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PMC9700334
core_pubmed_pmc
Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration
Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration Abstract Abstract Purpose: Bilastine is a second-generation antihistamine that has been shown to be effective for treatment of allergic conjunctivitis. The objective of this study was to eva...
PMC10892118
core_pubmed_pmc
Pharmacokinetic Analysis of Levodropropizine and Its Potential Therapeutic Advantages Considering Eosinophil Levels and Clinical Indications
Pharmacokinetic Analysis of Levodropropizine and Its Potential Therapeutic Advantages Considering Eosinophil Levels and Clinical Indications Abstract Abstract Levodropropizine is a non-narcotic, non-centrally acting antitussive that inhibits the cough reflex triggered by neuropeptides. Despite the active clinical appli...
PMC12959021
core_pubmed_pmc
Population-based study of pharmacogenetics and pharmacokinetics in Southern African patients with multidrug-resistant tuberculosis (PoPG): a protocol for the Namibian cohort
Population-based study of pharmacogenetics and pharmacokinetics in Southern African patients with multidrug-resistant tuberculosis (PoPG): a protocol for the Namibian cohort Abstract Abstract Abstract Background Multidrug-resistant tuberculosis (MDR-TB) is an urgent public health challenge in Namibia, with profound soc...
PMC6974929
core_pubmed_pmc
Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Burkina Faso: an open label trial
Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Burkina Faso: an open label trial Abstract Abstract Background : Malaria during pregnancy is a major health risk for both the mother and the foetus. Pregnancy has been ...
PMC12447407
core_pubmed_pmc
Integrated experimental and computational study reveals enhanced antimicrobial efficacy of amoxicillin loaded in oleic acid nanoemulsion against multidrug-resistant Salmonella typhimurium
Integrated experimental and computational study reveals enhanced antimicrobial efficacy of amoxicillin loaded in oleic acid nanoemulsion against multidrug-resistant Salmonella typhimurium Abstract Abstract The escalating crisis of antimicrobial resistance (AMR) poses a severe threat to global health, demanding innovati...
PMC8060189
core_pubmed_pmc
Development of a Pediatric Relative Bioavailability/Bioequivalence Database and Identification of Putative Risk Factors Associated With Evaluation of Pediatric Oral Products
Development of a Pediatric Relative Bioavailability/Bioequivalence Database and Identification of Putative Risk Factors Associated With Evaluation of Pediatric Oral Products Abstract Abstract Generally, bioequivalence (BE) studies of drug products for pediatric patients are conducted in adults due to ethical reasons. G...
PMC5783347
core_pubmed_pmc
Safety and pharmacokinetics of the Fc-modified HIV-1 human monoclonal antibody VRC01LS: A Phase 1 open-label clinical trial in healthy adults
Safety and pharmacokinetics of the Fc-modified HIV-1 human monoclonal antibody VRC01LS: A Phase 1 open-label clinical trial in healthy adults Abstract Background VRC01 is a human broadly neutralizing monoclonal antibody (bnMAb) against the CD4-binding site of the HIV-1 envelope glycoprotein (Env) that is currently bein...
PMC6507620
core_pubmed_pmc
Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Poorly Water-Soluble Talinolol: Preparation, in vitro and in vivo Assessment
Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Poorly Water-Soluble Talinolol: Preparation, in vitro and in vivo Assessment Abstract Abstract Objective The aim of this study was to investigate the in vitro and in vivo performance of self-nanoemulsifying drug delivery systems (SNEDDSs) of talinolo...
PMC8532702
core_pubmed_pmc
Population Pharmacokinetic Modeling and Dose Optimization of Vancomycin in Chinese Patients with Augmented Renal Clearance
Population Pharmacokinetic Modeling and Dose Optimization of Vancomycin in Chinese Patients with Augmented Renal Clearance Abstract Abstract Patients with augmented renal clearance (ARC) have been described as having low vancomycin concentration. However, the pharmacokinetic model that best describes vancomycin in pati...
PMC8622898
core_pubmed_pmc
Disposition of Cefquinome in Turkeys ( Meleagris gallopavo ) Following Intravenous and Intramuscular Administration
Disposition of Cefquinome in Turkeys ( Meleagris gallopavo ) Following Intravenous and Intramuscular Administration Abstract Abstract The bioavailability and pharmacokinetics in turkeys of cefquinome (CFQ), a broad-spectrum 4th-generation cephalosporin antibiotic, were explored after a single injection of 2 mg/kg body ...
PMC5466632
core_pubmed_pmc
Clinical on-site monitoring of ß-lactam antibiotics for a personalized antibiotherapy
Clinical on-site monitoring of ß-lactam antibiotics for a personalized antibiotherapy Abstract An appropriate antibiotherapy is crucial for the safety and recovery of patients. Depending on the clinical conditions of patients, the required dose to effectively eradicate an infection may vary. An inadequate dosing not on...
PMC10661727
core_pubmed_pmc
Effects of Body Mass and Age on the Pharmacokinetics of Subcutaneous or Hyaluronidase-facilitated Subcutaneous Immunoglobulin G in Primary Immunodeficiency Diseases
Effects of Body Mass and Age on the Pharmacokinetics of Subcutaneous or Hyaluronidase-facilitated Subcutaneous Immunoglobulin G in Primary Immunodeficiency Diseases Abstract Purpose To assess the pharmacokinetics (PK) of subcutaneous immunoglobulin (SCIG) and hyaluronidase-facilitated SCIG (fSCIG) therapy across body m...
PMC10186384
core_pubmed_pmc
Optimizing and Evaluating the Transdermal Permeation of Hydrocortisone Transfersomes Formulation Based on Digital Analysis of the In Vitro Drug Release and Ex Vivo Studies
Optimizing and Evaluating the Transdermal Permeation of Hydrocortisone Transfersomes Formulation Based on Digital Analysis of the In Vitro Drug Release and Ex Vivo Studies Abstract Abstract Background : Transfersomes can be used to enhance transdermal drug delivery due to their flexibility and ability to incorporate va...
