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PMC5108473 | core_pubmed_pmc | Comparative Review of Approved Melatonin Agonists for the Treatment of Circadian Rhythm Sleep‐Wake Disorders | Comparative Review of Approved Melatonin Agonists for the Treatment of Circadian Rhythm Sleep‐Wake Disorders Abstract Circadian rhythm sleep‐wake disorders ( CRSWD s) are characterized by persistent or recurrent patterns of sleep disturbance related primarily to alterations of the circadian rhythm system or the misalig... |
PMC12245229 | core_pubmed_pmc | Assessment of lamivudine, zidovudine, lopinavir, and ritonavir plasma levels in HIV-positive pregnant women | Assessment of lamivudine, zidovudine, lopinavir, and ritonavir plasma levels in HIV-positive pregnant women Abstract Supplemental Digital Content is available in the text Abstract Simultaneous therapeutic drug monitoring (TDM) of combination antiretroviral therapy (cART) is critical during pregnancy in order to improve... |
PMC8647901 | core_pubmed_pmc | SCREENER, an educational game for teaching the Drug Discovery and Development process | SCREENER, an educational game for teaching the Drug Discovery and Development process Abstract Abstract Although the use of games as an educational strategy is an important current trend, there is practically no option available for training people on the Drug Discovery and Development (DDD) process. To fill this gap, ... |
PMC9290941 | core_pubmed_pmc | Individualization of the infusion rate of a soybean oil–based intravenous lipid emulsion for inpatients, based on baseline triglyceride concentrations: A population pharmacokinetic approach | Individualization of the infusion rate of a soybean oil–based intravenous lipid emulsion for inpatients, based on baseline triglyceride concentrations: A population pharmacokinetic approach Abstract Abstract Background A rapid infusion rate for intravenous lipid emulsion (ILE) can cause adverse effects; therefore, safe... |
PMC10500467 | core_pubmed_pmc | Association between busulfan exposure and survival in patients undergoing a CD34 + selected stem cell transplantation | Association between busulfan exposure and survival in patients undergoing a CD34 + selected stem cell transplantation Abstract Key Points • Busulfan exposure is associated with OS; 5-year survival with an exposure of ≥59.5 vs <59.5 mg × h/L was 67% (95% CI, 59-76) vs 40%. • In 25% of the patients, busulfan levels were ... |
PMC9095561 | core_pubmed_pmc | “De-Shrinking” EBEs: The Solution for Bayesian Therapeutic Drug Monitoring | “De-Shrinking” EBEs: The Solution for Bayesian Therapeutic Drug Monitoring Abstract Abstract Background Therapeutic drug monitoring (TDM) aims at individualising a dosage regimen and is increasingly being performed by estimating individual pharmacokinetic parameters via empirical Bayes estimates (EBEs). However, EBEs s... |
PMC8400137 | core_pubmed_pmc | In Vitro Evaluation of Poly(lactide-co-glycolide) In Situ Forming Gels for Bedaquiline Fumarate Salt and Pharmacokinetics Following Subcutaneous Injection in Rats | In Vitro Evaluation of Poly(lactide-co-glycolide) In Situ Forming Gels for Bedaquiline Fumarate Salt and Pharmacokinetics Following Subcutaneous Injection in Rats Abstract This study evaluated in vitro and in vivo drug release of bedaquiline from in situ forming gels (ISGs) containing 200 mg eq./g bedaquiline fumarate ... |
PMC5928904 | core_pubmed_pmc | Safety of panitumumab-IRDye800CW and cetuximab-IRDye800CW for fluorescence-guided surgical navigation in head and neck cancers | Safety of panitumumab-IRDye800CW and cetuximab-IRDye800CW for fluorescence-guided surgical navigation in head and neck cancers Abstract Abstract Purpose: To demonstrate the safety and feasibility of leveraging therapeutic antibodies for surgical imaging. Procedures: We conducted two phase I trials for anti-epidermal gr... |
PMC7939287 | core_pubmed_pmc | A pilot study evaluating GSK1070806 inhibition of interleukin-18 in renal transplant delayed graft function | A pilot study evaluating GSK1070806 inhibition of interleukin-18 in renal transplant delayed graft function Abstract Introduction Delayed graft function (DGF) following renal transplantation is a manifestation of acute kidney injury (AKI) leading to poor long-term outcome. Current treatments have limited effectiveness ... |
PMC7836931 | core_pubmed_pmc | Identification of the metabolites of ivermectin in humans | Identification of the metabolites of ivermectin in humans Abstract Abstract Mass drug administration of ivermectin has been proposed as a possible malaria elimination tool. Ivermectin exhibits a mosquito‐lethal effect well beyond its biological half‐life, suggesting the presence of active slowly eliminated metabolites.... |
PMC7835327 | core_pubmed_pmc | Cannabinoids: A New Perspective on Epileptogenesis and Seizure Treatment in Early Life in Basic and Clinical Studies | Cannabinoids: A New Perspective on Epileptogenesis and Seizure Treatment in Early Life in Basic and Clinical Studies Abstract Abstract Neural hyperexcitability in the event of damage during early life, such as hyperthermia, hypoxia, traumatic brain injury, status epilepticus, or a pre-existing neuroinflammatory conditi... |
PMC10837484 | core_pubmed_pmc | LTA4H inhibitor LYS006: Clinical PK/PD and safety in a randomized phase I clinical trial | LTA4H inhibitor LYS006: Clinical PK/PD and safety in a randomized phase I clinical trial Abstract Abstract LYS006 is a novel, highly potent and selective, new‐generation leukotriene A4 hydrolase (LTA4H) inhibitor in clinical development for the treatment of neutrophil‐driven inflammatory diseases. We describe the compl... |
PMC12389164 | core_pubmed_pmc | ADMET-Guided Docking and GROMACS Molecular Dynamics of Ziziphus lotus Phytochemicals Uncover Mutation-Agnostic Allosteric Stabilisers of the KRAS Switch-I/II Groove | ADMET-Guided Docking and GROMACS Molecular Dynamics of Ziziphus lotus Phytochemicals Uncover Mutation-Agnostic Allosteric Stabilisers of the KRAS Switch-I/II Groove Abstract Background/Objectives: Oncogenic KRAS drives ~30% of solid tumours, yet the only approved G12C-specific drugs benefit ≈ 13% of KRAS-mutant patient... |
