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PMC12714801
core_pubmed_pmc
Rumex Species: Phytochemistry, Pharmacology and Nutritional Potential for Food and Health Applications
Rumex Species: Phytochemistry, Pharmacology and Nutritional Potential for Food and Health Applications Abstract ABSTRACT The genus Rumex (Polygonaceae), comprising about 193 species, is widely distributed across temperate and subtropical regions of Europe, Asia, Africa, and North America, and has long been used in trad...
PMC9859632
core_pubmed_pmc
Pharmacokinetics of cannabidiol following single oral and oral transmucosal administration in dogs
Pharmacokinetics of cannabidiol following single oral and oral transmucosal administration in dogs Abstract Introduction In the last few years, different formulations containing cannabidiol (CBD) were tested with regard to its efficacy on chronic pain, refractory epilepsy, anxiety, aggressive behavior and atopic dermat...
PMC8761109
core_pubmed_pmc
Comparative Bioavailability Study of a New Vitamin D3 Orodispersible Film Versus a Marketed Oral Solution in Healthy Volunteers
Comparative Bioavailability Study of a New Vitamin D3 Orodispersible Film Versus a Marketed Oral Solution in Healthy Volunteers Abstract Abstract Background and Objective An orally disintegrating film (ODF) formulation of vitamin D3 that dissolves rapidly in the mouth without drinking or chewing may be a worthwhile alt...
PMC8780089
core_pubmed_pmc
A Pharmacokinetic Study of Mix-160 by LC-MS/MS: Oral Bioavailability of a Dosage Form of Citroflavonoids Mixture
A Pharmacokinetic Study of Mix-160 by LC-MS/MS: Oral Bioavailability of a Dosage Form of Citroflavonoids Mixture Abstract This study was performed to evaluate and compare the pharmacokinetic parameters between two dosage formulations of hesperidin and naringenin: mixture and tablet. Our objective was to determine that ...
PMC7063976
core_pubmed_pmc
Impact of Inaccurate Documentation of Sampling and Infusion Time in Model-Informed Precision Dosing
Impact of Inaccurate Documentation of Sampling and Infusion Time in Model-Informed Precision Dosing Abstract Abstract Background Routine clinical TDM data is often used to develop population pharmacokinetic (PK) models, which are applied in turn for model-informed precision dosing. The impact of uncertainty in document...
PMC4255731
core_pubmed_pmc
Peptide-Coated Liposomal Fasudil Enhances Site Specific Vasodilation in Pulmonary Arterial Hypertension
Peptide-Coated Liposomal Fasudil Enhances Site Specific Vasodilation in Pulmonary Arterial Hypertension Abstract Abstract This study sought to develop a liposomal delivery system of fasudil—an investigational drug for the treatment of pulmonary arterial hypertension (PAH)—that will preferentially accumulate in the PAH ...
PMC9890216
core_pubmed_pmc
Oral ciprofloxacin activity against ceftriaxone-resistant Escherichia coli in an in vitro bladder infection model
Oral ciprofloxacin activity against ceftriaxone-resistant Escherichia coli in an in vitro bladder infection model Abstract Abstract Objectives Pharmacodynamic profiling of oral ciprofloxacin dosing for urinary tract infections caused by ceftriaxone-resistant Escherichia coli isolates with ciprofloxacin MIC ≥ 0.25 mg/L....
PMC12756401
core_pubmed_pmc
Effect of itraconazole on pharmacokinetics of ZX-7101A tablets in healthy Chinese subjects
Effect of itraconazole on pharmacokinetics of ZX-7101A tablets in healthy Chinese subjects Abstract Aims A single-center, open label trial was conducted to evaluate the effects of itraconazole on the pharmacokinetics of ZX-7101A tablets in healthy Chinese adults. Methods Subjects took a single dose of 40 mg ZX-7101A ta...
PMC12597587
core_pubmed_pmc
A primary human Gut/Liver microphysiological system to estimate human oral bioavailability
A primary human Gut/Liver microphysiological system to estimate human oral bioavailability Abstract Oral bioavailability is a crucial pharmacokinetic (PK) parameter optimized by drug developers working on new therapeutic compounds. The goal is to obtain adequate systemic exposure and to establish safe and effective the...
PMC11982744
core_pubmed_pmc
Pharmacokinetic simulations for remdesivir and its metabolites in healthy subjects and patients with renal impairment
Pharmacokinetic simulations for remdesivir and its metabolites in healthy subjects and patients with renal impairment Abstract Abstract Introduction Remdesivir (RDV) is used for treating COVID-19 patients. This study aims to utilize an in silico pharmacokinetics model to simulate the pharmacokinetics of RDV, its interm...
PMC8969425
core_pubmed_pmc
External Evaluation of Risperidone Population Pharmacokinetic Models Using Opportunistic Pediatric Data
External Evaluation of Risperidone Population Pharmacokinetic Models Using Opportunistic Pediatric Data Abstract Abstract Risperidone is approved to treat schizophrenia in adolescents and autistic disorder and bipolar mania in children and adolescents. It is also used off-label in younger children for various psychiatr...
PMC6918283
core_pubmed_pmc
Oral Pharmacokinetics of a Chitosan-Based Nano- Drug Delivery System of Interferon Alpha
Oral Pharmacokinetics of a Chitosan-Based Nano- Drug Delivery System of Interferon Alpha Abstract Abstract Interferon alpha (IFNα) is a protein drug used to treat viral infections and cancer diseases. Due to its poor stability in the gastrointestinal tract, only parenteral administration ensures bioavailability, which ...
PMC11280059
core_pubmed_pmc
A Comprehensive Physiologically Based Pharmacokinetic Model for Predicting Vildagliptin Pharmacokinetics: Insights into Dosing in Renal Impairment
A Comprehensive Physiologically Based Pharmacokinetic Model for Predicting Vildagliptin Pharmacokinetics: Insights into Dosing in Renal Impairment Abstract Abstract Physiologically based pharmacokinetic (PBPK) modeling is of great importance in the field of medicine. This study aims to construct a PBPK model, which can...
