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PMC6240047
core_pubmed_pmc
OCT3 promoter haplotype is associated with metformin pharmacokinetics in Koreans
OCT3 promoter haplotype is associated with metformin pharmacokinetics in Koreans Abstract Abstract Organic cation transporter 3 (OCT3) is expressed in various organs in humans and plays an important role in the transport of organic cations and drugs including metformin. In this study, we identified genetic variations o...
PMC12022901
core_pubmed_pmc
Effect of the frequently used antiepileptic drugs carbamazepine, gabapentin, and pregabalin on the pharmacokinetics of edoxaban and other oral factor xa inhibitors in healthy volunteers
Effect of the frequently used antiepileptic drugs carbamazepine, gabapentin, and pregabalin on the pharmacokinetics of edoxaban and other oral factor xa inhibitors in healthy volunteers Abstract Abstract Purpose Pregabalin, gabapentin, and carbamazepine, a potent inducer of cytochrome P450 (CYP) 3A4 and P-glycoprotein,...
PMC7065368
core_pubmed_pmc
Preclinical studies on the toxicology, pharmacokinetics and safety of K1-70 TM a human monoclonal autoantibody to the TSH receptor with TSH antagonist activity
Preclinical studies on the toxicology, pharmacokinetics and safety of K1-70 TM a human monoclonal autoantibody to the TSH receptor with TSH antagonist activity Abstract Background The human monoclonal autoantibody K1-70™ binds to the TSH receptor (TSHR) with high affinity and blocks TSHR cyclic AMP stimulation by TSH a...
PMC12402448
core_pubmed_pmc
Pharmacokinetic analysis of selective TRPV2 inhibitor SET2 in rats
Pharmacokinetic analysis of selective TRPV2 inhibitor SET2 in rats Abstract Abstract The TRPV2 channel, which regulates calcium transients, has emerged as a potential therapeutic target in various diseases, including cardiovascular injury, neurodegeneration, and cancer. However, the absence of selective inhibitors has ...
PMC5517508
core_pubmed_pmc
Global deregulation of ginseng products may be a safety hazard to warfarin takers: solid evidence of ginseng-warfarin interaction
Global deregulation of ginseng products may be a safety hazard to warfarin takers: solid evidence of ginseng-warfarin interaction Abstract Recent global deregulation of ginseng as the table food raises our concern about the possible ginseng-warfarin interaction that could be life-threatening to patients who take warfar...
PMC4402683
core_pubmed_pmc
FIBT versus florbetaben and PiB: a preclinical comparison study with amyloid-PET in transgenic mice
FIBT versus florbetaben and PiB: a preclinical comparison study with amyloid-PET in transgenic mice Abstract Abstract Background Over the last decade, an increasing number of studies have been published on the use of amyloid-β (Aβ) PET imaging with different 18 F-radiopharmaceuticals for clinical characterization of Al...
PMC8143039
core_pubmed_pmc
Identifying Biological Signatures of N-Acetylcysteine for Non-Suicidal Self-Injury in Adolescents and Young Adults
Identifying Biological Signatures of N-Acetylcysteine for Non-Suicidal Self-Injury in Adolescents and Young Adults Abstract The prevalence of non-suicidal self-injury (NSSI) is high in adolescents and young adults. However, there is a paucity of evidence-based treatments to address this clinical problem. An open-label,...
PMC12510531
core_pubmed_pmc
Evaluating the pentapharmacological potency of otamixaban against lung cancer CDK2, transferase, oxidoreductase and signalling proteins
Evaluating the pentapharmacological potency of otamixaban against lung cancer CDK2, transferase, oxidoreductase and signalling proteins Abstract Abstract Lung cancer remains the leading cause of cancer-related mortality worldwide. With approximately 2.2 million new cases and 1.8 million deaths annually, it contributes ...
PMC11062945
core_pubmed_pmc
What are the optimal pharmacokinetic/pharmacodynamic targets for β-lactamase inhibitors? A systematic review
What are the optimal pharmacokinetic/pharmacodynamic targets for β-lactamase inhibitors? A systematic review Abstract Abstract Background Pharmacokinetic/pharmacodynamic (PK/PD) indices are widely used for the selection of optimum antibiotic doses. For β-lactam antibiotics, fT >MIC , best relates antibiotic exposure to...
PMC12607281
core_pubmed_pmc
Metabolism, pharmacokinetics, and bioavailability of cannabigerol in horses following intravenous and oral administration with micellar and oil formulations
Metabolism, pharmacokinetics, and bioavailability of cannabigerol in horses following intravenous and oral administration with micellar and oil formulations Abstract Abstract Introduction Cannabigerol (CBG) is a non-psychoactive cannabinoid with growing interest in veterinary medicine; however, its pharmacokinetic prof...
PMC12629865
core_pubmed_pmc
Advances in radiopharmaceuticals for cancer radiotheranostics: CCK2R targeting as a paradigm for translational innovation
Advances in radiopharmaceuticals for cancer radiotheranostics: CCK2R targeting as a paradigm for translational innovation Abstract Abstract Radiopharmaceuticals are reshaping the landscape of cancer therapy, offering a unique theranostic advantage that is becoming increasingly central to precision medicine. By labeling...
PMC3362725
core_pubmed_pmc
An open-label, phase 1 study evaluating safety, tolerability, and pharmacokinetics of linifanib (ABT-869) in Japanese patients with solid tumors
An open-label, phase 1 study evaluating safety, tolerability, and pharmacokinetics of linifanib (ABT-869) in Japanese patients with solid tumors Abstract Purpose This phase 1 study assessed the safety, tolerability, pharmacokinetics, and preliminary antitumor activity of linifanib in Japanese patients with advanced sol...
PMC12647876
core_pubmed_pmc
Anti-CD38 monoclonal antibody CM313 for systemic lupus erythematosus: a randomized, double-blind, placebo-controlled phase Ib/IIa trial
Anti-CD38 monoclonal antibody CM313 for systemic lupus erythematosus: a randomized, double-blind, placebo-controlled phase Ib/IIa trial Abstract Abstract CD38 is highly expressed on various immune cells, including long-lived plasma cells, making it a potential therapeutic target in autoimmune diseases. This phase Ib/II...
