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PMC6282492
core_pubmed_pmc
Risk–Benefit Assessment of Ethinylestradiol Using a Physiologically Based Pharmacokinetic Modeling Approach
Risk–Benefit Assessment of Ethinylestradiol Using a Physiologically Based Pharmacokinetic Modeling Approach Abstract Current formulations of combined oral contraceptives (COC) containing ethinylestradiol (EE) have ≤35 μg due to increased risks of cardiovascular diseases (CVD) with higher doses of EE. Low‐dose formulati...
PMC11044242
core_pubmed_pmc
Lysine-Polydopamine Nanocrystals Loaded with the Codrug Abemaciclib-Flurbiprofen for Oral Treatment of Cancer
Lysine-Polydopamine Nanocrystals Loaded with the Codrug Abemaciclib-Flurbiprofen for Oral Treatment of Cancer Abstract Nonsteroidal anti-inflammatory drugs (NSAIDs) combined with chemotherapeutic agents for the treatment of colorectal cancer (CRC) are a promising therapeutic strategy. NSAIDs can effectively boost the a...
PMC11171062
core_pubmed_pmc
In Vitro Lethality of Fenbendazole to the Eyeworm Oxyspirura petrowi
In Vitro Lethality of Fenbendazole to the Eyeworm Oxyspirura petrowi Abstract Simple Summary There are growing concerns about wildlife and livestock interactions and the impacts of those interactions on the sustainability of livestock. One of those concerns is the spillover of wildlife pathogens, including helminths, i...
PMC11873563
core_pubmed_pmc
Digital twin-enhanced three-organ microphysiological system for studying drug pharmacokinetics in pregnant women
Digital twin-enhanced three-organ microphysiological system for studying drug pharmacokinetics in pregnant women Abstract Background Pregnant women represent a vulnerable group in pharmaceutical research due to limited knowledge about drug metabolism and safety of commonly used corticosteroids like prednisone due to et...
PMC5017739
core_pubmed_pmc
Investigating the Effect of Ligand Amount and Injected Therapeutic Activity: A Simulation Study for 177 Lu-Labeled PSMA-Targeting Peptides
Investigating the Effect of Ligand Amount and Injected Therapeutic Activity: A Simulation Study for 177 Lu-Labeled PSMA-Targeting Peptides Abstract Abstract In molecular radiotherapy with 177 Lu-labeled prostate specific membrane antigen (PSMA) peptides, kidney and/or salivary glands doses limit the activity which can ...
PMC8123041
core_pubmed_pmc
Treatment of Multiple Myeloma and the Role of Melphalan in the Era of Modern Therapies—Current Research and Clinical Approaches
Treatment of Multiple Myeloma and the Role of Melphalan in the Era of Modern Therapies—Current Research and Clinical Approaches Abstract Multiple myeloma (MM) accounts for 10% of all hematological malignancies, and it is the second most common hematological neoplasm for which chemotherapy is an important pharmacologica...
PMC8377175
core_pubmed_pmc
Antidiabetic effect of bio-enhanced preparation of turmeric in streptozotocin-nicotinamide induced type 2 diabetic Wistar rats
Antidiabetic effect of bio-enhanced preparation of turmeric in streptozotocin-nicotinamide induced type 2 diabetic Wistar rats Abstract Background Poor oral bioavailability of curcumin, the active ingredient in turmeric, has limited its therapeutic use in various diseases including diabetes mellitus (DM). Objective(s) ...
PMC6048755
core_pubmed_pmc
Pharmacokinetics of mefloquine administered with artesunate in patients with uncomplicated falciparum malaria from the Brazilian Amazon basin
Pharmacokinetics of mefloquine administered with artesunate in patients with uncomplicated falciparum malaria from the Brazilian Amazon basin Abstract Background A fixed-dose combination of mefloquine with artesunate was evaluated in cases of falciparum malaria in the Brazilian Amazon basin with acceptable efficacy, sa...
PMC10169367
core_pubmed_pmc
First-in-human phase I/Ib study of QL1706 (PSB205), a bifunctional PD1/CTLA4 dual blocker, in patients with advanced solid tumors
First-in-human phase I/Ib study of QL1706 (PSB205), a bifunctional PD1/CTLA4 dual blocker, in patients with advanced solid tumors Abstract Abstract Background QL1706 (PSB205) is a single bifunctional MabPair (a novel technical platform) product consisting of two engineered monoclonal antibodies (anti-PD-1 IgG4 and anti...
PMC12745729
core_pubmed_pmc
Distinct Glucose Profiles with Daily and Weekly Growth Hormone Therapy Revealed by Continuous Glucose Monitoring
Distinct Glucose Profiles with Daily and Weekly Growth Hormone Therapy Revealed by Continuous Glucose Monitoring Abstract Abstract Context Somapacitan, a long-acting GH derivative, has been used to treat adult GH deficiency. Although the distinct pharmacokinetics of somapacitan compared with daily GH administration are...
PMC6421521
core_pubmed_pmc
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis Abstract A series of pleuromutilins modified by introduction of a boron-containing heterocycle on C(14) of the polycyclic core are described. These analogs were found to be potent anti- Wolbachia antib...
PMC12655427
core_pubmed_pmc
Does a Polycistronic 2A Design Enable Functional FcRn Production for Antibody Pharmacokinetic Studies?
Does a Polycistronic 2A Design Enable Functional FcRn Production for Antibody Pharmacokinetic Studies? Abstract Background/Objectives: The neonatal Fc receptor (FcRn) is a heterodimeric protein composed of a heavy α-chain with an MHC class I-like fold and β 2 -microglobulin. It plays a crucial role in maintaining the h...
PMC8615418
core_pubmed_pmc
Advanced Bioinformatics Tools in the Pharmacokinetic Profiles of Natural and Synthetic Compounds with Anti-Diabetic Activity
Advanced Bioinformatics Tools in the Pharmacokinetic Profiles of Natural and Synthetic Compounds with Anti-Diabetic Activity Abstract Diabetes represents a major health problem, involving a severe imbalance of blood sugar levels, which can disturb the nerves, eyes, kidneys, and other organs. Diabes management involves ...
