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PMC9414273 | core_pubmed_pmc | First-In-Human Phase I Study of a Next-Generation, Oral, TGFβ Receptor 1 Inhibitor, LY3200882, in Patients with Advanced Cancer | First-In-Human Phase I Study of a Next-Generation, Oral, TGFβ Receptor 1 Inhibitor, LY3200882, in Patients with Advanced Cancer Abstract Abstract Purpose: A novel, selective, next-generation transforming growth factor beta (TGFβ) receptor type-1 small molecule inhibitor, LY3200882, demonstrated promising preclinical da... |
PMC9965524 | core_pubmed_pmc | Antimicrobial Exposure in Critically Ill Patients with Sepsis-Associated Multi-Organ Dysfunction Requiring Extracorporeal Organ Support: A Narrative Review | Antimicrobial Exposure in Critically Ill Patients with Sepsis-Associated Multi-Organ Dysfunction Requiring Extracorporeal Organ Support: A Narrative Review Abstract Abstract Sepsis is a leading cause of disability and mortality worldwide. The pathophysiology of sepsis relies on the maladaptive host response to pathogen... |
PMC8987402 | core_pubmed_pmc | Non-compartmental toxicokinetic studies of the Nigerian Naja nigricollis venom | Non-compartmental toxicokinetic studies of the Nigerian Naja nigricollis venom Abstract Snakebite envenoming (SBE) is a neglected public health problem, especially in Asia, Latin America and Africa. There is inadequate knowledge of venom toxicokinetics especially from African snakes. To mimic a likely scenario of a sna... |
PMC5321811 | core_pubmed_pmc | Characterization of Contributing Factors to Variability in Morphine Clearance Through PBPK Modeling Implemented With OCT1 Transporter | Characterization of Contributing Factors to Variability in Morphine Clearance Through PBPK Modeling Implemented With OCT1 Transporter Abstract Morphine shows large interindividual variability in its pharmacokinetics; however, the cause of this has not been fully addressed. The variability in morphine disposition is con... |
PMC12353664 | core_pubmed_pmc | Status epilepticus in older adults: A critical review | Status epilepticus in older adults: A critical review Abstract Abstract Older adults (≥60 years of age) have the highest incidence of status epilepticus (SE) among adults and experience the highest morbidity and mortality. SE incidence increases with age in adulthood. A recent study from Austria estimated an incidence ... |
PMC4277127 | core_pubmed_pmc | A thorough QT study in the context of an uptitration regimen with selexipag, a selective oral prostacyclin receptor agonist | A thorough QT study in the context of an uptitration regimen with selexipag, a selective oral prostacyclin receptor agonist Abstract Abstract The effects of selexipag and its active metabolite ACT-333679 on cardiac repolarization were assessed in a thorough QT study as per International Conference on Harmonisation E14 ... |
PMC12561868 | core_pubmed_pmc | Gallic Acid from Elaeocarpus floribundus Stem Bark: A Potent Natural Antioxidant with Enzymatic and Pharmacokinetic Validation | Gallic Acid from Elaeocarpus floribundus Stem Bark: A Potent Natural Antioxidant with Enzymatic and Pharmacokinetic Validation Abstract Abstract The present study investigates the antioxidant potential of the stem bark of Elaeocarpus floribundus Blume through an integrated approach involving phytochemical isolation, in... |
PMC10059857 | core_pubmed_pmc | Does Cytokine-Release Syndrome Induced by CAR T-Cell Treatment Have an Impact on the Pharmacokinetics of Meropenem and Piperacillin/Tazobactam in Patients with Hematological Malignancies? Findings from an Observational Case-Control Study | Does Cytokine-Release Syndrome Induced by CAR T-Cell Treatment Have an Impact on the Pharmacokinetics of Meropenem and Piperacillin/Tazobactam in Patients with Hematological Malignancies? Findings from an Observational Case-Control Study Abstract Chimeric antigen receptor (CAR) T-cell therapy is a promising approach fo... |
PMC12457299 | core_pubmed_pmc | The effect of different combinations of flaxseed, melatonin, gum acacia, and betaine on diabetic rats with adenine-induced chronic kidney disease | The effect of different combinations of flaxseed, melatonin, gum acacia, and betaine on diabetic rats with adenine-induced chronic kidney disease Abstract Diabetes mellitus (DM) and chronic kidney disease (CKD) are associated with significant morbidity and mortality. Their progression is driven by inflammation, oxidati... |
PMC3078538 | core_pubmed_pmc | Assessment of receptor occupancy-over-time of two dopamine transporter inhibitors by [ 11 C]CIT and target controlled infusion | Assessment of receptor occupancy-over-time of two dopamine transporter inhibitors by [ 11 C]CIT and target controlled infusion Abstract Introduction Occupancy-over-time was determined for two dopamine transporter (DAT) inhibitors through modeling of their ability to displace the PET ligand [ 11 C]CIT. The tracer was he... |
PMC9099123 | core_pubmed_pmc | Effect of enzalutamide on PK of P‐gp and BCRP substrates in cancer patients: CYP450 induction may not always predict overall effect on transporters | Effect of enzalutamide on PK of P‐gp and BCRP substrates in cancer patients: CYP450 induction may not always predict overall effect on transporters Abstract Abstract Drug‐drug interaction (DDI) is an important consideration for clinical decision making in prostate cancer treatment. The objective of this study was to ev... |
PMC11503527 | core_pubmed_pmc | A Precision Engineered Interleukin-2 for Bolstering CD8 + T- and NK-cell Activity without Eosinophilia and Vascular Leak Syndrome in Nonhuman Primates | A Precision Engineered Interleukin-2 for Bolstering CD8 + T- and NK-cell Activity without Eosinophilia and Vascular Leak Syndrome in Nonhuman Primates Abstract Abstract We have created a precisely pegylated IL-2 [SAR-444245 (SAR’245) or pegenzileukin, previously THOR-707] designed for proliferation of target CD8 + T an... |
