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PMC5903480
core_pubmed_pmc
Pharmacokinetic interactions and tolerability of rosuvastatin and ezetimibe: an open-label, randomized, multiple-dose, crossover study in healthy male volunteers
Pharmacokinetic interactions and tolerability of rosuvastatin and ezetimibe: an open-label, randomized, multiple-dose, crossover study in healthy male volunteers Abstract Purpose Rosuvastatin is a synthetic 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor that effectively reduces low-density lipoprotein choles...
PMC5369547
core_pubmed_pmc
Micro-flow photosynthesis of new dienophiles for inverse-electron-demand Diels–Alder reactions. Potential applications for pretargeted in vivo PET imaging †
Micro-flow photosynthesis of new dienophiles for inverse-electron-demand Diels–Alder reactions. Potential applications for pretargeted in vivo PET imaging † Abstract New dienophiles were prepared with an innovative microfluidic setup. [ 18 F]3 is suitable for inverse-electron-demand Diels–Alder reactions and pretargeti...
PMC12649301
core_pubmed_pmc
Saliva as a TDM Matrix and Its Application in the Model‐Informed Precision Dosing
Saliva as a TDM Matrix and Its Application in the Model‐Informed Precision Dosing Abstract Abstract This study reviews the main points of saliva as a therapeutic drug monitoring (TDM) matrix, its advantages and limitations, the methods of saliva sample collection and testing, the types of drugs in saliva TDM, and the m...
PMC7641486
core_pubmed_pmc
A GFR-Based Method to Predict the Effect of Renal Impairment on the Exposure or Clearance of Renally Excreted Drugs: A Comparative Study Between a Simple GFR Method and a Physiologically Based Pharmacokinetic Model
A GFR-Based Method to Predict the Effect of Renal Impairment on the Exposure or Clearance of Renally Excreted Drugs: A Comparative Study Between a Simple GFR Method and a Physiologically Based Pharmacokinetic Model Abstract Objective The objective of this study was to compare the predictive performances of a glomerular...
PMC10305589
core_pubmed_pmc
Monitoring of Levosimendan Administration in Patients with Pulmonary Hypertension Undergoing Cardiac Surgery and Effect of Two Different Dosing Schemes on Hemodynamic and Echocardiographic Parameters
Monitoring of Levosimendan Administration in Patients with Pulmonary Hypertension Undergoing Cardiac Surgery and Effect of Two Different Dosing Schemes on Hemodynamic and Echocardiographic Parameters Abstract Abstract Introduction: The perioperative management of patients with pulmonary hypertension (PH) undergoing car...
PMC3141875
core_pubmed_pmc
Formulation and pharmacokinetic evaluation of a paclitaxel nanosuspension for intravenous delivery
Formulation and pharmacokinetic evaluation of a paclitaxel nanosuspension for intravenous delivery Abstract Paclitaxel is a diterpenoid isolated from Taxus brevifolia . It is effective for various cancers, especially ovarian and breast cancer. Due to its aqueous insolubility, it is administered dissolved in ethanol and...
PMC4478173
core_pubmed_pmc
Continuous Glucose Monitoring During Basal–Bolus Therapy Using Insulin Glargine 300 U mL −1 and Glargine 100 U mL −1 in Japanese People with Type 1 Diabetes Mellitus: A Crossover Pilot Study
Continuous Glucose Monitoring During Basal–Bolus Therapy Using Insulin Glargine 300 U mL −1 and Glargine 100 U mL −1 in Japanese People with Type 1 Diabetes Mellitus: A Crossover Pilot Study Abstract Introduction New insulin glargine 300 U mL −1 (Gla-300) is a basal insulin that shows more stable and prolonged pharmaco...
PMC7159184
core_pubmed_pmc
Baloxavir treatment of ferrets infected with influenza A(H1N1)pdm09 virus reduces onward transmission
Baloxavir treatment of ferrets infected with influenza A(H1N1)pdm09 virus reduces onward transmission Abstract Abstract Influenza viruses cause seasonal outbreaks and pose a continuous pandemic threat. Although vaccines are available for influenza control, their efficacy varies each season and a vaccine for a novel pan...
PMC7382816
core_pubmed_pmc
Effect of food on the pharmacokinetics of omeprazole, pantoprazole and rabeprazole
Effect of food on the pharmacokinetics of omeprazole, pantoprazole and rabeprazole Abstract Abstract Background The pharmacokinetics of proton pump inhibitors (PPIs) may be affected by food intake. We aimed to evaluate the effect of food on the pharmacokinetics of omeprazole, rabeprazole, and pantoprazole. Setting The ...
PMC7283506
core_pubmed_pmc
Application of a 3D Bioprinted Hepatocellular Carcinoma Cell Model in Antitumor Drug Research
Application of a 3D Bioprinted Hepatocellular Carcinoma Cell Model in Antitumor Drug Research Abstract Abstract The existing in vitro models for antitumor drug screening have great limitations. Many compounds that inhibit 2D cultured cells do not exhibit the same pharmacological effects in vivo , thereby wasting human ...
PMC3481481
core_pubmed_pmc
Assessing the efficacy of molecularly targeted agents on cell line-based platforms by using system identification
Assessing the efficacy of molecularly targeted agents on cell line-based platforms by using system identification Abstract Abstract Background Molecularly targeted agents (MTAs) are increasingly used for cancer treatment, the goal being to improve the efficacy and selectivity of cancer treatment by developing agents th...
PMC9714780
core_pubmed_pmc
Randomized phase I trial of antigen-specific tolerizing immunotherapy with peptide/calcitriol liposomes in ACPA + rheumatoid arthritis
Randomized phase I trial of antigen-specific tolerizing immunotherapy with peptide/calcitriol liposomes in ACPA + rheumatoid arthritis Abstract BACKGROUND Antigen-specific regulation of autoimmune disease is a major goal. In seropositive rheumatoid arthritis (RA), T cell help to autoreactive B cells matures the citrull...