PMC12891312 | core_pubmed_pmc | Therapeutic potential of diosgenin in hepatocellular carcinoma through molecular mechanisms and nanodelivery strategies | Therapeutic potential of diosgenin in hepatocellular carcinoma through molecular mechanisms and nanodelivery strategies Abstract Purpose The review aims to comprehensively examine the anticancer potential of diosgenin, a natural steroidal sapogenin, in the context of hepatocellular carcinoma (HCC). It highlights the un... |
PMC7732531 | core_pubmed_pmc | Comparable Intestinal and Hepatic First-Pass Effect of YL-IPA08 on the Bioavailability and Effective Brain Exposure, a Rapid Anti-PTSD and Anti-Depression Compound | Comparable Intestinal and Hepatic First-Pass Effect of YL-IPA08 on the Bioavailability and Effective Brain Exposure, a Rapid Anti-PTSD and Anti-Depression Compound Abstract Abstract YL-IPA08, exerting rapid antidepressant-like and anxiolytic-like effects on behaviors by translocator protein (TSPO) mediation, is a novel... |
PMC8225519 | core_pubmed_pmc | A semi-mechanistic exposure–response model to assess the effects of verinurad, a potent URAT1 inhibitor, on serum and urine uric acid in patients with hyperuricemia-associated diseases | A semi-mechanistic exposure–response model to assess the effects of verinurad, a potent URAT1 inhibitor, on serum and urine uric acid in patients with hyperuricemia-associated diseases Abstract Abstract Verinurad, a uric acid transporter 1 (URAT1) inhibitor, lowers serum uric acid by promoting its urinary excretion. Co... |
PMC6989255 | core_pubmed_pmc | Effect of plasma membrane monoamine transporter genetic variants on pharmacokinetics of metformin in humans | Effect of plasma membrane monoamine transporter genetic variants on pharmacokinetics of metformin in humans Abstract Metformin, an oral hypoglycemic agent belonging to biguanide class, is widely used to treat type 2 diabetes mellitus, and several drug transporters such as organic cation transporters (OCTs), multidrug a... |
PMC7104137 | core_pubmed_pmc | Self-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid | Self-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid Abstract Abstract Purpose Ferulic acid (FA) is a natural compound which is used to treat insomnia. However, its use is limited because of its poor oral bioavailability caused by extremely rapid elimination. The c... |
PMC8551587 | core_pubmed_pmc | Suppression of ovulation and pharmacokinetics following subcutaneous administration of various doses of Depo-Provera®: a randomized trial | Suppression of ovulation and pharmacokinetics following subcutaneous administration of various doses of Depo-Provera®: a randomized trial Abstract Objectives: To identify the lowest dose of Depo-Provera that, when administered off-label subcutaneously, suppressed ovulation and had a pharmacokinetic profile consistent w... |
PMC7356118 | core_pubmed_pmc | Assessment of OMT-28, a synthetic analog of omega-3 epoxyeicosanoids, in patients with persistent atrial fibrillation: Rationale and design of the PROMISE-AF phase II study | Assessment of OMT-28, a synthetic analog of omega-3 epoxyeicosanoids, in patients with persistent atrial fibrillation: Rationale and design of the PROMISE-AF phase II study Abstract Abstract We designed a placebo controlled, double-blind, randomized, dose-finding phase II study on OMT-28 in the maintenance of sinus rhy... |
PMC11359463 | core_pubmed_pmc | Effect of Interindividual Variability in Metabolic Clearance and Relative Bioavailability on Rifampicin Exposure in Tuberculosis Patients with and without HIV Co-Infection: Does Formulation Quality Matter? | Effect of Interindividual Variability in Metabolic Clearance and Relative Bioavailability on Rifampicin Exposure in Tuberculosis Patients with and without HIV Co-Infection: Does Formulation Quality Matter? Abstract Abstract The present study aims to characterise the pharmacokinetics of rifampicin (RIF) in tuberculosis ... |
PMC7468301 | core_pubmed_pmc | Dose–response assessment by quantitative MRI in a phase 1 clinical study of the anti-cancer vascular disrupting agent crolibulin | Dose–response assessment by quantitative MRI in a phase 1 clinical study of the anti-cancer vascular disrupting agent crolibulin Abstract Abstract The vascular disrupting agent crolibulin binds to the colchicine binding site and produces anti-vascular and apoptotic effects. In a multisite phase 1 clinical study of crol... |
PMC6105164 | core_pubmed_pmc | An early clinical trial of Salirasib, an oral RAS inhibitor, in Japanese patients with relapsed/refractory solid tumors | An early clinical trial of Salirasib, an oral RAS inhibitor, in Japanese patients with relapsed/refractory solid tumors Abstract Purpose Patients with RAS -positive tumors respond poorly to chemotherapies and have a few treatment options. Salirasib is an oral RAS inhibitor that competitively blocks the membrane associa... |
PMC4183595 | core_pubmed_pmc | Study on the Main Components Interaction from Flos Lonicerae and Fructus Forsythiae and Their Dissolution In Vitro and Intestinal Absorption in Rats | Study on the Main Components Interaction from Flos Lonicerae and Fructus Forsythiae and Their Dissolution In Vitro and Intestinal Absorption in Rats Abstract The Flos Lonicerae-Fructus Forsythiae herb couple is the basic components of Chinese herbal preparations (Shuang-Huang-Lian tablet, Yin-Qiao-Jie-Du tablet and Fuf... |
PMC6768900 | core_pubmed_pmc | A Prospective Clinical Study Characterizing the Influence of Morbid Obesity on the Pharmacokinetics of Gentamicin: Towards Individualized Dosing in Obese Patients | A Prospective Clinical Study Characterizing the Influence of Morbid Obesity on the Pharmacokinetics of Gentamicin: Towards Individualized Dosing in Obese Patients Abstract Background and Objective Gentamicin is an aminoglycoside antibiotic predominantly used in bloodstream infections. Although the prevalence of obesity... |
