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PMC10767306
core_pubmed_pmc
Phase I Dose-Escalation Study of the Safety and Pharmacokinetics of AGS15E Monotherapy in Patients with Metastatic Urothelial Carcinoma
Phase I Dose-Escalation Study of the Safety and Pharmacokinetics of AGS15E Monotherapy in Patients with Metastatic Urothelial Carcinoma Abstract Abstract Purpose: Effective treatment of locally advanced or metastatic urothelial carcinoma (mUC) remains an unmet need. Antibody–drug conjugates (ADC) providing targeted dru...
PMC10892084
core_pubmed_pmc
Quantitative Analysis of Cenobamate and Concomitant Anti-Seizure Medications in Human Plasma via Ultra-High Performance Liquid Chromatography–Tandem Mass Spectrometry
Quantitative Analysis of Cenobamate and Concomitant Anti-Seizure Medications in Human Plasma via Ultra-High Performance Liquid Chromatography–Tandem Mass Spectrometry Abstract Abstract Cenobamate (CNB) is a new anti-seizure medication (ASM) recently introduced in clinical practice after approval by the FDA and EMA for ...
PMC3118685
core_pubmed_pmc
Study of pharmacokinetics and tissue distribution of liposomal brucine for dermal administration
Study of pharmacokinetics and tissue distribution of liposomal brucine for dermal administration Abstract Objective: To evaluate the pharmacokinetics and tissue distribution of liposomal brucine (LB) for dermal application. Methods: Pharmacokinetics and tissue distribution were studied by in vivo animal testing. High p...
PMC12707326
core_pubmed_pmc
Overcoming Antimicrobial Resistance in Bacterial Keratitis With an Antibiotic-Eluting Contact Lens
Overcoming Antimicrobial Resistance in Bacterial Keratitis With an Antibiotic-Eluting Contact Lens Abstract Abstract Purpose Bacterial keratitis (BK) is a leading cause of corneal blindness globally, with an alarming rise in resistant infections. Current standard-of-care antibiotic eye drops or ointments suffer from lo...
PMC7415440
core_pubmed_pmc
First-in-Human Evaluation of the Safety, Tolerability, and Pharmacokinetics of a Neuroprotective Poly (ADP‐ribose) Polymerase‐1 Inhibitor, JPI-289, in Healthy Volunteers
First-in-Human Evaluation of the Safety, Tolerability, and Pharmacokinetics of a Neuroprotective Poly (ADP‐ribose) Polymerase‐1 Inhibitor, JPI-289, in Healthy Volunteers Abstract Background Poly (ADP-ribose) polymerase-1 (PARP-1) inhibitor has therapeutic potential for acute ischemic stroke by suppressing microglial ac...
PMC12909361
core_pubmed_pmc
A physics-informed neural network approach for estimating population-level pharmacokinetic parameters from aggregated concentration data
A physics-informed neural network approach for estimating population-level pharmacokinetic parameters from aggregated concentration data Abstract The pharmacokinetic literature is rich in aggregated concentration data that contain valuable information, yet tools to extract this information remain limited. This work int...
PMC11695783
core_pubmed_pmc
The novel pleuromutilin derivative 22–((4-((4-nitrophenyl)acetamido)phenyl)thio)deoxy pleuromutilin possesses robust anti-mycoplasma activity both in vitro and in vivo
The novel pleuromutilin derivative 22–((4-((4-nitrophenyl)acetamido)phenyl)thio)deoxy pleuromutilin possesses robust anti-mycoplasma activity both in vitro and in vivo Abstract Objective Mycoplasmas are structurally simple pathogenic microorganisms that can cause a wide range of diseases in humans and animals and conve...
PMC7383777
core_pubmed_pmc
The association between anti‐insulin aspart antibodies and the pharmacokinetic and pharmacodynamic characteristics of fast‐acting insulin aspart in children and adolescents with type 1 diabetes
The association between anti‐insulin aspart antibodies and the pharmacokinetic and pharmacodynamic characteristics of fast‐acting insulin aspart in children and adolescents with type 1 diabetes Abstract Abstract Background Fast‐acting insulin aspart (faster aspart) is a novel formulation of insulin aspart (IAsp) ensuri...
PMC5955748
core_pubmed_pmc
Investigation of the synergistic effects of haloperidol combined with Calculus Bovis Sativus in treating MK-801-induced schizophrenia in rats
Investigation of the synergistic effects of haloperidol combined with Calculus Bovis Sativus in treating MK-801-induced schizophrenia in rats Abstract Abstract Clinical studies that focused on treating schizophrenia showed that Calculus Bovis Sativus (CBS), a substitute of Calculus Bovis , when used in combination with...
PMC3425428
core_pubmed_pmc
Why Do SGLT2 Inhibitors Inhibit Only 30–50% of Renal Glucose Reabsorption in Humans?
Why Do SGLT2 Inhibitors Inhibit Only 30–50% of Renal Glucose Reabsorption in Humans? Abstract Abstract Sodium glucose cotransporter 2 (SGLT2) inhibition is a novel and promising treatment for diabetes under late-stage clinical development. It generally is accepted that SGLT2 mediates 90% of renal glucose reabsorption. ...
PMC3861587
core_pubmed_pmc
Icotinib combined with rapamycin in a renal transplant recipient with epidermal growth factor receptor-mutated non-small cell lung cancer: A case report
Icotinib combined with rapamycin in a renal transplant recipient with epidermal growth factor receptor-mutated non-small cell lung cancer: A case report Abstract As kidney transplant recipients are at increased risk of developing cancer, regular monitoring should be undertaken to monitor the balance between immunosuppr...
PMC11570312
core_pubmed_pmc
Development, optimization, and characterization of polymeric micelles to improve dasatinib oral bioavailability: Hep G2 cell cytotoxicity and in vivo pharmacokinetics for targeted liver cancer therapy
Development, optimization, and characterization of polymeric micelles to improve dasatinib oral bioavailability: Hep G2 cell cytotoxicity and in vivo pharmacokinetics for targeted liver cancer therapy Abstract The efficacy of dasatinib (DAS) in treating hepatocellular carcinoma (HCC) is hindered by its poor bioavailabi...
