id
stringlengths
9
11
source
stringclasses
1 value
title
stringlengths
15
560
text
stringlengths
2k
153k
PMC9333411
core_pubmed_pmc
An Interactive Generic Physiologically Based Pharmacokinetic (igPBPK) Modeling Platform to Predict Drug Withdrawal Intervals in Cattle and Swine: A Case Study on Flunixin, Florfenicol, and Penicillin G
An Interactive Generic Physiologically Based Pharmacokinetic (igPBPK) Modeling Platform to Predict Drug Withdrawal Intervals in Cattle and Swine: A Case Study on Flunixin, Florfenicol, and Penicillin G Abstract Abstract Violative chemical residues in edible tissues from food-producing animals are of global public healt...
PMC5658281
core_pubmed_pmc
Population Exposure‐Response Modeling Supported Selection of Naloxegol Doses in Phase III Studies in Patients With Opioid‐Induced Constipation
Population Exposure‐Response Modeling Supported Selection of Naloxegol Doses in Phase III Studies in Patients With Opioid‐Induced Constipation Abstract Naloxegol is approved for the treatment of opioid‐induced constipation (OIC) in adults with chronic noncancer pain. Population exposure‐response models were developed u...
PMC9470115
core_pubmed_pmc
Comparative pharmacokinetics and urinary excretion of arsenic and mercury after oral administration of realgar, cinnabar and AnGongNiuHuang Pill to rats
Comparative pharmacokinetics and urinary excretion of arsenic and mercury after oral administration of realgar, cinnabar and AnGongNiuHuang Pill to rats Abstract Abstract Realgar- and cinnabar-containing AnGongNiuHuang Pill (AGNHP) is widely used for treating encephalopathy syndrome. However, it raises great safety con...
PMC10222359
core_pubmed_pmc
Alternative Analysis Approaches for the Assessment of Pilot Bioavailability/Bioequivalence Studies
Alternative Analysis Approaches for the Assessment of Pilot Bioavailability/Bioequivalence Studies Abstract Abstract Pilot bioavailability/bioequivalence (BA/BE) studies are usually conducted and analysed similarly to pivotal studies. Their analysis and interpretation of results usually rely on the application of the a...
PMC12817811
core_pubmed_pmc
Medication Adjustment After Bariatric and Metabolic Surgery: A Review of Current Evidence and Clinical Practice Trends
Medication Adjustment After Bariatric and Metabolic Surgery: A Review of Current Evidence and Clinical Practice Trends Abstract Abstract Bariatric and metabolic surgery (BMS) is the most effective treatment for severe obesity and its related comorbidities. Rapid metabolic improvement following surgery frequently leads ...
PMC8933053
core_pubmed_pmc
Pharmacokinetics and safety of inhaled ivermectin in mice as a potential COVID-19 treatment
Pharmacokinetics and safety of inhaled ivermectin in mice as a potential COVID-19 treatment Abstract Abstract Pharmacokinetic limitations associated with oral ivermectin may limit its success as a potential COVID-19 treatment based on in vitro experiments which demonstrate antiviral efficacy against SARS-CoV-2 at high ...
PMC7767747
core_pubmed_pmc
Nose-to-Brain Delivery by Nanosuspensions-Based in situ Gel for Breviscapine
Nose-to-Brain Delivery by Nanosuspensions-Based in situ Gel for Breviscapine Abstract Abstract Purpose Nose-to-brain drug delivery is an effective approach for poorly soluble drugs to bypass the blood–brain barrier. A new drug intranasal delivery system, a nanosuspension-based in situ gel, was developed and evaluated t...
PMC7449215
core_pubmed_pmc
Caspofungin Weight-Based Dosing Supported by a Population Pharmacokinetic Model in Critically Ill Patients
Caspofungin Weight-Based Dosing Supported by a Population Pharmacokinetic Model in Critically Ill Patients Abstract The objective of this study was to develop a population pharmacokinetic model and to determine a dosing regimen for caspofungin in critically ill patients. Nine blood samples were drawn per dosing occasio...
PMC12046403
core_pubmed_pmc
The synergistic effect of the combination of polymyxin B and rifampicin in a murine neutropenic thigh infection model with E. coli and K. pneumoniae
The synergistic effect of the combination of polymyxin B and rifampicin in a murine neutropenic thigh infection model with E. coli and K. pneumoniae Abstract Abstract Background Antibiotic combination therapy is increasingly used to treat MDR pathogens. In vitro studies suggest that the polymyxin B/rifampicin combinati...
PMC10587758
core_pubmed_pmc
Deep-sea fungal metabolites as potential inhibitors of glucose-regulatory enzymes: In silico structure–activity analysis
Deep-sea fungal metabolites as potential inhibitors of glucose-regulatory enzymes: In silico structure–activity analysis Abstract Chronic diabetes mellites related hyperglycemia is a major cause of mortality and morbidity due to further complications like retinopathy, hypertension and cardiovascular diseases. Though se...
PMC3888672
core_pubmed_pmc
Effect of Complexation with Arabinogalactan on Pharmacokinetics of “Guest” Drugs in Rats: For Example, Warfarin
Effect of Complexation with Arabinogalactan on Pharmacokinetics of “Guest” Drugs in Rats: For Example, Warfarin Abstract Abstract A pharmacokinetic study of the warfarin (WF) : arabinogalactan (AG) complex with the 1 : 10 mass ratio after its intragastric introduction to Wistar rats at a dose of 5 mg/kg (WF dose in the...
PMC11318128
core_pubmed_pmc
Antimicrobial and cytotoxic activities of flavonoid and phenolics extracted from Sepia pharaonis ink (Mollusca: Cephalopoda)
Antimicrobial and cytotoxic activities of flavonoid and phenolics extracted from Sepia pharaonis ink (Mollusca: Cephalopoda) Abstract Abstract Background Several studies have been reported previously on the bioactivities of different extracts of marine molluscs. Therefore, we decided to evaluate the cytotoxic and antim...
PMC7556174
core_pubmed_pmc
Method for evaluating the human bioequivalence of acarbose based on pharmacodynamic parameters
Method for evaluating the human bioequivalence of acarbose based on pharmacodynamic parameters Abstract Abstract Objective To explore a method for evaluating the bioequivalence of acarbose based on pharmacodynamic parameters using a single-dose, randomized-sequence, three-way crossover study of acarbose test (T) and re...