PMC5949937
core_pubmed_pmc
Therapeutic drug monitoring of vedolizumab in inflammatory bowel disease: current data and future directions
Therapeutic drug monitoring of vedolizumab in inflammatory bowel disease: current data and future directions Abstract The introduction of vedolizumab, a lymphocyte adhesion inhibitor, has expanded the relatively limited therapeutic armamentarium available for Crohn’s disease and ulcerative colitis. Despite its effectiv...
PMC9428196
core_pubmed_pmc
Pharmacodynamic profiling of commonly prescribed antimicrobial drugs against Escherichia coli isolates from urinary tract
Pharmacodynamic profiling of commonly prescribed antimicrobial drugs against Escherichia coli isolates from urinary tract Abstract Since antimicrobial resistance among uropathogens against current first line agents has affected the management of severe urinary tract infection, we determined the likelihood that antibiot...
PMC5069309
core_pubmed_pmc
Pharmacokinetic Properties of Liraglutide as Adjunct to Insulin in Subjects with Type 1 Diabetes Mellitus
Pharmacokinetic Properties of Liraglutide as Adjunct to Insulin in Subjects with Type 1 Diabetes Mellitus Abstract Background The pharmacokinetic properties of liraglutide, a glucagon-like peptide-1 receptor agonist approved for the treatment of type 2 diabetes mellitus (T2D), have been established in healthy individua...
PMC7810645
core_pubmed_pmc
Phase I Study of Rucaparib in Combination with Bevacizumab in Ovarian Cancer Patients: Maximum Tolerated Dose and Pharmacokinetic Profile
Phase I Study of Rucaparib in Combination with Bevacizumab in Ovarian Cancer Patients: Maximum Tolerated Dose and Pharmacokinetic Profile Abstract Abstract Background Targeted agents, such as antiangiogenic drugs (e.g., bevacizumab) and poly(ADP-ribose) polymerase inhibitors (e.g., rucaparib), have been shown to improv...
PMC10140819
core_pubmed_pmc
Predicting Hydroxychloroquine Clearance in Healthy and Diseased Populations Using a Physiologically Based Pharmacokinetic Approach
Predicting Hydroxychloroquine Clearance in Healthy and Diseased Populations Using a Physiologically Based Pharmacokinetic Approach Abstract Hydroxychloroquine (HCQ), a congener of chloroquine, is widely used in prophylaxis and the treatment of malaria, and also as a cure for rheumatoid arthritis, systemic lupus erythem...
PMC11271717
core_pubmed_pmc
Remimazolam for sedation in gastrointestinal endoscopy: A comprehensive review
Remimazolam for sedation in gastrointestinal endoscopy: A comprehensive review Abstract Abstract Worldwide, a majority of routine endoscopic procedures are performed under some form of sedation to maximize patient comfort. Propofol, benzodiazepines and opioids continue to be widely used. However, in recent years, Remim...
PMC9795984
core_pubmed_pmc
Population Pharmacokinetics of Heptanoate in Healthy Subjects and Patients With Long‐Chain Fatty Acid Oxidation Disorders Treated With Triheptanoin
Population Pharmacokinetics of Heptanoate in Healthy Subjects and Patients With Long‐Chain Fatty Acid Oxidation Disorders Treated With Triheptanoin Abstract Abstract Triheptanoin is an odd‐carbon, medium‐chain triglyceride consisting of three fatty acids with seven carbons each on a glycerol backbone, indicated for the...
PMC8504844
core_pubmed_pmc
Safety, tolerability, pharmacokinetics, and pharmacodynamics of HBM9161, a novel FcRn inhibitor, in a phase I study for healthy Chinese volunteers
Safety, tolerability, pharmacokinetics, and pharmacodynamics of HBM9161, a novel FcRn inhibitor, in a phase I study for healthy Chinese volunteers Abstract Abstract Blockade of the binding between neonatal Fc receptor and IgG‐Fc reduces circulating IgG, and thus emerges as a potential therapy for IgG‐mediated autoimmun...
PMC4000408
core_pubmed_pmc
No clinically significant drug interactions between lenalidomide and P-glycoprotein substrates and inhibitors: results from controlled phase I studies in healthy volunteers
No clinically significant drug interactions between lenalidomide and P-glycoprotein substrates and inhibitors: results from controlled phase I studies in healthy volunteers Abstract Purpose Lenalidomide, a weak substrate of P-glycoprotein (P-gp) in vitro, is an oral anticancer drug eliminated predominantly via renal ex...
PMC10963524
core_pubmed_pmc
Inferring Parameters of Pyramidal Neuron Excitability in Mouse Models of Alzheimer’s Disease Using Biophysical Modeling and Deep Learning
Inferring Parameters of Pyramidal Neuron Excitability in Mouse Models of Alzheimer’s Disease Using Biophysical Modeling and Deep Learning Abstract Alzheimer’s disease (AD) is believed to occur when abnormal amounts of the proteins amyloid beta and tau aggregate in the brain, resulting in a progressive loss of neuronal ...
PMC11584741
core_pubmed_pmc
Integrative metabolomics and proteomics reveal the effect and mechanism of Zi Qi decoction on alleviating liver fibrosis
Integrative metabolomics and proteomics reveal the effect and mechanism of Zi Qi decoction on alleviating liver fibrosis Abstract Abstract Liver fibrosis is a common progressive liver disease that can cause liver dysfunction and lead to serious complications. Zi Qi decoction (ZQ) is a traditional formulation that exert...
PMC9740625
core_pubmed_pmc
Pharmacological Mechanism of NRICM101 for COVID-19 Treatments by Combined Network Pharmacology and Pharmacodynamics
Pharmacological Mechanism of NRICM101 for COVID-19 Treatments by Combined Network Pharmacology and Pharmacodynamics Abstract Abstract Symptom treatments for Coronavirus disease 2019 (COVID-19) infection and Long COVID are one of the most critical issues of the pandemic era. In light of the lack of standardized medicati...
