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PMC5544235
core_pubmed_pmc
Infection-stage adjusted dose of beta-lactams for parsimonious and efficient antibiotic treatments: A Pasteurella multocida experimental pneumonia in mice
Infection-stage adjusted dose of beta-lactams for parsimonious and efficient antibiotic treatments: A Pasteurella multocida experimental pneumonia in mice Abstract Abstract In this study, the impact of infection stage on clinically and microbiologically efficacious doses and on antibiotic consumption was assessed durin...
PMC11342789
core_pubmed_pmc
NANO-GBM trial of AGuIX nanoparticles with radiotherapy and temozolomide in the treatment of newly diagnosed Glioblastoma: Phase 1b outcomes and MRI-based biodistribution
NANO-GBM trial of AGuIX nanoparticles with radiotherapy and temozolomide in the treatment of newly diagnosed Glioblastoma: Phase 1b outcomes and MRI-based biodistribution Abstract Highlights • Phase 1b trial of the combination of intravenous AGuIX nanoparticles with RT and TMZ in GBM patients. • First-in-human phase 1b...
PMC10083270
core_pubmed_pmc
Population pharmacokinetics and model-based dosing evaluation of bedaquiline in multidrug-resistant tuberculosis patients
Population pharmacokinetics and model-based dosing evaluation of bedaquiline in multidrug-resistant tuberculosis patients Abstract Aims: Bedaquiline is now recommended to all patients in the treatment of multidrug-resistant tuberculosis (MDR-TB) using standard dosing regimens. As the ability to measure blood drug conce...
PMC8398005
core_pubmed_pmc
External Evaluation of Population Pharmacokinetic Models and Bayes-Based Dosing of Infliximab
External Evaluation of Population Pharmacokinetic Models and Bayes-Based Dosing of Infliximab Abstract Abstract Despite the well-demonstrated efficacy of infliximab in inflammatory diseases, treatment failure remains frequent. Dose adjustment using Bayesian methods has shown in silico its interest in achieving target p...
PMC4329518
core_pubmed_pmc
Influence of three coccidiostats on the pharmacokinetics of florfenicol in rabbits
Influence of three coccidiostats on the pharmacokinetics of florfenicol in rabbits Abstract Abstract In-feed Medication has been used for a long time to prevent coccidiosis, a worldwide protozoal disease in rabbits. Florfenicol (FFC) has been widely used in veterinary clinics for bacterial diseases treatment. Therefore...
PMC7786791
core_pubmed_pmc
Pharmacology-informed prediction of the risk posed to fish by mixtures of non-steroidal anti-inflammatory drugs (NSAIDs) in the environment
Pharmacology-informed prediction of the risk posed to fish by mixtures of non-steroidal anti-inflammatory drugs (NSAIDs) in the environment Abstract Highlights • The current environmental risk assessment does not include mechanistic evaluations. • We developed a pharmacology-informed framework to predict the risk of 25...
PMC4160888
core_pubmed_pmc
Pharmacogenetics of Statin-Induced Myopathy: A Focused Review of the Clinical Translation of Pharmacokinetic Genetic Variants
Pharmacogenetics of Statin-Induced Myopathy: A Focused Review of the Clinical Translation of Pharmacokinetic Genetic Variants Abstract Statins are the most commonly prescribed drugs in the United States and are extremely effective in reducing major cardiovascular events in the millions of Americans with hyperlipidemia....
PMC3726593
core_pubmed_pmc
Comparative pharmacokinetic and pharmacodynamic evaluation of branded and generic formulations of meloxicam in healthy male volunteers
Comparative pharmacokinetic and pharmacodynamic evaluation of branded and generic formulations of meloxicam in healthy male volunteers Abstract Abstract Purpose The primary aim of the present study was to assess the pharmacokinetic bioequivalence between a generic formulation of meloxicam 15 mg tablets (Meloxicam Hexal...
PMC11327957
core_pubmed_pmc
Exploring the Therapeutic Potential of High Dose Co-amoxiclav (1 gm) in Different Clinical Conditions: A Review
Exploring the Therapeutic Potential of High Dose Co-amoxiclav (1 gm) in Different Clinical Conditions: A Review Abstract Abstract Amoxicillin/clavulanate (co-amoxiclav) is a widely used antibiotic in community healthcare settings, combining amoxicillin and clavulanate potassium to combat β-lactamase-producing bacteria....
PMC5303205
core_pubmed_pmc
Comparative studies on the multi-component pharmacokinetics of Aristolochiae Fructus and honey-fried Aristolochiae Fructus extracts after oral administration in rats
Comparative studies on the multi-component pharmacokinetics of Aristolochiae Fructus and honey-fried Aristolochiae Fructus extracts after oral administration in rats Abstract Background Aristolochiae Fructus (AF) and honey-fried Aristolochiae Fructus (HAF) have been used in China for a long time as anti-tussive and exp...
PMC10326086
core_pubmed_pmc
Adavosertib (AZD1775) does not prolong the QTc interval in patients with advanced solid tumors: a phase I open-label study
Adavosertib (AZD1775) does not prolong the QTc interval in patients with advanced solid tumors: a phase I open-label study Abstract Purpose Adavosertib is a small-molecule, ATP-competitive inhibitor of Wee1 kinase. Molecularly targeted oncology agents have the potential to increase the risk of cardiovascular events, in...
PMC6451722
core_pubmed_pmc
Cardiovascular Risk Management and Hepatitis C: Combining Drugs
Cardiovascular Risk Management and Hepatitis C: Combining Drugs Abstract Direct-acting antivirals (DAAs) are known victims (substrate) and perpetrators (cause) of drug–drug interactions (DDIs). These DAAs are used for the treatment of hepatitis C virus (HCV) infections and are highly effective drugs. Drugs used for car...
PMC10828251
core_pubmed_pmc
A novel PSMA-targeting tracer with highly negatively charged linker demonstrates decreased salivary gland uptake in mice compared to [ 68 Ga]Ga-PSMA-11
A novel PSMA-targeting tracer with highly negatively charged linker demonstrates decreased salivary gland uptake in mice compared to [ 68 Ga]Ga-PSMA-11 Abstract Background The current generation of radiolabeled PSMA-targeting therapeutic agents is limited by prominent salivary gland binding, which results in dose-limit...
