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PMC7459170
core_pubmed_pmc
The HIV drug optimization agenda: promoting standards for earlier investigation and approvals of antiretroviral drugs for use in adolescents living with HIV
The HIV drug optimization agenda: promoting standards for earlier investigation and approvals of antiretroviral drugs for use in adolescents living with HIV Abstract Abstract Introduction Most clinical trials for new antiretroviral (ARV) agents are conducted among narrowly defined adult populations. Only after safety a...
PMC10362366
core_pubmed_pmc
Efficacy and safety of SIM0417 (SSD8432) plus ritonavir for COVID-19 treatment: a randomised, double-blind, placebo-controlled, phase 1b trial
Efficacy and safety of SIM0417 (SSD8432) plus ritonavir for COVID-19 treatment: a randomised, double-blind, placebo-controlled, phase 1b trial Abstract Summary Background SIM0417 (SSD8432) is an orally administered coronavirus main proteinase (3CL pro ) inhibitor with potential anti-SARS-CoV-2 activity. This study aime...
PMC11012829
core_pubmed_pmc
Self-Assembled Nanoparticles from Xie-Bai-San Decoction: Isolation, Characterization and Enhancing Oral Bioavailability
Self-Assembled Nanoparticles from Xie-Bai-San Decoction: Isolation, Characterization and Enhancing Oral Bioavailability Abstract Background Natural nanoparticles have been found to exist in traditional Chinese medicine (TCM) decoctions. However, whether natural nanoparticles can influence the oral bioavailability of ac...
PMC6925790
core_pubmed_pmc
Study on Pharmacokinetic and Bioavailability of Tamarixetin after Intravenous and Oral Administration to Rats
Study on Pharmacokinetic and Bioavailability of Tamarixetin after Intravenous and Oral Administration to Rats Abstract In this study, a sensitive and reliable HPLC-MS/MS method was established to quantify tamarixetin in rat plasma. This method was then applied to research on the pharmacokinetic and bioavailability of t...
PMC8206201
core_pubmed_pmc
Pharmacological and clinical evaluation of deferasirox formulations for treatment tailoring
Pharmacological and clinical evaluation of deferasirox formulations for treatment tailoring Abstract Deferasirox (DFX) is the newest among three different chelators available to treat iron overload in iron-loading anaemias, firstly released as Dispersible Tablets (DT) and more recently replaced by Film-Coated Tablets (...
PMC6597476
core_pubmed_pmc
MolMeDB: Molecules on Membranes Database
MolMeDB: Molecules on Membranes Database Abstract Abstract Biological membranes act as barriers or reservoirs for many compounds within the human body. As such, they play an important role in pharmacokinetics and pharmacodynamics of drugs and other molecular species. Until now, most membrane/drug interactions have been...
PMC12519522
core_pubmed_pmc
An In Vitro Calibration Model for Vancomycin Quantification in Brain Extracellular Fluid: Toward Improved Dosing in Postoperative Infections
An In Vitro Calibration Model for Vancomycin Quantification in Brain Extracellular Fluid: Toward Improved Dosing in Postoperative Infections Abstract ABSTRACT Postoperative central nervous system (CNS) infections are associated with high mortality and present a therapeutic challenge due to limited antibiotic penetratio...
PMC9318802
core_pubmed_pmc
Optimization of 2-Aminoquinazolin-4-(3 H )-one Derivatives as Potent Inhibitors of SARS-CoV-2: Improved Synthesis and Pharmacokinetic Properties
Optimization of 2-Aminoquinazolin-4-(3 H )-one Derivatives as Potent Inhibitors of SARS-CoV-2: Improved Synthesis and Pharmacokinetic Properties Abstract Abstract We previously reported the potent antiviral effect of the 2-aminoquinazolin-4-(3 H )-one 1, which shows significant activity (IC 50 = 0.23 μM) against severe...
PMC6027733
core_pubmed_pmc
First‐Pass CYP3A‐Mediated Metabolism of Midazolam in the Gut Wall and Liver in Preterm Neonates
First‐Pass CYP3A‐Mediated Metabolism of Midazolam in the Gut Wall and Liver in Preterm Neonates Abstract Abstract To predict first‐pass and systemic cytochrome P450 (CYP) 3A‐mediated metabolism of midazolam in preterm neonates, a physiological population pharmacokinetic model was developed describing intestinal and hep...
PMC12283299
core_pubmed_pmc
Population pharmacokinetic analysis of remimazolam after continuous infusion for sedation in critically ill patients
Population pharmacokinetic analysis of remimazolam after continuous infusion for sedation in critically ill patients Abstract Introduction The aim of the present prospective study was to model the population pharmacokinetics of remimazolam after continuous infusion in critically ill patients, and to provide a guide for...
PMC5516013
core_pubmed_pmc
A Predictive Mathematical Modeling Approach for the Study of Doxorubicin Treatment in Triple Negative Breast Cancer
A Predictive Mathematical Modeling Approach for the Study of Doxorubicin Treatment in Triple Negative Breast Cancer Abstract Doxorubicin forms the basis of chemotherapy regimens for several malignancies, including triple negative breast cancer (TNBC). Here, we present a coupled experimental/modeling approach to establi...
PMC11893874
core_pubmed_pmc
Enhancing antibiotic therapy through comprehensive pharmacokinetic/pharmacodynamic principles
Enhancing antibiotic therapy through comprehensive pharmacokinetic/pharmacodynamic principles Abstract Antibiotic therapy relies on understanding both pharmacokinetics (PK) and pharmacodynamics (PD), which respectively address drug absorption, distribution, and elimination, and the relationship between drug concentrati...
PMC8446031
core_pubmed_pmc
A novel antioxidant ergothioneine PET radioligand for in vivo imaging applications
A novel antioxidant ergothioneine PET radioligand for in vivo imaging applications Abstract Ergothioneine (ERGO) is a rare amino acid mostly found in fungi, including mushrooms, with recognized antioxidant activity to protect tissues from damage by reactive oxygen species (ROS) components. Prior to this publication, th...
