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PMC5760887
core_pubmed_pmc
Quantification of desloratadine in human plasma by LC-ESI-MS/MS and application to a pharmacokinetic study
Quantification of desloratadine in human plasma by LC-ESI-MS/MS and application to a pharmacokinetic study Abstract Abstract A simple, sensitive, and specific liquid chromatography tandem mass spectrometry (LC-MS/MS) method was developed for the quantification of desloratadine (DL) in human plasma using desloratadine-d...
PMC9122883
core_pubmed_pmc
Development of COVID-19 therapies: Nonclinical testing considerations
Development of COVID-19 therapies: Nonclinical testing considerations Abstract Therapies have been developed in the last couple of years to allow vaccination against, or treatment of patients with, COVID-19 using pathways such as Emergency Use Authorization (EUA) in the USA and Conditional Marketing Authorization (CMA)...
PMC11328074
core_pubmed_pmc
Determination of doxorubicin in plasma and tissues of mice by UPLC-MS/MS and its application to pharmacokinetic study
Determination of doxorubicin in plasma and tissues of mice by UPLC-MS/MS and its application to pharmacokinetic study Abstract Abstract A rapid and sensitive ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was established for the simultaneous determination of doxorubicin (DOX) ...
PMC6052413
core_pubmed_pmc
Influence of uridine diphosphate-glucuronosyltransferases (1A9) polymorphisms on mycophenolic acid pharmacokinetics in patients with renal transplant
Influence of uridine diphosphate-glucuronosyltransferases (1A9) polymorphisms on mycophenolic acid pharmacokinetics in patients with renal transplant Abstract Abstract Background: There are differences in pharmacokinetic of mycophenolic acid among individuals. The UGT1A9 enzyme is of special interest since it is the ma...
PMC12920435
core_pubmed_pmc
Efficacy and safety of desvenlafaxine in treating patients with major depressive disorder: a network meta-analysis
Efficacy and safety of desvenlafaxine in treating patients with major depressive disorder: a network meta-analysis Abstract Abstract Background and objective Desvenlafaxine (DVS), a commonly used serotonin-norepinephrine reuptake inhibitor (SNRI), is widely applied in the treatment of major depressive disorder (MDD). H...
PMC2954553
core_pubmed_pmc
Human Blood Concentrations of Cotinine, a Biomonitoring Marker for Tobacco Smoke, Extrapolated from Nicotine Metabolism in Rats and Humans and Physiologically Based Pharmacokinetic Modeling
Human Blood Concentrations of Cotinine, a Biomonitoring Marker for Tobacco Smoke, Extrapolated from Nicotine Metabolism in Rats and Humans and Physiologically Based Pharmacokinetic Modeling Abstract Abstract The present study defined a simplified physiologically based pharmacokinetic (PBPK) model for nicotine and its p...
PMC10362462
core_pubmed_pmc
Selection of potential natural compounds for poly-ADP-ribose polymerase (PARP) inhibition in glioblastoma therapy by in silico screening methods
Selection of potential natural compounds for poly-ADP-ribose polymerase (PARP) inhibition in glioblastoma therapy by in silico screening methods Abstract Glioblastoma (GBM), the most prevalent brain tumor, is one of the least treatable malignancies due to its propensity for intracranial spread, high proliferative poten...
PMC7946681
core_pubmed_pmc
Phase 1b Evaluation of Abaloparatide Solid Microstructured Transdermal System (Abaloparatide-sMTS) in Postmenopausal Women with Low Bone Mineral Density
Phase 1b Evaluation of Abaloparatide Solid Microstructured Transdermal System (Abaloparatide-sMTS) in Postmenopausal Women with Low Bone Mineral Density Abstract Abstract Background and Objective Abaloparatide, an anabolic osteoporosis treatment administered by subcutaneous (SC) injection, increases bone mineral densit...
PMC12718055
core_pubmed_pmc
Impact of Attaining an Aggressive Pharmacokinetic-Pharmacodynamic Target on the Clinical Efficacy of Continuous Infusion β-Lactam Therapy for Early Posttransplant Gram-Negative Infections in Critically Ill Orthotopic Liver Transplant Recipients: An Interim Analysis of a 3-Year Prospective, Observational Study
Impact of Attaining an Aggressive Pharmacokinetic-Pharmacodynamic Target on the Clinical Efficacy of Continuous Infusion β-Lactam Therapy for Early Posttransplant Gram-Negative Infections in Critically Ill Orthotopic Liver Transplant Recipients: An Interim Analysis of a 3-Year Prospective, Observational Study Abstract ...
PMC9859330
core_pubmed_pmc
The Yin-Yang Pharmacomicrobiomics on Treatment Response in Inflammatory Arthritides: A Narrative Review
The Yin-Yang Pharmacomicrobiomics on Treatment Response in Inflammatory Arthritides: A Narrative Review Abstract Abstract (1) Background: Gut microbiota (GM) is the set of microorganisms inhabiting the gastroenteric tract that seems to have a role in the pathogenesis of rheumatic diseases. Recently, many authors proved...
PMC5442175
core_pubmed_pmc
Oral Bioavailability and Plasma Disposition of Pefloxacin in Healthy Broiler Chickens
Oral Bioavailability and Plasma Disposition of Pefloxacin in Healthy Broiler Chickens Abstract The pharmacokinetics of pefloxacin after single 10 mg/kg BW intravenous (IV) and oral doses were studied in healthy broiler chickens. For 24 h, serial blood samples were obtained after IV and oral administration. Concentratio...
PMC9297311
core_pubmed_pmc
Specific staphylococcal cassette chromosome mec (SCC mec ) types and clonal complexes are associated with low-level amoxicillin/clavulanic acid and cefalotin resistance in methicillin-resistant Staphylococcus pseudintermedius
Specific staphylococcal cassette chromosome mec (SCC mec ) types and clonal complexes are associated with low-level amoxicillin/clavulanic acid and cefalotin resistance in methicillin-resistant Staphylococcus pseudintermedius Abstract Abstract Background Staphylococcus pseudintermedius is a common pathogen in dogs and ...