PMC5823406
core_pubmed_pmc
Vehicle development, pharmacokinetics and toxicity of the anti-invasive agent 4-fluoro-3’,4’,5’-trimethoxychalcone in rodents
Vehicle development, pharmacokinetics and toxicity of the anti-invasive agent 4-fluoro-3’,4’,5’-trimethoxychalcone in rodents Abstract Effective inhibitors of invasion and metastasis represent a serious unmet clinical need. We have recently identified 4-fluoro-3’,4’,5’-trimethoxychalcone or C16 as a potent anti-invasiv...
PMC9292719
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic bioequivalence of biosimilar MYL‐1601D with US and European insulin aspart in healthy volunteers: A randomized, double‐blind, crossover, euglycaemic glucose clamp study
Pharmacokinetic and pharmacodynamic bioequivalence of biosimilar MYL‐1601D with US and European insulin aspart in healthy volunteers: A randomized, double‐blind, crossover, euglycaemic glucose clamp study Abstract Abstract Aim To evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) bioequivalence (BE) of MYL‐1601...
PMC6314220
core_pubmed_pmc
An Intratumor Pharmacokinetic/Pharmacodynamic Model for the Hypoxia-Activated Prodrug Evofosfamide (TH-302): Monotherapy Activity is Not Dependent on a Bystander Effect 1 2
An Intratumor Pharmacokinetic/Pharmacodynamic Model for the Hypoxia-Activated Prodrug Evofosfamide (TH-302): Monotherapy Activity is Not Dependent on a Bystander Effect 1 2 Abstract Tumor hypoxia contributes to resistance to anticancer therapies. Hypoxia-activated prodrugs (HAPs) selectively target hypoxic cells and th...
PMC11821577
core_pubmed_pmc
Evaluating the antagonist effect of naltrexone implant via opioid challenge tests with escalating doses of hydromorphone injection in former heroin dependent patients
Evaluating the antagonist effect of naltrexone implant via opioid challenge tests with escalating doses of hydromorphone injection in former heroin dependent patients Abstract Abstract Opioid dependence is a serious, life-threatening condition with severe social impacts. Naltrexone (NTX) can weaken the effect of opioid...
PMC9761775
core_pubmed_pmc
YH29407 with anti-PD-1 ameliorates anti-tumor effects via increased T cell functionality and antigen presenting machinery in the tumor microenvironment
YH29407 with anti-PD-1 ameliorates anti-tumor effects via increased T cell functionality and antigen presenting machinery in the tumor microenvironment Abstract Among cancer cells, indoleamine 2, 3-dioxygenase1 (IDO1) activity has been implicated in improving the proliferation and growth of cancer cells and suppressing...
PMC7038265
core_pubmed_pmc
Model-Informed Drug Development, Pharmacokinetic/Pharmacodynamic Cutoff Value Determination, and Antibacterial Efficacy of Benapenem against Enterobacteriaceae
Model-Informed Drug Development, Pharmacokinetic/Pharmacodynamic Cutoff Value Determination, and Antibacterial Efficacy of Benapenem against Enterobacteriaceae Abstract Benapenem is a novel carbapenem. The objective of this study was to determine the pharmacokinetic (PK)/pharmacodynamic (PD) cutoff values and evaluate ...
PMC8157262
core_pubmed_pmc
Pharmacokinetic Drug Interaction between Tofacitinib and Voriconazole in Rats
Pharmacokinetic Drug Interaction between Tofacitinib and Voriconazole in Rats Abstract Fungal infections are prevalent in patients with immune diseases. Voriconazole, a triazole antifungal drug, inhibits the cytochromes CYP3A4 and CYP2C, and tofacitinib, a Janus kinase inhibitor for the treatment of rheumatoid arthriti...
PMC4980789
core_pubmed_pmc
DL-ADR: a novel deep learning model for classifying genomic variants into adverse drug reactions
DL-ADR: a novel deep learning model for classifying genomic variants into adverse drug reactions Abstract Abstract Background Genomic variations are associated with the metabolism and the occurrence of adverse reactions of many therapeutic agents. The polymorphisms on over 2000 locations of cytochrome P450 enzymes (CYP...
PMC3514394
core_pubmed_pmc
Daily administration of low molecular weight heparin increases Hepatocyte Growth Factor serum levels in gynaecological patients: pharmacokinetic parameters and clinical implications
Daily administration of low molecular weight heparin increases Hepatocyte Growth Factor serum levels in gynaecological patients: pharmacokinetic parameters and clinical implications Abstract Abstract Background Hepatocyte Growth Factor (HGF) enhances cytotoxicity of paclitaxel (PTX) and cisplatin (CDDP) in human ovaria...
PMC7305817
core_pubmed_pmc
A Systematic Review of Vancomycin Dosing in Patients with Hematologic Malignancies or Neutropenia
A Systematic Review of Vancomycin Dosing in Patients with Hematologic Malignancies or Neutropenia Abstract Objective To provide a comprehensive review of vancomycin dosing in patients with hematologic malignancies or neutropenia. Methods PubMed, Embase and the Cochrane Library were searched through April 2, 2020. Origi...
PMC11283669
core_pubmed_pmc
Computational Exploration of Berberis lycium Royle: A Hidden Treasure Trove for Antiviral Development
Computational Exploration of Berberis lycium Royle: A Hidden Treasure Trove for Antiviral Development Abstract Viral infections and associated illnesses account for approximately 3.5 million global fatalities and public health problems. Medicinal plants, with their wide therapeutic range and minimal side effects, have ...
PMC6406770
core_pubmed_pmc
A Personalized CYP2C19 Phenotype-Guided Dosing Regimen of Voriconazole Using a Population Pharmacokinetic Analysis
A Personalized CYP2C19 Phenotype-Guided Dosing Regimen of Voriconazole Using a Population Pharmacokinetic Analysis Abstract Abstract Highly variable and non-linear pharmacokinetics of voriconazole are mainly caused by CYP2C19 polymorphisms. This study aimed to develop a mechanistic population pharmacokinetic model incl...
