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PMC12777569
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic characterization of gepotidacin against Escherichia coli and Klebsiella pneumoniae in a neutropenic mouse thigh infection model
Pharmacokinetic and pharmacodynamic characterization of gepotidacin against Escherichia coli and Klebsiella pneumoniae in a neutropenic mouse thigh infection model Abstract ABSTRACT Gepotidacin is a novel first-in-class triazaacenaphthylene antibiotic developed for the treatment of uncomplicated gonorrhea and uncomplic...
PMC12569563
core_pubmed_pmc
Dose individualisation of antibiotics in critically ill patients with inflammation: A narrative review
Dose individualisation of antibiotics in critically ill patients with inflammation: A narrative review Abstract Abstract Due to extensive pathophysiological changes in critically ill patients, standard dosing of antibiotics may lead to inadequate drug exposure. This is concerning, as insufficient plasma drug concentrat...
PMC8846473
core_pubmed_pmc
Early Bactericidal Activity of Delpazolid (LCB01-0371) in Patients with Pulmonary Tuberculosis
Early Bactericidal Activity of Delpazolid (LCB01-0371) in Patients with Pulmonary Tuberculosis Abstract ABSTRACT Delpazolid, an oxazolidinone, has been studied in non-clinical studies of efficacy and toxicity and Phase 1 clinical studies. Delpazolid has in vitro activity against Gram-positive bacteria, including Mycoba...
PMC12708408
core_pubmed_pmc
Exploring the Interactions between Drugs and Metabolic Disturbances in CKD
Exploring the Interactions between Drugs and Metabolic Disturbances in CKD Abstract Abstract Key Points Kidney function was independently associated with free drug concentration; the latter concentration was higher in patients with a lower eGFR. The conformational changes in albumin induced by carbamylation may alter i...
PMC10242578
core_pubmed_pmc
From Oral to Subcutaneous Furosemide: The Road to Novel Opportunities to Manage Congestion
From Oral to Subcutaneous Furosemide: The Road to Novel Opportunities to Manage Congestion Abstract The steadily rising prevalence of heart failure (HF) and the associated increase in health care expenditures represent a significant burden for patients, caregivers, and society. Ambulatory management of worsening conges...
PMC11782446
core_pubmed_pmc
DREAMM-11, Part 2: Japanese phase I trial of belantamab mafodotin combination therapies in relapsed/refractory multiple myeloma
DREAMM-11, Part 2: Japanese phase I trial of belantamab mafodotin combination therapies in relapsed/refractory multiple myeloma Abstract Abstract DREAMM-11 ( NCT03828292 ) was a Phase 1, open-label, dose-escalation study of belantamab mafodotin in Japanese patients with relapsed/refractory multiple myeloma (RRMM). In P...
PMC5473956
core_pubmed_pmc
Safety/tolerability of the anti-semaphorin 4D Antibody VX15/2503 in a randomized phase 1 trial
Safety/tolerability of the anti-semaphorin 4D Antibody VX15/2503 in a randomized phase 1 trial Abstract Objective: To evaluate the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of VX15/2503 in a randomized, single-dose, dose-escalation, double-blind, placebo-controlled study enrolling adult pat...
PMC7125253
core_pubmed_pmc
Prediction of exposure-driven myelotoxicity of continuous infusion 5-fluorouracil by a semi-physiological pharmacokinetic–pharmacodynamic model in gastrointestinal cancer patients
Prediction of exposure-driven myelotoxicity of continuous infusion 5-fluorouracil by a semi-physiological pharmacokinetic–pharmacodynamic model in gastrointestinal cancer patients Abstract Abstract Purpose To describe 5-fluorouracil (5FU) pharmacokinetics, myelotoxicity and respective covariates using a simultaneous no...
PMC9494667
core_pubmed_pmc
Phytochemical Screening, Quantification, FT-IR Analysis, and In Silico Characterization of Potential Bio-active Compounds Identified in HR-LC/MS Analysis of the Polyherbal Formulation from Northeast India
Phytochemical Screening, Quantification, FT-IR Analysis, and In Silico Characterization of Potential Bio-active Compounds Identified in HR-LC/MS Analysis of the Polyherbal Formulation from Northeast India Abstract Abstract Diabetes is a group of metabolic disorders characterized by elevated blood sugar levels, leading ...
PMC5119013
core_pubmed_pmc
Pharmacokinetic Interactions between Tafenoquine and Dihydroartemisinin-Piperaquine or Artemether-Lumefantrine in Healthy Adult Subjects
Pharmacokinetic Interactions between Tafenoquine and Dihydroartemisinin-Piperaquine or Artemether-Lumefantrine in Healthy Adult Subjects Abstract Abstract Tafenoquine is in development as a single-dose treatment for relapse prevention in individuals with Plasmodium vivax malaria. Tafenoquine must be coadministered with...
PMC4324327
core_pubmed_pmc
A fixed-dose combination tablet of gemigliptin and metformin sustained release has comparable pharmacodynamic, pharmacokinetic, and tolerability profiles to separate tablets in healthy subjects
A fixed-dose combination tablet of gemigliptin and metformin sustained release has comparable pharmacodynamic, pharmacokinetic, and tolerability profiles to separate tablets in healthy subjects Abstract Background In type 2 diabetes mellitus, fixed-dose combination (FDC) can provide the complementary benefits of correc...
PMC6589951
core_pubmed_pmc
Phase Ib study of the combination of pexidartinib (PLX3397), a CSF-1R inhibitor, and paclitaxel in patients with advanced solid tumors
Phase Ib study of the combination of pexidartinib (PLX3397), a CSF-1R inhibitor, and paclitaxel in patients with advanced solid tumors Abstract Purpose: To evaluate the safety, recommended phase II dose (RP2D) and efficacy of pexidartinib, a colony stimulating factor receptor 1 (CSF-1R) inhibitor, in combination with w...
