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PMC9246802
core_pubmed_pmc
Drug Distribution in Brain and Cerebrospinal Fluids in Relation to IC 50 Values in Aging and Alzheimer’s Disease, Using the Physiologically Based LeiCNS-PK3.0 Model
Drug Distribution in Brain and Cerebrospinal Fluids in Relation to IC 50 Values in Aging and Alzheimer’s Disease, Using the Physiologically Based LeiCNS-PK3.0 Model Abstract Abstract Background Very little knowledge exists on the impact of Alzheimer’s disease on the CNS target site pharmacokinetics (PK). Aim To predict...
PMC8518774
core_pubmed_pmc
Randomized, Open‐Label, Single‐Dose, Parallel‐Group Pharmacokinetic Study of PF‐06410293 (adalimumab‐afzb), an Adalimumab Biosimilar, by Subcutaneous Dosing Using a Prefilled Syringe or a Prefilled Pen in Healthy Subjects
Randomized, Open‐Label, Single‐Dose, Parallel‐Group Pharmacokinetic Study of PF‐06410293 (adalimumab‐afzb), an Adalimumab Biosimilar, by Subcutaneous Dosing Using a Prefilled Syringe or a Prefilled Pen in Healthy Subjects Abstract Abstract This open‐label, single‐dose, randomized, parallel‐group, 2‐arm phase 1 bioequiv...
PMC11664478
core_pubmed_pmc
Research Progress on the Anti-Liver Cancer Mechanism and Toxicity of Rhubarb Anthraquinone
Research Progress on the Anti-Liver Cancer Mechanism and Toxicity of Rhubarb Anthraquinone Abstract Ethnopharmacological Relevance Rhubarb has the effect of breaking blood stasis and abnormal mass, and was often used to treat various tumor diseases including liver cancer in ancient China. Recipes containing rhubarb hav...
PMC12849343
core_pubmed_pmc
Optimal accompanying diagnosis design through external validation of population pharmacokinetic models for moxifloxacin in tuberculosis patients
Optimal accompanying diagnosis design through external validation of population pharmacokinetic models for moxifloxacin in tuberculosis patients Abstract Background We aimed to design an optimal accompanying diagnosis, defined as a model-informed limited sampling strategy (LSS) that uses validated population pharmacoki...
PMC12782372
core_pubmed_pmc
Pharmacokinetics and analgesic efficacy of fentanyl and buprenorphine in chicken embryos
Pharmacokinetics and analgesic efficacy of fentanyl and buprenorphine in chicken embryos Abstract Chicken embryos are able to process and receive noxious stimuli from embryonic day (ED) 13. In the context of animal welfare, analgesic refinement is highly recommended for painful procedures from this time onwards. In thi...
PMC6505506
core_pubmed_pmc
Scaling Drug Clearance from Adults to the Young Children for Drugs Undergoing Hepatic Metabolism: A Simulation Study to Search for the Simplest Scaling Method
Scaling Drug Clearance from Adults to the Young Children for Drugs Undergoing Hepatic Metabolism: A Simulation Study to Search for the Simplest Scaling Method Abstract Previous research showed that scaling drug clearance from adults to children based on body weight alone is not accurate for all hepatically cleared drug...
PMC6591635
core_pubmed_pmc
Advancing the Therapeutic Potential of Indoleamides for Tuberculosis
Advancing the Therapeutic Potential of Indoleamides for Tuberculosis Abstract Indole-2-carboxamide derivatives are inhibitors of MmpL3, the cell wall-associated mycolic acid transporter of Mycobacterium tuberculosis . In the present study, we characterized indoleamide effects on bacterial cell morphology and reevaluate...
PMC10702854
core_pubmed_pmc
Development of an in vitro pharmacokinetic/pharmacodynamic model in the presence of serum for studying micafungin activity against Candida albicans: a need for revision of CLSI susceptibility breakpoints
Development of an in vitro pharmacokinetic/pharmacodynamic model in the presence of serum for studying micafungin activity against Candida albicans: a need for revision of CLSI susceptibility breakpoints Abstract Abstract Background The CLSI breakpoint for micafungin and Candida albicans is 0.25 mg/L, higher than the C...
PMC8493764
core_pubmed_pmc
The Risk of Bleeding Complications in Intra-Articular Injections and Arthrocentesis in Patients on Novel Oral Anticoagulants: A Systematic Review
The Risk of Bleeding Complications in Intra-Articular Injections and Arthrocentesis in Patients on Novel Oral Anticoagulants: A Systematic Review Abstract Novel oral anticoagulants (NOACs) are increasingly prescribed blood-thinning medication. Surpassing Warfarin, NOACs are more favored and extensively used in paroxysm...
PMC3605053
core_pubmed_pmc
Systematic Prediction of Pharmacodynamic Drug-Drug Interactions through Protein-Protein-Interaction Network
Systematic Prediction of Pharmacodynamic Drug-Drug Interactions through Protein-Protein-Interaction Network Abstract Abstract Identifying drug-drug interactions (DDIs) is a major challenge in drug development. Previous attempts have established formal approaches for pharmacokinetic (PK) DDIs, but there is not a feasibl...
PMC8051852
core_pubmed_pmc
Clinical trial to evaluate pharmacokinetics and pharmacodynamics of medroxyprogesterone acetate after subcutaneous administration of Depo-Provera
Clinical trial to evaluate pharmacokinetics and pharmacodynamics of medroxyprogesterone acetate after subcutaneous administration of Depo-Provera Abstract Abstract Objective To evaluate the pharmacokinetics and pharmacodynamics of medroxyprogesterone acetate after a single subcutaneous injection in the abdomen of 150 o...
PMC2938261
core_pubmed_pmc
Integrated preclinical and clinical development of mTOR inhibitors in pancreatic cancer
Integrated preclinical and clinical development of mTOR inhibitors in pancreatic cancer Abstract Background: The purpose of this work was to determine the efficacy of inhibiting mammalian target of rapamycin (mTOR) in pancreatic cancer preclinical models and translate preclinical observations to the clinic. Methods: Te...
