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PMC5943940 | core_pubmed_pmc | Dopamine and Levodopa Prodrugs for the Treatment of Parkinson’s Disease | Dopamine and Levodopa Prodrugs for the Treatment of Parkinson’s Disease Abstract Background : Parkinson’s disease is an aggressive and progressive neurodegenerative disorder that depletes dopamine (DA) in the central nervous system. Dopamine replacement therapy, mainly through actual dopamine and its original prodrug l... |
PMC10143245 | core_pubmed_pmc | Profiling Docetaxel in Plasma and Urine Samples from a Pediatric Cancer Patient Using Ultrasound-Assisted Dispersive Liquid–Liquid Microextraction Combined with LC–MS/MS | Profiling Docetaxel in Plasma and Urine Samples from a Pediatric Cancer Patient Using Ultrasound-Assisted Dispersive Liquid–Liquid Microextraction Combined with LC–MS/MS Abstract Abstract In recent years, therapeutic drug monitoring (TDM) has been applied in docetaxel (DOC)-based anticancer therapy to precisely control... |
PMC11597719 | core_pubmed_pmc | Improved Malaria Therapy with Cationic Nanocapsules Demonstrated in Plasmodium berghei -Infected Rodents Using Whole Blood Surrogate Population PK/PD Modeling | Improved Malaria Therapy with Cationic Nanocapsules Demonstrated in Plasmodium berghei -Infected Rodents Using Whole Blood Surrogate Population PK/PD Modeling Abstract Abstract Objectives : Investigating how nanoparticle systems interact in whole blood (WB) is critical to evaluating the effectiveness of malaria therapy... |
PMC10974768 | core_pubmed_pmc | Exploration of Cytochrome P450-Related Interactions between Aflatoxin B1 and Tiamulin in Broiler Chickens | Exploration of Cytochrome P450-Related Interactions between Aflatoxin B1 and Tiamulin in Broiler Chickens Abstract Poultry may face simultaneous exposure to aflatoxin B1 (AFB1) and tiamulin (TIA), given mycotoxin contamination and antibiotic use. As both mycotoxins and antibiotics can affect cytochrome P450 enzymes (CY... |
PMC9968108 | core_pubmed_pmc | bioTCIs: Middle-to-Macro Biomolecular Targeted Covalent Inhibitors Possessing Both Semi-Permanent Drug Action and Stringent Target Specificity as Potential Antibody Replacements | bioTCIs: Middle-to-Macro Biomolecular Targeted Covalent Inhibitors Possessing Both Semi-Permanent Drug Action and Stringent Target Specificity as Potential Antibody Replacements Abstract Abstract Monoclonal antibody therapies targeting immuno-modulatory targets such as checkpoint proteins, chemokines, and cytokines hav... |
PMC10079506 | core_pubmed_pmc | Size-reduced fexuprazan 20 mg demonstrated the optimal bioavailability and bioequivalence with the reference formulation | Size-reduced fexuprazan 20 mg demonstrated the optimal bioavailability and bioequivalence with the reference formulation Abstract Abstract Fexuprazan (DWP14012), a potassium-competitive acid blocker, is a medical formulation prescribed to inhibit the secretion of gastric acid. The present study encompasses a comparativ... |
PMC5114317 | core_pubmed_pmc | The Role of Interaction Model in Simulation of Drug Interactions and QT Prolongation | The Role of Interaction Model in Simulation of Drug Interactions and QT Prolongation Abstract Computational modelling is a cornerstone of Comprehensive In Vitro Proarrhythmia Assay and is re-increasingly being used in drug development. Electrophysiological effects of drug-drug interactions can be predicted in silico, e... |
PMC7914535 | core_pubmed_pmc | Corneal Penetration of Low-Dose Atropine Eye Drops | Corneal Penetration of Low-Dose Atropine Eye Drops Abstract Major studies demonstrating the inhibition of myopia in children and juveniles by low-dose atropine eye drops provide little information on the manufacturing process and the exact composition of the atropine dilutions. However, corneal penetration might signif... |
PMC12623587 | core_pubmed_pmc | Safety and Effectiveness of Direct Oral Anticoagulants in Combination with Antiseizure Medications: Protocol for a Systematic Review and Meta-analysis | Safety and Effectiveness of Direct Oral Anticoagulants in Combination with Antiseizure Medications: Protocol for a Systematic Review and Meta-analysis Abstract Introduction The concurrent use of direct oral anticoagulants (DOACs) and antiseizure medications (ASMs) is increasingly common, particularly among patients wit... |
PMC12708698 | core_pubmed_pmc | When does the “third fluid space” open? | When does the “third fluid space” open? Abstract Abstract Recent kinetic studies show that the interstitial space contains two functional fluid compartments. This study explores the prerequisites for accumulation of infused crystalloid fluid in the remote slow-exchange space (“third fluid space¨, V t2 ). Volume kinetic... |
PMC11106373 | core_pubmed_pmc | Advancements and challenges in pharmacokinetic and pharmacodynamic research on the traditional Chinese medicine saponins: a comprehensive review | Advancements and challenges in pharmacokinetic and pharmacodynamic research on the traditional Chinese medicine saponins: a comprehensive review Abstract Recent research on traditional Chinese medicine (TCM) saponin pharmacokinetics has revealed transformative breakthroughs and challenges. The multicomponent nature of ... |
PMC11937999 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, and Safety of Subcutaneous and Intravenous Garadacimab Following Single‐Dose Administration in Healthy Japanese and White Adults | Pharmacokinetics, Pharmacodynamics, and Safety of Subcutaneous and Intravenous Garadacimab Following Single‐Dose Administration in Healthy Japanese and White Adults Abstract Abstract Garadacimab, an activated factor XII (FXIIa) inhibitor monoclonal antibody, is being evaluated for the long‐term prophylaxis of hereditar... |
