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PMC12473563
core_pubmed_pmc
An In Vitro–In Vivo Comparison of Two Levodopa Dry Powder Products for Inhalation: A Randomized Trial Comparing Inbrija and Levodopa Cyclops
An In Vitro–In Vivo Comparison of Two Levodopa Dry Powder Products for Inhalation: A Randomized Trial Comparing Inbrija and Levodopa Cyclops Abstract Background/Objectives : The pulmonary administration of levodopa enables a rapid absorption and onset of action, making it a suitable administration route for managing OF...
PMC12668587
core_pubmed_pmc
Remimazolam in elderly patients undergoing EBUS-TBNA: protocol for a randomized clinical trial
Remimazolam in elderly patients undergoing EBUS-TBNA: protocol for a randomized clinical trial Abstract Abstract Background: Endobronchial ultrasound-guided transbronchial needle aspiration (EBUS-TBNA) remains the diagnostic benchmark for mediastinal staging, though geriatric patients require optimized anesthesia due t...
PMC6175428
core_pubmed_pmc
Pharmacokinetics, Safety, and Tolerability of Oral Semaglutide in Subjects With Hepatic Impairment
Pharmacokinetics, Safety, and Tolerability of Oral Semaglutide in Subjects With Hepatic Impairment Abstract Abstract Semaglutide is a human glucagon‐like peptide‐1 analog that has been co‐formulated with the absorption enhancer, sodium N‐(8‐[2‐hydroxybenzoyl] amino) caprylate, for oral administration. This trial ( NCT0...
PMC11458730
core_pubmed_pmc
Serious gaming as potential training tool for recognition of adverse drug reactions: side-effect exposure—medical education ( SeeMe )
Serious gaming as potential training tool for recognition of adverse drug reactions: side-effect exposure—medical education ( SeeMe ) Abstract Abstract Purpose The recognition of adverse drug reactions (ADRs) is an important part of daily clinical work. However, medical education in this field is mostly drug-based and ...
PMC8226464
core_pubmed_pmc
Meta-Assessment of Metformin Absorption and Disposition Pharmacokinetics in Nine Species
Meta-Assessment of Metformin Absorption and Disposition Pharmacokinetics in Nine Species Abstract The objective of this study was to systematically assess literature datasets and quantitatively analyze metformin PK in plasma and some tissues of nine species. The pharmacokinetic (PK) parameters and profiles of metformin...
PMC9797722
core_pubmed_pmc
Pharmacokinetics of esomeprazole in goats ( Capra aegagrus hircus ) after intravenous and subcutaneous administration
Pharmacokinetics of esomeprazole in goats ( Capra aegagrus hircus ) after intravenous and subcutaneous administration Abstract Abstract Background Stressed and hospitalized goats are at risk of developing abomasal (gastric) ulceration, but there is a paucity of pharmacokinetic studies for proton pump inhibiting drugs, ...
PMC10044060
core_pubmed_pmc
Disulfiram: Mechanisms, Applications, and Challenges
Disulfiram: Mechanisms, Applications, and Challenges Abstract Background : Since disulfiram’s discovery in the 1940s and its FDA approval for alcohol use disorder, other indications have been investigated. This review describes potential clinical applications, associated risks, and challenges. Methods : For this narrat...
PMC7034140
core_pubmed_pmc
A review of clinical studies involving pregnant women registered in the Clinical Trials Registry of India
A review of clinical studies involving pregnant women registered in the Clinical Trials Registry of India Abstract Abstract Context and Aims: Pregnant women undergo physiological changes which influence the efficacy as well as safety of medications used. Very few drugs are tested and approved for medical conditions dur...
PMC5286499
core_pubmed_pmc
Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model
Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model Abstract The efficacy of HIV pre-exposure prophylaxis (PrEP) relies on adherence and may also depend on the route of HIV acquisition. Clinical studies of systemic tenofovir disoproxil fumarate (T...
PMC9940918
core_pubmed_pmc
Efficacy of nirsevimab against respiratory syncytial virus lower respiratory tract infections in preterm and term infants, and pharmacokinetic extrapolation to infants with congenital heart disease and chronic lung disease: a pooled analysis of randomised controlled trials
Efficacy of nirsevimab against respiratory syncytial virus lower respiratory tract infections in preterm and term infants, and pharmacokinetic extrapolation to infants with congenital heart disease and chronic lung disease: a pooled analysis of randomised controlled trials Abstract Background In a phase 2b trial and th...
PMC2905413
core_pubmed_pmc
Effect of cigarette smoking on the washout time of sevoflurane anesthesia
Effect of cigarette smoking on the washout time of sevoflurane anesthesia Abstract Abstract Background Cigarette smoking affects the pharmacodynamic and pharmacokinetic behavior of many drugs and causes deterioration of pulmonary mechanics. We have evaluated the effect of cigarette smoking on washout time after one min...
PMC9098428
core_pubmed_pmc
Clinical safety and pharmacokinetic evaluation of aqueous extract of Cocculus hirsutus, an anti-viral phytopharmacetical drug as a potential for the treatment of dengue and COVID-19
Clinical safety and pharmacokinetic evaluation of aqueous extract of Cocculus hirsutus, an anti-viral phytopharmacetical drug as a potential for the treatment of dengue and COVID-19 Abstract Background and aim Dengue a worldwide concern for public health has no effective vaccine or drug available for its prevention or ...
PMC8835305
core_pubmed_pmc
The Optimized Delivery of Triterpenes by Liposomal Nanoformulations: Overcoming the Challenges
The Optimized Delivery of Triterpenes by Liposomal Nanoformulations: Overcoming the Challenges Abstract Abstract The last decade has witnessed a sustained increase in the research development of modern-day chemo-therapeutics, especially for those used for high mortality rate pathologies. However, the therapeutic landsc...
PMC12314070
core_pubmed_pmc
A broad-spectrum antibiotic targets multiple-drug-resistant bacteria with dual binding targets and no detectable resistance
A broad-spectrum antibiotic targets multiple-drug-resistant bacteria with dual binding targets and no detectable resistance Abstract The rapid emergence of difficult-to-treat multidrug-resistant pathogens, combined with the scarcity of antibiotics possessing novel mechanisms, poses a significant threat to global public...
