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PMC10071078 | core_pubmed_pmc | PemBla: A Phase 1 study of intravesical pembrolizumab in recurrent non‐muscle‐invasive bladder cancer | PemBla: A Phase 1 study of intravesical pembrolizumab in recurrent non‐muscle‐invasive bladder cancer Abstract Abstract Objectives This study aimed to investigate the anti‐PD‐1 inhibitor pembrolizumab as a potential agent for use in non‐muscle‐invasive bladder cancer (NMIBC) by conducting a Phase 1 safety run‐in study ... |
PMC8801896 | core_pubmed_pmc | Feasibility of Catalpol Intranasal Administration and Its Protective Effect on Acute Cerebral Ischemia in Rats via Anti-Oxidative and Anti-Apoptotic Mechanisms | Feasibility of Catalpol Intranasal Administration and Its Protective Effect on Acute Cerebral Ischemia in Rats via Anti-Oxidative and Anti-Apoptotic Mechanisms Abstract Purpose Catalpol is the main active component of Rehmannia glutinosa, which has a variety of pharmacological activities, including anti-inflammatory an... |
PMC8697541 | core_pubmed_pmc | Multiple Sclerosis in Children: Differential Diagnosis, Prognosis, and Disease-Modifying Treatment | Multiple Sclerosis in Children: Differential Diagnosis, Prognosis, and Disease-Modifying Treatment Abstract Pediatric-onset multiple sclerosis (POMS) is a rare neuroinflammatory and neurodegenerative disease that has a significant impact on long-term physical and cognitive patient outcomes. A small percentage of multip... |
PMC9887206 | core_pubmed_pmc | Cationic biopolymer decorated Asiatic Acid and Centella asiatica extract incorporated liposomes for treating early-stage Alzheimer’s disease: An In-vitro and In-vivo investigation | Cationic biopolymer decorated Asiatic Acid and Centella asiatica extract incorporated liposomes for treating early-stage Alzheimer’s disease: An In-vitro and In-vivo investigation Abstract Abstract Background: Asiatic acid (AA) is a naturally occurring triterpenoid derivative of Centella asiatica (CA) with neuroprotect... |
PMC6409069 | core_pubmed_pmc | Recognition and Optimization of Ingredients Treating Nitroglycerin-Induced Migraine Rats from Wuzhuyu Decoction | Recognition and Optimization of Ingredients Treating Nitroglycerin-Induced Migraine Rats from Wuzhuyu Decoction Abstract Abstract Wuzhuyu decoction (WZYD) has been clinically used to treat migraine effectively since Eastern Han Dynasty of ancient China. However, its antimigrainic ingredients remain unclear. In present ... |
PMC11315827 | core_pubmed_pmc | Comparative CNS Pharmacology of the Bruton’s Tyrosine Kinase (BTK) Inhibitor Tolebrutinib Versus Other BTK Inhibitor Candidates for Treating Multiple Sclerosis | Comparative CNS Pharmacology of the Bruton’s Tyrosine Kinase (BTK) Inhibitor Tolebrutinib Versus Other BTK Inhibitor Candidates for Treating Multiple Sclerosis Abstract Background and objectives Tolebrutinib is a covalent BTK inhibitor designed and selected for potency and CNS exposure to optimize impact on BTK-depende... |
PMC3909260 | core_pubmed_pmc | Phase I dose-escalation study of oral vinflunine in combination with erlotinib in pre-treated and unselected EGFR patients with locally advanced or metastatic non-small-cell lung cancer | Phase I dose-escalation study of oral vinflunine in combination with erlotinib in pre-treated and unselected EGFR patients with locally advanced or metastatic non-small-cell lung cancer Abstract Abstract Background Erlotinib, the epidermal growth factor receptor tyrosine kinase inhibitor, and the intra-venous vinflunin... |
PMC8648509 | core_pubmed_pmc | Obesity and anesthetic pharmacology: simulation of target-controlled infusion models of propofol and remifentanil | Obesity and anesthetic pharmacology: simulation of target-controlled infusion models of propofol and remifentanil Abstract Abstract The prevalence of obesity is increasing, resulting in an increase in the number of surgeries performed to treat obesity and diseases induced by obesity. The associated comorbidities as wel... |
PMC9537572 | core_pubmed_pmc | Elucidation of the binding mechanism of astragaloside IV derivative with human serum albumin and its cardiotoxicity in zebrafish embryos | Elucidation of the binding mechanism of astragaloside IV derivative with human serum albumin and its cardiotoxicity in zebrafish embryos Abstract LS-102 is a new derivative of astragaloside IV (AGS IV) that has been shown to possess potentially significant cardioprotective effects. However, there are no reports concern... |
PMC6624401 | core_pubmed_pmc | Pharmacodynamics of rituximab on B lymphocytes in paediatric patients with autoimmune diseases | Pharmacodynamics of rituximab on B lymphocytes in paediatric patients with autoimmune diseases Abstract Abstract Aims Rituximab is a chimeric IgG‐1 monoclonal antibody that depletes B cells, aiding in the treatment of several conditions including autoimmune diseases. It is not licensed for use in children. This study a... |
PMC12489742 | core_pubmed_pmc | Safety, Pharmacokinetics, and Immunogenicity of Astegolimab, an Anti‐ST2 Monoclonal Antibody, in Randomized, Phase I Clinical Studies | Safety, Pharmacokinetics, and Immunogenicity of Astegolimab, an Anti‐ST2 Monoclonal Antibody, in Randomized, Phase I Clinical Studies Abstract ABSTRACT Astegolimab, a fully human immunoglobulin G2 monoclonal antibody, binds with high affinity to ST2, the interleukin‐33 receptor, thereby blocking ST2/interleukin‐33 bind... |
PMC12388967 | core_pubmed_pmc | Research Progress on Icariin Promoting Bone Injury Repair and Regeneration | Research Progress on Icariin Promoting Bone Injury Repair and Regeneration Abstract Abstract Icariin (ICA) is a bioactive flavonoid compound extracted from Epimedium plants. In recent years, it has attracted significant research interest in the field of bone tissue repair due to its pharmacological effects via multiple... |