PMC6343800
core_pubmed_pmc
Generation by phage display and characterization of drug-target complex-specific antibodies for pharmacokinetic analysis of biotherapeutics
Generation by phage display and characterization of drug-target complex-specific antibodies for pharmacokinetic analysis of biotherapeutics Abstract ABSTRACT Anti-idiotypic antibodies play an important role in pre-clinical and clinical development of therapeutic antibodies, where they are used for pharmacokinetic studi...
PMC10163007
core_pubmed_pmc
Pharmacodynamic activity of BMS-986156, a glucocorticoid-induced TNF receptor-related protein agonist, alone or in combination with nivolumab in patients with advanced solid tumors
Pharmacodynamic activity of BMS-986156, a glucocorticoid-induced TNF receptor-related protein agonist, alone or in combination with nivolumab in patients with advanced solid tumors Abstract Abstract Background The success of immune checkpoint inhibitors has revolutionized cancer treatment options and triggered developm...
PMC10108379
core_pubmed_pmc
Comparison of the pharmacokinetics of timosaponin AIII, timosaponin BIII, and mangiferin extracted from crude and salt-processed Anemarrhenae Rhizoma by UPLC-MS/MS
Comparison of the pharmacokinetics of timosaponin AIII, timosaponin BIII, and mangiferin extracted from crude and salt-processed Anemarrhenae Rhizoma by UPLC-MS/MS Abstract Abstract Processing is a traditional method for preparing decoctions of traditional Chinese medicine (TCM) that is imperative for reducing toxicity...
PMC4721027
core_pubmed_pmc
Pharmacokinetic Profile of Subcutaneous Testosterone Enanthate Delivered via a Novel, Prefilled Single‐Use Autoinjector: A Phase II Study
Pharmacokinetic Profile of Subcutaneous Testosterone Enanthate Delivered via a Novel, Prefilled Single‐Use Autoinjector: A Phase II Study Abstract Abstract Introduction Hypogonadism is one of the most common male endocrine problems. Although many treatments are currently available, unmet need exists for new testosteron...
PMC9240259
core_pubmed_pmc
A Randomized Controlled Dose-Escalation Study of LY06006, a Recombinant Humanized Monoclonal Antibody to RANKL, in Chinese Healthy Adults
A Randomized Controlled Dose-Escalation Study of LY06006, a Recombinant Humanized Monoclonal Antibody to RANKL, in Chinese Healthy Adults Abstract Abstract Background: This study was conducted to explore the safety, tolerance, pharmacokinetics, pharmacodynamics, and immunogenicity of LY06006, a recombinant humanized mo...
PMC6376718
core_pubmed_pmc
Analysis of the role of thrombomodulin in all-trans retinoic acid treatment of coagulation disorders in cancer patients
Analysis of the role of thrombomodulin in all-trans retinoic acid treatment of coagulation disorders in cancer patients Abstract Abstract Background Clinical studies have shown that all-trans retinoic acid (RA), which is often used in treatment of cancer patients, improves hemostatic parameters and bleeding complicatio...
PMC10058671
core_pubmed_pmc
Application of Minimal Physiologically-Based Pharmacokinetic Model to Simulate Lung and Trachea Exposure of Pyronaridine and Artesunate in Hamsters
Application of Minimal Physiologically-Based Pharmacokinetic Model to Simulate Lung and Trachea Exposure of Pyronaridine and Artesunate in Hamsters Abstract A fixed-dose combination of pyronaridine and artesunate, one of the artemisinin-based combination therapies, has been used as a potent antimalarial treatment regim...
PMC10146788
core_pubmed_pmc
Dried Blood Spot Sampling to Assess Rifampicin Exposure and Treatment Outcomes among Native and Non-Native Tuberculosis Patients in Paraguay: An Exploratory Study
Dried Blood Spot Sampling to Assess Rifampicin Exposure and Treatment Outcomes among Native and Non-Native Tuberculosis Patients in Paraguay: An Exploratory Study Abstract The aim of this study was to evaluate the difference in drug exposure of rifampicin in native versus non-native Paraguayan populations using dried b...
PMC5866997
core_pubmed_pmc
Pharmacogenetic Analysis of the Model‐Based Pharmacokinetics of Five Anti‐HIV Drugs: How Does This Influence the Effect of Aging?
Pharmacogenetic Analysis of the Model‐Based Pharmacokinetics of Five Anti‐HIV Drugs: How Does This Influence the Effect of Aging? Abstract Abstract Analysis of aging and pharmacogenetics (PGx) on antiretroviral pharmacokinetics (PKs) could inform precision dosing for older human HIV‐infected patients. Seventy‐four part...
PMC7952424
core_pubmed_pmc
Enteric reabsorption processes and their impact on drug pharmacokinetics
Enteric reabsorption processes and their impact on drug pharmacokinetics Abstract Abstract Enteric reabsorption occurs when a drug is secreted into the intestinal lumen and reabsorbed into the systemic circulation. This distribution process is evidenced by multiple peaks in pharmacokinetic profiles. Commonly, hepatobil...
PMC9537548
core_pubmed_pmc
A genome-wide association study of plasma concentrations of warfarin enantiomers and metabolites in sub-Saharan black-African patients
A genome-wide association study of plasma concentrations of warfarin enantiomers and metabolites in sub-Saharan black-African patients Abstract Abstract Diversity in pharmacogenomic studies is poor, especially in relation to the inclusion of black African patients. Lack of funding and difficulties in recruitment, toget...
PMC7412295
core_pubmed_pmc
Gut Microbiota Modulation: Implications for Infection Control and Antimicrobial Stewardship
Gut Microbiota Modulation: Implications for Infection Control and Antimicrobial Stewardship Abstract Abstract The human microbiome comprises a complex ecosystem of microbial communities that exist within the human body, the largest and most diverse of which are found within the human intestine. It has been increasingly...
