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PMC11181725
core_pubmed_pmc
Safety and Pharmacokinetics of Intravesical Chitosan/Interleukin-12 Immunotherapy in Murine Bladders
Safety and Pharmacokinetics of Intravesical Chitosan/Interleukin-12 Immunotherapy in Murine Bladders Abstract Abstract BACKGROUND: Intravesical administration of interleukin 12 (IL-12) co-formulated with the biopolymer, chitosan (CS/IL-12), has demonstrated remarkable antitumor activity against preclinical models of bl...
PMC12263804
core_pubmed_pmc
Rifampicin Exposure in Tuberculosis Patients with Comorbidities in Sub-Saharan Africa: Prioritising Populations for Treatment—A Systematic Review and Meta-analysis
Rifampicin Exposure in Tuberculosis Patients with Comorbidities in Sub-Saharan Africa: Prioritising Populations for Treatment—A Systematic Review and Meta-analysis Abstract Abstract Background and Objectives Emerging evidence suggests that comorbidities like human immunodeficiency virus (HIV) infection, diabetes mellit...
PMC5794840
core_pubmed_pmc
Effects of Metformin and Furosemide on Rosuvastatin Pharmacokinetics in Healthy Volunteers: Implications for Their Use as Probe Drugs in a Transporter Cocktail
Effects of Metformin and Furosemide on Rosuvastatin Pharmacokinetics in Healthy Volunteers: Implications for Their Use as Probe Drugs in a Transporter Cocktail Abstract Abstract Background In a recently described probe drug cocktail for clinically relevant drug transporters containing digoxin, furosemide, metformin and...
PMC7919190
core_pubmed_pmc
Population Pharmacokinetics of Phosphocreatine and Its Metabolite Creatine in Children With Myocarditis
Population Pharmacokinetics of Phosphocreatine and Its Metabolite Creatine in Children With Myocarditis Abstract Objective: This study aimed to develop a parent-metabolite joint population pharmacokinetic model to characterize the pharmacokinetic (PK) profile for phosphocreatine (PCr) and its metabolite creatine (Cr) i...
PMC11641171
core_pubmed_pmc
In Silico Hydrolysis of Lupin ( Lupinus angustifolius L.) Conglutins with Plant Proteases Releases Antihypertensive and Antidiabetic Peptides That Are Bioavailable, Non-Toxic, and Gastrointestinal Digestion Stable
In Silico Hydrolysis of Lupin ( Lupinus angustifolius L.) Conglutins with Plant Proteases Releases Antihypertensive and Antidiabetic Peptides That Are Bioavailable, Non-Toxic, and Gastrointestinal Digestion Stable Abstract Abstract Lupin ( Lupinus angustifolius L.) proteins are potential sources of bioactive peptides (...
PMC12163317
core_pubmed_pmc
The food effect on the pharmacokinetics of TQB3616 capsule in Chinse healthy subjects: a randomized, open-label, single-center, two-period, two-sequence crossover phase I clinical trial
The food effect on the pharmacokinetics of TQB3616 capsule in Chinse healthy subjects: a randomized, open-label, single-center, two-period, two-sequence crossover phase I clinical trial Abstract Purpose The purpose of this study was to evaluate the food effect on the pharmacokinetics of TQB3616 capsule in Chinse health...
PMC6105922
core_pubmed_pmc
Verinurad combined with febuxostat in Japanese adults with gout or asymptomatic hyperuricaemia: a phase 2a, open-label study
Verinurad combined with febuxostat in Japanese adults with gout or asymptomatic hyperuricaemia: a phase 2a, open-label study Abstract Abstract Objectives Verinurad (RDEA3170) is a high-affinity inhibitor of the URAT1 transporter in clinical development for treating gout and asymptomatic hyperuricaemia. The aim of this ...
PMC6968529
core_pubmed_pmc
Effects of Fuzheng Huayu recipe on entecavir pharmacokinetics in normal and dimethylnitrosamine-induced hepatic fibrosis rats
Effects of Fuzheng Huayu recipe on entecavir pharmacokinetics in normal and dimethylnitrosamine-induced hepatic fibrosis rats Abstract Abstract Context Fuzheng Huayu recipe (FZHY) combined with entecavir (ETV) is used to treat the cirrhosis caused by chronic hepatitis B (CHB) infection. Objective To investigate the eff...
PMC9854584
core_pubmed_pmc
Synergistic Activity of Pep16, a Promising New Antibacterial Pseudopeptide against Multidrug-Resistant Organisms, in Combination with Colistin against Multidrug-Resistant Escherichia coli , In Vitro and in a Murine Peritonitis Model
Synergistic Activity of Pep16, a Promising New Antibacterial Pseudopeptide against Multidrug-Resistant Organisms, in Combination with Colistin against Multidrug-Resistant Escherichia coli , In Vitro and in a Murine Peritonitis Model Abstract Abstract Colistin is a drug of last resort to treat extreme drug-resistant Ent...
PMC3689905
core_pubmed_pmc
Bioequivalence of Eslicarbazepine Acetate from Two Different Sources of its Active Product Ingredient in Healthy Subjects
Bioequivalence of Eslicarbazepine Acetate from Two Different Sources of its Active Product Ingredient in Healthy Subjects Abstract Purpose To compare the bioavailability (BA) and pharmacokinetic (PK) properties and to demonstrate the bioequivalence (BE) between two active product ingredient (API) sources of eslicarbaze...
PMC12946599
core_pubmed_pmc
A Phase 1, Randomized, Placebo‐Controlled, Multiple‐Dose, Double‐Blind Study to Evaluate and Compare the Pharmacokinetics and Safety of Rimegepant in Healthy Adult Japanese and Caucasian Individuals
A Phase 1, Randomized, Placebo‐Controlled, Multiple‐Dose, Double‐Blind Study to Evaluate and Compare the Pharmacokinetics and Safety of Rimegepant in Healthy Adult Japanese and Caucasian Individuals Abstract Abstract This Phase 1, randomized, placebo‐controlled, double‐blind study assessed the pharmacokinetic profile o...
