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PMC5697187
core_pubmed_pmc
Pharmacokinetics of Mycophenolic Acid after Intravenous Administration of Mycophenolate Mofetil to Healthy Cats
Pharmacokinetics of Mycophenolic Acid after Intravenous Administration of Mycophenolate Mofetil to Healthy Cats Abstract Abstract Background Mycophenolate mofetil (MMF), the prodrug of mycophenolic acid (MPA), is becoming increasingly popular as an alternative immunosuppressant in feline medicine. Pharmacokinetic infor...
PMC11064538
core_pubmed_pmc
Use of multiple pharmacodynamic measures to deconstruct the Nix-TB regimen in a short-course murine model of tuberculosis
Use of multiple pharmacodynamic measures to deconstruct the Nix-TB regimen in a short-course murine model of tuberculosis Abstract ABSTRACT A major challenge for tuberculosis (TB) drug development is to prioritize promising combination regimens from a large and growing number of possibilities. This includes demonstrati...
PMC9435033
core_pubmed_pmc
Radiolabeled Trastuzumab Solid Lipid Nanoparticles for Breast Cancer Cell: in Vitro and in Vivo Studies
Radiolabeled Trastuzumab Solid Lipid Nanoparticles for Breast Cancer Cell: in Vitro and in Vivo Studies Abstract Abstract Radiolabeled trastuzumab (TRZ) loaded solid lipid nanoparticles (SLNs) were prepared by high shear homogenization and sonication techniques. The apoptosis mechanism of TRZ-SLNs was studied only with...
PMC8992967
core_pubmed_pmc
Ambient Temperature and External Causes of Death in Japan from 1979 to 2015: A Time-Stratified Case-Crossover Analysis
Ambient Temperature and External Causes of Death in Japan from 1979 to 2015: A Time-Stratified Case-Crossover Analysis Abstract Abstract Background: Although substantial evidence suggests that high and low temperatures are adversely associated with nonaccidental mortality, few studies have focused on exploring the risk...
PMC9311319
core_pubmed_pmc
Effect of molecular size on interstitial pharmacokinetics and tissue catabolism of antibodies
Effect of molecular size on interstitial pharmacokinetics and tissue catabolism of antibodies Abstract ABSTRACT Advances in antibody engineering have enabled the construction of novel molecular formats in diverse shapes and sizes, providing new opportunities for biologic therapies and expanding the need to understand h...
PMC3934594
core_pubmed_pmc
Nanodrugs: pharmacokinetics and safety
Nanodrugs: pharmacokinetics and safety Abstract Abstract To date, various nanodrug systems have been developed for different routes of administration, which include dendrimers, nanocrystals, emulsions, liposomes, solid lipid nanoparticles, micelles, and polymeric nanoparticles. Nanodrug systems have been employed to im...
PMC6174210
core_pubmed_pmc
Preclinical and Clinical Pharmacology of Hydrocodone for Chronic Pain: A Mini Review
Preclinical and Clinical Pharmacology of Hydrocodone for Chronic Pain: A Mini Review Abstract Hydrocodone is one of the most prescribed oral analgesic drugs and it is one of the most abused drugs in general population. It is a mu-opioid agonist predominantly metabolized to the O-demethylated product hydromorphone and t...
PMC4221688
core_pubmed_pmc
AMG 900, a potent inhibitor of aurora kinases causes pharmacodynamic changes in p-Histone H3 immunoreactivity in human tumor xenografts and proliferating mouse tissues
AMG 900, a potent inhibitor of aurora kinases causes pharmacodynamic changes in p-Histone H3 immunoreactivity in human tumor xenografts and proliferating mouse tissues Abstract Background The Aurora family of serine-threonine kinases are essential regulators of cell division in mammalian cells. Aurora-A and –B expressi...
PMC11591452
core_pubmed_pmc
Impact of Extracorporeal Membrane Oxygenation (ECMO) on Serum Concentrations of Cefepime †
Impact of Extracorporeal Membrane Oxygenation (ECMO) on Serum Concentrations of Cefepime † Abstract Abstract ECMO is becoming widely used as a life-saving measure for critically ill patients. However, there is limited data on pharmacokinetics and the dosing of beta-lactam antibiotics in ECMO. In this study, we evaluate...
PMC11798909
core_pubmed_pmc
Real‐world interpatient variability in the pharmacokinetics of levetiracetam
Real‐world interpatient variability in the pharmacokinetics of levetiracetam Abstract Abstract Background Levetiracetam (LEV) is an antiepileptic drug (AED) used to treat a variety of seizures in adult and pediatric populations. It is an ideal AED due to its favorable pharmacokinetic (PK) and pharmacodynamic profile an...
PMC4186400
core_pubmed_pmc
XG-102 administered to healthy male volunteers as a single intravenous infusion: a randomized, double-blind, placebo-controlled, dose-escalating study
XG-102 administered to healthy male volunteers as a single intravenous infusion: a randomized, double-blind, placebo-controlled, dose-escalating study Abstract Abstract The aim of the study is to evaluate the safety, tolerability and pharmacokinetics (PK) of the JNK inhibitor XG-102 in a randomized, double blind, place...
PMC3900564
core_pubmed_pmc
Heterogeneity of Tumor Vasculature and Antiangiogenic Intervention: Insights from MR Angiography and DCE-MRI
Heterogeneity of Tumor Vasculature and Antiangiogenic Intervention: Insights from MR Angiography and DCE-MRI Abstract Purpose Solid tumor vasculature is highly heterogeneous, which presents challenges to antiangiogenic intervention as well as the evaluation of its therapeutic efficacy. The aim of this study is to evalu...
PMC12473325
core_pubmed_pmc
Applications of PBPK Modeling to Estimate Drug Metabolism and Related ADME Processes in Specific Populations
Applications of PBPK Modeling to Estimate Drug Metabolism and Related ADME Processes in Specific Populations Abstract Background: Physiologically based pharmacokinetic (PBPK) models utilize computer-based simulations to predict the pharmacokinetics of drugs. By using mathematical modeling techniques consisting of diffe...
