id
stringlengths
9
11
source
stringclasses
1 value
title
stringlengths
15
560
text
stringlengths
2k
153k
PMC10904703
core_pubmed_pmc
Pharmacodynamics and biodistribution of [195mPt]cisplatin(CISSPECT®) in head and neck squamous cell carcinoma
Pharmacodynamics and biodistribution of [195mPt]cisplatin(CISSPECT®) in head and neck squamous cell carcinoma Abstract Abstract Background Cisplatin- based chemoradiotherapy is a crucial pillar in the treatment of HNSCC. The use of cisplatin comes with high toxicity rates as 35% of patients cannot sustain the planned d...
PMC8295151
core_pubmed_pmc
Efficacy and Safety of Bevacizumab Biosimilar FKB238 Versus Originator Bevacizumab: Results from AVANA, a Phase III Trial in Patients with Non-Squamous Non-Small-Cell Lung Cancer (non-sq-NSCLC)
Efficacy and Safety of Bevacizumab Biosimilar FKB238 Versus Originator Bevacizumab: Results from AVANA, a Phase III Trial in Patients with Non-Squamous Non-Small-Cell Lung Cancer (non-sq-NSCLC) Abstract Background Bevacizumab is an antiangiogenic recombinant humanized monoclonal antibody that inhibits tumor growth. FKB...
PMC5954141
core_pubmed_pmc
Structure-guided Discovery of Dual-recognition Chemibodies
Structure-guided Discovery of Dual-recognition Chemibodies Abstract Small molecules and antibodies each have advantages and limitations as therapeutics. Here, we present for the first time to our knowledge, the structure-guided design of “chemibodies” as small molecule-antibody hybrids that offer dual recognition of a ...
PMC10781787
core_pubmed_pmc
Direct oral anticoagulants and the risk of adverse clinical outcomes among patients with different body weight categories: a large hospital-based study
Direct oral anticoagulants and the risk of adverse clinical outcomes among patients with different body weight categories: a large hospital-based study Abstract Objective Through predictable pharmacokinetics—including a convenient fixed-dose regimen, direct oral anticoagulants (DOACs) are preferred over previous treatm...
PMC11941735
core_pubmed_pmc
Perioperative Drug Management of Systemic Therapies in Breast Cancer: A Literature Review and Treatment Recommendations
Perioperative Drug Management of Systemic Therapies in Breast Cancer: A Literature Review and Treatment Recommendations Abstract Abstract Breast cancer accounts for about 30% of all new female cancers each year, and its incidence is increasing 0.6% per year. An enhanced understanding of the molecular mechanisms of carc...
PMC11111615
core_pubmed_pmc
A Phase 1a Study to Evaluate Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of RO7303509, an Anti-TGFβ3 Antibody, in Healthy Volunteers
A Phase 1a Study to Evaluate Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of RO7303509, an Anti-TGFβ3 Antibody, in Healthy Volunteers Abstract Abstract Introduction Transforming growth factor beta (TGFβ) cytokines (TGFβ1, TGFβ2, and TGFβ3) play critical roles in tissue fibrosis. However, treatment with ...
PMC12235324
core_pubmed_pmc
Population Pharmacokinetics and Exposure–Response Analyses for Capivasertib in Combination With Fulvestrant in Patients With Breast Cancer
Population Pharmacokinetics and Exposure–Response Analyses for Capivasertib in Combination With Fulvestrant in Patients With Breast Cancer Abstract ABSTRACT Capivasertib is a potent, selective pan‐AKT inhibitor. In the Phase III CAPItello‐291 trial in patients with aromatase inhibitor‐resistant, hormone receptor (HR)‐p...
PMC12010960
core_pubmed_pmc
Revolutionizing Patient-Reported Outcomes Analysis for Oncology Drug Development Using Population Models
Revolutionizing Patient-Reported Outcomes Analysis for Oncology Drug Development Using Population Models Abstract Abstract Patient-reported outcomes (PRO) play a crucial role as clinical endpoint in oncology trials. Traditional statistical methods, such as hypothesis testing, have been commonly used by pharmaceutical i...
PMC5655776
core_pubmed_pmc
The Effect of Renal Impairment on the Pharmacokinetics and Pharmacodynamics of Ertugliflozin in Subjects With Type 2 Diabetes Mellitus
The Effect of Renal Impairment on the Pharmacokinetics and Pharmacodynamics of Ertugliflozin in Subjects With Type 2 Diabetes Mellitus Abstract Abstract Ertugliflozin is a highly selective and potent inhibitor of the sodium‐glucose cotransporter 2 in development for the treatment of type 2 diabetes mellitus. The glycem...
PMC8518113
core_pubmed_pmc
Vancomycin area under the curves estimated with pharmacokinetic equations using trough‐only data
Vancomycin area under the curves estimated with pharmacokinetic equations using trough‐only data Abstract Abstract What is known and objective The revised vancomycin monitoring guidelines recommend targeting an area under the curve (AUC) of 400–600 mg*hr/L for serious methicillin‐resistant Staphylococcus aureus (MRSA) ...
PMC6170330
core_pubmed_pmc
A Scalable Method for Squalenoylation and Assembly of Multifunctional 64 Cu-Labeled Squalenoylated Gemcitabine Nanoparticles
A Scalable Method for Squalenoylation and Assembly of Multifunctional 64 Cu-Labeled Squalenoylated Gemcitabine Nanoparticles Abstract Abstract Squalenoylation of gemcitabine, a front-line therapy for pancreatic cancer, allows for improved cellular-level and system-wide drug delivery. The established methods to conjugat...
PMC11694538
core_pubmed_pmc
Efficacy, safety, and pharmacokinetics of teclistamab in Chinese patients with relapsed/refractory multiple myeloma from the China cohort of MajesTEC‐1
Efficacy, safety, and pharmacokinetics of teclistamab in Chinese patients with relapsed/refractory multiple myeloma from the China cohort of MajesTEC‐1 Abstract Abstract Introduction Teclistamab, the first approved B‐cell maturation antigen‐directed bispecific antibody for treatment of triple‐class exposed relapsed/ref...