PMC12321606
core_pubmed_pmc
Lower baseline amyloid beta burden is associated with greater percent of amyloid beta positron emission tomography reduction and better clinical outcomes in the aducanumab Phase 3 trials ENGAGE and EMERGE in early Alzheimer's disease
Lower baseline amyloid beta burden is associated with greater percent of amyloid beta positron emission tomography reduction and better clinical outcomes in the aducanumab Phase 3 trials ENGAGE and EMERGE in early Alzheimer's disease Abstract Abstract Background Aducanumab is a human immunoglobulin G1 anti-amyloid beta...
PMC5098440
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of DSTA4637A: A novel THIOMAB™ antibody antibiotic conjugate against Staphylococcus aureus in mice
Pharmacokinetics and pharmacodynamics of DSTA4637A: A novel THIOMAB™ antibody antibiotic conjugate against Staphylococcus aureus in mice Abstract ABSTRACT DSTA4637A, a novel THIOMAB™ antibody antibiotic conjugate (TAC) against Staphylococcus aureus ( S. aureus ), is currently being investigated as a potential therapy a...
PMC11054683
core_pubmed_pmc
Antiviral Chemotherapy in Avian Medicine—A Review
Antiviral Chemotherapy in Avian Medicine—A Review Abstract Abstract This review article describes the current knowledge about the use of antiviral chemotherapeutics in avian species, such as farm poultry and companion birds. Specific therapeutics are described in alphabetical order including classic antiviral drugs, su...
PMC10583639
core_pubmed_pmc
Preclinical characterization of an mRNA-encoded anti-Claudin 18.2 antibody
Preclinical characterization of an mRNA-encoded anti-Claudin 18.2 antibody Abstract ABSTRACT IMAB362/Zolbetuximab, a first-in-class IgG1 antibody directed against the cancer-associated gastric-lineage marker CLDN18.2, has recently been reported to have met its primary endpoint in two phase 3 trials as a first-line trea...
PMC3585965
core_pubmed_pmc
Pharmacokinetics, Safety, and Tolerability of GLPG0259, a Mitogen-Activated Protein Kinase-Activated Protein Kinase 5 (MAPKAPK5) Inhibitor, Given as Single and Multiple Doses to Healthy Male Subjects
Pharmacokinetics, Safety, and Tolerability of GLPG0259, a Mitogen-Activated Protein Kinase-Activated Protein Kinase 5 (MAPKAPK5) Inhibitor, Given as Single and Multiple Doses to Healthy Male Subjects Abstract Background and Objectives GLPG0259 is a small-molecule inhibitor of mitogen-activated protein kinase-activated ...
PMC8907671
core_pubmed_pmc
Ovulation suppression following subcutaneous administration of depot medroxyprogesterone acetate
Ovulation suppression following subcutaneous administration of depot medroxyprogesterone acetate Abstract Abstract Objectives To characterize the relationship between serum medroxyprogesterone acetate (MPA) concentrations and ovulation suppression, and to estimate the risk of ovulation for investigational subcutaneous ...
PMC6032914
core_pubmed_pmc
Phase 1b Trial of Ficlatuzumab, a Humanized Hepatocyte Growth Factor Inhibitory Monoclonal Antibody, in Combination With Gefitinib in Asian Patients With NSCLC
Phase 1b Trial of Ficlatuzumab, a Humanized Hepatocyte Growth Factor Inhibitory Monoclonal Antibody, in Combination With Gefitinib in Asian Patients With NSCLC Abstract Abstract Hepatocyte growth factor (HGF)/c‐Met pathway dysregulation is a mechanism for epidermal growth factor receptor (EGFR) tyrosine kinase inhibito...
PMC10838831
core_pubmed_pmc
Review of Adalimumab Biosimilar SB5 in Immune-Mediated Inflammatory Diseases
Review of Adalimumab Biosimilar SB5 in Immune-Mediated Inflammatory Diseases Abstract Abstract SB5 is an approved biosimilar of adalimumab, a recombinant monoclonal anti-tumor necrosis factor (TNF) antibody. The approval of SB5 was based on the comparison with reference adalimumab in analytical studies, pharmacokinetic...
PMC9747113
core_pubmed_pmc
Population pharmacokinetic and pharmacodynamic modeling of evobrutinib in healthy adult participants
Population pharmacokinetic and pharmacodynamic modeling of evobrutinib in healthy adult participants Abstract Abstract Evobrutinib, a Bruton's tyrosine kinase (BTK) inhibitor, has shown therapeutic potential in relapsing multiple sclerosis. This analysis aimed to develop pharmacokinetic (PK) and pharmacodynamic (PD; BT...
PMC8280265
core_pubmed_pmc
Mathematical Model Predicts that Acceleration of Diabetic Wound Healing is Dependent on Spatial Distribution of VEGF-A mRNA (AZD8601)
Mathematical Model Predicts that Acceleration of Diabetic Wound Healing is Dependent on Spatial Distribution of VEGF-A mRNA (AZD8601) Abstract Introduction Pharmacologic approaches for promoting angiogenesis have been utilized to accelerate healing of chronic wounds in diabetic patients with varying degrees of success....
PMC11495486
core_pubmed_pmc
Ideal Time to Conduct a Pharmacokinetic Investigation After Delivery to Fully Capture the Effect of Pregnancy on Drug Exposure
Ideal Time to Conduct a Pharmacokinetic Investigation After Delivery to Fully Capture the Effect of Pregnancy on Drug Exposure Abstract Abstract Background The World Health Organization is pushing to accelerate the study of new human immunodeficiency virus drugs in pregnant women. However, regulatory guidelines do not ...
PMC8843022
core_pubmed_pmc
Pharmacodynamic evaluation and safety assessment of treatment with antibodies to serum amyloid P component in patients with cardiac amyloidosis: an open-label Phase 2 study and an adjunctive immuno-PET imaging study
Pharmacodynamic evaluation and safety assessment of treatment with antibodies to serum amyloid P component in patients with cardiac amyloidosis: an open-label Phase 2 study and an adjunctive immuno-PET imaging study Abstract Background In a Phase I study treatment with the serum amyloid P component (SAP) depleter mirid...