PMC10222324 | core_pubmed_pmc | Secondary Metabolites Isolated from Artemisia afra and Artemisia annua and Their Anti-Malarial, Anti-Inflammatory and Immunomodulating Properties—Pharmacokinetics and Pharmacodynamics: A Review | Secondary Metabolites Isolated from Artemisia afra and Artemisia annua and Their Anti-Malarial, Anti-Inflammatory and Immunomodulating Properties—Pharmacokinetics and Pharmacodynamics: A Review Abstract Abstract There are over 500 species of the genus Artemisia in the Asteraceae family distributed over the globe, with ... |
PMC6409735 | core_pubmed_pmc | A Cell-Level Systems PK-PD Model to Characterize In Vivo Efficacy of ADCs | A Cell-Level Systems PK-PD Model to Characterize In Vivo Efficacy of ADCs Abstract Abstract Here, we have presented the development of a systems pharmacokinetics-pharmacodynamics (PK-PD) model for antibody-drug conjugates (ADCs), which uses intracellular target occupancy to drive in-vivo efficacy. The model is built ba... |
PMC8420715 | core_pubmed_pmc | Screening of Key Fungal Strains in the Fermentation Process of the Chinese Medicinal Preparation “Lianzhifan Solution” Based on Metabolic Profiling and High-Throughput Sequencing Technology | Screening of Key Fungal Strains in the Fermentation Process of the Chinese Medicinal Preparation “Lianzhifan Solution” Based on Metabolic Profiling and High-Throughput Sequencing Technology Methods Materials and Reagents Coptis root, the dried rhizome of Coptis chinensis Franch (batch #470330), gardenia fruit, the drie... |
PMC11609621 | core_pubmed_pmc | A Preoperative Window-of-Opportunity Study of Oral SERD, Imlunestrant, in Newly Diagnosed ER-Positive, HER2-Negative Early Breast Cancer: Results from the EMBER-2 Study | A Preoperative Window-of-Opportunity Study of Oral SERD, Imlunestrant, in Newly Diagnosed ER-Positive, HER2-Negative Early Breast Cancer: Results from the EMBER-2 Study Abstract Abstract Purpose: Imlunestrant is an oral selective estrogen receptor degrader with favorable safety and preliminary efficacy in patients with... |
PMC9734692 | core_pubmed_pmc | In-silico docking studies of selected phytochemicals against papain like protease of SARS-Cov-2 | In-silico docking studies of selected phytochemicals against papain like protease of SARS-Cov-2 Abstract Abstract The SARS-Cov-2 virus, which is evolving continuously and causing adverse effects throughout the world, needs an effective drug molecule for its treatment. There are several receptors of SARS Cov-2 which are... |
PMC8285835 | core_pubmed_pmc | Impact of cumulative fluid balance on the pharmacokinetics of extended infusion meropenem in critically ill patients with sepsis | Impact of cumulative fluid balance on the pharmacokinetics of extended infusion meropenem in critically ill patients with sepsis Abstract Abstract Background Meropenem dosing for septic critically patients is difficult due to pathophysiological changes associated with sepsis as well as supportive symptomatic therapies.... |
PMC11952145 | core_pubmed_pmc | External Validation of a Pharmacokinetic Model Developed for Vancomycin Administration via Target-Controlled Infusion | External Validation of a Pharmacokinetic Model Developed for Vancomycin Administration via Target-Controlled Infusion Abstract Purpose Target-controlled infusion (TCI) could provide a patient-tailored approach for vancomycin dosing. This study aimed to externally evaluate the predictive performance of a previously cons... |
PMC5915605 | core_pubmed_pmc | Using a Vancomycin PBPK Model in Special Populations to Elucidate Case‐Based Clinical PK Observations | Using a Vancomycin PBPK Model in Special Populations to Elucidate Case‐Based Clinical PK Observations Abstract Abstract Simultaneous changes in several physiological factors may contribute to the large pharmacokinetic (PK) variability of vancomycin. This study was designed to systematically characterize the effects of ... |
PMC7494976 | core_pubmed_pmc | Efficacy of favipiravir for an end stage renal disease patient on maintenance hemodialysis infected with novel coronavirus disease 2019 | Efficacy of favipiravir for an end stage renal disease patient on maintenance hemodialysis infected with novel coronavirus disease 2019 Abstract Abstract Background Novel coronavirus disease 2019 (COVID-19) refers to infection with the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) pathogen, and has sprea... |
PMC12642550 | core_pubmed_pmc | A Precisely Controlled Long-Acting Immunosuppression Platform Enables Prolonged Survival of Vascularized Composite Allografts | A Precisely Controlled Long-Acting Immunosuppression Platform Enables Prolonged Survival of Vascularized Composite Allografts Abstract Vascularized composite allotransplantation (VCA) restores complex tissue defects but demands lifelong systemic immunosuppression. Oral tacrolimus (TAC) is limited by a narrow therapeuti... |
PMC5402961 | core_pubmed_pmc | The novel carboxylesterase 1 variant c.662A>G may decrease the bioactivation of oseltamivir in humans | The novel carboxylesterase 1 variant c.662A>G may decrease the bioactivation of oseltamivir in humans Abstract Background Human carboxylesterase 1 (CES1) is a serine esterase that hydrolyses various exogenous and endogenous compounds including oseltamivir, a prodrug used to treat influenza. A novel CES1 c.662A>G single... |
PMC7435660 | core_pubmed_pmc | Oral Bioavailability Evaluation of Celastrol-Encapsulated Silk Fibroin Nanoparticles Using an Optimized LC-MS/MS Method | Oral Bioavailability Evaluation of Celastrol-Encapsulated Silk Fibroin Nanoparticles Using an Optimized LC-MS/MS Method Abstract Celastrol (CL), a compound isolated from Tripterygium wilfordii , possesses various bioactivities such as antitumor, anti-inflammatory and anti-obesity effects. In previous studies, we develo... |
PMC8841484 | core_pubmed_pmc | Pharmacokinetics and safety of a novel influenza treatment (baloxavir marboxil) in Korean subjects compared with Japanese subjects | Pharmacokinetics and safety of a novel influenza treatment (baloxavir marboxil) in Korean subjects compared with Japanese subjects Abstract Abstract Baloxavir marboxil, a novel influenza therapeutic agent, is a prodrug rapidly metabolized into its active form, baloxavir acid, which inhibits cap‐dependent endonuclease. ... |
