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PMC12865717 | core_pubmed_pmc | Commentary: Immunogenicity of dupilumab in adult and pediatric patients with atopic dermatitis | Commentary: Immunogenicity of dupilumab in adult and pediatric patients with atopic dermatitis Statistical Analysis Reliance on descriptive statistics The investigators relied primarily on descriptive summaries, which cannot disentangle relationships among ADA formation, pharmacokinetics, and clinical outcomes. Inferen... |
PMC12489000 | core_pubmed_pmc | Structural and energetic basis of marine phytochemicals as dengue NS1 protein inhibitors | Structural and energetic basis of marine phytochemicals as dengue NS1 protein inhibitors Abstract Dengue, spread by Aedes aegypti and Aedes albopictus , causes 390 million infections, 50 million illnesses, and 24,000 fatalities, including over 4.5 million in 2023. This work finds DENV NS1 protein anti-virals beyond CYD... |
PMC4958143 | core_pubmed_pmc | Isavuconazole Population Pharmacokinetic Analysis Using Nonparametric Estimation in Patients with Invasive Fungal Disease (Results from the VITAL Study) | Isavuconazole Population Pharmacokinetic Analysis Using Nonparametric Estimation in Patients with Invasive Fungal Disease (Results from the VITAL Study) Abstract Isavuconazonium sulfate (Cresemba; Astellas Pharma Inc.), a water-soluble prodrug of the triazole antifungal agent isavuconazole, is available for the treatme... |
PMC11741474 | core_pubmed_pmc | Influence of solvent, sex, and age on pharmacokinetic and acute behavioral effects of vaporized cannabis extract in mice | Influence of solvent, sex, and age on pharmacokinetic and acute behavioral effects of vaporized cannabis extract in mice Abstract Abstract The legalization of cannabis in several states across the US has increased the need to better understand its effects on the body, brain, and behavior, particularly in different popu... |
PMC4898033 | core_pubmed_pmc | Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions | Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions Abstract The purpose of this study was to prepare Brucea javanica oil cationic nanoemulsions (BJO-CN) with BJO as drug as well as oil phase and chitosan as cationic inducer, to explore the practical suitabili... |
PMC11963282 | core_pubmed_pmc | Modified titration of donanemab reduces ARIA risk and maintains amyloid reduction | Modified titration of donanemab reduces ARIA risk and maintains amyloid reduction Abstract Abstract INTRODUCTION TRAILBLAZER‐ALZ 6 ( NCT05738486 ) is a multicenter, double‐blind, ongoing phase 3b study in early symptomatic Alzheimer's disease. METHODS Participants ( n = 843) were randomized 1:1:1:1 (standard + three al... |
PMC6407021 | core_pubmed_pmc | Potential Role of Flavonoids in Treating Chronic Inflammatory Diseases with a Special Focus on the Anti-Inflammatory Activity of Apigenin | Potential Role of Flavonoids in Treating Chronic Inflammatory Diseases with a Special Focus on the Anti-Inflammatory Activity of Apigenin Abstract Inflammation has been reported to be intimately linked to the development or worsening of several non-infectious diseases. A number of chronic conditions such as cancer, dia... |
PMC10862873 | core_pubmed_pmc | Cardiovascular and Locomotor Effects of Binary Mixtures of Common “Bath Salts” Constituents: Studies with Methylone, MDPV, and Caffeine in Rats | Cardiovascular and Locomotor Effects of Binary Mixtures of Common “Bath Salts” Constituents: Studies with Methylone, MDPV, and Caffeine in Rats Abstract Abstract Background and Purpose: The use of “Bath Salts” drug preparations has been associated with high rates of toxicity and death. Preparations often contain mixtur... |
PMC4497360 | core_pubmed_pmc | A randomized cross-over comparison of short-term exposure of once-daily extended release tacrolimus and twice-daily tacrolimus on renal function in healthy volunteers | A randomized cross-over comparison of short-term exposure of once-daily extended release tacrolimus and twice-daily tacrolimus on renal function in healthy volunteers Abstract Calcineurin inhibitor nephrotoxicity remains an issue for transplant recipients. The pharmacokinetic profile (PK) of the once-daily tacrolimus e... |
PMC4284724 | core_pubmed_pmc | Polymer Coated CaAl-Layered Double Hydroxide Nanomaterials for Potential Calcium Supplement | Polymer Coated CaAl-Layered Double Hydroxide Nanomaterials for Potential Calcium Supplement Abstract Abstract We have successfully prepared layered double hydroxide (LDH) nanomaterials containing calcium and aluminum ions in the framework (CaAl-LDH). The surface of CaAl-LDH was coated with enteric polymer, Eudragit ® L... |
PMC9843304 | core_pubmed_pmc | Target concentration achievement for efficacy and safety of patients with osteosarcoma treated with high-dose methotrexate based on individual pharmacokinetics: A retrospective study | Target concentration achievement for efficacy and safety of patients with osteosarcoma treated with high-dose methotrexate based on individual pharmacokinetics: A retrospective study Abstract In the high-dose methotrexate (HD-MTX) treatment of patients with osteosarcoma, a dose-adjustment method using individual pharma... |
PMC11266315 | core_pubmed_pmc | Population Pharmacokinetic Modeling of Abacavir/Dolutegravir/Lamivudine to Support a Fixed-Dose Combination in Children with HIV-1 | Population Pharmacokinetic Modeling of Abacavir/Dolutegravir/Lamivudine to Support a Fixed-Dose Combination in Children with HIV-1 Abstract Abstract Introduction Once-daily fixed-dose combinations (FDC) containing abacavir (ABC), dolutegravir (DTG), and lamivudine (3TC) have been approved in the US for adults and child... |
PMC8895218 | core_pubmed_pmc | Kinetics of iron absorption from ferrous fumarate with and without galacto-oligosaccharides determined from stable isotope appearance curves in women | Kinetics of iron absorption from ferrous fumarate with and without galacto-oligosaccharides determined from stable isotope appearance curves in women Abstract ABSTRACT Background Prebiotic galacto-oligosaccharides (GOS) are novel enhancers of iron absorption from ferrous fumarate (FeFum). However, the mechanism(s) of t... |