PMC12202194
core_pubmed_pmc
Efanesoctocog Alfa Population Pharmacokinetics and Repeated Time‐To‐Event Analysis of Bleeds in Adults, Adolescents, and Children with Severe Hemophilia A
Efanesoctocog Alfa Population Pharmacokinetics and Repeated Time‐To‐Event Analysis of Bleeds in Adults, Adolescents, and Children with Severe Hemophilia A Abstract Abstract Efanesoctocog alfa is a first‐in‐class high‐sustained factor VIII (HSF) replacement therapy for treatment of hemophilia A. This article presents po...
PMC10647616
core_pubmed_pmc
Side-Chain Modified [ 99m Tc]Tc-DT1 Mimics: A Comparative Study in NTS 1 R-Positive Models
Side-Chain Modified [ 99m Tc]Tc-DT1 Mimics: A Comparative Study in NTS 1 R-Positive Models Abstract Radiolabeled neurotensin analogs have been developed as candidates for theranostic use against neurotensin subtype 1 receptor (NTS 1 R)-expressing cancer. However, their fast degradation by two major peptidases, neprilys...
PMC5989019
core_pubmed_pmc
Effects of leucovorin (folinic acid) in the methotrexate-treated rat brain
Effects of leucovorin (folinic acid) in the methotrexate-treated rat brain Abstract Folinic acid (FA) is generally administered to patients with CNS tumors in order to treat severe neurological disorders caused by methotrexate (MTX); therefore, we herein examined the effects of the co-administration of FA on MTX concen...
PMC10044979
core_pubmed_pmc
Immunosuppressive Therapy of Biopsy-Proven, Virus-Negative, Autoimmune/Immune-Mediated Myocarditis—Focus on Azathioprine: A Review of Existing Evidence and Future Perspectives
Immunosuppressive Therapy of Biopsy-Proven, Virus-Negative, Autoimmune/Immune-Mediated Myocarditis—Focus on Azathioprine: A Review of Existing Evidence and Future Perspectives Abstract Abstract Simple Summary Myocarditis is one of the leading causes of acute and chronic heart failure, adverse ventricular remodelling, a...
PMC8960278
core_pubmed_pmc
Characterizing Pharmacokinetics in Children With Obesity—Physiological, Drug, Patient, and Methodological Considerations
Characterizing Pharmacokinetics in Children With Obesity—Physiological, Drug, Patient, and Methodological Considerations Abstract Childhood obesity is an alarming public health problem. The pediatric obesity rate has quadrupled in the past 30 years, and currently nearly 20% of United States children and 9% of children ...
PMC7555481
core_pubmed_pmc
Nebulized ivermectin for COVID-19 and other respiratory diseases, a proof of concept, dose-ranging study in rats
Nebulized ivermectin for COVID-19 and other respiratory diseases, a proof of concept, dose-ranging study in rats Abstract Ivermectin is a widely used antiparasitic drug with known efficacy against several single-strain RNA viruses. Recent data shows significant reduction of SARS-CoV-2 replication in vitro by ivermectin...
PMC4992876
core_pubmed_pmc
Monitoring Tumor Hypoxia Using 18 F-FMISO PET and Pharmacokinetics Modeling after Photodynamic Therapy
Monitoring Tumor Hypoxia Using 18 F-FMISO PET and Pharmacokinetics Modeling after Photodynamic Therapy Abstract Photodynamic therapy (PDT) is an efficacious treatment for some types of cancers. However, PDT-induced tumor hypoxia as a result of oxygen consumption and vascular damage can reduce the efficacy of this thera...
PMC4130380
core_pubmed_pmc
The pyrazinamide susceptibility breakpoint above which combination therapy fails
The pyrazinamide susceptibility breakpoint above which combination therapy fails Abstract Objectives To identify the pyrazinamide MIC above which standard combination therapy fails. Methods MICs of pyrazinamide were determined for Mycobacterium tuberculosis isolates, cultured from 58 patients in a previous randomized c...
PMC6590207
core_pubmed_pmc
Influence of Renal Function on Evolocumab Exposure, Pharmacodynamics, and Safety
Influence of Renal Function on Evolocumab Exposure, Pharmacodynamics, and Safety Abstract Abstract We evaluated the pharmacokinetics, pharmacodynamics, and safety of evolocumab, a fully human monoclonal antibody against proprotein convertase subtilisin kexin type 9 (PCSK9), in an open‐label, parallel‐design study in pa...
PMC12415810
core_pubmed_pmc
Pharmacokinetics of Amoxicillin in the Cat
Pharmacokinetics of Amoxicillin in the Cat Abstract ABSTRACT The pharmacokinetics and plasma protein binding of amoxicillin in cats has not been thoroughly investigated. In a single‐group sequential designed experimental study, amoxicillin was administered to six healthy cats intravenously, orally, and subcutaneously. ...
PMC12568254
core_pubmed_pmc
Absorption and Tissue Distribution of Environmental Pollutant HFPO-DA, and Its Effect on Hepatic Lipid Metabolism Reprogramming in Mice
Absorption and Tissue Distribution of Environmental Pollutant HFPO-DA, and Its Effect on Hepatic Lipid Metabolism Reprogramming in Mice Abstract Objective: Hexafluoropropylene oxide dimer acid (HFPO-DA), also known as GenX, is widely used globally, raising concerns about its safety and public health implications. Howev...
PMC12952630
core_pubmed_pmc
Cheminformatics-driven discovery of natural isoquinoline alkaloid inhibitors of Beta-secretase I for Alzheimer’s management
Cheminformatics-driven discovery of natural isoquinoline alkaloid inhibitors of Beta-secretase I for Alzheimer’s management Abstract Abstract Alzheimer’s disease (AD) is characterized by the gradual deterioration of cognitive functions, speech impairment, and memory loss. It can potentially be treated by targeting the ...
PMC5106233
core_pubmed_pmc
Treatment-resistant schizophrenia: current insights on the pharmacogenomics of antipsychotics
Treatment-resistant schizophrenia: current insights on the pharmacogenomics of antipsychotics Abstract Abstract Up to 30% of people with schizophrenia do not respond to two (or more) trials of dopaminergic antipsychotics. They are said to have treatment-resistant schizophrenia (TRS). Clozapine is still the only effecti...