PMC8451516
core_pubmed_pmc
Once- Versus Twice-Daily Angiotensin-Converting Enzyme Inhibitors for Blood Pressure Control in Adult Patients With Hypertension
Once- Versus Twice-Daily Angiotensin-Converting Enzyme Inhibitors for Blood Pressure Control in Adult Patients With Hypertension Abstract This review aimed to assess the efficacy and safety of once- versus twice-daily administration of angiotensin-converting enzyme (ACE) inhibitors for the management of hypertension. A...
PMC8231794
core_pubmed_pmc
The Role of Non-Enzymatic Degradation of Meropenem—Insights from the Bottle to the Body
The Role of Non-Enzymatic Degradation of Meropenem—Insights from the Bottle to the Body Abstract Several studies have addressed the poor stability of meropenem in aqueous solutions, though not considering the main degradation product, the open-ring metabolite (ORM) form. In the present work, we elucidate the metabolic ...
PMC4148150
core_pubmed_pmc
Optimized Inhibitors of Soluble Epoxide Hydrolase Improve in Vitro Target Residence Time and in Vivo Efficacy
Optimized Inhibitors of Soluble Epoxide Hydrolase Improve in Vitro Target Residence Time and in Vivo Efficacy Abstract Abstract Diabetes is affecting the life of millions of people. A large proportion of diabetic patients suffer from severe complications such as neuropathic pain, and current treatments for these compli...
PMC7557832
core_pubmed_pmc
Impact of Albumin and Omeprazole on Steady-State Population Pharmacokinetics of Voriconazole and Development of a Voriconazole Dosing Optimization Model in Thai Patients with Hematologic Diseases
Impact of Albumin and Omeprazole on Steady-State Population Pharmacokinetics of Voriconazole and Development of a Voriconazole Dosing Optimization Model in Thai Patients with Hematologic Diseases Abstract Abstract This study aimed to identify factors that significantly influence the pharmacokinetics of voriconazole in ...
PMC9525089
core_pubmed_pmc
Potency of the novel PolC DNA polymerase inhibitor CRS0540 in a disseminated Listeria monocytogenes intracellular hollow-fibre model
Potency of the novel PolC DNA polymerase inhibitor CRS0540 in a disseminated Listeria monocytogenes intracellular hollow-fibre model Abstract Abstract Background Listeriosis is an orphan disease, which is nevertheless fatal in immunocompromised people. CRS0540 is a novel PolC DNA polymerase inhibitor that has demonstra...
PMC10355117
core_pubmed_pmc
Review of adult gender transition medications: mechanisms, efficacy measures, and pharmacogenomic considerations
Review of adult gender transition medications: mechanisms, efficacy measures, and pharmacogenomic considerations Abstract Abstract Gender dysphoria is the imparity between a person’s experienced gender and their birth-assigned gender. Gender transition is the process of adapting a person’s sexual characteristics to mat...
PMC9087820
core_pubmed_pmc
Metabolism and pharmacokinetics of medium chain fatty acids after oral administration of royal jelly to healthy subjects
Metabolism and pharmacokinetics of medium chain fatty acids after oral administration of royal jelly to healthy subjects Abstract Abstract The unique fatty acids in royal jelly (RJ), 10-hydroxy-2-decenoic acid and 10-hydroxydecanoic acid are expected to be associated with many health benefits, but little is known on th...
PMC9251517
core_pubmed_pmc
Dosing Regimens of Immune Checkpoint Inhibitors: Attempts at Lower Dose, Less Frequency, Shorter Course
Dosing Regimens of Immune Checkpoint Inhibitors: Attempts at Lower Dose, Less Frequency, Shorter Course Abstract Abstract Immune checkpoint inhibitors (ICIs) are a revolutionary breakthrough in the field of cancer by modulating patient’s own immune system to exert anti-tumor effects. The clinical application of ICIs is...
PMC5914322
core_pubmed_pmc
A Novel Chronic Opioid Monitoring Tool to Assess Prescription Drug Steady State Levels in Oral Fluid
A Novel Chronic Opioid Monitoring Tool to Assess Prescription Drug Steady State Levels in Oral Fluid Abstract Abstract Objective Interpretation limitations of urine drug testing and the invasiveness of blood toxicology have motivated the desire for the development of simpler methods to assess biologically active drug l...
PMC11279551
core_pubmed_pmc
Pharmacokinetics and Enterohepatic Circulation of 2-(Quinoline-8-carboxamido)benzoic Acid (2-QBA) in Mice
Pharmacokinetics and Enterohepatic Circulation of 2-(Quinoline-8-carboxamido)benzoic Acid (2-QBA) in Mice Abstract Abstract The quinoline alkaloid 2-(quinoline-8-carboxamido)benzoic acid (2-QBA), which is isolated from Aspergillus sp. SCSIO06786, a deep sea-derived fungus, has been suggested as a therapeutic candidate ...
PMC6820739
core_pubmed_pmc
dendPoint: a web resource for dendrimer pharmacokinetics investigation and prediction
dendPoint: a web resource for dendrimer pharmacokinetics investigation and prediction Abstract Nanomedicine development currently suffers from a lack of efficient tools to predict pharmacokinetic behavior without relying upon testing in large numbers of animals, impacting success rates and development costs. This work ...
PMC7915865
core_pubmed_pmc
Pharmacokinetics and Safety of Rifamycin SV after Single and Multiple Doses of MMX ® Modified Release Tablets in Healthy Male and Female Volunteers
Pharmacokinetics and Safety of Rifamycin SV after Single and Multiple Doses of MMX ® Modified Release Tablets in Healthy Male and Female Volunteers Abstract Abstract The primary objective of this single- and multiple-dose pharmacokinetic study was the investigation of rifamycin SV’s pharmacokinetic profile in plasma an...
