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PMC6178183
core_pubmed_pmc
Development of a HPLC-MS/MS Method to Determine 11 Bioactive Compounds in Tongmai Yangxin Pill and Application to a Pharmacokinetic Study in Rats
Development of a HPLC-MS/MS Method to Determine 11 Bioactive Compounds in Tongmai Yangxin Pill and Application to a Pharmacokinetic Study in Rats Abstract Abstract A sensitive and reliable HPLC-MS/MS method has been developed and validated for simultaneous determination of eleven bioactive compounds (rhein, emodin, sti...
PMC9920503
core_pubmed_pmc
Potential Pharmacokinetic Interactions of Common Cardiovascular Drugs and Selected European and Latin American Herbal Medicines: A Scoping Review
Potential Pharmacokinetic Interactions of Common Cardiovascular Drugs and Selected European and Latin American Herbal Medicines: A Scoping Review Abstract Background: Herb–drug interactions are nowadays an important decision factor in many healthcare interventions. Patients with cardiovascular risk factors such as hype...
PMC4621921
core_pubmed_pmc
A first-in-human study of AMG 208, an oral MET inhibitor, in adult patients with advanced solid tumors
A first-in-human study of AMG 208, an oral MET inhibitor, in adult patients with advanced solid tumors Abstract Abstract Background This first-in-human study evaluated AMG 208, a small-molecule MET inhibitor, in patients with advanced solid tumors. Methods Three to nine patients were enrolled into one of seven AMG 208 ...
PMC12896376
core_pubmed_pmc
Latent Variable Indirect Response Modeling of Cendakimab Exposure–Response for Longitudinal Dysphagia Days Using a Combined Uniform‐Binomial Likelihood Framework
Latent Variable Indirect Response Modeling of Cendakimab Exposure–Response for Longitudinal Dysphagia Days Using a Combined Uniform‐Binomial Likelihood Framework Abstract ABSTRACT To characterize the relationship between cendakimab exposure and the longitudinal efficacy endpoint dysphagia days (DD), E–R analyses were p...
PMC10108266
core_pubmed_pmc
Pharmacokinetic characteristics of golidocitinib, a highly selective JAK1 inhibitor, in healthy adult participants
Pharmacokinetic characteristics of golidocitinib, a highly selective JAK1 inhibitor, in healthy adult participants Abstract Abstract Background Golidocitinib is an orally available, potent and highly selective JAK (Janus kinase)-1 inhibitor of JAK/STAT3 signaling under clinical development for the treatment of cancer a...
PMC9367477
core_pubmed_pmc
Novel Drug Delivery Method Targeting Para-Aortic Lymph Nodes by Retrograde Infusion of Paclitaxel into Pigs’ Thoracic Duct
Novel Drug Delivery Method Targeting Para-Aortic Lymph Nodes by Retrograde Infusion of Paclitaxel into Pigs’ Thoracic Duct Abstract Simple Summary For advanced cancer, surgery may not be possible at the site of lymph node metastasis, such as para-aortic lymph node metastasis. Systemic administration of anticancer drugs...
PMC10975492
core_pubmed_pmc
Forecasting Fetal Buprenorphine Exposure through Maternal–Fetal Physiologically Based Pharmacokinetic Modeling
Forecasting Fetal Buprenorphine Exposure through Maternal–Fetal Physiologically Based Pharmacokinetic Modeling Abstract Abstract Buprenorphine readily crosses the placenta, and with greater prenatal exposure, neonatal opioid withdrawal syndrome (NOWS) likely grows more severe. Current dosing strategies can be further i...
PMC10683511
core_pubmed_pmc
Zanubrutinib in Mantle Cell Lymphoma Management: A Comprehensive Review
Zanubrutinib in Mantle Cell Lymphoma Management: A Comprehensive Review Abstract Abstract Purpose The pharmacology, pharmacokinetics, pharmacodynamics, clinical efficacy, and safety of zanbrutinib are described. Summary Mantle cell lymphoma (MCL) is a mature B-cell lymphoma that is typically associated with unfavorable...
PMC6848912
core_pubmed_pmc
Population pharmacokinetics of pevonedistat alone or in combination with standard of care in patients with solid tumours or haematological malignancies
Population pharmacokinetics of pevonedistat alone or in combination with standard of care in patients with solid tumours or haematological malignancies Abstract Abstract Aims A population pharmacokinetic (PK) analysis was conducted to quantify the impact of patient‐specific and concurrent medication factors on pevonedi...
PMC12276283
core_pubmed_pmc
Modeling drug retention as memory effects in obese patients using fractional and augmented models
Modeling drug retention as memory effects in obese patients using fractional and augmented models Abstract Abstract Lipophilic anesthetic drugs accumulate in adipose tissue, leading to delayed release and prolonged effects, particularly in obese patients. This study proposes two novel physiologically motivated pharmaco...
PMC12144419
core_pubmed_pmc
Early preclinical development of Mycobacterium tuberculosis amino acid biosynthesis pathway inhibitor DRILS-1398 as a potential anti-TB drug
Early preclinical development of Mycobacterium tuberculosis amino acid biosynthesis pathway inhibitor DRILS-1398 as a potential anti-TB drug Abstract Summary The search for new anti-tubercular agents is vital for the fight against Mycobacterium tuberculosis , particularly given the rise of drug-resistant strains. DRILS...
PMC7485962
core_pubmed_pmc
A Single and Multiple Ascending Dose Study of Toll‐Like Receptor 7 Agonist (RO7020531) in Chinese Healthy Volunteers
A Single and Multiple Ascending Dose Study of Toll‐Like Receptor 7 Agonist (RO7020531) in Chinese Healthy Volunteers Abstract Toll‐like receptor 7 (TLR7) agonists modulate broad spectrum immune activity and are evaluated in the treatment of human diseases, including cancer and chronic viral infection. RO7020531, an ora...
PMC10324452
core_pubmed_pmc
Improved antibody pharmacokinetics by disruption of contiguous positive surface potential and charge reduction using alternate human framework
Improved antibody pharmacokinetics by disruption of contiguous positive surface potential and charge reduction using alternate human framework Abstract ABSTRACT Optimal pharmacokinetic (PK) properties of therapeutic monoclonal antibodies (mAbs) are essential to achieve the desired pharmacological benefits in patients. ...