PMC7960626 | core_pubmed_pmc | Phase I study assessing the mass balance, pharmacokinetics, and excretion of [ 14 C]-pevonedistat, a NEDD8-activating enzyme inhibitor in patients with advanced solid tumors | Phase I study assessing the mass balance, pharmacokinetics, and excretion of [ 14 C]-pevonedistat, a NEDD8-activating enzyme inhibitor in patients with advanced solid tumors Abstract Summary Pevonedistat (TAK-924/MLN4924) is an investigational small-molecule inhibitor of the NEDD8-activating enzyme that has demonstrate... |
PMC5289425 | core_pubmed_pmc | A Comparative Analysis of Drug-Induced Hepatotoxicity in Clinically Relevant Situations | A Comparative Analysis of Drug-Induced Hepatotoxicity in Clinically Relevant Situations Abstract Drug-induced toxicity is a significant problem in clinical care. A key problem here is a general understanding of the molecular mechanisms accompanying the transition from desired drug effects to adverse events following ad... |
PMC9290983 | core_pubmed_pmc | Multiparametric magnetic resonance imaging to characterize cabotegravir long‐acting formulation depot kinetics in healthy adult volunteers | Multiparametric magnetic resonance imaging to characterize cabotegravir long‐acting formulation depot kinetics in healthy adult volunteers Abstract Aim Cabotegravir long‐acting (LA) intramuscular (IM) injection is being investigated for HIV preexposure prophylaxis due to its potent antiretroviral activity and infrequen... |
PMC11636681 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of antibacterial peptide NZX in Staphylococcus aureus mastitis mouse model | Pharmacokinetics and pharmacodynamics of antibacterial peptide NZX in Staphylococcus aureus mastitis mouse model Abstract Abstract Staphylococcus aureus is associated with dairy mastitis, which causes serious economic losses to dairy farming industry. Antibacterial peptide NZX showed good antibacterial activity against... |
PMC9579403 | core_pubmed_pmc | A drug‐disease model for predicting survival in an Ebola outbreak | A drug‐disease model for predicting survival in an Ebola outbreak Abstract Abstract REGN‐EB3 (Inmazeb) is a cocktail of three human monoclonal antibodies approved for treatment of Ebola infection. This paper describes development of a mathematical model linking REGN‐EB3’s inhibition of Ebola virus to survival in a non‐... |
PMC6832453 | core_pubmed_pmc | Limonin: A Review of Its Pharmacology, Toxicity, and Pharmacokinetics | Limonin: A Review of Its Pharmacology, Toxicity, and Pharmacokinetics Abstract Limonin is a natural tetracyclic triterpenoid compound, which widely exists in Euodia rutaecarpa (Juss.) Benth., Phellodendron chinense Schneid., and Coptis chinensis Franch. Its extensive pharmacological effects have attracted considerable ... |
PMC9305550 | core_pubmed_pmc | Pharmacokinetic Drug Interaction Between Raloxifene and Cholecalciferol in Healthy Volunteers | Pharmacokinetic Drug Interaction Between Raloxifene and Cholecalciferol in Healthy Volunteers Abstract Abstract Osteoporosis is a common skeletal disorder, often leading to fragility fracture. Combination therapy with raloxifene, a selective estrogen receptor modulator, and cholecalciferol (vitamin D 3 ) has been propo... |
PMC6374012 | core_pubmed_pmc | Quantitative systems pharmacology of interferon alpha administration: A multi-scale approach | Quantitative systems pharmacology of interferon alpha administration: A multi-scale approach Abstract The therapeutic effect of a drug is governed by its pharmacokinetics which determine the downstream pharmacodynamic response within the cellular network. A complete understanding of the drug-effect relationship therefo... |
PMC3858972 | core_pubmed_pmc | Biological Activities and Pharmacokinetics of Praeruptorins from Peucedanum Species: A Systematic Review | Biological Activities and Pharmacokinetics of Praeruptorins from Peucedanum Species: A Systematic Review Abstract Abstract Praeruptorins belonging to the angular-type pyranocoumarins are bioactive constituents that have been isolated from some Peucedanum species such as P. praeruptorum , which is used in traditional Ch... |
PMC8739384 | core_pubmed_pmc | Impact of Plasma Donepezil Concentration on Behavioral and Psychological Symptoms of Dementia in Patients with Alzheimer's Disease | Impact of Plasma Donepezil Concentration on Behavioral and Psychological Symptoms of Dementia in Patients with Alzheimer's Disease Abstract Abstract Background/Aims The behavioral and psychological symptoms of dementia (BPSD) detract from the quality of life of not only dementia patients but also their family members a... |
PMC12956187 | core_pubmed_pmc | Fc-gamma receptors type3A (rs396991) genotyping for predicting infliximab efficacy and immunogenicity in ulcerative colitis: An observational study of Iraqi cohort | Fc-gamma receptors type3A (rs396991) genotyping for predicting infliximab efficacy and immunogenicity in ulcerative colitis: An observational study of Iraqi cohort Abstract Abstract Anti-tumor necrosis factor treatments for inflammatory bowel disease face challenges like primary nonresponse and secondary loss of respon... |
PMC8011718 | core_pubmed_pmc | First-line palliative systemic therapy alternated with electrostatic pressurised intraperitoneal aerosol chemotherapy (oxaliplatin) for isolated unresectable colorectal peritoneal metastases: protocol of a multicentre, single-arm, phase II study (CRC-PIPAC-II) | First-line palliative systemic therapy alternated with electrostatic pressurised intraperitoneal aerosol chemotherapy (oxaliplatin) for isolated unresectable colorectal peritoneal metastases: protocol of a multicentre, single-arm, phase II study (CRC-PIPAC-II) Abstract Introduction Despite its increasing use, first-lin... |