PMC7069653
core_pubmed_pmc
PK/PD modeling of 5‐hydroxytryptophan (5‐HTP) challenge test with cortisol measurement in serum and saliva
PK/PD modeling of 5‐hydroxytryptophan (5‐HTP) challenge test with cortisol measurement in serum and saliva Abstract Abstract This research was planned to build a Pharmacokinetic/Pharmacodynamic (PK/PD) model of 5‐hydroxytryptophan (5‐HTP) challenge study including a circadian rhythm component of cortisol and to predict...
PMC8230491
core_pubmed_pmc
Unexpected Salt/Cocrystal Polymorphism of the Ketoprofen–Lysine System: Discovery of a New Ketoprofen– l -Lysine Salt Polymorph with Different Physicochemical and Pharmacokinetic Properties
Unexpected Salt/Cocrystal Polymorphism of the Ketoprofen–Lysine System: Discovery of a New Ketoprofen– l -Lysine Salt Polymorph with Different Physicochemical and Pharmacokinetic Properties Abstract Ketoprofen– l -lysine salt (KLS) is a widely used nonsteroidal anti-inflammatory drug. Here, we studied deeply the solid-...
PMC12816744
core_pubmed_pmc
Influences of formulations and administration routes on docetaxel tissue distribution in mice
Influences of formulations and administration routes on docetaxel tissue distribution in mice Abstract Abstract Docetaxel (DTX) is an antimicrotubular chemotherapy drug widely used for treating various cancers. The objective of this study was to evaluate the impact of formulations and administration routes on DTX tissu...
PMC9252017
core_pubmed_pmc
Avatrombopag ethnic sensitivity analysis in chronic liver disease and thrombocytopenia patients: individual-level pooled analysis
Avatrombopag ethnic sensitivity analysis in chronic liver disease and thrombocytopenia patients: individual-level pooled analysis Abstract Abstract Introduction: Few data have been published on the ethnic sensitivity of effectiveness, pharmacokinetics (PK), and pharmacodynamics (PD) of avatrombopag for the management o...
PMC11360395
core_pubmed_pmc
Edaravone for the Treatment of Motor Neurone Disease: A Critical Review of Approved and Alternative Formulations against a Proposed Quality Target Product Profile
Edaravone for the Treatment of Motor Neurone Disease: A Critical Review of Approved and Alternative Formulations against a Proposed Quality Target Product Profile Abstract Abstract Edaravone is one of two main drugs for treating motor neurone disease (MND). This review proposes a specific quality target product profile...
PMC8647766
core_pubmed_pmc
Caffeine and EGCG Alleviate High-Trans Fatty Acid and High-Carbohydrate Diet-Induced NASH in Mice: Commonality and Specificity
Caffeine and EGCG Alleviate High-Trans Fatty Acid and High-Carbohydrate Diet-Induced NASH in Mice: Commonality and Specificity Abstract Caffeine and epigallocatechin-3-gallate (EGCG), which respectively, are the main functional extracts from coffee and green tea, and present protective effects against non-alcoholic fat...
PMC6848240
core_pubmed_pmc
Personalised Warfarin Dosing in Children Post-cardiac Surgery
Personalised Warfarin Dosing in Children Post-cardiac Surgery Abstract Abstract Warfarin dosing is challenging due to a multitude of factors affecting its pharmacokinetics (PK) and pharmacodynamics (PD). A novel personalised dosing algorithm predicated on a warfarin PK/PD model and incorporating CYP2C9 and VKORC1 genot...
PMC3128931
core_pubmed_pmc
A Workflow for Global Sensitivity Analysis of PBPK Models
A Workflow for Global Sensitivity Analysis of PBPK Models Abstract Physiologically based pharmacokinetic (PBPK) models have a potentially significant role in the development of a reliable predictive toxicity testing strategy. The structure of PBPK models are ideal frameworks into which disparate in vitro and in vivo da...
PMC6100312
core_pubmed_pmc
A UPLC-ESI-MS/MS Method for Simultaneous Quantitation of Chlorogenic Acid, Scutellarin, and Scutellarein in Rat Plasma: Application to a Comparative Pharmacokinetic Study in Sham-Operated and MCAO Rats after Oral Administration of Erigeron breviscapus Extract
A UPLC-ESI-MS/MS Method for Simultaneous Quantitation of Chlorogenic Acid, Scutellarin, and Scutellarein in Rat Plasma: Application to a Comparative Pharmacokinetic Study in Sham-Operated and MCAO Rats after Oral Administration of Erigeron breviscapus Extract Abstract Abstract Erigeron breviscapus , a traditional Chine...
PMC12890613
core_pubmed_pmc
Prediction of infliximab and anti-drug antibody concentrations in patients with inflammatory bowel disease using machine learning models with real-world data from a prospective cohort study
Prediction of infliximab and anti-drug antibody concentrations in patients with inflammatory bowel disease using machine learning models with real-world data from a prospective cohort study Abstract Abstract Background Although population pharmacokinetic models are the standard approach for identifying inter-individual...
PMC8070266
core_pubmed_pmc
Preclinical Evaluation of Recombinant Human IL15 Protein Fused with Albumin Binding Domain on Anti-PD-L1 Immunotherapy Efficiency and Anti-Tumor Immunity in Colon Cancer and Melanoma
Preclinical Evaluation of Recombinant Human IL15 Protein Fused with Albumin Binding Domain on Anti-PD-L1 Immunotherapy Efficiency and Anti-Tumor Immunity in Colon Cancer and Melanoma Abstract Abstract Simple Summary In this manuscript, we reported that a newly developed recombinant human IL15 fused with albumin binding...
PMC3234901
core_pubmed_pmc
Evaluation of pharmacokinetics, user handling, and tolerability of peginterferon alfa-2a (40 kDa) delivered via a disposable autoinjector device
Evaluation of pharmacokinetics, user handling, and tolerability of peginterferon alfa-2a (40 kDa) delivered via a disposable autoinjector device Abstract Abstract Background Peginterferon alfa-2a (40 kDa) is currently administered using a prefilled syringe. The peginterferon alfa-2a disposable autoinjector is a new saf...