PMC12210374
core_pubmed_pmc
Is an extended dose of subcutaneous nadroparin anticoagulation equally safe and feasible compared to unfractionated heparin anticoagulation during extracorporeal membrane oxygenation in critically ill COVID-19 patients?
Is an extended dose of subcutaneous nadroparin anticoagulation equally safe and feasible compared to unfractionated heparin anticoagulation during extracorporeal membrane oxygenation in critically ill COVID-19 patients? Abstract Abstract Background Unfractionated heparin (UFH) is the traditional anticoagulant of choice...
PMC12825037
core_pubmed_pmc
Factor XIII Deficiency: A Review of Biology, Testing, and Treatment
Factor XIII Deficiency: A Review of Biology, Testing, and Treatment Abstract Factor XIII (FXIII) deficiency is a rare bleeding disorder characterized by unstable hemostatic clots due to defective fibrin cross‑linking. Congenital FXIII deficiency arises from variants in the F13A1 (FXIII-A subunit) or F13B (FXIII-B subun...
PMC9467812
core_pubmed_pmc
Optimization Method of an Antibreast Cancer Drug Candidate Based on Machine Learning
Optimization Method of an Antibreast Cancer Drug Candidate Based on Machine Learning Abstract Abstract Breast cancer is a common but serious and even lethal disease. Fortunately, compared with other cancers, breast cancer treatments currently are relatively well developed. The use of specific drugs is typically essenti...
PMC12968622
core_pubmed_pmc
Empagliflozin in paediatric heart failure: model-based optimisation of a pharmacokinetic bridging study
Empagliflozin in paediatric heart failure: model-based optimisation of a pharmacokinetic bridging study Abstract Aims Current therapy for paediatric heart failure is still unsatisfactory, and trials in this population have often failed. Here we apply a model-based approach to optimise the study design and increase the ...
PMC9656205
core_pubmed_pmc
In Vitro/In Vivo Translation of Synergistic Combination of MDM2 and MEK Inhibitors in Melanoma Using PBPK/PD Modelling: Part I
In Vitro/In Vivo Translation of Synergistic Combination of MDM2 and MEK Inhibitors in Melanoma Using PBPK/PD Modelling: Part I Abstract Translation of the synergy between the Siremadlin (MDM2 inhibitor) and Trametinib (MEK inhibitor) combination observed in vitro into in vivo synergistic efficacy in melanoma requires e...
PMC10087697
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Oral NLRP3 Inflammasome Inhibitor ZYIL1: First‐in‐Human Phase 1 Studies (Single Ascending Dose and Multiple Ascending Dose)
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Oral NLRP3 Inflammasome Inhibitor ZYIL1: First‐in‐Human Phase 1 Studies (Single Ascending Dose and Multiple Ascending Dose) Abstract Abstract ZYIL1 is a nucleotide‐binding oligomerization domain, leucine rich repeat and pyrin domain‐containing 3 (NLRP3...
PMC7496533
core_pubmed_pmc
Base and Covariate Population Pharmacokinetic Analyses of Dupilumab Using Phase 3 Data
Base and Covariate Population Pharmacokinetic Analyses of Dupilumab Using Phase 3 Data Abstract Abstract Population pharmacokinetic base and covariate models were developed to study functional dupilumab for regulatory submissions, using data from healthy volunteers and patients with moderate‐to‐severe atopic dermatitis...
PMC8047518
core_pubmed_pmc
mRNA therapeutics in cancer immunotherapy
mRNA therapeutics in cancer immunotherapy Abstract Abstract Synthetic mRNA provides a template for the synthesis of any given protein, protein fragment or peptide and lends itself to a broad range of pharmaceutical applications, including different modalities of cancer immunotherapy. With the ease of rapid, large scale...
PMC7144329
core_pubmed_pmc
Effects of naringenin on the pharmacokinetics of tofacitinib in rats
Effects of naringenin on the pharmacokinetics of tofacitinib in rats Abstract Abstract Context Naringenin and tofacitinib are often used together for treatment of rheumatoid arthritis in Chinese clinics. Objective This experiment investigates the effect of naringenin on the pharmacokinetics of tofacitinib in rats. Mate...
PMC11357621
core_pubmed_pmc
An Evaluation of Sex-Specific Pharmacokinetics and Bioavailability of Kokusaginine: An In Vitro and In Vivo Investigation
An Evaluation of Sex-Specific Pharmacokinetics and Bioavailability of Kokusaginine: An In Vitro and In Vivo Investigation Abstract Abstract Kokusaginine is a bioactive ingredient extracted from Ruta graveolens L., which has a range of biological activities. Its pharmacokinetic (PK) properties are particularly important...
PMC3947679
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Comparison of Chinese Herbal Ointment Liu-He-Dan and Micron Liu-He-Dan Ointment in Rats with Acute Pancreatitis
Pharmacokinetic and Pharmacodynamic Comparison of Chinese Herbal Ointment Liu-He-Dan and Micron Liu-He-Dan Ointment in Rats with Acute Pancreatitis Abstract Abstract Aim . To compare the pharmacokinetics and pharmacodynamics of herbal ointment Liu-He-Dan (LHD) and micron LHD (MLHD) in rats with acute pancreatitis (AP)....
PMC2938295
core_pubmed_pmc
Lacosamide for the prevention of partial onset seizures in epileptic adults
Lacosamide for the prevention of partial onset seizures in epileptic adults Abstract Lacosamide is a newly registered antiepileptic drug with dual mechanisms of action. It selectively enhances slow inactivation of voltage-gated sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibit...
PMC9032436
core_pubmed_pmc
Transdermal Glipizide Delivery System Based on Chitosan-Coated Deformable Liposomes: Development, Ex Vivo, and In Vivo Studies
Transdermal Glipizide Delivery System Based on Chitosan-Coated Deformable Liposomes: Development, Ex Vivo, and In Vivo Studies Abstract The current study aimed to develop and evaluate a sustained-release transdermal Glipizide (GLP) film to overcome its oral administration problems. Chitosan (CS)-coated deformable lipos...