PMC10603446 | core_pubmed_pmc | AdvanTIG-105: a phase I dose escalation study of the anti-TIGIT monoclonal antibody ociperlimab in combination with tislelizumab in patients with advanced solid tumors | AdvanTIG-105: a phase I dose escalation study of the anti-TIGIT monoclonal antibody ociperlimab in combination with tislelizumab in patients with advanced solid tumors Abstract Abstract Background Ociperlimab, a novel, humanized monoclonal antibody (mAb), binds to T-cell immunoreceptor with immunoglobulin and immunorec... |
PMC9271626 | core_pubmed_pmc | Dexmedetomidine in Children on Extracorporeal Membrane Oxygenation: Pharmacokinetic Data Exploration Using Previously Published Models | Dexmedetomidine in Children on Extracorporeal Membrane Oxygenation: Pharmacokinetic Data Exploration Using Previously Published Models Abstract Abstract Background Dexmedetomidine is a sedative and analgesic increasingly used in children supported with extracorporeal membrane oxygenation (ECMO). No data is available to... |
PMC10215229 | core_pubmed_pmc | Antifungals: From Pharmacokinetics to Clinical Practice | Antifungals: From Pharmacokinetics to Clinical Practice Abstract The use of antifungal drugs started in the 1950s with polyenes nystatin, natamycin and amphotericin B-deoxycholate (AmB). Until the present day, AmB has been considered to be a hallmark in the treatment of invasive systemic fungal infections. Nevertheless... |
PMC9037101 | core_pubmed_pmc | The development and validation of a sensitive HPLC-MS/MS method for the quantitative and pharmacokinetic study of the seven components of Buddleja lindleyana Fort. † | The development and validation of a sensitive HPLC-MS/MS method for the quantitative and pharmacokinetic study of the seven components of Buddleja lindleyana Fort. † Abstract Buddleja lindleyana Fort., a traditional Chinese medicine, has demonstrated anti-inflammatory, immunomodulatory, antidementia, neuroprotective, a... |
PMC8224736 | core_pubmed_pmc | Simplified Iohexol-Based Method for Measurement of Glomerular Filtration Rate in Goats and Pigs | Simplified Iohexol-Based Method for Measurement of Glomerular Filtration Rate in Goats and Pigs Abstract Abstract Simple Summary To improve the treatment of patients with kidney disease, new therapies are being developed. Before being used on humans, such therapies need to be tested on animals with kidney disease becau... |
PMC5716967 | core_pubmed_pmc | Model selection criteria for dynamic brain PET studies | Model selection criteria for dynamic brain PET studies Abstract Abstract Background Several criteria exist to identify the optimal model for quantification of tracer kinetics. The purpose of this study was to evaluate the correspondence in kinetic model preference identification for brain PET studies among five model s... |
PMC9978589 | core_pubmed_pmc | In vivo pharmacokinetic/pharmacodynamic evaluation of cefepime/taniborbactam combination against cefepime-non-susceptible Enterobacterales and Pseudomonas aeruginosa in a murine pneumonia model | In vivo pharmacokinetic/pharmacodynamic evaluation of cefepime/taniborbactam combination against cefepime-non-susceptible Enterobacterales and Pseudomonas aeruginosa in a murine pneumonia model Abstract Abstract Background Cefepime/taniborbactam is a cephalosporin/bicyclic boronate β-lactamase inhibitor combination in ... |
PMC11542432 | core_pubmed_pmc | Treatment with novel topoisomerase inhibitors in Ewing sarcoma models reveals heterogeneity of tumor response | Treatment with novel topoisomerase inhibitors in Ewing sarcoma models reveals heterogeneity of tumor response Abstract Abstract Introduction The topoisomerase 1 (TOP1) inhibitor irinotecan is a standard-of-care agent for relapsed Ewing sarcoma (EWS), but its efficacy is limited by chemical instability, rapid clearance ... |
PMC12673726 | core_pubmed_pmc | Technical guidelines for non-clinical pharmacological research of traditional Chinese medicine (TCM) formulae | Technical guidelines for non-clinical pharmacological research of traditional Chinese medicine (TCM) formulae Abstract Abstract Non-clinical pharmacology of traditional Chinese medicine (TCM) formulae plays a crucial role in elucidating their therapeutic mechanisms. With the integration of cutting-edge disciplines such... |
PMC12440289 | core_pubmed_pmc | Phase I Dose-Escalation Results for the Delta-Like Ligand 3/CD3 IgG-Like T-Cell Engager Obrixtamig (BI 764532) in Patients With Delta-Like Ligand 3+ Small Cell Lung Cancer or Neuroendocrine Carcinomas | Phase I Dose-Escalation Results for the Delta-Like Ligand 3/CD3 IgG-Like T-Cell Engager Obrixtamig (BI 764532) in Patients With Delta-Like Ligand 3+ Small Cell Lung Cancer or Neuroendocrine Carcinomas Abstract Abstract PURPOSE We report phase I results for obrixtamig (BI 764532), a delta-like ligand 3 (DLL3)/CD3 IgG-li... |
PMC7436235 | core_pubmed_pmc | GC-MS Phytochemical Profiling, Pharmacological Properties, and In Silico Studies of Chukrasia velutina Leaves: A Novel Source for Bioactive Agents | GC-MS Phytochemical Profiling, Pharmacological Properties, and In Silico Studies of Chukrasia velutina Leaves: A Novel Source for Bioactive Agents Abstract Chukrasia velutina is a local medicinal plant commonly known as chikrassy in Bangladesh, India, China, and other South Asian countries. The leaves, bark, and seeds ... |
PMC4911387 | core_pubmed_pmc | A Mathematical Model of Levodopa Medication Effect on Basal Ganglia in Parkinson's Disease: An Application to the Alternate Finger Tapping Task | A Mathematical Model of Levodopa Medication Effect on Basal Ganglia in Parkinson's Disease: An Application to the Alternate Finger Tapping Task Abstract Abstract Malfunctions in the neural circuitry of the basal ganglia (BG), induced by alterations in the dopaminergic system, are responsible for an array of motor disor... |
PMC8160721 | core_pubmed_pmc | Hydrotalcite–Niclosamide Nanohybrid as Oral Formulation towards SARS-CoV-2 Viral Infections | Hydrotalcite–Niclosamide Nanohybrid as Oral Formulation towards SARS-CoV-2 Viral Infections Abstract Abstract COVID-19 has been affecting millions of individuals worldwide and, thus far, there is no accurate therapeutic strategy. This critical situation necessitates novel formulations for already existing, FDA approved... |