PMC8236590 | core_pubmed_pmc | PK/PD Modeling to Assess Rifaximin Clinical Dosage in a Mouse Model of Staphylococcus aureus- Induced Mastitis | PK/PD Modeling to Assess Rifaximin Clinical Dosage in a Mouse Model of Staphylococcus aureus- Induced Mastitis Abstract Staphylococcus aureus ( S. aureus ) is a common pathogen that causes mastitis, an infection of the milk-secreting tissue of the udder, in dairy cows, and presents a huge economic problem for the dairy... |
PMC11207139 | core_pubmed_pmc | Unveiling potent inhibitors for schistosomiasis through ligand-based drug design, molecular docking, molecular dynamics simulations and pharmacokinetics predictions | Unveiling potent inhibitors for schistosomiasis through ligand-based drug design, molecular docking, molecular dynamics simulations and pharmacokinetics predictions Abstract Schistosomiasis is a neglected tropical disease which imposes a considerable and enduring impact on affected regions, leading to persistent morbid... |
PMC12776344 | core_pubmed_pmc | Computational identification of Azadirachta indica compounds targeting trypanothione reductase in Leishmania infantum | Computational identification of Azadirachta indica compounds targeting trypanothione reductase in Leishmania infantum Abstract Abstract Motivation: Leishmania infantum is the primary cause of VL, and its trypanothione reductase (TR) creates a favorable environment in the host, making TR an attractive drug target. This ... |
PMC11463930 | core_pubmed_pmc | Target-controlled infusion – Past, present, and future | Target-controlled infusion – Past, present, and future Abstract Abstract Target-controlled infusion (TCI) is a novel drug delivery system wherein a microprocessor calculates the rate of drug to be infused based upon the target plasma or effect site concentration set by the operator. It has found its place in the operat... |
PMC11903327 | core_pubmed_pmc | Assessment of Food Effect and pH ‐Dependent Drug–Drug Interactions of Fruquintinib in Healthy Subjects | Assessment of Food Effect and pH ‐Dependent Drug–Drug Interactions of Fruquintinib in Healthy Subjects Abstract ABSTRACT This two‐sequence, three‐period study ( NCT04645940 ) was designed to evaluate the effect of food and concomitant rabeprazole, a proton pump inhibitor, on the pharmacokinetics (PK) and safety of fruq... |
PMC10745581 | core_pubmed_pmc | Population Pharmacokinetic and Pharmacodynamic Analysis for Maximizing the Effectiveness of Ceftobiprole in the Treatment of Severe Methicillin-Resistant Staphylococcal Infections | Population Pharmacokinetic and Pharmacodynamic Analysis for Maximizing the Effectiveness of Ceftobiprole in the Treatment of Severe Methicillin-Resistant Staphylococcal Infections Abstract Abstract Ceftobiprole is a fifth-generation cephalosporin used for different Gram-positive bacterial infections. A population pharm... |
PMC11954713 | core_pubmed_pmc | Exposure to Rifampicin and its Metabolite 25-Deacetylrifampicin Rapidly Decreases During Tuberculosis Therapy | Exposure to Rifampicin and its Metabolite 25-Deacetylrifampicin Rapidly Decreases During Tuberculosis Therapy Abstract Abstract Background and Objective Limited information is available on the pharmacokinetics of rifampicin (RIF) along with that of its active metabolite, 25-deacetylrifampicin (25-dRIF). This study aime... |
PMC4747995 | core_pubmed_pmc | Comparative pharmacokinetics, safety, and tolerability of two sources of ch14.18 in pediatric patients with high-risk neuroblastoma following myeloablative therapy | Comparative pharmacokinetics, safety, and tolerability of two sources of ch14.18 in pediatric patients with high-risk neuroblastoma following myeloablative therapy Abstract Purpose Dinutuximab (Unituxin™; ch14.18), a monoclonal antibody against disialoganglioside, improved survival as part of post-consolidation therapy... |
PMC12621112 | core_pubmed_pmc | A Phase 1 Study to Assess the Effect of Fruquintinib on the Pharmacokinetics of P‐gp and BCRP Substrates in Healthy Subjects | A Phase 1 Study to Assess the Effect of Fruquintinib on the Pharmacokinetics of P‐gp and BCRP Substrates in Healthy Subjects Abstract ABSTRACT Fruquintinib, a highly selective, oral inhibitor of all three vascular endothelial growth factor receptors (−1, −2, and −3), is approved for previously treated metastatic colore... |
PMC9025560 | core_pubmed_pmc | A Comparison of Evans Blue and 4-( p -Iodophenyl)butyryl Albumin Binding Moieties on an Integrin α v β 6 Binding Peptide | A Comparison of Evans Blue and 4-( p -Iodophenyl)butyryl Albumin Binding Moieties on an Integrin α v β 6 Binding Peptide Abstract Serum albumin binding moieties (ABMs) such as the Evans blue (EB) dye fragment and the 4-( p -iodophenyl)butyryl (IP) have been used to improve the pharmacokinetic profile of many radiopharm... |
PMC7827085 | core_pubmed_pmc | Interactions of Potential Anti-COVID-19 Compounds with Multispecific ABC and OATP Drug Transporters | Interactions of Potential Anti-COVID-19 Compounds with Multispecific ABC and OATP Drug Transporters Abstract Abstract During the COVID-19 pandemic, several repurposed drugs have been proposed to alleviate the major health effects of the disease. These drugs are often applied with analgesics or non-steroid anti-inflamma... |
PMC12733749 | core_pubmed_pmc | Thrombus Composition and the Evolving Role of Tenecteplase in Acute Ischemic Stroke | Thrombus Composition and the Evolving Role of Tenecteplase in Acute Ischemic Stroke Abstract Acute ischemic stroke (AIS) is a leading cause of disability and death worldwide, requiring rapid reperfusion to minimize damage. Current treatments, including intravenous thrombolysis (IVT) with alteplase (rt-PA) and mechanica... |