PMC4350154
core_pubmed_pmc
Diagnosing malabsorption with systemic lipid profiling: pharmacokinetics of pentadecanoic acid and triheptadecanoic acid following oral administration in healthy subjects and subjects with cystic fibrosis
Diagnosing malabsorption with systemic lipid profiling: pharmacokinetics of pentadecanoic acid and triheptadecanoic acid following oral administration in healthy subjects and subjects with cystic fibrosis Abstract Abstract Objective: A Malabsorption Blood Test (MBT) is proposed as an alternative method to the 72-hour s...
PMC7601486
core_pubmed_pmc
The Role of Natural Compounds and their Nanocarriers in the Treatment of CNS Inflammation
The Role of Natural Compounds and their Nanocarriers in the Treatment of CNS Inflammation Abstract Neuroinflammation, which is involved in various inflammatory cascades in nervous tissues, can result in persistent and chronic apoptotic neuronal cell death and programmed cell death, triggering various degenerative disor...
PMC9326886
core_pubmed_pmc
Update of green tea interactions with cardiovascular drugs and putative mechanisms
Update of green tea interactions with cardiovascular drugs and putative mechanisms Abstract Abstract Many patients treated with cardiovascular (CV) drugs drink green tea (GT), either as a cultural tradition or persuaded of its putative beneficial effects for health. Yet, GT may affect the pharmacokinetics and pharmacod...
PMC7758017
core_pubmed_pmc
Donepezil and Rivastigmine: Pharmacokinetic Profile and Brain-targeting After Intramuscular Administration in Rats
Donepezil and Rivastigmine: Pharmacokinetic Profile and Brain-targeting After Intramuscular Administration in Rats Abstract Current palliative pharmacotherapy of Alzheimer’s disease based on the cholinergic hypothesis led to the development of four cholinesterase inhibitors. These compounds can bring prolongation of th...
PMC9802051
core_pubmed_pmc
Safety, Pharmacokinetics, and Efficacy of Olorinab, a Peripherally Acting, Highly Selective, Full Agonist of the Cannabinoid Receptor 2, in a Phase 2a Study of Patients With Chronic Abdominal Pain Associated With Crohn’s Disease
Safety, Pharmacokinetics, and Efficacy of Olorinab, a Peripherally Acting, Highly Selective, Full Agonist of the Cannabinoid Receptor 2, in a Phase 2a Study of Patients With Chronic Abdominal Pain Associated With Crohn’s Disease Abstract Abstract Background This randomized, open-label phase 2a study investigated the sa...
PMC9144238
core_pubmed_pmc
Virtual Prospection of Marine Cyclopeptides as Therapeutics by Means of Conceptual DFT and Computational ADMET
Virtual Prospection of Marine Cyclopeptides as Therapeutics by Means of Conceptual DFT and Computational ADMET Abstract Abstract Bioactive peptides are chemical compounds created through the covalent bonding of amino acids, known as amide or peptide bonds. Due to their unusual chemistry and various biological effects, ...
PMC12955047
core_pubmed_pmc
Design, synthesis, and evaluation of novel triazole-based carbohydrazide derivatives with notable antioxidant activity: an integrated experimental and DFT study
Design, synthesis, and evaluation of novel triazole-based carbohydrazide derivatives with notable antioxidant activity: an integrated experimental and DFT study Abstract Abstract A series of novel heterocyclic compounds based on 5-methyl-1-( p -tolyl)-1 H -1,2,3-triazole-4-carbohydrazide were designed, synthesized, and...
PMC6568180
core_pubmed_pmc
The Circadian Clock Gene Bmal1 Controls Intestinal Exporter MRP2 and Drug Disposition
The Circadian Clock Gene Bmal1 Controls Intestinal Exporter MRP2 and Drug Disposition Abstract Abstract The intestinal exporter MRP2 plays an important role in disposition and elimination of a wide range of drugs. Here, we aimed to clarify the impact of circadian clock on intestinal MRP2, and to determine the molecular...
PMC6950057
core_pubmed_pmc
Toxicity, Pharmacokinetics, and Gut Microbiome of Oral Administration of Sesterterpene MHO7 Derived from a Marine Fungus
Toxicity, Pharmacokinetics, and Gut Microbiome of Oral Administration of Sesterterpene MHO7 Derived from a Marine Fungus Abstract Sesterterpene MHO7 derived from mangrove fungus is a novel estrogen receptor degrader for the treatment of breast cancer. To explore its safety and pharmacokinetics in vivo, Log P/D values, ...
PMC11259781
core_pubmed_pmc
Three steps toward dose optimization for oncology dose finding
Three steps toward dose optimization for oncology dose finding Abstract Abstract Background Traditional dose selection for oncology registration trials typically employs a one- or two-step single maximum tolerated dose (MTD) approach. However, this approach may not be appropriate for molecularly targeted therapy, which...
PMC8985840
core_pubmed_pmc
Pharmacometrics Approaches and its Applications in Diabetes: An Overview
Pharmacometrics Approaches and its Applications in Diabetes: An Overview Abstract Abstract Type 2 diabetes mellitus is the most prevalent and progressive in nature. As the time progress, the multifaceted complications and comorbidities associated to diabetes worsen in the form of macrovascular or microvascular or both....
PMC3474726
core_pubmed_pmc
Detoxifying Antitumoral Drugs via Nanoconjugation: The Case of Gold Nanoparticles and Cisplatin
Detoxifying Antitumoral Drugs via Nanoconjugation: The Case of Gold Nanoparticles and Cisplatin Abstract Abstract Nanoparticles (NPs) have emerged as a potential tool to improve cancer treatment. Among the proposed uses in imaging and therapy, their use as a drug delivery scaffold has been extensively highlighted. Howe...
PMC7918775
core_pubmed_pmc
Quality by Design Applied Development of Immediate-Release Rabeprazole Sodium Dry-Coated Tablet
Quality by Design Applied Development of Immediate-Release Rabeprazole Sodium Dry-Coated Tablet Abstract The aim of this study was to develop immediate-release oral rabeprazole sodium tablets with rapid efficacy and gastric stability for the treatment of gastroesophageal reflux disease. Rabeprazole sodium is a commonly...