PMC11925105 | core_pubmed_pmc | Bioanalytical method validation to quantify ketorolac in human vitreous and aqueous via surrogate matrix of human plasma | Bioanalytical method validation to quantify ketorolac in human vitreous and aqueous via surrogate matrix of human plasma Abstract Abstract Purpose Intracameral phenylephrine 1.0%/ketorolac 0.3% (OMIDRIA ® ) is used during cataract surgery to prevent intraoperative miosis and reduce postoperative pain. Although studied ... |
PMC11026229 | core_pubmed_pmc | The Effect of Levetiracetam Compared with Enzyme-Inducing Antiseizure Medications on Apixaban and Rivaroxaban Peak Plasma Concentrations | The Effect of Levetiracetam Compared with Enzyme-Inducing Antiseizure Medications on Apixaban and Rivaroxaban Peak Plasma Concentrations Abstract Background and Objective Post-stroke epilepsy represents an important clinical challenge as it often requires both treatment with direct oral anticoagulants (DOACs) and antis... |
PMC8069869 | core_pubmed_pmc | PK/PD Analysis of Marbofloxacin by Monte Carlo Simulation against Mycoplasma agalactiae in Plasma and Milk of Lactating Goats after IV, SC and SC-Long Acting Formulations Administration | PK/PD Analysis of Marbofloxacin by Monte Carlo Simulation against Mycoplasma agalactiae in Plasma and Milk of Lactating Goats after IV, SC and SC-Long Acting Formulations Administration Abstract Abstract Simple Summary In some countries like Spain and France, contagious agalactia (CA) is a highly relevant issue. CA is ... |
PMC4557013 | core_pubmed_pmc | Eribulin in Cancer Treatment | Eribulin in Cancer Treatment Abstract Halichondrin B is a complex, natural, polyether macrolide derived from marine sponges. Eribulin is a structurally-simplified, synthetic, macrocyclic ketone analogue of Halichondrin B. Eribulin was approved by United States Food and Drug Administration in 2010 as a third-line therap... |
PMC10942698 | core_pubmed_pmc | Quantitative pharmacokinetic and biodistribution studies for fluorescent imaging agents | Quantitative pharmacokinetic and biodistribution studies for fluorescent imaging agents Abstract Abstract Pharmacokinetics and biodistribution studies are essential for characterizing fluorescent agents in vivo . However, few simple methods based on fluorescence imaging are available that account for tissue optical pro... |
PMC9283735 | core_pubmed_pmc | A phase I randomized, double‐blind , single subcutaneous dose escalation study to determine the safety, tolerability, and pharmacokinetics of rezafungin in healthy adult subjects | A phase I randomized, double‐blind , single subcutaneous dose escalation study to determine the safety, tolerability, and pharmacokinetics of rezafungin in healthy adult subjects Abstract Abstract Rezafungin is a novel echinocandin being developed for the treatment and prevention of invasive fungal infections. The obje... |
PMC6182869 | core_pubmed_pmc | Safety, tolerability and efficacy of the glutaminyl cyclase inhibitor PQ912 in Alzheimer’s disease: results of a randomized, double-blind, placebo-controlled phase 2a study | Safety, tolerability and efficacy of the glutaminyl cyclase inhibitor PQ912 in Alzheimer’s disease: results of a randomized, double-blind, placebo-controlled phase 2a study Abstract Background PQ912 is an inhibitor of the glutaminyl cyclase enzyme that plays a central role in the formation of synaptotoxic pyroglutamate... |
PMC9838834 | core_pubmed_pmc | Improvement of Antialveolar echinococcosis efficacy of novel Albendazole-Bile acids Derivatives with Enhanced Oral Bioavailability | Improvement of Antialveolar echinococcosis efficacy of novel Albendazole-Bile acids Derivatives with Enhanced Oral Bioavailability Abstract Alveolar echinococcosis (AE) is a chronic and fatal infectious parasitic disease, which has not been well-researched. Current recommended therapies for AE by the World Health Organ... |
PMC4625863 | core_pubmed_pmc | Quantitative Systems Pharmacology Approaches Applied to Microphysiological Systems (MPS): Data Interpretation and Multi-MPS Integration | Quantitative Systems Pharmacology Approaches Applied to Microphysiological Systems (MPS): Data Interpretation and Multi-MPS Integration Abstract Our goal in developing Microphysiological Systems (MPS) technology is to provide an improved approach for more predictive preclinical drug discovery via a highly integrated ex... |
PMC7698100 | core_pubmed_pmc | Pharmacokinetics of Marine-Derived Drugs | Pharmacokinetics of Marine-Derived Drugs Abstract Abstract Marine organisms represent an excellent source of innovative compounds that have the potential for the development of new drugs. The pharmacokinetics of marine drugs has attracted increasing interest in recent decades due to its effective and potential contribu... |
PMC7351053 | core_pubmed_pmc | Concerns about pharmacokinetic (PK) and pharmacokinetic-pharmacodynamic (PK-PD) studies in the new therapeutic area of COVID-19 infection | Concerns about pharmacokinetic (PK) and pharmacokinetic-pharmacodynamic (PK-PD) studies in the new therapeutic area of COVID-19 infection Abstract In the context of the COVID-19 pandemic, several drugs have been repurposed as potential candidates for the treatment of COVID-19 infection. While preliminary choices were e... |
PMC11839408 | core_pubmed_pmc | Bioanalytical method development, in-vivo pharmacokinetic evaluation, ex-vivo platelet aggregation inhibition activity of a novel solid dispersion formulation of ticagrelor | Bioanalytical method development, in-vivo pharmacokinetic evaluation, ex-vivo platelet aggregation inhibition activity of a novel solid dispersion formulation of ticagrelor Abstract Background Ticagrelor, a potential antithrombotic drug indicated for cardiovascular events with acute coronary syndrome, has been restrict... |
PMC12002915 | core_pubmed_pmc | Anti-cariogenic potential and pharmacokinetics of Licorice and Xylitol infused chewing gum | Anti-cariogenic potential and pharmacokinetics of Licorice and Xylitol infused chewing gum Abstract Background Dental caries remains a global health challenge despite advancements in prevention. Traditional approaches focus on mechanical plaque removal and fluoride use, but innovative, non-invasive solutions are increa... |
