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PMC3813088 | core_pubmed_pmc | Evaluation of Carbamazepine (CBZ) Supersaturatable Self-Microemulsifying (S-SMEDDS) Formulation In-vitro and In-vivo | Evaluation of Carbamazepine (CBZ) Supersaturatable Self-Microemulsifying (S-SMEDDS) Formulation In-vitro and In-vivo Abstract Abstract The supersaturatable self-microemulsifying drug delivery system (S-SMEDDS) represents a new thermodynamically stable formulation approach wherein it is designed to contain a reduced amo... |
PMC7380081 | core_pubmed_pmc | Paracetamol vs. Ibuprofen in Preterm Infants With Hemodynamically Significant Patent Ductus Arteriosus: A Non-inferiority Randomized Clinical Trial Protocol | Paracetamol vs. Ibuprofen in Preterm Infants With Hemodynamically Significant Patent Ductus Arteriosus: A Non-inferiority Randomized Clinical Trial Protocol Abstract Background: Currently, the first line treatment of persistent ductus arteriosus (PDA) is either indomethacin or ibuprofen. However, the potentially life-t... |
PMC8326816 | core_pubmed_pmc | The role of lumateperone in the treatment of schizophrenia | The role of lumateperone in the treatment of schizophrenia Abstract Abstract Schizophrenia is a devastating mental disorder resulting in marked morbidity and mortality despite the optimal use of all currently available interventions. For this reason, the release of lumateperone (Captyla R ), also known as ITI-007, an o... |
PMC6763577 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Integration of Doxycycline Against Mycoplasma hyopneumoniae in an In Vitro Model | Pharmacokinetic/Pharmacodynamic Integration of Doxycycline Against Mycoplasma hyopneumoniae in an In Vitro Model Abstract Abstract Doxycycline is a broad-spectrum antibacterial drug. It is used widely to treat diseases caused by Mycoplasma species. We investigated the antibacterial activity of doxycycline against the M... |
PMC8954607 | core_pubmed_pmc | Impact of Pharmacokinetic and Pharmacodynamic Properties of Monoclonal Antibodies in the Management of Psoriasis | Impact of Pharmacokinetic and Pharmacodynamic Properties of Monoclonal Antibodies in the Management of Psoriasis Abstract The treatment of psoriasis has been revolutionized by the emergence of biological therapies. Monoclonal antibodies (mAb) generally have complex pharmacokinetic (PK) properties with nonlinear distrib... |
PMC11823644 | core_pubmed_pmc | Comparing two-sample log-linear exposure estimation with Bayesian model-informed precision dosing of tobramycin in adult patients with cystic fibrosis | Comparing two-sample log-linear exposure estimation with Bayesian model-informed precision dosing of tobramycin in adult patients with cystic fibrosis Abstract ABSTRACT Tobramycin dosing in patients with cystic fibrosis (CF) is challenged by its high pharmacokinetic (PK) variability and narrow therapeutic window. Doses... |
PMC2848657 | core_pubmed_pmc | Simultaneous determination of three major bioactive saponins of Panax notoginseng using liquid chromatography-tandem mass spectrometry and a pharmacokinetic study | Simultaneous determination of three major bioactive saponins of Panax notoginseng using liquid chromatography-tandem mass spectrometry and a pharmacokinetic study Abstract Background Panax notoginseng saponins (PNS), the main active components of Radix Notoginseng, has been used for treating atherosclerosis, cerebral i... |
PMC7833764 | core_pubmed_pmc | Discovery and optimization of a novel anti-GUCY2c x CD3 bispecific antibody for the treatment of solid tumors | Discovery and optimization of a novel anti-GUCY2c x CD3 bispecific antibody for the treatment of solid tumors Abstract ABSTRACT We report here the discovery and optimization of a novel T cell retargeting anti-GUCY2C x anti-CD3ε bispecific antibody for the treatment of solid tumors. Using a combination of hybridoma, pha... |
PMC5858514 | core_pubmed_pmc | A paclitaxel prodrug with bifunctional folate and albumin binding moieties for both passive and active targeted cancer therapy | A paclitaxel prodrug with bifunctional folate and albumin binding moieties for both passive and active targeted cancer therapy Abstract Abstract Folate receptor (FR) has proven to be a valuable target for chemotherapy using folic acid (FA) conjugates. However, FA-conjugated chemotherapeutics still have low therapeutic ... |
PMC7708267 | core_pubmed_pmc | Formoterol for the Treatment of Chronic Obstructive Pulmonary Disease | Formoterol for the Treatment of Chronic Obstructive Pulmonary Disease Abstract Abstract Bronchodilators, including long-acting β 2 -agonists and long-acting muscarinic antagonists, are the mainstay for treatment of patients with chronic obstructive pulmonary disease (COPD) to prevent exacerbations or reduce symptoms. F... |
PMC5096008 | core_pubmed_pmc | Randomized, double‐blind clinical trial comparing basal insulin peglispro and insulin glargine, in combination with prandial insulin lispro, in patients with type 1 diabetes: IMAGINE 3 | Randomized, double‐blind clinical trial comparing basal insulin peglispro and insulin glargine, in combination with prandial insulin lispro, in patients with type 1 diabetes: IMAGINE 3 Abstract Aims To compare the efficacy and safety of basal insulin peglispro ( BIL ), which has a flat pharmacokinetic and pharmacodynam... |
PMC9245287 | core_pubmed_pmc | Prevalence of potentially inappropriate medications among old people with major neurocognitive disorder in 2012 and 2017 | Prevalence of potentially inappropriate medications among old people with major neurocognitive disorder in 2012 and 2017 Abstract Background The increased risk of adverse drug reactions due to age-related altered pharmacokinetics and pharmacodynamics is a challenge when prescribing medications to older people, and espe... |
PMC11461509 | core_pubmed_pmc | Named entity recognition of pharmacokinetic parameters in the scientific literature | Named entity recognition of pharmacokinetic parameters in the scientific literature Abstract Abstract The development of accurate predictions for a new drug’s absorption, distribution, metabolism, and excretion profiles in the early stages of drug development is crucial due to high candidate failure rates. The absence ... |