PMC10868414
core_pubmed_pmc
Enhancing oral bioavailability of andrographolide using solubilizing agents and bioenhancer: comparative pharmacokinetics of Andrographis paniculata formulations in beagle dogs
Enhancing oral bioavailability of andrographolide using solubilizing agents and bioenhancer: comparative pharmacokinetics of Andrographis paniculata formulations in beagle dogs Abstract Abstract Context The therapeutic potential of andrographolide is hindered by its poor oral bioavailability and unpredictable pharmacok...
PMC6448051
core_pubmed_pmc
Influence of hemodialysis on pramipexole pharmacokinetics: Lessons from two cases and literature review
Influence of hemodialysis on pramipexole pharmacokinetics: Lessons from two cases and literature review Abstract Background: Restless legs syndrome (RLS) is not a rare condition in patients on long-term dialysis. Pramipexole is a small molecule used in the treatment of idiopathic and uremic RLS. Although some informati...
PMC4428790
core_pubmed_pmc
In Silico and In Vitro Analysis of Bacoside A Aglycones and Its Derivatives as the Constituents Responsible for the Cognitive Effects of Bacopa monnieri
In Silico and In Vitro Analysis of Bacoside A Aglycones and Its Derivatives as the Constituents Responsible for the Cognitive Effects of Bacopa monnieri Abstract Bacopa monnieri has been used in Ayurvedic medicine to improve memory and cognition. The active constituent responsible for its pharmacological effects is bac...
PMC5877436
core_pubmed_pmc
A first-in-human phase I study to determine the maximum tolerated dose of the oral Src/ABL inhibitor AZD0424
A first-in-human phase I study to determine the maximum tolerated dose of the oral Src/ABL inhibitor AZD0424 Abstract Background: Src is involved in cancer invasion and metastasis. AZD0424, an oral inhibitor of Src and ABL1, has shown evidence of anti-tumour activity in pre-clinical studies. Methods: A phase Ia, dose e...
PMC4752336
core_pubmed_pmc
Developing a Physiologically-Based Pharmacokinetic Model Knowledgebase in Support of Provisional Model Construction
Developing a Physiologically-Based Pharmacokinetic Model Knowledgebase in Support of Provisional Model Construction Abstract Abstract Developing physiologically-based pharmacokinetic (PBPK) models for chemicals can be resource-intensive, as neither chemical-specific parameters nor in vivo pharmacokinetic data are easil...
PMC11813957
core_pubmed_pmc
New approach to busulfan dosing in infants and children based on a population pharmacokinetic analysis
New approach to busulfan dosing in infants and children based on a population pharmacokinetic analysis Abstract Purpose Apply population pharmacokinetic modeling to a single institution busulfan therapeutic drug monitoring (TDM) data set from infants and children to refine dosing methods. Methods One-compartment pharma...
PMC10090294
core_pubmed_pmc
Bacterial growth and ceftriaxone activity in individual ascitic fluids in an in vitro model of spontaneous bacterial peritonitis
Bacterial growth and ceftriaxone activity in individual ascitic fluids in an in vitro model of spontaneous bacterial peritonitis Abstract Abstract Introduction: The environment of the infection site affects bacterial growth and antibiotic activity. When bacterial growth and antibiotic activity are studied in body fluid...
PMC7154137
core_pubmed_pmc
Nanoformulations of Herbal Extracts in Treatment of Neurodegenerative Disorders
Nanoformulations of Herbal Extracts in Treatment of Neurodegenerative Disorders Abstract Nanotechnology is one of the methods that influenced human life in different ways and is a substantial approach that assists to overcome the multiple limitations of various diseases, particularly neurodegenerative disorders (NDs). ...
PMC5741288
core_pubmed_pmc
TRPV1 antagonist JNJ-39439335 (mavatrep) demonstrates proof of pharmacology in healthy men: a first-in-human, double-blind, placebo-controlled, randomized, sequential group study
TRPV1 antagonist JNJ-39439335 (mavatrep) demonstrates proof of pharmacology in healthy men: a first-in-human, double-blind, placebo-controlled, randomized, sequential group study Abstract JNJ-39439335 engages and antagonizes transient receptor potential vanilloid subtype 1 in a dose range that is well tolerated and hen...
PMC10018692
core_pubmed_pmc
Disulfide Bridged Nanoparticles of Thiolated Sodium Alginate and Eudragit RS100 for Oral Delivery of Paclitaxel: In Vitro and In Vivo Evaluation
Disulfide Bridged Nanoparticles of Thiolated Sodium Alginate and Eudragit RS100 for Oral Delivery of Paclitaxel: In Vitro and In Vivo Evaluation Abstract Abstract Most biopharmaceutics classification system (BCS) class IV drugs have limited oral bioavailability due to poor solubility and poorer permeability. This work ...
PMC11434802
core_pubmed_pmc
Evaluation of Population Pharmacokinetic Models of Micafungin: Implications for Dosing Regimen Optimization in Critically Ill Patients
Evaluation of Population Pharmacokinetic Models of Micafungin: Implications for Dosing Regimen Optimization in Critically Ill Patients Abstract Micafungin (MFG) is a widely used echinocandin antifungal agent for treating invasive candidiasis, particularly in critically ill patients. However, its pharmacokinetics can be...
PMC8474273
core_pubmed_pmc
Expansion Phase 1 Study of Pegargiminase Plus Pemetrexed and Cisplatin in Patients With Argininosuccinate Synthetase 1–Deficient Mesothelioma: Safety, Efficacy, and Resistance Mechanisms
Expansion Phase 1 Study of Pegargiminase Plus Pemetrexed and Cisplatin in Patients With Argininosuccinate Synthetase 1–Deficient Mesothelioma: Safety, Efficacy, and Resistance Mechanisms Abstract Introduction Pegargiminase (ADI-PEG 20; ADI) degrades arginine and potentiates pemetrexed (Pem) cytotoxicity in argininosucc...
