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PMC4407950
core_pubmed_pmc
Pharmacokinetics of Dolutegravir When Administered With Mineral Supplements in Healthy Adult Subjects
Pharmacokinetics of Dolutegravir When Administered With Mineral Supplements in Healthy Adult Subjects Abstract Abstract All commercially available integrase inhibitors are 2-metal binders and may be affected by co-administration with metal cations. The purpose of this study was to evaluate the effect of calcium and iro...
PMC10013581
core_pubmed_pmc
Effect of Food on the Pharmacokinetics and Safety of a Novel c-Met Inhibitor SCC244: A Randomized Phase I Study in Healthy Subjects
Effect of Food on the Pharmacokinetics and Safety of a Novel c-Met Inhibitor SCC244: A Randomized Phase I Study in Healthy Subjects Abstract Abstract Objective This study aimed to investigate the effect of food on the pharmacokinetics and safety profiles of SCC244, a novel oral c-Met inhibitor in healthy Chinese male s...
PMC10904421
core_pubmed_pmc
Pharmacokinetic–Pharmacodynamic Modelling in Hemophilia A: Relating Thrombin and Plasmin Generation to Factor VIII Activity After Administration of a VWF/FVIII Concentrate
Pharmacokinetic–Pharmacodynamic Modelling in Hemophilia A: Relating Thrombin and Plasmin Generation to Factor VIII Activity After Administration of a VWF/FVIII Concentrate Abstract Background Hemophilia A patients are treated with factor (F) VIII prophylactically to prevent bleeding. In general, dosage and frequency ar...
PMC11136736
core_pubmed_pmc
Employing zero-inflated beta distribution in an exposure-response analysis of TYK2/JAK1 inhibitor brepocitinib in patients with plaque psoriasis
Employing zero-inflated beta distribution in an exposure-response analysis of TYK2/JAK1 inhibitor brepocitinib in patients with plaque psoriasis Abstract Abstract Brepocitinib is an oral selective dual TYK2/JAK1 inhibitor and based on its cytokine inhibition profile is expected to provide therapeutic benefit in the tre...
PMC5760765
core_pubmed_pmc
Simultaneous determination of telmisartan and amlodipine in human plasma by LC–MS/MS and its application in a human pharmacokinetic study
Simultaneous determination of telmisartan and amlodipine in human plasma by LC–MS/MS and its application in a human pharmacokinetic study Abstract Abstract A rapid and sensitive liquid chromatography–tandem mass spectrometric (LC–MS/MS) assay method has been developed and fully validated for the simultaneous quantifica...
PMC3345231
core_pubmed_pmc
Short Communication: Is Ethanol-Based Hand Sanitizer Involved in Acute Pancreatitis after Excessive Disinfection?—An Evaluation with the Use of PBPK Model
Short Communication: Is Ethanol-Based Hand Sanitizer Involved in Acute Pancreatitis after Excessive Disinfection?—An Evaluation with the Use of PBPK Model Abstract Abstract An occupational physician reported to the French Health Products Safety Agency (Afssaps) a case of adverse effect of acute pancreatitis (AP) in a t...
PMC12911810
core_pubmed_pmc
Phase 1 open-label study of ASP9801, an oncolytic virus, in patients with advanced or metastatic solid tumors
Phase 1 open-label study of ASP9801, an oncolytic virus, in patients with advanced or metastatic solid tumors Abstract Abstract Purpose ASP9801, an oncolytic virus encoding interleukin-7 and interleukin-12, was assessed for safety, tolerability, pharmacokinetics, and antitumor activity in patients with advanced solid t...
PMC6027455
core_pubmed_pmc
Old Drugs as New Treatments for Neurodegenerative Diseases
Old Drugs as New Treatments for Neurodegenerative Diseases Abstract Neurodegenerative diseases are increasing in number, given that the general global population is becoming older. They manifest themselves through mechanisms that are not fully understood, in many cases, and impair memory, cognition and movement. Curren...
PMC7217345
core_pubmed_pmc
A phase I dose-escalation study of enzalutamide in combination with the AKT inhibitor AZD5363 (capivasertib) in patients with metastatic castration-resistant prostate cancer
A phase I dose-escalation study of enzalutamide in combination with the AKT inhibitor AZD5363 (capivasertib) in patients with metastatic castration-resistant prostate cancer Abstract Background Activation of the PI3K/AKT/mTOR pathway through loss of phosphatase and tensin homolog (PTEN) occurs in approximately 50% of p...
PMC12868287
core_pubmed_pmc
Gingerenone A attenuates diabetic vascular remodeling through AMPK/mTOR/S6K1 signaling
Gingerenone A attenuates diabetic vascular remodeling through AMPK/mTOR/S6K1 signaling Abstract Abstract Diabetes accelerates vascular remodeling and contributes to restenosis after revascularization, in part through oxidative stress-driven dysfunction of vascular smooth muscle cells (VSMCs). Gingerenone A (Gin A), a g...
PMC12823315
core_pubmed_pmc
Talazoparib Formulation Bridging in Cancer Patients—Challenges and the Critical Role of Model‐Informed Drug Development in Approval Despite Failed Bioequivalence
Talazoparib Formulation Bridging in Cancer Patients—Challenges and the Critical Role of Model‐Informed Drug Development in Approval Despite Failed Bioequivalence Abstract ABSTRACT Talazoparib is a poly(ADP‐ribose) polymerase inhibitor approved for the treatment of breast and prostate cancer. Commercialization of a soft...
PMC4314245
core_pubmed_pmc
Human Health Effects of Dichloromethane: Key Findings and Scientific Issues
Human Health Effects of Dichloromethane: Key Findings and Scientific Issues Abstract Abstract Background: The U.S. EPA’s Integrated Risk Information System (IRIS) completed an updated toxicological review of dichloromethane in November 2011. Objectives: In this commentary we summarize key results and issues of this rev...
