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PMC7545837
core_pubmed_pmc
The impact of therapeutic-dose induced intestinal enrofloxacin concentrations in healthy pigs on fecal Escherichia coli populations
The impact of therapeutic-dose induced intestinal enrofloxacin concentrations in healthy pigs on fecal Escherichia coli populations Abstract Abstract Background Knowledge of therapy-induced intestinal tract concentrations of antimicrobials allows for interpretation and prediction of antimicrobial resistance selection w...
PMC5777431
core_pubmed_pmc
Population pharmacodynamic modelling of midazolam induced sedation in terminally ill adult patients
Population pharmacodynamic modelling of midazolam induced sedation in terminally ill adult patients Abstract Abstract Aims Midazolam is the drug of choice for palliative sedation and is titrated to achieve the desired level of sedation. A previous pharmacokinetic (PK) study showed that variability between patients coul...
PMC12384571
core_pubmed_pmc
Enhancement of Protein–Protein Interactions by Destabilizing Mutations Revealed by HDX-MS
Enhancement of Protein–Protein Interactions by Destabilizing Mutations Revealed by HDX-MS Abstract Abstract Enhancing protein–protein interactions is a key therapeutic strategy to ensure effective protein function in terms of pharmacokinetics and pharmacodynamics and can be accomplished with methods like directed evolu...
PMC9861776
core_pubmed_pmc
Development and Evaluation of Solid Lipid Nanoparticles for the Clearance of Aβ in Alzheimer’s Disease
Development and Evaluation of Solid Lipid Nanoparticles for the Clearance of Aβ in Alzheimer’s Disease Abstract Abstract Aggregation of Amyloid-β (Aβ) leads to the formation and deposition of neurofibrillary tangles and plaques which is the main pathological hallmark of Alzheimer’s disease (AD). The bioavailability of ...
PMC5599452
core_pubmed_pmc
Cost-Effectiveness of Posaconazole Tablets for Invasive Fungal Infections Prevention in Acute Myelogenous Leukemia or Myelodysplastic Syndrome Patients in Spain
Cost-Effectiveness of Posaconazole Tablets for Invasive Fungal Infections Prevention in Acute Myelogenous Leukemia or Myelodysplastic Syndrome Patients in Spain Abstract Introduction Posaconazole is superior to fluconazole (FLU) and itraconazole (ITRA) in the prevention of invasive fungal diseases (IFDs) in neutropenic...
PMC12307992
core_pubmed_pmc
The Potential Influence of Associated Antidepressants on the Pharmacokinetic Profile of Esketamine in Patients Affected by Treatment-resistant Depression
The Potential Influence of Associated Antidepressants on the Pharmacokinetic Profile of Esketamine in Patients Affected by Treatment-resistant Depression Abstract Abstract Introduction/Objective Esketamine is administered intranasally in combination with at least another antidepressant in patients with treatment-resist...
PMC12256221
core_pubmed_pmc
Pharmacological basis for medicinal use of Cymbopogon proximus Hochst. ex A. Rich. Essential oil in hyperactive gastrointestinal disorders
Pharmacological basis for medicinal use of Cymbopogon proximus Hochst. ex A. Rich. Essential oil in hyperactive gastrointestinal disorders Abstract Background Cymbopogon is used in traditional medicine in tropical and subtropical regions to treat various ailments. However, no research has yet provided a detailed pharma...
PMC7548405
core_pubmed_pmc
Pharmacokinetics and tissue distribution of remdesivir and its metabolites nucleotide monophosphate, nucleotide triphosphate, and nucleoside in mice
Pharmacokinetics and tissue distribution of remdesivir and its metabolites nucleotide monophosphate, nucleotide triphosphate, and nucleoside in mice Abstract Remdesivir (RDV) exerts anti-severe acute respiratory coronavirus 2 activity following metabolic activation in the target tissues. However, the pharmacokinetics a...
PMC7355888
core_pubmed_pmc
Chiral Aspects of Local Anesthetics
Chiral Aspects of Local Anesthetics Abstract Thanks to the progress made in chemical technology (particularly in the methodologies of stereoselective syntheses and analyses) along with regulatory measures, the number of new chiral drugs registered in the form of pure enantiomers has increased over the past decade. In a...
PMC5975025
core_pubmed_pmc
Alzheimer's disease progression model using disability assessment for dementia scores from bapineuzumab trials
Alzheimer's disease progression model using disability assessment for dementia scores from bapineuzumab trials Abstract Abstract Objective Disability assessment for dementia (DAD) measurements from two phase-3 studies of bapineuzumab in APOE ε4 noncarrier and carrier Alzheimer's disease (AD) patients were integrated to...
PMC7854444
core_pubmed_pmc
Pharmacokinetics and Safety of INL-001 (Bupivacaine HCl) Implants Compared with Bupivacaine HCl Infiltration After Open Unilateral Inguinal Hernioplasty
Pharmacokinetics and Safety of INL-001 (Bupivacaine HCl) Implants Compared with Bupivacaine HCl Infiltration After Open Unilateral Inguinal Hernioplasty Abstract Abstract Introduction Surgical site infiltration with bupivacaine HCl results in short-lived analgesia for postsurgical pain and carries the risk of systemic ...
PMC6682782
core_pubmed_pmc
Extended Half-Life Coagulation Factors: A New Era in the Management of Hemophilia Patients
Extended Half-Life Coagulation Factors: A New Era in the Management of Hemophilia Patients Abstract Abstract Despite effective factor replacement and various treatment schedules, there remain several challenges and unmet needs in the prophylactic treatment of hemophilia limiting its adoption and thereby posing an incre...
PMC11138134
core_pubmed_pmc
Quantitative systems pharmacology modeling of macrophage‐targeted therapy combined with PD‐L1 inhibition in advanced NSCLC
Quantitative systems pharmacology modeling of macrophage‐targeted therapy combined with PD‐L1 inhibition in advanced NSCLC Abstract Abstract Immune checkpoint inhibitors remained the standard‐of‐care treatment for advanced non‐small cell lung cancer (NSCLC) for the past decade. In unselected patients, anti‐PD‐(L)1 mono...