PMC9025605 | core_pubmed_pmc | Polymerized β-Cyclodextrin-Based Injectable Hydrogel for Sustained Release of 5-Fluorouracil/Methotrexate Mixture in Breast Cancer Management: In Vitro and In Vivo Analytical Validations | Polymerized β-Cyclodextrin-Based Injectable Hydrogel for Sustained Release of 5-Fluorouracil/Methotrexate Mixture in Breast Cancer Management: In Vitro and In Vivo Analytical Validations Abstract Abstract An inclusion complexation, between polymerized β-cyclodextrin and cholesterol end-capping branched polyethylene gly... |
PMC9503558 | core_pubmed_pmc | Insights into the Pharmacogenetics of Tacrolimus Pharmacokinetics and Pharmacodynamics | Insights into the Pharmacogenetics of Tacrolimus Pharmacokinetics and Pharmacodynamics Abstract The influence of pharmacogenetics in tacrolimus pharmacokinetics and pharmacodynamics needs further investigation, considering its potential in assisting clinicians to predict the optimal starting dosage and the need for a p... |
PMC6835836 | core_pubmed_pmc | Plasma Kinetics of Choline and Choline Metabolites After A Single Dose of Superba Boost TM Krill Oil or Choline Bitartrate in Healthy Volunteers | Plasma Kinetics of Choline and Choline Metabolites After A Single Dose of Superba Boost TM Krill Oil or Choline Bitartrate in Healthy Volunteers Abstract As an essential nutrient, the organic water-soluble compound choline is important for human health. Choline is required for numerous biological processes, including t... |
PMC12819455 | core_pubmed_pmc | Encapsulation of the lipidated TLR7/8 agonist INI-4001 into ionic liposomes impacts H7 influenza antigen-specific immune responses | Encapsulation of the lipidated TLR7/8 agonist INI-4001 into ionic liposomes impacts H7 influenza antigen-specific immune responses Abstract Abstract Toll-like receptors (TLRs) are the best characterized family of Pattern Recognition Receptor-targeting adjuvants. Activation of TLR7/8 in particular, enhances antigen pres... |
PMC3407247 | core_pubmed_pmc | Integrative Gene Expression Profiling Reveals G6PD-Mediated Resistance to RNA-Directed Nucleoside Analogues in B-Cell Neoplasms | Integrative Gene Expression Profiling Reveals G6PD-Mediated Resistance to RNA-Directed Nucleoside Analogues in B-Cell Neoplasms Abstract The nucleoside analogues 8-amino-adenosine and 8-chloro-adenosine have been investigated in the context of B-lineage lymphoid malignancies by our laboratories due to the selective cyt... |
PMC8803906 | core_pubmed_pmc | Metabolite Identification and Pharmacokinetic Behavior of Diaveridine in the Plasma of Pigs and Chickens Based on Radioactive Tracing Coupled With LC/MS-IT-TOF Assay | Metabolite Identification and Pharmacokinetic Behavior of Diaveridine in the Plasma of Pigs and Chickens Based on Radioactive Tracing Coupled With LC/MS-IT-TOF Assay Abstract Abstract Diaveridine (DVD) is widely used for the prevention and treatment of coccidiosis and leucocytozoonosis infections in food-producing anim... |
PMC10140208 | core_pubmed_pmc | Efficacy and Safety of CMAB008 Compared with Innovator Infliximab in Patients with Moderate-to-Severe Rheumatoid Arthritis Receiving Concomitant Methotrexate: A Randomized, Double-blind, Multi-center, Phase III Non-inferiority Study | Efficacy and Safety of CMAB008 Compared with Innovator Infliximab in Patients with Moderate-to-Severe Rheumatoid Arthritis Receiving Concomitant Methotrexate: A Randomized, Double-blind, Multi-center, Phase III Non-inferiority Study Abstract Objectives The aim of this work is to verify the non-inferior efficacy and saf... |
PMC11939005 | core_pubmed_pmc | Comparison of Molnupiravir Exposure‐Response Relationships for Virology Response and Mechanism of Action Biomarkers With Clinical Outcomes in Treatment of COVID ‐19 | Comparison of Molnupiravir Exposure‐Response Relationships for Virology Response and Mechanism of Action Biomarkers With Clinical Outcomes in Treatment of COVID ‐19 Abstract ABSTRACT Molnupiravir, an orally administered drug for the treatment of mild‐to‐moderate COVID‐19, is a prodrug of the ribonucleoside β‐D‐N4‐hydro... |
PMC8593125 | core_pubmed_pmc | Evaluation of the Effect of Proton Pump Inhibitors on the Efficacy of Dacomitinib and Gefitinib in Patients with Advanced Non-Small Cell Lung Cancer and EGFR-Activating Mutations | Evaluation of the Effect of Proton Pump Inhibitors on the Efficacy of Dacomitinib and Gefitinib in Patients with Advanced Non-Small Cell Lung Cancer and EGFR-Activating Mutations Abstract Abstract Introduction Dacomitinib and gefitinib are irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors ... |
PMC12521063 | core_pubmed_pmc | A Pharmacometric Workflow for Resolving Model Instability in Model Use‐Reuse Settings | A Pharmacometric Workflow for Resolving Model Instability in Model Use‐Reuse Settings Abstract ABSTRACT The development of fit‐for‐purpose pharmacokinetic‐pharmacodynamic (PKPD) models based on clinical and pre‐clinical data is a critically important process in model informed drug development. This process is often ham... |
PMC7825777 | core_pubmed_pmc | Improved Manufacturability and In Vivo Comparative Pharmacokinetics of Dapagliflozin Cocrystals in Beagle Dogs and Human Volunteers | Improved Manufacturability and In Vivo Comparative Pharmacokinetics of Dapagliflozin Cocrystals in Beagle Dogs and Human Volunteers Abstract Dapagliflozin (DAP), which improves glycemic control in patients with type 2 diabetes mellitus, has poor physical properties against heat and moisture, thus hindering its manufact... |
PMC5488074 | core_pubmed_pmc | Evaluation of the Pharmacokinetics and Pharmacodynamics of Prasugrel in Japanese Elderly Subjects | Evaluation of the Pharmacokinetics and Pharmacodynamics of Prasugrel in Japanese Elderly Subjects Abstract Background and Objective An increased incidence in bleeding events has been reported in Western elderly patients receiving prasugrel. Therefore, doses in Japanese elderly subjects need to be carefully determined. ... |
