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PMC7760865
core_pubmed_pmc
Low Oral Bioavailability and Partial Gut Microbiotic and Phase II Metabolism of Brussels/Witloof Chicory Sesquiterpene Lactones in Healthy Humans
Low Oral Bioavailability and Partial Gut Microbiotic and Phase II Metabolism of Brussels/Witloof Chicory Sesquiterpene Lactones in Healthy Humans Abstract Free and glycosylated sesquiterpene lactones (SLs), which are abundant in leafy vegetables including Brussels/witloof chicory, possess health-promoting effects in vi...
PMC6787415
core_pubmed_pmc
Donepezil Treatment for Alzheimer's Disease in Chronic Dialysis Patients
Donepezil Treatment for Alzheimer's Disease in Chronic Dialysis Patients Abstract Abstract Donepezil is one of the cholinesterase inhibitors that are indicated for the treatment of mild to moderate Alzheimer's disease (AD). Pharmacokinetic analysis has shown that donepezil is primarily eliminated by renal excretion rat...
PMC8206290
core_pubmed_pmc
Clinical Pharmacokinetics of Oral Sodium Selenite and Dosing Implications in the Treatment of Patients with Metastatic Cancer
Clinical Pharmacokinetics of Oral Sodium Selenite and Dosing Implications in the Treatment of Patients with Metastatic Cancer Abstract Abstract Background Selenite is a radiosensitizer and inhibitor of androgen receptor expression and function. In a phase I study ( NCT02184533 ) in 15 subjects with metastatic cancer re...
PMC5351011
core_pubmed_pmc
A Phase I Randomized Study of a Specifically Engineered, pH‐Sensitive PCSK9 Inhibitor RN317 (PF‐05335810) in Hypercholesterolemic Subjects on Statin Therapy
A Phase I Randomized Study of a Specifically Engineered, pH‐Sensitive PCSK9 Inhibitor RN317 (PF‐05335810) in Hypercholesterolemic Subjects on Statin Therapy Abstract Abstract This phase I study assessed the safety, tolerability, pharmacokinetics, and pharmacodynamics of RN317 (PF‐05335810), a specifically engineered, p...
PMC6983930
core_pubmed_pmc
Bioactive indanes: Development and validation of an LC-MS/MS bioanalytical method for the determination of PH46A, a new potential anti-inflammatory agent, in dog and rat plasma and its application to a pharmacokinetic study in dog
Bioactive indanes: Development and validation of an LC-MS/MS bioanalytical method for the determination of PH46A, a new potential anti-inflammatory agent, in dog and rat plasma and its application to a pharmacokinetic study in dog Abstract Highlights • Selective and sensitive determination by LC—MS/MS of PH46A, a new c...
PMC9049199
core_pubmed_pmc
Simultaneous quantification of five biomarkers in ethanolic extract of Cassia occidentalis Linn. stem using liquid chromatography tandem mass spectrometry: application to its pharmacokinetic studies
Simultaneous quantification of five biomarkers in ethanolic extract of Cassia occidentalis Linn. stem using liquid chromatography tandem mass spectrometry: application to its pharmacokinetic studies Abstract Cassia occidentalis L. stem extract is used as a purgative, febrifuge, and diuretic, and in the treatment of flu...
PMC6777137
core_pubmed_pmc
A Physiology-Based Model of Human Bile Acid Metabolism for Predicting Bile Acid Tissue Levels After Drug Administration in Healthy Subjects and BRIC Type 2 Patients
A Physiology-Based Model of Human Bile Acid Metabolism for Predicting Bile Acid Tissue Levels After Drug Administration in Healthy Subjects and BRIC Type 2 Patients Abstract Drug-induced liver injury (DILI) is a matter of concern in the course of drug development and patient safety, often leading to discontinuation of ...
PMC9391940
core_pubmed_pmc
In silico Drug Repurposing of Anticancer Drug 5-FU and Analogues Against SARS-CoV-2 Main Protease: Molecular Docking, Molecular Dynamics Simulation, Pharmacokinetics and Chemical Reactivity Studies
In silico Drug Repurposing of Anticancer Drug 5-FU and Analogues Against SARS-CoV-2 Main Protease: Molecular Docking, Molecular Dynamics Simulation, Pharmacokinetics and Chemical Reactivity Studies Abstract Abstract Background Since the last COVID-19 outbreak, several approaches have been given a try to quickly tackle ...
PMC5563351
core_pubmed_pmc
Pharmacokinetics of Rytary ® , An Extended-Release Capsule Formulation of Carbidopa–Levodopa
Pharmacokinetics of Rytary ® , An Extended-Release Capsule Formulation of Carbidopa–Levodopa Abstract Abstract Parkinson’s disease (PD) is a chronic progressive neurological disorder characterized by resting tremor, rigidity, bradykinesia, gait disturbance, and postural instability. Levodopa, the precursor to dopamine,...
PMC5948259
core_pubmed_pmc
A phase I study to assess the mass balance, excretion, and pharmacokinetics of [ 14 C]-ixazomib, an oral proteasome inhibitor, in patients with advanced solid tumors
A phase I study to assess the mass balance, excretion, and pharmacokinetics of [ 14 C]-ixazomib, an oral proteasome inhibitor, in patients with advanced solid tumors Abstract Summary This two-part, phase I study evaluated the mass balance, excretion, pharmacokinetics (PK), and safety of ixazomib in patients with advanc...
PMC7549214
core_pubmed_pmc
Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria
Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria Abstract Abstract Background Emergence of anti-malarial drug resistance and perpetual increase in malaria incidence necessitates the development of novel anti-malarials. Histone deacetylases (HDAC) has been shown...
PMC9200067
core_pubmed_pmc
Estimation of brain receptor occupancy for trazodone immediate release and once a day formulations
Estimation of brain receptor occupancy for trazodone immediate release and once a day formulations Abstract Abstract Trazodone is approved for the treatment of major depressive disorders, marketed as immediate release (IR), prolonged release, and once a day (OAD) formulation. The different formulations allow different ...