PMC3048208 | core_pubmed_pmc | Phase I clinical, pharmacokinetic and pharmacodynamic study of SB939, an oral histone deacetylase (HDAC) inhibitor, in patients with advanced solid tumours | Phase I clinical, pharmacokinetic and pharmacodynamic study of SB939, an oral histone deacetylase (HDAC) inhibitor, in patients with advanced solid tumours Abstract Abstract Background: SB939 is an orally available, competitive histone deacetylase (HDAC) inhibitor selective for class I, II and IV histone deacetylases. ... |
PMC9010276 | core_pubmed_pmc | A phase I, randomized, double‐blind, placebo‐controlled, single‐ and multiple dose escalation study evaluating the safety, pharmacokinetics and pharmacodynamics of VX‐128, a highly selective Na v 1.8 inhibitor, in healthy adults | A phase I, randomized, double‐blind, placebo‐controlled, single‐ and multiple dose escalation study evaluating the safety, pharmacokinetics and pharmacodynamics of VX‐128, a highly selective Na v 1.8 inhibitor, in healthy adults Abstract Abstract Selective inhibition of certain voltage‐gated sodium channels (Na v s), s... |
PMC3399132 | core_pubmed_pmc | The pharmacokinetics of Hemiscorpius lepturus scorpion venom and Razi antivenom following intramuscular administration in rat | The pharmacokinetics of Hemiscorpius lepturus scorpion venom and Razi antivenom following intramuscular administration in rat Abstract Abstract Hemiscorpius lepturus ( H. lepturus) is one of the most dangerous scorpions in Iran. Intramuscular administration (IM) of available Razi antivenom to H. lepturus venom is used ... |
PMC11097621 | core_pubmed_pmc | Machine learning framework to predict pharmacokinetic profile of small molecule drugs based on chemical structure | Machine learning framework to predict pharmacokinetic profile of small molecule drugs based on chemical structure Abstract Abstract Accurate prediction of a new compound's pharmacokinetic (PK) profile is pivotal for the success of drug discovery programs. An initial assessment of PK in preclinical species and humans is... |
PMC7036065 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics, and pharmacodynamics of low dose lysergic acid diethylamide (LSD) in healthy older volunteers | Safety, tolerability, pharmacokinetics, and pharmacodynamics of low dose lysergic acid diethylamide (LSD) in healthy older volunteers Abstract Abstract Research has shown that psychedelics, such as lysergic acid diethylamide (LSD), have profound anti-inflammatory properties mediated by 5-HT 2A receptor signaling, suppo... |
PMC8832977 | core_pubmed_pmc | PBPK Modelling of Dexamethasone in Patients With COVID-19 and Liver Disease | PBPK Modelling of Dexamethasone in Patients With COVID-19 and Liver Disease Abstract The aim of the study was to apply Physiologically-Based Pharmacokinetic (PBPK) modelling to predict the effect of liver disease (LD) on the pharmacokinetics (PK) of dexamethasone (DEX) in the treatment of COVID-19. A whole-body PBPK mo... |
PMC9317752 | core_pubmed_pmc | Protein Abundance of Drug Transporters in Human Hepatitis C Livers | Protein Abundance of Drug Transporters in Human Hepatitis C Livers Abstract Transmembrane drug transport in hepatocytes is one of the major determinants of drug pharmacokinetics. In the present study, ABC transporters (P-gp, MRP1, MRP2, MRP3, MRP4, BCRP, and BSEP) and SLC transporters (MCT1, NTCP, OAT2, OATP1B1, OATP1B... |
PMC8448094 | core_pubmed_pmc | Lesion Penetration and Activity Limit the Utility of Second-Line Injectable Agents in Pulmonary Tuberculosis | Lesion Penetration and Activity Limit the Utility of Second-Line Injectable Agents in Pulmonary Tuberculosis Abstract ABSTRACT Amikacin and kanamycin are second-line injectables used in the treatment of multidrug-resistant tuberculosis (MDR-TB) based on the clinical utility of streptomycin, another aminoglycoside and f... |
PMC4111883 | core_pubmed_pmc | Characterisation of the Clinical Pharmacokinetics of Actinomycin D and the Influence of ABCB1 Pharmacogenetic Variation on Actinomycin D Disposition in Children with Cancer | Characterisation of the Clinical Pharmacokinetics of Actinomycin D and the Influence of ABCB1 Pharmacogenetic Variation on Actinomycin D Disposition in Children with Cancer Abstract Background and Objective Despite its important role in cancer treatment, there is currently very limited available information concerning ... |
PMC10785239 | core_pubmed_pmc | Inhalation of panaxadiol alleviates lung inflammation via inhibiting TNFA/TNFAR and IL7/IL7R signaling between macrophages and epithelial cells | Inhalation of panaxadiol alleviates lung inflammation via inhibiting TNFA/TNFAR and IL7/IL7R signaling between macrophages and epithelial cells Abstract Abstract Background Lung inflammation occurs in many lung diseases, but has limited effective therapeutics. Ginseng and its derivatives have anti-inflammatory effects,... |
PMC3945208 | core_pubmed_pmc | Neuroprotective Potential of Peroxisome Proliferator Activated Receptor- α Agonist in Cognitive Impairment in Parkinson's Disease: Behavioral, Biochemical, and PBPK Profile | Neuroprotective Potential of Peroxisome Proliferator Activated Receptor- α Agonist in Cognitive Impairment in Parkinson's Disease: Behavioral, Biochemical, and PBPK Profile Abstract Parkinson's disease (PD) is a common neurodegenerative disorder affecting 1% of the population by the age of 65 years and 4-5% of the popu... |
PMC6308302 | core_pubmed_pmc | Identification of Pharmacokinetic Markers for Guanxin Danshen Drop Pills in Rats by Combination of Pharmacokinetics, Systems Pharmacology, and Pharmacodynamic Assays | Identification of Pharmacokinetic Markers for Guanxin Danshen Drop Pills in Rats by Combination of Pharmacokinetics, Systems Pharmacology, and Pharmacodynamic Assays Abstract Abstract This paper reported a feasibility study strategy of identifying pharmacokinetic (PK) markers for a cardiovascular herbal medicine, Guanx... |