PMC8042240
core_pubmed_pmc
Stoichiometry of multi-specific immune checkpoint RNA Abs for T cell activation and tumor inhibition using ultra-stable RNA nanoparticles
Stoichiometry of multi-specific immune checkpoint RNA Abs for T cell activation and tumor inhibition using ultra-stable RNA nanoparticles Abstract Immunotherapy has become a revolutionary subject in cancer therapy during the past few years. Immune checkpoint-targeting antibodies (Abs) could boost anticancer immune resp...
PMC7689752
core_pubmed_pmc
Prediction of Drug Exposure in Critically Ill Encephalopathic Neonates Treated With Therapeutic Hypothermia Based on a Pooled Population Pharmacokinetic Analysis of Seven Drugs and Five Metabolites
Prediction of Drug Exposure in Critically Ill Encephalopathic Neonates Treated With Therapeutic Hypothermia Based on a Pooled Population Pharmacokinetic Analysis of Seven Drugs and Five Metabolites Abstract Drug dosing in encephalopathic neonates treated with therapeutic hypothermia is challenging; exposure is dependen...
PMC9391720
core_pubmed_pmc
Pharmacokinetic and clinical effects of two bupivacaine concentrations on axillary brachial plexus block
Pharmacokinetic and clinical effects of two bupivacaine concentrations on axillary brachial plexus block Abstract Introduction The risk of systemic bupivacaine toxicity is a persistent problem, which makes its pharmacokinetic study fundamental for regional anesthesia safety. There is little evidence of its influence on...
PMC10662720
core_pubmed_pmc
Evaluating pediatric tuberculosis dosing guidelines: A model-based individual data pooled analysis
Evaluating pediatric tuberculosis dosing guidelines: A model-based individual data pooled analysis Abstract Abstract Background The current World Health Organization (WHO) pediatric tuberculosis dosing guidelines lead to suboptimal drug exposures. Identifying factors altering the exposure of these drugs in children is ...
PMC4100259
core_pubmed_pmc
Valerian: No Evidence for Clinically Relevant Interactions
Valerian: No Evidence for Clinically Relevant Interactions Abstract In recent popular publications as well as in widely used information websites directed to cancer patients, valerian is claimed to have a potential of adverse interactions with anticancer drugs. This questions its use as a safe replacement for, for exam...
PMC5444177
core_pubmed_pmc
Pharmacokinetics and Tolerance of the Phage Endolysin-Based Candidate Drug SAL200 after a Single Intravenous Administration among Healthy Volunteers
Pharmacokinetics and Tolerance of the Phage Endolysin-Based Candidate Drug SAL200 after a Single Intravenous Administration among Healthy Volunteers Abstract ABSTRACT This study was a phase 1, single-center, randomized, double-blind, placebo-controlled, single-dosing, and dose-escalating study of intravenous SAL200. It...
PMC6089804
core_pubmed_pmc
Optimization of a drug transporter probe cocktail: potential screening tool for transporter‐mediated drug–drug interactions
Optimization of a drug transporter probe cocktail: potential screening tool for transporter‐mediated drug–drug interactions Abstract Abstract Aims Previous pharmacokinetic characterization of a transporter probe cocktail containing digoxin (P‐gp), furosemide (OAT1, OAT3), metformin (OCT2, MATE1, MATE2‐K) and rosuvastat...
PMC12209947
core_pubmed_pmc
Respiratory syncytial virus-attributable hospitalizations among adults in high- and middle-income countries: application of the Global Burden of Disease framework
Respiratory syncytial virus-attributable hospitalizations among adults in high- and middle-income countries: application of the Global Burden of Disease framework Abstract Summary Background Respiratory syncytial virus (RSV) in adults is typically underdiagnosed due to non-specific symptoms, infrequent routine testing,...
PMC10087439
core_pubmed_pmc
Dose optimization of cefotaxime as pre‐emptive treatment in critically ill adult patients: A population pharmacokinetic study
Dose optimization of cefotaxime as pre‐emptive treatment in critically ill adult patients: A population pharmacokinetic study Abstract Abstract Aims To describe the pharmacokinetics (PK) of cefotaxime as pre‐emptive treatment in critically ill adult patients, including covariates and to determine the probability of tar...
PMC11598116
core_pubmed_pmc
The Role of Simulation Science in Public Health at the Agency for Toxic Substances and Disease Registry: An Overview and Analysis of the Last Decade
The Role of Simulation Science in Public Health at the Agency for Toxic Substances and Disease Registry: An Overview and Analysis of the Last Decade Abstract Environmental exposures are ubiquitous and play a significant, and sometimes understated, role in public health as they can lead to the development of various chr...
PMC8467142
core_pubmed_pmc
An in vivo pharmacokinetic study of metformin microparticles as an oral sustained release formulation in rabbits
An in vivo pharmacokinetic study of metformin microparticles as an oral sustained release formulation in rabbits Abstract Background Metformin hydrochloride is a biguanide derivative that has been widely used to treat type 2 diabetes in humans. In veterinary medicine, metformin has shown increasing potential for diabet...
PMC10733810
core_pubmed_pmc
Mechanisms behind changes of neurodegeneration biomarkers in plasma induced by sleep deprivation
Mechanisms behind changes of neurodegeneration biomarkers in plasma induced by sleep deprivation Abstract Abstract Acute sleep deprivation has been shown to affect cerebrospinal fluid and plasma concentrations of biomarkers associated with neurodegeneration, though the mechanistic underpinnings remain unknown. This stu...
PMC12314178
core_pubmed_pmc
Pharmacotherapy variability and precision medicine in neurocritical care
Pharmacotherapy variability and precision medicine in neurocritical care Abstract Pharmacotherapy variability is defined as the variability in drug response among and within individuals that is attributed to the inter and intra-individual differences in the action and disposition of drugs. Neurological and medical comp...
