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PMC12310257
core_pubmed_pmc
From Intravenous to Subcutaneous Infliximab: the Same but Different? Real-World Evidence from a Tertiary Center
From Intravenous to Subcutaneous Infliximab: the Same but Different? Real-World Evidence from a Tertiary Center Abstract Summary Introduction. Recently, a subcutaneous formulation of infliximab was approved. The switch from intravenous infliximab to subcutaneous infliximab may improve convenience, but data on pharmacok...
PMC9795609
core_pubmed_pmc
Safety and microbiological activity of phage therapy in persons with cystic fibrosis colonized with Pseudomonas aeruginosa: study protocol for a phase 1b/2, multicenter, randomized, double-blind, placebo-controlled trial
Safety and microbiological activity of phage therapy in persons with cystic fibrosis colonized with Pseudomonas aeruginosa: study protocol for a phase 1b/2, multicenter, randomized, double-blind, placebo-controlled trial Abstract Background Bacteriophages (phages) are a promising anti-infective option for human disease...
PMC9996297
core_pubmed_pmc
Real pandemic world results of pharmacokinetic-tailored personalized prophylaxis of bleeds in Polish children and adolescents with severe hemophilia A
Real pandemic world results of pharmacokinetic-tailored personalized prophylaxis of bleeds in Polish children and adolescents with severe hemophilia A Abstract Introduction In 2020, the new nationwide protocol of prophylaxis in Polish plasma-derived FVIII (pdFVIII) previously treated patients (PTPs) with severe hemophi...
PMC9056459
core_pubmed_pmc
Superior Bioavailability of a Novel Curcumin Formulation in Healthy Humans Under Fasting Conditions
Superior Bioavailability of a Novel Curcumin Formulation in Healthy Humans Under Fasting Conditions Abstract Abstract Background Despite its broad range of biological activities, use of curcumin is limited because of poor bioavailability. Here we report a novel curcumin formulation, Curcuwin Ultra+ (CU+), with superior...
PMC11535787
core_pubmed_pmc
Toward a Clinical Decision Support System for Monitoring Therapeutic Antituberculosis Medical Drugs in Tanzania (Project TuberXpert): Protocol for an Algorithm' Development and Implementation
Toward a Clinical Decision Support System for Monitoring Therapeutic Antituberculosis Medical Drugs in Tanzania (Project TuberXpert): Protocol for an Algorithm' Development and Implementation Abstract Abstract Background The end tuberculosis (TB) strategy requires a novel patient treatment approach contrary to the one-...
PMC12650536
core_pubmed_pmc
First Evidence of Anti- Plasmodium vivax (Plasmodiidae): Activity of the Essential Oil and 6-Ishwarone Isolated from Piper alatipetiolatum Yunck. (Piperaceae)
First Evidence of Anti- Plasmodium vivax (Plasmodiidae): Activity of the Essential Oil and 6-Ishwarone Isolated from Piper alatipetiolatum Yunck. (Piperaceae) Abstract Abstract Background/Objectives : In the Brazilian Amazon, which accounts for over 99% of national malaria cases, 34,260 cases were reported as of August...
PMC12409579
core_pubmed_pmc
An LC–MS/MS Assay of Irsenontrine, a Novel Phosphodiesterase‑9 Inhibitor, in Human Plasma, Urine and Cerebrospinal Fluid for Application to Clinical Pharmacokinetic Studies
An LC–MS/MS Assay of Irsenontrine, a Novel Phosphodiesterase‑9 Inhibitor, in Human Plasma, Urine and Cerebrospinal Fluid for Application to Clinical Pharmacokinetic Studies Abstract Irsenontrine is a novel phosphodiesterase-9 inhibitor that has been developed for the treatment of cognitive dysfunction. To assess the ph...
PMC9295372
core_pubmed_pmc
Development of a particle swarm optimization-backpropagation artificial neural network model and effects of age and gender on pharmacokinetics study of omeprazole enteric-coated tablets in Chinese population
Development of a particle swarm optimization-backpropagation artificial neural network model and effects of age and gender on pharmacokinetics study of omeprazole enteric-coated tablets in Chinese population Abstract Abstract Background The effects of age and gender were explored on pharmacokinetics study of omeprazole...
PMC3666662
core_pubmed_pmc
Nanoemulsion loaded with lycobetaine–oleic acid ionic complex: physicochemical characteristics, in vitro, in vivo evaluation, and antitumor activity
Nanoemulsion loaded with lycobetaine–oleic acid ionic complex: physicochemical characteristics, in vitro, in vivo evaluation, and antitumor activity Abstract Background Intravenous injection of lycobetaine was found to show significant cytotoxic activity against (inter alia) Lewis lung carcinoma, but its therapeutic us...
PMC6595297
core_pubmed_pmc
Effect of CYP3A inhibitors on the pharmacokinetics of pevonedistat in patients with advanced solid tumours
Effect of CYP3A inhibitors on the pharmacokinetics of pevonedistat in patients with advanced solid tumours Abstract Aims This phase I study evaluated the effects of the moderate cytochrome P450 (CYP) 3A inhibitor fluconazole and the strong CYP3A/P‐glycoprotein (P‐gp) inhibitor itraconazole on the pharmacokinetics of th...
PMC10366676
core_pubmed_pmc
Bibliometric Analysis of Global Trends in Remimazolam-Related Research Over the Past 15 Years: Compared with Propofol
Bibliometric Analysis of Global Trends in Remimazolam-Related Research Over the Past 15 Years: Compared with Propofol Abstract Abstract Purpose Although remimazolam is a popular novel anesthetic, there is a lack of data in the literature about current and future trends. Therefore, the aim of this study was to explore e...
PMC5968193
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Tildipirosin Against Pasteurella multocida in a Murine Lung Infection Model
Pharmacokinetics and Pharmacodynamics of Tildipirosin Against Pasteurella multocida in a Murine Lung Infection Model Abstract Abstract Tildipirosin, a 16-membered-ring macrolide antimicrobial, has recently been approved for the treatment of swine respiratory disease and bovine respiratory disease. This macrolide is ext...
