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PMC11842995
core_pubmed_pmc
Phase I dose-escalation and pharmacodynamic study of STING agonist E7766 in advanced solid tumors
Phase I dose-escalation and pharmacodynamic study of STING agonist E7766 in advanced solid tumors Abstract Abstract E7766 is a novel stimulator of interferon genes (STING) agonist, capable of potent activation of immune cells and generating strong antitumor response in preclinical murine tumor models. Here we present t...
PMC11329366
core_pubmed_pmc
First‐in‐human study evaluating safety, pharmacokinetics, and pharmacodynamics of lorundrostat, a novel and highly selective aldosterone synthase inhibitor
First‐in‐human study evaluating safety, pharmacokinetics, and pharmacodynamics of lorundrostat, a novel and highly selective aldosterone synthase inhibitor Abstract Abstract Dysregulation of the mineralocorticoid hormone aldosterone is an increasingly prevalent cause of hypertension. Aldosterone synthase (CYP11B2) shar...
PMC11141581
core_pubmed_pmc
Mechanism of Qiguiyin Decoction Sensitizing Levofloxacin Against Multidrug-Resistant Pseudomonas aeruginosa Infection Based on PK-PD and Antibody Chip Technology
Mechanism of Qiguiyin Decoction Sensitizing Levofloxacin Against Multidrug-Resistant Pseudomonas aeruginosa Infection Based on PK-PD and Antibody Chip Technology Abstract Background Qiguiyin decoction (QGYD) is a traditional Chinese medicine (TCM) and its combined application with levofloxacin (LVFX) has been confirmed...
PMC8923173
core_pubmed_pmc
Dose Selection for Phase III Clinical Evaluation of Gepotidacin (GSK2140944) in the Treatment of Uncomplicated Urinary Tract Infections
Dose Selection for Phase III Clinical Evaluation of Gepotidacin (GSK2140944) in the Treatment of Uncomplicated Urinary Tract Infections Abstract ABSTRACT Antibiotics are the current standard-of-care treatment for uncomplicated urinary tract infections (uUTIs). However, increasing rates of bacterial antibiotic resistanc...
PMC12246403
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic characterization of remimazolam in older Japanese adults who underwent general anesthesia at early stage of infusion
Pharmacokinetic and pharmacodynamic characterization of remimazolam in older Japanese adults who underwent general anesthesia at early stage of infusion Abstract The pharmacokinetic and pharmacodynamic characteristics of remimazolam (RMZ), a novel ultrashort-acting anesthetic, administration alone in clinical practice ...
PMC4173659
core_pubmed_pmc
Generation and characterization of tabalumab, a human monoclonal antibody that neutralizes both soluble and membrane-bound B-cell activating factor
Generation and characterization of tabalumab, a human monoclonal antibody that neutralizes both soluble and membrane-bound B-cell activating factor Abstract Abstract B-cell activating factor (BAFF) is a B-cell survival factor with a key role in B-cell homeostasis and tolerance. Dysregulated BAFF expression may contribu...
PMC11056802
core_pubmed_pmc
The Rise of Remimazolam: A Review of Pharmacology, Clinical Efficacy, and Safety Profiles
The Rise of Remimazolam: A Review of Pharmacology, Clinical Efficacy, and Safety Profiles Abstract Anesthesiologists often use benzodiazepines (BZDs) due to their remarkable amnestic and anxiolytic capabilities. Because of this, they are perfect for use during the perioperative phase, when patients' anxiety levels are ...
PMC10092046
core_pubmed_pmc
The Role of PD Biomarkers in Biosimilar Development – To Get the Right Answer One Must First Ask the Right Question
The Role of PD Biomarkers in Biosimilar Development – To Get the Right Answer One Must First Ask the Right Question Abstract Abstract The potential for pharmacodynamic (PD) biomarkers to improve the efficiency of biosimilar product development and regulatory approval formed the premise for the virtual workshop Pharmaco...
PMC7496923
core_pubmed_pmc
Utility of systemic voriconazole in equine keratomycosis based on pharmacokinetic‐pharmacodynamic analysis of tear fluid following oral administration
Utility of systemic voriconazole in equine keratomycosis based on pharmacokinetic‐pharmacodynamic analysis of tear fluid following oral administration Abstract Abstract Objective To clarify the detailed pharmacokinetics (PK) of orally administered voriconazole in tear fluid (TF) of horses for evaluating the efficacy of...
PMC7415763
core_pubmed_pmc
A comparison of thyroidal protection by stable iodine or perchlorate in the case of acute or prolonged radioiodine exposure
A comparison of thyroidal protection by stable iodine or perchlorate in the case of acute or prolonged radioiodine exposure Abstract In the case of a nuclear power plant accident, repetitive/prolonged radioiodine release may occur. Radioiodine accumulates in the thyroid and by irradiation enhances the risk of cancer. L...
PMC11561734
core_pubmed_pmc
Population Pharmacokinetic/Pharmacodynamic Study of Linezolid in Hospital-Acquired Pneumonia Patients with Renal Insufficiency
Population Pharmacokinetic/Pharmacodynamic Study of Linezolid in Hospital-Acquired Pneumonia Patients with Renal Insufficiency Abstract Purpose The optimal treatment strategy in patients with hospital-acquired pneumonia (HAP) due to Gram-positive bacteria and renal insufficiency remains challenging. The objective of th...
PMC7455751
core_pubmed_pmc
Preparation, Characterization and in vivo Study of Borneol-Baicalin-Liposomes for Treatment of Cerebral Ischemia-Reperfusion Injury
Preparation, Characterization and in vivo Study of Borneol-Baicalin-Liposomes for Treatment of Cerebral Ischemia-Reperfusion Injury Abstract Abstract Purpose Baicalin (BA) has a good neuroprotective effect, but it is eliminated quickly in the body and does not easily reach the brain. In this experiment, borneol (BO) wa...