PMC11444064
core_pubmed_pmc
Optimize Vancomycin Dose in Surgical Ward Patients with Augmented Renal Clearance Determined by Chronic Kidney Disease Epidemiology Collaboration Equation
Optimize Vancomycin Dose in Surgical Ward Patients with Augmented Renal Clearance Determined by Chronic Kidney Disease Epidemiology Collaboration Equation Abstract Background In the field of postoperative care, infections caused by Gram-positive bacteria pose a major clinical challenge. Vancomycin is a key therapeutic ...
PMC10499408
core_pubmed_pmc
A phase I study comparing the pharmacokinetics and safety of HS628 (tocilizumab biosimilar) and reference tocilizumab in healthy male subjects
A phase I study comparing the pharmacokinetics and safety of HS628 (tocilizumab biosimilar) and reference tocilizumab in healthy male subjects Abstract Abstract This study aimed to evaluate the pharmacokinetic (PK) similarity of the proposed biosimilar HS628 compared with the reference tocilizumab (Actemra®) and also t...
PMC3714141
core_pubmed_pmc
A Study of Potential Pharmacokinetic and Pharmacodynamic Interactions between Dextromethorphan/Quinidine and Memantine in Healthy Volunteers
A Study of Potential Pharmacokinetic and Pharmacodynamic Interactions between Dextromethorphan/Quinidine and Memantine in Healthy Volunteers Abstract Abstract Background and Objective: Dextromethorphan/quinidine (DMQ) is the first agent indicated for the treatment of pseudobulbar affect. Dextromethorphan, the active in...
PMC7340323
core_pubmed_pmc
Single-cell radioluminescence microscopy with two-fold higher sensitivity using dual scintillator configuration
Single-cell radioluminescence microscopy with two-fold higher sensitivity using dual scintillator configuration Abstract Radioluminescence microscopy (RLM) is an imaging technique that allows quantitative analysis of clinical radiolabeled drugs and probes in single cells. However, the modality suffers from slow data ac...
PMC7756259
core_pubmed_pmc
Pharmacodynamic monitoring of factor VIII replacement therapy in hemophilia A: Combining thrombin and plasmin generation
Pharmacodynamic monitoring of factor VIII replacement therapy in hemophilia A: Combining thrombin and plasmin generation Abstract Abstract Background Clinical severity of hemophilia A (HA) varies, possibly due to interplay of many factors in the hemostatic pathway. Pharmacokinetic monitoring of factor VIII (FVIII) repl...
PMC12090063
core_pubmed_pmc
Evaluating the Impact of Hepatic or Renal Impairment on Tanimilast ( CHF6001 ) Pharmacokinetics: Two Open‐Label, Parallel‐Group, Single‐Center Studies
Evaluating the Impact of Hepatic or Renal Impairment on Tanimilast ( CHF6001 ) Pharmacokinetics: Two Open‐Label, Parallel‐Group, Single‐Center Studies Abstract ABSTRACT Tanimilast is an inhaled phosphodiesterase‐4 inhibitor in development for chronic obstructive pulmonary disease and asthma. We conducted two studies to...
PMC5963640
core_pubmed_pmc
Discovery and Preclinical Development of Netarsudil, a Novel Ocular Hypotensive Agent for the Treatment of Glaucoma
Discovery and Preclinical Development of Netarsudil, a Novel Ocular Hypotensive Agent for the Treatment of Glaucoma Abstract Abstract Purpose: Rho-associated protein kinase (ROCK) inhibitors lower intraocular pressure (IOP) by increasing aqueous outflow through the trabecular meshwork (TM). The preclinical characteriza...
PMC9827845
core_pubmed_pmc
Active Pharmaceutical Ingredient Uptake by Zebrafish ( Danio rerio ) Oct2 (slc22a2) Transporter Expressed in Xenopus laevis Oocytes
Active Pharmaceutical Ingredient Uptake by Zebrafish ( Danio rerio ) Oct2 (slc22a2) Transporter Expressed in Xenopus laevis Oocytes Abstract Abstract Uptake of active pharmaceutical ingredients (APIs) across the gill epithelium of fish is via either a passive or facilitated transport process, with the latter being more...
PMC9794042
core_pubmed_pmc
Extended regimen of a levonorgestrel/ethinyl estradiol transdermal delivery system: Predicted serum hormone levels using a population pharmacokinetic model
Extended regimen of a levonorgestrel/ethinyl estradiol transdermal delivery system: Predicted serum hormone levels using a population pharmacokinetic model Abstract Abstract Objective This study employed population pharmacokinetic (popPK) models to predict levonorgestrel (LNG) and ethinyl estradiol (EE) exposure after ...
PMC11706418
core_pubmed_pmc
Is the GFR‐based scaling approach adequate for predicting pediatric renal clearance of drugs with passive tubular reabsorption? Insights from PBPK modeling
Is the GFR‐based scaling approach adequate for predicting pediatric renal clearance of drugs with passive tubular reabsorption? Insights from PBPK modeling Abstract Abstract Empirical maturation models (e.g., Johnson and Rhodin models) for glomerular filtration rate (GFR) are commonly used as scaling factors for predic...
PMC4761111
core_pubmed_pmc
NALDB: nucleic acid ligand database for small molecules targeting nucleic acid
NALDB: nucleic acid ligand database for small molecules targeting nucleic acid Abstract Nucleic acid ligand database (NALDB) is a unique database that provides detailed information about the experimental data of small molecules that were reported to target several types of nucleic acid structures. NALDB is the first li...
PMC6998185
core_pubmed_pmc
Intravenous versus subcutaneous route pharmacokinetics of paracetamol (acetaminophen) in palliative care patients: study protocol for a randomized trial (ParaSCIVPallia)
Intravenous versus subcutaneous route pharmacokinetics of paracetamol (acetaminophen) in palliative care patients: study protocol for a randomized trial (ParaSCIVPallia) Abstract Background Among palliative care (PC) patients who are administered paracetamol, the subcutaneous (SC) route is often an alternative to the i...
PMC9589728
core_pubmed_pmc
Physiologically-based pharmacokinetic model for pulmonary disposition of protein therapeutics in humans
Physiologically-based pharmacokinetic model for pulmonary disposition of protein therapeutics in humans Abstract Lung related disorders like COPD and Asthma, as well as various infectious diseases, form a major therapeutic area which would benefit from a predictive and adaptable mathematical model for describing pulmon...
