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PMC10284592 | core_pubmed_pmc | Oral pharmacokinetics of a pharmaceutical preparation of florfenicol in broiler chickens | Oral pharmacokinetics of a pharmaceutical preparation of florfenicol in broiler chickens Abstract Introduction The use of florfenicol must follow particular pharmacokinetic/pharmacodynamic (PK/PD) ratios, i.e., it requires achieving serum concentrations at or slightly above the pathogen's minimum inhibitory concentrati... |
PMC9964503 | core_pubmed_pmc | Effects of Apigenin on Pharmacokinetics of Dasatinib and Probable Interaction Mechanism | Effects of Apigenin on Pharmacokinetics of Dasatinib and Probable Interaction Mechanism Abstract Abstract Dasatinib (DAS), a narrow-therapeutic index drug, Bcr-Abl, and Src family kinases multitarget inhibitor have been approved for chronic myelogenous leukemia (CML) and Ph-positive acute lymphocytic leukemia (Ph+ ALL)... |
PMC7488402 | core_pubmed_pmc | Pharmacokinetics of anticoagulant edoxaban in overdose in a Japanese patient transported to hospital | Pharmacokinetics of anticoagulant edoxaban in overdose in a Japanese patient transported to hospital Abstract Background The anticoagulant edoxaban is used clinically at doses of 30–60 mg/day; however, we experienced a patient who had taken an overdose of edoxaban of 750 mg. We investigated the pharmacokinetics of edox... |
PMC11365823 | core_pubmed_pmc | The Effect of Concomitant Administration of Proton Pump Inhibitors on the Pharmacokinetics of CDK4/6 Inhibitors in Rats: Implications for the Evaluation of Hepatic and Transporter-Mediated Drug–Drug Interactions | The Effect of Concomitant Administration of Proton Pump Inhibitors on the Pharmacokinetics of CDK4/6 Inhibitors in Rats: Implications for the Evaluation of Hepatic and Transporter-Mediated Drug–Drug Interactions Abstract Abstract Background and Objectives Numerous clinical concerns have been expressed regarding the pot... |
PMC5605887 | core_pubmed_pmc | Development and evaluation of Desvenlafaxine loaded PLGA-chitosan nanoparticles for brain delivery | Development and evaluation of Desvenlafaxine loaded PLGA-chitosan nanoparticles for brain delivery Abstract Abstract Depression is a debilitating psychiatric condition that remains the second most common cause of disability worldwide. Currently, depression affects more than 4 per cent of the world’s population. Most of... |
PMC11734590 | core_pubmed_pmc | First-in-Human Study of 23ME-00610, an Antagonistic Antibody for Genetically Validated CD200R1 Immune Checkpoint, in Participants with Advanced Solid Malignancies | First-in-Human Study of 23ME-00610, an Antagonistic Antibody for Genetically Validated CD200R1 Immune Checkpoint, in Participants with Advanced Solid Malignancies Abstract Abstract Purpose: In this phase 1 portion of a first-in-human phase 1/2a study ( NCT05199272 ), 23ME-00610 was evaluated in participants with advanc... |
PMC8638300 | core_pubmed_pmc | Gallium-68 Labeling of the Cyclin-Dependent Kinase 4/6 Inhibitors as Positron Emission Tomography Radiotracers for Tumor Imaging | Gallium-68 Labeling of the Cyclin-Dependent Kinase 4/6 Inhibitors as Positron Emission Tomography Radiotracers for Tumor Imaging Abstract Abstract Cyclin-dependent kinase 4 and 6 (CDK4/6) have emerged as interesting therapeutic drug targets with many potential applications in anti-tumors, especially in breast cancer. A... |
PMC4613513 | core_pubmed_pmc | LRRK2 dephosphorylation increases its ubiquitination | LRRK2 dephosphorylation increases its ubiquitination Abstract LRRK2 is normally phosphorylated at Ser910/935/955/973, but is dephosphorylated in certain PD associated mutations and after kinase inhibition. We ascribe a novel functional significance to the regulation of Ser910/935 as a switch for LRRK2 ubiquitination fo... |
PMC9404958 | core_pubmed_pmc | Model-Informed Translation of In Vitro Effects of Short-, Prolonged- and Continuous-Infusion Meropenem against Pseudomonas aeruginosa to Clinical Settings | Model-Informed Translation of In Vitro Effects of Short-, Prolonged- and Continuous-Infusion Meropenem against Pseudomonas aeruginosa to Clinical Settings Abstract Pharmacokinetic-pharmacodynamic (PKPD) models have met increasing interest as tools to identify potential efficacious antibiotic dosing regimens in vitro an... |