PMC7004103
core_pubmed_pmc
Sofosbuvir and Ribavirin Therapy for Children Aged 3 to <12 Years With Hepatitis C Virus Genotype 2 or 3 Infection
Sofosbuvir and Ribavirin Therapy for Children Aged 3 to <12 Years With Hepatitis C Virus Genotype 2 or 3 Infection Abstract Currently, the only approved hepatitis C virus (HCV) treatment for children aged <12 years is pegylated interferon plus ribavirin. In an open‐label study, we evaluated the safety and efficacy of s...
PMC12159082
core_pubmed_pmc
Leveraging Model Master Files for Long-Acting Injectables
Leveraging Model Master Files for Long-Acting Injectables Abstract Abstract The U.S. Food and Drug Administration (FDA) and the Center for Research on Complex Generics (CRCG) hosted a public workshop on May 2–3, 2024, titled “Considerations and Potential Regulatory Applications for a Model Master File”. The workshop ai...
PMC8565507
core_pubmed_pmc
Age-Specific Dose Regimens of Dexmedetomidine for Pediatric Patients in Intensive Care Following Elective Surgery: A Phase 3, Multicenter, Open-Label Clinical Trial in Japan
Age-Specific Dose Regimens of Dexmedetomidine for Pediatric Patients in Intensive Care Following Elective Surgery: A Phase 3, Multicenter, Open-Label Clinical Trial in Japan Abstract Supplemental Digital Content is available in the text. OBJECTIVES: To demonstrate the efficacy, safety, and pharmacokinetics of dexmedeto...
PMC10622740
core_pubmed_pmc
Pooled analysis of three pharmacokinetic studies comparing biosimilar MB02 and reference bevacizumab
Pooled analysis of three pharmacokinetic studies comparing biosimilar MB02 and reference bevacizumab Abstract Abstract Aim The aim of this study was to add robustness and provide further evidence on the bioequivalence, safety and immunogenicity between MB02 and reference bevacizumab. No similar study has been performed...
PMC8538675
core_pubmed_pmc
Nutraceuticals for Peripheral Vestibular Pathology: Properties, Usefulness, Future Perspectives and Medico-Legal Aspects
Nutraceuticals for Peripheral Vestibular Pathology: Properties, Usefulness, Future Perspectives and Medico-Legal Aspects Abstract Abstract Vestibular disorders may generate complex signs and symptoms, which may alter patients’ balance and the quality of life. Dizziness and vertigo can strongly affect daily activities a...
PMC8813803
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modelling of Inhaled Nemiralisib: Mechanistic Components for Pulmonary Absorption, Systemic Distribution, and Oral Absorption
Physiologically Based Pharmacokinetic Modelling of Inhaled Nemiralisib: Mechanistic Components for Pulmonary Absorption, Systemic Distribution, and Oral Absorption Abstract Background and Objectives Physiologically based pharmacokinetic (PBPK) modelling has evolved to accommodate different routes of drug administration...
PMC7225193
core_pubmed_pmc
An Integrated Dialysis Pharmacometric (IDP) Model to Evaluate the Pharmacokinetics in Patients Undergoing Renal Replacement Therapy
An Integrated Dialysis Pharmacometric (IDP) Model to Evaluate the Pharmacokinetics in Patients Undergoing Renal Replacement Therapy Abstract Purpose Clearance via renal replacement therapy (RRT) can significantly alter the pharmacokinetic profile of drugs. The aim of this study was (i) to improve the use of clinical tr...
PMC10666227
core_pubmed_pmc
Assessment of Novel Mesothelin-Specific Human Antibody Domain VH-Fc Fusion Proteins-Based PET Agents
Assessment of Novel Mesothelin-Specific Human Antibody Domain VH-Fc Fusion Proteins-Based PET Agents Abstract Mesothelin (MSLN) is a tumor-associated antigen found in a variety of cancers and is a target for imaging and therapeutic applications in MSLN-expressing tumors. We have developed high affinity anti-MSLN human ...
PMC4123858
core_pubmed_pmc
A pilot study of leukocyte expression patterns for drug metabolizing enzyme and transporter transcripts in autoimmune glomerulonephritis
A pilot study of leukocyte expression patterns for drug metabolizing enzyme and transporter transcripts in autoimmune glomerulonephritis Abstract Objective: Leukocyte mRNA expression patterns of drug metabolizing enzyme genes and transporter genes that are relevant for the disposition of cyclophosphamide and mycophenol...
PMC12552610
core_pubmed_pmc
Development of [ 18 F]ACI-19626 as a first-in-class brain PET tracer for imaging TDP-43 pathology
Development of [ 18 F]ACI-19626 as a first-in-class brain PET tracer for imaging TDP-43 pathology Abstract Aggregated TDP-43 is a hallmark of frontotemporal dementia (FTD), amyotrophic lateral sclerosis (ALS), and limbic-predominant age-related TDP-43 encephalopathy (LATE), and a common co-pathology in other neurodegen...
PMC5038276
core_pubmed_pmc
Phase I Study Assessing the Pharmacokinetic Profile, Safety, and Tolerability of a Single Dose of Ceftazidime-Avibactam in Hospitalized Pediatric Patients
Phase I Study Assessing the Pharmacokinetic Profile, Safety, and Tolerability of a Single Dose of Ceftazidime-Avibactam in Hospitalized Pediatric Patients Abstract Abstract This study aimed to investigate the pharmacokinetics (PK), safety, and tolerability of a single dose of ceftazidime-avibactam in pediatric patients...
PMC4675922
core_pubmed_pmc
Usefulness of serum cystatin C to determine the dose of vancomycin in neonate
Usefulness of serum cystatin C to determine the dose of vancomycin in neonate Abstract Abstract Purpose The vancomycin dosage regimen is regularly modified according to the patient's glomerular filtration rate (GFR). In the present study, we aimed to assess the usefulness of serum cystatin C (Cys-C) concentration, comp...