PMC7551497 | core_pubmed_pmc | Novel Snakebite Therapeutics Must Be Tested in Appropriate Rescue Models to Robustly Assess Their Preclinical Efficacy | Novel Snakebite Therapeutics Must Be Tested in Appropriate Rescue Models to Robustly Assess Their Preclinical Efficacy Abstract Abstract In the field of antivenom research, development, and manufacture, it is often advised to follow the World Health Organization’s (WHO) guidelines for the production, control, and regul... |
PMC11232374 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of HRS9432(A) injection in healthy Chinese subjects: a phase-I randomized, double-blind, dose escalation, placebo-controlled study | Safety, tolerability, and pharmacokinetics of HRS9432(A) injection in healthy Chinese subjects: a phase-I randomized, double-blind, dose escalation, placebo-controlled study Abstract ABSTRACT HRS9432(A) is a long-acting echinocandin antifungal medication primarily used to treat invasive fungal infections, particularly ... |
PMC4133866 | core_pubmed_pmc | Novel AGLP-1 albumin fusion protein as a long-lasting agent for type 2 diabetes | Novel AGLP-1 albumin fusion protein as a long-lasting agent for type 2 diabetes Abstract Glucagon like peptide-1 (GLP-1) regulates glucose mediated-insulin secretion, nutrient accumulation, and β-cell growth. Despite the potential therapeutic usage for type 2 diabetes (T2D), GLP-1 has a short half-life in vivo ( t 1/2 ... |
PMC9714378 | core_pubmed_pmc | Genetic variations in relation to bleeding and pharmacodynamics of dabigatran in Chinese patients with nonvalvular atrial fibrillation: A nationwide multicentre prospective cohort study | Genetic variations in relation to bleeding and pharmacodynamics of dabigatran in Chinese patients with nonvalvular atrial fibrillation: A nationwide multicentre prospective cohort study Abstract Abstract Introduction To identify the potential factors responsible for the individual variability of dabigatran, we investig... |
PMC5901201 | core_pubmed_pmc | Preparation, characterization and systemic application of self-assembled hydroxyethyl starch nanoparticles-loaded flavonoid Morin for hyperuricemia therapy | Preparation, characterization and systemic application of self-assembled hydroxyethyl starch nanoparticles-loaded flavonoid Morin for hyperuricemia therapy Abstract Abstract Background Morin, one of the most widely distributed flavonoids in plants, has been identified as a potent antihyperuricemic agent. Its poor water... |
PMC7757094 | core_pubmed_pmc | Dose adjustment for tyrosine kinase inhibitors in non-small cell lung cancer patients with hepatic or renal function impairment | Dose adjustment for tyrosine kinase inhibitors in non-small cell lung cancer patients with hepatic or renal function impairment Abstract In recent years, a number of tyrosine kinase inhibitors (TKIs) have been approved for the treatment of non-small cell lung cancer. These novel treatments exhibit improved efficacy and... |
PMC12500084 | core_pubmed_pmc | A comparative computational analysis of IFN-alpha pharmacokinetics and its induced cellular response in mice and humans | A comparative computational analysis of IFN-alpha pharmacokinetics and its induced cellular response in mice and humans Abstract Drug effects are difficult to investigate in detail in vivo . However, a mechanistic understanding of drug action is clearly beneficial for both pharmaceutical development as well as for opti... |
PMC4679359 | core_pubmed_pmc | Bispecific Antibody Conjugated Manganese-Based Magnetic Engineered Iron Oxide for Imaging of HER2/neu- and EGFR-Expressing Tumors | Bispecific Antibody Conjugated Manganese-Based Magnetic Engineered Iron Oxide for Imaging of HER2/neu- and EGFR-Expressing Tumors Abstract The overexpression of HER2/neu and EGFR receptors plays important roles in tumorigenesis and tumor progression. Targeting these two receptors simultaneously can have a more widespre... |
PMC5132079 | core_pubmed_pmc | Effect of Cabotegravir on Cardiac Repolarization in Healthy Subjects | Effect of Cabotegravir on Cardiac Repolarization in Healthy Subjects Abstract Abstract A randomized, partial‐blind, repeat‐dose, 3‐period crossover study ( NCT02027454 ) assessed the effect of cabotegravir on QT interval in healthy subjects. To achieve a supratherapeutic dose, each subject received cabotegravir 150 mg ... |
PMC9278791 | core_pubmed_pmc | Elevated International Normalized Ratio Due to Apixaban in Patient With End-Stage Renal Disease on Hemodialysis | Elevated International Normalized Ratio Due to Apixaban in Patient With End-Stage Renal Disease on Hemodialysis Abstract Abstract Apixaban is known to prolong international normalized ratio (INR) per some observational and in vitro studies. In patients with elevated INR secondary to apixaban use, median INR of 1.4-1.7 ... |
PMC12177340 | core_pubmed_pmc | Scutellaria baicalensis Georgi in metabolic-associated fatty liver disease treatment: research progress | Scutellaria baicalensis Georgi in metabolic-associated fatty liver disease treatment: research progress Abstract Metabolic associated fatty liver disease (MAFLD), previously known as nonalcoholic fatty liver disease (NAFLD), is a common liver condition marked by excessive fat accumulation exceeding 5% in the liver with... |
PMC11835421 | core_pubmed_pmc | Current Use of Physiologically Based Pharmacokinetic modeling in New Medicinal Product Approvals at EMA | Current Use of Physiologically Based Pharmacokinetic modeling in New Medicinal Product Approvals at EMA Abstract Physiologically Based Pharmacokinetic (PBPK) Models are routinely used in drug development and therefore appear frequently in marketing authorization applications (MAAs) to the European Medicines Agency (EMA... |