PMC6063739
core_pubmed_pmc
Quantitative Systems Pharmacology Modeling of Acid Sphingomyelinase Deficiency and the Enzyme Replacement Therapy Olipudase Alfa Is an Innovative Tool for Linking Pathophysiology and Pharmacology
Quantitative Systems Pharmacology Modeling of Acid Sphingomyelinase Deficiency and the Enzyme Replacement Therapy Olipudase Alfa Is an Innovative Tool for Linking Pathophysiology and Pharmacology Abstract Abstract Acid sphingomyelinase deficiency (ASMD) is a rare lysosomal storage disorder with heterogeneous clinical m...
PMC5857122
core_pubmed_pmc
A randomised, double-blind, placebo-controlled phase 1 study of the safety, tolerability and pharmacodynamics of volixibat in overweight and obese but otherwise healthy adults: implications for treatment of non-alcoholic steatohepatitis
A randomised, double-blind, placebo-controlled phase 1 study of the safety, tolerability and pharmacodynamics of volixibat in overweight and obese but otherwise healthy adults: implications for treatment of non-alcoholic steatohepatitis Abstract Abstract Background Accumulation of toxic free cholesterol in hepatocytes ...
PMC12345971
core_pubmed_pmc
Substituted 1,4-naphthoquinones for potential anticancer therapeutics: In vitro cytotoxic effects and QSAR-guided design of new analogs
Substituted 1,4-naphthoquinones for potential anticancer therapeutics: In vitro cytotoxic effects and QSAR-guided design of new analogs Abstract Abstract 1,4-Naphthoquinone is a promising pharmacophore in drug discovery due to its unique redox reactive nature and wide-ranging bioactivities. Herein, a series of 1,4-naph...
PMC6175098
core_pubmed_pmc
Population Pharmacokinetic Analysis of Fluticasone Furoate/Umeclidinium/Vilanterol via a Single Inhaler in Patients with COPD
Population Pharmacokinetic Analysis of Fluticasone Furoate/Umeclidinium/Vilanterol via a Single Inhaler in Patients with COPD Abstract Abstract A population pharmacokinetic analysis was conducted from a subset of samples obtained from the Lung Function and Quality of Life Assessment in Chronic Obstructive Pulmonary Dis...
PMC8143347
core_pubmed_pmc
Metabolism and Interspecies Variation of IMMH-010, a Programmed Cell Death Ligand 1 Inhibitor Prodrug
Metabolism and Interspecies Variation of IMMH-010, a Programmed Cell Death Ligand 1 Inhibitor Prodrug Abstract Abstract IMMH-010 is an ester prodrug of YPD-29B, a potent programmed cell death ligand 1 (PD-L1) inhibitor. The metabolism of IMMH-010 was investigated and compared in various species. Four metabolites of IMM...
PMC11438061
core_pubmed_pmc
Addressing health equity for breastfeeding women: primaquine for Plasmodium vivax radical cure
Addressing health equity for breastfeeding women: primaquine for Plasmodium vivax radical cure Abstract Abstract Plasmodium vivax malaria remains a global health challenge, with approximately 6.9 million estimated cases in 2022. The parasite has a dormant liver stage, the hypnozoite, which reactivates to cause repeated...
PMC9211420
core_pubmed_pmc
Population Pharmacokinetics of Remdesivir and GS-441524 in Hospitalized COVID-19 Patients
Population Pharmacokinetics of Remdesivir and GS-441524 in Hospitalized COVID-19 Patients Abstract ABSTRACT The objective of this study was to describe the population pharmacokinetics of remdesivir and GS-441524 in hospitalized coronavirus disease 2019 (COVID-19) patients. A prospective observational pharmacokinetic st...
PMC4211262
core_pubmed_pmc
Model-Based Exposure–Response Analysis of Apixaban to Quantify Bleeding Risk in Special Populations of Subjects Undergoing Orthopedic Surgery
Model-Based Exposure–Response Analysis of Apixaban to Quantify Bleeding Risk in Special Populations of Subjects Undergoing Orthopedic Surgery Abstract Abstract Population pharmacokinetic (PK) and exposure–response analyses of apixaban were performed using data from phase I–III studies to predict bleeding risks for pati...
PMC6768889
core_pubmed_pmc
A drug–drug interaction study to assess the potential effect of acid-reducing agent, lansoprazole, on quizartinib pharmacokinetics
A drug–drug interaction study to assess the potential effect of acid-reducing agent, lansoprazole, on quizartinib pharmacokinetics Abstract Purpose Quizartinib, a potent, selective FMS-like tyrosine kinase 3 ( FLT3 ) inhibitor, is currently in phase 3 development for patients with FLT3 –internal tandem duplication-muta...
PMC5393287
core_pubmed_pmc
Pharmacokinetics of coadministration of levothyroxine sodium and alendronate sodium new effervescent formulation
Pharmacokinetics of coadministration of levothyroxine sodium and alendronate sodium new effervescent formulation Abstract Abstract Summary No clinically important pharmacokinetic interference of alendronate occurred between a new effervescent formulation of alendronate and levothyroxine when coadministered. The combina...
PMC9369325
core_pubmed_pmc
MATE1 Deficiency Exacerbates Dofetilide-Induced Proarrhythmia
MATE1 Deficiency Exacerbates Dofetilide-Induced Proarrhythmia Abstract Abstract Dofetilide is a rapid delayed rectifier potassium current inhibitor widely used to prevent the recurrence of atrial fibrillation and flutter. The clinical use of this drug is associated with increases in QTc interval, which predispose patie...
PMC4993938
core_pubmed_pmc
Comparative Pharmacokinetics and Bioavailability of Epimedin C in Rat after Intramuscular Administration of Epimedin C, a Combination of Four Flavonoid Glycosides and Purified Herba Epimedii Extract
Comparative Pharmacokinetics and Bioavailability of Epimedin C in Rat after Intramuscular Administration of Epimedin C, a Combination of Four Flavonoid Glycosides and Purified Herba Epimedii Extract Abstract Abstract Chuan-Ke-Zhi (CKZ), a purified Herba Epimedii extract, is a potent Chinese medicine preparation whose m...
