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PMC12209202
core_pubmed_pmc
Research progress and molecular mechanism of oridonin in the treatment of malignant melanoma
Research progress and molecular mechanism of oridonin in the treatment of malignant melanoma Abstract Malignant Melanoma (MM) is a highly invasive and easily metastasizing skin cancer. Although current treatments have made certain progress in targeted therapy and immunotherapy, drug resistance and side effects remain u...
PMC4467260
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Vilanterol, a Novel Inhaled Long-Acting β-Agonist, in Children Aged 5–11 Years with Persistent Asthma: A Randomized Trial
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Vilanterol, a Novel Inhaled Long-Acting β-Agonist, in Children Aged 5–11 Years with Persistent Asthma: A Randomized Trial Abstract Abstract This multi-center, randomized, double-blind, placebo-controlled, two-way crossover study was designed to characteriz...
PMC12343092
core_pubmed_pmc
Longitudinal Evaluation of Bone Safety in Children and Adolescents With HIV-1 Starting Tenofovir Alafenamide-Containing Antiretroviral Therapy
Longitudinal Evaluation of Bone Safety in Children and Adolescents With HIV-1 Starting Tenofovir Alafenamide-Containing Antiretroviral Therapy Abstract Abstract Background Adult participants taking tenofovir alafenamide (TAF) in clinical trials had a better bone safety profile than those taking tenofovir disoproxil fum...
PMC5395227
core_pubmed_pmc
Population pharmacokinetic modelling of rupatadine solution in 6–11 year olds and optimisation of the experimental design in younger children
Population pharmacokinetic modelling of rupatadine solution in 6–11 year olds and optimisation of the experimental design in younger children Abstract Abstract Aims To optimise a pharmacokinetic (PK) study design of rupatadine for 2–5 year olds by using a population PK model developed with data from a study in 6–11 yea...
PMC12079145
core_pubmed_pmc
Pharmacokinetics of Dexmedetomidine in an In Vitro Circuit Model and In Vivo Extracorporeal Membrane Oxygenation Rat Model
Pharmacokinetics of Dexmedetomidine in an In Vitro Circuit Model and In Vivo Extracorporeal Membrane Oxygenation Rat Model Abstract Background and objectives: Extracorporeal membrane oxygenation (ECMO) causes variability in the pharmacokinetics (PK) of drugs. Fluctuations in the PK profile of dexmedetomidine (DEX) migh...
PMC12217465
core_pubmed_pmc
Population pharmacokinetics of meropenem-vaborbactam in acutely ill hospitalized patients with various degrees of renal dysfunction including continuous renal replacement therapy
Population pharmacokinetics of meropenem-vaborbactam in acutely ill hospitalized patients with various degrees of renal dysfunction including continuous renal replacement therapy Abstract ABSTRACT Real-world meropenem-vaborbactam (MVB) pharmacokinetic-pharmacodynamic (PK/PD) attainment data in patients with renal dysfu...
PMC6761531
core_pubmed_pmc
Population Pharmacokinetics of the Antituberculosis Agent Pretomanid
Population Pharmacokinetics of the Antituberculosis Agent Pretomanid Abstract A population pharmacokinetic (PopPK) model for pretomanid was developed using data from 14 studies in the pretomanid development program: six phase 1 studies, six phase 2 studies, and two phase 3 studies. The final analysis data set contained...
PMC9290068
core_pubmed_pmc
Multicompartmental pharmacokinetic evaluation of long‐acting cabotegravir in healthy adults for HIV preexposure prophylaxis
Multicompartmental pharmacokinetic evaluation of long‐acting cabotegravir in healthy adults for HIV preexposure prophylaxis Abstract Abstract Aims Cabotegravir is an integrase strand transfer inhibitor in clinical development as long‐acting (LA) injectable HIV preexposure prophylaxis. Methods This phase I study assesse...
PMC4559079
core_pubmed_pmc
Pharmacokinetics and safety of ixazomib plus lenalidomide–dexamethasone in Asian patients with relapsed/refractory myeloma: a phase 1 study
Pharmacokinetics and safety of ixazomib plus lenalidomide–dexamethasone in Asian patients with relapsed/refractory myeloma: a phase 1 study Abstract Abstract Background The oral proteasome inhibitor ixazomib is under phase 3 clinical investigation in multiple myeloma (MM) in combination with lenalidomide–dexamethasone....
PMC12618388
core_pubmed_pmc
Hybrid Population Pharmacokinetic–Machine Learning Modeling to Predict Infliximab Pharmacokinetics in Pediatric and Young Adult Patients with Crohn’s Disease
Hybrid Population Pharmacokinetic–Machine Learning Modeling to Predict Infliximab Pharmacokinetics in Pediatric and Young Adult Patients with Crohn’s Disease Abstract Abstract Background and Objective Population pharmacokinetic (PK) model-based Bayesian estimation is widely used for dose individualization, particularly...
PMC5697635
core_pubmed_pmc
Pharmacokinetic, Pharmacodynamic, and Safety Profile of a Novel Anti‐CD28 Domain Antibody Antagonist in Healthy Subjects
Pharmacokinetic, Pharmacodynamic, and Safety Profile of a Novel Anti‐CD28 Domain Antibody Antagonist in Healthy Subjects Abstract Abstract We report pharmacokinetics, pharmacodynamics, and safety of a novel anti‐CD28 domain antibody antagonist (lulizumab pegol) in healthy subjects following single‐ or multiple‐dose adm...
PMC6767117
core_pubmed_pmc
Relative and Absolute Bioavailability Study of Emicizumab to Bridge Drug Products and Subcutaneous Injection Sites in Healthy Volunteers
Relative and Absolute Bioavailability Study of Emicizumab to Bridge Drug Products and Subcutaneous Injection Sites in Healthy Volunteers Abstract Abstract Emicizumab (ACE910) is a bispecific antibody that is a novel, subcutaneously injectable treatment for patients with hemophilia A. This study assessed the relative bi...