PMC8212774
core_pubmed_pmc
IV and oral fosfomycin pharmacokinetics in neonates with suspected clinical sepsis
IV and oral fosfomycin pharmacokinetics in neonates with suspected clinical sepsis Abstract Abstract Background Fosfomycin has the potential to be re-purposed as part of a combination therapy to treat neonatal sepsis where resistance to current standard of care (SOC) is common. Limited data exist on neonatal fosfomycin...
PMC10954928
core_pubmed_pmc
Towards More Robust Evaluation of the Predictive Performance of Physiologically Based Pharmacokinetic Models: Using Confidence Intervals to Support Use of Model-Informed Dosing in Clinical Care
Towards More Robust Evaluation of the Predictive Performance of Physiologically Based Pharmacokinetic Models: Using Confidence Intervals to Support Use of Model-Informed Dosing in Clinical Care Abstract Background and Objective With the rise in the use of physiologically based pharmacokinetic (PBPK) modeling over the p...
PMC5302152
core_pubmed_pmc
A review of perioperative anesthesia and analgesia for infants: updates and trends to watch
A review of perioperative anesthesia and analgesia for infants: updates and trends to watch Abstract Abstract This review focuses on pharmacokinetics and pharmacodynamics of opioid and non-opioid analgesics in neonates and infants. The unique physiology of this population differs from that of adults and impacts drug ha...
PMC8532701
core_pubmed_pmc
Pharmacokinetic Parameters and Tissue Withdrawal Intervals for Sheep Administered Multiple Oral Doses of Meloxicam
Pharmacokinetic Parameters and Tissue Withdrawal Intervals for Sheep Administered Multiple Oral Doses of Meloxicam Abstract Simple Summary Meloxicam is an anti-inflammatory drug used to treat pain and inflammation in ruminants including sheep, and pharmacokinetic studies are needed to protect the food supply from drug ...
PMC11802711
core_pubmed_pmc
Pharmacokinetics of Zilurgisertib With and Without Food from Single and Multiple Ascending Dose Phase 1 Studies in Healthy Adults
Pharmacokinetics of Zilurgisertib With and Without Food from Single and Multiple Ascending Dose Phase 1 Studies in Healthy Adults Abstract Background and Objectives The oral, potent, and highly selective activin receptor-like kinase 2 (ALK2) inhibitor zilurgisertib (INCB000928) is in development as a treatment for fibr...
PMC5394958
core_pubmed_pmc
Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia
Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia Abstract Abstract A vailable tyrosine kinase inhibitors for chronic myeloid leukemia bind in an adenosine 5′-triphosphate-binding pocket and are affected by evolving mutations that confer re...
PMC10794775
core_pubmed_pmc
The application of mirabilite in traditional Chinese medicine and its chemical constituents, processing methods, pharmacology, toxicology and clinical research
The application of mirabilite in traditional Chinese medicine and its chemical constituents, processing methods, pharmacology, toxicology and clinical research Abstract Abstract Purpose: This study reviews the use of mirabilite in traditional Chinese medicine and various preparations by describing its chemical composit...
PMC11455768
core_pubmed_pmc
Clinical Assessment of Breast Cancer Resistance Protein (BCRP)-Mediated Drug–Drug Interactions of Sepiapterin with Curcumin and Rosuvastatin in Healthy Volunteers
Clinical Assessment of Breast Cancer Resistance Protein (BCRP)-Mediated Drug–Drug Interactions of Sepiapterin with Curcumin and Rosuvastatin in Healthy Volunteers Abstract Background and Objective Sepiapterin, also known as PTC923 and CNSA-001, is a synthetic form of endogenous sepiapterin being developed as a novel or...
PMC11320736
core_pubmed_pmc
Advances in Physiologically Based Pharmacokinetic (PBPK) Modeling of Nanomaterials
Advances in Physiologically Based Pharmacokinetic (PBPK) Modeling of Nanomaterials Abstract Abstract Nanoparticles (NPs) have been widely used to improve the pharmacokinetic properties and tissue distribution of small molecules such as targeting to a specific tissue of interest, enhancing their systemic circulation, an...
PMC12057369
core_pubmed_pmc
The effect of pregnancy on the population pharmacokinetics of levofloxacin in South Africans with rifampicin-resistant tuberculosis
The effect of pregnancy on the population pharmacokinetics of levofloxacin in South Africans with rifampicin-resistant tuberculosis Abstract ABSTRACT Levofloxacin is a key drug in the prevention and treatment of rifampicin-resistant tuberculosis (RR-TB). There are limited data describing the effect of pregnancy on the ...
PMC5909210
core_pubmed_pmc
Shorter treatment for minimal tuberculosis (TB) in children (SHINE): a study protocol for a randomised controlled trial
Shorter treatment for minimal tuberculosis (TB) in children (SHINE): a study protocol for a randomised controlled trial Abstract Abstract Background Tuberculosis (TB) in children is frequently paucibacillary and non-severe forms of pulmonary TB are common. Evidence for tuberculosis treatment in children is largely extr...
PMC8332591
core_pubmed_pmc
Effect of Kidney or Hepatic Impairment on the Pharmacokinetics and Pharmacodynamics of Somapacitan: Two Open-Label, Parallel-Group Trials
Effect of Kidney or Hepatic Impairment on the Pharmacokinetics and Pharmacodynamics of Somapacitan: Two Open-Label, Parallel-Group Trials Abstract Introduction Somapacitan is a long-acting growth hormone (GH) derivative being developed for once-weekly dosing in patients with GH deficiency (GHD). Our objective was to ev...
PMC12736570
core_pubmed_pmc
The Absorption, Distribution, Excretion, and In Vitro Hepatic Microsomal Metabolism of the Novel CDK Compound XMD12 in Sprague-Dawley Rats
The Absorption, Distribution, Excretion, and In Vitro Hepatic Microsomal Metabolism of the Novel CDK Compound XMD12 in Sprague-Dawley Rats Abstract Background : Cyclin-dependent kinase 4/6 (CDK4/6) represents one of the clinically validated and therapeutically effective anticancer targets. Methods : This study establis...