PMC6590304 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of dapagliflozin in combination with insulin in Japanese patients with type 1 diabetes | Pharmacokinetics and pharmacodynamics of dapagliflozin in combination with insulin in Japanese patients with type 1 diabetes Abstract Abstract Aims To assess the pharmacokinetics/pharmacodynamics (PK/PD) of dapagliflozin, a sodium‐glucose co‐transporter 2 inhibitor that increases urinary glucose excretion (UGE) and its... |
PMC12452009 | core_pubmed_pmc | Dual character of surface engineering on SN38 prodrug nano-assemblies: divergent effects on in vitro and in vivo behavior | Dual character of surface engineering on SN38 prodrug nano-assemblies: divergent effects on in vitro and in vivo behavior Abstract Abstract Background Surface engineering has emerged as a promising strategy to enhance the performance of nanomedicines. In particular, the PEGylation levels for chemotherapy drug 7-Ethyl-1... |
PMC8685414 | core_pubmed_pmc | Therapeutic Drug Monitoring and Individualized Medicine of Dasatinib: Focus on Clinical Pharmacokinetics and Pharmacodynamics | Therapeutic Drug Monitoring and Individualized Medicine of Dasatinib: Focus on Clinical Pharmacokinetics and Pharmacodynamics Abstract Abstract Dasatinib is an oral second-generation tyrosine kinase inhibitor known to be used widely in Philadelphia chromosome-positive (Ph + ) chronic myeloid leukemia (CML) and Ph + acu... |
PMC9303366 | core_pubmed_pmc | Plasma concentrations of methylphenidate enantiomers in adults with ADHD and substance use disorder, with focus on high doses and relationship to carboxylesterase activity | Plasma concentrations of methylphenidate enantiomers in adults with ADHD and substance use disorder, with focus on high doses and relationship to carboxylesterase activity Abstract Abstract Scarce data are available on methylphenidate (MPH) plasma concentrations reached after doses higher than 180 mg. The interindividu... |
PMC5435348 | core_pubmed_pmc | Modelling of the cancer cell cycle as a tool for rational drug development: A systems pharmacology approach to cyclotherapy | Modelling of the cancer cell cycle as a tool for rational drug development: A systems pharmacology approach to cyclotherapy Abstract The dynamic of cancer is intimately linked to a dysregulation of the cell cycle and signalling pathways. It has been argued that selectivity of treatments could exploit loss of checkpoint... |
PMC12566152 | core_pubmed_pmc | The Genetic Polymorphisms of CYP2C9 and VKORC1 in the Saudi Population and Their Impact on Anticoagulant Management | The Genetic Polymorphisms of CYP2C9 and VKORC1 in the Saudi Population and Their Impact on Anticoagulant Management Abstract Abstract Background and objectives : Warfarin is a commonly used anticoagulant with a narrow therapeutic index that requires a precise dose to achieve efficacy and safety. Genetic variations in t... |
PMC8460590 | core_pubmed_pmc | Hepatic drug-metabolizing enzymes and drug transporters in Wilson’s disease patients with liver failure | Hepatic drug-metabolizing enzymes and drug transporters in Wilson’s disease patients with liver failure Abstract Background Wilson’s disease is a genetic disorder inherited in a recessive manner, caused by mutations in the copper-transporter ATP7B. Although it is a well-known disease, currently available treatments are... |
PMC10298085 | core_pubmed_pmc | Optimization of Potential Nanoemulgels for Boosting Transdermal Glimepiride Delivery and Upgrading Its Anti-Diabetic Activity | Optimization of Potential Nanoemulgels for Boosting Transdermal Glimepiride Delivery and Upgrading Its Anti-Diabetic Activity Abstract Abstract Transdermal drug delivery has been widely adopted as a plausible alternative to the oral route of administration, especially for drugs with poor systemic bioavailability. The o... |
PMC3889190 | core_pubmed_pmc | Development of a Positive-readout Mouse Model of siRNA Pharmacodynamics | Development of a Positive-readout Mouse Model of siRNA Pharmacodynamics Abstract Development of RNAi-based therapeutics has the potential to revolutionize treatment options for a range of human diseases. However, as with gene therapy, a major barrier to progress is the lack of methods to achieve and measure efficient d... |
PMC10363543 | core_pubmed_pmc | Characterization of the central nervous system penetrant and selective purine P2X7 receptor antagonist JNJ-54175446 in patients with major depressive disorder | Characterization of the central nervous system penetrant and selective purine P2X7 receptor antagonist JNJ-54175446 in patients with major depressive disorder Abstract JNJ-54175446 is a selective purine P2X7 receptor (P2X7R) antagonist that attenuates microglial IL-1β/IL-18 release. In healthy volunteers, JNJ-54175446 ... |
PMC9659592 | core_pubmed_pmc | MLN2238 exerts its anti-tumor effects via regulating ROS/JNK/mitochondrial signaling pathways in intrahepatic cholangiocarcinoma | MLN2238 exerts its anti-tumor effects via regulating ROS/JNK/mitochondrial signaling pathways in intrahepatic cholangiocarcinoma Abstract Abstract Background: Intrahepatic Cholangiocarcinoma (iCCA) is a highly malignant tumor with limited treatment options that contributes largely to cancer-related deaths worldwide. Co... |
PMC12405466 | core_pubmed_pmc | Pharmacokinetic Assessment of Drug Efflux from Erythrocytes Loaded with Corticosteroid Esters | Pharmacokinetic Assessment of Drug Efflux from Erythrocytes Loaded with Corticosteroid Esters Abstract Abstract Purpose Drugs can be found in erythrocytes (RBC) in accordance with their physicochemical and specific binding properties, but particularly high concentrations can be attained using an ex vivo hypotonic pre-s... |