PMC7894971
core_pubmed_pmc
Recent Achievements and Challenges in Prolonging the Serum Half-Lives of Therapeutic IgG Antibodies Through Fc Engineering
Recent Achievements and Challenges in Prolonging the Serum Half-Lives of Therapeutic IgG Antibodies Through Fc Engineering Abstract Abstract Association of FcRn molecules to the Fc region of IgG in acidified endosomes and subsequent dissociation of the interaction in neutral pH serum enables IgG molecules to be recycle...
PMC9427879
core_pubmed_pmc
Pharmacokinetics of Imeglimin in Caucasian and Japanese Healthy Subjects
Pharmacokinetics of Imeglimin in Caucasian and Japanese Healthy Subjects Abstract Abstract Background Imeglimin is a first-in-class novel oral antidiabetic marketed in Japan as TWYMEEG ® to treat type 2 diabetes mellitus. Its mode of action is distinct from all other anti-hyperglycemic classes. Objective To assess the ...
PMC12105979
core_pubmed_pmc
Letter to the FDA Proposing Major Changes in the US Clozapine Package Insert Supported by Clozapine Experts Worldwide. Part I
Letter to the FDA Proposing Major Changes in the US Clozapine Package Insert Supported by Clozapine Experts Worldwide. Part I Abstract Abstract Purpose/Background Clozapine was approved in the United States (US) using 1989 regulations and knowledge. After 30 years, many sections of the US package insert (PI) are outdat...
PMC7326703
core_pubmed_pmc
Daratumumab monotherapy for patients with intermediate-risk or high-risk smoldering multiple myeloma: a randomized, open-label, multicenter, phase 2 study (CENTAURUS)
Daratumumab monotherapy for patients with intermediate-risk or high-risk smoldering multiple myeloma: a randomized, open-label, multicenter, phase 2 study (CENTAURUS) Abstract Current guidelines for smoldering multiple myeloma (SMM) recommend active monitoring until the onset of multiple myeloma (MM) before initiating ...
PMC10819155
core_pubmed_pmc
Use of Exposure Data to Establish Causality in Drug–Adverse Event Relationships: An Example with Desvenlafaxine
Use of Exposure Data to Establish Causality in Drug–Adverse Event Relationships: An Example with Desvenlafaxine Abstract Abstract Causality algorithms help establish relationships between drug use and adverse event (AE) occurrence. High drug exposure leads to a higher likelihood of an AE being classified as an adverse ...
PMC11960678
core_pubmed_pmc
Subtherapeutic Meropenem Antibiotic Exposure in Children With Septic Shock Assessed by Noncompartmental Pharmacokinetic Analysis in a Prospective Dataset
Subtherapeutic Meropenem Antibiotic Exposure in Children With Septic Shock Assessed by Noncompartmental Pharmacokinetic Analysis in a Prospective Dataset Abstract Abstract OBJECTIVES: To define meropenem plasma concentrations and pharmacodynamic exposure metrics in children with septic shock during the first 3 days of ...
PMC11131409
core_pubmed_pmc
Gene polymorphism as a cause of hemorrhagic complications in patients with non-valvular atrial fibrillation treated with oral vitamin K-independent anticoagulants
Gene polymorphism as a cause of hemorrhagic complications in patients with non-valvular atrial fibrillation treated with oral vitamin K-independent anticoagulants Abstract Abstract Atrial fibrillation (AF) accounts for 40% of all cardiac arrhythmias and is associated with a high risk of stroke and systemic thromboembol...
PMC3997831
core_pubmed_pmc
Population Pharmacokinetic Modelling of Recombinant Factor IX Fc Fusion Protein (rFIXFc) in Patients with Haemophilia B
Population Pharmacokinetic Modelling of Recombinant Factor IX Fc Fusion Protein (rFIXFc) in Patients with Haemophilia B Abstract Background and Objectives Recombinant factor IX Fc fusion protein (rFIXFc) is a clotting factor developed using monomeric Fc fusion technology to prolong the circulating half-life of factor I...
PMC12476157
core_pubmed_pmc
Topical Application of Everolimus Attenuates Lens-Induced Myopia Through mTORC1 Suppression
Topical Application of Everolimus Attenuates Lens-Induced Myopia Through mTORC1 Suppression Abstract Abstract Purpose The mechanistic target of rapamycin complex 1 (mTORC1) signaling has been reported to regulate lens-induced myopia (LIM) in guinea pigs. To address the challenge of delivering lipophilic mTORC1 inhibito...
PMC4842915
core_pubmed_pmc
Safety, pharmacokinetics and pharmacodynamics of the anti‐hepcidin Spiegelmer lexaptepid pegol in healthy subjects
Safety, pharmacokinetics and pharmacodynamics of the anti‐hepcidin Spiegelmer lexaptepid pegol in healthy subjects Abstract Abstract Background and Purpose Anaemia of chronic disease is characterized by impaired erythropoiesis due to functional iron deficiency, often caused by excessive hepcidin. Lexaptepid pegol, a pe...
PMC5069706
core_pubmed_pmc
A Dose-Escalation Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Efficacy of 2 and 4 Weeks of Twice-Daily Ocular Trabodenoson in Adults with Ocular Hypertension or Primary Open-Angle Glaucoma
A Dose-Escalation Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Efficacy of 2 and 4 Weeks of Twice-Daily Ocular Trabodenoson in Adults with Ocular Hypertension or Primary Open-Angle Glaucoma Abstract Abstract Purpose: To evaluate the safety and ocular hypotensive efficacy of 4 trabodenoson doses adm...
PMC9008867
core_pubmed_pmc
A phase 1 study of the safety, pharmacokinetics and pharmacodynamics of escalating doses followed by dose expansion of the selective inhibitor of nuclear export (SINE) selinexor in Asian patients with advanced or metastatic malignancies
A phase 1 study of the safety, pharmacokinetics and pharmacodynamics of escalating doses followed by dose expansion of the selective inhibitor of nuclear export (SINE) selinexor in Asian patients with advanced or metastatic malignancies Abstract Purpose: This phase 1 study aims to evaluate the tolerability and the reco...
