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PMC7007438
core_pubmed_pmc
Fast-Acting Insulin Aspart: A Review of its Pharmacokinetic and Pharmacodynamic Properties and the Clinical Consequences
Fast-Acting Insulin Aspart: A Review of its Pharmacokinetic and Pharmacodynamic Properties and the Clinical Consequences Abstract Fast-acting insulin aspart (faster aspart) is insulin aspart (IAsp) with two added excipients, l -arginine and niacinamide, to ensure formulation stability with accelerated initial absorptio...
PMC12597552
core_pubmed_pmc
Inhibitory effects of Δ 8-tetrahydrocannabinol on major hepatic cytochrome P450 enzymes and implications for drug disposition 🅂
Inhibitory effects of Δ 8-tetrahydrocannabinol on major hepatic cytochrome P450 enzymes and implications for drug disposition 🅂 Abstract Abstract The increased use of cannabis in many parts of the United States and other countries has led to a need for a more comprehensive understanding of cannabis constituents and th...
PMC5817081
core_pubmed_pmc
Sex Differences in the Effects of a Kappa Opioid Receptor Antagonist in the Forced Swim Test
Sex Differences in the Effects of a Kappa Opioid Receptor Antagonist in the Forced Swim Test Abstract There is growing evidence that kappa opioid receptor (KOR) antagonists could be a useful class of therapeutics for treating depression and anxiety. However, the overwhelming majority of preclinical investigations exami...
PMC8429912
core_pubmed_pmc
Time effect of rutaecarpine on caffeine pharmacokinetics in rats
Time effect of rutaecarpine on caffeine pharmacokinetics in rats Abstract Abstract Rutaecarpine is reported as a potent inducer of CYP1A2 enzyme in rats. There are natural herbal supplements containing rutaecarpine that are designed to enhance the CYP1A2-dependent removal of caffeine from blood so that people can have ...
PMC12312594
core_pubmed_pmc
Indian medicinal phytocompounds for targeting apoptosis and high-penetrance genes in triple-negative breast cancer: an in-silico exploration
Indian medicinal phytocompounds for targeting apoptosis and high-penetrance genes in triple-negative breast cancer: an in-silico exploration Abstract Triple-negative breast cancer (TNBC) presents a significant therapeutic challenge due to its aggressive nature, lack of hormone receptors, and limited targeted treatment ...
PMC6446049
core_pubmed_pmc
No synergistic effect of subtherapeutic doses of donepezil and EVP-6124 in healthy elderly subjects in a scopolamine challenge model
No synergistic effect of subtherapeutic doses of donepezil and EVP-6124 in healthy elderly subjects in a scopolamine challenge model Abstract Abstract Introduction Donepezil is a widely used cholinesterase inhibitor in the management of Alzheimer's disease. Despite large-scaled evidence for its efficacy, elevated perip...
PMC12245853
core_pubmed_pmc
Lymphatic uptake and pharmacokinetics of lipid conjugated brush PEG polymers is altered by interactions with albumin and lipoproteins
Lymphatic uptake and pharmacokinetics of lipid conjugated brush PEG polymers is altered by interactions with albumin and lipoproteins Abstract Abstract Introduction Increased recognition of the role of lymphatics in disease has brought increased focus on the design of lymph-directed delivery systems for imaging agents ...
PMC9217867
core_pubmed_pmc
Therapeutic drug monitoring of atomoxetine in children and adolescents with attention-deficit/ hyperactivity disorder: a naturalistic study
Therapeutic drug monitoring of atomoxetine in children and adolescents with attention-deficit/ hyperactivity disorder: a naturalistic study Abstract Abstract The selective norepinephrine reuptake inhibitor atomoxetine is potentially among the first-line pharmacotherapy options for ADHD. Therapeutic drug monitoring (TDM...
PMC11681108
core_pubmed_pmc
Pharmacogenomic landscape of the Thai population from genome sequencing of 949 individuals
Pharmacogenomic landscape of the Thai population from genome sequencing of 949 individuals Abstract Inter-individual variability in drug responses is significantly influenced by genetic factors, underscoring the importance of population-specific pharmacogenomic studies to optimize clinical outcomes. In this study, we a...
PMC11780097
core_pubmed_pmc
Advanced bioanalytical techniques for pharmacokinetic studies of nanocarrier drug delivery systems
Advanced bioanalytical techniques for pharmacokinetic studies of nanocarrier drug delivery systems Abstract Significant investment in nanocarrier drug delivery systems (Nano-DDSs) has yielded only a limited number of successfully marketed nanomedicines, highlighting a low rate of clinical translation. A primary contrib...
PMC6340874
core_pubmed_pmc
Targeting CD74 in multiple myeloma with the novel, site-specific antibody-drug conjugate STRO-001
Targeting CD74 in multiple myeloma with the novel, site-specific antibody-drug conjugate STRO-001 Abstract Abstract STRO-001 is a site-specific, predominantly single-species, fully human, aglycosylated anti-CD74 antibody-drug conjugate incorporating a non-cleavable linker-maytansinoid warhead with a drug-antibody ratio...
PMC10056844
core_pubmed_pmc
Implementation of Systematic Bioanalysis of Antibody–Drug Conjugates for Preclinical Pharmacokinetic Study of Ado-Trastuzumab Emtansine (T-DM1) in Rats
Implementation of Systematic Bioanalysis of Antibody–Drug Conjugates for Preclinical Pharmacokinetic Study of Ado-Trastuzumab Emtansine (T-DM1) in Rats Abstract Abstract Antibody–drug conjugates (ADCs) are composed of monoclonal antibodies covalently bound to cytotoxic drugs by a linker. They are designed to selectivel...
PMC12683832
core_pubmed_pmc
Tumor marker–guided precision BNCT for CA19-9–positive cancers: a new paradigm in molecularly targeted chemoradiation therapy
Tumor marker–guided precision BNCT for CA19-9–positive cancers: a new paradigm in molecularly targeted chemoradiation therapy Abstract Abstract Background Boron neutron capture therapy (BNCT) is a molecularly targeted chemoradiation modality that relies on boron delivery agents such as p-borophenylalanine (BPA), which ...