PMC11858278
core_pubmed_pmc
Environmentally Friendly Synthesis of New Mono- and Bis-Pyrazole Derivatives; In Vitro Antimicrobial, Antifungal, and Antioxidant Activity; and In Silico Studies: DFT, ADMETox, and Molecular Docking
Environmentally Friendly Synthesis of New Mono- and Bis-Pyrazole Derivatives; In Vitro Antimicrobial, Antifungal, and Antioxidant Activity; and In Silico Studies: DFT, ADMETox, and Molecular Docking Abstract Abstract Background/Objectives: Antimicrobial resistance and oxidative stress are major global health challenges...
PMC10810248
core_pubmed_pmc
Safety, tolerability, pharmacodynamic and wellbeing effects of SPL026 (dimethyltryptamine fumarate) in healthy participants: a randomized, placebo-controlled phase 1 trial
Safety, tolerability, pharmacodynamic and wellbeing effects of SPL026 (dimethyltryptamine fumarate) in healthy participants: a randomized, placebo-controlled phase 1 trial Abstract Abstract Background Due to their potential impact on mood and wellbeing there has been increasing interest in the potential of serotonergic...
PMC7911036
core_pubmed_pmc
Quantification of BNN27, a novel neuroprotective 17‐spiroepoxy dehydroepiandrosterone derivative in the blood and retina of rodents, after single intraperitoneal administration
Quantification of BNN27, a novel neuroprotective 17‐spiroepoxy dehydroepiandrosterone derivative in the blood and retina of rodents, after single intraperitoneal administration Abstract Abstract BNN27 is a novel 17‐spiroepoxy derivative of the neurosteroid Dehydroepiandrosterone with neuroprotective properties. The pur...
PMC9041753
core_pubmed_pmc
Development of stealth liposomal formulation of celecoxib: In vitro and in vivo evaluation
Development of stealth liposomal formulation of celecoxib: In vitro and in vivo evaluation Abstract Abstract Celecoxib (CLB) is a highly hydrophobic selective cyclo-oxygenase inhibitor with high plasma protein binding and undergoes extensive hepatic metabolism. CLB is highly effective in the treatment of osteo and rheu...
PMC9669261
core_pubmed_pmc
Efficacy and Pharmacodynamic Target Attainment for Ceftazidime–Avibactam Off-Label Dose Regimens in Patients with Continuous or Intermittent Venovenous Hemodialysis: Two Case Reports
Efficacy and Pharmacodynamic Target Attainment for Ceftazidime–Avibactam Off-Label Dose Regimens in Patients with Continuous or Intermittent Venovenous Hemodialysis: Two Case Reports Abstract Abstract Limited data are available for ceftazidime–avibactam (CZA) dosing in patients receiving renal replacement therapy, espe...
PMC11618211
core_pubmed_pmc
Pharmacodynamics (PD), Pharmacokinetics (PK) and PK-PD Modeling of NRF2 Activating Dietary Phytochemicals in Cancer Prevention and in Health
Pharmacodynamics (PD), Pharmacokinetics (PK) and PK-PD Modeling of NRF2 Activating Dietary Phytochemicals in Cancer Prevention and in Health Abstract Purpose of Review Dietary phytochemicals, bioactive compounds derived from plants, have gained increasing attention for their potential role in cancer prevention. Among t...
PMC7246848
core_pubmed_pmc
Comparative Cerebroprotective Potential of d - and l -Carnosine Following Ischemic Stroke in Mice
Comparative Cerebroprotective Potential of d - and l -Carnosine Following Ischemic Stroke in Mice Abstract l -carnosine is an attractive therapeutic agent for acute ischemic stroke based on its robust preclinical cerebroprotective properties and wide therapeutic time window. However, large doses are needed for efficacy...
PMC11813913
core_pubmed_pmc
Population dynamics analysis of the interaction between tacrolimus and voriconazole in renal transplant recipients
Population dynamics analysis of the interaction between tacrolimus and voriconazole in renal transplant recipients Abstract Abstract Background The concurrent administration of tacrolimus and voriconazole in kidney transplant recipients can lead to drug interactions, potentially resulting in severe adverse reactions. T...
PMC12034845
core_pubmed_pmc
Utilizing Physiologically Based Pharmacokinetic Models to Support Rational Medication in Chinese Elderly Population
Utilizing Physiologically Based Pharmacokinetic Models to Support Rational Medication in Chinese Elderly Population Abstract Background China is undergoing a pronounced shift towards an aging society, wherein the elderly constitute a prominent demographic relying significantly on medications. The imperative of administ...
PMC12513044
core_pubmed_pmc
Effects of Lacosamide, Pregabalin, and Tapentadol on Peripheral Nerve Excitability: A Randomized, Double-blind, Placebo-controlled, Crossover, Multicenter Trial in Healthy Subjects
Effects of Lacosamide, Pregabalin, and Tapentadol on Peripheral Nerve Excitability: A Randomized, Double-blind, Placebo-controlled, Crossover, Multicenter Trial in Healthy Subjects Abstract Abstract Background: Chronic pain is a leading cause of disability globally, with limited treatment options and frequent adverse e...
PMC11562027
core_pubmed_pmc
Development of ion-triggered in situ gel containing ketoconazole/hydroxypropyl-β-cyclodextrin for ocular delivery: in vitro and in vivo evaluation
Development of ion-triggered in situ gel containing ketoconazole/hydroxypropyl-β-cyclodextrin for ocular delivery: in vitro and in vivo evaluation Abstract Abstract The application of ketoconazole (KET) in ocular drug delivery is restricted by its poor aqueous solubility though its broad-spectrum antifungal activity. T...
PMC9828147
core_pubmed_pmc
DFinder: a novel end-to-end graph embedding-based method to identify drug–food interactions
DFinder: a novel end-to-end graph embedding-based method to identify drug–food interactions Abstract Abstract Motivation Drug–food interactions (DFIs) occur when some constituents of food affect the bioaccessibility or efficacy of the drug by involving in drug pharmacodynamic and/or pharmacokinetic processes. Many comp...