PMC3168802
core_pubmed_pmc
Evaluation of Antiangiogenic Effects of a New Synthetic Candidate Drug KR-31831 on Xenografted Ovarian Carcinoma Using Dynamic Contrast Enhanced MRI
Evaluation of Antiangiogenic Effects of a New Synthetic Candidate Drug KR-31831 on Xenografted Ovarian Carcinoma Using Dynamic Contrast Enhanced MRI Abstract Objective The purpose of this research was to investigate the anti-angiogenic inhibitory effect of KR-31831, a newly developed anti-angiogenic agent, on an in viv...
PMC11271328
core_pubmed_pmc
Evaluating the Clinical Impact and Feasibility of Therapeutic Drug Monitoring of Pazopanib in a Real-World Soft-Tissue Sarcoma Cohort
Evaluating the Clinical Impact and Feasibility of Therapeutic Drug Monitoring of Pazopanib in a Real-World Soft-Tissue Sarcoma Cohort Abstract Abstract Introduction and Objective Pazopanib is registered for metastatic renal cell carcinoma and soft-tissue sarcoma (STS). Its variable pharmacokinetic (PK) characteristics ...
PMC3910013
core_pubmed_pmc
A Multiscale Model of Interleukin-6–Mediated Immune Regulation in Crohn's Disease and Its Application in Drug Discovery and Development
A Multiscale Model of Interleukin-6–Mediated Immune Regulation in Crohn's Disease and Its Application in Drug Discovery and Development Abstract Abstract In this study, we have developed a multiscale systems model of interleukin (IL)-6–mediated immune regulation in Crohn's disease, by integrating intracellular signalin...
PMC10684410
core_pubmed_pmc
A Phase I, Open-Label, Fixed Sequence Study to Investigate the Effect of Cytochrome P450 2D6 Inhibition on the Pharmacokinetics of Ulotaront in Healthy Subjects
A Phase I, Open-Label, Fixed Sequence Study to Investigate the Effect of Cytochrome P450 2D6 Inhibition on the Pharmacokinetics of Ulotaront in Healthy Subjects Abstract Background Ulotaront is a novel psychotropic agent with agonist activity at trace amine-associated receptor 1 (TAAR1) and 5-hydroxytryptamine type 1A ...
PMC4263162
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of tiotropium solution and tiotropium powder in chronic obstructive pulmonary disease
Pharmacokinetics and pharmacodynamics of tiotropium solution and tiotropium powder in chronic obstructive pulmonary disease Abstract The aim of the study was to characterize pharmacokinetics of tiotropium solution 5 µg compared to powder 18 µg and assess dose-dependency of tiotropium solution pharmacodynamics in compar...
PMC12823312
core_pubmed_pmc
A Mechanism‐Based Multi‐Level Population PK/PD Model for Potassium‐Competitive Acid Blockers
A Mechanism‐Based Multi‐Level Population PK/PD Model for Potassium‐Competitive Acid Blockers Abstract ABSTRACT Potassium‐competitive acid blockers (PCABs) are emerging alternatives to proton pump inhibitors for the treatment of acid‐related diseases. However, due to the complex, nonlinear interaction between drug expos...
PMC12920096
core_pubmed_pmc
Discovery and development of a new oxazolidinone with reduced toxicity for the treatment of tuberculosis
Discovery and development of a new oxazolidinone with reduced toxicity for the treatment of tuberculosis Abstract Abstract Linezolid, an oxazolidinone, is a cornerstone of treatment regimens for highly drug-resistant tuberculosis but cannot be used in drug-susceptible disease because of toxicity. This toxicity results ...
PMC8925113
core_pubmed_pmc
Safety, Pharmacokinetics, and Pharmacodynamics of Oral Venglustat in Patients with Parkinson’s Disease and a GBA Mutation: Results from Part 1 of the Randomized, Double-Blinded, Placebo-Controlled MOVES-PD Trial
Safety, Pharmacokinetics, and Pharmacodynamics of Oral Venglustat in Patients with Parkinson’s Disease and a GBA Mutation: Results from Part 1 of the Randomized, Double-Blinded, Placebo-Controlled MOVES-PD Trial Abstract Abstract Background: Glucocerebrosidase gene ( GBA ) mutations influence risk and prognosis of Park...
PMC4141831
core_pubmed_pmc
Determinants of the Over-Anticoagulation Response during Warfarin Initiation Therapy in Asian Patients Based on Population Pharmacokinetic-Pharmacodynamic Analyses
Determinants of the Over-Anticoagulation Response during Warfarin Initiation Therapy in Asian Patients Based on Population Pharmacokinetic-Pharmacodynamic Analyses Abstract To clarify pharmacokinetic-pharmacodynamic (PK-PD) factors associated with the over-anticoagulation response in Asians during warfarin induction th...
PMC4809567
core_pubmed_pmc
Perioperative Use of Clevidipine: A Systematic Review and Meta-Analysis
Perioperative Use of Clevidipine: A Systematic Review and Meta-Analysis Abstract Abstract Background Clevidipine is an ultrashort-acting drug for rapid reduction of blood pressure by selectively acting on the L-type Ca2+ channels on arteriolar smooth muscle. The drug’s ultrashort action in reducing the blood pressure i...
PMC12928660
core_pubmed_pmc
Development and validation of a method for quantitation of CTx-1 for the assessment of biosimilarity of FKS518, a denosumab biosimilar
Development and validation of a method for quantitation of CTx-1 for the assessment of biosimilarity of FKS518, a denosumab biosimilar Abstract ABSTRACT Fresenius Kabi has developed FKS518, a fully human monoclonal antibody biosimilar to denosumab. The clinical development program included two randomized comparative tr...
PMC6995987
core_pubmed_pmc
Population Pharmacokinetic Analysis of Fluticasone Furoate/Umeclidinium Bromide/Vilanterol in Patients with Chronic Obstructive Pulmonary Disease
Population Pharmacokinetic Analysis of Fluticasone Furoate/Umeclidinium Bromide/Vilanterol in Patients with Chronic Obstructive Pulmonary Disease Abstract Background Population pharmacokinetic methods were used to characterize the pharmacokinetics of fluticasone furoate (FF), umeclidinium (UMEC), and vilanterol (VI) in...