PMC3205073
core_pubmed_pmc
A phase I trial of PR-104, a pre-prodrug of the bioreductive prodrug PR-104A, given weekly to solid tumour patients
A phase I trial of PR-104, a pre-prodrug of the bioreductive prodrug PR-104A, given weekly to solid tumour patients Abstract Abstract Background The phosphate ester PR-104 is rapidly converted in vivo to the alcohol PR-104A, a nitrogen mustard prodrug that is metabolised to hydroxylamine (PR-104H) and amine (PR-104M) D...
PMC5501099
core_pubmed_pmc
Ivermectin susceptibility and sporontocidal effect in Greater Mekong Subregion Anopheles
Ivermectin susceptibility and sporontocidal effect in Greater Mekong Subregion Anopheles Abstract Abstract Background Novel vector control methods that can directly target outdoor malaria transmission are urgently needed in the Greater Mekong Subregion (GMS) to accelerate malaria elimination and artemisinin resistance ...
PMC9848415
core_pubmed_pmc
Docetaxel prodrug and hematoporphyrin co-assembled nanoparticles for anti-tumor combination of chemotherapy and photodynamic therapy
Docetaxel prodrug and hematoporphyrin co-assembled nanoparticles for anti-tumor combination of chemotherapy and photodynamic therapy Abstract Abstract To realize the synergistic anti-tumor effect of chemotherapy and photodynamic therapy, the mono sulfide-modified docetaxel (DTX) prodrugs (DSD) provided by our laborator...
PMC3502552
core_pubmed_pmc
A dimerized urea-based inhibitor of the prostate-specific membrane antigen for 68 Ga-PET imaging of prostate cancer
A dimerized urea-based inhibitor of the prostate-specific membrane antigen for 68 Ga-PET imaging of prostate cancer Abstract Background Alternative positron-emission tomography (PET) probes like labeled inhibitors of the prostate-specific membrane antigen (PSMA) are of emerging clinical impact as they show the ability ...
PMC3013709
core_pubmed_pmc
DrugBank 3.0: a comprehensive resource for ‘Omics’ research on drugs
DrugBank 3.0: a comprehensive resource for ‘Omics’ research on drugs Abstract DrugBank ( http://www.drugbank.ca ) is a richly annotated database of drug and drug target information. It contains extensive data on the nomenclature, ontology, chemistry, structure, function, action, pharmacology, pharmacokinetics, metaboli...
PMC12439005
core_pubmed_pmc
Recommended Phase II Doses of Talquetamab in Patients With Relapsed/Refractory Multiple Myeloma From MonumenTAL‐1: Clinical Pharmacology Results
Recommended Phase II Doses of Talquetamab in Patients With Relapsed/Refractory Multiple Myeloma From MonumenTAL‐1: Clinical Pharmacology Results Abstract Abstract Talquetamab is the first and only GPRC5D × CD3 bispecific antibody approved for relapsed/refractory multiple myeloma (RRMM). In the phase I/II MonumenTAL‐1 s...
PMC12649055
core_pubmed_pmc
Clinical Pharmacology Approaches to Predict Efficacy of Monoclonal Antibodies Against Emerging SARS ‐ CoV ‐2 Variants
Clinical Pharmacology Approaches to Predict Efficacy of Monoclonal Antibodies Against Emerging SARS ‐ CoV ‐2 Variants Abstract ABSTRACT The onset of the global COVID‐19 pandemic created an urgent need for therapeutic monoclonal antibody (mAb) development, while the rapid mutation of the SARS‐CoV‐2 virus and emergence o...
PMC5402680
core_pubmed_pmc
Improving the clinical management of traumatic brain injury through the pharmacokinetic modeling of peripheral blood biomarkers
Improving the clinical management of traumatic brain injury through the pharmacokinetic modeling of peripheral blood biomarkers Abstract Background Blood biomarkers of neurovascular damage are used clinically to diagnose the presence severity or absence of neurological diseases, but data interpretation is confounded by...
PMC12566643
core_pubmed_pmc
Phage to ESKAPE: Personalizing Therapy for MDR Infections—A Comprehensive Clinical Review
Phage to ESKAPE: Personalizing Therapy for MDR Infections—A Comprehensive Clinical Review Abstract Abstract The proliferation of multidrug-resistant (MDR) ESKAPE pathogens— Enterococcus faecium , Staphylococcus aureus , Klebsiella pneumoniae , Acinetobacter baumannii , Pseudomonas aeruginosa , and Enterobacter spp.—con...
PMC3524248
core_pubmed_pmc
Safety, Tolerability, Pharmacodynamics and Pharmacokinetics of Umeclidinium and Vilanterol Alone and in Combination: A Randomized Crossover Trial
Safety, Tolerability, Pharmacodynamics and Pharmacokinetics of Umeclidinium and Vilanterol Alone and in Combination: A Randomized Crossover Trial Abstract Abstract Umeclidinium bromide (GSK573719; UMEC), a new long-acting muscarinic receptor antagonist (LAMA), is in development with vilanterol ( GW642444 ; VI), a selec...
PMC2882366
core_pubmed_pmc
Rapamycin Pharmacokinetic and Pharmacodynamic Relationships in Osteosarcoma: A Comparative Oncology Study in Dogs
Rapamycin Pharmacokinetic and Pharmacodynamic Relationships in Osteosarcoma: A Comparative Oncology Study in Dogs Abstract Background Signaling through the mTOR pathway contributes to growth, progression and chemoresistance of several cancers. Accordingly, inhibitors have been developed as potentially valuable therapeu...
PMC7217818
core_pubmed_pmc
A Population Pharmacokinetic Model Does Not Predict the Optimal Starting Dose of Tacrolimus in Pediatric Renal Transplant Recipients in a Prospective Study: Lessons Learned and Model Improvement
A Population Pharmacokinetic Model Does Not Predict the Optimal Starting Dose of Tacrolimus in Pediatric Renal Transplant Recipients in a Prospective Study: Lessons Learned and Model Improvement Abstract Background and Objective Bodyweight-based dosing of tacrolimus is considered standard care. Currently, at first stea...