PMC12358300
core_pubmed_pmc
Evaluation of Four Semi‐Mechanistic Models for Predicting Glycemic Control With a Glucagon Receptor Antagonist in People With Type 2 Diabetes
Evaluation of Four Semi‐Mechanistic Models for Predicting Glycemic Control With a Glucagon Receptor Antagonist in People With Type 2 Diabetes Abstract ABSTRACT Glycated hemoglobin (HbA1c) is the gold standard for measuring long‐term glycemic efficacy over at least 3 months in Type 2 diabetes (T2D). Being able to predic...
PMC11574905
core_pubmed_pmc
Unlocking Benzosampangine’s Potential: A Computational Approach to Investigating, Its Role as a PD-L1 Inhibitor in Tumor Immune Evasion via Molecular Docking, Dynamic Simulation, and ADMET Profiling
Unlocking Benzosampangine’s Potential: A Computational Approach to Investigating, Its Role as a PD-L1 Inhibitor in Tumor Immune Evasion via Molecular Docking, Dynamic Simulation, and ADMET Profiling Abstract Abstract The interaction between programmed cell death protein 1 (PD-1) and its ligand PD-L1 plays a crucial rol...
PMC7791651
core_pubmed_pmc
Pharmacokinetics of indacaterol, glycopyrronium and mometasone furoate administered as an inhaled fixed-dose combination in Japanese and Caucasian healthy subjects
Pharmacokinetics of indacaterol, glycopyrronium and mometasone furoate administered as an inhaled fixed-dose combination in Japanese and Caucasian healthy subjects Abstract Background A once-daily (o.d.) fixed-dose combination of indacaterol acetate (IND), glycopyrronium bromide (GLY), and mometasone furoate (MF) deliv...
PMC8679518
core_pubmed_pmc
Epicatechin is a promising novel inhibitor of SARS-CoV-2 entry by disrupting interactions between angiotensin-converting enzyme type 2 and the viral receptor binding domain: A computational/simulation study
Epicatechin is a promising novel inhibitor of SARS-CoV-2 entry by disrupting interactions between angiotensin-converting enzyme type 2 and the viral receptor binding domain: A computational/simulation study Abstract Abstract Angiotensin-converting enzyme 2 (ACE2) is the first target of SARS-CoV-2 and a key functional h...
PMC3675301
core_pubmed_pmc
Long-Term Anticoagulation in the Extreme Elderly with the Newer Antithrombotics: Safe or Sorry?
Long-Term Anticoagulation in the Extreme Elderly with the Newer Antithrombotics: Safe or Sorry? Abstract Background and Objectives The prevalence of atrial fibrillation (AF) doubles in the extreme elderly and is higher than in the rest of the population. Warfarin therapy to prevent thromboembolic events secondary to AF...
PMC3644256
core_pubmed_pmc
Evaluation of propofol anesthesia in morbidly obese children and adolescents
Evaluation of propofol anesthesia in morbidly obese children and adolescents Abstract Background Poor characterization of propofol pharmacokinetics and pharmacodynamics in the morbidly obese (MO) pediatric population poses dosing challenges. This study was conducted to evaluate propofol total intravenous anesthesia (TI...
PMC9237441
core_pubmed_pmc
Molecular Pathways and Roles for Vitamin K2-7 as a Health-Beneficial Nutraceutical: Challenges and Opportunities
Molecular Pathways and Roles for Vitamin K2-7 as a Health-Beneficial Nutraceutical: Challenges and Opportunities Abstract Vitamin K2-7, also known as menaquinone-7 (MK-7) is a form of vitamin K that has health-beneficial effects in osteoporosis, cardiovascular disease, inflammation, cancer, Alzheimer’s disease, diabete...
PMC12009869
core_pubmed_pmc
Paeoniflorin: a review of its pharmacology, pharmacokinetics and toxicity in diabetes
Paeoniflorin: a review of its pharmacology, pharmacokinetics and toxicity in diabetes Abstract Abstract The escalating global prevalence of diabetes underscores the urgency of addressing its treatment and associated complications. Paeoniflorin, a monoterpenoid glycoside compound, has garnered substantial attention in r...
PMC6133194
core_pubmed_pmc
Pharmacokinetic Evaluation of a 1-Day Treatment Initiation Option for Starting Long-Acting Aripiprazole Lauroxil for Schizophrenia
Pharmacokinetic Evaluation of a 1-Day Treatment Initiation Option for Starting Long-Acting Aripiprazole Lauroxil for Schizophrenia Abstract Supplemental digital content is available in the text. Abstract Background Aripiprazole lauroxil (AL), a long-acting injectable antipsychotic for the treatment of schizophrenia, re...
PMC6359037
core_pubmed_pmc
Effects of Piperazine Derivative on Paclitaxel Pharmacokinetics
Effects of Piperazine Derivative on Paclitaxel Pharmacokinetics Abstract Paclitaxel (PTX) is an anticancer agent that is used to treat many cancers but it has a very low oral bioavailability due, at least in part, to the drug efflux transporter, P-glycoprotein (P-gp). Therefore, this study was performed to enhance oral...
PMC11245884
core_pubmed_pmc
Difficulties associated with the interpretation of postmortem toxicology
Difficulties associated with the interpretation of postmortem toxicology Abstract Abstract While postmortem (PM) toxicology results provide valuable information towards ascertaining both the cause and manner of death in coronial cases, there are also significant difficulties associated with the interpretation of PM dru...
PMC7602742
core_pubmed_pmc
Physiologically-Based Pharmacokinetic/Pharmacodynamic Model of MBQ-167 to Predict Tumor Growth Inhibition in Mice
Physiologically-Based Pharmacokinetic/Pharmacodynamic Model of MBQ-167 to Predict Tumor Growth Inhibition in Mice Abstract Abstract MBQ-167 is a dual inhibitor of the Rho GTPases Rac and Cdc42 that has shown promising results as an anti-cancer therapeutic at the preclinical stage. This drug has been tested in vitro and...