PMC8182805 | core_pubmed_pmc | Phase 1 randomized study on the safety, tolerability, and pharmacodynamic cognitive and electrophysiological effects of a dopamine D 1 receptor positive allosteric modulator in patients with schizophrenia | Phase 1 randomized study on the safety, tolerability, and pharmacodynamic cognitive and electrophysiological effects of a dopamine D 1 receptor positive allosteric modulator in patients with schizophrenia Abstract ASP4345, a novel dopamine D 1 receptor positive allosteric modulator, is being evaluated for the treatment... |
PMC8066963 | core_pubmed_pmc | Rutin Is a Low Micromolar Inhibitor of SARS-CoV-2 Main Protease 3CLpro: Implications for Drug Design of Quercetin Analogs | Rutin Is a Low Micromolar Inhibitor of SARS-CoV-2 Main Protease 3CLpro: Implications for Drug Design of Quercetin Analogs Abstract The pandemic, due to severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has stimulated the search for antivirals to tackle COVID-19 infection. Molecules with known pharmacokineti... |
PMC3392792 | core_pubmed_pmc | Safety, pharmacokinetics, and biologic activity of pateclizumab, a novel monoclonal antibody targeting lymphotoxin α: results of a phase I randomized, placebo-controlled trial | Safety, pharmacokinetics, and biologic activity of pateclizumab, a novel monoclonal antibody targeting lymphotoxin α: results of a phase I randomized, placebo-controlled trial Abstract Abstract Introduction Pateclizumab (MLTA3698A) is a humanized mAb against lymphotoxin α (LTα), a transiently expressed cytokine on acti... |
PMC4359187 | core_pubmed_pmc | Effect of a Modified Saquinavir/Ritonavir Dosing Regimen with Lower Dose Lead-In Phase on QTc Interval, Pharmacokinetics, Antiviral Activity and Safety in Treatment-Naïve HIV-1-Infected Patients | Effect of a Modified Saquinavir/Ritonavir Dosing Regimen with Lower Dose Lead-In Phase on QTc Interval, Pharmacokinetics, Antiviral Activity and Safety in Treatment-Naïve HIV-1-Infected Patients Abstract Abstract Background Saquinavir/ritonavir (1000/100 mg twice daily [BID]) is associated with dose- and exposure-depen... |
PMC10302853 | core_pubmed_pmc | Liquid Chromatography-Tandem Mass Spectrometry Method for Detection and Quantification of Meloxicam and 5′-Carboxymeloxicam in Oral Fluid Samples | Liquid Chromatography-Tandem Mass Spectrometry Method for Detection and Quantification of Meloxicam and 5′-Carboxymeloxicam in Oral Fluid Samples Abstract A sensitive, selective and particularly fast method of liquid chromatography-tandem mass spectrometry (LC-MS/MS) was developed and validated for the determination of... |
PMC9886810 | core_pubmed_pmc | Vaccination Opportunities in Multiple Sclerosis Patients Treated with Cladribine Tablets | Vaccination Opportunities in Multiple Sclerosis Patients Treated with Cladribine Tablets Abstract Abstract COVID 19 pandemic and mass vaccination campaigns have revealed the situation of the most vulnerable patients. In this work, we focused our attention to patients who have Multiple Sclerosis (MS), particularly in tr... |
PMC5075066 | core_pubmed_pmc | Cefazolin and Ertapenem, a Synergistic Combination Used To Clear Persistent Staphylococcus aureus Bacteremia | Cefazolin and Ertapenem, a Synergistic Combination Used To Clear Persistent Staphylococcus aureus Bacteremia Abstract Ertapenem and cefazolin were used in combination to successfully clear refractory methicillin-susceptible Staphylococcus aureus (MSSA) bacteremia. In addition, recent work has demonstrated activity of c... |
PMC12648864 | core_pubmed_pmc | Analysis of sex difference in strychnine-intoxicated rat based on the combination of metabolic kinetics and metabolomics | Analysis of sex difference in strychnine-intoxicated rat based on the combination of metabolic kinetics and metabolomics Abstract Background Drug metabolism va-specific dosing. Strychnine, the primary active compound in strychnine-based alkaloids, is used for treatment of hemiplegia or amblyopia. However, knowledge of ... |
PMC12217021 | core_pubmed_pmc | Feasibility of serial measurement of nitrite for pharmacodynamic monitoring and precision prescribing in urinary tract infections | Feasibility of serial measurement of nitrite for pharmacodynamic monitoring and precision prescribing in urinary tract infections Abstract Abstract Background The ability to monitor host- and bacteria-specific biomarkers along with antimicrobial drug concentration at the site of infection offers potential for individua... |