PMC12641136 | core_pubmed_pmc | Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Kuwait and the United Arab Emirates: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints | Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Kuwait and the United Arab Emirates: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints Abstract Abstract Objectives To determine antibiotic susceptibility of Streptococcus pneumoniae and Haemophilus influ... |
PMC7373747 | core_pubmed_pmc | Melaleuca armillaris Essential Oil in Combination With Rifaximin Against Staphylococcus aureus Isolated of Dairy Cows | Melaleuca armillaris Essential Oil in Combination With Rifaximin Against Staphylococcus aureus Isolated of Dairy Cows Abstract Staphylococcus aureus is the major subclinical mastitis-causing pathogen in dairy cows. In some European and Latin American countries, rifaximin (RIF) is a commonly used therapy at drying off. ... |
PMC9691146 | core_pubmed_pmc | Gentamicin Pharmacokinetics and Optimal Dosage in Infant Patients: A Case Report and Literature Review | Gentamicin Pharmacokinetics and Optimal Dosage in Infant Patients: A Case Report and Literature Review Abstract Gentamicin is an aminoglycoside antibiotic that is mostly used for the pediatric population. While the pediatric population is classified into neonates, infants, children, and adolescents based on development... |
PMC12388885 | core_pubmed_pmc | Systemic Metabolic Alterations Induced by Etodolac in Healthy Individuals | Systemic Metabolic Alterations Induced by Etodolac in Healthy Individuals Abstract Abstract Background/Objective: Pharmacological interventions often exert systemic effects beyond their primary targets, underscoring the need for a comprehensive evaluation of their metabolic impact. Etodolac is a nonsteroidal anti-infla... |
PMC7518311 | core_pubmed_pmc | CAR Chase: Where Do Engineered Cells Go in Humans? | CAR Chase: Where Do Engineered Cells Go in Humans? Abstract Abstract Chimeric antigen receptor (CAR) – and T-cell receptor (TCR) – modified T-cells are rapidly emerging as a viable treatment option for cancer patients. While initial clinical trials for these CAR T cells showed response rates of over 90% in some cases, ... |
PMC4886153 | core_pubmed_pmc | The pharmacokinetics of dexmedetomidine during long-term infusion in critically ill pediatric patients. A Bayesian approach with informative priors | The pharmacokinetics of dexmedetomidine during long-term infusion in critically ill pediatric patients. A Bayesian approach with informative priors Abstract Abstract The purpose of this study was to assess the pharmacokinetics of dexmedetomidine in the ICU settings during the prolonged infusion and to compare it with t... |
PMC10847580 | core_pubmed_pmc | Continuous long-range measurement of tonic dopamine with advanced FSCV for pharmacodynamic analysis of levodopa-induced dyskinesia in Parkinson’s disease | Continuous long-range measurement of tonic dopamine with advanced FSCV for pharmacodynamic analysis of levodopa-induced dyskinesia in Parkinson’s disease Abstract Levodopa, a dopamine prodrug, alleviates the motor symptoms of Parkinson’s disease (PD), but its chronic use gives rise to levodopa-induced dyskinesia (LID).... |
PMC8329445 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modelling for Nicotine and Cotinine Clearance in Pregnant Women | Physiologically Based Pharmacokinetic Modelling for Nicotine and Cotinine Clearance in Pregnant Women Abstract Abstract Introduction: Physiologically based pharmacokinetic (PBPK) models for the absorption, disposition, metabolism and excretion (ADME) of nicotine and its major metabolite cotinine in pregnant women (p-PB... |
PMC12227459 | core_pubmed_pmc | Nectin-4-Targeting Radiotracers: Novel Theranostic Agents for Precision Oncology in Cancer | Nectin-4-Targeting Radiotracers: Novel Theranostic Agents for Precision Oncology in Cancer Abstract Nectin cell adhesion molecule 4 (Nectin-4) is specifically overexpressed in most cancers of epithelial origin but downregulated in normal tissue, representing an ideal target for positron emission tomography imaging. The... |
PMC8927014 | core_pubmed_pmc | Efficacy and Safety of HSK3486 for Anesthesia/Sedation in Patients Undergoing Fiberoptic Bronchoscopy: A Multicenter, Double-Blind, Propofol-Controlled, Randomized, Phase 3 Study | Efficacy and Safety of HSK3486 for Anesthesia/Sedation in Patients Undergoing Fiberoptic Bronchoscopy: A Multicenter, Double-Blind, Propofol-Controlled, Randomized, Phase 3 Study Abstract Abstract Background Fiberoptic bronchoscopy is a complex procedure with the need for sufficient patient anesthesia/sedation while ma... |
PMC4373598 | core_pubmed_pmc | Pharmacokinetic drug interactions with clopidogrel: updated review and risk management in combination therapy | Pharmacokinetic drug interactions with clopidogrel: updated review and risk management in combination therapy Abstract Abstract Background Coprescribing of clopidogrel and other drugs is common. Available reviews have addressed the drug–drug interactions (DDIs) when clopidogrel is as an object drug, or focused on combi... |
PMC9281498 | core_pubmed_pmc | The Effects of Cumulative Dose and Polymorphisms in CYP2B6 on the Mitotane Plasma Trough Concentrations in Chinese Patients With Advanced Adrenocortical Carcinoma | The Effects of Cumulative Dose and Polymorphisms in CYP2B6 on the Mitotane Plasma Trough Concentrations in Chinese Patients With Advanced Adrenocortical Carcinoma Abstract Mitotane is the only drug approved to treat adrenocortical carcinoma (ACC), and a relationship of pharmacokinetic/pharmacodynamic has been character... |
PMC11715065 | core_pubmed_pmc | Dabigatran pharmacokinetic-pharmacodynamic in sheep: Informing dose for anticoagulation during cardiopulmonary bypass | Dabigatran pharmacokinetic-pharmacodynamic in sheep: Informing dose for anticoagulation during cardiopulmonary bypass Abstract Abstract Background The effect of the anticoagulant, dabigatran, and its antagonist, idarucizumab, on coagulation remains poorly quantified. There are few pharmacokinetic-pharmacodynamic data a... |