PMC3072355
core_pubmed_pmc
A phase I trial to evaluate the safety and pharmacokinetics of low-dose methotrexate as an anti-malarial drug in Kenyan adult healthy volunteers
A phase I trial to evaluate the safety and pharmacokinetics of low-dose methotrexate as an anti-malarial drug in Kenyan adult healthy volunteers Abstract Background Previous investigations indicate that methotrexate, an old anticancer drug, could be used at low doses to treat malaria. A phase I evaluation was conducted...
PMC9338108
core_pubmed_pmc
Pharmacokinetic Drug–Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer
Pharmacokinetic Drug–Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer Abstract Abstract Background and Objective Trilaciclib is a cyclin-dependent kinase 4/6 inhibitor indicated to ...
PMC8279894
core_pubmed_pmc
Improved Speech Intelligibility in Subjects With Stable Sensorineural Hearing Loss Following Intratympanic Dosing of FX-322 in a Phase 1b Study
Improved Speech Intelligibility in Subjects With Stable Sensorineural Hearing Loss Following Intratympanic Dosing of FX-322 in a Phase 1b Study Abstract Objectives: There are no approved pharmacologic therapies for chronic sensorineural hearing loss (SNHL). The combination of CHIR99021+valproic acid (CV, FX-322) has be...
PMC8047719
core_pubmed_pmc
Time course of efficacy of ubrogepant for the acute treatment of migraine: Clinical implications
Time course of efficacy of ubrogepant for the acute treatment of migraine: Clinical implications Abstract Background The full utility of an acute treatment requires examination of the entire time course of effect during a migraine attack. Here the time course of effect of ubrogepant is evaluated. Methods ACHIEVE-I and ...
PMC10232980
core_pubmed_pmc
Infant exposure to Fluvoxamine through placenta and human milk: a case series - A contribution from the ConcePTION project
Infant exposure to Fluvoxamine through placenta and human milk: a case series - A contribution from the ConcePTION project Abstract Abstract Introduction Fluvoxamine is widely used to treat depression during pregnancy and lactation. However, limited data are available on its transfer to the fetus or in human milk. This...
PMC9963644
core_pubmed_pmc
Influence of Age and Sex on the Pharmacokinetics of Midazolam and the Depth of Sedation in Pediatric Patients Undergoing Minor Surgeries
Influence of Age and Sex on the Pharmacokinetics of Midazolam and the Depth of Sedation in Pediatric Patients Undergoing Minor Surgeries Abstract Whether age and sex influence the depth of sedation and the pharmacokinetics of midazolam is currently unknown. The influence of age and sex was investigated in 117 children ...
PMC12256699
core_pubmed_pmc
Advances in the Clinical Use of Clopidogrel: A Review of Individualized Treatment Strategies and Monitoring Optimization Based on Genetic Polymorphisms
Advances in the Clinical Use of Clopidogrel: A Review of Individualized Treatment Strategies and Monitoring Optimization Based on Genetic Polymorphisms Abstract Abstract This paper systematically reviews recent advances in clopidogrel clinical applications to optimize therapeutic precision and medication safety. Using ...
PMC11225994
core_pubmed_pmc
Pharmacokinetic Interactions Between the Fixed-Dose Combination of Ezetimibe/Rosuvastatin 10/20 Mg and the Fixed-Dose Combination of Telmisartan/Amlodipine 80/5 Mg in Healthy Subjects
Pharmacokinetic Interactions Between the Fixed-Dose Combination of Ezetimibe/Rosuvastatin 10/20 Mg and the Fixed-Dose Combination of Telmisartan/Amlodipine 80/5 Mg in Healthy Subjects Abstract Background Management of hypertension and hyperlipidemia, which are common comorbid risk factors for cardiovascular diseases, r...
PMC4449367
core_pubmed_pmc
Comparison of the Safety, Tolerability, and Pharmacokinetics of Fidaxomicin in Healthy Japanese and Caucasian Subjects
Comparison of the Safety, Tolerability, and Pharmacokinetics of Fidaxomicin in Healthy Japanese and Caucasian Subjects Abstract Background and Objectives Fidaxomicin treatment of Clostridium difficile infection is known to produce minimal systemic exposure, as the antibacterial (antibiotic) remains primarily in the gut...
PMC5563343
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of Pazopanib: Towards Optimized Dosing
Clinical Pharmacokinetics and Pharmacodynamics of Pazopanib: Towards Optimized Dosing Abstract Abstract Pazopanib is an inhibitor of the vascular endothelial growth factor receptor, platelet-derived growth factor receptor, fibroblast growth factor receptor and stem cell receptor c-Kit, and has been approved for the tre...
PMC8757813
core_pubmed_pmc
The Development of an ex vivo Flow System to Assess Acute Arterial Drug Retention of Cardiovascular Intravascular Devices
The Development of an ex vivo Flow System to Assess Acute Arterial Drug Retention of Cardiovascular Intravascular Devices Abstract Abstract Purpose: The goal of this study was to develop an ex vivo system capable of rapidly evaluating arterial drug levels in living, isolated porcine carotid arteries. Methods: A vascula...
PMC7182630
core_pubmed_pmc
Oral Azacitidine and Cedazuridine Approximate Parenteral Azacitidine Efficacy in Murine Model
Oral Azacitidine and Cedazuridine Approximate Parenteral Azacitidine Efficacy in Murine Model Abstract Abstract Background DNA methyltransferase inhibitors (DNMTis) improve survival for patients with myelodysplastic syndromes (MDS) and those with acute myeloid leukemia (AML) unable to receive standard cytotoxic chemoth...
PMC10314621
core_pubmed_pmc
Study design and rationale of EXPLORER-CN: a phase III, randomised, double-blind, placebo-controlled clinical study to evaluate the efficacy and safety of mavacamten in Chinese adults with symptomatic obstructive hypertrophic cardiomyopathy
Study design and rationale of EXPLORER-CN: a phase III, randomised, double-blind, placebo-controlled clinical study to evaluate the efficacy and safety of mavacamten in Chinese adults with symptomatic obstructive hypertrophic cardiomyopathy Abstract Abstract Introduction Hypertrophic cardiomyopathy (HCM) is a primary m...