PMC7577017
core_pubmed_pmc
Kinetic‐Pharmacodynamic Model of Platelet Time Course in Patients With Moderate‐to‐Severe Atopic Dermatitis Treated With Oral Janus Kinase 1 Inhibitor Abrocitinib
Kinetic‐Pharmacodynamic Model of Platelet Time Course in Patients With Moderate‐to‐Severe Atopic Dermatitis Treated With Oral Janus Kinase 1 Inhibitor Abrocitinib Abstract The oral Janus kinase 1 (JAK1) inhibitor abrocitinib reduced signs and symptoms of atopic dermatitis (AD) in a placebo‐controlled, randomized, doubl...
PMC11472027
core_pubmed_pmc
Disposition of orally administered atuliflapon, a novel 5‐lipoxygenase‐activating protein inhibitor in healthy participants
Disposition of orally administered atuliflapon, a novel 5‐lipoxygenase‐activating protein inhibitor in healthy participants Abstract Abstract In this study, the mass balance, pharmacokinetics (PK) and metabolism of atuliflapon, a novel 5‐lipoxygenase‐activating protein inhibitor, were investigated in healthy male subje...
PMC4740560
core_pubmed_pmc
Pharmacokinetics and Exposure-Response Relationships of Dasotraline in the Treatment of Attention-Deficit/Hyperactivity Disorder in Adults
Pharmacokinetics and Exposure-Response Relationships of Dasotraline in the Treatment of Attention-Deficit/Hyperactivity Disorder in Adults Abstract Abstract Background and Objectives Dasotraline is a novel inhibitor of dopamine and norepinephrine reuptake currently being investigated in clinical studies for the treatme...
PMC10057873
core_pubmed_pmc
In Silico Identification of Peptides with PPARγ Antagonism in Protein Hydrolysate from Rice ( Oryza sativa )
In Silico Identification of Peptides with PPARγ Antagonism in Protein Hydrolysate from Rice ( Oryza sativa ) Abstract At least half the population in industrialized countries suffers from obesity due to excessive accumulation of adipose tissue. Recently, rice ( Oryza sativa ) proteins have been considered valuable sour...
PMC10530683
core_pubmed_pmc
Anti-Rheumatoid Arthritis Pharmacodynamic Substances Screening of Periploca forrestii Schltr.: Component Analyses In Vitro and In Vivo Combined with Multi-Technical Metabolomics
Anti-Rheumatoid Arthritis Pharmacodynamic Substances Screening of Periploca forrestii Schltr.: Component Analyses In Vitro and In Vivo Combined with Multi-Technical Metabolomics Abstract Abstract The purpose of this study was to elucidate the metabolic action patterns of P. forrestii against rheumatoid arthritis (RA) u...
PMC9293229
core_pubmed_pmc
Pharmacokinetics of testosterone therapies in relation to diurnal variation of serum testosterone levels as men age
Pharmacokinetics of testosterone therapies in relation to diurnal variation of serum testosterone levels as men age Abstract Abstract Background To improve symptoms associated with testosterone deficiency, many testosterone therapies are available that aim to restore serum testosterone (T) levels to the normal physiolo...
PMC10797514
core_pubmed_pmc
Glucocorticoids with or without fludrocortisone in septic shock: a narrative review from a biochemical and molecular perspective
Glucocorticoids with or without fludrocortisone in septic shock: a narrative review from a biochemical and molecular perspective Abstract Summary Two randomised controlled trials have reported a reduction in mortality when adjunctive hydrocortisone is administered in combination with fludrocortisone compared with place...
PMC10357944
core_pubmed_pmc
Biological activity and structure–activity relationship of dehydrodieugenol B analogues against visceral leishmaniasis †
Biological activity and structure–activity relationship of dehydrodieugenol B analogues against visceral leishmaniasis † Abstract Abstract Visceral leishmaniasis is a neglected protozoan disease with high mortality. Existing treatments exhibit a number of limitations, resulting in a significant challenge for public hea...
PMC6275223
core_pubmed_pmc
A Systematic Review on the Pharmacokinetics of Cannabidiol in Humans
A Systematic Review on the Pharmacokinetics of Cannabidiol in Humans Abstract Background: Cannabidiol is being pursued as a therapeutic treatment for multiple conditions, usually by oral delivery. Animal studies suggest oral bioavailability is low, but literature in humans is not sufficient. The aim of this review was ...
PMC10647271
core_pubmed_pmc
Phyllanthi Tannin Loaded Solid Lipid Nanoparticles for Lung Cancer Therapy: Preparation, Characterization, Pharmacodynamics and Safety Evaluation
Phyllanthi Tannin Loaded Solid Lipid Nanoparticles for Lung Cancer Therapy: Preparation, Characterization, Pharmacodynamics and Safety Evaluation Abstract Abstract The objective of the present study was to develop PTF-loaded solid lipid nanoparticles (PTF-SLNs) and investigate their efficacy in treating lung cancer. Th...
PMC7746380
core_pubmed_pmc
In vitro and in vivo efficacy of the novel oral proteasome inhibitor NNU546 in multiple myeloma
In vitro and in vivo efficacy of the novel oral proteasome inhibitor NNU546 in multiple myeloma Abstract Proteasome inhibition demonstrates highly effective impact on multiple myeloma (MM) treatment. Here, we aimed to examine anti-tumor efficiency and underlying mechanisms of a novel well tolerated orally applicable pr...
PMC6505380
core_pubmed_pmc
An Extensively Humanized Mouse Model to Predict Pathways of Drug Disposition and Drug/Drug Interactions, and to Facilitate Design of Clinical Trials
An Extensively Humanized Mouse Model to Predict Pathways of Drug Disposition and Drug/Drug Interactions, and to Facilitate Design of Clinical Trials Abstract Abstract Species differences in drug metabolism and disposition can confound the extrapolation of in vivo PK data to man and also profoundly compromise drug effic...