PMC4607679
core_pubmed_pmc
Intestinal Absorption of Ergostane and Lanostane Triterpenoids from Antrodia cinnamomea Using Caco-2 Cell Monolayer Model
Intestinal Absorption of Ergostane and Lanostane Triterpenoids from Antrodia cinnamomea Using Caco-2 Cell Monolayer Model Abstract Abstract Antrodia cinnamomea is a precious medicinal mushroom. It exhibits promising therapeutic effects on cancer, intoxication, hypertension, hepatitis, and inflammation. Its major bioact...
PMC8687347
core_pubmed_pmc
System‐based strategies for p53 recovery
System‐based strategies for p53 recovery Abstract Abstract The authors have proposed a systems theory‐based novel drug design approach for the p53 pathway. The pathway is taken as a dynamic system represented by ordinary differential equations‐based mathematical model. Using control engineering practices, the system an...
PMC7565829
core_pubmed_pmc
Treatment of COVID-19 Patients Post-Bariatric Surgery: Issues for Consideration
Treatment of COVID-19 Patients Post-Bariatric Surgery: Issues for Consideration Abstract Abstract As COVID-19 has been expanding rapidly around the world, the types of patients and their backgrounds vary. The substantially altered GI anatomy/physiology after bariatric surgery presents new challenges to the field of ora...
PMC7092583
core_pubmed_pmc
Phase-I trial of survivin inhibition with EZN-3042 in dogs with spontaneous lymphoma
Phase-I trial of survivin inhibition with EZN-3042 in dogs with spontaneous lymphoma Abstract Background Lymphoma is a common cancer in dogs. While most dogs receiving chemotherapy experience remission, very few are cured, and median survival times are generally in the 12-month range. Novel approaches to treatment are ...
PMC12066549
core_pubmed_pmc
Untargeted metabolic analysis in serum samples reveals metabolic signature in children with congenital heart failure on enalapril therapy
Untargeted metabolic analysis in serum samples reveals metabolic signature in children with congenital heart failure on enalapril therapy Abstract Introduction Enalapril is an angiotensin-converting enzyme (ACE) inhibitor (ACEi) which is widely used in the management of (paediatric) hypertension and heart failure (HF)....
PMC10941504
core_pubmed_pmc
Nivolumab and ipilimumab population pharmacokinetics in support of pediatric dose recommendations—Going beyond the body‐size effect
Nivolumab and ipilimumab population pharmacokinetics in support of pediatric dose recommendations—Going beyond the body‐size effect Abstract Abstract Body size has historically been considered the primary source of difference in the pharmacokinetics (PKs) of monoclonal antibodies (mAbs) between children aged greater th...
PMC5593165
core_pubmed_pmc
Comparison of a New Intranasal Naloxone Formulation to Intramuscular Naloxone: Results from Hypothesis‐generating Small Clinical Studies
Comparison of a New Intranasal Naloxone Formulation to Intramuscular Naloxone: Results from Hypothesis‐generating Small Clinical Studies Abstract Abstract Easy‐to‐use naloxone formulations are needed to help address the opioid overdose epidemic. The pharmacokinetics of i.v., i.m., and a new i.n. naloxone formulation (2...
PMC7176675
core_pubmed_pmc
Possibility of cancer-stem-cell-targeted radioimmunotherapy for acute myelogenous leukemia using 211 At-CXCR4 monoclonal antibody
Possibility of cancer-stem-cell-targeted radioimmunotherapy for acute myelogenous leukemia using 211 At-CXCR4 monoclonal antibody Abstract To explore stem-cell-targeted radioimmunotherapy with α-particles in acute myelogenous leukemia (AML), pharmacokinetics and dosimetry of the 211 At-labeled anti-C-X-C chemokine rece...
PMC12394284
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Firsekibart, an Anti-interleukin-1β Monoclonal Antibody, in Healthy Chinese Participants: A Randomized, Double-Blind, Placebo-Controlled Phase 1 Study
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Firsekibart, an Anti-interleukin-1β Monoclonal Antibody, in Healthy Chinese Participants: A Randomized, Double-Blind, Placebo-Controlled Phase 1 Study Abstract Introduction The pro-inflammatory cytokine interleukin-1β (IL-1β) is an important therapeutic ta...
PMC6676638
core_pubmed_pmc
PK/PD modeling of Ceftiofur Sodium against Haemophilus parasuis infection in pigs
PK/PD modeling of Ceftiofur Sodium against Haemophilus parasuis infection in pigs Abstract Abstract Background Ceftiofur Sodium is widely used in China. Our aim was to determine Ceftiofur Sodium activity and optimize dosing regimens against the pathogen Haemophilus parasuis using an in vitro and ex vivo pharmacokinetic...
PMC11949125
core_pubmed_pmc
CYP3A Genotype Is Associated With Variability in the Exposure and Clearance of the Novel Oncogenic Transcription Inhibitor Lurbinectedin
CYP3A Genotype Is Associated With Variability in the Exposure and Clearance of the Novel Oncogenic Transcription Inhibitor Lurbinectedin Abstract ABSTRACT Lurbinectedin is an oncogenic transcription inhibitor indicated for the treatment of small cell lung cancer (SCLC), which has also shown activity against other malig...
PMC5833160
core_pubmed_pmc
Development of Molecularly Targeted Agents and Immunotherapies in Glioblastoma: A Personalized Approach
Development of Molecularly Targeted Agents and Immunotherapies in Glioblastoma: A Personalized Approach Abstract Over the past decade, precision cancer medicine has driven major advances in the management of advanced solid tumours with the identification and targeting of putative driver aberrations transforming the cli...
PMC10810935
core_pubmed_pmc
Cubosomal functionalized block copolymer platform for dual delivery of linagliptin and empagliflozin: Recent advances in synergistic strategies for maximizing control of high-risk type II diabetes
Cubosomal functionalized block copolymer platform for dual delivery of linagliptin and empagliflozin: Recent advances in synergistic strategies for maximizing control of high-risk type II diabetes Abstract Abstract A well-made chitosan-PVP block copolymer platform was equipped with highly ordered and uniform nano-chann...