PMC8732856 | core_pubmed_pmc | Japanese subgroup analysis of the phase 3 MONARCH 3 study of abemaciclib as initial therapy for patients with hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer | Japanese subgroup analysis of the phase 3 MONARCH 3 study of abemaciclib as initial therapy for patients with hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer Abstract Background This was a Japanese subpopulation analysis of MONARCH 3, a randomized, double-blind, place... |
PMC9148403 | core_pubmed_pmc | 1,3,5-triazines inhibit osteosarcoma and avert lung metastasis in a patient-derived orthotopic xenograft mouse model with favorable pharmacokinetics | 1,3,5-triazines inhibit osteosarcoma and avert lung metastasis in a patient-derived orthotopic xenograft mouse model with favorable pharmacokinetics Abstract Abstract Objective(s): Osteosarcoma is a major solid malignant tumor of bone, possessing significant burden on healthcare due to non-availability of specific anti... |
PMC3257033 | core_pubmed_pmc | A phase 1, single-dose study of fresolimumab, an anti-TGF-β antibody, in treatment-resistant primary focal segmental glomerulosclerosis | A phase 1, single-dose study of fresolimumab, an anti-TGF-β antibody, in treatment-resistant primary focal segmental glomerulosclerosis Abstract Primary focal segmental glomerulosclerosis (FSGS) is a disease with poor prognosis and high unmet therapeutic need. Here, we evaluated the safety and pharmacokinetics of singl... |
PMC11227837 | core_pubmed_pmc | Nipocalimab, an anti-FcRn monoclonal antibody, in participants with moderate to severe active rheumatoid arthritis and inadequate response or intolerance to anti-TNF therapy: results from the phase 2a IRIS-RA study | Nipocalimab, an anti-FcRn monoclonal antibody, in participants with moderate to severe active rheumatoid arthritis and inadequate response or intolerance to anti-TNF therapy: results from the phase 2a IRIS-RA study Abstract Objectives To investigate the efficacy, safety, pharmacokinetics and pharmacodynamics of nipocal... |
PMC12001263 | core_pubmed_pmc | Model‐Informed Recommendation of Mavacamten Posology for Chinese Adults With Obstructive Hypertrophic Cardiomyopathy | Model‐Informed Recommendation of Mavacamten Posology for Chinese Adults With Obstructive Hypertrophic Cardiomyopathy Abstract ABSTRACT Mavacamten is a cardiac myosin inhibitor for adults with obstructive hypertrophic cardiomyopathy (HCM). Dose optimization is performed 4 weeks after starting mavacamten, guided by perio... |
PMC12648368 | core_pubmed_pmc | Model‐based evaluation of the interaction between ritonavir‐boosted atazanavir and rifampicin in Ugandan adults with HIV | Model‐based evaluation of the interaction between ritonavir‐boosted atazanavir and rifampicin in Ugandan adults with HIV Abstract Aim Concomitant treatment of tuberculosis (TB) and human immunodeficiency virus (HIV) is complicated by drug‐drug interactions (DDI). This analysis aimed to characterize the DDI between rito... |
PMC5614982 | core_pubmed_pmc | Impact of Gastric H + /K + -ATPase rs2733743 on the Intragastric pH-Values of Dexlansoprazole Injection in Chinese Subjects | Impact of Gastric H + /K + -ATPase rs2733743 on the Intragastric pH-Values of Dexlansoprazole Injection in Chinese Subjects Abstract Background: Not all patients with acid-related disorders receiving proton pump inhibitor (PP) treatment get adequate gastric pH control. The genetic variation of receptors, metabolic enzy... |
PMC6064589 | core_pubmed_pmc | No QTc Prolongation with Semaglutide: A Thorough QT Study in Healthy Subjects | No QTc Prolongation with Semaglutide: A Thorough QT Study in Healthy Subjects Abstract Abstract Introduction Semaglutide is a glucagon-like peptide-1 (GLP-1) analog approved for the once-weekly treatment of type 2 diabetes. The objective of this 16-week, double-blind, single-center thorough QT study was to confirm that... |
PMC11437156 | core_pubmed_pmc | Non-clinical evaluation of pmIL12 gene therapy for approval of the phase I clinical study | Non-clinical evaluation of pmIL12 gene therapy for approval of the phase I clinical study Abstract Immunotherapeutic drugs are promising medicines for cancer treatment. A potential candidate for immunotherapy is interleukin-12 (IL-12), a cytokine well known for its ability to mediate antitumor activity. We developed a ... |
PMC5946936 | core_pubmed_pmc | Relative Bioavailability, Intranasal Abuse Potential, and Safety of Benzhydrocodone/Acetaminophen Compared with Hydrocodone Bitartrate/Acetaminophen in Recreational Drug Abusers | Relative Bioavailability, Intranasal Abuse Potential, and Safety of Benzhydrocodone/Acetaminophen Compared with Hydrocodone Bitartrate/Acetaminophen in Recreational Drug Abusers Abstract Abstract Objectives Benzhydrocodone is a hydrocodone prodrug that has been combined with acetaminophen (APAP) in a novel immediate-re... |
PMC6280896 | core_pubmed_pmc | Population pharmacokinetic modeling of flurbiprofen, the active metabolite of flurbiprofen axetil, in Chinese patients with postoperative pain | Population pharmacokinetic modeling of flurbiprofen, the active metabolite of flurbiprofen axetil, in Chinese patients with postoperative pain Abstract Abstract Background Flurbiprofen axetil, a lipid-microsphere-carrier targeting preparation, is a non-steroidal anti-inflammatory drug indicated for the treatment of pos... |
PMC6520475 | core_pubmed_pmc | Development of a Population Pharmacokinetic Model of Vancomycin and its Application in Chinese Geriatric Patients with Pulmonary Infections | Development of a Population Pharmacokinetic Model of Vancomycin and its Application in Chinese Geriatric Patients with Pulmonary Infections Abstract Background The optimal use of vancomycin in the elderly requires information about the drug’s pharmacokinetics and the influence of various factors on the drug’s dispositi... |
PMC7735731 | core_pubmed_pmc | Application of Magnetic Core–Shell Imprinted Nanoconjugates for the Analysis of Hordenine in Human Plasma-Preliminary Data on Pharmacokinetic Study after Oral Administration | Application of Magnetic Core–Shell Imprinted Nanoconjugates for the Analysis of Hordenine in Human Plasma-Preliminary Data on Pharmacokinetic Study after Oral Administration Abstract In this paper, we developed and validated a new analytical method to determine the pharmacokinetic profile of hordenine in plasma samples... |
