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PMC3394467 | core_pubmed_pmc | Pharmacokinetics, tissue distribution, and excretion of zinc oxide nanoparticles | Pharmacokinetics, tissue distribution, and excretion of zinc oxide nanoparticles Abstract Abstract Background This study explored the pharmacokinetics, tissue distribution, and excretion profile of zinc oxide (ZnO) nanoparticles with respect to their particle size in rats. Methods Two ZnO nanoparticles of different siz... |
PMC10687521 | core_pubmed_pmc | Effect of “magic chlorine” in drug discovery: an in silico approach † | Effect of “magic chlorine” in drug discovery: an in silico approach † Abstract Abstract The chlorine atom plays a vital role in drug design, yet the benefits of chlorine in 250 FDA-approved chlorine-containing drugs have not been studied properly. To see the “magic chloro” effect, computational studies have been carrie... |
PMC5788205 | core_pubmed_pmc | Drug Interactions of Metformin Involving Drug Transporter Proteins | Drug Interactions of Metformin Involving Drug Transporter Proteins Abstract Abstract Metformin is a most widely used medication all around the world to treat Type 2 diabetes mellitus. It is also found to be effective against various conditions including, Prediabetes, Gestational diabetes mellitus (GDM), Polycystic Ovar... |
PMC9718031 | core_pubmed_pmc | Systematic review of efficacy, safety and pharmacokinetics of intravenous and intraventricular vancomycin for central nervous system infections | Systematic review of efficacy, safety and pharmacokinetics of intravenous and intraventricular vancomycin for central nervous system infections Abstract Objective: The decision of vancomycin dosage for central nervous system (CNS) infections is still a challenge because its bactericidal nature in cerebrospinal fluid (C... |
PMC9545794 | core_pubmed_pmc | Befovacimab, an anti‐tissue factor pathway inhibitor antibody: Early termination of the multiple‐dose, dose‐escalating Phase 2 study due to thrombosis | Befovacimab, an anti‐tissue factor pathway inhibitor antibody: Early termination of the multiple‐dose, dose‐escalating Phase 2 study due to thrombosis Abstract Abstract Introduction Befovacimab (formerly BAY 1093884) is a fully human monoclonal antibody able to bind to tissue factor pathway inhibitor (TFPI) and develop... |
PMC12843472 | core_pubmed_pmc | Genetic Markers of Methotrexate Treatment Failure in Psoriasis | Genetic Markers of Methotrexate Treatment Failure in Psoriasis Abstract Abstract Background: Pharmacogenetic markers associated with the need to switch patients from methotrexate (MTX) to biologic agents in moderate-to-severe psoriasis remain insufficiently studied. The pharmacokinetics of MTX depend on the individual ... |
PMC12711802 | core_pubmed_pmc | Physiologically-based pharmacokinetic modeling and simulation for initial dose optimization of levetiracetam in pediatrics | Physiologically-based pharmacokinetic modeling and simulation for initial dose optimization of levetiracetam in pediatrics Abstract Introduction Optimizing levetiracetam (LEV) dosing in children is challenging due to high pharmacokinetic variability, which often necessitates empirical dose titration. This study aimed t... |
PMC7325319 | core_pubmed_pmc | Pharmacokinetic Modeling of Intrathecally Administered Recombinant Human Arylsulfatase A (TAK‐611) in Children With Metachromatic Leukodystrophy | Pharmacokinetic Modeling of Intrathecally Administered Recombinant Human Arylsulfatase A (TAK‐611) in Children With Metachromatic Leukodystrophy Abstract Metachromatic leukodystrophy (MLD) is a lysosomal storage disease caused by deficient arylsulfatase A (ASA) activity, which leads to neuronal sulfatide accumulation a... |
PMC7137434 | core_pubmed_pmc | Efficacy data of halogenated phenazine and quinoline agents and an NH125 analogue to veterinary mycoplasmas | Efficacy data of halogenated phenazine and quinoline agents and an NH125 analogue to veterinary mycoplasmas Abstract Background Mycoplasmas primarily cause respiratory or urogenital tract infections impacting avian, bovine, canine, caprine, murine, and reptilian hosts. In animal husbandry, mycoplasmas cause reduced fee... |
PMC7818330 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Three Different Formulations of Insulin Aspart: A Randomized, Double-Blind, Crossover Study in Men With Type 1 Diabetes | Pharmacokinetics and Pharmacodynamics of Three Different Formulations of Insulin Aspart: A Randomized, Double-Blind, Crossover Study in Men With Type 1 Diabetes Abstract OBJECTIVE To investigate the pharmacokinetic and pharmacodynamic properties and safety of a novel formulation of insulin aspart (AT247) versus two cur... |
PMC6754918 | core_pubmed_pmc | A Loading Dose of IV Salbutamol in an Adolescent with Severe Acute Asthma and Cardiac Arrest | A Loading Dose of IV Salbutamol in an Adolescent with Severe Acute Asthma and Cardiac Arrest Abstract Abstract Severe acute asthma (SAA) can lead to respiratory failure and can be fatal. For rational use of intravenous (IV) bronchodilators, evidence regarding the pharmacokinetics and pharmacodynamics is lacking in chil... |
PMC4126759 | core_pubmed_pmc | Evaluation of Sexual Dimorphism in the Efficacy and Safety of Simvastatin/Atorvastatin Therapy in a Southern Brazilian Cohort | Evaluation of Sexual Dimorphism in the Efficacy and Safety of Simvastatin/Atorvastatin Therapy in a Southern Brazilian Cohort Abstract Background Dyslipidemia is the primary risk factor for cardiovascular disease, and statins have been effective in controlling lipid levels. Sex differences in the pharmacokinetics and p... |
PMC7993252 | core_pubmed_pmc | Pharmacokinetics of Sugammadex Dosed by Actual and Ideal Body Weight in Patients With Morbid Obesity Undergoing Surgery | Pharmacokinetics of Sugammadex Dosed by Actual and Ideal Body Weight in Patients With Morbid Obesity Undergoing Surgery Abstract Abstract This analysis of a published study ( NCT03346070 ) evaluated the pharmacokinetics (PKs) of sugammadex dosed by actual body weight (ABW) or ideal body weight (IBW) for reversal of mod... |