PMC8388171
core_pubmed_pmc
ModraDoc006 , an oral docetaxel formulation in combination with ritonavir ( ModraDoc006 /r), in metastatic castration‐resistant prostate cancer patients: A phase Ib study
ModraDoc006 , an oral docetaxel formulation in combination with ritonavir ( ModraDoc006 /r), in metastatic castration‐resistant prostate cancer patients: A phase Ib study Abstract Abstract Background ModraDoc006 is an oral formulation of docetaxel, which is co‐administered with the cytochrome P450 3A4 and P‐glycoprotei...
PMC7037682
core_pubmed_pmc
Herb–Drug Interaction of Red Ginseng Extract and Ginsenoside Rc with Valsartan in Rats
Herb–Drug Interaction of Red Ginseng Extract and Ginsenoside Rc with Valsartan in Rats Abstract The purpose of this study was to investigate the herb–drug interactions involving red ginseng extract (RGE) or ginsenoside Rc with valsartan, a substrate for organic anion transporting polypeptide (OATP/Oatp) transporters. I...
PMC12500319
core_pubmed_pmc
Therapeutic potential of iron oxide nanoparticles for cutaneous leishmaniasis: a systematic review of in vitro and in viv o studies
Therapeutic potential of iron oxide nanoparticles for cutaneous leishmaniasis: a systematic review of in vitro and in viv o studies Abstract Abstract The treatment of cutaneous leishmaniasis (CL) is challenged by limited therapeutic options, high drug toxicity, and frequent treatment failure. In this context, iron oxid...
PMC10958125
core_pubmed_pmc
A phase I study of docetaxel plus synthetic lycopene in metastatic prostate cancer patients
A phase I study of docetaxel plus synthetic lycopene in metastatic prostate cancer patients Abstract Abstract Purpose Our preclinical studies showed that lycopene enhanced the anti‐prostate cancer efficacy of docetaxel in animal models. A phase I trial (NCT0149519) was conducted to identify an optimum dose of synthetic...
PMC4942499
core_pubmed_pmc
FG-3019, a Human Monoclonal Antibody Recognizing Connective Tissue Growth Factor, is Subject to Target-Mediated Drug Disposition
FG-3019, a Human Monoclonal Antibody Recognizing Connective Tissue Growth Factor, is Subject to Target-Mediated Drug Disposition Abstract Abstract Purpose To evaluate and model the pharmacokinetic and pharmacodynamic behavior in rats of FG-3019, a human monoclonal antibody targeting connective tissue growth factor (CTG...
PMC8708498
core_pubmed_pmc
3D Printed Buccal Films for Prolonged-Release of Propranolol Hydrochloride: Development, Characterization and Bioavailability Prediction
3D Printed Buccal Films for Prolonged-Release of Propranolol Hydrochloride: Development, Characterization and Bioavailability Prediction Abstract Gelatin-polyvinylpyrrolidone (PVP) and gelatin-poly(vinyl alcohol) (PVA) mucoadhesive buccal films loaded with propranolol hydrochloride (PRH) were prepared by semi-solid ext...
PMC4967628
core_pubmed_pmc
Synergism between rocuronium and cisatracurium: comparison of the Minto and Greco interaction models
Synergism between rocuronium and cisatracurium: comparison of the Minto and Greco interaction models Abstract Abstract Background This study was conducted to investigate the pharmacodynamic interaction between rocuronium and cisatracurium using the response surface model, which is not subject to the limitations of trad...
PMC12289712
core_pubmed_pmc
A semi-mechanistic population pharmacokinetic-pharmacodynamic model to assess downstream drug-target effects on erythropoiesis
A semi-mechanistic population pharmacokinetic-pharmacodynamic model to assess downstream drug-target effects on erythropoiesis Abstract Abstract Erythropoiesis is a complex process that results in the production of erythrocytes from hematopoietic stem cells in the bone marrow. This work aimed to develop a population ph...
PMC7760511
core_pubmed_pmc
Trastuzumab Emtansine Plus Non-Pegylated Liposomal Doxorubicin in HER2-Positive Metastatic Breast Cancer (Thelma): A Single-Arm, Multicenter, Phase Ib Trial
Trastuzumab Emtansine Plus Non-Pegylated Liposomal Doxorubicin in HER2-Positive Metastatic Breast Cancer (Thelma): A Single-Arm, Multicenter, Phase Ib Trial Abstract Simple Summary Considering the favorable overall safety profile of trastuzumab emtansine (T-DM1), the low expected rate of cardiotoxicity, and the synergi...
PMC6989224
core_pubmed_pmc
Comparison of various estimation methods for the parameters of Michaelis-Menten equation based on in vitro elimination kinetic simulation data
Comparison of various estimation methods for the parameters of Michaelis-Menten equation based on in vitro elimination kinetic simulation data Abstract Abstract The Michaelis-Menten equation is one of the best-known models describing the enzyme kinetics of in vitro drug elimination experiments, and takes a form of equa...
PMC7214819
core_pubmed_pmc
Population Pharmacokinetics and Dosage Optimization of Teicoplanin in Children With Different Renal Functions
Population Pharmacokinetics and Dosage Optimization of Teicoplanin in Children With Different Renal Functions Abstract Objective The purposes of our study were to investigate the population pharmacokinetics of teicoplanin in Chinese children with different renal functions and to propose the appropriate dosing regimen f...
PMC9865168
core_pubmed_pmc
Preparation of Solid Dispersion of Polygonum Cuspidatum Extract by Hot Melt Extrusion to Enhance Oral Bioavailability of Resveratrol
Preparation of Solid Dispersion of Polygonum Cuspidatum Extract by Hot Melt Extrusion to Enhance Oral Bioavailability of Resveratrol Abstract The aim of this study was to improve the solubility, bioavailability, and stability of resveratrol (RES-SD) Solid Dispersion in Polygonum cuspidatum extract (PCE) by hot melt ext...
PMC12825014
core_pubmed_pmc
Population pharmacokinetics of tofacitinib in patients with active ankylosing spondylitis
Population pharmacokinetics of tofacitinib in patients with active ankylosing spondylitis Abstract Abstract Objective: To characterize tofacitinib pharmacokinetics (PK) in patients with active ankylosing spondylitis (AS) and estimate the effects of covariates on variability of PK parameters. Materials and methods: Pool...