PMC9710098
core_pubmed_pmc
The PBPK LeiCNS-PK3.0 framework predicts Nirmatrelvir (but not Remdesivir or Molnupiravir) to achieve effective concentrations against SARS-CoV-2 in human brain cells
The PBPK LeiCNS-PK3.0 framework predicts Nirmatrelvir (but not Remdesivir or Molnupiravir) to achieve effective concentrations against SARS-CoV-2 in human brain cells Abstract SARS-CoV-2 was shown to infect and persist in the human brain cells for up to 230 days, highlighting the need to treat the brain viral load. The...
PMC9540501
core_pubmed_pmc
Population Pharmacokinetic Models for Direct Oral Anticoagulants: A Systematic Review and Clinical Appraisal Using Exposure Simulation
Population Pharmacokinetic Models for Direct Oral Anticoagulants: A Systematic Review and Clinical Appraisal Using Exposure Simulation Abstract Available data have shown an association between direct oral anticoagulant (DOAC) plasma concentration and clinical, particularly bleeding, events. Factors that may influence D...
PMC10564307
core_pubmed_pmc
First-in-Human, Phase I Dose-Escalation and Dose-Expansion Study of Trophoblast Cell-Surface Antigen 2–Directed Antibody-Drug Conjugate Datopotamab Deruxtecan in Non–Small-Cell Lung Cancer: TROPION-PanTumor01
First-in-Human, Phase I Dose-Escalation and Dose-Expansion Study of Trophoblast Cell-Surface Antigen 2–Directed Antibody-Drug Conjugate Datopotamab Deruxtecan in Non–Small-Cell Lung Cancer: TROPION-PanTumor01 Abstract Abstract PURPOSE This first-in-human, dose-escalation and dose-expansion study evaluated the safety, t...
PMC8606554
core_pubmed_pmc
Quantitative Analysis of the Efficacy of PARP Inhibitors as Maintenance Therapy in Recurrent Ovarian Cancer
Quantitative Analysis of the Efficacy of PARP Inhibitors as Maintenance Therapy in Recurrent Ovarian Cancer Abstract Objective: This study aimed to establish a pharmacodynamic model and to screen reasonable covariates to quantitatively describe the efficacy of poly (ADP-ribose) polymerase inhibitors (PARPis) as mainten...
PMC4898026
core_pubmed_pmc
Isavuconazole in the treatment of invasive aspergillosis and mucormycosis infections
Isavuconazole in the treatment of invasive aspergillosis and mucormycosis infections Abstract We have a limited arsenal with which to treat invasive fungal infections caused by Aspergillus and Mucorales. The morbidity and mortality for both pathogens remains high. A triazole antifungal, isavuconazole, was recently gran...
PMC8953076
core_pubmed_pmc
Prodrug Therapies for Infectious and Neurodegenerative Diseases
Prodrug Therapies for Infectious and Neurodegenerative Diseases Abstract Prodrugs are bioreversible drug derivatives which are metabolized into a pharmacologically active drug following chemical or enzymatic modification. This approach is designed to overcome several obstacles that are faced by the parent drug in physi...
PMC8019741
core_pubmed_pmc
Efficacy Prediction of Four Pharmaceutical Formulations for Intramammary Administration Containing Aloe vera (L.) Burm. f. Combined With Ceftiofur or Cloxacillin in Lactating Cows as an Alternative Therapy to Treat Mastitis Caused by Staphylococcus aureus
Efficacy Prediction of Four Pharmaceutical Formulations for Intramammary Administration Containing Aloe vera (L.) Burm. f. Combined With Ceftiofur or Cloxacillin in Lactating Cows as an Alternative Therapy to Treat Mastitis Caused by Staphylococcus aureus Abstract Synergy or additive effect between Aloe vera (L.) Burm....
PMC3734837
core_pubmed_pmc
A combination of cilostazol and Ginkgo biloba extract protects against cisplatin-induced Cochleo-vestibular dysfunction by inhibiting the mitochondrial apoptotic and ERK pathways
A combination of cilostazol and Ginkgo biloba extract protects against cisplatin-induced Cochleo-vestibular dysfunction by inhibiting the mitochondrial apoptotic and ERK pathways Abstract Cisplatin ( cis -diammine-dichloroplatinum; CDDP) is an anticancer drug that induces significant hearing loss and balance dysfunctio...
PMC4716580
core_pubmed_pmc
Agent‐Based Modeling in Systems Pharmacology
Agent‐Based Modeling in Systems Pharmacology Abstract Modeling and simulation (M&S) techniques provide a platform for knowledge integration and hypothesis testing to gain insights into biological systems that would not be possible a priori . Agent‐based modeling (ABM) is an M&S technique that focuses on describing indi...
PMC11315871
core_pubmed_pmc
Evaluation of Ornidazole Tablets Bioequivalence in Chinese Healthy Participants Under Fasted and Fed Conditions Using Pharmacokinetic Parameters
Evaluation of Ornidazole Tablets Bioequivalence in Chinese Healthy Participants Under Fasted and Fed Conditions Using Pharmacokinetic Parameters Abstract Background and Objective Ornidazole, the third generation of nitroimidazole derivatives after metronidazole and tinidazole, it exerts both bactericidal and antiprotoz...
PMC8074352
core_pubmed_pmc
Clinical Impact of Revised Ciprofloxacin Breakpoint in Patients with Urinary Tract Infections by Enterobacteriaceae
Clinical Impact of Revised Ciprofloxacin Breakpoint in Patients with Urinary Tract Infections by Enterobacteriaceae Abstract Abstract In 2018, the Clinical and Laboratory Standards Institute (CLSI) revised ciprofloxacin (CIP)-susceptible breakpoint for Enterobacteriaceae from ≤1 μg/mL to ≤0.25 μg/mL, based on pharmacok...
PMC3231982
core_pubmed_pmc
Immunogenicity of panitumumab in combination chemotherapy clinical trials
Immunogenicity of panitumumab in combination chemotherapy clinical trials Abstract Abstract Background Panitumumab is a fully human antibody against the epidermal growth factor receptor that is indicated for the treatment of metastatic colorectal cancer (mCRC) after disease progression on standard chemotherapy. The pur...