PMC6152131 | core_pubmed_pmc | Pharmacokinetic Study of Biotransformation Products from an Anxiolytic Fraction of Tilia americana | Pharmacokinetic Study of Biotransformation Products from an Anxiolytic Fraction of Tilia americana Abstract An anxiolytic fraction of Tilia americana standardized in tiliroside, rutin, quercitrin, quercetin glucoside, and kaempferol was obtained. After oral administration of the fraction, the above-mentioned flavonoids... |
PMC10066765 | core_pubmed_pmc | Translational Pharmacokinetic/Pharmacodynamic Model for mRNA-3927, an Investigational Therapeutic for the Treatment of Propionic Acidemia | Translational Pharmacokinetic/Pharmacodynamic Model for mRNA-3927, an Investigational Therapeutic for the Treatment of Propionic Acidemia Abstract Propionic acidemia (PA) is an ultrarare disorder caused by deficiency of the mitochondrial enzyme, propionyl-CoA carboxylase (PCC), composed of PCCA and PCCB subunits. An en... |
PMC11106552 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of single‐ and multiple‐ascending doses of olamkicept: Results from randomized, placebo‐controlled, first‐in‐human phase I trials | Safety, tolerability, and pharmacokinetics of single‐ and multiple‐ascending doses of olamkicept: Results from randomized, placebo‐controlled, first‐in‐human phase I trials Abstract Abstract Olamkicept selectively inhibits the cytokine interleukin‐6 (IL‐6) trans‐signaling pathway without blocking the classic pathway an... |
PMC7028136 | core_pubmed_pmc | One piece of the puzzle: Population pharmacokinetics of FVIII during perioperative Haemate P ® /Humate P ® treatment in von Willebrand disease patients | One piece of the puzzle: Population pharmacokinetics of FVIII during perioperative Haemate P ® /Humate P ® treatment in von Willebrand disease patients Abstract Abstract Introduction Many patients with von Willebrand disease (VWD) are treated on demand with von Willebrand factor and factor VIII (FVIII) containing conce... |
PMC4488187 | core_pubmed_pmc | Lisdexamfetamine Dimesylate Effects on the Pharmacokinetics of Cytochrome P450 Substrates in Healthy Adults in an Open-Label, Randomized, Crossover Study | Lisdexamfetamine Dimesylate Effects on the Pharmacokinetics of Cytochrome P450 Substrates in Healthy Adults in an Open-Label, Randomized, Crossover Study Abstract Introduction This open-label, randomized, two-period drug interaction study assessed lisdexamfetamine dimesylate (LDX) effects on cytochrome P450 (CYP) enzym... |
PMC7497526 | core_pubmed_pmc | Nanoparticles Presenting Potent TLR7/8 Agonists Enhance Anti-PD-L1 Immunotherapy in Cancer Treatment | Nanoparticles Presenting Potent TLR7/8 Agonists Enhance Anti-PD-L1 Immunotherapy in Cancer Treatment Abstract Cancer immunotherapy can be augmented with toll-like receptor agonist (TLRa) adjuvants, which interact with immune cells to elicit potent immune activation. Despite their potential, use of many TLRa compounds h... |
PMC6250621 | core_pubmed_pmc | Improved Glycemic Control with Insulin Glargine 300 U/mL (Toujeo ® ) in Patients with Type 2 Diabetes: Real-World Effectiveness in Switzerland | Improved Glycemic Control with Insulin Glargine 300 U/mL (Toujeo ® ) in Patients with Type 2 Diabetes: Real-World Effectiveness in Switzerland Abstract Abstract Introduction Insulin glargine 300 U/mL (Gla-300, Toujeo ® ) is a long-acting, once-daily basal insulin with improved—more stable and smoother—pharmacokinetic a... |
PMC8156151 | core_pubmed_pmc | Target inhibition of galectin-3 by inhaled TD139 in patients with idiopathic pulmonary fibrosis | Target inhibition of galectin-3 by inhaled TD139 in patients with idiopathic pulmonary fibrosis Abstract Galectin (Gal)-3 is a profibrotic β-galactoside-binding lectin that plays a key role in the pathogenesis of idiopathic pulmonary fibrosis (IPF) and IPF exacerbations. TD139 is a novel and potent small-molecule inhib... |
PMC12864425 | core_pubmed_pmc | Very low enalapril and enalaprilat exposure via human milk: a case report from the ConcePTION project | Very low enalapril and enalaprilat exposure via human milk: a case report from the ConcePTION project Abstract Introduction Ongoing maternal and clinical hesitancy in breastfeeding-related shared decision-making is driven by limited safety data on maternal pharmacotherapy. Theoretical exposure to maternal enalapril and... |
PMC5599948 | core_pubmed_pmc | Preclinical and Healthy Volunteer Studies of Potential Drug–Drug Interactions Between Tenapanor and Phosphate Binders | Preclinical and Healthy Volunteer Studies of Potential Drug–Drug Interactions Between Tenapanor and Phosphate Binders Abstract Abstract Tenapanor (RDX5791, AZD1722), a first‐in‐class small molecule with minimal systemic availability, is an inhibitor of the sodium/hydrogen exchanger isoform 3. Tenapanor acts locally in ... |
PMC12205756 | core_pubmed_pmc | Marstacimab for the Treatment of Hemophilia A or B | Marstacimab for the Treatment of Hemophilia A or B Abstract Abstract Hemophilia A and B, caused by deficiencies of coagulation factors VIII or IX, result in impaired thrombin generation with consequent spontaneous or trauma-related bleeding, particularly hemarthroses. Although prophylactic factor replacement therapy re... |
PMC9320958 | core_pubmed_pmc | Intravenous Perampanel as an Interchangeable Alternative to Oral Perampanel: A Randomized, Crossover, Phase I Pharmacokinetic and Safety Study | Intravenous Perampanel as an Interchangeable Alternative to Oral Perampanel: A Randomized, Crossover, Phase I Pharmacokinetic and Safety Study Abstract Abstract Intravenous (IV) drug administration enables treatment of epilepsy when oral administration is temporarily not feasible. Perampanel is a once‐daily antiseizure... |