PMC7356940
core_pubmed_pmc
Comparison between Colistin Sulfate Dry Powder and Solution for Pulmonary Delivery
Comparison between Colistin Sulfate Dry Powder and Solution for Pulmonary Delivery Abstract To assess the difference in the fate of the antibiotic colistin (COLI) after its pulmonary delivery as a powder or a solution, we developed a COLI powder and evaluated the COLI pharmacokinetic properties in rats after pulmonary ...
PMC12182535
core_pubmed_pmc
Cutting-edge dynamics and research hotspots on boswellic acid in cancer: a bibliometrics analysis from 1994 to 2024
Cutting-edge dynamics and research hotspots on boswellic acid in cancer: a bibliometrics analysis from 1994 to 2024 Abstract Abstract Background Recent studies have highlighted the potential of boswellic acid as a promising therapeutic option in cancer treatment. Despite its growing relevance, there has been a lack of ...
PMC5317174
core_pubmed_pmc
CRISPR knockout rat cytochrome P450 3A1/2 model for advancing drug metabolism and pharmacokinetics research
CRISPR knockout rat cytochrome P450 3A1/2 model for advancing drug metabolism and pharmacokinetics research Abstract Abstract Cytochrome P450 (CYP) 3A accounts for nearly 30% of the total CYP enzymes in the human liver and participates in the metabolism of over 50% of clinical drugs. Moreover, CYP3A plays an important ...
PMC8442490
core_pubmed_pmc
Asenapine: an atypical antipsychotic with atypical formulations
Asenapine: an atypical antipsychotic with atypical formulations Abstract Asenapine is a second-generation (atypical) antipsychotic medication not available in a pill that can be swallowed; rather, it is commercialized in sublingual and transdermal formulations. This is a consequence of extensive first-pass metabolism i...
PMC12557390
core_pubmed_pmc
Exploiting the Cryptic αD Pocket of Casein Kinase 2α (CK2α) to Deliver Highly Potent and Selective Type 1 Inhibitors
Exploiting the Cryptic αD Pocket of Casein Kinase 2α (CK2α) to Deliver Highly Potent and Selective Type 1 Inhibitors Abstract Abstract Casein kinase 2α (CK2α) is an oncology drug target that acts as a positive regulator of many tumorigenic signaling pathways. We previously reported that CK2α has a unique cryptic bindin...
PMC9228122
core_pubmed_pmc
Cell Fate following Irradiation of MDA-MB-231 and MCF-7 Breast Cancer Cells Pre-Exposed to the Tetrahydroisoquinoline Sulfamate Microtubule Disruptor STX3451
Cell Fate following Irradiation of MDA-MB-231 and MCF-7 Breast Cancer Cells Pre-Exposed to the Tetrahydroisoquinoline Sulfamate Microtubule Disruptor STX3451 Abstract A tetrahydroisoquinoline (THIQ) core is able to mimic the A and B rings of 2-methoxyestradiol (2ME2), an endogenous estrogen metabolite that demonstrates...
PMC12567144
core_pubmed_pmc
Development of Co-Amorphous Systems for Inhalation Therapy—Part 2: In Silico Guided Co-Amorphous Rifampicin–Moxifloxacin and –Ethambutol Formulations
Development of Co-Amorphous Systems for Inhalation Therapy—Part 2: In Silico Guided Co-Amorphous Rifampicin–Moxifloxacin and –Ethambutol Formulations Abstract Background/Objectives: Tuberculosis (TB) remains a global health challenge due to long treatment durations, poor adherence, and growing drug resistance. Inhalabl...
PMC11275143
core_pubmed_pmc
Energy Metabolism and Metformin: Effects on Ischemia-Reperfusion Injury in Kidney Transplantation
Energy Metabolism and Metformin: Effects on Ischemia-Reperfusion Injury in Kidney Transplantation Abstract Metformin (MTF) is the only biguanide included in the World Health Organization’s list of essential medicines; representing a widespread drug in the management of diabetes mellitus. With its accessibility and affo...
PMC6758592
core_pubmed_pmc
Evaluation of Information in Summaries of Product Characteristics (SmPCs) on the Use of a Medicine in Patients With Hepatic Impairment
Evaluation of Information in Summaries of Product Characteristics (SmPCs) on the Use of a Medicine in Patients With Hepatic Impairment Abstract Background: In 2005, the European Medicines Agency (EMA) released guidance on pharmacokinetic studies in patients with hepatic impairment. This guidance describes the design of...
PMC4332912
core_pubmed_pmc
Synovial fluid pharmacokinetics of tulathromycin, gamithromycin and florfenicol after a single subcutaneous dose in cattle
Synovial fluid pharmacokinetics of tulathromycin, gamithromycin and florfenicol after a single subcutaneous dose in cattle Abstract Background Deep digital septic conditions represent some of the most refractory causes of severe lameness in cattle. The objective of this study was to determine the distribution of tulath...
PMC6212960
core_pubmed_pmc
Exposure of Breast and Lung Cancer Cells to a Novel Estrone Analog Prior to Radiation Enhances Bcl-2-Mediated Cell Death
Exposure of Breast and Lung Cancer Cells to a Novel Estrone Analog Prior to Radiation Enhances Bcl-2-Mediated Cell Death Abstract Abstract Following exposure of cells to gamma-radiation, a cascade of intracellular consequences may be observed in a semitemporal manner. This includes deoxyribonucleic acid (DNA) damage an...
PMC6017115
core_pubmed_pmc
Inhibitory Effect of Sauchinone on UDP-Glucuronosyltransferase (UGT) 2B7 Activity
Inhibitory Effect of Sauchinone on UDP-Glucuronosyltransferase (UGT) 2B7 Activity Abstract Abstract Herb–drug interaction (HDI) limits clinical application of herbs and drugs, and inhibition of herbs towards uridine diphosphate (UDP)-glucuronosyltransferases (UGTs) has gained attention as one of the important reasons t...