PMC11215529
core_pubmed_pmc
Tenofovir, emtricitabine, lamivudine and dolutegravir concentrations in plasma and urine following drug intake cessation in a randomized controlled directly observed pharmacokinetic trial to aid point-of-care testing
Tenofovir, emtricitabine, lamivudine and dolutegravir concentrations in plasma and urine following drug intake cessation in a randomized controlled directly observed pharmacokinetic trial to aid point-of-care testing Abstract Abstract Background Poor adherence to ART and pre-exposure prophylaxis (PrEP) can impact patie...
PMC8835811
core_pubmed_pmc
Floating Ricobendazole Delivery Systems: A 3D Printing Method by Co-Extrusion of Sodium Alginate and Calcium Chloride
Floating Ricobendazole Delivery Systems: A 3D Printing Method by Co-Extrusion of Sodium Alginate and Calcium Chloride Abstract Abstract At present, the use of benzimidazole drugs in veterinary medicine is strongly limited by both pharmacokinetics and formulative issues. In this research, the possibility of applying an ...
PMC12785687
core_pubmed_pmc
In Vivo Target Engagement Assessment of Nintedanib in a Double-Hit Bleomycin Lung Fibrosis Rat Model
In Vivo Target Engagement Assessment of Nintedanib in a Double-Hit Bleomycin Lung Fibrosis Rat Model Abstract Abstract Nintedanib is an anti-fibrotic medication endowed with a multi-kinase inhibitor profile and approved for the treatment of Idiopathic Pulmonary Fibrosis (IPF). Nintedanib is believed to inhibit mainly V...
PMC8048550
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of Mevidalen (LY3154207), a Centrally Acting Dopamine D1 Receptor‐Positive Allosteric Modulator (D1PAM), in Healthy Subjects
Safety, Tolerability, and Pharmacokinetics of Mevidalen (LY3154207), a Centrally Acting Dopamine D1 Receptor‐Positive Allosteric Modulator (D1PAM), in Healthy Subjects Abstract Abstract Activation of the brain dopamine D1 receptor has attracted attention because of its promising role in neuropsychiatric diseases. Altho...
PMC12540506
core_pubmed_pmc
PEGylated Asparaginase in Children with Acute Lymphoblastic Leukemia Treated within the AIEOP-BFM ALL 2009 Trial: Population Pharmacokinetics and Drug Exposure
PEGylated Asparaginase in Children with Acute Lymphoblastic Leukemia Treated within the AIEOP-BFM ALL 2009 Trial: Population Pharmacokinetics and Drug Exposure Abstract Abstract Background and Objectives Focusing on pharmacokinetic-derived individual dose-intensity parameter values (DIPs), we modeled the pharmacokineti...
PMC12257888
core_pubmed_pmc
A Kinetic Model of Antigen‐Dependent IgG Oligomerization and Complement Binding
A Kinetic Model of Antigen‐Dependent IgG Oligomerization and Complement Binding Abstract Abstract The classical complement pathway (CCP) is an essential part of the immune system, activated when complement protein C1 binds to IgG antibody oligomers on the surface of pathogens, infected or malignant cells, culminating i...
PMC12334052
core_pubmed_pmc
In Silico identification and modelling of FDA-approved drugs targeting T-type calcium channels
In Silico identification and modelling of FDA-approved drugs targeting T-type calcium channels Abstract Studies have shown that inhibition of the Ca v 3.1 T-type calcium channel can prevent or suppress neurological diseases, such as epileptic seizures and diabetic neuropathy. In this study, we aimed to use in silico si...
PMC9286720
core_pubmed_pmc
Robust physiologically based pharmacokinetic model of rifampicin for predicting drug–drug interactions via P‐glycoprotein induction and inhibition in the intestine, liver, and kidney
Robust physiologically based pharmacokinetic model of rifampicin for predicting drug–drug interactions via P‐glycoprotein induction and inhibition in the intestine, liver, and kidney Abstract Abstract P‐glycoprotein (P‐gp) is an efflux transporter that plays an important role in the pharmacokinetics of its substrate, a...
PMC4243878
core_pubmed_pmc
Effects of boceprevir and telaprevir on the pharmacokinetics of dolutegravir
Effects of boceprevir and telaprevir on the pharmacokinetics of dolutegravir Abstract Aims The aim was to evaluate the effect of boceprevir and telaprevir on dolutegravir pharmacokinetics (PK); the effect of dolutegravir on boceprevir and telaprevir PK was assessed through comparison with historical data for each hepat...
PMC8865449
core_pubmed_pmc
Comparison of rat and rabbit embryo–fetal developmental toxicity data for 379 pharmaceuticals: on the nature and severity of developmental effects
Comparison of rat and rabbit embryo–fetal developmental toxicity data for 379 pharmaceuticals: on the nature and severity of developmental effects Abstract Regulatory non-clinical safety testing of human pharmaceuticals typically requires embryo–fetal developmental toxicity (EFDT) testing in two species (one rodent and...
PMC3532009
core_pubmed_pmc
Use of natural molecules as anti-angiogenic inhibitors for vascular endothelial growth factor receptor
Use of natural molecules as anti-angiogenic inhibitors for vascular endothelial growth factor receptor Abstract Angiogenesis refers to the formation of new blood vessels, controlled by certain chemicals, which on stimulation repairs damaged cells or form new ones. Other chemicals, called angiogenesis inhibitors, signal...
PMC10697989
core_pubmed_pmc
Cross species extrapolation of the disruption of thyroid hormone synthesis by oxyfluorfen using in vitro data, physiologically based pharmacokinetic (PBPK), and thyroid hormone kinetics models
Cross species extrapolation of the disruption of thyroid hormone synthesis by oxyfluorfen using in vitro data, physiologically based pharmacokinetic (PBPK), and thyroid hormone kinetics models Abstract Highlights • A computational model combining kinetics of the oxyfluorofen, and thyroid hormones synthesis, distributio...
PMC7484917
core_pubmed_pmc
MTXPK.org: A Clinical Decision Support Tool Evaluating High‐Dose Methotrexate Pharmacokinetics to Inform Post‐Infusion Care and Use of Glucarpidase
MTXPK.org: A Clinical Decision Support Tool Evaluating High‐Dose Methotrexate Pharmacokinetics to Inform Post‐Infusion Care and Use of Glucarpidase Abstract Abstract Methotrexate (MTX), an antifolate, is administered at high doses to treat malignancies in children and adults. However, there is considerable interpatient...