PMC6759287
core_pubmed_pmc
Effect Of Chinese Herb Danzhi Xiaoyao Pills On Pharmacokinetics Of Venlafaxine In Beagles
Effect Of Chinese Herb Danzhi Xiaoyao Pills On Pharmacokinetics Of Venlafaxine In Beagles Abstract Abstract Objective To investigate the effects of Chinese herb Danzhi Xiaoyao pills on the pharmacokinetics of venlafaxine and its metabolites O-desmethylvenlafaxine (ODV) and N-desmethylvenlafaxine (NDV) in beagles by usi...
PMC6757420
core_pubmed_pmc
Identifying the active components of Baihe–Zhimu decoction that ameliorate depressive disease by an effective integrated strategy: a systemic pharmacokinetics study combined with classical depression model tests
Identifying the active components of Baihe–Zhimu decoction that ameliorate depressive disease by an effective integrated strategy: a systemic pharmacokinetics study combined with classical depression model tests Abstract Abstract Background Modern pharmacological studies have demonstrated that Baihe–Zhimu decoction (BZ...
PMC7038301
core_pubmed_pmc
A Subcutaneous Implant of Tenofovir Alafenamide Fumarate Causes Local Inflammation and Tissue Necrosis in Rabbits and Macaques
A Subcutaneous Implant of Tenofovir Alafenamide Fumarate Causes Local Inflammation and Tissue Necrosis in Rabbits and Macaques Abstract We describe the in vitro and in vivo evaluation of a subcutaneous reservoir implant delivering tenofovir alafenamide hemifumarate (TAF) for the prevention of HIV infection. These long-...
PMC10657194
core_pubmed_pmc
An Integrative Approach to Study the Inhibition of Providencia vermicola FabD Using C2-Quaternary Indolinones
An Integrative Approach to Study the Inhibition of Providencia vermicola FabD Using C2-Quaternary Indolinones Abstract Background The present study investigates the potential bioactivity of twelve experimentally designed C-2 quaternary indolinones against Providencia spp., a bacterial group of the Enterobacteriaceae fa...
PMC6685729
core_pubmed_pmc
User-Centered Development of an Online Platform for Drug Dosing Recommendations in Pediatrics
User-Centered Development of an Online Platform for Drug Dosing Recommendations in Pediatrics Abstract Abstract Background Drug therapy in pediatric patients is a complex process. Children are subject to continuous growth and variation in drug-metabolizing enzyme activity, requiring continuous adaption of dosages. In G...
PMC11389886
core_pubmed_pmc
Developing Parametric and Nonparametric Models for Model-Informed Precision Dosing: A Quality Improvement Effort in Vancomycin for Patients With Obesity
Developing Parametric and Nonparametric Models for Model-Informed Precision Dosing: A Quality Improvement Effort in Vancomycin for Patients With Obesity Abstract Supplemental Digital Content is Available in the Text. Background: Both parametric and nonparametric methods have been proposed to support model-informed prec...
PMC4079632
core_pubmed_pmc
Asunaprevir, a protease inhibitor for the treatment of hepatitis C infection
Asunaprevir, a protease inhibitor for the treatment of hepatitis C infection Abstract Abstract According to the World Health Organization, approximately 150 million people worldwide are chronic carriers of hepatitis C virus (HCV). HCV infection can evolve into cirrhosis of the liver and its complications, which are ult...
PMC8839099
core_pubmed_pmc
Enhancing Ocular Bioavailability of Ciprofloxacin Using Colloidal Lipid-Based Carrier for the Management of Post-Surgical Infection
Enhancing Ocular Bioavailability of Ciprofloxacin Using Colloidal Lipid-Based Carrier for the Management of Post-Surgical Infection Abstract Conjunctivitis and endogenous bacterial endophthalmitis mostly occurred after ophthalmic surgery. Therefore, the present study aimed to maximize the ocular delivery of ciprofloxac...
PMC8892746
core_pubmed_pmc
Exposure–response analyses of cabozantinib in patients with metastatic renal cell cancer
Exposure–response analyses of cabozantinib in patients with metastatic renal cell cancer Abstract Abstract Aim In the registration trial, cabozantinib exposure ≥ 750 ng/mL correlated to improved tumor size reduction, response rate and progression free survival (PFS) in patients with metastatic renal cell cancer (mRCC)....
PMC11047404
core_pubmed_pmc
Comparative Efficacy of Continuous Ceftazidime Infusion vs. Intermittent Bolus against In Vitro Ceftazidime-Susceptible and -Resistant Pseudomonas aeruginosa Biofilm
Comparative Efficacy of Continuous Ceftazidime Infusion vs. Intermittent Bolus against In Vitro Ceftazidime-Susceptible and -Resistant Pseudomonas aeruginosa Biofilm Abstract Background : As the anti-biofilm pharmacokinetic/pharmacodynamic (PK/PD) properties of antibiotics are not well-defined, we have evaluated the PK...
PMC5034805
core_pubmed_pmc
Evaluation of CYP3A‐mediated drug–drug interactions with romidepsin in patients with advanced cancer
Evaluation of CYP3A‐mediated drug–drug interactions with romidepsin in patients with advanced cancer Abstract Abstract Two multicenter, single‐arm, single‐infusion, open‐label studies were conducted to evaluate the effect of ketoconazole (a strong CYP3A inhibitor) or rifampin (a strong CYP3A inducer) daily for 5 days o...
PMC9585207
core_pubmed_pmc
SeDeM tool-driven full factorial design for osmotic drug delivery of tramadol HCl: Formulation development, physicochemical evaluation, and in-silico PBPK modeling for predictive pharmacokinetic evaluation using GastroPlus™
SeDeM tool-driven full factorial design for osmotic drug delivery of tramadol HCl: Formulation development, physicochemical evaluation, and in-silico PBPK modeling for predictive pharmacokinetic evaluation using GastroPlus™ Abstract The study is based on using SeDeM expert system in developing controlled-release tramad...
PMC10925492
core_pubmed_pmc
Effects of Aripiprazole on Olanzapine Population Pharmacokinetics and Initial Dosage Optimization in Schizophrenia Patients
Effects of Aripiprazole on Olanzapine Population Pharmacokinetics and Initial Dosage Optimization in Schizophrenia Patients Abstract Objective Olanzapine has already been used to treat schizophrenia patients; however, the initial dosage recommendation when multiple drugs are used in combination, remains unclear. The pu...