PMC3715401
core_pubmed_pmc
Improving Pharmacokinetic-Pharmacodynamic Modeling to Investigate Anti-Infective Chemotherapy with Application to the Current Generation of Antimalarial Drugs
Improving Pharmacokinetic-Pharmacodynamic Modeling to Investigate Anti-Infective Chemotherapy with Application to the Current Generation of Antimalarial Drugs Abstract Abstract Mechanism-based pharmacokinetic-pharmacodynamic (PK/PD) modelling is the standard computational technique for simulating drug treatment of infe...
PMC6847989
core_pubmed_pmc
In Situ Forming Injectable Hydrogel For Encapsulation Of Nanoiguratimod And Sustained Release Of Therapeutics
In Situ Forming Injectable Hydrogel For Encapsulation Of Nanoiguratimod And Sustained Release Of Therapeutics Abstract Background Iguratimod (IGUR) is a novel disease-modifying antirheumatic drug used for treating rheumatoid arthritis (RA). To improve its bioavailability and to alleviate gastrointestinal side effects, ...
PMC10823124
core_pubmed_pmc
Pharmacokinetics of intravenously and trans-dermally administered fluralaner in healthy laying shaver hens: fluralaner in chickens
Pharmacokinetics of intravenously and trans-dermally administered fluralaner in healthy laying shaver hens: fluralaner in chickens Abstract Abstract Ectoparasite infestations negatively affect both backyard and commercial chicken flocks in the United States. Fluralaner is an isoxazoline shown to be efficacious in treat...
PMC10951218
core_pubmed_pmc
Antiemetic activity of abietic acid possibly through the 5HT 3 and muscarinic receptors interaction pathways
Antiemetic activity of abietic acid possibly through the 5HT 3 and muscarinic receptors interaction pathways Abstract Abstract The present study was designed to evaluate the antiemetic activity of abietic acid (AA) using in vivo and in silico studies. To assess the effect, doses of 50 mg/kg b.w. copper sulfate (CuSO 4 ...
PMC4021528
core_pubmed_pmc
Pharmacokinetically guided sunitinib dosing: a feasibility study in patients with advanced solid tumours
Pharmacokinetically guided sunitinib dosing: a feasibility study in patients with advanced solid tumours Abstract Background: Plasma exposure of sunitinib shows large inter-individual variation. Therefore, a pharmacokinetic (PK) study was performed to determine safety and feasibility of sunitinib dosing based on PK lev...
PMC6146203
core_pubmed_pmc
Vortioxetine Differentially Modulates MK-801-Induced Changes in Visual Signal Detection Task Performance and Locomotor Activity
Vortioxetine Differentially Modulates MK-801-Induced Changes in Visual Signal Detection Task Performance and Locomotor Activity Abstract Attention impairment is a common feature of Major Depressive Disorder (MDD), and MDD-associated cognitive dysfunction may play an important role in determining functional status among...
PMC9557078
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic integration of tilmicosin against Mycoplasma gallisepticum in the target infection site in chickens
Pharmacokinetic and Pharmacodynamic integration of tilmicosin against Mycoplasma gallisepticum in the target infection site in chickens Abstract Abstract Mycoplasma gallisepticum ( M. gallisepticum ) is a primary respiratory pathogen of poultry and causes significant economic losses to the poultry industry. There were ...
PMC11044790
core_pubmed_pmc
Abemaciclib pharmacology and interactions in the treatment of HR+/HER2− breast cancer: a critical review
Abemaciclib pharmacology and interactions in the treatment of HR+/HER2− breast cancer: a critical review Abstract Abstract Abemaciclib (ABE) in combination with endocrine therapy represents the mainstay treatment for either endocrine-resistant metastatic or high-risk early-stage HR+/HER2− breast cancer patients. Hence,...
PMC6296114
core_pubmed_pmc
Tigecycline in critically ill patients on continuous renal replacement therapy: a population pharmacokinetic study
Tigecycline in critically ill patients on continuous renal replacement therapy: a population pharmacokinetic study Abstract Abstract Background Tigecycline is a vital antibiotic treatment option for infections caused by multiresistant bacteria in the intensive care unit (ICU). Acute kidney injury (AKI) is a common comp...
PMC6308823
core_pubmed_pmc
Vancomycin Removal During High-Volume Peritoneal Dialysis in Acute Kidney Injury Patients: A Prospective Cohort Clinical Study
Vancomycin Removal During High-Volume Peritoneal Dialysis in Acute Kidney Injury Patients: A Prospective Cohort Clinical Study Abstract Introduction Vancomycin pharmacokinetic data in patients with acute kidney injury (AKI) on high-volume peritoneal dialysis (HVPD) are lacking. The aims were to study the pharmacokineti...
PMC7849190
core_pubmed_pmc
Multispecies Evaluation of a Long-Acting Tenofovir Alafenamide Subdermal Implant for HIV Prophylaxis
Multispecies Evaluation of a Long-Acting Tenofovir Alafenamide Subdermal Implant for HIV Prophylaxis Abstract New HIV-1 infection rates far outpace the targets set by global health organizations, despite important progress in curbing the progression of the epidemic. Long-acting (LA) formulations delivering antiretrovir...
PMC12648365
core_pubmed_pmc
Effect of vepdegestrant, a PROTAC oestrogen receptor degrader, on dabigatran and rosuvastatin pharmacokinetics in healthy participants
Effect of vepdegestrant, a PROTAC oestrogen receptor degrader, on dabigatran and rosuvastatin pharmacokinetics in healthy participants Abstract Abstract Aims To evaluate the effects of vepdegestrant, a PROteolysis TArgeting Chimera (PROTAC) oestrogen receptor degrader, on the pharmacokinetics of dabigatran (a P‐glycopr...
PMC12896392
core_pubmed_pmc
Model‐Based Meta‐Analysis With MonolixSuite: A Tutorial for Longitudinal Categorical and Continuous Data
Model‐Based Meta‐Analysis With MonolixSuite: A Tutorial for Longitudinal Categorical and Continuous Data Abstract ABSTRACT Model‐based meta‐analysis (MBMA) informs key drug development decisions by integrating data, published or unpublished, from multiple studies. Due to these various sources of information and the use...
