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PMC5728039
core_pubmed_pmc
Safety, Pharmacokinetics, Pharmacodynamics, and Antitumor Activity of Necuparanib Combined with Nab‐Paclitaxel and Gemcitabine in Patients with Metastatic Pancreatic Cancer: Phase I Results
Safety, Pharmacokinetics, Pharmacodynamics, and Antitumor Activity of Necuparanib Combined with Nab‐Paclitaxel and Gemcitabine in Patients with Metastatic Pancreatic Cancer: Phase I Results Abstract Abstract Lessons Learned. Despite the compelling preclinical rationale of evaluating the genetically engineered heparin d...
PMC3791841
core_pubmed_pmc
Prospective Trial of a Novel Nomogram to Achieve Updated Vancomycin Trough Concentrations
Prospective Trial of a Novel Nomogram to Achieve Updated Vancomycin Trough Concentrations Abstract Abstract Purpose . To determine if the use of a novel vancomycin nomogram predicts dosing regimens that achieve target trough concentrations equal to or more accurate than dosing regimens calculated using traditional phar...
PMC4544506
core_pubmed_pmc
An Open-Label Investigation into Drug–Drug Interactions Between Multiple Doses of Daclatasvir and Single-Dose Cyclosporine or Tacrolimus in Healthy Subjects
An Open-Label Investigation into Drug–Drug Interactions Between Multiple Doses of Daclatasvir and Single-Dose Cyclosporine or Tacrolimus in Healthy Subjects Abstract Abstract Background and Objective Chronic hepatitis C virus (HCV) infection is a major cause of liver transplantation. Drug–drug interactions (DDIs) with ...
PMC12648932
core_pubmed_pmc
Safety and pharmacodynamics of the ferroportin inhibitor vamifeport in patients with non-transfusion-dependent β-thalassemia: results from a randomized phase 2a study
Safety and pharmacodynamics of the ferroportin inhibitor vamifeport in patients with non-transfusion-dependent β-thalassemia: results from a randomized phase 2a study Abstract Abstract Background Non-transfusion-dependent beta-thalassemia (β-NTDT) is characterized by ineffective erythropoiesis, increased intestinal iro...
PMC7005849
core_pubmed_pmc
Inhaled milrinone in cardiac surgical patients: a pilot randomized controlled trial of jet vs. mesh nebulization
Inhaled milrinone in cardiac surgical patients: a pilot randomized controlled trial of jet vs. mesh nebulization Abstract Abstract Inhaled milrinone administered before cardiopulmonary bypass (CPB) reduces the severity of pulmonary hypertension during cardiac surgery. However, milrinone pharmacokinetics has not been de...
PMC12680674
core_pubmed_pmc
Population pharmacokinetic characteristics of tacrolimus in Chinese lung transplant recipients and optimisation of dosing regimen during the early post-transplantation phase
Population pharmacokinetic characteristics of tacrolimus in Chinese lung transplant recipients and optimisation of dosing regimen during the early post-transplantation phase Abstract Purpose This study aimed to establish a population pharmacokinetic model and optimise tacrolimus dosing regimens in Chinese lung transpla...
PMC6017357
core_pubmed_pmc
In Vitro Inhibitory Effects of Synthetic Cannabinoid EAM-2201 on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes
In Vitro Inhibitory Effects of Synthetic Cannabinoid EAM-2201 on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes Abstract Abstract EAM-2201, a synthetic cannabinoid, is a potent agonist of the cannabinoid receptors that is widely abused as an illicit recreational drug in comb...
PMC4927104
core_pubmed_pmc
Dynamic PET Measures of Tau Accumulation in Cognitively Normal Older Adults and Alzheimer’s Disease Patients Measured Using [18F] THK-5351
Dynamic PET Measures of Tau Accumulation in Cognitively Normal Older Adults and Alzheimer’s Disease Patients Measured Using [18F] THK-5351 Abstract Background [ 18 F]THK5351, a recently-developed positron emission tomography (PET) tracer for measuring tau neurofibrillary tangle accumulation, may help researchers examin...
PMC12328545
core_pubmed_pmc
Anticancer potential of 2,2′-bipyridine hydroxamic acid derivatives in head and neck cancer therapy
Anticancer potential of 2,2′-bipyridine hydroxamic acid derivatives in head and neck cancer therapy Abstract Abstract The genesis of head and neck cancer (HNC) is attributed to the combined influence of genetic and epigenetic irregularities. While surgical resection and radiotherapy remain primary treatment modalities,...
PMC11322287
core_pubmed_pmc
Phytochemical screening, antioxidant, anti-diabetic, and anti-obesity activities, formulation, and characterization of a self-nanoemulsion system loaded with pomegranate ( Punica granatum ) seed oil
Phytochemical screening, antioxidant, anti-diabetic, and anti-obesity activities, formulation, and characterization of a self-nanoemulsion system loaded with pomegranate ( Punica granatum ) seed oil Abstract Abstract Pomegranate ( Punica granatum ) is a tree of the Punicaceae family that is widespread all over the worl...
PMC4613459
core_pubmed_pmc
Repurposing metformin: an old drug with new tricks in its binding pockets
Repurposing metformin: an old drug with new tricks in its binding pockets Abstract Improvements in healthcare and nutrition have generated remarkable increases in life expectancy worldwide. This is one of the greatest achievements of the modern world yet it also presents a grave challenge: as more people survive into l...
PMC12059079
core_pubmed_pmc
Investigation into the pharmacodynamics and pharmacokinetics of recombinant human interferon alfa-2b vaginal suppository following process optimization in chinese rhesus macaque
Investigation into the pharmacodynamics and pharmacokinetics of recombinant human interferon alfa-2b vaginal suppository following process optimization in chinese rhesus macaque Abstract Abstract Recombinant human interferon Alfa-2b vaginal suppository is a gynecological preparation mainly made of interferon, commonly ...