PMC11043204
core_pubmed_pmc
Pharmacokinetics/pharmacodynamics of ivosidenib in advanced IDH1 -mutant cholangiocarcinoma: findings from the phase III ClarIDHy study
Pharmacokinetics/pharmacodynamics of ivosidenib in advanced IDH1 -mutant cholangiocarcinoma: findings from the phase III ClarIDHy study Abstract Abstract Purpose Report pharmacokinetic (PK)/pharmacodynamic (PD) findings from the phase III ClarIDHy study and any association between PK/PD parameters and treatment outcome...
PMC7691962
core_pubmed_pmc
Hydroxyurea Optimization through Precision Study (HOPS): study protocol for a randomized, multicenter trial in children with sickle cell anemia
Hydroxyurea Optimization through Precision Study (HOPS): study protocol for a randomized, multicenter trial in children with sickle cell anemia Abstract Abstract Background Sickle cell disease (SCD) is a severe and devastating hematological disorder that affects over 100,000 persons in the USA and millions worldwide. H...
PMC6444299
core_pubmed_pmc
Pharmacokinetic analysis for the differentiation of pituitary microadenoma subtypes through dynamic contrast-enhanced magnetic resonance imaging
Pharmacokinetic analysis for the differentiation of pituitary microadenoma subtypes through dynamic contrast-enhanced magnetic resonance imaging Abstract The value of pharmacokinetic parameters derived from dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) in distinguishing pituitary microadenoma subtypes ...
PMC8877620
core_pubmed_pmc
Antiviral Effects of Artemisinin and Its Derivatives against SARS-CoV-2 Main Protease: Computational Evidences and Interactions with ACE2 Allelic Variants
Antiviral Effects of Artemisinin and Its Derivatives against SARS-CoV-2 Main Protease: Computational Evidences and Interactions with ACE2 Allelic Variants Abstract Fighting against the emergent coronavirus disease (COVID-19) remains a big challenge at the front of the world communities. Recent research has outlined the...
PMC4957413
core_pubmed_pmc
No clinically significant pharmacokinetic interactions between dolutegravir and daclatasvir in healthy adult subjects
No clinically significant pharmacokinetic interactions between dolutegravir and daclatasvir in healthy adult subjects Abstract Abstract Background Daclatasvir (DCV) is an NS5A replication complex inhibitor recently approved for chronic hepatitis C virus treatment. Methods To assess drug interactions between the HIV int...
PMC8429405
core_pubmed_pmc
Pharmacokinetic profile and effect on bone markers and muscle strength of two daily dosage regimens of calcifediol in osteopenic/osteoporotic postmenopausal women
Pharmacokinetic profile and effect on bone markers and muscle strength of two daily dosage regimens of calcifediol in osteopenic/osteoporotic postmenopausal women Abstract Abstract Background At present, although cholecalciferol represents the form of vitamin D of choice for the treatment of vitamin D deficiency, there...
PMC9272739
core_pubmed_pmc
Addressing bedaquiline treatment interruptions in the treatment of drug-resistant TB
Addressing bedaquiline treatment interruptions in the treatment of drug-resistant TB Abstract SUMMARY SETTING: The recommended dosing regimen for bedaquiline (BDQ), consisting of a 2-week loading phase (400 mg/day), followed by a maintenance phase (200 mg three times/week), might pose challenges when treatment is inter...
PMC7034088
core_pubmed_pmc
Effect of verapamil on the pharmacokinetics of hydroxycamptothecin and its potential mechanism
Effect of verapamil on the pharmacokinetics of hydroxycamptothecin and its potential mechanism Abstract Abstract Context Hydroxycamptothecin (HCPT) has antitumor activity in various cancers, but its poor bioavailability and efflux limit its clinical application. Verapamil has been demonstrated to improve the bioavailab...
PMC8874425
core_pubmed_pmc
Pharmacogenomics-Guided Pharmacotherapy in Patients with Major Depressive Disorder or Bipolar Disorder Affected by Treatment-Resistant Depressive Episodes: A Long-Term Follow-Up Study
Pharmacogenomics-Guided Pharmacotherapy in Patients with Major Depressive Disorder or Bipolar Disorder Affected by Treatment-Resistant Depressive Episodes: A Long-Term Follow-Up Study Abstract Abstract Treatment-resistant depression (TRD) reduces affected patients’ quality of life and leads to important social health c...
PMC10251743
core_pubmed_pmc
Disposition of a single oral dose of a cannabidiol medication in healthy cats
Disposition of a single oral dose of a cannabidiol medication in healthy cats Abstract Abstract The historical use of the marijuana plant for medicinal purposes is long. One of the historical uses has been for the treatment of epilepsy. Recently, the Food and Drug Administration has approved a highly purified cannabidi...
PMC3828007
core_pubmed_pmc
Pharmacometric Analyses to Support Early Development Decisions for LY2878735: A Novel Serotonin Norepinephrine Reuptake Inhibitor
Pharmacometric Analyses to Support Early Development Decisions for LY2878735: A Novel Serotonin Norepinephrine Reuptake Inhibitor Abstract Abstract LY2878735 is a novel dual serotonin (5-hydroxytryptamine (5-HT)) and norepinephrine (NE) reuptake inhibitor (SNRI) in development for chronic pain indications. In vitro pro...
PMC8318725
core_pubmed_pmc
Influence of SULT1A1*2 Polymorphism on Plasma Efavirenz Concentration in Thai HIV-1 Patients
Influence of SULT1A1*2 Polymorphism on Plasma Efavirenz Concentration in Thai HIV-1 Patients Abstract Abstract Purpose Plasma efavirenz (EFV) concentrations within therapeutic levels are essential to successfully treat patients suffering from human immunodeficiency virus (HIV) type 1. In addition to the drug-metabolizi...
PMC9694039
core_pubmed_pmc
Systems Biology Approach for Personalized Hemostasis Correction
Systems Biology Approach for Personalized Hemostasis Correction Abstract Abstract The correction of blood coagulation impairments of a bleeding or thrombotic nature employs standard protocols where the type of drug, its dose and the administration regime are stated. However, for a group of patients, such an approach ma...