PMC12756205
core_pubmed_pmc
Establishment of a Vancomycin Population Pharmacokinetic Model for Pediatric Patients Based on the Non-Linear Mixed-Effects Model
Establishment of a Vancomycin Population Pharmacokinetic Model for Pediatric Patients Based on the Non-Linear Mixed-Effects Model Abstract Background and Objectives Vancomycin (VCM) pharmacokinetic parameters vary widely between individuals. Existing models developed domestically and internationally may not apply unive...
PMC6352291
core_pubmed_pmc
A phase 1 clinical trial of the sigma-2 receptor complex allosteric antagonist CT1812, a novel therapeutic candidate for Alzheimer's disease
A phase 1 clinical trial of the sigma-2 receptor complex allosteric antagonist CT1812, a novel therapeutic candidate for Alzheimer's disease Abstract Background Elayta (CT1812) is a novel allosteric antagonist of the sigma-2 receptor complex that prevents and displaces binding of Aβ oligomers to neurons. By stopping a ...
PMC11992005
core_pubmed_pmc
Interoccasion variability in population pharmacokinetic models: identifiability, influence, interdependencies and derived study design recommendations
Interoccasion variability in population pharmacokinetic models: identifiability, influence, interdependencies and derived study design recommendations Abstract Abstract Modeling interoccasion variability (IOV) of pharmacokinetic parameters is challenging in sparse study designs. We conducted a simulation study with sto...
PMC9580069
core_pubmed_pmc
Cardiovascular Drug Interactions With Nirmatrelvir/Ritonavir in Patients With COVID-19
Cardiovascular Drug Interactions With Nirmatrelvir/Ritonavir in Patients With COVID-19 Abstract Abstract Nirmatrelvir-ritonavir (NMVr) is used to treat symptomatic, nonhospitalized patients with coronavirus disease-2019 (COVID-19) who are at high risk of progression to severe disease. Patients with cardiovascular risk ...
PMC8037814
core_pubmed_pmc
Polymorphic Characterization, Pharmacokinetics, and Anti-Inflammatory Activity of Ginsenoside Compound K Polymorphs
Polymorphic Characterization, Pharmacokinetics, and Anti-Inflammatory Activity of Ginsenoside Compound K Polymorphs Abstract Abstract Polymorphism exhibits different physicochemical properties, which can impact the bioavailability and bioactivity of solid drugs. This study focused on identifying the polymorphs of ginse...
PMC12811193
core_pubmed_pmc
A Phase 1 Open‐Label Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of a Single Intranasal Dose of Zavegepant in Healthy Chinese Adults
A Phase 1 Open‐Label Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of a Single Intranasal Dose of Zavegepant in Healthy Chinese Adults Abstract Abstract Zavegepant is the only calcitonin gene‐related peptide antagonist approved as a nasal spray in the United States for acute treatment of migraine in ...
PMC9143622
core_pubmed_pmc
The Chemical Scaffold of Theranostic Radiopharmaceuticals: Radionuclide, Bifunctional Chelator, and Pharmacokinetics Modifying Linker
The Chemical Scaffold of Theranostic Radiopharmaceuticals: Radionuclide, Bifunctional Chelator, and Pharmacokinetics Modifying Linker Abstract Therapeutic radiopharmaceuticals have been researched extensively in the last decade as a result of the growing research interest in personalized medicine to improve diagnostic ...
PMC8463782
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic profiles of baicalin against Mycoplasma gallisepticum in an in vivo infection model
Pharmacokinetic/pharmacodynamic profiles of baicalin against Mycoplasma gallisepticum in an in vivo infection model Abstract Mycoplasma gallisepticum ( M. gallisepticum ), a devastating avian pathogen that commonly causes chronic respiratory disease in chicken, is responsible for tremendous economic losses to the poult...
PMC9167810
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Dose Optimization of Cefiderocol during Continuous Renal Replacement Therapy
Pharmacokinetics, Pharmacodynamics, and Dose Optimization of Cefiderocol during Continuous Renal Replacement Therapy Abstract Abstract Background The need for continuous renal replacement therapy (CRRT) in critically ill patients with serious infections is associated with clinical failure, emergence of resistance, and ...
PMC6439167
core_pubmed_pmc
PF-06881893 (Nivestym™), a Filgrastim Biosimilar, Versus US-Licensed Filgrastim Reference Product (US-Neupogen ® ): Pharmacokinetics, Pharmacodynamics, Immunogenicity, and Safety of Single or Multiple Subcutaneous Doses in Healthy Volunteers
PF-06881893 (Nivestym™), a Filgrastim Biosimilar, Versus US-Licensed Filgrastim Reference Product (US-Neupogen ® ): Pharmacokinetics, Pharmacodynamics, Immunogenicity, and Safety of Single or Multiple Subcutaneous Doses in Healthy Volunteers Abstract Abstract Background Three comparative clinical studies assessed the p...
PMC11405193
core_pubmed_pmc
Drug-drug interaction between diltiazem and tacrolimus in relation to CYP3A5 genotype status in Chinese pediatric patients with nephrotic range proteinuria: a retrospective study
Drug-drug interaction between diltiazem and tacrolimus in relation to CYP3A5 genotype status in Chinese pediatric patients with nephrotic range proteinuria: a retrospective study Abstract Abstract Background Tacrolimus is widely used to treat pediatric nephrotic range proteinuria (NRP). Diltiazem, a CYP3A4/5 inhibitor,...
PMC10964439
core_pubmed_pmc
Improving Antimicrobial Resistance Awareness Among Medical Students in India: The Sensitization of Medical Students on Antimicrobial Resistance (SOS-AMR) Study
Improving Antimicrobial Resistance Awareness Among Medical Students in India: The Sensitization of Medical Students on Antimicrobial Resistance (SOS-AMR) Study Abstract OBJECTIVES To evaluate the impact of an online educational intervention on improving knowledge of antimicrobial resistance (AMR) and stewardship among ...
PMC8130027
core_pubmed_pmc
Immuno-pharmacokinetics of Meglumine Antimoniate in Patients With Cutaneous Leishmaniasis Caused by Leishmania ( Viannia )
Immuno-pharmacokinetics of Meglumine Antimoniate in Patients With Cutaneous Leishmaniasis Caused by Leishmania ( Viannia ) Abstract Abstract Background Control of cutaneous leishmaniasis (CL) relies on chemotherapy, yet gaps in our understanding of the determinants of therapeutic outcome impede optimization of antileis...