PMC11705821
core_pubmed_pmc
Antimicrobial susceptibility testing of Dermabacter hominis
Antimicrobial susceptibility testing of Dermabacter hominis Abstract ABSTRACT Dermabacter hominis, a short gram-positive rod, is a part of the human skin flora, but can also cause infections (e.g., skin and soft tissue infections, bone and joint infections, abscesses, peritoneal dialysis-associated peritonitis, and bac...
PMC3211444
core_pubmed_pmc
Development of Polysorbate 80/Phospholipid mixed micellar formation for docetaxel and assessment of its in vivo distribution in animal models
Development of Polysorbate 80/Phospholipid mixed micellar formation for docetaxel and assessment of its in vivo distribution in animal models Abstract Abstract Docetaxel (DTX) is a very important member of taxoid family. Despite several alternative delivery systems reported recently, DTX formulated by Polysorbate 80 an...
PMC4833483
core_pubmed_pmc
Advances in Insulin Therapy: A Review of New Insulin Glargine 300 Units/mL in the Management of Diabetes
Advances in Insulin Therapy: A Review of New Insulin Glargine 300 Units/mL in the Management of Diabetes Abstract Abstract In Brief New insulin glargine 300 units/mL (Gla-300) is a formulation of insulin glargine that has a more constant pharmacokinetic profile with a prolonged duration of action. The EDITION clinical ...
PMC12845451
core_pubmed_pmc
Open-Label Phase II Study of Olokizumab in Adolescent Patients with Polyarticular Juvenile Idiopathic Arthritis: Results of the 24-Week Treatment Period
Open-Label Phase II Study of Olokizumab in Adolescent Patients with Polyarticular Juvenile Idiopathic Arthritis: Results of the 24-Week Treatment Period Abstract Abstract Background/Objectives : This study aimed to evaluate the pharmacokinetics (PK), effectiveness, and safety of the direct interleukin-6 (IL-6) inhibito...
PMC8389922
core_pubmed_pmc
First-in-Class Cyclic Temporin L Analogue: Design, Synthesis, and Antimicrobial Assessment
First-in-Class Cyclic Temporin L Analogue: Design, Synthesis, and Antimicrobial Assessment Abstract Abstract The pharmacodynamic and pharmacokinetic properties of bioactive peptides can be modulated by introducing conformational constraints such as intramolecular macrocyclizations, which can involve either the backbone...
PMC3263413
core_pubmed_pmc
RGD-modified poly(D,L-lactic acid) nanoparticles enhance tumor targeting of oridonin
RGD-modified poly(D,L-lactic acid) nanoparticles enhance tumor targeting of oridonin Abstract Abstract Objective The purpose of this study was to develop an active targeting strategy to improve the therapeutic antitumor efficacy of oridonin (ORI), the main active ingredient in the medicinal herb Rabdosia rubescens . Me...
PMC9240352
core_pubmed_pmc
Case Report: Bosentan and Sildenafil Exposure in Human Milk - A Contribution From the ConcePTION Project
Case Report: Bosentan and Sildenafil Exposure in Human Milk - A Contribution From the ConcePTION Project Abstract Abstract Introduction: Quantitative information on disposition of maternal medicines in human milk remains a major knowledge gap. This case report presents the clinical and pharmacokinetic data of a single ...
PMC7576624
core_pubmed_pmc
A mechanistic pharmacokinetic model with drug and antidrug antibody interplay, and its application for assessing the impact of immunogenicity response on bioequivalence testing
A mechanistic pharmacokinetic model with drug and antidrug antibody interplay, and its application for assessing the impact of immunogenicity response on bioequivalence testing Abstract Abstract Aims Single‐dose pharmacokinetic (PK) studies in healthy subjects have been the design of choice for bioequivalence determina...
PMC11966821
core_pubmed_pmc
Catecholamines in sepsis: pharmacological insights and clinical applications—a narrative review
Catecholamines in sepsis: pharmacological insights and clinical applications—a narrative review Abstract Abstract Catecholamines, essential neurotransmitters and hormones, play a critical role in the body’s physiological response to stress and are pivotal in the management of various clinical conditions, particularly i...
PMC3502231
core_pubmed_pmc
IBC’s 23rd Antibody Engineering and 10th Antibody Therapeutics Conferences and the Annual Meeting of The Antibody Society
IBC’s 23rd Antibody Engineering and 10th Antibody Therapeutics Conferences and the Annual Meeting of The Antibody Society Abstract Abstract Now in its 23rd and 10th years, respectively, the Antibody Engineering and Antibody Therapeutics conferences are the Annual Meeting of The Antibody Society. The scientific program ...
PMC8701823
core_pubmed_pmc
EGb 761 ® Does Not Affect Blood Coagulation and Bleeding Time in Patients with Probable Alzheimer’s Dementia—Secondary Analysis of a Randomized, Double-Blind Placebo-Controlled Trial
EGb 761 ® Does Not Affect Blood Coagulation and Bleeding Time in Patients with Probable Alzheimer’s Dementia—Secondary Analysis of a Randomized, Double-Blind Placebo-Controlled Trial Abstract Following reports of bleeding upon Ginkgo intake, we assessed whether Ginkgo extract EGb 761 ® affects coagulation or platelet f...
PMC12066255
core_pubmed_pmc
Rational design of allosteric inhibitors targeting C797S mutant EGFR in NSCLC: an integrative in silico and in-vitro study
Rational design of allosteric inhibitors targeting C797S mutant EGFR in NSCLC: an integrative in silico and in-vitro study Abstract Background The emergence of the C797S mutation in the epidermal growth factor receptor (EGFR) significantly limits the efficacy of covalent inhibitors in treating non-small cell lung cance...