PMC11496375
core_pubmed_pmc
Dose-Ranging Effects of the Intracerebral Administration of Atsttrin in Experimental Model of Parkinson’s Disease Induced by 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in Mice
Dose-Ranging Effects of the Intracerebral Administration of Atsttrin in Experimental Model of Parkinson’s Disease Induced by 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in Mice Abstract Abstract Parkinson’s disease is one of the most common neurodegenerative disorders characterized by a multitude of motor and n...
PMC10298338
core_pubmed_pmc
Optimization of Mass Spectrometry Imaging for Drug Metabolism and Distribution Studies in the Zebrafish Larvae Model: A Case Study with the Opioid Antagonist Naloxone
Optimization of Mass Spectrometry Imaging for Drug Metabolism and Distribution Studies in the Zebrafish Larvae Model: A Case Study with the Opioid Antagonist Naloxone Abstract Zebrafish (ZF; Danio rerio ) larvae have emerged as a promising in vivo model in drug metabolism studies. Here, we set out to ready this model f...
PMC12592279
core_pubmed_pmc
Influence of genetic polymorphisms on gefitinib pharmacokinetics and adverse drug reactions in non-small cell lung cancer patients
Influence of genetic polymorphisms on gefitinib pharmacokinetics and adverse drug reactions in non-small cell lung cancer patients Abstract Gefitinib is a first-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) used in the treatment of non-small cell lung cancer (NSCLC). It is metaboliz...
PMC6722910
core_pubmed_pmc
Physicochemical, Pharmacokinetic, and Toxicity Evaluation of Methoxy Poly(ethylene glycol)- b -Poly( d , l -Lactide) Polymeric Micelles Encapsulating Alpinumisoflavone Extracted from Unripe Cudrania tricuspidata Fruit
Physicochemical, Pharmacokinetic, and Toxicity Evaluation of Methoxy Poly(ethylene glycol)- b -Poly( d , l -Lactide) Polymeric Micelles Encapsulating Alpinumisoflavone Extracted from Unripe Cudrania tricuspidata Fruit Abstract Abstract Alpinumisoflavone, a major compound in unripe Cudrania tricuspidata fruit is reporte...
PMC8923729
core_pubmed_pmc
Quantitative systems pharmacology model for Alzheimer’s disease to predict the effect of aducanumab on brain amyloid
Quantitative systems pharmacology model for Alzheimer’s disease to predict the effect of aducanumab on brain amyloid Abstract Abstract Alzheimer's disease (AD) is an irreversible, progressive brain disorder that impairs memory and cognitive function. Dysregulation of the amyloid‐β (Aβ) pathway and amyloid plaque accumu...
PMC5771045
core_pubmed_pmc
In Vitro Metabolite Profiling of ADB-FUBINACA, A New Synthetic Cannabinoid
In Vitro Metabolite Profiling of ADB-FUBINACA, A New Synthetic Cannabinoid Abstract Metabolite profiling of novel psychoactive substances (NPS) is critical for documenting drug consumption. N-(1-amino-3,3-dimethyl-1-oxobutan-2-yl)-1-(4-fluorobenzyl)-1H-indazole-3-carboxamide (ADB-FUBINACA) is an emerging synthetic cann...
PMC6501043
core_pubmed_pmc
Tolerability and efficacy of durvalumab in Japanese patients with advanced solid tumors
Tolerability and efficacy of durvalumab in Japanese patients with advanced solid tumors Abstract Blockade of programmed cell death ligand‐1 with durvalumab has shown efficacy and safety in large, international studies of patients with advanced solid tumors. A phase 1, non‐randomized, open‐label multicenter study was in...
PMC8351941
core_pubmed_pmc
Mathematical modeling of N-803 treatment in SIV-infected non-human primates
Mathematical modeling of N-803 treatment in SIV-infected non-human primates Abstract Abstract Immunomodulatory drugs could contribute to a functional cure for Human Immunodeficiency Virus (HIV). Interleukin-15 (IL-15) promotes expansion and activation of CD8 + T cell and natural killer (NK) cell populations. In one stu...
PMC4215482
core_pubmed_pmc
Quercetin declines plasma exposure of metoprolol tartrate in the rat model
Quercetin declines plasma exposure of metoprolol tartrate in the rat model Abstract The study was undertaken to evaluate the effect of quercetin on the pharmacokinetics of Metoprolol tartrate. A single dose in vivo pharmacokinetic study was carried out in rat models. In this study, rats were treated with quercetin (10 ...
PMC12272518
core_pubmed_pmc
The feasibility of pharmacokinetic‐based dosing of hydroxyurea for children with sickle cell anaemia in Uganda: Baseline results of the alternative dosing and prevention of transfusions trial
The feasibility of pharmacokinetic‐based dosing of hydroxyurea for children with sickle cell anaemia in Uganda: Baseline results of the alternative dosing and prevention of transfusions trial Abstract Abstract Pharmacokinetic (PK)‐guided dosing of hydroxyurea for children with sickle cell anaemia (SCA) could optimize d...
PMC8938885
core_pubmed_pmc
First-in-human phase I clinical trial of a TLR4-binding DNA aptamer, ApTOLL: Safety and pharmacokinetics in healthy volunteers
First-in-human phase I clinical trial of a TLR4-binding DNA aptamer, ApTOLL: Safety and pharmacokinetics in healthy volunteers Abstract Abstract ApTOLL is an aptamer that antagonizes Toll-like receptor 4 and improves functional outcomes in models of ischemic stroke and myocardial infarction. The aim of this study was t...
PMC6349072
core_pubmed_pmc
pH as a potential therapeutic target to improve temozolomide antitumor efficacy : A mechanistic modeling study
pH as a potential therapeutic target to improve temozolomide antitumor efficacy : A mechanistic modeling study Abstract Abstract Despite intensive treatments including temozolomide (TMZ) administration, glioblastoma patient prognosis remains dismal and innovative therapeutic strategies are urgently needed. A systems ph...