PMC7618164 | core_pubmed_pmc | D3/Penta 21 clinical trial design: a randomised non-inferiority trial with nested drug licensing substudy to assess dolutegravir and lamivudine fixed dose formulations for the maintenance of virological suppression in children with HIV-1 infection, aged 2 to 15 years | D3/Penta 21 clinical trial design: a randomised non-inferiority trial with nested drug licensing substudy to assess dolutegravir and lamivudine fixed dose formulations for the maintenance of virological suppression in children with HIV-1 infection, aged 2 to 15 years Abstract Background There is increasing interest in ... |
PMC6311004 | core_pubmed_pmc | Systems biology approaches in the study of Chinese herbal formulae | Systems biology approaches in the study of Chinese herbal formulae Abstract Abstract Systems biology is an academic field that attempts to integrate different levels of information to understand how biological systems function. It is the study of the composition of all components of a biological system and their intera... |
PMC7794789 | core_pubmed_pmc | Evaluation of the Physicochemical Properties, Pharmacokinetics, and In Vitro Anticancer Effects of Docetaxel and Osthol Encapsulated in Methoxy Poly(ethylene glycol)- b -Poly(caprolactone) Polymeric Micelles | Evaluation of the Physicochemical Properties, Pharmacokinetics, and In Vitro Anticancer Effects of Docetaxel and Osthol Encapsulated in Methoxy Poly(ethylene glycol)- b -Poly(caprolactone) Polymeric Micelles Abstract Abstract Docetaxel (DTX), a taxane-based anticancer drug, and osthol (OTH), a coumarin-derivative compo... |
PMC10633951 | core_pubmed_pmc | Lacosamide dosing in patients receiving continuous renal replacement therapy | Lacosamide dosing in patients receiving continuous renal replacement therapy Abstract Background Lacosamide is one of the anticonvulsants used in critically ill patients. This study aimed to suggest appropriate lacosamide dosing regimens in critically ill patients receiving continuous renal replacement therapy (CRRT) v... |
PMC4006832 | core_pubmed_pmc | Efficacy of a Metalloproteinase Inhibitor in Spinal Cord Injured Dogs | Efficacy of a Metalloproteinase Inhibitor in Spinal Cord Injured Dogs Abstract Matrix metalloproteinase-9 is elevated within the acutely injured murine spinal cord and blockade of this early proteolytic activity with GM6001, a broad-spectrum matrix metalloproteinase inhibitor, results in improved recovery after spinal ... |
PMC8959326 | core_pubmed_pmc | Effects of berberine on the pharmacokinetics of florfenicol and levels of cytochrome P450 3A37, multidrug resistance 1, and chicken xenobiotic‐sensing orphan nuclear receptor mRNA expression in broilers | Effects of berberine on the pharmacokinetics of florfenicol and levels of cytochrome P450 3A37, multidrug resistance 1, and chicken xenobiotic‐sensing orphan nuclear receptor mRNA expression in broilers Abstract Abstract Background Berberine (BBR) is always used in combination with florfenicol for treating avian in Chi... |
PMC6132367 | core_pubmed_pmc | Innovation at the Intersection of Clinical Trials and Real‐World Data Science to Advance Patient Care | Innovation at the Intersection of Clinical Trials and Real‐World Data Science to Advance Patient Care Abstract Abstract While efficacy and safety data collected from randomized clinical trials are the evidentiary standard for determining market authorization, this alone may no longer be sufficient to address the needs ... |
PMC8765298 | core_pubmed_pmc | Emergence of Resistance in HIV-1 Integrase with Dolutegravir Treatment in a Pediatric Population from the IMPAACT P1093 Study | Emergence of Resistance in HIV-1 Integrase with Dolutegravir Treatment in a Pediatric Population from the IMPAACT P1093 Study Abstract ABSTRACT P1093 is a multicenter, open-label, phase I/II study of pharmacokinetics, safety, and tolerability of dolutegravir plus an optimized background regimen in pediatric participant... |
PMC12508957 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Efavirenz Nanoparticles: from Animal Model to Human Extrapolation | Physiologically Based Pharmacokinetic Modeling of Efavirenz Nanoparticles: from Animal Model to Human Extrapolation Abstract The present work aims to establish a formulation-specific, physiologically based pharmacokinetic (PBPK) model for efavirenz (EFV) nanocrystals that have shown increased dissolution and were produ... |
PMC5082287 | core_pubmed_pmc | Characterisation of equine satellite cell transcriptomic profile response to β -hydroxy- β -methylbutyrate (HMB) | Characterisation of equine satellite cell transcriptomic profile response to β -hydroxy- β -methylbutyrate (HMB) Abstract Abstract β -Hydroxy- β -methylbutyrate (HMB) is a popular ergogenic aid used by human athletes and as a supplement to sport horses, because of its ability to aid muscle recovery, improve performance... |
PMC12013038 | core_pubmed_pmc | Current progress and remaining challenges of peptide–drug conjugates (PDCs): next generation of antibody-drug conjugates (ADCs)? | Current progress and remaining challenges of peptide–drug conjugates (PDCs): next generation of antibody-drug conjugates (ADCs)? Abstract Abstract Drug conjugates have emerged as a promising alternative delivery system designed to deliver an ultra-toxic payload directly to the target cancer cells, maximizing therapeuti... |
PMC11706417 | core_pubmed_pmc | Population pharmacokinetic modeling of zavegepant, a calcitonin gene‐related peptide receptor antagonist, in healthy adults and patients with migraine | Population pharmacokinetic modeling of zavegepant, a calcitonin gene‐related peptide receptor antagonist, in healthy adults and patients with migraine Abstract Abstract Zavegepant (ZAVZPRET™) is a high‐affinity, selective, small‐molecule calcitonin gene‐related peptide receptor antagonist available for acute treatment ... |