PMC11918604
core_pubmed_pmc
The hidden pharmacokinetic challenge: diarrhea’s influence on cyclosporine therapy: a case series
The hidden pharmacokinetic challenge: diarrhea’s influence on cyclosporine therapy: a case series Abstract Background: Cyclosporine is used as an immunosuppressive drug to improve graft survival rates in the field of organ transplantation. Therapeutic drug monitoring [TDM] of cyclosporine in transplant patients is cruc...
PMC5870420
core_pubmed_pmc
Disease burden and the role of pharmacogenomics in African populations
Disease burden and the role of pharmacogenomics in African populations Abstract Background. The burden of communicable and non-communicable diseases in Sub-Saharan Africa poses a challenge in achieving quality healthcare. Although therapeutic drugs have generally improved health, their efficacy differs from individual ...
PMC6560505
core_pubmed_pmc
Development of visual predictive checks accounting for multimodal parameter distributions in mixture models
Development of visual predictive checks accounting for multimodal parameter distributions in mixture models Abstract The assumption of interindividual variability being unimodally distributed in nonlinear mixed effects models does not hold when the population under study displays multimodal parameter distributions. Mix...
PMC8604209
core_pubmed_pmc
A first‐in‐human study of KMRC011, a potential treatment for acute radiation syndrome, to explore tolerability, pharmacokinetics, and pharmacodynamics
A first‐in‐human study of KMRC011, a potential treatment for acute radiation syndrome, to explore tolerability, pharmacokinetics, and pharmacodynamics Abstract Abstract KMRC011 is a novel Toll‐like receptor 5 agonist under development as a treatment for acute radiation syndrome (ARS). The aim of this first‐in‐human stu...
PMC11496122
core_pubmed_pmc
Induction of cytochrome P450 via upregulation of CAR and PXR: a potential mechanism for altered florfenicol metabolism by macranthoidin B in vivo
Induction of cytochrome P450 via upregulation of CAR and PXR: a potential mechanism for altered florfenicol metabolism by macranthoidin B in vivo Abstract Introduction Macranthoidin B (MB) is a primary active component of Flos Lonicerae. In Chinese veterinary clinics, Flos Lonicerae is frequently used in combination wi...
PMC11769347
core_pubmed_pmc
Development of Novel Fluticasone/Salmeterol/Tiotropium-Loaded Dry Powder Inhaler and Bioequivalence Assessment to Commercial Products in Rats
Development of Novel Fluticasone/Salmeterol/Tiotropium-Loaded Dry Powder Inhaler and Bioequivalence Assessment to Commercial Products in Rats Abstract Abstract Background / Objectives : Inhaler devices have been developed for the effective delivery of inhaled medications used in the treatment of pulmonary diseases. How...
PMC3705320
core_pubmed_pmc
Pharmacokinetics of High-Dose Weekly Oral Vitamin D3 Supplementation during the Third Trimester of Pregnancy in Dhaka, Bangladesh
Pharmacokinetics of High-Dose Weekly Oral Vitamin D3 Supplementation during the Third Trimester of Pregnancy in Dhaka, Bangladesh Abstract A pharmacokinetic study was conducted to assess the biochemical dose-response and tolerability of high-dose prenatal vitamin D3 supplementation in Dhaka, Bangladesh (23°N). Pregnant...
PMC8752109
core_pubmed_pmc
Physiologically‐based pharmacokinetic modeling to evaluate in vitro‐to‐in vivo extrapolation for intestinal P‐glycoprotein inhibition
Physiologically‐based pharmacokinetic modeling to evaluate in vitro‐to‐in vivo extrapolation for intestinal P‐glycoprotein inhibition Abstract Abstract As one of the key components in model‐informed drug discovery and development, physiologically‐based pharmacokinetic (PBPK) modeling linked with in vitro‐to‐in vivo ext...
PMC11762835
core_pubmed_pmc
Neuroprotective Potential of Origanum majorana L. Essential Oil Against Scopolamine-Induced Memory Deficits and Oxidative Stress in a Zebrafish Model
Neuroprotective Potential of Origanum majorana L. Essential Oil Against Scopolamine-Induced Memory Deficits and Oxidative Stress in a Zebrafish Model Abstract Origanum majorana L., also known as sweet marjoram, is a plant with multiple uses, both in the culinary field and traditional medicine, because of its major anti...
PMC5516189
core_pubmed_pmc
Population‐Based Pharmacokinetic and Exposure‐Efficacy Analyses of Peginterferon Beta‐1a in Patients With Relapsing Multiple Sclerosis
Population‐Based Pharmacokinetic and Exposure‐Efficacy Analyses of Peginterferon Beta‐1a in Patients With Relapsing Multiple Sclerosis Abstract Abstract Peginterferon beta‐1a reduced annualized relapse rate as compared with placebo and was approved to treat multiple sclerosis patients. A population pharmacokinetic and ...
PMC5903334
core_pubmed_pmc
Evaluation of Marbofloxacin in Beagle Dogs After Oral Dosing: Preclinical Safety Evaluation and Comparative Pharmacokinetics of Two Different Tablets
Evaluation of Marbofloxacin in Beagle Dogs After Oral Dosing: Preclinical Safety Evaluation and Comparative Pharmacokinetics of Two Different Tablets Abstract The current study evaluates a tested marbofloxacin tablet (MBT) (Petsen), in terms of bioavailability and pharmacokinetics (PK) in a comparison of the commercial...
PMC8841796
core_pubmed_pmc
Life-Threatening Docetaxel Toxicity in a Patient With Reduced-Function CYP3A Variants: A Case Report
Life-Threatening Docetaxel Toxicity in a Patient With Reduced-Function CYP3A Variants: A Case Report Abstract Abstract Docetaxel therapy occasionally causes severe and life-threatening toxicities. Some docetaxel toxicities are related to exposure, and inter-individual variability in exposure has been described based on...