PMC8175851
core_pubmed_pmc
Effects of Genetic Polymorphism in CYP2D6, CYP2C19, and the Organic Cation Transporter OCT1 on Amitriptyline Pharmacokinetics in Healthy Volunteers and Depressive Disorder Patients
Effects of Genetic Polymorphism in CYP2D6, CYP2C19, and the Organic Cation Transporter OCT1 on Amitriptyline Pharmacokinetics in Healthy Volunteers and Depressive Disorder Patients Abstract Abstract The tricyclic antidepressant amitriptyline is frequently prescribed but its use is limited by its narrow therapeutic rang...
PMC8301557
core_pubmed_pmc
First‐in‐human trial assessing the pharmacokinetic‐pharmacodynamic profile of a novel recombinant human chorionic gonadotropin in healthy women and men of reproductive age
First‐in‐human trial assessing the pharmacokinetic‐pharmacodynamic profile of a novel recombinant human chorionic gonadotropin in healthy women and men of reproductive age Abstract Abstract The purpose of this first‐in‐human trial was to examine the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of a novel re...
PMC6399183
core_pubmed_pmc
Palbociclib in combination with letrozole in patients with estrogen receptor–positive, human epidermal growth factor receptor 2–negative advanced breast cancer: PALOMA-2 subgroup analysis of Japanese patients
Palbociclib in combination with letrozole in patients with estrogen receptor–positive, human epidermal growth factor receptor 2–negative advanced breast cancer: PALOMA-2 subgroup analysis of Japanese patients Abstract Background In PALOMA-2, palbociclib–letrozole significantly improved progression-free survival (PFS) v...
PMC8388861
core_pubmed_pmc
Apply a Physiologically Based Pharmacokinetic Model to Promote the Development of Enrofloxacin Granules: Predict Withdrawal Interval and Toxicity Dose
Apply a Physiologically Based Pharmacokinetic Model to Promote the Development of Enrofloxacin Granules: Predict Withdrawal Interval and Toxicity Dose Abstract Enrofloxacin (ENR) granules were developed to prevent and control the infections caused by foodborne zoonotic intestinal pathogens in our previous studies. To p...
PMC7708381
core_pubmed_pmc
Application of a Two-Analyte Integrated Population Pharmacokinetic Model to Evaluate the Impact of Intrinsic and Extrinsic Factors on the Pharmacokinetics of Polatuzumab Vedotin in Patients with Non-Hodgkin Lymphoma
Application of a Two-Analyte Integrated Population Pharmacokinetic Model to Evaluate the Impact of Intrinsic and Extrinsic Factors on the Pharmacokinetics of Polatuzumab Vedotin in Patients with Non-Hodgkin Lymphoma Abstract Abstract Purpose The established two-analyte integrated population pharmacokinetic model was ap...
PMC12892838
core_pubmed_pmc
A Matched Case‐Control Study to Evaluate Predicted Drug Exposures and Neutropenia during Valganciclovir Prophylaxis in Pediatric Solid Organ Transplant Recipients
A Matched Case‐Control Study to Evaluate Predicted Drug Exposures and Neutropenia during Valganciclovir Prophylaxis in Pediatric Solid Organ Transplant Recipients Abstract ABSTRACT Background Neutropenia during valganciclovir (VGCV) prophylaxis for cytomegalovirus infection in pediatric solid organ transplant (pSOT) re...
PMC7915613
core_pubmed_pmc
Targeting for Success: Demonstrating Proof-of-Concept with Mechanistic Early Phase Clinical Pharmacology Studies for Disease-Modification in Neurodegenerative Disorders
Targeting for Success: Demonstrating Proof-of-Concept with Mechanistic Early Phase Clinical Pharmacology Studies for Disease-Modification in Neurodegenerative Disorders Abstract The clinical failure rate for disease-modifying treatments (DMTs) that slow or stop disease progression has been nearly 100% for the major neu...
PMC11434873
core_pubmed_pmc
Gene Therapy in the Light of Lifestyle Diseases: Budesonide, Acetaminophen and Simvastatin Modulates rAAV Transduction Efficiency
Gene Therapy in the Light of Lifestyle Diseases: Budesonide, Acetaminophen and Simvastatin Modulates rAAV Transduction Efficiency Abstract Abstract Recombinant AAV (rAAV) vectors are increasingly favored for gene therapy due to their useful features of vectorology, such as transfection of dividing and nondividing cells...
PMC5256876
core_pubmed_pmc
Pharmacokinetic Evaluation of a Single Intramuscular High Dose versus an Oral Long-Term Supplementation of Cholecalciferol
Pharmacokinetic Evaluation of a Single Intramuscular High Dose versus an Oral Long-Term Supplementation of Cholecalciferol Abstract Background and Objectives Vitamin D deficiency is frequent during the winter and occurs throughout the year in the elderly or patients suffering from autoimmune diseases. The objective of ...
PMC6587988
core_pubmed_pmc
Toward Better Understanding of Insulin Therapy by Translation of a PK‐PD Model to Visualize Insulin and Glucose Action Profiles
Toward Better Understanding of Insulin Therapy by Translation of a PK‐PD Model to Visualize Insulin and Glucose Action Profiles Abstract Abstract Insulin replacement therapy is a fundamental treatment for glycemic control for managing diabetes. The engineering of insulin analogues has focused on providing formulations ...
PMC12781760
core_pubmed_pmc
Condensation of fluconazole and zinc undecylanate particles using low-pressure RF plasma: a novel drug combination approach
Condensation of fluconazole and zinc undecylanate particles using low-pressure RF plasma: a novel drug combination approach Abstract Background Fluconazole (FCZ), a triazole antifungal agent, is routinely used in the treatment of various Candida infections, including oropharyngeal, esophageal, vulvovaginal candidiasis,...
PMC11099041
core_pubmed_pmc
Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs
Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs Abstract Background Proteolysis-targeting chimeras (PROTACs) are being developed for therapeutic use. However, they have poor pharmacokinetic profiles and their tissue distribution kinetics are not known. Methods A typical von Hippe...