PMC12963441
core_pubmed_pmc
Safety and biologic activity of a bispecific T cell receptor targeting HIV Gag in males living with HIV: a first-in-human trial
Safety and biologic activity of a bispecific T cell receptor targeting HIV Gag in males living with HIV: a first-in-human trial Abstract HIV persistence in reservoirs despite antiretroviral therapy (ART) is a barrier to a permanent cure. We present the affinity-enhanced TCR bispecific IMC-M113V as a potential therapeut...
PMC8426472
core_pubmed_pmc
Optimized pharmacological control over the AAV-Gene-Switch vector for regulable gene therapy
Optimized pharmacological control over the AAV-Gene-Switch vector for regulable gene therapy Abstract Gene therapy in its current design is an irreversible process. It cannot be stopped in case of unwanted side effects, nor can expression levels of therapeutics be adjusted to individual patient’s needs. Thus, the Gene-...
PMC6161187
core_pubmed_pmc
Clopidogrel Pharmacokinetics in Malaysian Population Groups: The Impact of Inter-Ethnic Variability
Clopidogrel Pharmacokinetics in Malaysian Population Groups: The Impact of Inter-Ethnic Variability Abstract Malaysia is a multi-ethnic society whereby the impact of pharmacogenetic differences between ethnic groups may contribute significantly to variability in clinical therapy. One of the leading causes of mortality ...
PMC10955231
core_pubmed_pmc
Assessing the relative contribution of CYP3A-and P-gp-mediated pathways to the overall disposition and drug-drug interaction of dabigatran etexilate using a comprehensive mechanistic physiological-based pharmacokinetic model
Assessing the relative contribution of CYP3A-and P-gp-mediated pathways to the overall disposition and drug-drug interaction of dabigatran etexilate using a comprehensive mechanistic physiological-based pharmacokinetic model Abstract Dabigatran etexilate (DABE) is a clinical probe substrate for studying drug-drug inter...
PMC4965493
core_pubmed_pmc
Population pharmacokinetics of bevacizumab in cancer patients with external validation
Population pharmacokinetics of bevacizumab in cancer patients with external validation Abstract Background Bevacizumab is approved for various cancers. This analysis aimed to comprehensively evaluate bevacizumab pharmacokinetics and the influence of patient variables on bevacizumab pharmacokinetics. Methods Rich and sp...
PMC7499191
core_pubmed_pmc
Phase II Dose Selection for Alpha Synuclein–Targeting Antibody Cinpanemab (BIIB054) Based on Target Protein Binding Levels in the Brain
Phase II Dose Selection for Alpha Synuclein–Targeting Antibody Cinpanemab (BIIB054) Based on Target Protein Binding Levels in the Brain Abstract Abstract This modeling and simulation analysis was aimed at selecting doses of cinpanemab (BIIB054), a monoclonal antibody targeting aggregated α‐synuclein, for a phase II stu...
PMC7866158
core_pubmed_pmc
Evaluation of Poorly Soluble Drugs’ Dissolution Rate by Laser Scattering in Different Water Isotopologues
Evaluation of Poorly Soluble Drugs’ Dissolution Rate by Laser Scattering in Different Water Isotopologues Abstract Abstract The most important task in the design of dosage forms is to modify the pharmaceutical substances structure in order to increase solubilization, targeted delivery, controlled rate of drug administr...
PMC7794963
core_pubmed_pmc
Nanomedicine Reformulation of Chloroquine and Hydroxychloroquine
Nanomedicine Reformulation of Chloroquine and Hydroxychloroquine Abstract The chloroquine family of antimalarials has a long history of use, spanning many decades. Despite this extensive clinical experience, novel applications, including use in autoimmune disorders, infectious disease, and cancer, have only recently be...
PMC12555105
core_pubmed_pmc
Intranasal Naloxone During Recurrent Exercise in Individuals with Type‐1 Diabetes Mellitus: Evaluation of the Clinical Predictors of Pharmacokinetics and Exposure–Response
Intranasal Naloxone During Recurrent Exercise in Individuals with Type‐1 Diabetes Mellitus: Evaluation of the Clinical Predictors of Pharmacokinetics and Exposure–Response Abstract Abstract Impaired awareness of hypoglycemia (IAH) impacts 25%‐30% of individuals with type 1 diabetes mellitus (T1D), potentially leading t...
PMC8765319
core_pubmed_pmc
Pharmacokinetics of Oral Formulations of Gepotidacin (GSK2140944), a Triazaacenaphthylene Bacterial Type II Topoisomerase Inhibitor, in Healthy Adult and Adolescent Participants
Pharmacokinetics of Oral Formulations of Gepotidacin (GSK2140944), a Triazaacenaphthylene Bacterial Type II Topoisomerase Inhibitor, in Healthy Adult and Adolescent Participants Abstract ABSTRACT Gepotidacin is a novel, first-in-class triazaacenaphthylene antibiotic that may provide a new treatment option for antibioti...
PMC6561985
core_pubmed_pmc
Sunitinib in pediatric patients with advanced gastrointestinal stromal tumor: results from a phase I/II trial
Sunitinib in pediatric patients with advanced gastrointestinal stromal tumor: results from a phase I/II trial Abstract Background Sunitinib is approved for treatment of adults with imatinib-resistant gastrointestinal stromal tumor (GIST) or imatinib intolerance. Methods This single-arm, multicenter, multinational phase...
PMC7201409
core_pubmed_pmc
Fixed Dosing of Liposomal Amphotericin B in Morbidly Obese Individuals
Fixed Dosing of Liposomal Amphotericin B in Morbidly Obese Individuals Abstract Abstract In this prospective study, we examined the pharmacokinetics of 1 and 2 mg/kg liposomal amphotericin B in 16 morbidly obese individuals (104–177 kg). Body size had no effect on clearance. We recommend a fixed dose in patients ≥100 k...
PMC9720949
core_pubmed_pmc
Prediction of polyreactive and nonspecific single-chain fragment variables through structural biochemical features and protein language-based descriptors
Prediction of polyreactive and nonspecific single-chain fragment variables through structural biochemical features and protein language-based descriptors Abstract Background Monoclonal antibodies (mAbs) have been used as therapeutic agents, which must overcome many developability issues after the discovery from in vitr...
