abstract Abstract The pharmacokinetics of marbofloxacin in pigs were evaluated as a function of dose and animal age ... |
PMC7547843 | core_pubmed_pmc | Development of Rifapentine-Loaded PLGA-Based Nanoparticles: In vitro Characterisation and in vivo Study in Mice | Development of Rifapentine-Loaded PLGA-Based Nanoparticles: In vitro Characterisation and in vivo Study in Mice Abstract Background Tuberculosis (TB) is a leading cause of death amongst infectious diseases. The poor response to antitubercular agents necessitates the long-term use of high drug doses, resulting in low pa... |
PMC7658085 | core_pubmed_pmc | Population Pharmacokinetic–Pharmacodynamic Relationships of Sarilumab Using Disease Activity Score 28-Joint C-Reactive Protein and Absolute Neutrophil Counts in Patients with Rheumatoid Arthritis | Population Pharmacokinetic–Pharmacodynamic Relationships of Sarilumab Using Disease Activity Score 28-Joint C-Reactive Protein and Absolute Neutrophil Counts in Patients with Rheumatoid Arthritis Abstract Background Sarilumab is a human monoclonal antibody blocking the interleukin-6 receptor alpha (IL-6Rɑ) approved for... |
PMC8674007 | core_pubmed_pmc | Evaluation of the estimation and classification performance of NONMEM when applying mixture model for drug clearance | Evaluation of the estimation and classification performance of NONMEM when applying mixture model for drug clearance Abstract Abstract Maximum likelihood estimation of parameters involving mixture model is known to have significant and specific patterns of errors. Population pharmacokinetic (PopPK) modeling using NONME... |
PMC9578159 | core_pubmed_pmc | Evaluation of Vancomycin Accumulation in Patients With Obesity | Evaluation of Vancomycin Accumulation in Patients With Obesity Abstract Abstract Background Current vancomycin guidelines recommend early and frequent area-under-the-curve monitoring in patients with obesity. Vancomycin's volume of distribution is likely altered in patients with obesity, which may result in lower serum... |
PMC10087179 | core_pubmed_pmc | A pharmacometrics model to define docetaxel target in early breast cancer | A pharmacometrics model to define docetaxel target in early breast cancer Abstract Abstract Aims We aimed to study the relation between pharmacokinetics (PK) and pharmacodynamics (PD) of docetaxel in early breast cancer and recommend a target exposure. Methods A PK/PD study was performed in 27 early breast cancer patie... |
PMC6343228 | core_pubmed_pmc | Case Report: Three's a crowd: a case report examining the diagnostic and pharmacokinetic challenges in HIV-tuberculous meningitis-malaria co-infection | Case Report: Three's a crowd: a case report examining the diagnostic and pharmacokinetic challenges in HIV-tuberculous meningitis-malaria co-infection Abstract In 2016, 10.4 million cases of tuberculosis (TB) were reported globally. Malaria also continues to be a global public health threat. Due to marked epidemiologic... |
PMC8504851 | core_pubmed_pmc | Pharmacokinetic, pharmacodynamic, and immunogenic rationale for optimal dosing of pegvaliase, a PEGylated bacterial enzyme, in adult patients with phenylketonuria | Pharmacokinetic, pharmacodynamic, and immunogenic rationale for optimal dosing of pegvaliase, a PEGylated bacterial enzyme, in adult patients with phenylketonuria Abstract Abstract Phenylketonuria (PKU), a deficiency in the activity of the enzyme phenylalanine hydroxylase, leads to toxic levels of phenylalanine (Phe) i... |
PMC3489562 | core_pubmed_pmc | Pharmacokinetic analysis of topical tobramycin in equine tears by automated immunoassay | Pharmacokinetic analysis of topical tobramycin in equine tears by automated immunoassay Abstract Background Ophthalmic antibiotic therapy in large animals is often used empirically because of the lack of pharmacokinetics studies. The purpose of the study was to determine the pharmacokinetics of topical tobramycin 0.3% ... |