PMC12372832
core_pubmed_pmc
Combatting antibiotic resistance in Gardnerella vaginalis : A comparative in silico investigation for drug target identification
Combatting antibiotic resistance in Gardnerella vaginalis : A comparative in silico investigation for drug target identification Abstract Gardnerella vaginalis is the most frequently identified bacterium in approximately 95% of bacterial vaginosis (BV) cases. This species often exhibits resistance to multiple antibioti...
PMC8002378
core_pubmed_pmc
Evaluation of Hydroxychloroquine Blood Concentrations and Effects in Childhood-Onset Systemic Lupus Erythematosus
Evaluation of Hydroxychloroquine Blood Concentrations and Effects in Childhood-Onset Systemic Lupus Erythematosus Abstract Abstract Background: Hydroxychloroquine (HCQ) is an antimalarial agent given to patients with systemic lupus erythematosus (SLE) as first-line therapy. It alleviates childhood-onset systemic lupus ...
PMC12633518
core_pubmed_pmc
Network-based disease fingerprinting with neuroinflammation PET imaging
Network-based disease fingerprinting with neuroinflammation PET imaging Abstract Abstract Neuroinflammation is a hallmark of numerous neurodegenerative, psychiatric, and chronic pain disorders and can be assessed in vivo with 18 kDa translocator protein (TSPO) positron emission tomography (PET). However, conventional q...
PMC8598303
core_pubmed_pmc
In vitro antibiotic activity against intraosteoblastic Staphylococcus aureus : a narrative review of the literature
In vitro antibiotic activity against intraosteoblastic Staphylococcus aureus : a narrative review of the literature Abstract Abstract Staphylococcus aureus – a major aetiological agent of bone and joint infection (BJI) – is associated with a high risk of relapse and chronicity, in part due to its ability to invade and ...
PMC9124359
core_pubmed_pmc
A semimechanistic population pharmacokinetic and pharmacodynamic model incorporating autoinduction for the dose justification of TAS‐114
A semimechanistic population pharmacokinetic and pharmacodynamic model incorporating autoinduction for the dose justification of TAS‐114 Abstract Abstract TAS‐114 is a dual deoxyuridine triphosphatase (dUTPase) and dihydropyrimidine dehydrogenase (DPD) inhibitor expected to widen the therapeutic index of capecitabine. ...
PMC4640545
core_pubmed_pmc
Polymorphic Variants of SCN1A and EPHX1 Influence Plasma Carbamazepine Concentration, Metabolism and Pharmacoresistance in a Population of Kosovar Albanian Epileptic Patients
Polymorphic Variants of SCN1A and EPHX1 Influence Plasma Carbamazepine Concentration, Metabolism and Pharmacoresistance in a Population of Kosovar Albanian Epileptic Patients Abstract Abstract Aim The present study aimed to evaluate the effects of gene variants in key genes influencing pharmacokinetic and pharmacodynam...
PMC6936434
core_pubmed_pmc
How delayed and non-adherent treatment contribute to onward transmission of malaria: a modelling study
How delayed and non-adherent treatment contribute to onward transmission of malaria: a modelling study Abstract Abstract Introduction Artemether-lumefantrine (AL) is the most widely-recommended treatment for uncomplicated Plasmodium falciparum malaria. Its efficacy has been extensively assessed in clinical trials. In r...
PMC12813646
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Immunogenicity of a BTLA Agonist Antibody (Venanprubart) in Healthy Participants, Patients with Systemic Lupus Erythematosus, and Patients with Psoriasis: Results From Three Phase 1 Studies
Safety, Tolerability, Pharmacokinetics, and Immunogenicity of a BTLA Agonist Antibody (Venanprubart) in Healthy Participants, Patients with Systemic Lupus Erythematosus, and Patients with Psoriasis: Results From Three Phase 1 Studies Abstract Abstract Venanprubart (LY3361237), an agonist antibody to B and T lymphocyte ...
PMC8086018
core_pubmed_pmc
Effect of body mass index on pharmacokinetics of paclitaxel in patients with early breast cancer
Effect of body mass index on pharmacokinetics of paclitaxel in patients with early breast cancer Abstract ABSTRACT Background Paclitaxel is dosed according to body surface area (BSA) but there is scant information on actual drug exposure in overweight and obese patients. Methods Early breast cancer patients receiving p...
PMC4474860
core_pubmed_pmc
Defining the Pharmacodynamic Profile and Therapeutic Index of NHS-IL12 Immunocytokine in Dogs with Malignant Melanoma
Defining the Pharmacodynamic Profile and Therapeutic Index of NHS-IL12 Immunocytokine in Dogs with Malignant Melanoma Abstract Abstract Background Interleukin (IL)-12 is a pro-inflammatory cytokine that mediates T-helper type 1 responses and cytotoxic T-cell activation, contributing to its utility as anti-cancer agent....
PMC4168384
core_pubmed_pmc
Population pharmacokinetics of levodopa in subjects with advanced Parkinson's disease: levodopa-carbidopa intestinal gel infusion vs . oral tablets
Population pharmacokinetics of levodopa in subjects with advanced Parkinson's disease: levodopa-carbidopa intestinal gel infusion vs . oral tablets Abstract Abstract Aims Levodopa-carbidopa intestinal gel (LCIG) provides continuous levodopa-carbidopa delivery through intrajejunal infusion. This study characterized the ...
PMC4600319
core_pubmed_pmc
Pharmacokinetic interactions between artesunate-mefloquine and ritonavir-boosted lopinavir in healthy Thai adults
Pharmacokinetic interactions between artesunate-mefloquine and ritonavir-boosted lopinavir in healthy Thai adults Abstract Abstract Background Concomitant use of anti-malarial and antiretroviral drugs is increasingly frequent in malaria and HIV endemic regions. The aim of the study was to investigate the pharmacokineti...