PMC6143907
core_pubmed_pmc
Combination of magnetic resonance imaging and targeted contrast agent for the diagnosis of myocardial infarction
Combination of magnetic resonance imaging and targeted contrast agent for the diagnosis of myocardial infarction Abstract Abstract Myocardial infarction is one of the most common human cerebrovascular conditions and frequently leads to ischemic stroke. Evidence has indicated that magnetic resonance imaging (MRI) is a p...
PMC10819565
core_pubmed_pmc
Effects of H2-Receptor Antagonists on the Exposure of Dacomitinib
Effects of H2-Receptor Antagonists on the Exposure of Dacomitinib Abstract Abstract Dacomitinib is an irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor indicated for the treatment of patients with advanced non-small-cell lung cancer (NSCLC) and EGFR-activating mutations. Proton-pump inhibit...
PMC11762574
core_pubmed_pmc
Relative Forgiveness of Different Allopurinol Implementation Patterns in People with Gout and their Impact on Clinical Outcomes: a Simulation Study
Relative Forgiveness of Different Allopurinol Implementation Patterns in People with Gout and their Impact on Clinical Outcomes: a Simulation Study Abstract Abstract Background and Objective Adherence to urate-lowering therapy among people with gout is poor, so it is important to understand which day-to-day medication-...
PMC9271885
core_pubmed_pmc
Pre-clinical evaluation of antiviral activity of nitazoxanide against SARS-CoV-2
Pre-clinical evaluation of antiviral activity of nitazoxanide against SARS-CoV-2 Abstract Summary Background To address the emergence of SARS-CoV-2, multiple clinical trials in humans were rapidly started, including those involving an oral treatment by nitazoxanide, despite no or limited pre-clinical evidence of antivi...
PMC3306781
core_pubmed_pmc
First dose in children: physiological insights into pharmacokinetic scaling approaches and their implications in paediatric drug development
First dose in children: physiological insights into pharmacokinetic scaling approaches and their implications in paediatric drug development Abstract Dose selection for “first in children” trials often relies on scaling of the pharmacokinetics from adults to children. Commonly used approaches are physiologically-based ...
PMC12239117
core_pubmed_pmc
The pharmacokinetics of hexylresorcinol-containing lozenges and their antimicrobial efficacy against oral and respiratory microorganisms
The pharmacokinetics of hexylresorcinol-containing lozenges and their antimicrobial efficacy against oral and respiratory microorganisms Abstract ABSTRACT Background Hexylresorcinol (HR) lozenges provide symptomatic relief for sore throats. Despite its recognised anaesthetic and antiseptic properties, evidence of HR ba...
PMC3459840
core_pubmed_pmc
Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes , a potential antitumor drug
Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes , a potential antitumor drug Abstract Abstract Purpose To investigate the growth inhibition activity of Flammulina velutipes sterol (FVS) against certain human cancer cell lines (gastric SGC and colon LoVo) and to evaluat...
PMC8911561
core_pubmed_pmc
Quantification of Venetoclax for Therapeutic Drug Monitoring in Chinese Acute Myeloid Leukemia Patients by a Validated UPLC-MS/MS Method
Quantification of Venetoclax for Therapeutic Drug Monitoring in Chinese Acute Myeloid Leukemia Patients by a Validated UPLC-MS/MS Method Abstract Venetoclax has emerged as a breakthrough for treatment of leukemia with a wide interindividual variability in pharmacokinetics. Herein, a rapid, sensitive, and reliable UPLC-...
PMC12932621
core_pubmed_pmc
Therapeutic drug monitoring of daptomycin in a critically ill patient cohort
Therapeutic drug monitoring of daptomycin in a critically ill patient cohort Abstract Background Pharmacokinetics of antimicrobial agents are altered in critically ill patients. Therefore, therapeutic drug monitoring (TDM) has gained much attention in recent years. Specifically, the role of TDM for daptomycin, its pote...
PMC4467250
core_pubmed_pmc
Pharmacokinetics of Single-Dose Dolutegravir in HIV-Seronegative Subjects With Moderate Hepatic Impairment Compared to Healthy Matched Controls
Pharmacokinetics of Single-Dose Dolutegravir in HIV-Seronegative Subjects With Moderate Hepatic Impairment Compared to Healthy Matched Controls Abstract This study evaluated dolutegravir pharmacokinetics (PK) in subjects with moderate hepatic impairment compared to matched, healthy controls. In this open-label, paralle...
PMC10842770
core_pubmed_pmc
Photobac derived from bacteriochlorophyll-a shows potential for treating brain tumor in animal models by photodynamic therapy with desired pharmacokinetics and limited toxicity in rats and dogs
Photobac derived from bacteriochlorophyll-a shows potential for treating brain tumor in animal models by photodynamic therapy with desired pharmacokinetics and limited toxicity in rats and dogs Abstract Photobac is a near infrared photosensitizer (PS) derived from naturally occurring bacteriochlorophyll-a, with a poten...
PMC6276942
core_pubmed_pmc
Closed-Loop Intravenous Drug Administration Using Photoplethysmography
Closed-Loop Intravenous Drug Administration Using Photoplethysmography Abstract Abstract An optically-based injection control system has been developed for preclinical use for an intravenous drug delivery application. Current clinical drug delivery for oncology typically provides for intravenous administration without ...
PMC4546409
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics with Extended Dosing of CC-486 in Patients with Hematologic Malignancies
Pharmacokinetics and Pharmacodynamics with Extended Dosing of CC-486 in Patients with Hematologic Malignancies Abstract Abstract CC-486 (oral azacitidine) is an epigenetic modifier in development for patients with myelodysplastic syndromes and acute myeloid leukemia. In part 1 of this two-part study, a 7-day CC-486 dos...