PMC6538570
core_pubmed_pmc
First-in-human phase 1 study of novel dUTPase inhibitor TAS-114 in combination with S-1 in Japanese patients with advanced solid tumors
First-in-human phase 1 study of novel dUTPase inhibitor TAS-114 in combination with S-1 in Japanese patients with advanced solid tumors Abstract Summary Background This first-in-human phase 1 study assessed the safety of TAS-114, a novel deoxyuridine triphosphatase inhibitor, combined with S-1 to determine its maximum ...
PMC7027517
core_pubmed_pmc
Development of a Subcutaneous Fixed‐Dose Combination of Pertuzumab and Trastuzumab: Results From the Phase Ib Dose‐Finding Study
Development of a Subcutaneous Fixed‐Dose Combination of Pertuzumab and Trastuzumab: Results From the Phase Ib Dose‐Finding Study Abstract Abstract Adding pertuzumab to trastuzumab (both monoclonal antibodies targeting human epidermal growth factor receptor 2 [HER2]) has proven survival benefits when combined with chemo...
PMC12484422
core_pubmed_pmc
Population Pharmacokinetics and Exposure–Response Relationships of Etrolizumab in Patients with Moderately‐to‐Severely Active Crohn's Disease
Population Pharmacokinetics and Exposure–Response Relationships of Etrolizumab in Patients with Moderately‐to‐Severely Active Crohn's Disease Abstract Abstract This study aimed to characterize the pharmacokinetics (PK) of etrolizumab, an IgG1‐humanized monoclonal anti‐β7 integrin antibody, and assess its exposure–respo...
PMC4914069
core_pubmed_pmc
Development of self-nanoemulsifying drug delivery systems for the enhancement of solubility and oral bioavailability of fenofibrate, a poorly water-soluble drug
Development of self-nanoemulsifying drug delivery systems for the enhancement of solubility and oral bioavailability of fenofibrate, a poorly water-soluble drug Abstract Abstract Background Self-nanoemulsifying drug delivery systems (SNEDDS) have become a popular formulation option as nanocarriers for poorly water-solu...
PMC10823477
core_pubmed_pmc
Novel Psilocin Prodrugs with Altered Pharmacological Properties as Candidate Therapies for Treatment-Resistant Anxiety Disorders
Novel Psilocin Prodrugs with Altered Pharmacological Properties as Candidate Therapies for Treatment-Resistant Anxiety Disorders Abstract Abstract The psychedelic prodrug psilocybin has shown therapeutic benefits for the treatment of numerous psychiatric conditions. Despite positive clinical end points targeting depres...
PMC3172043
core_pubmed_pmc
Dosing regimens of oral ciprofloxacin for children with severe malnutrition: a population pharmacokinetic study with Monte Carlo simulation
Dosing regimens of oral ciprofloxacin for children with severe malnutrition: a population pharmacokinetic study with Monte Carlo simulation Abstract Abstract Background Severe malnutrition is frequently complicated by sepsis, leading to high case fatality. Oral ciprofloxacin is a potential alternative to the standard p...
PMC12291498
core_pubmed_pmc
Identification of a moxidectin dose for 4- to 11-year-old children to support registration and potential use for onchocerciasis elimination: results of an open-label pharmacokinetic and safety study
Identification of a moxidectin dose for 4- to 11-year-old children to support registration and potential use for onchocerciasis elimination: results of an open-label pharmacokinetic and safety study Abstract Abstract Background The WHO and onchocerciasis-endemic countries target elimination of the transmission of Oncho...
PMC3751365
core_pubmed_pmc
Pharmacokinetics of flunixin meglumine in mature swine after intravenous, intramuscular and oral administration
Pharmacokinetics of flunixin meglumine in mature swine after intravenous, intramuscular and oral administration Abstract Abstract Background The purpose of this study was to determine intravenous (IV), intramuscular (IM) and oral (PO) FM PK in mature swine. Appropriate pain management for lameness in swine is a critica...
PMC11650737
core_pubmed_pmc
Developing MYC Degraders Bearing the Von Hippel–Lindau Ligand to Target the “Undruggable” MYC
Developing MYC Degraders Bearing the Von Hippel–Lindau Ligand to Target the “Undruggable” MYC Abstract Abstract Although small-molecule inhibitors with moderate efficacy targeting MYC have been previously described, to this point, research efforts have failed to bring a suitable small-molecule MYC inhibitor to the clin...
PMC4227173
core_pubmed_pmc
The Pharmacokinetics and Pharmacodynamics of Lidocaine-Loaded Biodegradable Poly(lactic- co -glycolic acid) Microspheres
The Pharmacokinetics and Pharmacodynamics of Lidocaine-Loaded Biodegradable Poly(lactic- co -glycolic acid) Microspheres Abstract The purpose of this study was to develop novel lidocaine microspheres. Microspheres were prepared by the oil-in-water (o/w) emulsion technique using poly( d , l -lactide- co -glycolide acid)...
PMC11653107
core_pubmed_pmc
Development of a UPLC-MS/MS method for the determination of sulfatinib and its no interaction with myricetin in rats
Development of a UPLC-MS/MS method for the determination of sulfatinib and its no interaction with myricetin in rats Abstract Introduction Sulfatinib is a novel oral tyrosine kinase inhibitor (TKI) with selective inhibition of fibroblast growth factor (FGFR), colony-stimulating factor 1 receptor (CSF-1R) and vascular e...
PMC4994799
core_pubmed_pmc
Effects of roflumilast in COPD patients receiving inhaled corticosteroid/long-acting β 2 -agonist fixed-dose combination: RE 2 SPOND rationale and study design
Effects of roflumilast in COPD patients receiving inhaled corticosteroid/long-acting β 2 -agonist fixed-dose combination: RE 2 SPOND rationale and study design Abstract Abstract Background Roflumilast, a once-daily, selective phosphodiesterase-4 inhibitor, reduces the risk of COPD exacerbations in patients with severe ...