PMC12515829
core_pubmed_pmc
Obesity: a challenge for emergency medical teams—a narrative review
Obesity: a challenge for emergency medical teams—a narrative review Abstract Abstract The global rise in obesity presents significant challenges for emergency medical services (EMS), particularly in prehospital care settings. This narrative review examines the multifaceted impact of obesity on emergency interventions, ...
PMC4950608
core_pubmed_pmc
Public health and chronic low chlordecone exposures in Guadeloupe; Part 2: Health impacts, and benefits of prevention
Public health and chronic low chlordecone exposures in Guadeloupe; Part 2: Health impacts, and benefits of prevention Abstract Background Inhabitants of Guadeloupe are chronically exposed to low doses of chlordecone via local food due to its past use in banana plantations. The corresponding health impacts have not been...
PMC12130357
core_pubmed_pmc
A Phase 1C, Open Label, Single Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of DM199 Administered Intravenously with a Polyvinyl Chloride Bag in Adult Healthy Subjects and Adults Recently Taking Angiotensin‐Converting Enzyme Inhibitors
A Phase 1C, Open Label, Single Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of DM199 Administered Intravenously with a Polyvinyl Chloride Bag in Adult Healthy Subjects and Adults Recently Taking Angiotensin‐Converting Enzyme Inhibitors Abstract Abstract This small phase 1C, open‐label...
PMC12001274
core_pubmed_pmc
Translational Physiologically Based Pharmacokinetic Modeling to Predict Human Pulmonary Kinetics After Lung Delivery
Translational Physiologically Based Pharmacokinetic Modeling to Predict Human Pulmonary Kinetics After Lung Delivery Abstract ABSTRACT Predicting human lung exposure with reasonable certainty of orally inhaled drugs based on preclinical studies remains a challenge for drug development. We have developed a comprehensive...
PMC5250654
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Safety of Entospletinib, a Novel pSYK Inhibitor, Following Single and Multiple Oral Dosing in Healthy Volunteers
Pharmacokinetics, Pharmacodynamics, and Safety of Entospletinib, a Novel pSYK Inhibitor, Following Single and Multiple Oral Dosing in Healthy Volunteers Abstract Background and Objectives Entospletinib is a selective, reversible, adenosine triphosphate-competitive small-molecule spleen tyrosine kinase (SYK) inhibitor t...
PMC5904350
core_pubmed_pmc
Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?
Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions? Abstract Abstract All drugs have both favorable therapeutic and untoward adverse effects. Conventional opioid analgesics possess both analgesia and adverse react...
PMC6950821
core_pubmed_pmc
Bioactivity Evaluation of a Novel Formulated Curcumin
Bioactivity Evaluation of a Novel Formulated Curcumin Abstract Abstract Curcumin has been used as a traditional medicine and/or functional food in several cultures because of its health benefits including anticancer properties. However, poor oral bioavailability of curcumin has limited its oral usage as a food suppleme...
PMC5599937
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling Suggests Limited Drug–Drug Interaction Between Clopidogrel and Dasabuvir
Physiologically Based Pharmacokinetic Modeling Suggests Limited Drug–Drug Interaction Between Clopidogrel and Dasabuvir Abstract Dasabuvir, a nonnucleoside NS5B polymerase inhibitor, is a sensitive substrate of cytochrome P450 (CYP) 2C8 with a potential for drug–drug interaction (DDI) with clopidogrel. A physiologicall...
PMC11602945
core_pubmed_pmc
Nedosiran population pharmacokinetic and pharmacodynamic modelling and simulation to guide clinical development and dose selection in patients with primary hyperoxaluria type 1
Nedosiran population pharmacokinetic and pharmacodynamic modelling and simulation to guide clinical development and dose selection in patients with primary hyperoxaluria type 1 Abstract Abstract Aim To characterize pharmacokinetic and pharmacodynamic profiles of nedosiran in patients with primary hyperoxaluria type 1 (...
PMC6570664
core_pubmed_pmc
Target attainment of cefotaxime in critically ill children with meningococcal septic shock as a model for cefotaxime dosing in severe pediatric sepsis
Target attainment of cefotaxime in critically ill children with meningococcal septic shock as a model for cefotaxime dosing in severe pediatric sepsis Abstract Abstract Reduced target attainment of β-lactam antibiotics is reported in critically ill patients. However, as target attainment of cefotaxime in severely ill p...
PMC7672844
core_pubmed_pmc
Systemic elucidation on the potential bioactive compounds and hypoglycemic mechanism of Polygonum multiflorum based on network pharmacology
Systemic elucidation on the potential bioactive compounds and hypoglycemic mechanism of Polygonum multiflorum based on network pharmacology Abstract Abstract Background Diabetes is a complex metabolic disease characterized by hyperglycemia, plaguing the whole world. However, the action mode of multi-component and multi...
PMC8143539
core_pubmed_pmc
Using Pharmacogenetics of Direct Oral Anticoagulants to Predict Changes in Their Pharmacokinetics and the Risk of Adverse Drug Reactions
Using Pharmacogenetics of Direct Oral Anticoagulants to Predict Changes in Their Pharmacokinetics and the Risk of Adverse Drug Reactions Abstract Abstract Dabigatran, rivaroxaban, apixaban, and edoxaban are direct oral anticoagulants (DOACs) that are increasingly used worldwide. Taking into account their widespread use...
PMC9999729
core_pubmed_pmc
APRIL: A double-blind, placebo-controlled, randomized, Phase Ib/IIa clinical study of ApTOLL for the treatment of acute ischemic stroke
APRIL: A double-blind, placebo-controlled, randomized, Phase Ib/IIa clinical study of ApTOLL for the treatment of acute ischemic stroke Abstract Abstract In the reperfusion era, a new paradigm of treating patients with endovascular treatment (EVT) and neuroprotective drugs is emerging as a promising therapeutic option ...
PMC7102878
core_pubmed_pmc
Comparison of Pharmacokinetics of Aprepitant in Healthy Chinese and Caucasian Subjects
Comparison of Pharmacokinetics of Aprepitant in Healthy Chinese and Caucasian Subjects Abstract Purpose Aprepitant is used to prevent nausea and vomiting associated with moderately and highly emetogenic chemotherapy. In this open-label, 2-period study, the safety, tolerability, and pharmacokinetics (PK) of aprepitant (...