PMC11211018 | core_pubmed_pmc | Exposure–Response Relationship between VWF/FVIII Activity and Spontaneous Bleeding Events Following Recombinant VWF Prophylaxis in Severe VWD | Exposure–Response Relationship between VWF/FVIII Activity and Spontaneous Bleeding Events Following Recombinant VWF Prophylaxis in Severe VWD Abstract Background Recombinant von Willebrand factor (rVWF, vonicog alfa, Takeda Pharmaceuticals USA) is indicated in adults diagnosed with von Willebrand disease (VWD). In this... |
PMC11512085 | core_pubmed_pmc | Comparison of Two Methods of Antepartum Anticoagulation: Continuation of Enoxaparin until Scheduled Induction of Labor Versus Transitioning to Heparin with Spontaneous Labor | Comparison of Two Methods of Antepartum Anticoagulation: Continuation of Enoxaparin until Scheduled Induction of Labor Versus Transitioning to Heparin with Spontaneous Labor Abstract Abstract Pregnancy is a hypercoagulable state. There is a lack of strong evidence-based guidance regarding management when anticoagulatio... |
PMC9053904 | core_pubmed_pmc | A rapid and reliable CE-LIF method for the quantitative analysis of miRNA-497 in plasma and organs and its application to a pharmacokinetic and biodistribution study † | A rapid and reliable CE-LIF method for the quantitative analysis of miRNA-497 in plasma and organs and its application to a pharmacokinetic and biodistribution study † Abstract MicroRNAs (miRNAs) are involved in the pathogenesis of many human diseases, and various miRNAs have been reported and developed as therapeutic ... |
PMC7040082 | core_pubmed_pmc | Comparison of the gamma-Pareto convolution with conventional methods of characterising metformin pharmacokinetics in dogs | Comparison of the gamma-Pareto convolution with conventional methods of characterising metformin pharmacokinetics in dogs Abstract A model was developed for long term metformin tissue retention based upon temporally inclusive models of serum/plasma concentration ( \documentclass[12pt]{minimal} \usepackage{amsmath} \use... |
PMC11575912 | core_pubmed_pmc | Phase I/Ib Trial of Inavolisib Plus Palbociclib and Endocrine Therapy for PIK3CA -Mutated, Hormone Receptor–Positive, Human Epidermal Growth Factor Receptor 2–Negative Advanced or Metastatic Breast Cancer | Phase I/Ib Trial of Inavolisib Plus Palbociclib and Endocrine Therapy for PIK3CA -Mutated, Hormone Receptor–Positive, Human Epidermal Growth Factor Receptor 2–Negative Advanced or Metastatic Breast Cancer Abstract PURPOSE To investigate the safety, tolerability, pharmacokinetics (PK), and preliminary antitumor activity... |
PMC9533297 | core_pubmed_pmc | Systemic exposure to propranolol in patients with chronic liver disease and its correlation with portal blood flow | Systemic exposure to propranolol in patients with chronic liver disease and its correlation with portal blood flow Abstract Propranolol is a beta-blocker used for the prevention of variceal bleeding in cirrhotic patients. We investigated the pharmacokinetics of propranolol in patients with chronic liver disease compare... |
PMC10651782 | core_pubmed_pmc | The von Willebrand factor–binding aptamer rondaptivon pegol as a treatment for severe and nonsevere hemophilia A | The von Willebrand factor–binding aptamer rondaptivon pegol as a treatment for severe and nonsevere hemophilia A Abstract Key Points • Rondaptivon pegol is a first-in-class prohemostatic molecule that prolongs the half-life of both endogenous FVIII and substituted FVIII. • Rondaptivon pegol could be used to enable once... |
PMC9073255 | core_pubmed_pmc | Pharmacokinetics, distribution, and excretion of sodium oligomannate, a recently approved anti-Alzheimer's disease drug in China | Pharmacokinetics, distribution, and excretion of sodium oligomannate, a recently approved anti-Alzheimer's disease drug in China Abstract The National Medical Products Administration has authorized sodium oligomannate for treating mild-to-moderate Alzheimer's disease. In this study, an LC-MS/MS method was developed and... |
PMC11858989 | core_pubmed_pmc | Pharmacokinetics of Non-Psychotropic Phytocannabinoids | Pharmacokinetics of Non-Psychotropic Phytocannabinoids Abstract Abstract Cannabinoids are widely recognized for their potential therapeutic effects, making them significant and valuable candidates for medical research and applications across various fields. This review aims to analyze the pharmacokinetics of Cannabidio... |
PMC3486908 | core_pubmed_pmc | Integrating Cellular Metabolism into a Multiscale Whole-Body Model | Integrating Cellular Metabolism into a Multiscale Whole-Body Model Abstract Cellular metabolism continuously processes an enormous range of external compounds into endogenous metabolites and is as such a key element in human physiology. The multifaceted physiological role of the metabolic network fulfilling the catalyt... |
PMC11393366 | core_pubmed_pmc | Population Pharmacokinetic Modeling and Simulation for Dose Optimization of GB-5001, a Long-Acting Intramuscular Injection of Donepezil, in Healthy Participants | Population Pharmacokinetic Modeling and Simulation for Dose Optimization of GB-5001, a Long-Acting Intramuscular Injection of Donepezil, in Healthy Participants Abstract Abstract Introduction GB-5001 is an intramuscular (IM) formulation of donepezil under development for the treatment of Alzheimer’s disease. The object... |
PMC12067382 | core_pubmed_pmc | Design and Biodistribution of PEGylated Core–Shell X-ray Fluorescent Nanoparticle Contrast Agents | Design and Biodistribution of PEGylated Core–Shell X-ray Fluorescent Nanoparticle Contrast Agents Abstract Abstract Nanoparticle (NP) uptake by macrophages and their accumulation in undesired organs such as the liver and spleen constitute a major barrier to the effective delivery of NPs to targeted tissues for bioimagi... |