PMC9506478
core_pubmed_pmc
Enteric Polymer–Based Amorphous Solid Dispersions Enhance Oral Absorption of the Weakly Basic Drug Nintedanib via Stabilization of Supersaturation
Enteric Polymer–Based Amorphous Solid Dispersions Enhance Oral Absorption of the Weakly Basic Drug Nintedanib via Stabilization of Supersaturation Abstract Abstract The pH–induced crystallization of weakly basic drugs in the small intestine limits oral bioavailability. In this study, we investigated the solubilization ...
PMC5440938
core_pubmed_pmc
Clinical outcomes of linezolid and vancomycin in patients with nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus stratified by baseline renal function: a retrospective, cohort analysis
Clinical outcomes of linezolid and vancomycin in patients with nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus stratified by baseline renal function: a retrospective, cohort analysis Abstract Background The primary objective of this study is to assess whether baseline renal function impacts t...
PMC4233664
core_pubmed_pmc
Synergistic Effects of Clopidogrel and Fufang Danshen Dripping Pills by Modulation of the Metabolism Target and Pharmacokinetics
Synergistic Effects of Clopidogrel and Fufang Danshen Dripping Pills by Modulation of the Metabolism Target and Pharmacokinetics Abstract Background and Objective. The aim was to evaluate the synergistic effects of clopidogrel and FDDP by modulating the metabolism target and the pharmacokinetics. Methods . The inhibiti...
PMC12821322
core_pubmed_pmc
Key refinements to a large animal model for measurement of real-time lymphatic transport
Key refinements to a large animal model for measurement of real-time lymphatic transport Abstract Abstract Background The inability to directly measure real-time lymphatic transport hinders our understanding of lymphatic disorders and effective monitoring of therapeutic interventions. Here, we report three refinements ...
PMC7526649
core_pubmed_pmc
A Systematic Review of the Pharmacology, Toxicology and Pharmacokinetics of Matrine
A Systematic Review of the Pharmacology, Toxicology and Pharmacokinetics of Matrine Abstract Matrine (MT) is a naturally occurring alkaloid and an bioactive component of Chinese herbs, such as Sophora flavescens and Radix Sophorae tonkinensis . Emerging evidence suggests that MT possesses anti-cancer, anti-inflammatory...
PMC6413085
core_pubmed_pmc
A Validated HPLC-MS/MS Assay for 14- O -[(4,6-Diaminopyrimidine-2-yl)thioacetyl] Mutilin in Biological Samples and Its Pharmacokinetic, Distribution and Excretion via Urine and Feces in Rats
A Validated HPLC-MS/MS Assay for 14- O -[(4,6-Diaminopyrimidine-2-yl)thioacetyl] Mutilin in Biological Samples and Its Pharmacokinetic, Distribution and Excretion via Urine and Feces in Rats Abstract 14- O -[(4,6-Diaminopyrimidine-2-yl)thioacetyl] mutilin (DPTM), a novel pleuromutilin candidate with a substituted pyrim...
PMC11775449
core_pubmed_pmc
A review of the Bovis Calculus ’s intervention mechanism and clinical application in ischemic stroke
A review of the Bovis Calculus ’s intervention mechanism and clinical application in ischemic stroke Abstract Abstract Background Bovis Calculus (BC), also named Niuhuang in Chinese, is utilized as a resuscitation drug in Traditional Chinese Medicine (TCM) for the treatment of neurological disorders. Ischemic stroke (I...
PMC10574780
core_pubmed_pmc
Phloretin Transfersomes for Transdermal Delivery: Design, Optimization, and In Vivo Evaluation
Phloretin Transfersomes for Transdermal Delivery: Design, Optimization, and In Vivo Evaluation Abstract Abstract Background: Phloretin (Phl) is a flavonoid compound that contains multiple phenolic hydroxyl groups. It is found in many plants, such as apple leaves, lychee pericarp, and begonia, and has various biological...
PMC8201088
core_pubmed_pmc
Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate
Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate Abstract The dissolution rate is the rate-limiting step for Biopharmaceutics Classification System (BCS) class II drugs to enhance their in vivo pharmacokinetic behaviors. There are some factors affecting the dissolution ...
PMC7857882
core_pubmed_pmc
Ethnopharmacology, Phytochemistry, and Pharmacological Properties of Thymus satureioides Coss.
Ethnopharmacology, Phytochemistry, and Pharmacological Properties of Thymus satureioides Coss. Abstract Abstract Thymus satureioides Coss. (Lamiaceae) is a Moroccan medicinal plant locally known as “Azkouni” or “Zaitra.” It is widely used in traditional medicine to treat various ailments, including hypertension, diabet...
PMC5937873
core_pubmed_pmc
Improving the biopharmaceutical attributes of mangiferin using vitamin E-TPGS co-loaded self-assembled phosholipidic nano-mixed micellar systems
Improving the biopharmaceutical attributes of mangiferin using vitamin E-TPGS co-loaded self-assembled phosholipidic nano-mixed micellar systems Abstract Abstract The current research work encompasses the development, characterization, and evaluation of self-assembled phospholipidic nano-mixed miceller system (SPNMS) o...
PMC4696409
core_pubmed_pmc
Parsing interindividual drug variability: an emerging role for systems pharmacology
Parsing interindividual drug variability: an emerging role for systems pharmacology Abstract There is notable interindividual heterogeneity in drug response, affecting both drug efficacy and toxicity, resulting in patient harm and the inefficient utilization of limited healthcare resources. Pharmacogenomics is at the f...
PMC12340244
core_pubmed_pmc
Safety, pharmacokinetics, and potential benefits of TSH-receptor-specific monoclonal autoantibody K1-70 TM in Japanese Graves’ disease patients: results of a phase 1 trial
Safety, pharmacokinetics, and potential benefits of TSH-receptor-specific monoclonal autoantibody K1-70 TM in Japanese Graves’ disease patients: results of a phase 1 trial Abstract Abstract This phase 1 dose-escalation study evaluated the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of K1-70 TM...
PMC6435120
core_pubmed_pmc
Single- and multiple-dose tolerability, safety, pharmacokinetics, and pharmacodynamics of the dual endothelin receptor antagonist aprocitentan in healthy adult and elderly subjects
Single- and multiple-dose tolerability, safety, pharmacokinetics, and pharmacodynamics of the dual endothelin receptor antagonist aprocitentan in healthy adult and elderly subjects Abstract Background Aprocitentan is an orally active, dual endothelin (ET) receptor antagonist developed for the treatment of hypertension ...