PMC4990024
core_pubmed_pmc
Preclinical Pharmacokinetics, Tissue Distribution, and Plasma Protein Binding of Sodium (±)-5-Bromo-2-(α-Hydroxypentyl) Benzoate (BZP), an Innovative Potent Anti-ischemic Stroke Agent
Preclinical Pharmacokinetics, Tissue Distribution, and Plasma Protein Binding of Sodium (±)-5-Bromo-2-(α-Hydroxypentyl) Benzoate (BZP), an Innovative Potent Anti-ischemic Stroke Agent Abstract Abstract Sodium (±)-5-bromo-2-(α-hydroxypentyl) benzoate (BZP) is a potential cardiovascular drug and exerts potent neuroprotec...
PMC9885713
core_pubmed_pmc
Population pharmacokinetic analysis of TQ-B3203 following intravenous administration of TQ-B3203 liposome injection in Chinese patients with advanced solid tumors
Population pharmacokinetic analysis of TQ-B3203 following intravenous administration of TQ-B3203 liposome injection in Chinese patients with advanced solid tumors Abstract Background: TQ-B3203 is a novel topoisomerase I inhibitor currently in development for the treatment of advanced solid tumors. Great differences in ...
PMC10539271
core_pubmed_pmc
Safety, Pharmacokinetics and Preliminary Efficacy of IL4-Rα Monoclonal Antibody AK120 in Both Healthy and Atopic Dermatitis Subjects: A Phase I, Randomized, Two-Part, Double-Blind, Placebo-Controlled, Dose-Escalation, First-In-Human Clinical Study
Safety, Pharmacokinetics and Preliminary Efficacy of IL4-Rα Monoclonal Antibody AK120 in Both Healthy and Atopic Dermatitis Subjects: A Phase I, Randomized, Two-Part, Double-Blind, Placebo-Controlled, Dose-Escalation, First-In-Human Clinical Study Abstract Introduction Interleukin-4 (IL-4) and interleukin-13 (IL-13) ar...
PMC11768319
core_pubmed_pmc
Examining Prenylated Xanthones as Potential Inhibitors Against Ketohexokinase C Isoform for the Treatment of Fructose-Driven Metabolic Disorders: An Integrated Computational Approach
Examining Prenylated Xanthones as Potential Inhibitors Against Ketohexokinase C Isoform for the Treatment of Fructose-Driven Metabolic Disorders: An Integrated Computational Approach Abstract Background/Objectives: Fructose-driven metabolic disorders, such as obesity, non-alcoholic fatty liver disease (NAFLD), dyslipid...
PMC12567155
core_pubmed_pmc
LC-MS/MS Method Development and Validation for Clinical Pharmacokinetics and Therapeutic Drug Monitoring of Potassium-Competitive Acid Blocker Vonoprazan-Based Triple Therapy for H. pylori in Human Plasma
LC-MS/MS Method Development and Validation for Clinical Pharmacokinetics and Therapeutic Drug Monitoring of Potassium-Competitive Acid Blocker Vonoprazan-Based Triple Therapy for H. pylori in Human Plasma Abstract Abstract Background: A novel triple therapy regimen for Helicobacter pylori eradication, recently approved...
PMC12041214
core_pubmed_pmc
Acute hypobaric hypoxia attenuates the anti-fatigue effects of pitolisant by downregulating the expression of organic cation transporter 1 and P-glycoprotein
Acute hypobaric hypoxia attenuates the anti-fatigue effects of pitolisant by downregulating the expression of organic cation transporter 1 and P-glycoprotein Abstract Abstract Objective This study investigates the effects of acute hypobaric hypoxia (HH) on the anti-fatigue properties of pitolisant and explores the unde...
PMC5538301
core_pubmed_pmc
Pharmacology of Thiopurine Therapy in Inflammatory Bowel Disease and Complete Blood Cell Count Outcomes: A 5-Year Database Study
Pharmacology of Thiopurine Therapy in Inflammatory Bowel Disease and Complete Blood Cell Count Outcomes: A 5-Year Database Study Abstract Supplemental Digital Content is Available in the Text. Background: Thiopurines are the prerequisite for immunomodulation in inflammatory bowel disease (IBD) therapy. When administere...
PMC10962676
core_pubmed_pmc
An integrated strategy to evaluate active substances of Astragali Radix-Carthami Flos combination on the treatment of cerebral ischemia reperfusion injury based on TQSM polypharmacokinetics and pharmacodynamics
An integrated strategy to evaluate active substances of Astragali Radix-Carthami Flos combination on the treatment of cerebral ischemia reperfusion injury based on TQSM polypharmacokinetics and pharmacodynamics Abstract Abstract As a classic herb pair, Astragali Radix-Carthami Flos (AR-CF) has revealed good biological ...
PMC12299796
core_pubmed_pmc
Pharmacokinetics of Molnupiravir in Cats with Naturally Occurring Feline Infectious Peritonitis
Pharmacokinetics of Molnupiravir in Cats with Naturally Occurring Feline Infectious Peritonitis Abstract Antiviral drugs like EIDD-2801 (molnupiravir; MPV) have been successfully used in the treatment of feline infectious peritonitis (FIP). The previous study of the pharmacokinetics of MPV in healthy cats showed promis...
PMC6709996
core_pubmed_pmc
Suppression of the photoparoxysmal response in photosensitive epilepsy with cenobamate (YKP3089)
Suppression of the photoparoxysmal response in photosensitive epilepsy with cenobamate (YKP3089) Abstract Objective To evaluate the effect of cenobamate in patients with photoparoxysmal-EEG response (PPR) to intermittent photic stimulation (IPS) as proof of principle of efficacy in patients with epilepsy. Methods In th...