PMC9889419
core_pubmed_pmc
KM-408, a novel phenoxyalkyl derivative as a potential anticonvulsant and analgesic compound for the treatment of neuropathic pain
KM-408, a novel phenoxyalkyl derivative as a potential anticonvulsant and analgesic compound for the treatment of neuropathic pain Abstract Background Epilepsy frequently coexists with neuropathic pain. Our approach is based on the search for active compounds with multitarget profiles beneficial in terms of potential s...
PMC7789169
core_pubmed_pmc
Fluralaner as a novel treatment for sarcoptic mange in the bare-nosed wombat ( Vombatus ursinus ): safety, pharmacokinetics, efficacy and practicable use
Fluralaner as a novel treatment for sarcoptic mange in the bare-nosed wombat ( Vombatus ursinus ): safety, pharmacokinetics, efficacy and practicable use Abstract Abstract Background Sarcoptic mange causes significant animal welfare and occasional conservation concerns for bare-nosed wombats ( Vombatus ursinus ) throug...
PMC4396834
core_pubmed_pmc
Differences in pharmacokinetics of apple polyphenols after standardized oral consumption of unprocessed apple juice
Differences in pharmacokinetics of apple polyphenols after standardized oral consumption of unprocessed apple juice Abstract Background Polyphenols are chemical compounds of the secondary plant metabolism. High concentrations can be found in various fruits including apples, berries and grapes. Polyphenols are associate...
PMC10030671
core_pubmed_pmc
First-in-human phase I study of the OX40 agonist GSK3174998 with or without pembrolizumab in patients with selected advanced solid tumors (ENGAGE-1)
First-in-human phase I study of the OX40 agonist GSK3174998 with or without pembrolizumab in patients with selected advanced solid tumors (ENGAGE-1) Abstract Background The phase I first-in-human study ENGAGE-1 evaluated the humanized IgG1 OX40 agonistic monoclonal antibody GSK3174998 alone (Part 1 (P1)) or in combinat...
PMC4827904
core_pubmed_pmc
Pharmacogenetics in type 2 diabetes: influence on response to oral hypoglycemic agents
Pharmacogenetics in type 2 diabetes: influence on response to oral hypoglycemic agents Abstract Abstract Type 2 diabetes is one of the leading causes of morbidity and mortality, consuming a significant proportion of public health spending. Oral hypoglycemic agents (OHAs) are the frontline treatment approaches after lif...
PMC6981165
core_pubmed_pmc
Comparison of short-acting versus extended-release nifedipine: Effects on hemodynamics and sympathetic activity in patients with stable coronary artery disease
Comparison of short-acting versus extended-release nifedipine: Effects on hemodynamics and sympathetic activity in patients with stable coronary artery disease Abstract We investigated the impact of short-acting and extended release nifedipine on sympathetic activity using radiotracer methodology in patients with stabl...
PMC7719377
core_pubmed_pmc
Evaluation of the Effect of Maribavir on Cardiac Repolarization in Healthy Participants: Thorough QT/QTc Study
Evaluation of the Effect of Maribavir on Cardiac Repolarization in Healthy Participants: Thorough QT/QTc Study Abstract Maribavir is an orally bioavailable benzimidazole riboside in clinical development for treatment of cytomegalovirus infection in patients who undergo transplantation. Maribavir was evaluated in a thor...
PMC10995192
core_pubmed_pmc
VISTA checkpoint inhibition by pH-selective antibody SNS-101 with optimized safety and pharmacokinetic profiles enhances PD-1 response
VISTA checkpoint inhibition by pH-selective antibody SNS-101 with optimized safety and pharmacokinetic profiles enhances PD-1 response Abstract Abstract VISTA, an inhibitory myeloid-T-cell checkpoint, holds promise as a target for cancer immunotherapy. However, its effective targeting has been impeded by issues such as...
PMC7924008
core_pubmed_pmc
Pharmacodynamic Drug–Drug Interaction on Human Peripheral Blood Mononuclear Cells Between Everolimus and Tacrolimus at the Therapeutic Concentration Range in Renal Transplantation
Pharmacodynamic Drug–Drug Interaction on Human Peripheral Blood Mononuclear Cells Between Everolimus and Tacrolimus at the Therapeutic Concentration Range in Renal Transplantation Abstract Abstract Background Everolimus (EVL) plus tacrolimus (TAC) therapy is effective and safe in renal transplantation. However, the pha...
PMC8160673
core_pubmed_pmc
The Influence of Pharmacogenetics on the Clinical Relevance of Pharmacokinetic Drug–Drug Interactions: Drug–Gene, Drug–Gene–Gene and Drug–Drug–Gene Interactions
The Influence of Pharmacogenetics on the Clinical Relevance of Pharmacokinetic Drug–Drug Interactions: Drug–Gene, Drug–Gene–Gene and Drug–Drug–Gene Interactions Abstract Abstract Drug interactions are a well-known cause of adverse drug events, and drug interaction databases can help the clinician to recognize and avoid...
PMC7162492
core_pubmed_pmc
Pharmacological and pharmacokinetic profile of the novel ocular hypotensive prodrug CKLP1 in Dutch-belted pigmented rabbits
Pharmacological and pharmacokinetic profile of the novel ocular hypotensive prodrug CKLP1 in Dutch-belted pigmented rabbits Abstract Elevated intraocular pressure is the only treatable risk factor for glaucoma, an eye disease that is the leading cause of irreversible blindness worldwide. We have identified cromakalim p...
PMC7551666
core_pubmed_pmc
Prediction of Clearance of Monoclonal and Polyclonal Antibodies and Non-Antibody Proteins in Children: Application of Allometric Scaling
Prediction of Clearance of Monoclonal and Polyclonal Antibodies and Non-Antibody Proteins in Children: Application of Allometric Scaling Abstract Abstract Allometric scaling can be used for the extrapolation of pharmacokinetic parameters from adults to children. The objective of this study was to predict clearance of t...
PMC10359069
core_pubmed_pmc
Pharmacokinetics of acetaminophen after a single Oral administration of 20 or 40 mg/kg to 7–9 Day-old foals
Pharmacokinetics of acetaminophen after a single Oral administration of 20 or 40 mg/kg to 7–9 Day-old foals Abstract Abstract Background Acetaminophen is utilized in human infants for pain management and fever. Neonatal foals might benefit from administration of acetaminophen but effective and safe dosage regimens for ...