PMC9402995
core_pubmed_pmc
Leveraging Predictive Pharmacometrics-Based Algorithms to Enhance Perinatal Care—Application to Neonatal Jaundice
Leveraging Predictive Pharmacometrics-Based Algorithms to Enhance Perinatal Care—Application to Neonatal Jaundice Abstract The field of medicine is undergoing a fundamental change, transforming towards a modern data-driven patient-oriented approach. This paradigm shift also affects perinatal medicine as predictive algo...
PMC5035321
core_pubmed_pmc
Preferential binding to dopamine D 3 over D 2 receptors by cariprazine in patients with schizophrenia using PET with the D 3 /D 2 receptor ligand [ 11 C]-(+)-PHNO
Preferential binding to dopamine D 3 over D 2 receptors by cariprazine in patients with schizophrenia using PET with the D 3 /D 2 receptor ligand [ 11 C]-(+)-PHNO Abstract Rationale Second-generation antipsychotics occupy dopamine D 2 receptors and act as antagonists or partial agonists at these receptors. While these ...
PMC12691601
core_pubmed_pmc
Intrapulmonary penetration and pharmacokinetics of siderophore cephalosporin HRS-8427 injection in Chinese healthy subjects
Intrapulmonary penetration and pharmacokinetics of siderophore cephalosporin HRS-8427 injection in Chinese healthy subjects Abstract ABSTRACT HRS-8427, a novel siderophore cephalosporin antibiotic, is under development for treating Gram-negative infections. This study evaluated the intrapulmonary penetration and pharma...
PMC11494894
core_pubmed_pmc
PBPK modeling of recombinant factor IX Fc fusion protein (rFIXFc) and rFIX to characterize the binding to type 4 collagen in the extravascular space
PBPK modeling of recombinant factor IX Fc fusion protein (rFIXFc) and rFIX to characterize the binding to type 4 collagen in the extravascular space Abstract Abstract Patients with severe and sometimes moderate hemophilia B are prophylactically treated with factor IX concentrates to prevent bleeding. For some time now,...
PMC9671412
core_pubmed_pmc
Childhood exposures to environmental chemicals and neurodevelopmental outcomes in congenital heart disease
Childhood exposures to environmental chemicals and neurodevelopmental outcomes in congenital heart disease Abstract Background Children with congenital heart defects have an increased risk of neurodevelopmental disability. The impact of environmental chemical exposures during daily life on neurodevelopmental outcomes i...
PMC8138292
core_pubmed_pmc
Comprehensive assessment of exposure to clozapine in association with side effects among patients with treatment-resistant schizophrenia: a population pharmacokinetic study
Comprehensive assessment of exposure to clozapine in association with side effects among patients with treatment-resistant schizophrenia: a population pharmacokinetic study Abstract Abstract Background: There have been scarce data on the distribution of clozapine concentrations in comparison with the recommended range ...
PMC10970023
core_pubmed_pmc
Drug–Drug Interactions of FXI Inhibitors: Clinical Relevance
Drug–Drug Interactions of FXI Inhibitors: Clinical Relevance Abstract Abstract Inhibitors of the factor FXI represent a new class of anticoagulant agents that are facing clinical approval for the treatment of acute coronary syndrome (ACS), venous thromboembolism (VTE), and stroke prevention of atrial fibrillation (AF)....
PMC12854056
core_pubmed_pmc
Quantifying uncertainty of tuberculosis drug susceptibility range from single-microplate test
Quantifying uncertainty of tuberculosis drug susceptibility range from single-microplate test Abstract Highlights • A numerical uncertainty range quantification from single-plate experiments. • Overcome possible overfitting with the four-parametric Hill’s function. • Processed dataset for first- and second-line antimyc...
PMC10758923
core_pubmed_pmc
Conversion of raltegravir carrying a 1,3,4-oxadiazole ring to a hydrolysis product upon pH changes decreases its antiviral activity
Conversion of raltegravir carrying a 1,3,4-oxadiazole ring to a hydrolysis product upon pH changes decreases its antiviral activity Abstract Abstract Raltegravir (RAL), a human immunodeficiency virus (HIV)-1 integrase inhibitor, has been administered as part of antiretroviral therapy. Studies in patients with HIV-1 hav...
PMC6398984
core_pubmed_pmc
Galleria mellonella as a model system to study virulence potential of mucormycetes and evaluation of antifungal treatment
Galleria mellonella as a model system to study virulence potential of mucormycetes and evaluation of antifungal treatment Abstract Abstract Mucorales can cause cutaneous to deep-seated infections, mainly in the immunocompromised host, resulting in high mortality rates due to late and inefficient treatment. In this stud...
PMC11697095
core_pubmed_pmc
Sex differences in the pharmacokinetics of anticancer drugs: a systematic review
Sex differences in the pharmacokinetics of anticancer drugs: a systematic review Abstract Abstract Background In addition to the effect of body weight, a patient’s sex can influence the pharmacokinetics (PK) of anticancer agents, and thereby their activity and safety. The magnitude and relevance of sex differences, how...
PMC9518266
core_pubmed_pmc
Strategic developments in the drug delivery of natural product dihydromyricetin: applications, prospects, and challenges
Strategic developments in the drug delivery of natural product dihydromyricetin: applications, prospects, and challenges Abstract Abstract Dihydromyricetin (DHM) is an important natural flavonoid that has attracted much attention because of its various functions such as protecting the cardiovascular system and liver, t...
PMC12706405
core_pubmed_pmc
Modeling and Simulation Identifies Endocytosis Uptake Rate and Fraction Unbound as Important Predictors of Oligonucleotide Pharmacokinetics
Modeling and Simulation Identifies Endocytosis Uptake Rate and Fraction Unbound as Important Predictors of Oligonucleotide Pharmacokinetics Abstract ABSTRACT Therapeutic oligonucleotides (TOs) represent an emerging modality, which offers a promising alternative treatment option, particularly for intracellular targets. ...