PMC10226698
core_pubmed_pmc
Investigation renin inhibitor activity from flavonoids derivates by in silico study
Investigation renin inhibitor activity from flavonoids derivates by in silico study Abstract Flavonoids have various pharmacological activities, such as antihypertensive, anticancer, and and antidiabetic effects. Several studies have shown that luteolin, quercetin, kaempferol, myricetin, naringenin, hesperetin, and epi...
PMC9614231
core_pubmed_pmc
Bioequivalence of two tablet formulations of cefpodoxime proxetil in beagle dogs
Bioequivalence of two tablet formulations of cefpodoxime proxetil in beagle dogs Abstract Abstract The pharmacokinetic profiles and bioequivalence of two cefpodoxime proxetil tablets were investigated in Beagle dogs. A single-dose, four-way complete replication and crossover design was used in the present study. A tota...
PMC12266627
core_pubmed_pmc
Milk and plasma pharmacokinetics of single‐dose ubrogepant in healthy lactating women
Milk and plasma pharmacokinetics of single‐dose ubrogepant in healthy lactating women Abstract Abstract Objective The objectives of this study were to evaluate the safety, plasma and milk pharmacokinetics, excretion in breast milk, and the relative infant dose of ubrogepant following a single oral dose. Background Ubro...
PMC8488464
core_pubmed_pmc
Efficacy and safety of moxidectin and albendazole compared to ivermectin and albendazole co-administration in adolescents infected with Trichuris trichiura : a randomized controlled trial protocol
Efficacy and safety of moxidectin and albendazole compared to ivermectin and albendazole co-administration in adolescents infected with Trichuris trichiura : a randomized controlled trial protocol Abstract Background: Infections with soil-transmitted helminths (STHs) predominantly affect impoverished populations in tro...
PMC4181826
core_pubmed_pmc
Chimeric antibodies with extended half-life in ferrets
Chimeric antibodies with extended half-life in ferrets Abstract Background Ferrets have long been used as a disease model for the study of influenza vaccines, but a more recent use has been for the study of human monoclonal antibodies directed against influenza viruses. Published data suggest that human antibodies are ...
PMC4435638
core_pubmed_pmc
Phase I trial of volasertib, a Polo-like kinase inhibitor, plus platinum agents in solid tumors: safety, pharmacokinetics and activity
Phase I trial of volasertib, a Polo-like kinase inhibitor, plus platinum agents in solid tumors: safety, pharmacokinetics and activity Abstract Summary Background This trial evaluated the maximum tolerated dose (MTD), safety, pharmacokinetics, and activity of volasertib, a selective Polo-like kinase 1 inhibitor that in...
PMC11895370
core_pubmed_pmc
Comparison of PDE-5 inhibitors used in erectile dysfunction with some candidate molecules: A study involving molecular docking, ADMET, DFT, biological target, and activity
Comparison of PDE-5 inhibitors used in erectile dysfunction with some candidate molecules: A study involving molecular docking, ADMET, DFT, biological target, and activity Abstract Erectile dysfunction (ED) is a urological condition defined as the inability of a man to achieve or maintain an erection. This condition ne...
PMC3995273
core_pubmed_pmc
Electronic cigarettes and nicotine clinical pharmacology
Electronic cigarettes and nicotine clinical pharmacology Abstract Objective To review the available literature evaluating electronic cigarette (e-cigarette) nicotine clinical pharmacology in order to understand the potential impact of e-cigarettes on individual users, nicotine dependence and public health. Methods Lite...
PMC8541972
core_pubmed_pmc
Phase I study of daily and weekly regimens of the orally administered MDM2 antagonist idasanutlin in patients with advanced tumors
Phase I study of daily and weekly regimens of the orally administered MDM2 antagonist idasanutlin in patients with advanced tumors Abstract Abstract Summary Aim The oral MDM2 antagonist idasanutlin inhibits the p53-MDM2 interaction, enabling p53 activation, tumor growth inhibition, and increased survival in xenograft m...
PMC8919964
core_pubmed_pmc
PET Molecular Imaging in Drug Development: The Imaging and Chemistry Perspective
PET Molecular Imaging in Drug Development: The Imaging and Chemistry Perspective Abstract Positron emission tomography with selective radioligands advances the drug discovery and development process by revealing information about target engagement, proof of mechanism, pharmacokinetic and pharmacodynamic profiles. Posit...
PMC8331077
core_pubmed_pmc
Ocrelizumab for the Treatment of Multiple Sclerosis: Safety, Efficacy, and Pharmacology
Ocrelizumab for the Treatment of Multiple Sclerosis: Safety, Efficacy, and Pharmacology Abstract Abstract The success of selective B-cells depleting therapies, as the anti-CD20 antibodies, in patients with multiple sclerosis (MS) has confirmed that B-cells are critical in the immune pathogenesis of the disease. Ocreliz...
PMC9305210
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics and safety assessment of multiple doses of soticlestat in healthy volunteers
Pharmacokinetics, pharmacodynamics and safety assessment of multiple doses of soticlestat in healthy volunteers Abstract Aims Soticlestat, a first‐in‐class inhibitor of cholesterol 24‐hydroxylase (also known as cytochrome P450 46A1), is currently in development for the treatment of developmental and epileptic encephalo...
PMC3171651
core_pubmed_pmc
Influence of mild and moderate hepatic impairment on axitinib pharmacokinetics
Influence of mild and moderate hepatic impairment on axitinib pharmacokinetics Abstract Summary Objective: To evaluate the effects of hepatic impairment on the pharmacokinetics and safety of a single, oral axitinib dose in subjects with mild or moderate hepatic impairment. Methods: In this phase I, open-label, parallel...
PMC11813737
core_pubmed_pmc
Are all measures of liver K p u u a function of F H , as determined following oral dosing, or have we made a critical error in defining hepatic drug clearance?
Are all measures of liver K p u u a function of F H , as determined following oral dosing, or have we made a critical error in defining hepatic drug clearance? Abstract Abstract Here we present, utilizing universally accepted relationships for hepatic clearance at steady state, that for all models of hepatic eliminatio...