PMC5423977 | core_pubmed_pmc | Safety, pharmacokinetics, and pharmacodynamics of BMS-986142, a novel reversible BTK inhibitor, in healthy participants | Safety, pharmacokinetics, and pharmacodynamics of BMS-986142, a novel reversible BTK inhibitor, in healthy participants Abstract Abstract Purpose BMS-986142 is an oral, small-molecule reversible inhibitor of Bruton’s tyrosine kinase. The main objectives of our phase I studies were to characterize the safety and tolerab... |
PMC12733122 | core_pubmed_pmc | Rescuing Verubecestat: An Integrative Molecular Modeling and Simulation Approach for Designing Next-Generation BACE1 Inhibitors | Rescuing Verubecestat: An Integrative Molecular Modeling and Simulation Approach for Designing Next-Generation BACE1 Inhibitors Abstract β-site amyloid precursor protein cleaving enzyme 1 (BACE1) is a central therapeutic target in Alzheimer’s disease, as it catalyzes the rate-limiting step in amyloid-β production. Veru... |
PMC3362754 | core_pubmed_pmc | A Comprehensive Review of the Pharmacodynamics, Pharmacokinetics, and Clinical Effects of the Neutral Endopeptidase Inhibitor Racecadotril | A Comprehensive Review of the Pharmacodynamics, Pharmacokinetics, and Clinical Effects of the Neutral Endopeptidase Inhibitor Racecadotril Abstract Abstract Racecadotril, via its active metabolite thiorphan, is an inhibitor of the enzyme neutral endopeptidase (NEP, EC 3.4.24.11), thereby increasing exposure to NEP subs... |
PMC11175687 | core_pubmed_pmc | Pharmacokinetic-Pharmacodynamic Evidence From a Phase 3 Trial to Support Flat-Dosing of Rifampicin for Tuberculosis | Pharmacokinetic-Pharmacodynamic Evidence From a Phase 3 Trial to Support Flat-Dosing of Rifampicin for Tuberculosis Abstract Abstract Background The optimal dosing strategy for rifampicin in treating drug-susceptible tuberculosis (TB) is still highly debated. In the phase 3 clinical trial Study 31/ACTG 5349 ( NCT024107... |
PMC7249474 | core_pubmed_pmc | Population Pharmacokinetic–Pharmacodynamic Modeling of Inotersen, an Antisense Oligonucleotide for Treatment of Patients with Hereditary Transthyretin Amyloidosis | Population Pharmacokinetic–Pharmacodynamic Modeling of Inotersen, an Antisense Oligonucleotide for Treatment of Patients with Hereditary Transthyretin Amyloidosis Abstract Abstract A population pharmacokinetic (PK) and pharmacodynamic (PD) model was developed for inotersen to evaluate exposure–response relationships an... |
PMC6836807 | core_pubmed_pmc | Pharmacotherapy of Lower Respiratory Tract Infections in Elderly—Focused on Antibiotics | Pharmacotherapy of Lower Respiratory Tract Infections in Elderly—Focused on Antibiotics Abstract Lower respiratory tract infections (LRTIs) refer to the inflammation of the trachea, bronchi, bronchioles, and lung tissue. Old people have an increased risk of developing LRTIs compared to young adults. The prevalence of L... |
PMC12843011 | core_pubmed_pmc | Neurological Benefits of Seaweed-Derived Compounds | Neurological Benefits of Seaweed-Derived Compounds Abstract Seaweed represents a diverse group of marine organisms rich in bioactive compounds that have attracted interest for their potential relevance in neurological research. Recent studies highlight their ability to modulate neuroinflammation, oxidative stress, syna... |
PMC10088079 | core_pubmed_pmc | A model‐based meta analysis study of sodium glucose co‐transporter‐2 inhibitors | A model‐based meta analysis study of sodium glucose co‐transporter‐2 inhibitors Abstract Abstract Type 2 diabetes mellitus (T2DM) agent sodium‐glucose co‐transporter 2 (SGLT2) inhibitors show special benefits in reducing body weight and heart failure risks. To accelerate clinical development for novel SGLT2 inhibitors,... |
PMC10393882 | core_pubmed_pmc | Vancomycin population pharmacokinetics analysis in Chinese paediatric patients with varying degrees of renal function and ages: development of new practical dosing recommendations | Vancomycin population pharmacokinetics analysis in Chinese paediatric patients with varying degrees of renal function and ages: development of new practical dosing recommendations Abstract Abstract Objectives To describe the pharmacokinetics of vancomycin in a large Chinese paediatric cohort with varying degrees of ren... |
PMC12775886 | core_pubmed_pmc | Comparative Real-World Safety Profiles of Six Selective Serotonin Reuptake Inhibitors: A Global Pharmacovigilance Analysis | Comparative Real-World Safety Profiles of Six Selective Serotonin Reuptake Inhibitors: A Global Pharmacovigilance Analysis Abstract Background Selective serotonin reuptake inhibitors (SSRIs) represent the cornerstone of modern antidepressant therapy, yet critical knowledge gaps persist regarding their comparative real-... |
PMC9501129 | core_pubmed_pmc | A Pharmacokinetic Dose-Optimization Study of Cabotegravir and Bictegravir in a Mouse Pregnancy Model | A Pharmacokinetic Dose-Optimization Study of Cabotegravir and Bictegravir in a Mouse Pregnancy Model Abstract Abstract Animal pregnancy models can be useful tools to study HIV antiretroviral safety and toxicity and to perform mechanistic studies that are not easily performed in humans. Utilization of clinically relevan... |
PMC11939980 | core_pubmed_pmc | Opportunities and Challenges in Antibody–Drug Conjugates for Cancer Therapy: A New Era for Cancer Treatment | Opportunities and Challenges in Antibody–Drug Conjugates for Cancer Therapy: A New Era for Cancer Treatment Abstract Simple Summary Antibody–drug conjugates (ADCs) comprise a cytotoxic small molecule paired with a monoclonal antibody via a chemical linker. The antibody component reduces the cytotoxic effects on off-tar... |