PMC7066107
core_pubmed_pmc
Phase I study of the indoleamine 2,3-dioxygenase 1 inhibitor navoximod (GDC-0919) as monotherapy and in combination with the PD-L1 inhibitor atezolizumab in Japanese patients with advanced solid tumours
Phase I study of the indoleamine 2,3-dioxygenase 1 inhibitor navoximod (GDC-0919) as monotherapy and in combination with the PD-L1 inhibitor atezolizumab in Japanese patients with advanced solid tumours Abstract Summary Navoximod (GDC-0919) is a small molecule inhibitor of indoleamine-2,3-dioxygenase 1. This study inve...
PMC5073492
core_pubmed_pmc
Evaluating the safety and dosing of drugs in patients with liver cirrhosis by literature review and expert opinion
Evaluating the safety and dosing of drugs in patients with liver cirrhosis by literature review and expert opinion Abstract Introduction Liver cirrhosis can have a major impact on drug pharmacokinetics and pharmacodynamics. Patients with cirrhosis often suffer from potentially preventable adverse drug reactions. Guidel...
PMC9683076
core_pubmed_pmc
Effects of a ritonavir‐containing regimen on the pharmacokinetics of sirolimus or everolimus in healthy adult subjects
Effects of a ritonavir‐containing regimen on the pharmacokinetics of sirolimus or everolimus in healthy adult subjects Abstract Abstract The immunosuppressive agents sirolimus and everolimus are sensitive CYP3A4 substrates with narrow therapeutic index. Ritonavir is a strong CYP3A inhibitor. A phase 1 study was conduct...
PMC11152975
core_pubmed_pmc
Polycaprolactone – Vitamin E TPGS micelles for delivery of paclitaxel: In vitro and in vivo evaluation
Polycaprolactone – Vitamin E TPGS micelles for delivery of paclitaxel: In vitro and in vivo evaluation Abstract This study aimed to present findings on a paclitaxel (PTX)-loaded polymeric micellar formulation based on polycaprolactone-vitamin E TPGS (PCL-TPGS) and evaluate its in vitro anticancer activity as well as it...
PMC5093939
core_pubmed_pmc
Teicoplanin-based antimicrobial therapy in Staphylococcus aureus bone and joint infection: tolerance, efficacy and experience with subcutaneous administration
Teicoplanin-based antimicrobial therapy in Staphylococcus aureus bone and joint infection: tolerance, efficacy and experience with subcutaneous administration Abstract Abstract Background Staphylococci represent the first etiologic agents of bone and joint infection (BJI), leading glycopeptides use, especially in case ...
PMC10955611
core_pubmed_pmc
Clinical evaluation of PF614, a novel TAAP prodrug of oxycodone, versus OxyContin in a multi‐ascending dose study with a bioequivalence arm in healthy volunteers
Clinical evaluation of PF614, a novel TAAP prodrug of oxycodone, versus OxyContin in a multi‐ascending dose study with a bioequivalence arm in healthy volunteers Abstract Abstract PF614, a trypsin‐activated abuse protection oxycodone prodrug designed to reduce recreational drug abuse, was compared to OxyContin for safe...
PMC3896282
core_pubmed_pmc
Comparative steady-state pharmacokinetic study of an extended-release formulation of itopride and its immediate-release reference formulation in healthy volunteers
Comparative steady-state pharmacokinetic study of an extended-release formulation of itopride and its immediate-release reference formulation in healthy volunteers Abstract Abstract Background This study was conducted to compare the oral bioavailability of an itopride extended-release (ER) formulation with that of the ...
PMC8286234
core_pubmed_pmc
Bioanalysis of niclosamide in plasma using liquid chromatography-tandem mass and application to pharmacokinetics in rats and dogs
Bioanalysis of niclosamide in plasma using liquid chromatography-tandem mass and application to pharmacokinetics in rats and dogs Abstract Niclosamide, which is an anti-tapeworm drug, was developed in 1958. However, recent studies have demonstrated the antiviral effects of niclosamide against the SARS-CoV-2 virus, whic...
PMC5510082
core_pubmed_pmc
Population pharmacokinetics of rituximab in patients with diffuse large B‐cell lymphoma and association with clinical outcome
Population pharmacokinetics of rituximab in patients with diffuse large B‐cell lymphoma and association with clinical outcome Abstract Abstract Aims Pharmacokinetic (PK) studies suggest that there is a room for improvement in clinical use of rituximab through more individualized treatment. The objective of this study w...
PMC7443423
core_pubmed_pmc
Optimizing Predictive Performance of Bayesian Forecasting for Vancomycin Concentration in Intensive Care Patients
Optimizing Predictive Performance of Bayesian Forecasting for Vancomycin Concentration in Intensive Care Patients Abstract Purpose Bayesian forecasting is crucial for model-based dose optimization based on therapeutic drug monitoring (TDM) data of vancomycin in intensive care (ICU) patients. We aimed to evaluate the pe...
PMC11790873
core_pubmed_pmc
Regulation of adipocyte differentiation and lipid metabolism by novel synthetic chromenes exploring anti-obesity and broader therapeutic potential
Regulation of adipocyte differentiation and lipid metabolism by novel synthetic chromenes exploring anti-obesity and broader therapeutic potential Abstract Abstract Obesity poses a significant global health challenge, necessitating the search for novel therapeutic agents to address this epidemic. Chromenes, known for t...
PMC3111455
core_pubmed_pmc
Matrix Metalloproteinase-8 Mediates the Unfavorable Systemic Impact of Local Irradiation on Pharmacokinetics of Anti-Cancer Drug 5-Fluorouracil
Matrix Metalloproteinase-8 Mediates the Unfavorable Systemic Impact of Local Irradiation on Pharmacokinetics of Anti-Cancer Drug 5-Fluorouracil Abstract Abstract Concurrent chemoradiation with 5-fluorouracil (5-FU) is widely accepted for cancer treatment. However, the interactions between radiation and 5-FU remain uncl...
PMC10212792
core_pubmed_pmc
A detailed biochemical characterization, toxicological assessment and molecular docking studies of Launaea fragilis : An important medicinal xero-halophyte
A detailed biochemical characterization, toxicological assessment and molecular docking studies of Launaea fragilis : An important medicinal xero-halophyte Abstract Abstract Launaea fragilis (Asso) Pau (Family: Asteraceae) is a wild medicinal plant that has been used in the folklore as a potential treatment for numerou...