PMC3302012
core_pubmed_pmc
Development and Stability Studies of Novel Liposomal Vancomycin Formulations
Development and Stability Studies of Novel Liposomal Vancomycin Formulations Abstract A promising strategy to improve the therapeutic efficiency of antimicrobial agents is targeted therapy. Although vancomycin has been considered a gold standard for the therapy of MRSA pneumonia, clinical failure rates have also been r...
PMC7597899
core_pubmed_pmc
Effect of heterocycle content on metal binding isostere coordination †
Effect of heterocycle content on metal binding isostere coordination † Abstract Bioisostere replacement is a core concept in modern medicinal chemistry and in this work new metal-binding isosteres (MBIs) are synthesized and evaluated for use in metalloenzyme inhibitors. Abstract Bioisostere replacement is a core concep...
PMC5915148
core_pubmed_pmc
A phase 1 study of lirilumab (antibody against killer immunoglobulin-like receptor antibody KIR2D; IPH2102) in patients with solid tumors and hematologic malignancies
A phase 1 study of lirilumab (antibody against killer immunoglobulin-like receptor antibody KIR2D; IPH2102) in patients with solid tumors and hematologic malignancies Abstract Abstract Purpose Anti-KIR monoclonal antibodies (mAbs) can enhance the antitumor responses of natural killer (NK) cells. We evaluated the safety...
PMC7532679
core_pubmed_pmc
Ultrasound-triggered therapeutic microbubbles enhance the efficacy of cytotoxic drugs by increasing circulation and tumor drug accumulation and limiting bioavailability and toxicity in normal tissues
Ultrasound-triggered therapeutic microbubbles enhance the efficacy of cytotoxic drugs by increasing circulation and tumor drug accumulation and limiting bioavailability and toxicity in normal tissues Abstract Abstract Most cancer patients receive chemotherapy at some stage of their treatment which makes improving the e...
PMC11326114
core_pubmed_pmc
Antibiotic discovery with artificial intelligence for the treatment of Acinetobacter baumannii infections
Antibiotic discovery with artificial intelligence for the treatment of Acinetobacter baumannii infections Abstract ABSTRACT Global challenges presented by multidrug-resistant Acinetobacter baumannii infections have stimulated the development of new treatment strategies. We reported that outer membrane protein W (OmpW) ...
PMC5737230
core_pubmed_pmc
Multiple Weekly Dalbavancin Dosing for the Treatment of Native Vertebral Osteomyelitis Caused by Methicillin-Resistant Staphylococcus Aureus : A Case Report
Multiple Weekly Dalbavancin Dosing for the Treatment of Native Vertebral Osteomyelitis Caused by Methicillin-Resistant Staphylococcus Aureus : A Case Report Abstract Patient: Male, 58 Final Diagnosis: Vertebral osteomyelitis Symptoms: Back pain Medication: Dalbavancin Clinical Procedure: — Specialty: Infectious Disease...
PMC12524187
core_pubmed_pmc
Optimizing Anti-PD1 Immunotherapy: An Overview of Pharmacokinetics, Biomarkers, and Therapeutic Drug Monitoring
Optimizing Anti-PD1 Immunotherapy: An Overview of Pharmacokinetics, Biomarkers, and Therapeutic Drug Monitoring Abstract Abstract Simple Summary The purpose of this review is to explore the therapeutic optimization of anti-PD-1 drugs by focusing on pharmacokinetic (PK) principles. The article discusses how interpatient...
PMC7993281
core_pubmed_pmc
Assessment of Target Engagement in a First‐in‐Human Trial with Sinbaglustat, an Iminosugar to Treat Lysosomal Storage Disorders
Assessment of Target Engagement in a First‐in‐Human Trial with Sinbaglustat, an Iminosugar to Treat Lysosomal Storage Disorders Abstract In this first‐in‐human study, the tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of single and multiple oral doses of sinbaglustat, a dual inhibitor of glucosylceramid...
PMC8504811
core_pubmed_pmc
Effects of vancomycin‐induced gut microbiome alteration on the pharmacodynamics of metformin in healthy male subjects
Effects of vancomycin‐induced gut microbiome alteration on the pharmacodynamics of metformin in healthy male subjects Abstract Abstract Metformin is a major treatment for type 2 diabetes. This study was conducted to investigate the impact of gut microbiome dysbiosis on the pharmacokinetics and antihyperglycemic effects...
PMC6889675
core_pubmed_pmc
Mangosteen ( Garcinia mangostana ) flesh supplementation attenuates biochemical and morphological changes in the liver and kidney of high fat diet-induced obese rats
Mangosteen ( Garcinia mangostana ) flesh supplementation attenuates biochemical and morphological changes in the liver and kidney of high fat diet-induced obese rats Abstract Background Mangosteen is a native fruit from Southeast Asia. It is rich in phenolic compounds such as xanthones, anthocyanins and phenolic acids....
PMC3144367
core_pubmed_pmc
AAPS Workshop Report: Strategies to Address Therapeutic Protein–Drug Interactions during Clinical Development
AAPS Workshop Report: Strategies to Address Therapeutic Protein–Drug Interactions during Clinical Development Abstract Therapeutic proteins (TPs) are increasingly combined with small molecules and/or with other TPs. However preclinical tools and in vitro test systems for assessing drug interaction potential of TPs such...
PMC6935304
core_pubmed_pmc
A Novel Liposomal S-Propargyl-Cysteine: A Sustained Release of Hydrogen Sulfide Reducing Myocardial Fibrosis via TGF-β1/Smad Pathway
A Novel Liposomal S-Propargyl-Cysteine: A Sustained Release of Hydrogen Sulfide Reducing Myocardial Fibrosis via TGF-β1/Smad Pathway Abstract Purpose S-propargyl-cysteine (SPRC; alternatively known as ZYZ-802) is a novel modulator of endogenous tissue H 2 S concentrations with known cardioprotective and anti-inflammato...