PMC7992791
core_pubmed_pmc
Provider perspectives on beta-lactam therapeutic drug monitoring programs in the critically ill: a protocol for a multicenter mixed-methods study
Provider perspectives on beta-lactam therapeutic drug monitoring programs in the critically ill: a protocol for a multicenter mixed-methods study Abstract Abstract Background Beta-lactams (i.e., penicillins, cephalosporins, carbapenems, monobactams) are the most widely used class of antibiotics in critically ill patien...
PMC8759125
core_pubmed_pmc
Phase 1b study of the BET protein inhibitor RO6870810 with venetoclax and rituximab in patients with diffuse large B-cell lymphoma
Phase 1b study of the BET protein inhibitor RO6870810 with venetoclax and rituximab in patients with diffuse large B-cell lymphoma Abstract Key Points BET inhibitor RO6870810+venetoclax+rituximab has a manageable safety profile in relapsed/refractory diffuse large B-cell lymphoma. A clinically relevant signal of antitu...
PMC8261257
core_pubmed_pmc
In vitro - in vivo - in silico approach in the development of inhaled drug products: Nanocrystal-based formulations with budesonide as a model drug
In vitro - in vivo - in silico approach in the development of inhaled drug products: Nanocrystal-based formulations with budesonide as a model drug Abstract Abstract This study aims to understand the absorption patterns of three different kinds of inhaled formulations via in silico modeling using budesonide (BUD) as a ...
PMC5404400
core_pubmed_pmc
TX-004HR vaginal estradiol has negligible to very low systemic absorption of estradiol
TX-004HR vaginal estradiol has negligible to very low systemic absorption of estradiol Abstract Abstract Objective: To evaluate the pharmacokinetics of TX-004HR vaginal estradiol softgel capsules when used for treating moderate-to-severe dyspareunia in postmenopausal women with vulvar and vaginal atrophy. Methods: A su...
PMC11563624
core_pubmed_pmc
Selective protease inhibitors from secondary metabolites of Philippine medicinal plants against porcine epidemic diarrhea virus: A computational veterinary drug discovery approach
Selective protease inhibitors from secondary metabolites of Philippine medicinal plants against porcine epidemic diarrhea virus: A computational veterinary drug discovery approach Abstract Abstract Background: Porcine epidemic diarrhea virus (PEDV) is a recurring coronavirus that causes severe diarrhea in pigs with hig...
PMC10800175
core_pubmed_pmc
Pharmacodynamic effects of molidustat on erythropoiesis in healthy cats
Pharmacodynamic effects of molidustat on erythropoiesis in healthy cats Abstract Abstract Background Inhibition of hypoxia‐inducible factor prolyl hydroxylase (HIF‐PH) stimulates erythropoiesis in rats, dogs, monkeys, and humans. Hypothesis/Objective Determine if molidustat, a novel HIF‐PH inhibitor, stimulates erythro...
PMC9312292
core_pubmed_pmc
Administration of Altrenogest to Maintain Pregnancy in Asian Elephants ( Elephas maximus )
Administration of Altrenogest to Maintain Pregnancy in Asian Elephants ( Elephas maximus ) Abstract Abstract Simple Summary The Asian Elephant ( Elephas maximus ) is an IUCN (International Union of the Conservation of Nature) Endangered species that has interacted with humans for centuries. Despite advances in captive ...
PMC6150365
core_pubmed_pmc
Simultaneous Determination of Seven Components in Rat Plasma by the UPLC-MS/MS Method and Application of Pharmacokinetic Studies to SimiaoYong’an Decoction
Simultaneous Determination of Seven Components in Rat Plasma by the UPLC-MS/MS Method and Application of Pharmacokinetic Studies to SimiaoYong’an Decoction Abstract SimiaoYong’an Decoction (SYD) is a classical traditional Chinese prescription that is used for the treatment of gangrene, heat-clearing, detoxification and...
PMC7891399
core_pubmed_pmc
Effect of Pregnancy and Concomitant Antiretrovirals on the Pharmacokinetics of Tenofovir in Women With HIV Receiving Tenofovir Disoproxil Fumarate‐Based Antiretroviral Therapy Versus Women With HBV Receiving Tenofovir Disoproxil Fumarate Monotherapy
Effect of Pregnancy and Concomitant Antiretrovirals on the Pharmacokinetics of Tenofovir in Women With HIV Receiving Tenofovir Disoproxil Fumarate‐Based Antiretroviral Therapy Versus Women With HBV Receiving Tenofovir Disoproxil Fumarate Monotherapy Abstract Abstract Tenofovir disoproxil fumarate (TDF) is recommended a...
PMC4109680
core_pubmed_pmc
Identification and Preclinical Pharmacology of the γ -Secretase Modulator BMS-869780
Identification and Preclinical Pharmacology of the γ -Secretase Modulator BMS-869780 Abstract Alzheimer's disease is the most prevalent cause of dementia and is associated with accumulation of amyloid- β peptide (A β ), particularly the 42-amino acid A β 1-42, in the brain. A β 1-42 levels can be decreased by γ -secret...
PMC11347199
core_pubmed_pmc
Population pharmacokinetics and dosing optimisation of imipenem in critically ill patients
Population pharmacokinetics and dosing optimisation of imipenem in critically ill patients Abstract Objective The objective of this study was to explore factors that affect the clearance of imipenem in critically ill patients and to provide a dosing regimen for such patients. Methods A prospective open-label study enro...
PMC4153563
core_pubmed_pmc
Biological Time Series Analysis Using a Context Free Language: Applicability to Pulsatile Hormone Data
Biological Time Series Analysis Using a Context Free Language: Applicability to Pulsatile Hormone Data Abstract Abstract We present a novel approach for analyzing biological time-series data using a context-free language (CFL) representation that allows the extraction and quantification of important features from the t...
PMC9768325
core_pubmed_pmc
Pharmacokinetics, bioavailability, and excretion of ponazuril in piglets
Pharmacokinetics, bioavailability, and excretion of ponazuril in piglets Abstract Ponazuril is a triazine anticoccidial drug which is the main metabolite of toltrazuril in animals, it has excellent activity against many protozoa, including Cystoisospora suis , and has broad application prospects in the control of swine...