PMC5869712 | core_pubmed_pmc | Discovery of a highly selective JAK3 inhibitor for the treatment of rheumatoid arthritis | Discovery of a highly selective JAK3 inhibitor for the treatment of rheumatoid arthritis Abstract Abstract Janus tyrosine kinase 3 (JAK3) is expressed in lymphoid cells and is involved in the signalling of T cell functions. The development of a selective JAK3 inhibitor has been shown to have a potential benefit in the ... |
PMC12227375 | core_pubmed_pmc | Host Biomarkers and Antibiotic Tissue Penetration in Sepsis: Insights from Moxifloxacin | Host Biomarkers and Antibiotic Tissue Penetration in Sepsis: Insights from Moxifloxacin Abstract Abstract Background and Objective Sepsis-induced pathophysiological changes may lead to pharmacokinetic variability which alters antibiotic concentrations at the host infection site. This poses a challenge in clinical pract... |
PMC7256117 | core_pubmed_pmc | Risk of major bleeding among users of direct oral anticoagulants combined with interacting drugs: A population‐based nested case–control study | Risk of major bleeding among users of direct oral anticoagulants combined with interacting drugs: A population‐based nested case–control study Abstract Abstract Aims To assess the association between concurrent use of potential pharmacokinetic or pharmacodynamic interacting drugs and major bleeding among direct oral an... |
PMC9823088 | core_pubmed_pmc | The oral selective estrogen receptor degrader GDC-0810 (ARN-810) in postmenopausal women with hormone receptor-positive HER2-negative (HR + /HER2 −) advanced/metastatic breast cancer | The oral selective estrogen receptor degrader GDC-0810 (ARN-810) in postmenopausal women with hormone receptor-positive HER2-negative (HR + /HER2 −) advanced/metastatic breast cancer Abstract Abstract Purpose GDC-0810 (ARN-810) is a novel, non-steroidal, orally bioavailable, selective estrogen receptor degrader (SERD) ... |
PMC6554524 | core_pubmed_pmc | g-Nomic: a new pharmacogenetics interpretation software | g-Nomic: a new pharmacogenetics interpretation software Abstract Abstract We present g-Nomic, a pharmacogenetics interpretation software that analyzes globally a prescribed medication taking into account the personal background genetics, drug–drug interactions, lifestyle, nutritional supplements, inhibitors, inducers, ... |
PMC8776457 | core_pubmed_pmc | Review of the Chemical Composition, Pharmacological Effects, Pharmacokinetics, and Quality Control of Boswellia carterii | Review of the Chemical Composition, Pharmacological Effects, Pharmacokinetics, and Quality Control of Boswellia carterii Abstract Objective This review aimed to systematically summarize studies that investigated the bioactivities of compounds and extracts from Boswellia. Methods A literature review on the pharmacologic... |
PMC8926977 | core_pubmed_pmc | Man vs. machine: comparison of pharmacogenetic expert counselling with a clinical medication support system in a study with 200 genotyped patients | Man vs. machine: comparison of pharmacogenetic expert counselling with a clinical medication support system in a study with 200 genotyped patients Abstract Abstract Background Medication problems such as strong side effects or inefficacy occur frequently. At our university hospital, a consultation group of specialists ... |
PMC6448534 | core_pubmed_pmc | Formulation design, characterization, and in vitro and in vivo evaluation of nanostructured lipid carriers containing a bile salt for oral delivery of gypenosides | Formulation design, characterization, and in vitro and in vivo evaluation of nanostructured lipid carriers containing a bile salt for oral delivery of gypenosides Abstract Background Gypenosides (GPS) have been used as traditional medicine for centuries with various pharmacological effects. However, its therapeutic eff... |
PMC4836878 | core_pubmed_pmc | Clinical Validation of Therapeutic Drug Monitoring of Imipenem in Spent Effluent in Critically Ill Patients Receiving Continuous Renal Replacement Therapy: A Pilot Study | Clinical Validation of Therapeutic Drug Monitoring of Imipenem in Spent Effluent in Critically Ill Patients Receiving Continuous Renal Replacement Therapy: A Pilot Study Abstract Objectives The primary objective of this pilot study was to investigate whether the therapeutic drug monitoring of imipenem could be performe... |