PMC9473365
core_pubmed_pmc
Use of the SGLT2 inhibitor canagliflozin for control of refractory equine hyperinsulinemia and laminitis
Use of the SGLT2 inhibitor canagliflozin for control of refractory equine hyperinsulinemia and laminitis Abstract Abstract Background: Hyperinsulinemia associated with pituitary pars intermedia dysfunction (PPID) and/or equine metabolic syndrome is well documented to put horses at high risk of laminitis. While dietary ...
PMC6616205
core_pubmed_pmc
Influence of Obesity and Type 2 Diabetes Mellitus on the Pharmacokinetics of Tramadol After Single Oral Dose Administration
Influence of Obesity and Type 2 Diabetes Mellitus on the Pharmacokinetics of Tramadol After Single Oral Dose Administration Abstract Abstract Background and Objectives The number of overweight, obese and diabetic patients is constantly increasing. Metabolic disorders may affect the pharmacokinetics of drugs, e.g., by a...
PMC9122503
core_pubmed_pmc
Safety, Pharmacokinetics and Pharmacodynamics of Spectrum Red Softgels in Healthy Participants
Safety, Pharmacokinetics and Pharmacodynamics of Spectrum Red Softgels in Healthy Participants Abstract Abstract Due to a lack of published pharmacokinetic (PK) and/or pharmacodynamic (PD) data, informed physician and patient decision-making surrounding appropriate dosing of cannabis for medical purposes is limited. Th...
PMC3224475
core_pubmed_pmc
Renal and neurological side effects of colistin in critically ill patients
Renal and neurological side effects of colistin in critically ill patients Abstract Abstract Colistin is a complex polypeptide antibiotic composed mainly of colistin A and B. It was abandoned from clinical use in the 1970s because of significant renal and, to a lesser extent, neurological toxicity. Actually, colistin i...
PMC10716330
core_pubmed_pmc
Computer-aided identification of Mycobacterium tuberculosis resuscitation-promoting factor B (RpfB) inhibitors from Gymnema sylvestre natural products
Computer-aided identification of Mycobacterium tuberculosis resuscitation-promoting factor B (RpfB) inhibitors from Gymnema sylvestre natural products Abstract Abstract Tuberculosis (TB), an infectious disease caused by multi-drug resistant Mycobacterium tuberculosis (Mtb), has been a global health concern. Mtb affects...
PMC4646778
core_pubmed_pmc
Engineered binding to erythrocytes induces immunological tolerance to E. coli asparaginase
Engineered binding to erythrocytes induces immunological tolerance to E. coli asparaginase Abstract Abstract Antigen-specific immune responses to protein drugs can hinder efficacy and compromise safety because of drug neutralization and secondary clinical complications. We report a tolerance induction strategy to preve...
PMC11206427
core_pubmed_pmc
Renal Replacement Therapy as a New Indicator of Voriconazole Clearance in a Population Pharmacokinetic Analysis of Critically Ill Patients
Renal Replacement Therapy as a New Indicator of Voriconazole Clearance in a Population Pharmacokinetic Analysis of Critically Ill Patients Abstract Abstract Aims: The pharmacokinetic (PK) profiles of voriconazole in intensive care unit (ICU) patients differ from that in other patients. We aimed to develop a population ...
PMC9797042
core_pubmed_pmc
Outcomes of modern antiretroviral therapy in obese individuals living with HIV
Outcomes of modern antiretroviral therapy in obese individuals living with HIV Abstract Abstract Obesity is a global epidemic and people living with HIV (PLWH) are showing similar obesity trends to those in the general population. Obesity is manifested by several physiological features that can alter volume of distribu...
PMC12629108
core_pubmed_pmc
Subcutaneous injections of cabotegravir plus rilpivirine long-acting in virally suppressed adults with HIV-1
Subcutaneous injections of cabotegravir plus rilpivirine long-acting in virally suppressed adults with HIV-1 Abstract Abstract Objective: To evaluate subcutaneous anterior abdominal injections of long-acting cabotegravir plus rilpivirine (CAB + RPV LA) in participants with more than 3 years’ experience with intramuscul...
PMC9112930
core_pubmed_pmc
Exposure–Efficacy Analyses Support Optimal Dosing Regimens of Ceftolozane/Tazobactam in Participants with Hospital-Acquired/Ventilator-Associated Bacterial Pneumonia in ASPECT-NP
Exposure–Efficacy Analyses Support Optimal Dosing Regimens of Ceftolozane/Tazobactam in Participants with Hospital-Acquired/Ventilator-Associated Bacterial Pneumonia in ASPECT-NP Abstract ABSTRACT An exposure–efficacy analysis of the phase 3 ASPECT-NP trial was performed to evaluate the relationship between plasma expo...
PMC9025148
core_pubmed_pmc
Comparative Pharmacokinetics of Sulfadiazine and Its Metabolite N4-Acetyl Sulfadiazine in Grass Carp ( Ctenopharyngodon idella ) at Different Temperatures after Oral Administration
Comparative Pharmacokinetics of Sulfadiazine and Its Metabolite N4-Acetyl Sulfadiazine in Grass Carp ( Ctenopharyngodon idella ) at Different Temperatures after Oral Administration Abstract In this study, the plasma pharmacokinetics and tissue disposition of sulfadiazine (SDZ) and its main metabolite, N 4 -acetyl sulfa...
PMC9257742
core_pubmed_pmc
iBCS: 1. Principles and Framework of an Inhalation-Based Biopharmaceutics Classification System
iBCS: 1. Principles and Framework of an Inhalation-Based Biopharmaceutics Classification System Abstract Abstract For oral drugs, the formulator and discovery chemist have a tool available to them that can be used to navigate the risks associated with the selection and development of immediate release oral drugs and dr...
PMC7558518
core_pubmed_pmc
Evaluation of Intravenous Fosfomycin Disodium Dosing Regimens in Critically Ill Patients for Treatment of Carbapenem-Resistant Enterobacterales Infections Using Monte Carlo Simulation
Evaluation of Intravenous Fosfomycin Disodium Dosing Regimens in Critically Ill Patients for Treatment of Carbapenem-Resistant Enterobacterales Infections Using Monte Carlo Simulation Abstract Abstract There are limited intravenous fosfomycin disodium (IVFOS) dosing regimens to treat carbapenem-resistant Enterobacteral...