PMC12339816 | core_pubmed_pmc | Impact of Continuous Renal Replacement Therapy with Polyacrylonitrile-Derived Filter on Caspofungin Concentration: A Retrospective Study | Impact of Continuous Renal Replacement Therapy with Polyacrylonitrile-Derived Filter on Caspofungin Concentration: A Retrospective Study Abstract Introduction Caspofungin pharmacokinetics may be altered in critically ill patients. In vitro studies suggest significant drug adsorption with polyacrylonitrile (PAN) membran... |
PMC6110378 | core_pubmed_pmc | Exposure–Response Analysis of Micafungin in Neonatal Candidiasis | Exposure–Response Analysis of Micafungin in Neonatal Candidiasis Abstract Background: Neonatal candidiasis causes significant morbidity and mortality in high risk infants. The micafungin dosage regimen of 10 mg/kg established for the treatment of neonatal candidiasis is based on a laboratory animal model of neonatal he... |
PMC7614585 | core_pubmed_pmc | REFINE (REduced Frequency ImmuNE checkpoint inhibition in cancers): A multi-arm phase II basket trial testing reduced intensity immunotherapy across different cancers | REFINE (REduced Frequency ImmuNE checkpoint inhibition in cancers): A multi-arm phase II basket trial testing reduced intensity immunotherapy across different cancers Abstract Abstract Background Immune checkpoint inhibitors (ICI) have revolutionised treating advanced cancers. ICI are administered intravenously every 2... |
PMC10619670 | core_pubmed_pmc | Astragalin: a food-origin flavonoid with therapeutic effect for multiple diseases | Astragalin: a food-origin flavonoid with therapeutic effect for multiple diseases Abstract Naturally occurring flavonoids have long been utilized as essential templates for the development of novel drugs and as critical ingredients for functional foods. Astragalin (AG) is a natural flavonoid that can be isolated from a... |
PMC8877911 | core_pubmed_pmc | Anti-VEGF Drugs Dynamics: Relevance for Clinical Practice | Anti-VEGF Drugs Dynamics: Relevance for Clinical Practice Abstract Background: A drug and disease assessment model was used to evaluate the impact of different treatment regimens on intravitreal ranibizumab, bevacizumab, aflibercept, and brolucizumab concentrations and the proportion of free vascular endothelial growth... |
PMC11380339 | core_pubmed_pmc | A phase 3, randomized, double-blind, active-controlled clinical trial to compare BAT1806/BIIB800, a tocilizumab biosimilar, with tocilizumab reference product in participants with moderate-to-severe rheumatoid arthritis with inadequate response to methotrexate: treatment period 2 analysis (week 24 to week 48) | A phase 3, randomized, double-blind, active-controlled clinical trial to compare BAT1806/BIIB800, a tocilizumab biosimilar, with tocilizumab reference product in participants with moderate-to-severe rheumatoid arthritis with inadequate response to methotrexate: treatment period 2 analysis (week 24 to week 48) Abstract ... |
PMC4350951 | core_pubmed_pmc | In vitro dynamic pharmacokinetic/pharmacodynamic(PK/PD) modeling and PK/PD cutoff of cefquinome against Haemophilus parasuis | In vitro dynamic pharmacokinetic/pharmacodynamic(PK/PD) modeling and PK/PD cutoff of cefquinome against Haemophilus parasuis Abstract Background Haemophilus parasuis ( H. parasuis ) causes Glässer’s disease and multisystem infectious disease. It is one of the major causes of nursery mortality in swine herds. Cefquinome... |
PMC9225776 | core_pubmed_pmc | Proteolysis-targeting chimaeras (PROTACs) as pharmacological tools and therapeutic agents: advances and future challenges | Proteolysis-targeting chimaeras (PROTACs) as pharmacological tools and therapeutic agents: advances and future challenges Abstract Abstract Proteolysis-targeting chimaeras (PROTACs) have been developed to be an emerging technology for targeted protein degradation and attracted the favour of academic institutions, large... |
PMC6284558 | core_pubmed_pmc | Non-neutralizing antibodies increase endogenous circulating Ang1 levels | Non-neutralizing antibodies increase endogenous circulating Ang1 levels Abstract ABSTRACT Ang1 is a soluble ligand to receptor Tie2, and increasing the circulating Ang1 level may improve vascular stabilization under certain disease conditions. Here, we found that the circulating Ang1 level was significantly increased i... |
PMC6826847 | core_pubmed_pmc | Single-Dose Pharmacokinetics and Preliminary Safety Assessment with Use of CBD-Rich Hemp Nutraceutical in Healthy Dogs and Cats | Single-Dose Pharmacokinetics and Preliminary Safety Assessment with Use of CBD-Rich Hemp Nutraceutical in Healthy Dogs and Cats Abstract Abstract Simple Summary The use of cannabidiol (CBD)-rich hemp-based nutraceuticals is increasing in dogs and cats for disorders related to anxiety, seizures, cancer and pain. To date... |
PMC12521043 | core_pubmed_pmc | Moving From Point‐Based Analysis to Systems‐Based Modeling: Knowledge Integration to Address Antimicrobial Resistance | Moving From Point‐Based Analysis to Systems‐Based Modeling: Knowledge Integration to Address Antimicrobial Resistance Abstract ABSTRACT Optimizing antibiotic therapy requires a holistic bench‐to‐bedside approach with interdisciplinary collaboration between pharmacologists, clinicians, microbiologists, and computational... |
PMC4590874 | core_pubmed_pmc | Comparative Pharmacokinetics of Cefquinome (Cobactan 2.5%) following Repeated Intramuscular Administrations in Sheep and Goats | Comparative Pharmacokinetics of Cefquinome (Cobactan 2.5%) following Repeated Intramuscular Administrations in Sheep and Goats Abstract Abstract The comparative pharmacokinetic profile of cefquinome was studied in sheep and goats following repeated intramuscular (IM) administrations of 2 mg/kg body weight. Cefquinome c... |