PMC7343746
core_pubmed_pmc
(2 S , 4 R )-4-[ 18 F]Fluoroglutamine for In vivo PET Imaging of Glioma Xenografts in Mice: an Evaluation of Multiple Pharmacokinetic Models
(2 S , 4 R )-4-[ 18 F]Fluoroglutamine for In vivo PET Imaging of Glioma Xenografts in Mice: an Evaluation of Multiple Pharmacokinetic Models Abstract Purpose The glutamine analogue (2 S , 4 R )-4-[ 18 F]fluoroglutamine ([ 18 F]FGln) was investigated to further characterize its pharmacokinetics and acquire in vivo posit...
PMC5033576
core_pubmed_pmc
In Silico Oncology : Quantification of the In Vivo Antitumor Efficacy of Cisplatin-Based Doublet Therapy in Non-Small Cell Lung Cancer (NSCLC) through a Multiscale Mechanistic Model
In Silico Oncology : Quantification of the In Vivo Antitumor Efficacy of Cisplatin-Based Doublet Therapy in Non-Small Cell Lung Cancer (NSCLC) through a Multiscale Mechanistic Model Abstract The 5-year survival of non-small cell lung cancer patients can be as low as 1% in advanced stages. For patients with resectable d...
PMC3740399
core_pubmed_pmc
Carfilzomib in multiple myeloma patients with renal impairment: pharmacokinetics and safety
Carfilzomib in multiple myeloma patients with renal impairment: pharmacokinetics and safety Abstract Abstract This phase 2 study assessed the safety, pharmacokinetics, pharmacodynamics and efficacy of carfilzomib, a selective proteasome inhibitor, in patients with multiple myeloma and varying degrees of renal impairmen...
PMC6369151
core_pubmed_pmc
Cardiac Effects of a Single Dose of Pimobendan in Cats With Hypertrophic Cardiomyopathy; A Randomized, Placebo-Controlled, Crossover Study
Cardiac Effects of a Single Dose of Pimobendan in Cats With Hypertrophic Cardiomyopathy; A Randomized, Placebo-Controlled, Crossover Study Abstract Abstract Background: Pimobendan has been shown to impart a significant survival benefit in cardiomyopathic cats who receive it as part of heart failure therapy. However, us...
PMC11053426
core_pubmed_pmc
The Impact of Paediatric Obesity on Drug Pharmacokinetics: A Virtual Clinical Trials Case Study with Amlodipine
The Impact of Paediatric Obesity on Drug Pharmacokinetics: A Virtual Clinical Trials Case Study with Amlodipine Abstract Abstract The incidence of paediatric obesity continues to rise worldwide and contributes to a range of diseases including cardiovascular disease. Obesity in children has been shown to impact upon the...
PMC9328439
core_pubmed_pmc
Harmonizing and improving European education in prescribing: An overview of digital educational resources used in clinical pharmacology and therapeutics
Harmonizing and improving European education in prescribing: An overview of digital educational resources used in clinical pharmacology and therapeutics Abstract Abstract Aim Improvement and harmonization of European clinical pharmacology and therapeutics (CPT) education is urgently required. Because digital educationa...
PMC6354808
core_pubmed_pmc
A Translational Pharmacokinetic Rat Model of Cerebral Spinal Fluid and Plasma Concentrations of Cefepime
A Translational Pharmacokinetic Rat Model of Cerebral Spinal Fluid and Plasma Concentrations of Cefepime Abstract This study defines the transit of cefepime between plasma and cerebral spinal fluid (CSF) in a rat model. Male Sprague-Dawley rats received cefepime intravenously. Plasma samples were obtained via a second ...
PMC12967872
core_pubmed_pmc
Review of Existing Approaches and Potential Role of Pharmacometrics in the Interpretation of Prognostic Circulating Serum Biomarkers in Advanced NSCLC
Review of Existing Approaches and Potential Role of Pharmacometrics in the Interpretation of Prognostic Circulating Serum Biomarkers in Advanced NSCLC Abstract ABSTRACT Circulating serum biomarkers have prognostic value in patients with advanced NSCLC, yet their potential still remains underappreciated at present. This...
PMC4254862
core_pubmed_pmc
Ocular Pharmacokinetics of a Novel Loteprednol Etabonate 0.4% Ophthalmic Formulation
Ocular Pharmacokinetics of a Novel Loteprednol Etabonate 0.4% Ophthalmic Formulation Abstract Abstract Introduction Topical ophthalmic formulations of corticosteroids are commonly used to treat a variety of ocular diseases and conditions that have an inflammatory component. The purpose of this study was to evaluate the...
PMC8224043
core_pubmed_pmc
Novel Pharmacokinetic/Pharmacodynamic Parameters Quantify the Exposure–Effect Relationship of Levofloxacin against Fluoroquinolone-Resistant Escherichia coli
Novel Pharmacokinetic/Pharmacodynamic Parameters Quantify the Exposure–Effect Relationship of Levofloxacin against Fluoroquinolone-Resistant Escherichia coli Abstract Abstract Minimal inhibitory concentration-based pharmacokinetic/pharmacodynamic (PK/PD) indices are commonly applied to antibiotic dosing optimisation, b...
PMC12769998
core_pubmed_pmc
Effect of Amiodarone on Apixaban Exposure in Patients after Cardiac Surgery—A Population Pharmacokinetic Study
Effect of Amiodarone on Apixaban Exposure in Patients after Cardiac Surgery—A Population Pharmacokinetic Study Abstract Aim To investigate the effect of amiodarone on apixaban pharmacokinetics in cardiac surgery patients with postoperative atrial fibrillation. Methods Apixaban concentrations of postoperative cardiac su...
PMC8949503
core_pubmed_pmc
Radiosynthesis and Preclinical Evaluation of Bispecific PSMA/FAP Heterodimers for Tumor Imaging
Radiosynthesis and Preclinical Evaluation of Bispecific PSMA/FAP Heterodimers for Tumor Imaging Abstract Abstract Due to tumor heterogeneity and complex tumor–stromal interactions in multicellular systems, the efficiency of monospecific tracers for tumor diagnosis and therapy is currently limited. In light of the evide...