PMC11619427
core_pubmed_pmc
Development of an HPLC–UV method for quantification of posaconazole in low-volume plasma samples: design of experiments and machine learning models
Development of an HPLC–UV method for quantification of posaconazole in low-volume plasma samples: design of experiments and machine learning models Abstract Abstract Posaconazole (PCZ) is a triazole antifungal agent with a broad-spectrum activity. Our research aims to present a novel approach by combining a 2-level fra...
PMC10827494
core_pubmed_pmc
An increase in urinary primaquine and a reduction in urinary primaquine-5,6-orthoquinone in the Thai population with CYP2D6 reduced enzyme function
An increase in urinary primaquine and a reduction in urinary primaquine-5,6-orthoquinone in the Thai population with CYP2D6 reduced enzyme function Abstract Abstract Objectives Primaquine is metabolized by the cytochrome P450-2D6 enzyme (CYP2D6) to an active primaquine-5,6-orthoquinone (POQ). No relationships of CYP2D6...
PMC6731456
core_pubmed_pmc
International Union of Basic and Clinical Pharmacology. CVII. Structure and Pharmacology of the Apelin Receptor with a Recommendation that Elabela/Toddler Is a Second Endogenous Peptide Ligand
International Union of Basic and Clinical Pharmacology. CVII. Structure and Pharmacology of the Apelin Receptor with a Recommendation that Elabela/Toddler Is a Second Endogenous Peptide Ligand Abstract The predicted protein encoded by the APJ gene discovered in 1993 was originally classified as a class A G protein-coup...
PMC11372835
core_pubmed_pmc
Age-Specific ADME Gene Expression in Infant Intestinal Enteroids
Age-Specific ADME Gene Expression in Infant Intestinal Enteroids Abstract Abstract In childhood, developmental changes and environmental interactions highly affect orally dosed drug disposition across the age range. To optimize dosing regimens and ensure safe use of drugs in pediatric patients, understanding this age-d...
PMC12930010
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics and safety of vutiglabridin after multiple oral administrations in healthy female and obese subjects
Pharmacokinetics, pharmacodynamics and safety of vutiglabridin after multiple oral administrations in healthy female and obese subjects Abstract Abstract Aims Vutiglabridin (HSG4112) is a novel drug under clinical development for antiobesity treatment. This study aimed to evaluate the pharmacokinetics (PKs) and safety ...
PMC4834746
core_pubmed_pmc
Metabolism of AM404 From Acetaminophen at Human Therapeutic Dosages in the Rat Brain
Metabolism of AM404 From Acetaminophen at Human Therapeutic Dosages in the Rat Brain Abstract Background: Acetaminophen, an analgesic and antipyretic drug, has been used clinically for more than a century. Previous studies showed that acetaminophen undergoes metabolic transformations to form an analgesic compound, N-(4...
PMC6507817
core_pubmed_pmc
Effects of Danshen tablets on pharmacokinetics of amlodipine in rats
Effects of Danshen tablets on pharmacokinetics of amlodipine in rats Abstract Abstract Context: Danshen tablets (DST), an effective traditional Chinese multi-herbal formula, are often combined with amlodipine (ALDP) for treating coronary heart disease. Objective: This study investigated the effects of DST on the pharma...
PMC12953123
core_pubmed_pmc
Genetic variability and response to sertraline in pediatric populations: a review on pharmacogenetics, pharmacokinetics, and the risk of adverse events
Genetic variability and response to sertraline in pediatric populations: a review on pharmacogenetics, pharmacokinetics, and the risk of adverse events Abstract Anxiety disorders in the pediatric population represent a highly prevalent mental health concern whose pharmacological management has been consolidated through...
PMC9163985
core_pubmed_pmc
Pharmacokinetic Assessment of Staphylococcal Phage K Following Parenteral and Intra-articular Administration in Rabbits
Pharmacokinetic Assessment of Staphylococcal Phage K Following Parenteral and Intra-articular Administration in Rabbits Abstract Abstract The therapeutic value of phage as an alternative to antibiotics for the treatment of bacterial infections is being considered in the wake of mounting antibiotic resistance. In this s...
PMC11253962
core_pubmed_pmc
Effect of dexamethasone pretreatment using deep learning on the surgical effect of patients with gastrointestinal tumors
Effect of dexamethasone pretreatment using deep learning on the surgical effect of patients with gastrointestinal tumors Abstract Abstract To explore the application efficacy and significance of deep learning in anesthesia management for gastrointestinal tumors (GITs) surgery, 80 elderly patients with GITs who underwen...
PMC5985193
core_pubmed_pmc
Gender Dependency in Streoselective Pharmacokinetics of Tramadol and Its Phase I Metabolites in Relation to CYP2D6 Phenotype in Iranian Population
Gender Dependency in Streoselective Pharmacokinetics of Tramadol and Its Phase I Metabolites in Relation to CYP2D6 Phenotype in Iranian Population Abstract Abstract The stereoselective pharmacokinetic of Tramadol (T) and its main metabolites concerning the influence of CYP2D6 phenotype and gender on the phase I metabol...
PMC11428226
core_pubmed_pmc
Artificial Intelligence to Close the Gap between Pharmacokinetic/Pharmacodynamic Targets and Clinical Outcomes in Critically Ill Patients: A Narrative Review on Beta Lactams
Artificial Intelligence to Close the Gap between Pharmacokinetic/Pharmacodynamic Targets and Clinical Outcomes in Critically Ill Patients: A Narrative Review on Beta Lactams Abstract Antimicrobial dosing can be a complex challenge. Although a solid rationale exists for a link between antibiotic exposure and outcome, co...
