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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...