PMC9609097
core_pubmed_pmc
Pharmacometric Modeling of the Impact of Azelastine Nasal Spray on SARS-CoV-2 Viral Load and Related Symptoms in COVID-19 Patients
Pharmacometric Modeling of the Impact of Azelastine Nasal Spray on SARS-CoV-2 Viral Load and Related Symptoms in COVID-19 Patients Abstract Abstract The histamine-1 receptor antagonist azelastine was recently found to impact SARS-CoV-2 viral kinetics in a Phase 2 clinical trial (CARVIN). Thus, we investigated the relat...
PMC10725261
core_pubmed_pmc
Tutorial on model selection and validation of model input into precision dosing software for model‐informed precision dosing
Tutorial on model selection and validation of model input into precision dosing software for model‐informed precision dosing Abstract Abstract There has been rising interest in using model‐informed precision dosing to provide personalized medicine to patients at the bedside. This methodology utilizes population pharmac...
PMC5701813
core_pubmed_pmc
PK-PD Analysis of Marbofloxacin against Streptococcus suis in Pigs
PK-PD Analysis of Marbofloxacin against Streptococcus suis in Pigs Abstract Marbofloxacin is a fluoroquinolone antibiotic and highly effective treatment for respiratory diseases. Here we aimed to evaluate the ex vivo activity of marbofloxacin against Streptococcus suis in pig serum, as well as the optimal dosages schem...
PMC8248190
core_pubmed_pmc
Pharmacokinetics of meropenem in children with sepsis undergoing extracorporeal life support: A prospective observational study
Pharmacokinetics of meropenem in children with sepsis undergoing extracorporeal life support: A prospective observational study Abstract Summary What is known and Objective Meropenem, a broad‐spectrum carbapenem, is frequently used to treat severe bacterial infections in critically ill children. Recommendations for mer...
PMC11615922
core_pubmed_pmc
Quantitative pharmacodynamics functional evaluation of Chinese medicine Qizhu formula in mice with dynamic near-infrared photoacoustic imaging
Quantitative pharmacodynamics functional evaluation of Chinese medicine Qizhu formula in mice with dynamic near-infrared photoacoustic imaging Abstract Background & Aims Effective anti-fibrotic drugs and new non-invasive evaluation methods for liver fibrosis (LF) are urgently needed. Our study aimed to evaluate the his...
PMC4128785
core_pubmed_pmc
44 Sc: An Attractive Isotope for Peptide-Based PET Imaging
44 Sc: An Attractive Isotope for Peptide-Based PET Imaging Abstract The overexpression of integrin α v β 3 has been linked to tumor aggressiveness and metastasis in several cancer types. Because of its high affinity, peptides containing the arginine–glycine–aspartic acid (RGD) motif have been proven valuable vectors fo...
PMC12506027
core_pubmed_pmc
AntiviralDB: an expert-curated database of antiviral agents against human infectious diseases
AntiviralDB: an expert-curated database of antiviral agents against human infectious diseases Abstract ABSTRACT Viral infectious diseases have caused millions of deaths worldwide. Antiviral agents are critical for controlling these infections; however, an open-access database dedicated specifically to antiviral agents ...
PMC8016788
core_pubmed_pmc
Evaluation of the Pharmacokinetics and Exposure–Response Relationship of Dapagliflozin in Patients without Diabetes and with Chronic Kidney Disease
Evaluation of the Pharmacokinetics and Exposure–Response Relationship of Dapagliflozin in Patients without Diabetes and with Chronic Kidney Disease Abstract Abstract Background and Objective Dapagliflozin, a sodium-glucose co-transporter inhibitor, was originally developed as an oral glucose-lowering drug for the treat...
PMC12947315
core_pubmed_pmc
Evaluation of Drug–Drug Interaction Potential Between the Oral Antibiotic Zoliflodacin and the CYP3A4 Inhibitor Itraconazole: A Phase 1 Study in Healthy Participants
Evaluation of Drug–Drug Interaction Potential Between the Oral Antibiotic Zoliflodacin and the CYP3A4 Inhibitor Itraconazole: A Phase 1 Study in Healthy Participants Abstract ABSTRACT Zoliflodacin is a first‐in‐class oral spiropyrimidinetrione antibiotic being developed for patients with uncomplicated gonorrhea, includ...
PMC4955259
core_pubmed_pmc
Abediterol, a novel long-acting β 2 -agonist: bronchodilation, safety, tolerability and pharmacokinetic results from a single-dose, dose-ranging, active-comparator study in patients with COPD
Abediterol, a novel long-acting β 2 -agonist: bronchodilation, safety, tolerability and pharmacokinetic results from a single-dose, dose-ranging, active-comparator study in patients with COPD Abstract Background Abediterol is a novel, once-daily long-acting β 2 -agonist in development for the treatment of chronic obstr...
PMC12947316
core_pubmed_pmc
Population PK – PD Modeling of Danicopan Add‐On Therapy in Participants With Paroxysmal Nocturnal Hemoglobinuria Treated With Ravulizumab or Eculizumab
Population PK – PD Modeling of Danicopan Add‐On Therapy in Participants With Paroxysmal Nocturnal Hemoglobinuria Treated With Ravulizumab or Eculizumab Abstract ABSTRACT Danicopan is a first‐in‐class orally administered complement factor D inhibitor, approved as an add‐on therapy to ravulizumab or eculizumab for the tr...
PMC11023281
core_pubmed_pmc
Pharmacokinetic profile of oral and subcutaneous administration of paracetamol in the koala ( Phascolarctos cinereus ) and prediction of its analgesic efficacy
Pharmacokinetic profile of oral and subcutaneous administration of paracetamol in the koala ( Phascolarctos cinereus ) and prediction of its analgesic efficacy Abstract Abstract The pharmacokinetic profile of paracetamol in koalas is described when administered orally at 15 mg/kg; followed by the same dose, administere...
PMC8708464
core_pubmed_pmc
Development of a Model-Informed Dosing Tool to Optimise Initial Antibiotic Dosing—A Translational Example for Intensive Care Units
Development of a Model-Informed Dosing Tool to Optimise Initial Antibiotic Dosing—A Translational Example for Intensive Care Units Abstract The prevalence and mortality rates of severe infections are high in intensive care units (ICUs). At the same time, the high pharmacokinetic variability observed in ICU patients inc...