PMC8642003
core_pubmed_pmc
Effect of Sijunzi Pills on Pharmacokinetics of Omeprazole in Beagle Dogs by HPLC-UV: A Herb-Drug Interaction Study
Effect of Sijunzi Pills on Pharmacokinetics of Omeprazole in Beagle Dogs by HPLC-UV: A Herb-Drug Interaction Study Abstract A sensitive high-performance liquid chromatography (HPLC-UV) method for determination of omeprazole in beagle dog plasma was developed and to investigate the effect of Sijunzi pills (SJZPs) on the...
PMC4303958
core_pubmed_pmc
Population Pharmacokinetics of Ceftolozane/Tazobactam in Healthy Volunteers, Subjects With Varying Degrees of Renal Function and Patients With Bacterial Infections
Population Pharmacokinetics of Ceftolozane/Tazobactam in Healthy Volunteers, Subjects With Varying Degrees of Renal Function and Patients With Bacterial Infections Abstract Ceftolozane/tazobactam is a novel antipseudomonal cephalosporin and β-lactamase inhibitor in clinical development for treatment of complicated urin...
PMC4538270
core_pubmed_pmc
Systemic exposure to menthol following administration of peppermint oil to paediatric patients
Systemic exposure to menthol following administration of peppermint oil to paediatric patients Abstract Abstract Objective Peppermint oil (PMO) has been used to treat abdominal ailments dating to ancient Egypt, Greece and Rome. Despite its increasing paediatric use, as in irritable bowel syndrome (IBS) treatment, the p...
PMC4419161
core_pubmed_pmc
The effect of food on the pharmacokinetics of oral ibrutinib in healthy participants and patients with chronic lymphocytic leukemia
The effect of food on the pharmacokinetics of oral ibrutinib in healthy participants and patients with chronic lymphocytic leukemia Abstract Abstract Purpose To assess ibrutinib pharmacokinetics under fasted and fed conditions, impact of food-intake timing, and the safety and tolerability. Methods Three studies were an...
PMC5351001
core_pubmed_pmc
Translational Pharmacokinetic/Pharmacodynamic Analysis of MYO‐029 Antibody for Muscular Dystrophy
Translational Pharmacokinetic/Pharmacodynamic Analysis of MYO‐029 Antibody for Muscular Dystrophy Abstract Abstract Suppression of the myostatin (GDF‐8) pathway has emerged as an important therapeutic paradigm for muscle‐wasting disorders. In this study, we conducted a translational pharmacokinetic/pharmacodynamic (PK/...
PMC11862789
core_pubmed_pmc
L‐carnitine for valproic acid‐induced toxicity
L‐carnitine for valproic acid‐induced toxicity Abstract Aims Review the effectiveness and dosing of L‐carnitine for valproic‐acid induced toxicity. Methods A literature review of the pharmacokinetics and clinical use of L‐carnitine was performed. Results Valproic acid is a fatty acid used for numerous therapeutic indic...
PMC3903492
core_pubmed_pmc
Schisandra chinensis Peptidoglycan-Assisted Transmembrane Transport of Lignans Uniquely Altered the Pharmacokinetic and Pharmacodynamic Mechanisms in Human HepG2 Cell Model
Schisandra chinensis Peptidoglycan-Assisted Transmembrane Transport of Lignans Uniquely Altered the Pharmacokinetic and Pharmacodynamic Mechanisms in Human HepG2 Cell Model Abstract Abstract Schisandra chinensis (Turz Baill) ( S. chinensis ) (SC) fruit is a hepatoprotective herb containing many lignans and a large amou...
PMC8403308
core_pubmed_pmc
MEDI6012: Recombinant Human Lecithin Cholesterol Acyltransferase, High‐Density Lipoprotein, and Low‐Density Lipoprotein Receptor–Mediated Reverse Cholesterol Transport
MEDI6012: Recombinant Human Lecithin Cholesterol Acyltransferase, High‐Density Lipoprotein, and Low‐Density Lipoprotein Receptor–Mediated Reverse Cholesterol Transport Abstract Abstract Background MEDI6012 is recombinant human lecithin cholesterol acyltransferase, the rate‐limiting enzyme in reverse cholesterol transpo...
PMC4846779
core_pubmed_pmc
Dose Optimization of Efavirenz Based on Individual CYP2B6 Polymorphisms in Chinese Patients Positive for HIV
Dose Optimization of Efavirenz Based on Individual CYP2B6 Polymorphisms in Chinese Patients Positive for HIV Abstract Abstract The purpose of this study was to investigate the impact of CYP2B6‐G516T polymorphisms on the pharmacokinetics (PKs) of efavirenz among the Chinese population and to propose doses for different ...
PMC10149080
core_pubmed_pmc
In silico Prediction of Malvaviscus arboreus Metabolites and Green Synthesis of Silver Nanoparticles – Opportunities for Safer Anti-Bacterial and Anti-Cancer Precision Medicine
In silico Prediction of Malvaviscus arboreus Metabolites and Green Synthesis of Silver Nanoparticles – Opportunities for Safer Anti-Bacterial and Anti-Cancer Precision Medicine Abstract Introduction Biogenic silver nanoparticles (AgNPs) may be a feasible therapeutic option in the research and development towards select...
PMC5440587
core_pubmed_pmc
Clinical Efficacy and Residue Depletion of 10% Enrofloxacin Enteric-Coated Granules in Pigs
Clinical Efficacy and Residue Depletion of 10% Enrofloxacin Enteric-Coated Granules in Pigs Abstract A new, more palatable formulation of 10% enrofloxacin enteric-coated granules was investigated to evaluate the pharmacokinetic effect in plasma, the residue elimination in tissues and the clinical efficacy against Actin...