PMC10042765
core_pubmed_pmc
First-in-Human Study of INCB062079, a Fibroblast Growth Factor Receptor 4 Inhibitor, in Patients with Advanced Solid Tumors
First-in-Human Study of INCB062079, a Fibroblast Growth Factor Receptor 4 Inhibitor, in Patients with Advanced Solid Tumors Abstract Introduction Fibroblast growth factor receptor (FGFR)-4/FGF19 pathway dysregulation is implicated in hepatobiliary and other solid tumors. INCB062079, an oral, selective, FGFR4 inhibitor,...
PMC10818600
core_pubmed_pmc
In Silico Design, Synthesis, and Evaluation of Novel Enantiopure Isoxazolidines as Promising Dual Inhibitors of α-Amylase and α-Glucosidase
In Silico Design, Synthesis, and Evaluation of Novel Enantiopure Isoxazolidines as Promising Dual Inhibitors of α-Amylase and α-Glucosidase Abstract Abstract Isoxazolidine derivatives were designed, synthesized, and characterized using different spectroscopic techniques and elemental analysis and then evaluated for the...
PMC10458368
core_pubmed_pmc
Cariprazine in Pediatric Patients with Autism Spectrum Disorder: Results of a Pharmacokinetic, Safety and Tolerability Study
Cariprazine in Pediatric Patients with Autism Spectrum Disorder: Results of a Pharmacokinetic, Safety and Tolerability Study Abstract Objective: Cariprazine is a dopamine D 3 -preferring D 3 /D 2 and serotonin 5-HT 1A receptor partial agonist approved to treat adults with schizophrenia and manic/mixed or depressive epi...
PMC12504290
core_pubmed_pmc
Exploring the potential of computer simulation models in drug testing and biomedical research: a systematic review
Exploring the potential of computer simulation models in drug testing and biomedical research: a systematic review Abstract Abstract Introduction The growing limitations of animal models in drug testing and biomedical research, including ethical concerns, high costs, and poor translational relevance to human biology, h...
PMC8611040
core_pubmed_pmc
A comprehensive breath test that confirms recent use of inhaled cannabis within the impairment window
A comprehensive breath test that confirms recent use of inhaled cannabis within the impairment window Abstract Abstract Legalization of cannabis for medicinal and/or recreational use is expanding globally. Although cannabis is being regulated country by country, an accurate recent use test with indisputable results cor...
PMC12816771
core_pubmed_pmc
Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry
Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry Abstract Interest in piperazine scaffolds continues to rise due to their broad relevance across anti‐infective, anticancer, and neuroactive research. This review examines reports published from 2014 to 2024 and organizes current d...
PMC4846043
core_pubmed_pmc
Daptomycin: an evidence-based review of its role in the treatment of Gram-positive infections
Daptomycin: an evidence-based review of its role in the treatment of Gram-positive infections Abstract Infections caused by Gram-positive pathogens remain a major public health burden and are associated with high morbidity and mortality. Increasing rates of infection with Gram-positive bacteria and the emergence of res...
PMC9364583
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic parameters of vancomycin for predicting clinical outcome of enterococcal bacteremia
Pharmacokinetic/pharmacodynamic parameters of vancomycin for predicting clinical outcome of enterococcal bacteremia Abstract Abstract Purpose To find pharmacokinetic/pharmacodynamic parameters of vancomycin associated with the optimal outcome of severe infection due to Enterococcus species. Methods We retrospectively r...
PMC9303319
core_pubmed_pmc
Pharmacokinetics and Safety of Intravenous Ferric Pyrophosphate Citrate: Equivalence to Administration via Dialysate
Pharmacokinetics and Safety of Intravenous Ferric Pyrophosphate Citrate: Equivalence to Administration via Dialysate Abstract Abstract Ferric pyrophosphate citrate (FPC) is indicated to maintain hemoglobin in patients with stage 5 hemodialysis‐dependent chronic kidney disease on chronic hemodialysis by addition to the ...
PMC3979125
core_pubmed_pmc
A phase Ib multiple ascending dose study evaluating safety, pharmacokinetics, and early clinical response of brodalumab, a human anti-IL-17R antibody, in methotrexate-resistant rheumatoid arthritis
A phase Ib multiple ascending dose study evaluating safety, pharmacokinetics, and early clinical response of brodalumab, a human anti-IL-17R antibody, in methotrexate-resistant rheumatoid arthritis Abstract Abstract Introduction The aim of this study was to evaluate the safety, pharmacokinetics, and clinical response o...
PMC10725274
core_pubmed_pmc
Evaluation of the effect of erenumab on migraine‐specific questionnaire in patients with chronic and episodic migraine
Evaluation of the effect of erenumab on migraine‐specific questionnaire in patients with chronic and episodic migraine Abstract Abstract Erenumab is a fully human anti‐canonical calcitonin gene‐related peptide receptor monoclonal antibody approved for migraine prevention. The Migraine‐Specific Quality‐of‐Life Questionn...
PMC3661042
core_pubmed_pmc
Long-term effects of gastric bypass and duodenal switch on systemic exposure of atorvastatin
Long-term effects of gastric bypass and duodenal switch on systemic exposure of atorvastatin Abstract Background A previous study of 22 patients undergoing either gastric bypass or duodenal switch showed increased systemic exposure of atorvastatin acid 3–8 weeks after surgery in the majority of patients. This study aim...
PMC9354714
core_pubmed_pmc
Neuroprotective Properties of Bis-Sulfonamide Derivatives Against 6-OHDA-Induced Parkinson's Model via Sirtuin 1 Activity and in silico Pharmacokinetic Properties
Neuroprotective Properties of Bis-Sulfonamide Derivatives Against 6-OHDA-Induced Parkinson's Model via Sirtuin 1 Activity and in silico Pharmacokinetic Properties Abstract Parkinson's disease (PD) is considered one of the health problems in the aging society. Due to the limitations of currently available drugs in preve...