PMC11938312
core_pubmed_pmc
Prediction of human pharmacokinetics of Fc-engineered therapeutic monoclonal antibodies using human FcRn transgenic mice
Prediction of human pharmacokinetics of Fc-engineered therapeutic monoclonal antibodies using human FcRn transgenic mice Abstract ABSTRACT Human FcRn transgenic mice (Tg32) have been widely used to evaluate the pharmacokinetics of mAbs and predict human pharmacokinetics. This study aims to establish an approach for pre...
PMC8786932
core_pubmed_pmc
Bicyclic azetidines target acute and chronic stages of Toxoplasma gondii by inhibiting parasite phenylalanyl t-RNA synthetase
Bicyclic azetidines target acute and chronic stages of Toxoplasma gondii by inhibiting parasite phenylalanyl t-RNA synthetase Abstract Toxoplasma gondii commonly infects humans and while most infections are controlled by the immune response, currently approved drugs are not capable of clearing chronic infection in huma...
PMC10270346
core_pubmed_pmc
Implications of reducing antibiotic treatment duration for antimicrobial resistance in hospital settings: A modelling study and meta-analysis
Implications of reducing antibiotic treatment duration for antimicrobial resistance in hospital settings: A modelling study and meta-analysis Abstract Abstract Background Reducing antibiotic treatment duration is a key component of hospital antibiotic stewardship interventions. However, its effectiveness in reducing an...
PMC9584878
core_pubmed_pmc
Evaluation of analgesic and anti-inflammatory activity of purine-2,6-dione-based TRPA1 antagonists with PDE4/7 inhibitory activity
Evaluation of analgesic and anti-inflammatory activity of purine-2,6-dione-based TRPA1 antagonists with PDE4/7 inhibitory activity Abstract Background To verify the validity of the proposed pain treatment approach, which is based on concomitant blocking of the Transient Receptor Potential Ankyrin 1 (TRPA1) channel and ...
PMC12468923
core_pubmed_pmc
Dose-Related Pharmacokinetic and Pharmacodynamic Effects of Intramuscular Epinephrine in Healthy Neonatal Piglets
Dose-Related Pharmacokinetic and Pharmacodynamic Effects of Intramuscular Epinephrine in Healthy Neonatal Piglets Abstract Abstract Highlights What are the main findings? Intramuscular epinephrine produced dose-dependent cardiovascular effects in newborn piglets. A dose of 0.1 mg/kg IM epinephrine achieved hemodynamic ...
PMC12683145
core_pubmed_pmc
Quantitative LC-MS/MS profiling of N-Acetylcysteine in chicken plasma: Method validation and pharmacokinetic characterization
Quantitative LC-MS/MS profiling of N-Acetylcysteine in chicken plasma: Method validation and pharmacokinetic characterization Abstract Abstract N-Acetylcysteine (NAC), an essential precursor in glutathione synthesis, exhibits broad therapeutic potential but remains pharmacokinetically (PK) poorly characterized in poult...
PMC7839396
core_pubmed_pmc
Molecular dynamics analysis of phytochemicals from Ageratina adenophora against COVID-19 main protease (M pro ) and human angiotensin-converting enzyme 2 (ACE2)
Molecular dynamics analysis of phytochemicals from Ageratina adenophora against COVID-19 main protease (M pro ) and human angiotensin-converting enzyme 2 (ACE2) Abstract The outbreak of COVID-19 created unprecedented strain in the healthcare system. Various research revealed that COVID-19 main protease (M pro ) and hum...
PMC12960310
core_pubmed_pmc
Use of a Cystatin C-Based GFR Equation in a Population Pharmacokinetic Model of Methotrexate Clearance in Adult Patients with Lymphoma
Use of a Cystatin C-Based GFR Equation in a Population Pharmacokinetic Model of Methotrexate Clearance in Adult Patients with Lymphoma Abstract Background High-dose methotrexate (HDMTX) is a key treatment for lymphoma with central nervous system involvement. Whether incorporating cystatin C into glomerular filtration r...
PMC4504337
core_pubmed_pmc
Cardiovascular effects of basal insulins
Cardiovascular effects of basal insulins Abstract Abstract Basal insulin is an important component of treatment for both type 1 and type 2 diabetes. One of the principal aims of treatment in patients with diabetes is the prevention of diabetic complications, including cardiovascular disease. There is some evidence, alt...
PMC3984342
core_pubmed_pmc
Preclinical characterization of an anti-methamphetamine monoclonal antibody for human use
Preclinical characterization of an anti-methamphetamine monoclonal antibody for human use Abstract Ch-mAb7F9, a human-mouse chimeric monoclonal antibody (mAb) designed to bind (+)-methamphetamine (METH) with high affinity and specificity, was produced as a treatment medication for METH abuse. In these studies, we prese...
PMC6345873
core_pubmed_pmc
Quantitative analysis, pharmacokinetics and metabolomics study for the comprehensive characterization of the salt-processing mechanism of Psoraleae Fructus
Quantitative analysis, pharmacokinetics and metabolomics study for the comprehensive characterization of the salt-processing mechanism of Psoraleae Fructus Abstract Abstract Research based on quantitative analysis, pharmacokinetics and metabolomics was conducted to explore the effects of salt-processing on Psoraleae Fr...
PMC11474527
core_pubmed_pmc
Transporter Protein Expression of Corneal Epithelium in Rabbit and Porcine: Evaluation of Models for Ocular Drug Transport Study
Transporter Protein Expression of Corneal Epithelium in Rabbit and Porcine: Evaluation of Models for Ocular Drug Transport Study Abstract Abstract The transcorneal route is the main entry route for drugs to the intraocular parts, after topical administration. The outer surface, the corneal epithelium (CE), forms the ra...
PMC6921057
core_pubmed_pmc
Development and Evaluation of Physiologically Based Pharmacokinetic Drug–Disease Models for Predicting Rifampicin Exposure in Tuberculosis and Cirrhosis Populations
Development and Evaluation of Physiologically Based Pharmacokinetic Drug–Disease Models for Predicting Rifampicin Exposure in Tuberculosis and Cirrhosis Populations Abstract Abstract The physiologically based pharmacokinetic (PBPK) approach facilitates the construction of novel drug–disease models by allowing incorpora...