PMC4280904
core_pubmed_pmc
Imepitoin as novel treatment option for canine idiopathic epilepsy: pharmacokinetics, distribution, and metabolism in dogs
Imepitoin as novel treatment option for canine idiopathic epilepsy: pharmacokinetics, distribution, and metabolism in dogs Abstract Abstract Imepitoin is a novel anti-epileptic licensed in the European Union for the treatment of canine idiopathic epilepsy. The aim of this study was to characterize the pharmacokinetics ...
PMC3275936
core_pubmed_pmc
Pharmacokinetics of Oral Taurine in Healthy Volunteers
Pharmacokinetics of Oral Taurine in Healthy Volunteers Abstract Abstract Taurine, a sulfur-containing amino acid, is a normal constituent of the human diet. Little is known of the pharmacokinetics of taurine in man after oral administration. We studied the pharmacokinetics of 4 g taurine in eight healthy male volunteer...
PMC9888313
core_pubmed_pmc
Tools to develop antibiotic combinations that target drug tolerance in Mycobacterium tuberculosis
Tools to develop antibiotic combinations that target drug tolerance in Mycobacterium tuberculosis Abstract Abstract Combination therapy is necessary to treat tuberculosis to decrease the rate of disease relapse and prevent the acquisition of drug resistance, and shorter regimens are urgently needed. The adaptation of M...
PMC8152487
core_pubmed_pmc
Current Evidence, Challenges, and Opportunities of Physiologically Based Pharmacokinetic Models of Atorvastatin for Decision Making
Current Evidence, Challenges, and Opportunities of Physiologically Based Pharmacokinetic Models of Atorvastatin for Decision Making Abstract Abstract Atorvastatin (ATS) is the gold-standard treatment worldwide for the management of hypercholesterolemia and prevention of cardiovascular diseases associated with dyslipide...
PMC4364324
core_pubmed_pmc
Rotigotine transdermal system as add-on to oral dopamine agonist in advanced Parkinson’s disease: an open-label study
Rotigotine transdermal system as add-on to oral dopamine agonist in advanced Parkinson’s disease: an open-label study Abstract Abstract Background Achieving optimal symptom control with minimal side effects is a major goal in clinical practice. Dual-agent dopamine receptor agonist (DA) therapy in Parkinson’s disease (P...
PMC6822834
core_pubmed_pmc
Pharmacokinetics and Bioequivalence of Memantine Tablet and a New Dry Syrup Formulation in Healthy Japanese Males: Two Single-Dose Crossover Studies
Pharmacokinetics and Bioequivalence of Memantine Tablet and a New Dry Syrup Formulation in Healthy Japanese Males: Two Single-Dose Crossover Studies Abstract Abstract Introduction Memantine hydrochloride, an N-methyl-D-aspartate receptor antagonist, is used to treat Alzheimer’s disease (AD). A new dry syrup formulation...
PMC12392120
core_pubmed_pmc
Neurobiology of psilocybin: a comprehensive overview and comparative analysis of experimental models
Neurobiology of psilocybin: a comprehensive overview and comparative analysis of experimental models Abstract Psilocybin, a compound found in Psilocybe mushrooms, is emerging as a promising treatment for neurodegenerative and psychiatric disorders, including major depressive disorder. Its potential therapeutic effects ...
PMC6781320
core_pubmed_pmc
Intracellular Delivery of siRNAs Targeting AKT and ERBB2 Genes Enhances Chemosensitization of Breast Cancer Cells in a Culture and Animal Model
Intracellular Delivery of siRNAs Targeting AKT and ERBB2 Genes Enhances Chemosensitization of Breast Cancer Cells in a Culture and Animal Model Abstract Pharmacotherapy as the mainstay in the management of breast cancer suffers from various drawbacks, including non-targeted biodistribution, narrow therapeutic and safet...
PMC11706420
core_pubmed_pmc
Establishing a physiologically based pharmacokinetic framework for aldehyde oxidase and dual aldehyde oxidase‐CYP substrates
Establishing a physiologically based pharmacokinetic framework for aldehyde oxidase and dual aldehyde oxidase‐CYP substrates Abstract Abstract Aldehyde oxidase (AO) contributes to the clearance of many approved and investigational small molecule drugs, which are often dual substrates of AO and drug‐metabolizing enzymes...
PMC12845205
core_pubmed_pmc
Ketamine in Diabetes Care: Metabolic Insights and Clinical Applications
Ketamine in Diabetes Care: Metabolic Insights and Clinical Applications Abstract Abstract Background: Depression and diabetic neuropathy (DN) commonly complicate diabetes and impair glycemic control and quality of life. Ketamine and its S-enantiomer, esketamine, provide rapid antidepressant and analgesic effects, yet d...
PMC10822982
core_pubmed_pmc
Case report: Twice-daily tolvaptan dosing regimen in a challenging case of hyponatremia due to SIAD
Case report: Twice-daily tolvaptan dosing regimen in a challenging case of hyponatremia due to SIAD Abstract Background Syndrome of inappropriate antidiuresis (SIAD) is one of the most frequent causes of euvolemic hyponatremia (serum sodium levels < 135 mEq/L) and it represents more than 35% of hyponatremia cases in ho...
PMC4506051
core_pubmed_pmc
Pharmacokinetic Profiles of Active Ingredients and Its Metabolites Derived from Rikkunshito, a Ghrelin Enhancer, in Healthy Japanese Volunteers: A Cross-Over, Randomized Study
Pharmacokinetic Profiles of Active Ingredients and Its Metabolites Derived from Rikkunshito, a Ghrelin Enhancer, in Healthy Japanese Volunteers: A Cross-Over, Randomized Study Abstract Background Rikkunshito, a traditional Japanese (Kampo) medicine, has been used to treat upper gastrointestinal disorders such as functi...
PMC8524798
core_pubmed_pmc
Prevalence of drug-drug interactions in older people before and after hospital admission: analysis from the OPERAM trial
Prevalence of drug-drug interactions in older people before and after hospital admission: analysis from the OPERAM trial Abstract Abstract ( N = 351) Background Drug-drug interactions (DDIs) are highly prevalent in older patients but little is known about prevalence of DDIs over time. Our main objective was to assess c...