PMC12059892
core_pubmed_pmc
Quantum Evaluation of a Comprehensive Set of Carboxylic Acid Bioisosteres: Gas versus Solvated Phases
Quantum Evaluation of a Comprehensive Set of Carboxylic Acid Bioisosteres: Gas versus Solvated Phases Abstract Abstract In drug design, bioisosterism is used to enhance the pharmacokinetic and pharmacodynamic properties of a drug molecule while maintaining its biological activity. This study investigates the use of a q...
PMC8613110
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of Cefiderocol
Clinical Pharmacokinetics and Pharmacodynamics of Cefiderocol Abstract Abstract Cefiderocol is a new broad-spectrum cephalosporin antibiotic with promising activity against various Gram-negative bacteria including carbapenem-resistant strains. A chlorocatechol group in the C-3 side chain provides cefiderocol with a sid...
PMC3548110
core_pubmed_pmc
Pharmacokinetics of transdermal buprenorphine patch in the elderly
Pharmacokinetics of transdermal buprenorphine patch in the elderly Abstract Purpose Transdermal buprenorphine patches provide comparable pain relief to that of low-potency opioids in elderly individuals. However, specific data on their use in elderly individuals is limited. This study investigated and compared the PK o...
PMC4883261
core_pubmed_pmc
Pharmacokinetics and Bioequivalence Study of Hydroxychloroquine Sulfate Tablets in Chinese Healthy Volunteers by LC–MS/MS
Pharmacokinetics and Bioequivalence Study of Hydroxychloroquine Sulfate Tablets in Chinese Healthy Volunteers by LC–MS/MS Abstract Introduction Hydroxychloroquine (HCQ), 4-aminoquinoline, is an antimalarial drug and has become a basic therapy for rheumatic disease treatment. It can stabilize the condition of SLE patien...
PMC10602056
core_pubmed_pmc
Optimal Designs for Nonlinear Mixed-effects Models Using Competitive Swarm Optimizer with Mutated Agents
Optimal Designs for Nonlinear Mixed-effects Models Using Competitive Swarm Optimizer with Mutated Agents Abstract Abstract Nature-inspired meta-heuristic algorithms are increasingly used in many disciplines to tackle challenging optimization problems. Our focus is to apply a newly proposed nature-inspired meta-heuristi...
PMC6103555
core_pubmed_pmc
Enhancing anticancer effects, decreasing risks and solving practical problems facing 3-bromopyruvate in clinical oncology: 10 years of research experience
Enhancing anticancer effects, decreasing risks and solving practical problems facing 3-bromopyruvate in clinical oncology: 10 years of research experience Abstract 3-Bromopyruvate (3BP) is a promising powerful general anticancer agent. Unfortunately, 3BP release faces many practical and biochemical problems in clinical...
PMC12368744
core_pubmed_pmc
Anti‐KIT Barzolvolimab for Chronic Spontaneous Urticaria
Anti‐KIT Barzolvolimab for Chronic Spontaneous Urticaria Abstract ABSTRACT Background Chronic spontaneous urticaria (CSU) is characterized by mast cell (MC)‐mediated wheals and/or angioedema without identifiable triggers and is driven by MC activation. Barzolvolimab—a monoclonal anti‐KIT antibody—depletes MCs by inhibi...
PMC10627564
core_pubmed_pmc
Gout Treatment and Clinical Considerations: The Role of Pegloticase, Colchicine, and Febuxostat
Gout Treatment and Clinical Considerations: The Role of Pegloticase, Colchicine, and Febuxostat Abstract Gout treatment has evolved rapidly in recent decades, and various drugs have been designed for acute and chronic management. Three medications used to treat gout include pegloticase, colchicine, and febuxostat. When...
PMC9337647
core_pubmed_pmc
The influence of metformin transporter gene SLC22A1 and SLC47A1 variants on steady-state pharmacokinetics and glycemic response
The influence of metformin transporter gene SLC22A1 and SLC47A1 variants on steady-state pharmacokinetics and glycemic response Abstract Abstract Interindividual variation is important in the response to metformin as the first-line therapy for type-2 diabetes mellitus (T2DM). Considering that OCT1 and MATE1 transporter...
PMC6212520
core_pubmed_pmc
Postmortem Toxicology of New Synthetic Opioids
Postmortem Toxicology of New Synthetic Opioids Abstract One hundred fifteen Americans die every day from opioid overdose. These overdose fatalities have been augmented by the increased availability of potent synthetic opioids, such as fentanyl and its derivatives. The death rate of synthetic opioids, other than methado...
PMC8707824
core_pubmed_pmc
Probing In Silico the Benzimidazole Privileged Scaffold for the Development of Drug-like Anti-RSV Agents
Probing In Silico the Benzimidazole Privileged Scaffold for the Development of Drug-like Anti-RSV Agents Abstract Abstract Targeting the fusion (F) protein has been recognized as a fruitful strategy for the development of anti-RSV agents. Despite the considerable efforts so far put into the development of RSV F protein...
PMC4020363
core_pubmed_pmc
Carbon Nanotubes: An Emerging Drug Carrier for Targeting Cancer Cells
Carbon Nanotubes: An Emerging Drug Carrier for Targeting Cancer Cells Abstract Abstract During recent years carbon nanotubes (CNTs) have been attracted by many researchers as a drug delivery carrier. CNTs are the third allotropic form of carbon-fullerenes which were rolled into cylindrical tubes. To be integrated into ...
PMC12786577
core_pubmed_pmc
Inflammation and Resolution in Obesity-Related Cardiovascular Disease
Inflammation and Resolution in Obesity-Related Cardiovascular Disease Abstract Abstract Obesity-associated inflammation underlies much of cardiometabolic pathology, reflecting the convergence of chronic, low-grade systemic immune activation with region-specific maladaptation of adipose depots. Among these, epicardial a...
PMC3528055
core_pubmed_pmc
Development of a High-Performance Liquid Chromatographic Method for Determination of Letrozole in Wistar Rat Serum and its Application in Pharmacokinetic Studies
Development of a High-Performance Liquid Chromatographic Method for Determination of Letrozole in Wistar Rat Serum and its Application in Pharmacokinetic Studies Abstract Abstract A fast, sensitive, and specific reversed-phase high-performance liquid chromatographic (RP–HPLC) method for the determination of letrozole i...