PMC5811830
core_pubmed_pmc
Effects of Strong CYP3A Inhibition and Induction on the Pharmacokinetics of Ixazomib, an Oral Proteasome Inhibitor: Results of Drug‐Drug Interaction Studies in Patients With Advanced Solid Tumors or Lymphoma and a Physiologically Based Pharmacokinetic Analysis
Effects of Strong CYP3A Inhibition and Induction on the Pharmacokinetics of Ixazomib, an Oral Proteasome Inhibitor: Results of Drug‐Drug Interaction Studies in Patients With Advanced Solid Tumors or Lymphoma and a Physiologically Based Pharmacokinetic Analysis Abstract Abstract At clinically relevant ixazomib concentra...
PMC9135852
core_pubmed_pmc
Comparison of docetaxel pharmacokinetics between castration-resistant and hormone-sensitive metastatic prostate cancer patients
Comparison of docetaxel pharmacokinetics between castration-resistant and hormone-sensitive metastatic prostate cancer patients Abstract Abstract Purpose Recently, docetaxel treatment of metastatic prostate cancer patients shifted towards the hormone-sensitive stage of the disease. There are contradictive reports on di...
PMC8253284
core_pubmed_pmc
Guidelines for clinical evaluation of anti‐cancer drugs
Guidelines for clinical evaluation of anti‐cancer drugs Abstract Abstract Clinical studies intended for regulatory approval must demonstrate the clinical benefits of the drug in a target population. Clinical development of a drug proceeds by stepwise clinical studies; after safety and pharmacokinetics are evaluated and...
PMC3019387
core_pubmed_pmc
A Study on Drug-Drug Interaction of Esomeprazole and Anti-Diabetic Drugs
A Study on Drug-Drug Interaction of Esomeprazole and Anti-Diabetic Drugs Abstract Drug–drug interaction between esomeprazole at therapeutic and higher doses and sulfonylureas was studied. Sulfonylureas (tolbutamide 40 mg/kg and glibenclamide 40 µg/kg) were administered and the time to onset of hypoglycemia, the duratio...
PMC11871391
core_pubmed_pmc
Pharmacological characteristics of once‐weekly insulin icodec in Japanese individuals with type 1 diabetes
Pharmacological characteristics of once‐weekly insulin icodec in Japanese individuals with type 1 diabetes Abstract ABSTRACT Introduction Insulin icodec is a basal insulin designed for once‐weekly administration. This study assessed the pharmacological properties of icodec in Japanese individuals with type 1 diabetes (...
PMC9553667
core_pubmed_pmc
Pharmacokinetic Analysis of Diosgenin in Rat Plasma by a UPLC-MS/MS Approach
Pharmacokinetic Analysis of Diosgenin in Rat Plasma by a UPLC-MS/MS Approach Abstract Abstract Diosgenin, a steroidal sapogenin, has attracted attention worldwide owing to its pharmacological properties, including antitumor, cardiovascular protective, hypolipidemic, and anti-inflammatory effects. The current diosgenin ...
PMC9228185
core_pubmed_pmc
Accurate Mass Identification of an Interfering Water Adduct and Strategies in Development and Validation of an LC-MS/MS Method for Quantification of MPI8, a Potent SARS-CoV-2 Main Protease Inhibitor, in Rat Plasma in Pharmacokinetic Studies
Accurate Mass Identification of an Interfering Water Adduct and Strategies in Development and Validation of an LC-MS/MS Method for Quantification of MPI8, a Potent SARS-CoV-2 Main Protease Inhibitor, in Rat Plasma in Pharmacokinetic Studies Abstract Abstract MPI8, a peptidyl aldehyde, is a potent antiviral agent agains...
PMC6009946
core_pubmed_pmc
Phase Ia study of the indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor navoximod (GDC-0919) in patients with recurrent advanced solid tumors
Phase Ia study of the indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor navoximod (GDC-0919) in patients with recurrent advanced solid tumors Abstract Background Indoleamine-2,3-dioxygenase 1 (IDO1) catalyzes the oxidation of tryptophan into kynurenine and is partially responsible for acquired immune tolerance associated ...
PMC6478707
core_pubmed_pmc
Simultaneous Determination of Selegiline, Desmethylselegiline, R/S-methamphetamine, and R/S-amphetamine on Dried Urine Spots by LC/MS/MS: Application to a Pharmacokinetic Study in Urine
Simultaneous Determination of Selegiline, Desmethylselegiline, R/S-methamphetamine, and R/S-amphetamine on Dried Urine Spots by LC/MS/MS: Application to a Pharmacokinetic Study in Urine Abstract Objective: Chiral analysis is a crucial method to differentiate selegiline intake from drug abuse. A dried urine spot (DUS) a...
PMC6130577
core_pubmed_pmc
Rational screening of peroxisome proliferator-activated receptor-γ agonists from natural products: potential therapeutics for heart failure
Rational screening of peroxisome proliferator-activated receptor-γ agonists from natural products: potential therapeutics for heart failure Abstract Abstract Context: Peroxisome proliferator-activated receptor-γ (PPARγ) is a member of the nuclear hormone receptor superfamily of ligand-activated transcription factors. A...
PMC8107152
core_pubmed_pmc
Fixed Dose of Cemiplimab in Patients with Advanced Malignancies Based on Population Pharmacokinetic Analysis
Fixed Dose of Cemiplimab in Patients with Advanced Malignancies Based on Population Pharmacokinetic Analysis Abstract Introduction This study outlined cemiplimab intravenous (IV) dosing strategy to move from body weight (BW)-based 3 mg/kg every-2-week (Q2W) dosing in first-in-human study (study 1423; NCT02383212 ) to f...
PMC6602180
core_pubmed_pmc
Mathematical models for cytarabine-derived myelosuppression in acute myeloid leukaemia
Mathematical models for cytarabine-derived myelosuppression in acute myeloid leukaemia Abstract Abstract We investigate the personalisation and prediction accuracy of mathematical models for white blood cell (WBC) count dynamics during consolidation treatment using intermediate or high-dose cytarabine (Ara-C) in acute ...
PMC11757988
core_pubmed_pmc
QbD-Driven preparation, characterization, and pharmacokinetic investigation of daidzein-l oaded nano-cargos of hydroxyapatite
QbD-Driven preparation, characterization, and pharmacokinetic investigation of daidzein-l oaded nano-cargos of hydroxyapatite Abstract Abstract The repercussions of hormone replacement therapy (HRT) and bisphosphonates pose serious clinical challenges and warrant novel therapies for osteoporosis in menopausal women. To...