PMC11971100 | core_pubmed_pmc | Population Pharmacokinetic-Pharmacodynamic (popPK/PD) Relationship of Orismilast, A Potent and Selective PDE4B/D Inhibitor, in Atopic Dermatitis | Population Pharmacokinetic-Pharmacodynamic (popPK/PD) Relationship of Orismilast, A Potent and Selective PDE4B/D Inhibitor, in Atopic Dermatitis Abstract Introduction Orismilast is a novel oral selective inhibitor of phosphodiesterase 4B and 4D subtypes (PDE4B/D) in clinical development for treatment of atopic dermatit... |
PMC6202340 | core_pubmed_pmc | Development and single dose clinical pharmacokinetics investigation of novel zein assisted- alpha lipoic acid nanoencapsulation of vardenafil | Development and single dose clinical pharmacokinetics investigation of novel zein assisted- alpha lipoic acid nanoencapsulation of vardenafil Abstract Abstract The aim of this study was to utilize the biocompatibility of the natural ingredients zein and alpha lipoic acid (ALA) as a novel nanosphere matrix formulation t... |
PMC12607478 | core_pubmed_pmc | Topical Ruxolitinib and Delgocitinib Versus Systemic JAK Inhibitors: A Comparative Safety Review | Topical Ruxolitinib and Delgocitinib Versus Systemic JAK Inhibitors: A Comparative Safety Review Abstract Abstract Janus Kinase Inhibitors (JAKi) represent a novel class of drugs for the treatment of chronic inflammatory skin diseases. Topical JAKi (t-JAKi) offer targeted therapy at potentially reduced systemic side ef... |
PMC11061430 | core_pubmed_pmc | A physiologically based pharmacokinetic/pharmacodynamic model to determine dosage regimens and withdrawal intervals of aditoprim against Streptococcus suis | A physiologically based pharmacokinetic/pharmacodynamic model to determine dosage regimens and withdrawal intervals of aditoprim against Streptococcus suis Abstract Abstract Introduction: Streptococcus suis ( S. suis ) is a zoonotic pathogen threatening public health. Aditoprim (ADP), a novel veterinary medicine, exhib... |
PMC7474130 | core_pubmed_pmc | Comparative pharmacokinetics of six major compounds in normal and insomnia rats after oral administration of Ziziphi Spinosae Semen aqueous extract | Comparative pharmacokinetics of six major compounds in normal and insomnia rats after oral administration of Ziziphi Spinosae Semen aqueous extract Abstract Ziziphi Spinosae Semen (ZSS), a traditional Chinese medicine, is used in clinics for the treatment of insomnia in China and other Asian countries. Herein, we descr... |
PMC4394614 | core_pubmed_pmc | Quantification of the Forgiveness of Drugs to Imperfect Adherence | Quantification of the Forgiveness of Drugs to Imperfect Adherence Abstract The circumstance of how sensitive therapeutic success is under imperfect adherence is driven by the property known as forgiveness. To date, no studies have considered variability in the pharmacokinetic-pharmacodynamic process in conjunction with... |
PMC4330041 | core_pubmed_pmc | Clinical pharmacokinetics of AZD3199, an inhaled ultra-long-acting β 2 -adrenoreceptor agonist (uLABA) | Clinical pharmacokinetics of AZD3199, an inhaled ultra-long-acting β 2 -adrenoreceptor agonist (uLABA) Abstract Abstract Objective The clinical pharmacokinetics of AZD3199, an ultra-long-acting β 2 -agonist, were investigated in healthy volunteers and patients with asthma or chronic obstructive pulmonary disease (COPD)... |
PMC9319709 | core_pubmed_pmc | The Role of Interventional Irisin on Heart Molecular Physiology | The Role of Interventional Irisin on Heart Molecular Physiology Abstract Abstract Irisin, encoded by the FNDC5 (fibronectin type III domain containing 5) gene, is a novel myokine that has been implicated as an essential mediator of exercise benefits. Effects of irisin on heart physiology is still ambiguous. This study ... |
PMC10291925 | core_pubmed_pmc | Concentrations and association between exposure to mixed perfluoroalkyl and polyfluoroalkyl substances and glycometabolism among adolescents | Concentrations and association between exposure to mixed perfluoroalkyl and polyfluoroalkyl substances and glycometabolism among adolescents Abstract Abstract Background Perfluoroalkyl and polyfluoroalkyl substances (PFASs) are widely used for industrial and commercial purposes and have received increasing attention du... |