PMC10385456 | core_pubmed_pmc | More Than Pigments: The Potential of Astaxanthin and Bacterioruberin-Based Nanomedicines | More Than Pigments: The Potential of Astaxanthin and Bacterioruberin-Based Nanomedicines Abstract Abstract Carotenoids are natural products regulated by the food sector, currently used as feed dyes and as antioxidants in dietary supplements and composing functional foods for human consumption. Of the nearly one thousan... |
PMC12479246 | core_pubmed_pmc | Pulmonary Rhizopus arrhizus infection treated with high-dose liposomal amphotericin B in a heart transplant recipient under ECMO: a case report | Pulmonary Rhizopus arrhizus infection treated with high-dose liposomal amphotericin B in a heart transplant recipient under ECMO: a case report Abstract Pulmonary mucormycosis caused by Rhizopus arrhizus is an emergent, fulminant threat in immunocompromised hosts, yet therapeutic success remains elusive when extracorpo... |
PMC9031611 | core_pubmed_pmc | Phase I Targeted Combination Trial of Sorafenib and GW5074 in Patients with Advanced Refractory Solid Tumors | Phase I Targeted Combination Trial of Sorafenib and GW5074 in Patients with Advanced Refractory Solid Tumors Abstract Abstract Background: Combination therapy with the administration of GW5074 and sorafenib significantly induced necrotic death in various cancer cells in vivo, as well as prolonging the survival of an an... |
PMC3658534 | core_pubmed_pmc | Esomeprazole and aspirin fixed combination for the prevention of cardiovascular events | Esomeprazole and aspirin fixed combination for the prevention of cardiovascular events Abstract Abstract Low dose aspirin therapy plays a fundamental role in both the primary and secondary prevention of cardiovascular events. Although the evidence using low dose aspirin for secondary prevention is well-established, the... |
PMC9835126 | core_pubmed_pmc | Developmental pharmacokinetics of indomethacin in preterm neonates: Severely decreased drug clearance in the first week of life | Developmental pharmacokinetics of indomethacin in preterm neonates: Severely decreased drug clearance in the first week of life Abstract Abstract Indomethacin is used commonly in preterm neonates for the prevention of intracranial hemorrhage and closure of an abnormally open cardiac vessel. Due to biomedical advances, ... |
PMC12443122 | core_pubmed_pmc | Developing decision support algorithm for hypertension medications for use in a digital therapeutic system | Developing decision support algorithm for hypertension medications for use in a digital therapeutic system Abstract Introduction Adherence to hypertension medications is low among older people, and there is limited guidance on the safety of taking a missed medication. Knowing the window of time when an older individual... |
PMC7346150 | core_pubmed_pmc | Acute Maternal Fasting or Fluid Abstention Does Not Significantly Affect the Macronutrient Composition of Human Milk: Clinical and Clinical Research Relevance | Acute Maternal Fasting or Fluid Abstention Does Not Significantly Affect the Macronutrient Composition of Human Milk: Clinical and Clinical Research Relevance Abstract Abstract There are guidelines on lactation following maternal analgo-sedative exposure, but these do not consider the effect of maternal fasting or flui... |
PMC12521053 | core_pubmed_pmc | Predicting Systemic and Liver Bosentan Exposure Using Physiologically‐Based Pharmacokinetic Modeling | Predicting Systemic and Liver Bosentan Exposure Using Physiologically‐Based Pharmacokinetic Modeling Abstract ABSTRACT Bosentan is the first approved oral medication for pulmonary arterial hypertension, yet the black‐box warning on its labeling implies a substantial risk of liver injury associated with bosentan exposur... |
PMC2957581 | core_pubmed_pmc | Effects of erythromycin on voriconazole pharmacokinetics and association with CYP2C19 polymorphism | Effects of erythromycin on voriconazole pharmacokinetics and association with CYP2C19 polymorphism Abstract Abstract Purpose To assess the impacts of erythromycin on the pharmacokinetics of voriconazole and its association with CYP2C19 genotypes in healthy Chinese male subjects. Methods A single-center, open, crossover... |
PMC11742468 | core_pubmed_pmc | Population pharmacokinetics and exposure-response analysis of durvalumab in combination with gemcitabine and cisplatin in patients with advanced biliary tract cancer | Population pharmacokinetics and exposure-response analysis of durvalumab in combination with gemcitabine and cisplatin in patients with advanced biliary tract cancer Abstract Abstract Purpose Durvalumab in combination with gemcitabine/cisplatin has shown a favorable benefit-risk profile in the TOPAZ-1 study for advance... |
PMC9340303 | core_pubmed_pmc | Transporter hypothesis in pharmacoresistant epilepsies. Is it at the central or peripheral level? | Transporter hypothesis in pharmacoresistant epilepsies. Is it at the central or peripheral level? Abstract Abstract The multidrug‐resistance (MDR) phenotype is typically observed in patients with refractory epilepsy (RE) whose seizures are not controlled despite receiving several combinations of more than two antiseizu... |
PMC12799537 | core_pubmed_pmc | Downregulation of hepatic sulfotransferase 1E1 expression associated with decreased expression of multidrug resistance–associated protein 2 | Downregulation of hepatic sulfotransferase 1E1 expression associated with decreased expression of multidrug resistance–associated protein 2 Abstract Abstract Changes in the expression of drug-metabolizing enzymes and transporters can alter the pharmacokinetics of drugs, potentially affecting their efficacy and safety. ... |
PMC6862065 | core_pubmed_pmc | Coix Seed Extract Enhances the Anti-Pancreatic Cancer Efficacy of Gemcitabine through Regulating ABCB1- and ABCG2-Mediated Drug Efflux: A Bioluminescent Pharmacokinetic and Pharmacodynamic Study | Coix Seed Extract Enhances the Anti-Pancreatic Cancer Efficacy of Gemcitabine through Regulating ABCB1- and ABCG2-Mediated Drug Efflux: A Bioluminescent Pharmacokinetic and Pharmacodynamic Study Abstract Abstract A deep insight into the function and kinetics of ATP-binding cassette (ABC) transporters may aid in the dev... |