PMC10701866
core_pubmed_pmc
Characterization of Sesuvium sesuvioides Using High-Performance Liquid Chromatography and Validation of Its In Vivo Anti-hyperthyroidism Effect via Suppressing Oxidative Stress and Inflammatory Markers
Characterization of Sesuvium sesuvioides Using High-Performance Liquid Chromatography and Validation of Its In Vivo Anti-hyperthyroidism Effect via Suppressing Oxidative Stress and Inflammatory Markers Abstract Sesuvium sesuvioides was used to treat inflammation, arthritis, gout, and thyroid dysfunction. The current st...
PMC8688421
core_pubmed_pmc
The activation fragment of PAR2 is elevated in serum from patients with rheumatoid arthritis and reduced in response to anti-IL6R treatment
The activation fragment of PAR2 is elevated in serum from patients with rheumatoid arthritis and reduced in response to anti-IL6R treatment Abstract Osteoarthritis (OA) and rheumatoid arthritis (RA) are serious and painful diseases. Protease-activated receptor 2 (PAR2) is involved in the pathology of both OA and RA inc...
PMC10871121
core_pubmed_pmc
Marine-Derived Compounds as Potential Inhibitors of Hsp90 for Anticancer and Antimicrobial Drug Development: A Comprehensive In Silico Study
Marine-Derived Compounds as Potential Inhibitors of Hsp90 for Anticancer and Antimicrobial Drug Development: A Comprehensive In Silico Study Abstract Marine compounds constitute a diverse and invaluable resource for the discovery of bioactive substances with promising applications in the pharmaceutical development of a...
PMC9596707
core_pubmed_pmc
Engineering of HIV-1 neutralizing antibody CAP256V2LS for manufacturability and improved half life
Engineering of HIV-1 neutralizing antibody CAP256V2LS for manufacturability and improved half life Abstract Abstract The broadly neutralizing antibody (bNAb) CAP256-VRC26.25 has exceptional potency against HIV-1 and has been considered for clinical use. During the characterization and production of this bNAb, we observ...
PMC9313840
core_pubmed_pmc
Liquid Biopsy for Patient Characterization in Cardiovascular Disease: Verification against Markers of Cytochrome P450 and P‐Glycoprotein Activities
Liquid Biopsy for Patient Characterization in Cardiovascular Disease: Verification against Markers of Cytochrome P450 and P‐Glycoprotein Activities Abstract Abstract Precision dosing strategies require accounting for between‐patient variability in pharmacokinetics together with subsequent pharmacodynamic differences. L...
PMC9578421
core_pubmed_pmc
A Systems-Based Analysis of Mono- and Combination Therapy for Carbapenem-Resistant Klebsiella pneumoniae Bloodstream Infections
A Systems-Based Analysis of Mono- and Combination Therapy for Carbapenem-Resistant Klebsiella pneumoniae Bloodstream Infections Abstract ABSTRACT Antimicrobial resistance is a global threat. As “proof-of-concept,” we employed a system-based approach to identify patient, bacterial, and drug variables contributing to mor...
PMC11358568
core_pubmed_pmc
Evaluation of FVIII pharmacokinetic profiles in Korean hemophilia A patients assessed with myPKFiT: a retrospective chart review
Evaluation of FVIII pharmacokinetic profiles in Korean hemophilia A patients assessed with myPKFiT: a retrospective chart review Abstract Purpose This study aimed to investigate the pharmacokinetics (PK) of factor VIII (FVIII) in Korean patients, as limited information is available on the PK of FVIII in this population...
PMC12695885
core_pubmed_pmc
Optimization of thrombopoietin mimetic peptide fusion proteins with albumin-binding domain for enhanced bioactivity and extended half-life
Optimization of thrombopoietin mimetic peptide fusion proteins with albumin-binding domain for enhanced bioactivity and extended half-life Abstract Primary immune thrombocytopenia is an autoimmune disorder marked by accelerated platelet destruction and reduced production, posing risks of severe bleeding and mortality. ...
PMC9302630
core_pubmed_pmc
Mechanistic Modeling of Primaquine Pharmacokinetics, Gametocytocidal Activity, and Mosquito Infectivity
Mechanistic Modeling of Primaquine Pharmacokinetics, Gametocytocidal Activity, and Mosquito Infectivity Abstract Abstract Clinical studies have shown that adding a single 0.25 mg base/kg dose of primaquine to standard antimalarial regimens rapidly sterilizes Plasmodium falciparum gametocytes. However, the mechanism of ...
PMC7859673
core_pubmed_pmc
Microengineered systems with iPSC-derived cardiac and hepatic cells to evaluate drug adverse effects
Microengineered systems with iPSC-derived cardiac and hepatic cells to evaluate drug adverse effects Abstract Abstract Hepatic and cardiac drug adverse effects are among the leading causes of attrition in drug development programs, in part due to predictive failures of current animal or in vitro models. Hepatocytes and...
PMC3172894
core_pubmed_pmc
A randomised, phase II study of intetumumab, an anti- α v -integrin mAb, alone and with dacarbazine in stage IV melanoma
A randomised, phase II study of intetumumab, an anti- α v -integrin mAb, alone and with dacarbazine in stage IV melanoma Abstract Background: α v integrins are involved in angiogenesis and melanoma tumourigenesis. Intetumumab (CNTO 95) is a fully human anti- α v -integrin monoclonal antibody. Methods: In a multicentre,...
PMC11579100
core_pubmed_pmc
Computing optimal drug dosing regarding efficacy and safety: the enhanced OptiDose method in NONMEM
Computing optimal drug dosing regarding efficacy and safety: the enhanced OptiDose method in NONMEM Abstract Recently, an optimal dosing algorithm (OptiDose) was developed to compute the optimal drug doses for any pharmacometrics model for a given dosing scenario. In the present work, we enhance the OptiDose concept to...