PMC8941156 | core_pubmed_pmc | Single dose oral pharmacokinetic profile rubraxanthone in mice | Single dose oral pharmacokinetic profile rubraxanthone in mice Abstract Rubraxanthone is a main active constituent of kandis ( Garcinia cowa Roxb), has showed many biological activity including antimicrobial, anti hypercholesterolemic, antiplatelet, antioxidant, cytotoxic, and anti-inflammatory properties. To the best ... |
PMC3627472 | core_pubmed_pmc | In vitro and in vivo evaluation of a sublingual fentanyl wafer formulation | In vitro and in vivo evaluation of a sublingual fentanyl wafer formulation Abstract Abstract Background The objective of this study was to prepare a novel fentanyl wafer formulation by a freeze-drying method, and to evaluate its in vitro and in vivo release characteristics, including its bioavailability via the subling... |
PMC4164907 | core_pubmed_pmc | Bioavailability of AREDS1 micronutrients from softgel capsules and tablets: a pilot study | Bioavailability of AREDS1 micronutrients from softgel capsules and tablets: a pilot study Abstract Abstract Purpose The benefits of antioxidant micronutrients in slowing progression to advanced stages of age-related macular degeneration (AMD) was supported by the 4/day tablet form investigated in the Age-related Eye Di... |
PMC4913203 | core_pubmed_pmc | Long-term study of the impact of methotrexate on serum cytokines and lymphocyte subsets in patients with active rheumatoid arthritis: correlation with pharmacokinetic measures | Long-term study of the impact of methotrexate on serum cytokines and lymphocyte subsets in patients with active rheumatoid arthritis: correlation with pharmacokinetic measures Abstract Abstract Objective To describe changes in immune parameters observed during long-term methotrexate (MTX) therapy in patients with activ... |
PMC12655802 | core_pubmed_pmc | Effectiveness, Safety, and Real-World Experience of Brolucizumab: A Systematic Review | Effectiveness, Safety, and Real-World Experience of Brolucizumab: A Systematic Review Abstract Abstract Background/Objectives: Brolucizumab is a humanized single-chain antibody fragment with a molecular weight of approximately 26 kilodaltons (scFv, ~26 kDa) targeting all VEGF-A isoforms. Intravitreal brolucizumab (6 mg... |
PMC9742156 | core_pubmed_pmc | Emergence of phenotypic and genotypic antimicrobial resistance in Mycobacterium tuberculosis | Emergence of phenotypic and genotypic antimicrobial resistance in Mycobacterium tuberculosis Abstract Concentration dependency of phenotypic and genotypic isoniazid-rifampicin resistance emergence was investigated to obtain a mechanistic understanding on how anti-mycobacterial drugs facilitate the emergence of bacteria... |
PMC12891543 | core_pubmed_pmc | A repurposing Dapagliflozin via polymeric nanogels for colorectal cancer therapy | A repurposing Dapagliflozin via polymeric nanogels for colorectal cancer therapy Abstract Abstract Dapagliflozin (DAPA), a selective SGLT2 inhibitor approved for type 2 diabetes, shows emerging potential for repurposing in oncology due to its anti-inflammatory and antiproliferative properties. However, its poor solubil... |
PMC7318247 | core_pubmed_pmc | Safety and Efficacy of Teduglutide in Pediatric Patients With Intestinal Failure due to Short Bowel Syndrome: A 24‐Week, Phase III Study | Safety and Efficacy of Teduglutide in Pediatric Patients With Intestinal Failure due to Short Bowel Syndrome: A 24‐Week, Phase III Study Abstract Abstract Background This study evaluated the safety and efficacy of teduglutide in pediatric patients with short bowel syndrome–associated intestinal failure (SBS‐IF). Method... |
PMC9603373 | core_pubmed_pmc | A High Daptomycin Dose Is Associated with Better Bacterial Clearance in Infections Caused by Vancomycin-Resistant Enterococcus faecium Regardless of Daptomycin Minimum Inhibitory Concentration in a Rat Infective Endocarditis Model | A High Daptomycin Dose Is Associated with Better Bacterial Clearance in Infections Caused by Vancomycin-Resistant Enterococcus faecium Regardless of Daptomycin Minimum Inhibitory Concentration in a Rat Infective Endocarditis Model Abstract ABSTRACT A high daptomycin dose has been suggested for treating vancomycin-resis... |
PMC12260160 | core_pubmed_pmc | Dashboard-Guided Anti-TNF Induction: An Effective Strategy to Minimize Immunogenicity While Avoiding Immunomodulators—A Single-Center Cohort Study | Dashboard-Guided Anti-TNF Induction: An Effective Strategy to Minimize Immunogenicity While Avoiding Immunomodulators—A Single-Center Cohort Study Abstract Abstract Background Proactive therapeutic drug monitoring facilitates early dose optimization to prevent primary and secondary failure to antitumor necrosis factor ... |
PMC8699239 | core_pubmed_pmc | Developing a Nationwide Infrastructure for Therapeutic Drug Monitoring of Targeted Oral Anticancer Drugs: The ON-TARGET Study Protocol | Developing a Nationwide Infrastructure for Therapeutic Drug Monitoring of Targeted Oral Anticancer Drugs: The ON-TARGET Study Protocol Abstract Simple Summary Relationships between drug concentrations in blood and efficacy and/or toxicity have been reported for up to 80% of oral anticancer drugs (OADs). Most OADs exhib... |
PMC7235595 | core_pubmed_pmc | Implications of nonlinearity, confounding, and interactions for estimating exposure concentration-response functions in quantitative risk analysis | Implications of nonlinearity, confounding, and interactions for estimating exposure concentration-response functions in quantitative risk analysis Abstract Abstract Recent advances in understanding of biological mechanisms and adverse outcome pathways for many exposure-related diseases show that certain common mechanis... |
PMC11812931 | core_pubmed_pmc | MDMA pharmacokinetics: A population and physiologically based pharmacokinetics model‐informed analysis | MDMA pharmacokinetics: A population and physiologically based pharmacokinetics model‐informed analysis Abstract Abstract Midomafetamine (3,4‐methylenedioxymethamphetamine [MDMA]) is under the U.S. Food and Drug Administration review for treatment of post‐traumatic stress disorder in adults. MDMA is metabolized by CYP2D... |