PMC10821532
core_pubmed_pmc
Sex and Cross-Sex Testosterone Treatment Alters Gamma-Hydroxybutyrate Acid Toxicokinetics and Toxicodynamics in Rats
Sex and Cross-Sex Testosterone Treatment Alters Gamma-Hydroxybutyrate Acid Toxicokinetics and Toxicodynamics in Rats Abstract Abstract Γ-hydroxybutyric acid (GHB) is widely abused due to its sedative/hypnotic and euphoric effects. In recent years, GHB use has witnessed a notable rise within the LGBTQ+ community. GHB is...
PMC9090408
core_pubmed_pmc
Mechanochemical preparation of triptolide-loaded self-micelle solid dispersion with enhanced oral bioavailability and improved anti-tumor activity
Mechanochemical preparation of triptolide-loaded self-micelle solid dispersion with enhanced oral bioavailability and improved anti-tumor activity Abstract Abstract Triptolide (TP), a compound isolated from a Chinese medicinal herb, possesses potent anti-tumor, immunosuppressive, and anti-inflammatory properties, but w...
PMC5283701
core_pubmed_pmc
Abuse Potential with Oral Route of Administration of a Hydrocodone Extended-Release Tablet Formulated with Abuse-Deterrence Technology in Nondependent, Recreational Opioid Users
Abuse Potential with Oral Route of Administration of a Hydrocodone Extended-Release Tablet Formulated with Abuse-Deterrence Technology in Nondependent, Recreational Opioid Users Abstract Objective . To compare the oral abuse potential of hydrocodone extended-release (ER) tablet developed with CIMA ® Abuse-Deterrence Te...
PMC4070462
core_pubmed_pmc
Pharmacokinetics of a Prototype Formulation of Sublingual Testosterone and a Buspirone Tablet, Versus an Advanced Combination Tablet of Testosterone and Buspirone in Healthy Premenopausal Women
Pharmacokinetics of a Prototype Formulation of Sublingual Testosterone and a Buspirone Tablet, Versus an Advanced Combination Tablet of Testosterone and Buspirone in Healthy Premenopausal Women Abstract The study aimed to compare the kinetics of two novel combination drug products for Female Sexual Interest/Arousal Dis...
PMC4055052
core_pubmed_pmc
Modulation of β-amyloid by a single dose of GSK933776 in patients with mild Alzheimer’s disease: a phase I study
Modulation of β-amyloid by a single dose of GSK933776 in patients with mild Alzheimer’s disease: a phase I study Abstract Abstract Introduction In this study, we evaluated the safety and pharmacodynamic effects of the Fc-inactivated anti-β-amyloid (anti-Aβ) monoclonal antibody GSK933776 in patients with mild Alzheimer’...
PMC5363337
core_pubmed_pmc
Oral Human Abuse Potential of Oxycodone DETERx ® (Xtampza ® ER)
Oral Human Abuse Potential of Oxycodone DETERx ® (Xtampza ® ER) Abstract Abstract Oxycodone DETERx ® (Collegium Pharmaceutical Inc, Canton, Massachusetts) is an extended‐release, microsphere‐in‐capsule, abuse‐deterrent formulation designed to retain its extended‐release properties after tampering (eg, chewing/crushing)...
PMC8180459
core_pubmed_pmc
Anthelmintics for drug repurposing: Opportunities and challenges
Anthelmintics for drug repurposing: Opportunities and challenges Abstract Abstract Drug repositioning is defined as a process to identify a new application for drugs. This approach is critical as it takes advantage of well-known pharmacokinetics, pharmacodynamics, and toxicity profiles of the drugs; thus, the chance of...
PMC11622284
core_pubmed_pmc
Plain Language Summary of Publication: Does crushing vibegron 75 mg tablet affect its safety or the amount of vibegron in the body over time in healthy adults?
Plain Language Summary of Publication: Does crushing vibegron 75 mg tablet affect its safety or the amount of vibegron in the body over time in healthy adults? Abstract What is this summary about? This is a plain language summary of an article published in the journal Clinical Pharmacology in Drug Development . It is a...
PMC7282138
core_pubmed_pmc
Clinical application of the AUC-guided dosage adjustment of docetaxel-based chemotherapy for patients with solid tumours: a single centre, prospective and randomised control study
Clinical application of the AUC-guided dosage adjustment of docetaxel-based chemotherapy for patients with solid tumours: a single centre, prospective and randomised control study Abstract Background Docetaxel (DTX) is a widely used anti-tumour drug, and its dosage is solely determined by body surface area (BSA). Adver...
PMC10339702
core_pubmed_pmc
A linked physiologically based pharmacokinetic model for hydroxychloroquine and metabolite desethylhydroxychloroquine in SARS‐CoV‐2(−)/(+) populations
A linked physiologically based pharmacokinetic model for hydroxychloroquine and metabolite desethylhydroxychloroquine in SARS‐CoV‐2(−)/(+) populations Abstract Abstract Hydroxychloroquine (HCQ) is Food and Drug Administration (FDA)‐approved for malaria, systemic and chronic discoid lupus erythematosus, and rheumatoid a...
PMC6828621
core_pubmed_pmc
Estimating the optimal dose of flupentixol decanoate in the maintenance treatment of schizophrenia—a systematic review of the literature
Estimating the optimal dose of flupentixol decanoate in the maintenance treatment of schizophrenia—a systematic review of the literature Abstract Rationale The licensed dose range for the long-acting injectable antipsychotic flupentixol decanoate (Depixol®) in the treatment of schizophrenia is very broad. This provides...
PMC4265406
core_pubmed_pmc
The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine
The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine Abstract Background Dihydroartemisinin (DHA) is a component of artemisinin-based combin...
PMC3899454
core_pubmed_pmc
Insulin Degludec: Pharmacokinetic Properties in Subjects with Hepatic Impairment
Insulin Degludec: Pharmacokinetic Properties in Subjects with Hepatic Impairment Abstract Abstract Background and Objective Insulin degludec is a basal insulin with a slow and distinct absorption mechanism resulting in an ultra-long, flat, and stable pharmacokinetic profile in patients with diabetes mellitus. The aim o...