PMC9475238
core_pubmed_pmc
Phase Ib Study of the BET Inhibitor GS-5829 as Monotherapy and Combined with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer
Phase Ib Study of the BET Inhibitor GS-5829 as Monotherapy and Combined with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer Abstract Abstract Purpose: A phase Ib study (1604) was conducted to evaluate the safety and efficacy of GS-5829, an oral bromodomain and extraterminal inhibitor, alo...
PMC8632238
core_pubmed_pmc
Recent Advances in Pharmaceutical Cocrystals: From Bench to Market
Recent Advances in Pharmaceutical Cocrystals: From Bench to Market Abstract Abstract The pharmacokinetics profile of active pharmaceutical ingredients (APIs) in the solid pharmaceutical dosage forms is largely dependent on the solid-state characteristics of the chemicals to understand the physicochemical properties by ...
PMC5874726
core_pubmed_pmc
Comparison Study of Two Differently Clicked 18 F-Folates—Lipophilicity Plays a Key Role
Comparison Study of Two Differently Clicked 18 F-Folates—Lipophilicity Plays a Key Role Abstract Abstract Within the last decade, several folate-based radiopharmaceuticals for Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET) have been evaluated; however, there is still a lack of...
PMC12521070
core_pubmed_pmc
Pharmacometric Model‐Based Sample Size Allocation for a Region of Interest in a Multi‐Regional Phase 2 Trial: A Case Study of an Anti‐Psoriatic Drug
Pharmacometric Model‐Based Sample Size Allocation for a Region of Interest in a Multi‐Regional Phase 2 Trial: A Case Study of an Anti‐Psoriatic Drug Abstract ABSTRACT Phase 2 trials have historically focused on characterizing the dose‐exposure‐response relationship in relatively homogeneous patient populations before p...
PMC3414206
core_pubmed_pmc
Enhanced bioavailability and efficiency of curcumin for the treatment of asthma by its formulation in solid lipid nanoparticles
Enhanced bioavailability and efficiency of curcumin for the treatment of asthma by its formulation in solid lipid nanoparticles Abstract Abstract Curcumin has shown considerable pharmacological activity, including anti-inflammatory, but its poor bioavailability and rapid metabolization have limited its application. The...
PMC8235661
core_pubmed_pmc
Photoelectric Dye, NK-5962, as a Potential Drug for Preventing Retinal Neurons from Apoptosis: Pharmacokinetic Studies Based on Review of the Evidence
Photoelectric Dye, NK-5962, as a Potential Drug for Preventing Retinal Neurons from Apoptosis: Pharmacokinetic Studies Based on Review of the Evidence Abstract NK-5962 is a key component of photoelectric dye-based retinal prosthesis (OUReP). In testing the safety and efficacy, NK-5962 was safe in all tests for the biol...
PMC7898311
core_pubmed_pmc
Physiologically based pharmacokinetic model of renally cleared antibacterial drugs in Chinese renal impairment patients
Physiologically based pharmacokinetic model of renally cleared antibacterial drugs in Chinese renal impairment patients Abstract Abstract To preliminarily develop physiologically based population models for Chinese renal impairment patients and to evaluate the prediction performance of new population models by renally ...
PMC6598723
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Integration and Resistance Analysis of Tilmicosin Against Mycoplasma gallisepticum in an In Vitro Dynamic Model
Pharmacokinetic and Pharmacodynamic Integration and Resistance Analysis of Tilmicosin Against Mycoplasma gallisepticum in an In Vitro Dynamic Model Abstract Mycoplasma gallisepticum is the major pathogen causing chronic respiratory disease in chickens. In the present study, we successfully established a one-compartment...
PMC6017968
core_pubmed_pmc
Use of an UHPLC-MS/MS Method for Determination of Kuraridin and Characterization of Its Metabolites in Rat Plasma after Oral Administration
Use of an UHPLC-MS/MS Method for Determination of Kuraridin and Characterization of Its Metabolites in Rat Plasma after Oral Administration Abstract Kuraridin is an active natural prenylated flavonoid ingredient originating from the well-known traditional Chinese medicine Sophora flavescens Ait., that possesses various...
PMC12436239
core_pubmed_pmc
Distinct patient, tumour and chimeric antigen receptor T‐cell characteristics are associated with initiating versus sustaining responses to idecabtagene vicleucel in relapsed and refractory multiple myeloma
Distinct patient, tumour and chimeric antigen receptor T‐cell characteristics are associated with initiating versus sustaining responses to idecabtagene vicleucel in relapsed and refractory multiple myeloma Abstract Summary Idecabtagene vicleucel (ide‐cel), a B‐cell maturation antigen (BCMA)‐directed autologous chimeri...
PMC6859083
core_pubmed_pmc
Population Pharmacokinetic Modeling Of On-Demand And Surgical Use Of Nonacog Beta Pegol (N9-GP) And rFIXFc Based Upon The paradigm 7 Comparative Pharmacokinetic Study
Population Pharmacokinetic Modeling Of On-Demand And Surgical Use Of Nonacog Beta Pegol (N9-GP) And rFIXFc Based Upon The paradigm 7 Comparative Pharmacokinetic Study Abstract Abstract Aim/objective Understanding pharmacokinetic (PK) differences between standard and extended half-life (EHL) products is important, parti...
PMC4224072
core_pubmed_pmc
Exploring BSEP inhibition-mediated toxicity with a mechanistic model of drug-induced liver injury
Exploring BSEP inhibition-mediated toxicity with a mechanistic model of drug-induced liver injury Abstract Inhibition of the bile salt export pump (BSEP) has been linked to incidence of drug-induced liver injury (DILI), presumably by the accumulation of toxic bile acids in the liver. We have previously constructed and ...
