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PMC3597034
core_pubmed_pmc
An in vivo large-scale chemical screening platform using Drosophila for anti-cancer drug discovery
An in vivo large-scale chemical screening platform using Drosophila for anti-cancer drug discovery Abstract SUMMARY Anti-cancer drug development involves enormous expenditure and risk. For rapid and economical identification of novel, bioavailable anti-tumour chemicals, the use of appropriate in vivo tumour models suit...
PMC12394218
core_pubmed_pmc
Post marketing safety assessment of the novel postpartum depression drug, Zuranolone: evidence from real-world pharmacovigilance analysis based on the FDA adverse event reporting system
Post marketing safety assessment of the novel postpartum depression drug, Zuranolone: evidence from real-world pharmacovigilance analysis based on the FDA adverse event reporting system Abstract Abstract Objective Zuranolone, the latest oral medication for postpartum depression, was approved in the United States in Aug...
PMC12158835
core_pubmed_pmc
Advances in Physiologically Based Pharmacokinetic (PBPK) Modeling and its Regulatory Utility to Support Oral Drug Product Development and Harmonization
Advances in Physiologically Based Pharmacokinetic (PBPK) Modeling and its Regulatory Utility to Support Oral Drug Product Development and Harmonization Abstract This report summarizes the proceedings of Session 1 of the one-day public workshop titled “ Advances in PBPK Modeling and its Regulatory Utility for Oral Drug ...
PMC12449379
core_pubmed_pmc
Population pharmacokinetic analysis of fluorouracil and oxaliplatin in the absence or presence of zolbetuximab in locally advanced unresectable or metastatic gastric or gastroesophageal junction adenocarcinoma
Population pharmacokinetic analysis of fluorouracil and oxaliplatin in the absence or presence of zolbetuximab in locally advanced unresectable or metastatic gastric or gastroesophageal junction adenocarcinoma Abstract Abstract Purpose Zolbetuximab, a monoclonal antibody targeting claudin 18.2 (CLDN18.2), is approved i...
PMC9981942
core_pubmed_pmc
Pharmacokinetics and tissue distribution of Ramulus Mori (Sangzhi) alkaloids in rats and its effects on liver enzyme activity
Pharmacokinetics and tissue distribution of Ramulus Mori (Sangzhi) alkaloids in rats and its effects on liver enzyme activity Abstract Ramulus Mori (Sangzhi) alkaloids (SZ-A) derived from twigs of mulberry ( Morus alba L., genus Morus in the Moraceae family) was approved by the National Medical Products Administration ...
PMC7268171
core_pubmed_pmc
First-in-human phase I trial of anti-hepatocyte growth factor antibody (YYB101) in refractory solid tumor patients
First-in-human phase I trial of anti-hepatocyte growth factor antibody (YYB101) in refractory solid tumor patients Abstract Background: YYB101, a humanized monoclonal antibody against hepatocyte growth factor (HGF), has shown safety and efficacy in vitro and in vivo . This is a first-in-human trial of this antibody. Ma...
PMC9525081
core_pubmed_pmc
Population pharmacokinetics of apramycin from first-in-human plasma and urine data to support prediction of efficacious dose
Population pharmacokinetics of apramycin from first-in-human plasma and urine data to support prediction of efficacious dose Abstract Abstract Background Apramycin is under development for human use as EBL-1003, a crystalline free base of apramycin, in face of increasing incidence of multidrug-resistant bacteria. Both ...
PMC4279949
core_pubmed_pmc
Melatonin as a potential therapy for sepsis: a phase I dose escalation study and an ex vivo whole blood model under conditions of sepsis
Melatonin as a potential therapy for sepsis: a phase I dose escalation study and an ex vivo whole blood model under conditions of sepsis Abstract Abstract Sepsis is a massive inflammatory response mediated by infection, characterized by oxidative stress, release of cytokines, and mitochondrial dysfunction. Melatonin ac...
PMC6073839
core_pubmed_pmc
Pharmacokinetics and Bioavailability Study of a Prednisolone Tablet as a Single Oral Dose in Bangladeshi Healthy Volunteers
Pharmacokinetics and Bioavailability Study of a Prednisolone Tablet as a Single Oral Dose in Bangladeshi Healthy Volunteers Abstract The aim of the study was to assess the pharmacokinetic and bioavailability of 2 formulations of 5-mg prednisolone tablets, reference product (Teva UK Limited) and Pred (Eskayef Bangladesh...
PMC9032182
core_pubmed_pmc
Tailoring of Selenium-Plated Novasomes for Fine-Tuning Pharmacokinetic and Tumor Uptake of Quercetin: In Vitro Optimization and In Vivo Radiobiodistribution Assessment in Ehrlich Tumor-Bearing Mice
Tailoring of Selenium-Plated Novasomes for Fine-Tuning Pharmacokinetic and Tumor Uptake of Quercetin: In Vitro Optimization and In Vivo Radiobiodistribution Assessment in Ehrlich Tumor-Bearing Mice Abstract Abstract Quercetin (QRC) is a bioflavonoid with anti-inflammatory, antioxidant, and anticancer activities, yet QR...
PMC11698297
core_pubmed_pmc
Raw Ocimum sanctum L. leaf extract modulates the pharmacokinetic of ceftriaxone and increases its bioavailability in staphylococcal mastitis
Raw Ocimum sanctum L. leaf extract modulates the pharmacokinetic of ceftriaxone and increases its bioavailability in staphylococcal mastitis Abstract Abstract BACKGROUND: To study the pharmacokinetic interaction of cephalosporin antibiotic ceftriaxone (CFT) with raw undiluted Ocimum sanctum L. leaf juice in chronic sta...
PMC10501326
core_pubmed_pmc
A Phase I Study of the Pan-Notch Inhibitor CB-103 for Patients with Advanced Adenoid Cystic Carcinoma and Other Tumors
A Phase I Study of the Pan-Notch Inhibitor CB-103 for Patients with Advanced Adenoid Cystic Carcinoma and Other Tumors Abstract Abstract Purpose: CB-103 selectively inhibits the CSL–NICD (Notch intracellular domain) interaction leading to transcriptional downregulation of oncogenic Notch pathway activation. This dose-e...