PMC4378277 | core_pubmed_pmc | Turoctocog alfa: an evidence-based review of its potential in the treatment of hemophilia A | Turoctocog alfa: an evidence-based review of its potential in the treatment of hemophilia A Abstract Turoctocog alfa is the first B-domain-truncated third generation recombinant coagulation factor VIII (FVIII) product. Nonclinical in vitro and animal model studies have demonstrated that turoctocog alfa has similar func... |
PMC8982068 | core_pubmed_pmc | A novel LC-MS/MS method for simultaneous estimation of acalabrutinib and its active metabolite acalabrutinib M 27 in human plasma and application to a human pharmacokinetic study † | A novel LC-MS/MS method for simultaneous estimation of acalabrutinib and its active metabolite acalabrutinib M 27 in human plasma and application to a human pharmacokinetic study † Abstract Abstract A simple, specific, selective and accurate bioanalytical method was developed and validated for simultaneous estimation o... |
PMC12844234 | core_pubmed_pmc | Experimental Models and Translational Strategies in Neuroprotective Drug Development with Emphasis on Alzheimer’s Disease | Experimental Models and Translational Strategies in Neuroprotective Drug Development with Emphasis on Alzheimer’s Disease Abstract Neurodegenerative diseases (NDDs), including Alzheimer’s disease (AD), Parkinson’s disease (PD), amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD), are becoming more pre... |
PMC3689919 | core_pubmed_pmc | Evaluation of Crushed Ticagrelor Tablet Doses: Recovery Following Crushing and Naso-gastric Tube Passage Ex Vivo | Evaluation of Crushed Ticagrelor Tablet Doses: Recovery Following Crushing and Naso-gastric Tube Passage Ex Vivo Abstract Abstract Background Orally available ticagrelor in combination with low-dose aspirin (75–100 mg/day) is indicated for adult patients with acute coronary syndromes. However, patients with swallowing ... |
PMC10054246 | core_pubmed_pmc | Pretreatment with P2Y 12 Receptor Inhibitors in Acute Coronary Syndromes—Is the Current Standpoint of ESC Experts Sufficiently Supported? | Pretreatment with P2Y 12 Receptor Inhibitors in Acute Coronary Syndromes—Is the Current Standpoint of ESC Experts Sufficiently Supported? Abstract Excessive platelet reactivity plays a pivotal role in the pathogenesis of acute myocardial infarction. Today, the vast majority of patients presenting with acute coronary sy... |
PMC5745467 | core_pubmed_pmc | Fosfomycin: Pharmacological, Clinical and Future Perspectives | Fosfomycin: Pharmacological, Clinical and Future Perspectives Abstract Abstract Fosfomycin is a bactericidal, low-molecular weight, broad-spectrum antibiotic, with putative activity against several bacteria, including multidrug-resistant Gram-negative bacteria, by irreversibly inhibiting an early stage in cell wall syn... |
PMC4229638 | core_pubmed_pmc | Relationships between pazopanib exposure and clinical safety and efficacy in patients with advanced renal cell carcinoma | Relationships between pazopanib exposure and clinical safety and efficacy in patients with advanced renal cell carcinoma Abstract Abstract Background: Pazopanib, an oral angiogenesis inhibitor targeting vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit, is approve... |
PMC6942527 | core_pubmed_pmc | Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine | Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine Abstract Introduction The surface charge of nanoparticles, such as nanospheres (NS) and nanocapsules (NC), has been studied with the purpose of improving the in vivo performance of drugs. The aim of... |
PMC9114338 | core_pubmed_pmc | Fundamental aspects of long-acting tenofovir alafenamide delivery from subdermal implants for HIV prophylaxis | Fundamental aspects of long-acting tenofovir alafenamide delivery from subdermal implants for HIV prophylaxis Abstract Global efforts aimed at preventing human immunodeficiency virus type one (HIV-1) infection in vulnerable populations appear to be stalling, limiting our ability to control the epidemic. Long-acting, co... |