PMC8578052 | core_pubmed_pmc | Mixing Matrix-corrected Whole-body Pharmacokinetic Modeling Using Longitudinal Micro-computed Tomography and Fluorescence-mediated Tomography | Mixing Matrix-corrected Whole-body Pharmacokinetic Modeling Using Longitudinal Micro-computed Tomography and Fluorescence-mediated Tomography Abstract Abstract Purpose Pharmacokinetic modeling can be applied to quantify the kinetics of fluorescently labeled compounds using longitudinal micro-computed tomography and flu... |
PMC8923725 | core_pubmed_pmc | Berkeley Madonna Version 10–A simulation package for solving mathematical models | Berkeley Madonna Version 10–A simulation package for solving mathematical models Abstract Abstract Berkeley Madonna is a software program that provides an easy and intuitive environment for graphically building and numerically solving mathematical equations. Our users range from college undergraduates with little or no... |
PMC8725867 | core_pubmed_pmc | Development of a naringenin microemulsion as a prospective ophthalmic delivery system for the treatment of corneal neovascularization: in vitro and in vivo evaluation | Development of a naringenin microemulsion as a prospective ophthalmic delivery system for the treatment of corneal neovascularization: in vitro and in vivo evaluation Abstract Abstract Naringenin, a flavonoid, possesses antiangiogenic potential and inhibits corneal neovascularization (CNV); however, its therapeutic use... |
PMC5758843 | core_pubmed_pmc | Influences of Anlotinib on Cytochrome P450 Enzymes in Rats Using a Cocktail Method | Influences of Anlotinib on Cytochrome P450 Enzymes in Rats Using a Cocktail Method Abstract Abstract The present study aimed to investigate the effect of anlotinib (AL3818) on pharmacokinetics of cytochrome P450 (CYP) enzymes (CYP1A2, CYP2C6, CYP2D1, CYP2D2, and CYP3A1/2) by using five cocktail probe drugs in vivo. Aft... |
PMC8944676 | core_pubmed_pmc | Orthopaedic Implant-Associated Staphylococcal Infections: A Critical Reappraisal of Unmet Clinical Needs Associated with the Implementation of the Best Antibiotic Choice | Orthopaedic Implant-Associated Staphylococcal Infections: A Critical Reappraisal of Unmet Clinical Needs Associated with the Implementation of the Best Antibiotic Choice Abstract Abstract Infections associated with orthopaedic implants represent a major health concern characterized by a remarkable incidence of morbidit... |
PMC10197533 | core_pubmed_pmc | Auranofin Inhibition of Thioredoxin Reductase Sensitizes Lung Neuroendocrine Tumor Cells (NETs) and Small Cell Lung Cancer (SCLC) Cells to Sorafenib as well as Inhibiting SCLC Xenograft Growth | Auranofin Inhibition of Thioredoxin Reductase Sensitizes Lung Neuroendocrine Tumor Cells (NETs) and Small Cell Lung Cancer (SCLC) Cells to Sorafenib as well as Inhibiting SCLC Xenograft Growth Abstract Thioredoxin Reductase (TrxR) is a key enzyme in hydroperoxide detoxification through peroxiredoxin enzymes and in thio... |
PMC12209991 | core_pubmed_pmc | First‐in‐Human Phase 1 Study to Evaluate the Clinical Pharmacology Properties of RBN‐3143, a Novel Inhibitor of Mono‐Adenosine Diphosphate Ribosyltransferase‐PARP14 | First‐in‐Human Phase 1 Study to Evaluate the Clinical Pharmacology Properties of RBN‐3143, a Novel Inhibitor of Mono‐Adenosine Diphosphate Ribosyltransferase‐PARP14 Abstract Abstract RBN‐3143 is an inhibitor of PARP14 in development for inflammatory diseases. Multiple assessments were conducted to evaluate the clinical... |
PMC7238241 | core_pubmed_pmc | Lack of Correlation between In Vitro and In Vivo Studies on the Inhibitory Effects of (‒)-Sophoranone on CYP2C9 Is Attributable to Low Oral Absorption and Extensive Plasma Protein Binding of (‒)-Sophoranone | Lack of Correlation between In Vitro and In Vivo Studies on the Inhibitory Effects of (‒)-Sophoranone on CYP2C9 Is Attributable to Low Oral Absorption and Extensive Plasma Protein Binding of (‒)-Sophoranone Abstract (‒)-Sophoranone (SPN) is a bioactive component of Sophora tonkinensis with various pharmacological activ... |
PMC12327010 | core_pubmed_pmc | Population pharmacokinetics of pyrazinamide and isoniazid in plasma and cerebrospinal fluid from South African adults with tuberculous meningitis | Population pharmacokinetics of pyrazinamide and isoniazid in plasma and cerebrospinal fluid from South African adults with tuberculous meningitis Abstract ABSTRACT Pyrazinamide and isoniazid are first-line drugs for tuberculous meningitis (TBM), but limited information is available on their plasma pharmacokinetics, and... |
PMC9335923 | core_pubmed_pmc | Multiphysics pharmacokinetic model for targeted nanoparticles | Multiphysics pharmacokinetic model for targeted nanoparticles Abstract Abstract Nanoparticles (NP) are being increasingly explored as vehicles for targeted drug delivery because they can overcome free therapeutic limitations by drug encapsulation, thereby increasing solubility and transport across cell membranes. Howev... |
PMC10974779 | core_pubmed_pmc | Conjugated Linoleic Acid–Carboxymethyl Chitosan Polymeric Micelles to Improve the Solubility and Oral Bioavailability of Paclitaxel | Conjugated Linoleic Acid–Carboxymethyl Chitosan Polymeric Micelles to Improve the Solubility and Oral Bioavailability of Paclitaxel Abstract Abstract Oral delivery, the most common method of therapeutic administration, has two significant obstacles: drug solubility and permeability. The challenges of current oral medic... |
PMC10404122 | core_pubmed_pmc | Optimal Teicoplanin Dosage Regimens in Critically Ill Patients: Population Pharmacokinetics and Dosing Simulations Based on Renal Function and Infection Type | Optimal Teicoplanin Dosage Regimens in Critically Ill Patients: Population Pharmacokinetics and Dosing Simulations Based on Renal Function and Infection Type Abstract Purpose To develop a population pharmacokinetic model describing teicoplanin concentrations in patients hospitalized in intensive care unit (ICU) and to ... |
PMC5902553 | core_pubmed_pmc | Pharmacodynamics of mutant- IDH1 inhibitors in glioma patients probed by in vivo 3D MRS imaging of 2-hydroxyglutarate | Pharmacodynamics of mutant- IDH1 inhibitors in glioma patients probed by in vivo 3D MRS imaging of 2-hydroxyglutarate Abstract Inhibitors of the mutant isocitrate dehydrogenase 1 ( IDH1 ) entered recently in clinical trials for glioma treatment. Mutant IDH1 produces high levels of 2-hydroxyglurate (2HG), thought to ini... |