PMC8419969 | core_pubmed_pmc | Pharmacokinetic herb-drug interactions between Aidi injection and doxorubicin in rats with diethylnitrosamine-induced hepatocellular carcinoma | Pharmacokinetic herb-drug interactions between Aidi injection and doxorubicin in rats with diethylnitrosamine-induced hepatocellular carcinoma Abstract Abstract Background Aidi Injection (ADI), a Chinese herbal preparation with anti-cancer activity, is used for the treatment of hepatocellular carcinoma (HCC). Several c... |
PMC9907211 | core_pubmed_pmc | Identification of Pyrazole Derivatives of Usnic Acid as Novel Inhibitor of SARS-CoV-2 Main Protease Through Virtual Screening Approaches | Identification of Pyrazole Derivatives of Usnic Acid as Novel Inhibitor of SARS-CoV-2 Main Protease Through Virtual Screening Approaches Abstract Abstract The infection produced by the SARS-CoV-2 virus remains a significant health crisis worldwide. The lack of specific medications for COVID-19 necessitates a concerted ... |
PMC5699789 | core_pubmed_pmc | Predicting tacrolimus concentrations in children receiving a heart transplant using a population pharmacokinetic model | Predicting tacrolimus concentrations in children receiving a heart transplant using a population pharmacokinetic model Abstract Abstract Objective Immunosuppressant therapy plays a pivotal role in transplant success and longevity. Tacrolimus, a primary immunosuppressive agent, is well known to exhibit significant pharm... |
PMC10087070 | core_pubmed_pmc | First‐in‐human study with SAR445088: A novel selective classical complement pathway inhibitor | First‐in‐human study with SAR445088: A novel selective classical complement pathway inhibitor Abstract Abstract SAR445088 is an anti‐C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system and has the potential to provide clinical benefit in the treatment... |
PMC8214503 | core_pubmed_pmc | The Effect of Single-Dose Ougan Juice Application on the Pharmacokinetics of Erlotinib | The Effect of Single-Dose Ougan Juice Application on the Pharmacokinetics of Erlotinib Abstract Abstract The aim of our study was to investigate the effects of single-dose Ougan (Citrus reticulata cv. Suavissima) juice application on the pharmacokinetics of erlotinib in vivo. Twelve Sprague-Dawley rats were randomly di... |
PMC8505328 | core_pubmed_pmc | Antimicrobial Dose Reduction in Continuous Renal Replacement Therapy: Myth or Real Need? A Practical Approach for Guiding Dose Optimization of Novel Antibiotics | Antimicrobial Dose Reduction in Continuous Renal Replacement Therapy: Myth or Real Need? A Practical Approach for Guiding Dose Optimization of Novel Antibiotics Abstract Abstract Acute kidney injury represents a common complication in critically ill patients affected by septic shock and in many cases continuous renal r... |
PMC6160962 | core_pubmed_pmc | Pharmacokinetics and Anti-Gastric Ulceration Activity of Oral Administration of Aceclofenac and Esomeprazole in Rats | Pharmacokinetics and Anti-Gastric Ulceration Activity of Oral Administration of Aceclofenac and Esomeprazole in Rats Abstract Abstract This study examined the effects of esomeprazole on aceclofenac pharmacokinetics and gastrointestinal complications in rats. Aceclofenac alone, or in combination with esomeprazole, was o... |
PMC4700065 | core_pubmed_pmc | Insulin Aspart in the Management of Diabetes Mellitus: 15 Years of Clinical Experience | Insulin Aspart in the Management of Diabetes Mellitus: 15 Years of Clinical Experience Abstract Limiting excessive postprandial glucose excursions is an important component of good overall glycemic control in diabetes mellitus. Pharmacokinetic studies have shown that insulin aspart, which is structurally identical to r... |
PMC7868135 | core_pubmed_pmc | Kochiae Fructus, the Fruit of Common Potherb Kochia scoparia (L.) Schrad: A Review on Phytochemistry, Pharmacology, Toxicology, Quality Control, and Pharmacokinetics | Kochiae Fructus, the Fruit of Common Potherb Kochia scoparia (L.) Schrad: A Review on Phytochemistry, Pharmacology, Toxicology, Quality Control, and Pharmacokinetics Abstract Abstract Kochiae Fructus (KF) is the fruit of an annual potherb Kochia scoparia (Linn.) Schrad and has been traditionally used for the treatment ... |
PMC12622633 | core_pubmed_pmc | Multi-omics evidence supports PROC as a potential predictor of VTE risk: A Mendelian randomization study | Multi-omics evidence supports PROC as a potential predictor of VTE risk: A Mendelian randomization study Abstract Venous thromboembolism (VTE) is a common cardiovascular condition whose etiology is closely linked to a range of factors, including trauma, immobilization, and environmental influences. The application of m... |
PMC12114834 | core_pubmed_pmc | Quinoline Quest: Kynurenic Acid Strategies for Next-Generation Therapeutics via Rational Drug Design | Quinoline Quest: Kynurenic Acid Strategies for Next-Generation Therapeutics via Rational Drug Design Abstract Abstract Background: Quinoline-derived metabolites exhibit notable chemical complexity. What causes minor structural alterations to induce significant changes in disease outcomes? Historically, eclipsed by more... |
PMC8160209 | core_pubmed_pmc | A hybrid modeling approach for assessing mechanistic models of small molecule partitioning in vivo using a machine learning-integrated modeling platform | A hybrid modeling approach for assessing mechanistic models of small molecule partitioning in vivo using a machine learning-integrated modeling platform Abstract Prediction of the first-in-human dosing regimens is a critical step in drug development and requires accurate quantitation of drug distribution. Traditional i... |
PMC12272319 | core_pubmed_pmc | Characterization of Apixaban Pharmacokinetics/Pharmacodynamics and Dose Assessment in Pediatric Patients with Congenital or Acquired Heart Disease | Characterization of Apixaban Pharmacokinetics/Pharmacodynamics and Dose Assessment in Pediatric Patients with Congenital or Acquired Heart Disease Abstract Abstract Apixaban is an oral direct inhibitor of factor Xa (FXa) that could be a treatment option for thromboembolism prevention in children with congenital or acqu... |