PMC11168782 | core_pubmed_pmc | A phase 1 study of regorafenib and sildenafil in adults with advanced solid tumors | A phase 1 study of regorafenib and sildenafil in adults with advanced solid tumors Abstract The purpose of this study is to establish the recommended phase 2 dose for regorafenib in combination with sildenafil for patients with advanced solid tumors. Secondary outcomes included identification of antitumor effects of re... |
PMC9159829 | core_pubmed_pmc | Pharmacokinetic Difference of Six Active Constituents of Huangqi Liuyi Decoction between Control and Diabetic Nephropathy Mouse Models | Pharmacokinetic Difference of Six Active Constituents of Huangqi Liuyi Decoction between Control and Diabetic Nephropathy Mouse Models Abstract Huangqi Liuyi decoction is a famous traditional Chinese medicine (TCM) that has been widely used in China for the management of diabetes since the Song Dynasty. Today, it is co... |
PMC9441147 | core_pubmed_pmc | Characterization of Selective and Potent JAK1 Inhibitors Intended for the Inhaled Treatment of Asthma | Characterization of Selective and Potent JAK1 Inhibitors Intended for the Inhaled Treatment of Asthma Abstract Abstract Purpose Janus kinase 1 (JAK1) is implicated in multiple inflammatory pathways that are critical for the pathogenesis of asthma, including the interleukin (IL)-4, IL-5, IL-13, and thymic stromal lympho... |
PMC4897097 | core_pubmed_pmc | Time to Analgesia Onset and Pharmacokinetics After Separate and Combined Administration of Liposome Bupivacaine and Bupivacaine HCl: Considerations for Clinicians | Time to Analgesia Onset and Pharmacokinetics After Separate and Combined Administration of Liposome Bupivacaine and Bupivacaine HCl: Considerations for Clinicians Abstract Background: Liposome bupivacaine is a prolonged-release bupivacaine formulation indicated for single-dose administration into the surgical site to p... |
PMC12355016 | core_pubmed_pmc | Alemtuzumab Exposure and T Lymphocyte Depletion: A Population Pharmacokinetic‐Pharmacodynamic Model of Alemtuzumab Induction Therapy for Kidney Transplantation | Alemtuzumab Exposure and T Lymphocyte Depletion: A Population Pharmacokinetic‐Pharmacodynamic Model of Alemtuzumab Induction Therapy for Kidney Transplantation Abstract Abstract Alemtuzumab is a T cell‐depleting monoclonal antibody that is used for the prevention of kidney transplant rejection. The duration of lymphode... |
PMC4376785 | core_pubmed_pmc | Improvement in Plasma Drug Activity during the Early Treatment Interval among Tanzanian Patients with Multidrug-Resistant Tuberculosis | Improvement in Plasma Drug Activity during the Early Treatment Interval among Tanzanian Patients with Multidrug-Resistant Tuberculosis Abstract Abstract Background Individual pharmacokinetic variability may be common in patients treated for multidrug-resistant tuberculosis (MDR-TB) but data are sparse from resource-lim... |
PMC7678894 | core_pubmed_pmc | Real-time TDM-based optimization of continuous-infusion meropenem for improving treatment outcome of febrile neutropenia in oncohaematological patients: results from a prospective, monocentric, interventional study | Real-time TDM-based optimization of continuous-infusion meropenem for improving treatment outcome of febrile neutropenia in oncohaematological patients: results from a prospective, monocentric, interventional study Abstract Abstract Objectives To assess the role that real-time therapeutic drug monitoring (TDM)-guided o... |
PMC8376132 | core_pubmed_pmc | Pharmacometric analysis linking immunoglobulin exposure to clinical efficacy outcomes in chronic inflammatory demyelinating polyneuropathy | Pharmacometric analysis linking immunoglobulin exposure to clinical efficacy outcomes in chronic inflammatory demyelinating polyneuropathy Abstract Abstract The two main objectives of this analysis were to (i) characterize the relationship between immunoglobulin (Ig) exposure and chronic inflammatory demyelinating poly... |
PMC11315872 | core_pubmed_pmc | Pharmacokinetics of a Fixed-Dose Combination Product of Amlodipine, Losartan, Ezetimibe, and Rosuvastatin and Its Comparison with Co-administration of Four Individual Components in Healthy Participants | Pharmacokinetics of a Fixed-Dose Combination Product of Amlodipine, Losartan, Ezetimibe, and Rosuvastatin and Its Comparison with Co-administration of Four Individual Components in Healthy Participants Abstract Background and Objective This study aimed to assess and compare the pharmacokinetics, safety, and tolerabilit... |
PMC12375975 | core_pubmed_pmc | Preclinical common data elements for general pharmacological studies (pharmacokinetic sample collection, tolerability, and drug administration). A report of the TASK3‐WG1A General Pharmacology Working Group of the ILAE/AES Joint Translational Task Force | Preclinical common data elements for general pharmacological studies (pharmacokinetic sample collection, tolerability, and drug administration). A report of the TASK3‐WG1A General Pharmacology Working Group of the ILAE/AES Joint Translational Task Force Abstract Abstract Growing concerns over rigor and reproducibility ... |
PMC9326879 | core_pubmed_pmc | PXR as a mediator of herb–drug interaction | PXR as a mediator of herb–drug interaction Abstract Medicinal herbs have been a part of human medicine for thousands of years. The herb–drug interaction is an extension of drug–drug interaction, in which the consumptions of herbs cause alterations in the metabolism of drugs the patients happen to take at the same time.... |
PMC5983509 | core_pubmed_pmc | Change in plasma lactate concentration during arctigenin administration in a phase I clinical trial in patients with gemcitabine-refractory pancreatic cancer | Change in plasma lactate concentration during arctigenin administration in a phase I clinical trial in patients with gemcitabine-refractory pancreatic cancer Abstract Abstract Arctigenin is evaluated for antitumor efficacy in patients with pancreatic cancer. It has an inhibitory activity on mitochondrial complex I.Ther... |