PMC7449176
core_pubmed_pmc
Safety, Pharmacokinetics, and Activity of High-Dose Ivermectin and Chloroquine against the Liver Stage of Plasmodium cynomolgi Infection in Rhesus Macaques
Safety, Pharmacokinetics, and Activity of High-Dose Ivermectin and Chloroquine against the Liver Stage of Plasmodium cynomolgi Infection in Rhesus Macaques Abstract Previously, ivermectin (1 to 10 mg/kg of body weight) was shown to inhibit the liver-stage development of Plasmodium berghei in orally dosed mice. Here, iv...
PMC6355582
core_pubmed_pmc
Population Pharmacodynamics of Amphotericin B Deoxycholate for Disseminated Infection Caused by Talaromyces marneffei
Population Pharmacodynamics of Amphotericin B Deoxycholate for Disseminated Infection Caused by Talaromyces marneffei Abstract Amphotericin B deoxycholate (DAmB) is a first-line agent for the initial treatment of talaromycosis. However, little is known about the population pharmacokinetics and pharmacodynamics of DAmB ...
PMC7672136
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling of CFTR Modulation in People with Cystic Fibrosis Transitioning from Mono or Dual Regimens to Triple-Combination Elexacaftor/Tezacaftor/Ivacaftor
Physiologically Based Pharmacokinetic Modeling of CFTR Modulation in People with Cystic Fibrosis Transitioning from Mono or Dual Regimens to Triple-Combination Elexacaftor/Tezacaftor/Ivacaftor Abstract Introduction The triple-combination (TC) cystic fibrosis transmembrane conductance regulator (CFTR) modulator regimen ...
PMC12570591
core_pubmed_pmc
Therapeutic drug monitoring of busulfan in pediatric patients: a 5-year observational study
Therapeutic drug monitoring of busulfan in pediatric patients: a 5-year observational study Abstract Abstract Background Busulfan is a chemotherapeutic agent used in conditioning regimens before hematopoietic stem cell transplantation (HSCT) in pediatric patients. Due to its pharmacokinetic variability, therapeutic dru...
PMC8424008
core_pubmed_pmc
Methylprednisolone Plasma Concentrations During Cardiac Surgery With Cardiopulmonary Bypass in Pediatric Patients
Methylprednisolone Plasma Concentrations During Cardiac Surgery With Cardiopulmonary Bypass in Pediatric Patients Abstract Introduction: To our knowledge, methylprednisolone pharmacokinetics and plasma concentrations have not been comprehensively investigated in children with congenital heart disease undergoing cardiac...
PMC4381611
core_pubmed_pmc
The small molecule tyrosine kinase inhibitor NVP-BHG712 antagonizes ABCC10-mediated paclitaxel resistance: a preclinical and pharmacokinetic study
The small molecule tyrosine kinase inhibitor NVP-BHG712 antagonizes ABCC10-mediated paclitaxel resistance: a preclinical and pharmacokinetic study Abstract Paclitaxel exhibits clinical activity against a wide variety of solid tumors. However, resistance to paclitaxel significantly attenuates the response to chemotherap...
PMC4224024
core_pubmed_pmc
Effect of honokiol on the induction of drug-metabolizing enzymes in human hepatocytes
Effect of honokiol on the induction of drug-metabolizing enzymes in human hepatocytes Abstract Honokiol, 2-(4-hydroxy-3-prop-2-enyl-phenyl)-4-prop-2-enyl-phenol, an active component of Magnolia officinalis and Magnolia grandiflora , exerts various pharmacological activities such as antitumorigenic, antioxidative, anti-...
PMC12337672
core_pubmed_pmc
Targeted protein degradation with small molecules for cancer immunotherapy
Targeted protein degradation with small molecules for cancer immunotherapy Abstract Immunotherapy has transformed cancer treatment, marked by the approval of numerous antibody-based drugs. However, the limitations of antibodies in pharmacokinetics including long half-lives, limited oral bioavailability and immunogenici...
PMC6380015
core_pubmed_pmc
Efficacy and safety of AZD7594, an inhaled non-steroidal selective glucocorticoid receptor modulator, in patients with asthma: a phase 2a randomized, double blind, placebo-controlled crossover trial
Efficacy and safety of AZD7594, an inhaled non-steroidal selective glucocorticoid receptor modulator, in patients with asthma: a phase 2a randomized, double blind, placebo-controlled crossover trial Abstract Abstract Background Inhaled corticosteroids reduce inflammation in asthma but chronic use may cause adverse effe...
PMC8467909
core_pubmed_pmc
Increased Bioavailability of β-Alanine by a Novel Controlled-Release Powder Blend Compared to a Slow-Release Tablet
Increased Bioavailability of β-Alanine by a Novel Controlled-Release Powder Blend Compared to a Slow-Release Tablet Abstract Background: β-Alanine is a sport supplement with increasing popularity due to its consistent ability to improve physical performance, with the downside of requiring several weeks of supplementati...
PMC12857578
core_pubmed_pmc
A phase I study targeting the APE1/Ref-1 redox signaling protein with APX3330: first clinical agent targeting APE1/Ref-1 in cancer
A phase I study targeting the APE1/Ref-1 redox signaling protein with APX3330: first clinical agent targeting APE1/Ref-1 in cancer Abstract Abstract Background APX3330 is an oral agent targeting the redox signaling activity of APE1/Ref-1 (Ref-1), a key regulator of transcription factors involved in inflammation and tum...
PMC9455857
core_pubmed_pmc
Design, Synthesis, Molecular Modeling and Anti-Hyperglycemic Evaluation of Quinazoline-Sulfonylurea Hybrids as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) and Sulfonylurea Receptor (SUR) Agonists
Design, Synthesis, Molecular Modeling and Anti-Hyperglycemic Evaluation of Quinazoline-Sulfonylurea Hybrids as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) and Sulfonylurea Receptor (SUR) Agonists Abstract New quinazoline-sulfonylurea hybrids were prepared and examined for their in vivo anti-hyperglycemic a...