PMC11839910 | core_pubmed_pmc | Mass spectrometry methods and mathematical PK/PD model for decision tree-guided covalent drug development | Mass spectrometry methods and mathematical PK/PD model for decision tree-guided covalent drug development Abstract Covalent drug discovery efforts are growing rapidly but have major unaddressed limitations. These include high false positive rates during hit-to-lead identification; the inherent uncoupling of covalent dr... |
PMC12923488 | core_pubmed_pmc | Small-molecule therapies for pediatric inflammatory bowel disease: toward precision medicine | Small-molecule therapies for pediatric inflammatory bowel disease: toward precision medicine Abstract Abstract Background Pediatric inflammatory bowel disease (pIBD) often begins early in life, progresses rapidly, and is associated with impaired growth and delayed development. These challenges demand treatment strategi... |
PMC8956549 | core_pubmed_pmc | First-in-human, open-label, phase 1/2 study of the monoclonal antibody programmed cell death protein-1 (PD-1) inhibitor cetrelimab (JNJ-63723283) in patients with advanced cancers | First-in-human, open-label, phase 1/2 study of the monoclonal antibody programmed cell death protein-1 (PD-1) inhibitor cetrelimab (JNJ-63723283) in patients with advanced cancers Abstract Abstract Purpose To assess the safety, pharmacokinetics, pharmacodynamics, and preliminary efficacy of cetrelimab (JNJ-63723283), a... |
PMC5919849 | core_pubmed_pmc | A Phase I/II Study for Dose-finding, and to Investigate the Safety, Pharmacokinetics and Preliminary Efficacy of NK012, an SN-38-Incorporating Macromolecular Polymeric Micelle, in Patients with Multiple Myeloma | A Phase I/II Study for Dose-finding, and to Investigate the Safety, Pharmacokinetics and Preliminary Efficacy of NK012, an SN-38-Incorporating Macromolecular Polymeric Micelle, in Patients with Multiple Myeloma Abstract Objective Multiple myeloma (MM) is the second most common hematological cancer. An attempt to treat ... |
PMC9328361 | core_pubmed_pmc | Therapeutic index of inhaled corticosteroids in asthma: A dose–response comparison on airway hyperresponsiveness and adrenal axis suppression | Therapeutic index of inhaled corticosteroids in asthma: A dose–response comparison on airway hyperresponsiveness and adrenal axis suppression Abstract Abstract Aims To compare the airway potency, systemic activity and therapeutic index of three inhaled corticosteroids that differ in glucocorticoid receptor binding affi... |
PMC6769096 | core_pubmed_pmc | Apixaban: A Clinical Pharmacokinetic and Pharmacodynamic Review | Apixaban: A Clinical Pharmacokinetic and Pharmacodynamic Review Abstract Apixaban is an oral, direct factor Xa inhibitor that inhibits both free and clot-bound factor Xa, and has been approved for clinical use in several thromboembolic disorders, including reduction of stroke risk in non-valvular atrial fibrillation, t... |
PMC11520145 | core_pubmed_pmc | In silico molecular targets, docking, dynamics simulation and physiologically based pharmacokinetics modeling of oritavancin | In silico molecular targets, docking, dynamics simulation and physiologically based pharmacokinetics modeling of oritavancin Abstract Introduction Oritavancin is a semi-synthetic lipoglycopeptide antibiotic primarily used to treat serious infections caused by Gram-positive bacteria. The aim of this study was to elucida... |
PMC9220922 | core_pubmed_pmc | Givinostat-Liposomes: Anti-Tumor Effect on 2D and 3D Glioblastoma Models and Pharmacokinetics | Givinostat-Liposomes: Anti-Tumor Effect on 2D and 3D Glioblastoma Models and Pharmacokinetics Abstract Simple Summary Glioblastoma is the most common malignant brain tumor with a high grade of recurrence, invasiveness, and aggressiveness. Currently, there are no curative treatments; therefore, the discovery of novel mo... |
PMC6833033 | core_pubmed_pmc | Optimizing Hydroxyurea Treatment for Sickle Cell Disease Patients: The Pharmacokinetic Approach | Optimizing Hydroxyurea Treatment for Sickle Cell Disease Patients: The Pharmacokinetic Approach Abstract Background: Hydroxyurea (HU) is a FDA- and EMA-approved drug that earned an important place in the treatment of patients with severe sickle cell anemia (SCA) by showing its efficacy in many studies. This medication ... |
PMC3689907 | core_pubmed_pmc | Absence of Pharmacokinetic and Pharmacodynamic Interactions between Almorexant and Warfarin in Healthy Subjects | Absence of Pharmacokinetic and Pharmacodynamic Interactions between Almorexant and Warfarin in Healthy Subjects Abstract Abstract Background and Objective Almorexant is the first representative of the new class of orexin receptor antagonists, which could become a new treatment option for insomnia. The present study inv... |
PMC8401952 | core_pubmed_pmc | The Effect of Plasma Protein Binding on the Therapeutic Monitoring of Antiseizure Medications | The Effect of Plasma Protein Binding on the Therapeutic Monitoring of Antiseizure Medications Abstract Abstract Epilepsy is a widely diffused neurological disorder including a heterogeneous range of syndromes with different aetiology, severity and prognosis. Pharmacological treatments are based on the use, either in mo... |
PMC8430033 | core_pubmed_pmc | Safety, Pharmacokinetics, and Pharmacodynamics of a Single Bolus of the γ-aminobutyric Acid (GABA) Receptor Potentiator HSK3486 in Healthy Chinese Elderly and Non-elderly | Safety, Pharmacokinetics, and Pharmacodynamics of a Single Bolus of the γ-aminobutyric Acid (GABA) Receptor Potentiator HSK3486 in Healthy Chinese Elderly and Non-elderly Abstract Background: The present clinical trial investigated the potential influences of dosage and age on the pharmacokinetic properties and safety ... |