PMC9407455
core_pubmed_pmc
A specific JMJD6 inhibitor potently suppresses multiple types of cancers both in vitro and in vivo
A specific JMJD6 inhibitor potently suppresses multiple types of cancers both in vitro and in vivo Abstract Significance JMJD6 is overexpressed in multiple types of cancers and promotes tumorigenesis. The enzymatic activity of JMJD6 is often tightly linked to its cellular functions. Thus, development of effective inhib...
PMC7322761
core_pubmed_pmc
Current status of in vivo bioanalysis of nano drug delivery systems
Current status of in vivo bioanalysis of nano drug delivery systems Abstract The development of nano drug delivery systems (NDDSs) provides new approaches to fighting against diseases. The NDDSs are specially designed to serve as carriers for the delivery of active pharmaceutical ingredients (APIs) to their target site...
PMC10565503
core_pubmed_pmc
Optimization of the dosage regimen of zoledronic acid with a kinetic-pharmacodynamic model and exposure-response analysis
Optimization of the dosage regimen of zoledronic acid with a kinetic-pharmacodynamic model and exposure-response analysis Abstract Abstract Purpose: In order to support the dose optimization of zoledronic acid, the kinetic-pharmacodynamic model and exposure-response analysis were used to describe the changes in bone mi...
PMC10819079
core_pubmed_pmc
A Pharmacodynamic Study of Aminoglycosides against Pathogenic E. coli through Monte Carlo Simulation
A Pharmacodynamic Study of Aminoglycosides against Pathogenic E. coli through Monte Carlo Simulation Abstract Abstract This research focuses on combating the increasing problem of antimicrobial resistance, especially in Escherichia coli ( E. coli ), by assessing the efficacy of aminoglycosides. The study specifically a...
PMC12823327
core_pubmed_pmc
Exposure‐Response Analysis for Time‐to‐Event Data in the Presence of Adaptive Dosing: Efficient Approaches and Pitfalls
Exposure‐Response Analysis for Time‐to‐Event Data in the Presence of Adaptive Dosing: Efficient Approaches and Pitfalls Abstract ABSTRACT Analyzing exposure‐response (E‐R) relationships for time‐to‐event (TTE) endpoints presents challenges due to the inherent time‐dependent nature of the data. Some authors address thes...
PMC8919144
core_pubmed_pmc
Drug dosing in hospitalized obese patients with COVID-19
Drug dosing in hospitalized obese patients with COVID-19 Abstract Abstract Obesity is highly prevalent in hospitalized patients admitted with COVID-19. Evidence based guidelines are available for COVID-19-related therapies but dosing information specific to patients with obesity is lacking. Failure to account for the p...
PMC8313761
core_pubmed_pmc
Population Pharmacokinetics of High-Dose Methotrexate in Chinese Pediatric Patients With Acute Lymphoblastic Leukemia
Population Pharmacokinetics of High-Dose Methotrexate in Chinese Pediatric Patients With Acute Lymphoblastic Leukemia Abstract High-dose methotrexate (HD-MTX) is widely used in pediatric acute lymphoblastic leukemia (ALL) treatment regimens. In this study, we aimed to develop a population pharmacokinetic (PK) model of ...
PMC8277120
core_pubmed_pmc
The Spectrum of Mechanism-Oriented Models and Methods for Explanations of Biological Phenomena
The Spectrum of Mechanism-Oriented Models and Methods for Explanations of Biological Phenomena Abstract Developing and improving mechanism-oriented computational models to better explain biological phenomena is a dynamic and expanding frontier. As the complexity of targeted phenomena has increased, so too has the diver...
PMC2990584
core_pubmed_pmc
Phase Ib study of CP-868,596, a PDGFR inhibitor, combined with docetaxel with or without axitinib, a VEGFR inhibitor
Phase Ib study of CP-868,596, a PDGFR inhibitor, combined with docetaxel with or without axitinib, a VEGFR inhibitor Abstract Background: Tumoural interstitial hypertension, possibly modulated by platelet-derived and vascular endothelial growth factor receptors (PDGFR and VEGFR), may mediate resistance to chemotherapy....
PMC12631542
core_pubmed_pmc
In Vivo and In Silico Evaluation of a Polyphenol Fraction Extracted From Argania spinosa L. Press‐Cake Against Ethylene Glycol‐Induced Calcium Oxalate Urolithiasis in Rats: Biochemical, Histopathological, and Molecular Modeling Analyses
In Vivo and In Silico Evaluation of a Polyphenol Fraction Extracted From Argania spinosa L. Press‐Cake Against Ethylene Glycol‐Induced Calcium Oxalate Urolithiasis in Rats: Biochemical, Histopathological, and Molecular Modeling Analyses Abstract ABSTRACT In Morocco, Argania spinosa L. is traditionally used to treat kid...
PMC6383703
core_pubmed_pmc
First‐in‐Asian Phase I Study of the Anti‐Fibroblast Growth Factor 23 Monoclonal Antibody, Burosumab: Safety and Pharmacodynamics in Adults With X‐linked Hypophosphatemia
First‐in‐Asian Phase I Study of the Anti‐Fibroblast Growth Factor 23 Monoclonal Antibody, Burosumab: Safety and Pharmacodynamics in Adults With X‐linked Hypophosphatemia Abstract ABSTRACT X‐linked hypophosphatemia (XLH) is a disease caused by abnormally elevated FGF23 levels, which cause persistent hypophosphatemia acc...
PMC11363577
core_pubmed_pmc
Phase 0 trials/ Intra-Target-Microdosing (ITM) and the lung: a review
Phase 0 trials/ Intra-Target-Microdosing (ITM) and the lung: a review Abstract The COVID-19 pandemic has highlighted the importance of efficient drug discovery in respiratory disease. The traditional set up of clinical trials is expensive and allows for significant attrition of new drugs, many of which undergo extensiv...