PMC12560410
core_pubmed_pmc
Multi spectroscopic investigations with molecular docking and molecular dynamics simulation of the binding mechanism of molnupiravir to bovine serum albumin
Multi spectroscopic investigations with molecular docking and molecular dynamics simulation of the binding mechanism of molnupiravir to bovine serum albumin Abstract Abstract Molnupiravir (MOL) is a recently developed oral antiviral drug. MOL has been clinically evaluated for its efficacy against COVID-19. In this work...
PMC8604232
core_pubmed_pmc
REGN1908‐1909 monoclonal antibodies block Fel d 1 in cat allergic subjects: Translational pharmacokinetics and pharmacodynamics
REGN1908‐1909 monoclonal antibodies block Fel d 1 in cat allergic subjects: Translational pharmacokinetics and pharmacodynamics Abstract Abstract REGN1908‐1909, a 1:1 cocktail of two fully human IgG 4 monoclonal antibodies (mAbs), REGN1908 and REGN1909, is being evaluated for treatment of cat allergy. Both REGN1908 and...
PMC9136018
core_pubmed_pmc
SLC4A4 , FRAS1 , and SULT1A1 Genetic Variations Associated With Dabigatran Metabolism in a Healthy Chinese Population
SLC4A4 , FRAS1 , and SULT1A1 Genetic Variations Associated With Dabigatran Metabolism in a Healthy Chinese Population Abstract Abstract Background: The purpose of this study was to identify genetic variations associated with the metabolism of dabigatran in healthy Chinese subjects, with particular focus given to pharma...
PMC9917191
core_pubmed_pmc
In Vitro/In Vivo Translation of Synergistic Combination of MDM2 and MEK Inhibitors in Melanoma Using PBPK/PD Modelling: Part III
In Vitro/In Vivo Translation of Synergistic Combination of MDM2 and MEK Inhibitors in Melanoma Using PBPK/PD Modelling: Part III Abstract The development of in vitro/in vivo translational methods and a clinical trial framework for synergistically acting drug combinations are needed to identify optimal therapeutic condi...
PMC2920546
core_pubmed_pmc
Preclinical Pharmacology of BA-TPQ, a Novel Synthetic Iminoquinone Anticancer Agent
Preclinical Pharmacology of BA-TPQ, a Novel Synthetic Iminoquinone Anticancer Agent Abstract Marine natural products and their synthetic derivatives represent a major source of novel candidate anti-cancer compounds. We have recently tested the anti-cancer activity of more than forty novel compounds based on an iminoqui...
PMC4710382
core_pubmed_pmc
Formulation, Pharmacokinetic, and Efficacy Studies of Mannosylated Self-Emulsifying Solid Dispersions of Noscapine
Formulation, Pharmacokinetic, and Efficacy Studies of Mannosylated Self-Emulsifying Solid Dispersions of Noscapine Abstract Purpose To formulate hydroxypropyl methylcellulose-stabilized self-emulsifying solid dispersible carriers of noscapine to enhance oral bioavailability. Methods Formulation of noscapine (Nos) self-...
PMC9598487
core_pubmed_pmc
The Issue of Pharmacokinetic-Driven Drug-Drug Interactions of Antibiotics: A Narrative Review
The Issue of Pharmacokinetic-Driven Drug-Drug Interactions of Antibiotics: A Narrative Review Abstract Abstract Patients in intensive care units (ICU) are at high risk to experience potential drug-drug interactions (pDDIs) because of the complexity of their drug regimens. Such pDDIs may be driven by pharmacokinetic or ...
PMC8397627
core_pubmed_pmc
Effects of Repeated Oral Administration of Esaxerenone on the Pharmacokinetics of Midazolam in Healthy Japanese Males
Effects of Repeated Oral Administration of Esaxerenone on the Pharmacokinetics of Midazolam in Healthy Japanese Males Abstract Background and Objective Esaxerenone showed the potential to inhibit and induce activity against cytochrome P450 (CYP) 3A in in vitro studies. We investigated whether repeated administration of...
PMC9257750
core_pubmed_pmc
Evaluation of the Success of High-Throughput Physiologically Based Pharmacokinetic (HT-PBPK) Modeling Predictions to Inform Early Drug Discovery
Evaluation of the Success of High-Throughput Physiologically Based Pharmacokinetic (HT-PBPK) Modeling Predictions to Inform Early Drug Discovery Abstract Abstract Minimizing in vitro and in vivo testing in early drug discovery with the use of physiologically based pharmacokinetic (PBPK) modeling and machine learning (M...
PMC11668346
core_pubmed_pmc
Gut microbiota trigger host liver immune responses that affect drug-metabolising enzymes
Gut microbiota trigger host liver immune responses that affect drug-metabolising enzymes Abstract Abstract There is increasing evidence that the intestinal microbiota plays an integral role in disease pathogenesis and treatment. Specifically, the intestinal microbiota significantly influences the pharmacokinetics and p...
PMC11209715
core_pubmed_pmc
A novel selenium analog of HDACi-based twin drug induces apoptosis and cell cycle arrest via CDC25A to improve prostate cancer therapy
A novel selenium analog of HDACi-based twin drug induces apoptosis and cell cycle arrest via CDC25A to improve prostate cancer therapy Abstract Abstract Cancer therapy has moved from single agents to more mechanism-based targeted approaches. In recent years, the combination of HDAC inhibitors and other anticancer chemi...
PMC10882206
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Design and selection of drug properties to increase the public health impact of next-generation seasonal malaria chemoprevention: a modelling study
Design and selection of drug properties to increase the public health impact of next-generation seasonal malaria chemoprevention: a modelling study Abstract Summary Background Seasonal malaria chemoprevention (SMC) is recommended for disease control in settings with moderate to high Plasmodium falciparum transmission a...