PMC11534596
core_pubmed_pmc
Green rush and red warnings: Retrospective chart review of adverse events of interactions between cannabinoids and psychotropic drugs
Green rush and red warnings: Retrospective chart review of adverse events of interactions between cannabinoids and psychotropic drugs Abstract Abstract Aim Our objective was to systematically assess the prevalence and clinical features of adverse events related to interactions between cannabinoids and psychotropic drug...
PMC8143107
core_pubmed_pmc
Mechanistic Modelling Identifies and Addresses the Risks of Empiric Concentration-Guided Sorafenib Dosing
Mechanistic Modelling Identifies and Addresses the Risks of Empiric Concentration-Guided Sorafenib Dosing Abstract Abstract The primary objective of this study is to evaluate the capacity of concentration-guided sorafenib dosing protocols to increase the proportion of patients that achieve a sorafenib maximal concentra...
PMC10338392
core_pubmed_pmc
Estradiol and Spironolactone Plasma Pharmacokinetics Among Brazilian Transgender Women Using HIV Pre-Exposure Prophylaxis: Analysis of Potential Interactions
Estradiol and Spironolactone Plasma Pharmacokinetics Among Brazilian Transgender Women Using HIV Pre-Exposure Prophylaxis: Analysis of Potential Interactions Abstract Background and Objective An important barrier to HIV prevention among transgender women (TGW) is the concern that oral pre-exposure prophylaxis (PrEP) ne...
PMC11207434
core_pubmed_pmc
A Physiologically Based Pharmacokinetic (PBPK) Study to Assess the Adjuvanticity of Three Peptides in an Oral Vaccine
A Physiologically Based Pharmacokinetic (PBPK) Study to Assess the Adjuvanticity of Three Peptides in an Oral Vaccine Abstract Following up on the first PBPK model for an oral vaccine built for alpha-tocopherol, three peptides are explored in this article to verify if they could support an oral vaccine formulation as a...
PMC4145418
core_pubmed_pmc
Sarilumab, a fully human monoclonal antibody against IL-6Rα in patients with rheumatoid arthritis and an inadequate response to methotrexate: efficacy and safety results from the randomised SARIL-RA-MOBILITY Part A trial
Sarilumab, a fully human monoclonal antibody against IL-6Rα in patients with rheumatoid arthritis and an inadequate response to methotrexate: efficacy and safety results from the randomised SARIL-RA-MOBILITY Part A trial Abstract Objectives To evaluate safety and efficacy of weekly (qw) and every other week (q2w) dosin...
PMC3757857
core_pubmed_pmc
Design and Development of Polyethylene Oxide Based Matrix Tablets for Verapamil Hydrochloride
Design and Development of Polyethylene Oxide Based Matrix Tablets for Verapamil Hydrochloride Abstract In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of verapamil ...
PMC4966608
core_pubmed_pmc
Evaluation of a glycoengineered monoclonal antibody via LC-MS analysis in combination with multiple enzymatic digestion
Evaluation of a glycoengineered monoclonal antibody via LC-MS analysis in combination with multiple enzymatic digestion Abstract ABSTRACT Glycosylation affects the efficacy, safety and pharmacokinetics/pharmacodynamics properties of therapeutic monoclonal antibodies (mAbs), and glycoengineering is now being used to pro...
PMC11225352
core_pubmed_pmc
A multicenter, randomized, double-blind, placebo-controlled ascending dose study to evaluate the safety, tolerability, pharmacokinetics (PK) and pharmacodynamic (PD) effects of Posiphen in subjects with early Alzheimer’s Disease
A multicenter, randomized, double-blind, placebo-controlled ascending dose study to evaluate the safety, tolerability, pharmacokinetics (PK) and pharmacodynamic (PD) effects of Posiphen in subjects with early Alzheimer’s Disease Abstract Background Amyloid beta protein (Aβ) is a treatment target in Alzheimer’s Disease ...
PMC9329971
core_pubmed_pmc
Pharmacokinetic Characterization and Comparative Bioavailability of an Innovative Orodispersible Fixed-Dose Combination of Ivermectin and Albendazole: A Single Dose, Open Label, Sequence Randomized, Crossover Clinical Trial in Healthy Volunteers
Pharmacokinetic Characterization and Comparative Bioavailability of an Innovative Orodispersible Fixed-Dose Combination of Ivermectin and Albendazole: A Single Dose, Open Label, Sequence Randomized, Crossover Clinical Trial in Healthy Volunteers Abstract Soil-transmitted helminths are intestinal worm diseases transmitt...
PMC8246954
core_pubmed_pmc
First‐in‐Human, Single‐ and Multiple‐Ascending‐Dose Studies in Healthy Subjects to Assess Pharmacokinetics, Pharmacodynamics, and Safety/Tolerability of Iberdomide, a Novel Cereblon E3 Ligase Modulator
First‐in‐Human, Single‐ and Multiple‐Ascending‐Dose Studies in Healthy Subjects to Assess Pharmacokinetics, Pharmacodynamics, and Safety/Tolerability of Iberdomide, a Novel Cereblon E3 Ligase Modulator Abstract Abstract Pharmacokinetics, pharmacodynamics, and safety/tolerability of iberdomide (CC‐220), a highly potent ...
PMC9193593
core_pubmed_pmc
Gender Differences in Levodopa Pharmacokinetics in Levodopa-Naïve Patients With Parkinson’s Disease
Gender Differences in Levodopa Pharmacokinetics in Levodopa-Naïve Patients With Parkinson’s Disease Abstract Abstract Background Levodopa (LD) is the most effective drug in the treatment of Parkinson’s disease (PD). Unfortunately, prolonged use of LD leads to complications, mainly motor/non-motor fluctuations (MNMF) an...
PMC2854761
core_pubmed_pmc
Probabilistic Modeling of Dietary Arsenic Exposure and Dose and Evaluation with 2003–2004 NHANES Data
Probabilistic Modeling of Dietary Arsenic Exposure and Dose and Evaluation with 2003–2004 NHANES Data Abstract Abstract Background Dietary exposure from food to toxic inorganic arsenic (iAs) in the general U.S. population has not been well studied. Objectives The goal of this research was to quantify dietary As exposur...