PMC10783034
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic evaluation of the atypical tetracyclines chelocardin and amidochelocardin in murine infection models
Pharmacokinetic and pharmacodynamic evaluation of the atypical tetracyclines chelocardin and amidochelocardin in murine infection models Abstract ABSTRACT The quest for novel anti-infectives against drug-resistant pathogens of the so-called ESKAPE panel is accompanied by intensive research aiming to find treatment opti...
PMC8761492
core_pubmed_pmc
Preclinical and randomized phase I studies of plitidepsin in adults hospitalized with COVID-19
Preclinical and randomized phase I studies of plitidepsin in adults hospitalized with COVID-19 Abstract This proof-of-concept study shows that plitidepsin, a marine peptide that inhibits SARS-CoV-2 replication, has a favorable safety profile and may be an efficacious treatment for patients with COVID-19. Abstract Pliti...
PMC8296590
core_pubmed_pmc
Evaluating risk detection methods to uncover ontogenic-mediated adverse drug effect mechanisms in children
Evaluating risk detection methods to uncover ontogenic-mediated adverse drug effect mechanisms in children Abstract Background Identifying adverse drugs effects (ADEs) in children, overall and within pediatric age groups, is essential for preventing disability and death from marketed drugs. At the same time, however, d...
PMC7221104
core_pubmed_pmc
Combining Isotopic Tracer Techniques to Increase Efficiency of Clinical Pharmacokinetic Trials in Oncology
Combining Isotopic Tracer Techniques to Increase Efficiency of Clinical Pharmacokinetic Trials in Oncology Abstract With increasing numbers of drugs tested in oncology for smaller patient populations, fewer patients are available to answer important clinical pharmacological questions in the timeframe of clinical drug d...
PMC8040281
core_pubmed_pmc
First-in-human study of the safety, pharmacokinetics, and pharmacodynamics of first-in-class fatty acid synthase inhibitor TVB-2640 alone and with a taxane in advanced tumors
First-in-human study of the safety, pharmacokinetics, and pharmacodynamics of first-in-class fatty acid synthase inhibitor TVB-2640 alone and with a taxane in advanced tumors Abstract Background We conducted a first-in-human dose-escalation study with the oral FASN inhibitor TVB-2640 to determine the maximum tolerated ...
PMC12771092
core_pubmed_pmc
Crovalimab Rescue Therapy in a Case With Genetic Complement Mediated Thrombotic Microangiopathy
Crovalimab Rescue Therapy in a Case With Genetic Complement Mediated Thrombotic Microangiopathy Abstract Complement mediated thrombotic microangiopathy (C-TMA) is a rare disease resulting in kidney failure and other organ manifestations. Current treatments include the complement C5 blockers eculizumab and ravulizumab a...
PMC8231986
core_pubmed_pmc
Changes in the Pharmacokinetics and Pharmacodynamics of Sildenafil in Cigarette and Cannabis Smokers
Changes in the Pharmacokinetics and Pharmacodynamics of Sildenafil in Cigarette and Cannabis Smokers Abstract Abstract Sildenafil citrate, a widely-used oral therapy for erectile dysfunction, is a cytochrome P3A4 (CYP3A4) enzyme substrate. Studies have reported that this substrate has an inhibitory effect on CYP3A4 enz...
PMC10354432
core_pubmed_pmc
Preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin
Preparation of caffeic acid grafted chitosan self-assembled micelles to enhance oral bioavailability and antibacterial activity of quercetin Abstract Quercetin (QR) is a naturally occurring flavonoid organic compound that has poor solubility in water and highly unstable in alkaline conditions, resulting in limited abso...
PMC4662814
core_pubmed_pmc
Single-dose pharmacokinetics of 2 or 3 tablets of biphasic immediate-release/extended-release hydrocodone bitartrate/acetaminophen (MNK-155) under fed and fasted conditions: two randomized open-label trials
Single-dose pharmacokinetics of 2 or 3 tablets of biphasic immediate-release/extended-release hydrocodone bitartrate/acetaminophen (MNK-155) under fed and fasted conditions: two randomized open-label trials Abstract Background Biphasic immediate-release (IR)/extended-release (ER) hydrocodone bitartrate (HB)/acetaminoph...
PMC12386734
core_pubmed_pmc
A Reassessment of Sarcopenia from a Redox Perspective as a Basis for Preventive and Therapeutic Interventions
A Reassessment of Sarcopenia from a Redox Perspective as a Basis for Preventive and Therapeutic Interventions Abstract The use of a wide variety of antioxidants has been advocated as a means to prevent, delay the progression of, or counteract the adverse consequences of sarcopenia, such as loss of muscle strength, musc...
PMC5869561
core_pubmed_pmc
Drugs Being Eliminated via the Same Pathway Will Not Always Require Similar Pediatric Dose Adjustments
Drugs Being Eliminated via the Same Pathway Will Not Always Require Similar Pediatric Dose Adjustments Abstract For scaling drug plasma clearance (CLp) from adults to children, extrapolations of population pharmacokinetic (PopPK) covariate models between drugs sharing an elimination pathway have enabled accelerated dev...
PMC8227048
core_pubmed_pmc
Application of Deep Neural Networks as a Prescreening Tool to Assign Individualized Absorption Models in Pharmacokinetic Analysis
Application of Deep Neural Networks as a Prescreening Tool to Assign Individualized Absorption Models in Pharmacokinetic Analysis Abstract A specific model for drug absorption is necessarily assumed in pharmacokinetic (PK) analyses following extravascular dosing. Unfortunately, an inappropriate absorption model may for...
PMC4509534
core_pubmed_pmc
Phase 1 safety, tolerability, and pharmacokinetic study of single ascending doses of XM17 (recombinant human follicle-stimulating hormone) in downregulated healthy women
Phase 1 safety, tolerability, and pharmacokinetic study of single ascending doses of XM17 (recombinant human follicle-stimulating hormone) in downregulated healthy women Abstract Background XM17 is a recombinant human follicle-stimulating hormone (follitropin alfa) for stimulation of multifollicular development in wome...
