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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... |
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