PMC12305873
core_pubmed_pmc
Chlorinated biscoumarins inhibit chikungunya virus replication in cell-based and animal models
Chlorinated biscoumarins inhibit chikungunya virus replication in cell-based and animal models Abstract ABSTRACT Biscoumarin derivatives were evaluated for antiviral activity against chikungunya virus (CHIKV), a re-emerging mosquito-borne alphavirus with no approved treatment. Compounds 3 and 4 demonstrated potent in v...
PMC3234146
core_pubmed_pmc
Pain management in the elderly at the end of life
Pain management in the elderly at the end of life Abstract Background: The treatment of older adults with pain is complex and affected by age-related changes in pharmacokinetics and pharmacodynamics. Chronic pain encompasses a complex array of sensory-discriminatory, motivational-affective, and cognitive-evaluative com...
PMC12030279
core_pubmed_pmc
Development and Evaluation of Bilayer Sustained-Release Tablets of Ruxolitinib Using Discriminative Pharmacokinetic Analysis and IVIVC
Development and Evaluation of Bilayer Sustained-Release Tablets of Ruxolitinib Using Discriminative Pharmacokinetic Analysis and IVIVC Abstract Abstract Objectives : This study explores the development and evaluation of a bilayer sustained-release (SR) tablet formulation of ruxolitinib. As a BCS Class 1 drug, ruxolitin...
PMC11612618
core_pubmed_pmc
Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Abstract Abstract p53 is known as the guardian of the genome and is one of the most important tumor suppressors. It is inactivated in most tumors, either via tumor protein p53 ( TP53 ) g...
PMC12820339
core_pubmed_pmc
Open‐Label Study Assessing Relative and Absolute Bioavailability of Oral Camizestrant Formulations and Food Effects in Healthy Postmenopausal Women
Open‐Label Study Assessing Relative and Absolute Bioavailability of Oral Camizestrant Formulations and Food Effects in Healthy Postmenopausal Women Abstract ABSTRACT Camizestrant is the next‐generation oral selective estrogen receptor degrader and complete estrogen receptor antagonist in Phase 3 development for hormone...
PMC4813732
core_pubmed_pmc
Comparison of biological activities of human antithrombins with high-mannose or complex-type nonfucosylated N-linked oligosaccharides
Comparison of biological activities of human antithrombins with high-mannose or complex-type nonfucosylated N-linked oligosaccharides Abstract The structure of the N-linked oligosaccharides attached to antithrombin (AT) has been shown to affect its anticoagulant activity and pharmacokinetics. Human AT has biantennary c...
PMC8602434
core_pubmed_pmc
Pharmacokinetics of the Melanocortin Type 1 Receptor Agonist PL8177 After Subcutaneous Administration
Pharmacokinetics of the Melanocortin Type 1 Receptor Agonist PL8177 After Subcutaneous Administration Abstract Background and Objective PL8177 is a selective melanocortin 1 receptor agonist in development for the treatment of various immunologic and inflammatory conditions. Here we describe the pharmacokinetics of PL81...
PMC6979379
core_pubmed_pmc
Pharmacodynamic comparison of different antimicrobial regimens against Staphylococcus aureus bloodstream infections with elevated vancomycin minimum inhibitory concentration
Pharmacodynamic comparison of different antimicrobial regimens against Staphylococcus aureus bloodstream infections with elevated vancomycin minimum inhibitory concentration Abstract Abstract Background Staphylococcus aureus is one of the major causes of bloodstream infections (BSI) worldwide, representing a major chal...
PMC7024785
core_pubmed_pmc
A Single- and Multiple-Dose Study to Evaluate the Pharmacokinetics of Fixed-Dose Grazoprevir/Elbasvir in Healthy Chinese Participants
A Single- and Multiple-Dose Study to Evaluate the Pharmacokinetics of Fixed-Dose Grazoprevir/Elbasvir in Healthy Chinese Participants Abstract Abstract Purpose The burden of hepatitis C virus infection is particularly high in Asian countries, and new treatments are urgently needed. The purpose of this study was to char...
PMC6631472
core_pubmed_pmc
Kaempferol: A Key Emphasis to Its Anticancer Potential
Kaempferol: A Key Emphasis to Its Anticancer Potential Abstract Abstract A marked decrease in human cancers, including breast cancer, bone cancer, and cervical cancer, has been linked to the consumption of vegetable and fruit, and the corresponding chemoprotective effect has been associated with the presence of several...
PMC9071514
core_pubmed_pmc
Relationship of anifrolumab pharmacokinetics with efficacy and safety in patients with systemic lupus erythematosus
Relationship of anifrolumab pharmacokinetics with efficacy and safety in patients with systemic lupus erythematosus Abstract Abstract Objectives To characterize the relationship of anifrolumab pharmacokinetics with efficacy and safety in patients with moderate to severe SLE despite standard therapy, using pooled data f...
PMC10154123
core_pubmed_pmc
Repurposing antifungals: population pharmacokinetics of itraconazole and hydroxy-itraconazole following administration of a nanocrystal formulation
Repurposing antifungals: population pharmacokinetics of itraconazole and hydroxy-itraconazole following administration of a nanocrystal formulation Abstract Abstract Objectives To describe itraconazole and hydroxy-itraconazole pharmacokinetics following intravenous (IV) administration of a previously developed nanocrys...
PMC11555770
core_pubmed_pmc
First-in-human phase 1 dose-escalation results with livmoniplimab, an antibody targeting the GARP:TGF-ß1 complex, as monotherapy and in combination with the anti–PD-1 antibody budigalimab in patients with advanced solid tumors
First-in-human phase 1 dose-escalation results with livmoniplimab, an antibody targeting the GARP:TGF-ß1 complex, as monotherapy and in combination with the anti–PD-1 antibody budigalimab in patients with advanced solid tumors Abstract Abstract Background Transforming growth factor (TGF)-ß1 is a pleiotropic cytokine th...