PMC6374970 | core_pubmed_pmc | Design, characterization and comparison of transdermal delivery of colchicine via borneol-chemically-modified and borneol-physically-modified ethosome | Design, characterization and comparison of transdermal delivery of colchicine via borneol-chemically-modified and borneol-physically-modified ethosome Abstract Abstract Gout is a kind of joint disease characterized by the accumulation of monosodium urate (MSU) crystals in the joint and its surrounding tissue, causing p... |
PMC8876044 | core_pubmed_pmc | Carisoprodol Single and Multiple Dose PK-PD. Part II: Pharmacodynamics Evaluation Method for Central Muscle Relaxants. Double-Blind Placebo-Controlled Clinical Trial in Healthy Volunteers | Carisoprodol Single and Multiple Dose PK-PD. Part II: Pharmacodynamics Evaluation Method for Central Muscle Relaxants. Double-Blind Placebo-Controlled Clinical Trial in Healthy Volunteers Abstract Centrally acting skeletal muscle relaxants (CMR) such as carisoprodol are used to treat acute, painful musculoskeletal cond... |
PMC8932706 | core_pubmed_pmc | Intraperitoneal pharmacokinetics of vancomycin in patients on automated peritoneal dialysis | Intraperitoneal pharmacokinetics of vancomycin in patients on automated peritoneal dialysis Abstract Abstract It is unclear if the pharmacokinetics of vancomycin are the same during automated peritoneal dialysis (APD), where cycler exchanges may affect the systemic, peritoneal, and urinary disposition of drug. We condu... |
PMC4393081 | core_pubmed_pmc | Elucidating the Influence of Gold Nanoparticles on the Binding of Salvianolic Acid B and Rosmarinic Acid to Bovine Serum Albumin | Elucidating the Influence of Gold Nanoparticles on the Binding of Salvianolic Acid B and Rosmarinic Acid to Bovine Serum Albumin Abstract Salvianolic acid B and rosmarinic acid are two main water-soluble active ingredients from Salvia miltiorrhiza with important pharmacological activities and clinical applications. The... |
PMC7684025 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Factors Contribute to Synergism between Let-7c-5p and 5-Fluorouracil in Inhibiting Hepatocellular Carcinoma Cell Viability | Pharmacokinetic and Pharmacodynamic Factors Contribute to Synergism between Let-7c-5p and 5-Fluorouracil in Inhibiting Hepatocellular Carcinoma Cell Viability Abstract Abstract Pharmacological interventions for hepatocellular carcinoma (HCC) are hindered by complex factors, and rational combination therapy may be devel... |
PMC7821288 | core_pubmed_pmc | Population Pharmacokinetic Analysis of BMS‐986166, a Novel Selective Sphingosine‐1‐Phosphate‐1 Receptor Modulator, and Exposure‐Response Assessment of Lymphocyte Counts and Heart Rate in Healthy Participants | Population Pharmacokinetic Analysis of BMS‐986166, a Novel Selective Sphingosine‐1‐Phosphate‐1 Receptor Modulator, and Exposure‐Response Assessment of Lymphocyte Counts and Heart Rate in Healthy Participants Abstract Abstract Sphingosine‐1‐phosphate (S1P) binding to the S1P‐1 receptor (S1P1R) controls the egress of lym... |
PMC5399635 | core_pubmed_pmc | Pharmacologic Profile of Naloxegol, a Peripherally Acting µ -Opioid Receptor Antagonist, for the Treatment of Opioid-Induced Constipation | Pharmacologic Profile of Naloxegol, a Peripherally Acting µ -Opioid Receptor Antagonist, for the Treatment of Opioid-Induced Constipation Abstract Opioid-induced constipation (OIC) is a common side effect of opioid pharmacotherapy for the management of pain because opioid agonists bind to µ -opioid receptors in the ent... |
PMC6393559 | core_pubmed_pmc | Enhancing bioactivity, physicochemical, and pharmacokinetic properties of a nano-sized, anti-VEGFR2 Adnectin, through PASylation technology | Enhancing bioactivity, physicochemical, and pharmacokinetic properties of a nano-sized, anti-VEGFR2 Adnectin, through PASylation technology Abstract Abstract The crucial role of VEGF receptor 2 (VEGFR2) signaling in the angiogenesis and metastasis of solid tumors has prompted the development of inhibitors with minimal ... |