PMC12919259
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic relationship of a novel pleuromutilin derivative APTM against Mycoplasma gallisepticum
Pharmacokinetic/pharmacodynamic relationship of a novel pleuromutilin derivative APTM against Mycoplasma gallisepticum Abstract Abstract Mycoplasma gallisepticum (MG) is a primary avian pathogen that causes chronic respiratory disease, leading to significant economic losses in the poultry industry. This study aimed to ...
PMC5641543
core_pubmed_pmc
Selective Essential Oils from Spice or Culinary Herbs Have High Activity against Stationary Phase and Biofilm Borrelia burgdorferi
Selective Essential Oils from Spice or Culinary Herbs Have High Activity against Stationary Phase and Biofilm Borrelia burgdorferi Abstract Although the majority of patients with acute Lyme disease can be cured with the standard 2–4 week antibiotic treatment, about 10–20% of patients continue suffering from chronic sym...
PMC11573843
core_pubmed_pmc
Population Pharmacokinetic Modelling of Norepinephrine in Healthy Volunteers Prior to and During General Anesthesia
Population Pharmacokinetic Modelling of Norepinephrine in Healthy Volunteers Prior to and During General Anesthesia Abstract Abstract Background Intraoperation hypotension (IOH) is commonly observed in patients undergoing surgery under general anesthesia, and even a brief episode of IOH can lead to unfavorable outcomes...
PMC11551066
core_pubmed_pmc
Safety, pharmacokinetics, and pharmacodynamics of sofnobrutinib, a novel non‐covalent BTK inhibitor, in healthy subjects: First‐in‐human phase I study
Safety, pharmacokinetics, and pharmacodynamics of sofnobrutinib, a novel non‐covalent BTK inhibitor, in healthy subjects: First‐in‐human phase I study Abstract Abstract Bruton's tyrosine kinase (BTK) is a potential therapeutic target for allergic and autoimmune diseases. This first‐in‐human phase I study evaluated safe...
PMC9032145
core_pubmed_pmc
Cocaine: An Updated Overview on Chemistry, Detection, Biokinetics, and Pharmacotoxicological Aspects including Abuse Pattern
Cocaine: An Updated Overview on Chemistry, Detection, Biokinetics, and Pharmacotoxicological Aspects including Abuse Pattern Abstract Abstract Cocaine is one of the most consumed stimulants throughout the world, as official sources report. It is a naturally occurring sympathomimetic tropane alkaloid derived from the le...
PMC12941253
core_pubmed_pmc
Vitamin K Prophylaxis in Newborns: A Narrative Review of the Molecular Basis, Clinical Evidence, and Comparative Effectiveness of Intramuscular Versus Oral Administration and Parental Hesitation
Vitamin K Prophylaxis in Newborns: A Narrative Review of the Molecular Basis, Clinical Evidence, and Comparative Effectiveness of Intramuscular Versus Oral Administration and Parental Hesitation Abstract Vitamin K prophylaxis represents a paradigmatic example of how molecular mechanisms directly translate into effectiv...
PMC3825543
core_pubmed_pmc
Sunitinib combined with pemetrexed and carboplatin in patients with advanced solid malignancies—results of a phase I dose-escalation study
Sunitinib combined with pemetrexed and carboplatin in patients with advanced solid malignancies—results of a phase I dose-escalation study Abstract Summary Objectives The maximum tolerated dose (MTD) and overall safety of sunitinib plus pemetrexed and carboplatin was determined in patients with advanced solid malignanc...
PMC6158767
core_pubmed_pmc
Vistusertib (dual m-TORC1/2 inhibitor) in combination with paclitaxel in patients with high-grade serous ovarian and squamous non-small-cell lung cancer
Vistusertib (dual m-TORC1/2 inhibitor) in combination with paclitaxel in patients with high-grade serous ovarian and squamous non-small-cell lung cancer Abstract Abstract Background We have previously shown that raised p-S6K levels correlate with resistance to chemotherapy in ovarian cancer. We hypothesised that inhibi...
PMC9747611
core_pubmed_pmc
Results from a phase 1, randomized, double-blind, multiple ascending dose study characterizing the pharmacokinetics and demonstrating the safety and selectivity of the aldosterone synthase inhibitor baxdrostat in healthy volunteers
Results from a phase 1, randomized, double-blind, multiple ascending dose study characterizing the pharmacokinetics and demonstrating the safety and selectivity of the aldosterone synthase inhibitor baxdrostat in healthy volunteers Abstract Abstract Baxdrostat is a selective inhibitor of aldosterone synthase designed f...
PMC12944049
core_pubmed_pmc
Impact of Neonatal Fc Receptor on Transferrin Receptor Antibody Fusion Protein Pharmacokinetics †
Impact of Neonatal Fc Receptor on Transferrin Receptor Antibody Fusion Protein Pharmacokinetics † Abstract Abstract Background : Transferrin receptor-targeting monoclonal antibodies (TfRMAbs) enhance brain drug delivery by facilitating TfR-mediated transcytosis across the blood–brain barrier (BBB). Data suggest that ch...
PMC11365851
core_pubmed_pmc
Precision Medicine Strategies to Improve Isoniazid Therapy in Patients with Tuberculosis
Precision Medicine Strategies to Improve Isoniazid Therapy in Patients with Tuberculosis Abstract Abstract Due to interindividual variability in drug metabolism and pharmacokinetics, traditional isoniazid fixed-dose regimens may lead to suboptimal or toxic isoniazid concentrations in the plasma of patients with tubercu...
PMC10663184
core_pubmed_pmc
Cytochrome P450 activity in rheumatoid arthritis patients during continuous IL-6 receptor antagonist therapy
Cytochrome P450 activity in rheumatoid arthritis patients during continuous IL-6 receptor antagonist therapy Abstract Abstract Background Inflammation suppresses cytochrome P450 (CYP) enzyme activity, and single-dose interleukin 6 receptor antagonists (anti-IL-6R) reverse this effect. Here, we assess the impact of cont...