PMC12471887 | core_pubmed_pmc | Safety, Pharmacokinetics, and Food Effect of the RORα Agonist TB-840, a Novel Candidate for Metabolic Dysfunction-Associated Steatohepatitis (MASH): A Randomized First-in-Human Study in Healthy Volunteers | Safety, Pharmacokinetics, and Food Effect of the RORα Agonist TB-840, a Novel Candidate for Metabolic Dysfunction-Associated Steatohepatitis (MASH): A Randomized First-in-Human Study in Healthy Volunteers Abstract Abstract TB-840 is a novel RORα agonist being developed by Therasid Bioscience Inc. for the treatment of m... |
PMC4453610 | core_pubmed_pmc | Combination of letrozole, metronomic cyclophosphamide and sorafenib is well-tolerated and shows activity in patients with primary breast cancer | Combination of letrozole, metronomic cyclophosphamide and sorafenib is well-tolerated and shows activity in patients with primary breast cancer Abstract Abstract Purpose: To assess whether the combination of letrozole, metronomic cyclophosphamide and sorafenib (LCS) is well tolerated and shows activity in primary breas... |
PMC5098526 | core_pubmed_pmc | Effects of renal function on pharmacokinetics and pharmacodynamics of lesinurad in adult volunteers | Effects of renal function on pharmacokinetics and pharmacodynamics of lesinurad in adult volunteers Abstract Introduction Lesinurad is a selective uric acid reabsorption inhibitor approved for the treatment of gout in combination with a xanthine oxidase inhibitor (XOI) in patients who have not achieved target serum uri... |
PMC6738369 | core_pubmed_pmc | Prediction of Drug–Drug Interactions Between Opioids and Overdosed Benzodiazepines Using Physiologically Based Pharmacokinetic (PBPK) Modeling and Simulation | Prediction of Drug–Drug Interactions Between Opioids and Overdosed Benzodiazepines Using Physiologically Based Pharmacokinetic (PBPK) Modeling and Simulation Abstract Background Researchers have long been interested in the potential drug–drug interactions (DDIs) between opioids and benzodiazepines. However, much remain... |
PMC9821162 | core_pubmed_pmc | Foretinib Is Effective against Triple-Negative Breast Cancer Cells MDA-MB-231 In Vitro and In Vivo by Down-Regulating p-MET/HGF Signaling | Foretinib Is Effective against Triple-Negative Breast Cancer Cells MDA-MB-231 In Vitro and In Vivo by Down-Regulating p-MET/HGF Signaling Abstract Abstract This study investigated the antitumor effects of foretinib on triple-negative breast cancer cells MDA-MB-231 xenograft tumors in vivo underlying phosphorylated mese... |
PMC11961573 | core_pubmed_pmc | Feasibility and efficacy of therapeutic drug monitoring of abiraterone in metastatic castration resistant prostate cancer patients | Feasibility and efficacy of therapeutic drug monitoring of abiraterone in metastatic castration resistant prostate cancer patients Abstract Abstract Background Previous studies demonstrated better outcomes for mCRPC (metastatic castration resistant prostate cancer) patients with higher abiraterone exposure (minimal pla... |
PMC4112049 | core_pubmed_pmc | Pharmacokinetics of afatinib in subjects with mild or moderate hepatic impairment | Pharmacokinetics of afatinib in subjects with mild or moderate hepatic impairment Abstract Purpose Afatinib, an oral irreversible ErbB family blocker, undergoes minimal metabolism by non-enzyme-catalysed adduct formation with proteins or nucleophilic small molecules and is predominantly non-renally excreted via the ent... |
PMC6585716 | core_pubmed_pmc | Protein catalyzed capture agents with tailored performance for in vitro and in vivo applications | Protein catalyzed capture agents with tailored performance for in vitro and in vivo applications Abstract Abstract We report on peptide‐based ligands matured through the protein catalyzed capture (PCC) agent method to tailor molecular binders for in vitro sensing/diagnostics and in vivo pharmacokinetics parameters. A v... |
PMC10065422 | core_pubmed_pmc | Self-Assembling Lecithin-Based Mixed Polymeric Micelles for Nose to Brain Delivery of Clozapine: In-vivo Assessment of Drug Efficacy via Radiobiological Evaluation | Self-Assembling Lecithin-Based Mixed Polymeric Micelles for Nose to Brain Delivery of Clozapine: In-vivo Assessment of Drug Efficacy via Radiobiological Evaluation Abstract Abstract Purpose The research objective is to design intranasal brain targeted CLZ loaded lecithin based polymeric micelles (CLZ- LbPM) aiming to i... |
PMC12313750 | core_pubmed_pmc | A Randomized Phase I Trial Evaluating Safety and Pharmacokinetics of Single and Multiple Ascending Doses of Eclitasertib, a RIPK1 Inhibitor, in Healthy Participants | A Randomized Phase I Trial Evaluating Safety and Pharmacokinetics of Single and Multiple Ascending Doses of Eclitasertib, a RIPK1 Inhibitor, in Healthy Participants Abstract Abstract Introduction Receptor-interacting protein kinase 1 (RIPK1) is a master regulator of inflammation and necroptotic cell death and is implic... |
PMC7179635 | core_pubmed_pmc | A Novel Inhaled Dry-Powder Formulation of Ribavirin Allows for Efficient Lung Delivery in Healthy Participants and Those with Chronic Obstructive Pulmonary Disease in a Phase 1 Study | A Novel Inhaled Dry-Powder Formulation of Ribavirin Allows for Efficient Lung Delivery in Healthy Participants and Those with Chronic Obstructive Pulmonary Disease in a Phase 1 Study Abstract Chronic obstructive pulmonary disease (COPD) is an inflammatory lung condition, causing progressive decline in lung function lea... |
PMC12804884 | core_pubmed_pmc | Novel niclosamide-derived Schiff bases as a dual-targeted anticancer agents | Novel niclosamide-derived Schiff bases as a dual-targeted anticancer agents Abstract Abstract Nicosamide (NIC), an approved anthelmintic medication, has demonstrated encouraging antitumor action. To enhance NIC’s pharmacokinetic and pharmacodynamic characteristics and make it a potential anticancer drug, thirteen NIC-S... |