PMC3975451
core_pubmed_pmc
Pharmacokinetics of fluralaner in dogs following a single oral or intravenous administration
Pharmacokinetics of fluralaner in dogs following a single oral or intravenous administration Abstract Abstract Background Fluralaner is a novel systemic insecticide and acaricide. The purpose of these studies was to investigate the pharmacokinetic properties of fluralaner in Beagle dogs following single oral or intrave...
PMC7786013
core_pubmed_pmc
Nicotine pharmacokinetics of electronic cigarettes: A pooled data analysis from the literature
Nicotine pharmacokinetics of electronic cigarettes: A pooled data analysis from the literature Abstract Highlights • Evaluating the pharmacokinetics of nicotine absorption from electronic cigarettes. • Nicotine absorption into the blood is influenced by several factors. • These include e-liquid composition, user behavi...
PMC9263050
core_pubmed_pmc
Recent progress on vascular endothelial growth factor receptor inhibitors with dual targeting capabilities for tumor therapy
Recent progress on vascular endothelial growth factor receptor inhibitors with dual targeting capabilities for tumor therapy Abstract Vascular endothelial growth factor receptors (VEGFRs) are a family of receptor protein tyrosine kinases that play an important role in the regulation of tumor-induced angiogenesis. Curre...
PMC12355023
core_pubmed_pmc
Model‐Informed Precision Dosing of Busulfan for Children and Adults Undergoing Allogeneic Hematopoietic Stem Cell Transplantation: A Critical Evaluation of Current PK Models and Dose Recommendations
Model‐Informed Precision Dosing of Busulfan for Children and Adults Undergoing Allogeneic Hematopoietic Stem Cell Transplantation: A Critical Evaluation of Current PK Models and Dose Recommendations Abstract Busulfan is administered intravenously in conditioning regimens prior to allogeneic hematopoietic stem cell tran...
PMC10725267
core_pubmed_pmc
Combining pharmacometric models with predictive and prognostic biomarkers for precision therapy in Crohn's disease: A case study of brazikumab
Combining pharmacometric models with predictive and prognostic biomarkers for precision therapy in Crohn's disease: A case study of brazikumab Abstract Abstract Pharmacometric models were used to investigate the utility of biomarkers in predicting the efficacy (Crohn's Disease Activity Index [CDAI]) of brazikumab and p...
PMC9561539
core_pubmed_pmc
Fluoxetine pharmacokinetics and tissue distribution quantitatively supports a therapeutic role in COVID-19 at a minimum dose of 20 mg per day
Fluoxetine pharmacokinetics and tissue distribution quantitatively supports a therapeutic role in COVID-19 at a minimum dose of 20 mg per day Abstract Abstract Background. Various in vitro studies have shown fluoxetine inhibits multiple variants of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) pathog...
PMC10367002
core_pubmed_pmc
Development of a UPLC-ESI-MS/MS method for the determination of triamcinolone acetonide in human plasma and evaluation of its bioequivalence after a single intramuscular injection in healthy volunteers
Development of a UPLC-ESI-MS/MS method for the determination of triamcinolone acetonide in human plasma and evaluation of its bioequivalence after a single intramuscular injection in healthy volunteers Abstract Abstract Introduction: Triamcinolone acetonide (TA) is commonly used in the treatment of various inflammatory...
PMC9859815
core_pubmed_pmc
Pharmacokinetics and bioequivalence evaluation of omeprazole and sodium bicarbonate dry suspensions in healthy Chinese volunteers
Pharmacokinetics and bioequivalence evaluation of omeprazole and sodium bicarbonate dry suspensions in healthy Chinese volunteers Abstract Omeprazole and sodium bicarbonate dry suspension are effective treatments for acid-related disorders. This study compared the bioequivalence and safety of the two formulations of om...
PMC8164448
core_pubmed_pmc
Fixed Dose Single Tablet Formulation with Differential Release of Amlodipine Besylate and Simvastatin and Its Pharmacokinetic Profile: QbD and Risk Assessment Approach
Fixed Dose Single Tablet Formulation with Differential Release of Amlodipine Besylate and Simvastatin and Its Pharmacokinetic Profile: QbD and Risk Assessment Approach Abstract Abstract Purpose A differential release fixed dose matrix tablet of amlodipine besylate (AML-B) and simvastatin (SIM) was formulated to enhance...
PMC7310148
core_pubmed_pmc
A study to assess the correlation between plasma, oral fluid and urine concentrations of flunixin meglumine with the tissue residue depletion profile in finishing-age swine
A study to assess the correlation between plasma, oral fluid and urine concentrations of flunixin meglumine with the tissue residue depletion profile in finishing-age swine Abstract Abstract Background Flunixin meglumine (FM) was investigated for the effectiveness of plasma, oral fluid, and urine concentrations to pred...
PMC11529441
core_pubmed_pmc
Establishment and validation of a population pharmacokinetic model for apatinib in patients with tumors
Establishment and validation of a population pharmacokinetic model for apatinib in patients with tumors Abstract Objective This study aimed to develop a population pharmacokinetic (PPK) model for oral apatinib in Chinese oncology patients and investigate the factors influencing the pharmacokinetics of apatinib. Methods...
PMC9441699
core_pubmed_pmc
In silico investigation and potential therapeutic approaches of natural products for COVID-19: Computer-aided drug design perspective
In silico investigation and potential therapeutic approaches of natural products for COVID-19: Computer-aided drug design perspective Abstract The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has caused a substantial number of deaths around the world, making it a serious and pressing public health hazar...
PMC9947016
core_pubmed_pmc
In vitro to clinical translational pharmacokinetic/pharmacodynamic modeling of doxorubicin (DOX) and dexrazoxane (DEX) interactions: Safety assessment and optimization
In vitro to clinical translational pharmacokinetic/pharmacodynamic modeling of doxorubicin (DOX) and dexrazoxane (DEX) interactions: Safety assessment and optimization Abstract Despite high anticancer activity, doxorubicin (DOX)-induced cardiotoxicity (DIC) limits the extensive utility of DOX in a clinical setting. Amo...