PMC11536652
core_pubmed_pmc
Measurement of tepotinib by UPLC‒MS/MS and its interaction with naringenin in rats
Measurement of tepotinib by UPLC‒MS/MS and its interaction with naringenin in rats Abstract Abstract We established a method based on ultra performance liquid chromatography tandem mass spectrometry (UPLC‒MS/MS) to quantitatively measure tepotinib, which was validated as acceptable and used in the evaluation of food-dr...
PMC7044105
core_pubmed_pmc
Retrospective cohort study of statin therapy effect on resected colorectal liver metastases
Retrospective cohort study of statin therapy effect on resected colorectal liver metastases Abstract BACKGROUND Above and beyond their role in cardiovascular risk reduction, statins appear to have a chemopreventive role in some gastro-intestinal cancers. In the quest for new chemopreventive agents, some existing establ...
PMC9469690
core_pubmed_pmc
Does the choice of applied physiologically‐based pharmacokinetics platform matter? A case study on simvastatin disposition and drug–drug interaction
Does the choice of applied physiologically‐based pharmacokinetics platform matter? A case study on simvastatin disposition and drug–drug interaction Abstract Abstract Physiologically‐based pharmacokinetic (PBPK) models have an important role in drug discovery/development and decision making in regulatory submissions. T...
PMC10146360
core_pubmed_pmc
Synergistic Encapsulation of Paclitaxel and Sorafenib by Methoxy Poly(Ethylene Glycol)- b -Poly(Caprolactone) Polymeric Micelles for Ovarian Cancer Therapy
Synergistic Encapsulation of Paclitaxel and Sorafenib by Methoxy Poly(Ethylene Glycol)- b -Poly(Caprolactone) Polymeric Micelles for Ovarian Cancer Therapy Abstract Abstract Ovarian cancer has a high mortality rate due to difficult detection at an early stage. It is necessary to develop a novel anticancer treatment tha...
PMC12960686
core_pubmed_pmc
AI-driven virtual screening platform identifies novel NSUN2 inhibitor candidates for targeted cancer therapy: a computational drug discovery approach
AI-driven virtual screening platform identifies novel NSUN2 inhibitor candidates for targeted cancer therapy: a computational drug discovery approach Abstract The RNA cytosine-5 methyltransferase NSUN2 is an emerging therapeutic target in precision oncology, with aberrant overexpression driving tumor progression, metas...
PMC9822353
core_pubmed_pmc
Ameliorative Effect of Structurally Divergent Oleanane Triterpenoid, 3-Epifriedelinol from Ipomoea batatas against BPA-Induced Gonadotoxicity by Targeting PARP and NF-κB Signaling in Rats
Ameliorative Effect of Structurally Divergent Oleanane Triterpenoid, 3-Epifriedelinol from Ipomoea batatas against BPA-Induced Gonadotoxicity by Targeting PARP and NF-κB Signaling in Rats Abstract The pentacyclic triterpenoids (PTs) of plant origin are reputed to restrain prostate cancer (PCa) cell proliferation. This ...
PMC10347199
core_pubmed_pmc
Pharmacokinetic Analyses of Liposomal and Non-Liposomal Multivitamin/Mineral Formulations
Pharmacokinetic Analyses of Liposomal and Non-Liposomal Multivitamin/Mineral Formulations Abstract Recent research supports previous contentions that encapsulating vitamins and minerals with liposomes help improve overall bioavailability. This study examined whether ingesting a liposomal multivitamin and mineral supple...
PMC7934061
core_pubmed_pmc
Insulin Fused to Apolipoprotein A-I Reduces Body Weight and Steatosis in DB/DB Mice
Insulin Fused to Apolipoprotein A-I Reduces Body Weight and Steatosis in DB/DB Mice Abstract Abstract Background: Targeting long-lasting insulins to the liver may improve metabolic alterations that are not corrected with current insulin replacement therapies. However, insulin is only able to promote lipogenesis but not...
PMC6773840
core_pubmed_pmc
Oral Anti-Tumour Necrosis Factor Domain Antibody V565 Provides High Intestinal Concentrations, and Reduces Markers of Inflammation in Ulcerative Colitis Patients
Oral Anti-Tumour Necrosis Factor Domain Antibody V565 Provides High Intestinal Concentrations, and Reduces Markers of Inflammation in Ulcerative Colitis Patients Abstract Abstract V565 is an engineered TNFα-neutralising single domain antibody formulated into enteric coated mini-tablets to enable release in the intestin...
PMC9290503
core_pubmed_pmc
Safety, pharmacokinetics and pharmacodynamics of TAK‐418, a novel inhibitor of the epigenetic modulator lysine‐specific demethylase 1A
Safety, pharmacokinetics and pharmacodynamics of TAK‐418, a novel inhibitor of the epigenetic modulator lysine‐specific demethylase 1A Abstract Abstract Aims Dysregulation of histone methylation epigenetic marks may result in intellectual and developmental disability, as seen in Kabuki syndrome. Animal data suggest tha...
PMC12701728
core_pubmed_pmc
Real-World Comparative Study of Ultra-Low-Dose Rivaroxaban in Very Elderly Patients with Atrial Fibrillation
Real-World Comparative Study of Ultra-Low-Dose Rivaroxaban in Very Elderly Patients with Atrial Fibrillation Abstract Background Optimal dosing of rivaroxaban in very elderly (≥80 years) nonvalvular atrial fibrillation (AF) patients remains debated, particularly concerning ultra-low-dose (5 mg daily) regimens derived f...
PMC8233004
core_pubmed_pmc
Chemistry, Pharmacology and Therapeutic Potential of Swertiamarin – A Promising Natural Lead for New Drug Discovery and Development
Chemistry, Pharmacology and Therapeutic Potential of Swertiamarin – A Promising Natural Lead for New Drug Discovery and Development Abstract Abstract Swertiamarin, a seco-iridoid glycoside, is mainly found in Enicostemma littorale Blume ( E. littorale ) and exhibits therapeutic activities for various diseases. The pres...