PMC7447503
core_pubmed_pmc
The “Warrior” system: a new useful emergency simulator to train clinical pharmacists in emergency medicine
The “Warrior” system: a new useful emergency simulator to train clinical pharmacists in emergency medicine Abstract Abstract Clinical pharmacists are indispensable providers of emergency medical services. However, the training of Chinese clinical pharmacists in medical emergency skills is apparently insufficient. The c...
PMC6416235
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Properties of l -Ornithine l -Aspartate (LOLA) in Hepatic Encephalopathy
Pharmacokinetic and Pharmacodynamic Properties of l -Ornithine l -Aspartate (LOLA) in Hepatic Encephalopathy Abstract l -Ornithine l -aspartate (LOLA), a stable salt of l -ornithine and l -aspartate, readily dissociates into its constituent amino acids that are readily absorbed by active transport, distributed, and met...
PMC11964075
core_pubmed_pmc
Dosing and Safety Profile of Aficamten in Symptomatic Obstructive Hypertrophic Cardiomyopathy: Results From SEQUOIA‐HCM
Dosing and Safety Profile of Aficamten in Symptomatic Obstructive Hypertrophic Cardiomyopathy: Results From SEQUOIA‐HCM Abstract Abstract Background Aficamten, a novel cardiac myosin inhibitor, reversibly reduces cardiac hypercontractility in obstructive hypertrophic cardiomyopathy. We present a prespecified analysis o...
PMC10508722
core_pubmed_pmc
Efficient ultrasound-mediated drug delivery to orthotopic liver tumors – Direct comparison of doxorubicin-loaded nanobubbles and microbubbles
Efficient ultrasound-mediated drug delivery to orthotopic liver tumors – Direct comparison of doxorubicin-loaded nanobubbles and microbubbles Abstract Liver metastasis is a major obstacle in treating aggressive cancers, and current therapeutic options often prove insufficient. To overcome these challenges, there has be...
PMC9036243
core_pubmed_pmc
A Physiologically Based Pharmacokinetic Framework for Quantifying Antibody Distribution Gradients from Tumors to Tumor-Draining Lymph Nodes
A Physiologically Based Pharmacokinetic Framework for Quantifying Antibody Distribution Gradients from Tumors to Tumor-Draining Lymph Nodes Abstract Immune checkpoint blockades prescribed in the neoadjuvant setting are now under active investigation for many types of tumors, and many have shown early success. The prima...
PMC8830998
core_pubmed_pmc
Meta-Analysis of Drug Delivery Approaches for Treating Intracellular Infections
Meta-Analysis of Drug Delivery Approaches for Treating Intracellular Infections Abstract Abstract This meta-analysis aims to evaluate the trend, methodological quality and completeness of studies on intracellular delivery of antimicrobial agents. PubMed, Embase, and reference lists of related reviews were searched to i...
PMC2872310
core_pubmed_pmc
A New View of Alcohol Metabolism and Alcoholism—Role of the High- K m Class III Alcohol Dehydrogenase (ADH3)
A New View of Alcohol Metabolism and Alcoholism—Role of the High- K m Class III Alcohol Dehydrogenase (ADH3) Abstract Abstract The conventional view is that alcohol metabolism is carried out by ADH1 (Class I) in the liver. However, it has been suggested that another pathway plays an important role in alcohol metabolism...
PMC4128066
core_pubmed_pmc
Modulation of imidazoline I 2 binding sites by CR4056 relieves postoperative hyperalgesia in male and female rats
Modulation of imidazoline I 2 binding sites by CR4056 relieves postoperative hyperalgesia in male and female rats Abstract Background and Purpose CR4056 is a novel imidazoline-2 (I 2 ) ligand exhibiting potent analgesic activity in animal models of pain. In this study, we investigated the effects of CR4056 in a well-es...
PMC4199218
core_pubmed_pmc
Comparison of Two Clinical Protocols for Total Intravenous Anesthesia (TIVA) for Breast Surgery Using Propofol Combined With Either Sufentanil or Alfentanil
Comparison of Two Clinical Protocols for Total Intravenous Anesthesia (TIVA) for Breast Surgery Using Propofol Combined With Either Sufentanil or Alfentanil Abstract Abstract Background: Sufentanil and alfentanil have pharmacokinetic and dynamic properties which make them favourable substances for total intravenous ane...
PMC6380433
core_pubmed_pmc
Single cell-produced and in vitro -assembled anti-FcRH5/CD3 T-cell dependent bispecific antibodies have similar in vitro and in vivo properties
Single cell-produced and in vitro -assembled anti-FcRH5/CD3 T-cell dependent bispecific antibodies have similar in vitro and in vivo properties Abstract ABSTRACT Bispecific antibody production using single host cells has been a new advancement in the antibody engineering field. We previously showed comparable in vitro ...
PMC11992666
core_pubmed_pmc
Recommended approaches for integration of population pharmacokinetic modelling with precision dosing in clinical practice
Recommended approaches for integration of population pharmacokinetic modelling with precision dosing in clinical practice Abstract Abstract Current methods of dose determination have contributed to suboptimal and inequitable health outcomes in underrepresented patient populations. The persistent demand to individualise...
PMC11971068
core_pubmed_pmc
Efficacy and Safety of 611 in Chinese Adults with Moderate-to-Severe Atopic Dermatitis: Results from a Phase II Trial
Efficacy and Safety of 611 in Chinese Adults with Moderate-to-Severe Atopic Dermatitis: Results from a Phase II Trial Abstract Introduction Atopic dermatitis (AD) is a chronic inflammatory skin disease. 611, a humanized monoclonal antibody, selectively targets the interleukin (IL)-4 receptor alpha, thereby inhibiting t...
PMC11395065
core_pubmed_pmc
Computational Screening of T-Muurolol for an Alternative Antibacterial Solution against Staphylococcus aureus Infections: An In Silico Approach for Phytochemical-Based Drug Discovery
Computational Screening of T-Muurolol for an Alternative Antibacterial Solution against Staphylococcus aureus Infections: An In Silico Approach for Phytochemical-Based Drug Discovery Abstract Abstract Staphylococcus aureus infections present a significant threat to the global healthcare system. The increasing resistanc...