PMC4790317
core_pubmed_pmc
Utilizing Monte Carlo Simulations to Optimize Institutional Empiric Antipseudomonal Therapy
Utilizing Monte Carlo Simulations to Optimize Institutional Empiric Antipseudomonal Therapy Abstract Abstract Pseudomonas aeruginosa is a common pathogen implicated in nosocomial infections with increasing resistance to a limited arsenal of antibiotics. Monte Carlo simulation provides antimicrobial stewardship teams wi...
PMC4515243
core_pubmed_pmc
Phase 1 pharmacokinetic study of the oral pan-AKT inhibitor MK-2206 in Japanese patients with advanced solid tumors
Phase 1 pharmacokinetic study of the oral pan-AKT inhibitor MK-2206 in Japanese patients with advanced solid tumors Abstract Abstract Purpose MK-2206 is an oral, highly selective inhibitor of AKT. The safety, tolerability, pharmacokinetics (PK), and anti-tumor activity of MK-2206 was evaluated in Japanese patients with...
PMC5412584
core_pubmed_pmc
Exposure-Response Relationships during Free-Access Intravenous Alcohol Self-Administration in Nondependent Drinkers: Influence of Alcohol Expectancies and Impulsivity
Exposure-Response Relationships during Free-Access Intravenous Alcohol Self-Administration in Nondependent Drinkers: Influence of Alcohol Expectancies and Impulsivity Abstract Abstract Background: Self-administration is a hallmark of all addictive drugs, including alcohol. Human laboratory models of alcohol self-admini...
PMC3439798
core_pubmed_pmc
Pharmacokinetics of drospirenone and ethinylestradiol in Caucasian and Japanese women
Pharmacokinetics of drospirenone and ethinylestradiol in Caucasian and Japanese women Abstract Objective To investigate the pharmacokinetics of drospirenone (DRSP) and ethinylestradiol (EE) in Caucasian and Japanese women. Method Three open-label, non-randomised studies were performed to assess the pharmacokinetics fol...
PMC4762905
core_pubmed_pmc
Polymorphisms in the ABCB1 gene and effect on outcome and toxicity in childhood acute lymphoblastic leukemia
Polymorphisms in the ABCB1 gene and effect on outcome and toxicity in childhood acute lymphoblastic leukemia Abstract Abstract The membrane transporter P-glycoprotein, encoded by the ABCB1 gene, influences the pharmacokinetics of anti-cancer drugs. We hypothesized that variants of ABCB1 affect outcome and toxicity in c...
PMC12299168
core_pubmed_pmc
Preparation and Evaluation of Long-Acting Injectable Levocetirizine Prodrug Formulation
Preparation and Evaluation of Long-Acting Injectable Levocetirizine Prodrug Formulation Abstract Background/Objectives : Levocetirizine (LCZ) is a second-generation antihistamine with minimal central nervous system effects. However, its short half-life necessitates daily dosing, potentially reducing adherence in pediat...
PMC5387714
core_pubmed_pmc
Glycoengineering of pertuzumab and its impact on the pharmacokinetic/pharmacodynamic properties
Glycoengineering of pertuzumab and its impact on the pharmacokinetic/pharmacodynamic properties Abstract Abstract Pertuzumab is an antihuman HER2 antibody developed for HER2 positive breast cancer. Glycosylation profiles are always the important issue for antibody based therapy. Previous findings have suggested the imp...
PMC5009327
core_pubmed_pmc
Noninvasive mapping of the redox status of dimethylnitrosamine-induced hepatic fibrosis using in vivo dynamic nuclear polarization-magnetic resonance imaging
Noninvasive mapping of the redox status of dimethylnitrosamine-induced hepatic fibrosis using in vivo dynamic nuclear polarization-magnetic resonance imaging Abstract Abstract Hepatic fibrosis is a chronic disorder caused by viral infection and/or metabolic, genetic and cholestatic disorders. A noninvasive procedure th...
PMC12185614
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Modelling and Monte Carlo Simulations to Predict Cytomegalovirus Viral Load in Pediatric Transplant Recipients Treated with (val)Ganciclovir
Pharmacokinetic/Pharmacodynamic Modelling and Monte Carlo Simulations to Predict Cytomegalovirus Viral Load in Pediatric Transplant Recipients Treated with (val)Ganciclovir Abstract Abstract Background and Objectives Cytomegalovirus (CMV) infection poses significant challenges in pediatric transplant recipients. Gancic...
PMC8604827
core_pubmed_pmc
Development of PBPK model for intra-articular injection in human: methotrexate solution and rheumatoid arthritis case study
Development of PBPK model for intra-articular injection in human: methotrexate solution and rheumatoid arthritis case study Abstract Abstract A physiologically based model describing the dissolution, diffusion, and transfer of drug from the intra-articular (IA) space to the plasma, was developed for GastroPlus® v9.8. T...
PMC6610295
core_pubmed_pmc
First evaluation of tapentadol oral solution for the treatment of moderate to severe acute pain in children aged 6 to <18
First evaluation of tapentadol oral solution for the treatment of moderate to severe acute pain in children aged 6 to <18 Abstract Abstract Background This is the first clinical trial in the global pediatric clinical development program for the use of the analgesic tapentadol in children and adolescents. Patients and m...
PMC9146797
core_pubmed_pmc
[ 99m Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging
[ 99m Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging Abstract Abstract Certain receptors are often overexpressed during tumor occurrence and development and closely correlate with carcinogenesis. Owing to its overexpression on the cell membrane and cytoplasm of various tumors, plectin,...
PMC7857992
core_pubmed_pmc
Combined docking methods and molecular dynamics to identify effective antiviral 2, 5-diaminobenzophenonederivatives against SARS-CoV-2
Combined docking methods and molecular dynamics to identify effective antiviral 2, 5-diaminobenzophenonederivatives against SARS-CoV-2 Abstract Abstract The aim of this work is to contribute to the research in finding lead compounds for clinical use, to identify new drugs that target the SARS-CoV-2 virus main protease ...
PMC9791580
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Editorial: Model-informed drug development and evidence-based translational pharmacology
Editorial: Model-informed drug development and evidence-based translational pharmacology Modeling 2 Application of model-informed drug development (MIDD) There is a long-standing history of applying MIDD to inform regulatory decisions at the FDA ( Madabushi et al., 2022 ). In the early 90s, the utilities of MIDD were l...