PMC10297013 | core_pubmed_pmc | Exploiting an Interleukin-15 Heterodimeric Agonist (N803) for Effective Immunotherapy of Solid Malignancies | Exploiting an Interleukin-15 Heterodimeric Agonist (N803) for Effective Immunotherapy of Solid Malignancies Abstract Abstract Identifying effective immunotherapies for solid tumors remains challenging despite the significant clinical responses observed in subsets of patients treated with immune checkpoint inhibitors. I... |
PMC7089879 | core_pubmed_pmc | Pharmacokinetics of Active Ingredients of Salvia miltiorrhiza and Carthamus tinctorius in Compatibility in Normal and Cerebral Ischemia Rats: A Comparative Study | Pharmacokinetics of Active Ingredients of Salvia miltiorrhiza and Carthamus tinctorius in Compatibility in Normal and Cerebral Ischemia Rats: A Comparative Study Abstract Background and Objective Dan-Hong injection, which comprises extracts of Salvia miltiorrhiza and Carthamus tinctorius , promotes blood circulation an... |
PMC3837869 | core_pubmed_pmc | Impact of Bolus Dosing versus Continuous Infusion of Piperacillin and Tazobactam on the Development of Antimicrobial Resistance in Pseudomonas aeruginosa | Impact of Bolus Dosing versus Continuous Infusion of Piperacillin and Tazobactam on the Development of Antimicrobial Resistance in Pseudomonas aeruginosa Abstract Abstract Management of nosocomial pneumonia is frequently complicated by bacterial resistance. Extended infusions of beta-lactams are increasingly being used... |
PMC8376134 | core_pubmed_pmc | Excipient knowledgebase: Development of a comprehensive tool for understanding the disposition and interaction potential of common excipients | Excipient knowledgebase: Development of a comprehensive tool for understanding the disposition and interaction potential of common excipients Abstract Abstract Although the use of excipients is widespread, a thorough understanding of the drug interaction potential of these compounds remains a frequent topic of current ... |
PMC2873993 | core_pubmed_pmc | Comparative Therapeutic Effects of Velaglucerase Alfa and Imiglucerase in a Gaucher Disease Mouse Model | Comparative Therapeutic Effects of Velaglucerase Alfa and Imiglucerase in a Gaucher Disease Mouse Model Abstract Gaucher disease type 1 is caused by the defective activity of the lysosomal enzyme, acid β-glucosidase (GCase). Regular infusions of purified recombinant GCase are the standard of care for reversing hematolo... |
PMC7105240 | core_pubmed_pmc | Quantitative analysis of an anti-viral immune escape compound ML-7 in feline plasma using ultra performance liquid chromatography/electrospray ionization mass spectrometry | Quantitative analysis of an anti-viral immune escape compound ML-7 in feline plasma using ultra performance liquid chromatography/electrospray ionization mass spectrometry Abstract Abstract An analytical method for the quantitative measurement of ML-7, a product with possible anti-immune escape activity for feline infe... |
PMC12358650 | core_pubmed_pmc | Integrative green synthesis and molecular simulation of ibrutinib cocrystals for enhanced biopharmaceutical performance and in vivo pharmacokinetics | Integrative green synthesis and molecular simulation of ibrutinib cocrystals for enhanced biopharmaceutical performance and in vivo pharmacokinetics Abstract Abstract Bruton's tyrosine kinase (BTK) inhibitor, Ibrutinib (IBR), belongs to class II of the Biopharmaceutics Classification System (BCS). CYP3A4 enzyme forces ... |
PMC11845331 | core_pubmed_pmc | Teicoplanin pharmacokinetics in critically ill patients on extracorporeal organ support: a retrospective analysis | Teicoplanin pharmacokinetics in critically ill patients on extracorporeal organ support: a retrospective analysis Abstract Background Extracorporeal membrane oxygenation (ECMO) can alter the pharmacokinetics of diverse antimicrobials, posing challenges in achieving therapeutic drug levels. Some literature suggests that... |
PMC11816286 | core_pubmed_pmc | Curcumin and Its Derivatives in Hepatology: Therapeutic Potential and Advances in Nanoparticle Formulations | Curcumin and Its Derivatives in Hepatology: Therapeutic Potential and Advances in Nanoparticle Formulations Abstract Simple Summary Liver diseases are a significant contributor to global mortality, representing an escalating public health concern worldwide. Natural compounds, particularly herbal derivatives, remain a p... |
PMC9692621 | core_pubmed_pmc | Pharmacokinetics of Phenprocoumon in Emergency Situations–Results of the Prospective Observational RADOA-Registry (Reversal Agent Use in Patients Treated with Direct Oral Anticoagulants or Vitamin K Antagonists Registry) | Pharmacokinetics of Phenprocoumon in Emergency Situations–Results of the Prospective Observational RADOA-Registry (Reversal Agent Use in Patients Treated with Direct Oral Anticoagulants or Vitamin K Antagonists Registry) Abstract Background: Phenprocoumon has been used as an oral anticoagulant in patients with thromboe... |
PMC8995271 | core_pubmed_pmc | Phase Ib Dose-Finding Study of Varlitinib Combined with Weekly Paclitaxel With or Without Carboplatin ± Trastuzumab in Advanced Solid Tumors | Phase Ib Dose-Finding Study of Varlitinib Combined with Weekly Paclitaxel With or Without Carboplatin ± Trastuzumab in Advanced Solid Tumors Abstract Abstract Background Varlitinib is a highly potent, small-molecule, pan-HER inhibitor targeting HER1, HER2, and HER4. It has demonstrated activity in gastric, biliary trac... |
PMC9756503 | core_pubmed_pmc | Pharmacodynamic properties for inhibition of cAMP- and cGMP elimination by pentoxifylline remain unaltered in vitro during hypothermia | Pharmacodynamic properties for inhibition of cAMP- and cGMP elimination by pentoxifylline remain unaltered in vitro during hypothermia Abstract Abstract Background Rewarming from hypothermia is associated with severe complications, one of which is hypothermia-induced cardiac dysfunction. This condition is characterized... |