PMC9431184 | core_pubmed_pmc | In Vitro Activity of New β-Lactam–β-Lactamase Inhibitor Combinations and Comparators against Clinical Isolates of Gram-Negative Bacilli: Results from the China Antimicrobial Surveillance Network (CHINET) in 2019 | In Vitro Activity of New β-Lactam–β-Lactamase Inhibitor Combinations and Comparators against Clinical Isolates of Gram-Negative Bacilli: Results from the China Antimicrobial Surveillance Network (CHINET) in 2019 Abstract ABSTRACT Novel β-lactam–β-lactamase inhibitor combinations (BLBLIs) are in clinical development for... |
PMC11227592 | core_pubmed_pmc | A randomised trial of malaria vaccine R21/Matrix-M™ with and without antimalarial drugs in Thai adults | A randomised trial of malaria vaccine R21/Matrix-M™ with and without antimalarial drugs in Thai adults Abstract In preparation for mass vaccinations with R21/Matrix-M™ combined with mass administrations of dihydroartemisinin, piperaquine, and a single low dose primaquine we assessed the tolerability, safety, and potent... |
PMC12496225 | core_pubmed_pmc | Preclinical Evaluation of a Novel Molecule Targeting Nucleoside Homeostasis to Restore Energy Metabolism and Cognitive Function in Alzheimer's Disease | Preclinical Evaluation of a Novel Molecule Targeting Nucleoside Homeostasis to Restore Energy Metabolism and Cognitive Function in Alzheimer's Disease Abstract ABSTRACT Alzheimer's disease (AD) is the most prevalent cause of dementia, characterized by progressive cognitive decline and cerebral metabolic impairment. Yet... |
PMC6895071 | core_pubmed_pmc | Is Meropenem as a Monotherapy Truly Incompetent for Meropenem-Nonsusceptible Bacterial Strains? A Pharmacokinetic/Pharmacodynamic Modeling With Monte Carlo Simulation | Is Meropenem as a Monotherapy Truly Incompetent for Meropenem-Nonsusceptible Bacterial Strains? A Pharmacokinetic/Pharmacodynamic Modeling With Monte Carlo Simulation Abstract Infections due to meropenem-nonsusceptible bacterial strains (MNBSs) with meropenem minimum inhibitory concentrations (MICs) ≥ 16 mg/L have beco... |
PMC10177727 | core_pubmed_pmc | Evaluation of the Drug–Drug Interaction Potential of Ensitrelvir Fumaric Acid with Cytochrome P450 3A Substrates in Healthy Japanese Adults | Evaluation of the Drug–Drug Interaction Potential of Ensitrelvir Fumaric Acid with Cytochrome P450 3A Substrates in Healthy Japanese Adults Abstract Background Management of drug–drug interactions (DDIs) for ensitrelvir, a novel 3-chymotrypsin-like protease inhibitor of SARS-CoV-2 infection is crucial. A previous clini... |
PMC10572082 | core_pubmed_pmc | Delivery of the Brainshuttle™ amyloid-beta antibody fusion trontinemab to non-human primate brain and projected efficacious dose regimens in humans | Delivery of the Brainshuttle™ amyloid-beta antibody fusion trontinemab to non-human primate brain and projected efficacious dose regimens in humans Abstract ABSTRACT There are few treatments that slow neurodegeneration in Alzheimer’s disease (AD), and while therapeutic antibodies are being investigated in clinical tria... |
PMC9365747 | core_pubmed_pmc | Ethnicity evaluation of ferric pyrophosphate citrate among Asian and Non-Asian populations: a population pharmacokinetics analysis | Ethnicity evaluation of ferric pyrophosphate citrate among Asian and Non-Asian populations: a population pharmacokinetics analysis Abstract Purpose To evaluate the potential ethnic differences of ferric pyrophosphate citrate (FPC, Triferic) in healthy subjects and patients with hemodialysis-dependent stage 5 chronic ki... |
PMC3892602 | core_pubmed_pmc | Safety, pharmacokinetics and efficacy of artemisinins in pregnancy | Safety, pharmacokinetics and efficacy of artemisinins in pregnancy Abstract Malaria in pregnancy can lead to serious maternal and fetal morbidity and mortality. Access to the most effective antimalarials in pregnancy is essential. Resistance to current therapies is high for all antimalarial therapies except artemisinin... |
PMC11450061 | core_pubmed_pmc | Dose Justification for Asciminib in Patients with Philadelphia Chromosome-Positive Chronic Myeloid Leukemia with and Without the T315I Mutation | Dose Justification for Asciminib in Patients with Philadelphia Chromosome-Positive Chronic Myeloid Leukemia with and Without the T315I Mutation Abstract Abstract Background and Objective Asciminib is approved in patients with Philadelphia chromosome-positive chronic myeloid leukemia in chronic phase (Ph+ CML-CP) treate... |