PMC10303435
core_pubmed_pmc
Plasma and Urine Pharmacokinetics of Oral Fosfomycin Tromethamine in Dogs
Plasma and Urine Pharmacokinetics of Oral Fosfomycin Tromethamine in Dogs Abstract Abstract Simple Summary Fosfomycin tromethamine, an oral formulation of Fosfomycin, is the most commonly used formulation in humans due to its improved oral bioavailability. However, the information on Fosfomycin tromethamine in dogs is ...
PMC5066705
core_pubmed_pmc
Assessment of Disease‐Related Therapeutic Protein Drug‐Drug Interaction for Etrolizumab in Patients With Moderately to Severely Active Ulcerative Colitis
Assessment of Disease‐Related Therapeutic Protein Drug‐Drug Interaction for Etrolizumab in Patients With Moderately to Severely Active Ulcerative Colitis Abstract Abstract The efficacy and safety of etrolizumab, a humanized IgG1 mAb, were evaluated in patients with ulcerative colitis (UC) in a phase 2 study (EUCALYPTUS...
PMC11149109
core_pubmed_pmc
Validation of single nucleotide polymorphisms potentially related to R-CHOP resistance in diffuse large B-cell lymphoma patients
Validation of single nucleotide polymorphisms potentially related to R-CHOP resistance in diffuse large B-cell lymphoma patients Abstract Aim: Diffuse large B-cell lymphoma (DLBCL) is the most common B-cell non-Hodgkin lymphoma (NHL). Despite the availability of clinical and molecular algorithms applied for the predict...
PMC10967220
core_pubmed_pmc
Moderate- to vigorous-intensity physical activities for hemophilia A patients during low-dose pharmacokinetic-guided extended half-life factor VIII prophylaxis
Moderate- to vigorous-intensity physical activities for hemophilia A patients during low-dose pharmacokinetic-guided extended half-life factor VIII prophylaxis Abstract Abstract Background Low-dose pharmacokinetic (PK)-guided extended half-life (EHL) factor VIII (FVIII) prophylaxis can reduce the bleeding risk in hemop...
PMC11782195
core_pubmed_pmc
Pharmacodynamic characteristics and influencing factors of tapentadol for chronic pain relief under dose titration
Pharmacodynamic characteristics and influencing factors of tapentadol for chronic pain relief under dose titration Abstract Objective The aim of this study was to establish a pharmacodynamic model of tapentadol analgesia under dose titration conditions, to quantitatively analyze the time-effect relationship of the drug...
PMC9740200
core_pubmed_pmc
Phase 1 and 2 Randomized Clinical Studies Determine Lack of Efficacy for Anti-IL-17C Antibody MOR106 in Moderate–Severe Atopic Dermatitis
Phase 1 and 2 Randomized Clinical Studies Determine Lack of Efficacy for Anti-IL-17C Antibody MOR106 in Moderate–Severe Atopic Dermatitis Abstract Abstract Interleukin 17C (IL-17C) modulates epithelial inflammation and has a possible role in atopic dermatitis (AD) pathology. Four randomized clinical studies (Phase 1 an...
PMC12414044
core_pubmed_pmc
Population Pharmacokinetic and Pharmacodynamic Modelling and Simulation for Nedosiran Clinical Development and Dose Guidance in Pediatric Patients with Primary Hyperoxaluria Type 1
Population Pharmacokinetic and Pharmacodynamic Modelling and Simulation for Nedosiran Clinical Development and Dose Guidance in Pediatric Patients with Primary Hyperoxaluria Type 1 Abstract Background and Objectives Nedosiran (Rivfloza ® ) is an RNA interference (RNAi) therapy approved for individuals aged ≥ 2 years wi...
PMC8285519
core_pubmed_pmc
Evaluation of the Pharmacokinetics of Trazpiroben (TAK-906), a Peripherally Selective D 2 /D 3 Dopamine Receptor Antagonist, in the Presence and Absence of Itraconazole, a Potent CYP 3A4 Inhibitor
Evaluation of the Pharmacokinetics of Trazpiroben (TAK-906), a Peripherally Selective D 2 /D 3 Dopamine Receptor Antagonist, in the Presence and Absence of Itraconazole, a Potent CYP 3A4 Inhibitor Abstract Purpose Treatment options for gastroparesis, such as metoclopramide and domperidone, are limited because of safety...
PMC5794835
core_pubmed_pmc
Model-based optimization of G-CSF treatment during cytotoxic chemotherapy
Model-based optimization of G-CSF treatment during cytotoxic chemotherapy Abstract Purpose Although G-CSF is widely used to prevent or ameliorate leukopenia during cytotoxic chemotherapies, its optimal use is still under debate and depends on many therapy parameters such as dosing and timing of cytotoxic drugs and G-CS...
PMC11256175
core_pubmed_pmc
Tricaprylin‐based drug crystalline suspension for intramuscular long‐acting delivery of entecavir with alleviated local inflammation
Tricaprylin‐based drug crystalline suspension for intramuscular long‐acting delivery of entecavir with alleviated local inflammation Abstract Abstract In order to ensure prolonged pharmacokinetic profile along with local tolerability at the injection site, tricaprylin‐based drug crystalline suspension (TS) was designed...
PMC9720577
core_pubmed_pmc
Suspected adverse drug reactions of the type 2 antidiabetic drug class dipeptidyl‐peptidase IV inhibitors (DPP4i): Can polypharmacology help explain?
Suspected adverse drug reactions of the type 2 antidiabetic drug class dipeptidyl‐peptidase IV inhibitors (DPP4i): Can polypharmacology help explain? Abstract Abstract To interpret the relationship between the polypharmacology of dipeptidyl‐peptidase IV inhibitors (DPP4i) and their suspected adverse drug reaction (ADR)...
PMC7808974
core_pubmed_pmc
Population Pharmacokinetics of Clotting Factor Concentrates and Desmopressin in Hemophilia
Population Pharmacokinetics of Clotting Factor Concentrates and Desmopressin in Hemophilia Abstract Abstract Hemophilia A and B are bleeding disorders caused by a deficiency of clotting factor VIII and IX, respectively. Patients with severe hemophilia (< 0.01 IU mL −1 ) and some patients with moderate hemophilia (0.01–...