PMC3737010
core_pubmed_pmc
Ocular pharmacokinetics of bimatoprost formulated in DuraSite compared to bimatoprost 0.03% ophthalmic solution in pigmented rabbit eyes
Ocular pharmacokinetics of bimatoprost formulated in DuraSite compared to bimatoprost 0.03% ophthalmic solution in pigmented rabbit eyes Abstract Purpose To compare the aqueous humor (AH) and iris-ciliary body (ICB) concentration of bimatoprost in rabbit eyes treated with ISV-215 (0.03% bimatoprost formulated in DuraSi...
PMC12943068
core_pubmed_pmc
ADMET-Guided Design and In Silico Planning of Boron Delivery Systems for BNCT: From Transport and Biodistribution to PBPK-Informed Irradiation Windows
ADMET-Guided Design and In Silico Planning of Boron Delivery Systems for BNCT: From Transport and Biodistribution to PBPK-Informed Irradiation Windows Abstract BNCT (Boron Neutron Capture Therapy) is a binary radiotherapeutic modality in which high LET (Linear Energy Transfer) particles are generated from 10 B(n,α) 7 L...
PMC12272316
core_pubmed_pmc
Confirmation of Fixed Quarterly Riliprubart Regimen in Patients with Cold Agglutinin Disease Using Population PK/PD and Exposure‐Response Analyses
Confirmation of Fixed Quarterly Riliprubart Regimen in Patients with Cold Agglutinin Disease Using Population PK/PD and Exposure‐Response Analyses Abstract Abstract Riliprubart is a second‐generation, humanized immunoglobulin G4 that inhibits only the activated form of the C1s component of the proximal classical comple...
PMC11178655
core_pubmed_pmc
Dosimetry and pharmacokinetics of [ 177 Lu]Lu-satoreotide tetraxetan in patients with progressive neuroendocrine tumours
Dosimetry and pharmacokinetics of [ 177 Lu]Lu-satoreotide tetraxetan in patients with progressive neuroendocrine tumours Abstract Abstract Purpose To evaluate the dosimetry and pharmacokinetics of the novel radiolabelled somatostatin receptor antagonist [ 177 Lu]Lu-satoreotide tetraxetan in patients with advanced neuro...
PMC5641200
core_pubmed_pmc
A phase I study of the SRC kinase inhibitor dasatinib with trastuzumab and paclitaxel as first line therapy for patients with HER2-overexpressing advanced breast cancer. GEICAM/2010-04 study
A phase I study of the SRC kinase inhibitor dasatinib with trastuzumab and paclitaxel as first line therapy for patients with HER2-overexpressing advanced breast cancer. GEICAM/2010-04 study Abstract Abstract The anti-HER2 antibody trastuzumab have shown clinical activity in combination with chemotherapy in different b...
PMC8359354
core_pubmed_pmc
Constructing a representative in‐silico population for paediatric simulations: Application to HIV‐positive African children
Constructing a representative in‐silico population for paediatric simulations: Application to HIV‐positive African children Abstract Abstract Aims Simulations are an essential tool for investigating scenarios in pharmacokinetics‐pharmacodynamics. The models used during simulation often include the effect of highly corr...
PMC11289668
core_pubmed_pmc
Cheminformatics-based identification of phosphorylated RET tyrosine kinase inhibitors for human cancer
Cheminformatics-based identification of phosphorylated RET tyrosine kinase inhibitors for human cancer Abstract Background Rearranged during transfection (RET), an oncogenic protein, is associated with various cancers, including non-small-cell lung cancer (NSCLC), papillary thyroid cancer (PTC), pancreatic cancer, medu...
PMC4937651
core_pubmed_pmc
Identification of metabolites of dalfampridine (4-aminopyridine) in dog and rat
Identification of metabolites of dalfampridine (4-aminopyridine) in dog and rat Abstract Background Dalfampridine (4-aminopyridine; 4-AP) is a potassium channel blocker available in the United States to improve walking in patients with multiple sclerosis as demonstrated by an increase in walking speed. Its pharmacokine...
PMC8955067
core_pubmed_pmc
Preliminary Bioequivalence of an Oral Pimobendan Solution Formulation with Reference Solution Formulation in Beagle Dogs
Preliminary Bioequivalence of an Oral Pimobendan Solution Formulation with Reference Solution Formulation in Beagle Dogs Abstract Abstract Oral capsule and tablet formulations of pimobendan are widely used but may present difficulties for accurately dosing small patients. This study aimed to compare the pharmacokinetic...
PMC8292240
core_pubmed_pmc
Development of a Prototype, Once-Daily, Modified-Release Formulation for the Short Half-Life RIPK1 Inhibitor GSK2982772
Development of a Prototype, Once-Daily, Modified-Release Formulation for the Short Half-Life RIPK1 Inhibitor GSK2982772 Abstract Abstract Purpose GSK2982772 is a selective inhibitor of receptor-interacting protein kinase-1, with a 2–3 h half-life. This study evaluated if a once-daily modified-release formulation of GSK...
PMC11954716
core_pubmed_pmc
Population Pharmacokinetics of Cobicistat and its Effect on the Pharmacokinetics of the Anticancer Drug Olaparib
Population Pharmacokinetics of Cobicistat and its Effect on the Pharmacokinetics of the Anticancer Drug Olaparib Abstract Abstract Objectives Pharmacokinetic (PK) boosting is the intentional use of strong inhibitors of metabolic enzymes or transporters to boost the systemic exposure of a therapeutic drug. PK boosting i...
PMC4454520
core_pubmed_pmc
Allopregnanolone Preclinical Acute Pharmacokinetic and Pharmacodynamic Studies to Predict Tolerability and Efficacy for Alzheimer’s Disease
Allopregnanolone Preclinical Acute Pharmacokinetic and Pharmacodynamic Studies to Predict Tolerability and Efficacy for Alzheimer’s Disease Abstract To develop allopregnanolone as a therapeutic for Alzheimer’s disease, we investigated multiple formulations and routes of administration in translationally relevant animal...
PMC3558987
core_pubmed_pmc
Activity of AFN-1252, a novel FabI inhibitor, against Staphylococcus aureus in an in vitro pharmacodynamic model simulating human pharmacokinetics
Activity of AFN-1252, a novel FabI inhibitor, against Staphylococcus aureus in an in vitro pharmacodynamic model simulating human pharmacokinetics Abstract Abstract AFN-1252, a potent enoyl-ACP reductase (FabI) inhibitor, is under development for the treatment of Staphylococcus aureus infections. The activity of AFN-12...