PMC12845374
core_pubmed_pmc
Cinobufagin as a Potential Intervention Against Liver Cancer—A Comprehensive Review
Cinobufagin as a Potential Intervention Against Liver Cancer—A Comprehensive Review Abstract Liver cancer remains a significant global health challenge, with hepatocellular carcinoma (HCC) being the most prevalent form. Despite advancements in treatment, high recurrence rates and the limited efficacy of conventional th...
PMC8504805
core_pubmed_pmc
Applicability of ancestral genotyping in pharmacogenomic research with hormonal contraception
Applicability of ancestral genotyping in pharmacogenomic research with hormonal contraception Abstract Abstract To compare etonogestrel pharmacokinetic and pharmacodynamic outcomes by both self‐reported race/ethnicity and genetically determined ancestry among contraceptive implant users. We conducted a secondary analys...
PMC11434026
core_pubmed_pmc
Development and Validation of an LC-MS/MS Assay for the Quantitation of MO-OH-Nap Tropolone in Mouse Plasma: Application to In Vitro and In Vivo Pharmacokinetic Studies
Development and Validation of an LC-MS/MS Assay for the Quantitation of MO-OH-Nap Tropolone in Mouse Plasma: Application to In Vitro and In Vivo Pharmacokinetic Studies Abstract Abstract A rapid, selective, and sensitive liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) method was developed and val...
PMC8377513
core_pubmed_pmc
Impact of Serum Proteins on the Uptake and RNAi Activity of GalNAc-Conjugated siRNAs
Impact of Serum Proteins on the Uptake and RNAi Activity of GalNAc-Conjugated siRNAs Abstract Serum protein interactions are evaluated during the drug development process since they determine the free drug concentration in blood and thereby can influence the drug's pharmacokinetic and pharmacodynamic properties. While ...
PMC10702772
core_pubmed_pmc
Pragmatic physiologically-based pharmacokinetic modeling to support clinical implementation of optimized gentamicin dosing in term neonates and infants: proof-of-concept
Pragmatic physiologically-based pharmacokinetic modeling to support clinical implementation of optimized gentamicin dosing in term neonates and infants: proof-of-concept Abstract Abstract Introduction Modeling and simulation can support dosing recommendations for clinical practice, but a simple framework is missing. In...
PMC8961007
core_pubmed_pmc
Predicting Nanoparticle Delivery to Tumors Using Machine Learning and Artificial Intelligence Approaches
Predicting Nanoparticle Delivery to Tumors Using Machine Learning and Artificial Intelligence Approaches Abstract Abstract Background Low delivery efficiency of nanoparticles (NPs) to the tumor is a critical barrier in the field of cancer nanomedicine. Strategies on how to improve NP tumor delivery efficiency remain to...
PMC8927781
core_pubmed_pmc
Quantification of Fetal Renal Function Using Fetal Urine Production Rate and Its Reflection on the Amniotic and Fetal Creatinine Levels During Pregnancy
Quantification of Fetal Renal Function Using Fetal Urine Production Rate and Its Reflection on the Amniotic and Fetal Creatinine Levels During Pregnancy Abstract Adequate prediction of fetal exposure of drugs excreted by the kidney requires the incorporation of time-varying renal function parameters into a pharmacokine...
PMC7470780
core_pubmed_pmc
Comparative strategies for stem cell biodistribution in a preclinical study
Comparative strategies for stem cell biodistribution in a preclinical study Abstract Abstract Stem cell therapy represents the potential alternative effective strategy for some diseases that lack effective treatment currently. Correspondingly, it is crucial to establish high-sensitive and reliable quantification assay ...
PMC8246438
core_pubmed_pmc
Target-based drug discovery, ADMET profiling and bioactivity studies of antibiotics as potential inhibitors of SARS-CoV-2 main protease (M pro )
Target-based drug discovery, ADMET profiling and bioactivity studies of antibiotics as potential inhibitors of SARS-CoV-2 main protease (M pro ) Abstract Abstract A recent outbreak of a new strain of Coronavirus (SARS-CoV-2) has become a global health burden, which has resulted in deaths. No proven drug has been found ...
PMC9847229
core_pubmed_pmc
CuAAC ensembled 1,2,3-triazole linked nanogels for targeted drug delivery: a review
CuAAC ensembled 1,2,3-triazole linked nanogels for targeted drug delivery: a review Abstract Copper( i ) catalyzed alkyne azide cycloaddition (CuAAC), the quintessential example of ‘click chemistry’, provides an adaptable and adequate platform for the synthesis of nanogels for sustained drug release at targeted sites b...
PMC9727091
core_pubmed_pmc
Safety, pharmacokinetics, and pharmacodynamics of SHR7280, an oral gonadotropin-releasing hormone antagonist in healthy premenopausal women
Safety, pharmacokinetics, and pharmacodynamics of SHR7280, an oral gonadotropin-releasing hormone antagonist in healthy premenopausal women Abstract Background: Treatment with gonadotropin-releasing hormone (GnRH) antagonists is a powerful strategy to suppress gonadotropin activity in women with sex hormone-dependent d...
PMC11459968
core_pubmed_pmc
Prospectively predicting BPaMZ phase IIb/III trial outcomes using a translational mouse-to-human platform
Prospectively predicting BPaMZ phase IIb/III trial outcomes using a translational mouse-to-human platform Abstract ABSTRACT Despite known treatments, tuberculosis (TB) remains the world’s top infectious killer, highlighting the pressing need for new drug regimens. To prioritize the most efficacious drugs for clinical t...
PMC5847195
core_pubmed_pmc
Applications of bacteriophages versus phage enzymes to combat and cure bacterial infections: an ambitious and also a realistic application?
Applications of bacteriophages versus phage enzymes to combat and cure bacterial infections: an ambitious and also a realistic application? Abstract Bacteriophages (phages) are viruses that infect bacteria. The “predator–prey” interactions are recognized as a potentially effective way to treat infections. Phages, as we...