PMC11876737
core_pubmed_pmc
Side-by-Side Comparison of the In Vivo Performance of [ 212 Pb]Pb-DOTAMTATE and Other SSTR2-Targeting Compounds
Side-by-Side Comparison of the In Vivo Performance of [ 212 Pb]Pb-DOTAMTATE and Other SSTR2-Targeting Compounds Abstract There are numerous versions of octreotide and octreotate, including DOTAMTATE, DOTATATE, JR11, and lead-specific chelator (PSC)-PEG2-TOC. These peptides, which can be either analogs or antagonists, a...
PMC9469207
core_pubmed_pmc
Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction
Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction Abstract Abstract Myeloperoxidase is a promising therapeutic target for treatment of patients suffering from heart failure with preserved ejection fraction (HFpE...
PMC12817137
core_pubmed_pmc
In Vitro Evaluation and Network Pharmacology Analysis of the Antimicrobial Activity of Pistacia lentiscus
In Vitro Evaluation and Network Pharmacology Analysis of the Antimicrobial Activity of Pistacia lentiscus Abstract Background Chios mastic gum, a natural resin derived from the mastic tree, has a history of traditional use for its beneficial effects on the gastrointestinal system, its anti‐inflammatory properties, and ...
PMC9784597
core_pubmed_pmc
Cross-Species Translation of Biophase Half-Life and Potency of GalNAc-Conjugated siRNAs
Cross-Species Translation of Biophase Half-Life and Potency of GalNAc-Conjugated siRNAs Abstract Abstract Small interfering RNAs (siRNAs) with N -acetylgalactosamine (GalNAc) conjugation for improved liver uptake represent an emerging class of drugs to treat liver diseases. Understanding how pharmacokinetics and pharma...
PMC7789515
core_pubmed_pmc
Predicting chemosensitivity using drug perturbed gene dynamics
Predicting chemosensitivity using drug perturbed gene dynamics Abstract Abstract Background One of the current directions of precision medicine is the use of computational methods to aid in the diagnosis, prognosis, and treatment of disease based on data driven approaches. For instance, in oncology, there has been a pa...
PMC11775835
core_pubmed_pmc
Pharmacokinetics of 7,8-dihydroxyflavone in neonatal mice with hypoxia-ischemia related brain injury
Pharmacokinetics of 7,8-dihydroxyflavone in neonatal mice with hypoxia-ischemia related brain injury Abstract Abstract Introduction 7,8-Dihydroxyflavone (7,8-DHF) is a promising translational therapy in several brain injury models, including the neonatal hypoxia-ischemia (HI) model in mice. However, the neuroprotective...
PMC12610367
core_pubmed_pmc
Andrographolide and Its Derivatives: A Comprehensive Review of Anti-Infective Properties and Clinical Potential
Andrographolide and Its Derivatives: A Comprehensive Review of Anti-Infective Properties and Clinical Potential Abstract Andrographis paniculata , a medicinal plant widely found in Asia, contains andrographolide as its main active compound, known for its wide-ranging pharmacological effects, including anti-inflammatory...
PMC12655659
core_pubmed_pmc
Population Pharmacokinetics of Radotinib in Healthy Volunteers and Patients with Chronic Myeloid Leukemia
Population Pharmacokinetics of Radotinib in Healthy Volunteers and Patients with Chronic Myeloid Leukemia Abstract Background/Objectives : Radotinib is a second-generation tyrosine kinase inhibitor (TKI) that has been used for treatment of chronic myeloid leukemia (CML). This study was performed for the first time to c...
PMC4151581
core_pubmed_pmc
Pharmacokinetics and Biodistribution of Zinc-Enriched Yeast in Rats
Pharmacokinetics and Biodistribution of Zinc-Enriched Yeast in Rats Abstract Zinc-enriched yeast (ZnY) and zinc sulfate (ZnSO 4 ) are considered zinc (Zn) supplements currently available. The purpose of the investigation was to compare and evaluate pharmacokinetics and biodistribution of ZnY and ZnSO 4 in rats. ZnY or ...
PMC5993131
core_pubmed_pmc
Safety and efficacy of obinutuzumab in Chinese patients with B-cell lymphomas: a secondary analysis of the GERSHWIN trial
Safety and efficacy of obinutuzumab in Chinese patients with B-cell lymphomas: a secondary analysis of the GERSHWIN trial Abstract Abstract Background Patients with relapsed/refractory B-cell lymphomas have limited treatment options. GERSHWIN is an open-label, single-arm, phase Ib study of obinutuzumab monotherapy in C...
PMC4594707
core_pubmed_pmc
Evaluation of the QT effect of a combination of piperaquine and a novel anti‐malarial drug candidate OZ439, for the treatment of uncomplicated malaria
Evaluation of the QT effect of a combination of piperaquine and a novel anti‐malarial drug candidate OZ439, for the treatment of uncomplicated malaria Abstract Abstract Aims The aim was to investigate the QT effect of a single dose combination regimen of piperaquine phosphate (PQP) and a novel aromatic trioxolane, OZ43...
PMC11266319
core_pubmed_pmc
Characterizing Day 1 Area Under the Curve Following Vancomycin Loading Dose Administration in Adult Hospitalized Patients Using Non-Trapezoidal Linear Pharmacokinetic Equations: A Retrospective Observational Study
Characterizing Day 1 Area Under the Curve Following Vancomycin Loading Dose Administration in Adult Hospitalized Patients Using Non-Trapezoidal Linear Pharmacokinetic Equations: A Retrospective Observational Study Abstract Abstract Introduction Methicillin-resistant Staphylococcus aureus (MRSA) infections are a serious...
PMC5856892
core_pubmed_pmc
Explaining Ethnic Variability of Transporter Substrate Pharmacokinetics in Healthy Asian and Caucasian Subjects with Allele Frequencies of OATP1B1 and BCRP: A Mechanistic Modeling Analysis
Explaining Ethnic Variability of Transporter Substrate Pharmacokinetics in Healthy Asian and Caucasian Subjects with Allele Frequencies of OATP1B1 and BCRP: A Mechanistic Modeling Analysis Abstract Abstract Background Ethnic variability in the pharmacokinetics of organic anion transporting polypeptide (OATP) 1B1 substr...