PMC3876094
core_pubmed_pmc
The Effects of H 2 S on the Activities of CYP2B6, CYP2D6, CYP3A4, CYP2C19 and CYP2C9 in Vivo in Rat
The Effects of H 2 S on the Activities of CYP2B6, CYP2D6, CYP3A4, CYP2C19 and CYP2C9 in Vivo in Rat Abstract Hydrogen sulfide (H 2 S) is a colorless, flammable, extremely hazardous gas with a “rotten egg” smell. The human body produces small amounts of H 2 S and uses it as a signaling molecule. The cocktail method was ...
PMC8389010
core_pubmed_pmc
Pharmacokinetic Behaviour of Enrofloxacin after Single Intramuscular Dosage in American Black Vultures ( Coragyps atratus )
Pharmacokinetic Behaviour of Enrofloxacin after Single Intramuscular Dosage in American Black Vultures ( Coragyps atratus ) Abstract The aim of the study was to investigate the intramuscular pharmacokinetics of enrofloxacin in black vultures ( Coragyps atratus ). The pharmacokinetics of a single intramuscular dose (10 ...
PMC12024831
core_pubmed_pmc
In Vitro–In Silico Approach in the Development of Clopidogrel Solid Dispersion Formulations
In Vitro–In Silico Approach in the Development of Clopidogrel Solid Dispersion Formulations Abstract Abstract The aim of this study was to investigate the influence of solid dispersion (SD) formulation factors on improvement of the bioavailability and pharmacokinetic profile of clopidogrel after peroral administration ...
PMC10793175
core_pubmed_pmc
Activity prediction, structure-based drug design, molecular docking, and pharmacokinetic studies of 1,4-dihydropyridines derivatives as α-amylase inhibitors
Activity prediction, structure-based drug design, molecular docking, and pharmacokinetic studies of 1,4-dihydropyridines derivatives as α-amylase inhibitors Abstract Objectives Diabetes places a substantial economic burden on countries worldwide. The costs associated with diabetes management, including healthcare servi...
PMC8837543
core_pubmed_pmc
Multiphysics Modelling and Simulation of Thrombolysis via Activated Platelet-Targeted Nanomedicine
Multiphysics Modelling and Simulation of Thrombolysis via Activated Platelet-Targeted Nanomedicine Abstract Abstract Purpose This study establishes a multiphysics simulation platform for both conventional and targeted thrombolysis using tissue plasminogen activator (tPA). Based on our computational results, the effects...
PMC10787407
core_pubmed_pmc
Regulation of polysaccharide in Wu‐tou decoction on intestinal microflora and pharmacokinetics of small molecular compounds in AIA rats
Regulation of polysaccharide in Wu‐tou decoction on intestinal microflora and pharmacokinetics of small molecular compounds in AIA rats Abstract Wu-tou decoction (WTD), a traditional Chinese medicine prescription, is used to treat rheumatoid arthritis (RA). It works by controlling intestinal flora and its metabolites, ...
PMC9077764
core_pubmed_pmc
Mechanism in the existent difference in form of wogonin/wogonoside between plasma and intestine/liver in rats
Mechanism in the existent difference in form of wogonin/wogonoside between plasma and intestine/liver in rats Abstract Wogonin (WO) and its glucuronide, wogonoside (WG) exhibit various beneficial bioactivities that may have potential for the development of novel drugs. In this study, we determined their pharmacokinetic...
PMC8227288
core_pubmed_pmc
Dalbavancin for the Treatment of Prosthetic Joint Infections: A Narrative Review
Dalbavancin for the Treatment of Prosthetic Joint Infections: A Narrative Review Abstract Dalbavancin (DAL) is a lipoglycopeptide with bactericidal activity against a very wide range of Gram-positive microorganisms. It also has unique pharmacokinetic properties, namely a prolonged half-life (around 181 h), which allows...
PMC8955068
core_pubmed_pmc
Lipid Nanocarriers Overlaid with Chitosan for Brain Delivery of Berberine via the Nasal Route
Lipid Nanocarriers Overlaid with Chitosan for Brain Delivery of Berberine via the Nasal Route Abstract Abstract This research aimed to design, optimize, and evaluate berberine-laden nanostructured lipid carriers overlaid with chitosan (BER-CTS-NLCs) for efficient brain delivery via the intranasal route. The nanostructu...
PMC5880182
core_pubmed_pmc
Antibody-modified liposomes for tumor-targeting delivery of timosaponin AIII
Antibody-modified liposomes for tumor-targeting delivery of timosaponin AIII Abstract Abstract Introduction Timosaponin AIII (TAIII), as a steroid saponin in Anemarrhena asphodeloides , has favorable potential as an antitumor candidate. However, its hydrophobicity and low bioavailability severely limit its in vivo anti...
PMC6505179
core_pubmed_pmc
Vedolizumab trough level monitoring in inflammatory bowel disease: a state-of-the-art overview
Vedolizumab trough level monitoring in inflammatory bowel disease: a state-of-the-art overview Abstract Abstract Background Therapeutic drug monitoring involves therapeutic modifications based on the measurement of drug levels and antidrug antibodies. The viability of therapeutic drug monitoring in vedolizumab-treated ...
PMC5021784
core_pubmed_pmc
Weekly paclitaxel therapy for gastric cancer in patients with renal dysfunction: A case report
Weekly paclitaxel therapy for gastric cancer in patients with renal dysfunction: A case report Abstract Abstract A 57-year-old woman was admitted to National Defense Medical College hospital for treatment of gastric cancer with pyloric stenosis. She had been diagnosed with chronic kidney disease (CKD) 10 years prior, b...
PMC8711013
core_pubmed_pmc
A Novel Eye Drop Formulation for Potential Treatment of Neovascular Age-Related Macular Degeneration
A Novel Eye Drop Formulation for Potential Treatment of Neovascular Age-Related Macular Degeneration Abstract Purpose Drug delivery to posterior ocular tissues via topical eye drop administration is arduous due to the unique anatomy and physiology of the eye. Therefore, treatments for posterior eye disease have to be a...