PMC10797866
core_pubmed_pmc
Evaluating the efficacy of different antibiotics against Neisseria gonorrhoeae : a pharmacokinetic/pharmacodynamic analysis using Monte Carlo simulation
Evaluating the efficacy of different antibiotics against Neisseria gonorrhoeae : a pharmacokinetic/pharmacodynamic analysis using Monte Carlo simulation Abstract Background With the widespread use of antibiotics, antimicrobial resistance in Neisseria gonorrhoeae is worsening. The objective of this study was to evaluate...
PMC10512552
core_pubmed_pmc
Chemical composition, pharmacology and pharmacokinetic studies of GuHong injection in the treatment of ischemic stroke
Chemical composition, pharmacology and pharmacokinetic studies of GuHong injection in the treatment of ischemic stroke Abstract Abstract GuHong injection is composed of safflower and N -acetyl-L-glutamine. It is widely used in clinical for cerebrovascular diseases, such as ischemic stroke and related diseases. The obje...
PMC12637429
core_pubmed_pmc
Quantitative Calibration of a Spatial QSP Model Identifies Fibroblast Impact on HCC Immunotherapy
Quantitative Calibration of a Spatial QSP Model Identifies Fibroblast Impact on HCC Immunotherapy Abstract Computational models are increasingly used to predict treatment response and optimize cancer therapy strategies. Among these, quantitative systems pharmacology (QSP) models mechanistically simulate tumor progressi...
PMC5723108
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic interaction between ezetimibe and rosuvastatin in healthy male subjects
Pharmacokinetic and pharmacodynamic interaction between ezetimibe and rosuvastatin in healthy male subjects Abstract Abstract Background and objective Rosuvastatin and ezetimibe are commonly applied in lipid-lowering pharmacotherapy. However, the pharmacokinetic (PK) interaction was not clear by the coadministration of...
PMC6823932
core_pubmed_pmc
Homotaurine Treatment Enhances CD4 + and CD8 + Regulatory T Cell Responses and Synergizes with Low-Dose Anti-CD3 to Enhance Diabetes Remission in Type 1 Diabetic Mice
Homotaurine Treatment Enhances CD4 + and CD8 + Regulatory T Cell Responses and Synergizes with Low-Dose Anti-CD3 to Enhance Diabetes Remission in Type 1 Diabetic Mice Abstract Immune cells express γ-aminobutyric acid receptors (GABA-R), and GABA administration can inhibit effector T cell responses in models of autoimmu...
PMC8308911
core_pubmed_pmc
Pharmacokinetic Study of Anti-osteoarthritic Compounds of a Standardized Fraction from Sphaeralcea Angustifolia
Pharmacokinetic Study of Anti-osteoarthritic Compounds of a Standardized Fraction from Sphaeralcea Angustifolia Abstract Sphaeralcea angustifolia has been widely used in inflammatory conditions such as blows, bruises, fractures, and wounds. The compounds identified as active in plants and suspension cell culture of S. ...
PMC12153801
core_pubmed_pmc
Targeting the Undruggable: Recent Progress in PROTAC-Induced Transcription Factor Degradation
Targeting the Undruggable: Recent Progress in PROTAC-Induced Transcription Factor Degradation Abstract Simple Summary This manuscript reviews recent advancements in the development of PROTACs (proteolysis-targeting chimeras) designed to target transcription factors (TFs), which have been considered an undruggable targe...
PMC12304797
core_pubmed_pmc
Consideration of ethnic differences in approvals for anti‐HIV medicines in Japan: Evaluation based on pharmacokinetic studies and post‐marketing data
Consideration of ethnic differences in approvals for anti‐HIV medicines in Japan: Evaluation based on pharmacokinetic studies and post‐marketing data Abstract More than 30 anti‐HIV drugs have been approved in Japan using data from dossiers submitted to the United States or European regulatory authorities since 1998. Th...
PMC10462524
core_pubmed_pmc
Pudexacianinium (ASP5354) chloride for ureter visualization in participants undergoing laparoscopic, minimally invasive colorectal surgery
Pudexacianinium (ASP5354) chloride for ureter visualization in participants undergoing laparoscopic, minimally invasive colorectal surgery Abstract Background Intraoperative ureteral injury, a serious complication of abdominopelvic surgeries, can be avoided through ureter visualization. Near-infrared fluorescence imagi...
PMC6330464
core_pubmed_pmc
Superior silybin bioavailability of silybin–phosphatidylcholine complex in oily-medium soft-gel capsules versus conventional silymarin tablets in healthy volunteers*
Superior silybin bioavailability of silybin–phosphatidylcholine complex in oily-medium soft-gel capsules versus conventional silymarin tablets in healthy volunteers* Abstract Abstract Background Fibrosis is a response to chronic liver disease that results in excessive accumulation of extracellular matrix proteins and f...
PMC11026214
core_pubmed_pmc
CNS Viral Infections—What to Consider for Improving Drug Treatment: A Plea for Using Mathematical Modeling Approaches
CNS Viral Infections—What to Consider for Improving Drug Treatment: A Plea for Using Mathematical Modeling Approaches Abstract Abstract Neurotropic viruses may cause meningitis, myelitis, encephalitis, or meningoencephalitis. These inflammatory conditions of the central nervous system (CNS) may have serious and devasta...
PMC6811417
core_pubmed_pmc
Daily Dosing for Bedaquiline in Patients with Tuberculosis
Daily Dosing for Bedaquiline in Patients with Tuberculosis Abstract The bedaquiline regimen for the treatment of multidrug-resistant tuberculosis (MDR-TB) in adults is a loading dose of 400 mg QD for 2 weeks followed by 200 mg thrice weekly (TIW) for 22 weeks. Most TB antibiotics administered with bedaquiline are given...
PMC3264864
core_pubmed_pmc
Administration of Thimerosal to Infant Rats Increases Overflow of Glutamate and Aspartate in the Prefrontal Cortex: Protective Role of Dehydroepiandrosterone Sulfate
Administration of Thimerosal to Infant Rats Increases Overflow of Glutamate and Aspartate in the Prefrontal Cortex: Protective Role of Dehydroepiandrosterone Sulfate Abstract Thimerosal, a mercury-containing vaccine preservative, is a suspected factor in the etiology of neurodevelopmental disorders. We previously showe...