PMC6225157 | core_pubmed_pmc | Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro Efficacy | Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro Efficacy Abstract Abstract With the aim improving drug delivery, liposomes have been employed as carriers for chemotherapeutics achieving promising results; their co-encapsulation with magnetic n... |
PMC7403138 | core_pubmed_pmc | Influence of Drug–Drug Interactions on the Pharmacokinetics of Atorvastatin and Its Major Active Metabolite ortho -OH-Atorvastatin in Aging People Living with HIV | Influence of Drug–Drug Interactions on the Pharmacokinetics of Atorvastatin and Its Major Active Metabolite ortho -OH-Atorvastatin in Aging People Living with HIV Abstract Abstract Background People living with HIV (PLWH) are aging and experience age-related physiological changes and comorbidities. Atorvastatin is a wi... |
PMC3927118 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Profile of Empagliflozin, a Sodium Glucose Co-Transporter 2 Inhibitor | Pharmacokinetic and Pharmacodynamic Profile of Empagliflozin, a Sodium Glucose Co-Transporter 2 Inhibitor Abstract Abstract Empagliflozin is an orally active, potent and selective inhibitor of sodium glucose co-transporter 2 (SGLT2), currently in clinical development to improve glycaemic control in adults with type 2 d... |
PMC4309801 | core_pubmed_pmc | Angiotensin Converting Enzyme Inhibitors (ACEI) and doxorubicin pharmacokinetics in women receiving adjuvant breast cancer treatment | Angiotensin Converting Enzyme Inhibitors (ACEI) and doxorubicin pharmacokinetics in women receiving adjuvant breast cancer treatment Abstract Purpose Doxorubicin (DOX) chemotherapy can cause cardiac complications. Angiotensin converting enzyme inhibitors (ACEI) may protect against these complications. We performed a ph... |
PMC12024220 | core_pubmed_pmc | Antimicrobial Dosing During Continuous Venovenous Hemodiafiltration in Septic Shock Patients: A Prospective, Multicenter Study Protocol | Antimicrobial Dosing During Continuous Venovenous Hemodiafiltration in Septic Shock Patients: A Prospective, Multicenter Study Protocol Abstract Background: Sepsis is a major global health issue and the leading cause of death in critically ill patients, with rising incidence and associated healthcare costs. Early admin... |
PMC12845042 | core_pubmed_pmc | Off-Label Ustekinumab and Vedolizumab in Pediatric Anti-TNFα Refractory IBD: Therapeutic Drug Monitoring Insights from a Case Series | Off-Label Ustekinumab and Vedolizumab in Pediatric Anti-TNFα Refractory IBD: Therapeutic Drug Monitoring Insights from a Case Series Abstract Background : Vedolizumab and ustekinumab are increasingly used off-label in pediatric inflammatory bowel disease (IBD) unresponsive or refractory to anti–TNFα therapy. Despite th... |
PMC9821128 | core_pubmed_pmc | Clinical Pharmacokinetics of Approved RNA Therapeutics | Clinical Pharmacokinetics of Approved RNA Therapeutics Abstract RNA-mediated drugs are a rapidly growing class of therapeutics. Over the last five years, the list of FDA-approved RNA therapeutics has expanded owing to their unique targets and prolonged pharmacological effects. Their absorption, distribution, metabolism... |
PMC6371059 | core_pubmed_pmc | Isolated hemopericardium after initiation of rivaroxaban: Implications and potential mechanisms | Isolated hemopericardium after initiation of rivaroxaban: Implications and potential mechanisms Abstract Direct oral anticoagulants have become increasingly used for atrial fibrillation and venothromboembolic disease. Thus far, there have been a few published cases of pericardial effusion associated with rivaroxban. Ho... |
PMC7785804 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of the Combination of Rhein and Curcumin in the Treatment of Chronic Kidney Disease in Rats | Pharmacokinetics and Pharmacodynamics of the Combination of Rhein and Curcumin in the Treatment of Chronic Kidney Disease in Rats Abstract Objectives: The interaction between the components of traditional Chinese medicine (TCM) is an important basis for their synergy. Rhein and curcumin exert various pharmacological ac... |
PMC7994819 | core_pubmed_pmc | Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers | Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers Abstract Abstract The formula of a standardized extract of Centella asiatica (ECa 233) was modified to improve its dissolution, with implications for pharmacokinetics and metabol... |
PMC9160923 | core_pubmed_pmc | A Candidate Drug Screen Strategy: The Discovery of Oroxylin A in Scutellariae Radix Against Sepsis via the Correlation Analysis Between Plant Metabolomics and Pharmacodynamics | A Candidate Drug Screen Strategy: The Discovery of Oroxylin A in Scutellariae Radix Against Sepsis via the Correlation Analysis Between Plant Metabolomics and Pharmacodynamics Abstract Abstract Sepsis is an acute systemic infectious disease with high mortality, which urgently needs more effective treatment. Scutellaria... |
PMC9796714 | core_pubmed_pmc | The pharmacology of blinatumomab: state of the art on pharmacodynamics, pharmacokinetics, adverse drug reactions and evaluation in clinical trials | The pharmacology of blinatumomab: state of the art on pharmacodynamics, pharmacokinetics, adverse drug reactions and evaluation in clinical trials Abstract Abstract What is known and objective Bispecific drugs (BDs) belong to the family of immunotherapies along with checkpoint inhibitors and CAR‐T cells. In the field o... |
PMC7495282 | core_pubmed_pmc | Effects of itraconazole and rifampicin on the single‐dose pharmacokinetics of the nonsteroidal mineralocorticoid receptor blocker esaxerenone in healthy Japanese subjects | Effects of itraconazole and rifampicin on the single‐dose pharmacokinetics of the nonsteroidal mineralocorticoid receptor blocker esaxerenone in healthy Japanese subjects Abstract Abstract Aims To investigate the effects of the strong cytochrome P450 (CYP) 3A inhibitor itraconazole and the strong CYP3A inducer rifampic... |