PMC8184714
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of ampreloxetine, a novel, selective norepinephrine reuptake inhibitor, in symptomatic neurogenic orthostatic hypotension
Pharmacokinetics and pharmacodynamics of ampreloxetine, a novel, selective norepinephrine reuptake inhibitor, in symptomatic neurogenic orthostatic hypotension Abstract Abstract Purpose Ampreloxetine is a novel, selective, long-acting norepinephrine reuptake (NET) inhibitor being investigated as a once-daily oral treat...
PMC8949207
core_pubmed_pmc
Development and Optimization of Nanolipid-Based Formulation of Diclofenac Sodium: In Vitro Characterization and Preclinical Evaluation
Development and Optimization of Nanolipid-Based Formulation of Diclofenac Sodium: In Vitro Characterization and Preclinical Evaluation Abstract In the present research study, we formulate bilosomes (BMs) of diclofenac (DC) for oral delivery for enhancement of therapeutic efficacy (anti-inflammatory disease). The BMS we...
PMC6158327
core_pubmed_pmc
Negative Allosteric Modulators of mGlu 7 Receptor as Putative Antipsychotic Drugs
Negative Allosteric Modulators of mGlu 7 Receptor as Putative Antipsychotic Drugs Abstract The data concerning antipsychotic-like activity of negative allosteric modulators (NAMs)/antagonists of mGlu 7 receptors are limited. The only available ligands for this receptor are MMPIP and ADX71743 . In the present studies, w...
PMC3912697
core_pubmed_pmc
Learning gain of pharmacy students after introducing guided inquiry learning with computer simulation in a pharmacology class in Fiji
Learning gain of pharmacy students after introducing guided inquiry learning with computer simulation in a pharmacology class in Fiji Abstract Purpose: Active learning methods such as problem-based learning have been widely adopted in health professions education, although guided inquiry learning has been used only in ...
PMC4632757
core_pubmed_pmc
Microanalysis, Pharmacokinetics and Tissue Distribution of Polysaccharide-Protein Complexes from Longan Pulp in Mice
Microanalysis, Pharmacokinetics and Tissue Distribution of Polysaccharide-Protein Complexes from Longan Pulp in Mice Abstract Abstract A high performance size exclusion-fluorescence detection (HPSEC-FD) method combined with fluorescein isothiocyanate (FITC) prelabeling was established for the microanalysis of polysacch...
PMC7689203
core_pubmed_pmc
Translational Development Strategies for TAK-063, a Phosphodiesterase 10A Inhibitor
Translational Development Strategies for TAK-063, a Phosphodiesterase 10A Inhibitor Abstract Abstract Background TAK-063 is an inhibitor of phosphodiesterase 10A (PDE10A), an enzyme highly expressed in medium spiny neurons of the striatum. PDE10A hydrolyzes both cyclic adenosine monophosphate and cyclic guanosine monop...
PMC8086230
core_pubmed_pmc
Pharmacokinetics-based identification of pseudoaldosterogenic compounds originating from Glycyrrhiza uralensis roots (Gancao) after dosing LianhuaQingwen capsule
Pharmacokinetics-based identification of pseudoaldosterogenic compounds originating from Glycyrrhiza uralensis roots (Gancao) after dosing LianhuaQingwen capsule Abstract LianhuaQingwen capsule, prepared from an herbal combination, is officially recommended as treatment for COVID-19 in China. Of the serial pharmacokine...
PMC10805439
core_pubmed_pmc
Efficacy, Safety, Pharmacokinetics, and Immunogenicity of DRL-Trastuzumab Versus Herceptin in Human Epidermal Growth Factor Receptor 2–Positive Metastatic Breast Cancer: A Randomized Controlled Trial
Efficacy, Safety, Pharmacokinetics, and Immunogenicity of DRL-Trastuzumab Versus Herceptin in Human Epidermal Growth Factor Receptor 2–Positive Metastatic Breast Cancer: A Randomized Controlled Trial Abstract Abstract PURPOSE Dr Reddy's Laboratories Trastuzumab (DRL_TZ) is a biosimilar to Herceptin under development. T...
PMC10628589
core_pubmed_pmc
Phase I Study of Entinostat, Atezolizumab, Carboplatin, and Etoposide in Previously Untreated Extensive-Stage Small Cell Lung Cancer, ETCTN 10399
Phase I Study of Entinostat, Atezolizumab, Carboplatin, and Etoposide in Previously Untreated Extensive-Stage Small Cell Lung Cancer, ETCTN 10399 Abstract Abstract Background CREBBP and EP300 mutations occur at a frequency of 15% and 13%, respectively, in small cell lung cancer (SCLC), and preclinical models demonstrat...
PMC9474693
core_pubmed_pmc
Assessing Prolongation of the Corrected QT Interval with Bedaquiline and Delamanid Coadministration to Predict the Cardiac Safety of Simplified Dosing Regimens
Assessing Prolongation of the Corrected QT Interval with Bedaquiline and Delamanid Coadministration to Predict the Cardiac Safety of Simplified Dosing Regimens Abstract Abstract Delamanid and bedaquiline are two drugs approved to treat drug‐resistant tuberculosis, and each have been associated with corrected QT interva...
PMC12655182
core_pubmed_pmc
Clinical Efficacy and Pharmacokinetics of Antivenom Viperfav ® in Vipera ammodytes ammodytes Envenomation
Clinical Efficacy and Pharmacokinetics of Antivenom Viperfav ® in Vipera ammodytes ammodytes Envenomation Abstract Background: In Europe, Vipera ammodytes ammodytes ( Vaa , nose-horned viper) is considered the most venomous of the European vipers. The antivenom Viperfav ® , composed of polyvalent equine F(ab′) 2 fragme...
PMC5066754
core_pubmed_pmc
Guaifenesin Pharmacokinetics Following Single‐Dose Oral Administration in Children Aged 2 to 17 Years
Guaifenesin Pharmacokinetics Following Single‐Dose Oral Administration in Children Aged 2 to 17 Years Abstract Abstract This study characterized guaifenesin pharmacokinetics in children aged 2 to 17 years (n = 40) who received a single oral dose of guaifenesin (age‐based doses of 100‐400 mg) 2 hours after breakfast. Pl...