PMC9655391
core_pubmed_pmc
Losartan Potassium and Verapamil Hydrochloride Compound Transdermal Drug Delivery System: Formulation and Characterization
Losartan Potassium and Verapamil Hydrochloride Compound Transdermal Drug Delivery System: Formulation and Characterization Abstract Abstract In this study, we developed a sustained-release transdermal delivery system containing losartan potassium (LP) and verapamil hydrochloride (VPH). LP and VPH have low bioavailabili...
PMC6618279
core_pubmed_pmc
A Phase 1, Open‐Label, Parallel‐Group, Single‐Dose Trial of the Pharmacokinetics and Safety of Cannabidiol (CBD) in Subjects With Mild to Severe Hepatic Impairment
A Phase 1, Open‐Label, Parallel‐Group, Single‐Dose Trial of the Pharmacokinetics and Safety of Cannabidiol (CBD) in Subjects With Mild to Severe Hepatic Impairment Abstract Abstract The pharmacokinetics and safety of a single oral dose of 200‐mg plant‐derived pharmaceutical formulation of highly purified cannabidiol (C...
PMC11247111
core_pubmed_pmc
Elucidating nonlinear pharmacokinetics of telmisartan: Integration of target‐mediated drug disposition and OATP1B3‐mediated hepatic uptake in a physiologically based model
Elucidating nonlinear pharmacokinetics of telmisartan: Integration of target‐mediated drug disposition and OATP1B3‐mediated hepatic uptake in a physiologically based model Abstract Abstract Telmisartan, a selective inhibitor of angiotensin II receptor type 1 (AT1), demonstrates nonlinear pharmacokinetics (PK) when oral...
PMC8650840
core_pubmed_pmc
Period 2 Regulates CYP2B10 Expression and Activity in Mouse Liver
Period 2 Regulates CYP2B10 Expression and Activity in Mouse Liver Abstract Abstract CYP2B10 is responsible for metabolism and detoxification of many clinical drugs. Here, we aimed to investigate a potential role of Period 2 (PER2) in regulating expression of hepatic CYP2B10. Regulatory effects of PER2 on hepatic expres...
PMC11900651
core_pubmed_pmc
Development and validation of a population pharmacokinetic model of vancomycin for patients of advanced age
Development and validation of a population pharmacokinetic model of vancomycin for patients of advanced age Abstract Background Population pharmacokinetic (PPK) models of vancomycin (VCM) commonly use creatinine clearance (CLcr) as a covariate for clearance (CL). However, relying on CLcr in patients of advanced age may...
PMC6157686
core_pubmed_pmc
Model‐Based Prediction of Plasma Concentration and Enterohepatic Circulation of Total Bile Acids in Humans
Model‐Based Prediction of Plasma Concentration and Enterohepatic Circulation of Total Bile Acids in Humans Abstract Bile acids released postprandially can modify the rate and extent of lipophilic compounds’ absorption. This study aimed to predict the enterohepatic circulation ( EHC ) of total bile acids ( TBAs ) in res...
PMC8205042
core_pubmed_pmc
Preparation and characterization of paclitaxel palmitate albumin nanoparticles with high loading efficacy: an in vitro and in vivo anti-tumor study in mouse models
Preparation and characterization of paclitaxel palmitate albumin nanoparticles with high loading efficacy: an in vitro and in vivo anti-tumor study in mouse models Abstract Abstract Background Combination of the prodrug technique with an albumin nano drug-loaded system is a novel promising approach for cancer treatment...
PMC5042055
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of a human monoclonal anti‐FGF23 antibody (KRN23) in the first multiple ascending‐dose trial treating adults with X‐linked hypophosphatemia
Pharmacokinetics and pharmacodynamics of a human monoclonal anti‐FGF23 antibody (KRN23) in the first multiple ascending‐dose trial treating adults with X‐linked hypophosphatemia Abstract Abstract In X‐linked hypophosphatemia (XLH), serum fibroblast growth factor 23 (FGF23) is increased and results in reduced renal maxi...
PMC8602220
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Modeling of a Cell-Penetrating Peptide Phosphorodiamidate Morpholino Oligomer in mdx Mice
Pharmacokinetic/Pharmacodynamic Modeling of a Cell-Penetrating Peptide Phosphorodiamidate Morpholino Oligomer in mdx Mice Abstract Abstract Purpose Peptide-conjugated phosphorodiamidate morpholino oligomers (PPMOs) have shown promise in treating Duchenne muscular dystrophy (DMD). We evaluated a semi-mechanistic pharmac...
PMC12535277
core_pubmed_pmc
A Phase 2a Trial of Myeloperoxidase Inhibitor Mitiperstat in Non‐Cirrhotic Metabolic Dysfunction‐Associated Steatohepatitis
A Phase 2a Trial of Myeloperoxidase Inhibitor Mitiperstat in Non‐Cirrhotic Metabolic Dysfunction‐Associated Steatohepatitis Abstract ABSTRACT Background and Aims Neutrophil myeloperoxidase is involved in different inflammatory diseases, including metabolic dysfunction‐associated steatohepatitis (MASH). Mitiperstat is a...
PMC11203542
core_pubmed_pmc
Chronic Treatment with Oxcarbazepine Attenuates Its Anticonvulsant Effect in the Maximal Electroshock Model in Mice
Chronic Treatment with Oxcarbazepine Attenuates Its Anticonvulsant Effect in the Maximal Electroshock Model in Mice Abstract The objective of this study was to assess the impact of acute and chronic treatment with oxcarbazepine on its anticonvulsant activity, neurological adverse effects, and protective index in mice. ...
PMC6463642
core_pubmed_pmc
Phellodendri Cortex: A Phytochemical, Pharmacological, and Pharmacokinetic Review
Phellodendri Cortex: A Phytochemical, Pharmacological, and Pharmacokinetic Review Abstract Background Phellodendri Cortex (PC) or Huang Bai. According to the scientific database of China Plant Species and Chinese pharmacopeia 2015 edition, PC has two main species which are Phellodendron amurense Rupr (PAR) or “Guan Hua...