PMC5291330
core_pubmed_pmc
Docetaxel-loaded PLGA and PLGA-PEG nanoparticles for intravenous application: pharmacokinetics and biodistribution profile
Docetaxel-loaded PLGA and PLGA-PEG nanoparticles for intravenous application: pharmacokinetics and biodistribution profile Abstract Docetaxel is a highly potent anticancer agent being used in a wide spectrum of cancer types. There are important matters of concern regarding the drug’s pharmacokinetics related to the con...
PMC7227120
core_pubmed_pmc
Caffeine preserves quiet sleep in preterm neonates
Caffeine preserves quiet sleep in preterm neonates Abstract Abstract Caffeine is widely used in preterm neonates suffering from apnea of prematurity (AOP), and it has become one of the most frequently prescribed medications in neonatal intensive care units. Goal of this study is to investigate how caffeine citrate trea...
PMC10663723
core_pubmed_pmc
In vitro anticancer evaluation of Enceleamycin A and its underlying mechanism †
In vitro anticancer evaluation of Enceleamycin A and its underlying mechanism † Abstract It has become more crucial than ever to find novel anticancer compounds due to the rise in cancer mortality and resistance to the present chemotherapeutic drugs. Naphthoquinones are regarded as privileged structures for their abili...
PMC7473964
core_pubmed_pmc
Application of Pharmacokinetic-Pharmacodynamic Modeling to Inform Translation of In Vitro NaV1.7 Inhibition to In Vivo Pharmacological Response in Non-human Primate
Application of Pharmacokinetic-Pharmacodynamic Modeling to Inform Translation of In Vitro NaV1.7 Inhibition to In Vivo Pharmacological Response in Non-human Primate Abstract Abstract Purpose This work describes a staged approach to the application of pharmacokinetic-pharmacodynamic (PK-PD) modeling in the voltage-gated...
PMC10845918
core_pubmed_pmc
Structure-activity relationship and target investigation of 2-aryl quinolines with nematocidal activity
Structure-activity relationship and target investigation of 2-aryl quinolines with nematocidal activity Abstract Within the context of our anthelmintic discovery program, we recently identified and evaluated a quinoline derivative, called ABX464 or obefazimod, as a nematocidal candidate; synthesised a series of analogu...
PMC7054374
core_pubmed_pmc
An exploratory, randomised, placebo-controlled, 14 day trial of the soluble guanylate cyclase stimulator praliciguat in participants with type 2 diabetes and hypertension
An exploratory, randomised, placebo-controlled, 14 day trial of the soluble guanylate cyclase stimulator praliciguat in participants with type 2 diabetes and hypertension Abstract Abstract Aims/hypothesis Praliciguat (IW-1973), a soluble guanylate cyclase stimulator, amplifies nitric oxide signalling. This exploratory ...
PMC11799833
core_pubmed_pmc
Multi-pronged molecular insights into flavonoid-mediated inhibition of squalene epoxidase: a pathway to novel therapeutics
Multi-pronged molecular insights into flavonoid-mediated inhibition of squalene epoxidase: a pathway to novel therapeutics Abstract Squalene epoxidase (SQLE) is a crucial enzyme in the sterol biosynthesis pathway and a promising target for therapeutic intervention in hypercholesterolemia and fungal infections. This stu...
PMC12236304
core_pubmed_pmc
Phase 1 study of zavondemstat (TACH101), a first-in-class KDM4 inhibitor, in patients with advanced solid tumors
Phase 1 study of zavondemstat (TACH101), a first-in-class KDM4 inhibitor, in patients with advanced solid tumors Abstract Abstract Background This was a first-in-human, phase I, dose-escalation study evaluating the safety, pharmacokinetics, and preliminary efficacy of zavondemstat (TACH101), an epigenetic targeting inh...
PMC12378308
core_pubmed_pmc
A Drug–Drug Interaction Study Evaluating the Pharmacokinetic Consequences of Obicetrapib Therapy on Atorvastatin or Rosuvastatin Levels in Healthy Volunteers
A Drug–Drug Interaction Study Evaluating the Pharmacokinetic Consequences of Obicetrapib Therapy on Atorvastatin or Rosuvastatin Levels in Healthy Volunteers Abstract Abstract Objective Obicetrapib, a selective cholesteryl ester transfer protein inhibitor in development for the treatment of dyslipidemia and cardiovascu...
PMC9542378
core_pubmed_pmc
Evaluation of Lorlatinib Cerebrospinal Fluid Concentrations in Relation to Target Concentrations for Anaplastic Lymphoma Kinase (ALK) Inhibition
Evaluation of Lorlatinib Cerebrospinal Fluid Concentrations in Relation to Target Concentrations for Anaplastic Lymphoma Kinase (ALK) Inhibition Abstract Abstract Lorlatinib is a third‐generation, brain‐penetrant anaplastic lymphoma kinase (ALK) and c‐ros oncogene 1 (ROS1) tyrosine kinase inhibitor (TKI) with robust in...
PMC7262448
core_pubmed_pmc
Disconnect between signalling potency and in vivo efficacy of pharmacokinetically optimised biased glucagon-like peptide-1 receptor agonists
Disconnect between signalling potency and in vivo efficacy of pharmacokinetically optimised biased glucagon-like peptide-1 receptor agonists Abstract Abstract Objective The objective of this study was to determine how pharmacokinetically advantageous acylation impacts on glucagon-like peptide-1 receptor (GLP-1R) signal...
PMC9867073
core_pubmed_pmc
Tailoring Apixaban in Nanostructured Lipid Carrier Enhancing Its Oral Bioavailability and Anticoagulant Activity
Tailoring Apixaban in Nanostructured Lipid Carrier Enhancing Its Oral Bioavailability and Anticoagulant Activity Abstract Apixaban (Apx), an oral anticoagulant drug, is a direct factor Xa inhibitor for the prophylaxis against venous thromboembolism. Apx has limited oral bioavailability and poor water solubility. The go...
PMC10221670
core_pubmed_pmc
Machine Learning for Exposure-Response Analysis: Methodological Considerations and Confirmation of Their Importance via Computational Experimentations
Machine Learning for Exposure-Response Analysis: Methodological Considerations and Confirmation of Their Importance via Computational Experimentations Abstract Exposure-response (E-R) is a key aspect of pharmacometrics analysis that supports drug dose selection. Currently, there is a lack of understanding of the techni...