PMC7389645
core_pubmed_pmc
Pharmacokinetic interactions of esaxerenone with amlodipine and digoxin in healthy Japanese subjects
Pharmacokinetic interactions of esaxerenone with amlodipine and digoxin in healthy Japanese subjects Abstract Abstract Background To investigate the effects of coadministration of esaxerenone with amlodipine on the pharmacokinetics (PK) of each drug, and of esaxerenone on the PK of digoxin. Methods In three open-label,...
PMC3717066
core_pubmed_pmc
Integrated pharmacokinetics/pharmacodynamics parameters-based dosing guidelines of enrofloxacin in grass carp Ctenopharyngodon idella to minimize selection of drug resistance
Integrated pharmacokinetics/pharmacodynamics parameters-based dosing guidelines of enrofloxacin in grass carp Ctenopharyngodon idella to minimize selection of drug resistance Abstract Abstract Background Antibiotic resistance has become a serious global problem and is steadily increasing worldwide in almost every bacte...
PMC8672215
core_pubmed_pmc
Impact of pharmacokinetics to reduce bleeding in a cohort of patients with severe hemophilia A in a personalized comprehensive management program
Impact of pharmacokinetics to reduce bleeding in a cohort of patients with severe hemophilia A in a personalized comprehensive management program Abstract In recent decades, hemophilia A treatment has been focused on body weight, without taking pharmacokinetic parameters into account. Previous research has shown that t...
PMC10460054
core_pubmed_pmc
Multiplex Quantitative Analysis of 9 Compounds of Scutellaria baicalensis Georgi in the Plasma of Respiratory Syncytial Virus-Infected Mice Based on HPLC-MS/MS and Pharmacodynamic Effect Correlation Analysis
Multiplex Quantitative Analysis of 9 Compounds of Scutellaria baicalensis Georgi in the Plasma of Respiratory Syncytial Virus-Infected Mice Based on HPLC-MS/MS and Pharmacodynamic Effect Correlation Analysis Abstract According to traditional Chinese medicine, Scutellaria baicalensis Georgi possesses the therapeutic pro...
PMC5324684
core_pubmed_pmc
First‐in‐human assessment of PRX002, an anti–α‐synuclein monoclonal antibody, in healthy volunteers
First‐in‐human assessment of PRX002, an anti–α‐synuclein monoclonal antibody, in healthy volunteers Abstract ABSTRACT Background : α‐Synuclein is a major component of pathologic inclusions that characterize Parkinson's disease. PRX002 is an antibody that targets α‐synuclein, and its murine parent antibody 9E4 has been ...
PMC3687097
core_pubmed_pmc
Impact of Voglibose on the Pharmacokinetics of Dapagliflozin in Japanese Patients with Type 2 Diabetes
Impact of Voglibose on the Pharmacokinetics of Dapagliflozin in Japanese Patients with Type 2 Diabetes Abstract Abstract Introduction Dapagliflozin is an orally administered selective sodium-glucose cotransporter 2 (SGLT2) inhibitor under development for the treatment of type 2 diabetes mellitus (T2DM). Dapagliflozin l...
PMC5278730
core_pubmed_pmc
Estimation of the In Vivo MIC of Cipargamin in Uncomplicated Plasmodium falciparum Malaria
Estimation of the In Vivo MIC of Cipargamin in Uncomplicated Plasmodium falciparum Malaria Abstract ABSTRACT The MIC of an antimalarial drug for a particular infection is the drug level associated with a net parasite multiplication rate of one per asexual cycle. To ensure the cure of malaria, the MIC must be exceeded u...
PMC8287028
core_pubmed_pmc
Pharmacokinetics and Biologic Activity of Apixaban in Healthy Dogs
Pharmacokinetics and Biologic Activity of Apixaban in Healthy Dogs Abstract Abstract Thrombosis is common in critically ill dogs and causes considerable morbidity and mortality. The direct factor Xa inhibitor apixaban is safe, efficacious, and convenient in humans. This study aimed to determine the pharmacokinetics (PK...
PMC11749210
core_pubmed_pmc
Interaction studies unveil potential binding sites on bovine serum albumin for gut metabolite trimethylamine n-oxide (TMAO)
Interaction studies unveil potential binding sites on bovine serum albumin for gut metabolite trimethylamine n-oxide (TMAO) Abstract Abstract Trimethylamine-N-oxide (TMAO) is gut microbiota-derived metabolite, plays a critical role in human health and diseases such as metabolic, cardiovascular, colorectal cancer and, n...
PMC4945769
core_pubmed_pmc
Neutrophil maturation rate determines the effects of dipeptidyl peptidase 1 inhibition on neutrophil serine protease activity
Neutrophil maturation rate determines the effects of dipeptidyl peptidase 1 inhibition on neutrophil serine protease activity Abstract Background and Purpose Neutrophil serine proteases (NSPs) are activated by dipeptidyl peptidase 1 (DPP1) during neutrophil maturation. The effects of neutrophil turnover rate on NSP act...
PMC8585847
core_pubmed_pmc
Population Pharmacokinetics and Pharmacodynamics of Vericiguat in Patients with Heart Failure and Reduced Ejection Fraction
Population Pharmacokinetics and Pharmacodynamics of Vericiguat in Patients with Heart Failure and Reduced Ejection Fraction Abstract Abstract Background Vericiguat, a stimulator of soluble guanylate cyclase, has been developed as a first-in-class therapy for worsening chronic heart failure in adults with left ventricul...
PMC7248705
core_pubmed_pmc
A Pharmacokinetic and Pharmacodynamic Evaluation of the Anti-Hepatocellular Carcinoma Compound 4- N -Carbobenzoxy-gemcitabine (Cbz-dFdC)
A Pharmacokinetic and Pharmacodynamic Evaluation of the Anti-Hepatocellular Carcinoma Compound 4- N -Carbobenzoxy-gemcitabine (Cbz-dFdC) Abstract Abstract Gemcitabine (dFdC) demonstrates significant effectiveness against solid tumors in vitro and in vivo; however, its clinical application is limited because it tends to...