PMC5968569 | core_pubmed_pmc | Integrating rare genetic variants into pharmacogenetic drug response predictions | Integrating rare genetic variants into pharmacogenetic drug response predictions Abstract Background Variability in genes implicated in drug pharmacokinetics or drug response can modulate treatment efficacy or predispose to adverse drug reactions. Besides common genetic polymorphisms, recent sequencing projects reveale... |
PMC4485797 | core_pubmed_pmc | Effect of renal impairment on the pharmacokinetics of levomilnacipran following a single oral dose of levomilnacipran extended-release capsule in humans | Effect of renal impairment on the pharmacokinetics of levomilnacipran following a single oral dose of levomilnacipran extended-release capsule in humans Abstract Purpose Levomilnacipran extended-release (ER) is indicated for treatment of major depressive disorder in adults. We evaluated the pharmacokinetic and safety p... |
PMC10384837 | core_pubmed_pmc | Retrospective Long-Term Evaluation of Miltefosine-Allopurinol Treatment in Canine Leishmaniosis | Retrospective Long-Term Evaluation of Miltefosine-Allopurinol Treatment in Canine Leishmaniosis Abstract Miltefosine-Allopurinol (MIL-AL) combination is reported to be one of the most effective treatments for canine leishmaniosis, thanks to its oral administration and MIL-documented low impact on renal function. Howeve... |
PMC11843511 | core_pubmed_pmc | Therapeutic Drug Distribution across the Mouse Brain Is Heterogeneous as Revealed by In Vivo, Spatially Resolved Aptamer-Based Sensing | Therapeutic Drug Distribution across the Mouse Brain Is Heterogeneous as Revealed by In Vivo, Spatially Resolved Aptamer-Based Sensing Abstract Drug discovery for central nervous system (CNS) targets is a high stakes process with estimated success rates below ten percent. Dose scaling, penetration through the blood–bra... |
PMC4819767 | core_pubmed_pmc | PGMD: a comprehensive manually curated pharmacogenomic database | PGMD: a comprehensive manually curated pharmacogenomic database Abstract The PharmacoGenomic Mutation Database (PGMD) is a comprehensive manually curated pharmacogenomics database. Two major sources of PGMD data are peer-reviewed literature and Food and Drug Administration (FDA) and European Medicines Agency (EMA) drug... |
PMC9543267 | core_pubmed_pmc | Pharmacokinetics of intravenous, oral transmucosal, and intranasal buprenorphine in healthy male dogs | Pharmacokinetics of intravenous, oral transmucosal, and intranasal buprenorphine in healthy male dogs Abstract Abstract Effective management of pain in animals is of critical importance but options are limited for treating acute pain in dogs on an outpatient basis. The objective of this study was to compare the plasma ... |
PMC10392001 | core_pubmed_pmc | ‘Walking epidural’: comparison of the analgesic efficacy of levobupivacaine 0.0625% + fentanyl 2mcg/mL versus ropivacaine 0.075% + fentanyl 2mcg/mL | ‘Walking epidural’: comparison of the analgesic efficacy of levobupivacaine 0.0625% + fentanyl 2mcg/mL versus ropivacaine 0.075% + fentanyl 2mcg/mL Abstract Introduction Epidural infusion with low local anesthetic concentrations with opiates decrease the severity of the motor blockade associated. The present study aims... |
PMC8623792 | core_pubmed_pmc | Variability of Tacrolimus Trough Concentration in Liver Transplant Patients: Which Role of Inflammation? | Variability of Tacrolimus Trough Concentration in Liver Transplant Patients: Which Role of Inflammation? Abstract Tacrolimus presents high intra and inter-individual variability in its blood trough concentration (Cmin). Knowledge of the factors that are involved in tacrolimus Cmin variability is thus clinically importa... |
PMC8838750 | core_pubmed_pmc | Peptide Self-Assembled Nanostructures: From Models to Therapeutic Peptides | Peptide Self-Assembled Nanostructures: From Models to Therapeutic Peptides Abstract Abstract Self-assembly is the most suitable approach to obtaining peptide-based materials on the nano- and mesoscopic scales. Applications span from peptide drugs for personalized therapy to light harvesting and electron conductive medi... |
PMC6412790 | core_pubmed_pmc | Multi-Organs-on-Chips: Towards Long-Term Biomedical Investigations | Multi-Organs-on-Chips: Towards Long-Term Biomedical Investigations Abstract Abstract With advantageous features such as minimizing the cost, time, and sample size requirements, organ-on-a-chip (OOC) systems have garnered enormous interest from researchers for their ability for real-time monitoring of physical parameter... |
PMC12322071 | core_pubmed_pmc | Nutritional status, body composition and chemotherapy dosing in children and young people with cancer: a systematic review by the SIOP nutrition network | Nutritional status, body composition and chemotherapy dosing in children and young people with cancer: a systematic review by the SIOP nutrition network Abstract Abstract Abstract Malnutrition (undernutrition or overweight/obesity) might significantly impact the pharmacokinetics and pharmacodynamics of antineoplastic d... |
PMC6921499 | core_pubmed_pmc | Right Dose Right Now: bedside data-driven personalized antibiotic dosing in severe sepsis and septic shock — rationale and design of a multicenter randomized controlled superiority trial | Right Dose Right Now: bedside data-driven personalized antibiotic dosing in severe sepsis and septic shock — rationale and design of a multicenter randomized controlled superiority trial Abstract Background Antibiotic exposure is often inadequate in critically ill patients with severe sepsis or septic shock and this is... |
PMC7877839 | core_pubmed_pmc | Pediatric Pharmacokinetics and Dose Predictions: A Report of a Satellite Meeting to the 10th Juvenile Toxicity Symposium | Pediatric Pharmacokinetics and Dose Predictions: A Report of a Satellite Meeting to the 10th Juvenile Toxicity Symposium Abstract On April 24, 2019, a symposium on Pediatric Pharmacokinetics and Dose Predictions was held as a satellite meeting to the 10th Juvenile Toxicity Symposium. This symposium brought together sci... |