PMC3369128
core_pubmed_pmc
Pharmacokinetic-Pharmacodynamic Modeling of the D 2 and 5-HT 2A Receptor Occupancy of Risperidone and Paliperidone in Rats
Pharmacokinetic-Pharmacodynamic Modeling of the D 2 and 5-HT 2A Receptor Occupancy of Risperidone and Paliperidone in Rats Abstract Purpose A pharmacokinetic-pharmacodynamic (PK-PD) model was developed to describe the time course of brain concentration and dopamine D 2 and serotonin 5-HT 2A receptor occupancy (RO) of t...
PMC6722784
core_pubmed_pmc
Erythrocyte Encapsulated Thymidine Phosphorylase for the Treatment of Patients with Mitochondrial Neurogastrointestinal Encephalomyopathy: Study Protocol for a Multi-Centre, Multiple Dose, Open Label Trial
Erythrocyte Encapsulated Thymidine Phosphorylase for the Treatment of Patients with Mitochondrial Neurogastrointestinal Encephalomyopathy: Study Protocol for a Multi-Centre, Multiple Dose, Open Label Trial Abstract Mitochondrial neurogastrointestinal encephalomyopathy (MNGIE) is an autosomal recessive disorder which pr...
PMC7404706
core_pubmed_pmc
Improved Antithrombotic Activity and Diminished Bleeding Side Effect of a PEGylated α IIb β 3 Antagonist, Disintegrin
Improved Antithrombotic Activity and Diminished Bleeding Side Effect of a PEGylated α IIb β 3 Antagonist, Disintegrin Abstract Polymer polyethylene glycol (PEG), or PEGylation of polypeptides improves protein drug stability by decreasing degradation and reducing renal clearance. To produce a pharmaceutical disintegrin ...
PMC10314757
core_pubmed_pmc
Trastuzumab Charge Variants: a Study on Physicochemical and Pharmacokinetic Properties
Trastuzumab Charge Variants: a Study on Physicochemical and Pharmacokinetic Properties Abstract Background: Post-translational modifications in bioprocessing and storage of recombinant mAbs are the main sources of charge variants. While the profile of these kinds of variants is considered an important quality attribute...
PMC12451260
core_pubmed_pmc
IPH5201, an Anti-CD39 mAb, as Monotherapy or in Combination with Durvalumab in Advanced Solid Tumors
IPH5201, an Anti-CD39 mAb, as Monotherapy or in Combination with Durvalumab in Advanced Solid Tumors Abstract Abstract Purpose: Blocking enzymatic activity of cluster of differentiation 39 (CD39) with IPH5201 may promote antitumor immunity by increasing immunostimulatory ATP and reducing immunosuppressive adenosine lev...
PMC10395004
core_pubmed_pmc
The roles of Cyp1a2 and Cyp2d in pharmacokinetic profiles of serotonin and norepinephrine reuptake inhibitor duloxetine and its metabolites in mice
The roles of Cyp1a2 and Cyp2d in pharmacokinetic profiles of serotonin and norepinephrine reuptake inhibitor duloxetine and its metabolites in mice Abstract Duloxetine (DLX) is widely used to treat major depressive disorder. Little is known about the mechanistic basis for DLX-related adverse effects (e.g., liver injury...
PMC10423460
core_pubmed_pmc
Anesthetic Effect of 2% Amitriptyline Versus 2% Lidocaine: A Comparative Evaluation
Anesthetic Effect of 2% Amitriptyline Versus 2% Lidocaine: A Comparative Evaluation Abstract Abstract Introduction A common dental problem is the fear of pain during needle prick for giving local anesthesia (LA). The needle prick pain during dental procedures often varies with sex and age. Perception of pain depends on...
PMC8003007
core_pubmed_pmc
Particle Forming Amorphous Solid Dispersions: A Mechanistic Randomized Pharmacokinetic Study in Humans
Particle Forming Amorphous Solid Dispersions: A Mechanistic Randomized Pharmacokinetic Study in Humans Abstract Amorphous solid dispersions (ASDs) are a promising drug-delivery strategy to overcome poor solubility through formulation. Currently, the understanding of drug absorption mechanisms from ASDs in humans is inc...
PMC11116644
core_pubmed_pmc
Pharmacodynamic monitoring by residual gene expression of the nuclear factor of activated T cell-regulated genes in lung transplant recipients and its correlation with tacrolimus blood levels
Pharmacodynamic monitoring by residual gene expression of the nuclear factor of activated T cell-regulated genes in lung transplant recipients and its correlation with tacrolimus blood levels Abstract Abstract Introduction Trough blood levels (C 0 ) of tacrolimus are used to adjust drug dosage, but they do not consiste...
PMC4972987
core_pubmed_pmc
Effect of vitamin K 2 on the anticoagulant activity of warfarin during the perioperative period of catheter ablation: Population analysis of retrospective clinical data
Effect of vitamin K 2 on the anticoagulant activity of warfarin during the perioperative period of catheter ablation: Population analysis of retrospective clinical data Abstract Background Catheter ablation is a non-medication therapy for atrial fibrillation, and during the procedure, warfarin is withdrawn in the preop...
PMC3995549
core_pubmed_pmc
Dose selection method for pharmacokinetic study in hemodialysis patients using a subpharmacological dose: oseltamivir as a model drug
Dose selection method for pharmacokinetic study in hemodialysis patients using a subpharmacological dose: oseltamivir as a model drug Abstract Background Dose selection is an important step in pharmacokinetic (PK) studies of hemodialysis patients. We propose a simulation-based dose-selection method for PK studies of he...
PMC3076582
core_pubmed_pmc
Influences on the pharmacokinetics of oxycodone: a multicentre cross-sectional study in 439 adult cancer patients
Influences on the pharmacokinetics of oxycodone: a multicentre cross-sectional study in 439 adult cancer patients Abstract Abstract Objective Oxycodone is widely used for the treatment of cancer pain, but little is known of its pharmacokinetics in cancer pain patients. The aim of this study was to explore the relations...