PMC11938432
core_pubmed_pmc
Long-Acting Growth Hormone for Pediatric Growth Hormone Deficiency
Long-Acting Growth Hormone for Pediatric Growth Hormone Deficiency Abstract Abstract Long-acting growth hormone (LAGH) has the potential to improve adherence and outcomes over daily somatropin in growth hormone deficiency (GHD). Whereas daily somatropin products are molecularly identical, LAGHs are molecularly distinct...
PMC4070280
core_pubmed_pmc
Effect of Experimentally Induced Hepatic and Renal Failure on the Pharmacokinetics of Topiramate in Rats
Effect of Experimentally Induced Hepatic and Renal Failure on the Pharmacokinetics of Topiramate in Rats Abstract Abstract We aimed to investigate the effect of induced hepatic and renal failure on the pharmacokinetics of topiramate (TPM) in rats. Twenty-four Sprague-Dawley rats were used in this study. Renal or hepati...
PMC10282079
core_pubmed_pmc
Design, synthesis, in vitro anti-α-glucosidase evaluations, and computational studies of new phthalimide-phenoxy-1,2,3-triazole- N -phenyl (or benzyl) acetamides as potential anti-diabetic agents
Design, synthesis, in vitro anti-α-glucosidase evaluations, and computational studies of new phthalimide-phenoxy-1,2,3-triazole- N -phenyl (or benzyl) acetamides as potential anti-diabetic agents Abstract Abstract An important target in the treatment of type 2 diabetes is α-glucosidase. Inhibition of this enzyme led to...
PMC7554750
core_pubmed_pmc
Obstacles against the Marketing of Curcumin as a Drug
Obstacles against the Marketing of Curcumin as a Drug Abstract Abstract Among the extensive public and scientific interest in the use of phytochemicals to prevent or treat human diseases in recent years, natural compounds have been highly investigated to elucidate their therapeutic effect on chronic human diseases incl...
PMC12238501
core_pubmed_pmc
Pharmacokinetic evaluation of two oral Resveratrol formulations in a randomized, open-label, crossover study in healthy fasting subjects
Pharmacokinetic evaluation of two oral Resveratrol formulations in a randomized, open-label, crossover study in healthy fasting subjects Abstract Abstract Resveratrol is widely used in the fields of medicine and health supplements; however, its poor stability and low relative bioavailability limit its applications. Thi...
PMC12824865
core_pubmed_pmc
HFD-induced Alterations in Renal Tubular Oatp4c1-P-gp Transport Systems in Mice: Impact on Digoxin Renal Excretion and Gadolinium-Enhanced Radiological Manifestations
HFD-induced Alterations in Renal Tubular Oatp4c1-P-gp Transport Systems in Mice: Impact on Digoxin Renal Excretion and Gadolinium-Enhanced Radiological Manifestations Abstract Objective The clearance of digoxin in obese patients with renal impairment is reduced, leading to elevated serum concentrations and increased ri...
PMC12706398
core_pubmed_pmc
Rosuvastatin PBPK Modeling: Incorporating Liver Concentrations and Effects of Ethnicity, Genetic Polymorphisms, Lactone Formation, DDI and Pregnancy
Rosuvastatin PBPK Modeling: Incorporating Liver Concentrations and Effects of Ethnicity, Genetic Polymorphisms, Lactone Formation, DDI and Pregnancy Abstract ABSTRACT Rosuvastatin (RSV), a potent HMG‐CoA reductase inhibitor, is widely used for the management of hyperlipidemia and prevention of cardiovascular disease. I...
PMC11739736
core_pubmed_pmc
The Impact of Dexamethasone and Prednisone on Apixaban and Rivaroxaban Exposure in COVID‐19 Patients: A Physiologically Based Pharmacokinetic Modeling Study
The Impact of Dexamethasone and Prednisone on Apixaban and Rivaroxaban Exposure in COVID‐19 Patients: A Physiologically Based Pharmacokinetic Modeling Study Abstract Dexamethasone (DEX) is currently the treatment of choice for patients with oxygen‐dependent COVID‐19. It has been observed, primarily in vitro , that dexa...
PMC12695791
core_pubmed_pmc
Case Report: A pharmacist-led precision therapy framework for managing invasive fungal infection in CSF1R-Related leukoencephalopathy post Allo-HSCT
Case Report: A pharmacist-led precision therapy framework for managing invasive fungal infection in CSF1R-Related leukoencephalopathy post Allo-HSCT Abstract Abstract Introduction Hereditary diffuse leukoencephalopathy with spheroids (HDLS), caused by CSF1R mutations, is a rare autosomal dominant leukodystrophy charact...
PMC8698108
core_pubmed_pmc
Pharmacokinetic Profile of Fentanyl in the Koala ( Phascolarctos cinereus ) after Intravenous Administration, and Absorption via a Transdermal Patch
Pharmacokinetic Profile of Fentanyl in the Koala ( Phascolarctos cinereus ) after Intravenous Administration, and Absorption via a Transdermal Patch Abstract Abstract Simple Summary Koalas can be injured by cars and bushfires, and be affected by painful infectious diseases. When koalas undergo surgery to repair broken ...
PMC10011485
core_pubmed_pmc
Safety, tolerability, pharmacokinetics, pharmacodynamics, and efficacy of WBP216, a novel IL-6 monoclonal antibody, in patients with rheumatoid arthritis: A phase Ia randomized placebo-controlled study
Safety, tolerability, pharmacokinetics, pharmacodynamics, and efficacy of WBP216, a novel IL-6 monoclonal antibody, in patients with rheumatoid arthritis: A phase Ia randomized placebo-controlled study Abstract Background WBP216 is a novel human immunoglobulin G1 (IgG1) monoclonal antibody for interleukin (IL)-6. We ai...
PMC9170314
core_pubmed_pmc
Oral NAloxone to overcome the moRphine effect in acute COronary syndrome patients treated with TICagrelor — NARCOTIC trial
Oral NAloxone to overcome the moRphine effect in acute COronary syndrome patients treated with TICagrelor — NARCOTIC trial Abstract Abstract Background Numerous worldwide clinical trials have proven the indisputably negative influence of morphine on the pharmacokinetics and pharmacodynamics of P2Y 12 receptor inhibitor...