PMC9841533
core_pubmed_pmc
Microtubule-Stabilizing 1,2,4-Triazolo[1,5- a ]pyrimidines as Candidate Therapeutics for Neurodegenerative Disease: Matched Molecular Pair Analyses and Computational Studies Reveal New Structure–Activity Insights
Microtubule-Stabilizing 1,2,4-Triazolo[1,5- a ]pyrimidines as Candidate Therapeutics for Neurodegenerative Disease: Matched Molecular Pair Analyses and Computational Studies Reveal New Structure–Activity Insights Abstract Abstract Microtubule (MT)-stabilizing 1,2,4-triazolo[1,5- a ]pyrimidines (TPDs) hold promise as ca...
PMC9783281
core_pubmed_pmc
Nano and Microemulsions for the Treatment of Depressive and Anxiety Disorders: An Efficient Approach to Improve Solubility, Brain Bioavailability and Therapeutic Efficacy
Nano and Microemulsions for the Treatment of Depressive and Anxiety Disorders: An Efficient Approach to Improve Solubility, Brain Bioavailability and Therapeutic Efficacy Abstract Abstract Most drugs used for the treatment of depression, anxiety and related disorders have low absorption, high metabolism, low brain targ...
PMC12413561
core_pubmed_pmc
A Randomized Trial on the Combined Effect of Ponesimod and Propranolol on Heart Rate, Cardiac Safety, and Pharmacokinetics in Healthy Adults
A Randomized Trial on the Combined Effect of Ponesimod and Propranolol on Heart Rate, Cardiac Safety, and Pharmacokinetics in Healthy Adults Abstract ABSTRACT The objective of this phase 1 study was to evaluate the pharmacokinetics (PK), pharmacodynamics, and cardiac effect following administration of ponesimod (a sele...
PMC7877818
core_pubmed_pmc
A Strategy to Treat COVID‐19 Disease With Targeted Delivery of Inhalable Liposomal Hydroxychloroquine: A Preclinical Pharmacokinetic Study
A Strategy to Treat COVID‐19 Disease With Targeted Delivery of Inhalable Liposomal Hydroxychloroquine: A Preclinical Pharmacokinetic Study Abstract Abstract Severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) is a newly identified pathogen causing the coronavirus disease 2019 (COVID‐19) pandemic. Hydroxychloro...
PMC5296733
core_pubmed_pmc
Functional Coupling of Human Microphysiology Systems: Intestine, Liver, Kidney Proximal Tubule, Blood-Brain Barrier and Skeletal Muscle
Functional Coupling of Human Microphysiology Systems: Intestine, Liver, Kidney Proximal Tubule, Blood-Brain Barrier and Skeletal Muscle Abstract Abstract Organ interactions resulting from drug, metabolite or xenobiotic transport between organs are key components of human metabolism that impact therapeutic action and to...
PMC5786104
core_pubmed_pmc
Increased Exposure of Tacrolimus by Co-administered Mycophenolate Mofetil: Population Pharmacokinetic Analysis in Healthy Volunteers
Increased Exposure of Tacrolimus by Co-administered Mycophenolate Mofetil: Population Pharmacokinetic Analysis in Healthy Volunteers Abstract Abstract The objective of the study was to investigate the pharmacokinetic drug-drug interactions between tacrolimus (TAC) and mycophenolate mofetil (MMF) in healthy Korean male ...
PMC7395386
core_pubmed_pmc
Recent advance in treatment of osteoarthritis by bioactive components from herbal medicine
Recent advance in treatment of osteoarthritis by bioactive components from herbal medicine Abstract Abstract Osteoarthritis (OA) is a common chronic articular degenerative disease, and characterized by articular cartilage degradation, synovial inflammation/immunity, and subchondral bone lesion, etc. The disease affects...
PMC7688533
core_pubmed_pmc
Prospective validation of a model‐informed precision dosing tool for vancomycin in intensive care patients
Prospective validation of a model‐informed precision dosing tool for vancomycin in intensive care patients Abstract Aims Vancomycin is an important antibiotic for critically ill patients with Gram‐positive bacterial infections. Critically ill patients typically have severely altered pathophysiology, which leads to inef...
PMC12516731
core_pubmed_pmc
Optimization of Physicochemical Properties and ADME for 2,4-Substituted 1 H ‑Pyrrolo[2,3 b ]pyridines Inhibitors of Trypanosome Proliferation
Optimization of Physicochemical Properties and ADME for 2,4-Substituted 1 H ‑Pyrrolo[2,3 b ]pyridines Inhibitors of Trypanosome Proliferation Abstract Abstract Neglected tropical diseases, such as human African trypanosomiasis (HAT), require novel treatments that can populate the clinical pipeline in the event of risin...
PMC6128275
core_pubmed_pmc
RGD-modified nanoliposomes containing quercetin for lung cancer targeted treatment
RGD-modified nanoliposomes containing quercetin for lung cancer targeted treatment Abstract Abstract Purpose The aim of this study was to prepare RGD-modified nanoliposomes containing quercetin (QCT) distearoyl-L-a-phosphatidylethanolamine-polyethylene glycol 2000-RGD-liposomes ([DSPE]-PEG2000-RGD-LPs/QCT) for lung can...
PMC7604266
core_pubmed_pmc
Pharmacokinetics of Oral Prednisone at Various Doses in Dogs: Preliminary Findings Using a Naïve Pooled-Data Approach
Pharmacokinetics of Oral Prednisone at Various Doses in Dogs: Preliminary Findings Using a Naïve Pooled-Data Approach Abstract Abstract This pilot study aimed to determine the plasma pharmacokinetics of prednisone and its active metabolite prednisolone following oral prednisone administration in dogs—using dosing regim...