PMC10967270 | core_pubmed_pmc | Intrapulmonary and Systemic Pharmacokinetics of Colistin Following Nebulization of Low-Dose Colistimethate Sodium in Patients with Ventilator-Associated Pneumonia Caused by Carbapenem-Resistant Acinetobacter baumannii | Intrapulmonary and Systemic Pharmacokinetics of Colistin Following Nebulization of Low-Dose Colistimethate Sodium in Patients with Ventilator-Associated Pneumonia Caused by Carbapenem-Resistant Acinetobacter baumannii Abstract Colistimethate sodium (CMS) nebulization is associated with reduced systemic toxicity compare... |
PMC10650097 | core_pubmed_pmc | A Phase I Trial of Sirolimus with “7&3” Induction Chemotherapy in Patients with Newly Diagnosed Acute Myeloid Leukemia | A Phase I Trial of Sirolimus with “7&3” Induction Chemotherapy in Patients with Newly Diagnosed Acute Myeloid Leukemia Abstract Abstract Simple Summary Relapsed or refractory AML remains common and difficult to treat, with no standard of care. Therefore, improving upfront therapy to prevent relapse in younger AML patie... |
PMC9686637 | core_pubmed_pmc | Population Pharmacokinetics of Orally Administered Clindamycin to Treat Prosthetic Joint Infections: A Prospective Study | Population Pharmacokinetics of Orally Administered Clindamycin to Treat Prosthetic Joint Infections: A Prospective Study Abstract Abstract A population PK model of clindamycin orally administered to patients with prosthetic joint infections (PJIs) was developed using NONMEM 7.5. Monte-Carlo simulations were run to dete... |
PMC12736283 | core_pubmed_pmc | A Comparative Study of Changes in Huanglian Jiedu Decoction with Combined Decoction and Single Decoction Based on Metabolomics-Physical Characterization-Transcriptomics Correlation Analysis | A Comparative Study of Changes in Huanglian Jiedu Decoction with Combined Decoction and Single Decoction Based on Metabolomics-Physical Characterization-Transcriptomics Correlation Analysis Abstract Background: Using Huanglian Jiedu decoction (HJD) as a model, this study systematically compares the traditionally prepar... |
PMC3000965 | core_pubmed_pmc | Hsp90 (Heat Shock Protein 90) Inhibitor Occupancy Is a Direct Determinant of Client Protein Degradation and Tumor Growth Arrest in Vivo * | Hsp90 (Heat Shock Protein 90) Inhibitor Occupancy Is a Direct Determinant of Client Protein Degradation and Tumor Growth Arrest in Vivo * Abstract Several Hsp90 (heat shock protein 90) inhibitors are currently under clinical evaluation as anticancer agents. However, the correlation between the duration and magnitude of... |
PMC12750381 | core_pubmed_pmc | Highly Potent Phosphinic HIV‑1 Protease Inhibitors: Synthesis, In Vitro Evaluation, and Docking Studies | Highly Potent Phosphinic HIV‑1 Protease Inhibitors: Synthesis, In Vitro Evaluation, and Docking Studies Abstract In the search for effective HIV-1 protease inhibitors, the design of symmetrical phosphinic pseudopeptides derived from a dual addition of hypophosphorous acid to acrylates ( PACs ) has emerged as a promisin... |
PMC9013650 | core_pubmed_pmc | Pharmacokinetics of alectinib and its metabolite M4 in a patient with advanced lung adenocarcinoma undergoing hemodialysis: A case report | Pharmacokinetics of alectinib and its metabolite M4 in a patient with advanced lung adenocarcinoma undergoing hemodialysis: A case report Abstract Abstract This study presents the first detailed pharmacokinetic data of alectinib and its metabolite M4 in a patient with anaplastic lymphoma kinase (ALK)‐rearranged lung ad... |
PMC12051630 | core_pubmed_pmc | Selective Mapping of Brain COX-1 with [11C]PS13: Pharmacokinetic Evidence from human PET Imaging | Selective Mapping of Brain COX-1 with [11C]PS13: Pharmacokinetic Evidence from human PET Imaging Abstract Abstract Background and aim Arachidonic acid is converted by cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) to prostaglandin H2, which has proinflammatory properties. The new PET radioligand [11 C]PS13 exhib... |
PMC7854383 | core_pubmed_pmc | Cellular Uptake of Psychostimulants – Are High- and Low-Affinity Organic Cation Transporters Drug Traffickers? | Cellular Uptake of Psychostimulants – Are High- and Low-Affinity Organic Cation Transporters Drug Traffickers? Abstract Abstract Psychostimulants are used therapeutically and for illegal recreational purposes. Many of these are inhibitors of the presynaptic noradrenaline, dopamine, and serotonin transporters (NET, DAT,... |
PMC5751239 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, Tolerability, and Food Effect of Cenerimod, a Selective S1P 1 Receptor Modulator in Healthy Subjects | Pharmacokinetics, Pharmacodynamics, Tolerability, and Food Effect of Cenerimod, a Selective S1P 1 Receptor Modulator in Healthy Subjects Abstract The pharmacokinetics, pharmacodynamics, tolerability, and food effect of cenerimod, a potent sphingosine-1-phosphate subtype 1 receptor modulator, were investigated in three ... |
PMC5725197 | core_pubmed_pmc | KEAP1 and done? Targeting the NRF2 pathway with sulforaphane | KEAP1 and done? Targeting the NRF2 pathway with sulforaphane Abstract Background Since the re-discovery of sulforaphane in 1992 and the recognition of the bioactivity of this phytochemical, many studies have examined its mode of action in cells, animals and humans. Broccoli, especially as young sprouts, is a rich sourc... |
PMC7883827 | core_pubmed_pmc | Antibacterial Activities of Echinops kebericho Mesfin Tuber Extracts and Isolation of the Most Active Compound, Dehydrocostus Lactone | Antibacterial Activities of Echinops kebericho Mesfin Tuber Extracts and Isolation of the Most Active Compound, Dehydrocostus Lactone Abstract Abstract Echinops kebericho Mesfin is traditionally used for the treatment of various infectious diseases. This study investigated antibacterial activity of the essential oil (E... |
PMC4648947 | core_pubmed_pmc | A phase 1 study of lenvatinib, multiple receptor tyrosine kinase inhibitor, in Japanese patients with advanced solid tumors | A phase 1 study of lenvatinib, multiple receptor tyrosine kinase inhibitor, in Japanese patients with advanced solid tumors Abstract Abstract Purpose This phase 1 study aimed to assess the tolerability, safety, pharmacokinetics (PK), pharmacodynamics, and preliminary efficacy of lenvatinib capsules in Japanese patients... |