PMC7783676
core_pubmed_pmc
Bioavailability and hepatoprotection enhancement of berberine and its nanoparticles prepared by liquid antisolvent method
Bioavailability and hepatoprotection enhancement of berberine and its nanoparticles prepared by liquid antisolvent method Abstract The study was devised to prepare berberine nanoparticles by anti-solvent precipitation method and were assessed for their hepatoprotective effect in Male Sprague-Dawley rats against carbon ...
PMC5057353
core_pubmed_pmc
Systematic analysis of the polyphenol metabolome using the Phenol‐Explorer database
Systematic analysis of the polyphenol metabolome using the Phenol‐Explorer database Abstract Scope The Phenol‐Explorer web database details 383 polyphenol metabolites identified in human and animal biofluids from 221 publications. Here, we exploit these data to characterize and visualize the polyphenol metabolome, the ...
PMC6024342
core_pubmed_pmc
Rucaparib in ovarian cancer: an update on safety, efficacy and place in therapy
Rucaparib in ovarian cancer: an update on safety, efficacy and place in therapy Abstract Rucaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor and potent inhibitor of PARP1, PARP2 and PARP3 enzymes. Phase II and III trials have documented that rucaparib has single-agent antitumor activity in patients with high-g...
PMC10890472
core_pubmed_pmc
Therapeutic Drug Monitoring for Biologic and Small-Molecule Therapies for Inflammatory Bowel Disease
Therapeutic Drug Monitoring for Biologic and Small-Molecule Therapies for Inflammatory Bowel Disease Abstract Abstract Background: Inflammatory bowel disease (IBD), encompassing ulcerative colitis and Crohn’s disease, necessitates long-term medical therapy to manage symptoms and prevent complications. Therapeutic drug ...
PMC11787236
core_pubmed_pmc
Population Pharmacokinetics of Trofinetide in a Pediatric Population Aged 2–4 Years with Rett Syndrome
Population Pharmacokinetics of Trofinetide in a Pediatric Population Aged 2–4 Years with Rett Syndrome Abstract Abstract Introduction Weight-banded trofinetide dosing improved physician- and caregiver-rated efficacy measures and had acceptable tolerability in patients aged 2‒4 years (DAFFODIL study) and 5‒20 years (LAV...
PMC9315532
core_pubmed_pmc
Chemical and Pharmacological Properties of Decoquinate: A Review of Its Pharmaceutical Potential and Future Perspectives
Chemical and Pharmacological Properties of Decoquinate: A Review of Its Pharmaceutical Potential and Future Perspectives Abstract Abstract Decoquinate (DQ) is an antimicrobial agent commonly used as a feed additive for birds for human consumption. Its use as an additive is well established, but DQ has the potential for...
PMC10088086
core_pubmed_pmc
Deriving mechanism‐based pharmacodynamic models by reducing quantitative systems pharmacology models: An application to warfarin
Deriving mechanism‐based pharmacodynamic models by reducing quantitative systems pharmacology models: An application to warfarin Abstract Abstract Quantitative systems pharmacology (QSP) models integrate comprehensive qualitative and quantitative knowledge about pharmacologically relevant processes. We previously propo...
PMC7680849
core_pubmed_pmc
Pulse Dosing of Antibiotic Enhances Killing of a Staphylococcus aureus Biofilm
Pulse Dosing of Antibiotic Enhances Killing of a Staphylococcus aureus Biofilm Abstract Abstract Biofilms are highly tolerant to antibiotics and underlie the recalcitrance of many chronic infections. We demonstrate that mature Staphylococcus aureus biofilms can be substantially sensitized to the treatment by pulse dosi...
PMC9544041
core_pubmed_pmc
Pharmacokinetics of piperacillin and tazobactam in critically Ill patients treated with continuous kidney replacement therapy: A mini‐review and population pharmacokinetic analysis
Pharmacokinetics of piperacillin and tazobactam in critically Ill patients treated with continuous kidney replacement therapy: A mini‐review and population pharmacokinetic analysis Abstract Abstract What is known and objective Timely and appropriate dosing of antibiotics is essential for the treatment of bacterial seps...
PMC5732473
core_pubmed_pmc
Linking physiologically-based pharmacokinetic and genome-scale metabolic networks to understand estradiol biology
Linking physiologically-based pharmacokinetic and genome-scale metabolic networks to understand estradiol biology Abstract Abstract Background Estrogen is a vital hormone that regulates many biological functions within the body. These include roles in the development of the secondary sexual organs in both sexes, plus u...
PMC6624389
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic modelling for renal function dependent urinary glucose excretion effect of ipragliflozin, a selective sodium–glucose cotransporter 2 inhibitor, both in healthy subjects and patients with type 2 diabetes mellitus
Pharmacokinetic and pharmacodynamic modelling for renal function dependent urinary glucose excretion effect of ipragliflozin, a selective sodium–glucose cotransporter 2 inhibitor, both in healthy subjects and patients with type 2 diabetes mellitus Abstract Aims To provide a model‐based prediction of individual urinary ...
PMC8988824
core_pubmed_pmc
Subcutaneous in situ gel delivered leuprolide acetate's consistent and prolonged drug delivery maintains effective testosterone suppression independent of age and weight in men with prostate cancer
Subcutaneous in situ gel delivered leuprolide acetate's consistent and prolonged drug delivery maintains effective testosterone suppression independent of age and weight in men with prostate cancer Abstract Abstract Objectives To assess the impact of patient age and weight on the pharmacokinetics (PK), testosterone (T)...
PMC4215596
core_pubmed_pmc
Pharmacokinetics of plasma-derived C1-esterase inhibitor after subcutaneous versus intravenous administration in subjects with mild or moderate hereditary angioedema: the PASSION study
Pharmacokinetics of plasma-derived C1-esterase inhibitor after subcutaneous versus intravenous administration in subjects with mild or moderate hereditary angioedema: the PASSION study Abstract Abstract Background Hereditary angioedema (HAE) is a rare disease caused by C1-esterase inhibitor (C1-INH) deficiency, charact...