PMC3638148 | core_pubmed_pmc | Effects of Urotensin II Receptor Antagonist, GSK1440115, in Asthma | Effects of Urotensin II Receptor Antagonist, GSK1440115, in Asthma Abstract Background: Urotensin II (U-II) is highly expressed in the human lung and has been implicated in regulating respiratory physiology in preclinical studies. Our objective was to test antagonism of the urotensin (UT) receptor by GSK1440115, a nove... |
PMC8395935 | core_pubmed_pmc | Effects of Rapamycin on Insulin Brain Endothelial Cell Binding and Blood–Brain Barrier Transport | Effects of Rapamycin on Insulin Brain Endothelial Cell Binding and Blood–Brain Barrier Transport Abstract Rapamycin is an exogenous compound that has been shown to improve cognition in Alzheimer’s disease mouse models and can regulate pathways downstream of the insulin receptor signaling pathway. Insulin is also known ... |
PMC6136859 | core_pubmed_pmc | A multicenter phase 1 study of solitomab (MT110, AMG 110), a bispecific EpCAM/CD3 T-cell engager (BiTE®) antibody construct, in patients with refractory solid tumors | A multicenter phase 1 study of solitomab (MT110, AMG 110), a bispecific EpCAM/CD3 T-cell engager (BiTE®) antibody construct, in patients with refractory solid tumors Abstract ABSTRACT We assessed the tolerability and antitumor activity of solitomab, a bispecific T-cell engager (BiTE®) antibody construct targeting epith... |
PMC11173994 | core_pubmed_pmc | Exploring the Therapeutic Potential of Petiveria alliacea L. Phytochemicals: A Computational Study on Inhibiting SARS-CoV-2’s Main Protease (Mpro) | Exploring the Therapeutic Potential of Petiveria alliacea L. Phytochemicals: A Computational Study on Inhibiting SARS-CoV-2’s Main Protease (Mpro) Abstract The outbreak of SARS-CoV-2, also known as the COVID-19 pandemic, is still a critical risk factor for both human life and the global economy. Although, several promi... |
PMC5765475 | core_pubmed_pmc | Phase III Randomized Study of SB5, an Adalimumab Biosimilar, Versus Reference Adalimumab in Patients With Moderate‐to‐Severe Rheumatoid Arthritis | Phase III Randomized Study of SB5, an Adalimumab Biosimilar, Versus Reference Adalimumab in Patients With Moderate‐to‐Severe Rheumatoid Arthritis Abstract Abstract Objective SB5 is a biosimilar agent for adalimumab (ADA). The aim of this study was to evaluate the efficacy, pharmacokinetics (PK), safety, and immunogenic... |
PMC12707957 | core_pubmed_pmc | Population Pharmacokinetics and Dose Optimization of Valganciclovir and Ganciclovir in Lung Transplant Recipients | Population Pharmacokinetics and Dose Optimization of Valganciclovir and Ganciclovir in Lung Transplant Recipients Abstract Abstract Objective The primary goal of this study was to evaluate the pharmacokinetics (PK) of ganciclovir (GCV) and its prodrug valganciclovir (VGCV) in a large cohort of lung transplant recipient... |
PMC9273249 | core_pubmed_pmc | Comparative effects of fentanyl versus morphine on platelet inhibition induced by ticagrelor in patients with ST-segment elevation myocardial infarction: Full results of the PERSEUS randomized trial | Comparative effects of fentanyl versus morphine on platelet inhibition induced by ticagrelor in patients with ST-segment elevation myocardial infarction: Full results of the PERSEUS randomized trial Abstract Background Morphine reduces absorption and delays action onset of potent oral P2Y 12 receptor inhibitors in pati... |
PMC5488144 | core_pubmed_pmc | Comparison of a Novel Formulation of Abiraterone Acetate vs. the Originator Formulation in Healthy Male Subjects: Two Randomized, Open-Label, Crossover Studies | Comparison of a Novel Formulation of Abiraterone Acetate vs. the Originator Formulation in Healthy Male Subjects: Two Randomized, Open-Label, Crossover Studies Abstract Abstract Background and Objective Abiraterone acetate is approved for the treatment of metastatic castration-resistant prostate cancer. The originator ... |
PMC10383755 | core_pubmed_pmc | Preclinical Evaluation of Long-Acting Emtricitabine Semi-Solid Prodrug Nanoparticle Formulations | Preclinical Evaluation of Long-Acting Emtricitabine Semi-Solid Prodrug Nanoparticle Formulations Abstract Long-acting injectable (LAI) formulations promise to deliver patient benefits by overcoming issues associated with non-adherence. A preclinical assessment of semi-solid prodrug nanoparticle (SSPN) LAI formulations ... |
PMC8425836 | core_pubmed_pmc | Surviving Sepsis Campaign: Research Opportunities for Infection and Blood Purification Therapies | Surviving Sepsis Campaign: Research Opportunities for Infection and Blood Purification Therapies Abstract OBJECTIVES: Patients with infection can develop sepsis, and their mortality can be high. An important aspect in the treatment of sepsis is adequate management of the infection. DATA SOURCES: Using a modified Delphi... |
PMC6035265 | core_pubmed_pmc | Anti-survivin effect of the small molecule inhibitor YM155 in RCC cells is mediated by time-dependent inhibition of the NF-κB pathway | Anti-survivin effect of the small molecule inhibitor YM155 in RCC cells is mediated by time-dependent inhibition of the NF-κB pathway Abstract Abstract Constitutive activation of the NF-κB signaling cascade is associated with tumourigenesis and poor prognosis in many human cancers including RCC. YM155, a small molecule... |
PMC6786992 | core_pubmed_pmc | Minor contribution of cytochrome P450 3A activity on fentanyl exposure in palliative care cancer patients | Minor contribution of cytochrome P450 3A activity on fentanyl exposure in palliative care cancer patients Abstract Abstract Transdermal fentanyl is widely used to control pain in cancer patients. The high pharmacokinetic variability of fentanyl is assumed to be due to cytochrome P450 3A-mediated (CYP3A) N-dealkylation ... |
