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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 ... |
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