PMC11247122
core_pubmed_pmc
Population pharmacokinetics of imetelstat, a first‐in‐class oligonucleotide telomerase inhibitor
Population pharmacokinetics of imetelstat, a first‐in‐class oligonucleotide telomerase inhibitor Abstract Abstract Imetelstat is a novel, first‐in‐class, oligonucleotide telomerase inhibitor in development for the treatment of hematologic malignancies including lower‐risk myelodysplastic syndromes and myelofibrosis. A ...
PMC8416343
core_pubmed_pmc
A Facile Procedure for One-Pot Stable Conjugation of Two Proglucagon Cysteine-Containing Peptide Analogs
A Facile Procedure for One-Pot Stable Conjugation of Two Proglucagon Cysteine-Containing Peptide Analogs Abstract Abstract Optimization of peptides for therapeutic purposes often includes chemical conjugation or modification with substituents that serve to broaden pharmacology or improve pharmacokinetics. We report a c...
PMC9353711
core_pubmed_pmc
A Novel Berberine–Glycyrrhizic Acid Complex Formulation Enhanced the Prevention Effect to Doxorubicin-Induced Cardiotoxicity by Pharmacokinetic Modulation of Berberine in Rats
A Novel Berberine–Glycyrrhizic Acid Complex Formulation Enhanced the Prevention Effect to Doxorubicin-Induced Cardiotoxicity by Pharmacokinetic Modulation of Berberine in Rats Abstract Developing a new drug delivery system is one of the useful approaches to overcome the limited use of berberine (BBR) to enhance its abs...
PMC11074474
core_pubmed_pmc
Nivolumab plus ONC201 plus in microsatellite stable (MSS) metastatic colorectal cancer (mCRC) patients: a Brown University Oncology Research Group phase Ib/II study (BrUOG379)
Nivolumab plus ONC201 plus in microsatellite stable (MSS) metastatic colorectal cancer (mCRC) patients: a Brown University Oncology Research Group phase Ib/II study (BrUOG379) Abstract Abstract Background Immune checkpoint inhibitors alone, or in combination with chemotherapy failed to provide meaningful clinical activ...
PMC5011461
core_pubmed_pmc
Pharmacokinetics of oseltamivir in infants under the age of 1 year
Pharmacokinetics of oseltamivir in infants under the age of 1 year Abstract Background Oseltamivir is the only antiviral treatment recommended for influenza in young children over the age of 1 year. There is scant data on oseltamivir pharmacokinetics (PK) in infants <1 year. We set out to perform PK measurements in inf...
PMC7285563
core_pubmed_pmc
Epinephrine delivery via EpiPen ® Auto-Injector or manual syringe across participants with a wide range of skin-to-muscle distances
Epinephrine delivery via EpiPen ® Auto-Injector or manual syringe across participants with a wide range of skin-to-muscle distances Abstract Abstract Background Intramuscular (IM) injection of epinephrine (adrenaline) at the mid-anterolateral (AL) thigh is the international standard therapy for acute anaphylaxis. Conce...
PMC6084602
core_pubmed_pmc
Evaluation of the Relative Intranasal Abuse Potential of a Hydrocodone Extended-Release Tablet Formulated with Abuse-Deterrence Technology in Nondependent, Recreational Opioid Users
Evaluation of the Relative Intranasal Abuse Potential of a Hydrocodone Extended-Release Tablet Formulated with Abuse-Deterrence Technology in Nondependent, Recreational Opioid Users Abstract Abstract Objective To assess the intranasal abuse potential of hydrocodone extended-release (ER) tablets developed with CIMA Abus...
PMC9938066
core_pubmed_pmc
A proof of concept reinforcement learning based tool for non parametric population pharmacokinetics workflow optimization
A proof of concept reinforcement learning based tool for non parametric population pharmacokinetics workflow optimization Abstract Abstract The building of population pharmacokinetic models can be described as an iterative process in which given a model and a dataset, the pharmacometrician introduces some changes to th...
PMC12818054
core_pubmed_pmc
Understanding Pharmacokinetic-Drug Interactions With Drugs Approved by the US Food and Drug Administration in 2024 to Better Manage the Risk of Drug Interactions With Concomitant Medications: A Review of Clinical Data From New Drug Applications
Understanding Pharmacokinetic-Drug Interactions With Drugs Approved by the US Food and Drug Administration in 2024 to Better Manage the Risk of Drug Interactions With Concomitant Medications: A Review of Clinical Data From New Drug Applications Abstract Abstract Objective This analysis aimed to provide a mechanistic un...
PMC6358270
core_pubmed_pmc
Quantitative Systems Toxicology Analysis of In Vitro Mechanistic Assays Reveals Importance of Bile Acid Accumulation and Mitochondrial Dysfunction in TAK-875-Induced Liver Injury
Quantitative Systems Toxicology Analysis of In Vitro Mechanistic Assays Reveals Importance of Bile Acid Accumulation and Mitochondrial Dysfunction in TAK-875-Induced Liver Injury Abstract Abstract TAK-875 (fasiglifam), a GPR40 agonist in development for the treatment of type 2 diabetes (T2D), was voluntarily terminated...
PMC7183353
core_pubmed_pmc
Effect of diabetes mellitus on TB drug concentrations in Tanzanian patients
Effect of diabetes mellitus on TB drug concentrations in Tanzanian patients Abstract Abstract Background Diabetes mellitus (DM) is associated with poor TB treatment outcome. Previous studies examining the effect of DM on TB drug concentrations yielded conflicting results. No studies have been conducted to date in an Af...
PMC4235188
core_pubmed_pmc
Effects of Danshen Ethanol Extract on the Pharmacokinetics of Fexofenadine in Healthy Volunteers
Effects of Danshen Ethanol Extract on the Pharmacokinetics of Fexofenadine in Healthy Volunteers Abstract Abstract This study investigated the effect of multidose administration of danshen ethanol extract on fexofenadine pharmacokinetics in healthy volunteers. A sequential, open-label, two-period pharmacokinetic intera...