PMC5012889 | core_pubmed_pmc | Cardiac action of the first G protein biased small molecule apelin agonist | Cardiac action of the first G protein biased small molecule apelin agonist Abstract Abstract Apelin peptide analogues displaying bias towards G protein signalling pathways have beneficial cardiovascular actions compared with the native peptide in humans in vivo . Our aim was to determine whether small molecule agonists... |
PMC8953954 | core_pubmed_pmc | Pharmacokinetic Evaluation of a Novel Transdermal Ketoprofen Formulation in Healthy Dogs | Pharmacokinetic Evaluation of a Novel Transdermal Ketoprofen Formulation in Healthy Dogs Abstract Dogs undergo various surgical procedures such as castration, ovariohysterectomy, and other orthopedic procedures, which are known to cause inflammation and pain. Non-steroidal anti-inflammatory drugs (NSAIDs) are very effe... |
PMC12845442 | core_pubmed_pmc | Mathematical Modeling of Local Drug Delivery in the Oral Cavity: From Release Kinetics to Mini-PBPK and Local PK/PD with Applications to Periodontal Therapies | Mathematical Modeling of Local Drug Delivery in the Oral Cavity: From Release Kinetics to Mini-PBPK and Local PK/PD with Applications to Periodontal Therapies Abstract Abstract Background/Objectives: Mathematical modelling provides a quantitative way to describe the fate and action of drugs in the oral cavity, where tr... |
PMC5746161 | core_pubmed_pmc | Concise Review: Quantitative Detection and Modeling the In Vivo Kinetics of Therapeutic Mesenchymal Stem/Stromal Cells | Concise Review: Quantitative Detection and Modeling the In Vivo Kinetics of Therapeutic Mesenchymal Stem/Stromal Cells Abstract Abstract Mesenchymal stem/stromal cells (MSCs) present a promising tool in cell‐based therapy for treatment of various diseases. Currently, optimization of treatment protocols in clinical stud... |
PMC5915071 | core_pubmed_pmc | Influence of aprepitant and localization of the patch on fentanyl exposure in patients with cancer using transdermal fentanyl | Influence of aprepitant and localization of the patch on fentanyl exposure in patients with cancer using transdermal fentanyl Abstract Background and Objectives The cutaneous fentanyl patch is widely used to treat continuous pain in patients with cancer. Its use is hampered by a high inter- and intrapatient pharmacokin... |
PMC10082216 | core_pubmed_pmc | Safe drugs with high potential to block malaria transmission revealed by a spleen-mimetic screening | Safe drugs with high potential to block malaria transmission revealed by a spleen-mimetic screening Abstract Abstract Malaria parasites like Plasmodium falciparum multiply in red blood cells (RBC), which are cleared from the bloodstream by the spleen when their deformability is altered. Drug-induced stiffening of Plasm... |
PMC6412613 | core_pubmed_pmc | Administration of DDAVP did not improve the pharmacokinetics of FVIII concentrate in a clinically significant manner | Administration of DDAVP did not improve the pharmacokinetics of FVIII concentrate in a clinically significant manner Abstract Abstract Background: The half-life and mean residence time (MRT) of infused recombinant factor VIII (FVIII) concentrate are associated with pre-infusion levels of von Willebrand factor (VWF) in ... |
PMC5634662 | core_pubmed_pmc | Reversibility of the effects of natalizumab on peripheral immune cell dynamics in MS patients | Reversibility of the effects of natalizumab on peripheral immune cell dynamics in MS patients Abstract Objective: To characterize the reversibility of natalizumab-mediated changes in pharmacokinetics/pharmacodynamics in patients with multiple sclerosis (MS) following therapy interruption. Methods: Pharmacokinetic/pharm... |
PMC12746370 | core_pubmed_pmc | AZD0449, an inhaled JAK1 inhibitor, in healthy participants and patients with mild asthma | AZD0449, an inhaled JAK1 inhibitor, in healthy participants and patients with mild asthma Abstract Aims Inhaled corticosteroids (ICS) plus bronchodilator are recommended for the treatment of asthma. Targeting the JAK1‐dependent pathway may be an alternative for asthma management in patients with incomplete response to ... |
PMC3551254 | core_pubmed_pmc | Functional Polymorphisms in Xenobiotic Metabolizing Enzymes and Their Impact on the Therapy of Breast Cancer | Functional Polymorphisms in Xenobiotic Metabolizing Enzymes and Their Impact on the Therapy of Breast Cancer Abstract Abstract Breast cancer is the top cancer among women, and its incidence is increasing worldwide. Although the mortality tends to decrease due to early detection and treatment, there is great variability... |
PMC11459966 | core_pubmed_pmc | Oral pharmacokinetics and efficacy of oral phospholipid remdesivir nucleoside prodrugs against SARS-CoV-2 in mice | Oral pharmacokinetics and efficacy of oral phospholipid remdesivir nucleoside prodrugs against SARS-CoV-2 in mice Abstract ABSTRACT Oral broad-spectrum antivirals are urgently needed for the treatment of many emerging and contemporary RNA viruses. We previously synthesized 1- O -octadecyl-2- O -benzyl- sn -glyceryl-P-R... |
PMC6273141 | core_pubmed_pmc | LC-UV Determination of Baicalin in Rabbit Plasma and Tissues for Application in Pharmacokinetics and Tissue Distribution Studies of Baicalin after Intravenous Administration of Liposomal and Injectable Formulations | LC-UV Determination of Baicalin in Rabbit Plasma and Tissues for Application in Pharmacokinetics and Tissue Distribution Studies of Baicalin after Intravenous Administration of Liposomal and Injectable Formulations Abstract Abstract A simple and sensitive LC-UV method to investigate the pharmacokinetics and biodistribu... |
PMC10002520 | core_pubmed_pmc | Protein Abundance of Drug Metabolizing Enzymes in Human Hepatitis C Livers | Protein Abundance of Drug Metabolizing Enzymes in Human Hepatitis C Livers Abstract Abstract Hepatic drug metabolizing enzymes (DMEs), whose activity may be affected by liver diseases, are major determinants of drug pharmacokinetics. Hepatitis C liver samples in different functional states, i.e., the Child–Pugh class A... |