PMC9366781
core_pubmed_pmc
Toward the Development of GE11-Based Radioligands for Imaging of Epidermal Growth Factor Receptor-Positive Tumors
Toward the Development of GE11-Based Radioligands for Imaging of Epidermal Growth Factor Receptor-Positive Tumors Abstract The epidermal growth factor receptor (EGFR) is closely associated with tumor development and progression and thus an important target structure for imaging and therapy of various tumors. As a resul...
PMC10410045
core_pubmed_pmc
High daily caffeine intake is associated with lower propofol requirements for anesthetic induction
High daily caffeine intake is associated with lower propofol requirements for anesthetic induction Abstract Background and Aims: There is significant interindividual variation in the dose of propofol required for anesthetic induction. Factors dictating this are poorly described, but understanding them would be useful f...
PMC6376464
core_pubmed_pmc
A Synthetic Receptor as a Specific Antidote for Paraquat Poisoning
A Synthetic Receptor as a Specific Antidote for Paraquat Poisoning Abstract Abstract Accidental or suicidal ingestion of the world's most widely used herbicide, paraquat (PQ), may result in rapid multi-organ failure with a 60% fatality rate due to the absence of an effective detoxification solution. Effective, specific...
PMC8288812
core_pubmed_pmc
Targeting neurons in the gastrointestinal tract to treat Parkinson's disease ☆
Targeting neurons in the gastrointestinal tract to treat Parkinson's disease ☆ Abstract Background Parkinson's disease (PD) is associated with α-synuclein (αS) aggregation within the enteric nervous system (ENS) and constipation. Squalamine displaces proteins that are electrostatically bound to intracellular membranes ...
PMC9751427
core_pubmed_pmc
Transcriptome expression profile of compound-K-enriched red ginseng extract (DDK-401) in Korean volunteers and its apoptotic properties
Transcriptome expression profile of compound-K-enriched red ginseng extract (DDK-401) in Korean volunteers and its apoptotic properties Abstract Ginseng and ginsenosides have been reported to have various pharmacological effects, but their efficacies depend on intestinal absorption. Compound K (CK) is gaining prominenc...
PMC8400480
core_pubmed_pmc
Synthesis, Antibacterial and Pharmacokinetic Evaluation of Novel Derivatives of Harmine N 9 -Cinnamic Acid
Synthesis, Antibacterial and Pharmacokinetic Evaluation of Novel Derivatives of Harmine N 9 -Cinnamic Acid Abstract Abstract A series of 16 new derivatives of harmine N 9 -Cinnamic acid were synthesized and fully characterized using NMR and MS. The in vitro antibacterial evaluation revealed that most of the synthesized...
PMC7223046
core_pubmed_pmc
Selecting the dosage of ceftazidime–avibactam in the perfect storm of nosocomial pneumonia
Selecting the dosage of ceftazidime–avibactam in the perfect storm of nosocomial pneumonia Abstract Abstract Purpose Ceftazidime–avibactam is a novel β-lactam/β-lactamase inhibitor combination recently approved in Europe and the USA for the treatment of adults with hospital-acquired pneumonia (HAP) and ventilator-assoc...
PMC5599193
core_pubmed_pmc
A Phase Ib Dose‐Escalation Study of the Safety, Tolerability, and Pharmacokinetics of Cobimetinib and Duligotuzumab in Patients with Previously Treated Locally Advanced or Metastatic Cancers with Mutant KRAS
A Phase Ib Dose‐Escalation Study of the Safety, Tolerability, and Pharmacokinetics of Cobimetinib and Duligotuzumab in Patients with Previously Treated Locally Advanced or Metastatic Cancers with Mutant KRAS Abstract Abstract Lessons Learned. Cobimetinib and duligotuzumab were well tolerated as single agents and in com...
PMC11921369
core_pubmed_pmc
Advances in Chinese herbal medicine in modulating mitochondria to treat myocardial ischemia-reperfusion injury: a narrative review
Advances in Chinese herbal medicine in modulating mitochondria to treat myocardial ischemia-reperfusion injury: a narrative review Abstract Background and Objective The urgent need to identify pathways that can mitigate myocardial ischemia-reperfusion injury (MIRI) has become a central focus in cardiovascular treatment...
PMC8145937
core_pubmed_pmc
Population Pharmacokinetic Modelling and Simulation to Determine the Optimal Dose of Nanoparticulated Sorafenib to the Reference Sorafenib
Population Pharmacokinetic Modelling and Simulation to Determine the Optimal Dose of Nanoparticulated Sorafenib to the Reference Sorafenib Abstract Sorafenib, an oral multikinase inhibitor, exhibits a highly variable absorption profile due to enterohepatic reabsorption and poor solubility. SYO-1644 improved the solubil...
PMC6923548
core_pubmed_pmc
A Phase 1 Study of Intravenous Busulfan as a Conditioning Regimen for Multiple Myeloma
A Phase 1 Study of Intravenous Busulfan as a Conditioning Regimen for Multiple Myeloma Abstract Abstract The efficacy of melphalan (MEL) 140 mg/m 2 pre-transplant conditioning versus MEL 200 mg/m 2 for the elderly is still debated. We hypothesized that single-agent intravenous busulfan (BU) would show significant anti-...
PMC5479098
core_pubmed_pmc
High-dose zolpidem dependence - Psychostimulant effects? A case report and literature review
High-dose zolpidem dependence - Psychostimulant effects? A case report and literature review Abstract Abstract Zolpidem, an imidazoline nonbenzodiazepine sedative drug, is used widely. Initial reports showed minimal abuse potential. However, multiple reports have appeared of dose escalation and abuse. Subjective effect...