PMC7297476
core_pubmed_pmc
Comparison of Vancomycin Pharmacokinetics in Cystic Fibrosis Patients Pre and Post-lung Transplant
Comparison of Vancomycin Pharmacokinetics in Cystic Fibrosis Patients Pre and Post-lung Transplant Abstract Background: Vancomycin is commonly used to treat acute cystic fibrosis (CF) exacerbations associated with methicillin-resistant Staphylococcus aureus (MRSA). Multiple studies have demonstrated pharmacokinetic dif...
PMC7866862
core_pubmed_pmc
Screening, Optimization, and Bioavailability Research of Natural Deep Eutectic Solvent Extracts from Radix Pueraria
Screening, Optimization, and Bioavailability Research of Natural Deep Eutectic Solvent Extracts from Radix Pueraria Abstract Abstract Natural deep eutectic solvent (NaDES) is generally considered as a greener alternative to fossil solvent, with great potential in various areas. In the present work, 25 different NaDESs ...
PMC8866711
core_pubmed_pmc
Knowledge Gaps in the Pharmacokinetics of Therapeutic Proteins in Pediatric Patients
Knowledge Gaps in the Pharmacokinetics of Therapeutic Proteins in Pediatric Patients Abstract Abstract Therapeutic proteins such as monoclonal antibodies and their derivatives, fusions proteins, hormone analogs and enzymes for replacement therapy are an ever-growing mainstay in our pharmacopoeia. While a growing number...
PMC8667943
core_pubmed_pmc
Pharmacokinetics of ponazuril after administration of a single oral dose to green turtles ( Chelonia mydas )
Pharmacokinetics of ponazuril after administration of a single oral dose to green turtles ( Chelonia mydas ) Abstract Abstract The coccidian protozoan, Caryospora cheloniae , has been associated with severe enteritis and encephalitis in immature farm-raised green turtles ( Chelonia mydas ) in the Cayman Islands, immatu...
PMC9781550
core_pubmed_pmc
Pharmacogenetic Dose Modeling Based on CYP2C19 Allelic Phenotypes
Pharmacogenetic Dose Modeling Based on CYP2C19 Allelic Phenotypes Abstract Pharmacogenetic variability in drug metabolism leads to patient vulnerability to side effects and to therapeutic failure. Our purpose was to introduce a systematic statistical methodology to estimate quantitative dose adjustments based on pharma...
PMC10253730
core_pubmed_pmc
Sustaining Life versus Altering Life-Saving Drugs: Insights to Explain the Paradoxical Effect of Extracorporeal Membrane Oxygenation on Drugs
Sustaining Life versus Altering Life-Saving Drugs: Insights to Explain the Paradoxical Effect of Extracorporeal Membrane Oxygenation on Drugs Abstract Abstract There has been a substantial increase in the use of extracorporeal membrane oxygenation (ECMO) support in critically ill adults. Understanding the complex chang...
PMC3373380
core_pubmed_pmc
Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor
Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor Abstract Background Dipeptidylpeptidase 4 (DPP4) inhibitors have clinical benefit in patients with type 2 diabetes mellitus by incr...
PMC12473039
core_pubmed_pmc
Interventions for Neglected Diseases Caused by Kinetoplastid Parasites: A One Health Approach to Drug Discovery, Development, and Deployment
Interventions for Neglected Diseases Caused by Kinetoplastid Parasites: A One Health Approach to Drug Discovery, Development, and Deployment Abstract Abstract Kinetoplastids are protozoa that possess a unique organelle called a kinetoplast. These include the parasites Trypanosoma cruzi , T. brucei and related African t...
PMC5914277
core_pubmed_pmc
Effects of Genetic Polymorphisms of CYP2B6 on the Pharmacokinetics of Bupropion and Hydroxybupropion in Healthy Chinese Subjects
Effects of Genetic Polymorphisms of CYP2B6 on the Pharmacokinetics of Bupropion and Hydroxybupropion in Healthy Chinese Subjects Abstract Abstract Background Bupropion (BUP) is an antidepressant and its pharmacological activity is mediated by its major metabolite, hydroxybupropion (HBUP). We investigated the effects of...
PMC10224275
core_pubmed_pmc
Application of Sucrose Acetate Isobutyrate in Development of Co-Amorphous Formulations of Tacrolimus for Bioavailability Enhancement
Application of Sucrose Acetate Isobutyrate in Development of Co-Amorphous Formulations of Tacrolimus for Bioavailability Enhancement Abstract The focus of the present work was to develop co-amorphous dispersion (CAD) formulations of tacrolimus (TAC) using sucrose acetate isobutyrate as a carrier, evaluate by in vitro a...
PMC10459842
core_pubmed_pmc
Evaluation of Pharmacokinetic Feasibility of Febuxostat/L-pyroglutamic Acid Cocrystals in Rats and Mice
Evaluation of Pharmacokinetic Feasibility of Febuxostat/L-pyroglutamic Acid Cocrystals in Rats and Mice Abstract Febuxostat (FBX), a selective xanthine oxidase inhibitor, belongs to BCS class II, showing low solubility and high permeability with a moderate F value (<49%). Recently, FBX/L-pyroglutamic acid cocrystal (FB...
PMC11365876
core_pubmed_pmc
Impact of Third-Generation Antiseizure Medications on People with Epilepsy in a Low-Income Population: The Brivaracetam Experience in a Real-World Study
Impact of Third-Generation Antiseizure Medications on People with Epilepsy in a Low-Income Population: The Brivaracetam Experience in a Real-World Study Abstract Background Third-generation antiseizure medications, such as brivaracetam, are recognized for their superior safety, tolerability, and pharmacokinetic profile...
PMC7453069
core_pubmed_pmc
Comparative Population Pharmacokinetics of Darunavir in SARS-CoV-2 Patients vs. HIV Patients: The Role of Interleukin-6
Comparative Population Pharmacokinetics of Darunavir in SARS-CoV-2 Patients vs. HIV Patients: The Role of Interleukin-6 Abstract Abstract Background Darunavir is an anti-HIV protease inhibitor repurposed for SARS-CoV-2 treatment. Objective The aim of this study was to assess the population pharmacokinetics of darunavir...