PMC6262195
core_pubmed_pmc
Pharmacokinetics of Glucocorticoid Replacement Before and After Bariatric Surgery in Patients With Adrenal Insufficiency
Pharmacokinetics of Glucocorticoid Replacement Before and After Bariatric Surgery in Patients With Adrenal Insufficiency Abstract Abstract Adequate glucocorticoid replacement in patients with primary or secondary adrenal insufficiency is essential to maintain general well-being. Little is known about the effects of bar...
PMC5192970
core_pubmed_pmc
Integrated Two‐Analyte Population Pharmacokinetic Model for Antibody–Drug Conjugates in Patients: Implications for Reducing Pharmacokinetic Sampling
Integrated Two‐Analyte Population Pharmacokinetic Model for Antibody–Drug Conjugates in Patients: Implications for Reducing Pharmacokinetic Sampling Abstract Abstract An integrated pharmacokinetics (PK) model that simultaneously describes concentrations of total antibody (Tab) and antibody‐conjugated monomethyl aurista...
PMC6431368
core_pubmed_pmc
Population Pharmacokinetics of Clozapine and Norclozapine and Switchability Assessment between Brands in Uruguayan Patients with Schizophrenia
Population Pharmacokinetics of Clozapine and Norclozapine and Switchability Assessment between Brands in Uruguayan Patients with Schizophrenia Abstract Clozapine (CZP) is an atypical antipsychotic agent commonly used in the treatment of schizophrenia. It is metabolized primarily by CYP1A2 enzyme, yielding a pharmacolog...
PMC9828395
core_pubmed_pmc
Physiologically‐Based Pharmacokinetic Model Development, Validation, and Application for Prediction of Eliglustat Drug–Drug Interactions
Physiologically‐Based Pharmacokinetic Model Development, Validation, and Application for Prediction of Eliglustat Drug–Drug Interactions Abstract Abstract Eliglustat is a glucosylceramide synthase inhibitor indicated as a long‐term substrate reduction therapy for adults with type 1 Gaucher disease, a lysosomal rare dis...
PMC3651527
core_pubmed_pmc
From evidence based medicine to mechanism based medicine. Reviewing the role of pharmacogenetics
From evidence based medicine to mechanism based medicine. Reviewing the role of pharmacogenetics Abstract Abstract Aim of the review The translation of evidence based medicine to a specific patient presents a considerable challenge. We present by means of the examples nortriptyline, tramadol, clopidogrel, coumarins, ab...
PMC12164272
core_pubmed_pmc
Ruthenium(II) Polypyridyl Complexes Containing COUBPY Ligands as Potent Photosensitizers for the Efficient Phototherapy of Hypoxic Tumors
Ruthenium(II) Polypyridyl Complexes Containing COUBPY Ligands as Potent Photosensitizers for the Efficient Phototherapy of Hypoxic Tumors Abstract Abstract Hypoxia, a hallmark of many solid tumors, is linked to increased cancer aggressiveness, metastasis, and resistance to conventional therapies, leading to poor patien...
PMC7376292
core_pubmed_pmc
Model‐Based Analysis Reveals a Sustained and Dose‐Dependent Acceleration of Wound Healing by VEGF‐A mRNA (AZD8601)
Model‐Based Analysis Reveals a Sustained and Dose‐Dependent Acceleration of Wound Healing by VEGF‐A mRNA (AZD8601) Abstract Intradermal delivery of AZD8601, an mRNA designed to produce vascular endothelial growth factor A (VEGF‐A), has previously been shown to accelerate cutaneous wound healing in a murine diabetic mod...
PMC10446811
core_pubmed_pmc
Gemcitabine enhances pharmacokinetic exposure of the major components of Danggui Buxue Decoction in rat via the promotion of intestinal permeability and down-regulation of CYP3A for combination treatment of non-small cell lung cancer
Gemcitabine enhances pharmacokinetic exposure of the major components of Danggui Buxue Decoction in rat via the promotion of intestinal permeability and down-regulation of CYP3A for combination treatment of non-small cell lung cancer Abstract Abstract Context Danggui Buxue Decoction (DBD), a traditional Chinese medicin...
PMC7419005
core_pubmed_pmc
Non-invasive monitoring of drug action: A new live in vitro assay design for Chagas’ disease drug discovery
Non-invasive monitoring of drug action: A new live in vitro assay design for Chagas’ disease drug discovery Abstract New assay designs are needed to improve the predictive value of the Trypanosoma cruzi in vitro tests used as part of the Chagas' disease drug development pipeline. Here, we employed a green fluorescent p...
PMC4033946
core_pubmed_pmc
Update on the Genetic Polymorphisms of Drug-Metabolizing Enzymes in Antiepileptic Drug Therapy
Update on the Genetic Polymorphisms of Drug-Metabolizing Enzymes in Antiepileptic Drug Therapy Abstract Genetic polymorphisms in the genes that encode drug-metabolizing enzymes are implicated in the inter-individual variability in the pharmacokinetics and pharmaco-dynamics of antiepileptic drugs (AEDs). However, the cl...
PMC6157667
core_pubmed_pmc
Population Pharmacokinetic/Pharmacodynamic Analysis of Nociceptive Pain Models Following an Oral Pregabalin Dose Administration to Healthy Subjects
Population Pharmacokinetic/Pharmacodynamic Analysis of Nociceptive Pain Models Following an Oral Pregabalin Dose Administration to Healthy Subjects Abstract Abstract A battery of pain models can be used in clinical trials to investigate the efficacy and to establish the concentration‐effect relationship of novel analge...
PMC12521060
core_pubmed_pmc
The Basel Modeling and Simulation Seminar: 20 Editions of Fostering Local Exchange in Pharmacometrics
The Basel Modeling and Simulation Seminar: 20 Editions of Fostering Local Exchange in Pharmacometrics Abstract ABSTRACT This year marks the 20th edition of the Basel Modeling and Simulation (M&S) Seminar, an initiative rooted in a commitment to promoting the exchange of the latest advancements in pharmacometrics and re...
PMC12399714
core_pubmed_pmc
Sex-related differences in the efficacy and toxicity of cancer treatments
Sex-related differences in the efficacy and toxicity of cancer treatments Abstract Differences between the biological sexes have long been observed in cancer incidence and prevalence, and in treatment outcomes including efficacy and toxicity. Ideally, there should be sufficient information to improve the individualizat...