PMC10698726 | core_pubmed_pmc | Stereoselective Inhibition of High- and Low-Affinity Organic Cation Transporters | Stereoselective Inhibition of High- and Low-Affinity Organic Cation Transporters Abstract Abstract Many drugs have chiral centers and are therapeutically applied as racemates. Thus, the stereoselectivity in their interactions with membrane transporters needs to be addressed. Here, we studied stereoselectivity in inhibi... |
PMC12387622 | core_pubmed_pmc | Modulatory Effects of Caffeine on Imatinib Binding: A Molecular Docking Study Targeting CYP3A4 | Modulatory Effects of Caffeine on Imatinib Binding: A Molecular Docking Study Targeting CYP3A4 Abstract Caffeine is a widely consumed psychoactive compound known to influence drug metabolism and efficacy through interactions with key enzymes such as cytochrome P450 3A4 (CYP3A4). This study investigates the molecular im... |
PMC12658809 | core_pubmed_pmc | Multibatch Fingerprint Integrated with Multi-Indicator Efficacy for Quality Evaluation of Sanhua Decoction and Investigation of Its Mechanistic Basis against Cerebral Ischemia-Reperfusion Injury | Multibatch Fingerprint Integrated with Multi-Indicator Efficacy for Quality Evaluation of Sanhua Decoction and Investigation of Its Mechanistic Basis against Cerebral Ischemia-Reperfusion Injury Abstract Building upon the spectrum-effect relationship theory in traditional Chinese medicine, ultraperformance liquid chrom... |
PMC10439950 | core_pubmed_pmc | CD98hc is a target for brain delivery of biotherapeutics | CD98hc is a target for brain delivery of biotherapeutics Abstract Brain exposure of systemically administered biotherapeutics is highly restricted by the blood-brain barrier (BBB). Here, we report the engineering and characterization of a BBB transport vehicle targeting the CD98 heavy chain (CD98hc or SLC3A2) of hetero... |
PMC12897505 | core_pubmed_pmc | Determination of correlation of clearance with clinical outcomes for inflammatory bowel disease | Determination of correlation of clearance with clinical outcomes for inflammatory bowel disease Abstract Abstract BACKGROUND Low drug concentrations have been linked to antidrug antibody (ADA) formation. High clearance is a major reason for low drug levels leading to treatment failure in patients with inflammatory bowe... |
PMC6482280 | core_pubmed_pmc | Reproducibility of Quantitative Systems Pharmacology Models: Current Challenges and Future Opportunities | Reproducibility of Quantitative Systems Pharmacology Models: Current Challenges and Future Opportunities Abstract The provision of model code is required for publication in CPT: Pharmacometrics & Systems Pharmacology , enabling quantitative systems pharmacology (QSP) model availability. A searchable repository of publi... |
PMC6205862 | core_pubmed_pmc | Clinical Insights for Cervical Ripening and Labor Induction Using Prostaglandins | Clinical Insights for Cervical Ripening and Labor Induction Using Prostaglandins Abstract Abstract Cervical ripening is often the first component of labor induction and is used to facilitate the softening and thinning of the cervix in preparation for labor. Common methods used for cervical ripening include both mechani... |
PMC7271599 | core_pubmed_pmc | Oral arsenic trioxide ORH-2014 pharmacokinetic and safety profile in patients with advanced hematologic disorders | Oral arsenic trioxide ORH-2014 pharmacokinetic and safety profile in patients with advanced hematologic disorders Abstract Daily intravenous arsenic trioxide administered with all-trans retinoid acid, the standard-of-care for acute promyelocytic leukemia, is costly and challenging to administer. ORH-2014 is a novel, or... |
PMC10376077 | core_pubmed_pmc | Supporting Machine Learning Model in the Treatment of Chronic Pain | Supporting Machine Learning Model in the Treatment of Chronic Pain Abstract Abstract Conventional therapy options for chronic pain are still insufficient and patients most frequently request alternative medical treatments, such as medical cannabis. Although clinical evidence supports the use of cannabis for pain, very ... |