PMC4515255
core_pubmed_pmc
Flucytosine Pharmacokinetics in a Critically Ill Patient Receiving Continuous Renal Replacement Therapy
Flucytosine Pharmacokinetics in a Critically Ill Patient Receiving Continuous Renal Replacement Therapy Abstract Purpose . A case report evaluating flucytosine dosing in a critically ill patient receiving continuous renal replacement therapy. Summary . This case report outlines an 81-year-old male who was receiving con...
PMC5564636
core_pubmed_pmc
Physiologically based pharmacokinetic modeling for predicting irinotecan exposure in human body
Physiologically based pharmacokinetic modeling for predicting irinotecan exposure in human body Abstract Colorectal cancer is the third leading cause of cancer-related deaths in the United States. Treatment of colorectal cancer remains a challenge to clinicians as well as drug developers. Irinotecan, a Camptothecin der...
PMC7924576
core_pubmed_pmc
Ivacaftor in Infants Aged 4 to <12 Months with Cystic Fibrosis and a Gating Mutation. Results of a Two-Part Phase 3 Clinical Trial
Ivacaftor in Infants Aged 4 to <12 Months with Cystic Fibrosis and a Gating Mutation. Results of a Two-Part Phase 3 Clinical Trial Abstract Rationale: We previously reported that ivacaftor was safe and well tolerated in cohorts aged 12 to <24 months with cystic fibrosis and gating mutations in the ARRIVAL study; here, ...
PMC10578491
core_pubmed_pmc
Localization of unlabeled bepirovirsen antisense oligonucleotide in murine tissues using in situ hybridization and CARS imaging
Localization of unlabeled bepirovirsen antisense oligonucleotide in murine tissues using in situ hybridization and CARS imaging Abstract Abstract Current methods for detecting unlabeled antisense oligonucleotide (ASO) drugs rely on immunohistochemistry (IHC) and/or conjugated molecules, which lack sufficient sensitivit...
PMC8651363
core_pubmed_pmc
Pharmacodynamic Evaluation of the Gexia Zhuyu Decoction in the Treatment of NAFLD and the Molecular Mechanism Underlying the TRPM4 Pathway Regulation
Pharmacodynamic Evaluation of the Gexia Zhuyu Decoction in the Treatment of NAFLD and the Molecular Mechanism Underlying the TRPM4 Pathway Regulation Abstract Abstract Nonalcoholic fatty liver disease (NAFLD) is a clinicopathological syndrome of abnormal lipid deposition in the liver mediated by nonalcohol intake. The ...
PMC12584911
core_pubmed_pmc
Therapeutic optimization against bacteria carrying metalloenzymes: the battle for class B
Therapeutic optimization against bacteria carrying metalloenzymes: the battle for class B Abstract The spread of metallo-β-lactamases (MBL)-producing Gram-negative bacilli represents a global health challenge, associated with increased mortality rates. The prevalence of MBL-producing isolates, particularly of New Delhi...
PMC10591048
core_pubmed_pmc
Excessive concentrations of kinase inhibitors in translational studies impede effective drug repurposing
Excessive concentrations of kinase inhibitors in translational studies impede effective drug repurposing Abstract Summary Drug repositioning seeks to leverage existing clinical knowledge to identify alternative clinical settings for approved drugs. However, repositioning efforts fail to demonstrate improved success rat...
PMC3573510
core_pubmed_pmc
Interactions of Rosiglitazone and Anti-Arrhythmic Drugs in Animal Model
Interactions of Rosiglitazone and Anti-Arrhythmic Drugs in Animal Model Abstract Abstract Background: Diabetes increases the risk of vascular problems by two times compared with a healthy individual, with deposition of fats in blood vessel and this includes cardiovascular disease. The treatment regimens for patients su...
PMC6966185
core_pubmed_pmc
Integrated Two‐Analyte Population Pharmacokinetic Model of Polatuzumab Vedotin in Patients With Non‐Hodgkin Lymphoma
Integrated Two‐Analyte Population Pharmacokinetic Model of Polatuzumab Vedotin in Patients With Non‐Hodgkin Lymphoma Abstract Abstract A two‐analyte integrated population pharmacokinetic (PK) model that simultaneously describes concentrations of antibody‐conjugated monomethyl auristatin E (acMMAE) and unconjugated MMAE...
PMC12148007
core_pubmed_pmc
Clozapine plasma level toxicity induced by a pharmacokinetic interaction with bupropion: A case report
Clozapine plasma level toxicity induced by a pharmacokinetic interaction with bupropion: A case report Abstract Abstract Introduction Clozapine is the gold-standard antipsychotic treatment for patients with treatment-resistant schizophrenia. Prescribers must be vigilant in ensuring that all risk evaluation mitigation s...
PMC11755617
core_pubmed_pmc
Rat as a Predictive Model for Human Clearance and Bioavailability of Monoclonal Antibodies
Rat as a Predictive Model for Human Clearance and Bioavailability of Monoclonal Antibodies Abstract Background: The prediction of human clearance (CL) and subcutaneous (SC) bioavailability is a critical aspect of monoclonal antibody (mAb) selection for clinical development. While monkeys are a well-accepted model for p...
PMC5153293
core_pubmed_pmc
Comparison of oral absorption models for pregabalin: usefulness of transit compartment model
Comparison of oral absorption models for pregabalin: usefulness of transit compartment model Abstract Abstract Pregabalin is an anticonvulsant used for the treatment of neuropathic pain and partial seizure in adults. The aim of this study was to develop a population pharmacokinetic (PK) model to describe the absorption...
PMC12375325
core_pubmed_pmc
Herb-Drug Interaction Between Sailuotong and Pitavastatin: A Systematic Pharmacokinetic Investigation and Mechanism Analysis
Herb-Drug Interaction Between Sailuotong and Pitavastatin: A Systematic Pharmacokinetic Investigation and Mechanism Analysis Abstract Propose Sailuotong (SLT), a standardized Chinese herbal preparation for vascular dementia (VaD), is frequently co-administered with pitavastatin (PIV). Potential herb-drug interactions (...