PMC12957623
core_pubmed_pmc
Results of a phase II open-label, multiple-dose study of vamorolone (VBP15-006) in 7- to < 18-year-old boys with duchenne muscular dystrophy
Results of a phase II open-label, multiple-dose study of vamorolone (VBP15-006) in 7- to < 18-year-old boys with duchenne muscular dystrophy Abstract Abstract Background Vamorolone is a dissociative glucocorticoid receptor agonist for treating Duchenne muscular dystrophy (DMD). The VBP15-006 study assessed vamorolone s...
PMC12892071
core_pubmed_pmc
Country-level prediction of blood type distribution in hemophilia A in support of factor VIII consumption
Country-level prediction of blood type distribution in hemophilia A in support of factor VIII consumption Abstract Abstract Background Hemophilia A is an inherited bleeding disorder resulting from a lack of factor (F)VIII. Patients with blood type O show faster decay in their FVIII pharmacokinetics and may require high...
PMC6984741
core_pubmed_pmc
The gut microbiome: an orchestrator of xenobiotic metabolism
The gut microbiome: an orchestrator of xenobiotic metabolism Abstract Microbes inhabiting the intestinal tract of humans represent a site for xenobiotic metabolism. The gut microbiome, the collection of microorganisms in the gastrointestinal tract, can alter the metabolic outcome of pharmaceuticals, environmental toxic...
PMC9413422
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Circulation Time-Optimized Albumin Nanoplatform for Quantitative Visualization of Lung Metastasis via Targeting of Macrophages
Circulation Time-Optimized Albumin Nanoplatform for Quantitative Visualization of Lung Metastasis via Targeting of Macrophages Abstract The development of molecular imaging probes to identify key cellular changes within lung metastases may lead to noninvasive detection of metastatic lesions in the lung. In this study, ...
PMC10033473
core_pubmed_pmc
Entrectinib dose confirmation in pediatric oncology patients: pharmacokinetic considerations
Entrectinib dose confirmation in pediatric oncology patients: pharmacokinetic considerations Abstract Purpose Entrectinib is a central nervous system-active potent inhibitor of tropomyosin receptor kinase (TRK), with anti-tumor activity against neurotrophic NTRK gene fusion-positive tumors. This study investigates the ...
PMC11458483
core_pubmed_pmc
Population pharmacokinetic study in children with vascular anomalies: body weight as a key variable in predicting the initial dose and dosing frequency of sirolimus
Population pharmacokinetic study in children with vascular anomalies: body weight as a key variable in predicting the initial dose and dosing frequency of sirolimus Abstract Abstract Background The main challenges faced when using sirolimus in children with vascular anomalies (VAs) still include significant pharmacokin...
PMC5259903
core_pubmed_pmc
The effect of captopril on the performance of the control strategies of BJUT-II VAD
The effect of captopril on the performance of the control strategies of BJUT-II VAD Abstract Background With the development of left ventricular assist device (LVAD), the long-term support has been paid more attention by various researchers. According to previous researches, the combination of LVAD and pharmacological ...
PMC11914710
core_pubmed_pmc
Navigating the intersection of mental health and kidney health: a systematic review of antidepressant safety in renal impairment
Navigating the intersection of mental health and kidney health: a systematic review of antidepressant safety in renal impairment Abstract Depression is a prevalent mental health condition that significantly impacts adults with impaired renal function, yet the safety and efficacy of antidepressants in this population re...
PMC10573141
core_pubmed_pmc
Randomized Phase II Study of the Safety and Efficacy of Semorinemab in Participants With Mild-to-Moderate Alzheimer Disease: Lauriet
Randomized Phase II Study of the Safety and Efficacy of Semorinemab in Participants With Mild-to-Moderate Alzheimer Disease: Lauriet Abstract Background and Objectives Accumulation of tau pathology in Alzheimer disease (AD) correlates with cognitive decline. Anti-tau immunotherapies were proposed as potential intervent...
PMC7994214
core_pubmed_pmc
Which Analysis Approach Is Adequate to Leverage Clinical Microdialysis Data? A Quantitative Comparison to Investigate Exposure and Response Exemplified by Levofloxacin
Which Analysis Approach Is Adequate to Leverage Clinical Microdialysis Data? A Quantitative Comparison to Investigate Exposure and Response Exemplified by Levofloxacin Abstract Purpose Systematic comparison of analysis methods of clinical microdialysis data for impact on target-site drug exposure and response. Methods ...
PMC5408228
core_pubmed_pmc
Pluronic based β-cyclodextrin polyrotaxanes for treatment of Niemann-Pick Type C disease
Pluronic based β-cyclodextrin polyrotaxanes for treatment of Niemann-Pick Type C disease Abstract Abstract Niemann-Pick Type C disease (NPC) is a rare metabolic disorder characterized by disruption of normal cholesterol trafficking within the cells of the body. There are no FDA approved treatments available for NPC pat...
PMC3155116
core_pubmed_pmc
Early postoperative cognitive dysfunction and postoperative delirium after anaesthesia with various hypnotics: study protocol for a randomised controlled trial - The PINOCCHIO trial
Early postoperative cognitive dysfunction and postoperative delirium after anaesthesia with various hypnotics: study protocol for a randomised controlled trial - The PINOCCHIO trial Abstract Abstract Background Postoperative delirium can result in increased postoperative morbidity and mortality, major demand for postop...
PMC6581936
core_pubmed_pmc
Impact of Intracellular Concentrations on Metabolic Drug-Drug Interaction Studies
Impact of Intracellular Concentrations on Metabolic Drug-Drug Interaction Studies Abstract Abstract Accurate prediction of drug-drug interactions (DDI) is a challenging task in drug discovery and development. It requires determination of enzyme inhibition in vitro which is highly system-dependent for many compounds. Th...
PMC8343172
core_pubmed_pmc
Intranasal temperature-sensitive hydrogels of cannabidiol inclusion complex for the treatment of post-traumatic stress disorder
Intranasal temperature-sensitive hydrogels of cannabidiol inclusion complex for the treatment of post-traumatic stress disorder Abstract Abstract Post-traumatic stress disorder (PTSD) is a psychiatric disease that seriously affects brain function. Currently, selective serotonin reuptake inhibitors (SSRIs) are used to t...