PMC12481774 | core_pubmed_pmc | Herb-drug interaction of Astragali Radix based on in vitro incubation and pharmacokinetic assessment | Herb-drug interaction of Astragali Radix based on in vitro incubation and pharmacokinetic assessment Abstract Abstract Background Astragali Radix (AR) is extensively utilized in Asia for its various pharmacological effects. With the widespread use of AR, the risk of herb-drug interactions (HDIs) mediated by cytochrome ... |
PMC7356515 | core_pubmed_pmc | A Minimal PKPD Interaction Model for Evaluating Synergy Effects of Combined NSCLC Therapies | A Minimal PKPD Interaction Model for Evaluating Synergy Effects of Combined NSCLC Therapies Abstract Abstract This paper introduces a mathematical compartmental formulation of dose-effect synergy modelling for multiple therapies in non small cell lung cancer (NSCLC): antiangiogenic, immuno- and radiotherapy. The model ... |
PMC6269309 | core_pubmed_pmc | Inhibition of Btk by Btk-specific concentrations of ibrutinib and acalabrutinib delays but does not block platelet aggregation mediated by glycoprotein VI | Inhibition of Btk by Btk-specific concentrations of ibrutinib and acalabrutinib delays but does not block platelet aggregation mediated by glycoprotein VI Abstract Abstract Ibrutinib and acalabrutinib are irreversible inhibitors of Bruton tyrosine kinase used in the treatment of B-cell malignancies. They bind irreversi... |
PMC9674142 | core_pubmed_pmc | Implications of nasal delivery of bromelain on its pharmacokinetics, tissue distribution and pharmacodynamic profile—A preclinical study | Implications of nasal delivery of bromelain on its pharmacokinetics, tissue distribution and pharmacodynamic profile—A preclinical study Abstract Abstract Asthma is a polygenic chronic inflammatory respiratory disease devastating the quality of life and state economies. Therefore, utilization of natural products as a t... |
PMC9372425 | core_pubmed_pmc | Pharmacokinetics of vaginal versus buccal misoprostol for labor induction at term | Pharmacokinetics of vaginal versus buccal misoprostol for labor induction at term Abstract Abstract The IMPROVE study ( NCT02408315 ) compared the efficacy and safety of vaginal and buccal administration of misoprostol for full‐term, uncomplicated labor induction. This report compares the pharmacokinetics of misoprosto... |
PMC7520464 | core_pubmed_pmc | Predicted Efficacy of Once-Daily Extended-Release Oxcarbazepine (Oxtellar XR ® ) Monotherapy in Adults and Children with Partial-Onset Seizures: Exposure-Response Modeling and Simulation | Predicted Efficacy of Once-Daily Extended-Release Oxcarbazepine (Oxtellar XR ® ) Monotherapy in Adults and Children with Partial-Onset Seizures: Exposure-Response Modeling and Simulation Abstract Purpose We conducted exposure-response modeling and simulations to compare the predicted efficacy of extended-release oxcarb... |
PMC11220827 | core_pubmed_pmc | Next-generation risk assessment read-across case study: application of a 10-step framework to derive a safe concentration of daidzein in a body lotion | Next-generation risk assessment read-across case study: application of a 10-step framework to derive a safe concentration of daidzein in a body lotion Abstract Abstract Introduction: We performed an exposure-based Next Generation Risk Assessment case read-across study using New Approach Methodologies (NAMs) to determin... |
PMC12355582 | core_pubmed_pmc | Selective modulation of orexinergic receptors by neem-derived phytochemicals: Computational analysis of structure-activity relationships | Selective modulation of orexinergic receptors by neem-derived phytochemicals: Computational analysis of structure-activity relationships Abstract Orexinergic system dysfunction is the fundamental basis for several neurological illnesses like narcolepsy, insomnia, and drug dependency, yet none of the existing medication... |
PMC11503241 | core_pubmed_pmc | The preclinical pharmacokinetics of Tolinapant—A dual cIAP1/XIAP antagonist with in vivo efficacy | The preclinical pharmacokinetics of Tolinapant—A dual cIAP1/XIAP antagonist with in vivo efficacy Abstract Abstract AT‐IAP (1‐{6‐[(4‐fluorophenyl)methyl]‐3,3‐dimethyl‐1H,2H,3H‐pyrrolo[3,2‐b]pyridin‐1‐yl}‐2‐[(2R,5R)‐5‐methyl‐2‐{[(3R)‐3‐methylmorpholin‐4‐yl]methyl}piperazin‐1‐yl]ethan‐1‐one) was identified as a novel pot... |
PMC8944423 | core_pubmed_pmc | Pharmacodynamics of Ceftriaxone, Ertapenem, Fosfomycin and Gentamicin in Neisseria gonorrhoeae | Pharmacodynamics of Ceftriaxone, Ertapenem, Fosfomycin and Gentamicin in Neisseria gonorrhoeae Abstract Abstract Objectives: To assess the in vitro effect of select antimicrobials on the growth of N. gonorrhoeae and its pharmacodynamic parameters. Methods: Time–kill assays were performed on two reference N. gonorrhoeae... |
PMC9502676 | core_pubmed_pmc | The Impact of Low Cardiac Output on Propofol Pharmacokinetics across Age Groups—An Investigation Using Physiologically Based Pharmacokinetic Modelling | The Impact of Low Cardiac Output on Propofol Pharmacokinetics across Age Groups—An Investigation Using Physiologically Based Pharmacokinetic Modelling Abstract Abstract Background: pathophysiological changes such as low cardiac output (LCO) impact pharmacokinetics, but its extent may be different throughout pediatrics ... |
PMC7482441 | core_pubmed_pmc | Rimeporide as a first- in-class NHE-1 inhibitor: Results of a phase Ib trial in young patients with Duchenne Muscular Dystrophy | Rimeporide as a first- in-class NHE-1 inhibitor: Results of a phase Ib trial in young patients with Duchenne Muscular Dystrophy Abstract Abstract Rimeporide, a first-in-class sodium/proton exchanger Type 1 inhibitor (NHE-1 inhibitor) is repositioned by EspeRare for patients with Duchenne Muscular Dystrophy (DMD). Histori... |
PMC4650734 | core_pubmed_pmc | FV-162 is a novel, orally bioavailable, irreversible proteasome inhibitor with improved pharmacokinetics displaying preclinical efficacy with continuous daily dosing | FV-162 is a novel, orally bioavailable, irreversible proteasome inhibitor with improved pharmacokinetics displaying preclinical efficacy with continuous daily dosing Abstract Abstract Approved proteasome inhibitors have advanced the treatment of multiple myeloma but are associated with serious toxicities, poor pharmaco... |