PMC3430287
core_pubmed_pmc
Pharmacokinetics and Tissue Distribution Study of Praeruptorin D from Radix Peucedani in Rats by High-Performance Liquid Chromatography (HPLC)
Pharmacokinetics and Tissue Distribution Study of Praeruptorin D from Radix Peucedani in Rats by High-Performance Liquid Chromatography (HPLC) Abstract Abstract Praeruptorin D (PD), a major pyranocoumarin isolated from Radix Peucedani, exhibited antitumor and anti-inflammatory activities. The aim of this study was to i...
PMC12048420
core_pubmed_pmc
A phase I dose-escalation and expansion study of RMX1002, a selective E-type prostanoid receptor 4 antagonist, as monotherapy and in combination with anti-PD-1 antibody in advanced solid tumors
A phase I dose-escalation and expansion study of RMX1002, a selective E-type prostanoid receptor 4 antagonist, as monotherapy and in combination with anti-PD-1 antibody in advanced solid tumors Abstract Abstract RMX1002 (grapiprant) is a selective E-type prostanoid receptor 4 (EP4) antagonist and a promising candidate ...
PMC3923730
core_pubmed_pmc
Translation of TRO40303 from myocardial infarction models to demonstration of safety and tolerance in a randomized Phase I trial
Translation of TRO40303 from myocardial infarction models to demonstration of safety and tolerance in a randomized Phase I trial Abstract Background Although reperfusion injury has been shown to be responsible for cardiomyocytes death after an acute myocardial infarction, there is currently no drug on the market that r...
PMC10698161
core_pubmed_pmc
Investigation of monoclonal antibody CSX-1004 for fentanyl overdose
Investigation of monoclonal antibody CSX-1004 for fentanyl overdose Abstract Abstract The opioid crisis in the United States is primarily driven by the highly potent synthetic opioid fentanyl leading to >70,000 overdose deaths annually; thus, new therapies for fentanyl overdose are urgently needed. Here, we present the...
PMC11768299
core_pubmed_pmc
Utilisation of the Innovative [18F]-Labelled Radiotracer [18F]-BIBD-071 Within HR+ Breast Cancer Xenograft Mouse Models
Utilisation of the Innovative [18F]-Labelled Radiotracer [18F]-BIBD-071 Within HR+ Breast Cancer Xenograft Mouse Models Abstract Abstract Background/Objectives: Aromatase plays a crucial role in the conversion of androgens to oestrogens and is often overexpressed in hormone-dependent tumours, particularly breast cancer...
PMC11102127
core_pubmed_pmc
Bioinformatics Study of Flavonoids From Genus Erythrina As Ace2 inhibitor Candidates For Covid-19 Treatment
Bioinformatics Study of Flavonoids From Genus Erythrina As Ace2 inhibitor Candidates For Covid-19 Treatment Abstract Purpose This study aimed to screen potential drug candidates from the flavonoids of the genus Erythrina for the Corona Virus Disease 2019 (COVID-19) treatment. Patients and Methods A comprehensive screen...
PMC9298550
core_pubmed_pmc
Population Pharmacokinetics and Initial Dosage Optimization of Tacrolimus in Pediatric Hematopoietic Stem Cell Transplant Patients
Population Pharmacokinetics and Initial Dosage Optimization of Tacrolimus in Pediatric Hematopoietic Stem Cell Transplant Patients Abstract Background: There is a substantial lack of tacrolimus pharmacokinetic information in pediatric hematopoietic stem cell transplant (HSCT) patients. This study aimed to develop popul...
PMC4453950
core_pubmed_pmc
A phase I dose-escalation study of eribulin and S-1 for metastatic breast cancer
A phase I dose-escalation study of eribulin and S-1 for metastatic breast cancer Abstract Abstract Background: We evaluated the safety, maximum-tolerated dose (MTD), pharmacokinetics, recommended dose for phase II (P2RD), and preliminary anticancer activity of a combination eribulin and S-1 therapeutic in metastatic br...
PMC11532938
core_pubmed_pmc
A first‐in‐human, randomized study of the safety, pharmacokinetics and pharmacodynamics of povetacicept, an enhanced dual BAFF/APRIL antagonist, in healthy adults
A first‐in‐human, randomized study of the safety, pharmacokinetics and pharmacodynamics of povetacicept, an enhanced dual BAFF/APRIL antagonist, in healthy adults Abstract Abstract Therapeutic agents targeting the tumor necrosis factor (TNF) superfamily cytokines B‐cell activating factor (BAFF, BLyS) and/or A PRolifera...
PMC11284834
core_pubmed_pmc
Phase I study of the safety and clinical activity of the interleukin-8 inhibitor AMY109 combined with atezolizumab in patients with advanced solid cancers
Phase I study of the safety and clinical activity of the interleukin-8 inhibitor AMY109 combined with atezolizumab in patients with advanced solid cancers Abstract Abstract Background Immunosuppressive conditions within the tumor microenvironment (TME) can allow tumors to evade the immune system, including by hampering...
PMC10916390
core_pubmed_pmc
Clofazimine as a substitute for rifampicin improves efficacy of Mycobacterium avium pulmonary disease treatment in the hollow-fiber model
Clofazimine as a substitute for rifampicin improves efficacy of Mycobacterium avium pulmonary disease treatment in the hollow-fiber model Abstract ABSTRACT Mycobacterium avium complex pulmonary disease is treated with an azithromycin, ethambutol, and rifampicin regimen, with limited efficacy. The role of rifampicin is ...
PMC6271950
core_pubmed_pmc
LC-MS/MS Determination and Pharmacokinetic Study of Dehydrocorydaline in Rat Plasma after Oral Administration of Dehydrocorydaline and Corydalis yanhusuo Extract
LC-MS/MS Determination and Pharmacokinetic Study of Dehydrocorydaline in Rat Plasma after Oral Administration of Dehydrocorydaline and Corydalis yanhusuo Extract Abstract A rapid, sensitive and selective liquid chromatography/tandem mass spectrometry method (LC-MS/MS) was developed and validated for determination of de...
PMC5110608
core_pubmed_pmc
dOFV distributions: a new diagnostic for the adequacy of parameter uncertainty in nonlinear mixed-effects models applied to the bootstrap
dOFV distributions: a new diagnostic for the adequacy of parameter uncertainty in nonlinear mixed-effects models applied to the bootstrap Abstract Abstract Knowledge of the uncertainty in model parameters is essential for decision-making in drug development. Contrarily to other aspects of nonlinear mixed effects models...