PMC12215774 | core_pubmed_pmc | Development and evaluation of cepharanthine-β-cyclodextrin inclusion complex oral tablets for prevention and treatment of COVID-19 lung injury | Development and evaluation of cepharanthine-β-cyclodextrin inclusion complex oral tablets for prevention and treatment of COVID-19 lung injury Abstract Abstract The symptoms of coronavirus disease 2019 (COVID-19) range from severe lung disease to milder manifestations, such as cough and throat irritation. As a bisbenzy... |
PMC9962320 | core_pubmed_pmc | External Evaluation of Population Pharmacokinetic Models of Methotrexate for Model-Informed Precision Dosing in Pediatric Patients with Acute Lymphoid Leukemia | External Evaluation of Population Pharmacokinetic Models of Methotrexate for Model-Informed Precision Dosing in Pediatric Patients with Acute Lymphoid Leukemia Abstract Background: Methotrexate (MTX) is a key immunosuppressant for children with acute lymphoid leukemia (ALL), and it has a narrow therapeutic window and r... |
PMC6394776 | core_pubmed_pmc | Ongoing Phase I Studies of Immune Checkpoint Inhibitors in China | Ongoing Phase I Studies of Immune Checkpoint Inhibitors in China Abstract This article outlines the ongoing phase I studies of immune checkpoint inhibitors (ICI) in China, shedding light on the status quo of ICI research and development in China and identifying challenges for future early‐phase studies in the era of im... |
PMC12598904 | core_pubmed_pmc | Pharmacokinetics of Single Dose and Multidose Oral Gabapentin in Goats ( Capra aegagrus hircus ) | Pharmacokinetics of Single Dose and Multidose Oral Gabapentin in Goats ( Capra aegagrus hircus ) Abstract ABSTRACT There is a shifting public perception of animal welfare that has increased demand for establishing pain management strategies in livestock. Gabapentin is often utilized in practice to mitigate neuropathic ... |
PMC12397550 | core_pubmed_pmc | Predictive Modeling of Pharmacokinetic Drug–Drug and Herb–Drug Interactions in Oncology: Insights From PBPK Studies | Predictive Modeling of Pharmacokinetic Drug–Drug and Herb–Drug Interactions in Oncology: Insights From PBPK Studies Abstract Physiologically based pharmacokinetic (PBPK) modeling is increasingly used to anticipate, quantify, and strategically manage drug–drug (DDI) and herb–drug (HDI) interactions that can alter the ex... |
PMC7920315 | core_pubmed_pmc | Spontaneous and Engineered Large Animal Models of Neurofibromatosis Type 1 | Spontaneous and Engineered Large Animal Models of Neurofibromatosis Type 1 Abstract Animal models are crucial to understanding human disease biology and developing new therapies. By far the most common animal used to investigate prevailing questions about human disease is the mouse. Mouse models are powerful tools for ... |
PMC12455468 | core_pubmed_pmc | The influence of renal impairment on the pharmacokinetics of rimegepant: Results of a phase 1, open‐label, single‐dose, parallel‐group study | The influence of renal impairment on the pharmacokinetics of rimegepant: Results of a phase 1, open‐label, single‐dose, parallel‐group study Abstract Abstract Objective The objective of this study was to investigate the pharmacokinetics of rimegepant in participants with mild, moderate, or severe renal impairment compa... |
PMC11088408 | core_pubmed_pmc | Nanosuspension-Loaded Dissolving Microneedle Patches for Enhanced Transdermal Delivery of a Highly Lipophilic Cannabidiol | Nanosuspension-Loaded Dissolving Microneedle Patches for Enhanced Transdermal Delivery of a Highly Lipophilic Cannabidiol Abstract Abstract Purpose Transdermal Drug Delivery System (TDDS) offers a promising alternative for delivering poorly soluble drugs, challenged by the stratum corneum’s barrier effect, which restri... |
PMC11679838 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics Evaluation of Amoxicillin Against Staphylococcus pseudintermedius in Dogs | Pharmacokinetics and Pharmacodynamics Evaluation of Amoxicillin Against Staphylococcus pseudintermedius in Dogs Abstract Abstract Antibiotic resistance in bacteria from companion animals poses significant public health risks. Prudent antibiotic use, particularly through pharmacokinetics/pharmacodynamics modeling, is cr... |
PMC12327665 | core_pubmed_pmc | Multi-scale computational modeling towards efficacy in radiopharmaceutical therapies while minimizing side effects: Modeling of amino acid infusion | Multi-scale computational modeling towards efficacy in radiopharmaceutical therapies while minimizing side effects: Modeling of amino acid infusion Abstract Amino acid infusion (AAI) is a technique used in radiopharmaceutical therapy (RPT) to reduce toxicity in kidney and increase clearance rate of radiopharmaceuticals... |
PMC7024201 | core_pubmed_pmc | Iridoids: Research Advances in Their Phytochemistry, Biological Activities, and Pharmacokinetics | Iridoids: Research Advances in Their Phytochemistry, Biological Activities, and Pharmacokinetics Abstract Abstract Iridoids are a class of active compounds that widely exist in the plant kingdom. In recent years, with advances in phytochemical research, many compounds with novel structure and outstanding activity have ... |
PMC3818912 | core_pubmed_pmc | META-ANALYSIS OF CYP2D6 METABOLIZER PHENOTYPE AND METOPROLOL PHARMACOKINETICS | META-ANALYSIS OF CYP2D6 METABOLIZER PHENOTYPE AND METOPROLOL PHARMACOKINETICS Abstract Metoprolol, a commonly prescribed beta-blocker, is primarily metabolized by cytochrome P450 2D6 (CYP2D6), an enzyme with substantial genetic heterogeneity. Several smaller studies have shown that metoprolol pharmacokinetics is influe... |
PMC6344987 | core_pubmed_pmc | Critical pharmacokinetic and pharmacodynamic drug-herb interactions in rats between warfarin and pomegranate peel or guava leaves extracts | Critical pharmacokinetic and pharmacodynamic drug-herb interactions in rats between warfarin and pomegranate peel or guava leaves extracts Abstract Abstract Background In-depth information of potential drug-herb interactions between warfarin and herbal compounds with suspected anticoagulant blood thinning effects is ne... |