PMC10293147
core_pubmed_pmc
Pharmacokinetics and Bioequivalence of Abiraterone Acetate Tablets in Healthy Chinese Volunteers: An Open, Randomized, Single-Dose, Three-Period, Three-Sequence Crossover Study
Pharmacokinetics and Bioequivalence of Abiraterone Acetate Tablets in Healthy Chinese Volunteers: An Open, Randomized, Single-Dose, Three-Period, Three-Sequence Crossover Study Abstract Background and Objective Abiraterone acetate tablet is an inhibitor of androgen synthesis, primarily for the treatment of metastatic c...
PMC12828435
core_pubmed_pmc
Fatal Flaw in the Folate Pathway: Methotrexate-Bactrim Interaction, Misleading Levels, and a Cautionary Case
Fatal Flaw in the Folate Pathway: Methotrexate-Bactrim Interaction, Misleading Levels, and a Cautionary Case Abstract Methotrexate (MTX) is one of the most commonly prescribed medications for rheumatoid arthritis and other autoimmune disorders. While therapeutic drug monitoring (TDM) protocols are well-established for ...
PMC3329936
core_pubmed_pmc
Physiologically Based Structure of Mean Residence Time
Physiologically Based Structure of Mean Residence Time Abstract Abstract A mean residence time (MRT) is an important pharmacokinetic parameter. To the author's knowledge, however, a physiologically based structure of MRT (thereafter MRT structure) has not been published so far. Primarily this is because MRT structures ...
PMC9549404
core_pubmed_pmc
Population pharmacokinetics of voriconazole and initial dosage optimization in patients with talaromycosis
Population pharmacokinetics of voriconazole and initial dosage optimization in patients with talaromycosis Abstract The high variability and unpredictability of the plasma concentration of voriconazole (VRC) pose a major challenge for clinical administration. The aim of this study was to develop a population pharmacoki...
PMC6058611
core_pubmed_pmc
Fabrication of a drug delivery system that enhances antifungal drug corneal penetration
Fabrication of a drug delivery system that enhances antifungal drug corneal penetration Abstract Abstract Fungal keratitis (FK) remains a severe eye disease, and effective therapies are limited by drug shortages and critical ocular barriers. Despite the high antifungal potency and broad spectrum of econazole, its stron...
PMC6534959
core_pubmed_pmc
Exploring Sirolimus Pharmacokinetic Variability Using Data Available from the Routine Clinical Care of Renal Transplant Patients – Population Pharmacokinetic Approach
Exploring Sirolimus Pharmacokinetic Variability Using Data Available from the Routine Clinical Care of Renal Transplant Patients – Population Pharmacokinetic Approach Abstract Summary Background Due to wide intra- and inter-individual pharmacokinetic variability and narrow therapeutic index of sirolimus, the therapeuti...
PMC7086161
core_pubmed_pmc
Current status of rivaroxaban in elderly patients with pulmonary embolism (Review)
Current status of rivaroxaban in elderly patients with pulmonary embolism (Review) Abstract Abstract Acute pulmonary embolism (PE) occurs with a high incidence rate in elderly patients, demonstrating complex clinical manifestations, as well as a difficult anticoagulant treatment strategy. Currently, there is limited un...
PMC10357296
core_pubmed_pmc
Engineering cytokines for cancer immunotherapy: a systematic review
Engineering cytokines for cancer immunotherapy: a systematic review Abstract Abstract Cytokines are pivotal mediators of cell communication in the tumor microenvironment. Multiple cytokines are involved in the host antitumor response, but the production and function of these cytokines are usually dysregulated during ma...
PMC11760135
core_pubmed_pmc
Phage therapy in the management of respiratory and pulmonary infections: a systematic review
Phage therapy in the management of respiratory and pulmonary infections: a systematic review Abstract Background: Lower respiratory tract infections (LRTIs) pose a significant threat to global health, causing more than 2 million deaths worldwide. This menace is intensified by the alarming increase in drug resistance, w...
PMC10743313
core_pubmed_pmc
Evaluation of Chelator-to-Antibody Ratio on Development of 89 Zr-iPET Tracer for Imaging of PD-L1 Expression on Tumor
Evaluation of Chelator-to-Antibody Ratio on Development of 89 Zr-iPET Tracer for Imaging of PD-L1 Expression on Tumor Abstract Abstract 89 Zr-iPET has been widely used for preclinical and clinical immunotherapy studies to predict patient stratification or evaluate therapeutic efficacy. In this study, we prepared and ev...
PMC6851952
core_pubmed_pmc
Sepsis Care Pathway 2019
Sepsis Care Pathway 2019 Abstract Editorial Background: Sepsis, a medical emergency and life-threatening disorder, results from abnormal host response to infection that leads to acute organ dysfunction 1 . Sepsis is a major killer across all ages and countries and remains the most common cause of admission and death in...
PMC11211924
core_pubmed_pmc
Determination of a vancomycin nephrotoxicity threshold and assessment of target attainment in hematology patients
Determination of a vancomycin nephrotoxicity threshold and assessment of target attainment in hematology patients Abstract Abstract An area‐under‐the‐curve (AUC 24 )‐based approach is recommended to guide vancomycin therapeutic drug monitoring (TDM), yet trough concentrations are still commonly used despite associated ...
PMC9672880
core_pubmed_pmc
Bayesian method application: Integrating mathematical modeling into clinical pharmacy through vancomycin therapeutic monitoring
Bayesian method application: Integrating mathematical modeling into clinical pharmacy through vancomycin therapeutic monitoring Abstract Abstract The most recent consensus guidelines for dosing and monitoring vancomycin recommended the use of area‐under‐the‐curve with Bayesian estimation for therapeutic monitoring. As ...