PMC4622453
core_pubmed_pmc
Brivaracetam: review of its pharmacology and potential use as adjunctive therapy in patients with partial onset seizures
Brivaracetam: review of its pharmacology and potential use as adjunctive therapy in patients with partial onset seizures Abstract Abstract Brivaracetam (BRV), a high-affinity synaptic vesicle protein 2A ligand, reported to be 10–30-fold more potent than levetiracetam (LEV), is highly effective in a wide range of experi...
PMC11253374
core_pubmed_pmc
Modelling the nicotine pharmacokinetic profile for e-cigarettes using real time monitoring of consumers’ physiological measurements and mouth level exposure
Modelling the nicotine pharmacokinetic profile for e-cigarettes using real time monitoring of consumers’ physiological measurements and mouth level exposure Abstract Abstract Pharmacokinetic (PK) studies can provide essential information on abuse liability of nicotine and tobacco products but are intrusive and must be ...
PMC12775995
core_pubmed_pmc
Synthesis, characterization, and anticancer evaluation of N- Heterocyclic entities: ADME profiling and In Silico predictions
Synthesis, characterization, and anticancer evaluation of N- Heterocyclic entities: ADME profiling and In Silico predictions Abstract This study aimed to synthesize a novel series of N -heterocyclic compounds and evaluate their integrated pharmacological potential by coupling in vitro selective cytotoxicity on tumor an...
PMC4816034
core_pubmed_pmc
Tolerability and pharmacokinetics of oxaloacetate 100 mg capsules in Alzheimer's subjects
Tolerability and pharmacokinetics of oxaloacetate 100 mg capsules in Alzheimer's subjects Abstract Abstract Bioenergetics and bioenergetic-related functions are altered in Alzheimer's disease (AD) subjects. These alterations represent therapeutic targets and provide an underlying rationale for modifying brain bioenerge...
PMC7719384
core_pubmed_pmc
Febuxostat, But Not Allopurinol, Markedly Raises the Plasma Concentrations of the Breast Cancer Resistance Protein Substrate Rosuvastatin
Febuxostat, But Not Allopurinol, Markedly Raises the Plasma Concentrations of the Breast Cancer Resistance Protein Substrate Rosuvastatin Abstract Xanthine oxidase inhibitors febuxostat and allopurinol are commonly used in the treatment of gout. Febuxostat inhibits the breast cancer resistance protein (BCRP) in vitro ....
PMC8492975
core_pubmed_pmc
Methylprednisolone in Pediatric Cardiac Surgery: Is There Enough Evidence?
Methylprednisolone in Pediatric Cardiac Surgery: Is There Enough Evidence? Abstract Abstract Corticosteroids have been used to decrease the inflammatory response to cardiac surgery and cardiopulmonary bypass in children for decades. Sparse information is present concerning the pharmacokinetics and pharmacodynamics of c...
PMC4615734
core_pubmed_pmc
First-in-human uPAR PET: Imaging of Cancer Aggressiveness
First-in-human uPAR PET: Imaging of Cancer Aggressiveness Abstract A first-in-human clinical trial with Positron Emission Tomography (PET) imaging of the urokinase-type plasminogen activator receptor (uPAR) in patients with breast, prostate and bladder cancer, is described. uPAR is expressed in many types of human canc...
PMC6913762
core_pubmed_pmc
Drug–Drug Interactions Of Amiodarone And Quinidine On The Pharmacokinetics Of Eliglustat In Rats
Drug–Drug Interactions Of Amiodarone And Quinidine On The Pharmacokinetics Of Eliglustat In Rats Abstract Background Eliglustat, a new oral substrate-reduction therapy, was recently approved as a first-line therapy for Gaucher's disease type 1 (GD1) patients. Purpose The purpose of the present study was to develop and ...
PMC4996894
core_pubmed_pmc
Lack of Effect of Vortioxetine on the Pharmacokinetics and Pharmacodynamics of Ethanol, Diazepam, and Lithium
Lack of Effect of Vortioxetine on the Pharmacokinetics and Pharmacodynamics of Ethanol, Diazepam, and Lithium Abstract Introduction Because the multimodal antidepressant vortioxetine is likely to be coadministered with other central nervous system (CNS)-active drugs, potential drug–drug interactions warrant examination...
PMC6944222
core_pubmed_pmc
Development and Application of a Life-Stage Physiologically Based Pharmacokinetic (PBPK) Model to the Assessment of Internal Dose of Pyrethroids in Humans
Development and Application of a Life-Stage Physiologically Based Pharmacokinetic (PBPK) Model to the Assessment of Internal Dose of Pyrethroids in Humans Abstract Abstract To address concerns around age-related sensitivity to pyrethroids, a life-stage physiologically based pharmacokinetic (PBPK) model, supported by in...
PMC12952245
core_pubmed_pmc
Phase 1 clinical trial of the ataxia telangiectasia and Rad3-related inhibitor berzosertib with irinotecan in patients with advanced solid tumors (ETCTN 9938)
Phase 1 clinical trial of the ataxia telangiectasia and Rad3-related inhibitor berzosertib with irinotecan in patients with advanced solid tumors (ETCTN 9938) Abstract Abstract Background: Ataxia telangiectasia and Rad3-related (ATR) inhibition with berzosertib potentiates the efficacy of irinotecan in preclinical mode...
PMC10832099
core_pubmed_pmc
Two rare flavonoid glycosides from Litsea glutinosa (Lour.) C. B. Rob.: experimental and computational approaches endorse antidiabetic potentiality
Two rare flavonoid glycosides from Litsea glutinosa (Lour.) C. B. Rob.: experimental and computational approaches endorse antidiabetic potentiality Abstract Background Litsea glutinosa (Lour.) C. B. Rob. belongs to the Litsea genus and is categorized under the family of Lauraceae . The study aimed to investigate the ph...