PMC8993713
core_pubmed_pmc
Pharmacokinetic-pharmacodynamic relationships of pour-on administered eprinomectin in nematode-infected lactating female and male castrated dairy breed goats
Pharmacokinetic-pharmacodynamic relationships of pour-on administered eprinomectin in nematode-infected lactating female and male castrated dairy breed goats Abstract Abstract Eprinomectin (EPM), a macrocyclic lactone with low excretion in milk and high efficacy against endoparasites and ectoparasites, is widely used i...
PMC9104399
core_pubmed_pmc
Enhanced Oral Bioavailability of β-Caryophyllene in Healthy Subjects Using the VESIsorb ® Formulation Technology, a Novel Self-Emulsifying Drug Delivery System (SEDDS)
Enhanced Oral Bioavailability of β-Caryophyllene in Healthy Subjects Using the VESIsorb ® Formulation Technology, a Novel Self-Emulsifying Drug Delivery System (SEDDS) Abstract Abstract β-Caryophyllene (BCP), a common constituent of many spice and food plants, is gaining increased attention due to recent research ident...
PMC6400122
core_pubmed_pmc
Acid-responsive nanoparticles as a novel oxidative stress-inducing anticancer therapeutic agent for colon cancer
Acid-responsive nanoparticles as a novel oxidative stress-inducing anticancer therapeutic agent for colon cancer Abstract Objective Nanoparticles can efficiently carry and deliver anticancer agents to tumor sites. Mounting evidence indicates that many types of cancer cells, including colon cancer, have a weakly acidic ...
PMC11911599
core_pubmed_pmc
Predicting Pharmacokinetics in Rats Using Machine Learning: A Comparative Study Between Empirical, Compartmental, and PBPK ‐Based Approaches
Predicting Pharmacokinetics in Rats Using Machine Learning: A Comparative Study Between Empirical, Compartmental, and PBPK ‐Based Approaches Abstract ABSTRACT A successful drug needs to combine several properties including high potency and good pharmacokinetic (PK) properties to sustain efficacious plasma concentration...
PMC3236511
core_pubmed_pmc
Effects of Selected Anionic β -Cyclodextrins on Persistence of Blood Glucose Lowering by Insulin Glargine after Subcutaneous Injection to Rats
Effects of Selected Anionic β -Cyclodextrins on Persistence of Blood Glucose Lowering by Insulin Glargine after Subcutaneous Injection to Rats Abstract Insulin glargine is a synthetic long-acting insulin product used for patients with diabetes mellitus. In this study, to obtain the further desirable blood-glucose lower...
PMC11247110
core_pubmed_pmc
A physiologically‐based pharmacokinetic precision dosing approach to manage dasatinib drug–drug interactions
A physiologically‐based pharmacokinetic precision dosing approach to manage dasatinib drug–drug interactions Abstract Abstract Dasatinib, a second‐generation tyrosine kinase inhibitor, is approved for treating chronic myeloid and acute lymphoblastic leukemia. As a sensitive cytochrome P450 (CYP) 3A4 substrate and weak ...
PMC11823298
core_pubmed_pmc
The effect of carbamazepine, a strong CYP3A inducer, on the pharmacokinetics of zongertinib in healthy male volunteers
The effect of carbamazepine, a strong CYP3A inducer, on the pharmacokinetics of zongertinib in healthy male volunteers Abstract Abstract Introduction Zongertinib (BI 1810631) is a potent, selective, and epidermal growth factor receptor (EGFR) wild‐type sparing human epidermal growth factor receptor 2 (HER2) inhibitor. ...
PMC9835120
core_pubmed_pmc
Model‐based population pharmacokinetic analysis of tislelizumab in patients with advanced tumors
Model‐based population pharmacokinetic analysis of tislelizumab in patients with advanced tumors Abstract Abstract Tislelizumab, a humanized immunoglobulin G4 monoclonal antibody, is a programmed cell death protein 1 (PD‐1) inhibitor designed to minimize Fc gamma receptor binding on macrophages to limit antibody‐depend...
PMC12209834
core_pubmed_pmc
Model-based translation of the PKPD-relationship for linezolid and vancomycin on methicillin-resistant Staphylococcus aureus : from in vitro time–kill experiments to a mouse pneumonia model
Model-based translation of the PKPD-relationship for linezolid and vancomycin on methicillin-resistant Staphylococcus aureus : from in vitro time–kill experiments to a mouse pneumonia model Abstract Abstract Objectives MRSA is one of the main pathogens that cause nosocomial pneumonia. Based on longitudinal in vitro and...
PMC9981759
core_pubmed_pmc
Inhaled milrinone in cardiac surgical patients: pharmacokinetic and pharmacodynamic exploration
Inhaled milrinone in cardiac surgical patients: pharmacokinetic and pharmacodynamic exploration Abstract Abstract Mean arterial pressure to mean pulmonary arterial pressure ratio (mAP/mPAP) has been identified as a strong predictor of perioperative complications in cardiac surgery. We therefore investigated the pharmac...
PMC4471402
core_pubmed_pmc
Effects of the Chinese Herbal Formulation ( Liu Wei Di Huang Wan ) on the Pharmacokinetics of Isoflavones in Postmenopausal Women
Effects of the Chinese Herbal Formulation ( Liu Wei Di Huang Wan ) on the Pharmacokinetics of Isoflavones in Postmenopausal Women Abstract A combination of soy isoflavones and Liu Wei Di Huang Wan (LWDHW) is potentially effective for postmenopausal women with intolerable vasomotor episodes who are not suitable candidat...
PMC12251332
core_pubmed_pmc
Review of the Safety and Clinical Considerations of Vasoconstrictor Agents in Dental Anesthesia During Pregnancy
Review of the Safety and Clinical Considerations of Vasoconstrictor Agents in Dental Anesthesia During Pregnancy Abstract Background : The use of vasoconstrictors in dental anesthesia during pregnancy raises clinical concerns due to their potential effects on uteroplacental blood flow and fetal well-being. Despite wide...