PMC4472613
core_pubmed_pmc
Dolutegravir Has No Effect on the Pharmacokinetics of Oral Contraceptives With Norgestimate and Ethinyl Estradiol
Dolutegravir Has No Effect on the Pharmacokinetics of Oral Contraceptives With Norgestimate and Ethinyl Estradiol Abstract Abstract Background: Dolutegravir (DTG; Tivicay; ViiV Healthcare, Research Triangle Park, NC) is an HIV-1-unboosted integrase inhibitor with no cytochrome P450 or uridine 5′diphosphate-glucuronosyl...
PMC11144121
core_pubmed_pmc
Pharmacokinetic and neuroimmune pharmacogenetic impacts on slow-release morphine cancer pain control and adverse effects
Pharmacokinetic and neuroimmune pharmacogenetic impacts on slow-release morphine cancer pain control and adverse effects Abstract Abstract The aim was to determine if opioid neuroimmunopharmacology pathway gene polymorphisms alter serum morphine, morphine-3-glucuronide and morphine-6-glucuronide concentration-response ...
PMC9365372
core_pubmed_pmc
A Novel Third-generation EGFR Tyrosine Kinase Inhibitor Abivertinib for EGFR T790M-mutant Non–Small Cell Lung Cancer: a Multicenter Phase I/II Study
A Novel Third-generation EGFR Tyrosine Kinase Inhibitor Abivertinib for EGFR T790M-mutant Non–Small Cell Lung Cancer: a Multicenter Phase I/II Study Abstract Abstract Purpose: To establish recommended phase II dose (RP2D) in phase I and evaluate safety and efficacy of abivertinib in patients with EGFR Thr790Met point m...
PMC9963006
core_pubmed_pmc
Surfactant and Block Copolymer Nanostructures: From Design and Development to Nanomedicine Preclinical Studies
Surfactant and Block Copolymer Nanostructures: From Design and Development to Nanomedicine Preclinical Studies Abstract Abstract The medical application of nanotechnology in the field of drug delivery has so far exhibited many efforts in treating simple to extremely complicated and life-threatening human conditions, wi...
PMC11873646
core_pubmed_pmc
Real-time platelet P2Y 12 receptor occupancy as a promising pharmacodynamics biomarker for bridging the gap between PK/PD of clopidogrel therapy
Real-time platelet P2Y 12 receptor occupancy as a promising pharmacodynamics biomarker for bridging the gap between PK/PD of clopidogrel therapy Abstract Abstract Clopidogrel effectively inhibits platelet aggregation in response to ADP by irreversibly binding to the platelet P2Y 12 receptor through its active metabolit...
PMC3994220
core_pubmed_pmc
Nanosuspension delivery of paclitaxel to xenograft mice can alter drug disposition and anti-tumor activity
Nanosuspension delivery of paclitaxel to xenograft mice can alter drug disposition and anti-tumor activity Abstract Abstract Paclitaxel is a common chemotherapeutic agent that is effective against various cancers. The poor aqueous solubility of paclitaxel necessitates a large percentage of Cremophor EL:ethanol (USP) in...
PMC5724581
core_pubmed_pmc
A Randomized, Two-Way Crossover Study to Evaluate the Pharmacokinetics of Caffeine Delivered Using Caffeinated Chewing Gum Versus a Marketed Caffeinated Beverage in Healthy Adult Volunteers
A Randomized, Two-Way Crossover Study to Evaluate the Pharmacokinetics of Caffeine Delivered Using Caffeinated Chewing Gum Versus a Marketed Caffeinated Beverage in Healthy Adult Volunteers Abstract Abstract Background: This study was conducted to compare the pharmacokinetics of caffeine delivered using caffeinated che...
PMC7464672
core_pubmed_pmc
Use of Supplemented or Human Material to Simulate PD Behavior of Antibiotics at the Target Site In Vitro
Use of Supplemented or Human Material to Simulate PD Behavior of Antibiotics at the Target Site In Vitro Abstract In antimicrobial drug development, in vitro antibiotic susceptibility testing is conducted in standard growth media, such as Mueller–Hinton broth (MHB). These growth media provide optimal bacterial growth, ...
PMC11962789
core_pubmed_pmc
A randomized, open-label, two-period crossover study to evaluate the bioequivalence and food effect between two formulations of regorafenib in healthy adult participants
A randomized, open-label, two-period crossover study to evaluate the bioequivalence and food effect between two formulations of regorafenib in healthy adult participants Abstract Abstract Background This research aimed to compare the bioequivalence of a test formulation (regorafenib produced by Beijing SL Pharmaceutica...
PMC4975851
core_pubmed_pmc
Exploration of a potent PI3 kinase/mTOR inhibitor as a novel anti-fibrotic agent in IPF
Exploration of a potent PI3 kinase/mTOR inhibitor as a novel anti-fibrotic agent in IPF Abstract Abstract Rationale Idiopathic pulmonary fibrosis (IPF) is the most rapidly progressive and fatal of all fibrotic conditions with no curative therapies. Common pathomechanisms between IPF and cancer are increasingly recognis...
PMC12783267
core_pubmed_pmc
Population Pharmacokinetics Analysis of Infliximab in up to 10-Year-Old Patients with Paediatric Inflammatory Bowel Disease: Label-Recommended Dose Fails to Achieve Therapeutic Target Concentration
Population Pharmacokinetics Analysis of Infliximab in up to 10-Year-Old Patients with Paediatric Inflammatory Bowel Disease: Label-Recommended Dose Fails to Achieve Therapeutic Target Concentration Abstract Background and Objectives Younger patients with paediatric inflammatory bowel disease (IBD) may require higher in...
PMC4661214
core_pubmed_pmc
Effect of Kidney Function on Drug Kinetics and Dosing in Neonates, Infants, and Children
Effect of Kidney Function on Drug Kinetics and Dosing in Neonates, Infants, and Children Abstract Neonates, infants, and children differ from adults in many aspects, not just in age, weight, and body composition. Growth, maturation and environmental factors affect drug kinetics, response and dosing in pediatric patient...