PMC11452328
core_pubmed_pmc
A first-in-human phase I study of a novel MDM2/p53 inhibitor alrizomadlin in advanced solid tumors
A first-in-human phase I study of a novel MDM2/p53 inhibitor alrizomadlin in advanced solid tumors Abstract Abstract Background The mouse double minute 2 homolog (MDM2) oncogene exerts oncogenic activities in many cancers and represents a potential therapeutic target. This trial evaluated the safety, pharmacokinetics, ...
PMC10572019
core_pubmed_pmc
Randomized Phase 2 Clinical Trial of Olaratumab in Combination with Gemcitabine and Docetaxel in Advanced Soft Tissue Sarcomas
Randomized Phase 2 Clinical Trial of Olaratumab in Combination with Gemcitabine and Docetaxel in Advanced Soft Tissue Sarcomas Abstract Simple Summary Soft tissue sarcomas (STSs) are rare and highly heterogeneous tumors that are difficult to treat. Gemcitabine plus docetaxel is an effective treatment for advanced STS. ...
PMC5107198
core_pubmed_pmc
Pharmacokinetics and Dosing of Ceftobiprole Medocaril for the Treatment of Hospital- and Community-Acquired Pneumonia in Different Patient Populations
Pharmacokinetics and Dosing of Ceftobiprole Medocaril for the Treatment of Hospital- and Community-Acquired Pneumonia in Different Patient Populations Abstract Abstract Hospital-acquired pneumonia (HAP) and community-acquired pneumonia (CAP) are among the most common infections treated in the hospital setting, and toge...
PMC11823603
core_pubmed_pmc
Fluoroquinolones and rifampin combination in the backdrop of heteroresistant tuberculosis
Fluoroquinolones and rifampin combination in the backdrop of heteroresistant tuberculosis Abstract ABSTRACT The impact of heteroresistance on tuberculosis (TB) treatment outcomes is unclear, as is the role of different rifampin and isoniazid exposures on developing resistance mutations. Hollow fiber system model of TB ...
PMC11533100
core_pubmed_pmc
Combining data on the bioavailability of midazolam and physiologically‐based pharmacokinetic modeling to investigate intestinal CYP3A4 ontogeny
Combining data on the bioavailability of midazolam and physiologically‐based pharmacokinetic modeling to investigate intestinal CYP3A4 ontogeny Abstract Abstract Pediatric physiologically‐based modeling in drug development has grown in the past decade and optimizing the underlying systems parameters is important in rel...
PMC9323266
core_pubmed_pmc
Competitive Metabolism of Polycyclic Aromatic Hydrocarbons (PAHs): An Assessment Using In Vitro Metabolism and Physiologically Based Pharmacokinetic (PBPK) Modeling
Competitive Metabolism of Polycyclic Aromatic Hydrocarbons (PAHs): An Assessment Using In Vitro Metabolism and Physiologically Based Pharmacokinetic (PBPK) Modeling Abstract Abstract Humans are routinely exposed to complex mixtures such as polycyclic aromatic hydrocarbons (PAHs) rather than to single compounds, as are ...
PMC7679072
core_pubmed_pmc
Physiologically‐Based Pharmacokinetic Modeling for the Prediction of a Drug–Drug Interaction of Combined Effects on P‐glycoprotein and Cytochrome P450 3A
Physiologically‐Based Pharmacokinetic Modeling for the Prediction of a Drug–Drug Interaction of Combined Effects on P‐glycoprotein and Cytochrome P450 3A Abstract Abstract Direct oral anticoagulants, such as apixaban and rivaroxaban, are important for the treatment and prophylaxis of venous thromboembolism and to reduc...
PMC8377765
core_pubmed_pmc
Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Represents an Oral Formulation of Resveratrol With Better Gastric Absorption and Bioavailability Respect to Pure Resveratrol
Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Represents an Oral Formulation of Resveratrol With Better Gastric Absorption and Bioavailability Respect to Pure Resveratrol Abstract Resveratrol attracts great interest because of the plethora of in vitro effects at the micromolar concentration range. Unfortuna...
PMC7241478
core_pubmed_pmc
Effects of puerarin on the pharmacokinetics of astragaloside IV in rats and its potential mechanism
Effects of puerarin on the pharmacokinetics of astragaloside IV in rats and its potential mechanism Abstract Abstract Context Puerarin and astragaloside IV (AS-IV) are sometimes used together for the treatment of disease in Chinese clinics, however, the drug–drug interaction between puerarin and AS-IV is still unknown....
PMC3326922
core_pubmed_pmc
Pharmacokinetic interaction of garlic and atorvastatin in dyslipidemic rats
Pharmacokinetic interaction of garlic and atorvastatin in dyslipidemic rats Abstract Objective: To assess pharmacokinetic interaction of garlic with atorvastatin in dyslipidemic rats. Materials and Methods: Sprague Dawley rats with induced dyslipidemia were divided into five groups of eight rats each. Group 1 was given...
PMC9574719
core_pubmed_pmc
Population pharmacokinetic analysis for tisotumab vedotin in patients with locally advanced and/or metastatic solid tumors
Population pharmacokinetic analysis for tisotumab vedotin in patients with locally advanced and/or metastatic solid tumors Abstract Abstract Tisotumab vedotin is an investigational antibody–drug conjugate (ADC) for treatment of solid tumors expressing tissue factor with accelerated approval from the US Food and Drug Ad...
PMC6130634
core_pubmed_pmc
Comparative pharmacokinetics of chlorogenic acid in beagles after oral administrations of single compound, the extracts of Lonicera japanica , and the mixture of chlorogenic acid, baicalin, and Forsythia suspense
Comparative pharmacokinetics of chlorogenic acid in beagles after oral administrations of single compound, the extracts of Lonicera japanica , and the mixture of chlorogenic acid, baicalin, and Forsythia suspense Abstract Abstract Context: Chlorogenic acid (ChA) is the major compound in Shuang-Huang-Lian (SHL), which i...
PMC6664239
core_pubmed_pmc
Method Validation for Simultaneous Quantification of Olmesartan and Hydrochlorothiazide in Human Plasma Using LC-MS/MS and Its Application Through Bioequivalence Study in Healthy Volunteers
Method Validation for Simultaneous Quantification of Olmesartan and Hydrochlorothiazide in Human Plasma Using LC-MS/MS and Its Application Through Bioequivalence Study in Healthy Volunteers Abstract Abstract A new, simple, sensitive, selective, rapid, and high-throughput liquid chromatography-tandem mass spectrometry (...