PMC12069051
core_pubmed_pmc
Modification of biopharmaceutical parameters of flavonoids: a review
Modification of biopharmaceutical parameters of flavonoids: a review Abstract Flavonoids are natural organic compounds that are derivatives of diphenylpropane. This group of polyphenols can be found in multiple natural sources and they exhibit a variety of biological effects. Despite the wide array of beneficial proper...
PMC6226119
core_pubmed_pmc
Evaluation of the Cardiac Safety of Long‐Acting Endectocide Moxidectin in a Randomized Concentration‐QT Study
Evaluation of the Cardiac Safety of Long‐Acting Endectocide Moxidectin in a Randomized Concentration‐QT Study Abstract Abstract Potential effects on cardiac repolarization of single doses of moxidectin, a potent long‐acting macrocyclic lactone endectocide, were assessed in a concentration‐QT (c‐QT; exposure‐response) s...
PMC6700797
core_pubmed_pmc
Efficacy and safety of dihydroartemisinin–piperaquine for treatment of Plasmodium falciparum uncomplicated malaria in adult patients on antiretroviral therapy in Malawi and Mozambique: an open label non-randomized interventional trial
Efficacy and safety of dihydroartemisinin–piperaquine for treatment of Plasmodium falciparum uncomplicated malaria in adult patients on antiretroviral therapy in Malawi and Mozambique: an open label non-randomized interventional trial Abstract Background HIV-infected individuals on antiretroviral therapy (ART) require ...
PMC11913886
core_pubmed_pmc
Pharmacokinetic Profiles of Lansoprazole in Patients With Morbid Obesity Post‐Roux‐en‐Y Gastric Bypass Surgery
Pharmacokinetic Profiles of Lansoprazole in Patients With Morbid Obesity Post‐Roux‐en‐Y Gastric Bypass Surgery Abstract ABSTRACT Data on the effects of Roux‐en‐Y gastric bypass (RYGB) surgery on lansoprazole pharmacokinetics in morbidly obese patients are limited. This study aimed to evaluate the impact of RYGB surgery...
PMC9347938
core_pubmed_pmc
Complement blockade with eculizumab for treatment of severe Coronavirus Disease 2019 in pregnancy: A case series
Complement blockade with eculizumab for treatment of severe Coronavirus Disease 2019 in pregnancy: A case series Abstract Abstract Problem We evaluated eculizumab, a complement protein C5 inhibitor, for treatment of severe COVID‐19 in pregnant and postpartum individuals. Method of Study Protocol ECU‐COV‐401 (clinicaltr...
PMC3942469
core_pubmed_pmc
Evaluation of Fentanyl Disposition and Effects in Newborn Piglets as an Experimental Model for Human Neonates
Evaluation of Fentanyl Disposition and Effects in Newborn Piglets as an Experimental Model for Human Neonates Abstract Background Fentanyl is widely used off-label in NICU. Our aim was to investigate its cerebral, cardiovascular and pulmonary effects as well as pharmacokinetics in an experimental model for neonates. Me...
PMC12799729
core_pubmed_pmc
Concurrent Administration of Triazoles with Chemotherapeutic and/or Immunosuppressant Agents Known to Have Moderate-to-Severe Drug-Drug Interactions in Patients with Hematologic Malignancies Hospitalized for Invasive Aspergillosis
Concurrent Administration of Triazoles with Chemotherapeutic and/or Immunosuppressant Agents Known to Have Moderate-to-Severe Drug-Drug Interactions in Patients with Hematologic Malignancies Hospitalized for Invasive Aspergillosis Abstract Abstract Background Triazoles are widely used for treatment and prevention of in...
PMC12166256
core_pubmed_pmc
First‐in‐Human Single and Multiple Ascending Dose Studies of Balinatunfib, a Small Molecule Inhibitor of TNFR1 Signaling in Healthy Participants
First‐in‐Human Single and Multiple Ascending Dose Studies of Balinatunfib, a Small Molecule Inhibitor of TNFR1 Signaling in Healthy Participants Abstract Oral small molecule inhibitors of tumor necrosis factor alpha (TNFα) are emerging as attractive therapeutic agents for the treatment of various autoimmune diseases. B...
PMC8540413
core_pubmed_pmc
Population Pharmacokinetics of Levetiracetam and Dosing Evaluation in Critically Ill Patients with Normal or Augmented Renal Function
Population Pharmacokinetics of Levetiracetam and Dosing Evaluation in Critically Ill Patients with Normal or Augmented Renal Function Abstract Abstract Levetiracetam is a broad-spectrum antiepileptic drug commonly used in intensive care units (ICUs). The objective of this study is to evaluate the adequacy of levetirace...
PMC9107969
core_pubmed_pmc
Seizure Deterioration with Increased Levetiracetam Blood Concentration during the Postpartum Period in Refractory Temporal Lobe Epilepsy
Seizure Deterioration with Increased Levetiracetam Blood Concentration during the Postpartum Period in Refractory Temporal Lobe Epilepsy Abstract Abstract We evaluated a 39-year-old pregnant woman with right temporal lobe epilepsy. During the second trimester, seizure deterioration was responsive to an increased daily ...
PMC5642591
core_pubmed_pmc
Pharmacokinetics and drug-drug interaction between enalapril, enalaprilat and felodipine extended release (ER) in healthy subjects
Pharmacokinetics and drug-drug interaction between enalapril, enalaprilat and felodipine extended release (ER) in healthy subjects Abstract Since angiotensin-converting enzyme (ACE) inhibitors and calcium antagonists have complimentary mechanisms of action, enalapril, an ACE inhibitor, is used in combination with felod...
PMC10063703
core_pubmed_pmc
Phase I Study of Safety and Pharmacokinetics of RO7297089, an Anti-BCMA/CD16a Bispecific Antibody, in Patients with Relapsed, Refractory Multiple Myeloma
Phase I Study of Safety and Pharmacokinetics of RO7297089, an Anti-BCMA/CD16a Bispecific Antibody, in Patients with Relapsed, Refractory Multiple Myeloma Abstract Introduction This phase 1 trial assessed the safety, pharmacokinetics, and preliminary antitumor activity of RO7297089, an anti-BCMA/CD16a bispecific antibod...