PMC6138504
core_pubmed_pmc
Relative bioavailability of bedaquiline tablets suspended in water: Implications for dosing in children
Relative bioavailability of bedaquiline tablets suspended in water: Implications for dosing in children Abstract Aims Bedaquiline is an important novel drug for treatment of multidrug‐resistant tuberculosis, but no paediatric formulation is yet available. This work aimed to explore the possibility of using the existing...
PMC8234734
core_pubmed_pmc
Pharmacokinetics and Molecular Modeling Indicate nAChRα4-Derived Peptide HAEE Goes through the Blood–Brain Barrier
Pharmacokinetics and Molecular Modeling Indicate nAChRα4-Derived Peptide HAEE Goes through the Blood–Brain Barrier Abstract One of the treatment strategies for Alzheimer’s disease (AD) is based on the use of pharmacological agents capable of binding to beta-amyloid (Aβ) and blocking its aggregation in the brain. Previo...
PMC3685454
core_pubmed_pmc
Azilsartan/chlorthalidone combination therapy for blood pressure control
Azilsartan/chlorthalidone combination therapy for blood pressure control Abstract Background Edarbyclor ® is a combined angiotensin receptor blocker (ARB) and thiazide-like diuretic (azilsartan and chlorthalidone), and was approved on December 20, 2011 by the US Food and Drug Administration (FDA) for hypertension manag...
PMC4226674
core_pubmed_pmc
A phase I trial of the HIV protease inhibitor nelfinavir in adults with solid tumors
A phase I trial of the HIV protease inhibitor nelfinavir in adults with solid tumors Abstract Nelfinavir is an HIV protease inhibitor being repurposed as an anti-cancer agent in preclinical models and in small oncology trials, yet the MTD of nelfinavir has not been determined. Therefore, we conducted a Phase Ia study t...
PMC12476844
core_pubmed_pmc
Pharmacodynamics of Vancomycin Against Coagulase‐Negative Staphylococci Bloodstream Infections
Pharmacodynamics of Vancomycin Against Coagulase‐Negative Staphylococci Bloodstream Infections Abstract ABSTRACT The recommended therapeutic target for vancomycin for serious methicillin‐resistant S. aureus infections is an area under the concentration–time curve (AUC) over 24 h to a minimum inhibitory concentration (M...
PMC12649297
core_pubmed_pmc
Recent Utilization of Pediatric Extrapolation and Modeling and Simulation Approaches in Pediatric Drug Development in Japan
Recent Utilization of Pediatric Extrapolation and Modeling and Simulation Approaches in Pediatric Drug Development in Japan Abstract Abstract In Japan, the percentage of approved drugs with pediatric indications increased to 30% in 2010‐2015, but no further increase was observed through 2020. The Ministry of Health, La...
PMC9409045
core_pubmed_pmc
Identification of Potential Cytochrome P450 3A5 Inhibitors: An Extensive Virtual Screening through Molecular Docking, Negative Image-Based Screening, Machine Learning and Molecular Dynamics Simulation Studies
Identification of Potential Cytochrome P450 3A5 Inhibitors: An Extensive Virtual Screening through Molecular Docking, Negative Image-Based Screening, Machine Learning and Molecular Dynamics Simulation Studies Abstract Cytochrome P450 3A5 (CYP3A5) is one of the crucial CYP family members and has already proven to be an ...
PMC10658504
core_pubmed_pmc
Oral cytarabine ocfosfate pharmacokinetics and assessment of leukocyte biomarkers in normal dogs
Oral cytarabine ocfosfate pharmacokinetics and assessment of leukocyte biomarkers in normal dogs Abstract Abstract Background Cytosine arabinoside (Ara‐C) is a nucleoside analog prodrug utilized for immunomodulatory effects mediated by its active metabolite Ara‐CTP. Optimal dosing protocols for immunomodulation in dogs...
PMC10005750
core_pubmed_pmc
Development of a Rapid LC-MS/MS Method for Simultaneous Quantification of Donepezil and Tadalafil in Rat Plasma: Its Application in a Pharmacokinetic Interaction Study after Oral Administration in Rats
Development of a Rapid LC-MS/MS Method for Simultaneous Quantification of Donepezil and Tadalafil in Rat Plasma: Its Application in a Pharmacokinetic Interaction Study after Oral Administration in Rats Abstract Abstract This study aimed to establish a simple and sensitive analytical method to simultaneously quantify do...
PMC7847843
core_pubmed_pmc
Population Pharmacokinetics and Dose Optimization of Ganciclovir in Critically Ill Children
Population Pharmacokinetics and Dose Optimization of Ganciclovir in Critically Ill Children Abstract Objective: The present study aims to establish a population pharmacokinetic model of ganciclovir and optimize the dosing regimen in critically ill children suffering from cytomegalovirus related disease. Methods: A tota...
PMC9016406
core_pubmed_pmc
Prescription drugs and mitochondrial metabolism
Prescription drugs and mitochondrial metabolism Abstract Abstract Mitochondria are central to the physiology and survival of nearly all eukaryotic cells and house diverse metabolic processes including oxidative phosphorylation, reactive oxygen species buffering, metabolite synthesis/exchange, and Ca 2+ sequestration. M...
PMC6804673
core_pubmed_pmc
The Effect Of Food On The Pharmacokinetic Properties And Bioequivalence Of Two Formulations Of Levocetirizine Dihydrochloride In Healthy Chinese Volunteers
The Effect Of Food On The Pharmacokinetic Properties And Bioequivalence Of Two Formulations Of Levocetirizine Dihydrochloride In Healthy Chinese Volunteers Abstract Purpose The aim of this study is to assess the bioequivalence of a new generic formulation and the branded formulation of levocetirizine dihydrochloride in...
PMC10010340
core_pubmed_pmc
The Wnt Pathway Inhibitor RXC004 Blocks Tumor Growth and Reverses Immune Evasion in Wnt Ligand–dependent Cancer Models
The Wnt Pathway Inhibitor RXC004 Blocks Tumor Growth and Reverses Immune Evasion in Wnt Ligand–dependent Cancer Models Abstract Abstract Wnt signaling is implicated in the etiology of gastrointestinal tract cancers. Targeting Wnt signaling is challenging due to on-target toxicity concerns and lack of druggable pathway ...