PMC8703483 | core_pubmed_pmc | Overdose of Quetiapine—A Case Report with QT Prolongation | Overdose of Quetiapine—A Case Report with QT Prolongation Abstract Quetiapine is an atypical antipsychotic drug used to treat bipolar disorder, schizophrenia, and major depressive disorder. Although several studies describe the adverse effects of intoxication with Quetiapine, only a few report an extreme overdose witho... |
PMC8111401 | core_pubmed_pmc | Radiation Increases Bioavailability of Lisinopril, a Mitigator of Radiation-Induced Toxicities | Radiation Increases Bioavailability of Lisinopril, a Mitigator of Radiation-Induced Toxicities Abstract Abstract There are no FDA-approved drugs to mitigate the delayed effects of radiation exposure that may occur after a radiological attack or nuclear accident. To date, angiotensin-converting enzyme inhibitors are one... |
PMC6857463 | core_pubmed_pmc | Copenhagen Head Injury Ciclosporin Study: A Phase IIa Safety, Pharmacokinetics, and Biomarker Study of Ciclosporin in Severe Traumatic Brain Injury Patients | Copenhagen Head Injury Ciclosporin Study: A Phase IIa Safety, Pharmacokinetics, and Biomarker Study of Ciclosporin in Severe Traumatic Brain Injury Patients Abstract Abstract Traumatic brain injury (TBI) contributes to almost one third of all trauma-related deaths, and those that survive often suffer from long-term phy... |
PMC10892419 | core_pubmed_pmc | UHPLC-MS/MS Assay for Quantification of Legubicin, a Novel Doxorubicin-Based Legumain-Activated Prodrug, and Its Application to Pharmacokinetic and Tissue Distribution Studies | UHPLC-MS/MS Assay for Quantification of Legubicin, a Novel Doxorubicin-Based Legumain-Activated Prodrug, and Its Application to Pharmacokinetic and Tissue Distribution Studies Abstract Legubicin, a novel prodrug based on doxorubicin, has both albumin-binding and legumain-activating properties. The aim of this study was... |
PMC4046020 | core_pubmed_pmc | A combined model of human erythropoiesis and granulopoiesis under growth factor and chemotherapy treatment | A combined model of human erythropoiesis and granulopoiesis under growth factor and chemotherapy treatment Abstract Abstract Background Haematotoxicity of conventional chemotherapies often results in delays of treatment or reduction of chemotherapy dose. To ameliorate these side-effects, patients are routinely treated ... |
PMC3053490 | core_pubmed_pmc | Effect of Acute Administration of an Herbal Preparation on Blood Pressure and Heart Rate in Humans | Effect of Acute Administration of an Herbal Preparation on Blood Pressure and Heart Rate in Humans Abstract Abstract Confusion and controversy exist regarding the cardiovascular effects of dietary supplements containing caffeine and Citrus aurantium (bitter orange) extract. The primary protoalkaloidal ingredient in bit... |
PMC11365999 | core_pubmed_pmc | Individualized regimen of Posaconazole oral suspension in Chinese HSCT patients based on population pharmacokinetic model | Individualized regimen of Posaconazole oral suspension in Chinese HSCT patients based on population pharmacokinetic model Abstract To establish a population pharmacokinetic (PopPK) model of posaconazole suspension in Chinese hematopoietic stem cell transplantation (HSCT) patients and to recommend an optimal dosing regi... |
PMC6970501 | core_pubmed_pmc | Population Pharmacokinetics of Clozapine: A Systematic Review | Population Pharmacokinetics of Clozapine: A Systematic Review Abstract Background and Objective Clozapine is a second-generation antipsychotic drug that is considered the most effective treatment for refractory schizophrenia. Several clozapine population pharmacokinetic models have been introduced in the last decades. ... |
PMC3587396 | core_pubmed_pmc | Cubic phase nanoparticles for sustained release of ibuprofen: formulation, characterization, and enhanced bioavailability study | Cubic phase nanoparticles for sustained release of ibuprofen: formulation, characterization, and enhanced bioavailability study Abstract Abstract In order to improve the oral bioavailability of ibuprofen, ibuprofen-loaded cubic nanoparticles were prepared as a delivery system for aqueous formulations. The cubic inner s... |
PMC4841112 | core_pubmed_pmc | Preclinical pharmacodynamic evaluation of antibiotic nitroxoline for anticancer drug repurposing | Preclinical pharmacodynamic evaluation of antibiotic nitroxoline for anticancer drug repurposing Abstract Abstract The established urinary antibiotic nitroxoline has recently regained considerable attention, due to its potent activities in inhibiting angiogenesis, inducing apoptosis and blocking cancer cell invasion. T... |
PMC6333391 | core_pubmed_pmc | Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin | Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin Abstract Abstract Purpose Rebaudioside A (RA) has nanocarrier characteristics that allow it to self-assemble into micelles in aqueous solutions. The purpose of this study was to determine if a sel... |
PMC11706904 | core_pubmed_pmc | Do P-glycoprotein-mediated drug-drug interactions at the blood-brain barrier impact morphine brain distribution? | Do P-glycoprotein-mediated drug-drug interactions at the blood-brain barrier impact morphine brain distribution? Abstract Abstract P-glycoprotein (P-gp) is a key efflux transporter and may be involved in drug-drug interactions (DDIs) at the blood-brain barrier (BBB), which could lead to changes in central nervous syste... |
PMC6028885 | core_pubmed_pmc | Increased Metformin Clearance in Overweight and Obese Adolescents: A Pharmacokinetic Substudy of a Randomized Controlled Trial | Increased Metformin Clearance in Overweight and Obese Adolescents: A Pharmacokinetic Substudy of a Randomized Controlled Trial Abstract Background In view of the increased use of metformin in obese adolescents, the aim of this study was to determine the pharmacokinetics of metformin in overweight and obese adolescents.... |
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