PMC12008329
core_pubmed_pmc
Identification of Novel Potential Herbal Drug Targets against Beta-Catenin in the Treatment of Oral Squamous Cell Carcinoma
Identification of Novel Potential Herbal Drug Targets against Beta-Catenin in the Treatment of Oral Squamous Cell Carcinoma Abstract Abstract Objective: The study aims to identify potential pharmacophore models for targeting beta-catenin, a crucial protein involved in the development of oral squamous cell carcinoma (OS...
PMC9240740
core_pubmed_pmc
Morphine analgesia in male inbred genetic diversity mice recapitulates the among‐individual variance in response to morphine in humans
Morphine analgesia in male inbred genetic diversity mice recapitulates the among‐individual variance in response to morphine in humans Abstract Abstract Morphine is a widely used analgesic, but its use in clinical precision medicine is limited by the variance in response among individuals. Although previous studies hav...
PMC8624696
core_pubmed_pmc
Antidepressants and Circadian Rhythm: Exploring Their Bidirectional Interaction for the Treatment of Depression
Antidepressants and Circadian Rhythm: Exploring Their Bidirectional Interaction for the Treatment of Depression Abstract Abstract Scientific evidence that circadian rhythms affect pharmacokinetics and pharmacodynamics has highlighted the importance of drug dosing-time. Circadian oscillations alter drug absorption, dist...
PMC8700093
core_pubmed_pmc
Pediatric Atypical Hemolytic Uremic Syndrome Advances
Pediatric Atypical Hemolytic Uremic Syndrome Advances Abstract Atypical hemolytic uremic syndrome (aHUS) is a rare disorder characterized by dysregulation of the alternate pathway. The diagnosis of aHUS is one of exclusion, which complicates its early detection and corresponding intervention to mitigate its high rate o...
PMC11180387
core_pubmed_pmc
In-vitro evaluation of different antimicrobial combinations with and without colistin against carbapenem-resistant Acinetobacter baumannii clinical isolates
In-vitro evaluation of different antimicrobial combinations with and without colistin against carbapenem-resistant Acinetobacter baumannii clinical isolates Abstract Abstract Background Carbapenem-resistant Acinetobacter baumannii (CRAB) infections are one of the most common causes of nosocomial infections and have hig...
PMC11999052
core_pubmed_pmc
Systematic review and meta‐analysis of vancomycin therapeutic level for treatment of vancomycin‐sensitive enterococcal infections
Systematic review and meta‐analysis of vancomycin therapeutic level for treatment of vancomycin‐sensitive enterococcal infections Abstract Abstract Aims Evidence on the optimal targets of vancomycin for treating other Gram‐positive infections apart from methicillin‐resistant Staphylococcus aureus (MRSA) is lacking. Thi...
PMC3196562
core_pubmed_pmc
Assessing Antiangiogenic Therapy Response by DCE-MRI: Development of a Physiology Driven Multi-Compartment Model Using Population Pharmacometrics
Assessing Antiangiogenic Therapy Response by DCE-MRI: Development of a Physiology Driven Multi-Compartment Model Using Population Pharmacometrics Abstract Abstract Dynamic contrast enhanced (DCE-) MRI is commonly applied for the monitoring of antiangiogenic therapy in oncology. Established pharmacokinetic (PK) analysis...
PMC8645997
core_pubmed_pmc
Population Pharmacokinetics of Polymyxin B in Obese Patients for Resistant Gram-Negative Infections
Population Pharmacokinetics of Polymyxin B in Obese Patients for Resistant Gram-Negative Infections Abstract Polymyxin B is an effective but potentially nephrotoxic antibiotic that is commonly used to treat resistant Gram-negative infections. As a weight-based dosing drug, obese patients may be at a high risk of nephro...
PMC7823749
core_pubmed_pmc
The Neonatal and Juvenile Pig in Pediatric Drug Discovery and Development
The Neonatal and Juvenile Pig in Pediatric Drug Discovery and Development Abstract Pharmacotherapy in pediatric patients is challenging in view of the maturation of organ systems and processes that affect pharmacokinetics and pharmacodynamics. Especially for the youngest age groups and for pediatric-only indications, n...
PMC10272068
core_pubmed_pmc
Predicting the effect of different folate doses on [ 68 Ga]Ga-PSMA-11 organ and tumor uptake using physiologically based pharmacokinetic modeling
Predicting the effect of different folate doses on [ 68 Ga]Ga-PSMA-11 organ and tumor uptake using physiologically based pharmacokinetic modeling Abstract Abstract Background Folate intake might reduce [ 68 Ga]Ga-PSMA-11 uptake in tissues due to a competitive binding to the PSMA receptor. For diagnostic imaging, this c...
PMC3461035
core_pubmed_pmc
Sodium Bicarbonate Treatment during Transient or Sustained Lactic Acidemia in Normoxic and Normotensive Rats
Sodium Bicarbonate Treatment during Transient or Sustained Lactic Acidemia in Normoxic and Normotensive Rats Abstract Abstract Introduction Lactic acidosis is a frequent cause of poor outcome in the intensive care settings. We set up an experimental model of lactic acid infusion in normoxic and normotensive rats to inv...
PMC8502793
core_pubmed_pmc
Towards Fixed Dosing of Tocilizumab in ICU-Admitted COVID-19 Patients: Results of an Observational Population Pharmacokinetic and Descriptive Pharmacodynamic Study
Towards Fixed Dosing of Tocilizumab in ICU-Admitted COVID-19 Patients: Results of an Observational Population Pharmacokinetic and Descriptive Pharmacodynamic Study Abstract Background and Objective In the randomized controlled trial REMAP-CAP, it was shown that next to dexamethasone, the interleukin (IL)-6 receptor ant...
PMC7237643
core_pubmed_pmc
A Physiology-Based Pharmacokinetic Framework to Support Drug Development and Dose Precision During Therapeutic Hypothermia in Neonates
A Physiology-Based Pharmacokinetic Framework to Support Drug Development and Dose Precision During Therapeutic Hypothermia in Neonates Abstract Abstract Therapeutic hypothermia (TH) is standard treatment for neonates (≥36 weeks) with perinatal asphyxia (PA) and hypoxic–ischemic encephalopathy. TH reduces mortality and ...