PMC10458111
core_pubmed_pmc
A Comparative Pharmacokinetic Study of Fexuprazan 10 mg: Demonstrating Bioequivalence with the Reference Formulation and Evaluating Steady State
A Comparative Pharmacokinetic Study of Fexuprazan 10 mg: Demonstrating Bioequivalence with the Reference Formulation and Evaluating Steady State Abstract Abstract Fexuprazan is a potassium-competitive acid blocker approved for treating gastric-acid-related diseases. Although the effectiveness of the recent formulation ...
PMC5390600
core_pubmed_pmc
A Review of Modern Control Strategies for Clinical Evaluation of Propofol Anesthesia Administration Employing Hypnosis Level Regulation
A Review of Modern Control Strategies for Clinical Evaluation of Propofol Anesthesia Administration Employing Hypnosis Level Regulation Abstract Abstract Regulating the depth of hypnosis during surgery is one of the major objectives of an anesthesia infusion system. Continuous administration of Propofol infusion during...
PMC4911353
core_pubmed_pmc
Pharmacologic Inhibition of Host Phosphodiesterase-4 Improves Isoniazid-Mediated Clearance of Mycobacterium tuberculosis
Pharmacologic Inhibition of Host Phosphodiesterase-4 Improves Isoniazid-Mediated Clearance of Mycobacterium tuberculosis Abstract The lengthy duration of multidrug therapy needed to cure tuberculosis (TB) poses significant challenges for global control of the disease. Moreover, chronic inflammation associated with TB l...
PMC9053899
core_pubmed_pmc
Estimation of median effective effect-site concentration (EC50) during target-controlled infusion of propofol for dilatation and curettage – A prospective observational study
Estimation of median effective effect-site concentration (EC50) during target-controlled infusion of propofol for dilatation and curettage – A prospective observational study Abstract Background and Aims: Propofol is the drug of choice for sedation in daycare procedures due to its pharmacokinetic properties. Propofol d...
PMC12430588
core_pubmed_pmc
Chemical Characterization, Sensory Evaluation, and Biological Activity in Neuronal Cells of Essential Oils (Rose, Eucalyptus, Lemon, and Clove) Used for Olfactory Training
Chemical Characterization, Sensory Evaluation, and Biological Activity in Neuronal Cells of Essential Oils (Rose, Eucalyptus, Lemon, and Clove) Used for Olfactory Training Abstract Abstract Essential oils (EOs) are natural mixtures of volatile compounds characterized by beneficial pharmacological effects. The repeated ...
PMC8778523
core_pubmed_pmc
Synovial and Systemic Pharmacokinetics of Florfenicol and PK/PD Integration against Streptococcus suis in Pigs
Synovial and Systemic Pharmacokinetics of Florfenicol and PK/PD Integration against Streptococcus suis in Pigs Abstract Florfenicol is a member of the phenicol group, a broad-spectrum antibacterial agent. It has been used for a long time in veterinary medicine, but there are some factors regarding its pharmacokinetic c...
PMC6479946
core_pubmed_pmc
Potential Pharmacokinetic Drug–Drug Interaction Between Harmine, a Cholinesterase Inhibitor, and Memantine, a Non-Competitive N -Methyl- d -Aspartate Receptor Antagonist
Potential Pharmacokinetic Drug–Drug Interaction Between Harmine, a Cholinesterase Inhibitor, and Memantine, a Non-Competitive N -Methyl- d -Aspartate Receptor Antagonist Abstract Harmine (HAR) is a beta-carboline alkaloid widely distributed in nature. It exhibits psychopharmacological effects of improving learning and ...
PMC9822287
core_pubmed_pmc
The Fate and Intermediary Metabolism of Soyasapogenol in the Rat
The Fate and Intermediary Metabolism of Soyasapogenol in the Rat Abstract Abstract Research suggests that soyasaponins are poorly absorbed in the GI tract and that soyasaponin aglycones or soyasapogenols are absorbed faster and in greater amounts than the corresponding soyasaponins. Therefore, it is important to unders...
PMC8605459
core_pubmed_pmc
Pharmacological blockage of the AHR-CYP1A1 axis: a call for in vivo evidence
Pharmacological blockage of the AHR-CYP1A1 axis: a call for in vivo evidence Abstract The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that can be activated by structurally diverse compounds arising from the environment and the microbiota and host metabolism. Expanding evidence has been sh...
PMC12083661
core_pubmed_pmc
Younger Age Is Associated with Favorable Outcomes in Adult Dogs with Hemangiosarcoma Receiving Adjuvant Doxorubicin Chemotherapy: Results from the PRO-DOX Study
Younger Age Is Associated with Favorable Outcomes in Adult Dogs with Hemangiosarcoma Receiving Adjuvant Doxorubicin Chemotherapy: Results from the PRO-DOX Study Abstract Abstract Background Canine hemangiosarcoma is a common and aggressive vascular malignancy predominantly affecting dogs over six years of age. Despite ...
PMC6029141
core_pubmed_pmc
Population Pharmacokinetics of Vancomycin in Chinese ICU Neonates: Initial Dosage Recommendations
Population Pharmacokinetics of Vancomycin in Chinese ICU Neonates: Initial Dosage Recommendations Abstract Abstract The main goal of our study was to characterize the population pharmacokinetics of vancomycin in critically ill Chinese neonates to develop a pharmacokinetic model and investigate factors that have signifi...
PMC10900551
core_pubmed_pmc
Pharmacokinetics and bioequivalence evaluation of two oral formulations of cotrimoxazole tablets in healthy Chinese volunteers under fasting conditions
Pharmacokinetics and bioequivalence evaluation of two oral formulations of cotrimoxazole tablets in healthy Chinese volunteers under fasting conditions Abstract Abstract This bioequivalence study was conducted to evaluate two oral formulations of cotrimoxazole tablets in healthy Chinese subjects. All 26 subjects recrui...