PMC3463610
core_pubmed_pmc
Chemical Analysis and Transplacental Transfer of Oseltamivir and Oseltamivir Carboxylic Acid in Pregnant Rats
Chemical Analysis and Transplacental Transfer of Oseltamivir and Oseltamivir Carboxylic Acid in Pregnant Rats Abstract In view of the limited information on the pharmacokinetics of oseltamivir (OSE) during pregnancy, this study aims to evaluate the placental transportation of OSE and its active metabolite oseltamivir c...
PMC10975973
core_pubmed_pmc
Comprehensive Review on Chiral Stationary Phases in Single-Column Simultaneous Chiral–Achiral HPLC Separation Methods
Comprehensive Review on Chiral Stationary Phases in Single-Column Simultaneous Chiral–Achiral HPLC Separation Methods Abstract This comprehensive review explores the utilization of chiral stationary phases (CSPs) in the context of single-column simultaneous chiral–achiral high-performance liquid chromatography (HPLC) s...
PMC6005007
core_pubmed_pmc
Construction of homogeneous antibody–drug conjugates using site-selective protein chemistry
Construction of homogeneous antibody–drug conjugates using site-selective protein chemistry Abstract The use of site-selective chemical drug-conjugation strategies enables the construction of antibody–drug conjugates (ADCs) with superior therapeutic efficacy.” Abstract Systemic chemotherapy, the current standard of car...
PMC8389554
core_pubmed_pmc
Differential Diagnosis and Treatment of Itching in Children and Adolescents
Differential Diagnosis and Treatment of Itching in Children and Adolescents Abstract Itching is prevalent in children with skin disorders and associated with effects on their mood, quality of life, and social functioning. Surprisingly, there are no data on childhood prevalence of pruritus in the general population. The...
PMC12588892
core_pubmed_pmc
Enhanced pharmacokinetic and therapeutic of GSH-responsive mPEG- b -P(HPMA)-SGI1776 conjugate for osteosarcoma
Enhanced pharmacokinetic and therapeutic of GSH-responsive mPEG- b -P(HPMA)-SGI1776 conjugate for osteosarcoma Abstract Abstract Introduction SGI-1776 represents the first serine/threonine kinase inhibitor to be utilized in the treatment of osteosarcoma. It is severely restricted by poor aqueous solubility, short degra...
PMC8420316
core_pubmed_pmc
Population pharmacokinetics of favipiravir in patients with COVID‐19
Population pharmacokinetics of favipiravir in patients with COVID‐19 Abstract Abstract The antiretroviral drug favipiravir (FPV) inhibits RNA‐dependent RNA polymerase. It has been developed for the treatment of the novel coronavirus (severe acute respiratory syndrome coronavirus 2) infection disease, coronavirus diseas...
PMC10963286
core_pubmed_pmc
Safety, pharmacokinetics, and pharmacodynamics of nomlabofusp (CTI‐1601) in Friedreich's ataxia
Safety, pharmacokinetics, and pharmacodynamics of nomlabofusp (CTI‐1601) in Friedreich's ataxia Abstract Abstract Objective Current treatments for Friedreich's ataxia, a neurodegenerative disorder characterized by decreased intramitochondrial frataxin, do not address low frataxin concentrations. Nomlabofusp (previously...
PMC10812518
core_pubmed_pmc
Comparative Pharmacokinetics and Bioequivalence of Pour-On Ivermectin Formulations in Korean Hanwoo Cattle
Comparative Pharmacokinetics and Bioequivalence of Pour-On Ivermectin Formulations in Korean Hanwoo Cattle Abstract Abstract This study aimed to conduct a bioequivalence study of applying three pour-on ivermectin formulations at a dose of 1 mg/kg on the back of Korean native beef cattle (Hanwoo). To conduct bioequivale...
PMC9665077
core_pubmed_pmc
Intra-articular injection PLGA blends sustained-release microspheres loaded with meloxicam: preparation, optimization, evaluation in vitro and in vivo
Intra-articular injection PLGA blends sustained-release microspheres loaded with meloxicam: preparation, optimization, evaluation in vitro and in vivo Abstract Abstract Meloxicam (MLX) is a commonly used drug in the clinical treatment of osteoarthritis, but it is associated with gastrointestinal adverse reactions. Ther...
PMC10220905
core_pubmed_pmc
GC/MS Profiling, Antibacterial, Anti-Quorum Sensing, and Antibiofilm Properties of Anethum graveolens L. Essential Oil: Molecular Docking Study and In-Silico ADME Profiling
GC/MS Profiling, Antibacterial, Anti-Quorum Sensing, and Antibiofilm Properties of Anethum graveolens L. Essential Oil: Molecular Docking Study and In-Silico ADME Profiling Abstract Abstract Anethum graveolens L. has been known as an aromatic, medicinal, and culinary herb since ancient times. The main purpose of this s...
PMC5339363
core_pubmed_pmc
A Phase Ib open label, randomized, safety study of SANGUINATE™ in patients with sickle cell anemia
A Phase Ib open label, randomized, safety study of SANGUINATE™ in patients with sickle cell anemia Abstract Abstract Background Treatment of sickle cell anemia is a challenging task and despite the well understood genetic and biochemical pathway of sickle hemoglobin, current therapy continues to be limited to the sympt...
PMC7608132
core_pubmed_pmc
Alflutinib (AST2818), primarily metabolized by CYP3A4, is a potent CYP3A4 inducer
Alflutinib (AST2818), primarily metabolized by CYP3A4, is a potent CYP3A4 inducer Abstract Abstract Alflutinib (AST2818) is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Previous study has shown that after multiple dosages, alflutin...