PMC7271755
core_pubmed_pmc
Survey on request form content and result reporting in therapeutic drug monitoring service among laboratories in Czechia and Slovakia
Survey on request form content and result reporting in therapeutic drug monitoring service among laboratories in Czechia and Slovakia Abstract Abstract Introduction The aim of the study was to investigate current practice and policies of therapeutic drug monitoring (TDM) service requesting and result reporting in Czech...
PMC4281350
core_pubmed_pmc
Effect of Concomitant Icosapent Ethyl (Eicosapentaenoic Acid Ethyl Ester) on the Pharmacokinetics of Atorvastatin
Effect of Concomitant Icosapent Ethyl (Eicosapentaenoic Acid Ethyl Ester) on the Pharmacokinetics of Atorvastatin Abstract Abstract Background and Objective Icosapent ethyl is a high-purity prescription form of eicosapentaenoic acid ethyl ester approved as an adjunct to diet to reduce triglyceride levels in adult patie...
PMC9967574
core_pubmed_pmc
Development of Janus Particles as Potential Drug Delivery Systems for Diabetes Treatment and Antimicrobial Applications
Development of Janus Particles as Potential Drug Delivery Systems for Diabetes Treatment and Antimicrobial Applications Abstract Janus particles have emerged as a novel and smart material that could improve pharmaceutical formulation, drug delivery, and theranostics. Janus particles have two distinct compartments that ...
PMC8116505
core_pubmed_pmc
The Development of a Juvenile Porcine Augmented Renal Clearance Model Through Continuous Infusion of Lipopolysaccharides: An Exploratory Study
The Development of a Juvenile Porcine Augmented Renal Clearance Model Through Continuous Infusion of Lipopolysaccharides: An Exploratory Study Abstract Augmented renal clearance (ARC) as observed in the critically ill (pediatric) population can have a major impact on the pharmacokinetics and posology of renally excrete...
PMC12332157
core_pubmed_pmc
A preclinical study on the influence of linkers in [ 68 Ga]Ga-NOTA-X-RM26 radiotracers for PET imaging of GRPR expression
A preclinical study on the influence of linkers in [ 68 Ga]Ga-NOTA-X-RM26 radiotracers for PET imaging of GRPR expression Abstract Background Gastrin-releasing peptide receptor (GRPR) is overexpressed in several cancers, including prostate and breast, making it an attractive target for radiopharmaceutical development. ...
PMC4718940
core_pubmed_pmc
Preclinical studies of 5-fluoro-2′-deoxycytidine and tetrahydrouridine in pediatric brain tumors
Preclinical studies of 5-fluoro-2′-deoxycytidine and tetrahydrouridine in pediatric brain tumors Abstract Abstract Chemotherapies active in preclinical studies frequently fail in the clinic due to lack of efficacy, which limits progress for rare cancers since only small numbers of patients are available for clinical tr...
PMC7072103
core_pubmed_pmc
Simultaneous Determination of 13 Constituents of Radix Polygoni Multiflori in Rat Plasma and Its Application in a Pharmacokinetic Study
Simultaneous Determination of 13 Constituents of Radix Polygoni Multiflori in Rat Plasma and Its Application in a Pharmacokinetic Study Abstract Abstract Radix Polygoni Multiflori (RPM) has been widely used to treat various diseases in Asian countries for many centuries. Although, stilbenes and anthraquinones, two majo...
PMC4573195
core_pubmed_pmc
Potential drug–drug interactions in Alzheimer patients with behavioral symptoms
Potential drug–drug interactions in Alzheimer patients with behavioral symptoms Abstract The use of multi drug regimens among the elderly population has increased tremendously over the last decade although the benefits of medications are always accompanied by potential harm, even when prescribed at recommended doses. T...
PMC8480260
core_pubmed_pmc
Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres
Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres Abstract Abstract In the present study, we describe the development of betaxolol hydrochloride and montmorillonite with ion exchange in a single formulation to create a novel micro-interactive dual-functioning sustain...
PMC8505367
core_pubmed_pmc
Clinical Pharmacokinetics of Oral Semaglutide: Analyses of Data from Clinical Pharmacology Trials
Clinical Pharmacokinetics of Oral Semaglutide: Analyses of Data from Clinical Pharmacology Trials Abstract Objective The absorption, distribution and elimination of oral semaglutide, the first oral glucagon-like peptide-1 receptor agonist for treating type 2 diabetes, was investigated using a population pharmacokinetic...
PMC10574475
core_pubmed_pmc
Development and Validation of a UHPLC–MS/MS Method for the Quantification of a Novel PYGB Inhibitor in Plasma: Application to Pharmacokinetic Studies
Development and Validation of a UHPLC–MS/MS Method for the Quantification of a Novel PYGB Inhibitor in Plasma: Application to Pharmacokinetic Studies Abstract Abstract In previous studies, we reported compound 1 (5-chloro- N -(4-oxo-2,2-dipropyl-3,4-dihydro-2 H -benzo[ e ]oxazin-6-yl)-1 H -indole-2-carboxamide) as a no...
PMC10610403
core_pubmed_pmc
Predicting Maternal and Infant Tetrahydrocannabinol Exposure in Lactating Cannabis Users: A Physiologically Based Pharmacokinetic Modeling Approach
Predicting Maternal and Infant Tetrahydrocannabinol Exposure in Lactating Cannabis Users: A Physiologically Based Pharmacokinetic Modeling Approach Abstract A knowledge gap exists in infant tetrahydrocannabinol (THC) data to guide breastfeeding recommendations for mothers who use cannabis. In the present study, a paire...
PMC11102930
core_pubmed_pmc
Nonclinical pharmacodynamics of boron neutron capture therapy using direct intratumoral administration of a folate receptor targeting novel boron carrier
Nonclinical pharmacodynamics of boron neutron capture therapy using direct intratumoral administration of a folate receptor targeting novel boron carrier Abstract Abstract Background Boron neutron capture therapy (BNCT) is a precise particle radiation therapy known for its unique cellular targeting ability. The develop...