PMC7848319
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic effects of 2 registered omeprazole preparations and varying dose rates in horses
Pharmacokinetic and pharmacodynamic effects of 2 registered omeprazole preparations and varying dose rates in horses Abstract Abstract Background Omeprazole preparations vary in bioavailability in horses. Hypothesis/Objectives To characterize the pharmacokinetics and pharmacodynamics of an existing enteric‐coated oral ...
PMC11539209
core_pubmed_pmc
Intrapulmonary pharmacokinetics of SPR719 following oral administration of SPR720 to healthy volunteers
Intrapulmonary pharmacokinetics of SPR719 following oral administration of SPR720 to healthy volunteers Abstract ABSTRACT SPR720 is a phosphate ester prodrug that is converted rapidly in vivo to SPR719, the active moiety, which exhibits potent in vitro activity against clinically relevant mycobacterial species includin...
PMC6911327
core_pubmed_pmc
Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles
Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles Abstract Abstract Background Most of the oral drugs have the properties of weak intestinal absorption and low bioavailability, which leads to little treatment to diseases. By nanotechnology, these ...
PMC12129919
core_pubmed_pmc
Engineered celastrol liposomes with glycyrrhizic acid augment synergistic antitumor efficacy in breast cancer
Engineered celastrol liposomes with glycyrrhizic acid augment synergistic antitumor efficacy in breast cancer Abstract Abstract Background/Objectives Breast cancer treatment remains challenged by the non-specific distribution and systemic toxicity of conventional chemotherapeutics. Celastrol (CEL), a natural compound w...
PMC3668123
core_pubmed_pmc
Analysis of the potential effect of ponatinib on the QTc interval in patients with refractory hematological malignancies
Analysis of the potential effect of ponatinib on the QTc interval in patients with refractory hematological malignancies Abstract Purpose Cardiac dysfunction, particularly QT interval prolongation, has been observed with tyrosine kinase inhibitors approved to treat chronic myeloid leukemia. This study examines the effe...
PMC12279635
core_pubmed_pmc
Expanding Horizons of Buprenorphine: A Comprehensive Narrative Review of Its Pharmacological Properties and Clinical Applications in Chronic Pain
Expanding Horizons of Buprenorphine: A Comprehensive Narrative Review of Its Pharmacological Properties and Clinical Applications in Chronic Pain Abstract Buprenorphine has gained significant attention for its unique pharmacological properties, making it a valuable tool in chronic pain management. Unlike traditional op...
PMC11494900
core_pubmed_pmc
Evaluation of model‐integrated evidence approaches for pharmacokinetic bioequivalence studies using model averaging methods
Evaluation of model‐integrated evidence approaches for pharmacokinetic bioequivalence studies using model averaging methods Abstract Abstract Conventional approaches for establishing bioequivalence (BE) between test and reference formulations using non‐compartmental analysis (NCA) may demonstrate low power in pharmacok...
PMC4560520
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, and tolerability of LC350189 , a novel xanthine oxidase inhibitor, in healthy subjects
Pharmacokinetics, pharmacodynamics, and tolerability of LC350189 , a novel xanthine oxidase inhibitor, in healthy subjects Abstract Introduction LC350189 is a novel selective xanthine oxidase inhibitor under clinical development for the management of hyperuricemia in gout patients. The aim of this study was to evaluate...
PMC5404516
core_pubmed_pmc
A Phase I, Randomized, Double-Blinded, Placebo- and Moxifloxacin-Controlled, Four-Period Crossover Study To Evaluate the Effect of Gepotidacin on Cardiac Conduction as Assessed by 12-Lead Electrocardiogram in Healthy Volunteers
A Phase I, Randomized, Double-Blinded, Placebo- and Moxifloxacin-Controlled, Four-Period Crossover Study To Evaluate the Effect of Gepotidacin on Cardiac Conduction as Assessed by 12-Lead Electrocardiogram in Healthy Volunteers Abstract ABSTRACT Gepotidacin is a novel, first-in-class triazaacenaphthylene antibiotic in ...
PMC3087488
core_pubmed_pmc
Safety and Pharmacokinetics of Motesanib in Combination with Panitumumab and Gemcitabine-Cisplatin in Patients with Advanced Cancer
Safety and Pharmacokinetics of Motesanib in Combination with Panitumumab and Gemcitabine-Cisplatin in Patients with Advanced Cancer Abstract Abstract Purpose . The aim of this study was to assess the safety and tolerability of motesanib (an orally administered small-molecule antagonist of vascular endothelial growth fa...
PMC11812935
core_pubmed_pmc
Exposure–response modeling of liver fat imaging endpoints in non‐alcoholic fatty liver disease populations administered ervogastat alone and co‐administered with clesacostat
Exposure–response modeling of liver fat imaging endpoints in non‐alcoholic fatty liver disease populations administered ervogastat alone and co‐administered with clesacostat Abstract Abstract Non‐alcoholic fatty liver disease and non‐alcoholic steatohepatitis describe a collection of liver conditions characterized by t...
PMC5763333
core_pubmed_pmc
Single‐Center Evaluation of the Pharmacokinetics and Safety of the Angiotensin II Receptor Antagonist Azilsartan Medoxomil in Mild to Moderate Hepatic Impairment
Single‐Center Evaluation of the Pharmacokinetics and Safety of the Angiotensin II Receptor Antagonist Azilsartan Medoxomil in Mild to Moderate Hepatic Impairment Abstract Abstract Azilsartan medoxomil (AZL‐M) is a potent angiotensin II receptor blocker that decreases blood pressure in a dose‐dependent manner. It is a p...
PMC9027311
core_pubmed_pmc
Comparative Study of Ocular Pharmacokinetics of Topical 0.3% Gatifloxacin Eye Gel and Solution in Rabbits
Comparative Study of Ocular Pharmacokinetics of Topical 0.3% Gatifloxacin Eye Gel and Solution in Rabbits Abstract Abstract Few articles have reported drug concentrations of different ophthalmic dosage forms in the ocular tissues. This study aimed to determine the ocular pharmacokinetics of gatifloxacin 0.3% eye gel (G...