PMC9186144
core_pubmed_pmc
Scientific rationale for a higher dose of nusinersen
Scientific rationale for a higher dose of nusinersen Abstract Abstract Objective The long‐term favorable safety profile of nusinersen provides an opportunity to consider a higher dose. We report on the relationships between nusinersen cerebrospinal fluid (CSF) exposure, biomarker levels, and clinical efficacy. Methods ...
PMC8166722
core_pubmed_pmc
Subcellular spatio-temporal intravital kinetics of aflatoxin B 1 and ochratoxin A in liver and kidney
Subcellular spatio-temporal intravital kinetics of aflatoxin B 1 and ochratoxin A in liver and kidney Abstract Abstract Local accumulation of xenobiotics in human and animal tissues may cause adverse effects. Large differences in their concentrations may exist between individual cell types, often due to the expression ...
PMC7500464
core_pubmed_pmc
Evaluating the Therapeutic Efficacy of Si-Wu-Tang Decoction and Concentrated Extract in Follicular Maldevelopment-Related Menstrual Disorders Through Pharmacokinetic/Pharmacodynamic Studies
Evaluating the Therapeutic Efficacy of Si-Wu-Tang Decoction and Concentrated Extract in Follicular Maldevelopment-Related Menstrual Disorders Through Pharmacokinetic/Pharmacodynamic Studies Abstract Abstract Si-Wu-Tang (SWT), a traditional Chinese formula, is commonly used to relieve menstrual discomfort and climacteri...
PMC6003532
core_pubmed_pmc
Inhaled glycopyrrolate for the treatment of chronic obstructive pulmonary disease
Inhaled glycopyrrolate for the treatment of chronic obstructive pulmonary disease Abstract Abstract Long-acting muscarinic antagonists (LAMAs), along with long-acting β 2 -agonists (LABAs), are the mainstay for treatment of patients with COPD. Glycopyrrolate, or glycopyrronium bromide, like other LAMAs, inhibits parasy...
PMC11366951
core_pubmed_pmc
Medicinal potential of embelin and its nanoformulations: An update on the molecular mechanism and various applications
Medicinal potential of embelin and its nanoformulations: An update on the molecular mechanism and various applications Abstract Abstract Natural herbs have garnered significant research recently as their components target multiple disease signaling pathways, making them highly potential for various disease prevention a...
PMC10335428
core_pubmed_pmc
Identifying biomarkers of treatment response to ciclosporin in atopic dermatitis through multiomic predictive modelling: DERMATOMICS study protocol
Identifying biomarkers of treatment response to ciclosporin in atopic dermatitis through multiomic predictive modelling: DERMATOMICS study protocol Abstract Abstract Introduction There is a need to optimise the management of atopic dermatitis (AD), improving the efficacy of treatments and reducing the toxicity associat...
PMC8358502
core_pubmed_pmc
Differences in the placental pharmacokinetics of vedolizumab and ustekinumab during pregnancy in women with inflammatory bowel disease: a prospective multicentre study
Differences in the placental pharmacokinetics of vedolizumab and ustekinumab during pregnancy in women with inflammatory bowel disease: a prospective multicentre study Abstract Background: Vedolizumab demonstrated different placental pharmacokinetics than other immunoglobulin G1 antibodies, leading to lower drug levels...
PMC6267540
core_pubmed_pmc
A Physiologically-Based Pharmacokinetic Model to Describe Ciprofloxacin Pharmacokinetics Over the Entire Span of Life
A Physiologically-Based Pharmacokinetic Model to Describe Ciprofloxacin Pharmacokinetics Over the Entire Span of Life Abstract Abstract Background Physiologically-based pharmacokinetic (PBPK) modeling has received growing interest as a useful tool for the assessment of drug pharmacokinetics by continuous knowledge inte...
PMC11531812
core_pubmed_pmc
Pharmacokinetics of once-daily darunavir/ritonavir in second-line treatment in African children with HIV
Pharmacokinetics of once-daily darunavir/ritonavir in second-line treatment in African children with HIV Abstract Abstract Background Darunavir is a potent HIV protease inhibitor with a high barrier to resistance. We conducted a nested pharmacokinetic sub-study within CHAPAS-4 to evaluate darunavir exposure in African ...
PMC12024055
core_pubmed_pmc
Influence of N-Acetyl-L-Cysteine on the Pharmacokinetics and Antibacterial Activity of Marbofloxacin in Chickens
Influence of N-Acetyl-L-Cysteine on the Pharmacokinetics and Antibacterial Activity of Marbofloxacin in Chickens Abstract Abstract Background/Objectives : Marbofloxacin, a second-generation fluoroquinolone, is used to control economically significant poultry diseases caused by pathogenic bacteria such as Staphylococcus...
PMC12812960
core_pubmed_pmc
Preclinical pharmacological profiles of cofrogliptin, a novel and bi-weekly DPP-4 inhibitor
Preclinical pharmacological profiles of cofrogliptin, a novel and bi-weekly DPP-4 inhibitor Abstract Abstract Objective DPP-4 inhibitors are now established agents for glycaemic control in diabetes. Herein, this study systematically characterized cofrogliptin and elucidated its pharmacology, pharmacokinetics, and thera...
PMC7214642
core_pubmed_pmc
Mechanistic Multiscale Pharmacokinetic Model for the Anticancer Drug 2’,2’‐difluorodeoxycytidine (Gemcitabine) in Pancreatic Cancer
Mechanistic Multiscale Pharmacokinetic Model for the Anticancer Drug 2’,2’‐difluorodeoxycytidine (Gemcitabine) in Pancreatic Cancer Abstract Abstract The aim of this work is to build a mechanistic multiscale pharmacokinetic model for the anticancer drug 2’,2’‐difluorodeoxycytidine (gemcitabine, dFdC), able to describe ...