PMC10715200
core_pubmed_pmc
In vitro pharmacodynamics of nemonoxacin and other antimicrobial agents against Mycoplasma pneumoniae
In vitro pharmacodynamics of nemonoxacin and other antimicrobial agents against Mycoplasma pneumoniae Abstract ABSTRACT Mycoplasma pneumoniae is the causative agent of respiratory infections in children and adults. Macrolide still plays a significant role in treating infections by M. pneumoniae . However, macrolide-res...
PMC9578397
core_pubmed_pmc
Population Pharmacokinetic Modeling of Bedaquiline among Multidrug-Resistant Pulmonary Tuberculosis Patients from China
Population Pharmacokinetic Modeling of Bedaquiline among Multidrug-Resistant Pulmonary Tuberculosis Patients from China Abstract ABSTRACT Bedaquiline has been widely used as a part of combination dosage regimens for the treatment of multidrug-resistant tuberculosis (MDR-TB) patients with limited options. Although the e...
PMC12858553
core_pubmed_pmc
One Subcutaneous 2-ml Injection of Mirikizumab is Bioequivalent to Two 1-ml Subcutaneous Injections in Healthy Participants
One Subcutaneous 2-ml Injection of Mirikizumab is Bioequivalent to Two 1-ml Subcutaneous Injections in Healthy Participants Abstract Introduction Mirikizumab, an anti-interleukin-23 p19 monoclonal antibody, is approved for treating adults with moderately to severely active ulcerative colitis and Crohn’s disease. For ul...
PMC9379332
core_pubmed_pmc
Validation and clinical application of a method to quantify efavirenz in cervicovaginal secretions from flocked swabs using liquid chromatography tandem mass spectrometry
Validation and clinical application of a method to quantify efavirenz in cervicovaginal secretions from flocked swabs using liquid chromatography tandem mass spectrometry Abstract Abstract Background : A liquid chromatography tandem mass spectrometry method to quantify drugs in dried cervicovaginal secretions from floc...
PMC5216561
core_pubmed_pmc
A randomized, seven-day study to assess the efficacy and safety of a glycopyrrolate/formoterol fumarate fixed-dose combination metered dose inhaler using novel Co-Suspension™ Delivery Technology in patients with moderate-to-very severe chronic obstructive pulmonary disease
A randomized, seven-day study to assess the efficacy and safety of a glycopyrrolate/formoterol fumarate fixed-dose combination metered dose inhaler using novel Co-Suspension™ Delivery Technology in patients with moderate-to-very severe chronic obstructive pulmonary disease Abstract Background Long-acting muscarinic ant...
PMC8604223
core_pubmed_pmc
An open‐label, nonrandomized, phase Ib feasibility study of cusatuzumab in patients with nasopharyngeal carcinoma
An open‐label, nonrandomized, phase Ib feasibility study of cusatuzumab in patients with nasopharyngeal carcinoma Abstract Abstract CD70 is expressed in up to 80% of nasopharyngeal carcinoma (NPC) cases. Cusatuzumab is a humanized anti‐CD70 monoclonal antibody, with dual action mechanisms: induction of cytotoxicity aga...
PMC7447659
core_pubmed_pmc
Pharmacokinetics, Safety, and Tolerability of a 2-Month Dose Interval Regimen of the Long-Acting Injectable Antipsychotic Aripiprazole Lauroxil: Results From a 44-Week Phase I Study
Pharmacokinetics, Safety, and Tolerability of a 2-Month Dose Interval Regimen of the Long-Acting Injectable Antipsychotic Aripiprazole Lauroxil: Results From a 44-Week Phase I Study Abstract Abstract Background Aripiprazole lauroxil (AL) is a long-acting injectable antipsychotic approved for treatment of schizophrenia ...
PMC10703637
core_pubmed_pmc
Achillea millefolium : Mechanism of action, pharmacokinetic, clinical drug-drug interactions and tolerability
Achillea millefolium : Mechanism of action, pharmacokinetic, clinical drug-drug interactions and tolerability Abstract Background Achillea millefolium , known as Yarrow, is a medicinal plant in the Asteraceae family which is one of the oldest known botanicals used by humans and itis one of the most important medicinal ...
PMC6875038
core_pubmed_pmc
Comparative Pharmacokinetic Studies of Four Ginsenosides in Rat Plasma by UPLC-MS/MS after Oral Administration of Panax quinquefolius - Acorus gramineus and Panax quinquefolius Extracts
Comparative Pharmacokinetic Studies of Four Ginsenosides in Rat Plasma by UPLC-MS/MS after Oral Administration of Panax quinquefolius - Acorus gramineus and Panax quinquefolius Extracts Abstract Panax quinquefolius (PQ) and Acorus gramineus (AG) are drug target pairs in traditional Chinese medicine (TCM), which are use...
PMC4182452
core_pubmed_pmc
In Silico, Experimental, Mechanistic Model for Extended-Release Felodipine Disposition Exhibiting Complex Absorption and a Highly Variable Food Interaction
In Silico, Experimental, Mechanistic Model for Extended-Release Felodipine Disposition Exhibiting Complex Absorption and a Highly Variable Food Interaction Abstract The objective of this study was to develop and explore new, in silico experimental methods for deciphering complex, highly variable absorption and food int...
PMC10350552
core_pubmed_pmc
Investigation of the GnRH antagonist degarelix isomerization in biological matrices
Investigation of the GnRH antagonist degarelix isomerization in biological matrices Abstract Abstract One of the main objectives of peptide drug design is the improvement of peptide pharmacokinetics with maintaining biological activity, which can be achieved by the complex modifications of the primary structure of the ...
PMC10665255
core_pubmed_pmc
Posaconazole exposure in critically ill ICU patients: a need for action
Posaconazole exposure in critically ill ICU patients: a need for action Abstract Purpose Posaconazole is an antifungal drug currently being used for prophylaxis and treatment of invasive fungal infections such as aspergillosis. To date, therapeutic drug monitoring (TDM) of posaconazole is recommended with the use of or...