PMC9914162
core_pubmed_pmc
Managing uncertainty in antifungal dosing: antibiograms, therapeutic drug monitoring and drug-drug interactions
Managing uncertainty in antifungal dosing: antibiograms, therapeutic drug monitoring and drug-drug interactions Abstract Purpose of review A number of pharmacokinetic and pharmacodynamic factors in critically ill or severely immunosuppressed patients influence the effectiveness of antifungal therapy making dosing less ...
PMC12278411
core_pubmed_pmc
CMD-OPT model enables the discovery of a potent and selective RIPK2 inhibitor as preclinical candidate for the treatment of acute liver injury
CMD-OPT model enables the discovery of a potent and selective RIPK2 inhibitor as preclinical candidate for the treatment of acute liver injury Abstract Abstract Acute liver injury (ALI) serves as a critical precursor and major etiological factor in the progression and ultimate manifestation of various hepatic disorders...
PMC9263096
core_pubmed_pmc
Population Pharmacokinetic Model of AST-001, L-Isomer of Serine, Combining Endogenous Production and Exogenous Administration in Healthy Subjects
Population Pharmacokinetic Model of AST-001, L-Isomer of Serine, Combining Endogenous Production and Exogenous Administration in Healthy Subjects Abstract Abstract AST-001 is an L-isomer of serine that has protective effects on neurological disorders. This study aimed to establish a population pharmacokinetic (PK) mode...
PMC12944451
core_pubmed_pmc
Predictive Performance of Bayesian Methods to Forecast Vancomycin Concentration for Therapeutic Drug Monitoring in Critically Ill Pediatric Patients
Predictive Performance of Bayesian Methods to Forecast Vancomycin Concentration for Therapeutic Drug Monitoring in Critically Ill Pediatric Patients Abstract Abstract Background: This study aimed to evaluate different Bayesian algorithms and the first-order pharmacokinetics (PK) equation approach for forecasting vancom...
PMC5460240
core_pubmed_pmc
Translational learning from clinical studies predicts drug pharmacokinetics across patient populations
Translational learning from clinical studies predicts drug pharmacokinetics across patient populations Abstract Abstract Early indication of late-stage failure of novel candidate drugs could be facilitated by continuous integration, assessment, and transfer of knowledge acquired along pharmaceutical development program...
PMC12721056
core_pubmed_pmc
Antimicrobial pharmacokinetics and stewardship in critically Ill adult patients receiving ECMO: Challenges, evidence, and future directions
Antimicrobial pharmacokinetics and stewardship in critically Ill adult patients receiving ECMO: Challenges, evidence, and future directions Abstract Abstract Infection is a common indication and complication for extracorporeal membrane oxygenation (ECMO), and adult ECMO recipients face increased nosocomial infection ri...
PMC9944862
core_pubmed_pmc
Clinical effect of different doses of ciprofol for induction of general anesthesia in elderly patients: A randomized, controlled trial
Clinical effect of different doses of ciprofol for induction of general anesthesia in elderly patients: A randomized, controlled trial Abstract Abstract Ciprofol is a newly developed intravenous anesthetic agent with improved pharmacokinetic properties. Compared to propofol, ciprofol exhibits stronger binding to the GA...
PMC11256402
core_pubmed_pmc
Steady-state pharmacokinetics of lamivudine in end-stage kidney failure persons with detectable and undetectable HIV-1 RNA in peritoneal dialysis effluent
Steady-state pharmacokinetics of lamivudine in end-stage kidney failure persons with detectable and undetectable HIV-1 RNA in peritoneal dialysis effluent Abstract Background Renally adjusted lamivudine dosages are effective. However, some of the kidney failure patients managed with lamivudine-containing regimens are f...
PMC5944575
core_pubmed_pmc
Initial Clinical Experience with AZD5718, a Novel Once Daily Oral 5‐Lipoxygenase Activating Protein Inhibitor
Initial Clinical Experience with AZD5718, a Novel Once Daily Oral 5‐Lipoxygenase Activating Protein Inhibitor Abstract Abstract We evaluated safety, tolerability, pharmacokinetics, and pharmacodynamics of AZD5718, a novel 5‐lipooxygenase activating protein (FLAP) inhibitor, in a randomized, single‐blind, placebo‐contro...
PMC9047529
core_pubmed_pmc
Semi-Mechanistic Pharmacokinetic-Pharmacodynamic Model of Camostat Mesylate-Predicted Efficacy against SARS-CoV-2 in COVID-19
Semi-Mechanistic Pharmacokinetic-Pharmacodynamic Model of Camostat Mesylate-Predicted Efficacy against SARS-CoV-2 in COVID-19 Abstract ABSTRACT The SARS-CoV-2 coronavirus, which causes COVID-19, uses a viral surface spike protein for host cell entry and the human cell-surface transmembrane serine protease, TMPRSS2, to ...
PMC10882417
core_pubmed_pmc
Analysis of Drugs Prescribed to Elderly Patients in a Tertiary Health Care Center in Raipur, Central India: An Observational Study
Analysis of Drugs Prescribed to Elderly Patients in a Tertiary Health Care Center in Raipur, Central India: An Observational Study Abstract Background Most elderly patients suffer from multiple diseases and are on multiple drugs for treatment. Polypharmacy in the elderly, physiological changes with old age, changes in ...
PMC10443802
core_pubmed_pmc
Targeting a xenobiotic transporter to ameliorate vincristine-induced sensory neuropathy
Targeting a xenobiotic transporter to ameliorate vincristine-induced sensory neuropathy Abstract Abstract Vincristine is a widely used chemotherapeutic drug for the treatment of multiple malignant diseases that causes a dose-limiting peripheral neurotoxicity. There is no clinically effective preventative treatment for ...
PMC8273902
core_pubmed_pmc
A Phase I Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of TPN171H, a Novel Phosphodiesterase Type 5 Inhibitor, in Healthy Subjects
A Phase I Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of TPN171H, a Novel Phosphodiesterase Type 5 Inhibitor, in Healthy Subjects Abstract Purpose TPN171H is a novel, potent and selective phosphodiesterase type 5 (PDE5) inhibitor for the treatment of pulmonary arterial hypertension (PAH). The objec...