PMC8879439
core_pubmed_pmc
The Hitchhiker’s Guide to Human Therapeutic Nanoparticle Development
The Hitchhiker’s Guide to Human Therapeutic Nanoparticle Development Abstract Nanomedicine plays an essential role in developing new therapies through novel drug delivery systems, diagnostic and imaging systems, vaccine development, antibacterial tools, and high-throughput screening. One of the most promising drug deli...
PMC4645961
core_pubmed_pmc
Once vs. twice-daily lopinavir/ritonavir in HIV-1-infected children
Once vs. twice-daily lopinavir/ritonavir in HIV-1-infected children Abstract Objective: To evaluate whether once daily (q.d.) lopinavir/ritonavir is noninferior to twice daily (b.i.d.) dosing in children. Design: International, multicentre, phase II/III, randomized, open-label, noninferiority trial (KONCERT/PENTA18/ANR...
PMC8523120
core_pubmed_pmc
Midazolam Infusion and Disease Severity Affect the Level of Sedation in Children: A Parametric Time-to-Event Analysis
Midazolam Infusion and Disease Severity Affect the Level of Sedation in Children: A Parametric Time-to-Event Analysis Abstract Aim In critically ill mechanically ventilated children, midazolam is used first line for sedation, however its exact sedative effects have been difficult to quantify. In this analysis, we use p...
PMC11350857
core_pubmed_pmc
Loading Dose of Ceftazidime Needs to Be Increased in Critically Ill Patients: A Retrospective Study to Evaluate Recommended Loading Dose with Pharmacokinetic Modelling
Loading Dose of Ceftazidime Needs to Be Increased in Critically Ill Patients: A Retrospective Study to Evaluate Recommended Loading Dose with Pharmacokinetic Modelling Abstract Abstract To rapidly achieve ceftazidime target concentrations, a 2 g loading dose (LD) is recommended before continuous infusion, but its adequ...
PMC12439290
core_pubmed_pmc
Incorporating Multiple Imputation Into Tanezumab Dose–Response Modeling of WOMAC Pain CFB Across Six Randomized Placebo‐Controlled Phase 3 Trials
Incorporating Multiple Imputation Into Tanezumab Dose–Response Modeling of WOMAC Pain CFB Across Six Randomized Placebo‐Controlled Phase 3 Trials Abstract ABSTRACT Multiple imputation is increasingly being used to deal with missing data in clinical trials. It is a simulation approach leading to multiple analyses of a p...
PMC11099362
core_pubmed_pmc
Insulin therapy in type 2 diabetes: Insights into clinical efficacy, patient-reported outcomes, and adherence challenges
Insulin therapy in type 2 diabetes: Insights into clinical efficacy, patient-reported outcomes, and adherence challenges Abstract Insulin therapy plays a crucial role in the management of type 2 diabetes as the disease progresses. Over the past century, insulin formulations have undergone significant modifications and ...
PMC12623377
core_pubmed_pmc
The effect of Chinese medicine therapeutics on HIV/AIDS: a systematic review and network meta-analysis
The effect of Chinese medicine therapeutics on HIV/AIDS: a systematic review and network meta-analysis Abstract Background Although antiretroviral therapy (ART) effectively suppresses HIV, incomplete immune reconstitution affects 20%–30% of adherent patients. Chinese Medicine (CM) demonstrates potential as a complement...
PMC8074807
core_pubmed_pmc
Prodigiosin induced the caspase-dependent apoptosis in human chronic myelogenous leukemia K562 cell
Prodigiosin induced the caspase-dependent apoptosis in human chronic myelogenous leukemia K562 cell Abstract Abstract Background and purpose: Chronic myeloid leukemia (CML) as a myeloproliferative disease is characterized by increased cellularity of bone marrow. Implementing the latest treatment protocols is currently ...
PMC12338680
core_pubmed_pmc
Model-informed Deep Q-Networks to Guide Infliximab Dosing in Pediatric Crohn’s Disease
Model-informed Deep Q-Networks to Guide Infliximab Dosing in Pediatric Crohn’s Disease Abstract Abstract Model-informed precision dosing (MIPD) utilizes pharmacokinetic/pharmacodynamic (PK/PD) models to optimize drug therapy. However, conventional MIPD often requires manual simulation and regimen selection, which are t...
PMC4666011
core_pubmed_pmc
Pharmacokinetics of the first combination 17β-estradiol/progesterone capsule in clinical development for menopausal hormone therapy
Pharmacokinetics of the first combination 17β-estradiol/progesterone capsule in clinical development for menopausal hormone therapy Abstract Abstract Objective: This study aims to compare the pharmacokinetics and oral bioavailability of a capsule combining 17β-estradiol and progesterone in a non–peanut oil–containing f...
PMC10302384
core_pubmed_pmc
Predictions of the Biological Effects of Several Acyclic Monoterpenes as Chemical Constituents of Essential Oils Extracted from Plants
Predictions of the Biological Effects of Several Acyclic Monoterpenes as Chemical Constituents of Essential Oils Extracted from Plants Abstract Abstract Acyclic terpenes are biologically active natural products having applicability in medicine, pharmacy, cosmetics and other practices. Consequently, humans are exposed t...
PMC9127185
core_pubmed_pmc
A Pyridazinone Compound for Effectively Treating Non-alcoholic Steatohepatitis by Targeting THRβ
A Pyridazinone Compound for Effectively Treating Non-alcoholic Steatohepatitis by Targeting THRβ Abstract Developing effective therapies and medicines to conquer nonalcoholic steatohepatitis (NASH) is of great significance for public health and is faced with a major challenge. The activation of the thyroid hormone rece...
PMC10709979
core_pubmed_pmc
Pharmacokinetics of dexmedetomidine in anaesthetized horses following repeated subcutaneous administration and intravenous constant rate infusion
Pharmacokinetics of dexmedetomidine in anaesthetized horses following repeated subcutaneous administration and intravenous constant rate infusion Abstract Background The inclusion of dexmedetomidine (DEX) within a balanced general anaesthesia protocol is effective in improving the clinical outcome and recovery quality ...