PMC11785738
core_pubmed_pmc
Investigating new drugs from marine seaweed metabolites for cervical cancer therapy by molecular dynamic modeling approach
Investigating new drugs from marine seaweed metabolites for cervical cancer therapy by molecular dynamic modeling approach Abstract The etiology of cervical cancer in women is attributed to the continuous infection of the human papillomavirus (HPV). The high costs and side effects of standard treatments and the limited...
PMC6352947
core_pubmed_pmc
Virtual design of novel Plasmodium falciparum cysteine protease falcipain-2 hybrid lactone–chalcone and isatin–chalcone inhibitors probing the S2 active site pocket
Virtual design of novel Plasmodium falciparum cysteine protease falcipain-2 hybrid lactone–chalcone and isatin–chalcone inhibitors probing the S2 active site pocket Abstract Abstract We report computer-aided design of new lactone–chalcone and isatin–chalcone (HLCIC) inhibitors of the falcipain-2 ( Pf FP-2). 3D models o...
PMC12206339
core_pubmed_pmc
Optimizing ibrutinib bioavailability: Formulation and assessment of hydroxypropyl-β-cyclodextrin-based nanosponge delivery systems
Optimizing ibrutinib bioavailability: Formulation and assessment of hydroxypropyl-β-cyclodextrin-based nanosponge delivery systems Abstract Background The current research aims to improve the oral bioavailability of ibrutinib (IBR), a class II drug with low solubility, through the formulation of nanosponges (NSPs) that...
PMC5030243
core_pubmed_pmc
Adherence and Patients' Experiences with the Use of Capecitabine in Daily Practice
Adherence and Patients' Experiences with the Use of Capecitabine in Daily Practice Abstract Abstract Introduction: Capecitabine is a widely prescribed oral anticancer agent. We studied medication adherence and explored its use in daily practice from a patients' perspective. Patients and Methods: Patients ( n = 92) star...
PMC11110198
core_pubmed_pmc
Pharmacokinetics of tenofovir alafenamide, emtricitabine, and dolutegravir in a patient on peritoneal dialysis
Pharmacokinetics of tenofovir alafenamide, emtricitabine, and dolutegravir in a patient on peritoneal dialysis Abstract Introduction Peritoneal dialysis (PD) is an effective renal replacement modality in people with HIV (PWH) with end-stage kidney disease (ESKD), particularly those with residual kidney function. Data o...
PMC7238081
core_pubmed_pmc
Imbalance of Drug Transporter-CYP450s Interplay by Diabetes and Its Clinical Significance
Imbalance of Drug Transporter-CYP450s Interplay by Diabetes and Its Clinical Significance Abstract Abstract The pharmacokinetics of a drug is dependent upon the coordinate work of influx transporters, enzymes and efflux transporters (i.e., transporter-enzyme interplay). The transporter–enzyme interplay may occur in liv...
PMC12632214
core_pubmed_pmc
An exploratory evaluation of the interaction risk between herbal products and pharmaceutical medicines used concurrently for disease management in Blantyre, Malawi
An exploratory evaluation of the interaction risk between herbal products and pharmaceutical medicines used concurrently for disease management in Blantyre, Malawi Abstract Abstract Context The use of herbal products in Malawi remains widespread and culturally significant, often occurring alongside pharmaceutical medic...
PMC8119179
core_pubmed_pmc
In vivo visualization of PARP inhibitor pharmacodynamics
In vivo visualization of PARP inhibitor pharmacodynamics Abstract Abstract BACKGROUND [ 18 F]FluorThanatrace ([ 18 F]FTT) is a radiolabeled poly (adenosine diphosphate-ribose) polymerase inhibitor (PARPi) that enables noninvasive quantification of PARP with potential to serve as a biomarker for patient selection for PA...
PMC9804248
core_pubmed_pmc
Fluorescence intensity and lifetime imaging of lipofuscin-like autofluorescence for label-free predicting clinical drug response in cancer
Fluorescence intensity and lifetime imaging of lipofuscin-like autofluorescence for label-free predicting clinical drug response in cancer Abstract Conventional techniques for in vitro cancer drug screening require labor-intensive formalin fixation, paraffin embedding, and dye staining of tumor tissues at fixed endpoin...
PMC11997519
core_pubmed_pmc
Optimizing Initial Vancomycin Dosing in Hospitalized Patients Using Machine Learning Approach for Enhanced Therapeutic Outcomes: Algorithm Development and Validation Study
Optimizing Initial Vancomycin Dosing in Hospitalized Patients Using Machine Learning Approach for Enhanced Therapeutic Outcomes: Algorithm Development and Validation Study Abstract Abstract Background Vancomycin is commonly dosed using standard weight–based methods before dose adjustments are made through therapeutic d...
PMC4162656
core_pubmed_pmc
Two phase I dose-escalation/pharmacokinetics studies of low temperature liposomal doxorubicin (LTLD) and mild local hyperthermia in heavily pretreated patients with local regionally recurrent breast cancer
Two phase I dose-escalation/pharmacokinetics studies of low temperature liposomal doxorubicin (LTLD) and mild local hyperthermia in heavily pretreated patients with local regionally recurrent breast cancer Abstract Purpose Unresectable chest wall recurrences of breast cancer (CWR) in heavily pretreated patients are esp...
PMC7896747
core_pubmed_pmc
Safety, tolerability, and pharmacokinetics of BAT8001 in patients with HER2‐positive breast cancer: An open‐label, dose‐escalation, phase I study
Safety, tolerability, and pharmacokinetics of BAT8001 in patients with HER2‐positive breast cancer: An open‐label, dose‐escalation, phase I study Abstract Abstract Background The introductions of anti‐ human epidermal growth factor receptor‐2 (HER2) agents have significantly improved the treatment outcome of patients w...
PMC6816392
core_pubmed_pmc
Durable blockade of PD-1 signaling links preclinical efficacy of sintilimab to its clinical benefit
Durable blockade of PD-1 signaling links preclinical efficacy of sintilimab to its clinical benefit Abstract ABSTRACT Blockade of immune checkpoint pathways by programmed cell death protein 1 (PD-1) antibodies has demonstrated broad clinical efficacy against a variety of malignancies. Sintilimab, a highly selective, fu...