PMC4269816
core_pubmed_pmc
Use of Propranolol Blockade to Explore the Pharmacology of GSK961081, a Bi-Functional Bronchodilator, in Healthy Volunteers: Results from Two Randomized Trials
Use of Propranolol Blockade to Explore the Pharmacology of GSK961081, a Bi-Functional Bronchodilator, in Healthy Volunteers: Results from Two Randomized Trials Abstract Purpose The objective of this study was to explore the pharmacology of GSK961081, a bi-functional bronchodilator, in healthy volunteers. Methods Two ra...
PMC9139162
core_pubmed_pmc
Gene Polymorphism of Biotransformation Enzymes and Ciprofloxacin Pharmacokinetics in Pediatric Patients with Cystic Fibrosis
Gene Polymorphism of Biotransformation Enzymes and Ciprofloxacin Pharmacokinetics in Pediatric Patients with Cystic Fibrosis Abstract Abstract (1) Background: Ciprofloxacin (CPF) is widely used for the treatment of cystic fibrosis, including pediatric patients, but its pharmacokinetics is poorly studied in this populat...
PMC5975062
core_pubmed_pmc
A phase 1 study to evaluate the safety and pharmacokinetics of PQ912, a glutaminyl cyclase inhibitor, in healthy subjects
A phase 1 study to evaluate the safety and pharmacokinetics of PQ912, a glutaminyl cyclase inhibitor, in healthy subjects Abstract Introduction Pyroglutamate-amyloid-β (pE-Aβ) peptides are major components of Aβ-oligomers and Aβ-plaques, which are regarded as key culprits of Alzheimer's disease (AD) pathology. PQ912 is...
PMC11632591
core_pubmed_pmc
Kinetics of Nirogacestat-Mediated Increases in B-cell Maturation Antigen on Plasma Cells Inform Therapeutic Combinations in Multiple Myeloma
Kinetics of Nirogacestat-Mediated Increases in B-cell Maturation Antigen on Plasma Cells Inform Therapeutic Combinations in Multiple Myeloma Abstract Abstract B-cell maturation antigen (BCMA) is the target of several investigational and approved drugs for multiple myeloma. BCMA expressed on plasma cells (PC) and multip...
PMC7158220
core_pubmed_pmc
Pharmacometrics and Machine Learning Partner to Advance Clinical Data Analysis
Pharmacometrics and Machine Learning Partner to Advance Clinical Data Analysis Abstract Clinical pharmacology is a multidisciplinary data sciences field that utilizes mathematical and statistical methods to generate maximal knowledge from data. Pharmacometrics (PMX) is a well‐recognized tool to characterize disease pro...
PMC11543957
core_pubmed_pmc
Safety of Co-Crystal of Tramadol-Celecoxib (CTC) in Patients with Acute Moderate-to-Severe Pain: Pooled Analysis of Three Phase 3 Randomized Trials
Safety of Co-Crystal of Tramadol-Celecoxib (CTC) in Patients with Acute Moderate-to-Severe Pain: Pooled Analysis of Three Phase 3 Randomized Trials Abstract Introduction Multi-modal analgesia is desirable for the management of acute pain since it can provide effective pain relief at lower doses, thereby aiding tolerabi...
PMC10906815
core_pubmed_pmc
Revolutionizing pharmacokinetics: the dawn of AI-powered analysis
Revolutionizing pharmacokinetics: the dawn of AI-powered analysis Abstract This editorial explores how artificial intelligence (AI) is revolutionizing the science of pharmacokinetics (PK). It discusses the challenges of conventional PK analysis and how AI has transformed this area. It highlights the promise of artifici...
PMC9531356
core_pubmed_pmc
VHHs as tools for therapeutic protein delivery to the central nervous system
VHHs as tools for therapeutic protein delivery to the central nervous system Abstract Background The blood brain barrier (BBB) limits the therapeutic perspective for central nervous system (CNS) disorders. Previously we found an anti-mouse transferrin receptor (TfR) VHH (Nb62) that was able to deliver a biologically ac...
PMC10349191
core_pubmed_pmc
A population pharmacokinetic and pharmacokinetic‐pharmacodynamic analysis of vupanorsen from phase I and phase II studies
A population pharmacokinetic and pharmacokinetic‐pharmacodynamic analysis of vupanorsen from phase I and phase II studies Abstract Abstract Vupanorsen (PF‐07285557) is a second‐generation ligand‐conjugated 2′O‐methoxyethyl modified antisense oligonucleotide designed to target angiopoietin‐like 3 (ANGPTL3) mRNA expresse...
PMC6321357
core_pubmed_pmc
Preparation, Characterization, and Pharmacokinetic Evaluation of Imperatorin Lipid Microspheres and Their Effect on the Proliferation of MDA-MB-231 Cells
Preparation, Characterization, and Pharmacokinetic Evaluation of Imperatorin Lipid Microspheres and Their Effect on the Proliferation of MDA-MB-231 Cells Abstract Imperatorin is a chemical compound belonging to the linear furanocoumarins. Imperatorin is attracting considerable attention because of its antitumor, antiba...
PMC11883216
core_pubmed_pmc
Clinical Pharmacology of Pemafibrate Extended-release Formulation in Patients with Hypertriglyceridemia—A Phase 2, Multicenter, Active-controlled, Randomized, Single-blind, Crossover study
Clinical Pharmacology of Pemafibrate Extended-release Formulation in Patients with Hypertriglyceridemia—A Phase 2, Multicenter, Active-controlled, Randomized, Single-blind, Crossover study Abstract Abstract Aims: Efficacy, safety, and pharmacokinetics of the selective PPARα modulator pemafibrate as once-daily extended-...
PMC5828254
core_pubmed_pmc
Study of Pharmacodynamic and Pharmacokinetic Interaction of Bojungikki-Tang with Aspirin in Healthy Subjects and Ischemic Stroke Patients
Study of Pharmacodynamic and Pharmacokinetic Interaction of Bojungikki-Tang with Aspirin in Healthy Subjects and Ischemic Stroke Patients Abstract Background Bojungikki-tang (BJIKT) is a widely used traditional herbal formula in China, Japan, and Korea. There have been reports that several herbs among BJIKT have intera...