PMC4209507
core_pubmed_pmc
Substantial Effect of Efavirenz Monotherapy on Bilirubin Levels in Healthy Volunteers
Substantial Effect of Efavirenz Monotherapy on Bilirubin Levels in Healthy Volunteers Abstract Abstract Background Efavirenz exhibits multiple interactions with drug-metabolizing enzymes and transporters, and for this reason efavirenz-based HIV therapy is associated with altered pharmacokinetics of coadministered drugs...
PMC9579312
core_pubmed_pmc
Predictive performance and verification of physiologically based pharmacokinetic model of propylthiouracil
Predictive performance and verification of physiologically based pharmacokinetic model of propylthiouracil Abstract Background: Propylthiouracil (PTU) treats hyperthyroidism and thyroid crisis in all age groups. A variety of serious adverse effects can occur during clinical use and require attention to its pharmacokine...
PMC5465324
core_pubmed_pmc
Lack of effect of oral cabotegravir on the pharmacokinetics of a levonorgestrel/ethinyl oestradiol‐containing oral contraceptive in healthy adult women
Lack of effect of oral cabotegravir on the pharmacokinetics of a levonorgestrel/ethinyl oestradiol‐containing oral contraceptive in healthy adult women Abstract Aims This study aimed to investigate whether cabotegravir (CAB), an integrase inhibitor in development for treatment and prevention of human immunodeficiency v...
PMC4045086
core_pubmed_pmc
Preclinical studies of N 3 -O-toluyl-fluorouracil-loaded lipid-based nanosuspensions in H 22 -bearing mice
Preclinical studies of N 3 -O-toluyl-fluorouracil-loaded lipid-based nanosuspensions in H 22 -bearing mice Abstract Abstract Purpose N 3 -O-toluyl-fluorouracil (TFU) is a potential antitumor prodrug of 5-fluorouracil (5-FU), but its poor solubility has limited its use in clinic. This study aimed to improve the bioavail...
PMC9124739
core_pubmed_pmc
Does the cytokine adsorber CytoSorb ® reduce vancomycin exposure in critically ill patients with sepsis or septic shock? a prospective observational study
Does the cytokine adsorber CytoSorb ® reduce vancomycin exposure in critically ill patients with sepsis or septic shock? a prospective observational study Abstract Background Hemadsorption of cytokines is used in critically ill patients with sepsis or septic shock. Concerns have been raised that the cytokine adsorber C...
PMC9635916
core_pubmed_pmc
Metabolism-involved drug interactions with traditional Chinese medicines in cardiovascular diseases
Metabolism-involved drug interactions with traditional Chinese medicines in cardiovascular diseases Abstract Herbal medicines have been widely used for the past millennia. Traditional Chinese medicine (TCM) is a major modality in Chinese medical care and has garnered global attention owing to its pharmacological effect...
PMC12093495
core_pubmed_pmc
The Relationship of Indomethacin Exposure With Efficacy and Renal Toxicity Outcomes for Preterm Infants in the Neonatal Intensive Care Unit
The Relationship of Indomethacin Exposure With Efficacy and Renal Toxicity Outcomes for Preterm Infants in the Neonatal Intensive Care Unit Abstract ABSTRACT Indomethacin is commonly used in the Neonatal Intensive Care Unit (NICU) for intraventricular hemorrhage (IVH) prophylaxis and patent ductus arteriosus (PDA) trea...
PMC12266210
core_pubmed_pmc
Safety of Drugs in Breastfeeding Women With CKD
Safety of Drugs in Breastfeeding Women With CKD Abstract Abstract Introduction The benefits of breastfeeding are widely recognized. Because of lack of evidence, women may forego breastfeeding or decline treatments that impact long-term renal survival. Therefore, we systematically reviewed the evidence on the breastfeed...
PMC8536606
core_pubmed_pmc
Principles of dose-setting in toxicology studies: the importance of kinetics for ensuring human safety
Principles of dose-setting in toxicology studies: the importance of kinetics for ensuring human safety Abstract Abstract Regulatory toxicology seeks to ensure that exposures to chemicals encountered in the environment, in the workplace, or in products pose no significant hazards and produce no harm to humans or other o...
PMC4029298
core_pubmed_pmc
Comparative preclinical pharmacokinetics study of 3,3′-diindolylmethane formulations: is personalized treatment and targeted chemoprevention in the horizon?
Comparative preclinical pharmacokinetics study of 3,3′-diindolylmethane formulations: is personalized treatment and targeted chemoprevention in the horizon? Abstract Background 3,3′-Diindolylmethane (DIM) is known as an agent of natural origin that provides protection against different cancers due to the broad spectrum...
PMC9146127
core_pubmed_pmc
Promising Antibacterial and Antifungal Agents Based on Thiolated Vitamin K3 Analogs: Synthesis, Bioevaluation, Molecular Docking
Promising Antibacterial and Antifungal Agents Based on Thiolated Vitamin K3 Analogs: Synthesis, Bioevaluation, Molecular Docking Abstract Abstract In the present study, we designed and synthesized thiolated VK3 analogs ( VK3a–g ) along with an extensive antimicrobial study. After the evaluation of the antibacterial and...
PMC10223997
core_pubmed_pmc
Screening and Elucidation of Chemical Structures of Novel Mammalian α-Glucosidase Inhibitors Targeting Anti-Diabetes Drug from Herbals Used by E De Ethnic Tribe in Vietnam
Screening and Elucidation of Chemical Structures of Novel Mammalian α-Glucosidase Inhibitors Targeting Anti-Diabetes Drug from Herbals Used by E De Ethnic Tribe in Vietnam Abstract Among ten extracts of indigenous medicinal plants, the MeOH extract of Terminalia triptera Stapf. (TTS) showed the most efficient mammalian...
PMC8673998
core_pubmed_pmc
A quantitative systems pharmacology approach to predict the safe‐equivalent dose of doxorubicin in patients with cardiovascular comorbidity
A quantitative systems pharmacology approach to predict the safe‐equivalent dose of doxorubicin in patients with cardiovascular comorbidity Abstract Abstract Patients with cardiovascular comorbidity are less tolerant to cardiotoxic drugs and should be treated with reduced doses to prevent cardiotoxicity. However, the s...