PMC12960313
core_pubmed_pmc
A Mycophenolate Pharmacokinetic Study with New Insights into Enterohepatic Recirculation in Kidney Transplant Recipients
A Mycophenolate Pharmacokinetic Study with New Insights into Enterohepatic Recirculation in Kidney Transplant Recipients Abstract Background Mycophenolic acid (MPA) has complex pharmacokinetics in part due to enterohepatic recirculation (EHR). A deeper understanding of MPA pharmacokinetics and specifically how EHR and ...
PMC11801603
core_pubmed_pmc
Probing the role of Coniferin and Tetrahydrocurcumin from Traditional Chinese medicine against PSAT1 in early-stage ovarian cancer: An in silico study
Probing the role of Coniferin and Tetrahydrocurcumin from Traditional Chinese medicine against PSAT1 in early-stage ovarian cancer: An in silico study Abstract Ovarian cancer, a formidable gynaecological malignancy, poses a significant global health challenge, and it is characterised by late-stage diagnosis and a high ...
PMC11232576
core_pubmed_pmc
Modeling the Simultaneous Dynamics of Proteins in Blood Plasma and the Cerebrospinal Fluid in Human In Vivo
Modeling the Simultaneous Dynamics of Proteins in Blood Plasma and the Cerebrospinal Fluid in Human In Vivo Abstract Abstract The analysis of protein dynamics or turnover in patients has the potential to reveal altered protein recycling, such as in Alzheimer’s disease, and to provide informative data regarding drug eff...
PMC12691659
core_pubmed_pmc
Risk factors of daptomycin overexposure: a case-control study
Risk factors of daptomycin overexposure: a case-control study Abstract ABSTRACT In our institution, therapeutic drug monitoring of daptomycin is performed routinely and cases of high trough concentrations have been observed in patients without known risk factors. The aim of this study was to identify risk factors of da...
PMC2879679
core_pubmed_pmc
What Is Causing the Reduced Drug-Placebo Difference in Recent Schizophrenia Clinical Trials and What Can be Done About It?
What Is Causing the Reduced Drug-Placebo Difference in Recent Schizophrenia Clinical Trials and What Can be Done About It? Abstract Abstract On September 18, 2007, a collaborative session between the International Society for CNS Clinical Trials and Methodology and the International Society for CNS Drug Development was...
PMC11835425
core_pubmed_pmc
Safety, Pharmacokinetics, and Pharmacodynamics of a First‐in‐Class ClC‐1 Inhibitor to Enhance Muscle Excitability: Phase I Randomized Controlled Trial
Safety, Pharmacokinetics, and Pharmacodynamics of a First‐in‐Class ClC‐1 Inhibitor to Enhance Muscle Excitability: Phase I Randomized Controlled Trial Abstract Abstract NMD670 is a first‐in‐class inhibitor of skeletal muscle‐specific chloride channel ClC‐1, developed to improve muscle weakness and fatigue in neuromuscu...
PMC9515473
core_pubmed_pmc
Genetic determinants of apixaban plasma levels and their relationship to bleeding and thromboembolic events
Genetic determinants of apixaban plasma levels and their relationship to bleeding and thromboembolic events Abstract Apixaban is a direct oral anticoagulant, a factor Xa inhibitor, used for the prevention of ischemic stroke in patients with atrial fibrillation. Despite using recommended dosing a few patients might stil...
PMC8298376
core_pubmed_pmc
New insights into the mechanisms underlying 5-fluorouracil-induced intestinal toxicity based on transcriptomic and metabolomic responses in human intestinal organoids
New insights into the mechanisms underlying 5-fluorouracil-induced intestinal toxicity based on transcriptomic and metabolomic responses in human intestinal organoids Abstract 5-Fluorouracil (5-FU) is a widely used chemotherapeutical that induces acute toxicity in the small and large intestine of patients. Symptoms can...
PMC12829806
core_pubmed_pmc
Pharmacokinetics of Dolutegravir, nucleoside analogues, and intracellular metabolites using plasma separation cards: A comparative analysis with traditional sampling methods in healthy volunteers
Pharmacokinetics of Dolutegravir, nucleoside analogues, and intracellular metabolites using plasma separation cards: A comparative analysis with traditional sampling methods in healthy volunteers Abstract Abstract Objectives Adherence to antiretroviral therapy is essential for achieving viral suppression. Plasma separa...
PMC12342024
core_pubmed_pmc
Application of machine learning in combination with mechanistic modeling to predict plasma exposure of small molecules
Application of machine learning in combination with mechanistic modeling to predict plasma exposure of small molecules Abstract Abstract Prediction of a new molecule’s exposure in plasma is a critical first step toward understanding its efficacy/toxicity profile and concluding whether it is a possible first-in-class, b...
PMC9483652
core_pubmed_pmc
The rationale for development of ligelizumab in food allergy
The rationale for development of ligelizumab in food allergy Abstract Food allergy (FA) is a growing healthcare problem worldwide and the rising prevalence in many countries can be attributed to lifestyle, environmental, and nutritional changes. Immunoglobulin E (IgE)-mediated FA is the most common form of FA affecting...
PMC8425464
core_pubmed_pmc
Direct oral anticoagulant plasma levels in hospitalized COVID-19 patients treated with dexamethasone
Direct oral anticoagulant plasma levels in hospitalized COVID-19 patients treated with dexamethasone Abstract Direct oral anticoagulants (DOACs) are not recommended in COVID-19 patients receiving dexamethasone because of potential drug-drug and drug-disease interactions affecting anticoagulant concentration and activit...
PMC10517295
core_pubmed_pmc
A randomized, double‐blind, comparative study of the pharmacodynamics and pharmacokinetics of GP40141 (romiplostim biosimilar) and reference romiplostim in healthy male volunteers
A randomized, double‐blind, comparative study of the pharmacodynamics and pharmacokinetics of GP40141 (romiplostim biosimilar) and reference romiplostim in healthy male volunteers Abstract Abstract Aims The pharmacodynamic (PD) similarity between GP40141, a proposed romiplostim biosimilar, and reference romiplostim was...