PMC6102747
core_pubmed_pmc
Quercetin-3-O-β-D-glucoside decreases the bioavailability of cyclosporin A through regulation of drug metabolizing enzymes, transporters and nuclear receptors in rats
Quercetin-3-O-β-D-glucoside decreases the bioavailability of cyclosporin A through regulation of drug metabolizing enzymes, transporters and nuclear receptors in rats Abstract Quercetin is a flavonoid compound that is widely present in food and drink. Quercetin-3-O-β-D-glucoside (Q3GA) is a major metabolite of querceti...
PMC12711370
core_pubmed_pmc
Preparation of 18β-Glycyrrhetinic Acid Liposome and Its Therapeutic Effect on Pulmonary Arterial Hypertension
Preparation of 18β-Glycyrrhetinic Acid Liposome and Its Therapeutic Effect on Pulmonary Arterial Hypertension Abstract Abstract Purpose 18β-Glycyrrhetinic acid liposomes (18β-GA-Lips) were developed to enhance lung-specific drug delivery and optimize the therapeutic management of pulmonary arterial hypertension (PAH). ...
PMC9794608
core_pubmed_pmc
Pharmacokinetics and tolerability of the dual TORC1/2 inhibitor sapanisertib in combination with the MEK inhibitor trametinib in dogs
Pharmacokinetics and tolerability of the dual TORC1/2 inhibitor sapanisertib in combination with the MEK inhibitor trametinib in dogs Abstract Abstract Activation of one or both the Ras/MAPK and PI3K/Akt/mTOR signal transduction pathways are known to mediate oncogenicity of several canine and human cancers, including m...
PMC7188703
core_pubmed_pmc
Pharmacokinetics of polatuzumab vedotin in combination with R/G-CHP in patients with B-cell non-Hodgkin lymphoma
Pharmacokinetics of polatuzumab vedotin in combination with R/G-CHP in patients with B-cell non-Hodgkin lymphoma Abstract Purpose The phase Ib/II open-label study ( NCT01992653 ) evaluated the antibody-drug conjugate polatuzumab vedotin (pola) plus rituximab/obinutuzumab, cyclophosphamide, doxorubicin, and prednisone (...
PMC10205783
core_pubmed_pmc
Characterization and translational development of IOA-289, a novel autotaxin inhibitor for the treatment of solid tumors
Characterization and translational development of IOA-289, a novel autotaxin inhibitor for the treatment of solid tumors Abstract Abstract Background Autotaxin-lysophosphatidic acid (ATX-LPA) signaling has a predominant role in immunological and fibrotic processes, including cancer. Several ATX inhibitors and LPA recep...
PMC6132549
core_pubmed_pmc
Population pharmacokinetics of levodopa/carbidopa microtablets in healthy subjects and Parkinson’s disease patients
Population pharmacokinetics of levodopa/carbidopa microtablets in healthy subjects and Parkinson’s disease patients Abstract Objectives Low dose, dispersible, levodopa/carbidopa microtablets with an automatic dose dispenser have been developed to facilitate individualized levodopa treatment. The aim of this study was t...
PMC8964862
core_pubmed_pmc
A Randomized, Open-Label, Single-Dose Study to Assess Safety and Systemic Exposure of Triamcinolone Acetonide Extended-Release in Patients With Hip Osteoarthritis
A Randomized, Open-Label, Single-Dose Study to Assess Safety and Systemic Exposure of Triamcinolone Acetonide Extended-Release in Patients With Hip Osteoarthritis Abstract Abstract Introduction Intra-articular (IA) corticosteroids, including triamcinolone acetonide (TA), are a recommended treatment for hip osteoarthrit...
PMC10725259
core_pubmed_pmc
Physiologically‐based pharmacokinetic model to predict doxorubicin and paclitaxel exposure in infants through breast milk
Physiologically‐based pharmacokinetic model to predict doxorubicin and paclitaxel exposure in infants through breast milk Abstract Abstract Limited information is available concerning infant exposure and safety when breastfed by mothers receiving chemotherapy. Whereas defining distribution to breast milk is important t...
PMC11794604
core_pubmed_pmc
Development of an mPBPK machine learning framework for early target pharmacology assessment of biotherapeutics
Development of an mPBPK machine learning framework for early target pharmacology assessment of biotherapeutics Abstract Development of antibodies often begins with the assessment and optimization of their physicochemical properties, and their efficient engagement with the target of interest. Decisions at the early opti...
PMC2959074
core_pubmed_pmc
Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine
Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine Abstract Background Artemether-lumefantrine is one of the most widely used anti-malarial drug combinations in the world with excellent tolerability and cure rates in adult and paediatric patie...
PMC9890763
core_pubmed_pmc
Pharmacokinetics of a microdosed cocktail of three direct oral anticoagulants in children with congenital heart defects: study protocol for a single-centre clinical trial (DOAC-Child)
Pharmacokinetics of a microdosed cocktail of three direct oral anticoagulants in children with congenital heart defects: study protocol for a single-centre clinical trial (DOAC-Child) Abstract Abstract Introduction Direct oral anticoagulants (DOACs) are direct inhibitors of coagulation factor Xa and are frequently used...
PMC5986181
core_pubmed_pmc
Toxicity Testing in the 21 st Century Beyond Environmental Chemicals
Toxicity Testing in the 21 st Century Beyond Environmental Chemicals Abstract Summary After the publication of the report titled Toxicity Testing in the 21 st Century – A Vision and a Strategy , many initiatives started to foster a major paradigm shift for toxicity testing – from apical endpoints in animal-based tests ...
PMC8572678
core_pubmed_pmc
Quantitative determination of D 4 -cystine in mice using LC-MS/MS and its application to the assessment of pharmacokinetics and bioavailability
Quantitative determination of D 4 -cystine in mice using LC-MS/MS and its application to the assessment of pharmacokinetics and bioavailability Abstract Abstract Cystine is the primary source material for the synthesis of glutathione. However, the pharmacokinetics and tissue distribution of cystine are largely unknown....