PMC9160745
core_pubmed_pmc
Pharmacokinetics and Genetic Factors of Atorvastatin in Healthy Korean Subjects
Pharmacokinetics and Genetic Factors of Atorvastatin in Healthy Korean Subjects Abstract Abstract Background: Statins are the most popular agents for the primary and secondary prevention of cardiovascular disease; however, the pharmacokinetic parameters and associated genetic factors in the Korean population have not b...
PMC10975877
core_pubmed_pmc
Plasma Concentrations of Oral Ondansetron in Hospitalized Dogs Exhibiting Clinical Signs of Nausea
Plasma Concentrations of Oral Ondansetron in Hospitalized Dogs Exhibiting Clinical Signs of Nausea Abstract Abstract Simple Summary Oral ondansetron is commonly prescribed to treat nausea and vomiting in dogs, but no studies have evaluated how well it is absorbed in clinical patients after oral administration. The obje...
PMC9741938
core_pubmed_pmc
A comparison of different methods for the first-in-pediatric dose selection
A comparison of different methods for the first-in-pediatric dose selection Abstract Abstract Background and Aim: To conduct a pediatric clinical trial, it is important to optimize pediatric dose as accurately as possible. This is mainly because due to ethical reasons, children cannot be given several doses to evaluate...
PMC7515939
core_pubmed_pmc
A phase I, randomized, single-dose pharmacokinetic study comparing sb8 (bevacizumab biosimilar) with reference bevacizumab in healthy volunteers
A phase I, randomized, single-dose pharmacokinetic study comparing sb8 (bevacizumab biosimilar) with reference bevacizumab in healthy volunteers Abstract Abstract Purpose To compare pharmacokinetics, safety, tolerability, and immunogenicity between SB8, a bevacizumab biosimilar, and the European Union (EU) and United S...
PMC10225222
core_pubmed_pmc
Isatuximab in combination with cemiplimab in patients with relapsed/refractory multiple myeloma: A phase 1/2 study
Isatuximab in combination with cemiplimab in patients with relapsed/refractory multiple myeloma: A phase 1/2 study Abstract Abstract Background Given the incurable nature of multiple myeloma (MM), efforts are made to improve the efficacy of anti‐CD38 monoclonal antibodies via combinations with other potentially synergi...
PMC8010682
core_pubmed_pmc
Influence of the Circadian Timing System on Tacrolimus Pharmacokinetics and Pharmacodynamics After Kidney Transplantation
Influence of the Circadian Timing System on Tacrolimus Pharmacokinetics and Pharmacodynamics After Kidney Transplantation Abstract Introduction: Tacrolimus is the backbone immunosuppressant after solid organ transplantation. Tacrolimus has a narrow therapeutic window with large intra- and inter-patient pharmacokinetic ...
PMC12474757
core_pubmed_pmc
Paving the way for future PSMA inhibitors: insights from comparative preclinical evaluations of structure modifications
Paving the way for future PSMA inhibitors: insights from comparative preclinical evaluations of structure modifications Abstract Abstract Background Prostate-specific membrane antigen (PSMA) is an established target for the imaging and treatment of prostate cancer. This study focused on the preclinical evaluation of th...
PMC7201037
core_pubmed_pmc
Model-Informed Precision Dosing of Vancomycin in Hospitalized Children: Implementation and Adoption at an Academic Children’s Hospital
Model-Informed Precision Dosing of Vancomycin in Hospitalized Children: Implementation and Adoption at an Academic Children’s Hospital Abstract Background Model-informed precision dosing (MIPD) can serve as a powerful tool during therapeutic drug monitoring (TDM) to help individualize dosing in populations with large p...
PMC10998725
core_pubmed_pmc
Ebselen: A Promising Repurposing Drug to Treat Infections Caused by Multidrug-Resistant Microorganisms
Ebselen: A Promising Repurposing Drug to Treat Infections Caused by Multidrug-Resistant Microorganisms Abstract Abstract Bacterial multiresistance to drugs is a rapidly growing global phenomenon. New resistance mechanisms have been described in different bacterial pathogens, threatening the effective treatment of even ...
PMC3558989
core_pubmed_pmc
In vitro activity (MICs and rate of kill) of AFN-1252, a novel FabI inhibitor, in the presence of serum and in combination with other antibiotics
In vitro activity (MICs and rate of kill) of AFN-1252, a novel FabI inhibitor, in the presence of serum and in combination with other antibiotics Abstract AFN-1252 is a novel inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 exhibits typical MIC 90 values of ⩽0·015 μg/ml ...
PMC11471595
core_pubmed_pmc
Quality by design-based approach for the development of an analytical method for quantifying ponatinib in rat plasma
Quality by design-based approach for the development of an analytical method for quantifying ponatinib in rat plasma Abstract Abstract Ponatinib is a potent tyrosine kinase inhibitor that is approved for the treatment of chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia. To furt...
PMC8381505
core_pubmed_pmc
Phase 1 clinical trial of the PI3Kδ inhibitor YY-20394 in patients with B-cell hematological malignancies
Phase 1 clinical trial of the PI3Kδ inhibitor YY-20394 in patients with B-cell hematological malignancies Abstract Abstract YY-20394, an oral phosphatidylinositol 3-kinase delta (PI3Kδ) inhibitor, was investigated in a first-in-human study of patients with relapsed or refractory B-cell malignancies. During dose escalat...
PMC9584355
core_pubmed_pmc
A Review of Population Pharmacokinetic Models of Posaconazole
A Review of Population Pharmacokinetic Models of Posaconazole Abstract Abstract Posaconazole is often used for the prophylaxis and treatment of invasive fungal infections (IFI). However, intra- and inter-individual differences and drug interactions affect the efficacy and safety of posaconazole. Precision dosing of pos...
PMC12358310
core_pubmed_pmc
Population Pharmacokinetics and Exposure–Response Relationships of Maribavir in Transplant Recipients With First Episode or Refractory Cytomegalovirus
Population Pharmacokinetics and Exposure–Response Relationships of Maribavir in Transplant Recipients With First Episode or Refractory Cytomegalovirus Abstract ABSTRACT Maribavir's anti‐cytomegalovirus (CMV) activity and favorable safety/tolerability profile is a welcomed addition to the CMV treatment armamentarium. To...