PMC8944491
core_pubmed_pmc
Use of Antimicrobials for Bloodstream Infections in the Intensive Care Unit, a Clinically Oriented Review
Use of Antimicrobials for Bloodstream Infections in the Intensive Care Unit, a Clinically Oriented Review Abstract Bloodstream infections (BSIs) in critically ill patients are associated with significant mortality. For patients with septic shock, antibiotics should be administered within the hour. Probabilistic treatme...
PMC12310844
core_pubmed_pmc
Safety, tolerability, and preliminary efficacy of nadunolimab, an anti-IL- 1 receptor accessory protein monoclonal antibody, in combination with pembrolizumab in patients with solid tumors
Safety, tolerability, and preliminary efficacy of nadunolimab, an anti-IL- 1 receptor accessory protein monoclonal antibody, in combination with pembrolizumab in patients with solid tumors Abstract Interleukin (IL)-1 signaling has an essential role in tumor progression and immunosuppression and is linked to acquired re...
PMC8504835
core_pubmed_pmc
3D cell culture models: Drug pharmacokinetics, safety assessment, and regulatory consideration
3D cell culture models: Drug pharmacokinetics, safety assessment, and regulatory consideration Abstract Abstract Nonclinical testing has served as a foundation for evaluating potential risks and effectiveness of investigational new drugs in humans. However, the current two‐dimensional (2D) in vitro cell culture systems...
PMC9580235
core_pubmed_pmc
Microwave assisted synthesis of 2-amino-4-chloro-pyrimidine derivatives: Anticancer and computational study on potential inhibitory action against COVID-19
Microwave assisted synthesis of 2-amino-4-chloro-pyrimidine derivatives: Anticancer and computational study on potential inhibitory action against COVID-19 Abstract We report microwave synthesis of seven unique pyrimidine anchored derivatives ( 1 – 7 ) incorporating multifunctional amino derivatives along with their in...
PMC8247401
core_pubmed_pmc
Evaluation of clinical and genetic factors in the population pharmacokinetics of carbamazepine
Evaluation of clinical and genetic factors in the population pharmacokinetics of carbamazepine Abstract Aims Carbamazepine can cause hypersensitivity reactions in ~10% of patients. An immunogenic effect can be produced by the electrophilic 10,11‐epoxide metabolite but not by carbamazepine. Hypothetically, certain singl...
PMC11652821
core_pubmed_pmc
Prediction of Cardiac ATTR Depletion by NI006 ( ALXN2220 ) Using Mechanistic PK / PD Modeling
Prediction of Cardiac ATTR Depletion by NI006 ( ALXN2220 ) Using Mechanistic PK / PD Modeling Abstract NI006 (aka ALXN2220) is a therapeutic antibody candidate in phase III clinical development for the depletion of amyloid transthyretin (ATTR) in patients with ATTR cardiomyopathy, an infiltrative cardiomyopathy leading...
PMC8275530
core_pubmed_pmc
Predictive performance of parent-metabolite population pharmacokinetic models of (S)-ketamine in healthy volunteers
Predictive performance of parent-metabolite population pharmacokinetic models of (S)-ketamine in healthy volunteers Abstract Purpose The recent repurposing of ketamine as treatment for pain and depression has increased the need for accurate population pharmacokinetic (PK) models to inform the design of new clinical tri...
PMC6853265
core_pubmed_pmc
The Bioequivalence and Effect of Food on the Pharmacokinetics of a Fixed‐Dose Combination Tablet Containing Rosuvastatin and Ezetimibe in Healthy Japanese Subjects
The Bioequivalence and Effect of Food on the Pharmacokinetics of a Fixed‐Dose Combination Tablet Containing Rosuvastatin and Ezetimibe in Healthy Japanese Subjects Abstract Abstract Certain patient populations are unable to achieve the recommended low‐density lipoprotein cholesterol goals with statin monotherapy alone....
PMC12423301
core_pubmed_pmc
Astrocytic monoamine oxidase B (MAOB)–gamma-aminobutyric acid (GABA) axis as a molecular brake on repair following spinal cord injury
Astrocytic monoamine oxidase B (MAOB)–gamma-aminobutyric acid (GABA) axis as a molecular brake on repair following spinal cord injury Abstract Neuroregeneration and remyelination rarely occur in the adult mammalian brain and spinal cord following central nervous system (CNS) injury. The glial scar has been proposed as ...
PMC12706400
core_pubmed_pmc
QPRapp: A Web‐Based Platform for PK/PD Simulations and Early Feasibility Analysis
QPRapp: A Web‐Based Platform for PK/PD Simulations and Early Feasibility Analysis Abstract ABSTRACT Quantitative pharmacology research application (QPRapp) is a web‐based, interactive, and easy to use Shiny for Python interface, which facilitates evaluation of dose‐exposure relationships, pharmacokinetic/pharmacodynami...
PMC4184705
core_pubmed_pmc
A clinical therapeutic protein drug–drug interaction study: coadministration of denosumab and midazolam in postmenopausal women with osteoporosis
A clinical therapeutic protein drug–drug interaction study: coadministration of denosumab and midazolam in postmenopausal women with osteoporosis Abstract Drug–disease interactions involving therapeutic proteins that target cytokines and potentially impact cytochrome P450 (CYP) enzymes have been of increased interest t...
PMC9608142
core_pubmed_pmc
Population pharmacokinetic analysis, renal safety, and dosing optimization of polymyxin B in lung transplant recipients with pneumonia: A prospective study
Population pharmacokinetic analysis, renal safety, and dosing optimization of polymyxin B in lung transplant recipients with pneumonia: A prospective study Abstract Objectives: This study aims to characterize the population pharmacokinetics of polymyxin B in lung transplant recipients and optimize its dosage regimens. ...
PMC3574535
core_pubmed_pmc
Determination of 17 β-Estradiol in Rabbit Plasma by Gas Chromatography with Flame Ionization Detection
Determination of 17 β-Estradiol in Rabbit Plasma by Gas Chromatography with Flame Ionization Detection Abstract This article describes gas chromatography-flame ionization detection method for determination of 17 β-estradiol in rabbit plasma. 17 β-estradiol and internal standard progesterone were extracted from plasma u...