PMC8775965
core_pubmed_pmc
Dynamic Contrast-Enhanced Magnetic Resonance Imaging for the Prediction of Monoclonal Antibody Tumor Disposition
Dynamic Contrast-Enhanced Magnetic Resonance Imaging for the Prediction of Monoclonal Antibody Tumor Disposition Abstract The prediction of monoclonal antibody (mAb) disposition within solid tumors for individual patients is difficult due to inter-patient variability in tumor physiology. Improved a priori prediction of...
PMC6004234
core_pubmed_pmc
Suboptimal Antituberculosis Drug Concentrations and Outcomes in Small and HIV‐Coinfected Children in India: Recommendations for Dose Modifications
Suboptimal Antituberculosis Drug Concentrations and Outcomes in Small and HIV‐Coinfected Children in India: Recommendations for Dose Modifications Abstract Abstract This work aimed to evaluate the once‐daily antituberculosis treatment as recommended by the new Indian pediatric guidelines. Isoniazid, rifampin, and pyraz...
PMC7682474
core_pubmed_pmc
Eftilagimod alpha, a soluble lymphocyte activation gene-3 (LAG-3) protein plus pembrolizumab in patients with metastatic melanoma
Eftilagimod alpha, a soluble lymphocyte activation gene-3 (LAG-3) protein plus pembrolizumab in patients with metastatic melanoma Abstract Abstract Background To evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of eftilagimod alpha (efti), a soluble lymphocyte activation gene-3 protein, in combi...
PMC8598183
core_pubmed_pmc
Treating insomnia symptoms with medicinal cannabis: a randomized, crossover trial of the efficacy of a cannabinoid medicine compared with placebo
Treating insomnia symptoms with medicinal cannabis: a randomized, crossover trial of the efficacy of a cannabinoid medicine compared with placebo Abstract Abstract Study Objectives This randomized, double-blind, placebo-controlled, crossover study was conducted to evaluate the safety and efficacy of 2 weeks of nightly ...
PMC5816749
core_pubmed_pmc
Genetic Parameter Estimates for Metabolizing Two Common Pharmaceuticals in Swine
Genetic Parameter Estimates for Metabolizing Two Common Pharmaceuticals in Swine Abstract In livestock, the regulation of drugs used to treat livestock has received increased attention and it is currently unknown how much of the phenotypic variation in drug metabolism is due to the genetics of an animal. Therefore, the...
PMC7511285
core_pubmed_pmc
Rectal Omeprazole in Infants With Gastroesophageal Reflux Disease: A Randomized Pilot Trial
Rectal Omeprazole in Infants With Gastroesophageal Reflux Disease: A Randomized Pilot Trial Abstract Abstract Background and Objective Omeprazole is a proton pump inhibitor that is used in acid suppression therapy in infants. Infants cannot swallow the oral tablets or capsules. Since, infants require a non-standard dos...
PMC11237172
core_pubmed_pmc
No dose adjustment of metformin or substrates of organic cation transporters (OCT)1 and OCT2 and multidrug and toxin extrusion protein (MATE)1/2K with fostemsavir coadministration based on modeling approaches
No dose adjustment of metformin or substrates of organic cation transporters (OCT)1 and OCT2 and multidrug and toxin extrusion protein (MATE)1/2K with fostemsavir coadministration based on modeling approaches Abstract Abstract Fostemsavir is an approved gp120‐directed attachment inhibitor and prodrug for the treatment ...
PMC5465826
core_pubmed_pmc
Stereospecific pharmacokinetic characterization of liquiritigenin in the rat
Stereospecific pharmacokinetic characterization of liquiritigenin in the rat Abstract Liquiritigenin is a chiral flavonoid present in licorice and other medicinal plants. The nature of its biological fate with respect to the individual enantiomers has not been examined. In this study, we characterize, for the first tim...
PMC11912748
core_pubmed_pmc
Image-Guided Monitoring of Mitochondria and Blood–Brain Barrier Dysfunction in Amyotrophic Lateral Sclerosis Mice
Image-Guided Monitoring of Mitochondria and Blood–Brain Barrier Dysfunction in Amyotrophic Lateral Sclerosis Mice Abstract Abstract Early detection of amyotrophic lateral sclerosis (ALS) progression is critical for improving disease management and therapeutic outcomes. However, the clinical heterogeneity and variabilit...
PMC12706417
core_pubmed_pmc
A Combined Modeling Approach to Predict the Effect of Gastric Emptying Delay on the Pharmacokinetics of Small Molecules
A Combined Modeling Approach to Predict the Effect of Gastric Emptying Delay on the Pharmacokinetics of Small Molecules Abstract ABSTRACT Dulaglutide, a long‐acting glucagon‐like peptide‐1 (GLP‐1) receptor agonist, is approved for improving glycemic control and reducing cardiovascular risks in patients with type 2 diab...
PMC11374901
core_pubmed_pmc
Quantifying trade-offs between therapeutic efficacy and resistance dissemination for enrofloxacin dose regimens in cattle
Quantifying trade-offs between therapeutic efficacy and resistance dissemination for enrofloxacin dose regimens in cattle Abstract Abstract The use of antimicrobial drugs in food-producing animals contributes to the selection pressure on pathogenic and commensal bacteria to become resistant. This study aims to evaluate...
PMC7049277
core_pubmed_pmc
Contribution of Trough Concentration Data in the Evaluation of Multiple-Dose Pharmacokinetics for Drugs with Delayed Distributional Equilibrium and Long Half-Life
Contribution of Trough Concentration Data in the Evaluation of Multiple-Dose Pharmacokinetics for Drugs with Delayed Distributional Equilibrium and Long Half-Life Abstract Abstract Purpose The performance of “trough sampling before reaching steady-state” and “serial sampling beyond the interval between steady-state” in...