PMC4654261
core_pubmed_pmc
Randomised clinical trial: safety, tolerability, pharmacokinetics and pharmacodynamics of repeated doses of TAK-438 (vonoprazan), a novel potassium-competitive acid blocker, in healthy male subjects
Randomised clinical trial: safety, tolerability, pharmacokinetics and pharmacodynamics of repeated doses of TAK-438 (vonoprazan), a novel potassium-competitive acid blocker, in healthy male subjects Abstract Background TAK-438 (vonoprazan) is a potassium-competitive acid blocker that reversibly inhibits gastric H + , K...
PMC5573760
core_pubmed_pmc
Pharmacokinetics of intravenous pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor [ 14 C]copanlisib (BAY 80-6946) in a mass balance study in healthy male volunteers
Pharmacokinetics of intravenous pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor [ 14 C]copanlisib (BAY 80-6946) in a mass balance study in healthy male volunteers Abstract Purpose To determine the pharmacokinetics of radiolabeled copanlisib (BAY 80-6946) in healthy male volunteers and to investigate the disp...
PMC2883082
core_pubmed_pmc
Comparison of plasma, venous and capillary blood levels of piperaquine in patients with uncomplicated falciparum malaria
Comparison of plasma, venous and capillary blood levels of piperaquine in patients with uncomplicated falciparum malaria Abstract Abstract Purpose Dihydroartemisinin-piperaquine (DP) is a fixed-dose artemisinin-based combination treatment. Field pharmacokinetic studies would be simplified and facilitated by being able ...
PMC9897767
core_pubmed_pmc
Assessments of CYP‑inhibition‑based drug–drug interaction between vonoprazan and poziotinib in vitro and in vivo
Assessments of CYP‑inhibition‑based drug–drug interaction between vonoprazan and poziotinib in vitro and in vivo Abstract Abstract Context Poziotinib and vonoprazan are two drugs mainly metabolized by CYP3A4. However, the drug-drug interaction between them is unknown. Objective To study the interaction mechanism and ph...
PMC12624184
core_pubmed_pmc
Early prediction of subsequent peg‐asparaginase inactivation in acute lymphoblastic leukaemia patients—A NOPHO ALL2008 study
Early prediction of subsequent peg‐asparaginase inactivation in acute lymphoblastic leukaemia patients—A NOPHO ALL2008 study Abstract Summary Polyethylene glycol (peg)‐asparaginase plays a crucial role in acute lymphoblastic leukaemia (ALL) treatment, yet its associated toxicity often leads to treatment discontinuation...
PMC11252345
core_pubmed_pmc
Thymoquinone’ potent impairment of multidrug-resistant Staphylococcus aureus NorA efflux pump activity
Thymoquinone’ potent impairment of multidrug-resistant Staphylococcus aureus NorA efflux pump activity Abstract Abstract The drug efflux pump is a crucial mechanism implicated in resistance to multiple antimicrobials. Thymoquinone (TQ) has evidently demonstrated multiple activities, antibacterial being the most effecti...
PMC4298284
core_pubmed_pmc
Characterization of hepatic enzyme activity in older adults with dementia: potential impact on personalizing pharmacotherapy
Characterization of hepatic enzyme activity in older adults with dementia: potential impact on personalizing pharmacotherapy Abstract Abstract Objective To determine the frequency of pharmacogenomic variants and concurrent medications that may alter the efficacy and tolerability of acetylcholinesterase inhibitors (AChE...
PMC6067949
core_pubmed_pmc
A First‐in‐Human Phase I Study of OPB‐111077, a Small‐Molecule STAT3 and Oxidative Phosphorylation Inhibitor, in Patients with Advanced Cancers
A First‐in‐Human Phase I Study of OPB‐111077, a Small‐Molecule STAT3 and Oxidative Phosphorylation Inhibitor, in Patients with Advanced Cancers Abstract Abstract Lessons Learned. OPB‐111077 is a novel inhibitor of STAT3 and mitochondrial oxidative phosphorylation that exhibited promising anticancer activity in preclini...
PMC6125541
core_pubmed_pmc
Bioequivalence of a Fixed-Dose Combination Tablet of the Complete Two-Drug Regimen of Dolutegravir and Rilpivirine for Treatment of HIV-1 Infection
Bioequivalence of a Fixed-Dose Combination Tablet of the Complete Two-Drug Regimen of Dolutegravir and Rilpivirine for Treatment of HIV-1 Infection Abstract A complete 2-drug regimen of dolutegravir at 50 mg and rilpivirine at 25 mg was approved to treat HIV-1 infection in virologically suppressed patients after demons...
PMC5932954
core_pubmed_pmc
Evaluation of Fluorine-18-Labeled α1(I)-N-Telopeptide Analogs as Substrate-Based Radiotracers for PET Imaging of Melanoma-Associated Lysyl Oxidase
Evaluation of Fluorine-18-Labeled α1(I)-N-Telopeptide Analogs as Substrate-Based Radiotracers for PET Imaging of Melanoma-Associated Lysyl Oxidase Abstract Abstract Accumulating evidence suggests an unequivocal role of lysyl oxidases as key players of tumor progression and metastasis, which renders this enzyme family h...
PMC12358311
core_pubmed_pmc
Shap‐Cov: An Explainable Machine Learning Based Workflow for Rapid Covariate Identification in Population Modeling
Shap‐Cov: An Explainable Machine Learning Based Workflow for Rapid Covariate Identification in Population Modeling Abstract ABSTRACT Covariate identification in population pharmacokinetic/pharmacodynamic (popPK/PD) modeling is a key component in model development that is often prone to bias, time‐consuming, and even in...
PMC12388891
core_pubmed_pmc
Melittin-Based Nanoparticles for Cancer Therapy: Mechanisms, Applications, and Future Perspectives
Melittin-Based Nanoparticles for Cancer Therapy: Mechanisms, Applications, and Future Perspectives Abstract Abstract Melittin, a cytolytic peptide derived from honeybee venom, has demonstrated potent anticancer activity through mechanisms such as membrane disruption, apoptosis induction, and modulation of key signaling...