PMC3232105
core_pubmed_pmc
Pharmacokinetics of dl -praeruptorin A after single-dose intravenous administration to rats with liver cirrhosis
Pharmacokinetics of dl -praeruptorin A after single-dose intravenous administration to rats with liver cirrhosis Abstract Background and the purpose of the study As a novel drug in the treatment of cardiac diseases, dl -praeruptorin A (Pd-Ia) is the major active component of traditional herbal medicine Peucedanum praer...
PMC8405293
core_pubmed_pmc
Pharmacokinetics and Pharmacological Activities of Berberine in Diabetes Mellitus Treatment
Pharmacokinetics and Pharmacological Activities of Berberine in Diabetes Mellitus Treatment Abstract Traditional Chinese medicine (TCM) has good clinical application prospects in diabetes treatment. In addition, TCM is less toxic and/or has fewer side effects and provides various therapeutic effects. Berberine (BBR) is...
PMC5087785
core_pubmed_pmc
Pharmacokinetics and relative bioavailability of fixed-dose combination of clopidogrel and aspirin versus coadministration of individual formulations in healthy Korean men
Pharmacokinetics and relative bioavailability of fixed-dose combination of clopidogrel and aspirin versus coadministration of individual formulations in healthy Korean men Abstract Background Simultaneous prescription of clopidogrel and low-dose aspirin is recommended for the treatment of acute coronary syndrome becaus...
PMC7232864
core_pubmed_pmc
Physiologically‐Based Pharmacokinetic Models for Evaluating Membrane Transporter Mediated Drug–Drug Interactions: Current Capabilities, Case Studies, Future Opportunities, and Recommendations
Physiologically‐Based Pharmacokinetic Models for Evaluating Membrane Transporter Mediated Drug–Drug Interactions: Current Capabilities, Case Studies, Future Opportunities, and Recommendations Abstract Physiologically‐based pharmacokinetic (PBPK) modeling has been extensively used to quantitatively translate in vitro da...
PMC12688074
core_pubmed_pmc
Ustekinumab Intravenous Reinduction after Secondary Loss of Response in Patients with Crohn’s Disease
Ustekinumab Intravenous Reinduction after Secondary Loss of Response in Patients with Crohn’s Disease Abstract Abstract Background The POWER study ( NCT03782376 ) evaluated efficacy and safety of a single ustekinumab intravenous (IV) reinduction dose versus placebo under continued ustekinumab subcutaneous (SC) treatmen...
PMC11850033
core_pubmed_pmc
Development and validation of long-acting recombinant human TSH using SAFA technology
Development and validation of long-acting recombinant human TSH using SAFA technology Abstract Thyrogen, a recombinant human thyroid-stimulating hormone (rhTSH), has a short half-life in the bloodstream, which necessitates multiple doses during treatment. Therefore, we developed a new long-acting rhTSH using anti-serum...
PMC10453289
core_pubmed_pmc
Nanotechnology-Based Drug Delivery Approaches of Mangiferin: Promises, Reality and Challenges in Cancer Chemotherapy
Nanotechnology-Based Drug Delivery Approaches of Mangiferin: Promises, Reality and Challenges in Cancer Chemotherapy Abstract Simple Summary The current review describes mangiferin (MGF), a secondary plant metabolite of a xanthone derivative obtained from mango plants and known for its therapeutic activities. It is pot...
PMC5872589
core_pubmed_pmc
Pharmacokinetic Comparisons of Typical Constituents in Curcumae Rhizoma and Vinegar-Processed Curcumae Rhizoma after Oral Administration to Rats
Pharmacokinetic Comparisons of Typical Constituents in Curcumae Rhizoma and Vinegar-Processed Curcumae Rhizoma after Oral Administration to Rats Abstract The Raw Curcumae Rhizoma (R-CR), included in the Chinese Pharmacopoeia Edition 2015 , is a well-known Chinese herbal medicine. However, the vinegar-processed Curcumae...
PMC11578128
core_pubmed_pmc
Population pharmacokinetic modeling of paired plasma–breast milk lamivudine data for estimation of infant exposure in breastfeeding mother–infant pairs
Population pharmacokinetic modeling of paired plasma–breast milk lamivudine data for estimation of infant exposure in breastfeeding mother–infant pairs Abstract Abstract Around 1.2 million women living with HIV give birth annually, majority of whom will breastfeed their infants while receiving antiretroviral therapy (A...
PMC4269627
core_pubmed_pmc
Population Pharmacokinetics of Cefazolin in Serum and Tissue for Patients with Complicated Skin and Soft Tissue Infections (cSSTI)
Population Pharmacokinetics of Cefazolin in Serum and Tissue for Patients with Complicated Skin and Soft Tissue Infections (cSSTI) Abstract Abstract Introduction Cefazolin is commonly used to treat complicated skin and soft tissue infections (cSSTI) caused by methicillin-susceptible Staphylococcus aureus (MSSA) and Ent...
PMC6876579
core_pubmed_pmc
Semimechanistic Pharmacodynamic Modeling of Aztreonam‐Avibactam Combination to Understand Its Antimicrobial Activity Against Multidrug‐Resistant Gram‐Negative Bacteria
Semimechanistic Pharmacodynamic Modeling of Aztreonam‐Avibactam Combination to Understand Its Antimicrobial Activity Against Multidrug‐Resistant Gram‐Negative Bacteria Abstract Aztreonam‐avibactam ( ATM ‐ AVI ) is a promising combination to treat serious infections caused by multidrug‐resistant ( MDR ) pathogens. Three...