PMC3697035
core_pubmed_pmc
Current Use and Developments Needed for Optimal Design in Pharmacometrics: A Study Performed Among DDMoRe's European Federation of Pharmaceutical Industries and Associations Members
Current Use and Developments Needed for Optimal Design in Pharmacometrics: A Study Performed Among DDMoRe's European Federation of Pharmaceutical Industries and Associations Members Results Results Results were obtained in November 2011 from all the 10 member companies of the DDMoRe consortium (100% response rate): Ast...
PMC10719472
core_pubmed_pmc
The use of microtracers in food‐effect trials: An alternative study design for toxic drugs with long half‐lives exemplified by the case for alectinib
The use of microtracers in food‐effect trials: An alternative study design for toxic drugs with long half‐lives exemplified by the case for alectinib Abstract Abstract The traditional design of food‐effect studies has a high patient burden for toxic drugs with long half‐lives (e.g., anticancer agents). Microtracers cou...
PMC6099197
core_pubmed_pmc
Ribociclib Bioavailability Is Not Affected by Gastric pH Changes or Food Intake: In Silico and Clinical Evaluations
Ribociclib Bioavailability Is Not Affected by Gastric pH Changes or Food Intake: In Silico and Clinical Evaluations Abstract Abstract Ribociclib (KISQALI), a cyclin‐dependent kinase 4/6 inhibitor approved for the first‐line treatment of HR+/HER2– advanced breast cancer with an aromatase inhibitor, is administered with ...
PMC12563750
core_pubmed_pmc
Fungal Biotransformation of Chloroflavanones and Antimicrobial Activity of Parent Compounds and Derived Products
Fungal Biotransformation of Chloroflavanones and Antimicrobial Activity of Parent Compounds and Derived Products Abstract Abstract This study explores the synthesis of chlorine-substituted flavanones and their biotechnologically derived glycosides in order to evaluate how structural modifications influence both antimic...
PMC7825708
core_pubmed_pmc
Ingested Ketone Ester Leads to a Rapid Rise of Acetyl-CoA and Competes with Glucose Metabolism in the Brain of Non-Fasted Mice
Ingested Ketone Ester Leads to a Rapid Rise of Acetyl-CoA and Competes with Glucose Metabolism in the Brain of Non-Fasted Mice Abstract The role of ketone bodies in the cerebral energy homeostasis of neurological diseases has begun to attract recent attention particularly in acute neurological diseases. In ketogenic th...
PMC11090691
core_pubmed_pmc
Magnetite nanoparticles: an emerging adjunctive tool for the improvement of cancer immunotherapy
Magnetite nanoparticles: an emerging adjunctive tool for the improvement of cancer immunotherapy Abstract Cancer immunotherapy has emerged as a groundbreaking field, offering promising and transformative tools for oncological research and treatment. However, it faces several limitations, including variations in cancer ...
PMC8234236
core_pubmed_pmc
Meropenem Pharmacokinetics and Target Attainment in Critically Ill Patients Are Not Affected by Extracorporeal Membrane Oxygenation: A Matched Cohort Analysis
Meropenem Pharmacokinetics and Target Attainment in Critically Ill Patients Are Not Affected by Extracorporeal Membrane Oxygenation: A Matched Cohort Analysis Abstract Existing evidence is inconclusive whether meropenem dosing should be adjusted in patients receiving extracorporeal membrane oxygenation (ECMO). Therefor...
PMC3299547
core_pubmed_pmc
Pharmacokinetics of iron isomaltoside 1000 in patients with inflammatory bowel disease
Pharmacokinetics of iron isomaltoside 1000 in patients with inflammatory bowel disease Abstract Abstract Background Iron isomaltoside 1000 is a novel injectable iron compound which offers potential advantages in the treatment of subjects with iron-deficiency anemia. We studied the pharmacokinetics (PK) of this novel co...
PMC8525492
core_pubmed_pmc
First-in-Human Evaluation of the Safety, Tolerability, and Pharmacokinetics of SPR720, a Novel Oral Bacterial DNA Gyrase (GyrB) Inhibitor for Mycobacterial Infections
First-in-Human Evaluation of the Safety, Tolerability, and Pharmacokinetics of SPR720, a Novel Oral Bacterial DNA Gyrase (GyrB) Inhibitor for Mycobacterial Infections Abstract ABSTRACT SPR720 (phosphate prodrug of SPR719) is a novel aminobenzimidazole bacterial DNA gyrase (GyrB) inhibitor in development for nontubercul...
PMC5658280
core_pubmed_pmc
Implications for Drug Characterization in Glucose Tolerance Tests Without Insulin: Simulation Study of Power and Predictions Using Model‐Based Analysis
Implications for Drug Characterization in Glucose Tolerance Tests Without Insulin: Simulation Study of Power and Predictions Using Model‐Based Analysis Abstract Abstract In antihyperglycemic drug development, drug effects are usually characterized using glucose provocations. Analyzing provocation data using pharmacomet...
PMC5913986
core_pubmed_pmc
Repurposing and Reformulation of the Antiparasitic Agent Flubendazole for Treatment of Cryptococcal Meningoencephalitis, a Neglected Fungal Disease
Repurposing and Reformulation of the Antiparasitic Agent Flubendazole for Treatment of Cryptococcal Meningoencephalitis, a Neglected Fungal Disease Abstract ABSTRACT Current therapeutic options for cryptococcal meningitis are limited by toxicity, global supply, and emergence of resistance. There is an urgent need to de...
PMC10859566
core_pubmed_pmc
Push forward LC-MS-based therapeutic drug monitoring and pharmacometabolomics for anti-tuberculosis precision dosing and comprehensive clinical management
Push forward LC-MS-based therapeutic drug monitoring and pharmacometabolomics for anti-tuberculosis precision dosing and comprehensive clinical management Abstract The spread of tuberculosis (TB), especially multidrug-resistant TB and extensively drug-resistant TB, has strongly motivated the research and development of...