PMC7656898
core_pubmed_pmc
Pulmonary infections complicating ARDS
Pulmonary infections complicating ARDS Abstract Pulmonary infection is one of the main complications occurring in patients suffering from acute respiratory distress syndrome (ARDS). Besides traditional risk factors, dysregulation of lung immune defenses and microbiota may play an important role in ARDS patients. Prone ...
PMC10027930
core_pubmed_pmc
Physiologically based pharmacokinetic-pharmacodynamic evaluation of meropenem in CKD and hemodialysis individuals
Physiologically based pharmacokinetic-pharmacodynamic evaluation of meropenem in CKD and hemodialysis individuals Abstract Abstract Objective: Chronic kidney disease (CKD) has significant effects on renal clearance of drugs. The application of antibiotics in CKD patients to achieve the desired therapeutic effect is cha...
PMC12081532
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Modeling of the Acute Heart Rate Effects of Delta-9 Tetrahydrocannabinol and Its Major Metabolites After Intravenous Injection in Healthy Volunteers
Pharmacokinetic/Pharmacodynamic Modeling of the Acute Heart Rate Effects of Delta-9 Tetrahydrocannabinol and Its Major Metabolites After Intravenous Injection in Healthy Volunteers Abstract Abstract Background and Objectives Cannabis consumption is increasing in both the recreational and medical settings. Tetrahydrocan...
PMC12845225
core_pubmed_pmc
Ligustilide: A Phytochemical with Potential in Combating Cancer Development and Progression—A Comprehensive and Critical Review
Ligustilide: A Phytochemical with Potential in Combating Cancer Development and Progression—A Comprehensive and Critical Review Abstract Cancer remains one of the leading global health challenges, with increasing resistance to conventional therapies hindering treatment efficacy. Ligustilide, a bioactive compound derive...
PMC9942619
core_pubmed_pmc
Oseltamivir phosphate for suspension is bioequivalent to TAMIFLU in healthy volunteers: a randomized, open-label clinical study
Oseltamivir phosphate for suspension is bioequivalent to TAMIFLU in healthy volunteers: a randomized, open-label clinical study Abstract Purpose The study was aimed at evaluating the bioequivalence and safety of oseltamivir phosphate for suspension, provided by Shenzhen Beimei Pharmaceutical Co. Ltd. and manufactured b...
PMC3559838
core_pubmed_pmc
Glucuronidation by UGT1A1 Is the Dominant Pathway of the Metabolic Disposition of Belinostat in Liver Cancer Patients
Glucuronidation by UGT1A1 Is the Dominant Pathway of the Metabolic Disposition of Belinostat in Liver Cancer Patients Abstract Abstract Belinostat is a hydroxamate class HDAC inhibitor that has demonstrated activity in peripheral T-cell lymphoma and is undergoing clinical trials for non-hematologic malignancies. We stu...
PMC11687313
core_pubmed_pmc
Population Pharmacokinetics and Dosing Optimization of Norvancomycin for Chinese Patients with Community-Acquired Pneumonia
Population Pharmacokinetics and Dosing Optimization of Norvancomycin for Chinese Patients with Community-Acquired Pneumonia Abstract Abstract Purpose Determining the optimal dosage of norvancomycin (NVCM) for Chinese patients with community-acquired pneumonia (CAP) caused by gram-positive cocci remains uncertain. This ...
PMC10182601
core_pubmed_pmc
Biological evaluation of novel gemcitabine analog in patient-derived xenograft models of pancreatic cancer
Biological evaluation of novel gemcitabine analog in patient-derived xenograft models of pancreatic cancer Abstract Gemcitabine (Gem) has been a standard first-line drug for pancreatic cancer (PCa) treatment; however, Gem's rapid metabolism and systemic instability (short half-life) limit its clinical outcome. The obje...
PMC7226283
core_pubmed_pmc
Curcumin β‐D‐glucuronide exhibits anti–tumor effects on oxaliplatin‐resistant colon cancer with less toxicity in vivo
Curcumin β‐D‐glucuronide exhibits anti–tumor effects on oxaliplatin‐resistant colon cancer with less toxicity in vivo Abstract Abstract The NF‐kappa B (NF‐κB) pathway plays a pivotal role in tumor progression and chemoresistance, and its inhibition has been shown to suppress tumor growth in a variety of preclinical mod...
PMC11768447
core_pubmed_pmc
Sorafenib-Loaded Silica-Containing Redox Nanoparticle Decreases Tumorigenic Potential of Lewis Lung Carcinoma
Sorafenib-Loaded Silica-Containing Redox Nanoparticle Decreases Tumorigenic Potential of Lewis Lung Carcinoma Abstract Background: Orally administered sorafenib has shown limited improvement in overall survival for non-small-cell lung cancer patients, likely due to poor pharmacokinetics and adverse effects, including g...
PMC8617869
core_pubmed_pmc
Anti-Hyperglycaemic Evaluation of Buddleia indica Leaves Using In Vitro, In Vivo and In Silico Studies and Its Correlation with the Major Phytoconstituents
Anti-Hyperglycaemic Evaluation of Buddleia indica Leaves Using In Vitro, In Vivo and In Silico Studies and Its Correlation with the Major Phytoconstituents Abstract Buddleia indica Lam. is an ornamental evergreen shrub with few reports concerning its phytoconstituents and biological activities. Herein, the antihypergly...
PMC7894888
core_pubmed_pmc
Optimization of Busulfan Dosing Regimen in Pediatric Patients Using a Population Pharmacokinetic Model Incorporating GST Mutations
Optimization of Busulfan Dosing Regimen in Pediatric Patients Using a Population Pharmacokinetic Model Incorporating GST Mutations Abstract Purpose The aim of this study was to develop a novel busulfan dosing regimen, based on a population pharmacokinetic (PPK) model in Chinese children, and to achieve better area unde...
PMC9787481
core_pubmed_pmc
A Transversal Approach Combining In Silico, In Vitro and In Vivo Models to Describe the Metabolism of the Receptor Interacting Protein 1 Kinase Inhibitor Sibiriline
A Transversal Approach Combining In Silico, In Vitro and In Vivo Models to Describe the Metabolism of the Receptor Interacting Protein 1 Kinase Inhibitor Sibiriline Abstract Sibiriline is a novel drug inhibiting receptor-interacting protein 1 kinase (RIPK1) and necroptosis, a regulated form of cell death involved in se...