PMC11670693 | core_pubmed_pmc | A phase I dose escalation study of the LRP5 antagonist BI 905681 in patients with advanced and metastatic solid tumors | A phase I dose escalation study of the LRP5 antagonist BI 905681 in patients with advanced and metastatic solid tumors Abstract Abstract Background The Wnt pathway is involved in proliferation and tissue homeostasis. Aberrant activation promotes cancer cell proliferation and survival. Inhibition of the low-density lipo... |
PMC9890214 | core_pubmed_pmc | Exploring the in situ evolution of nitrofurantoin resistance in clinically derived uropathogenic Escherichia coli isolates | Exploring the in situ evolution of nitrofurantoin resistance in clinically derived uropathogenic Escherichia coli isolates Abstract Abstract Background Nitrofurantoin has been re-introduced as a first-choice antibiotic to treat uncomplicated acute urinary tract infections in England and Wales. Highly effective against ... |
PMC10050777 | core_pubmed_pmc | Clinical Characteristics and Pharmacokinetics Change of Long-Term Responders to Antiprogrammed Cell Death Protein 1 Inhibitor Among Patients With Advanced NSCLC | Clinical Characteristics and Pharmacokinetics Change of Long-Term Responders to Antiprogrammed Cell Death Protein 1 Inhibitor Among Patients With Advanced NSCLC Abstract Abstract Introduction Immune checkpoint inhibitors (ICIs) induce long-term, durable responses in patients with advanced NSCLC. Nevertheless, these res... |
PMC11471892 | core_pubmed_pmc | A Smart CA IX-Targeting and pH-Responsive Nano-Mixed Micelles for Delivery of FB15 with Superior Anti-Breast Cancer Efficacy | A Smart CA IX-Targeting and pH-Responsive Nano-Mixed Micelles for Delivery of FB15 with Superior Anti-Breast Cancer Efficacy Abstract Background Breast cancer treatment has been a global puzzle, and targeted strategies based on the hypoxic tumor microenvironment (TME) have attracted extensive attention. As a signature ... |
PMC8206310 | core_pubmed_pmc | Population Pharmacokinetic Model of N -acetylmannosamine (ManNAc) and N -acetylneuraminic acid (Neu5Ac) in Subjects with GNE Myopathy | Population Pharmacokinetic Model of N -acetylmannosamine (ManNAc) and N -acetylneuraminic acid (Neu5Ac) in Subjects with GNE Myopathy Abstract Abstract Background GNE myopathy is a rare genetic muscle disease resulting from deficiency in an enzyme critical for the biosynthesis of N -acetylneuraminic acid (Neu5Ac, siali... |
PMC9667150 | core_pubmed_pmc | Untargeted metabolomics to evaluate polymyxin B toxicodynamics following direct intracerebroventricular administration into the rat brain | Untargeted metabolomics to evaluate polymyxin B toxicodynamics following direct intracerebroventricular administration into the rat brain Abstract Abstract There is a dearth of studies focused on understanding pharmacokinetics, pharmacodynamics and toxicodynamics of polymyxins following direct administration to the cen... |
PMC5680807 | core_pubmed_pmc | Protein engineering to increase the potential of a therapeutic antibody Fab for long-acting delivery to the eye | Protein engineering to increase the potential of a therapeutic antibody Fab for long-acting delivery to the eye Abstract ABSTRACT To date, ocular antibody therapies for the treatment of retinal diseases rely on injection of the drug into the vitreous chamber of the eye. Given the burden for patients undergoing this pro... |
PMC8584265 | core_pubmed_pmc | Stress Driven Discovery of Natural Products From Actinobacteria with Anti-Oxidant and Cytotoxic Activities Including Docking and ADMET Properties | Stress Driven Discovery of Natural Products From Actinobacteria with Anti-Oxidant and Cytotoxic Activities Including Docking and ADMET Properties Abstract Elicitation through abiotic stress, including chemical elicitors like heavy metals, is a new technique for drug discovery. In this research, the effect of heavy meta... |
PMC3249179 | core_pubmed_pmc | The relationship between clinical pharmacokinetics of aripiprazole and CYP2D6 genetic polymorphism: effects of CYP enzyme inhibition by coadministration of paroxetine or fluvoxamine | The relationship between clinical pharmacokinetics of aripiprazole and CYP2D6 genetic polymorphism: effects of CYP enzyme inhibition by coadministration of paroxetine or fluvoxamine Abstract Purpose To investigate the effects of coadministration of paroxetine or fluvoxamine on the pharmacokinetics of aripiprazole in he... |
PMC4754918 | core_pubmed_pmc | Population pharmacokinetic properties of artemisinin in healthy male Vietnamese volunteers | Population pharmacokinetic properties of artemisinin in healthy male Vietnamese volunteers Abstract Abstract Background Artemisinin-based combination therapy is recommended as first-line anti-malarial treatment worldwide. A combination of artemisinin with the long acting drug piperaquine has shown high efficacy and tol... |
PMC11088557 | core_pubmed_pmc | Impact of Viloxazine Extended-Release Capsules (Qelbree ® ) on Select Cytochrome P450 Enzyme Activity and Evaluation of CYP2D6 Genetic Polymorphisms on Viloxazine Pharmacokinetics | Impact of Viloxazine Extended-Release Capsules (Qelbree ® ) on Select Cytochrome P450 Enzyme Activity and Evaluation of CYP2D6 Genetic Polymorphisms on Viloxazine Pharmacokinetics Abstract Background and Objective Viloxazine extended-release (ER) [Qelbree ® ] is a nonstimulant attention-deficit/hyperactivity disorder (... |
PMC10578324 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of Zagotenemab in Participants with Symptomatic Alzheimer’s Disease: A Phase I Clinical Trial | Safety, Tolerability, and Pharmacokinetics of Zagotenemab in Participants with Symptomatic Alzheimer’s Disease: A Phase I Clinical Trial Abstract Abstract Background: Zagotenemab (LY3303560), a monoclonal antibody, preferentially binds to extracellular, misfolded, aggregated tau that has been implicated in Alzheimer’s ... |
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