PMC12745671
core_pubmed_pmc
Hormonal Contraceptives and Depression: A Proteomic Analysis Using Neuronal Models
Hormonal Contraceptives and Depression: A Proteomic Analysis Using Neuronal Models Abstract ABSTRACT Purpose Hormonal contraceptives are linked to a higher prevalence of depressive symptoms. Given their popularity in Western countries, understanding the biochemical effects on neuronal cells is crucial to minimizing men...
PMC6073741
core_pubmed_pmc
Genetic Susceptibility to Neurodegeneration in Amazon: Apolipoprotein E Genotyping in Vulnerable Populations Exposed to Mercury
Genetic Susceptibility to Neurodegeneration in Amazon: Apolipoprotein E Genotyping in Vulnerable Populations Exposed to Mercury Abstract Human exposure to mercury is a serious problem of public health in Amazon. As in other vulnerable populations throughout the world, Amazonian riverine populations are chronically expo...
PMC9785688
core_pubmed_pmc
Impact of Cytochrome Induction or Inhibition on the Plasma and Brain Kinetics of [ 11 C]metoclopramide, a PET Probe for P-Glycoprotein Function at the Blood-Brain Barrier
Impact of Cytochrome Induction or Inhibition on the Plasma and Brain Kinetics of [ 11 C]metoclopramide, a PET Probe for P-Glycoprotein Function at the Blood-Brain Barrier Abstract Abstract [ 11 C]metoclopramide PET imaging provides a sensitive and translational tool to explore P-glycoprotein (P-gp) function at the bloo...
PMC3601177
core_pubmed_pmc
Phase I clinical trial combining imatinib mesylate and IL-2 in refractory cancer patients
Phase I clinical trial combining imatinib mesylate and IL-2 in refractory cancer patients Abstract Abstract Imatinib mesylate (IM) is a small molecule inhibitor of protein tyrosine kinases. In addition to its direct effect on malignant cells, it has been suggested IM may activate of natural killer (NK) cells, hence exe...
PMC9122504
core_pubmed_pmc
Quantification of Usaramine and its N-Oxide Metabolite in Rat Plasma Using Liquid Chromatography-Tandem Mass Spectrometry
Quantification of Usaramine and its N-Oxide Metabolite in Rat Plasma Using Liquid Chromatography-Tandem Mass Spectrometry Abstract Abstract A sensitive, fast and robust liquid chromatography--tandem mass spectrometry (LC–MS-MS) method was developed and validated for the determination of usaramine (URM) and usaramine N-...
PMC12625133
core_pubmed_pmc
Population Pharmacokinetics and Exposure‐Response Modeling for Evinacumab in Children, Adolescents, and Adults With Homozygous Familial Hypercholesterolemia
Population Pharmacokinetics and Exposure‐Response Modeling for Evinacumab in Children, Adolescents, and Adults With Homozygous Familial Hypercholesterolemia Abstract ABSTRACT Evinacumab, an angiopoietin‐like 3 (ANGPTL3) inhibitor, significantly reduces low‐density lipoprotein cholesterol (LDL‐C), independent of low‐den...
PMC12521050
core_pubmed_pmc
Assessing Cytochrome P450 Drug Interaction Risk for Dordaviprone Using Physiologically Based Pharmacokinetic Modeling
Assessing Cytochrome P450 Drug Interaction Risk for Dordaviprone Using Physiologically Based Pharmacokinetic Modeling Abstract ABSTRACT A physiologically based pharmacokinetic (PBPK) model was developed and verified for dordaviprone, a small molecule with antitumor effects in glioma patients. The model was applied to a...
PMC4869670
core_pubmed_pmc
Safety, tolerability, pharmacokinetics, and pharmacodynamics of novel glucokinase activator HMS5552: results from a first-in-human single ascending dose study
Safety, tolerability, pharmacokinetics, and pharmacodynamics of novel glucokinase activator HMS5552: results from a first-in-human single ascending dose study Abstract Abstract Background HMS5552, a novel fourth-generation glucokinase (GK) activator, has demonstrated promising effects on glycemic control in preclinical...
PMC6719061
core_pubmed_pmc
Fusion of Lysostaphin to an Albumin Binding Domain Prolongs Its Half-Life and Bactericidal Activity in the Systemic Circulation
Fusion of Lysostaphin to an Albumin Binding Domain Prolongs Its Half-Life and Bactericidal Activity in the Systemic Circulation Abstract Abstract Antibacterial lysins are promising proteins that are active against both antibiotic-susceptible and antibiotic-resistant bacterial strains. However, a major limitation of ant...
PMC6058670
core_pubmed_pmc
Preparation and evaluation of injectable Rasagiline mesylate dual-controlled drug delivery system for the treatment of Parkinson’s disease
Preparation and evaluation of injectable Rasagiline mesylate dual-controlled drug delivery system for the treatment of Parkinson’s disease Abstract Abstract A microsphere–gel in situ forming implant (MS–Gel ISFI) dual-controlled drug delivery system was applied to a high water-soluble small-molecule compound Rasagiline...
PMC12736313
core_pubmed_pmc
Curcumin and Resveratrol vs. Ferrocene-Modified Polyphenols: Role in Enhancing Protective Properties in Human Keratinocytes
Curcumin and Resveratrol vs. Ferrocene-Modified Polyphenols: Role in Enhancing Protective Properties in Human Keratinocytes Abstract Background/Objectives : Resveratrol (RSV) and curcumin (CRC) have antioxidant, anti-inflammatory, photoprotective, and cell-repairing properties. We selected them to investigate the poten...
PMC11036873
core_pubmed_pmc
A pharmacokinetic study comparing the biosimilar HEC14028 and Dulaglutide (Trulicity®) in healthy Chinese subjects
A pharmacokinetic study comparing the biosimilar HEC14028 and Dulaglutide (Trulicity®) in healthy Chinese subjects Abstract Abstract This study aimed to evaluate the pharmacokinetics (PKs), safety, and immunogenicity of the biosimilar HEC14028 compared to reference Trulicity® (dulaglutide) in healthy male Chinese subje...