PMC7818398 | core_pubmed_pmc | Effects of ABCB1 , UGT1A1 , and UGT1A9 Genetic Polymorphisms on the Pharmacokinetics of Sitafloxacin Granules in Healthy Subjects | Effects of ABCB1 , UGT1A1 , and UGT1A9 Genetic Polymorphisms on the Pharmacokinetics of Sitafloxacin Granules in Healthy Subjects Abstract Abstract Sitafloxacin, a new fluoroquinolone, has strong antibacterial activity. We evaluated the effects of sitafloxacin granules in single‐dose and multidose cohorts and the effec... |
PMC9495787 | core_pubmed_pmc | Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics | Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics Abstract The low water solubility of pharmacoactive molecules limits their pharmacological potential, but the solubility parameter cannot compromise, and so different approaches are employed to enhance their bioavailability. Pharma... |
PMC12179808 | core_pubmed_pmc | Therapeutic Potential of Lavandula stoechas Aqueous Extract in Managing Diabetes and Its Complications: Insights From Biochemical and In Silico Studies | Therapeutic Potential of Lavandula stoechas Aqueous Extract in Managing Diabetes and Its Complications: Insights From Biochemical and In Silico Studies Abstract ABSTRACT Diabetes mellitus is a chronic metabolic disorder characterized by persistent hyperglycemia, commonly associated with dyslipidemia, oxidative stress, ... |
PMC6896057 | core_pubmed_pmc | Dual PDK1/Aurora Kinase A Inhibitors Reduce Pancreatic Cancer Cell Proliferation and Colony Formation | Dual PDK1/Aurora Kinase A Inhibitors Reduce Pancreatic Cancer Cell Proliferation and Colony Formation Abstract Deregulation of different intracellular signaling pathways is a common feature in cancer. Numerous studies indicate that persistent activation of the phosphoinositide 3-kinase (PI3K) pathway is often observed ... |
PMC11707430 | core_pubmed_pmc | Novel antibiotics against Staphylococcus aureus without detectable resistance by targeting proton motive force and FtsH | Novel antibiotics against Staphylococcus aureus without detectable resistance by targeting proton motive force and FtsH Abstract Abstract The increased prevalence of methicillin‐resistant Staphylococcus aureus (MRSA) and its biofilms poses a great threat to human health. Especially, S. aureus ‐related osteomyelitis was... |
PMC9367195 | core_pubmed_pmc | Assessment of Strategies for Safe Drug Discontinuation and Transition of Denosumab Treatment in PMO—Insights From a Mechanistic PK/PD Model of Bone Turnover | Assessment of Strategies for Safe Drug Discontinuation and Transition of Denosumab Treatment in PMO—Insights From a Mechanistic PK/PD Model of Bone Turnover Abstract Denosumab (Dmab) treatment against postmenopausal osteoporosis (PMO) has proven very efficient in increasing bone mineral density (BMD) and reducing the r... |
PMC9321338 | core_pubmed_pmc | Genetic Polymorphisms Associated with Vincristine Pharmacokinetics and Vincristine-Induced Peripheral Neuropathy in Pediatric Oncology Patients | Genetic Polymorphisms Associated with Vincristine Pharmacokinetics and Vincristine-Induced Peripheral Neuropathy in Pediatric Oncology Patients Abstract Abstract Simple Summary Vincristine is a type of chemotherapy that is often used in the treatment of children with cancer. The main side effect of vincristine is nerve... |
PMC10290043 | core_pubmed_pmc | Pharmacokinetics, safety, and antitumor activity of talazoparib monotherapy in Chinese patients with advanced solid tumors | Pharmacokinetics, safety, and antitumor activity of talazoparib monotherapy in Chinese patients with advanced solid tumors Abstract Abstract Talazoparib, a poly(ADP-ribose) polymerase inhibitor, has demonstrated efficacy in the treatment of advanced breast and prostate cancers in Western populations. This open-label, p... |
PMC12735962 | core_pubmed_pmc | Beyond Dysphagia in Parkinson’s Disease: 3D Printing of Orally Disintegrating Tablets (ODTs) for Optimized Treatment | Beyond Dysphagia in Parkinson’s Disease: 3D Printing of Orally Disintegrating Tablets (ODTs) for Optimized Treatment Abstract Abstract Parkinson’s disease (PD) is frequently complicated by dysphagia, undermining timely and reliable oral dopaminergic medication. Levodopa’s short half-life and delayed gastric emptying in... |
PMC9545287 | core_pubmed_pmc | Phage therapy for severe bacterial infections: a narrative review | Phage therapy for severe bacterial infections: a narrative review Abstract Summary Bacteriophage (phage) therapy is re‐emerging a century after it began. Activity against antibiotic‐resistant pathogens and a lack of serious side effects make phage therapy an attractive treatment option in refractory bacterial infection... |
PMC8275101 | core_pubmed_pmc | Evaluation of Ceftazidime/Avibactam Administration in Enterobacteriaceae and Pseudomonas aeruginosa Bloodstream Infections by Monte Carlo Simulation | Evaluation of Ceftazidime/Avibactam Administration in Enterobacteriaceae and Pseudomonas aeruginosa Bloodstream Infections by Monte Carlo Simulation Abstract Purpose To evaluate the administration regimen of ceftazidime/avibactam (CZA) for bloodstream infections caused by Enterobacteriaceae and Pseudomonas aeruginosa .... |
PMC12536179 | core_pubmed_pmc | Field safety and efficacy study with a cannabidiol/cannabidiol acid-rich hemp paste in cats with osteoarthritic pain | Field safety and efficacy study with a cannabidiol/cannabidiol acid-rich hemp paste in cats with osteoarthritic pain Abstract Abstract Objectives Feline osteoarthritis (OA) is a common, degenerative joint condition that is an important cause of chronic pain in cats. Cannabinoids have shown potential in reducing pain an... |