PMC10585311
core_pubmed_pmc
Macromolecules: Synthesis, antimicrobial, POM analysis and computational approaches of some glucoside derivatives bearing acyl moieties
Macromolecules: Synthesis, antimicrobial, POM analysis and computational approaches of some glucoside derivatives bearing acyl moieties Abstract Macromolecules i.e., carbohydrate derivatives are crucial to biochemical and medical research. Herein, we designed and synthesized eight methyl α-D-glucopyranoside (MGP) deriv...
PMC8597116
core_pubmed_pmc
Impact of Paroxetine, a Strong CYP2D6 Inhibitor, on SPN‐812 (Viloxazine Extended‐Release) Pharmacokinetics in Healthy Adults
Impact of Paroxetine, a Strong CYP2D6 Inhibitor, on SPN‐812 (Viloxazine Extended‐Release) Pharmacokinetics in Healthy Adults Abstract Abstract SPN‐812 (viloxazine extended‐release) is a novel nonstimulant recently approved as a treatment for attention‐deficit/hyperactivity disorder in children and adolescents. Given th...
PMC8451882
core_pubmed_pmc
Population pharmacokinetic analysis of RO5459072, a low water‐soluble drug exhibiting complex food–drug interactions
Population pharmacokinetic analysis of RO5459072, a low water‐soluble drug exhibiting complex food–drug interactions Abstract Abstract Aims RO5459072, a cathepsin‐S inhibitor, Biopharmaceutics Classification System class 2 and P‐glycoprotein substrate, exhibited complex, nonlinear pharmacokinetics (PK) while fasted tha...
PMC6709502
core_pubmed_pmc
In Vivo Pharmacodynamic Study of Cefiderocol, a Novel Parenteral Siderophore Cephalosporin, in Murine Thigh and Lung Infection Models
In Vivo Pharmacodynamic Study of Cefiderocol, a Novel Parenteral Siderophore Cephalosporin, in Murine Thigh and Lung Infection Models Abstract The pharmacokinetic (PK) and pharmacodynamic (PD) parameters which correlated with the in vivo efficacy of cefiderocol were evaluated using neutropenic murine thigh and lung inf...
PMC11764628
core_pubmed_pmc
Maintenance of prehospital anaesthesia in trauma patients: inconsistencies and variability in practice
Maintenance of prehospital anaesthesia in trauma patients: inconsistencies and variability in practice Abstract Background Literature on prehospital anaesthesia predominantly focuses on preparation and induction, while there is limited guidance on anaesthesia maintenance. The hypothesis of this study was that for preho...
PMC4740352
core_pubmed_pmc
Choice of antiretroviral drugs for continued treatment scale-up in a public health approach: what more do we need to know?
Choice of antiretroviral drugs for continued treatment scale-up in a public health approach: what more do we need to know? Abstract Introduction There have been several important developments in antiretroviral treatment in the past two years. Randomized clinical trials have been conducted to evaluate a lower dose of ef...
PMC6273050
core_pubmed_pmc
Icariin Metabolism by Human Intestinal Microflora
Icariin Metabolism by Human Intestinal Microflora Abstract Icariin is a major bioactive compound of Epimedii Herba, a traditional oriental medicine exhibiting anti-cancer, anti-inflammatory and anti-osteoporosis activities. Recently, the estrogenic activities of icariin drew significant attention, but the published sci...
PMC10651775
core_pubmed_pmc
An open-label, single-arm phase 2 trial of valemetostat for relapsed or refractory adult T-cell leukemia/lymphoma
An open-label, single-arm phase 2 trial of valemetostat for relapsed or refractory adult T-cell leukemia/lymphoma Abstract Key Points • This phase 2 study assessed the efficacy and safety of the dual EZH2 and EZH1 inhibitor valemetostat in patients with R/R ATL. • Valemetostat 200 mg orally once daily demonstrated prom...
PMC9142922
core_pubmed_pmc
Galactosylated Prodrugs: A Strategy to Improve the Profile of Nonsteroidal Anti-Inflammatory Drugs
Galactosylated Prodrugs: A Strategy to Improve the Profile of Nonsteroidal Anti-Inflammatory Drugs Abstract Abstract Carbohydrates are one of the most abundant and important classes of biomolecules. The variety in their structures makes them valuable carriers that can improve the pharmaceutical phase, pharmacokinetics ...
PMC3790897
core_pubmed_pmc
Vitamin C-driven epirubicin loading into liposomes
Vitamin C-driven epirubicin loading into liposomes Abstract The encapsulation of anticancer drugs in a liposome structure protects the drug during circulation and increases drug accumulation in the cancer tissue and antitumor activity while decreasing drug toxicity. This paper presents a new method of active drug loadi...
PMC9381917
core_pubmed_pmc
Contribution of machine learning to tumor growth inhibition modeling for hepatocellular carcinoma patients under Roblitinib (FGF401) drug treatment
Contribution of machine learning to tumor growth inhibition modeling for hepatocellular carcinoma patients under Roblitinib (FGF401) drug treatment Abstract Abstract Machine learning (ML) opens new perspectives in identifying predictive factors of efficacy among a large number of patients’ characteristics in oncology s...
PMC6343297
core_pubmed_pmc
Population pharmacokinetic-pharmacodynamic model of propofol in adolescents undergoing scoliosis surgery with intraoperative wake-up test: a study using Bispectral index and composite auditory evoked potentials as pharmacodynamic endpoints
Population pharmacokinetic-pharmacodynamic model of propofol in adolescents undergoing scoliosis surgery with intraoperative wake-up test: a study using Bispectral index and composite auditory evoked potentials as pharmacodynamic endpoints Abstract Abstract Background In adolescents limited data are available on the ph...