PMC8851091 | core_pubmed_pmc | Exposure driven dose escalation design with overdose control: Concept and first real life experience in an oncology phase I trial | Exposure driven dose escalation design with overdose control: Concept and first real life experience in an oncology phase I trial Abstract Abstract Background Escalation With Overdose Control (EWOC) designs are increasingly used to ensure dose-toxicity curve of investigational oncology drugs is efficiently characterize... |
PMC12881064 | core_pubmed_pmc | Design Optimization for Developing Population Pharmacokinetic Models in Critically Ill Children: Application to Teicoplanin, Piperacillin and Meropenem | Design Optimization for Developing Population Pharmacokinetic Models in Critically Ill Children: Application to Teicoplanin, Piperacillin and Meropenem Abstract Abstract Background and Objective Population pharmacokinetic (popPK) models in pediatric patients are essential to optimize dosing and ensure therapeutic effic... |
PMC11649707 | core_pubmed_pmc | Pharmacokinetics of Enteral Lormetazepam in Mechanically Ventilated ICU Patients with COVID-19: An Adjunct Sedative Study | Pharmacokinetics of Enteral Lormetazepam in Mechanically Ventilated ICU Patients with COVID-19: An Adjunct Sedative Study Abstract Abstract Background and Objective During the coronavirus disease 2019 (COVID-19) pandemic, sedative prescriptions surged, leading to shortages of midazolam. This study investigates lormetaz... |
PMC12549612 | core_pubmed_pmc | Optimizing antifungal dosing for invasive Cryptococcus infections: minimum inhibitory concentration distributions and pharmacokinetic/pharmacodynamic insights from 2010–2023 Antimicrobial Testing Leadership and Surveillance data | Optimizing antifungal dosing for invasive Cryptococcus infections: minimum inhibitory concentration distributions and pharmacokinetic/pharmacodynamic insights from 2010–2023 Antimicrobial Testing Leadership and Surveillance data Abstract Objective The 2024 global cryptococcosis treatment guidelines suggests that flucon... |
PMC4735769 | core_pubmed_pmc | Pediatric phase I trial of oral sorafenib and topotecan in refractory or recurrent pediatric solid malignancies | Pediatric phase I trial of oral sorafenib and topotecan in refractory or recurrent pediatric solid malignancies Abstract Abstract Targeted kinase inhibitors and camptothecins have shown preclinical and clinical activity in several cancers. This trial evaluated the maximum tolerated dose ( MTD ) and dose‐limiting toxici... |
PMC9171211 | core_pubmed_pmc | Rationale and design of a prospective study evaluating population pharmacokinetics and pharmacodynamics of rivaroxaban in Chinese patients with non-valvular atrial fibrillation | Rationale and design of a prospective study evaluating population pharmacokinetics and pharmacodynamics of rivaroxaban in Chinese patients with non-valvular atrial fibrillation Abstract Introduction Rivaroxaban is one of the most commonly used non-vitamin K antagonists for stroke prevention in patients with non-valvula... |
PMC12911304 | core_pubmed_pmc | Real world use of dalbavancin for bone and joint infections: a retrospective case series in adults and children | Real world use of dalbavancin for bone and joint infections: a retrospective case series in adults and children Abstract Background Bone and joint infections (BJIs) often require prolonged parenteral therapy, with challenges of hospitalization and vascular access [1–4]. Dalbavancin, a long-acting lipoglycopeptide, enab... |
PMC9046607 | core_pubmed_pmc | PBPK Modeling on Organs-on-Chips: An Overview of Recent Advancements | PBPK Modeling on Organs-on-Chips: An Overview of Recent Advancements Abstract Organ-on-a-chip (OoC) is a new and promising technology, which aims to improve the efficiency of drug development and realize personalized medicine by simulating in vivo environment in vitro . Physiologically based pharmacokinetic (PBPK) mode... |
PMC10967865 | core_pubmed_pmc | Impact of Pharmacogenetic Testing on Clozapine Treatment Efficacy in Patients with Treatment-Resistant Schizophrenia | Impact of Pharmacogenetic Testing on Clozapine Treatment Efficacy in Patients with Treatment-Resistant Schizophrenia Abstract Managing schizophrenia with clozapine poses a significant challenge due to prevalent therapeutic failures. The increasing interest in personalized medicine underscores the importance of integrat... |
PMC12291912 | core_pubmed_pmc | Halicin: A New Approach to Antibacterial Therapy, a Promising Avenue for the Post-Antibiotic Era | Halicin: A New Approach to Antibacterial Therapy, a Promising Avenue for the Post-Antibiotic Era Abstract Background: The global spread of antibiotic-resistant bacteria presents a major public health challenge and necessitates the development of innovative antimicrobial agents. Artificial intelligence (AI)-driven drug ... |
PMC6469250 | core_pubmed_pmc | Repurposing the KCa3.1 inhibitor senicapoc for Alzheimer's disease | Repurposing the KCa3.1 inhibitor senicapoc for Alzheimer's disease Abstract Abstract Objective Microglia play a pivotal role in the initiation and progression of Alzheimer's disease (AD). We here tested the therapeutic hypothesis that the Ca 2+ ‐activated potassium channel KCa3.1 constitutes a potential target for trea... |
PMC5787907 | core_pubmed_pmc | Pharmacokinetic Behavior of Phenytoin in Head Trauma and Cerebrovascular Accident Patients in an Iranian Population | Pharmacokinetic Behavior of Phenytoin in Head Trauma and Cerebrovascular Accident Patients in an Iranian Population Abstract Objective: Acute brain injury is one of the leading causes of morbidity and mortality worldwide. Phenytoin has been commonly used as an anticonvulsant agent for the treatment or prophylaxis of se... |
PMC3603431 | core_pubmed_pmc | From Pediatric Covariate Model to Semiphysiological Function for Maturation: Part I–Extrapolation of a Covariate Model From Morphine to Zidovudine | From Pediatric Covariate Model to Semiphysiological Function for Maturation: Part I–Extrapolation of a Covariate Model From Morphine to Zidovudine Abstract Abstract New approaches to expedite the development of safe and effective pediatric dosing regimens and first-in-child doses are urgently needed. Model-based approa... |