PMC8143339
core_pubmed_pmc
PK/PD Modeling of the PDE7 Inhibitor—GRMS-55 in a Mouse Model of Autoimmune Hepatitis
PK/PD Modeling of the PDE7 Inhibitor—GRMS-55 in a Mouse Model of Autoimmune Hepatitis Abstract Abstract This study aimed to assess the efficacy and explore the mechanisms of action of a potent phosphodiesterase (PDE)7A and a moderate PDE4B inhibitor GRMS-55 in a mouse model of autoimmune hepatitis (AIH). The concentrat...
PMC8109687
core_pubmed_pmc
Application of aerosol therapy in respiratory diseases in children: A Saudi expert consensus
Application of aerosol therapy in respiratory diseases in children: A Saudi expert consensus Abstract The Saudi Pediatric Pulmonology Association (SPPA) is a subsidiary of the Saudi Thoracic Society (STS), which consists of a group of Saudi experts with well-respected academic and clinical backgrounds in the fields of ...
PMC4394464
core_pubmed_pmc
Identification and Pharmacokinetics of Multiple Potential Bioactive Constituents after Oral Administration of Radix Astragali on Cyclophosphamide-Induced Immunosuppression in Balb/c Mice
Identification and Pharmacokinetics of Multiple Potential Bioactive Constituents after Oral Administration of Radix Astragali on Cyclophosphamide-Induced Immunosuppression in Balb/c Mice Abstract Radix Astragali (RA) is one of the commonly-used traditional Chinese medicines (TCMs) with an immunomodulatory effect confir...
PMC12482936
core_pubmed_pmc
Pharmacokinetics, Relative Bioavailability, and Safety of the SHR0302 Oral Solution and Tablets: A Single-Center, Randomized, Open-Label, Crossover (Two-Formulation, Two-Period) Phase I Trial in Healthy Chinese Volunteers
Pharmacokinetics, Relative Bioavailability, and Safety of the SHR0302 Oral Solution and Tablets: A Single-Center, Randomized, Open-Label, Crossover (Two-Formulation, Two-Period) Phase I Trial in Healthy Chinese Volunteers Abstract Abstract Purpose This study investigates the pharmacokinetic characteristics and relative...
PMC9968717
core_pubmed_pmc
Breakthrough: a first-in-class virtual simulator for dose optimization of ACE inhibitors in translational cardiovascular medicine
Breakthrough: a first-in-class virtual simulator for dose optimization of ACE inhibitors in translational cardiovascular medicine Abstract The renin–angiotensin–aldosterone-systems (RAAS) play a central role in the pathophysiology of congestive heart failure (CHF), justifying the use of angiotensin converting enzyme in...
PMC11052784
core_pubmed_pmc
Assessment of the Effects of Abrocitinib on the Pharmacokinetics of Probe Substrates of Cytochrome P450 1A2, 2B6 and 2C19 Enzymes and Hormonal Oral Contraceptives in Healthy Individuals
Assessment of the Effects of Abrocitinib on the Pharmacokinetics of Probe Substrates of Cytochrome P450 1A2, 2B6 and 2C19 Enzymes and Hormonal Oral Contraceptives in Healthy Individuals Abstract Abstract Background and Objective Abrocitinib is an oral small-molecule Janus kinase (JAK)-1 inhibitor approved for the treat...
PMC4317947
core_pubmed_pmc
Phase I dose-escalation study of buparlisib (BKM120), an oral pan-class I PI3K inhibitor, in Japanese patients with advanced solid tumors
Phase I dose-escalation study of buparlisib (BKM120), an oral pan-class I PI3K inhibitor, in Japanese patients with advanced solid tumors Abstract Buparlisib (BKM120) is an oral pan-phosphatidylinositol 3-kinase inhibitor, targeting all four isoforms of class I PI3K (α, β, γ and δ). This open-label Phase I dose-escalat...
PMC7898066
core_pubmed_pmc
Evaluation of bone and kidney toxicity of BT2-peg2, a potential carrier for the targeted delivery of antibiotics to bone
Evaluation of bone and kidney toxicity of BT2-peg2, a potential carrier for the targeted delivery of antibiotics to bone Abstract Previous studies have demonstrated that the bone targeting agent BT2-peg2 (BT2-minipeg2, 9 ), when conjugated to vancomycin and delivered systemically by intravenous (IV) or intraperitoneal ...
PMC6586010
core_pubmed_pmc
No Clinical Impact of CYP3A5 Gene Polymorphisms on the Pharmacokinetics and/or Efficacy of Maraviroc in Healthy Volunteers and HIV‐1–Infected Subjects
No Clinical Impact of CYP3A5 Gene Polymorphisms on the Pharmacokinetics and/or Efficacy of Maraviroc in Healthy Volunteers and HIV‐1–Infected Subjects Abstract Abstract Maraviroc is a C‐C chemokine receptor type‐5 antagonist approved for the treatment of HIV‐1. Previous studies show that cytochrome P450 3A5 (CYP3A5) pl...
PMC12904406
core_pubmed_pmc
Effects of matcha green tea on the pharmacokinetics of nadolol in rats
Effects of matcha green tea on the pharmacokinetics of nadolol in rats Abstract Abstract The concurrent use of herbal dietary supplements with prescription medications raises safety concerns due to the potential for clinically significant interactions. Matcha, a shade-grown green tea consumed as an ultra-fine powder, i...
PMC8592514
core_pubmed_pmc
Population pharmacokinetics and exposure–response modeling for evinacumab in homozygous familial hypercholesterolemia
Population pharmacokinetics and exposure–response modeling for evinacumab in homozygous familial hypercholesterolemia Abstract Abstract Evinacumab, an angiopoietin‐like protein 3 (ANGPTL3) inhibitor, has been shown to significantly reduce low‐density lipoprotein cholesterol (LDL‐C) in patients with homozygous familial ...
PMC7914841
core_pubmed_pmc
Systemic Delivery of hGhrelin Derivative by Lyophilizate for Dry Powder Inhalation System in Monkeys
Systemic Delivery of hGhrelin Derivative by Lyophilizate for Dry Powder Inhalation System in Monkeys Abstract Abstract Ghrelin is the peptide that increases the hunger sensation and food intake and is expected to be clinically applied for treatment of diseases such as cachexia and anorexia nervosa. In the clinical appl...