PMC7860987 | core_pubmed_pmc | Pharmacokinetics and Efficacy of a Potential Smallpox Therapeutic, Brincidofovir, in a Lethal Monkeypox Virus Animal Model | Pharmacokinetics and Efficacy of a Potential Smallpox Therapeutic, Brincidofovir, in a Lethal Monkeypox Virus Animal Model Abstract Preparedness activities against highly transmissible viruses with high mortality rates have been highlighted during the ongoing coronavirus disease 2019 (COVID-19) pandemic. Smallpox, caus... |
PMC9286722 | core_pubmed_pmc | Deep compartment models: A deep learning approach for the reliable prediction of time‐series data in pharmacokinetic modeling | Deep compartment models: A deep learning approach for the reliable prediction of time‐series data in pharmacokinetic modeling Abstract Abstract Nonlinear mixed effect (NLME) models are the gold standard for the analysis of patient response following drug exposure. However, these types of models are complex and time‐con... |
PMC10420659 | core_pubmed_pmc | Comparative Molecular Characterization and Pharmacokinetics of IgG1-Fc and Engineered Fc Human Antibody Variants to Insulin-like Growth Factor 2 Receptor (IGF2R) | Comparative Molecular Characterization and Pharmacokinetics of IgG1-Fc and Engineered Fc Human Antibody Variants to Insulin-like Growth Factor 2 Receptor (IGF2R) Abstract Abstract Novel therapeutic approaches are much needed for the treatment of osteosarcoma. Targeted radionuclide therapy (TRT) and radioimmunotherapy (... |
PMC4689483 | core_pubmed_pmc | The Molecular Engineering of an Anti-Idiotypic Antibody for Pharmacokinetic Analysis of a Fully Human Anti-Infective | The Molecular Engineering of an Anti-Idiotypic Antibody for Pharmacokinetic Analysis of a Fully Human Anti-Infective Abstract Abstract Anti-idiotype monoclonal antibodies represent a class of reagents that are potentially optimal for analyzing the pharmacokinetics of fully human, anti-infective antibodies that have bee... |
PMC7495280 | core_pubmed_pmc | The effects of aripiprazole and olanzapine on pupillary light reflex and its relationship with pharmacogenetics in a randomized multiple‐dose trial | The effects of aripiprazole and olanzapine on pupillary light reflex and its relationship with pharmacogenetics in a randomized multiple‐dose trial Abstract Aims Pupillography is a noninvasive and cost‐effective method to determine autonomic nerve activity. Genetic variants in cytochrome P450 ( CYP ), dopamine receptor... |
PMC12910912 | core_pubmed_pmc | Evaluation of adalimumab tapering regimens in children and adolescents with juvenile idiopathic arthritis in remission: a simulation study | Evaluation of adalimumab tapering regimens in children and adolescents with juvenile idiopathic arthritis in remission: a simulation study Abstract Abstract Background Adalimumab (ADM) in children with juvenile idiopathic arthritis (JIA) is usually dosed using fixed weight-based bands (label dosing: 20 mg for < 30 kg, ... |
PMC6676194 | core_pubmed_pmc | Population pharmacokinetic analysis of linezolid in patients with different types of shock: Effect of platelet count | Population pharmacokinetic analysis of linezolid in patients with different types of shock: Effect of platelet count Abstract Linezolid was approved by the Food and Drug Administration for the treatment of serious infections. However, patients with serious frequently develop shock, and it is currently elusive whether s... |
PMC4281952 | core_pubmed_pmc | Antibiotic stewardship in the intensive care unit | Antibiotic stewardship in the intensive care unit Abstract The rapid emergence and dissemination of antimicrobial-resistant microorganisms in ICUs worldwide constitute a problem of crisis dimensions. The root causes of this problem are multifactorial, but the core issues are clear. The emergence of antibiotic resistanc... |
PMC4099389 | core_pubmed_pmc | Serum TFF3 may be a pharamcodynamic marker of responses to chemotherapy in gastrointestinal cancers | Serum TFF3 may be a pharamcodynamic marker of responses to chemotherapy in gastrointestinal cancers Abstract Abstract Background As a secreted protein, serum trefoil factor 3 (TFF3) has been reported to be a biomarker of several malignancies. We further investigated whether TFF3 can be applied as a biomarker for and pr... |
PMC4452934 | core_pubmed_pmc | Integration of Physiologically-Based Pharmacokinetic Modeling into Early Clinical Development: An Investigation of the Pharmacokinetic Nonlinearity | Integration of Physiologically-Based Pharmacokinetic Modeling into Early Clinical Development: An Investigation of the Pharmacokinetic Nonlinearity Abstract BMS-911543, a promising anticancer agent, exhibited time-dependent and dose-dependent nonlinear pharmacokinetics (PKs) in its first-in-human (FIH) study. Initial p... |
PMC4787092 | core_pubmed_pmc | Modulation of Hepatic Cytochrome P450 Enzymes by Curcumin and its Pharmacokinetic Consequences in Sprague–dawley Rats | Modulation of Hepatic Cytochrome P450 Enzymes by Curcumin and its Pharmacokinetic Consequences in Sprague–dawley Rats Abstract Background: Curcumin (CUR) is a polyphenolic component derived from an herbal remedy and dietary spice turmeric ( Curcuma longa ). Objective: The aim of this study was to investigate inhibitory... |
PMC7156464 | core_pubmed_pmc | 5-Azacytidine inhaled dry powder formulation profoundly improves pharmacokinetics and efficacy for lung cancer therapy through genome reprogramming | 5-Azacytidine inhaled dry powder formulation profoundly improves pharmacokinetics and efficacy for lung cancer therapy through genome reprogramming Abstract Abstract Background Epigenetic therapy through demethylation of 5-methylcytosine has been largely ineffective in treating lung cancer, most likely due to poor tiss... |
PMC7653765 | core_pubmed_pmc | Pharmacodynamics and pharmacokinetics of a new type of recombinant insulin Lisargine injection | Pharmacodynamics and pharmacokinetics of a new type of recombinant insulin Lisargine injection Abstract Abstract Background Recombinant insulin Lisargine is a new type of insulin. In this study, we aimed to compare its pharmacodynamic (PD) and pharmacokinetic (PK) with Lantus. Methods The PD test was performed by explo... |