PMC10638505
core_pubmed_pmc
Pulmonary endothelium-targeted nanoassembly of indomethacin and superoxide dismutase relieves lung inflammation
Pulmonary endothelium-targeted nanoassembly of indomethacin and superoxide dismutase relieves lung inflammation Abstract Lung inflammation is an essential inducer of various diseases and is closely related to pulmonary-endothelium dysfunction. Herein, we propose a pulmonary endothelium-targeted codelivery system of ant...
PMC8203185
core_pubmed_pmc
Multiple Administrations of Itraconazole Increase Plasma Exposure to Pyrotinib in Chinese Healthy Adults
Multiple Administrations of Itraconazole Increase Plasma Exposure to Pyrotinib in Chinese Healthy Adults Abstract Purpose Pyrotinib, an irreversible human epidermal growth factor receptor 2 (HER2), is a epidermal growth factor receptor double-target tyrosine kinase inhibitor used for treating HER2-positive breast cance...
PMC10431052
core_pubmed_pmc
Physiologically‐based pharmacokinetic modeling of quinidine to establish a CYP3A4, P‐gp, and CYP2D6 drug–drug–gene interaction network
Physiologically‐based pharmacokinetic modeling of quinidine to establish a CYP3A4, P‐gp, and CYP2D6 drug–drug–gene interaction network Abstract Abstract The antiarrhythmic agent quinidine is a potent inhibitor of cytochrome P450 (CYP) 2D6 and P‐glycoprotein (P‐gp) and is therefore recommended for use in clinical drug–d...
PMC4061112
core_pubmed_pmc
Pharmacokinetics of BPA in Gliomas with Ultrasound Induced Blood-Brain Barrier Disruption as Measured by Microdialysis
Pharmacokinetics of BPA in Gliomas with Ultrasound Induced Blood-Brain Barrier Disruption as Measured by Microdialysis Abstract Abstract The blood-brain barrier (BBB) can be transiently disrupted by focused ultrasound (FUS) in the presence of microbubbles for targeted drug delivery. Previous studies have illustrated th...
PMC3142764
core_pubmed_pmc
Metformin as an energy restriction mimetic agent for breast cancer prevention
Metformin as an energy restriction mimetic agent for breast cancer prevention Abstract Abstract Background: This study examined whether metformin administration inhibited chemically induced mammary carcinogenesis in rats. In cancer prevention, metformin may act (1) indirectly through reducing systemic risk factors; or ...
PMC9101087
core_pubmed_pmc
A Sensitive LC-MS/MS Method for the Simultaneous Determination of Two Thia-Analogous Indirubin N -Glycosides and Indirubin-3′-Monoxime in Plasma and Cell Culture Medium
A Sensitive LC-MS/MS Method for the Simultaneous Determination of Two Thia-Analogous Indirubin N -Glycosides and Indirubin-3′-Monoxime in Plasma and Cell Culture Medium Abstract Abstract Indirubin was identified as an active component of Danggui Longhui Wan, an herbal mixture used in traditional Chinese medicine, and s...
PMC11372363
core_pubmed_pmc
HPN328, a Trispecific T Cell–Activating Protein Construct Targeting DLL3-Expressing Solid Tumors
HPN328, a Trispecific T Cell–Activating Protein Construct Targeting DLL3-Expressing Solid Tumors Abstract Abstract Delta-like ligand 3 (DLL3) is expressed in more than 70% of small cell lung cancers (SCLCs) and other neuroendocrine-derived tumor types. SCLC is highly aggressive, and limited therapeutic options lead to ...
PMC4108101
core_pubmed_pmc
Amikacin Pharmacokinetics During Continuous Veno-Venous Hemodialysis
Amikacin Pharmacokinetics During Continuous Veno-Venous Hemodialysis Abstract Introduction Little is known about the pharmacokinetics of amikacin during continuous renal replacement therapy. Methods This prospective observational study included patients admitted to an academic medical center who received amikacin thera...
PMC7198615
core_pubmed_pmc
Predicting circulating biomarker response and its impact on the survival of advanced melanoma patients treated with adjuvant therapy
Predicting circulating biomarker response and its impact on the survival of advanced melanoma patients treated with adjuvant therapy Abstract Abstract Advanced melanoma remains a disease with poor prognosis. Several serologic markers have been investigated to help monitoring and prognostication, but to date only lactat...
PMC10101612
core_pubmed_pmc
Tolvaptan for Children and Adolescents with Autosomal Dominant Polycystic Kidney Disease
Tolvaptan for Children and Adolescents with Autosomal Dominant Polycystic Kidney Disease Abstract Background Tolvaptan slows expansion of kidney volume and kidney function decline in adults with autosomal dominant polycystic kidney disease (ADPKD). Progression during childhood could be treated before irreversible kidne...
PMC4244559
core_pubmed_pmc
Ethnic comparison of pharmacokinetics of 18 F-florbetaben, a PET tracer for beta-amyloid imaging, in healthy Caucasian and Japanese subjects
Ethnic comparison of pharmacokinetics of 18 F-florbetaben, a PET tracer for beta-amyloid imaging, in healthy Caucasian and Japanese subjects Abstract Purpose 18 F-Florbetaben is a positron emission tomography (PET) tracer indicated for imaging cerebral beta-amyloid deposition in adult patients with cognitive impairment...
PMC12151714
core_pubmed_pmc
Quantitative analysis of nonsteroidal anti‐inflammatory drugs in dried blood spot from mountain ultra‐trail runners. Contribution of pharmacokinetic models for the interpretation of the results
Quantitative analysis of nonsteroidal anti‐inflammatory drugs in dried blood spot from mountain ultra‐trail runners. Contribution of pharmacokinetic models for the interpretation of the results Abstract Abstract Monitoring of drug use in athletes is of interest both for health and competition‐related issues. Considerin...