PMC10684661 | core_pubmed_pmc | Prognostic Value of Nivolumab Clearance in Non-Small Cell Lung Cancer Patients for Survival Early in Treatment | Prognostic Value of Nivolumab Clearance in Non-Small Cell Lung Cancer Patients for Survival Early in Treatment Abstract Abstract Introduction Immune checkpoint inhibitors improved survival of advanced stage non-small cell lung cancer patients, but the overall response rate remains low. A biomarker that identifies non-r... |
PMC12838764 | core_pubmed_pmc | Inhaled Insulin Decoded: Dispelling Myths and Presenting Clinical Evidence | Inhaled Insulin Decoded: Dispelling Myths and Presenting Clinical Evidence Abstract Despite advancements in prandial insulin therapeutics, real-world usage of these products is associated with challenges such as injection-related anxiety, an increased risk of hypoglycemia, and weight gain. Other factors contributing to... |
PMC8241100 | core_pubmed_pmc | Optimization on biodistribution and antitumor activity of tripterine using polymeric nanoparticles through RES saturation | Optimization on biodistribution and antitumor activity of tripterine using polymeric nanoparticles through RES saturation Abstract Abstract Systemic delivery of tripterine (TPR) is challenged by its insoluble property and unsuitable pharmacokinetics. This work aimed to develop polymeric nanoparticles (NPs) combined wit... |
PMC9742417 | core_pubmed_pmc | Quantitative effects of sodium–glucose cotransporter-2 inhibitors dapagliflozin and empagliflozin on quality of life in heart failure patients | Quantitative effects of sodium–glucose cotransporter-2 inhibitors dapagliflozin and empagliflozin on quality of life in heart failure patients Abstract The aim of the present study is to investigate the quantitative effects of sodium–glucose cotransporter-2 (SGLT-2) inhibitors on the quality of life in heart failure (H... |
PMC10609738 | core_pubmed_pmc | Total and Free Blood and Plasma Concentration Changes in Pregnancy for Medicines Highly Bound to Plasma Proteins: Application of Physiologically Based Pharmacokinetic Modelling to Understand the Impact on Efficacy | Total and Free Blood and Plasma Concentration Changes in Pregnancy for Medicines Highly Bound to Plasma Proteins: Application of Physiologically Based Pharmacokinetic Modelling to Understand the Impact on Efficacy Abstract Abstract Free drug concentrations are generally considered the pharmacologically active moiety an... |
PMC10197202 | core_pubmed_pmc | Recombinant Technologies Facilitate Drug Metabolism, Pharmacokinetics, and General Biomedical Research | Recombinant Technologies Facilitate Drug Metabolism, Pharmacokinetics, and General Biomedical Research Abstract Abstract The development of safe and effective medications requires a profound understanding of their pharmacokinetic (PK) and pharmacodynamic properties. PK studies have been built through investigation of e... |
PMC8143500 | core_pubmed_pmc | Current and Future Drug and Device Therapies for Pediatric Heart Failure Patients: Potential Lessons from Adult Trials | Current and Future Drug and Device Therapies for Pediatric Heart Failure Patients: Potential Lessons from Adult Trials Abstract Abstract This review discusses the potential drug and device therapies for pediatric heart failure (HF) due to reduced systolic function. It is important to realize that most drugs that are us... |
PMC7098856 | core_pubmed_pmc | Evaluation of the effect of P‐glycoprotein inhibition and induction on talazoparib disposition in patients with advanced solid tumours | Evaluation of the effect of P‐glycoprotein inhibition and induction on talazoparib disposition in patients with advanced solid tumours Abstract Aims In vitro data show that talazoparib is a substrate for P‐glycoprotein (P‐gp) and breast cancer resistance protein transporters. This open‐label, 2‐arm, drug–drug interacti... |
PMC11844307 | core_pubmed_pmc | Nanomicellar Prodrug Delivery of Glucose-Paclitaxel: A Strategy to Mitigate Paclitaxel Toxicity | Nanomicellar Prodrug Delivery of Glucose-Paclitaxel: A Strategy to Mitigate Paclitaxel Toxicity Abstract Abstract Background Paclitaxel-induced blood system disorders and peripheral neuropathy impede the progress of new formulations in clinical trials. Purpose of Study To mitigate these adverse effects by developing an... |
PMC6600263 | core_pubmed_pmc | Neuroprotective Effects of Red Ginseng Saponins in Scopolamine-Treated Rats and Activity Screening Based on Pharmacokinetics | Neuroprotective Effects of Red Ginseng Saponins in Scopolamine-Treated Rats and Activity Screening Based on Pharmacokinetics Abstract Abstract Ginseng has been used to alleviate age-related dementia and memory deterioration for thousands of years. This study investigated the protective effect of red ginseng saponins ag... |
PMC12674970 | core_pubmed_pmc | Nephrocast‐V: A Deep Learning Model for the Prediction of Vancomycin Trough Concentration Using Electronic Health Record Data | Nephrocast‐V: A Deep Learning Model for the Prediction of Vancomycin Trough Concentration Using Electronic Health Record Data Abstract ABSTRACT Introduction Vancomycin is a critical antibiotic for treating methicillin‐resistant Staphylococcus aureus and other gram‐positive bacterial infections, but achieving and mainta... |
PMC12533862 | core_pubmed_pmc | Computational structural studies of SGLT2-related polypharmacy | Computational structural studies of SGLT2-related polypharmacy Abstract Introduction Sodium Glucose Cotransporter 2 (SGLT2) is the main active transport protein involved in sodium and glucose reabsorption in the kidney. SGLT2 inhibitors (SGLT2i) are widely recommended for patients with diabetes, heart failure and chron... |
PMC9568489 | core_pubmed_pmc | O -Glycoproteomic analysis of engineered heavily glycosylated fusion proteins using nanoHILIC-MS | O -Glycoproteomic analysis of engineered heavily glycosylated fusion proteins using nanoHILIC-MS Abstract Abstract Recombinant protein engineering design affects therapeutic properties including protein efficacy, safety, and immunogenicity. Importantly, glycosylation modulates glycoprotein therapeutic pharmacokinetics,... |