PMC4361913
core_pubmed_pmc
Pharmacokinetics of Gefitinib in a Patient with Non-Small Cell Lung Cancer Undergoing Continuous Ambulatory Peritoneal Dialysis
Pharmacokinetics of Gefitinib in a Patient with Non-Small Cell Lung Cancer Undergoing Continuous Ambulatory Peritoneal Dialysis Abstract A 72-year-old man undergoing continuous ambulatory peritoneal dialysis (CAPD) for chronic renal failure and who had undergone right upper lobectomy for lung adenocarcinoma (pT2aN0M0) ...
PMC10449773
core_pubmed_pmc
A Phase 1/2A trial of idroxioleic acid: first-in-class sphingolipid regulator and glioma cell autophagy inducer with antitumor activity in refractory glioma
A Phase 1/2A trial of idroxioleic acid: first-in-class sphingolipid regulator and glioma cell autophagy inducer with antitumor activity in refractory glioma Abstract Background The first-in-class brain-penetrating synthetic hydroxylated lipid idroxioleic acid (2-OHOA; sodium 2-hydroxyoleate), activates sphingomyelin sy...
PMC10544331
core_pubmed_pmc
Viral dissemination and immune activation modulate antiretroviral drug levels in lymph nodes of SIV-infected rhesus macaques
Viral dissemination and immune activation modulate antiretroviral drug levels in lymph nodes of SIV-infected rhesus macaques Abstract Abstract Introduction and methods To understand the relationship between immunovirological factors and antiretroviral (ARV) drug levels in lymph nodes (LN) in HIV therapy, we analyzed dr...
PMC3419760
core_pubmed_pmc
The Safety and Pharmacokinetics of Cyanidin-3-Glucoside after 2-Week Administration of Black Bean Seed Coat Extract in Healthy Subjects
The Safety and Pharmacokinetics of Cyanidin-3-Glucoside after 2-Week Administration of Black Bean Seed Coat Extract in Healthy Subjects Abstract We analyzed the pharmacokinetics of C3G on data from twelve subjects, after 2-week multiple dosing of black bean (Phaseolus vulgaris, Cheongjakong-3-ho) seed coat extract, usi...
PMC5759734
core_pubmed_pmc
Population Pharmacokinetics of Fosdagrocorat (PF‐04171327), a Dissociated Glucocorticoid Receptor Agonist, in Patients With Rheumatoid Arthritis
Population Pharmacokinetics of Fosdagrocorat (PF‐04171327), a Dissociated Glucocorticoid Receptor Agonist, in Patients With Rheumatoid Arthritis Abstract Abstract Dissociated agonists of the glucocorticoid receptor (DAGRs) show similar antiinflammatory effects but improved tolerability compared with standard glucocorti...
PMC7584476
core_pubmed_pmc
Safety and efficacy of BAY1436032 in IDH1-mutant AML: phase I study results
Safety and efficacy of BAY1436032 in IDH1-mutant AML: phase I study results Abstract The mutant IDH1 (mIDH1) inhibitor BAY1436032 demonstrated robust activity in preclinical AML models, supporting clinical evaluation. In the current dose-escalation study, BAY1436032 was orally administered to 27 mIDH1 AML subjects acro...
PMC12006080
core_pubmed_pmc
Bibliometric analysis and knowledge mapping of diabetes mellitus combined with tuberculosis research: trends from 1995 to 2023
Bibliometric analysis and knowledge mapping of diabetes mellitus combined with tuberculosis research: trends from 1995 to 2023 Abstract Background The synergistic epidemic of diabetes mellitus and tuberculosis (DM-TB) has created a dual disease burden, challenging global health systems with complex pathophysiological i...
PMC9647038
core_pubmed_pmc
Affinity probes based on small-molecule inhibitors for tumor imaging
Affinity probes based on small-molecule inhibitors for tumor imaging Abstract Methods for molecular imaging of target areas, including optical imaging, radionuclide imaging, magnetic resonance imaging and other imaging technologies, are helpful for the early diagnosis and precise treatment of cancers. In addition to ca...
PMC3651819
core_pubmed_pmc
Warfarin dose prediction in children using pharmacometric bridging—comparison with published pharmacogenetic dosing algorithms
Warfarin dose prediction in children using pharmacometric bridging—comparison with published pharmacogenetic dosing algorithms Abstract Abstract Purpose Numerous studies have investigated causes of warfarin dose variability in adults, whereas studies in children are limited both in numbers and size. Mechanism-based pop...
PMC12938248
core_pubmed_pmc
Carbon Monoxide Therapy: Evidence and Prospects for Preventing and Treating Retinal Diseases
Carbon Monoxide Therapy: Evidence and Prospects for Preventing and Treating Retinal Diseases Abstract In carbon monoxide (CO) therapy, CO is administered at low concentrations as a controlled solution; this approach enables the drug to achieve its cytoprotective properties, including anti-inflammatory, anti-apoptotic, ...
PMC6272956
core_pubmed_pmc
In Vivo and in Vitro Study on Drug-Drug Interaction of Lovastatin and Berberine from Pharmacokinetic and HepG2 Cell Metabolism Studies
In Vivo and in Vitro Study on Drug-Drug Interaction of Lovastatin and Berberine from Pharmacokinetic and HepG2 Cell Metabolism Studies Abstract Background : We assumed that the pharmacokinetics of lovastatin could be changed by the induction effect of berberine. Methods : An UPLC-MS/MS method was developed and validate...
PMC8920424
core_pubmed_pmc
Chinese ICU physicians’ knowledge of antibiotic pharmacokinetics/pharmacodynamics (PK/PD): a cross-sectional survey
Chinese ICU physicians’ knowledge of antibiotic pharmacokinetics/pharmacodynamics (PK/PD): a cross-sectional survey Abstract Background Patients with sepsis have a high mortality rate, accumulated evidences suggest that an optimal antibiotic administration strategy based on pharmacokinetics/pharmacodynamics (PK/PD) can...