PMC3119073
core_pubmed_pmc
Pharmacological Blockade of Serotonin 5-HT 7 Receptor Reverses Working Memory Deficits in Rats by Normalizing Cortical Glutamate Neurotransmission
Pharmacological Blockade of Serotonin 5-HT 7 Receptor Reverses Working Memory Deficits in Rats by Normalizing Cortical Glutamate Neurotransmission Abstract Abstract The role of 5-HT 7 receptor has been demonstrated in various animal models of mood disorders; however its function in cognition remains largely speculative...
PMC8520749
core_pubmed_pmc
Multistate model for pharmacometric analyses of overall survival in HER2‐negative breast cancer patients treated with docetaxel
Multistate model for pharmacometric analyses of overall survival in HER2‐negative breast cancer patients treated with docetaxel Abstract Abstract The aim of this study was to develop a multistate model for overall survival (OS) analysis, based on parametric hazard functions and combined with an investigation of predict...
PMC6585851
core_pubmed_pmc
Bioequivalence of Olanzapine Given in Combination With Samidorphan as a Bilayer Tablet (ALKS 3831) Compared With Olanzapine‐Alone Tablets: Results From a Randomized, Crossover Relative Bioavailability Study
Bioequivalence of Olanzapine Given in Combination With Samidorphan as a Bilayer Tablet (ALKS 3831) Compared With Olanzapine‐Alone Tablets: Results From a Randomized, Crossover Relative Bioavailability Study Abstract Abstract The objective of this study was to evaluate the relative bioavailability of olanzapine in 3 ola...
PMC7032967
core_pubmed_pmc
A review of three years' experience of the first pharmacometrics company in Korea
A review of three years' experience of the first pharmacometrics company in Korea Abstract As the pharmaceutical industry in Korea is reaching the golden era of drug discovery due to increased investments in research and development and government funds, the need for a more efficient tool for the quantitative analysis ...
PMC7601252
core_pubmed_pmc
Progress in Clinical Trials of Photodynamic Therapy for Solid Tumors and the Role of Nanomedicine
Progress in Clinical Trials of Photodynamic Therapy for Solid Tumors and the Role of Nanomedicine Abstract Simple Summary Photodynamic therapy (PDT) has been undertaken with growing focus in recent studies to identify successful anticancer therapies. The field of PDT has evolved rapidly and is continuously being evalua...
PMC7505726
core_pubmed_pmc
A Meta-Analysis on the Performance of Cystatin C- versus Creatinine-based eGFR Equations in Predicting Vancomycin Clearance
A Meta-Analysis on the Performance of Cystatin C- versus Creatinine-based eGFR Equations in Predicting Vancomycin Clearance Abstract Background The objective of this study was to compare the performance of cystatin C- and creatinine-based estimated glomerular filtration rate (eGFR) equations in predicting the clearance...
PMC12655566
core_pubmed_pmc
Biodistribution and Toxicological Impact Assessment of Cerium Dioxide Nanoparticles in Murine Models: A Systematic Review of In Vivo and Ex Vivo Studies
Biodistribution and Toxicological Impact Assessment of Cerium Dioxide Nanoparticles in Murine Models: A Systematic Review of In Vivo and Ex Vivo Studies Abstract Background/Objectives: This review summarizes and analyzes current data on the toxicological effects of cerium dioxide nanoparticles (nanoceria) on various an...
PMC11357403
core_pubmed_pmc
pH-Sensitive In Situ Gel of Mirtazapine Invasomes for Rectal Drug Delivery: Protruded Bioavailability and Anti-Depressant Efficacy
pH-Sensitive In Situ Gel of Mirtazapine Invasomes for Rectal Drug Delivery: Protruded Bioavailability and Anti-Depressant Efficacy Abstract The present research emphasizes fabrication alongside the assessment of an innovative nano-vesicular membranous system known as invasomes (NVMs) laden with Mirtazapine for rectal a...
PMC10714982
core_pubmed_pmc
Population Pharmacokinetics of Isavuconazole in Adult: A Systematic Review
Population Pharmacokinetics of Isavuconazole in Adult: A Systematic Review Abstract Abstract Isavuconazole (ISA) is a second generation broad-spectrum triazole antifungal drug derived from voriconazole structure, and its oral capsules is currently the only oral preparation approved for invasive mucormycosis. In recent ...
PMC11578135
core_pubmed_pmc
Physiologically based pharmacokinetic modeling of drug–drug interactions between ritonavir‐boosted atazanavir and rifampicin in pregnancy
Physiologically based pharmacokinetic modeling of drug–drug interactions between ritonavir‐boosted atazanavir and rifampicin in pregnancy Abstract Abstract Ritonavir‐boosted atazanavir (ATV/r) and rifampicin are mainstays of second‐line antiretroviral and multiple anti‐TB regimens, respectively. Rifampicin induces CYP3...
PMC7318213
core_pubmed_pmc
Long‐term safety and efficacy of rIX‐FP prophylaxis with extended dosing intervals up to 21 days in adults/adolescents with hemophilia B
Long‐term safety and efficacy of rIX‐FP prophylaxis with extended dosing intervals up to 21 days in adults/adolescents with hemophilia B Abstract Abstract Background An international, multicenter extension study evaluated recombinant fusion protein linking recombinant coagulation factor IX (FIX) with recombinant human ...
PMC3033031
core_pubmed_pmc
Pharmacokinetic profile of an intradeltoid diclofenac injection in obese Indian volunteers
Pharmacokinetic profile of an intradeltoid diclofenac injection in obese Indian volunteers Abstract Background A new propylene glycol-free and reduced-volume formulation of diclofenac sodium 75 mg/mL designed for intradeltoid administration has been found to be bioequivalent to a reference formulation of diclofenac sod...
PMC10865485
core_pubmed_pmc
Phase 1 study of latozinemab in progranulin‐associated frontotemporal dementia
Phase 1 study of latozinemab in progranulin‐associated frontotemporal dementia Abstract Abstract INTRODUCTION Heterozygous mutations in the GRN gene lead to reduced progranulin (PGRN) levels in plasma and cerebrospinal fluid (CSF) and are causative of frontotemporal dementia (FTD) with > 90% penetrance. Latozinemab is ...