PMC6468623 | core_pubmed_pmc | Liposomal Irinotecan for Treatment of Colorectal Cancer in a Preclinical Model | Liposomal Irinotecan for Treatment of Colorectal Cancer in a Preclinical Model Abstract Colorectal cancer (CRC) is the most frequently diagnosed cancer and leading cause of cancer-related deaths worldwide. Because of the use of first-line CRC treatments, such as irinotecan (IRI), is hindered by dose-limiting side effec... |
PMC6032846 | core_pubmed_pmc | Randomized, controlled study of bleselumab (ASKP1240) pharmacokinetics and safety in patients with moderate‐to‐severe plaque psoriasis | Randomized, controlled study of bleselumab (ASKP1240) pharmacokinetics and safety in patients with moderate‐to‐severe plaque psoriasis Abstract Abstract This study evaluated the pharmacokinetics (PK), efficacy, safety, and tolerability of bleselumab – a fully‐human anti‐CD40 monoclonal recombinant IgG4. Patients with m... |
PMC10127017 | core_pubmed_pmc | Cerebrospinal fluid penetration of fosfomycin in patients with ventriculitis: an observational study | Cerebrospinal fluid penetration of fosfomycin in patients with ventriculitis: an observational study Abstract Abstract Background For treatment of ventriculitis, vancomycin and meropenem are frequently used as empiric treatment but cerebrospinal fluid (CSF) penetration is highly variable and may result in subtherapeuti... |
PMC10043246 | core_pubmed_pmc | Combined quantitative tuberculosis biomarker model for time-to-positivity and colony forming unit to support tuberculosis drug development | Combined quantitative tuberculosis biomarker model for time-to-positivity and colony forming unit to support tuberculosis drug development Abstract Abstract Biomarkers are quantifiable characteristics of biological processes. In Mycobacterium tuberculosis , common biomarkers used in clinical drug development are colony... |
PMC11970618 | core_pubmed_pmc | Oral delivery of the non-β-blocking R-carvedilol enantiomer for skin cancer chemoprevention in SKH-1 mice | Oral delivery of the non-β-blocking R-carvedilol enantiomer for skin cancer chemoprevention in SKH-1 mice Abstract Purpose Skin cancer remains the most prevalent cancer worldwide with its incidence continuously rising. Previous studies have demonstrated the efficacy of the β-blocker carvedilol and its non-β-blocking en... |
PMC9410668 | core_pubmed_pmc | Pharmacodynamic evaluation of piperacillin/tazobactam versus meropenem against extended-spectrum β-lactamase-producing and non-producing Escherichia coli clinical isolates in a hollow-fibre infection model | Pharmacodynamic evaluation of piperacillin/tazobactam versus meropenem against extended-spectrum β-lactamase-producing and non-producing Escherichia coli clinical isolates in a hollow-fibre infection model Abstract Abstract Background Urosepsis caused by extended-spectrum β-lactamase (ESBL)-producing Escherichia coli i... |
PMC7144122 | core_pubmed_pmc | The Effects of Intramuscular Naloxone Dose on Mu Receptor Displacement of Carfentanil in Rhesus Monkeys | The Effects of Intramuscular Naloxone Dose on Mu Receptor Displacement of Carfentanil in Rhesus Monkeys Abstract Naloxone (NLX) is a mu receptor antagonist used to treat acute opioid overdoses. Currently approved doses of naloxone to treat opioid overdoses are 4 mg intranasal (IN) and 2 mg intramuscular (IM). However, ... |
PMC6765700 | core_pubmed_pmc | Physiologically‐Based Pharmacokinetic Modeling of Atorvastatin Incorporating Delayed Gastric Emptying and Acid‐to‐Lactone Conversion | Physiologically‐Based Pharmacokinetic Modeling of Atorvastatin Incorporating Delayed Gastric Emptying and Acid‐to‐Lactone Conversion Abstract The drug–drug interaction profile of atorvastatin confirms that disposition is determined by cytochrome P450 (CYP) 3A4 and organic anion transporting polypeptides (OATPs). Drugs ... |
PMC11463968 | core_pubmed_pmc | Preclinical evaluation of targeted therapies for central nervous system metastases | Preclinical evaluation of targeted therapies for central nervous system metastases Abstract ABSTRACT The central nervous system (CNS) represents a site of sanctuary for many metastatic tumors when systemic therapies that control the primary tumor cannot effectively penetrate intracranial lesions. Non-small cell lung ca... |
PMC3313020 | core_pubmed_pmc | A phase I dose-escalation and pharmacokinetic study of enzastaurin and erlotinib in patients with advanced solid tumors | A phase I dose-escalation and pharmacokinetic study of enzastaurin and erlotinib in patients with advanced solid tumors Abstract Purpose Enzastaurin, an oral serine/threonine kinase inhibitor, targets the protein kinase C and AKT pathways with anti-tumor and anti-angiogenic effects. Erlotinib, an oral epidermal growth ... |
PMC10779231 | core_pubmed_pmc | Delineated 3-1-BenCarMethInYlPro-Phosphonic Acid’s Adroit Activity against Lung Cancer through Multitargeted Docking, MM\GBSA, QM-DFT and Multiscale Simulations | Delineated 3-1-BenCarMethInYlPro-Phosphonic Acid’s Adroit Activity against Lung Cancer through Multitargeted Docking, MM\GBSA, QM-DFT and Multiscale Simulations Abstract Abstract Lung cancer is a pervasive and challenging disease with limited treatment options, with global health challenges often present with complex m... |
PMC5778127 | core_pubmed_pmc | Long-acting injectable atovaquone nanomedicines for malaria prophylaxis | Long-acting injectable atovaquone nanomedicines for malaria prophylaxis Abstract Abstract Chemoprophylaxis is currently the best available prevention from malaria, but its efficacy is compromised by non-adherence to medication. Here we develop a long-acting injectable formulation of atovaquone solid drug nanoparticles ... |