PMC9356076
core_pubmed_pmc
An Integrated Pharmacological Counselling Approach to Guide Decision-Making in the Treatment with CDK4/6 Inhibitors for Metastatic Breast Cancer
An Integrated Pharmacological Counselling Approach to Guide Decision-Making in the Treatment with CDK4/6 Inhibitors for Metastatic Breast Cancer Abstract Abstract A wide inter-individual variability in the therapeutic response to cyclin-dependent kinases 4 and 6 inhibitors (CDKis) has been reported. We herein present a...
PMC6585772
core_pubmed_pmc
A Comprehensive Overview of the Clinical Pharmacokinetics of Clobazam
A Comprehensive Overview of the Clinical Pharmacokinetics of Clobazam Abstract Abstract Clobazam (CLB) is a 1,5‐benzodiazepine that has been widely used as an anxiolytic and antiseizure drug (ASD) since it was first synthesized over 50 years ago. CLB was approved in the United States in 2011 as adjunctive therapy for s...
PMC12800905
core_pubmed_pmc
Oroxylum indicum (L.) Bark Ameliorates Anxiety and Depression: Evidence From Experimental and Computational Studies
Oroxylum indicum (L.) Bark Ameliorates Anxiety and Depression: Evidence From Experimental and Computational Studies Abstract ABSTRACT This study evaluated the antioxidant and neuropharmacological potentials of methanol extract of Oroxylum indicum bark (MOIB) to advocate the scientific basis of its traditional use in me...
PMC9553801
core_pubmed_pmc
Single-Dose Pharmacokinetics of Milvexian in Participants with Normal Renal Function and Participants with Moderate or Severe Renal Impairment
Single-Dose Pharmacokinetics of Milvexian in Participants with Normal Renal Function and Participants with Moderate or Severe Renal Impairment Abstract Abstract Objective The aim of this study was to assess the effect of moderate or severe renal impairment on the pharmacokinetic (PK) properties of milvexian. Methods Th...
PMC6154226
core_pubmed_pmc
Safety of Insulin Lispro and a Biosimilar Insulin Lispro When Administered Through an Insulin Pump
Safety of Insulin Lispro and a Biosimilar Insulin Lispro When Administered Through an Insulin Pump Abstract Background: SAR342434 (U100; SAR-Lis; insulin lispro) is a biosimilar/follow-on to insulin lispro (U100; Ly-Lis). Similar pharmacokinetics/pharmacodynamics between the two products has been demonstrated in a hype...
PMC10060579
core_pubmed_pmc
A Phase 1 randomized study on the safety and pharmacokinetics of OCS-05, a neuroprotective disease modifying treatment for Acute Optic Neuritis and Multiple Sclerosis
A Phase 1 randomized study on the safety and pharmacokinetics of OCS-05, a neuroprotective disease modifying treatment for Acute Optic Neuritis and Multiple Sclerosis Abstract Abstract OCS-05 (aka BN201) is a peptidomimetic that binds to serum glucocorticoid kinase-2 (SGK2), displaying neuroprotective activity. The obj...
PMC9541463
core_pubmed_pmc
A Randomized Thorough QT Study of Apomorphine Sublingual Film in Patients With Parkinson's Disease
A Randomized Thorough QT Study of Apomorphine Sublingual Film in Patients With Parkinson's Disease Abstract Abstract A randomized thorough QT study was conducted to assess the effects of apomorphine sublingual film (SL‐APO) on corrected QT interval (QTc) and other cardiac conduction parameters in patients with Parkinso...
PMC10163451
core_pubmed_pmc
Efficacy and safety of ceftazidime–avibactam versus polymyxins in the treatment of carbapenem-resistant Enterobacteriaceae infection: a systematic review and meta-analysis
Efficacy and safety of ceftazidime–avibactam versus polymyxins in the treatment of carbapenem-resistant Enterobacteriaceae infection: a systematic review and meta-analysis Abstract Abstract Objectives Carbapenem-resistant Enterobacteriaceae is increasingly recognised as a significant public health concern. Ceftazidime-...
PMC6221065
core_pubmed_pmc
Sustained‐release ruxolitinib: Findings from a phase 1 study in healthy subjects and a phase 2 study in patients with myelofibrosis
Sustained‐release ruxolitinib: Findings from a phase 1 study in healthy subjects and a phase 2 study in patients with myelofibrosis Abstract Abstract Ruxolitinib is the first Janus kinase (JAK) inhibitor approved for the treatment of myelofibrosis, where its efficacy is often associated with cytopenia. It is possible t...
PMC10847190
core_pubmed_pmc
Identification and characterization of endogenous biomarkers for hepatic vectorial transport (OATP1B3-P-gp) function using metabolomics with serum pharmacology
Identification and characterization of endogenous biomarkers for hepatic vectorial transport (OATP1B3-P-gp) function using metabolomics with serum pharmacology Abstract Abstract The organic anion-transporting polypeptide 1B3 and P-glycoprotein (P-gp) provide efficient directional transport (OATP1B3-P-gp) from the blood...
PMC3877522
core_pubmed_pmc
Simvastatin Solid Lipid Nanoparticles for Oral Delivery: Formulation Development and In vivo Evaluation
Simvastatin Solid Lipid Nanoparticles for Oral Delivery: Formulation Development and In vivo Evaluation Abstract Solid lipid nanoparticles have been increasingly utilised for improving oral bioavailability of drugs. Simvastatin is biopharmaceutical class 2 drug with poor oral bioavailability of 5%. In the present study...
PMC3168450
core_pubmed_pmc
Clinical pharmacokinetics of ketoprofen enantiomers in wild type of Cyp 2c8 and Cyp 2c9 patients with rheumatoid arthritis
Clinical pharmacokinetics of ketoprofen enantiomers in wild type of Cyp 2c8 and Cyp 2c9 patients with rheumatoid arthritis Abstract Pharmacokinetics of ketoprofen (KTP) enantiomers has been studied in patients with rheumatoid arthritis (RA) following administration of a single oral dose of 100 mg rac-KTP during multidr...