PMC5500557
core_pubmed_pmc
Determining optimal dosing regimen of oral administration of dicloxacillin using Monte Carlo simulation
Determining optimal dosing regimen of oral administration of dicloxacillin using Monte Carlo simulation Abstract Background Dicloxacillin, a semisynthetic isoxazolyl penicillin, exhibits antimicrobial activity against a wide variety of Gram-positive bacteria, as well as stability against penicillinases and low level of...
PMC10188401
core_pubmed_pmc
Ravulizumab pharmacokinetics and pharmacodynamics in patients with generalized myasthenia gravis
Ravulizumab pharmacokinetics and pharmacodynamics in patients with generalized myasthenia gravis Abstract Abstract Introduction The terminal complement C5 inhibitor ravulizumab has a long elimination half-life, allowing maintenance dosing every 8 weeks. In the 26-week, double-blind, randomized, placebo-controlled perio...
PMC5080817
core_pubmed_pmc
Dynamic Contrast-Enhanced Magnetic Resonance Imaging as a Surrogate Biomarker for Bevacizumab in Colorectal Cancer Liver Metastasis: A Single-Arm, Exploratory Trial
Dynamic Contrast-Enhanced Magnetic Resonance Imaging as a Surrogate Biomarker for Bevacizumab in Colorectal Cancer Liver Metastasis: A Single-Arm, Exploratory Trial Abstract Purpose The purpose of this study is to investigate dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) and plasma cytokines and angiog...
PMC10459920
core_pubmed_pmc
Efficacy, Pharmacokinetics, and Toxicity Profiles of a Broad Anti-SARS-CoV-2 Neutralizing Antibody
Efficacy, Pharmacokinetics, and Toxicity Profiles of a Broad Anti-SARS-CoV-2 Neutralizing Antibody Abstract Abstract We recently reported the isolation and characterization of an anti-SARS-CoV-2 antibody, called IgG-A7, that protects transgenic mice expressing the human angiotensin-converting enzyme 2 (hACE-2) from an ...
PMC8868383
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Key Components of a Standardized Centella asiatica Product in Cognitively Impaired Older Adults: A Phase 1, Double-Blind, Randomized Clinical Trial
Pharmacokinetics and Pharmacodynamics of Key Components of a Standardized Centella asiatica Product in Cognitively Impaired Older Adults: A Phase 1, Double-Blind, Randomized Clinical Trial Abstract Abstract Centella asiatica is reputed in Eastern medicine to improve cognitive function in humans. Preclinical studies hav...
PMC4487954
core_pubmed_pmc
Laparoscopic Salpingo-oophorectomy in Conscious Sedation
Laparoscopic Salpingo-oophorectomy in Conscious Sedation Abstract Introduction: Conscious sedation has traditionally been used for laparoscopic tubal ligation. General anesthesia with endotracheal intubation may be associated with side effects, such as nausea, vomiting, cough, and dizziness, whereas sedation offers the...
PMC10780175
core_pubmed_pmc
In Silico and In Vivo Pharmacokinetic Evaluation of 84-B10, a Novel Drug Candidate against Acute Kidney Injury and Chronic Kidney Disease
In Silico and In Vivo Pharmacokinetic Evaluation of 84-B10, a Novel Drug Candidate against Acute Kidney Injury and Chronic Kidney Disease Abstract Acute kidney injury (AKI) and chronic kidney disease (CKD) have become public health problems due to high morbidity and mortality. Currently, drugs recommended for patients ...
PMC3750714
core_pubmed_pmc
Tinzaparin and other low-molecular-weight heparins: what is the evidence for differential dependence on renal clearance?
Tinzaparin and other low-molecular-weight heparins: what is the evidence for differential dependence on renal clearance? Abstract Abstract Since low-molecular-weight heparins (LMWHs) are eliminated preferentially via the kidneys, the potential for accumulation of these agents (and an increased risk of bleeding) is of p...
PMC8055417
core_pubmed_pmc
Network Pharmacology and Molecular Docking Suggest the Mechanism for Biological Activity of Rosmarinic Acid
Network Pharmacology and Molecular Docking Suggest the Mechanism for Biological Activity of Rosmarinic Acid Abstract Abstract Rosmarinic acid (RosA) is a natural phenolic acid compound, which is mainly extracted from Labiatae and Arnebia . At present, there is no systematic analysis of its mechanism. Therefore, we used...
PMC6710810
core_pubmed_pmc
Effects of Xuesaitong on the Pharmacokinetics of Losartan: An In Vivo UPLC-MS/MS Study
Effects of Xuesaitong on the Pharmacokinetics of Losartan: An In Vivo UPLC-MS/MS Study Abstract Abstract The aim of this study was to examine whether Xuesaitong, a multiherbal formulation for coronary heart disease, alters the pharmacokinetics of losartan. Adult male Sprague Dawley rats randomly received losartan (10 m...
PMC6027739
core_pubmed_pmc
Confidence and Prediction Intervals for Pharmacometric Models
Confidence and Prediction Intervals for Pharmacometric Models Abstract Abstract Supporting decision making in drug development is a key purpose of pharmacometric models. Pharmacokinetic models predict exposures under alternative posologies or in different populations. Pharmacodynamic models predict drug effects based o...
PMC9523648
core_pubmed_pmc
Teaching resources for the European Open Platform for Prescribing Education (EurOP 2 E)—a nominal group technique study
Teaching resources for the European Open Platform for Prescribing Education (EurOP 2 E)—a nominal group technique study Abstract The European Open Platform for Prescribing Education (EurOP 2 E) seeks to improve and harmonize European clinical pharmacology and therapeutics (CPT) education by facilitating international c...
PMC8434701
core_pubmed_pmc
PEGylated recombinant human hyaluronidase (PEGPH20) pre-treatment improves intra-tumour distribution and efficacy of paclitaxel in preclinical models
PEGylated recombinant human hyaluronidase (PEGPH20) pre-treatment improves intra-tumour distribution and efficacy of paclitaxel in preclinical models Abstract Abstract Background Scarce drug penetration in solid tumours is one of the possible causes of the limited efficacy of chemotherapy and is related to the altered ...