PMC11494914
core_pubmed_pmc
Bayesian sparse regression for exposure–response analyses of efficacy and safety endpoints to justify the clinical dose of valemetostat for adult T‐cell leukemia/lymphoma
Bayesian sparse regression for exposure–response analyses of efficacy and safety endpoints to justify the clinical dose of valemetostat for adult T‐cell leukemia/lymphoma Abstract Abstract Valemetostat is an oral inhibitor of enhancer of zeste homolog (EZH) 2 and EZH1 approved in Japan for the treatment of adult T‐cell...
PMC11206836
core_pubmed_pmc
Applying Physiologically Based Pharmacokinetic Modeling to Interpret Carbamazepine’s Nonlinear Pharmacokinetics and Its Induction Potential on Cytochrome P450 3A4 and Cytochrome P450 2C9 Enzymes
Applying Physiologically Based Pharmacokinetic Modeling to Interpret Carbamazepine’s Nonlinear Pharmacokinetics and Its Induction Potential on Cytochrome P450 3A4 and Cytochrome P450 2C9 Enzymes Abstract Carbamazepine (CBZ) is commonly prescribed for epilepsy and frequently used in polypharmacy. However, concerns arise...
PMC9045315
core_pubmed_pmc
In Silico Drug Discovery Strategies Identified ADMET Properties of Decoquinate RMB041 and Its Potential Drug Targets against Mycobacterium tuberculosis
In Silico Drug Discovery Strategies Identified ADMET Properties of Decoquinate RMB041 and Its Potential Drug Targets against Mycobacterium tuberculosis Abstract ABSTRACT The highly adaptive cellular response of Mycobacterium tuberculosis to various antibiotics and the high costs for clinical trials, hampers the develop...
PMC9981510
core_pubmed_pmc
A phase I first-in-man study to investigate the pharmacokinetics and safety of liposomal dexamethasone in patients with progressive multiple myeloma
A phase I first-in-man study to investigate the pharmacokinetics and safety of liposomal dexamethasone in patients with progressive multiple myeloma Abstract Despite the introduction of multiple new drugs and combination therapies, conventional dexamethasone remains a cornerstone in the treatment of multiple myeloma (M...
PMC5071684
core_pubmed_pmc
Adequacy of Rifampin Absorption after Jejunostomy Tube Administration
Adequacy of Rifampin Absorption after Jejunostomy Tube Administration Abstract It is not always possible to administer antituberculosis pharmacotherapy orally for reasons that may be a direct consequence of tuberculosis itself. To our knowledge, no published literature is available regarding antituberculosis drug absor...
PMC9917132
core_pubmed_pmc
Tenebrio molitor as a Simple and Cheap Preclinical Pharmacokinetic and Toxicity Model
Tenebrio molitor as a Simple and Cheap Preclinical Pharmacokinetic and Toxicity Model Abstract The progression of drugs into clinical phases requires proper toxicity assessment in animals and the correct identification of possible metabolites. Accordingly, different animal models are used to preliminarily evaluate toxi...
PMC11207389
core_pubmed_pmc
Investigating the Potential of Essential Oils from Citrus reticulata Leaves in Mitigating Memory Decline and Oxidative Stress in the Scopolamine-Treated Zebrafish Model
Investigating the Potential of Essential Oils from Citrus reticulata Leaves in Mitigating Memory Decline and Oxidative Stress in the Scopolamine-Treated Zebrafish Model Abstract Abstract Petitgrain essential oil (PGEO) is derived from the water distillation process on mandarin ( Citrus reticulata ) leaves. The chemical...
PMC6299694
core_pubmed_pmc
PET-MR and SPECT-MR multimodality probes: Development and challenges
PET-MR and SPECT-MR multimodality probes: Development and challenges Abstract Abstract Positron emission tomography (PET)-magnetic resonance (MR) or single photon emission computed tomography (SPECT)-MR hybrid imaging is being used in daily clinical practice. Due to its advantages over stand-alone PET, SPECT or MR imag...
PMC7295443
core_pubmed_pmc
IL-15 superagonist RLI has potent immunostimulatory properties on NK cells: implications for antimetastatic treatment
IL-15 superagonist RLI has potent immunostimulatory properties on NK cells: implications for antimetastatic treatment Abstract Background As the immune system is compromised in patients with cancer, therapeutic strategies to stimulate immunity appear promising, to avoid relapse and increase long-term overall survival. ...
PMC10523577
core_pubmed_pmc
Combining docking, molecular dynamics simulations, AD-MET pharmacokinetics properties, and MMGBSA calculations to create specialized protocols for running effective virtual screening campaigns on the autoimmune disorder and SARS-CoV-2 main protease
Combining docking, molecular dynamics simulations, AD-MET pharmacokinetics properties, and MMGBSA calculations to create specialized protocols for running effective virtual screening campaigns on the autoimmune disorder and SARS-CoV-2 main protease Abstract The development of novel medicines to treat autoimmune disease...
PMC8957249
core_pubmed_pmc
Building in-house PBPK modelling tools for oral drug administration from literature information
Building in-house PBPK modelling tools for oral drug administration from literature information Abstract The interest in using physiologically-based pharmacokinetic (PBPK) models as a support to the drug development decision making process has rapidly increased in the last years. These kind of models are examples of th...
PMC9299798
core_pubmed_pmc
Phase IIa Global Study Evaluating Rituximab for the Treatment of Pediatric Patients With Granulomatosis With Polyangiitis or Microscopic Polyangiitis
Phase IIa Global Study Evaluating Rituximab for the Treatment of Pediatric Patients With Granulomatosis With Polyangiitis or Microscopic Polyangiitis Abstract Abstract Objective To assess the safety, tolerability, pharmacokinetics, and efficacy of rituximab (RTX) in pediatric patients with granulomatosis with polyangii...
PMC9225059
core_pubmed_pmc
Model Informed Precision Dosing Tool Forecasts Trough Infliximab and Associates with Disease Status and Tumor Necrosis Factor-Alpha Levels of Inflammatory Bowel Diseases
Model Informed Precision Dosing Tool Forecasts Trough Infliximab and Associates with Disease Status and Tumor Necrosis Factor-Alpha Levels of Inflammatory Bowel Diseases Abstract Background: Substantial inter-and intra-individual variability of Infliximab (IFX) pharmacokinetics necessitates tailored dosing approaches. ...