PMC3626250
core_pubmed_pmc
Effects of Borneol on Pharmacokinetics and Tissue Distribution of Notoginsenoside R1 and Ginsenosides Rg1 and Re in Panax notoginseng in Rabbits
Effects of Borneol on Pharmacokinetics and Tissue Distribution of Notoginsenoside R1 and Ginsenosides Rg1 and Re in Panax notoginseng in Rabbits Abstract The purpose of this study is to investigate the effects of Borneol on the pharmacokinetics of notoginsenoside R1 (NGR1) and the ginsenosides Rg1 (GRg1) and Re (GRe) i...
PMC9920659
core_pubmed_pmc
Baicalin-Loaded Lipid–Polymer Hybrid Nanoparticles Inhibiting the Proliferation of Human Colon Cancer: Pharmacokinetics and In Vivo Evaluation
Baicalin-Loaded Lipid–Polymer Hybrid Nanoparticles Inhibiting the Proliferation of Human Colon Cancer: Pharmacokinetics and In Vivo Evaluation Abstract This research work is focused on pharmacokinetic and biochemical experiments to assess baicalin-loaded lipid–polymer hybrid nanoparticles (LPHNPs) with colon-targeting ...
PMC10687392
core_pubmed_pmc
Pharmacokinetics of a Modified-Release Dexamphetamine Sulfate Formulation Following Single and Multiple Dosing in Healthy Adults: Comparative Bioavailability with Immediate-Release Dexamphetamine Sulfate, between Strengths, Assessment of Food and Meal Composition Effects
Pharmacokinetics of a Modified-Release Dexamphetamine Sulfate Formulation Following Single and Multiple Dosing in Healthy Adults: Comparative Bioavailability with Immediate-Release Dexamphetamine Sulfate, between Strengths, Assessment of Food and Meal Composition Effects Abstract Abstract Background A modified-release ...
PMC11858561
core_pubmed_pmc
Evaluation of the validity of a perfluorooctane sulfonic acid exposure reconstruction using a measured serum concentration among workers with a wide range of exposure
Evaluation of the validity of a perfluorooctane sulfonic acid exposure reconstruction using a measured serum concentration among workers with a wide range of exposure Abstract Abstract Background Studies among workers with a wide range of exposure to perfluoroalkyl substances inform risk assessments. Perfluorooctane su...
PMC12151220
core_pubmed_pmc
Safety and feasibility of anlotinib in children with high risk, recurrent or refractory sarcomas: an open-label, single-centre, single-arm, phase Ia/Ib trial
Safety and feasibility of anlotinib in children with high risk, recurrent or refractory sarcomas: an open-label, single-centre, single-arm, phase Ia/Ib trial Abstract Summary Background Anlotinib is a novel highly potent multitargeted tyrosine kinase inhibitor. However, the safety, recommended dosage, pharmacokinetics ...
PMC6651454
core_pubmed_pmc
An Established HPLC-MS/MS Method for Evaluation of the Influence of Salt Processing on Pharmacokinetics of Six Compounds in Cuscutae Semen
An Established HPLC-MS/MS Method for Evaluation of the Influence of Salt Processing on Pharmacokinetics of Six Compounds in Cuscutae Semen Abstract A sensitive and effective method was developed for clarifying the pharmacokinetic properties of six compounds (including hyperin, chlorogenic acid, neochlorogenic acid, p-c...
PMC7344116
core_pubmed_pmc
Phase I study of vinblastine in combination with nilotinib in children, adolescents, and young adults with refractory or recurrent low-grade glioma
Phase I study of vinblastine in combination with nilotinib in children, adolescents, and young adults with refractory or recurrent low-grade glioma Abstract Abstract Background New rescue regimens are needed for pediatric refractory/recurrent low-grade glioma. Nilotinib is a tyrosine kinase inhibitor that has potential...
PMC12521836
core_pubmed_pmc
Total intravenous sedation with target-controlled infusion in dentistry: clinical experience with the third-generation Eleveld pharmacokinetic/pharmacodynamic model
Total intravenous sedation with target-controlled infusion in dentistry: clinical experience with the third-generation Eleveld pharmacokinetic/pharmacodynamic model Abstract Background Approximately 31% of adults experience dental anxiety, which represents a significant barrier to timely care and ultimately results in ...
PMC9960731
core_pubmed_pmc
Assessment of Antifungal Pharmacodynamics
Assessment of Antifungal Pharmacodynamics Abstract Abstract Pharmacokinetic-pharmacodynamic (PK-PD) analysis is of central importance to the progress of an antifungal agent into clinical use. It is crucial to ensure that preclinical studies give the best possible prediction of the way drugs are likely to behave in a cl...
PMC10386083
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modelling to Predict Imatinib Exposures in Cancer Patients with Renal Dysfunction: A Case Study
Physiologically Based Pharmacokinetic Modelling to Predict Imatinib Exposures in Cancer Patients with Renal Dysfunction: A Case Study Abstract Imatinib is mainly metabolised by CYP3A4 and CYP2C8 and is extensively bound to α-acid glycoprotein (AAG). A physiologically based pharmacokinetic (PBPK) model for imatinib desc...
PMC10893190
core_pubmed_pmc
Simultaneously Predicting the Pharmacokinetics of CES1-Metabolized Drugs and Their Metabolites Using Physiologically Based Pharmacokinetic Model in Cirrhosis Subjects
Simultaneously Predicting the Pharmacokinetics of CES1-Metabolized Drugs and Their Metabolites Using Physiologically Based Pharmacokinetic Model in Cirrhosis Subjects Abstract Hepatic carboxylesterase 1 (CES1) metabolizes numerous prodrugs into active ingredients or direct-acting drugs into inactive metabolites. We aim...
PMC3572390
core_pubmed_pmc
VKORC1-dependent pharmacokinetics of intravenous and oral phylloquinone (vitamin K1) mixed micelles formulation
VKORC1-dependent pharmacokinetics of intravenous and oral phylloquinone (vitamin K1) mixed micelles formulation Abstract Objective The pharmacokinetics of phylloquinone (vitamin K1) were evaluated in healthy human adult volunteers (15 male and 15 female) following oral and intravenous administration of a mixed micelles...