PMC8617944
core_pubmed_pmc
Preclinical Pharmacokinetics and Acute Toxicity in Rats of 5-{[(2E)-3-Bromo-3-carboxyprop-2-enoyl]amino}-2-hydroxybenzoic Acid: A Novel 5-Aminosalicylic Acid Derivative with Potent Anti-Inflammatory Activity
Preclinical Pharmacokinetics and Acute Toxicity in Rats of 5-{[(2E)-3-Bromo-3-carboxyprop-2-enoyl]amino}-2-hydroxybenzoic Acid: A Novel 5-Aminosalicylic Acid Derivative with Potent Anti-Inflammatory Activity Abstract Abstract Compound 5-{[(2E)-3-bromo-3-carboxyprop-2-enoyl]amino}-2-hydroxybenzoic acid ( C1 ), a new 5-a...
PMC5980962
core_pubmed_pmc
Interpretation the Hepatotoxicity Based on Pharmacokinetics Investigated Through Oral Administrated Different Extraction Parts of Polygonum multiflorum on Rats
Interpretation the Hepatotoxicity Based on Pharmacokinetics Investigated Through Oral Administrated Different Extraction Parts of Polygonum multiflorum on Rats Abstract The liver injury induced by Polygonum multiflorum (PM) used for clinical treatment has recently received widespread attention. This study aimed to dete...
PMC6698957
core_pubmed_pmc
ADME Considerations and Bioanalytical Strategies for Pharmacokinetic Assessments of Antibody-Drug Conjugates
ADME Considerations and Bioanalytical Strategies for Pharmacokinetic Assessments of Antibody-Drug Conjugates Abstract Abstract Antibody-drug conjugates (ADCs) are a unique class of biotherapeutics of inherent heterogeneity and correspondingly complex absorption, distribution, metabolism, and excretion (ADME) properties...
PMC3960763
core_pubmed_pmc
Metabotropic Glutamate Receptor 5 Negative Modulation in Phase I Clinical Trial: Potential Impact of Circadian Rhythm on the Neuropsychiatric Adverse Reactions—Do Hallucinations Matter?
Metabotropic Glutamate Receptor 5 Negative Modulation in Phase I Clinical Trial: Potential Impact of Circadian Rhythm on the Neuropsychiatric Adverse Reactions—Do Hallucinations Matter? Abstract Abstract Metabotropic Glutamate Receptor 5 (mGluR5) negative allosteric modulators (NAMs) may play a role in some psychiatric...
PMC4318187
core_pubmed_pmc
Development and Validation of a LC-MS/MS Method for the Simultaneous Estimation of Amlodipine and Valsartan in Human Plasma: Application to a Bioequivalence Study
Development and Validation of a LC-MS/MS Method for the Simultaneous Estimation of Amlodipine and Valsartan in Human Plasma: Application to a Bioequivalence Study Abstract Abstract A reliable, simple, and robust liquid chromatography-tandem mass spectro-metric (LC-MS/MS) method has been developed and validated that emp...
PMC8151202
core_pubmed_pmc
A Whole-Body Physiologically Based Pharmacokinetic Model Characterizing Interplay of OCTs and MATEs in Intestine, Liver and Kidney to Predict Drug-Drug Interactions of Metformin with Perpetrators
A Whole-Body Physiologically Based Pharmacokinetic Model Characterizing Interplay of OCTs and MATEs in Intestine, Liver and Kidney to Predict Drug-Drug Interactions of Metformin with Perpetrators Abstract Abstract Transmembrane transport of metformin is highly controlled by transporters including organic cation transpo...
PMC11500040
core_pubmed_pmc
Asia‐inclusive drug development leveraging principles of ICH E5 and E17 guidelines: Case studies illustrating quantitative clinical pharmacology as a foundational enabler
Asia‐inclusive drug development leveraging principles of ICH E5 and E17 guidelines: Case studies illustrating quantitative clinical pharmacology as a foundational enabler Abstract Abstract With the International Conference on Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) E17 guidelines...
PMC12428957
core_pubmed_pmc
The Identification of Gyrophoric Acid, a Phytochemical Derived from Lichen, as a Potent Inhibitor for Aggregation of Amyloid Beta Peptide: In Silico and Biochemical Evaluation
The Identification of Gyrophoric Acid, a Phytochemical Derived from Lichen, as a Potent Inhibitor for Aggregation of Amyloid Beta Peptide: In Silico and Biochemical Evaluation Abstract Abstract Alzheimer’s disease (AD) is characterized by amyloid-beta (Aβ) plaque accumulation and neurodegeneration. This study identifie...
PMC3256935
core_pubmed_pmc
Discovery of a Novel Class of Orally Active Trypanocidal N -Myristoyltransferase Inhibitors
Discovery of a Novel Class of Orally Active Trypanocidal N -Myristoyltransferase Inhibitors Abstract N -Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (HAT), which is caused by the parasitic protozoa Trypanosoma brucei . We report the optimization of a high throughput sc...
PMC12383776
core_pubmed_pmc
Bioequivalence and Pharmacokinetics of Low-Dose Anagrelide 0.5 mg Capsules in Healthy Volunteers
Bioequivalence and Pharmacokinetics of Low-Dose Anagrelide 0.5 mg Capsules in Healthy Volunteers Abstract Abstract Objectives : Anagrelide, an oral phosphodiesterase-3 inhibitor, is widely used to treat thrombocythemia. Evaluating the bioequivalence of low-dose formulations is essential to ensure consistent therapeutic...
PMC12771160
core_pubmed_pmc
Identification of New Small-Molecule SGLT2 Inhibitors: In-Silico Approach to Therapeutics for Diabetes-Related Complications
Identification of New Small-Molecule SGLT2 Inhibitors: In-Silico Approach to Therapeutics for Diabetes-Related Complications Abstract Abstract Sodium-glucose cotransporter-2 (SGLT2) is one of the six members of the SGLT protein family that plays a key role in glucose transport in humans. SGLT2 inhibitors are drugs used...
PMC11295983
core_pubmed_pmc
Open-label, dose-escalation FIGHT-101 study of pemigatinib combined with targeted therapy, chemotherapy, or immunotherapy in patients with advanced malignancies
Open-label, dose-escalation FIGHT-101 study of pemigatinib combined with targeted therapy, chemotherapy, or immunotherapy in patients with advanced malignancies Abstract Background Pemigatinib is an oral, potent, selective fibroblast growth factor receptor (FGFR) 1-3 inhibitor. FIGHT-101, a three-part, open-label, firs...