PMC9804925
core_pubmed_pmc
Preclinical and Phase 1 Assessment of Antisense Oligonucleotide Bepirovirsen in Hepatitis B Virus–Transgenic Mice and Healthy Human Volunteers: Support for Clinical Dose Selection and Evaluation of Safety, Tolerability, and Pharmacokinetics of Single and Multiple Doses
Preclinical and Phase 1 Assessment of Antisense Oligonucleotide Bepirovirsen in Hepatitis B Virus–Transgenic Mice and Healthy Human Volunteers: Support for Clinical Dose Selection and Evaluation of Safety, Tolerability, and Pharmacokinetics of Single and Multiple Doses Abstract Abstract Dose‐dependent reductions in hep...
PMC5874817
core_pubmed_pmc
Development and Validation of an UPLC-MS/MS Method for Pharmacokinetic Comparison of Five Alkaloids from JinQi Jiangtang Tablets and Its Monarch Drug Coptidis Rhizoma
Development and Validation of an UPLC-MS/MS Method for Pharmacokinetic Comparison of Five Alkaloids from JinQi Jiangtang Tablets and Its Monarch Drug Coptidis Rhizoma Abstract JinQi Jiangtang (JQJT) tablets, a Chinese patent medicine approved by the State Food and Drug Administration, are composed of Coptidis Rhizoma, ...
PMC10086168
core_pubmed_pmc
Stylopine: A potential natural metabolite to block vascular endothelial growth factor receptor 2 (VEGFR2) in osteosarcoma therapy
Stylopine: A potential natural metabolite to block vascular endothelial growth factor receptor 2 (VEGFR2) in osteosarcoma therapy Abstract Vascular endothelial growth factor (VEGF) signals cell survival, cell migration, osteogenesis, cell proliferation, angiogenesis, and vascular permeability by binding to VEGF recepto...
PMC4546827
core_pubmed_pmc
Kinetics of Phytosterol Metabolism in Neonates Receiving Parental Nutrition
Kinetics of Phytosterol Metabolism in Neonates Receiving Parental Nutrition Abstract Background Phytosterols in soybean oil (SO) lipids likely contribute to parenteral nutrition-associated liver disease (PNALD) in infants. No characterization of phytosterol metabolism has been done in infants receiving SO lipids. Metho...
PMC4693478
core_pubmed_pmc
CYP‐mediated drug–drug interactions with evacetrapib, an investigational CETP inhibitor: in vitro prediction and clinical outcome
CYP‐mediated drug–drug interactions with evacetrapib, an investigational CETP inhibitor: in vitro prediction and clinical outcome Abstract Aims Evacetrapib is a cholesteryl ester transfer protein (CETP) inhibitor under development for reducing cardiovascular events in patients with high risk vascular disease. CETP inhi...
PMC11992663
core_pubmed_pmc
Physiologically‐based pharmacokinetic modelling of long‐acting injectable cabotegravir and rilpivirine in pregnancy
Physiologically‐based pharmacokinetic modelling of long‐acting injectable cabotegravir and rilpivirine in pregnancy Abstract Abstract Aims Long‐acting cabotegravir and rilpivirine have been approved to manage HIV in adults, but data regarding safe use in pregnancy are limited. Physiologically‐based pharmacokinetic (PBP...
PMC10933594
core_pubmed_pmc
Genetic predisposition and high exposure to colistin in the early treatment period as independent risk factors for colistin‐induced nephrotoxicity
Genetic predisposition and high exposure to colistin in the early treatment period as independent risk factors for colistin‐induced nephrotoxicity Abstract Abstract Colistin is known to cause nephrotoxicity due to its extensive reabsorption and accumulation in renal tubules. In vitro studies have identified the functio...
PMC5372427
core_pubmed_pmc
Mechanistic prediction of food effects for Compound A tablet using PBPK model
Mechanistic prediction of food effects for Compound A tablet using PBPK model Abstract Physiologically based pharmacokinetic (PBPK) modeling has been extensively used to study the factors of effect drug absorption, distribution, metabolize and extraction progress in human. In this study, Compound A(CPD A) is a BCS Clas...
PMC12890838
core_pubmed_pmc
Oxygen-carrying nanovaccine potentiates cancer immunotherapy for heterogeneous solid tumors
Oxygen-carrying nanovaccine potentiates cancer immunotherapy for heterogeneous solid tumors Abstract The heterogeneity of cancer stem cells and the immunosuppressive hypoxic microenvironment are key challenges in the development of therapeutic vaccines for solid tumors. In this study, oxygen was attempted as an adjuvan...
PMC12668924
core_pubmed_pmc
In vivo pharmacokinetic evaluation of molnupiravir in patients with severe chronic kidney disease
In vivo pharmacokinetic evaluation of molnupiravir in patients with severe chronic kidney disease Abstract Abstract Introduction Molnupiravir (MPV) is an oral, potent ribonucleoside analog that inhibits the replication of SARS-CoV-2 and is indicated for the treatment of adults with COVID-19. Patients with COVID-19 are ...
PMC12965043
core_pubmed_pmc
A Randomized, Double‐Blind, Two‐Treatment, Two‐Period, Crossover Study Investigating the Systemic Bioavailability of a Novel Cocrystal Ubiquinol Formulation Compared with a Ubiquinone Formulation in Healthy Adults
A Randomized, Double‐Blind, Two‐Treatment, Two‐Period, Crossover Study Investigating the Systemic Bioavailability of a Novel Cocrystal Ubiquinol Formulation Compared with a Ubiquinone Formulation in Healthy Adults Abstract Abstract Coenzyme Q10 (CoQ10) is a naturally occurring biochemical cofactor found in all human ce...
PMC10815824
core_pubmed_pmc
Study on the Anti-Ulcerative Colitis Effect of Pseudo-Ginsenoside RT4 Based on Gut Microbiota, Pharmacokinetics, and Tissue Distribution
Study on the Anti-Ulcerative Colitis Effect of Pseudo-Ginsenoside RT4 Based on Gut Microbiota, Pharmacokinetics, and Tissue Distribution Abstract The purpose of this study was to explore the therapeutic effect of the oral administration of pseudo-ginsenoside RT4 (RT4) on ulcerative colitis (UC), and to determine the ra...