PMC5667778 | core_pubmed_pmc | Comparable pharmacokinetics and pharmacodynamics of two epoetin alfa formulations Eporon ® and Eprex ® following a single subcutaneous administration in healthy male volunteers | Comparable pharmacokinetics and pharmacodynamics of two epoetin alfa formulations Eporon ® and Eprex ® following a single subcutaneous administration in healthy male volunteers Abstract Abstract Purpose This study aimed to assess and compare the pharmacokinetic (PK) and pharmacodynamic (PD) properties following a singl... |
PMC10644204 | core_pubmed_pmc | Effects of the HIV‐1 maturation inhibitor GSK3640254 on QT interval in healthy participants | Effects of the HIV‐1 maturation inhibitor GSK3640254 on QT interval in healthy participants Abstract Abstract GSK3640254 (GSK'254) is a novel HIV‐1 maturation inhibitor with pharmacokinetics supporting once‐daily (QD) therapy for HIV‐1 treatment. This thorough QT/corrected QT (QTc) study evaluated the effect of GSK'254... |
PMC12705741 | core_pubmed_pmc | In vitro development and evaluation of chitosan–cellulose nanocrystal microspheres for controlled dexamethasone delivery in rheumatoid arthritis | In vitro development and evaluation of chitosan–cellulose nanocrystal microspheres for controlled dexamethasone delivery in rheumatoid arthritis Abstract Systemic glucocorticoids are effective in rheumatoid arthritis, but long-term exposure carries dose-dependent risks. We developed a “nano-in-micro” platform in which ... |
PMC10304291 | core_pubmed_pmc | THC-Reduced Cannabis sativa L.—How Does the Solvent Determine the Bioavailability of Cannabinoids Given Orally? | THC-Reduced Cannabis sativa L.—How Does the Solvent Determine the Bioavailability of Cannabinoids Given Orally? Abstract Abstract The bioavailability levels of cannabidiol (CBD) and tetrahydrocannabinol (THC) determine their pharmacological effects. Therefore, for medical purposes, it is essential to obtain extracts co... |
PMC9522955 | core_pubmed_pmc | First-in-human use of 11 C-CPPC with positron emission tomography for imaging the macrophage colony-stimulating factor 1 receptor | First-in-human use of 11 C-CPPC with positron emission tomography for imaging the macrophage colony-stimulating factor 1 receptor Abstract Abstract Purpose Study of the contribution of microglia to onset and course of several neuropsychiatric conditions is challenged by the fact that these resident immune cells often t... |
PMC7180003 | core_pubmed_pmc | Model‐Informed Drug Development for Everolimus Dosing Selection in Pediatric Infant Patients | Model‐Informed Drug Development for Everolimus Dosing Selection in Pediatric Infant Patients Abstract Everolimus is currently approved in Europe as an adjunctive therapy for patients aged ≥ 2 years with tuberous sclerosis complex (TSC)–associated treatment‐refractory partial‐onset seizures, based on the EXIST‐3 study (... |
PMC2895665 | core_pubmed_pmc | Ultra-Fast Analysis of Plasma and Intracellular Levels of HIV Protease Inhibitors in Children: A Clinical Application of MALDI Mass Spectrometry | Ultra-Fast Analysis of Plasma and Intracellular Levels of HIV Protease Inhibitors in Children: A Clinical Application of MALDI Mass Spectrometry Abstract Abstract HIV protease inhibitors must penetrate into cells to exert their action. Differences in the intracellular pharmacokinetics of these drugs may explain why som... |
PMC10272297 | core_pubmed_pmc | Prediction of gastric pH‐mediated drug exposure using physiologically‐based pharmacokinetic modeling: A case study of itraconazole | Prediction of gastric pH‐mediated drug exposure using physiologically‐based pharmacokinetic modeling: A case study of itraconazole Abstract Abstract Abnormal gastric acidity, including achlorhydria, can act as a significant source of variability in orally administered drugs especially with pH‐sensitive solubility profi... |
PMC11877961 | core_pubmed_pmc | Prevalence and risk factors of self-reported adverse drug events in elderly co-morbid patients in northeastern China: a cross-sectional study | Prevalence and risk factors of self-reported adverse drug events in elderly co-morbid patients in northeastern China: a cross-sectional study Abstract Background Older adults are vulnerable to adverse drug events given the pharmacokinetic and pharmacodynamic changes that coming with ageing, as well as they often take m... |
PMC12631063 | core_pubmed_pmc | Optimization of Bottom‐Up PBPK Model Development in SIMCYP via Retrospective Analysis of Clinical Human PK Data | Optimization of Bottom‐Up PBPK Model Development in SIMCYP via Retrospective Analysis of Clinical Human PK Data Abstract ABSTRACT Physiologically‐based pharmacokinetic (PBPK) modeling has become a major tool in drug discovery and development. Here, we describe the bottom‐up PBPK modeling approaches employed at AbbVie u... |
PMC4353852 | core_pubmed_pmc | The Affymetrix DMET Plus Platform Reveals Unique Distribution of ADME-Related Variants in Ethnic Arabs | The Affymetrix DMET Plus Platform Reveals Unique Distribution of ADME-Related Variants in Ethnic Arabs Abstract Background . The Affymetrix Drug Metabolizing Enzymes and Transporters (DMET) Plus Premier Pack has been designed to genotype 1936 gene variants thought to be essential for screening patients in personalized ... |
PMC8975765 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Tedizolid | Pharmacokinetics and Pharmacodynamics of Tedizolid Abstract Tedizolid is an oxazolidinone antibiotic with high potency against Gram-positive bacteria and currently prescribed in bacterial skin and skin-structure infections. The aim of the review was to summarize and critically review the key pharmacokinetic and pharmac... |
PMC6053836 | core_pubmed_pmc | Rethinking urinary antibiotic breakpoints: analysis of urinary antibiotic concentrations to treat multidrug resistant organisms | Rethinking urinary antibiotic breakpoints: analysis of urinary antibiotic concentrations to treat multidrug resistant organisms Abstract Objective The present study analyzed whether renally eliminated antibiotics achieve sufficient urinary concentrations based on their pharmacokinetic/pharmacodynamic principles to effe... |
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