PMC7687371
core_pubmed_pmc
Quantitative in Vitro to in Vivo Extrapolation (QIVIVE) for Predicting Reduced Anogenital Distance Produced by Anti-Androgenic Pesticides in a Rodent Model for Male Reproductive Disorders
Quantitative in Vitro to in Vivo Extrapolation (QIVIVE) for Predicting Reduced Anogenital Distance Produced by Anti-Androgenic Pesticides in a Rodent Model for Male Reproductive Disorders Abstract Abstract Background: Many pesticides can antagonize the androgen receptor (AR) or inhibit androgen synthesis in vitro but t...
PMC12565175
core_pubmed_pmc
Simulation of Propofol Target-Controlled Infusion up to Time of Delivery in Cesarean Section: A Bench Study
Simulation of Propofol Target-Controlled Infusion up to Time of Delivery in Cesarean Section: A Bench Study Abstract Abstract Background/Objectives : General anesthesia is occasionally required for cesarean delivery (CD). Propofol target-controlled infusion (TCI) enables dosing based on pharmacokinetic modeling. During...
PMC11837059
core_pubmed_pmc
Navigating pharmacokinetic and pharmacodynamics challenges of β-lactam antibiotics in patients with low body weight: efficacy, toxicity, and dosage optimization
Navigating pharmacokinetic and pharmacodynamics challenges of β-lactam antibiotics in patients with low body weight: efficacy, toxicity, and dosage optimization Abstract Background: Patients with low body weight (LBW) often exhibit altered pharmacokinetics (PK) in renal clearance and total body water. These changes com...
PMC4033571
core_pubmed_pmc
Efficacy and safety of extended-release oxcarbazepine (Oxtellar XR™) as adjunctive therapy in patients with refractory partial-onset seizures: a randomized controlled trial
Efficacy and safety of extended-release oxcarbazepine (Oxtellar XR™) as adjunctive therapy in patients with refractory partial-onset seizures: a randomized controlled trial Abstract Objective To evaluate the efficacy, tolerability, and safety of once-daily 1200 mg and 2400 mg SPN-804 (Oxtellar XR™, Supernus Pharmaceuti...
PMC9982508
core_pubmed_pmc
Building clinical pharmacology laboratory capacity in low- and middle-income countries: Experience from Uganda
Building clinical pharmacology laboratory capacity in low- and middle-income countries: Experience from Uganda Abstract Background Research and clinical use of clinical pharmacology laboratories are limited in low- and middle-income countries. We describe our experience in building and sustaining laboratory capacity fo...
PMC8472798
core_pubmed_pmc
Population Pharmacokinetics of Colistin Methanesulfonate Sodium and Colistin in Critically Ill Patients: A Systematic Review
Population Pharmacokinetics of Colistin Methanesulfonate Sodium and Colistin in Critically Ill Patients: A Systematic Review Abstract Understanding the pharmacokinetics parameter of colistin methanesulfonate sodium (CMS) and colistin is needed to optimize the dosage regimen in critically ill patients. However, there is...
PMC7092991
core_pubmed_pmc
Using medical claims database to develop a population disease progression model for leuprorelin-treated subjects with hormone-sensitive prostate cancer
Using medical claims database to develop a population disease progression model for leuprorelin-treated subjects with hormone-sensitive prostate cancer Abstract Androgen deprivation therapy (ADT) is a widely used treatment for patients with hormone-sensitive prostate cancer (PCa). However, duration of treatment respons...
PMC11829860
core_pubmed_pmc
Effects of the Japanese Kampo Medicines Rikkunshito, Shakuyakukanzoto and Goreisan on Lenvatinib Plasma Concentrations in Japanese Patients with Thyroid Cancer
Effects of the Japanese Kampo Medicines Rikkunshito, Shakuyakukanzoto and Goreisan on Lenvatinib Plasma Concentrations in Japanese Patients with Thyroid Cancer Abstract Abstract Background Kampo medicines are often used in Japan as therapy for the side effects induced by oral kinase inhibitors. However, the pharmacokin...
PMC7265929
core_pubmed_pmc
A comparison of five paediatric dosing guidelines for antibiotics
A comparison of five paediatric dosing guidelines for antibiotics Abstract Abstract Objective To compare dosing guidance in the paediatric formularies of high- and middle-income countries for 32 commonly prescribed antibiotics on the World Health Organization’s (WHO’s) 2017 Model list of essential medicines for childre...
PMC9939324
core_pubmed_pmc
Predicting disruptions to drug pharmacokinetics and the risk of adverse drug reactions in non-alcoholic steatohepatitis patients
Predicting disruptions to drug pharmacokinetics and the risk of adverse drug reactions in non-alcoholic steatohepatitis patients Abstract The liver plays a central role in the pharmacokinetics of drugs through drug metabolizing enzymes and transporters. Non-alcoholic steatohepatitis (NASH) causes disease-specific alter...
PMC10140995
core_pubmed_pmc
Heterogeneity in Vaccinal Immunity to SARS-CoV-2 Can Be Addressed by a Personalized Booster Strategy
Heterogeneity in Vaccinal Immunity to SARS-CoV-2 Can Be Addressed by a Personalized Booster Strategy Abstract SARS-CoV-2 vaccinations were initially shown to substantially reduce risk of severe disease and death. However, pharmacokinetic (PK) waning and rapid viral evolution degrade neutralizing antibody (nAb) binding ...
PMC12521046
core_pubmed_pmc
Mitigating Trastuzumab‐Doxorubicin Cardiotoxicity With Multiscale Quantitative Systems Toxicology and PBPK‐Toxicodynamic Predictive Modeling Framework
Mitigating Trastuzumab‐Doxorubicin Cardiotoxicity With Multiscale Quantitative Systems Toxicology and PBPK‐Toxicodynamic Predictive Modeling Framework Abstract ABSTRACT Doxorubicin (DOX) and trastuzumab (TmAb) are widely used to treat HER2‐positive breast cancer (BC), as monotherapies and in combination (DOX + TmAb). W...
PMC12655671
core_pubmed_pmc
Repurposing Auranofin for Oncology and Beyond: A Brief Overview of Clinical Trials as Mono- and Combination Therapy
Repurposing Auranofin for Oncology and Beyond: A Brief Overview of Clinical Trials as Mono- and Combination Therapy Abstract Abstract Auranofin (AF) is an oral gold(I) compound with a well-known pharmacological profile, currently used in the treatment of some severe forms of rheumatoid arthritis. Over the last twenty y...