PMC5055047
core_pubmed_pmc
Is it appropriate regarding patient preference to take Myrtol standardized enteric-coated soft capsules after a meal rather than at fasted state? A food–drug pharmacokinetic interaction study in healthy Chinese volunteers
Is it appropriate regarding patient preference to take Myrtol standardized enteric-coated soft capsules after a meal rather than at fasted state? A food–drug pharmacokinetic interaction study in healthy Chinese volunteers Abstract Background According to prescribing information for Myrtol standardized enteric-coated so...
PMC9865866
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Evaluation of Aztreonam/Amoxicillin/Clavulanate Combination against New Delhi Metallo-β-Lactamase and Serine-β-Lactamase Co-Producing Escherichia coli and Klebsiella pneumoniae
Pharmacokinetic/Pharmacodynamic Evaluation of Aztreonam/Amoxicillin/Clavulanate Combination against New Delhi Metallo-β-Lactamase and Serine-β-Lactamase Co-Producing Escherichia coli and Klebsiella pneumoniae Abstract Abstract This study aimed to examine specific niches and usage for the aztreonam/amoxicillin/clavulana...
PMC6366143
core_pubmed_pmc
Three patients with injection of intravitreal vascular endothelial growth factor inhibitors and subsequent exacerbation of chronic proteinuria and hypertension
Three patients with injection of intravitreal vascular endothelial growth factor inhibitors and subsequent exacerbation of chronic proteinuria and hypertension Abstract Abstract Vascular endothelial growth factor (VEGF) receptor inhibition is a commonly used tool to prevent vascular proliferation in tumors and retinal ...
PMC4853790
core_pubmed_pmc
In vivo 3D measurement of moxifloxacin and gatifloxacin distributions in the mouse cornea using multiphoton microscopy
In vivo 3D measurement of moxifloxacin and gatifloxacin distributions in the mouse cornea using multiphoton microscopy Abstract Moxifloxacin and gatifloxacin are fourth-generation fluoroquinolone antibiotics used in the clinic to prevent or treat ocular infections. Their pharmacokinetics in the cornea is usually measur...
PMC11725257
core_pubmed_pmc
A Pharmacokinetic/Pharmacodynamic Study of Esomeprazole Comparing a Dual Delayed-Release Formulation (YYD601) to a Conventional Formulation Following Multiple Administrations in Healthy Adult Subjects
A Pharmacokinetic/Pharmacodynamic Study of Esomeprazole Comparing a Dual Delayed-Release Formulation (YYD601) to a Conventional Formulation Following Multiple Administrations in Healthy Adult Subjects Abstract Background YYD601 is a new dual delayed-release formulation of esomeprazole, developed to enhance plasma expos...
PMC7029911
core_pubmed_pmc
Spectroscopic and molecular docking studies reveal binding characteristics of nazartinib (EGF816) to human serum albumin
Spectroscopic and molecular docking studies reveal binding characteristics of nazartinib (EGF816) to human serum albumin Abstract Abstract The interactions of novel anti-cancer therapeutic agents with the different plasma and tissue components, specifically serum albumins, have lately gained considerable attention due ...
PMC4074692
core_pubmed_pmc
Anticoagulant therapy in pediatrics
Anticoagulant therapy in pediatrics Abstract Abstract Thromboembolic episodes are disorders encountered in both children and adults, but relatively more common in adults. However, the occurrence of venous thromboembolism and use of anticoagulants in pediatrics are increasing. Unfractionated Heparin (UH) is used as a tr...
PMC12001254
core_pubmed_pmc
Population Pharmacokinetics and Exposure‐Response of Subcutaneous Atezolizumab in Patients With Non‐Small Cell Lung Cancer
Population Pharmacokinetics and Exposure‐Response of Subcutaneous Atezolizumab in Patients With Non‐Small Cell Lung Cancer Abstract ABSTRACT IMscin001 is a two‐part dose‐finding (Phase Ib) and ‐confirmation (Phase III) study to evaluate atezolizumab pharmacokinetics of subcutaneous (SC) compared with intravenous (IV) a...
PMC9574745
core_pubmed_pmc
An exposure‐response analysis of ponesimod clinical efficacy in a randomized phase III study in patients with relapsing multiple sclerosis
An exposure‐response analysis of ponesimod clinical efficacy in a randomized phase III study in patients with relapsing multiple sclerosis Abstract Abstract The efficacy of ponesimod and teriflunomide for the treatment of relapsing multiple sclerosis (MS) was compared in a randomized phase III trial. This study explore...
PMC10766039
core_pubmed_pmc
Predicting complex kidney drug handling using a physiologically‐based pharmacokinetic model informed by biomarker‐estimated secretory clearance and blood flow
Predicting complex kidney drug handling using a physiologically‐based pharmacokinetic model informed by biomarker‐estimated secretory clearance and blood flow Abstract Abstract Kidney function‐adjusted drug dosing is currently based solely on the estimated glomerular filtration rate (GFR), however, kidney drug handling...
PMC12086683
core_pubmed_pmc
Individualization of piperacillin dosage based on therapeutic drug monitoring with or without model-informed precision dosing: a scenario analysis
Individualization of piperacillin dosage based on therapeutic drug monitoring with or without model-informed precision dosing: a scenario analysis Abstract Abstract Background Model-informed precision dosing (MIPD) combines population pharmacokinetic knowledge with therapeutic drug monitoring (TDM) to optimize dosage a...
PMC8376145
core_pubmed_pmc
Multiscale model of hepatitis C virus dynamics in plasma and liver following combination therapy
Multiscale model of hepatitis C virus dynamics in plasma and liver following combination therapy Abstract Abstract This work explores the application of a physiologically structured population (PSP) framework in modeling hepatitis C virus (HCV) kinetics. To do so, a model was developed for the viral RNA load in plasma ...