PMC5594082
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Lisdexamfetamine Compared with D -Amphetamine in Healthy Subjects
Pharmacokinetics and Pharmacodynamics of Lisdexamfetamine Compared with D -Amphetamine in Healthy Subjects Abstract Rationale: Lisdexamfetamine is a prodrug of D -amphetamine used for the treatment of attention-deficit/hyperactivity disorder (ADHD). Lisdexamfetamine is thought to have a prolonged pharmacokinetic profil...
PMC12196235
core_pubmed_pmc
Enhancing the Pharmacological Properties of Triterpenes Through Acetylation: An Anticancer and Antioxidant Perspective
Enhancing the Pharmacological Properties of Triterpenes Through Acetylation: An Anticancer and Antioxidant Perspective Abstract Abstract This paper presents the influence of acetylation on the cytotoxic and antioxidant activity of natural triterpenes. Oleanolic acid, betulin, betulinic acid and other triterpenes have b...
PMC6524731
core_pubmed_pmc
Quantitative Mechanistic Modeling in Support of Pharmacological Therapeutics Development in Immuno-Oncology
Quantitative Mechanistic Modeling in Support of Pharmacological Therapeutics Development in Immuno-Oncology Abstract Abstract Following the approval, in recent years, of the first immune checkpoint inhibitor, there has been an explosion in the development of immuno-modulating pharmacological modalities for the treatmen...
PMC6989256
core_pubmed_pmc
Pharmacokinetics comparison of solifenacin tartrate and solifenacin succinate: a randomized, open-label, single-dose, 2-way crossover study in healthy male volunteers
Pharmacokinetics comparison of solifenacin tartrate and solifenacin succinate: a randomized, open-label, single-dose, 2-way crossover study in healthy male volunteers Abstract Abstract Solifenacin is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms. Solifenacin tartrate is a newly...
PMC10362213
core_pubmed_pmc
Phosphodiesterase-5 Inhibitors as Therapeutics for Cardiovascular Diseases: A Brief Review
Phosphodiesterase-5 Inhibitors as Therapeutics for Cardiovascular Diseases: A Brief Review Abstract Abstract Background: Three selective and most used inhibitors of PDE-5-sildenafil, vardenafil and tadalafil- have been successfully used for the treatment of erectile dysfunction. Erectile dysfunction and cardiovascular ...
PMC12802986
core_pubmed_pmc
OPERA-01: a phase III study of palazestrant for ER+, HER2– advanced breast cancer after CDK4/6 inhibitor therapy
OPERA-01: a phase III study of palazestrant for ER+, HER2– advanced breast cancer after CDK4/6 inhibitor therapy Abstract ABSTRACT Endocrine therapy (ET) resistance is a major concern when treating estrogen receptor-positive (ER+) human epidermal growth factor receptor 2-negative (HER2–) breast cancer. A combination of...
PMC4087670
core_pubmed_pmc
Herbal medicines in Brazil: pharmacokinetic profile and potential herb-drug interactions
Herbal medicines in Brazil: pharmacokinetic profile and potential herb-drug interactions Abstract A plethora of active compounds found in herbal medicines can serve as substrate for enzymes involved in the metabolism of xenobiotics. When a medicinal plant is co-administered with a conventional drug and little or no inf...
PMC5642013
core_pubmed_pmc
Pharmacokinetics and toxicity of subcutaneous administration of carboplatin in poloxamer 407 in a rodent model pilot study
Pharmacokinetics and toxicity of subcutaneous administration of carboplatin in poloxamer 407 in a rodent model pilot study Abstract The objectives of this study were to assess the pharmacokinetics and safety of subcutaneously delivered carboplatin in poloxamer 407 in rats. Carboplatin (5mg/rat) in 0.5ml poloxamer 407 (...
PMC7306617
core_pubmed_pmc
A Physiologically‐Based Quantitative Systems Pharmacology Model of the Incretin Hormones GLP‐1 and GIP and the DPP4 Inhibitor Sitagliptin
A Physiologically‐Based Quantitative Systems Pharmacology Model of the Incretin Hormones GLP‐1 and GIP and the DPP4 Inhibitor Sitagliptin Abstract Abstract Incretin hormones glucagon‐like peptide‐1 (GLP‐1) and glucose‐dependent insulinotropic polypeptide (GIP) play a major role in regulation of postprandial glucose and...
PMC11801451
core_pubmed_pmc
Effects of Subanesthetic Oromucosal Dexmedetomidine on Sleep in Humans: A Randomized, Controlled Pharmacokinetics–Pharmacodynamics Study
Effects of Subanesthetic Oromucosal Dexmedetomidine on Sleep in Humans: A Randomized, Controlled Pharmacokinetics–Pharmacodynamics Study Abstract Background: The locus coeruleus noradrenergic system may provide a potential new target for pharmacologic insomnia treatment, particularly in patients suffering from elevated...
PMC7504705
core_pubmed_pmc
CDK4/6 Inhibitors in Breast Cancer Treatment: Potential Interactions with Drug, Gene, and Pathophysiological Conditions
CDK4/6 Inhibitors in Breast Cancer Treatment: Potential Interactions with Drug, Gene, and Pathophysiological Conditions Abstract Palbociclib, ribociclib, and abemaciclib belong to the third generation of cyclin-dependent kinases inhibitors (CDKis), an established therapeutic class for advanced and metastatic breast can...
PMC12947848
core_pubmed_pmc
Population Pharmacokinetic Modeling and Target Attainment of Cefepime in Critically Ill Pediatric Patients
Population Pharmacokinetic Modeling and Target Attainment of Cefepime in Critically Ill Pediatric Patients Abstract Abstract Background Cefepime dosing guidelines are well defined in healthy populations but have not been studied extensively in critically ill children who often have significant alterations in antibiotic...