PMC4143594 | core_pubmed_pmc | Glucose-Lowering Effect of Insulin Degludec is Independent of Subcutaneous Injection Region | Glucose-Lowering Effect of Insulin Degludec is Independent of Subcutaneous Injection Region Abstract Background and Objectives Patients with diabetes mellitus inject insulin in different regions of the body. This study investigated the pharmacokinetic and pharmacodynamic properties of insulin degludec (IDeg), a new-gen... |
PMC12716557 | core_pubmed_pmc | Safety and potential efficacy of DM199, a tissue kallikrein-1 analogue, for treating pre-eclampsia and fetal growth restriction: study protocol for a South African, hospital-based phase I/II open-label trial | Safety and potential efficacy of DM199, a tissue kallikrein-1 analogue, for treating pre-eclampsia and fetal growth restriction: study protocol for a South African, hospital-based phase I/II open-label trial Abstract Abstract Introduction Pre-eclampsia and fetal growth restriction are leading causes of perinatal morbid... |
PMC5412838 | core_pubmed_pmc | A Novel NF‐κB Inhibitor, Edasalonexent (CAT‐1004), in Development as a Disease‐Modifying Treatment for Patients With Duchenne Muscular Dystrophy: Phase 1 Safety, Pharmacokinetics, and Pharmacodynamics in Adult Subjects | A Novel NF‐κB Inhibitor, Edasalonexent (CAT‐1004), in Development as a Disease‐Modifying Treatment for Patients With Duchenne Muscular Dystrophy: Phase 1 Safety, Pharmacokinetics, and Pharmacodynamics in Adult Subjects Abstract Abstract In Duchenne muscular dystrophy (DMD), NF‐κB is activated in skeletal muscle from in... |
PMC12895928 | core_pubmed_pmc | Pharmacologic and toxicologic confounders in brain death determination: a multidisciplinary guide | Pharmacologic and toxicologic confounders in brain death determination: a multidisciplinary guide Abstract Background The assessment of comatose ICU patients presents several challenges with respect to the etiology, depth and ultimate outcome. The acceptance in 1959 of the worst-outcome scenarios of coma, i.e. brain de... |
PMC5560723 | core_pubmed_pmc | Perilymph pharmacokinetics of marker applied through a cochlear implant in guinea pigs | Perilymph pharmacokinetics of marker applied through a cochlear implant in guinea pigs Abstract Patients undergoing cochlear implantation could benefit from a simultaneous application of drugs into the ear, helping preserve residual low-frequency hearing and afferent nerve fiber populations. One way to apply drugs is t... |
PMC4230310 | core_pubmed_pmc | The Simcyp Population Based Simulator: Architecture, Implementation, and Quality Assurance | The Simcyp Population Based Simulator: Architecture, Implementation, and Quality Assurance Abstract Developing a user-friendly platform that can handle a vast number of complex physiologically based pharmacokinetic and pharmacodynamic (PBPK/PD) models both for conventional small molecules and larger biologic drugs is a... |
PMC9650095 | core_pubmed_pmc | Investigation of the potential of Glycyrrhiza glabra as a bioavailability enhancer of Vitamin B12 | Investigation of the potential of Glycyrrhiza glabra as a bioavailability enhancer of Vitamin B12 Abstract Abstract Vitamin B12 deficiency is prevalent among individuals globally. Inadequate consumption of B12 rich diet and low bioavailability (due to diet based/physiological factors) are linked to the deficiency of Vi... |
PMC9373118 | core_pubmed_pmc | Effect of Flavonoid-Rich Extract From Dalbergiella welwitschii Leaf on Redox, Cholinergic, Monoaminergic, and Purinergic Dysfunction in Oxidative Testicular Injury: Ex Vivo and In Silico Studies | Effect of Flavonoid-Rich Extract From Dalbergiella welwitschii Leaf on Redox, Cholinergic, Monoaminergic, and Purinergic Dysfunction in Oxidative Testicular Injury: Ex Vivo and In Silico Studies Abstract Abstract The antioxidant, cholinergic, monoaminergic, and purinergic activities of flavonoid-rich extract from Dalbe... |
PMC11617584 | core_pubmed_pmc | mRNA-based platform for preventing and treating Staphylococcus aureus by targeted staphylococcal enterotoxin B | mRNA-based platform for preventing and treating Staphylococcus aureus by targeted staphylococcal enterotoxin B Abstract Staphylococcus aureus ( S. aureus ) possesses numerous virulence factors, with the increasing prevalence of drug-resistant strains heightening the threat posed by this pathogen. Staphylococcal enterot... |
PMC12851594 | core_pubmed_pmc | Pharmacomicrobiomics in inflammatory skin diseases: past, present, and the future | Pharmacomicrobiomics in inflammatory skin diseases: past, present, and the future Abstract Abstract This mini review article focuses on pharmacomicrobiomics, or the study of how the composition and activity of microorganisms in the body, in particular in the gut, impact drug pharmacokinetics and pharmacodynamics. This ... |
PMC7912632 | core_pubmed_pmc | Evaluation of Pharmacokinetic Drug–Drug Interactions: A Review of the Mechanisms, In Vitro and In Silico Approaches | Evaluation of Pharmacokinetic Drug–Drug Interactions: A Review of the Mechanisms, In Vitro and In Silico Approaches Abstract Pharmacokinetic drug–drug interactions (DDIs) occur when a drug alters the absorption, transport, distribution, metabolism or excretion of a co-administered agent. The occurrence of pharmacokinet... |
PMC4966629 | core_pubmed_pmc | Key factors influencing ADME properties of therapeutic proteins: A need for ADME characterization in drug discovery and development | Key factors influencing ADME properties of therapeutic proteins: A need for ADME characterization in drug discovery and development Abstract abstract Protein therapeutics represent a diverse array of biologics including antibodies, fusion proteins, and therapeutic replacement enzymes. Since their inception, they have r... |
PMC8164703 | core_pubmed_pmc | Downregulation of Renal MRPs Transporters in Acute Lymphoblastic Leukemia Mediated by the IL-6/STAT3/PXR Signaling Pathway | Downregulation of Renal MRPs Transporters in Acute Lymphoblastic Leukemia Mediated by the IL-6/STAT3/PXR Signaling Pathway Abstract Purpose Considering prior investigations on reductions of renal multidrug resistance-associated protein (MRP) 2 and 4 transporters in mice with acute lymphoblastic leukemia (ALL), we sough... |