PMC7309390
core_pubmed_pmc
Emerging and experimental treatments for COVID-19 and drug interactions with psychotropic agents
Emerging and experimental treatments for COVID-19 and drug interactions with psychotropic agents Abstract Abstract As yet, no agents have been approved for the treatment of COVID-19, although several experimental drugs are being used off licence. These may have serious adverse effects and potential drug interactions wi...
PMC11853828
core_pubmed_pmc
Nanometerizing Taxifolin Into Selenized Liposomes to Ameliorate Its Hypoglycemic Effect by Optimizing Drug Release and Bioavailability
Nanometerizing Taxifolin Into Selenized Liposomes to Ameliorate Its Hypoglycemic Effect by Optimizing Drug Release and Bioavailability Abstract Abstract Purpose Diabetes mellitus (DM) remains a significant health challenge, with traditional treatments often failing to provide lasting solutions. Taxifolin (Tax), a poten...
PMC12756200
core_pubmed_pmc
Multiple-Dose Up-Titration Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Omecamtiv Mecarbil in Healthy Chinese Subjects
Multiple-Dose Up-Titration Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Omecamtiv Mecarbil in Healthy Chinese Subjects Abstract Abstract Background and Objectives This phase I study was designed to evaluate the safety, tolerability, and pharmacokinetics of omecamtiv mecarbil with multiple oral do...
PMC3535414
core_pubmed_pmc
A Phase I study of pazopanib in combination with gemcitabine in patients with advanced solid tumors
A Phase I study of pazopanib in combination with gemcitabine in patients with advanced solid tumors Abstract Purpose Pazopanib plus gemcitabine combination therapy was explored in patients with advanced solid tumors. Methods In a modified 3 + 3 enrollment scheme, oral once-daily pazopanib was administered with intraven...
PMC11206891
core_pubmed_pmc
Effects of Surface IR783 Density on the In Vivo Behavior and Imaging Performance of Liposomes
Effects of Surface IR783 Density on the In Vivo Behavior and Imaging Performance of Liposomes Abstract Abstract Background: Nanoparticles conjugated with fluorescent probes have versatile applications, serving not only for targeted fluorescent imaging but also for evaluating the in vivo profiles of designed nanoparticl...
PMC11253705
core_pubmed_pmc
Exploring the multiple effects of nifedipine and captopril administration in spontaneously hypertensive rats through pharmacokinetic‐pharmacodynamic analyses
Exploring the multiple effects of nifedipine and captopril administration in spontaneously hypertensive rats through pharmacokinetic‐pharmacodynamic analyses Abstract Abstract This study assessed the pharmacokinetics (PKs) and pharmacodynamics (PDs) of two antihypertensive drugs, nifedipine and captopril, by exploring ...
PMC5107130
core_pubmed_pmc
Screening of a composite library of clinically used drugs and well-characterized pharmacological compounds for cystathionine β-synthase inhibition identifies benserazide as a drug potentially suitable for repurposing for the experimental therapy of colon cancer
Screening of a composite library of clinically used drugs and well-characterized pharmacological compounds for cystathionine β-synthase inhibition identifies benserazide as a drug potentially suitable for repurposing for the experimental therapy of colon cancer Abstract Cystathionine-β-synthase (CBS) has been recently ...
PMC8111650
core_pubmed_pmc
Pharmacogenetics of tenofovir and emtricitabine penetration into cerebrospinal fluid
Pharmacogenetics of tenofovir and emtricitabine penetration into cerebrospinal fluid Abstract Abstract Background Blood-cerebrospinal fluid (CSF) barrier transporters affect the influx and efflux of drugs. The antiretrovirals tenofovir and emtricitabine may be substrates of blood-brain barrier (BBB) and blood-CSF barri...
PMC3740249
core_pubmed_pmc
A Protocol for the Pharmacokinetics of Enteric Coated Mycophenolate Sodium in Lupus Nephritis (POEMSLUN): an open-label, randomised controlled trial
A Protocol for the Pharmacokinetics of Enteric Coated Mycophenolate Sodium in Lupus Nephritis (POEMSLUN): an open-label, randomised controlled trial Abstract Introduction Mycophenolate sodium, an enteric-coated tablet (EC-MPS), is as effective and safe as mycophenolate mofetil (MMF) in preventing transplant rejection. ...
PMC11487561
core_pubmed_pmc
Discovery of VU6016235: A Highly Selective, Orally Bioavailable, and Structurally Distinct Tricyclic M 4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM)
Discovery of VU6016235: A Highly Selective, Orally Bioavailable, and Structurally Distinct Tricyclic M 4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM) Abstract Abstract Herein, we report structure–activity relationship (SAR) studies to develop novel tricyclic M 4 PAM scaffolds with improved phar...
PMC11768354
core_pubmed_pmc
Liposomal Formulation of Hydroxychloroquine Can Inhibit Autophagy In Vivo
Liposomal Formulation of Hydroxychloroquine Can Inhibit Autophagy In Vivo Abstract Background/Objectives: Preclinical studies have shown that the anti-malarial drug hydroxychloroquine (HCQ) improves the anti-cancer effects of various therapeutic agents by impairing autophagy. These findings are difficult to translate i...
PMC2939787
core_pubmed_pmc
Effect of ABCB1 C3435T polymorphism on docetaxel pharmacokinetics according to menopausal status in breast cancer patients
Effect of ABCB1 C3435T polymorphism on docetaxel pharmacokinetics according to menopausal status in breast cancer patients Abstract Background: It can be hypothesised that inherited polymorphisms in the drug-transporter ABCB1 gene may interfere with interindividual variations in drug response in breast cancer patients....
PMC10046583
core_pubmed_pmc
Amivantamab-Vmjw: A Novel Treatment for Patients with NSCLC Harboring EGFR Exon 20 Insertion Mutation after Progression on Platinum-Based Chemotherapy
Amivantamab-Vmjw: A Novel Treatment for Patients with NSCLC Harboring EGFR Exon 20 Insertion Mutation after Progression on Platinum-Based Chemotherapy Abstract Objective: This study is a comprehensive review of the clinical pharmacology, pharmacokinetics, efficacy, safety, and clinical applicability of amivantamab-vmjw...