PMC6382135
core_pubmed_pmc
Metal based donepezil analogues designed to inhibit human acetylcholinesterase for Alzheimer’s disease
Metal based donepezil analogues designed to inhibit human acetylcholinesterase for Alzheimer’s disease Abstract Abstract Among neurodegenerative disorders, Alzheimer’s disease (AD) is one of the most common disorders showing slow progressive cognitive decline. Targeting acetylcholinesterase (AChE) is one of the major s...
PMC4226840
core_pubmed_pmc
An open-label study to determine the maximum tolerated dose of the multitargeted tyrosine kinase inhibitor CEP-11981 in patients with advanced cancer
An open-label study to determine the maximum tolerated dose of the multitargeted tyrosine kinase inhibitor CEP-11981 in patients with advanced cancer Abstract Summary Background This phase I study evaluated the pharmacokinetics and pharmacodynamics of CEP-11981, an oral vascular endothelial growth factor (VEGF) tyrosin...
PMC11380098
core_pubmed_pmc
Drug-Drug Interactions and the Clinical Tolerability of Colchicine Among Patients With COVID-19
Drug-Drug Interactions and the Clinical Tolerability of Colchicine Among Patients With COVID-19 Abstract Key Points Question Are drug-drug interactions associated with the clinical safety and efficacy of colchicine in people with COVID-19? Findings In this secondary analysis of the COLCORONA trial including 4432 patien...
PMC11842173
core_pubmed_pmc
Why the racing industry and equestrian disciplines need to implement population pharmacokinetics: To learn, explain, summarize, harmonize, and individualize
Why the racing industry and equestrian disciplines need to implement population pharmacokinetics: To learn, explain, summarize, harmonize, and individualize Abstract Abstract Population pharmacokinetics (POP PK) is a powerful pharmacokinetic tool, which measures quantitatively, and explains the variability in drug expo...
PMC5018035
core_pubmed_pmc
Pharmacokinetics of heroin and its metabolites in vitreous humor and blood in a living pig model
Pharmacokinetics of heroin and its metabolites in vitreous humor and blood in a living pig model Abstract Abstract Vitreous humor (VH) is an alternative matrix for drug analysis in forensic toxicology. However, little is known about the distribution of xenobiotics, such as opioids, into VH in living organisms. The aim ...
PMC9953069
core_pubmed_pmc
Molecular Screening of Bioactive Compounds of Garlic for Therapeutic Effects against COVID-19
Molecular Screening of Bioactive Compounds of Garlic for Therapeutic Effects against COVID-19 Abstract Abstract An outbreak of pneumonia occurred on December 2019 in Wuhan, China, which caused a serious public health emergency by spreading around the globe. Globally, natural products are being focused on more than synt...
PMC5996271
core_pubmed_pmc
Ibogaine Detoxification Transitions Opioid and Cocaine Abusers Between Dependence and Abstinence: Clinical Observations and Treatment Outcomes
Ibogaine Detoxification Transitions Opioid and Cocaine Abusers Between Dependence and Abstinence: Clinical Observations and Treatment Outcomes Abstract Abstract Ibogaine may be effective for transitioning opioid and cocaine dependent individuals to sobriety. American and European self-help groups provided public testim...
PMC10069847
core_pubmed_pmc
Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study
Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study Abstract Abstract Background Long-acting (LA) intramuscular cabotegravir and rilpivirine are prone to drug-drug interactions (DDI). However, given the long dosing interval, ...
PMC11292200
core_pubmed_pmc
Exposure–Response and Subgroup Analyses to Support Body Weight–Based Dosing of Brentuximab Vedotin in Children and Young Adults with Newly Diagnosed High-risk Classical Hodgkin Lymphoma
Exposure–Response and Subgroup Analyses to Support Body Weight–Based Dosing of Brentuximab Vedotin in Children and Young Adults with Newly Diagnosed High-risk Classical Hodgkin Lymphoma Abstract Abstract Purpose: The purpose of the study was to evaluate the relationships between brentuximab vedotin (BV) pharmacokinetic...
PMC3191584
core_pubmed_pmc
Pharmacokinetic research in children: an analysis of registered records of clinical trials
Pharmacokinetic research in children: an analysis of registered records of clinical trials Abstract Background Reported off-label/unlicensed prescribing rates in children range from 11% to 80%. Research into pharmacokinetic profiles of children's medicines is essential in the creation of more knowledge on the safety an...
PMC12775819
core_pubmed_pmc
Optimizing PSMA-617-based inhibitors through charged linker modifications: Insights into structure-activity relationships
Optimizing PSMA-617-based inhibitors through charged linker modifications: Insights into structure-activity relationships Abstract Abstract Rationale: The introduction of Pluvicto ® ([ 177 Lu]Lu-vipivotide tetraxetan; [ 177 Lu]Lu-PSMA-617) marks a milestone in radioligand therapy (RLT) for PSMA-positive metastatic cast...
PMC12511116
core_pubmed_pmc
Neurotherapeutics across blood–brain barrier: screening of BBB-permeable and CNS-active molecules for neurodegenerative disease
Neurotherapeutics across blood–brain barrier: screening of BBB-permeable and CNS-active molecules for neurodegenerative disease Abstract Neurotherapeutics that are effective in the central nervous system (CNS) of the brain require an accurate estimation of their uptake across the blood–brain barrier (BBB), a highly sel...
PMC9099119
core_pubmed_pmc
Pharmacokinetics, safety, and simulated efficacy of an influenza treatment, baloxavir marboxil, in Chinese individuals
Pharmacokinetics, safety, and simulated efficacy of an influenza treatment, baloxavir marboxil, in Chinese individuals Abstract Abstract Baloxavir marboxil is an endonuclease inhibitor indicated for the treatment of influenza in patients ≥12 years. No data exist for Chinese patients in global studies. This randomized, ...