PMC4767850
core_pubmed_pmc
The pharmacokinetics of high-dose methotrexate in people living with HIV on antiretroviral therapy
The pharmacokinetics of high-dose methotrexate in people living with HIV on antiretroviral therapy Abstract Purpose Clinical outcomes for lymphoma in people living with HIV (PLWH) are similar to those in the general public. However, a number of concerns remain including pharmacological interactions between cytotoxic ch...
PMC8215677
core_pubmed_pmc
Intra-Herb Interactions: Primary Metabolites in Coptidis Rhizoma Extract Improved the Pharmacokinetics of Oral Berberine Hydrochloride in Mice
Intra-Herb Interactions: Primary Metabolites in Coptidis Rhizoma Extract Improved the Pharmacokinetics of Oral Berberine Hydrochloride in Mice Abstract Primary plant metabolites can be used for artificial preparation of natural deep eutectic solvents (NADESs), which have strong dissolving capacity, good biocompatibilit...
PMC12812953
core_pubmed_pmc
Enhancing the structural stability of P29-targeted monoclonal antibodies via β-hydroxybutyrylation modification improves their therapeutic performance in alveolar echinococcosis
Enhancing the structural stability of P29-targeted monoclonal antibodies via β-hydroxybutyrylation modification improves their therapeutic performance in alveolar echinococcosis Abstract Background Alveolar echinococcosis (AE), a severe parasitic infection often likened to "parasitic cancer", still lacks effective trea...
PMC12471195
core_pubmed_pmc
Pharmacokinetic Profiling Using 3 H-Labeled Eggshell Membrane and Effects of Eggshell Membrane and Lysozyme Oral Supplementation on DSS-Induced Colitis and Human Gut Microbiota
Pharmacokinetic Profiling Using 3 H-Labeled Eggshell Membrane and Effects of Eggshell Membrane and Lysozyme Oral Supplementation on DSS-Induced Colitis and Human Gut Microbiota Abstract Abstract Eggshell membrane (ESM) is composed of approximately 90% protein. Our previous studies in healthy adults demonstrated that tw...
PMC7756545
core_pubmed_pmc
De‐mystifying the “Mixifusor”
De‐mystifying the “Mixifusor” Abstract Abstract Total intravenous anesthesia (TIVA) using a mixture of propofol and remifentanil in the same syringe has become an accepted technique in Pediatric Anesthesia. A survey by a group of respected UK anesthetists demonstrated a low incidence of serious complications, related t...
PMC9724289
core_pubmed_pmc
Inhaled seralutinib exhibits potent efficacy in models of pulmonary arterial hypertension
Inhaled seralutinib exhibits potent efficacy in models of pulmonary arterial hypertension Abstract Abstract Background Signalling through platelet-derived growth factor receptor (PDGFR), colony-stimulating factor 1 receptor (CSF1R) and mast/stem cell growth factor receptor kit (c-KIT) plays a critical role in pulmonary...
PMC7277591
core_pubmed_pmc
Urinary Pharmacokinetic and Pharmacodynamic Profiles of Fosfomycin against Extended-Spectrum β-Lactamase-Producing Escherichia coli with Canine Ex Vivo Modeling: A Pilot Study
Urinary Pharmacokinetic and Pharmacodynamic Profiles of Fosfomycin against Extended-Spectrum β-Lactamase-Producing Escherichia coli with Canine Ex Vivo Modeling: A Pilot Study Abstract Abstract Fosfomycin is a candidate drug for extended-spectrum β-lactamase (ESBL)-producing bacteria, but its efficacy is yet to be inve...
PMC11514964
core_pubmed_pmc
The preventive efficacy of lipid emulsion on the occurrence of local anesthetic systemic toxicity in patients receiving local infiltration analgesia for total joint arthroplasty
The preventive efficacy of lipid emulsion on the occurrence of local anesthetic systemic toxicity in patients receiving local infiltration analgesia for total joint arthroplasty Abstract Background Motor-sparing local infiltration analgesia (LIA) enhances recovery after total hip arthroplasty (THA) and total knee arthr...
PMC6133204
core_pubmed_pmc
Safety, Tolerability and Pharmacokinetics of MEDI8897, an Extended Half-life Single-dose Respiratory Syncytial Virus Prefusion F-targeting Monoclonal Antibody Administered as a Single Dose to Healthy Preterm Infants
Safety, Tolerability and Pharmacokinetics of MEDI8897, an Extended Half-life Single-dose Respiratory Syncytial Virus Prefusion F-targeting Monoclonal Antibody Administered as a Single Dose to Healthy Preterm Infants Abstract Background: MEDI8897 is a recombinant human monoclonal antibody being developed for prophylaxis...
PMC11429320
core_pubmed_pmc
Infliximab in Inflammatory Bowel Disease: Leveraging Physiologically Based Pharmacokinetic Modeling in the Clinical Context
Infliximab in Inflammatory Bowel Disease: Leveraging Physiologically Based Pharmacokinetic Modeling in the Clinical Context Abstract Abstract In this study, a physiologically based pharmacokinetic (PBPK) modeling framework was employed to explore infliximab exposure following intravenous (5 mg/kg) and subcutaneous admi...
PMC6190495
core_pubmed_pmc
Simultaneous determination of indapamide, perindopril and perindoprilat in human plasma or whole blood by UPLC-MS/MS and its pharmacokinetic application
Simultaneous determination of indapamide, perindopril and perindoprilat in human plasma or whole blood by UPLC-MS/MS and its pharmacokinetic application Abstract Simple and sensitive methods were developed for the determination of indapamide, perindopril and its active metabolite perindoprilat in human plasma or whole ...
PMC6461078
core_pubmed_pmc
Coptidis Rhizoma: a comprehensive review of its traditional uses, botany, phytochemistry, pharmacology and toxicology
Coptidis Rhizoma: a comprehensive review of its traditional uses, botany, phytochemistry, pharmacology and toxicology Abstract Abstract Context: Coptidis rhizome (CR), also known as Huanglian in Chinese, is the rhizome of Coptis chinensis Franch., C. deltoidea C.Y. Cheng et Hsiao, or C. teeta Wall (Ranunculaceae). It h...