PMC4937627
core_pubmed_pmc
Occurrence of drug–drug interactions in Adama Referral Hospital, Adama city, Ethiopia
Occurrence of drug–drug interactions in Adama Referral Hospital, Adama city, Ethiopia Abstract Abstract Objective Many medications have potential interactions with other drugs or substances when prescribed together. This study was intended to investigate the extent of poly-pharmacy, event of drug–drug interactions and ...
PMC12498006
core_pubmed_pmc
Anaesthesia Challenges in Patients With Chronic Kidney Disease: A Clinical Approach From Internal Medicine
Anaesthesia Challenges in Patients With Chronic Kidney Disease: A Clinical Approach From Internal Medicine Abstract Chronic kidney disease (CKD) poses significant challenges for perioperative anaesthetic management due to complex alterations in drug clearance, fluid and electrolyte balance, and increased cardiovascular...
PMC10892643
core_pubmed_pmc
Population Pharmacokinetic Model of Linezolid and Probability of Target Attainment in Patients with COVID-19-Associated Acute Respiratory Distress Syndrome on Veno-Venous Extracorporeal Membrane Oxygenation—A Step toward Correct Dosing
Population Pharmacokinetic Model of Linezolid and Probability of Target Attainment in Patients with COVID-19-Associated Acute Respiratory Distress Syndrome on Veno-Venous Extracorporeal Membrane Oxygenation—A Step toward Correct Dosing Abstract Abstract During veno-venous extracorporeal membrane oxygenation (vv ECMO) t...
PMC5445229
core_pubmed_pmc
Population Pharmacokinetics of Morphine in Patients With Nonalcoholic Steatohepatitis (NASH) and Healthy Adults
Population Pharmacokinetics of Morphine in Patients With Nonalcoholic Steatohepatitis (NASH) and Healthy Adults Abstract Altered expression and function of transporters in nonalcoholic steatohepatitis (NASH) patients may affect the pharmacokinetics (PK), efficacy, and safety of substrate drugs. A population pharmacokin...
PMC4542398
core_pubmed_pmc
Development, validation of liquid chromatography-tandem mass spectrometry method for simultaneous determination of rosuvastatin and metformin in human plasma and its application to a pharmacokinetic study
Development, validation of liquid chromatography-tandem mass spectrometry method for simultaneous determination of rosuvastatin and metformin in human plasma and its application to a pharmacokinetic study Abstract Abstract A new, simple and accurate liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for s...
PMC8302239
core_pubmed_pmc
Population pharmacokinetics and exposure–response analyses of varenicline in adolescent smokers
Population pharmacokinetics and exposure–response analyses of varenicline in adolescent smokers Abstract Abstract Varenicline is an approved smoking cessation aid in adults. Population pharmacokinetics (popPK) and exposure–response (ER) (continuous abstinence rates [CAR] weeks 9‒12 and nausea/vomiting incidence) for va...
PMC4248610
core_pubmed_pmc
Lower Loading Dose of Prasugrel Compared with Conventional Loading Doses of Clopidogrel and Prasugrel in Korean Patients Undergoing Elective Coronary Angiography: A Randomized Controlled Study Evaluating Pharmacodynamic Efficacy
Lower Loading Dose of Prasugrel Compared with Conventional Loading Doses of Clopidogrel and Prasugrel in Korean Patients Undergoing Elective Coronary Angiography: A Randomized Controlled Study Evaluating Pharmacodynamic Efficacy Abstract Background and Objectives Although prasugrel allows for rapid and potent platelet ...
PMC6921164
core_pubmed_pmc
Determining therapeutic trough ranges for linezolid
Determining therapeutic trough ranges for linezolid Abstract Abstract Linezolid (LZD) is an oxazolidinone approved for the treatment of gram-positive infections. Therapeutic drug monitoring is increasingly used to optimize LZD dosing. The therapeutic target for LZD is to achieve an area under the concentration-time cur...
PMC12506672
core_pubmed_pmc
A phase I study of HEC73543, an oral FLT3 inhibitor: the effect of food on pharmacokinetics after oral dosing in healthy Chinese volunteers
A phase I study of HEC73543, an oral FLT3 inhibitor: the effect of food on pharmacokinetics after oral dosing in healthy Chinese volunteers Abstract Objective This study evaluated the effect of food on the pharmacokinetics (PK) and safety of HEC73543. Methods This randomized, open-label, single-dose, phase I parallel t...
PMC9721384
core_pubmed_pmc
Addition of probenecid to oral β-lactam antibiotics: a systematic review and meta-analysis
Addition of probenecid to oral β-lactam antibiotics: a systematic review and meta-analysis Abstract Abstract Objectives To explore the literature comparing the pharmacokinetic and clinical outcomes from adding probenecid to oral β-lactams. Methods Medline and EMBASE were searched from inception to December 2021 for all...
PMC6767536
core_pubmed_pmc
A Randomized, Double‐Blind, Placebo‐Controlled, First‐Time‐in‐Human Study to Assess the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Ascending Doses of GSK3389404 in Healthy Subjects
A Randomized, Double‐Blind, Placebo‐Controlled, First‐Time‐in‐Human Study to Assess the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Ascending Doses of GSK3389404 in Healthy Subjects Abstract Abstract GSK3389404 is a liver‐targeted antisense oligonucleotide that inhibits synthesis of hepatitis B su...
PMC11372714
core_pubmed_pmc
In vitro antibacterial activity of danofloxacin against Escherichia coli isolated from pigeons and its pharmacokinetic in pigeons
In vitro antibacterial activity of danofloxacin against Escherichia coli isolated from pigeons and its pharmacokinetic in pigeons Abstract Abstract This experiment aimed to investigate the in vitro antimicrobial activity of danofloxacin against Escherichia coli ( E. coli ) isolated from pigeons, as well as the pharmaco...
PMC8246884
core_pubmed_pmc
Short‐duration treatment with the novel non‐nucleoside inhibitor CDI‐31244 plus sofosbuvir/velpatasvir for chronic hepatitis C: An open‐label study
Short‐duration treatment with the novel non‐nucleoside inhibitor CDI‐31244 plus sofosbuvir/velpatasvir for chronic hepatitis C: An open‐label study Abstract Abstract Combination regimens of direct‐acting antiviral agents (DAAs) for chronic genotype 1 hepatitis C virus (HCV) infection given for 8 or 12 weeks have high c...