PMC12764295
core_pubmed_pmc
Plasma Concentrations of Prophylactic Posaconazole and Risk Factors for Subtherapeutic Exposure in Taiwanese Patients with Hematologic Malignancies
Plasma Concentrations of Prophylactic Posaconazole and Risk Factors for Subtherapeutic Exposure in Taiwanese Patients with Hematologic Malignancies Abstract Background Posaconazole is widely used for antifungal prophylaxis in patients with hematologic malignancies. However, interindividual pharmacokinetic variability m...
PMC8107163
core_pubmed_pmc
Comparable Pharmacokinetics, Safety, and Tolerability of Etrolizumab Administered by Prefilled Syringe or Autoinjector in a Randomized Trial in Healthy Volunteers
Comparable Pharmacokinetics, Safety, and Tolerability of Etrolizumab Administered by Prefilled Syringe or Autoinjector in a Randomized Trial in Healthy Volunteers Abstract Introduction Etrolizumab is a novel, dual-action anti-β7 integrin antibody studied in phase 3 trials in patients with inflammatory bowel disease. An...
PMC8885207
core_pubmed_pmc
New Approach for Targeted Treatment of Mild COVID-19 by Honeysuckle through Network Pharmacology Analysis
New Approach for Targeted Treatment of Mild COVID-19 by Honeysuckle through Network Pharmacology Analysis Abstract Objective To investigate the potential pharmacological value of extracts from honeysuckle on patients with mild coronavirus disease 2019 (COVID-19) infection. Methods The active components and targets of h...
PMC11457669
core_pubmed_pmc
Immunoglobulin therapies for primary immunodeficiency diseases (part 1): understanding the pharmacokinetics
Immunoglobulin therapies for primary immunodeficiency diseases (part 1): understanding the pharmacokinetics Abstract Abstract Immunoglobulin G (IgG) therapies have been used for decades as standard treatment for patients with primary antibody deficiencies. Monitoring the pharmacokinetics (PK) of IgG is a key component ...
PMC6234579
core_pubmed_pmc
Biaryl scaffold-focused virtual screening for anti-aggregatory and neuroprotective effects in Alzheimer’s disease
Biaryl scaffold-focused virtual screening for anti-aggregatory and neuroprotective effects in Alzheimer’s disease Abstract Background Alzheimer’s disease (AD) is a primary cause of dementia in ageing population affecting more than 35 million people around the globe. It is a chronic neurodegenerative disease caused by d...
PMC11207075
core_pubmed_pmc
Heparin Dosing Regimen Optimization in Veno-Arterial Extracorporeal Membrane Oxygenation: A Pharmacokinetic Analysis
Heparin Dosing Regimen Optimization in Veno-Arterial Extracorporeal Membrane Oxygenation: A Pharmacokinetic Analysis Abstract Abstract Background. Unfractionated heparin is administered in patients undergoing veno-arterial extracorporeal membrane oxygenation (VA-ECMO). Anticoagulation monitoring is recommended, with an...
PMC5592851
core_pubmed_pmc
Phospho-valproic acid inhibits pancreatic cancer growth in mice: Enhanced efficacy by its formulation in poly-(L)-lactic acid-poly(ethylene glycol) nanoparticles
Phospho-valproic acid inhibits pancreatic cancer growth in mice: Enhanced efficacy by its formulation in poly-(L)-lactic acid-poly(ethylene glycol) nanoparticles Abstract Abstract Pancreatic cancer (PC) is one of the most difficult cancers to treat. Since the current chemotherapy is inadequate and various biological ap...
PMC11330185
core_pubmed_pmc
Population pharmacokinetic modeling of sotatercept in healthy participants and patients with pulmonary arterial hypertension
Population pharmacokinetic modeling of sotatercept in healthy participants and patients with pulmonary arterial hypertension Abstract Abstract Sotatercept is a breakthrough, first‐in‐class biologic, that is FDA‐approved for the treatment of pulmonary arterial hypertension (PAH). A population pharmacokinetic (PopPK) mod...
PMC12960017
core_pubmed_pmc
Evaluation of the Effect of Food and Formulation on the Pharmacokinetics of the SHP2 Inhibitor Migoprotafib Within a Phase I Study in Cancer Patients
Evaluation of the Effect of Food and Formulation on the Pharmacokinetics of the SHP2 Inhibitor Migoprotafib Within a Phase I Study in Cancer Patients Abstract ABSTRACT Migoprotafib is a potent and selective inhibitor of Src homology‐2 domain‐containing phosphatase 2 (SHP2) under investigation in Phase I (PhI) trials bo...
PMC9024011
core_pubmed_pmc
HINT: Hierarchical interaction network for clinical-trial-outcome predictions
HINT: Hierarchical interaction network for clinical-trial-outcome predictions Abstract Summary Clinical trials are crucial for drug development but often face uncertain outcomes due to safety, efficacy, or patient-recruitment problems. We propose the Hierarchical Interaction Network (HINT) to predict clinical trial out...
PMC4668604
core_pubmed_pmc
Pharmacokinetics/pharmacodynamics of marbofloxacin in a Pasteurella multocida serious murine lung infection model
Pharmacokinetics/pharmacodynamics of marbofloxacin in a Pasteurella multocida serious murine lung infection model Abstract Abstract Background Marbofloxacin is a third-generation fluoroquinolone developed solely for veterinary medicine with a broad spectrum of antibacterial activity against some Gram-positive and most ...
PMC9962402
core_pubmed_pmc
Fast and Simple Liquid Chromatography-Isotope Dilution Tandem Mass Spectrometry Method for Therapeutic Drug Monitoring of Dalbavancin in Long-Term Treatment of Subacute and/or Chronic Infections
Fast and Simple Liquid Chromatography-Isotope Dilution Tandem Mass Spectrometry Method for Therapeutic Drug Monitoring of Dalbavancin in Long-Term Treatment of Subacute and/or Chronic Infections Abstract Abstract Dalbavancin (DBV) is a long-acting antistaphylococcal lypoglycopeptide that is being increasingly used for ...