PMC10788539
core_pubmed_pmc
Repurposing celecoxib for colorectal cancer targeting via pH-triggered ultra-elastic nanovesicles: Pronounced efficacy through up-regulation of Wnt/β-catenin pathway in DMH-induced tumorigenesis
Repurposing celecoxib for colorectal cancer targeting via pH-triggered ultra-elastic nanovesicles: Pronounced efficacy through up-regulation of Wnt/β-catenin pathway in DMH-induced tumorigenesis Abstract Abstract Celecoxib (CLX), a selective inhibitor for cyclooxygenase 2 (COX-2), has manifested potential activity agai...
PMC5264215
core_pubmed_pmc
Canakinumab treatment for patients with active recurrent or chronic TNF receptor-associated periodic syndrome (TRAPS): an open-label, phase II study
Canakinumab treatment for patients with active recurrent or chronic TNF receptor-associated periodic syndrome (TRAPS): an open-label, phase II study Abstract Abstract Objective To evaluate the efficacy of canakinumab, a high-affinity human monoclonal anti-interleukin-1β antibody, in inducing complete or almost complete...
PMC8521408
core_pubmed_pmc
Impact of a vancomycin loading dose on the achievement of target vancomycin exposure in the first 24 h and on the accompanying risk of nephrotoxicity in critically ill patients
Impact of a vancomycin loading dose on the achievement of target vancomycin exposure in the first 24 h and on the accompanying risk of nephrotoxicity in critically ill patients Abstract Abstract Background The advocated pharmacokinetic/pharmacodynamic (PK/PD) target for vancomycin, AUC/MIC ≥ 400 mg·h/L, may not be reac...
PMC5901008
core_pubmed_pmc
Impact of the Norepinephrine Prodrug Droxidopa on the QTc Interval in Healthy Individuals
Impact of the Norepinephrine Prodrug Droxidopa on the QTc Interval in Healthy Individuals Abstract Abstract A double‐blind, 4‐period crossover study ( NCT01327066 ) was conducted to assess the effect of the novel norepinephrine prodrug droxidopa on the QT interval in in healthy subjects. Subjects were randomized to rec...
PMC11179707
core_pubmed_pmc
Joint modeling of tumor dynamics and progression‐free survival in advanced breast cancer: Leveraging data from amcenestrant early phase I–II trials
Joint modeling of tumor dynamics and progression‐free survival in advanced breast cancer: Leveraging data from amcenestrant early phase I–II trials Abstract Abstract A joint modeling framework was developed using data from 75 patients of early amcenestrant phase I–II AMEERA‐1‐2 dose escalation and expansion cohorts. A ...
PMC8245906
core_pubmed_pmc
Can remdesivir and its parent nucleoside GS-441524 be potential oral drugs? An in vitro and in vivo DMPK assessment
Can remdesivir and its parent nucleoside GS-441524 be potential oral drugs? An in vitro and in vivo DMPK assessment Abstract Abstract Remdesivir (RDV) is the only US Food and Drug Administration (FDA)-approved drug for treating COVID-19. However, RDV can only be given by intravenous route, and there is a pressing medic...
PMC4947994
core_pubmed_pmc
Inhibition of Poly(ADP-Ribose) Polymerase by Nucleic Acid Metabolite 7-Methylguanine
Inhibition of Poly(ADP-Ribose) Polymerase by Nucleic Acid Metabolite 7-Methylguanine Abstract The ability of 7-methylguanine, a nucleic acid metabolite, to inhibit poly(ADP-ribose)polymerase-1 (PARP-1) and poly(ADP-ribose)polymerase-2 (PARP-2) has been identified in silico and studied experimentally. The amino group at...
PMC4572077
core_pubmed_pmc
Clinical and In Vitro Studies on Impact of High-Dose Etoposide Pharmacokinetics Prior Allogeneic Hematopoietic Stem Cell Transplantation for Childhood Acute Lymphoblastic Leukemia on the Risk of Post-Transplant Leukemia Relapse
Clinical and In Vitro Studies on Impact of High-Dose Etoposide Pharmacokinetics Prior Allogeneic Hematopoietic Stem Cell Transplantation for Childhood Acute Lymphoblastic Leukemia on the Risk of Post-Transplant Leukemia Relapse Abstract The impact of etoposide (VP-16) plasma concentrations on the day of allogeneic hema...
PMC5762195
core_pubmed_pmc
Liquid chromatography–tandem mass spectrometry method for the estimation of adefovir in human plasma: Application to a pharmacokinetic study
Liquid chromatography–tandem mass spectrometry method for the estimation of adefovir in human plasma: Application to a pharmacokinetic study Abstract An analytical method based on solid phase extraction was developed and validated for analysis of adefovir in human plasma. Adefovir-d 4 was used as an internal standard a...
PMC10666625
core_pubmed_pmc
Exploring the benefits of in-diet versus repeated oral dosing of saracatinib (AZD0530) in chronic studies: insights into pharmacokinetics and animal welfare
Exploring the benefits of in-diet versus repeated oral dosing of saracatinib (AZD0530) in chronic studies: insights into pharmacokinetics and animal welfare Abstract Abstract Saracatinib/AZD0530 (SAR), a Src tyrosine kinase inhibitor, mitigates seizure-induced brain pathology in epilepsy models upon repeated oral dosin...
PMC10328216
core_pubmed_pmc
A State-of-the-Science Review of Interactions of Per- and Polyfluoroalkyl Substances (PFAS) with Renal Transporters in Health and Disease: Implications for Population Variability in PFAS Toxicokinetics
A State-of-the-Science Review of Interactions of Per- and Polyfluoroalkyl Substances (PFAS) with Renal Transporters in Health and Disease: Implications for Population Variability in PFAS Toxicokinetics Abstract Background: Per- and polyfluoroalkyl substances (PFAS) are ubiquitous in the environment and have been shown ...
PMC7763054
core_pubmed_pmc
Disposition of Cannabidiol Metabolites in Serum and Urine from Healthy Individuals Treated with Pharmaceutical Preparations of Medical Cannabis
Disposition of Cannabidiol Metabolites in Serum and Urine from Healthy Individuals Treated with Pharmaceutical Preparations of Medical Cannabis Abstract The use of cannabis flowering tops with standardized amounts of active phytocannabinoids was recently authorized in several countries to treat several painful patholog...