PMC6830151
core_pubmed_pmc
Use of classification and regression tree (CART), to identify hemoglobin A1C (HbA 1C ) cut-off thresholds predictive of poor tuberculosis treatment outcomes and associated risk factors
Use of classification and regression tree (CART), to identify hemoglobin A1C (HbA 1C ) cut-off thresholds predictive of poor tuberculosis treatment outcomes and associated risk factors Abstract Background Rifampin-based therapy potentially exacerbates glycemic control among TB patients who are already at high risk of h...
PMC12193388
core_pubmed_pmc
Sugar-Linked Diethyldithiocarbamate Derivatives: A Novel Class of Anticancer Agents
Sugar-Linked Diethyldithiocarbamate Derivatives: A Novel Class of Anticancer Agents Abstract Disulfiram (DSF), a well-known anti-alcoholism drug, exhibits potent anticancer activity via its metabolite, diethyldithiocarbamate (DDC), which forms a cytotoxic copper complex that selectively targets cancer stem cells. Howev...
PMC9270274
core_pubmed_pmc
Low-dose Dasatinib Ameliorates Hypertrophic Cardiomyopathy in Noonan Syndrome with Multiple Lentigines
Low-dose Dasatinib Ameliorates Hypertrophic Cardiomyopathy in Noonan Syndrome with Multiple Lentigines Abstract Abstract Purpose Noonan syndrome with multiple lentigines (NSML) is an autosomal dominant disorder presenting with hypertrophic cardiomyopathy (HCM). Up to 85% of NSML cases are caused by mutations in the PTP...
PMC12186298
core_pubmed_pmc
Phase 1 clinical trial of eneboparatide, a novel PTH receptor 1 agonist
Phase 1 clinical trial of eneboparatide, a novel PTH receptor 1 agonist Abstract Abstract Objective This study evaluated the safety, tolerability, pharmacodynamics (PD) and pharmacokinetics (PK) of eneboparatide (AZP-3601), a novel agonist of the PTH receptor 1 developed for the treatment of hypoparathyroidism. Design ...
PMC12847137
core_pubmed_pmc
Advancing Medulloblastoma Treatment: Molecular Mechanisms, Drug Repurposing, and Precision Therapies
Advancing Medulloblastoma Treatment: Molecular Mechanisms, Drug Repurposing, and Precision Therapies Abstract Medulloblastomas are the most common malignant pediatric brain tumors, representing approximately 20% of the central nervous system cancers in children. These tumors are highly heterogeneous and classified into...
PMC8958608
core_pubmed_pmc
Hodgkin Lymphoma on Hemodialysis Successfully Treated with Extended Courses of Brentuximab Vedotin
Hodgkin Lymphoma on Hemodialysis Successfully Treated with Extended Courses of Brentuximab Vedotin Abstract Chemotherapy for hemodialysis (HD) patients is a challenging situation because HD patients are generally frail, and the pharmacokinetics and pharmacodynamics of most chemotherapeutics in HD patients are unknown. ...
PMC11954719
core_pubmed_pmc
Influence of a Short Course of Ritonavir Used as Booster in Antiviral Therapies Against SARS-CoV-2 on the Exposure of Atorvastatin and Rosuvastatin
Influence of a Short Course of Ritonavir Used as Booster in Antiviral Therapies Against SARS-CoV-2 on the Exposure of Atorvastatin and Rosuvastatin Abstract Purpose Early antiviral treatment with nirmatrelvir/ritonavir is recommended for SARS-CoV-2-infected patients at high risk for severe courses. Such patients are us...
PMC7566547
core_pubmed_pmc
High in vitro activity of DIS-73285, a novel antimicrobial with a new mechanism of action, against MDR and XDR Neisseria gonorrhoeae
High in vitro activity of DIS-73285, a novel antimicrobial with a new mechanism of action, against MDR and XDR Neisseria gonorrhoeae Abstract Abstract Background The rising incidence of antimicrobial resistance in Neisseria gonorrhoeae may result in untreatable gonorrhoea in certain circumstances and development of nov...
PMC7253354
core_pubmed_pmc
Drug–drug–gene interactions and adverse drug reactions
Drug–drug–gene interactions and adverse drug reactions Abstract The economic and health burden caused by adverse drug reactions has increased dramatically in the last few years. This is likely to be mediated by increasing polypharmacy, which increases the likelihood for drug–drug interactions. Tools utilized by healthc...
PMC10497203
core_pubmed_pmc
Population Pharmacokinetic Modeling and Determination of Individual Exposure to Avalglucosidase Alfa in Adolescent and Adult Patients With Late-Onset Pompe Disease: Analysis of Pooled Data From Phase I to III Clinical Trials
Population Pharmacokinetic Modeling and Determination of Individual Exposure to Avalglucosidase Alfa in Adolescent and Adult Patients With Late-Onset Pompe Disease: Analysis of Pooled Data From Phase I to III Clinical Trials Abstract Abstract Background: Pompe disease is a rare genetic disorder caused by a deficiency o...
PMC9484246
core_pubmed_pmc
Intratumoral delivery of TransCon ™ TLR7/8 Agonist promotes sustained anti-tumor activity and local immune cell activation while minimizing systemic cytokine induction
Intratumoral delivery of TransCon ™ TLR7/8 Agonist promotes sustained anti-tumor activity and local immune cell activation while minimizing systemic cytokine induction Abstract Background Intratumoral (IT) delivery of toll-like receptor (TLR) agonists has shown encouraging anti-tumor benefit in preclinical and early cl...
PMC8846400
core_pubmed_pmc
Scoping Review of Antimalarial Drug Candidates in Phase I and II Drug Development
Scoping Review of Antimalarial Drug Candidates in Phase I and II Drug Development Abstract ABSTRACT The emergence and spread of parasite resistance to currently available antimalarials has highlighted the importance of developing novel antimalarials. This scoping review provides an overview of antimalarial drug candida...