PMC6047150
core_pubmed_pmc
Pharmacokinetic studies in children: recommendations for practice and research
Pharmacokinetic studies in children: recommendations for practice and research Abstract Abstract Optimising the dosing of medicines for neonates and children remains a challenge. The importance of pharmacokinetic (PK) and pharmacodynamic (PD) research is recognised both in medicines regulation and paediatric clinical p...
PMC12300969
core_pubmed_pmc
Supercomputing Multi-Ligand Modeling, Simulation, Wavelet Analysis and Surface Plasmon Resonance to Develop Novel Combination Drugs: A Case Study of Arbidol and Baicalein Against Main Protease of SARS-CoV-2
Supercomputing Multi-Ligand Modeling, Simulation, Wavelet Analysis and Surface Plasmon Resonance to Develop Novel Combination Drugs: A Case Study of Arbidol and Baicalein Against Main Protease of SARS-CoV-2 Abstract Abstract Background/Objectives : Combination therapies using traditional Chinese medicine and Western dr...
PMC12621197
core_pubmed_pmc
Development of Lipopeptides as Orthoflavivirin Inhibitors with Low Micromolar Broad-Spectrum Antiorthoflaviviral Activity
Development of Lipopeptides as Orthoflavivirin Inhibitors with Low Micromolar Broad-Spectrum Antiorthoflaviviral Activity Abstract Abstract Orthoflaviviral infections increasingly impact the global population; no specific therapeutic treatments are available. The orthoflaviviral protease NS2B-NS3 is a promising target ...
PMC10514676
core_pubmed_pmc
­Pharmacokinetics of antimalarial drugs used to treat uncomplicated malaria in breastfeeding mother-infant pairs: An observational pharmacokinetic study
­Pharmacokinetics of antimalarial drugs used to treat uncomplicated malaria in breastfeeding mother-infant pairs: An observational pharmacokinetic study Abstract Abstract Background: Data surrounding the exposure of the breastfed infant to drugs and any associated risks are sparse. Drugs usually are transferred to milk...
PMC3600728
core_pubmed_pmc
Comparisons of Analysis Methods for Proof-of-Concept Trials
Comparisons of Analysis Methods for Proof-of-Concept Trials Abstract Drug development struggles with high costs and time consuming processes. Hence, a need for new strategies has been accentuated by many stakeholders in drug development. This study proposes the use of pharmacometric models to rationalize drug developme...
PMC5564842
core_pubmed_pmc
Structural homologies between phenformin, lipitor and gleevec aim the same metabolic oncotarget in leukemia and melanoma
Structural homologies between phenformin, lipitor and gleevec aim the same metabolic oncotarget in leukemia and melanoma Abstract Phenformin's recently demonstrated efficacy in melanoma and Gleevec's demonstrated anti-proliferative action in chronic myeloid leukemia may lie within these drugs' significant pharmacokinet...
PMC9775493
core_pubmed_pmc
Identification of Potential Antimalarial Drug Candidates Targeting Falcipain-2 Protein of Malaria Parasite—A Computational Strategy
Identification of Potential Antimalarial Drug Candidates Targeting Falcipain-2 Protein of Malaria Parasite—A Computational Strategy Abstract Abstract Falcipain-2 (FP-2) is one of the main haemoglobinase of P. falciparum which is an important molecular target for the treatment of malaria. In this study, we have screened...
PMC3670858
core_pubmed_pmc
Effect of common single-nucleotide polymorphisms in acetylsalicylic acid metabolic pathway genes on platelet reactivity in patients with diabetes
Effect of common single-nucleotide polymorphisms in acetylsalicylic acid metabolic pathway genes on platelet reactivity in patients with diabetes Abstract Background Platelet reactivity in patients on acetylsalicylic acid (ASA) therapy can be influenced by physiological or pathological conditions affecting ASA pharmaco...
PMC11650862
core_pubmed_pmc
Linezolid Pharmacokinetic-Anemia Modeling in Children With Rifampicin-Resistant Tuberculosis
Linezolid Pharmacokinetic-Anemia Modeling in Children With Rifampicin-Resistant Tuberculosis Abstract Abstract Background Linezolid, a component of rifampicin-resistant/multidrug-resistant tuberculosis (RR/MDR-TB) treatment, is associated with treatment-limiting toxicities, including anemia. Patient-level and linezolid...
PMC8042450
core_pubmed_pmc
Effective delivery of STING agonist using exosomes suppresses tumor growth and enhances antitumor immunity
Effective delivery of STING agonist using exosomes suppresses tumor growth and enhances antitumor immunity Abstract The Stimulator of Interferon Genes (STING) pathway is implicated in the innate immune response and is important in both oncogenesis and cancer treatment. Specifically, activation of the cytosolic DNA sens...
PMC7859504
core_pubmed_pmc
Phase 2 trial to assess lebrikizumab in patients with idiopathic pulmonary fibrosis
Phase 2 trial to assess lebrikizumab in patients with idiopathic pulmonary fibrosis Abstract Abstract This phase 2, randomised, double-blind, placebo-controlled trial evaluated the efficacy and safety of lebrikizumab, an interleukin (IL)-13 monoclonal antibody, alone or with background pirfenidone therapy, in patients ...
PMC9215213
core_pubmed_pmc
Pharmacokinetics of Cannabidiol Following Intranasal, Intrarectal, and Oral Administration in Healthy Dogs
Pharmacokinetics of Cannabidiol Following Intranasal, Intrarectal, and Oral Administration in Healthy Dogs Abstract Abstract The therapeutic potential of cannabidiol (CBD), a non-psychtropic component of the Cannabis sativa plant, is substantiated more and more. We aimed to determine the pharmacokinetic behavior of CBD...
PMC10806681
core_pubmed_pmc
Intraperitoneal irinotecan with concomitant FOLFOX and bevacizumab for patients with unresectable colorectal peritoneal metastases: protocol of the multicentre, open-label, phase II, INTERACT-II trial
Intraperitoneal irinotecan with concomitant FOLFOX and bevacizumab for patients with unresectable colorectal peritoneal metastases: protocol of the multicentre, open-label, phase II, INTERACT-II trial Abstract Abstract Introduction The peritoneum is the second most affected organ for the dissemination of colorectal can...