PMC11538898
core_pubmed_pmc
Inetetamab for injection in combination with vinorelbine weekly or every three weeks in HER2-positive metastatic breast cancer: A multicenter, randomized, phase II clinical trial
Inetetamab for injection in combination with vinorelbine weekly or every three weeks in HER2-positive metastatic breast cancer: A multicenter, randomized, phase II clinical trial Abstract Abstract Objective We aimed to investigate the pharmacokinetics, safety, efficacy, and immunogenicity of different dosing regimens (...
PMC11280007
core_pubmed_pmc
Development of a Clonal and High-Yield Mammalian Cell Line for the Manufacturing of a Hyperactive Human DNase I with Extended Plasma Half-Life Using PASylation ® Technology
Development of a Clonal and High-Yield Mammalian Cell Line for the Manufacturing of a Hyperactive Human DNase I with Extended Plasma Half-Life Using PASylation ® Technology Abstract Abstract Cumulative evidence from several pre-clinical studies suggests that restoration of plasma DNase activity in a thrombo-inflammator...
PMC10708954
core_pubmed_pmc
Exploring the Effect of Compound Glycyrrhizin and Silybinin on the Metabolism of Pexidartinib in Rats Based on CYP3A4 and CYP2C9
Exploring the Effect of Compound Glycyrrhizin and Silybinin on the Metabolism of Pexidartinib in Rats Based on CYP3A4 and CYP2C9 Abstract Abstract Pexidartinib offered a new therapeutic option for adult patients with symptomatic tenosynovial giant cell tumor (TGCT) who were refractory to surgical treatment and had seve...
PMC6978557
core_pubmed_pmc
Pharmacodynamic Effects of Vorapaxar in Patients With and Without Diabetes Mellitus
Pharmacodynamic Effects of Vorapaxar in Patients With and Without Diabetes Mellitus Abstract Highlights • Vorapaxar reduces thrombotic cardiovascular events in patients with atherosclerotic disease, with enhanced effects in those with DM. • Adjunctive vorapaxar therapy reduces platelet-mediated thrombogenicity without ...
PMC9381898
core_pubmed_pmc
Finding the right hazard function for time‐to‐event modeling: A tutorial and Shiny application
Finding the right hazard function for time‐to‐event modeling: A tutorial and Shiny application Abstract Abstract Parametric time‐to‐event analysis is an important pharmacometric method to predict the probability of an event up until a certain time as a function of covariates and/or drug exposure. Modeling is performed ...
PMC8933379
core_pubmed_pmc
Evaluation of the absolute oral bioavailability of the anaplastic lymphoma kinase/c-ROS oncogene 1 kinase inhibitor lorlatinib in healthy participants
Evaluation of the absolute oral bioavailability of the anaplastic lymphoma kinase/c-ROS oncogene 1 kinase inhibitor lorlatinib in healthy participants Abstract Purpose Lorlatinib is a third-generation tyrosine kinase inhibitor currently approved for the treatment of anaplastic lymphoma kinase (ALK)-positive metastatic ...
PMC4076804
core_pubmed_pmc
Model-Based Optimal Design and Execution of the First-Inpatient Trial of the Anti-IL-6, Olokizumab
Model-Based Optimal Design and Execution of the First-Inpatient Trial of the Anti-IL-6, Olokizumab Abstract The first-in-patient study for olokizumab (OKZ) employed model-based, optimal design and adaptive execution to define the concentration–C-reactive protein (CRP) suppression response. Modeling and exploratory stat...
PMC9217727
core_pubmed_pmc
A randomised, open-label, cross-over clinical study to evaluate the pharmacokinetic, pharmacodynamic and safety and tolerability profiles of tobacco-free oral nicotine pouches relative to cigarettes
A randomised, open-label, cross-over clinical study to evaluate the pharmacokinetic, pharmacodynamic and safety and tolerability profiles of tobacco-free oral nicotine pouches relative to cigarettes Abstract Abstract Rationale Tobacco harm reduction (THR) involves encouraging adult smokers who would otherwise continue ...
PMC12389438
core_pubmed_pmc
Personalized Neonatal Therapy: Application of Magistral Formulas in Therapeutic Orphan Populations
Personalized Neonatal Therapy: Application of Magistral Formulas in Therapeutic Orphan Populations Abstract This review explores the potential of magistral formulas (MFs) as a viable option to meet the needs of neonates, given the lack of adequate therapies for this vulnerable group. The scientific literature on medici...
PMC7304110
core_pubmed_pmc
Optimal dosing time of Dachengqi decoction for protection of extrapancreatic organs in rats with experimental acute pancreatitis
Optimal dosing time of Dachengqi decoction for protection of extrapancreatic organs in rats with experimental acute pancreatitis Abstract Abstract BACKGROUND Acute pancreatitis (AP) is a pancreatic inflammatory disorder that is commonly complicated by extrapancreatic organ dysfunction. Dachengqi decoction (DCQD) has a ...
PMC12890151
core_pubmed_pmc
Coupled pharmacokinetic model unveils drug-drug interactions in plasma concentration
Coupled pharmacokinetic model unveils drug-drug interactions in plasma concentration Abstract In oral drug pharmacokinetics (PK), drug-drug interactions are inevitable, yet traditional compartmental models struggle to effectively quantify such processes. This study proposes a linearly coupled two-compartment PK model, ...
PMC12143955
core_pubmed_pmc
Potential Therapeutic Efficacy of Ferulic Acid and Its Derivatives in the Management of Cancers: A Comprehensive Analysis With Mechanistic Insight
Potential Therapeutic Efficacy of Ferulic Acid and Its Derivatives in the Management of Cancers: A Comprehensive Analysis With Mechanistic Insight Abstract Abstract Due to the increasing rate of cancer and the undesirable consequences of manufactured drugs, there is a growing interest in the development of natural prod...
PMC3427893
core_pubmed_pmc
A Novel Long-Acting Human Growth Hormone Fusion Protein (VRS-317): Enhanced In Vivo Potency and Half-Life
A Novel Long-Acting Human Growth Hormone Fusion Protein (VRS-317): Enhanced In Vivo Potency and Half-Life Abstract Abstract A novel recombinant human growth hormone (rhGH) fusion protein (VRS-317) was designed to minimize receptor-mediated clearance through a reduction in receptor binding without mutations to rhGH by g...