PMC6146668
core_pubmed_pmc
Absorption Characteristics of Combination Medication of Realgar and Indigo Naturalis : In Vitro Transport across MDCK-MDR1 Cells and In Vivo Pharmacokinetics in Mice after Oral Administration
Absorption Characteristics of Combination Medication of Realgar and Indigo Naturalis : In Vitro Transport across MDCK-MDR1 Cells and In Vivo Pharmacokinetics in Mice after Oral Administration Abstract Abstract Realgar and indigo naturalis are clinically combined to treat varieties of leukemia. Exploring the drug-drug i...
PMC3702506
core_pubmed_pmc
Importance of Ethnicity, CYP2B6 and ABCB1 Genotype for Efavirenz Pharmacokinetics and Treatment Outcomes: A Parallel-Group Prospective Cohort Study in Two Sub-Saharan Africa Populations
Importance of Ethnicity, CYP2B6 and ABCB1 Genotype for Efavirenz Pharmacokinetics and Treatment Outcomes: A Parallel-Group Prospective Cohort Study in Two Sub-Saharan Africa Populations Abstract Objectives We evaluated the importance of ethnicity and pharmacogenetic variations in determining efavirenz pharmacokinetics,...
PMC12951560
core_pubmed_pmc
Bioisostere-Driven Discovery of SePP: A Selenium-Containing Polypharmacological Agent Relevant to Fragile X Syndrome
Bioisostere-Driven Discovery of SePP: A Selenium-Containing Polypharmacological Agent Relevant to Fragile X Syndrome Abstract Abstract Diphenidine is a prototypical 1,2-diarylethylamine that functions as an uncompetitive N -methyl- d -aspartate receptor (NMDAR) antagonist and monoamine reuptake inhibitor. To examine th...
PMC8539387
core_pubmed_pmc
Impact of Tacrolimus Daily Dose Limitation in Renal Transplant Recipients Expressing CYP3A5: A Retrospective Study
Impact of Tacrolimus Daily Dose Limitation in Renal Transplant Recipients Expressing CYP3A5: A Retrospective Study Abstract Abstract The pharmacokinetic variability of tacrolimus can be partly explained by CYP3A5 activity. Our objective was to evaluate a tacrolimus sparing policy on renal graft outcome according to CYP...
PMC11494959
core_pubmed_pmc
Delivery strategies to improve piglets exposure to oral antimicrobials
Delivery strategies to improve piglets exposure to oral antimicrobials Abstract Background The widespread practice of delivering antimicrobials through drinking water to livestock leads to considerable variability in exposure levels among animals, raising concerns regarding disease outbreaks and the emergence of antimi...
PMC5298089
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Evaluation of the Drug‐Drug Interaction Between Isavuconazole and Warfarin in Healthy Subjects
Pharmacokinetic and Pharmacodynamic Evaluation of the Drug‐Drug Interaction Between Isavuconazole and Warfarin in Healthy Subjects Abstract Abstract This phase 1 trial evaluated pharmacokinetic and pharmacodynamic interactions between the novel triazole antifungal agent isavuconazole and warfarin in healthy adults. Mul...
PMC12809580
core_pubmed_pmc
An Observational Cohort Study of Targeted Antibiotic Treatments of Cystic Fibrosis Exacerbations
An Observational Cohort Study of Targeted Antibiotic Treatments of Cystic Fibrosis Exacerbations Abstract Abstract Background Cystic fibrosis (CF) pulmonary exacerbations shorten survival. Treatment guidelines omit minimal inhibitory concentration (MIC)–based antibiotic dose selection. We tested whether MIC-guided intr...
PMC10508611
core_pubmed_pmc
A randomized trial: The safety, pharmacokinetics and preliminary pharmacodynamics of ropivacaine oil delivery depot in healthy subjects
A randomized trial: The safety, pharmacokinetics and preliminary pharmacodynamics of ropivacaine oil delivery depot in healthy subjects Abstract Introduction Ropivacaine oil delivery depot (RODD) can slowly release ropivacaine and block nerves for a long timejavascript:;. The aim of the present work was to investigate ...
PMC12854050
core_pubmed_pmc
pH-responsive ZIF-8@quercetin nanoparticles induce pyroptosis for targeted gastric cancer therapy
pH-responsive ZIF-8@quercetin nanoparticles induce pyroptosis for targeted gastric cancer therapy Abstract Abstract Gastric cancer (GC) remains a major global health burden, with limited effective therapies and poor prognosis. Quercetin (Que), a natural flavonoid, exhibits anticancer activity but suffers from poor wate...
PMC9805152
core_pubmed_pmc
Efficacy, safety and bioequivalence of the human‐derived B‐domain‐deleted recombinant factor VIII TQG202 for prophylaxis in severe haemophilia A patients
Efficacy, safety and bioequivalence of the human‐derived B‐domain‐deleted recombinant factor VIII TQG202 for prophylaxis in severe haemophilia A patients Abstract Abstract Introduction Current treatment of severe haemophilia A includes prophylaxis with factor VIII (FVIII) replacement. The supply of plasma‐derived FVIII...
PMC10002493
core_pubmed_pmc
Direct Oral FXa Inhibitors Binding to Human Serum Albumin: Spectroscopic, Calorimetric, and Computational Studies
Direct Oral FXa Inhibitors Binding to Human Serum Albumin: Spectroscopic, Calorimetric, and Computational Studies Abstract Abstract Direct FXa inhibitors are an important class of bioactive molecules (rivaroxaban, apixaban, edoxaban, and betrixaban) applied for thromboprophylaxis in diverse cardiovascular pathologies. ...
PMC8799559
core_pubmed_pmc
Population Pharmacokinetics and Exposure–Response Analyses for Venetoclax in Combination with R-CHOP in Relapsed/Refractory and Previously Untreated Patients with Diffuse Large B Cell Lymphoma
Population Pharmacokinetics and Exposure–Response Analyses for Venetoclax in Combination with R-CHOP in Relapsed/Refractory and Previously Untreated Patients with Diffuse Large B Cell Lymphoma Abstract Introduction Outcomes remain poor in patients with diffuse large B cell lymphoma (DLBCL) who overexpress BCL-2 protein...