PMC6983506
core_pubmed_pmc
Pharmacokinetics of intravenous and inhaled salbutamol and tobramycin: An exploratory study to investigate the potential of exhaled breath condensate as a matrix for pharmacokinetic analysis
Pharmacokinetics of intravenous and inhaled salbutamol and tobramycin: An exploratory study to investigate the potential of exhaled breath condensate as a matrix for pharmacokinetic analysis Abstract Abstract Concentrations of drugs acting in the lungs are difficult to measure, resulting in relatively unknown local pha...
PMC5225912
core_pubmed_pmc
Currently used dosage regimens of vancomycin fail to achieve therapeutic levels in approximately 40% of intensive care unit patients
Currently used dosage regimens of vancomycin fail to achieve therapeutic levels in approximately 40% of intensive care unit patients Abstract Abstract Objective This study aimed to assess whether currently used dosages of vancomycin for treatment of serious gram-positive bacterial infections in intensive care unit pati...
PMC11677230
core_pubmed_pmc
Passive accumulation of alkaloids in inconspicuously colored frogs refines the evolutionary paradigm of acquired chemical defenses
Passive accumulation of alkaloids in inconspicuously colored frogs refines the evolutionary paradigm of acquired chemical defenses Abstract Abstract Understanding the origins of novel, complex phenotypes is a major goal in evolutionary biology. Poison frogs of the family Dendrobatidae have evolved the novel ability to ...
PMC10046529
core_pubmed_pmc
Tigecycline Immunodetection Using Developed Group-Specific and Selective Antibodies for Drug Monitoring Purposes
Tigecycline Immunodetection Using Developed Group-Specific and Selective Antibodies for Drug Monitoring Purposes Abstract Tigecycline (TGC), a third-generation tetracycline, is characterized by a more potent and broad antibacterial activity, and the ability to overcome different mechanisms of tetracycline resistance. T...
PMC8465253
core_pubmed_pmc
A Physiologically Based Pharmacokinetic Model for Predicting Diazepam Pharmacokinetics after Intravenous, Oral, Intranasal, and Rectal Applications
A Physiologically Based Pharmacokinetic Model for Predicting Diazepam Pharmacokinetics after Intravenous, Oral, Intranasal, and Rectal Applications Abstract Abstract Diazepam is one of the most prescribed anxiolytic and anticonvulsant that is administered through intravenous (IV), oral, intramuscular, intranasal, and r...
PMC8308331
core_pubmed_pmc
Pharmacodynamics of Oral Cholecalciferol in Healthy Individuals with Vitamin D Deficiency: A Randomized Open-Label Study
Pharmacodynamics of Oral Cholecalciferol in Healthy Individuals with Vitamin D Deficiency: A Randomized Open-Label Study Abstract Comparative pharmacodynamic (PD) analyses on different dosing schedules for cholecalciferol supplementation are limited. This was an open-label, randomized, parallel-group study involving 75...
PMC8666590
core_pubmed_pmc
Drug Transporters in the Kidney: Perspectives on Species Differences, Disease Status, and Molecular Docking
Drug Transporters in the Kidney: Perspectives on Species Differences, Disease Status, and Molecular Docking Abstract Abstract The kidneys are a pair of important organs that excretes endogenous waste and exogenous biological agents from the body. Numerous transporters are involved in the excretion process. The levels o...
PMC6531394
core_pubmed_pmc
A Translational Quantitative Systems Pharmacology Model for CD3 Bispecific Molecules: Application to Quantify T Cell-Mediated Tumor Cell Killing by P-Cadherin LP DART ®
A Translational Quantitative Systems Pharmacology Model for CD3 Bispecific Molecules: Application to Quantify T Cell-Mediated Tumor Cell Killing by P-Cadherin LP DART ® Abstract Abstract CD3 bispecific antibody constructs recruit cytolytic T cells to kill tumor cells, offering a potent approach to treat cancer. T cell ...
PMC7558499
core_pubmed_pmc
Multiple use applicator for vaginal tablets/vaginal inserts: compliance verification and suitability studies
Multiple use applicator for vaginal tablets/vaginal inserts: compliance verification and suitability studies Abstract Background A newly developed multiple use applicator for vaginal tablets/vaginal inserts* was evaluated for its general suitability. There are no standard procedures described in guidelines or general a...
PMC3862509
core_pubmed_pmc
Characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles
Characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles Abstract The high aqueous solubility, poor permeability, and absorption of berberine (BBR) result in its low plasma level after oral administration, which greatly limits its clinical application. BBR solid lipid na...
PMC4102965
core_pubmed_pmc
Silicon-Containing GABA Derivatives, Silagaba Compounds, as Orally Effective Agents for Treating Neuropathic Pain without Central-Nervous-System-Related Side Effects
Silicon-Containing GABA Derivatives, Silagaba Compounds, as Orally Effective Agents for Treating Neuropathic Pain without Central-Nervous-System-Related Side Effects Abstract Abstract Neuropathic pain is a chronic condition resulting from neuronal damage. Pregabalin, the ( S )-isomer of 3-isobutyl-γ-aminobutyric acid (...
PMC11735194
core_pubmed_pmc
Randomized Multicenter Study to Evaluate the Efficacy and Safety of Fexuprazan According to the Timing of Dosing in Patients With Erosive Esophagitis
Randomized Multicenter Study to Evaluate the Efficacy and Safety of Fexuprazan According to the Timing of Dosing in Patients With Erosive Esophagitis Abstract Abstract Background/Aims Fexuprazan, a novel potassium-competitive acid blocker, was developed for treating acid-related disorders. Pharmacokinetic and pharmacod...
PMC11144975
core_pubmed_pmc
Proton Pump Inhibitors and Cyclin-Dependent Kinase 4/6 Inhibitors in Patients With Breast Cancer
Proton Pump Inhibitors and Cyclin-Dependent Kinase 4/6 Inhibitors in Patients With Breast Cancer Abstract Abstract Background Proton pump inhibitors (PPIs) reduce the bioavailability of several anticancer drugs. The impact of PPIs co-administered with cyclin-dependent kinase 4 and 6 inhibitors is controversial. We aime...