PMC12581698
core_pubmed_pmc
Improved bioavailability and anti-nephrotoxicity efficacy of polydatin on cisplatin-induced AKI via a dual-targeting fucoidan delivery system
Improved bioavailability and anti-nephrotoxicity efficacy of polydatin on cisplatin-induced AKI via a dual-targeting fucoidan delivery system Abstract Abstract Acute kidney injury (AKI) is a common and serious complication in clinical practice, especially when using chemotherapy drug cisplatin, which severely limits it...
PMC9791083
core_pubmed_pmc
Cerebrospinal fluid concentrations of fluoroquinolones and carbapenems in tuberculosis meningitis
Cerebrospinal fluid concentrations of fluoroquinolones and carbapenems in tuberculosis meningitis Abstract Background: Tuberculosis meningitis (TBM) is the most lethal form of TB. It is difficult to treat in part due to poor or uncertain drug penetration into the central nervous system (CNS). To help fill this knowledg...
PMC10669563
core_pubmed_pmc
A Validated LC-MS/MS Method for Performing Belatacept Drug Monitoring in Renal Transplantation
A Validated LC-MS/MS Method for Performing Belatacept Drug Monitoring in Renal Transplantation Abstract Belatacept, a CTLA4-Ig, was designed to prevent rejection and graft loss in kidney transplant recipients. This immunotherapy showed a long-term clinical benefit mainly on renal function and better glycemic control bu...
PMC3338912
core_pubmed_pmc
Clinical, pharmacokinetic and pharmacodynamic evaluations of metronomic UFT and cyclophosphamide plus celecoxib in patients with advanced refractory gastrointestinal cancers
Clinical, pharmacokinetic and pharmacodynamic evaluations of metronomic UFT and cyclophosphamide plus celecoxib in patients with advanced refractory gastrointestinal cancers Abstract Abstract Aims To evaluate UFT and cyclophosphamide (CTX) based metronomic chemotherapy plus celecoxib (CXB) for the treatment of patients...
PMC12257258
core_pubmed_pmc
Investigating the Pharmacokinetics and Efficacy of Intramammary Ceftiofur Hydrochloride in Prevention of Udder Inflammation in Non‐Lactating Dairy Heifers
Investigating the Pharmacokinetics and Efficacy of Intramammary Ceftiofur Hydrochloride in Prevention of Udder Inflammation in Non‐Lactating Dairy Heifers Abstract ABSTRACT Mastitis is the most burdensome concern for the dairy cattle industry. Antimicrobials are often prophylactically administered to dairy cows at dry‐...
PMC2886126
core_pubmed_pmc
Methodological considerations in quantification of oncological FDG PET studies
Methodological considerations in quantification of oncological FDG PET studies Abstract Purpose This review aims to provide insight into the factors that influence quantification of glucose metabolism by FDG PET images in oncology as well as their influence on repeated measures studies (i.e. treatment response assessme...
PMC12114674
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling to Predict Lamotrigine Exposure in Special Populations to Facilitate Therapeutic Drug Monitoring and Guide Dosing Regimens
Physiologically Based Pharmacokinetic Modeling to Predict Lamotrigine Exposure in Special Populations to Facilitate Therapeutic Drug Monitoring and Guide Dosing Regimens Abstract Abstract Background : Lamotrigine plays a crucial role in the treatment of epilepsy and bipolar disorder in adults and children. However, its...
PMC5338879
core_pubmed_pmc
Usefulness of ambulatory blood pressure monitoring to assess the melanocortin receptor agonist bremelanotide
Usefulness of ambulatory blood pressure monitoring to assess the melanocortin receptor agonist bremelanotide Abstract Supplemental Digital Content is available in the text Background: Melanocortin receptor agonists that bind to the melanocortin receptor 4 may cause increases in blood pressure (BP). Bremelanotide is an ...
PMC4932481
core_pubmed_pmc
Current Trends in Development of Liposomes for Targeting Bacterial Biofilms
Current Trends in Development of Liposomes for Targeting Bacterial Biofilms Abstract Biofilm targeting represents a great challenge for effective antimicrobial therapy. Increased biofilm resistance, even with the elevated concentrations of very potent antimicrobial agents, often leads to failed therapeutic outcome. App...
PMC9280251
core_pubmed_pmc
A novel 5-Fluorocuracil multiple-nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancer
A novel 5-Fluorocuracil multiple-nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancer Abstract Abstract 5-Fluorouracil (5-FU) is a drug of choice for colorectal-cancer. But oral therapeutic efficacy of 5-FU is restricted due to their very little bioavailability because of ...
PMC12799505
core_pubmed_pmc
Can alternatives to animal testing yield useful information regarding biological mechanisms and drug discovery?
Can alternatives to animal testing yield useful information regarding biological mechanisms and drug discovery? Abstract Establish alternative strategies to standard animal experiments decrease animal utilization and simultaneously enhance the reliability of biological and disease models. This review highlights advance...
PMC4165439
core_pubmed_pmc
Covariates of intravenous paracetamol pharmacokinetics in adults
Covariates of intravenous paracetamol pharmacokinetics in adults Abstract Abstract Background Pharmacokinetic estimates for intravenous paracetamol in individual adult cohorts are different to a certain extent, and understanding the covariates of these differences may guide dose individualization. In order to assess co...
PMC7346118
core_pubmed_pmc
Polymyxins–Curcumin Combination Antimicrobial Therapy: Safety Implications and Efficacy for Infection Treatment
Polymyxins–Curcumin Combination Antimicrobial Therapy: Safety Implications and Efficacy for Infection Treatment Abstract Abstract The emergence of antimicrobial resistance in Gram-negative bacteria poses a huge health challenge. The therapeutic use of polymyxins (i.e., colistin and polymyxin B) is commonplace due to hi...