PMC12075740
core_pubmed_pmc
Physiologically Based and Population Pharmacokinetic Modeling of Midazolam in Children With Obesity Using Real‐World Data
Physiologically Based and Population Pharmacokinetic Modeling of Midazolam in Children With Obesity Using Real‐World Data Abstract ABSTRACT Children represent a highly complex and variable population for treatment, including interindividual differences in drug dose–exposure. Midazolam has been used as a sedative for ho...
PMC12924807
core_pubmed_pmc
Role of Cefiderocol in the Treatment of Carbapenem-Resistant Nonfermenting Gram-Negative Bacilli ( Acinetobacter baumannii , Pseudomonas aeruginosa , and Stenotrophomonas maltophilia ) Infections: An Expert Statement
Role of Cefiderocol in the Treatment of Carbapenem-Resistant Nonfermenting Gram-Negative Bacilli ( Acinetobacter baumannii , Pseudomonas aeruginosa , and Stenotrophomonas maltophilia ) Infections: An Expert Statement Abstract Abstract Introduction Infections caused by nonfermenting gram-negative bacilli (NF-GNB), parti...
PMC9804266
core_pubmed_pmc
Implications for sequencing of biologic therapy and choice of second anti‐TNF in patients with inflammatory bowel disease: results from the IMmunogenicity to Second Anti‐TNF therapy ( IMSAT ) therapeutic drug monitoring study
Implications for sequencing of biologic therapy and choice of second anti‐TNF in patients with inflammatory bowel disease: results from the IMmunogenicity to Second Anti‐TNF therapy ( IMSAT ) therapeutic drug monitoring study Abstract Summary Background Anti‐drug antibodies are associated with treatment failure to anti...
PMC12759048
core_pubmed_pmc
Single-blinded, stratified, dose ranging trial to assess pharmacokinetics and identify optimal dose of vitamin B12 in pregnancy in Tanzania
Single-blinded, stratified, dose ranging trial to assess pharmacokinetics and identify optimal dose of vitamin B12 in pregnancy in Tanzania Abstract Abstract Background Vitamin B12 is an essential cofactor for two enzymes that have critical functions in pregnancy, both for maternal health and fetal development. However...
PMC6034060
core_pubmed_pmc
Enantioselective pharmacokinetics of tramadol and its three main metabolites; impact of CYP2D6 , CYP2B6 , and CYP3A4 genotype
Enantioselective pharmacokinetics of tramadol and its three main metabolites; impact of CYP2D6 , CYP2B6 , and CYP3A4 genotype Abstract Abstract Tramadol is a complex drug, being metabolized by polymorphic enzymes and administered as a racemate with the (+)‐ and (−)‐enantiomers of the parent compound and metabolites sho...
PMC5285297
core_pubmed_pmc
Multiphenotype association study of patients randomized to initiate antiretroviral regimens in AIDS Clinical Trials Group protocol A5202
Multiphenotype association study of patients randomized to initiate antiretroviral regimens in AIDS Clinical Trials Group protocol A5202 Abstract Supplemental Digital Content is available in the text. Keywords: antiretroviral therapy, clinical trials, HIV-1, pharmacogenomics, phenome-wide association studies Abstract B...
PMC12835341
core_pubmed_pmc
Fluoroquinolone resistance in ESKAPE pathogens: evolutionary pathways, one health transmission, and clinical surveillance
Fluoroquinolone resistance in ESKAPE pathogens: evolutionary pathways, one health transmission, and clinical surveillance Abstract Fluoroquinolones (FQs) remain important treatments for many Gram-negative and some Gram-positive infections, but rapid resistance development is steadily reducing their clinical usefulness....
PMC3423151
core_pubmed_pmc
Peptide ligand and PEG-mediated long-circulating liposome targeted to FGFR overexpressing tumor in vivo
Peptide ligand and PEG-mediated long-circulating liposome targeted to FGFR overexpressing tumor in vivo Abstract Abstract Background and methods Paclitaxel, a widely used antitumor agent, has limited clinical application due to its hydrophobicity and systemic toxicity. To achieve sustained and targeted delivery of pacl...
PMC10482255
core_pubmed_pmc
A picogram BA-ELISA quantification assay for rLj-RGD3, a platelet fibrinogen receptor antagonist, in the rat plasma and its application to a pharmacokinetic study
A picogram BA-ELISA quantification assay for rLj-RGD3, a platelet fibrinogen receptor antagonist, in the rat plasma and its application to a pharmacokinetic study Abstract Abstract rLj-RGD3, a new member of the RGD (Arginine-Glycine-Aspartate)-motif toxin protein family obtained from Lampetra japonica by means of recom...
PMC4056350
core_pubmed_pmc
Meropenem and piperacillin/tazobactam prescribing in critically ill patients: does augmented renal clearance affect pharmacokinetic/pharmacodynamic target attainment when extended infusions are used?
Meropenem and piperacillin/tazobactam prescribing in critically ill patients: does augmented renal clearance affect pharmacokinetic/pharmacodynamic target attainment when extended infusions are used? Abstract Abstract Background Correct antibiotic dosing remains a challenge for the clinician. The aim of this study was ...
PMC8128070
core_pubmed_pmc
Analysis of Pharmacokinetics in the Cochlea of the Inner Ear
Analysis of Pharmacokinetics in the Cochlea of the Inner Ear Abstract Hearing loss affects >5% of the global population and therefore, has a great social and clinical impact. Sensorineural hearing loss, which can be caused by different factors, such as acoustic trauma, aging, and administration of certain classes of dr...
PMC7232584
core_pubmed_pmc
Dopamine Buffering Capacity Imaging: A Pharmacodynamic fMRI Method for Staging Parkinson Disease
Dopamine Buffering Capacity Imaging: A Pharmacodynamic fMRI Method for Staging Parkinson Disease Abstract Abstract We propose a novel pharmacological fMRI (phMRI) method for objectively quantifying disease severity in Parkinson disease (PD). It is based on the clinical observation that the benefit from a dose of levodo...