PMC9340256
core_pubmed_pmc
Population pharmacokinetics model for escitalopram in Chinese psychiatric patients: effect of CYP2C19 and age
Population pharmacokinetics model for escitalopram in Chinese psychiatric patients: effect of CYP2C19 and age Abstract Objective: To establish a population pharmacokinetic model in Chinese psychiatric patients to characterize escitalopram pharmacokinetic profile to identify factors influencing drug exposure, and throug...
PMC8411625
core_pubmed_pmc
Current treatments and future potential of surufatinib in neuroendocrine tumors (NETs)
Current treatments and future potential of surufatinib in neuroendocrine tumors (NETs) Abstract Neuroendocrine tumors (NETs) are rare, heterogeneous, often indolent tumors that predominantly originate in the lungs and gastrointestinal tract. An understanding of the biology and tumor microenvironment of NETs has led to ...
PMC10093626
core_pubmed_pmc
Mathematical Model of Clonal Evolution Proposes a Personalised Multi-Modal Therapy for High-Risk Neuroblastoma
Mathematical Model of Clonal Evolution Proposes a Personalised Multi-Modal Therapy for High-Risk Neuroblastoma Abstract Abstract Simple Summary Neuroblastoma is a rare type of cancer that usually affects children. The high-risk patients’ expected survival rate is less than 50%. One reason is the lack of precision in th...
PMC12946568
core_pubmed_pmc
Comparative Bioequivalence and Safety Evaluation of Ibuprofen/Phenylephrine Hydrochloride Fixed‐Dose Combination Tablets in Healthy Chinese Volunteers
Comparative Bioequivalence and Safety Evaluation of Ibuprofen/Phenylephrine Hydrochloride Fixed‐Dose Combination Tablets in Healthy Chinese Volunteers Abstract Abstract This single‐center, randomized, open‐label bioequivalence program compared two fixed‐dose combination (FDC) tablets containing ibuprofen (200 mg) and p...
PMC7595987
core_pubmed_pmc
Multiple-Dose Pharmacokinetics of Ozanimod and its Major Active Metabolites and the Pharmacodynamic and Pharmacokinetic Interactions with Pseudoephedrine, a Sympathomimetic Agent, in Healthy Subjects
Multiple-Dose Pharmacokinetics of Ozanimod and its Major Active Metabolites and the Pharmacodynamic and Pharmacokinetic Interactions with Pseudoephedrine, a Sympathomimetic Agent, in Healthy Subjects Abstract Introduction The aims of this study were to characterize the multiple-dose pharmacokinetics (PK) of ozanimod’s ...
PMC11802684
core_pubmed_pmc
Physiologically-Based Pharmacokinetic Modeling of Trofinetide in Moderate Renal Impairment for Phase 1 Clinical Study Dose Selection with Model Validation
Physiologically-Based Pharmacokinetic Modeling of Trofinetide in Moderate Renal Impairment for Phase 1 Clinical Study Dose Selection with Model Validation Abstract Background and Objectives Trofinetide, the first approved treatment for Rett syndrome (RTT), is primarily excreted unchanged in the urine; therefore, it is ...
PMC7139112
core_pubmed_pmc
Safety and tolerability of injectable Rilpivirine LA in HPTN 076: A phase 2 HIV pre-exposure prophylaxis study in women
Safety and tolerability of injectable Rilpivirine LA in HPTN 076: A phase 2 HIV pre-exposure prophylaxis study in women Abstract Abstract Background Daily oral TDF/FTC is protective against HIV infection when used for pre-exposure prophylaxis (PrEP). However, daily adherence to oral PrEP is difficult for many; therefor...
PMC3726665
core_pubmed_pmc
A Randomized Pilot Study of L-Arginine Infusion in Severe Falciparum Malaria: Preliminary Safety, Efficacy and Pharmacokinetics
A Randomized Pilot Study of L-Arginine Infusion in Severe Falciparum Malaria: Preliminary Safety, Efficacy and Pharmacokinetics Abstract Background Decreased nitric oxide (NO) and hypoargininemia are associated with severe falciparum malaria and may contribute to severe disease. Intravenous L-arginine increases endothe...
PMC4519338
core_pubmed_pmc
Experience with Subgam, a Subcutaneously Administered Human Normal Immunoglobulin (ClinicalTrials.gov - NCT02247141 )
Experience with Subgam, a Subcutaneously Administered Human Normal Immunoglobulin (ClinicalTrials.gov - NCT02247141 ) Abstract Background and Objectives A multi-centre, non-comparative study examining the efficacy and safety of Subgam, a normal immunoglobulin (IgG) given weekly as a rapid subcutaneous infusion to patie...
PMC12903901
core_pubmed_pmc
Dose Optimization of Tilmicosin against Pasteurella multocida in Swine by Physiologically Based Pharmacokinetic-Pharmacodynamic Model
Dose Optimization of Tilmicosin against Pasteurella multocida in Swine by Physiologically Based Pharmacokinetic-Pharmacodynamic Model Abstract Abstract Rising bacterial resistance leads to diminishing clinical efficacy of tilmicosin against Pasteurella multocida in porcine respiratory disease. This study aimed to optim...
PMC4792430
core_pubmed_pmc
A New Pharmacogenetic Algorithm to Predict the Most Appropriate Dosage of Acenocoumarol for Stable Anticoagulation in a Mixed Spanish Population
A New Pharmacogenetic Algorithm to Predict the Most Appropriate Dosage of Acenocoumarol for Stable Anticoagulation in a Mixed Spanish Population Abstract There is a strong association between genetic polymorphisms and the acenocoumarol dosage requirements. Genotyping the polymorphisms involved in the pharmacokinetics a...
PMC9158153
core_pubmed_pmc
Zibotentan in systemic sclerosis-associated chronic kidney disease: a phase II randomised placebo-controlled trial
Zibotentan in systemic sclerosis-associated chronic kidney disease: a phase II randomised placebo-controlled trial Abstract Background We report results from a phase II randomised placebo-controlled trial assessing zibotentan, a highly selective endothelin receptor antagonist (ERA), in chronic kidney disease (CKD) seco...