PMC11461495 | core_pubmed_pmc | Assessment of basic pharmacokinetic parameters of dapagliflozin in TTS formulations in male minipigs | Assessment of basic pharmacokinetic parameters of dapagliflozin in TTS formulations in male minipigs Abstract Given the extended time over which diabetes treatment is administered, the transdermal delivery system is anticipated to be a more suitable option for older individuals who may experience difficulty swallowing.... |
PMC12648360 | core_pubmed_pmc | Challenges in optimizing tacrolimus therapy in patients treated with rifampin: A case series | Challenges in optimizing tacrolimus therapy in patients treated with rifampin: A case series Abstract Tacrolimus is a cornerstone immunosuppressant in transplantation medicine with a narrow therapeutic window. Drug–drug interactions with strong CYP3A4 and P‐glycoprotein modulators, such as rifampin and azole antifungal... |
PMC9188284 | core_pubmed_pmc | Development and validation of a paper spray mass spectrometry method for the rapid quantitation of remdesivir and its active metabolite, GS-441524, in human plasma | Development and validation of a paper spray mass spectrometry method for the rapid quantitation of remdesivir and its active metabolite, GS-441524, in human plasma Abstract Highlights • Rapid PS-MS/MS quantification of remdesivir and its active metabolite, GS-441524, directly from plasma. • No sample preparation, short... |
PMC12072186 | core_pubmed_pmc | A Novel Small Molecule Enhances Stable Dopamine Delivery to the Brain in Models of Parkinson’s Disease | A Novel Small Molecule Enhances Stable Dopamine Delivery to the Brain in Models of Parkinson’s Disease Abstract Abstract Levodopa is the gold standard symptomatic treatment for Parkinson’s disease. Disease progression due to alpha-synuclein accumulation, brain inflammation, and the loss of dopamine neurons, as well as ... |
PMC10388668 | core_pubmed_pmc | Optimising prednisolone or prednisone replacement in adrenal insufficiency | Optimising prednisolone or prednisone replacement in adrenal insufficiency Abstract Context Patients with adrenal insufficiency (AI) have a higher mortality than the general population, possibly because of excess glucocorticoid exposure at inappropriate times. The cortisol circadian rhythm is difficult to mimic with tw... |
PMC4882719 | core_pubmed_pmc | Epigallocatechin Gallate Nanodelivery Systems for Cancer Therapy | Epigallocatechin Gallate Nanodelivery Systems for Cancer Therapy Abstract Abstract Cancer is one of the leading causes of morbidity and mortality all over the world. Conventional treatments, such as chemotherapy, are generally expensive, highly toxic and lack efficiency. Cancer chemoprevention using phytochemicals is e... |
PMC5080648 | core_pubmed_pmc | Applied Concepts in PBPK Modeling: How to Build a PBPK/PD Model | Applied Concepts in PBPK Modeling: How to Build a PBPK/PD Model Abstract Abstract The aim of this tutorial is to introduce the fundamental concepts of physiologically based pharmacokinetic/pharmacodynamic (PBPK/PD) modeling with a special focus on their practical implementation in a typical PBPK model building workflow... |
PMC6723536 | core_pubmed_pmc | Pharmacokinetic Evaluation of Metabolic Drug Interactions between Repaglinide and Celecoxib by a Bioanalytical HPLC Method for Their Simultaneous Determination with Fluorescence Detection | Pharmacokinetic Evaluation of Metabolic Drug Interactions between Repaglinide and Celecoxib by a Bioanalytical HPLC Method for Their Simultaneous Determination with Fluorescence Detection Abstract Abstract Since diabetes mellitus and osteoarthritis are highly prevalent diseases, combinations of antidiabetic agents like... |
PMC5834504 | core_pubmed_pmc | Development of an Injectable Slow-Release Metformin Formulation and Evaluation of Its Potential Antitumor Effects | Development of an Injectable Slow-Release Metformin Formulation and Evaluation of Its Potential Antitumor Effects Abstract Abstract Metformin is an antidiabetic drug which possesses antiproliferative activity in cancer cells when administered at high doses, due to its unfavorable pharmacokinetics. The aim of this work ... |
PMC5566571 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Evaluation of Marbofloxacin and PK/PD Modeling against Escherichia coli in Pigs | Pharmacokinetic and Pharmacodynamic Evaluation of Marbofloxacin and PK/PD Modeling against Escherichia coli in Pigs Abstract Abstract The aim of this study was to evaluate the activity of marbofloxacin and establish the optimal dose regimens for decreasing the development of fluoroquinolone resistance in pigs against E... |
PMC12935725 | core_pubmed_pmc | Do sex and gender matter in the pharmacological treatment of depression? | Do sex and gender matter in the pharmacological treatment of depression? Abstract Depression shows significant differences in prevalence, symptomology and treatment outcomes in men and women. Women have a twofold higher risk of depression than men and often present with different depression subtypes. These differences ... |
PMC12435188 | core_pubmed_pmc | Inner-wall biochar-coated pipette tip microextraction for rapid and sustainable determination of tyrosine kinase inhibitors in plasma | Inner-wall biochar-coated pipette tip microextraction for rapid and sustainable determination of tyrosine kinase inhibitors in plasma Abstract Abstract Tyrosine kinase inhibitors (TKIs) are critical in cancer therapy, but their clinical application is complicated by narrow therapeutic windows and significant interpatie... |
PMC10292217 | core_pubmed_pmc | Gene-nutrient interactions that impact magnesium homeostasis increase risk for neural tube defects in mice exposed to dolutegravir | Gene-nutrient interactions that impact magnesium homeostasis increase risk for neural tube defects in mice exposed to dolutegravir Abstract Abstract In 2018, data from a surveillance study in Botswana evaluating adverse birth outcomes raised concerns that women on antiretroviral therapy (ART) containing dolutegravir (D... |