PMC7932972 | core_pubmed_pmc | Population Pharmacokinetics of Revefenacin in Patients with Chronic Obstructive Pulmonary Disease | Population Pharmacokinetics of Revefenacin in Patients with Chronic Obstructive Pulmonary Disease Abstract Background and Objectives Revefenacin is a lung-selective, long-acting muscarinic antagonist indicated for the maintenance treatment of patients with chronic obstructive pulmonary disease. The objectives of this a... |
PMC5791368 | core_pubmed_pmc | Modeling the therapeutic efficacy of N F κ B synthetic decoy oligodeoxynucleotides (ODNs) | Modeling the therapeutic efficacy of N F κ B synthetic decoy oligodeoxynucleotides (ODNs) Abstract Background Transfection of NF κ B synthetic decoy Oligodeoxynucleotides (ODNs) has been proposed as a promising therapeutic strategy for a variety of diseases arising from constitutive activation of the eukaryotic transcr... |
PMC11650638 | core_pubmed_pmc | In Vivo Activity Profiling of Biosynthetic Darobactin D22 against Critical Gram-Negative Pathogens | In Vivo Activity Profiling of Biosynthetic Darobactin D22 against Critical Gram-Negative Pathogens Abstract In recent years, naturally occurring darobactins have emerged as a promising compound class to combat infections caused by critical Gram-negative pathogens. In this study, we describe the in vivo evaluation of de... |
PMC5053985 | core_pubmed_pmc | Dose Assessment of Cefquinome by Pharmacokinetic/Pharmacodynamic Modeling in Mouse Model of Staphylococcus aureus Mastitis | Dose Assessment of Cefquinome by Pharmacokinetic/Pharmacodynamic Modeling in Mouse Model of Staphylococcus aureus Mastitis Abstract Abstract This work aimed to characterize the mammary gland pharmacokinetics of cefquinome after an intramammary administration and integrate pharmacokinetic/pharmacodynamic model. The phar... |
PMC6080548 | core_pubmed_pmc | Safety and tolerability of quizartinib, a FLT3 inhibitor, in advanced solid tumors: a phase 1 dose-escalation trial | Safety and tolerability of quizartinib, a FLT3 inhibitor, in advanced solid tumors: a phase 1 dose-escalation trial Abstract Abstract Background Quizartinib, an inhibitor of class III receptor tyrosine kinases (RTKs), is currently in phase 3 development for the treatment of acute myeloid leukemia (AML) bearing internal... |
PMC4895521 | core_pubmed_pmc | Effect of Chronic Administration of Phenobarbital, or Bromide, on Pharmacokinetics of Levetiracetam in Dogs with Epilepsy | Effect of Chronic Administration of Phenobarbital, or Bromide, on Pharmacokinetics of Levetiracetam in Dogs with Epilepsy Abstract Abstract Background Levetiracetam (LEV) is a common add‐on antiepileptic drug (AED) in dogs with refractory seizures. Concurrent phenobarbital administration alters the disposition of LEV i... |
PMC5198968 | core_pubmed_pmc | Phase I study of nintedanib in Japanese patients with advanced hepatocellular carcinoma and liver impairment | Phase I study of nintedanib in Japanese patients with advanced hepatocellular carcinoma and liver impairment Abstract This phase I, dose‐escalation study evaluated the safety, preliminary efficacy and pharmacokinetics of nintedanib, a triple angiokinase inhibitor, in Japanese patients with advanced hepatocellular carci... |
PMC5655044 | core_pubmed_pmc | Reducing Antibacterial Development Risk for GSK1322322 by Exploring Potential Human Dose Regimens in Nonclinical Efficacy Studies Using Immunocompetent Rats | Reducing Antibacterial Development Risk for GSK1322322 by Exploring Potential Human Dose Regimens in Nonclinical Efficacy Studies Using Immunocompetent Rats Abstract ABSTRACT Directly testing proposed clinical dosing regimens in nonclinical studies can reduce the risk during the development of novel antibacterial agent... |
PMC11761482 | core_pubmed_pmc | Bioavailability study of enantiopure (S)-Equol in CD(SD)IGS rats | Bioavailability study of enantiopure (S)-Equol in CD(SD)IGS rats Abstract Abstract The therapeutic potential of (S)-Equol across various health domains, including mental health and oncology has been identified and studied enormously. However, the pharmacokinetic study on the enantiopure (S)-Equol in male and female rat... |
PMC7968617 | core_pubmed_pmc | No Abuse Potential of Silexan in Healthy Recreational Drug Users: A Randomized Controlled Trial | No Abuse Potential of Silexan in Healthy Recreational Drug Users: A Randomized Controlled Trial Abstract Abstract Background Silexan is a lavender essential oil with established anxiolytic and calming efficacy. Here we asked whether there is a potential for abuse in human patients. Methods We carried out a phase I abus... |
PMC8878141 | core_pubmed_pmc | Development of Sedative Dexmedetomidine Sublingual In Situ Gels: In Vitro and In Vivo Evaluations | Development of Sedative Dexmedetomidine Sublingual In Situ Gels: In Vitro and In Vivo Evaluations Abstract Intravenous dexmedetomidine (DEX) is currently approved by the FDA for the sedation of intubated patients in intensive care units to reduce anxiety and to augment postoperative analgesia. Bradycardia and hypotensi... |
PMC3853440 | core_pubmed_pmc | Head and neck irradiation modulates pharmacokinetics of 5-fluorouracil and cisplatin | Head and neck irradiation modulates pharmacokinetics of 5-fluorouracil and cisplatin Abstract Background 5-fluorouracil (5-FU) and cisplatin (CDDP) are used to enhance radiotherapy (RT) effect for head and neck (HN) cancers. However, the effect of local RT on systemic chemotherapeutics remains unclear. Here, we evaluat... |
PMC10858860 | core_pubmed_pmc | The effects of OPRM1 118A>G on methadone response in pain management in advanced cancer at end of life | The effects of OPRM1 118A>G on methadone response in pain management in advanced cancer at end of life Abstract Abstract Cancer pain is the most feared symptom at end of life. Methadone has advantages over other opioids but is associated with significant variability in clinical response, making dosing challenging in pr... |