PMC10534693
core_pubmed_pmc
A High-Performance Liquid Chromatography with Photodiode Array Detection Method for Simultaneous Determination of Three Compounds Isolated from Wikstroemia ganpi : Assessment of the Effects on Cytochrome P450-Mediated Metabolism In Vitro and In Vivo
A High-Performance Liquid Chromatography with Photodiode Array Detection Method for Simultaneous Determination of Three Compounds Isolated from Wikstroemia ganpi : Assessment of the Effects on Cytochrome P450-Mediated Metabolism In Vitro and In Vivo Abstract Abstract In natural products, the content and quality of the ...
PMC9902323
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Characteristics of Insulin Icodec After Subcutaneous Administration in the Thigh, Abdomen or Upper Arm in Individuals with Type 2 Diabetes Mellitus
Pharmacokinetic and Pharmacodynamic Characteristics of Insulin Icodec After Subcutaneous Administration in the Thigh, Abdomen or Upper Arm in Individuals with Type 2 Diabetes Mellitus Abstract Background and Objective Individuals with diabetes mellitus may prefer different body regions for subcutaneous insulin administ...
PMC6857198
core_pubmed_pmc
Can phenotypic data complement our understanding of antimycobacterial effects for drug combinations?
Can phenotypic data complement our understanding of antimycobacterial effects for drug combinations? Abstract Abstract Objectives To demonstrate how phenotypic cell viability data can provide insight into antimycobacterial effects for the isoniazid/rifampicin treatment backbone. Methods Data from a Mycobacterium komoss...
PMC10194899
core_pubmed_pmc
Identification of some bioactive compounds from Trignonella foenumgraecum as possible inhibitors of PPAR ϒ for diabetes treatment through molecular docking studies, pharmacophore modelling and ADMET profiling: An in-silico study
Identification of some bioactive compounds from Trignonella foenumgraecum as possible inhibitors of PPAR ϒ for diabetes treatment through molecular docking studies, pharmacophore modelling and ADMET profiling: An in-silico study Abstract Abstract Oral antidiabetic agents including the peroxisome proliferator-activated ...
PMC11858865
core_pubmed_pmc
Integrating In Vitro Dissolution and Physiologically Based Pharmacokinetic Modeling for Generic Drug Development: Evaluation of Amorphous Solid Dispersion Formulations for Tacrolimus
Integrating In Vitro Dissolution and Physiologically Based Pharmacokinetic Modeling for Generic Drug Development: Evaluation of Amorphous Solid Dispersion Formulations for Tacrolimus Abstract Abstract Objectives : Tacrolimus, a Biopharmaceutics Classification System (BCS) class II drug, is widely used for transplant pa...
PMC9448392
core_pubmed_pmc
Pharmacokinetic improvement provided by microneedle patch in delivering bee venom, a case study in combating scopolamine-induced neurodegeneration in mouse model
Pharmacokinetic improvement provided by microneedle patch in delivering bee venom, a case study in combating scopolamine-induced neurodegeneration in mouse model Abstract Abstract Much research has shown Bee venom to be an effective neuroprotective agent. However, the usual transdermal injection of bee venom poses many...
PMC12658801
core_pubmed_pmc
Rational Design and Greener Synthesis of Selenylated Indolamides as Potential Anti-Alzheimer’s Agents
Rational Design and Greener Synthesis of Selenylated Indolamides as Potential Anti-Alzheimer’s Agents Abstract This study presents the rational design and sustainable synthesis of selenylated indolamides as potential therapeutic agents for Alzheimer’s disease. Through computational approaches, including molecular docki...
PMC6122721
core_pubmed_pmc
Population pharmacokinetics of mefloquine given as a 3-day artesunate–mefloquine in patients with acute uncomplicated Plasmodium falciparum malaria in a multidrug-resistant area along the Thai–Myanmar border
Population pharmacokinetics of mefloquine given as a 3-day artesunate–mefloquine in patients with acute uncomplicated Plasmodium falciparum malaria in a multidrug-resistant area along the Thai–Myanmar border Abstract Abstract Background Low mefloquine exposure has been shown to contribute to treatment failure in patien...
PMC8157365
core_pubmed_pmc
Targeted and modular architectural polymers employing bioorthogonal chemistry for quantitative therapeutic delivery †
Targeted and modular architectural polymers employing bioorthogonal chemistry for quantitative therapeutic delivery † Abstract Abstract There remain several key challenges to existing therapeutic systems for cancer therapy, such as quantitatively determining the true, tissue-specific drug release profile in vivo , as w...
PMC10253381
core_pubmed_pmc
Evaluation of the Antiviral Efficacy of Subcutaneous Nafamostat Formulated with Glycyrrhizic Acid against SARS-CoV-2 in a Murine Model
Evaluation of the Antiviral Efficacy of Subcutaneous Nafamostat Formulated with Glycyrrhizic Acid against SARS-CoV-2 in a Murine Model Abstract The ongoing COVID-19 pandemic highlights the urgent need for effective antiviral agents and vaccines. Drug repositioning, which involves modifying existing drugs, offers a prom...
PMC8582402
core_pubmed_pmc
Do Lipid-based Nanoparticles Hold Promise for Advancing the Clinical Translation of Anticancer Alkaloids?
Do Lipid-based Nanoparticles Hold Promise for Advancing the Clinical Translation of Anticancer Alkaloids? Abstract Simple Summary Alkaloids are natural products that possess numerous pharmacological activities and have been exploited effectively to treat cancer. However, the clinically approved anticancer alkaloids are...
PMC7566116
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic integration for optimal dosage of cefquinome against Streptococcus equi subsp. equi in foals
Pharmacokinetic and pharmacodynamic integration for optimal dosage of cefquinome against Streptococcus equi subsp. equi in foals Abstract Abstract Cefquinome is administered in horses for the treatment of respiratory infection caused by Streptococcus equi subsp. zooepidemicus , and septicemia caused by Escherichia coli...