PMC7276750 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of Chloroquine in a Plasmodium vivax Volunteer Infection Study | Population Pharmacokinetics and Pharmacodynamics of Chloroquine in a Plasmodium vivax Volunteer Infection Study Abstract Abstract Chloroquine has been used for the treatment of malaria for > 70 years; however, chloroquine pharmacokinetic (PK) and pharmacodynamic (PD) profile in Plasmodium vivax malaria is poorly unders... |
PMC11595231 | core_pubmed_pmc | Alkamides in Zanthoxylum Species: Phytochemical Profiles and Local Anesthetic Activities | Alkamides in Zanthoxylum Species: Phytochemical Profiles and Local Anesthetic Activities Abstract Abstract Zanthoxylum species have long been utilized in traditional medicine; among their various properties, they provide an analgesic effect. Central to this medicinal application are alkamides, a class of alkaloids char... |
PMC7199743 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics Modeling of Torasemide and Furosemide After Oral Repeated Administration in Healthy Dogs | Population Pharmacokinetics and Pharmacodynamics Modeling of Torasemide and Furosemide After Oral Repeated Administration in Healthy Dogs Abstract Torasemide is a loop diuretic licensed in dogs for cardiogenic pulmonary oedema. The aim of this pharmacokinetic-pharmacodynamic (PK/PD) study was to define an optimally eff... |
PMC7318003 | core_pubmed_pmc | Population Pharmacokinetics and Exposure-Response Relationships of Baloxavir Marboxil in Influenza Patients at High Risk of Complications | Population Pharmacokinetics and Exposure-Response Relationships of Baloxavir Marboxil in Influenza Patients at High Risk of Complications Abstract Baloxavir marboxil, a prodrug of cap-dependent endonuclease inhibitor baloxavir acid, reduces the time to improvement of influenza symptoms in patients infected with type A ... |
PMC4629264 | core_pubmed_pmc | Pharmacokinetic analysis and tissue distribution of Vam3 in the rat by a validated LC-MS/MS method | Pharmacokinetic analysis and tissue distribution of Vam3 in the rat by a validated LC-MS/MS method Abstract Vam3 is a potential pharmacologically active ingredient isolated from Vitis amurensis Rupr. A rapid, simple and sensitive method to determine Vam3 levels in rat plasma and tissue was developed based on LC-MS/MS. ... |
PMC12356842 | core_pubmed_pmc | Microalgae-based Intestinal villi-targeting multistage biosystem for irritable bowel syndrome treatment | Microalgae-based Intestinal villi-targeting multistage biosystem for irritable bowel syndrome treatment Abstract Abstract Irritable Bowel Syndrome (IBS) is a chronic gastrointestinal disorder associated with dysregulation of the gut-brain axis. Current treatment approaches often lack long-term efficacy and target speci... |
PMC9112917 | core_pubmed_pmc | Pharmacokinetics of Oral Tebipenem Pivoxil Hydrobromide in Subjects with Various Degrees of Renal Impairment | Pharmacokinetics of Oral Tebipenem Pivoxil Hydrobromide in Subjects with Various Degrees of Renal Impairment Abstract ABSTRACT Tebipenem pivoxil hydrobromide (TBP-PI-HBr) is an oral carbapenem prodrug antimicrobial agent with broad-spectrum activity that includes multidrug-resistant (MDR) Enterobacterales . This study ... |
PMC11687176 | core_pubmed_pmc | Dual inhibition of LAG-3 and PD-1 with IBI110 and sintilimab in advanced solid tumors: the first-in-human phase Ia/Ib study | Dual inhibition of LAG-3 and PD-1 with IBI110 and sintilimab in advanced solid tumors: the first-in-human phase Ia/Ib study Abstract Background Co-inhibition of immune checkpoints lymphocyte-activation gene 3 (LAG-3) and PD-1 is believed to enhance cancer immunotherapy through synergistic effects. Herein, we evaluate t... |
PMC12746752 | core_pubmed_pmc | Exploratory Research of Intraductal Chemotherapy to Control the Focal Breast Lesion of Breast Cancer | Exploratory Research of Intraductal Chemotherapy to Control the Focal Breast Lesion of Breast Cancer Abstract Abstract Objective The standard treatment for locally advanced breast cancer (LABC) is neoadjuvant therapy combined with surgery with chemotherapy as the main means. Elderly female patients often lose treatment... |
PMC12604001 | core_pubmed_pmc | Molecular insights into nilvadipine–hemoglobin interactions: conformational dynamics and binding mechanisms | Molecular insights into nilvadipine–hemoglobin interactions: conformational dynamics and binding mechanisms Abstract Understanding the molecular basis of drug–protein interactions is essential for predicting pharmacokinetics and potential off-target effects. Here, we employ a combined experimental and computational app... |
PMC7993268 | core_pubmed_pmc | Clinical Pharmacology Studies Supporting Oligonucleotide Therapy Development: An Assessment of Therapies Approved and in Development Between 2012 and 2018 | Clinical Pharmacology Studies Supporting Oligonucleotide Therapy Development: An Assessment of Therapies Approved and in Development Between 2012 and 2018 Abstract Synthetic nucleotides that utilize RNA‐centric pharmacology can target diseases at the RNA level, thus altering protein expression in ways previously inacce... |
PMC9594513 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics and preliminary antitumour activity of an antisense oligonucleotide targeting STAT3 (danvatirsen) as monotherapy and in combination with durvalumab in Japanese patients with advanced solid malignancies: a phase 1 study | Safety, tolerability, pharmacokinetics and preliminary antitumour activity of an antisense oligonucleotide targeting STAT3 (danvatirsen) as monotherapy and in combination with durvalumab in Japanese patients with advanced solid malignancies: a phase 1 study Abstract Abstract Objectives We assessed the safety, tolerabil... |
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