PMC6347807
core_pubmed_pmc
Phase I clinical study of oral olaparib in pediatric patients with refractory solid tumors: study protocol
Phase I clinical study of oral olaparib in pediatric patients with refractory solid tumors: study protocol Abstract Abstract Background There is no established standard chemotherapy for recurrent pediatric solid tumors such as neuroblastoma and sarcoma. Since some of these tumor cells show dysfunctions in homologous re...
PMC6210332
core_pubmed_pmc
Impact of HACA on Immunomodulation and Treatment Toxicity Following ch14.18/CHO Long-Term Infusion with Interleukin-2: Results from a SIOPEN Phase 2 Trial
Impact of HACA on Immunomodulation and Treatment Toxicity Following ch14.18/CHO Long-Term Infusion with Interleukin-2: Results from a SIOPEN Phase 2 Trial Abstract GD 2 -directed immunotherapies improve survival of high-risk neuroblastoma (NB) patients (pts). Treatment with chimeric anti-GD 2 antibodies (Ab), such as c...
PMC5089609
core_pubmed_pmc
Randomised clinical trial: a phase 1, dose‐ranging study of the anti‐matrix metalloproteinase‐9 monoclonal antibody GS‐5745 versus placebo for ulcerative colitis
Randomised clinical trial: a phase 1, dose‐ranging study of the anti‐matrix metalloproteinase‐9 monoclonal antibody GS‐5745 versus placebo for ulcerative colitis Abstract Summary Background Matrix metalloproteinase‐9 is a proteolytic enzyme whose expression is increased in ulcerative colitis. Aim To evaluate the safety...
PMC6355467
core_pubmed_pmc
Development of a competitive enzyme-linked immunosorbent assay for therapeutic drug monitoring of afatinib
Development of a competitive enzyme-linked immunosorbent assay for therapeutic drug monitoring of afatinib Abstract Afatinib is an oral tyrosine kinase inhibitor (TKI) approved for treating advanced non-small cell lung cancer. It is necessary to develop a simple quantification method for TKIs in order to facilitate the...
PMC5828553
core_pubmed_pmc
Testosterone Diminishes Cabazitaxel Efficacy and Intratumoral Accumulation in a Prostate Cancer Xenograft Model ☆
Testosterone Diminishes Cabazitaxel Efficacy and Intratumoral Accumulation in a Prostate Cancer Xenograft Model ☆ Abstract Abstract Inactivation of the androgen receptor (AR) pathway by androgen deprivation therapy (ADT) is the mainstay of (metastatic) prostate cancer therapy. Ultimately, the AR pathway will be re-acti...
PMC5726127
core_pubmed_pmc
The CLOSED trial; CLOnidine compared with midazolam for SEDation of paediatric patients in the intensive care unit: study protocol for a multicentre randomised controlled trial
The CLOSED trial; CLOnidine compared with midazolam for SEDation of paediatric patients in the intensive care unit: study protocol for a multicentre randomised controlled trial Abstract Introduction Sedation is an essential part of paediatric critical care. Midazolam, often in combination with opioids, is the current g...
PMC5486349
core_pubmed_pmc
Community Response to Multiple Sound Sources: Integrating Acoustic and Contextual Approaches in the Analysis
Community Response to Multiple Sound Sources: Integrating Acoustic and Contextual Approaches in the Analysis Abstract Sufficient data refer to the relevant prevalence of sound exposure by mixed traffic sources in many nations. Furthermore, consideration of the potential effects of combined sound exposure is required in...
PMC7188053
core_pubmed_pmc
Effects of NT-814, a dual neurokinin 1 and 3 receptor antagonist, on vasomotor symptoms in postmenopausal women: a placebo-controlled, randomized trial
Effects of NT-814, a dual neurokinin 1 and 3 receptor antagonist, on vasomotor symptoms in postmenopausal women: a placebo-controlled, randomized trial Abstract Abstract Objectives: To evaluate the safety, pharmacokinetics, and preliminary efficacy of NT-814, a dual neurokinin 1,3 antagonist, in postmenopausal women wi...
PMC7345775
core_pubmed_pmc
A New Technological Advancement of the Drug-Induced Sleep Endoscopy (DISE) Procedure: The “All in One Glance” Strategy
A New Technological Advancement of the Drug-Induced Sleep Endoscopy (DISE) Procedure: The “All in One Glance” Strategy Abstract To illustrate a new technological advance in the standard drug-induced sleep endoscopy (DISE) model, a new machine was used, the Experimental 5 Video Stream System (5VsEs), which is capable of...
PMC4264455
core_pubmed_pmc
A Phase I study of cyclin-dependent kinase inhibitor, AT7519, in patients with advanced cancer: NCIC Clinical Trials Group IND 177
A Phase I study of cyclin-dependent kinase inhibitor, AT7519, in patients with advanced cancer: NCIC Clinical Trials Group IND 177 Abstract Background: AT7519 is a small-molecular inhibitor of multiple cyclin-dependent kinases (CDKs). It shows encouraging anti-cancer activity against multiple cell lines and in tumour x...
PMC11409070
core_pubmed_pmc
Pharmacodynamics of Sishen decoction in relieving rheumatoid arthritis: Chemical composition, regulatory pathway and online prediction simulation
Pharmacodynamics of Sishen decoction in relieving rheumatoid arthritis: Chemical composition, regulatory pathway and online prediction simulation Abstract As a commonly used traditional Chinese medicine formula for treating rheumatoid arthritis (RA), Sishen Decoction (SSD) has anti-inflammatory, analgesic and swelling ...
PMC12134156
core_pubmed_pmc
Pharmacokinetics of midazolam and hepatic cytochrome P450 3A activity in an in vivo extracorporeal membrane oxygenation rat model
Pharmacokinetics of midazolam and hepatic cytochrome P450 3A activity in an in vivo extracorporeal membrane oxygenation rat model Abstract Abstract Extracorporeal membrane oxygenation (ECMO) is increasingly being used in intensive care units. However, it can alter drug pharmacokinetics and lead to underexposure associa...