PMC11809555 | core_pubmed_pmc | Pharmacokinetics and ADME Characterization After Oral and Intravenous Administration of [ 14 C ]‐Ziftomenib in Healthy Male Participants | Pharmacokinetics and ADME Characterization After Oral and Intravenous Administration of [ 14 C ]‐Ziftomenib in Healthy Male Participants Abstract ABSTRACT Ziftomenib, a potent, selective inhibitor that binds menin at the lysine methyltransferase 2 interaction site, has demonstrated promising clinical activity with mana... |
PMC7021090 | core_pubmed_pmc | Is there a role for tedizolid in the treatment of non-tuberculous mycobacterial disease? | Is there a role for tedizolid in the treatment of non-tuberculous mycobacterial disease? Abstract Abstract Background Pulmonary infections caused by non-tuberculous mycobacteria (NTM) are hard to treat and have low cure rates despite intensive multidrug therapy. Objectives To assess the feasibility of tedizolid, a new ... |
PMC6271099 | core_pubmed_pmc | Synthesis and Biological Evaluation of Novel 2-Methoxypyridylamino-Substituted Riminophenazine Derivatives as Antituberculosis Agents | Synthesis and Biological Evaluation of Novel 2-Methoxypyridylamino-Substituted Riminophenazine Derivatives as Antituberculosis Agents Abstract Abstract Clofazimine, a member of the riminophenazine class, is one of the few antibiotics that are still active against multidrug-resistant Mycobacterium tuberculosis ( M. tube... |
PMC6273475 | core_pubmed_pmc | Pharmacokinetic Comparison of Scutellarin and Paeoniflorin in Sham-Operated and Middle Cerebral Artery Occlusion Ischemia and Reperfusion Injury Rats after Intravenous Administration of Xin-Shao Formula | Pharmacokinetic Comparison of Scutellarin and Paeoniflorin in Sham-Operated and Middle Cerebral Artery Occlusion Ischemia and Reperfusion Injury Rats after Intravenous Administration of Xin-Shao Formula Abstract Abstract Xin-Shao formula is a folk remedy widely used in China to prevent and cure stroke. Cerebral ischemi... |
PMC4811899 | core_pubmed_pmc | Design and Testing of an EHR-Integrated, Busulfan Pharmacokinetic Decision Support Tool for the Point-of-Care Clinician | Design and Testing of an EHR-Integrated, Busulfan Pharmacokinetic Decision Support Tool for the Point-of-Care Clinician Abstract Abstract Background: Busulfan demonstrates a narrow therapeutic index for which clinicians routinely employ therapeutic drug monitoring (TDM). However, operationalizing TDM can be fraught wit... |
PMC7474498 | core_pubmed_pmc | Drug repurposing approach to fight COVID-19 | Drug repurposing approach to fight COVID-19 Abstract Currently, there are no treatment options available for the deadly contagious disease, coronavirus disease 2019 (COVID-19). Drug repurposing is a process of identifying new uses for approved or investigational drugs and it is considered as a very effective strategy f... |
PMC12889304 | core_pubmed_pmc | Study of the pharmacokinetics of Ginkgolide J in rats by ultra-high-performance liquid chromatography tandem mass spectrometry | Study of the pharmacokinetics of Ginkgolide J in rats by ultra-high-performance liquid chromatography tandem mass spectrometry Abstract Abstract Background and objective: Ginkgolide J is an active ingredient extracted from Ginkgo biloba leaves and has potential therapeutic effects on Alzheimer’s disease and rheumatoid ... |
PMC12707344 | core_pubmed_pmc | Review on the management of intra-abdominal candidiasis | Review on the management of intra-abdominal candidiasis Abstract Intra-abdominal candidiasis, which includes Candida peritonitis and Candida produced intra-abdominal abscesses, accounts for 10-30% of all intra-abdominal infections diagnosed in the intensive care units. Intra-abdominal candidiasis is associated with lon... |
PMC5125756 | core_pubmed_pmc | Synthetic high-density lipoproteins for delivery of 10-hydroxycamptothecin | Synthetic high-density lipoproteins for delivery of 10-hydroxycamptothecin Abstract Abstract The purpose of this study was to develop a novel synthetic high-density lipoprotein (sHDL) nanoparticle delivery system for 10-hydroxycamptothecin (HCPT) for treatment of colon carcinoma. HDL is recognized by scavenger receptor... |