PMC6637297
core_pubmed_pmc
A Phase I Comparative Pharmacokinetic and Safety Study of Two Intravenous Formulations of Vinorelbine in Patients With Advanced Non-Small Cell Lung Cancer
A Phase I Comparative Pharmacokinetic and Safety Study of Two Intravenous Formulations of Vinorelbine in Patients With Advanced Non-Small Cell Lung Cancer Abstract Purpose: The aim of this study was to compare the pharmacokinetics and safety between two vinorelbine formulations [a new oil-in-water emulsion formulation ...
PMC12356476
core_pubmed_pmc
Transferrin conjugated pH/NIR-responsive black phosphorus nanoplatform: A novel multimodal approach for breast cancer theranostics
Transferrin conjugated pH/NIR-responsive black phosphorus nanoplatform: A novel multimodal approach for breast cancer theranostics Abstract Cancer is one of the foremost causes of death, posing a significant challenge to global health. Breast cancer is predominant cancer type in women globally. Nanotheranostic platform...
PMC11350887
core_pubmed_pmc
Pharmacokinetics of Doxycycline in Plasma and Milk after Intravenous and Intramuscular Administration in Dairy Goats
Pharmacokinetics of Doxycycline in Plasma and Milk after Intravenous and Intramuscular Administration in Dairy Goats Abstract Simple Summary Doxycycline is a tetracycline antibiotic used to treat bacterial infections in many species. Prior to the use of any antibacterial agent in veterinary medicine, pharmacokinetic st...
PMC6821791
core_pubmed_pmc
Phase I Trial of Pyragrel, a Novel Thromboxane Synthetase Inhibitor, to Evaluate the Safety, Tolerability, and Pharmacokinetics in Healthy Volunteers
Phase I Trial of Pyragrel, a Novel Thromboxane Synthetase Inhibitor, to Evaluate the Safety, Tolerability, and Pharmacokinetics in Healthy Volunteers Abstract Background and Objective: Inhibition of thrombosis and platelet aggregation through a thromboxane synthetase inhibitor proved to be an effective and promising tr...
PMC7965836
core_pubmed_pmc
Physiologically‐based pharmacokinetics modeling to investigate formulation factors influencing the generic substitution of dabigatran etexilate
Physiologically‐based pharmacokinetics modeling to investigate formulation factors influencing the generic substitution of dabigatran etexilate Abstract Abstract The exposure‐response relationship of direct acting oral anti‐coagulants (DOACs) for bleeding risk is steep relative to ischemic stroke reduction. As a result...
PMC6271780
core_pubmed_pmc
Determination of Bioactive Components in Chinese Herbal Formulae and Pharmacokinetics of Rhein in Rats by UPLC-MS/MS
Determination of Bioactive Components in Chinese Herbal Formulae and Pharmacokinetics of Rhein in Rats by UPLC-MS/MS Abstract Abstract Rhein (4,5-dihydroxy-9,10-dioxoanthracene-2-carboxylic acid, cassic acid) is a pharmacological active component found in Rheum palmatum L. the major herb of San-Huang-Xie-Xin-Tang (SHXX...
PMC3816925
core_pubmed_pmc
Needle-Free Jet Injection of Rapid-Acting Insulin Improves Early Postprandial Glucose Control in Patients With Diabetes
Needle-Free Jet Injection of Rapid-Acting Insulin Improves Early Postprandial Glucose Control in Patients With Diabetes Abstract Abstract OBJECTIVE Clamp studies have shown that the absorption and action of rapid-acting insulin are faster with injection by a jet injector than with administration by conventional pen. To...
PMC5578658
core_pubmed_pmc
Effects of arachidonyl-2’-chloroethylamide (ACEA) on the protective action of various antiepileptic drugs in the 6-Hz corneal stimulation model in mice
Effects of arachidonyl-2’-chloroethylamide (ACEA) on the protective action of various antiepileptic drugs in the 6-Hz corneal stimulation model in mice Abstract Abstract Accumulating evidence indicates that cannabinoid CB 1 receptor ligands play a pivotal role in seizures, not only in preclinical studies on animals, bu...
PMC8905711
core_pubmed_pmc
Peritransplantation ruxolitinib administration is safe and effective in patients with myelofibrosis: a pilot open-label study
Peritransplantation ruxolitinib administration is safe and effective in patients with myelofibrosis: a pilot open-label study Abstract Key Points Peritransplantation ruxolitinib was safe and well tolerated in patients with myelofibrosis, with MTD determined as 10 mg twice daily. Abstract We report results of our prospe...
PMC3522806
core_pubmed_pmc
The status of pharmacometrics in pregnancy: highlights from the 3rd American conference on pharmacometrics
The status of pharmacometrics in pregnancy: highlights from the 3rd American conference on pharmacometrics Abstract Abstract Physiological changes during pregnancy may alter drug pharmacokinetics. Therefore, mechanistic understanding of these changes and, ultimately, clinical studies in pregnant women are necessary to ...
PMC8300333
core_pubmed_pmc
In silico identification of natural products from Centella asiatica as severe acute respiratory syndromecoronavirus 2 main protease inhibitor
In silico identification of natural products from Centella asiatica as severe acute respiratory syndromecoronavirus 2 main protease inhibitor Abstract Severe acute respiratory syndrome-coronavirus 2 (SARS-CoV-2) main protease (S-CoV-2 Mpro) is one of the main targets in designing antiviral against SARS-CoV-2. Centella ...
PMC4579248
core_pubmed_pmc
Assessment of Alcohol-Induced Dose Dumping with a Hydrocodone Bitartrate Extended-Release Tablet Formulated with CIMA ® Abuse Deterrence Technology
Assessment of Alcohol-Induced Dose Dumping with a Hydrocodone Bitartrate Extended-Release Tablet Formulated with CIMA ® Abuse Deterrence Technology Abstract Abstract Background Greater drug content requirements for extended-release (ER) opioids necessitate greater protection against dose dumping. Hydrocodone ER employs...