PMC5754736
core_pubmed_pmc
Subcutaneous golimumab for children with active polyarticular-course juvenile idiopathic arthritis: results of a multicentre, double-blind, randomised-withdrawal trial
Subcutaneous golimumab for children with active polyarticular-course juvenile idiopathic arthritis: results of a multicentre, double-blind, randomised-withdrawal trial Abstract Objective This report aims to determine the safety, pharmacokinetics (PK) and efficacy of subcutaneous golimumab in active polyarticular-course...
PMC12444786
core_pubmed_pmc
Rapid deprotection and purification of ceftaroline free base from its phosphoramidate prodrug
Rapid deprotection and purification of ceftaroline free base from its phosphoramidate prodrug Abstract Abstract Contemporary pharmaceutical design often incorporates functional groups to improve the pharmacokinetic/pharmacodynamic profile of a desired active chemical entity. These compounds are known as prodrugs. While...
PMC8800323
core_pubmed_pmc
Beta-lactam dosing during continuous renal replacement therapy: a survey of practices in french intensive care units
Beta-lactam dosing during continuous renal replacement therapy: a survey of practices in french intensive care units Abstract Background Little information is available on current practice in beta-lactam dosing during continuous renal replacement therapy (CRRT). Optimized dosing is essential for improving outcomes, and...
PMC9841300
core_pubmed_pmc
Design and conduct considerations for studies in patients with hepatic impairment
Design and conduct considerations for studies in patients with hepatic impairment Abstract Abstract Despite the liver being the primary site for clearance of xenobiotics utilizing a myriad of mechanisms ranging from cytochrome P450 enzyme pathways, glucuronidation, and biliary excretion, there is a dearth of informatio...
PMC9046595
core_pubmed_pmc
Pharmacodynamic Evaluation of Zoliflodacin Treatment of Neisseria gonorrhoeae Strains With Amino Acid Substitutions in the Zoliflodacin Target GyrB Using a Dynamic Hollow Fiber Infection Model
Pharmacodynamic Evaluation of Zoliflodacin Treatment of Neisseria gonorrhoeae Strains With Amino Acid Substitutions in the Zoliflodacin Target GyrB Using a Dynamic Hollow Fiber Infection Model Abstract Abstract Novel antimicrobials for effective treatment of uncomplicated gonorrhea are essential, and the first-in-class...
PMC4228420
core_pubmed_pmc
DCE@urLAB: a dynamic contrast-enhanced MRI pharmacokinetic analysis tool for preclinical data
DCE@urLAB: a dynamic contrast-enhanced MRI pharmacokinetic analysis tool for preclinical data Abstract Background DCE@urLAB is a software application for analysis of dynamic contrast-enhanced magnetic resonance imaging data (DCE-MRI). The tool incorporates a friendly graphical user interface (GUI) to interactively sele...
PMC9858383
core_pubmed_pmc
Antiretroviral Levels in the Cerebrospinal Fluid: The Effect of Inflammation and Genetic Variants
Antiretroviral Levels in the Cerebrospinal Fluid: The Effect of Inflammation and Genetic Variants Abstract Neurocognitive impairments are common in people living with HIV. Some conditions, such as chronic inflammation, astrocyte infection and an impaired blood–brain barrier (BBBi), along with host genetic variants in t...
PMC5080787
core_pubmed_pmc
Decreased absorption of midazolam in the stomach due to low pH induced by co-administration of Banha-sasim-tang
Decreased absorption of midazolam in the stomach due to low pH induced by co-administration of Banha-sasim-tang Abstract Abstract Objectives Banha-sasim-tang (BST), which consists of seven different herbs, is one of the most popular herbal formulae for treating gastrointestinal disorders in Eastern Asia. The commonly u...
PMC12567097
core_pubmed_pmc
1-Nitro-2-Phenylethane as a Multitarget Candidate for Cognitive and Psychiatric Disorders: Insights from In Silico and Behavioral Approaches
1-Nitro-2-Phenylethane as a Multitarget Candidate for Cognitive and Psychiatric Disorders: Insights from In Silico and Behavioral Approaches Abstract Background/Objectives : Neurological and psychiatric disorders share overlapping mechanisms, such as oxidative stress, neuroinflammation, and neurotransmitter imbalance. ...
PMC8602797
core_pubmed_pmc
Natural Products for the Management of Castration-Resistant Prostate Cancer: Special Focus on Nanoparticles Based Studies
Natural Products for the Management of Castration-Resistant Prostate Cancer: Special Focus on Nanoparticles Based Studies Abstract Prostate cancer is the most common type of cancer among men and the second most frequent cause of cancer-related mortality around the world. The progression of advanced prostate cancer to c...
PMC5732384
core_pubmed_pmc
Cellular pharmacodynamic effects of Pycnogenol® in patients with severe osteoarthritis: a randomized controlled pilot study
Cellular pharmacodynamic effects of Pycnogenol® in patients with severe osteoarthritis: a randomized controlled pilot study Abstract Abstract Background The standardized maritime pine bark extract (Pycnogenol®) has previously shown symptom alleviating effects in patients suffering from moderate forms of knee osteoarthr...
PMC9290854
core_pubmed_pmc
The Posology of Dupilumab in Pediatric Patients With Atopic Dermatitis
The Posology of Dupilumab in Pediatric Patients With Atopic Dermatitis Abstract Dupilumab demonstrated efficacy with an acceptable safety profile in two randomized, double‐blind, placebo‐controlled, parallel‐group, phase III trials in adolescents (12–17 years; LIBERTY AD ADOL) and children (6–11 years; LIBERTY AD PEDS)...
PMC10766679
core_pubmed_pmc
The Effects of Bariatric Surgery on Pharmacokinetics of Drugs: a Review of Current Evidence
The Effects of Bariatric Surgery on Pharmacokinetics of Drugs: a Review of Current Evidence Abstract Purpose of Review Obesity constitutes a major public health concern and has been recognized as an epidemic. To date, bariatric surgery remains the most effective way for substantial long-lasting weight loss in severe ob...