PMC6704343
core_pubmed_pmc
A Phase I, Randomized, Single-Dose Study Evaluating the Biosimilarity of TAB008 to Bevacizumab in Healthy Volunteers
A Phase I, Randomized, Single-Dose Study Evaluating the Biosimilarity of TAB008 to Bevacizumab in Healthy Volunteers Abstract Abstract Objective: This study compared the pharmacokinetics (PK), safety, and immunogenicity of the biosimilar TAB008 monoclonal antibody to bevacizumab (Avastin ® ) in normal healthy Chinese m...
PMC11179696
core_pubmed_pmc
Clinical pharmacokinetics of leriglitazone and a translational approach using PBPK modeling to guide the selection of the starting dose in children
Clinical pharmacokinetics of leriglitazone and a translational approach using PBPK modeling to guide the selection of the starting dose in children Abstract Abstract Leriglitazone is a unique peroxisome proliferator‐activated receptor‐gamma (PPARγ) agonist that crosses the blood–brain barrier in humans and clinical tri...
PMC9332547
core_pubmed_pmc
Use of Pharmacogenetics to Optimize Immunosuppressant Therapy in Kidney-Transplanted Patients
Use of Pharmacogenetics to Optimize Immunosuppressant Therapy in Kidney-Transplanted Patients Abstract Immunosuppressant drugs (ISDs) are routinely used in clinical practice to maintain organ transplant survival. However, these drugs are characterized by a restricted therapeutic index, a high inter- and intra-individua...
PMC11327190
core_pubmed_pmc
Liposomal irinotecan ( HR070803 ) in combination with 5-fluorouracil and leucovorin in patients with advanced solid tumors: a phase 1b dose-escalation and expansion study
Liposomal irinotecan ( HR070803 ) in combination with 5-fluorouracil and leucovorin in patients with advanced solid tumors: a phase 1b dose-escalation and expansion study Abstract Abstract Abstract This phase 1b study aimed to evaluate the dose-limiting toxicity (DLT), maximum tolerated dose (MTD), pharmacokinetics, an...
PMC8938153
core_pubmed_pmc
Simultaneous Determination of Lamotrigine, Oxcarbazepine, Lacosamide, and Topiramate in Rat Plasma by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry
Simultaneous Determination of Lamotrigine, Oxcarbazepine, Lacosamide, and Topiramate in Rat Plasma by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry Abstract This study established an ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method to study the pharmacokinetics of ...
PMC8703605
core_pubmed_pmc
Enhancement of the Topical Bioavailability and Skin Whitening Effect of Genistein by Using Microemulsions as Drug Delivery Carriers
Enhancement of the Topical Bioavailability and Skin Whitening Effect of Genistein by Using Microemulsions as Drug Delivery Carriers Abstract Abstract Genistein, the most abundant isoflavone of the soy-derived phytoestrogen compounds, is a potent antioxidant and inhibitor of tyrosine kinase, which can inhibit UVB-induce...
PMC10658920
core_pubmed_pmc
An Integrative Approach to Elucidate Mechanisms Underlying the Pharmacokinetic Goldenseal-Midazolam Interaction: Application of In Vitro Assays and Physiologically Based Pharmacokinetic Models to Understand Clinical Observations
An Integrative Approach to Elucidate Mechanisms Underlying the Pharmacokinetic Goldenseal-Midazolam Interaction: Application of In Vitro Assays and Physiologically Based Pharmacokinetic Models to Understand Clinical Observations Abstract Abstract The natural product goldenseal is a clinical inhibitor of CYP3A activity,...
PMC11971217
core_pubmed_pmc
A randomized, two-armed, double-blind, single-dose, cross-over, bioequivalence clinical trial to compare pharmacokinetic parameters and safety of recombinant human factor VIII with Fc fusion produced by AryoGen Pharmed Company versus Elocta ® (reference product) in previously treated patients with severe haemophilia A
A randomized, two-armed, double-blind, single-dose, cross-over, bioequivalence clinical trial to compare pharmacokinetic parameters and safety of recombinant human factor VIII with Fc fusion produced by AryoGen Pharmed Company versus Elocta ® (reference product) in previously treated patients with severe haemophilia A ...
PMC12597964
core_pubmed_pmc
Exposure–Response Analysis of Donidalorsen for the Treatment of Hereditary Angioedema
Exposure–Response Analysis of Donidalorsen for the Treatment of Hereditary Angioedema Abstract ABSTRACT Hereditary angioedema (HAE) is characterized by recurrent attacks of severe tissue swelling. In the OASIS‐HAE phase 3 study ( NCT05139810 ), donidalorsen, an RNA‐targeted antisense oligonucleotide that reduces prekal...
PMC12466610
core_pubmed_pmc
Development and Validation of a Rapid LC-MS/MS Method for Quantifying Eravacycline in Epithelial Lining Fluid: Application to a Prospective Pulmonary Distribution Study in HAP/VAP Patients
Development and Validation of a Rapid LC-MS/MS Method for Quantifying Eravacycline in Epithelial Lining Fluid: Application to a Prospective Pulmonary Distribution Study in HAP/VAP Patients Abstract Abstract Background : Eravacycline exhibits potent activity against multidrug-resistant pathogens and holds promise for th...
PMC6585933
core_pubmed_pmc
Amenamevir: Studies of Potential CYP3A‐Mediated Pharmacokinetic Interactions With Midazolam, Cyclosporine, and Ritonavir in Healthy Volunteers
Amenamevir: Studies of Potential CYP3A‐Mediated Pharmacokinetic Interactions With Midazolam, Cyclosporine, and Ritonavir in Healthy Volunteers Abstract Abstract Amenamevir (formerly ASP2151) is a helicase‐primase inhibitor being developed for the treatment of herpesvirus infection. Amenamevir is both a substrate and in...
PMC8648480
core_pubmed_pmc
Pharmacokinetic Characterisation and Comparison of Bioavailability of Intranasal Fentanyl, Transmucosal, and Intravenous Administration through a Three-Way Crossover Study in 24 Healthy Volunteers
Pharmacokinetic Characterisation and Comparison of Bioavailability of Intranasal Fentanyl, Transmucosal, and Intravenous Administration through a Three-Way Crossover Study in 24 Healthy Volunteers Abstract Background For more than 60 years, the synthetic opioid fentanyl has been widely used in anaesthesia and analgesia...