PMC8076219
core_pubmed_pmc
Effect of four ABCB1 genetic polymorphisms on the accumulation of darunavir in HEK293 recombinant cell lines
Effect of four ABCB1 genetic polymorphisms on the accumulation of darunavir in HEK293 recombinant cell lines Abstract The intracellular penetration of darunavir, a second-generation HIV protease inhibitor, is limited by the activity of the efflux P-glycoprotein (ABCB1). ABCB1 expression and/or activity levels can vary ...
PMC7463457
core_pubmed_pmc
The Application of Inosine 5′-Monophosphate Dehydrogenase Activity Determination in Peripheral Blood Mononuclear Cells for Monitoring Mycophenolate Mofetil Therapy in Children with Nephrotic Syndrome
The Application of Inosine 5′-Monophosphate Dehydrogenase Activity Determination in Peripheral Blood Mononuclear Cells for Monitoring Mycophenolate Mofetil Therapy in Children with Nephrotic Syndrome Abstract Abstract In pediatric nephrotic syndrome, recommended mycophenolic acid (MPA) pharmacokinetics are higher than ...
PMC7878185
core_pubmed_pmc
Mass balance and pharmacokinetics of an oral dose of 14 C‐napabucasin in healthy adult male subjects
Mass balance and pharmacokinetics of an oral dose of 14 C‐napabucasin in healthy adult male subjects Abstract Abstract This phase 1, open‐label study assessed 14 C‐napabucasin absorption, metabolism, and excretion, napabucasin pharmacokinetics, and napabucasin metabolites (primary objectives); safety/tolerability were ...
PMC10215091
core_pubmed_pmc
Clinical Equivalence between Generic Versus Branded Antibiotics: Systematic Review and Meta-Analysis
Clinical Equivalence between Generic Versus Branded Antibiotics: Systematic Review and Meta-Analysis Abstract Regulatory authorities authorize the clinical use of generic drugs (GD) based on bioequivalence studies, which consist of the evaluation of pharmacokinetics after a single dose in vitro or in healthy individual...
PMC11098154
core_pubmed_pmc
Development of a physiologically‐based pharmacokinetic model to simulate the pharmacokinetics of intramuscular antiretroviral drugs
Development of a physiologically‐based pharmacokinetic model to simulate the pharmacokinetics of intramuscular antiretroviral drugs Abstract Abstract There is growing interest in the use of long‐acting (LA) injectable drugs to improve treatment adherence. However, their long elimination half‐life complicates the conduc...
PMC8420371
core_pubmed_pmc
Anti–SARS‐CoV‐2 Repurposing Drug Database: Clinical Pharmacology Considerations
Anti–SARS‐CoV‐2 Repurposing Drug Database: Clinical Pharmacology Considerations Abstract Abstract A critical step to evaluate the potential in vivo antiviral activity of a drug is to connect the in vivo exposure to its in vitro antiviral activity. The Anti–SARS‐CoV‐2 Repurposing Drug Database is a database that include...
PMC11845114
core_pubmed_pmc
Comprehensive Performance Evaluation of Ligand-Binding Assay–LC–MS/MS Method for Co-Dosed Monoclonal Anti-SARS-CoV-2 Antibodies (AZD7442)
Comprehensive Performance Evaluation of Ligand-Binding Assay–LC–MS/MS Method for Co-Dosed Monoclonal Anti-SARS-CoV-2 Antibodies (AZD7442) Abstract Abstract Aims: AZD7442 is a combination SARS-CoV-2 therapy comprising two co-dosed monoclonal antibodies. Materials & methods: The authors validated a hybrid ligand-binding ...
PMC7689764
core_pubmed_pmc
Application of Physiologically Based Pharmacokinetic Modeling to Predict Drug Exposure and Support Dosing Recommendations for Potential Drug‐Drug Interactions or in Special Populations: An Example Using Tofacitinib
Application of Physiologically Based Pharmacokinetic Modeling to Predict Drug Exposure and Support Dosing Recommendations for Potential Drug‐Drug Interactions or in Special Populations: An Example Using Tofacitinib Abstract Abstract Tofacitinib is an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis...
PMC12030177
core_pubmed_pmc
Fluconazole Dosing for the Prevention of Candida spp. Infections in Hemato-Oncologic Pediatric Patients: Population Pharmacokinetic Modeling and Probability of Target Attainment Simulations
Fluconazole Dosing for the Prevention of Candida spp. Infections in Hemato-Oncologic Pediatric Patients: Population Pharmacokinetic Modeling and Probability of Target Attainment Simulations Abstract Objectives : A population pharmacokinetic (popPK) model was used to evaluate fluconazole dosing regimens for Candida spp....
PMC11866507
core_pubmed_pmc
Pharmacokinetic modeling of prenatal vitamin D exposure and the impact on offspring asthma and pulmonary function
Pharmacokinetic modeling of prenatal vitamin D exposure and the impact on offspring asthma and pulmonary function Abstract Gestational 25-hydroxyvitamin D (25[OH]D) is important in fetal lung development and may influence offspring respiratory outcomes, making accurate exposure assessment essential to understand clinic...
PMC12439007
core_pubmed_pmc
Use of PopPK and E‐R Analyses toward Explaining Causal Link Between ADAMTS13 in Recombinant vs. Plasma‐Based Therapies and Clinical Effects in cTTP
Use of PopPK and E‐R Analyses toward Explaining Causal Link Between ADAMTS13 in Recombinant vs. Plasma‐Based Therapies and Clinical Effects in cTTP Abstract Congenital thrombotic thrombocytopenic purpura (cTTP) is an ultra‐rare, potentially life‐threatening condition caused by a deficiency of the blood enzyme ADAMTS13....
PMC9401156
core_pubmed_pmc
Comparative pharmacokinetics of valproic acid among Pakistani and South Korean patients: A population pharmacokinetic study
Comparative pharmacokinetics of valproic acid among Pakistani and South Korean patients: A population pharmacokinetic study Abstract Purpose The pharmacokinetics of valproic acid have been evaluated in a variety of populations however, the comparison in two different populations was yet to be reported. This study is ai...