PMC12706072
core_pubmed_pmc
Synthesis and antidiabetic evaluation of novel Tetrahydroacridine derivatives with computational insights
Synthesis and antidiabetic evaluation of novel Tetrahydroacridine derivatives with computational insights Abstract Abstract A new series of thirty-two tetrahydroacridine (THA) derivatives were rationally designed and synthesized via efficient multistep reactions involving nucleophilic aromatic substitution and Mannich ...
PMC11420381
core_pubmed_pmc
A joint model of longitudinal pharmacokinetic and time-to-event data to study exposure–response relationships: a proof-of-concept study with alectinib
A joint model of longitudinal pharmacokinetic and time-to-event data to study exposure–response relationships: a proof-of-concept study with alectinib Abstract Abstract Purpose In exposure–response analyses of oral targeted anticancer agents, longitudinal plasma trough concentrations are often aggregated into a single ...
PMC12484239
core_pubmed_pmc
Evaluation of silvestrol as a potential therapeutic agent for pediatric COVID-19: an interpreted computational and phytochemistry approach
Evaluation of silvestrol as a potential therapeutic agent for pediatric COVID-19: an interpreted computational and phytochemistry approach Abstract Abstract Background The persistent COVID-19 disease, induced by SARS-CoV-2, sparked great questions about the safety and efficacy of the existing therapies in pediatric pat...
PMC12675823
core_pubmed_pmc
Bioequivalence Study of Tadalafil Oral Soluble Film and Tadalafil Tablet in Healthy Chinese Volunteers Under Fasting Conditions
Bioequivalence Study of Tadalafil Oral Soluble Film and Tadalafil Tablet in Healthy Chinese Volunteers Under Fasting Conditions Abstract ABSTRACT To investigate if a newly developed tadalafil oral soluble film (OSF) was bioequivalent to the approved tadalafil tablets, a clinical study was conducted in healthy Chinese m...
PMC10821504
core_pubmed_pmc
(1 E ,3 E )-1,4-Dinitro-1,3-butadiene—Synthesis, Spectral Characteristics and Computational Study Based on MEDT, ADME and PASS Simulation
(1 E ,3 E )-1,4-Dinitro-1,3-butadiene—Synthesis, Spectral Characteristics and Computational Study Based on MEDT, ADME and PASS Simulation Abstract Abstract The chemistry of conjugated nitrodienes is becoming increasingly popular. These molecules are successfully applied in cycloaddition to synthesize six-membered rings...
PMC6088248
core_pubmed_pmc
FAME‐04: A Phase 1 trial to assess the safety, acceptability, pharmacokinetics and pharmacodynamics of film and gel formulations of tenofovir
FAME‐04: A Phase 1 trial to assess the safety, acceptability, pharmacokinetics and pharmacodynamics of film and gel formulations of tenofovir Abstract Abstract Introduction Fast‐dissolving vaginal film formulations release antiretroviral drugs directly into vaginal fluid and may be as efficient at drug delivery yet mor...
PMC11359575
core_pubmed_pmc
Co-Administration of Amiodarone Increases Bleeding by Affecting Rivaroxaban Pharmacokinetics in Patients with Atrial Fibrillation
Co-Administration of Amiodarone Increases Bleeding by Affecting Rivaroxaban Pharmacokinetics in Patients with Atrial Fibrillation Abstract This study aimed to investigate the impact of the drug–drug interaction between rivaroxaban and amiodarone on the clinical outcomes in patients with non-valvular atrial fibrillation...
PMC10885983
core_pubmed_pmc
A Novel Antibiotic, Rhodomyrtone: Pharmacokinetic Studies in a Murine Model and Optimization and Validation of High-Performance Liquid Chromatographic Method for Plasma Analysis
A Novel Antibiotic, Rhodomyrtone: Pharmacokinetic Studies in a Murine Model and Optimization and Validation of High-Performance Liquid Chromatographic Method for Plasma Analysis Abstract Rhodomyrtone has indisputable and undeniable potential as a new antibiotic for antibiotic-resistant Gram-positive bacteria. Therefore...
PMC5826130
core_pubmed_pmc
Antimicrobial Activity of Ibuprofen against Cystic Fibrosis-Associated Gram-Negative Pathogens
Antimicrobial Activity of Ibuprofen against Cystic Fibrosis-Associated Gram-Negative Pathogens Abstract ABSTRACT Clinical trials have demonstrated the benefits of ibuprofen therapy in cystic fibrosis (CF) patients, an effect that is currently attributed to ibuprofen's anti-inflammatory properties. Yet, a few previous r...
PMC12746435
core_pubmed_pmc
Population Pharmacokinetic Modeling of Oxcarbazepine and Its Active Metabolite 10-Monohydroxy Derivative to Inform Dosing in Children with Obesity
Population Pharmacokinetic Modeling of Oxcarbazepine and Its Active Metabolite 10-Monohydroxy Derivative to Inform Dosing in Children with Obesity Abstract Abstract Background Oxcarbazepine (OXZ) is an antiepileptic drug whose pharmacological effect is primarily mediated by its active metabolite, 10-monohydroxy derivat...
PMC10288853
core_pubmed_pmc
A phase Ib trial of combined PKC and MEK inhibition with sotrastaurin and binimetinib in patients with metastatic uveal melanoma
A phase Ib trial of combined PKC and MEK inhibition with sotrastaurin and binimetinib in patients with metastatic uveal melanoma Abstract Abstract Background Uveal melanoma is a disease characterized by constitutive activation of the G alpha pathway and downstream signaling of protein kinase C (PKC) and the mitogen-act...
PMC12796776
core_pubmed_pmc
Bioavailability of Oral Ondansetron in Dogs: A Crossover Study
Bioavailability of Oral Ondansetron in Dogs: A Crossover Study Abstract ABSTRACT The purpose of this study was to evaluate the pharmacokinetics of oral (PO) ondansetron compared to intravenous (IV) ondansetron in eight healthy client‐owned dogs. Dogs were randomized to one of two protocols in a crossover design, receiv...