PMC7759869
core_pubmed_pmc
Identification of Enzymes Oxidizing the Tyrosine Kinase Inhibitor Cabozantinib: Cabozantinib Is Predominantly Oxidized by CYP3A4 and Its Oxidation Is Stimulated by cyt b 5 Activity
Identification of Enzymes Oxidizing the Tyrosine Kinase Inhibitor Cabozantinib: Cabozantinib Is Predominantly Oxidized by CYP3A4 and Its Oxidation Is Stimulated by cyt b 5 Activity Abstract Abstract Herein, the in vitro metabolism of tyrosine kinase inhibitor cabozantinib, the drug used for the treatment of metastatic ...
PMC6195370
core_pubmed_pmc
The clinical relevance of progestogens in hormonal contraception: Present status and future developments
The clinical relevance of progestogens in hormonal contraception: Present status and future developments Abstract Abstract The contraceptive pill is an effective and very safe method to control pregnancies. It was developed 60 years ago, and despite, that the composition has been the same since it was first developed (...
PMC4752501
core_pubmed_pmc
EPICE-HIV: An Epidemiologic Cost-Effectiveness Model for HIV Treatment
EPICE-HIV: An Epidemiologic Cost-Effectiveness Model for HIV Treatment Abstract The goal of this research was to establish a new and innovative framework for cost-effectiveness modeling of HIV-1 treatment, simultaneously considering both clinical and epidemiological outcomes. EPICE-HIV is a multi-paradigm model based o...
PMC9794590
core_pubmed_pmc
Physiologically based pharmacokinetic modelling and simulation to predict the plasma concentration profile of schaftoside after oral administration of total flavonoids of Desmodium styracifolium
Physiologically based pharmacokinetic modelling and simulation to predict the plasma concentration profile of schaftoside after oral administration of total flavonoids of Desmodium styracifolium Abstract Abstract Introduction: The total flavonoids of Desmodium styracifolium (TFDS) are the flavonoid extracts purified fr...
PMC4203514
core_pubmed_pmc
Phase I trial of hydroxychloroquine with dose-intense temozolomide in patients with advanced solid tumors and melanoma
Phase I trial of hydroxychloroquine with dose-intense temozolomide in patients with advanced solid tumors and melanoma Abstract Blocking autophagy with hydroxychloroquine (HCQ) augments cell death associated with alkylating chemotherapy in preclinical models. This phase I study evaluated the maximum tolerated dose (MTD...
PMC2914736
core_pubmed_pmc
First administration to man of Org 25435, an intravenous anaesthetic: A Phase 1 Clinical Trial
First administration to man of Org 25435, an intravenous anaesthetic: A Phase 1 Clinical Trial Abstract Background Org 25435 is a new water-soluble alpha-amino acid ester intravenous anaesthetic which proved satisfactory in animal studies. This study aimed to assess the safety, tolerability and efficacy of Org 25435 an...
PMC9541965
core_pubmed_pmc
Kinetics of 5% and 20% albumin: A controlled crossover trial in volunteers
Kinetics of 5% and 20% albumin: A controlled crossover trial in volunteers Abstract Abstract Background Albumin for intravenous infusion is marketed in two concentrations, 20% and 5%, but how they compare with regard to plasma volume expansion over time is unclear. Methods In a prospective crossover study, 12 volunteer...
PMC5193001
core_pubmed_pmc
Modeling of Large Pharmacokinetic Data Using Nonlinear Mixed‐Effects: A Paradigm Shift in Veterinary Pharmacology. A Case Study With Robenacoxib in Cats
Modeling of Large Pharmacokinetic Data Using Nonlinear Mixed‐Effects: A Paradigm Shift in Veterinary Pharmacology. A Case Study With Robenacoxib in Cats Abstract Abstract The objective of this study was to model the pharmacokinetics (PKs) of robenacoxib in cats using a nonlinear mixed‐effects (NLME) approach, leveragin...
PMC9403128
core_pubmed_pmc
Drosophila melanogaster diabetes models and its usage in the research of anti-diabetes management with traditional Chinese medicines
Drosophila melanogaster diabetes models and its usage in the research of anti-diabetes management with traditional Chinese medicines Abstract Abstract The prevalence of diabetes mellitus (DM) is increasing rapidly worldwide, but the underlying molecular mechanisms of disease development have not been elucidated, and th...
PMC6856490
core_pubmed_pmc
Population Pharmacokinetics of Sarilumab in Patients with Rheumatoid Arthritis
Population Pharmacokinetics of Sarilumab in Patients with Rheumatoid Arthritis Abstract Background and Objective Sarilumab binds to the interleukin-6 receptor with high affinity, inhibiting cis and trans signaling by interleukin-6. Sarilumab has demonstrated efficacy and safety in patients with rheumatoid arthritis. Th...
PMC9664624
core_pubmed_pmc
Dual-labeled nanoparticles based on small extracellular vesicles for tumor detection
Dual-labeled nanoparticles based on small extracellular vesicles for tumor detection Abstract Abstract Background Small extracellular vesicles (sEVs) are emerging natural nanoplatforms in cancer diagnosis and therapy, through the incorporation of signal components or drugs in their structure. However, for their transla...
PMC8752106
core_pubmed_pmc
Pharmacokinetic‐pharmacodynamic modelling of the anti‐FcRn monoclonal antibody rozanolixizumab: Translation from preclinical stages to the clinic
Pharmacokinetic‐pharmacodynamic modelling of the anti‐FcRn monoclonal antibody rozanolixizumab: Translation from preclinical stages to the clinic Abstract Abstract Rozanolixizumab is a fully humanized high‐affinity anti‐human neonatal Fc receptor (FcRn) monoclonal antibody (mAb) that accelerates the removal of circulat...
PMC12527224
core_pubmed_pmc
Hit-to-Lead Optimization of Acetazolamide-Based Bacterial Carbonic Anhydrase Inhibitors with Efficacy In Vivo for Treatment of Vancomycin-Resistant Enterococci Septicemia
Hit-to-Lead Optimization of Acetazolamide-Based Bacterial Carbonic Anhydrase Inhibitors with Efficacy In Vivo for Treatment of Vancomycin-Resistant Enterococci Septicemia Abstract Abstract As one of the leading causes of hospital-acquired infections reported by the National Healthcare Safety Network, vancomycin-resista...