PMC5505051
core_pubmed_pmc
Vandetanib-eluting Radiopaque Beads: In vivo Pharmacokinetics, Safety and Toxicity Evaluation following Swine Liver Embolization
Vandetanib-eluting Radiopaque Beads: In vivo Pharmacokinetics, Safety and Toxicity Evaluation following Swine Liver Embolization Abstract PURPOSE: To evaluate the plasma and tissue pharmacokinetics, safety and toxicity following intra-arterial hepatic artery administration of Vandetanib (VTB)-eluting Radiopaque Beads (...
PMC5536290
core_pubmed_pmc
THPdb: Database of FDA-approved peptide and protein therapeutics
THPdb: Database of FDA-approved peptide and protein therapeutics Abstract Abstract THPdb ( http://crdd.osdd.net/raghava/thpdb/ ) is a manually curated repository of Food and Drug Administration (FDA) approved therapeutic peptides and proteins. The information in THPdb has been compiled from 985 research publications, 7...
PMC5526090
core_pubmed_pmc
Population Pharmacokinetic/Pharmacodynamic Modeling of Sunitinib by Dosing Schedule in Patients with Advanced Renal Cell Carcinoma or Gastrointestinal Stromal Tumor
Population Pharmacokinetic/Pharmacodynamic Modeling of Sunitinib by Dosing Schedule in Patients with Advanced Renal Cell Carcinoma or Gastrointestinal Stromal Tumor Abstract Abstract Background Sunitinib is a multi-targeted tyrosine kinase inhibitor used in the treatment of advanced renal cell carcinoma (RCC) and imati...
PMC9314132
core_pubmed_pmc
Physiological adaptations affecting drug pharmacokinetics in space: what do we really know? A critical review of the literature
Physiological adaptations affecting drug pharmacokinetics in space: what do we really know? A critical review of the literature Abstract Abstract As human spaceflight progresses with extended mission durations, the demand for effective and safe drugs will necessarily increase. To date, the accepted medications used dur...
PMC10651633
core_pubmed_pmc
Physiologically based absorption modeling to predict the bioequivalence of two cilostazol formulations
Physiologically based absorption modeling to predict the bioequivalence of two cilostazol formulations Abstract Abstract In vivo pharmacokinetic simulations and virtual bioequivalence (BE) evaluation of cilostazol have not yet been described for humans. Here, we successfully developed a physiologically based absorption...
PMC8793695
core_pubmed_pmc
Jatrorrhizine: A Review of Sources, Pharmacology, Pharmacokinetics and Toxicity
Jatrorrhizine: A Review of Sources, Pharmacology, Pharmacokinetics and Toxicity Abstract Jatrorrhizine, an isoquinoline alkaloid, is a bioactive metabolite in common medicinal plants, such as Berberis vernae Schneid., Tinospora sagittata (Oliv.) Gagnep. and Coptis chinensis Franch. These plants have been used for centu...
PMC12911231
core_pubmed_pmc
Troxipide nanosuspensions prevent indomethacin‑induced gastrointestinal lesions in adjuvant-induced arthritis rats
Troxipide nanosuspensions prevent indomethacin‑induced gastrointestinal lesions in adjuvant-induced arthritis rats Abstract Abstract Background Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for managing inflammatory disorders such as rheumatoid arthritis (RA); however, their long-term use is frequently...
PMC10407246
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of Single and Multiple Ascending Intravenous Infusions of PF-07304814 (Lufotrelvir) in Participants Hospitalized With COVID-19
Safety, Tolerability, and Pharmacokinetics of Single and Multiple Ascending Intravenous Infusions of PF-07304814 (Lufotrelvir) in Participants Hospitalized With COVID-19 Abstract Abstract Background An urgent need remains for antiviral therapies to treat patients hospitalized with COVID-19. PF-07304814—the prodrug (luf...
PMC9933240
core_pubmed_pmc
Formulation, Statistical Optimization, and In Vivo Pharmacodynamics of Cydonia oblonga Mucilage/Alginate Mucoadhesive Microspheres for the Delivery of Metformin HCl
Formulation, Statistical Optimization, and In Vivo Pharmacodynamics of Cydonia oblonga Mucilage/Alginate Mucoadhesive Microspheres for the Delivery of Metformin HCl Abstract In recent years, attention has shifted toward the utilization of natural polymers for encapsulation and sustained release of health-hazardous drug...
PMC11506926
core_pubmed_pmc
Predicting Food–Drug Interactions between Piperine and CYP3A4 Substrate Drugs Using PBPK Modeling
Predicting Food–Drug Interactions between Piperine and CYP3A4 Substrate Drugs Using PBPK Modeling Abstract Abstract Piperine has been reported to inhibit the enzyme activity of cytochrome P450 (CYP) 3A4. The aim of this study was to develop and validate a physiologically based pharmacokinetic (PBPK) model for piperine ...
PMC5756385
core_pubmed_pmc
Safety, tolerability and pharmacodynamics of apical sodium-dependent bile acid transporter inhibition with volixibat in healthy adults and patients with type 2 diabetes mellitus: a randomised placebo-controlled trial
Safety, tolerability and pharmacodynamics of apical sodium-dependent bile acid transporter inhibition with volixibat in healthy adults and patients with type 2 diabetes mellitus: a randomised placebo-controlled trial Abstract Background Pathogenesis in non-alcoholic steatohepatitis (NASH) involves abnormal cholesterol ...
PMC5760807
core_pubmed_pmc
Comparative pharmacokinetics of chlorogenic acid after oral administration in rats
Comparative pharmacokinetics of chlorogenic acid after oral administration in rats Abstract The present study was aimed at the comparison of the pharmacokinetics of pure chlorogenic acid and extract of Solanum lyratum Thunb. The animals were allocated to two groups, and were administered chlorogenic acid or extract of ...
PMC8213420
core_pubmed_pmc
Model‐based evaluation of image‐guided fractionated whole‐brain radiation therapy in pediatric diffuse intrinsic pontine glioma xenografts
Model‐based evaluation of image‐guided fractionated whole‐brain radiation therapy in pediatric diffuse intrinsic pontine glioma xenografts Abstract Abstract Radiation therapy (RT) is currently the standard treatment for diffuse intrinsic pontine glioma (DIPG), the most common cause of death in children with brain cance...