PMC8721355
core_pubmed_pmc
Nano-Honokiol ameliorates the cognitive deficits in TgCRND8 mice of Alzheimer’s disease via inhibiting neuropathology and modulating gut microbiota
Nano-Honokiol ameliorates the cognitive deficits in TgCRND8 mice of Alzheimer’s disease via inhibiting neuropathology and modulating gut microbiota Abstract Highlights • In the same content, Nano-HO could effectively enhance the bioactivity of HO remarkably and prolonged its circulation time in rats. • Nano-HO improved...
PMC10359000
core_pubmed_pmc
Oxamniquine derivatives overcome Praziquantel treatment limitations for Schistosomiasis
Oxamniquine derivatives overcome Praziquantel treatment limitations for Schistosomiasis Abstract Abstract Human schistosomiasis is a neglected tropical disease caused by Schistosoma mansoni , S . haematobium , and S . japonicum . Praziquantel (PZQ) is the method of choice for treatment. Due to constant selection pressu...
PMC4634315
core_pubmed_pmc
Fc glycans of therapeutic antibodies as critical quality attributes
Fc glycans of therapeutic antibodies as critical quality attributes Abstract Critical quality attributes (CQA) are physical, chemical, biological or microbiological properties or characteristics that must be within an appropriate limit, range or distribution to ensure the desired product quality, safety and efficacy. F...
PMC2846120
core_pubmed_pmc
Antipsychotic treatments for the elderly: efficacy and safety of aripiprazole
Antipsychotic treatments for the elderly: efficacy and safety of aripiprazole Abstract Delusions, hallucinations and other psychotic symptoms can accompany a number of conditions in late life. As such, elderly patients are commonly prescribed antipsychotic medications for the treatment of psychosis in both acute and ch...
PMC5119026
core_pubmed_pmc
Randomized, Open-Label Study of the Pharmacokinetics and Safety of Oral and Intravenous Administration of Omadacycline to Healthy Subjects
Randomized, Open-Label Study of the Pharmacokinetics and Safety of Oral and Intravenous Administration of Omadacycline to Healthy Subjects Abstract Omadacycline is a first-in-class aminomethylcycline antibiotic with microbiological activity against Gram-positive and Gram-negative aerobes and anaerobes and atypical bact...
PMC11684622
core_pubmed_pmc
Preliminary evaluation of ex vivo and in vivo skin permeability of aromatic amines
Preliminary evaluation of ex vivo and in vivo skin permeability of aromatic amines Abstract Abstract A potential link has been reported between skin exposure to aromatic amines, such as ortho-toluidine (OT) and 3,3′-dichloro-4,4′-diaminodiphenylmethane (MOCA), and bladder cancer cases observed in Japanese chemical fact...
PMC12144411
core_pubmed_pmc
A pharmacokinetic study and critical reappraisal of curcumin formulations enhancing bioavailability
A pharmacokinetic study and critical reappraisal of curcumin formulations enhancing bioavailability Abstract Summary This independent crossover study assessed curcumin bioavailability and excretion in nine healthy males receiving three formulations (AOV, Longvida, and NovaSOL) at about 570 mg, while AOV was also tested...
PMC8494385
core_pubmed_pmc
Nanostructured Valsartan Microparticles with Enhanced Bioavailability Produced by High-Throughput Electrohydrodynamic Room-Temperature Atomization
Nanostructured Valsartan Microparticles with Enhanced Bioavailability Produced by High-Throughput Electrohydrodynamic Room-Temperature Atomization Abstract Abstract The high-throughput drying and encapsulation technique called electrospraying assisted by pressurized gas (EAPG) was used for the first time to produce nan...
PMC12353477
core_pubmed_pmc
Machine Learning and Artificial Intelligence in Nanomedicine
Machine Learning and Artificial Intelligence in Nanomedicine Abstract ABSTRACT Nanomedicine harnesses nanoscale materials, such as lipid, polymeric, and inorganic nanoparticles, to deliver diagnostic or therapeutic agents for cancer, infectious disease, and neurological disorders, among others. However, translating pro...
PMC6957455
core_pubmed_pmc
A Summary Report of FSCJ Workshop “Future Challenges and Opportunities in Developing Methodologies for Improved Human Risk Assessments”
A Summary Report of FSCJ Workshop “Future Challenges and Opportunities in Developing Methodologies for Improved Human Risk Assessments” Abstract Abstract This is a summary report of FSCJ (Food Safety Commission of Japan) workshop entitled “Future Challenges and Opportunities in Developing Methodologies for Improved Hum...
PMC12855590
core_pubmed_pmc
Generation and characterisation of a humanised GLP-1 receptor mouse model for translational drug development
Generation and characterisation of a humanised GLP-1 receptor mouse model for translational drug development Abstract Summary Background Injectable peptide-based glucagon-like peptide-1 receptor (GLP1R) agonists (GLP1RAs) are effective treatments for obesity and diabetes but are limited by patient compliance and scalab...
PMC12511210
core_pubmed_pmc
Preclinical evaluation of sodium copper chlorophyllin: safety, pharmacokinetics, and therapeutic potential in breast cancer chemotherapy and cyclophosphamide-induced bladder toxicity
Preclinical evaluation of sodium copper chlorophyllin: safety, pharmacokinetics, and therapeutic potential in breast cancer chemotherapy and cyclophosphamide-induced bladder toxicity Abstract Sodium copper chlorophyllin (chlorophyllin, CHL), a semi-synthetic water-soluble derivative of green plant pigment chlorophyll, ...
PMC4431334
core_pubmed_pmc
Efficacy and safety of ascending methotrexate dose in combination with adalimumab: the randomised CONCERTO trial
Efficacy and safety of ascending methotrexate dose in combination with adalimumab: the randomised CONCERTO trial Abstract Objective CONCERTO was a randomised, double-blind, parallel-armed study of methotrexate (MTX) in combination with adalimumab to assess whether an increasing trend of efficacy and decreased safety ex...