PMC8860874
core_pubmed_pmc
Time course of human skeletal muscle nitrate and nitrite concentration changes following dietary nitrate ingestion
Time course of human skeletal muscle nitrate and nitrite concentration changes following dietary nitrate ingestion Abstract Dietary nitrate (NO 3 − ) ingestion can be beneficial for health and exercise performance. Recently, based on animal and limited human studies, a skeletal muscle NO 3 − reservoir has been suggeste...
PMC12238140
core_pubmed_pmc
Significant Predictors of Azithromycin in Population Pharmacokinetic Analysis: A Systematic Review
Significant Predictors of Azithromycin in Population Pharmacokinetic Analysis: A Systematic Review Abstract Abstract Azithromycin is widely used to treat infections caused by susceptible bacteria and is the first-line treatment for mycoplasma pneumonia in pediatric patients. However, in clinical practice, large between...
PMC6767045
core_pubmed_pmc
Therapeutic value of steroidal alkaloids in cancer: Current trends and future perspectives
Therapeutic value of steroidal alkaloids in cancer: Current trends and future perspectives Abstract Discovery and development of new potentially selective anticancer agents are necessary to prevent a global cancer health crisis. Currently, alternative medicinal agents derived from plants have been extensively investiga...
PMC10507961
core_pubmed_pmc
Development of an amoxicillin-radix scutellaria extract formulation and evaluation of its pharmacokinetics in pigs
Development of an amoxicillin-radix scutellaria extract formulation and evaluation of its pharmacokinetics in pigs Abstract Background A new antibacterial compound powder of amoxicillin (AMO)/Radix Scutellaria extract (RSE) was developed, and its pharmacokinetics were determined in pigs following oral administration. R...
PMC4767442
core_pubmed_pmc
Novel and potent anti-tumor and anti-metastatic di-2-pyridylketone thiosemicarbazones demonstrate marked differences in pharmacology between the first and second generation lead agents
Novel and potent anti-tumor and anti-metastatic di-2-pyridylketone thiosemicarbazones demonstrate marked differences in pharmacology between the first and second generation lead agents Abstract Di(2-pyridyl)ketone 4,4-dimethyl-3-thiosemicarbazone (Dp44mT) and di(2-pyridyl)ketone 4-cyclohexyl-4-methyl-3-thiosemicarbazon...
PMC12951459
core_pubmed_pmc
Fluorine-18 Radiolabeled Single-Chain Antibody Variable Fragment 1F4 Targets α1-Subunit Gamma-Aminobutyric Acid Type A Receptors in Mice
Fluorine-18 Radiolabeled Single-Chain Antibody Variable Fragment 1F4 Targets α1-Subunit Gamma-Aminobutyric Acid Type A Receptors in Mice Abstract Abstract Gamma-aminobutyric acid type A (GABA-A) receptors are the principal inhibitory neurotransmitter receptors in the central nervous system (CNS), but their functions in...
PMC4049400
core_pubmed_pmc
Pharmacokinetics of tramadol after subcutaneous administration in a critically ill population and in a healthy cohort
Pharmacokinetics of tramadol after subcutaneous administration in a critically ill population and in a healthy cohort Abstract Abstract Background Tramadol is an atypical centrally acting analgesic agent available as both oral and parenteral preparations. For patients who are unable to take tramadol orally, the subcuta...
PMC12081286
core_pubmed_pmc
Comparative modelling of foetal exposure to maternal long-acting injectable versus oral daily antipsychotics
Comparative modelling of foetal exposure to maternal long-acting injectable versus oral daily antipsychotics Abstract This study employed physiologically based pharmacokinetic (PBPK) modelling to compare the extent of foetal exposure between oral and long-acting injectable (LAI) aripiprazole and olanzapine. Adult and p...
PMC2956476
core_pubmed_pmc
Pazopanib for the Treatment of Patients with Advanced Renal Cell Carcinoma
Pazopanib for the Treatment of Patients with Advanced Renal Cell Carcinoma Abstract Dramatic advances in the care of patients with advanced renal cell carcinoma have occurred over the last ten years, including insights into the molecular pathogenesis of this disease, that have now been translated into paradigm-changing...
PMC9554458
core_pubmed_pmc
Physiologically-based pharmacokinetic modelling and dosing evaluation of gentamicin in neonates using PhysPK
Physiologically-based pharmacokinetic modelling and dosing evaluation of gentamicin in neonates using PhysPK Abstract Each year, infections caused around the 25% of neonatal deaths. Early empirical treatments help to reduce this mortality, although optimized dosing regimens are still lacking. The aims were to develop a...
PMC8618010
core_pubmed_pmc
Population Pharmacokinetic Analysis and Dosing Optimization of Prophylactic Fluconazole in Japanese Patients with Hematological Malignancy
Population Pharmacokinetic Analysis and Dosing Optimization of Prophylactic Fluconazole in Japanese Patients with Hematological Malignancy Abstract Abstract We conducted population pharmacokinetic (PPK) analysis and Monte Carlo simulations to determine the appropriate prophylactic dose of fluconazole to prevent invasiv...
PMC11066703
core_pubmed_pmc
Systematic Evaluation of Aegle marmelos-Derived Compounds: Potential Therapeutic Agents Against Inflammation and Oxidative Stress
Systematic Evaluation of Aegle marmelos-Derived Compounds: Potential Therapeutic Agents Against Inflammation and Oxidative Stress Abstract Aim This study aimed to evaluate the potential antioxidant and anti-inflammatory properties of Aegle marmelos active compounds through a multifaceted approach. The investigation enc...
PMC5593167
core_pubmed_pmc
A Proton Pump Inhibitor in the Reformulation Setting: Bioequivalence and Potential Implications for Long‐Term Safety
A Proton Pump Inhibitor in the Reformulation Setting: Bioequivalence and Potential Implications for Long‐Term Safety Abstract Abstract Proton pump inhibitors (PPIs) have become known for both their therapeutic effect and good safety profile. An application was submitted to the US Food and Drug Administration for approv...