PMC6171046
core_pubmed_pmc
Pharmacokinetics and safety/efficacy of levodopa pro-drug ONO-2160/carbidopa for Parkinson's disease
Pharmacokinetics and safety/efficacy of levodopa pro-drug ONO-2160/carbidopa for Parkinson's disease Abstract Abstract We conducted a phase I study investigating the efficacy, safety, and tolerability of ONO-2160, a newly developed levodopa pro-drug, and carbidopa compared with levodopa and carbidopa to stabilize levod...
PMC12179046
core_pubmed_pmc
Attenuation of the plasma volume response to crystalloid fluid used for goal-directed fluid therapy
Attenuation of the plasma volume response to crystalloid fluid used for goal-directed fluid therapy Abstract Abstract Background Goal-directed fluid therapy uses repeated bolus infusions of crystalloid or colloid fluid to increase the plasma volume for the purpose of challenging the patient’s position on the Frank-Star...
PMC4916778
core_pubmed_pmc
Impact of ATM and SLC22A1 Polymorphisms on Therapeutic Response to Metformin in Iranian Diabetic Patients
Impact of ATM and SLC22A1 Polymorphisms on Therapeutic Response to Metformin in Iranian Diabetic Patients Abstract Metabolic syndrome and its pathological sequel, type 2 diabetes are considered as important global health problems. Metformin is the most common drug prescribed for patients with this disorder. Consequentl...
PMC4222610
core_pubmed_pmc
Mercaptopurine/Methotrexate Maintenance Therapy of Childhood Acute Lymphoblastic Leukemia: Clinical Facts and Fiction
Mercaptopurine/Methotrexate Maintenance Therapy of Childhood Acute Lymphoblastic Leukemia: Clinical Facts and Fiction Abstract Supplemental Digital Content is available in the text. Key Words: leukemia, acute, lymphoblastic, maintenance therapy, 6-mercaptopurine, methotrexate, pharmacology, drug metabolism, pharmacokin...
PMC8546845
core_pubmed_pmc
Preclinical Evaluation of Recombinant Microbial Glycoside Hydrolases in the Prevention of Experimental Invasive Aspergillosis
Preclinical Evaluation of Recombinant Microbial Glycoside Hydrolases in the Prevention of Experimental Invasive Aspergillosis Abstract ABSTRACT Aspergillus fumigatus is a ubiquitous mold that can cause invasive pulmonary infections in immunocompromised patients. Within the lung, A. fumigatus forms biofilms that can enh...
PMC11884223
core_pubmed_pmc
Comparative bioavailability of single‐dose zavegepant during and between migraine attacks: A phase 1, randomized, open‐label, fixed‐sequence, two‐period study
Comparative bioavailability of single‐dose zavegepant during and between migraine attacks: A phase 1, randomized, open‐label, fixed‐sequence, two‐period study Abstract Abstract Objective To compare the rate and extent of absorption of zavegepant 10 mg (therapeutic dose) or 20 mg (supratherapeutic dose) nasal spray duri...
PMC9092181
core_pubmed_pmc
Sedation and analgesia from prolonged pain and stress during mechanical ventilation in preterm infants: is dexmedetomidine an alternative to current practice?
Sedation and analgesia from prolonged pain and stress during mechanical ventilation in preterm infants: is dexmedetomidine an alternative to current practice? Abstract Mechanical ventilation is an uncomfortable and potentially painful intervention. Opioids, such as morphine and fentanyl, are used for analgesia and seda...
PMC5133775
core_pubmed_pmc
Integrated Computational Approach for Virtual Hit Identification against Ebola Viral Proteins VP35 and VP40
Integrated Computational Approach for Virtual Hit Identification against Ebola Viral Proteins VP35 and VP40 Abstract Abstract The Ebola virus (EBOV) has been recognised for nearly 40 years, with the most recent EBOV outbreak being in West Africa, where it created a humanitarian crisis. Mortalities reported up to 30 Mar...
PMC9672460
core_pubmed_pmc
First-in-human study to investigate the safety and pharmacokinetics of salvianolic acid A and pharmacokinetic simulation using a physiologically based pharmacokinetic model
First-in-human study to investigate the safety and pharmacokinetics of salvianolic acid A and pharmacokinetic simulation using a physiologically based pharmacokinetic model Abstract Salvianolic acid A (SAA) is a water-soluble phenolic acid component from Salvia miltiorrhiza Bunge currently under development for myocard...
PMC3977662
core_pubmed_pmc
A systematic review of effectiveness and safety of different regimens of levonorgestrel oral tablets for emergency contraception
A systematic review of effectiveness and safety of different regimens of levonorgestrel oral tablets for emergency contraception Abstract Background Unintended pregnancy is a complex phenomenon which raise to take an emergency decision. Low contraceptive prevalence and high user failure rates are the leading causes of ...
PMC5706346
core_pubmed_pmc
A Mathematical Model to Predict HIV Virological Failure and Elucidate the Role of Lymph Node Drug Penetration
A Mathematical Model to Predict HIV Virological Failure and Elucidate the Role of Lymph Node Drug Penetration Abstract Abstract Preventing virological failure following HIV treatment remains a difficult task that is further complicated by the emergence of drug resistance. We have developed a mathematical model able to ...
PMC8247400
core_pubmed_pmc
Pharmacometric analyses to characterize the effect of CSL112 on apolipoprotein A‐I and cholesterol efflux capacity in acute myocardial infarction patients
Pharmacometric analyses to characterize the effect of CSL112 on apolipoprotein A‐I and cholesterol efflux capacity in acute myocardial infarction patients Abstract Abstract Aims To characterize relationships between apolipoprotein A‐I (apoA‐I) exposure and cholesterol efflux capacity (CEC) and covariate effects followi...
PMC12176722
core_pubmed_pmc
Characterization of in vivo binding kinetics and non-displaceable binding of [ 18 F]SynvesT-1 in the rat brain
Characterization of in vivo binding kinetics and non-displaceable binding of [ 18 F]SynvesT-1 in the rat brain Abstract Abstract Background The synaptic vesicle glycoprotein 2 A (SV2A) has been identified as a biomarker of interest for neurological pathology. The SV2A specific radiotracer [ 18 F]SynVesT-1 has shown goo...