PMC4623454
core_pubmed_pmc
The efficacy and safety of Montelukast sodium in the prevention of bronchopulmonary dysplasia
The efficacy and safety of Montelukast sodium in the prevention of bronchopulmonary dysplasia Abstract Purpose The purpose of this study was to evaluate the efficacy and safety of Montelukast sodium in the prevention of bronchopulmonarydysplasia (BPD). Methods The Interventional study was designed as a multicenter, pro...
PMC11005099
core_pubmed_pmc
Absorption and pharmacokinetics of bupivacaine after bilateral topical administration in tonsillar fossae for posttonsillectomy pain relief
Absorption and pharmacokinetics of bupivacaine after bilateral topical administration in tonsillar fossae for posttonsillectomy pain relief Abstract Abstract No previous studies have investigated the systemic absorption of bupivacaine when used topically for posttonsillectomy pain. The present study was undertaken to i...
PMC10334359
core_pubmed_pmc
Novel wine in an old bottle: Preventive and therapeutic potentials of andrographolide in atherosclerotic cardiovascular diseases
Novel wine in an old bottle: Preventive and therapeutic potentials of andrographolide in atherosclerotic cardiovascular diseases Abstract Abstract Atherosclerotic cardiovascular disease (ASCVD) frequently results in sudden death and poses a serious threat to public health worldwide. The drugs approved for the preventio...
PMC9919343
core_pubmed_pmc
Screening of Active Ingredients from Wendan Decoction in Alleviating Palmitic Acid-Induced Endothelial Cell Injury
Screening of Active Ingredients from Wendan Decoction in Alleviating Palmitic Acid-Induced Endothelial Cell Injury Abstract Abstract (1) Objective: Traditional Chinese medicine (TCM) plays an important role in the treatment of numerous illnesses. As a classic Chinese medicine, Wendan Decoction (WDD) encompasses a marve...
PMC7892868
core_pubmed_pmc
Interaction study of monoisoamyl dimercaptosuccinic acid with bovine serum albumin using biophysical and molecular docking approaches
Interaction study of monoisoamyl dimercaptosuccinic acid with bovine serum albumin using biophysical and molecular docking approaches Abstract Monoisoamyl 2,3-dimercaptosuccinic acid (MiADMSA), a lipophilic chelator has been evaluated for its potential use as an antidote in arsenic poisoning. The pharmacokinetics and p...
PMC10864930
core_pubmed_pmc
Multistate modeling for survival analysis in critically ill patients treated with meropenem
Multistate modeling for survival analysis in critically ill patients treated with meropenem Abstract Abstract Appropriate antibiotic dosing to ensure early and sufficient target attainment is crucial for improving clinical outcome in critically ill patients. Parametric survival analysis is a preferred modeling method t...
PMC8229588
core_pubmed_pmc
Analysis of Pembrolizumab in Human Plasma by LC-MS/HRMS. Method Validation and Comparison with Elisa
Analysis of Pembrolizumab in Human Plasma by LC-MS/HRMS. Method Validation and Comparison with Elisa Abstract Pembrolizumab is a humanized immunoglobulin G4-kappa anti-PD1 antibody used in the treatment of different solid tumors or haematological malignancies. A liquid chromatography coupled with a high resolution mass...
PMC12849519
core_pubmed_pmc
A phase 1, multicenter, open‐label study to evaluate the pharmacokinetics, safety, and tolerability of a single dose of rimegepant in children (aged ≥6 to <12 years) with a history of migraine
A phase 1, multicenter, open‐label study to evaluate the pharmacokinetics, safety, and tolerability of a single dose of rimegepant in children (aged ≥6 to <12 years) with a history of migraine Abstract Abstract Objective To evaluate pharmacokinetics (PK), safety, and tolerability of a weight‐adjusted dose of rimegepant...
PMC12278333
core_pubmed_pmc
Concentration–Response Analysis of the Combination of Pyronaridine and Piperaquine on Corrected QT Interval From a Randomized, Double‐Blind, Placebo‐Controlled Study in Healthy Adults of African Sub‐Saharan Origin
Concentration–Response Analysis of the Combination of Pyronaridine and Piperaquine on Corrected QT Interval From a Randomized, Double‐Blind, Placebo‐Controlled Study in Healthy Adults of African Sub‐Saharan Origin Abstract ABSTRACT A novel oral combination of the long‐acting antimalarials pyronaridine (PYR) and piperaq...
PMC8370625
core_pubmed_pmc
Integration of a physiologically-based pharmacokinetic model with a whole-body, organ-resolved genome-scale model for characterization of ethanol and acetaldehyde metabolism
Integration of a physiologically-based pharmacokinetic model with a whole-body, organ-resolved genome-scale model for characterization of ethanol and acetaldehyde metabolism Abstract Ethanol is one of the most widely used recreational substances in the world and due to its ubiquitous use, ethanol abuse has been the cau...
PMC12413702
core_pubmed_pmc
Results of the first-in-human, randomized, double-blind, placebo-controlled, single- and multiple-ascending dose study of BIIB113 in healthy volunteers
Results of the first-in-human, randomized, double-blind, placebo-controlled, single- and multiple-ascending dose study of BIIB113 in healthy volunteers Abstract Background Preclinical studies have demonstrated that inhibition of the O-linked β-N-acetylglucosaminidase enzyme increases tau O-linked β-N-acetylglucosaminyl...
PMC6791659
core_pubmed_pmc
Extrapolation of Hepatic Concentrations of Industrial Chemicals Using Pharmacokinetic Models to Predict Hepatotoxicity
Extrapolation of Hepatic Concentrations of Industrial Chemicals Using Pharmacokinetic Models to Predict Hepatotoxicity Abstract In this review, we describe the absorption rates (Caco-2 cell permeability) and hepatic/plasma pharmacokinetics of 53 diverse chemicals estimated by modeling virtual oral administration in rat...