PMC6643120 | core_pubmed_pmc | Anti-Tumor Activity and Pharmacokinetics of AP25-Fc Fusion Protein | Anti-Tumor Activity and Pharmacokinetics of AP25-Fc Fusion Protein Abstract Abstract AP25 is an anti-tumor peptide with a high affinity for integrins. It exerts its anti-tumor activity by inhibiting angiogenesis and by directly inhibiting the growth of tumor cells. Its half-life time in vivo is only about 50 minutes, w... |
PMC7884382 | core_pubmed_pmc | A Phase 1 study of RO6870810, a novel bromodomain and extra-terminal protein inhibitor, in patients with NUT carcinoma, other solid tumours, or diffuse large B-cell lymphoma | A Phase 1 study of RO6870810, a novel bromodomain and extra-terminal protein inhibitor, in patients with NUT carcinoma, other solid tumours, or diffuse large B-cell lymphoma Abstract Background Bromodomain and extra-terminal (BET) proteins are epigenetic readers that can drive carcinogenesis and therapy resistance. RO6... |
PMC12066900 | core_pubmed_pmc | The Pharmacokinetics of Subcutaneous Eprinomectin in Plasma and Milk in Dry Dairy Cattle | The Pharmacokinetics of Subcutaneous Eprinomectin in Plasma and Milk in Dry Dairy Cattle Abstract ABSTRACT Parasitic infections in dairy cattle reduce herd immunity, milk production, and conception rates. This leads to higher production costs, compromised animal welfare, and increased interest in extralabel drug use. T... |
PMC5343891 | core_pubmed_pmc | Cell Imaging Counting as a Novel Ex Vivo Approach for Investigating Drug-Induced Hepatotoxicity in Zebrafish Larvae | Cell Imaging Counting as a Novel Ex Vivo Approach for Investigating Drug-Induced Hepatotoxicity in Zebrafish Larvae Abstract Drug-induced liver injury (DILI) is the most common reason for failures during the drug development process and for safety-related withdrawal of drugs from the pharmaceutical market. Therefore, h... |
PMC9097234 | core_pubmed_pmc | Pevonedistat in East Asian patients with acute myeloid leukemia or myelodysplastic syndromes: a phase 1/1b study to evaluate safety, pharmacokinetics and activity as a single agent and in combination with azacitidine | Pevonedistat in East Asian patients with acute myeloid leukemia or myelodysplastic syndromes: a phase 1/1b study to evaluate safety, pharmacokinetics and activity as a single agent and in combination with azacitidine Abstract Pevonedistat, the first small-molecule inhibitor of NEDD8-activating enzyme, has demonstrated ... |
PMC12873951 | core_pubmed_pmc | Dynamical A β -Tau-Neurodegeneration Model Predicts Alzheimer’s Disease Mechanisms and Biomarker Progression | Dynamical A β -Tau-Neurodegeneration Model Predicts Alzheimer’s Disease Mechanisms and Biomarker Progression Abstract Alzheimer’s disease is characterised by the pathological interaction of two proteins, amyloid-beta (Aβ) and tau, which collectively drive neurodegeneration and cognitive decline. The progression of Aβ, ... |
PMC12464662 | core_pubmed_pmc | Real‐world population pharmacokinetics of tezacaftor‐ivacaftor in children with cystic fibrosis: The SYM‐CF study | Real‐world population pharmacokinetics of tezacaftor‐ivacaftor in children with cystic fibrosis: The SYM‐CF study Abstract Aims The clinical effectiveness of tezacaftor‐ivacaftor in children with cystic fibrosis (cwCF) varies; some patients respond while others do not or have adverse effects. The pharmacokinetics (PK) ... |
PMC11849382 | core_pubmed_pmc | A Chinese patient with cardiogenic stroke and warfarin resistance: a case report | A Chinese patient with cardiogenic stroke and warfarin resistance: a case report Abstract Abstract Background Warfarin is the most commonly used oral anticoagulant drug in clinical practice due to its effective anticoagulant effect and low cost. Warfarin plays a crucial role in the anticoagulant treatment of patients w... |
PMC9707501 | core_pubmed_pmc | Reanalysis of Trichloroethylene and Tetrachloroethylene Metabolism to Glutathione Conjugates Using Human, Rat, and Mouse Liver in Vitro Models to Improve Precision in Risk Characterization | Reanalysis of Trichloroethylene and Tetrachloroethylene Metabolism to Glutathione Conjugates Using Human, Rat, and Mouse Liver in Vitro Models to Improve Precision in Risk Characterization Abstract Abstract Background: Both trichloroethylene (TCE) and tetrachloroethylene (PCE) are high-priority chemicals subject to num... |
PMC12427342 | core_pubmed_pmc | Pharmacokinetics of Matrine in Pigs After Gavage Administration of Matrine Alone and in Combination with Amoxicillin | Pharmacokinetics of Matrine in Pigs After Gavage Administration of Matrine Alone and in Combination with Amoxicillin Abstract Simple Summary Matrine (MT), a quinolizidine alkaloid isolated from Sophora spp., has been demonstrated by previous studies to be a potential resistance reversal agent. Its use in combination wi... |
PMC12035585 | core_pubmed_pmc | A review on the role of extrapolation as basis for paediatric marketing authorization applications of medicines in the EU | A review on the role of extrapolation as basis for paediatric marketing authorization applications of medicines in the EU Abstract Aims For new medicines, drug companies obtain regulatory approval on the strategy to generate evidence in the paediatric population, which can be supported by extrapolation of evidence obta... |
PMC8253073 | core_pubmed_pmc | THE IMPACT OF ANTIEPILEPTIC TREATMENT IN PREGNANCY ON PERINATAL OUTCOME IN CROATIA – A SINGLE-CENTER STUDY | THE IMPACT OF ANTIEPILEPTIC TREATMENT IN PREGNANCY ON PERINATAL OUTCOME IN CROATIA – A SINGLE-CENTER STUDY Abstract SUMMARY Pregnancy can alter the natural course of epilepsy and affect pharmacokinetic profile of antiepileptic drugs (AEDs) making therapeutic management more demanding. Since there is no relevant populat... |
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