PMC11719906 | core_pubmed_pmc | CANBERRA: A Phase II Randomized Clinical Trial to Test the Therapeutic Potential of Oral Vicasinabin in Diabetic Retinopathy | CANBERRA: A Phase II Randomized Clinical Trial to Test the Therapeutic Potential of Oral Vicasinabin in Diabetic Retinopathy Abstract Abstract Objective Nonproliferative diabetic retinopathy (NPDR) is a progressive disease that can lead to blindness. Current therapies for NPDR are invasive and not extensively used or a... |
PMC3556473 | core_pubmed_pmc | Absorption, metabolism and excretion of [ 14 C]pomalidomide in humans following oral administration | Absorption, metabolism and excretion of [ 14 C]pomalidomide in humans following oral administration Abstract Abstract Purpose To investigate the pharmacokinetics and disposition of [ 14 C]pomalidomide following a single oral dose to healthy male subjects. Methods Eight subjects were administered a single 2 mg oral susp... |
PMC3652810 | core_pubmed_pmc | Long-Term Effects of Chronic Intermittent Ethanol Exposure in Adolescent and Adult Rats: Radial-Arm Maze Performance and Operant Food Reinforced Responding | Long-Term Effects of Chronic Intermittent Ethanol Exposure in Adolescent and Adult Rats: Radial-Arm Maze Performance and Operant Food Reinforced Responding Abstract Abstract Background Adolescence is not only a critical period of late-stage neurological development in humans, but is also a period in which ethanol consu... |
PMC9424819 | core_pubmed_pmc | Evaluation of commonly used cardiovascular drugs in inhibiting vonoprazan metabolism in vitro and in vivo | Evaluation of commonly used cardiovascular drugs in inhibiting vonoprazan metabolism in vitro and in vivo Abstract Abstract As a novel acid-suppressing drug, vonoprazan shows the potential to replace traditional proton-pump inhibitors. With its widespread use, some adverse effects that require further study have emerge... |
PMC7042011 | core_pubmed_pmc | Relationship between body weight and postmenstrual age in a Korean pediatric population | Relationship between body weight and postmenstrual age in a Korean pediatric population Abstract Weight is a covariate representative of body size and is known to influence drug disposition. Recently, with increased use of allometric scaling, this variable has become more significant in accounting for variability in ph... |
PMC9785192 | core_pubmed_pmc | A Physiologically-Based Pharmacokinetic Model of Ruxolitinib and Posaconazole to Predict CYP3A4-Mediated Drug–Drug Interaction Frequently Observed in Graft versus Host Disease Patients | A Physiologically-Based Pharmacokinetic Model of Ruxolitinib and Posaconazole to Predict CYP3A4-Mediated Drug–Drug Interaction Frequently Observed in Graft versus Host Disease Patients Abstract Ruxolitinib (RUX) is approved for the treatment of steroid-refractory acute and chronic graft versus host disease (GvHD). It i... |
PMC11859316 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Study of Folic Acid-Modified Chitosan–Stearic Acid Nanomicelles Loaded with Tetrandrine for Rheumatoid Arthritis | Pharmacokinetic and Pharmacodynamic Study of Folic Acid-Modified Chitosan–Stearic Acid Nanomicelles Loaded with Tetrandrine for Rheumatoid Arthritis Abstract Background: Rheumatoid arthritis (RA) is a chronic autoimmune disease, and it is currently incurable. Tetrandrine (TET) has an obvious curative effect with therap... |
PMC5315703 | core_pubmed_pmc | A phase 1/2a, dose-escalation, safety, pharmacokinetic, and preliminary efficacy study of intraperitoneal administration of BC-819 (H19-DTA) in subjects with recurrent ovarian/peritoneal cancer | A phase 1/2a, dose-escalation, safety, pharmacokinetic, and preliminary efficacy study of intraperitoneal administration of BC-819 (H19-DTA) in subjects with recurrent ovarian/peritoneal cancer Abstract Abstract Background H19 is a paternally imprinted, oncofetal gene expressed in various embryonic tissues and in 85% o... |
PMC8504818 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of single‐ and multiple‐dose administration of islatravir (MK‐8591) in adults without HIV | Safety, tolerability, and pharmacokinetics of single‐ and multiple‐dose administration of islatravir (MK‐8591) in adults without HIV Abstract Abstract Islatravir (MK‐8591) is a nucleoside analogue in development for the treatment and prevention of HIV‐1. Two phase 1 trials were conducted during initial evaluation of is... |
PMC5874827 | core_pubmed_pmc | Development of a Region-Specific Physiologically Based Pharmacokinetic Brain Model to Assess Hippocampus and Frontal Cortex Pharmacokinetics | Development of a Region-Specific Physiologically Based Pharmacokinetic Brain Model to Assess Hippocampus and Frontal Cortex Pharmacokinetics Abstract Central nervous system drug discovery and development is hindered by the impermeable nature of the blood–brain barrier. Pharmacokinetic modeling can provide a novel appro... |
PMC8448541 | core_pubmed_pmc | Targeting the mTOR pathway using novel ATP-competitive inhibitors, Torin1, Torin2 and XL388, in the treatment of glioblastoma | Targeting the mTOR pathway using novel ATP-competitive inhibitors, Torin1, Torin2 and XL388, in the treatment of glioblastoma Abstract Abstract Mechanistic target of rapamycin (mTOR), which functions via two multiprotein complexes termed mTORC1 and mTORC2, is positioned in the canonical phosphoinositide 3-kinase-relate... |
PMC9295592 | core_pubmed_pmc | Characterizing SARS-CoV-2 viral clearance kinetics to improve the design of antiviral pharmacometric studies | Characterizing SARS-CoV-2 viral clearance kinetics to improve the design of antiviral pharmacometric studies Abstract A consensus methodology for the pharmacometric assessment of candidate SARS-CoV-2 antiviral drugs would be useful for comparing trial results and improving trial design. The time to viral clearance, ass... |
PMC10320479 | core_pubmed_pmc | Efficacy and Imaging-Enabled Pharmacodynamic Profiling of KRAS G12C Inhibitors in Xenograft and Genetically Engineered Mouse Models of Cancer | Efficacy and Imaging-Enabled Pharmacodynamic Profiling of KRAS G12C Inhibitors in Xenograft and Genetically Engineered Mouse Models of Cancer Abstract Abstract KRAS is one of the most commonly mutated oncogenes in lung, colorectal, and pancreatic cancers. Recent clinical trials directly targeting KRAS G12C presented en... |