PMC8754575
core_pubmed_pmc
Pharmacokinetic Profile of Incremental Oral Doses of Dietary Nitrate in Young and Older Adults: A Crossover Randomized Clinical Trial
Pharmacokinetic Profile of Incremental Oral Doses of Dietary Nitrate in Young and Older Adults: A Crossover Randomized Clinical Trial Abstract ABSTRACT Background Dietary nitrate consumption can increase concentrations of nitrate and nitrite in blood, saliva, and urine. Whether the change in concentrations is influence...
PMC2883227
core_pubmed_pmc
A Supercritical Fluid Chromatography/Tandem Mass Spectrometry Method for the Simultaneous Quantification of Metformin and Gliclazide in Human Plasma
A Supercritical Fluid Chromatography/Tandem Mass Spectrometry Method for the Simultaneous Quantification of Metformin and Gliclazide in Human Plasma Abstract Abstract Present study reports the development and validation of a simultaneous estimation of metformin and gliclazide in human plasma using supercritical fluid c...
PMC11768435
core_pubmed_pmc
Effect of Staggered vs. Simultaneous Co-Administration of Bempedoic Acid on Pharmacokinetics of Pravastatin: Randomized, Cross-Over Clinical Trial in Healthy Volunteers
Effect of Staggered vs. Simultaneous Co-Administration of Bempedoic Acid on Pharmacokinetics of Pravastatin: Randomized, Cross-Over Clinical Trial in Healthy Volunteers Abstract Background/Objectives : Bempedoic acid (BA) is a novel cholesterol-lowering agent with proven positive effects on cardiovascular endpoints. Be...
PMC9088669
core_pubmed_pmc
Development and optimization of a high‐throughput screening assay for in vitro anti‐SARS‐CoV‐2 activity: Evaluation of 5676 Phase 1 Passed Structures
Development and optimization of a high‐throughput screening assay for in vitro anti‐SARS‐CoV‐2 activity: Evaluation of 5676 Phase 1 Passed Structures Abstract Abstract Although vaccines are currently used to control the coronavirus disease 2019 (COVID‐19) pandemic, treatment options are urgently needed for those who ca...
PMC9482228
core_pubmed_pmc
Probabilistic quotient’s work and pharmacokinetics’ contribution: countering size effect in metabolic time series measurements
Probabilistic quotient’s work and pharmacokinetics’ contribution: countering size effect in metabolic time series measurements Abstract Metabolomic time course analyses of biofluids are highly relevant for clinical diagnostics. However, many sampling methods suffer from unknown sample sizes, commonly known as size effe...
PMC12516915
core_pubmed_pmc
Association of Metabolic Genotype Composite CYP3A5*3 and CYP3A4*1B to Tacrolimus Pharmacokinetics in Stable Black and White Kidney Transplant Recipients
Association of Metabolic Genotype Composite CYP3A5*3 and CYP3A4*1B to Tacrolimus Pharmacokinetics in Stable Black and White Kidney Transplant Recipients Abstract ABSTRACT Interpatient variability in tacrolimus pharmacokinetics is due in part to variation in metabolism by cytochrome P‐450 3A5 and 3A4 and membrane transp...
PMC11985842
core_pubmed_pmc
Optimizing fluconazole dosing in acute renal failure patients undergoing continuous renal replacement therapy: A population pharmacokinetic/pharmacodynamic study
Optimizing fluconazole dosing in acute renal failure patients undergoing continuous renal replacement therapy: A population pharmacokinetic/pharmacodynamic study Abstract Abstract Fluconazole pharmacokinetics in acute renal failure (ARF) patients undergoing continuous renal replacement therapy (CRRT) are significantly ...
PMC9020015
core_pubmed_pmc
Determination and pharmacokinetics study of UK-5099 in mouse plasma by LC–MS/MS
Determination and pharmacokinetics study of UK-5099 in mouse plasma by LC–MS/MS Abstract Abstract Background UK-5099 is a potent mitochondrial acetone carrier inhibitor, that exhibits anticancer activity. Recently, the anti- Toxoplasma gondii activity of UK-5099 was proposed, and in vivo studies of its pharmacokinetics...
PMC9015648
core_pubmed_pmc
An Overview of the Evidence and Mechanism of Drug–Herb Interactions Between Propolis and Pharmaceutical Drugs
An Overview of the Evidence and Mechanism of Drug–Herb Interactions Between Propolis and Pharmaceutical Drugs Abstract Abstract With the growing interest in the medicinal use of propolis, numerous studies have reported significant interactions between propolis extract and pharmaceutical drugs which may result in great ...
PMC7273296
core_pubmed_pmc
Investigational treatments for COVID-19 may increase ventricular arrhythmia risk through drug interactions
Investigational treatments for COVID-19 may increase ventricular arrhythmia risk through drug interactions Abstract Many drugs that have been proposed for treatment of COVID-19 are reported to cause cardiac adverse events, including ventricular arrhythmias. In order to properly weigh risks against potential benefits, p...
PMC7576631
core_pubmed_pmc
Population pharmacokinetics of adalimumab biosimilar adalimumab‐adbm and reference product in healthy subjects and patients with rheumatoid arthritis to assess pharmacokinetic similarity
Population pharmacokinetics of adalimumab biosimilar adalimumab‐adbm and reference product in healthy subjects and patients with rheumatoid arthritis to assess pharmacokinetic similarity Abstract Aims Adalimumab‐adbm is a monoclonal antibody developed as a biosimilar to adalimumab (Humira, AbbVie Inc.). The key objecti...
PMC10788056
core_pubmed_pmc
Repaglinide–Solid Lipid Nanoparticles in Chitosan Patches for Transdermal Application: Box–Behnken Design, Characterization, and In Vivo Evaluation
Repaglinide–Solid Lipid Nanoparticles in Chitosan Patches for Transdermal Application: Box–Behnken Design, Characterization, and In Vivo Evaluation Abstract Abstract Background Repaglinide (REP) is an antidiabetic drug with limited oral bioavailability attributable to its low solubility and considerable first-pass hepa...