PMC11067344
core_pubmed_pmc
Role of therapeutic drug monitoring in the treatment of multi-drug resistant tuberculosis
Role of therapeutic drug monitoring in the treatment of multi-drug resistant tuberculosis Abstract Abstract Tuberculosis (TB) is a leading cause of mortality worldwide, and resistance to anti-tuberculosis drugs is a challenge to effective treatment. Multi-drug resistant TB (MDR-TB) can be difficult to treat, requiring ...
PMC10044023
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Target Attainment of Ceftazidime in Adult Patients on General Wards with Different Degrees of Renal Function: A Prospective Observational Bicenter Cohort Study
Pharmacokinetic/Pharmacodynamic Target Attainment of Ceftazidime in Adult Patients on General Wards with Different Degrees of Renal Function: A Prospective Observational Bicenter Cohort Study Abstract No prospective evidence exists on the pharmacokinetic/pharmacodynamic (PK/PD) target attainment of ceftazidime in adult...
PMC6440449
core_pubmed_pmc
One-step mechanochemical preparation and prominent antitumor activity of SN-38 self-micelle solid dispersion
One-step mechanochemical preparation and prominent antitumor activity of SN-38 self-micelle solid dispersion Abstract Abstract Purpose The purpose of this study was to overcome the clinical defects of 7-ethyl-10-hydroxycamptothecin (SN-38) and explore its characteristics and antitumor effects. Materials and methods An ...
PMC11788801
core_pubmed_pmc
Effect of Hematopoietic Stem Cell Transplantation Regimen on Tacrolimus Pharmacokinetics
Effect of Hematopoietic Stem Cell Transplantation Regimen on Tacrolimus Pharmacokinetics Abstract Abstract Objectives Treatment with tacrolimus requires strict control of the whole-blood concentration in patients undergoing allogeneic hematopoietic stem cell transplantation (HSCT). In patients undergoing cord blood tra...
PMC12707092
core_pubmed_pmc
Antitumor activity and structure–activity relationship of poly (ADP-ribose) polymerase (PARP)-based dual inhibitors
Antitumor activity and structure–activity relationship of poly (ADP-ribose) polymerase (PARP)-based dual inhibitors Abstract Abstract Poly(ADP-ribose) polymerase (PARP) inhibitors constitute a significant class of targeted anticancer therapies that leverage the principle of synthetic lethality in tumours deficient in h...
PMC9704089
core_pubmed_pmc
Factors determining the oral absorption and systemic disposition of zeaxanthin in rats: in vitro , in situ , and in vivo evaluations
Factors determining the oral absorption and systemic disposition of zeaxanthin in rats: in vitro , in situ , and in vivo evaluations Abstract Abstract Context Zeaxanthin is a yellow‑coloured dietary carotenoid widely recognized as an essential component of the macula. It exerts blue light filtering and antioxidant acti...
PMC12197275
core_pubmed_pmc
Preclinical Pharmacokinetic Evaluation of Mithramycin and Mithramycin SA Tryptophan-Conjugated Analog
Preclinical Pharmacokinetic Evaluation of Mithramycin and Mithramycin SA Tryptophan-Conjugated Analog Abstract Abstract Background : Mithramycin (MTM) is a polyketide anti-cancer natural product previously identified as an EWS-FLI1 inhibitor. This oncogenic transcription factor is a canonical target for drug developmen...
PMC6337497
core_pubmed_pmc
Potent Anti-Cancer Properties of Phthalimide-Based Curcumin Derivatives on Prostate Tumor Cells
Potent Anti-Cancer Properties of Phthalimide-Based Curcumin Derivatives on Prostate Tumor Cells Abstract Metastatic castration-resistant prostate cancer is commonly treated with chemotherapy, whose effect is less than satisfactory. This raised the need for novel agents for the treatment of prostate cancer. In the prese...
PMC10138475
core_pubmed_pmc
Qualitative assessment of healthy volunteer experience receiving subcutaneous infusions of high-dose benzathine penicillin G (SCIP) provides insights into design of late phase clinical studies
Qualitative assessment of healthy volunteer experience receiving subcutaneous infusions of high-dose benzathine penicillin G (SCIP) provides insights into design of late phase clinical studies Abstract Introduction Secondary prophylaxis to prevent rheumatic heart disease (RHD) progression, in the form of four-weekly in...
PMC9022370
core_pubmed_pmc
Demonstration of relative bioavailability of newly developed and innovator drug metaxalone 800 mg in healthy subjects under fed condition
Demonstration of relative bioavailability of newly developed and innovator drug metaxalone 800 mg in healthy subjects under fed condition Abstract Abstract The notable unbiased of this research work was to evaluate the well-being and effectiveness of metaxalone by administering the newly developed test and reference dr...
PMC11074091
core_pubmed_pmc
In silico investigation of cannabinoids from Cannabis sativa leaves as a potential anticancer drug to inhibit MAPK-ERK signaling pathway and EMT induction
In silico investigation of cannabinoids from Cannabis sativa leaves as a potential anticancer drug to inhibit MAPK-ERK signaling pathway and EMT induction Abstract Abstract Genes related to MAPK-ERK signaling pathways, and epithelial-mesenchymal transition induction is evolutionarily conserved and has crucial roles in ...
PMC10743492
core_pubmed_pmc
A Randomized, Open-Label, Single-Dose, Crossover Study of the Comparative Bioavailability of EPA and DHA in a Novel Liquid Crystalline Nanoparticle-Based Formulation of ω-3 Acid Ethyl Ester Versus Omacor ® Soft Capsule among Healthy Adults
A Randomized, Open-Label, Single-Dose, Crossover Study of the Comparative Bioavailability of EPA and DHA in a Novel Liquid Crystalline Nanoparticle-Based Formulation of ω-3 Acid Ethyl Ester Versus Omacor ® Soft Capsule among Healthy Adults Abstract Eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) are well kno...