PMC6884976
core_pubmed_pmc
Hepatic Arterial Chemoembolization With Arsenic Trioxide Eluting CalliSpheres Microspheres Versus Lipiodol Emulsion: Pharmacokinetics And Intratumoral Concentration In A Rabbit Liver Tumor Model
Hepatic Arterial Chemoembolization With Arsenic Trioxide Eluting CalliSpheres Microspheres Versus Lipiodol Emulsion: Pharmacokinetics And Intratumoral Concentration In A Rabbit Liver Tumor Model Abstract Abstract Background The objective of this study was to investigate the plasma pharmacokinetic profiles, intratumoral...
PMC11971150
core_pubmed_pmc
Advancing inclusive healthcare through PBPK modelling: predicting the impact of CYP genotypes and enzyme ontogenies on infant exposures of venlafaxine and its active metabolite O-desmethylvenlafaxine in lactation
Advancing inclusive healthcare through PBPK modelling: predicting the impact of CYP genotypes and enzyme ontogenies on infant exposures of venlafaxine and its active metabolite O-desmethylvenlafaxine in lactation Abstract Abstract About 15–20% of women experience postnatal depression and may seek advice about medicatio...
PMC7788882
core_pubmed_pmc
Potential challenges to sustained viral load suppression in the HIV treatment programme in South Africa: a narrative overview
Potential challenges to sustained viral load suppression in the HIV treatment programme in South Africa: a narrative overview Abstract Background South Africa, with one of the highest HIV prevalences in the world, introduced the universal test and treat (UTT) programme in September 2016. Barriers to sustained viral sup...
PMC6131115
core_pubmed_pmc
Distribution of Antisense Oligonucleotides in Rat Eyeballs Using MALDI Imaging Mass Spectrometry
Distribution of Antisense Oligonucleotides in Rat Eyeballs Using MALDI Imaging Mass Spectrometry Abstract Oligonucleotide-based therapeutics such as antisense oligonucleotides, small interfering RNAs (siRNAs), decoy and aptamer have been extensively developed. To investigate the pharmacokinetics of oligonucleotide ther...
PMC5260009
core_pubmed_pmc
Exploring the Pharmacokinetic Profile of Remifentanil in Mid-Trimester Gestations Undergoing Fetal Intervention Procedures
Exploring the Pharmacokinetic Profile of Remifentanil in Mid-Trimester Gestations Undergoing Fetal Intervention Procedures Abstract Background: Indications for surgery during pregnancy have increased. Specifically fetal interventions have increased from conditions that were considered lethal like twin-twin transfusion ...
PMC11469192
core_pubmed_pmc
Oral Delivery of the Vancomycin Derivative FU002 by a Surface‐Modified Liposomal Nanocarrier
Oral Delivery of the Vancomycin Derivative FU002 by a Surface‐Modified Liposomal Nanocarrier Abstract Abstract Oral delivery of peptide therapeutics faces multiple challenges due to their instability in the gastrointestinal tract and low permeation capability. In this study, the aim is to develop a liposomal nanocarrie...
PMC5859084
core_pubmed_pmc
Pathway-Based Analysis of Genome-Wide Association Data Identified SNPs in HMMR as Biomarker for Chemotherapy- Induced Neutropenia in Breast Cancer Patients
Pathway-Based Analysis of Genome-Wide Association Data Identified SNPs in HMMR as Biomarker for Chemotherapy- Induced Neutropenia in Breast Cancer Patients Abstract Neutropenia secondary to chemotherapy in breast cancer patients can be life-threatening and there are no biomarkers available to predict the risk of drug-i...
PMC7320716
core_pubmed_pmc
Evaluation of cytochrome P450-based drug metabolism in hemorrhagic shock rats that were transfused with native and an artificial red blood cell preparation, Hemoglobin-vesicles
Evaluation of cytochrome P450-based drug metabolism in hemorrhagic shock rats that were transfused with native and an artificial red blood cell preparation, Hemoglobin-vesicles Abstract Abstract Hemoglobin-vesicles (Hb-V) are being developed as red blood cell (RBC) substitutes. In this study, we report on quantitative ...
PMC8398766
core_pubmed_pmc
Do Small Molecules Activate the TrkB Receptor in the Same Manner as BDNF? Limitations of Published TrkB Low Molecular Agonists and Screening for Novel TrkB Orthosteric Agonists
Do Small Molecules Activate the TrkB Receptor in the Same Manner as BDNF? Limitations of Published TrkB Low Molecular Agonists and Screening for Novel TrkB Orthosteric Agonists Abstract TrkB is a tyrosine kinase receptor that is activated upon binding to brain-derived neurotrophic factor (BDNF). To date, the search for...
PMC9796926
core_pubmed_pmc
ECG Evaluation as Part of the Clinical Pharmacology Strategy in the Development of New Drugs: A Review of Current Practices and Opportunities Based on Five Case Studies
ECG Evaluation as Part of the Clinical Pharmacology Strategy in the Development of New Drugs: A Review of Current Practices and Opportunities Based on Five Case Studies Abstract Abstract The International Conference on Harmonization (ICH) E14 document was revised in 2015 to allow concentration–corrected QT interval (C–...
PMC8424631
core_pubmed_pmc
Non-uniformity of Changes in Drug-Metabolizing Enzymes and Transporters in Liver Cirrhosis: Implications for Drug Dosage Adjustment
Non-uniformity of Changes in Drug-Metabolizing Enzymes and Transporters in Liver Cirrhosis: Implications for Drug Dosage Adjustment Abstract Abstract Liver cirrhosis is a chronic disease that affects the liver structure, protein expression, and overall metabolic function. Abundance data for drug-metabolizing enzymes an...
PMC6058478
core_pubmed_pmc
Chitosan-based liposomal thermogels for the controlled delivery of pingyangmycin: design, optimization and in vitro and in vivo studies
Chitosan-based liposomal thermogels for the controlled delivery of pingyangmycin: design, optimization and in vitro and in vivo studies Abstract Abstract Pingyangmycin (PYM) has been applied clinically for many years to treat vascular malformations (VM) in China. The major limitation of PYM injections is quick diffusio...