PMC10458652
core_pubmed_pmc
Effect of Gut Microbiota on the Pharmacokinetics of Nifedipine in Spontaneously Hypertensive Rats
Effect of Gut Microbiota on the Pharmacokinetics of Nifedipine in Spontaneously Hypertensive Rats Abstract Abstract The pharmacokinetic variability of nifedipine widely observed in the clinic cannot be fully explained by pharmacogenomics. As a new factor affecting drug metabolism, how the gut microbiota affects the pha...
PMC11344531
core_pubmed_pmc
Phase I studies of davoceticept (ALPN-202), a PD-L1-dependent CD28 co-stimulator and dual PD-L1/CTLA-4 inhibitor, as monotherapy and in combination with pembrolizumab in advanced solid tumors (NEON-1 and NEON-2)
Phase I studies of davoceticept (ALPN-202), a PD-L1-dependent CD28 co-stimulator and dual PD-L1/CTLA-4 inhibitor, as monotherapy and in combination with pembrolizumab in advanced solid tumors (NEON-1 and NEON-2) Abstract Abstract Background Davoceticept (ALPN-202) is an Fc fusion of a CD80 variant immunoglobulin domain...
PMC9877749
core_pubmed_pmc
Physiologically‐based pharmacokinetic modeling of remdesivir and its metabolites in pregnant women with COVID ‐19
Physiologically‐based pharmacokinetic modeling of remdesivir and its metabolites in pregnant women with COVID ‐19 Abstract Abstract Pregnant individuals are at high risk for severe illness from COVID‐19, and there is an urgent need to identify safe and effective therapeutics for this population. Remdesivir (RDV) is a S...
PMC6311297
core_pubmed_pmc
Effects of Plasma Albumin on the Pharmacokinetics of Esomeprazole in ICU Patients
Effects of Plasma Albumin on the Pharmacokinetics of Esomeprazole in ICU Patients Abstract Objectives To evaluate the effects of plasma albumin on pharmacokinetics of esomeprazole in ICU patients. Methods This study was performed in 32 consecutive intensive care unit (ICU) patients. They were divided into two groups ac...
PMC11126055
core_pubmed_pmc
Pharmacokinetic and Environmental Risk Assessment of Prime-2-CoV, a Non-Replicating Orf Virus-Based Vaccine against SARS-CoV-2
Pharmacokinetic and Environmental Risk Assessment of Prime-2-CoV, a Non-Replicating Orf Virus-Based Vaccine against SARS-CoV-2 Abstract Abstract Viral vector vaccines represent a substantial advancement in immunization technology, offering numerous benefits over traditional vaccine modalities. The Orf virus (ORFV) stra...
PMC9835135
core_pubmed_pmc
Predicting the correct dose in children: Role of computational Pediatric Physiological‐based pharmacokinetics modeling tools
Predicting the correct dose in children: Role of computational Pediatric Physiological‐based pharmacokinetics modeling tools Abstract Abstract The pharmacokinetics (PKs) and safety of medications in particular groups can be predicted using the physiologically‐based pharmacokinetic (PBPK) model. Using the PBPK model may...
PMC6680484
core_pubmed_pmc
Detection of 13 Ginsenosides (Rb1, Rb2, Rc, Rd, Re, Rf, Rg1, Rg3, Rh2, F1, Compound K, 20( S )-Protopanaxadiol, and 20( S )-Protopanaxatriol) in Human Plasma and Application of the Analytical Method to Human Pharmacokinetic Studies Following Two Week-Repeated Administration of Red Ginseng Extract
Detection of 13 Ginsenosides (Rb1, Rb2, Rc, Rd, Re, Rf, Rg1, Rg3, Rh2, F1, Compound K, 20( S )-Protopanaxadiol, and 20( S )-Protopanaxatriol) in Human Plasma and Application of the Analytical Method to Human Pharmacokinetic Studies Following Two Week-Repeated Administration of Red Ginseng Extract Abstract Abstract We a...
PMC10520167
core_pubmed_pmc
Towards Model-Informed Precision Dosing of Voriconazole: Challenging Published Voriconazole Nonlinear Mixed-Effects Models with Real-World Clinical Data
Towards Model-Informed Precision Dosing of Voriconazole: Challenging Published Voriconazole Nonlinear Mixed-Effects Models with Real-World Clinical Data Abstract Background and Objectives Model-informed precision dosing (MIPD) frequently uses nonlinear mixed-effects (NLME) models to predict and optimize therapy outcome...
PMC7615782
core_pubmed_pmc
Treosulfan Exposure Predicts Thalassemia-Free Survival in Patients with Beta Thalassemia Major Undergoing Allogeneic Hematopoietic Cell Transplantation
Treosulfan Exposure Predicts Thalassemia-Free Survival in Patients with Beta Thalassemia Major Undergoing Allogeneic Hematopoietic Cell Transplantation Abstract Abstract A toxicity-reduced conditioning regimen with treosulfan, fludarabine, and thiotepa in patients with high-risk β-thalassemia major has significantly im...
PMC12962861
core_pubmed_pmc
Turoctocog alfa pegol versus recombinant factor VIII-Fc fusion protein: a head-to-head pharmacokinetics comparison
Turoctocog alfa pegol versus recombinant factor VIII-Fc fusion protein: a head-to-head pharmacokinetics comparison Methods Laboratory methods Coamatic FVIII reagent (Chromogenix, Werfen, Barcelona, Spain) was used in a chromogenic substrate assay (CSA) on an ACL TOP750® (Werfen). No specific calibrator was used to cons...
PMC5794849
core_pubmed_pmc
Absorption, Distribution, Metabolism, and Excretion of [ 14 C]-Volixibat in Healthy Men: Phase 1 Open-Label Study
Absorption, Distribution, Metabolism, and Excretion of [ 14 C]-Volixibat in Healthy Men: Phase 1 Open-Label Study Abstract Abstract Background and Objectives Volixibat is a potent inhibitor of the apical sodium-dependent bile acid transporter in development for the treatment of nonalcoholic steatohepatitis. This phase ...