PMC6863955
core_pubmed_pmc
Quantitation of a Novel Engineered Anti-infective Host Defense Peptide, ARV-1502: Pharmacokinetic Study of Different Doses in Rats and Dogs
Quantitation of a Novel Engineered Anti-infective Host Defense Peptide, ARV-1502: Pharmacokinetic Study of Different Doses in Rats and Dogs Abstract Abstract The designer proline-rich antimicrobial peptide (PrAMP) Chex1-Arg20 amide (ARV-1502) is active against Gram-negative and Gram-positive pathogens in different muri...
PMC6073835
core_pubmed_pmc
Multiscale Tumor Modeling With Drug Pharmacokinetic and Pharmacodynamic Profile Using Stochastic Hybrid System
Multiscale Tumor Modeling With Drug Pharmacokinetic and Pharmacodynamic Profile Using Stochastic Hybrid System Abstract Effective cancer treatment strategy requires an understanding of cancer behavior and development across multiple temporal and spatial scales. This has resulted into a growing interest in developing mu...
PMC12402790
core_pubmed_pmc
Development of a First-in-Class Click Chemistry–Based Cancer Therapeutic, from Preclinical Evaluation to a First-in-Human Dose Escalation Clinical Trial
Development of a First-in-Class Click Chemistry–Based Cancer Therapeutic, from Preclinical Evaluation to a First-in-Human Dose Escalation Clinical Trial Abstract Abstract Purpose: Achieving precise drug activation without associated toxicities is a significant challenge in developing cancer therapeutics. Click Activate...
PMC6032206
core_pubmed_pmc
Cytotoxicity of Plant-Mediated Synthesis of Metallic Nanoparticles: A Systematic Review
Cytotoxicity of Plant-Mediated Synthesis of Metallic Nanoparticles: A Systematic Review Abstract Abstract In the field of medicine, nanomaterials, especially those derived using the green method, offer promise as anti-cancer agents and drug carriers. However, the biosafety of metallic nanoparticles used as anti-cancer ...
PMC11687140
core_pubmed_pmc
External Validation of the Population Pharmacokinetic Models of Amisulpride and Remedial Strategies for Delayed or Missed Doses
External Validation of the Population Pharmacokinetic Models of Amisulpride and Remedial Strategies for Delayed or Missed Doses Abstract Abstract Objective This study aimed to evaluate the predictive performance of published amisulpride population pharmacokinetic (PopPK) models in schizophrenia patients with an externa...
PMC8957252
core_pubmed_pmc
Physiologically-based pharmacokinetic simulations in pharmacotherapy: selection of the optimal administration route for exogenous melatonin
Physiologically-based pharmacokinetic simulations in pharmacotherapy: selection of the optimal administration route for exogenous melatonin Abstract The benefits of melatonin on human body are drawing increasing attention from several researchers in different fields. While its role as cure for sleep disturbances (e.g.,...
PMC3612826
core_pubmed_pmc
Structural-Functional Analysis of 2,1,3-Benzoxadiazoles and Their N-oxides As HIV-1 Integrase Inhibitors
Structural-Functional Analysis of 2,1,3-Benzoxadiazoles and Their N-oxides As HIV-1 Integrase Inhibitors Abstract Abstract Human immunodeficiency virus type 1 integrase is one of the most attractive targets for the development of anti-HIV-1 inhibitors. The capacity of a series of 2,1,3-benzoxadiazoles (benzofurazans) a...
PMC7256326
core_pubmed_pmc
Pharmacokinetics of oral l -serine supplementation in a single patient
Pharmacokinetics of oral l -serine supplementation in a single patient Abstract Serine, a non-essential amino acid, has attracted clinical attention because of potential benefit in certain metabolic and neurological disorders. Despite the therapeutic potential, little is known about the pharmacokinetics of l -serine me...
PMC12672406
core_pubmed_pmc
Phenobarbital Bioequivalence in Chinese Population: Considering the Role of Food on Pharmacokinetics
Phenobarbital Bioequivalence in Chinese Population: Considering the Role of Food on Pharmacokinetics Abstract Abstract Epilepsy is one of the most severe neurological disorders in the world, which might seriously endanger the lives of patients. Phenobarbital is an important medicine clinically used for the treatment of...
PMC11550268
core_pubmed_pmc
Bilastine Reimagined: A Comprehensive Exploration of Pruritus Management With a Novel Antihistamine
Bilastine Reimagined: A Comprehensive Exploration of Pruritus Management With a Novel Antihistamine Abstract Abstract Managing pruritic conditions is essential due to their significant impact on patients' quality of life. Chronic urticaria (CU), characterized by persistent itching and hives, severely affects daily acti...
PMC10976223
core_pubmed_pmc
Design, Synthesis, and Biological Evaluation of Novel Coumarin Analogs Targeted against SARS-CoV-2
Design, Synthesis, and Biological Evaluation of Novel Coumarin Analogs Targeted against SARS-CoV-2 Abstract Abstract SARS-CoV, an RNA virus, is contagious and displays a remarkable degree of adaptability, resulting in intricate disease presentations marked by frequent genetic mutations that can ultimately give rise to ...
PMC10303681
core_pubmed_pmc
Is the Pharmacokinetics of First-Line Anti-TB Drugs a Cause of High Mortality Rates in TB Patients Admitted to the ICU? A Non-Compartmental Pharmacokinetic Analysis
Is the Pharmacokinetics of First-Line Anti-TB Drugs a Cause of High Mortality Rates in TB Patients Admitted to the ICU? A Non-Compartmental Pharmacokinetic Analysis Abstract Abstract Background: Patients with tuberculosis (TB) may develop multi-organ failure and require admission to intensive care. In these cases, the ...
PMC8694392
core_pubmed_pmc
HSA-Lys-161 covalent bound fluorescent dye for in vivo blood drug dynamic imaging and tumor mapping †
HSA-Lys-161 covalent bound fluorescent dye for in vivo blood drug dynamic imaging and tumor mapping † Abstract The specific combination of human serum albumin and fluorescent dye will endow superior performance to a coupled fluorescent platform for in vivo fluorescence labeling. In this study, we found that lysine-161 ...