PMC5051066 | core_pubmed_pmc | Pharmacokinetics of calycopterin and xanthmicrol, two polymethoxylated hydroxyflavones with anti-angiogenic activities from Dracocephalum kotschyi Bioss | Pharmacokinetics of calycopterin and xanthmicrol, two polymethoxylated hydroxyflavones with anti-angiogenic activities from Dracocephalum kotschyi Bioss Abstract Background Recently flavonoids have attracted the attention of researchers in the fight against cancer. Calycopterin and xanthomicrol, are two polymethoxylate... |
PMC6282494 | core_pubmed_pmc | Forecasting Clinical Dose–Response From Preclinical Studies in Tuberculosis Research: Translational Predictions With Rifampicin | Forecasting Clinical Dose–Response From Preclinical Studies in Tuberculosis Research: Translational Predictions With Rifampicin Abstract A crucial step for accelerating tuberculosis drug development is bridging the gap between preclinical and clinical trials. In this study, we developed a preclinical model‐informed tra... |
PMC11275529 | core_pubmed_pmc | Auranofin inhibition of thioredoxin reductase sensitizes lung neuroendocrine tumor cells (NETs) and small cell lung cancer (SCLC) cells to sorafenib as well as inhibiting SCLC xenograft growth | Auranofin inhibition of thioredoxin reductase sensitizes lung neuroendocrine tumor cells (NETs) and small cell lung cancer (SCLC) cells to sorafenib as well as inhibiting SCLC xenograft growth Abstract ABSTRACT Thioredoxin Reductase (TrxR) functions to recycle thioredoxin (Trx) during hydroperoxide metabolism mediated ... |
PMC7443725 | core_pubmed_pmc | Pharmacokinetic similarity demonstrated after crushing of the elbasvir/grazoprevir fixed-dose combination tablet for HCV infection | Pharmacokinetic similarity demonstrated after crushing of the elbasvir/grazoprevir fixed-dose combination tablet for HCV infection Abstract Abstract Background Finding a suitable treatment for HCV patients with swallowing disorders is still a major challenge. In practice, direct-acting antivirals are crushed without kn... |
PMC3273361 | core_pubmed_pmc | Intraperitoneal clearance as a potential biomarker of cisplatin after intraperitoneal perioperative chemotherapy: a population pharmacokinetic study | Intraperitoneal clearance as a potential biomarker of cisplatin after intraperitoneal perioperative chemotherapy: a population pharmacokinetic study Abstract Abstract Background: Intraperitoneal (IP) perioperative chemotherapy with cisplatin is an interesting option in ovarian cancer treatment. A combination of cisplat... |
PMC7586807 | core_pubmed_pmc | Oral Hypoxia‐Inducible Factor Prolyl Hydroxylase Inhibitor Roxadustat (FG‐4592) for Treatment of Anemia in Chronic Kidney Disease: A Placebo‐Controlled Study of Pharmacokinetic and Pharmacodynamic Profiles in Hemodialysis Patients | Oral Hypoxia‐Inducible Factor Prolyl Hydroxylase Inhibitor Roxadustat (FG‐4592) for Treatment of Anemia in Chronic Kidney Disease: A Placebo‐Controlled Study of Pharmacokinetic and Pharmacodynamic Profiles in Hemodialysis Patients Abstract Abstract Roxadustat (FG‐4592), an oral hypoxia‐inducible factor prolyl hydroxyla... |
PMC11731068 | core_pubmed_pmc | The potential of developing high hepatic clearance drugs via controlled release: Lessons from Kirchhoff’s Laws | The potential of developing high hepatic clearance drugs via controlled release: Lessons from Kirchhoff’s Laws Abstract When a new molecular entity is predicted to exhibit high clearance in humans, pharmaceutical sponsors almost universally search for similar acting back-up compounds that will demonstrate low clearance... |
PMC5367767 | core_pubmed_pmc | Etravirine combined with antiretrovirals other than darunavir/ritonavir for HIV-1-infected, treatment-experienced adults: Week 48 results of a phase IV trial | Etravirine combined with antiretrovirals other than darunavir/ritonavir for HIV-1-infected, treatment-experienced adults: Week 48 results of a phase IV trial Abstract Abstract Objective: VIOLIN (TMC125IFD3002; NCT01422330 ) evaluated the safety, tolerability, and pharmacokinetics of etravirine with antiretrovirals othe... |
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