PMC11823647
core_pubmed_pmc
Single-dose tolerability and pharmacokinetics of leritrelvir in Chinese patients with hepatic impairment and healthy matched controls
Single-dose tolerability and pharmacokinetics of leritrelvir in Chinese patients with hepatic impairment and healthy matched controls Abstract ABSTRACT This study evaluated the safety and pharmacokinetics (PK) of a single dose of leritrelvir, a novel inhibitor of 3-chymotrypsin-like cysteine protease (3CLpro), in patie...
PMC12567310
core_pubmed_pmc
Pharmacometrics in the Age of Large Language Models: A Vision of the Future
Pharmacometrics in the Age of Large Language Models: A Vision of the Future Abstract Abstract Background : Large Language Models (LLMs) have driven significant advances in artificial intelligence (AI), with transformative applications across numerous scientific fields, including biomedical research and drug development...
PMC12210708
core_pubmed_pmc
Comparative analysis of safety and efficacy between brand and generic lamotrigine products in the Saudi market
Comparative analysis of safety and efficacy between brand and generic lamotrigine products in the Saudi market Abstract Abstract Background Epilepsy is one of the most chronic neurological disorders worldwide. In 2023, the World Health Organization (WHO) estimates that approximately 50 million individuals globally woul...
PMC11823460
core_pubmed_pmc
Safety, Tolerability and Pharmacokinetics of the eNAMPT-Neutralizing ALT-100 Mab in Healthy Volunteers
Safety, Tolerability and Pharmacokinetics of the eNAMPT-Neutralizing ALT-100 Mab in Healthy Volunteers Abstract Introduction: Human and preclinical studies have highlighted eNAMPT (extracellular nicotinamide phosphoribosyl transferase) as a druggable TLR4 ligand and DAMP involved in the pathobiology of diverse inflamma...
PMC6854015
core_pubmed_pmc
In vitro Cytotoxicity and Pharmacokinetic Evaluation of Pharmacological Ascorbate in Dogs
In vitro Cytotoxicity and Pharmacokinetic Evaluation of Pharmacological Ascorbate in Dogs Abstract Abstract Background: High-dose, pharmacological ascorbate (P-AscH − ) is preferentially cytotoxic to human cancer cells in vitro . Investigations on the efficacy of P-AscH − as an adjuvant treatment for multiple human can...
PMC9633870
core_pubmed_pmc
Denosumab biosimilar (LY06006) in Chinese postmenopausal osteoporotic women: A randomized, double-blind, placebo-controlled, multicenter phase III study
Denosumab biosimilar (LY06006) in Chinese postmenopausal osteoporotic women: A randomized, double-blind, placebo-controlled, multicenter phase III study Abstract Abstract Objectives This study assessed the efficacy, safety, pharmacokinetics (PK), and immunogenicity profiles of a denosumab biosimilar (LY06006) in Chines...
PMC8427072
core_pubmed_pmc
Adverse Drug Reactions of Acetylcholinesterase Inhibitors in Older People Living with Dementia: A Comprehensive Literature Review
Adverse Drug Reactions of Acetylcholinesterase Inhibitors in Older People Living with Dementia: A Comprehensive Literature Review Abstract Abstract The rising of global geriatric population has contributed to increased prevalence of dementia. Dementia is a neurodegenerative disease, which is characterized by progressiv...
PMC10308769
core_pubmed_pmc
First reported double drug–drug interaction in a cancer renal patient under everolimus treatment: therapeutic drug monitoring and review of literature
First reported double drug–drug interaction in a cancer renal patient under everolimus treatment: therapeutic drug monitoring and review of literature Abstract Everolimus is an inhibitor of mammalian target of rapamycin (mTOR) used in both transplantation and cancer treatment (breast, renal and neuroendocrine). In tran...
PMC7584691
core_pubmed_pmc
The Effect of Low-Dose Ticagrelor on Platelet Function Profiles in Patients With Stable Coronary Artery Disease in Trinidad: The TWIST Pilot Study
The Effect of Low-Dose Ticagrelor on Platelet Function Profiles in Patients With Stable Coronary Artery Disease in Trinidad: The TWIST Pilot Study Abstract Abstract Introduction This prospective, pharmacodynamic study aimed to explore the potential applicability of a low-dose ticagrelor regimen in a heterogeneous Trini...
PMC8906567
core_pubmed_pmc
Case Report: Atypical HUS Presenting With Acute Rhabdomyolysis Highlights the Need for Individualized Eculizumab Dosing
Case Report: Atypical HUS Presenting With Acute Rhabdomyolysis Highlights the Need for Individualized Eculizumab Dosing Abstract Abstract Background Atypical hemolytic uremic syndrome (aHUS) is an ultra-rare orphan disease caused by dysregulated complement activation resulting in thrombotic microangiopathy. Although co...
PMC12014330
core_pubmed_pmc
Intrathecal administration of Anti-Nogo-A antibody in macaque monkeys: Pharmacokinetics, tissue penetration and target interaction
Intrathecal administration of Anti-Nogo-A antibody in macaque monkeys: Pharmacokinetics, tissue penetration and target interaction Abstract Abstract Intrathecal drug administration represents a promising method to deliver biologics effectively to the central nervous system (CNS). However, little is known about the tole...
PMC5165030
core_pubmed_pmc
Integration of pharmacometabolomics with pharmacokinetics and pharmacodynamics: towards personalized drug therapy
Integration of pharmacometabolomics with pharmacokinetics and pharmacodynamics: towards personalized drug therapy Abstract Abstract Personalized medicine, in modern drug therapy, aims at a tailored drug treatment accounting for inter-individual variations in drug pharmacology to treat individuals effectively and safely...
PMC8240349
core_pubmed_pmc
Phase I clinical trial to evaluate the safety and pharmacokinetics of capsule formulation of the standardized extract of Atractylodes lancea
Phase I clinical trial to evaluate the safety and pharmacokinetics of capsule formulation of the standardized extract of Atractylodes lancea Abstract Background and aim Atractylodes lancea (AL) has been demonstrated in a series of studies to be a potential candidate for the treatment of cholangiocarcinoma. The aim of t...