PMC10311666
core_pubmed_pmc
C–H Glycosylation of Native Carboxylic Acids: Discovery of Antidiabetic SGLT-2 Inhibitors
C–H Glycosylation of Native Carboxylic Acids: Discovery of Antidiabetic SGLT-2 Inhibitors Abstract C -Glycosides are critical motifs embedded in many bioactive natural products. The inert C -glycosides are privileged structures for developing therapeutic agents owing to their high chemical and metabolic stability. Desp...
PMC12710077
core_pubmed_pmc
Impact of Administration Time Errors on Clearance Estimation in Pharmacokinetic Analyses
Impact of Administration Time Errors on Clearance Estimation in Pharmacokinetic Analyses Abstract ABSTRACT This study aimed to comprehensively assess the impact of administration time errors on the estimation of clearance (CL), a key pharmacokinetic (PK) parameter used to predict appropriate maintenance dosing and drug...
PMC3003168
core_pubmed_pmc
Preparation and In vitro / In vivo characterization of spray dried microsphere formulation encapsulating 4-chlorocurcumin
Preparation and In vitro / In vivo characterization of spray dried microsphere formulation encapsulating 4-chlorocurcumin Abstract The objective of the present study was to prepare and characterize in vitro and in vivo performance of a sustained release microsphere formulation of 4-chlorocurcumin, a novel curcumin anal...
PMC12155331
core_pubmed_pmc
Targeted Gut Microbiota Modulation Enhances Levodopa Bioavailability and Motor Recovery in MPTP Parkinson’s Disease Models
Targeted Gut Microbiota Modulation Enhances Levodopa Bioavailability and Motor Recovery in MPTP Parkinson’s Disease Models Abstract Abstract Emerging evidence highlights the gut microbiota as a pivotal determinant of pharmacological efficacy. While Enterococcus faecalis ( E. faecalis )-derived tyrosine decarboxylases (...
PMC6151740
core_pubmed_pmc
Pharmacokinetics, Tissue Distribution, and Elimination of Three Active Alkaloids in Rats after Oral Administration of the Effective Fraction of Alkaloids from Ramulus Mori , an Innovative Hypoglycemic Agent
Pharmacokinetics, Tissue Distribution, and Elimination of Three Active Alkaloids in Rats after Oral Administration of the Effective Fraction of Alkaloids from Ramulus Mori , an Innovative Hypoglycemic Agent Abstract Abstract In this study, we systematically investigated the plasma pharmacokinetics, tissue distribution,...
PMC6418203
core_pubmed_pmc
Tracking Decitabine Incorporation into Malignant Myeloid Cell DNA in vitro and in vivo by LC-MS/MS with Enzymatic Digestion
Tracking Decitabine Incorporation into Malignant Myeloid Cell DNA in vitro and in vivo by LC-MS/MS with Enzymatic Digestion Abstract The DNA hypomethylating agents decitabine and 5-azacytidine are the only two drugs approved for treatment of all subtypes of the myeloid malignancy myelodysplastic syndromes (MDS). The ke...
PMC6157701
core_pubmed_pmc
Automated Scale Reduction of Nonlinear QSP Models With an Illustrative Application to a Bone Biology System
Automated Scale Reduction of Nonlinear QSP Models With an Illustrative Application to a Bone Biology System Abstract Integrating quantitative systems pharmacology ( QSP ) into pharmacokinetics/pharmacodynamics ( PKPD ) has resulted in models that are highly complex and often not amenable to further exploration via esti...
PMC12613194
core_pubmed_pmc
Pharmacokinetic evaluation of a long-acting, tasteless oral formulation of enrofloxacin in dogs
Pharmacokinetic evaluation of a long-acting, tasteless oral formulation of enrofloxacin in dogs Abstract Background: Owner medication compliance with the clinician’s prescription can influence the patient’s outcome, among other factors. Extending the dosing interval (DI) may improve medication compliance. Therefore, an...
PMC12654640
core_pubmed_pmc
Design, In Silico, and Experimental Evaluation of Novel Naproxen–Azetidinone Hybrids as Selective COX-2 Inhibitors
Design, In Silico, and Experimental Evaluation of Novel Naproxen–Azetidinone Hybrids as Selective COX-2 Inhibitors Abstract The therapeutic use of non-steroidal anti-inflammatory drugs (NSAIDs) is limited by gastrointestinal and renal adverse effects caused by non-selective COX-1 and COX-2 inhibition. To address this i...
PMC10583668
core_pubmed_pmc
Drug interaction potential of high-dose rifampicin in patients with pulmonary tuberculosis
Drug interaction potential of high-dose rifampicin in patients with pulmonary tuberculosis Abstract ABSTRACT Accumulating evidence supports the use of higher doses of rifampicin for tuberculosis (TB) treatment. Rifampicin is a potent inducer of metabolic enzymes and drug transporters, resulting in clinically relevant d...
PMC7477407
core_pubmed_pmc
In vivo studies of a peptidomimetic that targets EGFR dimerization in NSCLC
In vivo studies of a peptidomimetic that targets EGFR dimerization in NSCLC Abstract Studies related to lung cancer have shown a link between human epidermal growth factor receptor-2 (HER2) expression and poor prognosis in patients with non-small cell lung cancer (NSCLC). HER2 overexpression has been observed in 3-38% ...
PMC7905065
core_pubmed_pmc
Benefits of Zebrafish Xenograft Models in Cancer Research
Benefits of Zebrafish Xenograft Models in Cancer Research Abstract Abstract As a promising in vivo tool for cancer research, zebrafish have been widely applied in various tumor studies. The zebrafish xenograft model is a low-cost, high-throughput tool for cancer research that can be established quickly and requires onl...