PMC11787893
core_pubmed_pmc
Simulated achievement rate of β-lactams/nacubactam treatment in humans using instantaneous MIC-based PK/PD analysis
Simulated achievement rate of β-lactams/nacubactam treatment in humans using instantaneous MIC-based PK/PD analysis Abstract Abstract Background Nacubactam (NAC), a new diazabicyclooctane β-lactamase inhibitor, is being developed for use together with aztreonam (AZT) and cefepime (CFPM). However, the effective clinical...
PMC3916804
core_pubmed_pmc
The development and validation of an LC-MS/MS method for the determination of a new anti-malarial compound (TK900D) in human whole blood and its application to pharmacokinetic studies in mice
The development and validation of an LC-MS/MS method for the determination of a new anti-malarial compound (TK900D) in human whole blood and its application to pharmacokinetic studies in mice Abstract Abstract Background Malaria is one of the most lethal and life-threatening killer infectious diseases in the world, and...
PMC9574830
core_pubmed_pmc
Targeting COVID-19 pandemic: in silico evaluation of 2-hydroxy-1, 2-diphenylethanone N(4)-methyl-N(4)-phenylthiosemicarbazone as a potential inhibitor of SARS-CoV-2
Targeting COVID-19 pandemic: in silico evaluation of 2-hydroxy-1, 2-diphenylethanone N(4)-methyl-N(4)-phenylthiosemicarbazone as a potential inhibitor of SARS-CoV-2 Abstract The global spread of the COVID-19 pandemic caused by the etiological agent, severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), triggere...
PMC6096899
core_pubmed_pmc
Characterization of Intestinal and Hepatic CYP3A-Mediated Metabolism of Midazolam in Children Using a Physiological Population Pharmacokinetic Modelling Approach
Characterization of Intestinal and Hepatic CYP3A-Mediated Metabolism of Midazolam in Children Using a Physiological Population Pharmacokinetic Modelling Approach Abstract Purpose Changes in drug absorption and first-pass metabolism have been reported throughout the pediatric age range. Our aim is to characterize both i...
PMC11341832
core_pubmed_pmc
Novel cathepsin C inhibitor, BI 1291583, intended for treatment of bronchiectasis: Phase I characterization in healthy volunteers
Novel cathepsin C inhibitor, BI 1291583, intended for treatment of bronchiectasis: Phase I characterization in healthy volunteers Abstract Abstract Novel treatments are needed to reduce inflammation, improve symptoms, address exacerbations, and slow disease progression in bronchiectasis. Cathepsin C (CatC) inhibition p...
PMC10910237
core_pubmed_pmc
Pharmacokinetics of single dose doxycycline in the rectum, vagina, and urethra: implications for prevention of bacterial sexually transmitted infections
Pharmacokinetics of single dose doxycycline in the rectum, vagina, and urethra: implications for prevention of bacterial sexually transmitted infections Abstract Summary Background Clinical trials showed a single oral dose of doxycycline taken after sex protects against STIs among men who have sex with men (MSM) but no...
PMC10369431
core_pubmed_pmc
Cefepime extended infusion versus intermittent infusion: Clinical and cost evaluation
Cefepime extended infusion versus intermittent infusion: Clinical and cost evaluation Abstract Abstract Background: Extended infusion cefepime (1 gram every 6 hours administered over 3 hours) achieves pharmacodynamic efficacy against bacteria with a MIC of ≤8 mg/L in Monte Carlo simulations. This regimen has not been e...
PMC12519588
core_pubmed_pmc
Oral nanoliposomes functionalized with cRGD and polydopamine for enhanced antimalarial efficacy of disulfide bond-modified dihydroartemisinin prodrug
Oral nanoliposomes functionalized with cRGD and polydopamine for enhanced antimalarial efficacy of disulfide bond-modified dihydroartemisinin prodrug Abstract Abstract Malaria remains a global health crisis, with Plasmodium resistance underscoring the urgent need for advanced drug delivery strategies. To overcome the l...
PMC10954945
core_pubmed_pmc
Bayesian Vancomycin Model Selection for Therapeutic Drug Monitoring in Neonates
Bayesian Vancomycin Model Selection for Therapeutic Drug Monitoring in Neonates Abstract Background and Objective Pharmacokinetic models can inform drug dosing of vancomycin in neonates to optimize therapy. However, the model selected needs to describe the intended population to provide appropriate dose recommendations...
PMC11695905
core_pubmed_pmc
Model-informed drug development for antimicrobials: translational pharmacokinetic-pharmacodynamic modelling of apramycin to facilitate prediction of efficacious dose in complicated urinary tract infections
Model-informed drug development for antimicrobials: translational pharmacokinetic-pharmacodynamic modelling of apramycin to facilitate prediction of efficacious dose in complicated urinary tract infections Abstract Abstract Objectives The use of mouse models of complicated urinary tract infection (cUTI) has usually bee...
PMC12110727
core_pubmed_pmc
Capillary Filtration of Plasma Is Accelerated During General Anesthesia: A Secondary Population Volume Kinetic Analysis
Capillary Filtration of Plasma Is Accelerated During General Anesthesia: A Secondary Population Volume Kinetic Analysis Abstract Abstract How infusion fluids are distributed and eliminated is of importance to how much and how fast they should be administered. This manuscript applies population pharmacokinetic modeling ...
PMC11375879
core_pubmed_pmc
Antibiotic resistance challenge: evaluating anthraquinones as rifampicin monooxygenase inhibitors through integrated bioinformatics analysis
Antibiotic resistance challenge: evaluating anthraquinones as rifampicin monooxygenase inhibitors through integrated bioinformatics analysis Abstract Abstract Objective Antibiotic resistance poses a pressing and crucial global public health challenge, leading to significant clinical and health-related consequences. Sub...
PMC9326111
core_pubmed_pmc
Capsaicin: A Two-Decade Systematic Review of Global Research Output and Recent Advances Against Human Cancer
Capsaicin: A Two-Decade Systematic Review of Global Research Output and Recent Advances Against Human Cancer Abstract Capsaicin (8-methyl-N-vanillyl-6-nonenamide) is one of the most important natural products in the genus Capsicum. Due to its numerous biological effects, there has been extensive and increasing research...