PMC8206303 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Rivipansel in Healthy Subjects and Subjects with Sickle Cell Disease | Population Pharmacokinetic Analysis of Rivipansel in Healthy Subjects and Subjects with Sickle Cell Disease Abstract Background Sickle cell disease is an inherited blood disorder with reduced blood-carrying capacity. It is associated with a tendency to form microclots in blood vessels, leading to painful episodes known... |
PMC11333640 | core_pubmed_pmc | Pharmacokinetics, Safety, Tolerability, and Immunogenicity of BP02 (Trastuzumab Biosimilar) Compared to EU- and US-Approved Trastuzumab in Healthy Adult Male Volunteers: A Phase 1, Randomized, Double-Blind Study | Pharmacokinetics, Safety, Tolerability, and Immunogenicity of BP02 (Trastuzumab Biosimilar) Compared to EU- and US-Approved Trastuzumab in Healthy Adult Male Volunteers: A Phase 1, Randomized, Double-Blind Study Abstract Introduction This study evaluated the pharmacokinetic (PK) equivalence between BP02 (a proposed tra... |
PMC7662788 | core_pubmed_pmc | The Basal Pharmacology of Palmitoylethanolamide | The Basal Pharmacology of Palmitoylethanolamide Abstract Abstract Palmitoylethanolamide (PEA, N -hexadecanoylethanolamide) is an endogenous compound belonging to the family of N -acylethanolamines. PEA has anti-inflammatory and analgesic properties and is very well tolerated in humans. In the present article, the basal... |
PMC4485162 | core_pubmed_pmc | The application of global sensitivity analysis in the development of a physiologically based pharmacokinetic model for m -xylene and ethanol co-exposure in humans | The application of global sensitivity analysis in the development of a physiologically based pharmacokinetic model for m -xylene and ethanol co-exposure in humans Abstract Abstract Global sensitivity analysis (SA) was used during the development phase of a binary chemical physiologically based pharmacokinetic (PBPK) mo... |
PMC6078186 | core_pubmed_pmc | Comparison of biosimilar filgrastim with a reference product: pharmacokinetics, pharmacodynamics, and safety profiles in healthy volunteers | Comparison of biosimilar filgrastim with a reference product: pharmacokinetics, pharmacodynamics, and safety profiles in healthy volunteers Abstract Purpose Filgrastim, a granulocyte-colony stimulating factor, is used to treat patients with neutropenia, including neutropenic fever. Leucostim ® is a recombinant filgrast... |
PMC5567437 | core_pubmed_pmc | A randomised, controlled, two-Centre open-label study in healthy Japanese subjects to evaluate the effect on biomarkers of exposure of switching from a conventional cigarette to a tobacco heating product | A randomised, controlled, two-Centre open-label study in healthy Japanese subjects to evaluate the effect on biomarkers of exposure of switching from a conventional cigarette to a tobacco heating product Abstract Abstract Background Smoking is a leading cause of numerous human disorders including lung cancer, chronic o... |
PMC9146689 | core_pubmed_pmc | Targeting Peptide, Fluorescent Reagent Modified Magnetic Liposomes Coated with Rapamycin Target Early Atherosclerotic Plaque and Therapy | Targeting Peptide, Fluorescent Reagent Modified Magnetic Liposomes Coated with Rapamycin Target Early Atherosclerotic Plaque and Therapy Abstract Atherosclerosis is the leading cause of global morbidity and mortality. Its therapy requires research in several areas, such as diagnosis of early arteriosclerosis, improveme... |
PMC12653448 | core_pubmed_pmc | Effects of Extracorporeal Membrane Oxygenation Circuits on Drug Sequestration: A Review of Ex Vivo Experiments | Effects of Extracorporeal Membrane Oxygenation Circuits on Drug Sequestration: A Review of Ex Vivo Experiments Abstract Abstract Background: Extracorporeal membrane oxygenation (ECMO) can affect the disposition of drugs, notably by sequestering them in a circuit. This review aimed to provide a comprehensive summary of ... |
PMC12048447 | core_pubmed_pmc | PANTAX: a phase Ib clinical trial of the efflux pump inhibitor SCO-101 in combination with gemcitabine and nab -paclitaxel in non-resectable or metastatic pancreatic cancer | PANTAX: a phase Ib clinical trial of the efflux pump inhibitor SCO-101 in combination with gemcitabine and nab -paclitaxel in non-resectable or metastatic pancreatic cancer Abstract Abstract De novo or acquired resistance to chemotherapy is ubiquitous in pancreatic ductal adenocarcinoma (PDAC). SCO-101 is an oral compo... |
PMC3869895 | core_pubmed_pmc | A phase I study of the oral gamma secretase inhibitor R04929097 in combination with gemcitabine in patients with advanced solid tumors (PHL-078/CTEP 8575) | A phase I study of the oral gamma secretase inhibitor R04929097 in combination with gemcitabine in patients with advanced solid tumors (PHL-078/CTEP 8575) Abstract Summary Purpose To establish the recommended phase II dose of the oral γ-secretase inhibitor RO4929097 (RO) in combination with gemcitabine; secondary objec... |
PMC9177500 | core_pubmed_pmc | Population pharmacogenomics: an update on ethnogeographic differences and opportunities for precision public health | Population pharmacogenomics: an update on ethnogeographic differences and opportunities for precision public health Abstract Both safety and efficacy of medical treatment can vary depending on the ethnogeographic background of the patient. One of the reasons underlying this variability is differences in pharmacogenetic... |
PMC5446775 | core_pubmed_pmc | Interactions of 172 plant extracts with human organic anion transporter 1 (SLC22A6) and 3 (SLC22A8): a study on herb-drug interactions | Interactions of 172 plant extracts with human organic anion transporter 1 (SLC22A6) and 3 (SLC22A8): a study on herb-drug interactions Abstract Abstract Background Herb-drug interactions (HDIs) resulting from concomitant use of herbal products with clinical drugs may cause adverse reactions. Organic anion transporter 1... |