PMC7076525
core_pubmed_pmc
Pharmacokinetics and Intestinal Metabolism of Compound K in Rats and Mice
Pharmacokinetics and Intestinal Metabolism of Compound K in Rats and Mice Abstract We aimed to investigate the plasma concentration, tissue distribution, and elimination of compound K following the intravenous administration of compound K (2 mg/kg) in rats and mice. The plasma concentrations of compound K in mice were ...
PMC10288421
core_pubmed_pmc
Joint use of population pharmacokinetics and machine learning for optimizing antiepileptic treatment in pediatric population
Joint use of population pharmacokinetics and machine learning for optimizing antiepileptic treatment in pediatric population Abstract Purpose: Unpredictable drug efficacy and safety of combined antiepileptic therapy is a major challenge during pharmacotherapy decisions in everyday clinical practice. The aim of this stu...
PMC6151572
core_pubmed_pmc
Influence of Jiegeng on Pharmacokinetic Properties of Flavonoids and Saponins in Gancao
Influence of Jiegeng on Pharmacokinetic Properties of Flavonoids and Saponins in Gancao Abstract Abstract Jiegeng Gancao decoction, which is composed of Jiegeng and Gancao at a weight ratio of 1:2, was widely used for treating pharyngalgia and cough for thousands of years. Our previous work indicated that Gancao could ...
PMC10672331
core_pubmed_pmc
Early Exposure of Kidney Transplant Recipients with Chronic Antibody-Mediated Rejection to Tocilizumab—A Preliminary Study
Early Exposure of Kidney Transplant Recipients with Chronic Antibody-Mediated Rejection to Tocilizumab—A Preliminary Study Abstract Abstract Tocilizumab prevents clinical worsening of chronic antibody-mediated rejection (CAMR) of kidney transplant recipients. Optimization of this treatment is necessary. We identified t...
PMC8117003
core_pubmed_pmc
Pharmacokinetic Profile and Oral Bioavailability of Diosgenin, Charantin, and Hydroxychalcone From a Polyherbal Formulation
Pharmacokinetic Profile and Oral Bioavailability of Diosgenin, Charantin, and Hydroxychalcone From a Polyherbal Formulation Abstract Background: Diosgenin, charantin, and hydroxychalcone are utilized for standardization of popular antidiabetic herbal drugs Trigonella foenum-graecum L . belonging to family Fabaceae, Mom...
PMC10757808
core_pubmed_pmc
Preparation and Evaluation of Curcumin Derivatives Nanoemulsion Based on Turmeric Extract and Its Antidepressant Effect
Preparation and Evaluation of Curcumin Derivatives Nanoemulsion Based on Turmeric Extract and Its Antidepressant Effect Abstract Abstract Purpose The early stage of this study verified that a turmeric extract (TUR) including 59% curcumin (CU), 22% demethoxycurcumin (DMC), and 18% bisdemethoxycurcumin (BDMC), could enha...
PMC2955234
core_pubmed_pmc
Phase I clinical and pharmacokinetic study of sorafenib in combination with carboplatin and paclitaxel in patients with advanced non–small cell lung cancer
Phase I clinical and pharmacokinetic study of sorafenib in combination with carboplatin and paclitaxel in patients with advanced non–small cell lung cancer Abstract Summary Objectives Unsatisfactory efficacy of current treatments for advanced lung cancer has prompted the search for new therapies, with sorafenib, a mult...
PMC11652823
core_pubmed_pmc
Population Pharmacokinetics of Trimethoprim/Sulfamethoxazole: Dosage Optimization for Patients with Renal Insufficiency or Receiving Continuous Renal Replacement Therapy
Population Pharmacokinetics of Trimethoprim/Sulfamethoxazole: Dosage Optimization for Patients with Renal Insufficiency or Receiving Continuous Renal Replacement Therapy Abstract Abstract The goal of the study was to describe the population pharmacokinetics of trimethoprim, sulfamethoxazole, and N ‐acetyl sulfamethoxaz...
PMC9649448
core_pubmed_pmc
Challenges associated with test dose pharmacokinetic predictions of high dose melphalan exposure in patients with multiple myeloma
Challenges associated with test dose pharmacokinetic predictions of high dose melphalan exposure in patients with multiple myeloma Abstract Abstract Aim To evaluate the accuracy of melphalan test dose pharmacokinetic (PK) predictions of the subsequent high dose (HDM) area under the concentration-versus-time curve (AUC)...
PMC6458548
core_pubmed_pmc
Development of a UHPLC-MS/MS Method for the Determination of Quercetin in Milk and its Application to a Pharmacokinetic Study
Development of a UHPLC-MS/MS Method for the Determination of Quercetin in Milk and its Application to a Pharmacokinetic Study Abstract Abstract Introduction Quercetin is a polyphenolic flavonoid which has been used in traditional Chinese medicine as a natural therapeutic agent with a broad spectrum of activities (antio...
PMC8606670
core_pubmed_pmc
Baicalin Enhanced Oral Bioavailability of Sorafenib in Rats by Inducing Intestine Absorption
Baicalin Enhanced Oral Bioavailability of Sorafenib in Rats by Inducing Intestine Absorption Abstract Background: Sorafenib (SOR) is an oral, potent, selective, irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) used as the first-line therapy for advanced hepatocellular carcinoma (HCC). ...
PMC7267287
core_pubmed_pmc
The Approved Dose of Ivermectin Alone is not the Ideal Dose for the Treatment of COVID‐19
The Approved Dose of Ivermectin Alone is not the Ideal Dose for the Treatment of COVID‐19 Abstract Caly et al . 1 reported that ivermectin inhibited severe acute respiratory syndrome‐coronavirus 2 (SARS‐CoV‐2) in vitr o for up to 48 hours using ivermectin at 5 μM. The concentration resulting in 50% inhibition (IC 50 ; ...
PMC12426407
core_pubmed_pmc
Bibliometrics-guided cyberpharmacology and transcriptomics for multidimensional analysis of the antihepatic fibrosis mechanism of kaempferol
Bibliometrics-guided cyberpharmacology and transcriptomics for multidimensional analysis of the antihepatic fibrosis mechanism of kaempferol Abstract Abstract Introduction Hepatic Fibrosis (HF), a pathological remodeling process triggered by persistent liver damage, is marked by the excessive buildup of extracellular m...