PMC11223837
core_pubmed_pmc
Deep-PK: deep learning for small molecule pharmacokinetic and toxicity prediction
Deep-PK: deep learning for small molecule pharmacokinetic and toxicity prediction Abstract Abstract Evaluating pharmacokinetic properties of small molecules is considered a key feature in most drug development and high-throughput screening processes. Generally, pharmacokinetics, which represent the fate of drugs in the...
PMC9780129
core_pubmed_pmc
Microdialysis of Voriconazole and its N -Oxide Metabolite: Amalgamating Knowledge of Distribution and Metabolism Processes in Humans
Microdialysis of Voriconazole and its N -Oxide Metabolite: Amalgamating Knowledge of Distribution and Metabolism Processes in Humans Abstract Purpose Voriconazole is an essential antifungal drug whose complex pharmacokinetics with high interindividual variability impedes effective and safe therapy. By application of th...
PMC9095539
core_pubmed_pmc
Population Pharmacokinetics of Abrocitinib in Healthy Individuals and Patients with Psoriasis or Atopic Dermatitis
Population Pharmacokinetics of Abrocitinib in Healthy Individuals and Patients with Psoriasis or Atopic Dermatitis Abstract Abstract Background and Objective Abrocitinib is a Janus kinase 1 inhibitor in development for the treatment of atopic dermatitis (AD). This work characterized orally administered abrocitinib popu...
PMC6712883
core_pubmed_pmc
ELQ-331 as a prototype for extremely durable chemoprotection against malaria
ELQ-331 as a prototype for extremely durable chemoprotection against malaria Abstract Background The potential benefits of long-acting injectable chemoprotection (LAI-C) against malaria have been recently recognized, prompting a call for suitable candidate drugs to help meet this need. On the basis of its known pharmac...
PMC12439004
core_pubmed_pmc
Exposure‐Response Relationships for Axatilimab in Patients with Chronic Graft‐Versus‐Host Disease
Exposure‐Response Relationships for Axatilimab in Patients with Chronic Graft‐Versus‐Host Disease Abstract Axatilimab, a high‐affinity humanized monoclonal antibody that targets colony‐stimulating factor 1 receptor, is approved for the treatment of chronic graft‐versus‐host disease (cGVHD). Here, we describe the exposu...
PMC8437615
core_pubmed_pmc
Phytochemistry and Pharmacology of Thymus broussonetii Boiss
Phytochemistry and Pharmacology of Thymus broussonetii Boiss Abstract Abstract Thymus broussonetii Boiss ( T. broussonetii ) is a rare medicinal and aromatic plant. It is widely used in traditional medicine to treat several diseases, including diarrhea, fever, cough, irritation, skin diseases, rheumatism, respiratory a...
PMC5373843
core_pubmed_pmc
Folic acid-functionalized drug delivery platform of resveratrol based on Pluronic 127/D-α-tocopheryl polyethylene glycol 1000 succinate mixed micelles
Folic acid-functionalized drug delivery platform of resveratrol based on Pluronic 127/D-α-tocopheryl polyethylene glycol 1000 succinate mixed micelles Abstract Abstract A folic acid (FA)-functionalized drug vehicle platform based on Pluronic 127 (P127)/D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) mixed mice...
PMC4723016
core_pubmed_pmc
Dose comparison of conivaptan (Vaprisol ® ) in patients with euvolemic or hypervolemic hyponatremia – efficacy, safety, and pharmacokinetics
Dose comparison of conivaptan (Vaprisol ® ) in patients with euvolemic or hypervolemic hyponatremia – efficacy, safety, and pharmacokinetics Abstract Abstract Purpose This study aimed to evaluate the efficacy, safety, and pharmacokinetics of 20 and 40 mg/day conivaptan (Vaprisol ® ) in patients with hypervolemic or euv...
PMC8553537
core_pubmed_pmc
Exploring Hidden Issues in the Use of Antipsychotic Polypharmacy in the Treatment of Schizophrenia
Exploring Hidden Issues in the Use of Antipsychotic Polypharmacy in the Treatment of Schizophrenia Abstract The mainstay of schizophrenia treatment is pharmacological therapy using various antipsychotics including first- and second-generation antipsychotics which have different pharmacokinetic and pharmacodynamic prope...
PMC5221453
core_pubmed_pmc
Amiselimod, a novel sphingosine 1‐phosphate receptor‐1 modulator, has potent therapeutic efficacy for autoimmune diseases, with low bradycardia risk
Amiselimod, a novel sphingosine 1‐phosphate receptor‐1 modulator, has potent therapeutic efficacy for autoimmune diseases, with low bradycardia risk Abstract Background and Purpose We conducted preclinical and clinical studies to examine the pharmacological, particularly cardiac, effects of amiselimod (MT‐1303), a seco...
PMC3534641
core_pubmed_pmc
Concentration-Dependent Inhibitory Effect of Baicalin on the Plasma Protein Binding and Metabolism of Chlorzoxazone, a CYP2E1 Probe Substrate, in Rats In Vitro and In Vivo
Concentration-Dependent Inhibitory Effect of Baicalin on the Plasma Protein Binding and Metabolism of Chlorzoxazone, a CYP2E1 Probe Substrate, in Rats In Vitro and In Vivo Abstract Some of the components found in herbs may be inhibitors or inducers of cytochrome P450 enzymes, which may therefore result in undesired her...
PMC11998577
core_pubmed_pmc
Impact of Switching to Long-Acting Injectable Cabotegravir Plus Rilpivirine on Rectal HIV-1 RNA Shedding and Implications for Transmission Risk
Impact of Switching to Long-Acting Injectable Cabotegravir Plus Rilpivirine on Rectal HIV-1 RNA Shedding and Implications for Transmission Risk Abstract Abstract Background The impact of long-acting injectable cabotegravir plus rilpivirine (CAB/RPV) on rectal human immunodeficiency virus 1 (HIV-1) RNA dynamics and the ...