PMC11325272
core_pubmed_pmc
Safety and clinical activity of durvalumab combined with tremelimumab in recurrent/metastatic head and neck squamous cell carcinoma: a multicenter phase I study
Safety and clinical activity of durvalumab combined with tremelimumab in recurrent/metastatic head and neck squamous cell carcinoma: a multicenter phase I study Abstract Abstract Background Programmed cell death protein 1 (PD-1) inhibitors prolong survival versus chemotherapy in recurrent/metastatic head and neck squam...
PMC9414514
core_pubmed_pmc
In Vitro–In Vivo Relationship in Mini-Scale—Enabling Formulations of Corallopyronin A
In Vitro–In Vivo Relationship in Mini-Scale—Enabling Formulations of Corallopyronin A Abstract In vivo studies in mice provide a valuable model to test novel active pharmaceutical ingredients due to their low material need and the fact that mice are frequently used as a species for early efficacy models. However, precl...
PMC5326936
core_pubmed_pmc
Pharmacokinetic studies of the recombinant chicken interferon-α in broiler chickens
Pharmacokinetic studies of the recombinant chicken interferon-α in broiler chickens Abstract Abstract In this study, 24 male and female broiler chickens at 30-day-old were divided into three groups with 8 animals in each group. The animals were administered with recombinant chicken interferon-α (rChIFN-α) at a dose of ...
PMC10051608
core_pubmed_pmc
Multi-Compartmental Dissolution Method, an Efficient Tool for the Development of Enhanced Bioavailability Formulations Containing Poorly Soluble Acidic Drugs
Multi-Compartmental Dissolution Method, an Efficient Tool for the Development of Enhanced Bioavailability Formulations Containing Poorly Soluble Acidic Drugs Abstract Abstract The purpose of this study was to investigate the applicability of the Gastrointestinal Simulator (GIS), a multi-compartmental dissolution model,...
PMC11879141
core_pubmed_pmc
Quantitative evaluation of multiple treatment regimens for treatment-resistant depression
Quantitative evaluation of multiple treatment regimens for treatment-resistant depression Abstract Abstract Objective This study aims to quantitatively evaluate the efficacy and safety of various treatment regimens for treatment-resistant depression (TRD) across oral, intravenous, and intranasal routes to inform clinic...
PMC11881764
core_pubmed_pmc
Dose optimization of cefazolin in South African children undergoing cardiac surgery with cardiopulmonary bypass
Dose optimization of cefazolin in South African children undergoing cardiac surgery with cardiopulmonary bypass Abstract Abstract Cefazolin is an antibiotic used to prevent surgical site infections. During cardiac surgery with cardiopulmonary bypass (CPB), its efficacy target could be underachieved. We aimed to develop...
PMC8979758
core_pubmed_pmc
Prediction of metabolizing enzyme-mediated clinical drug interactions using in vitro information
Prediction of metabolizing enzyme-mediated clinical drug interactions using in vitro information Abstract Abstract Evaluation of drug interactions is an essential step in the new drug development process. Regulatory agencies, including U.S. Food and Drug Administrations and European Medicines Agency, have been publishe...
PMC12117050
core_pubmed_pmc
Effects of mallotus furetianus extract on CYP3A activities in rats
Effects of mallotus furetianus extract on CYP3A activities in rats Abstract Mallotus furetianus is traditionally used as folk medicine on Hainan Island, China. Given the significance of the pharmacokinetic interaction between herbs and drugs, we investigated the effects of Mallotus furetianus ethanol extract (MFE) on C...
PMC11335710
core_pubmed_pmc
Sitagliptin elevates plasma and CSF incretin levels following oral administration to nonhuman primates: relevance for neurodegenerative disorders
Sitagliptin elevates plasma and CSF incretin levels following oral administration to nonhuman primates: relevance for neurodegenerative disorders Abstract The endogenous incretins glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) possess neurotrophic, neuroprotective, and anti-neuro...
PMC10689135
core_pubmed_pmc
Drugs with a negative impact on cognitive function (Part 1): chronic kidney disease as a risk factor
Drugs with a negative impact on cognitive function (Part 1): chronic kidney disease as a risk factor Abstract ABSTRACT People living with chronic kidney disease (CKD) frequently suffer from mild cognitive impairment and/or other neurocognitive disorders. This review in two parts will focus on adverse drug reactions res...
PMC9686941
core_pubmed_pmc
Empirical Antibiotic Therapy for Gram-Negative Bacilli Ventilator-Associated Pneumonia: Observational Study and Pharmacodynamic Assessment
Empirical Antibiotic Therapy for Gram-Negative Bacilli Ventilator-Associated Pneumonia: Observational Study and Pharmacodynamic Assessment Abstract Abstract Background: Strong evidence suggests a correlation between pharmacodynamics (PD) index and antibiotic efficacy while dose adjustment should be considered in critic...
PMC6202471
core_pubmed_pmc
Semimechanistic Population Pharmacokinetic Model to Predict the Drug–Drug Interaction Between S ‐ketamine and Ticlopidine in Healthy Human Volunteers
Semimechanistic Population Pharmacokinetic Model to Predict the Drug–Drug Interaction Between S ‐ketamine and Ticlopidine in Healthy Human Volunteers Abstract Abstract Low‐dose oral S ‐ketamine is increasingly used in chronic pain therapy, but extensive cytochrome P450 (CYP) mediated metabolism makes it prone to pharma...
PMC10196432
core_pubmed_pmc
Interplay among malnutrition, chemoprevention, and the risk of malaria in young Ugandan children: Longitudinal pharmacodynamic and growth analysis
Interplay among malnutrition, chemoprevention, and the risk of malaria in young Ugandan children: Longitudinal pharmacodynamic and growth analysis Abstract Abstract African children are at risk of malaria and malnutrition. We quantified relationships between malaria and malnutrition among young Ugandan children in a hi...