PMC12188480
core_pubmed_pmc
Light-Induced Synthesis and Radiotheranostic Treatment of Gastric Cancer with 161 Tb-Labeled Monoclonal Antibodies
Light-Induced Synthesis and Radiotheranostic Treatment of Gastric Cancer with 161 Tb-Labeled Monoclonal Antibodies Abstract Abstract Radiolabeled monoclonal antibodies (mAbs) form a major branch of nuclear medicine and are used in the development of tracers for both diagnostic imaging and molecularly targeted radio­(im...
PMC12703978
core_pubmed_pmc
Advancing rare disease therapeutics through digital twins: Opportunities in drug development and precision dosing
Advancing rare disease therapeutics through digital twins: Opportunities in drug development and precision dosing Abstract Abstract Rare disease(s) (RD/RDs) are typically characterized by (i) genetically driven chronic, and life-threatening disease progression, (ii) delayed diagnoses, (iii) limited treatment options, a...
PMC11919272
core_pubmed_pmc
Development of a physiologically‐based pharmacokinetic model for Ritonavir characterizing exposure and drug interaction potential at both acute and steady‐state conditions
Development of a physiologically‐based pharmacokinetic model for Ritonavir characterizing exposure and drug interaction potential at both acute and steady‐state conditions Abstract Abstract Ritonavir (RTV) is a potent CYP3A inhibitor that is widely used as a pharmacokinetic (PK) enhancer to increase exposure to select ...
PMC8595129
core_pubmed_pmc
Pharmacokinetics and Disposition of Heparin-Binding Growth Factor Midkine Antisense Oligonucleotide Nanoliposomes in Experimental Animal Species and Prediction of Human Pharmacokinetics Using a Physiologically Based Pharmacokinetic Model
Pharmacokinetics and Disposition of Heparin-Binding Growth Factor Midkine Antisense Oligonucleotide Nanoliposomes in Experimental Animal Species and Prediction of Human Pharmacokinetics Using a Physiologically Based Pharmacokinetic Model Abstract Encapsulating the antisense oligonucleotide drug MK-ASODN with nanoliposo...
PMC7615401
core_pubmed_pmc
Antiviral efficacy of molnupiravir versus ritonavir-boosted nirmatrelvir in patients with early symptomatic COVID-19 (PLATCOV): an open-label, phase 2, randomised, controlled, adaptive trial
Antiviral efficacy of molnupiravir versus ritonavir-boosted nirmatrelvir in patients with early symptomatic COVID-19 (PLATCOV): an open-label, phase 2, randomised, controlled, adaptive trial Abstract Summary Background Molnupiravir and ritonavir-boosted nirmatrelvir are the two leading oral COVID-19 antiviral treatment...
PMC8504836
core_pubmed_pmc
Safety, tolerability, and pharmacokinetics of oral baicalein tablets in healthy Chinese subjects: A single‐center, randomized, double‐blind, placebo‐controlled multiple‐ascending‐dose study
Safety, tolerability, and pharmacokinetics of oral baicalein tablets in healthy Chinese subjects: A single‐center, randomized, double‐blind, placebo‐controlled multiple‐ascending‐dose study Abstract Abstract Baicalein is a biologically important flavonoid in extracted from the Scutellaria baicalensis Georgi, which can ...
PMC8678561
core_pubmed_pmc
Evaluation of new or repurposed treatments for COVID-19: protocol for the phase Ib/IIa DEFINE trial platform
Evaluation of new or repurposed treatments for COVID-19: protocol for the phase Ib/IIa DEFINE trial platform Abstract Abstract Introduction COVID-19 is a new viral-induced pneumonia caused by infection with a novel coronavirus, SARS-CoV-2. At present, there are few proven effective treatments. This early-phase experime...
PMC12119990
core_pubmed_pmc
Antiviral activity of newly synthesized pyrazole derivatives against Newcastle disease virus
Antiviral activity of newly synthesized pyrazole derivatives against Newcastle disease virus Abstract Abstract Newcastle disease virus (NDV) is a highly contagious poultry disease that affects the respiratory, nervous, and digestive systems, causing significant losses to the poultry industry. Pyrazole-based scaffolds h...
PMC9391489
core_pubmed_pmc
Herb-anticancer drug interactions in real life based on VigiBase, the WHO global database
Herb-anticancer drug interactions in real life based on VigiBase, the WHO global database Abstract Abstract Cancer patients could combine herbal treatments with their chemotherapy. We consulted VigiBase, a WHO database of individual case safety reports (ICSRs) which archives reports of suspected Adverse Drug Reactions ...
PMC2937314
core_pubmed_pmc
Effect of centchroman coadministration on the pharmacokinetics of metformin in rats
Effect of centchroman coadministration on the pharmacokinetics of metformin in rats Abstract Objectives: To study the effect of centchroman, a non-steroidal oral contraceptive, coadministration on the pharmacokinetics of metformin in rats. Materials and Methods: The pharmacokinetic interaction of metformin was studied ...
PMC12389637
core_pubmed_pmc
In Silico ADME Methods Used in the Evaluation of Natural Products
In Silico ADME Methods Used in the Evaluation of Natural Products Abstract Abstract The pharmaceutical industry faces significant challenges when promising drug candidates fail during development due to suboptimal ADME (absorption, distribution, metabolism, excretion) properties or toxicity concerns. Natural compounds ...
PMC6399170
core_pubmed_pmc
Palbociclib in combination with fulvestrant in patients with hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer: PALOMA-3 subgroup analysis of Japanese patients
Palbociclib in combination with fulvestrant in patients with hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer: PALOMA-3 subgroup analysis of Japanese patients Abstract Background In the double-blind, phase 3 PALOMA-3 study, palbociclib–fulvestrant significantly prolong...
PMC7667196
core_pubmed_pmc
The Impact of Surfactant Composition and Surface Charge of Niosomes on the Oral Absorption of Repaglinide as a BCS II Model Drug
The Impact of Surfactant Composition and Surface Charge of Niosomes on the Oral Absorption of Repaglinide as a BCS II Model Drug Abstract Background Niosomes, bilayer vesicles formed by the self-assembly of nonionic surfactants, are receiving increasing attention as potential oral drug delivery systems but the impact o...