PMC10661895
core_pubmed_pmc
Perinatal tuberculosis—An approach to an under-recognized diagnosis
Perinatal tuberculosis—An approach to an under-recognized diagnosis Abstract Abstract Tuberculosis (TB) in young infants (<3 months of age), often referred to as perinatal TB, is underdiagnosed, leading to severe morbidity and high mortality. Perinatal TB includes both congenital and postnatal transmission of Mycobacte...
PMC10893066
core_pubmed_pmc
Pharmacokinetic Modeling to Guide Preclinical Development of an Islatravir-Eluting Reservoir-Style Biodegradable Implant for Long-Acting HIV PrEP
Pharmacokinetic Modeling to Guide Preclinical Development of an Islatravir-Eluting Reservoir-Style Biodegradable Implant for Long-Acting HIV PrEP Abstract Long-acting injectable cabotegravir is more effective than daily oral PrEP at preventing HIV transmission due to improved adherence, but requires bi-monthly large-vo...
PMC9735573
core_pubmed_pmc
In Vivo Sustained Release of the Retrograde Transport Inhibitor Retro-2.1 Formulated in a Thermosensitive Hydrogel
In Vivo Sustained Release of the Retrograde Transport Inhibitor Retro-2.1 Formulated in a Thermosensitive Hydrogel Abstract Abstract A recently developed inhibitor of retrograde transport, namely Retro-2.1, proved to be a potent and broad-spectrum lead in vitro against intracellular pathogens, such as toxins, parasites...
PMC12291526
core_pubmed_pmc
Development of AL101 (GSK4527226), a progranulin-elevating monoclonal antibody, as a potential treatment for Alzheimer’s disease
Development of AL101 (GSK4527226), a progranulin-elevating monoclonal antibody, as a potential treatment for Alzheimer’s disease Abstract Abstract Background Alzheimer’s disease (AD) is characterized by amyloid plaques, tau tangles, and neuronal loss. Progranulin (PGRN) is a secreted immune regulator, lysosomal chapero...
PMC5527306
core_pubmed_pmc
Polymyxin Combinations Combat Escherichia coli Harboring mcr-1 and bla NDM-5 : Preparation for a Postantibiotic Era
Polymyxin Combinations Combat Escherichia coli Harboring mcr-1 and bla NDM-5 : Preparation for a Postantibiotic Era Abstract ABSTRACT The rapid increase of carbapenem resistance in Gram-negative bacteria has resurrected the importance of the polymyxin antibiotics. The recent discovery of plasmid-mediated polymyxin resi...
PMC11071455
core_pubmed_pmc
Exploring the PET in vivo generator 134 Ce as a theranostic match for 225 Ac
Exploring the PET in vivo generator 134 Ce as a theranostic match for 225 Ac Abstract Purpose: The radionuclide pair cerium-134/lanthanum-134 ( 134 Ce/ 134 La) was recently proposed as a suitable diagnostic counterpart for the therapeutic alpha-emitter actinium-225 ( 225 Ac). The unique properties of 134 Ce offer persp...
PMC9166823
core_pubmed_pmc
How to account for hallucinations in the interpretation of the antidepressant effects of psychedelics: a translational framework
How to account for hallucinations in the interpretation of the antidepressant effects of psychedelics: a translational framework Abstract Abstract Rationale Recent trials with psychedelics in major depressive disorder and treatment-resistant depression showed remarkable improvements in depressive symptoms that can last...
PMC8140393
core_pubmed_pmc
A Novel Integrated Pharmacokinetic-Pharmacodynamic Model to Evaluate Combination Therapy and Determine In Vivo Synergism
A Novel Integrated Pharmacokinetic-Pharmacodynamic Model to Evaluate Combination Therapy and Determine In Vivo Synergism Abstract Understanding pharmacokinetic (PK)-pharmacodynamic (PD) relationships is essential in translational research. Existing PK-PD models for combination therapy lack consideration of quantitative...
PMC12449142
core_pubmed_pmc
Self-assembling polypeptide-drug conjugates as innovative therapeutic candidates for glioblastoma treatment by enhancing intracranial residence time
Self-assembling polypeptide-drug conjugates as innovative therapeutic candidates for glioblastoma treatment by enhancing intracranial residence time Abstract Abstract Background Glioblastoma (GBM) is the most lethal and incurable brain tumor, with limited treatment options. Systemic delivery of many promising drugs has...
PMC5065076
core_pubmed_pmc
Achieving a physiological cortisol profile with once-daily dual-release hydrocortisone: a pharmacokinetic study
Achieving a physiological cortisol profile with once-daily dual-release hydrocortisone: a pharmacokinetic study Abstract Objective Oral once-daily dual-release hydrocortisone (DR-HC) replacement therapy was developed to provide a cortisol exposure−time profile that closely resembles the physiological cortisol profile. ...
PMC8505155
core_pubmed_pmc
Pharmacokinetics and Safety of Ceftobiprole in Pediatric Patients
Pharmacokinetics and Safety of Ceftobiprole in Pediatric Patients Abstract Supplemental Digital Content is available in the text. Background: Ceftobiprole, the active moiety of the prodrug ceftobiprole medocaril, is an advanced-generation, broad-spectrum, intravenous cephalosporin, which is currently approved for the t...
PMC6994493
core_pubmed_pmc
Preclinical development of a miR-132 inhibitor for heart failure treatment
Preclinical development of a miR-132 inhibitor for heart failure treatment Abstract Abstract Despite proven efficacy of pharmacotherapies targeting primarily global neurohormonal dysregulation, heart failure (HF) is a growing pandemic with increasing burden. Treatments mechanistically focusing at the cardiomyocyte leve...
PMC8877436
core_pubmed_pmc
Clinical Update on Patient-Controlled Analgesia for Acute Postoperative Pain
Clinical Update on Patient-Controlled Analgesia for Acute Postoperative Pain Abstract Patient-controlled analgesia (PCA) is an effective method for controlling acute pain, including postoperative pain in adults and in children from five years of age, pain resulting from labor, trauma, or other medical situations, or ch...