PMC10349190 | core_pubmed_pmc | Model‐informed pediatric dose selection of marzeptacog alfa (activated): An exposure matching strategy | Model‐informed pediatric dose selection of marzeptacog alfa (activated): An exposure matching strategy Abstract Abstract Marzeptacog alfa (activated) (MarzAA) is an activated recombinant human rFVII variant intended for subcutaneous (s.c.) administration to treat or prevent bleeding in individuals with hemophilia A (HA... |
PMC12468443 | core_pubmed_pmc | Chemical Composition of Clove and Fennel Seed Essential Oils and a Comparison of Their In Silico and In Vitro Antibacterial Activity with That of Their Main Compounds | Chemical Composition of Clove and Fennel Seed Essential Oils and a Comparison of Their In Silico and In Vitro Antibacterial Activity with That of Their Main Compounds Abstract This study aimed to assess the chemical composition and antibacterial potential of essential oils (EOs) from two plants: clove buds ( Syzygium a... |
PMC8999126 | core_pubmed_pmc | Influence of Umbelliferone on the Anticonvulsant and Neuroprotective Activity of Selected Antiepileptic Drugs: An In Vivo and In Vitro Study | Influence of Umbelliferone on the Anticonvulsant and Neuroprotective Activity of Selected Antiepileptic Drugs: An In Vivo and In Vitro Study Abstract Abstract Umbelliferone (7-hydroxycoumarin; UMB) is a coumarin with many biological properties, including antiepileptic activity. This study evaluated the effect of UMB on... |
PMC12062192 | core_pubmed_pmc | Therapeutics for Nipah virus disease: a systematic review to support prioritisation of drug candidates for clinical trials | Therapeutics for Nipah virus disease: a systematic review to support prioritisation of drug candidates for clinical trials Abstract Summary Nipah virus disease is a bat-borne zoonosis with person-to-person transmission, a case-fatality rate of 38–75%, and well recognised potential to cause a pandemic. The first reporte... |
PMC12001261 | core_pubmed_pmc | Model‐Informed Drug Development of a Sustained Release Formulation of Flucytosine in the Treatment of Cryptococcal Meningitis: A Case Study Using Physiologically Based Pharmacokinetic Modeling | Model‐Informed Drug Development of a Sustained Release Formulation of Flucytosine in the Treatment of Cryptococcal Meningitis: A Case Study Using Physiologically Based Pharmacokinetic Modeling Abstract ABSTRACT This paper presents a case study demonstrating the application of model‐informed drug development (MIDD) and ... |
PMC11816618 | core_pubmed_pmc | Pharmacokinetic profile and in vivo anticancer efficacy of anagrelide administered subcutaneously in rodents | Pharmacokinetic profile and in vivo anticancer efficacy of anagrelide administered subcutaneously in rodents Abstract Abstract Anagrelide (ANA) is a phosphodiesterase 3A (PDE3A) inhibitor, commonly prescribed for essential thrombocythemia. It also functions as a molecular glue, inducing complex formation between PDE3A ... |
PMC9401512 | core_pubmed_pmc | A Phase I Study of LSZ102, an Oral Selective Estrogen Receptor Degrader, with or without Ribociclib or Alpelisib, in Patients with Estrogen Receptor–Positive Breast Cancer | A Phase I Study of LSZ102, an Oral Selective Estrogen Receptor Degrader, with or without Ribociclib or Alpelisib, in Patients with Estrogen Receptor–Positive Breast Cancer Abstract Abstract Purpose: Data are sparse for oral selective estrogen receptor (ER) degraders (SERD) in cancer treatment. The investigational oral ... |
PMC6851049 | core_pubmed_pmc | STS-NLSP: A Network-Based Label Space Partition Method for Predicting the Specificity of Membrane Transporter Substrates Using a Hybrid Feature of Structural and Semantic Similarity | STS-NLSP: A Network-Based Label Space Partition Method for Predicting the Specificity of Membrane Transporter Substrates Using a Hybrid Feature of Structural and Semantic Similarity Abstract Membrane transport proteins play crucial roles in the pharmacokinetics of substrate drugs, the drug resistance in cancer and are ... |
PMC6280233 | core_pubmed_pmc | Pharmacokinetics and Tissue Distribution Study of Pinosylvin in Rats by Ultra-High-Performance Liquid Chromatography Coupled with Linear Trap Quadrupole Orbitrap Mass Spectrometry | Pharmacokinetics and Tissue Distribution Study of Pinosylvin in Rats by Ultra-High-Performance Liquid Chromatography Coupled with Linear Trap Quadrupole Orbitrap Mass Spectrometry Abstract Abstract Pinosylvin is a potential anti-inflammatory and antioxidant compound and the major effective medicinal ingredient in the r... |
PMC11453026 | core_pubmed_pmc | A narrative review on antimicrobial dosing in adult critically ill patients on extracorporeal membrane oxygenation | A narrative review on antimicrobial dosing in adult critically ill patients on extracorporeal membrane oxygenation Abstract Abstract The optimal dosing strategy of antimicrobial agents in critically ill patients receiving extracorporeal membrane oxygenation (ECMO) is unknown. We conducted comprehensive review of existi... |
PMC4598224 | core_pubmed_pmc | Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe | Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe Abstract Abstract Background The objective of this study was to compare the physicochemical characteristics, solubility, dissolution, and oral bioavailability of an ezetimib... |
PMC6100060 | core_pubmed_pmc | Echinacoside, an Inestimable Natural Product in Treatment of Neurological and other Disorders | Echinacoside, an Inestimable Natural Product in Treatment of Neurological and other Disorders Abstract Abstract Echinacoside (ECH), a natural phenylethanoid glycoside, was first isolated from Echinacea angustifolia DC. (Compositae) sixty years ago. It was found to possess numerous pharmacologically beneficial activitie... |
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