PMC12928622 | core_pubmed_pmc | Structure–activity insights and molecular modeling approaches of anti-TNBC agents: a comprehensive systematic review | Structure–activity insights and molecular modeling approaches of anti-TNBC agents: a comprehensive systematic review Abstract Abstract Aim Triple-negative breast cancer (TNBC) is a highly aggressive and treatment-resistant subtype of breast cancer, characterized by the lack of hormone receptor expression. This study ai... |
PMC6396318 | core_pubmed_pmc | The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K | The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K Abstract Irreversible covalent inhibitors can have a beneficial pharmacokinetic/pharmacodynamics profile but are still often avoided due to the risk of indiscriminate covalent reactivity and the resulting advers... |
PMC7712954 | core_pubmed_pmc | Review of the Novel Echinocandin Antifungal Rezafungin: Animal Studies and Clinical Data | Review of the Novel Echinocandin Antifungal Rezafungin: Animal Studies and Clinical Data Abstract Rezafungin is a novel echinocandin drug being developed as a first-line option for treatment and prevention of invasive fungal infections. As a result of a structural modification in its parent molecule anidulafungin, reza... |
PMC9230201 | core_pubmed_pmc | Sustained Consumption of a Decaffeinated Green Coffee Nutraceutical Has Limited Effects on Phenolic Metabolism and Bioavailability in Overweight/Obese Subjects | Sustained Consumption of a Decaffeinated Green Coffee Nutraceutical Has Limited Effects on Phenolic Metabolism and Bioavailability in Overweight/Obese Subjects Abstract Knowledge on the bioavailability of coffee (poly)phenols mostly come from single dose postprandial studies. This study aimed at investigating the effec... |
PMC6273305 | core_pubmed_pmc | Pharmacokinetic-Pharmacodynamic Modeling to Study the Antipyretic Effect of Qingkailing Injection on Pyrexia Model Rats | Pharmacokinetic-Pharmacodynamic Modeling to Study the Antipyretic Effect of Qingkailing Injection on Pyrexia Model Rats Abstract Abstract Qingkailing injection (QKLI) is a modern Chinese medicine preparation derived from a well-known classical formulation, An-Gong-Niu-Huang Wan. Although the clinical efficacy of QKLI h... |
PMC8629808 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of cyclopropylfentanyl in male rats | Pharmacokinetics and pharmacodynamics of cyclopropylfentanyl in male rats Abstract Abstract Background Illicitly manufactured fentanyl and its analogs are a major driving force behind the ongoing opioid crisis. Cyclopropylfentanyl is a fentanyl analog associated with many overdose deaths, but limited knowledge is avail... |
PMC9727203 | core_pubmed_pmc | Metals-triggered compound CDPDP exhibits anti-arthritic behavior by downregulating the inflammatory cytokines, and modulating the oxidative storm in mice models with extensive ADMET, docking and simulation studies | Metals-triggered compound CDPDP exhibits anti-arthritic behavior by downregulating the inflammatory cytokines, and modulating the oxidative storm in mice models with extensive ADMET, docking and simulation studies Abstract Abstract Triggering through abiotic stress, including chemical triggers like heavy metals, is a n... |
PMC7669784 | core_pubmed_pmc | Comparison of the ELISA and ECL Assay for Vedolizumab Anti-drug Antibodies: Assessing the Impact on Pharmacokinetics and Safety Outcomes of the Phase 3 GEMINI Trials | Comparison of the ELISA and ECL Assay for Vedolizumab Anti-drug Antibodies: Assessing the Impact on Pharmacokinetics and Safety Outcomes of the Phase 3 GEMINI Trials Abstract Abstract Vedolizumab immunogenicity has been assessed using an enzyme-linked immunosorbent assay (ELISA) with a ~ 0.5 μg/mL drug interference, wh... |
PMC7578827 | core_pubmed_pmc | Quantitative PCR methodology with a volume-based unit for the sophisticated cellular kinetic evaluation of chimeric antigen receptor T cells | Quantitative PCR methodology with a volume-based unit for the sophisticated cellular kinetic evaluation of chimeric antigen receptor T cells Abstract Abstract Although the cellular kinetics of chimeric antigen receptor T (CAR T) cells are expressed in units of copies/μg gDNA, this notation carries the risk of misrepres... |
PMC5447729 | core_pubmed_pmc | Selective Tissue Distribution Mediates Tissue-Dependent PPARγ Activation and Insulin Sensitization by INT131, a Selective PPARγ Modulator | Selective Tissue Distribution Mediates Tissue-Dependent PPARγ Activation and Insulin Sensitization by INT131, a Selective PPARγ Modulator Abstract Abstract The mechanisms underlying the enhancement of insulin sensitivity by selective peroxisome proliferator-activated receptor γ modulators (sPPARγMs) are still not compl... |
PMC7184321 | core_pubmed_pmc | Bioequivalence and pharmacodynamics of a generic dabigatran etexilate capsule in healthy Chinese subjects under fasting and fed conditions | Bioequivalence and pharmacodynamics of a generic dabigatran etexilate capsule in healthy Chinese subjects under fasting and fed conditions Abstract Abstract To assess bioequivalence of a generic dabigatran etexilate capsule in healthy Chinese subjects under fasting and fed conditions. This was an open‐label, single‐cen... |
PMC7078505 | core_pubmed_pmc | A mathematical model to predict nanomedicine pharmacokinetics and tumor delivery | A mathematical model to predict nanomedicine pharmacokinetics and tumor delivery Abstract Abstract Towards clinical translation of cancer nanomedicine, it is important to systematically investigate the various parameters related to nanoparticle (NP) physicochemical properties, tumor characteristics, and inter-individua... |
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