PMC11522854
core_pubmed_pmc
Pharmacokinetics and bioequivalence of two formulations of mifepristone tablets in healthy Chinese subjects under fasting conditions: a single-center, open, randomized, single-dose, double-period, two-sequence, crossover trial
Pharmacokinetics and bioequivalence of two formulations of mifepristone tablets in healthy Chinese subjects under fasting conditions: a single-center, open, randomized, single-dose, double-period, two-sequence, crossover trial Abstract Abstract Objective A bioequivalence (BE) study was performed to evaluate the pharmac...
PMC9366215
core_pubmed_pmc
A temporo-spatial pharmacometabolomics method to characterize pharmacokinetics and pharmacodynamics in the brain microregions by using ambient mass spectrometry imaging
A temporo-spatial pharmacometabolomics method to characterize pharmacokinetics and pharmacodynamics in the brain microregions by using ambient mass spectrometry imaging Abstract Abstract The brain is the most advanced organ with various complex structural and functional microregions. It is often challenging to understa...
PMC10312293
core_pubmed_pmc
Double-Blind, Placebo-Controlled Study of Bezlotoxumab in Children Receiving Antibacterial Treatment for Clostridioides difficile Infection (MODIFY III)
Double-Blind, Placebo-Controlled Study of Bezlotoxumab in Children Receiving Antibacterial Treatment for Clostridioides difficile Infection (MODIFY III) Abstract Abstract Background Therapies to prevent recurrence of Clostridioides difficile infection (CDI) in pediatric patients are needed. Bezlotoxumab is a fully huma...
PMC3827223
core_pubmed_pmc
Bioorthogonal Small Molecule Imaging Agents Allow Single-Cell Imaging of MET
Bioorthogonal Small Molecule Imaging Agents Allow Single-Cell Imaging of MET Abstract The hepatocyte growth factor receptor (MET) is a receptor tyrosine kinase (RTK) that has emerged as an important cancer target. Consequently, a number of different inhibitors varying in specificity are currently in clinical developmen...
PMC9232416
core_pubmed_pmc
A Population Pharmacokinetic Model of Whole-Blood and Intracellular Tacrolimus in Kidney Transplant Recipients
A Population Pharmacokinetic Model of Whole-Blood and Intracellular Tacrolimus in Kidney Transplant Recipients Abstract Abstract Background and Objective The tacrolimus concentration within peripheral blood mononuclear cells may correlate better with clinical outcomes after transplantation compared to concentrations me...
PMC10092050
core_pubmed_pmc
Effect of Trastuzumab Deruxtecan on QT / QTc Interval and Pharmacokinetics in HER2‐Positive or HER2‐Low Metastatic/Unresectable Breast Cancer
Effect of Trastuzumab Deruxtecan on QT / QTc Interval and Pharmacokinetics in HER2‐Positive or HER2‐Low Metastatic/Unresectable Breast Cancer Abstract HER2‐targeted anticancer therapies may be associated with cardiovascular adverse events. This study evaluated effects of the HER2‐targeted antibody–drug conjugate trastu...
PMC3909222
core_pubmed_pmc
E. coli Infection Modulates the Pharmacokinetics of Oral Enrofloxacin by Targeting P-Glycoprotein in Small Intestine and CYP450 3A in Liver and Kidney of Broilers
E. coli Infection Modulates the Pharmacokinetics of Oral Enrofloxacin by Targeting P-Glycoprotein in Small Intestine and CYP450 3A in Liver and Kidney of Broilers Abstract Abstract P-glycoprotein (P-gp) expression determines the absorption, distribution, metabolism and excretion of many drugs in the body. Also, up-regu...
PMC10058973
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modelling to Predict Pharmacokinetics of Enavogliflozin, a Sodium-Dependent Glucose Transporter 2 Inhibitor, in Humans
Physiologically Based Pharmacokinetic Modelling to Predict Pharmacokinetics of Enavogliflozin, a Sodium-Dependent Glucose Transporter 2 Inhibitor, in Humans Abstract Enavogliflozin is a sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor approved for clinical use in South Korea. As SGLT2 inhibitors are a treatme...
PMC9489536
core_pubmed_pmc
Identification of a novel fusion Iduronidase with improved activity in the cardiovascular system
Identification of a novel fusion Iduronidase with improved activity in the cardiovascular system Abstract Background Lysosomal diseases are a group of over 70 rare genetic conditions in which a protein deficiency (most often an enzyme deficiency) leads to multi-system disease. Current therapies for lysosomal diseases a...
PMC4545940
core_pubmed_pmc
Molecular Design of Bisphosphonate-Modified Proteins for Efficient Bone Targeting In Vivo
Molecular Design of Bisphosphonate-Modified Proteins for Efficient Bone Targeting In Vivo Abstract Abstract To establish a rational molecular design for bisphosphonate (BP)-modified proteins for efficient bone targeting, a pharmacokinetic study was performed using a series of alendronate (ALN), a nitrogen-containing BP...
PMC12105673
core_pubmed_pmc
Itraconazole Loaded Micelle Based on Methoxy Poly(Ethylene Glycol)-Poly(D, L-Lactic Acid) for Ocular Drug Delivery: In vitro and in vivo Evaluation
Itraconazole Loaded Micelle Based on Methoxy Poly(Ethylene Glycol)-Poly(D, L-Lactic Acid) for Ocular Drug Delivery: In vitro and in vivo Evaluation Abstract Abstract Purpose This study aimed to develop itraconazole (ITZ)-loaded polymer micelles using methoxy poly(ethylene glycol)-poly(D, L-lactic acid) (mPEG-PDLLA) as ...
PMC4153964
core_pubmed_pmc
Evaluation of Pharmacokinetic Drug Interactions Between Gemigliptin (Dipeptidylpeptidase-4 Inhibitor) and Glimepiride (Sulfonylurea) in Healthy Volunteers
Evaluation of Pharmacokinetic Drug Interactions Between Gemigliptin (Dipeptidylpeptidase-4 Inhibitor) and Glimepiride (Sulfonylurea) in Healthy Volunteers Abstract Abstract Purpose Gemigliptin is approved for the treatment of type II diabetes mellitus. Sulfonylureas are commonly used in combination with other antidiabe...