PMC3834176
core_pubmed_pmc
Effect of 1-methyl-1,2,3,4-tetrahydroisoquinoline on the protective action of various antiepileptic drugs in the maximal electroshock-induced seizure model: a type II isobolographic analysis
Effect of 1-methyl-1,2,3,4-tetrahydroisoquinoline on the protective action of various antiepileptic drugs in the maximal electroshock-induced seizure model: a type II isobolographic analysis Abstract The aim of this study was to characterize the interaction between 1-methyl-1,2,3,4-tetrahydroisoquinoline (1-MeTHIQ—an e...
PMC11235165
core_pubmed_pmc
Delocalized quinolinium-macrocyclic peptides, an atypical chemotype for CNS penetration
Delocalized quinolinium-macrocyclic peptides, an atypical chemotype for CNS penetration Abstract Abstract Macrocyclic drugs can address an increasing range of molecular targets but enabling central nervous system (CNS) access to these drugs has been viewed as an intractable problem. We designed and synthesized a series...
PMC4520642
core_pubmed_pmc
Phase I study of OPB-51602, an oral inhibitor of signal transducer and activator of transcription 3, in patients with relapsed/refractory hematological malignancies
Phase I study of OPB-51602, an oral inhibitor of signal transducer and activator of transcription 3, in patients with relapsed/refractory hematological malignancies Abstract Abstract We carried out a multicenter dose-escalation phase I study of oral OPB-51602, a signal transducer and activator of transcription 3 phosph...
PMC7386805
core_pubmed_pmc
Optimized Nanostructured Lipid Carriers Integrated into In Situ Nasal Gel for Enhancing Brain Delivery of Flibanserin
Optimized Nanostructured Lipid Carriers Integrated into In Situ Nasal Gel for Enhancing Brain Delivery of Flibanserin Abstract Abstract Background and Aim Flibanserin (FLB) is a multifunctional serotonergic agent used for treating hypoactive sexual desire disorder in premenopausal women via oral administration. FLB has...
PMC11561919
core_pubmed_pmc
State of the art of real-life concentration monitoring of rifampicin and its implementation contextualized in resource-limited settings: the Tanzanian case
State of the art of real-life concentration monitoring of rifampicin and its implementation contextualized in resource-limited settings: the Tanzanian case Abstract Abstract The unique medical and socio-economic situation in each country affected by TB creates different epidemiological contexts, thus providing exploita...
PMC8604221
core_pubmed_pmc
Pharmacokinetically guided dosing of oral sorafenib in pediatric hepatocellular carcinoma: A simulation study
Pharmacokinetically guided dosing of oral sorafenib in pediatric hepatocellular carcinoma: A simulation study Abstract Abstract Sorafenib improves outcomes in adult hepatocellular carcinoma; however, hand foot skin reaction (HFSR) is a dose limiting toxicity of sorafenib that limits its use. HFSR has been associated wi...
PMC6765694
core_pubmed_pmc
Nonlinear Mixed‐Effects Model Development and Simulation Using nlmixr and Related R Open‐Source Packages
Nonlinear Mixed‐Effects Model Development and Simulation Using nlmixr and Related R Open‐Source Packages Abstract nlmixr is a free and open‐source R package for fitting nonlinear pharmacokinetic (PK) , pharmacodynamic (PD), joint PK‐ PD , and quantitative systems pharmacology mixed‐effects models. Currently, nlmixr is ...
PMC7098443
core_pubmed_pmc
Plasma Concentrations of Tranexamic Acid in Postpartum Women After Oral Administration
Plasma Concentrations of Tranexamic Acid in Postpartum Women After Oral Administration Abstract Effective concentration of tranexamic acid can be achieved within 1 hour after oral administration in postpartum women. OBJECTIVE: To evaluate the pharmacokinetics of tranexamic acid after oral administration to postpartum w...
PMC7136367
core_pubmed_pmc
Model-based Prediction of the Long-term Glucose-Lowering Effects of Ipragliflozin, a Selective Sodium–Glucose Cotransporter 2 (SGLT2) Inhibitor, in Patients with Type 2 Diabetes Mellitus
Model-based Prediction of the Long-term Glucose-Lowering Effects of Ipragliflozin, a Selective Sodium–Glucose Cotransporter 2 (SGLT2) Inhibitor, in Patients with Type 2 Diabetes Mellitus Abstract Abstract Introduction Sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors inhibit the reabsorption of glucose from t...
PMC12330118
core_pubmed_pmc
Randomized single-dose crossover comparative bioavailability study of two novel oral cannabidiol (CBD) formulations in healthy volunteers under fed conditions, compared to a standard CBD isolate capsule
Randomized single-dose crossover comparative bioavailability study of two novel oral cannabidiol (CBD) formulations in healthy volunteers under fed conditions, compared to a standard CBD isolate capsule Abstract Background This study aimed to compare the pharmacokinetics and relative bioavailability of two novel cannab...
PMC12272526
core_pubmed_pmc
Population pharmacokinetics and dosing of dispersible moxifloxacin formulation in children with rifampicin‐resistant tuberculosis
Population pharmacokinetics and dosing of dispersible moxifloxacin formulation in children with rifampicin‐resistant tuberculosis Abstract Aims Moxifloxacin is a priority drug for treating rifampicin‐resistant tuberculosis (RR‐TB). We assessed the pharmacokinetics of a child‐friendly, dispersible 100 mg tablet moxiflox...
PMC12370162
core_pubmed_pmc
Population Pharmacokinetic-Pharmacogenetic (PopPK-PGx) Model of Efavirenz in HIV-1-Infected Patients
Population Pharmacokinetic-Pharmacogenetic (PopPK-PGx) Model of Efavirenz in HIV-1-Infected Patients Abstract Abstract Background and objectives Efavirenz (EFV) exhibits substantial inter-patient pharmacokinetics (PK) variability. Polymorphisms in genes involved in EFV metabolism have been associated with EFV exposure,...