PMC9594912
core_pubmed_pmc
Development of Paeonol Liposomes: Design, Optimization, in vitro and in vivo Evaluation
Development of Paeonol Liposomes: Design, Optimization, in vitro and in vivo Evaluation Abstract Abstract Background Ulcerative colitis (UC) is one of the intractable diseases recognized by the World Health Organization, and paeonol has been proven to have therapeutic effects. However, the low solubility of paeonol lim...
PMC6901834
core_pubmed_pmc
Herbal Interaction With Chemotherapeutic Drugs—A Focus on Clinically Significant Findings
Herbal Interaction With Chemotherapeutic Drugs—A Focus on Clinically Significant Findings Abstract Abstract One of the most consequential risks associated with the concomitant use of herbal products and chemotherapeutic agents is herb-drug interactions. The risk is higher in patients with chronic conditions taking mult...
PMC11768629
core_pubmed_pmc
Potential Interaction of Pinocembrin with Drug Transporters and Hepatic Drug-Metabolizing Enzymes
Potential Interaction of Pinocembrin with Drug Transporters and Hepatic Drug-Metabolizing Enzymes Abstract Background/Objectives : Pinocembrin is a promising drug candidate for treating ischemic stroke. The interaction of pinocembrin with drug transporters and drug-metabolizing enzymes is not fully revealed. The presen...
PMC6970364
core_pubmed_pmc
Epidural administration of ropivacaine and its effects on the pharmacodynamics of rocuronium: Randomized controlled trial. Interaction between ropivacaine and rocuronium
Epidural administration of ropivacaine and its effects on the pharmacodynamics of rocuronium: Randomized controlled trial. Interaction between ropivacaine and rocuronium Abstract Abstract Background: Potentiation of neuromuscular blocking agents by local anesthetics has been described in various clinical and experiment...
PMC5686869
core_pubmed_pmc
Determination of fenticonazole in human plasma by HPLC–MS/MS and its application to pharmacokinetic studies ☆
Determination of fenticonazole in human plasma by HPLC–MS/MS and its application to pharmacokinetic studies ☆ Abstract Two simple and sensitive high performance liquid chromatography–tandem mass spectrometry (HPLC–MS/MS) methods were developed and validated for the determination of fenticonazole in human plasma after p...
PMC10672114
core_pubmed_pmc
Food Administration and Not Genetic Variants Causes Pharmacokinetic Variability of Tadalafil and Finasteride
Food Administration and Not Genetic Variants Causes Pharmacokinetic Variability of Tadalafil and Finasteride Abstract Abstract Tadalafil and finasteride are used in combination for the management of benign prostatic hyperplasia (BPH). Genetic variations in genes involved in the metabolism and transport of tadalafil or ...
PMC12558759
core_pubmed_pmc
The kinetic behavior of matrine in pig intestinal lumen after oral administration and its physiologically based pharmacokinetic modeling
The kinetic behavior of matrine in pig intestinal lumen after oral administration and its physiologically based pharmacokinetic modeling Abstract Abstract Introduction Matrine (MT) has been found to restore the susceptibility of Escherichia coli to a variety of antibiotics in vitro. Nevertheless, the absence of pharmac...
PMC6777127
core_pubmed_pmc
Deciphering the Binding Mechanism of Noscapine with Lysozyme: Biophysical and Chemoinformatic Approaches
Deciphering the Binding Mechanism of Noscapine with Lysozyme: Biophysical and Chemoinformatic Approaches Abstract Lysozyme is a well-characterized protein in terms of its structure, dynamics, and functions. It has thus emerged as a potential target to understand protein–drug interactions. The aim of our study is to gai...
PMC12884199
core_pubmed_pmc
Update of the statement on safety of cannabidiol as a novel food
Update of the statement on safety of cannabidiol as a novel food Abstract Abstract During the assessment of cannabidiol (CBD) as a novel food, in 2022 the NDA Panel identified significant data gaps. Concerns focused on potential adverse effects on the liver, gastrointestinal tract, endocrine, nervous and reproductive s...
PMC7186891
core_pubmed_pmc
Transferrin-Modified Osthole PEGylated Liposomes Travel the Blood-Brain Barrier and Mitigate Alzheimer’s Disease-Related Pathology in APP/PS-1 Mice
Transferrin-Modified Osthole PEGylated Liposomes Travel the Blood-Brain Barrier and Mitigate Alzheimer’s Disease-Related Pathology in APP/PS-1 Mice Abstract Introduction Osthole (Ost) is a coumarin compound that strengthens hippocampal neurons and neural stem cells against Aβ oligomer-induced neurotoxicity in mice, and...
PMC8398642
core_pubmed_pmc
Pharmacokinetics and Toxicity Evaluation of a PLGA and Chitosan-Based Micro-Implant for Sustained Release of Methotrexate in Rabbit Vitreous
Pharmacokinetics and Toxicity Evaluation of a PLGA and Chitosan-Based Micro-Implant for Sustained Release of Methotrexate in Rabbit Vitreous Abstract Abstract The present research investigates the pharmacokinetics and toxicity of a chitosan (CS) and poly(lactic-co-glycolic) acid (PLGA)-based methotrexate (MTX) intravit...
PMC11758625
core_pubmed_pmc
Optimizing oral 3-hydroxybutyrate dosage using pharmacokinetic model to improve cognitive function and mood in healthy subjects
Optimizing oral 3-hydroxybutyrate dosage using pharmacokinetic model to improve cognitive function and mood in healthy subjects Abstract Introduction The brain uses ketones, mainly 3-hydroxybutyrate (3-HB), as an alternative energy source. Therefore, oral intake of 3-HB may help maintain brain health. Previous studies ...
PMC12772940
core_pubmed_pmc
Bayesian-Based Pharmacokinetic Framework Integrated with Therapeutic Drug Monitoring for Assessing Adherence to Antiseizure Medications: A Clinical Trial Simulation Study
Bayesian-Based Pharmacokinetic Framework Integrated with Therapeutic Drug Monitoring for Assessing Adherence to Antiseizure Medications: A Clinical Trial Simulation Study Abstract Abstract Background Adherence to antiseizure medications (ASMs) is a cornerstone of effective epilepsy management. However, current consensu...