PMC5488128
core_pubmed_pmc
A Population Dose–Response Model for Inhaled Technosphere Insulin Administered to Healthy Subjects
A Population Dose–Response Model for Inhaled Technosphere Insulin Administered to Healthy Subjects Abstract Technosphere insulin (TI), an inhaled insulin with a fast onset of action, provides a novel option for the control of prandial glucose. A euglycemic glucose clamp study was performed to compare the effects of TI ...
PMC4630395
core_pubmed_pmc
Evaluation of the Association Metformin: Plantago ovata Husk in Diabetic Rabbits
Evaluation of the Association Metformin: Plantago ovata Husk in Diabetic Rabbits Abstract Abstract In this experimental study we have investigated whether the inclusion of the dietary fiber Plantago ovata husk could be recommended as coadjuvant in treatments with oral hypoglycemic drugs. We evaluated the use of Plantag...
PMC4094568
core_pubmed_pmc
Drug delivery options to increase patient adherence and satisfaction in the management of rheumatoid arthritis – focus on subcutaneous tocilizumab
Drug delivery options to increase patient adherence and satisfaction in the management of rheumatoid arthritis – focus on subcutaneous tocilizumab Abstract Rheumatoid arthritis (RA) is a chronic, progressive, inflammatory disease associated with joint destruction. Tocilizumab (TCZ) is a humanized monoclonal anti-interl...
PMC9113852
core_pubmed_pmc
Pharmacokinetics of Direct Oral Anticoagulants in Emergency Situations: Results of the Prospective Observational RADOA-Registry
Pharmacokinetics of Direct Oral Anticoagulants in Emergency Situations: Results of the Prospective Observational RADOA-Registry Abstract Abstract Background Direct oral anticoagulants (DOACs) are increasingly used worldwide. Little is known so far about their pharmacokinetics in emergency situations. Methods A prospect...
PMC4483206
core_pubmed_pmc
Translocation of gold nanoparticles across the lung epithelial tissue barrier: Combining in vitro and in silico methods to substitute in vivo experiments
Translocation of gold nanoparticles across the lung epithelial tissue barrier: Combining in vitro and in silico methods to substitute in vivo experiments Abstract Background The lung epithelial tissue barrier represents the main portal for entry of inhaled nanoparticles (NPs) into the systemic circulation. Thus great e...
PMC12609464
core_pubmed_pmc
Does the Injection Site Matter During CPR? A Systematic Review and Meta-Analysis of Drug Pharmacokinetics and Pharmacodynamics
Does the Injection Site Matter During CPR? A Systematic Review and Meta-Analysis of Drug Pharmacokinetics and Pharmacodynamics Abstract Abstract Background: Cardiac arrest is a time-critical medical emergency during which prompt and effective drug delivery plays a key role in patient outcomes. Current resuscitation gui...
PMC3757598
core_pubmed_pmc
Pharmacokinetics of single-dose primaquine in patients with chronic kidney dysfunction
Pharmacokinetics of single-dose primaquine in patients with chronic kidney dysfunction Abstract Abstract Aim: The pharmacokinetics of primaquine has not been studied in special populations. Being a basic compound, preferential binding to alpha-1 acid glycoprotein and substrate for P-glycoprotein, may predispose the dru...
PMC12485380
core_pubmed_pmc
Antineoplastic Activity of a Novel Trispecific Single-Chain Antibody Targeting the hERG1/β1 Integrin Complex and TRAIL Receptors
Antineoplastic Activity of a Novel Trispecific Single-Chain Antibody Targeting the hERG1/β1 Integrin Complex and TRAIL Receptors Abstract Abstract Targeted therapies and immunotherapies have largely improved cancer treatment in the last years. One of the most promising approaches is the induction of tumor apoptosis by ...
PMC6310868
core_pubmed_pmc
A Strategy to Refine the Phenotyping Approach and Its Implementation to Predict Drug Clearance: A Physiologically Based Pharmacokinetic Simulation Study
A Strategy to Refine the Phenotyping Approach and Its Implementation to Predict Drug Clearance: A Physiologically Based Pharmacokinetic Simulation Study Abstract Abstract The phenotyping approach to predict drug metabolism activity is often hampered by a lack of correlation between the probe and the drug of interest. I...
PMC7467425
core_pubmed_pmc
Pharmacokinetics and Dialyzability of a Single Oral Dose of Amenamevir, an Anti-Herpes Drug, in Hemodialysis Patients
Pharmacokinetics and Dialyzability of a Single Oral Dose of Amenamevir, an Anti-Herpes Drug, in Hemodialysis Patients Abstract Abstract Introduction Amenamevir (ASP2151), a herpesvirus helicase-primase inhibitor, is currently used for the treatment of herpes zoster in Japan. Amenamevir is mainly metabolized in the live...
PMC11993590
core_pubmed_pmc
Repurposing FDA-approved drugs and natural compounds to inhibit the RNA-dependent RNA polymerase domain of dengue virus 2 or dengue virus 3
Repurposing FDA-approved drugs and natural compounds to inhibit the RNA-dependent RNA polymerase domain of dengue virus 2 or dengue virus 3 Abstract The dengue virus, a member of the arbovirus family, can cause a variety of clinical symptoms. However, there are currently no Food and Drug Administration-approved drugs a...
PMC9003539
core_pubmed_pmc
Evolution of Toll-like receptor 7/8 agonist therapeutics and their delivery approaches: From antiviral formulations to vaccine adjuvants
Evolution of Toll-like receptor 7/8 agonist therapeutics and their delivery approaches: From antiviral formulations to vaccine adjuvants Abstract Imidazoquinoline derivatives (IMDs) and related compounds function as synthetic agonists of Toll-like receptors 7 and 8 (TLR7/8) and one is FDA approved for topical antiviral...
PMC11580420
core_pubmed_pmc
Immunomodulatory activity of omadacycline in vitro and in a murine model of acute lung injury
Immunomodulatory activity of omadacycline in vitro and in a murine model of acute lung injury Abstract ABSTRACT Cystic fibrosis (CF) is characterized by chronic airway obstruction, infection, and inflammation leading to progressive loss of lung function and eventual respiratory failure. Omadacycline, a tetracycline ant...