PMC11091825
core_pubmed_pmc
The Basis for Weekly Insulin Therapy: Evolving Evidence With Insulin Icodec and Insulin Efsitora Alfa
The Basis for Weekly Insulin Therapy: Evolving Evidence With Insulin Icodec and Insulin Efsitora Alfa Abstract Abstract Basal insulin continues to be a vital part of therapy for many people with diabetes. First attempts to prolong the duration of insulin formulations were through the development of suspensions that req...
PMC5732797
core_pubmed_pmc
Pharmacodynamic and pharmacokinetic neoadjuvant study of hedgehog pathway inhibitor Sonidegib (LDE-225) in men with high-risk localized prostate cancer undergoing prostatectomy
Pharmacodynamic and pharmacokinetic neoadjuvant study of hedgehog pathway inhibitor Sonidegib (LDE-225) in men with high-risk localized prostate cancer undergoing prostatectomy Abstract Purpose To determine the pharmacodynamic effects of Sonidegib (LDE-225) in prostate tumor tissue from men with high-risk localized pro...
PMC4972814
core_pubmed_pmc
Etravirine Pharmacokinetics in HIV-Infected Pregnant Women
Etravirine Pharmacokinetics in HIV-Infected Pregnant Women Abstract Abstract Background: The study goal was to describe etravirine pharmacokinetics during pregnancy and postpartum in HIV-infected women. Methods: IMPAACT P1026s and PANNA are on-going, non-randomized, open-label, parallel-group, multi-center phase-IV pro...
PMC8841519
core_pubmed_pmc
Utilization of physiologically‐based pharmacokinetic model to assess disease‐mediated therapeutic protein‐disease‐drug interaction in immune‐mediated inflammatory diseases
Utilization of physiologically‐based pharmacokinetic model to assess disease‐mediated therapeutic protein‐disease‐drug interaction in immune‐mediated inflammatory diseases Abstract Abstract It is known that interleukin‐6 (IL‐6) can significantly modulate some key drug‐metabolizing enzymes, such as phase I cytochrome P4...
PMC10870849
core_pubmed_pmc
Phase 3 Open-Label Clinical Trial of Elexacaftor/Tezacaftor/Ivacaftor in Children Aged 2–5 Years with Cystic Fibrosis and at Least One F508del Allele
Phase 3 Open-Label Clinical Trial of Elexacaftor/Tezacaftor/Ivacaftor in Children Aged 2–5 Years with Cystic Fibrosis and at Least One F508del Allele Abstract Abstract Rationale Elexacaftor/tezacaftor/ivacaftor (ELX/TEZ/IVA) has been shown to be safe and effective in people with cystic fibrosis (CF) aged ⩾6 years with ...
PMC4544054
core_pubmed_pmc
Model-Based Once-Daily Darunavir/Ritonavir Dosing Recommendations in Pediatric HIV-1-Infected Patients Aged ≥ 3 to <12 Years
Model-Based Once-Daily Darunavir/Ritonavir Dosing Recommendations in Pediatric HIV-1-Infected Patients Aged ≥ 3 to <12 Years Abstract An existing population pharmacokinetic model of darunavir in adults was updated using pediatric data from two studies evaluating weight-based, once-daily dosing of darunavir/ritonavir (A...
PMC7030895
core_pubmed_pmc
Osimertinib in Patients With Epidermal Growth Factor Receptor Mutation–Positive Non–Small-Cell Lung Cancer and Leptomeningeal Metastases: The BLOOM Study
Osimertinib in Patients With Epidermal Growth Factor Receptor Mutation–Positive Non–Small-Cell Lung Cancer and Leptomeningeal Metastases: The BLOOM Study Abstract Abstract PURPOSE In this phase I study (BLOOM), osimertinib, a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), was ...
PMC9570207
core_pubmed_pmc
Pharmacokinetics of Myo -Inositol in a Wistar Rat Animal Model
Pharmacokinetics of Myo -Inositol in a Wistar Rat Animal Model Abstract Myo -inositol is the most popular inositol in living organisms, where it is present as a sugar alcohol, in a free form, and can also be described as a lipid. The aim of this study was to check the concentration change of a myo-inositol solution fro...
PMC8348438
core_pubmed_pmc
The Role of Supplementation with Natural Compounds in Post-Stroke Patients
The Role of Supplementation with Natural Compounds in Post-Stroke Patients Abstract Malnutrition is a serious problem in post-stroke patients. Importantly, it intensifies with hospitalization, and is related to both somatic and psychological reasons, as well as is associated with the insufficient knowledge of people wh...
PMC3125045
core_pubmed_pmc
Challenges and recommendations for conducting epidemiological studies in the field of epilepsy pharmacogenetics
Challenges and recommendations for conducting epidemiological studies in the field of epilepsy pharmacogenetics Abstract Abstract Epilepsy is one of the most prevalent neurological disorders, afflicting approximately 50 million Indians. Owing to affordability and easy availability, use of first-generation antiepileptic...
PMC10508168
core_pubmed_pmc
Lung microenvironments harbor Mycobacterium tuberculosis phenotypes with distinct treatment responses
Lung microenvironments harbor Mycobacterium tuberculosis phenotypes with distinct treatment responses Abstract ABSTRACT Tuberculosis lung lesions are complex and harbor heterogeneous microenvironments that influence antibiotic effectiveness. Major strides have been made recently in understanding drug pharmacokinetics i...
PMC7693064
core_pubmed_pmc
C3 inhibition with pegcetacoplan in subjects with paroxysmal nocturnal hemoglobinuria treated with eculizumab
C3 inhibition with pegcetacoplan in subjects with paroxysmal nocturnal hemoglobinuria treated with eculizumab Abstract Abstract Paroxysmal nocturnal hemoglobinuria (PNH) is an acquired, life‐threatening hematologic disease characterized by chronic complement‐mediated hemolysis and thrombosis. Despite treatment with ecu...
PMC10160416
core_pubmed_pmc
Olaparib and advanced ovarian cancer: Summary of the past and looking into the future
Olaparib and advanced ovarian cancer: Summary of the past and looking into the future Abstract Ovarian cancer (OC) is women’s eighth most common cancer, bearing the highest mortality rates of all female reproductive system malignancies. Poly (ADP-ribose) polymerase inhibitors (PARPis) have reshaped the treatment scenar...