PMC8646028
core_pubmed_pmc
Prediction of Survival After Partial Hepatectomy Using a Physiologically Based Pharmacokinetic Model of Indocyanine Green Liver Function Tests
Prediction of Survival After Partial Hepatectomy Using a Physiologically Based Pharmacokinetic Model of Indocyanine Green Liver Function Tests Abstract The evaluation of hepatic function and functional capacity of the liver are essential tasks in hepatology as well as in hepatobiliary surgery. Indocyanine green (ICG) i...
PMC5937443
core_pubmed_pmc
Intranasal Pharmacokinetics of Morphine ARER, a Novel Abuse-Deterrent Formulation: Results from a Randomized, Double-Blind, Four-Way Crossover Study in Nondependent, Opioid-Experienced Subjects
Intranasal Pharmacokinetics of Morphine ARER, a Novel Abuse-Deterrent Formulation: Results from a Randomized, Double-Blind, Four-Way Crossover Study in Nondependent, Opioid-Experienced Subjects Abstract Abstract Objective To investigate the pharmacokinetics (PK) of Morphine ARER, an extended-release (ER), abuse-deterre...
PMC5628903
core_pubmed_pmc
Novel multipurpose pod-intravaginal ring for the prevention of HIV, HSV, and unintended pregnancy: Pharmacokinetic evaluation in a macaque model
Novel multipurpose pod-intravaginal ring for the prevention of HIV, HSV, and unintended pregnancy: Pharmacokinetic evaluation in a macaque model Abstract Globally, women bear an uneven burden for sexual HIV acquisition. Results from two clinical trials evaluating intravaginal rings (IVRs) delivering the antiretroviral ...
PMC6697969
core_pubmed_pmc
Impact of antiretroviral treatment on height evolution of HIV infected children
Impact of antiretroviral treatment on height evolution of HIV infected children Abstract Abstract Background Antiretroviral treatment (ART) has been shown to have a beneficial effect on the weight evolution but its effect on height remains unclear. We described patterns of height evolution and identified predictors of ...
PMC5814843
core_pubmed_pmc
Pharmacokinetics of Diclofenac and Hydroxypropyl‐β‐Cyclodextrin (HPβCD) Following Administration of Injectable HPβCD‐Diclofenac in Subjects With Mild to Moderate Renal Insufficiency or Mild Hepatic Impairment
Pharmacokinetics of Diclofenac and Hydroxypropyl‐β‐Cyclodextrin (HPβCD) Following Administration of Injectable HPβCD‐Diclofenac in Subjects With Mild to Moderate Renal Insufficiency or Mild Hepatic Impairment Abstract Abstract Given their established analgesic properties, nonsteroidal anti‐inflammatory drugs (NSAIDs) r...
PMC12796560
core_pubmed_pmc
A Meta‐Analysis of International Flunixin Pharmacokinetics in Horses: Toward Regulatory Harmonization and Individualized Detection Times Using Bayesian Paradigm
A Meta‐Analysis of International Flunixin Pharmacokinetics in Horses: Toward Regulatory Harmonization and Individualized Detection Times Using Bayesian Paradigm Abstract ABSTRACT Flunixin meglumine is widely used to manage pain and inflammation in horses, and its regulation requires robust pharmacokinetic analysis for ...
PMC9465123
core_pubmed_pmc
Multi-stage virtual screening of natural products against p38α mitogen-activated protein kinase: predictive modeling by machine learning, docking study and molecular dynamics simulation
Multi-stage virtual screening of natural products against p38α mitogen-activated protein kinase: predictive modeling by machine learning, docking study and molecular dynamics simulation Abstract Abstract p38α is a mitogen-activated protein kinase (MAPK), and the signaling pathways involved are closely related to the in...
PMC6628388
core_pubmed_pmc
Pharmacokinetics of Human Recombinant Anti-Botulinum Toxin Antibodies in Rats
Pharmacokinetics of Human Recombinant Anti-Botulinum Toxin Antibodies in Rats Abstract Botulinum neurotoxins (BoNT) are potential biothreat agents due to their high lethality, potency, and ease of distribution, thus the development of antitoxins is a high priority to the US government. This study examined pre-clinical ...
PMC3643838
core_pubmed_pmc
The ECMO PK Project: an incremental research approach to advance understanding of the pharmacokinetic alterations and improve patient outcomes during extracorporeal membrane oxygenation
The ECMO PK Project: an incremental research approach to advance understanding of the pharmacokinetic alterations and improve patient outcomes during extracorporeal membrane oxygenation Abstract Background Extracorporeal membrane oxygenation (ECMO) is a supportive therapy and its success depends on optimal drug therapy...
PMC5856061
core_pubmed_pmc
Safety of high-dose daptomycin in patients with severe renal impairment
Safety of high-dose daptomycin in patients with severe renal impairment Abstract Abstract Background Treatment options are limited for infections due to multidrug-resistant Gram-positive pathogens. Daptomycin is a lipopeptide antibiotic with concentration-dependent killing characteristic and dose-dependent post-antibio...
PMC7828032
core_pubmed_pmc
Strengths and Challenges of Secretory Ribonucleases as AntiTumor Agents
Strengths and Challenges of Secretory Ribonucleases as AntiTumor Agents Abstract Approaches to develop effective drugs to kill cancer cells are mainly focused either on the improvement of the currently used chemotherapeutics or on the development of targeted therapies aimed at the selective destruction of cancer cells ...
PMC4633286
core_pubmed_pmc
Demonstration of Therapeutic Equivalence of Fluconazole Generic Products in the Neutropenic Mouse Model of Disseminated Candidiasis
Demonstration of Therapeutic Equivalence of Fluconazole Generic Products in the Neutropenic Mouse Model of Disseminated Candidiasis Abstract Abstract Some generics of antibacterials fail therapeutic equivalence despite being pharmaceutical equivalents of their innovators, but data are scarce with antifungals. We used t...
PMC7022715
core_pubmed_pmc
Montelukast Nanocrystals for Transdermal Delivery with Improved Chemical Stability
Montelukast Nanocrystals for Transdermal Delivery with Improved Chemical Stability Abstract Abstract A novel nanocrystal system of montelukast (MTK) was designed to improve the transdermal delivery, while ensuring chemical stability of the labile compound. MTK nanocrystal suspension was fabricated using acid-base neutr...