PMC10196418 | core_pubmed_pmc | Population pharmacokinetic modeling and simulation of maribavir to support dose selection and regulatory approval in adolescents with posttransplant refractory cytomegalovirus | Population pharmacokinetic modeling and simulation of maribavir to support dose selection and regulatory approval in adolescents with posttransplant refractory cytomegalovirus Abstract Abstract Maribavir was approved by the US Food and Drug Administration for the treatment of patients aged ≥12 years and weighing ≥35 kg... |
PMC8359227 | core_pubmed_pmc | Physiologically‐Based Pharmacokinetic Modeling in Renal and Hepatic Impairment Populations: A Pharmaceutical Industry Perspective | Physiologically‐Based Pharmacokinetic Modeling in Renal and Hepatic Impairment Populations: A Pharmaceutical Industry Perspective Abstract Abstract The predictive performance of physiologically‐based pharmacokinetics (PBPK) models for pharmacokinetics (PK) in renal impairment (RI) and hepatic impairment (HI) population... |
PMC7026080 | core_pubmed_pmc | Phenotypic high-throughput screening platform identifies novel chemotypes for necroptosis inhibition | Phenotypic high-throughput screening platform identifies novel chemotypes for necroptosis inhibition Abstract Regulated necrosis or necroptosis, mediated by receptor-interacting kinase 1 (RIPK1), RIPK3 and pseudokinase mixed lineage kinase domain-like protein (MLKL), contributes to the pathogenesis of inflammatory, inf... |
PMC9156977 | core_pubmed_pmc | Phase I study of PT-112, a novel pyrophosphate-platinum immunogenic cell death inducer, in advanced solid tumours | Phase I study of PT-112, a novel pyrophosphate-platinum immunogenic cell death inducer, in advanced solid tumours Abstract Summary Background PT-112, the first pyrophosphate-platinum conjugate, causes immunogenic cell death in experimental models, leading to recruitment of tumour-infiltrating lymphocytes. PT-112 also a... |
PMC4368859 | core_pubmed_pmc | Carrier-Mediated Cocaine Transport at the Blood-Brain Barrier as a Putative Mechanism in Addiction Liability | Carrier-Mediated Cocaine Transport at the Blood-Brain Barrier as a Putative Mechanism in Addiction Liability Abstract Abstract Background: The rate of entry of cocaine into the brain is a critical factor that influences neuronal plasticity and the development of cocaine addiction. Until now, passive diffusion has been ... |
PMC4860366 | core_pubmed_pmc | Prospective validation of a novel dosing scheme for intravenous busulfan in adult patients undergoing hematopoietic stem cell transplantation | Prospective validation of a novel dosing scheme for intravenous busulfan in adult patients undergoing hematopoietic stem cell transplantation Abstract Abstract The objective of this study was to externally validate a new dosing scheme for busulfan. Thirty-seven adult patients who received busulfan as conditioning thera... |
PMC12114871 | core_pubmed_pmc | Model-Based Evaluation of HangAmDan-B1 and Afatinib Combination Therapy in HCC827 Xenograft Mice with Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor | Model-Based Evaluation of HangAmDan-B1 and Afatinib Combination Therapy in HCC827 Xenograft Mice with Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor Abstract Objectives: HangAmDan-B1 (HAD-B1), a blended herbal mixture, has been investigated as an adjuvant therapy with afatinib (AFT) to treat n... |
PMC10674987 | core_pubmed_pmc | Sweet Cherry Extract as Permeation Enhancer of Tyrosine Kinase Inhibitors: A Promising Prospective for Future Oral Anticancer Therapies | Sweet Cherry Extract as Permeation Enhancer of Tyrosine Kinase Inhibitors: A Promising Prospective for Future Oral Anticancer Therapies Abstract Abstract Although patients would rather oral therapies to injections, the gastrointestinal tract’s low permeability makes this method limiting for most compounds, including an... |
PMC4786998 | core_pubmed_pmc | First-in-human, open-label dose-escalation and dose-expansion study of the safety, pharmacokinetics, and antitumor effects of an oral ALK inhibitor ASP3026 in patients with advanced solid tumors | First-in-human, open-label dose-escalation and dose-expansion study of the safety, pharmacokinetics, and antitumor effects of an oral ALK inhibitor ASP3026 in patients with advanced solid tumors Abstract Abstract Background ASP3026 is a second-generation anaplastic lymphoma kinase (ALK) inhibitor that has potent in vit... |
PMC5593162 | core_pubmed_pmc | No Pharmacokinetic Interaction Between the Hepatitis C Virus Inhibitors Elbasvir/Grazoprevir and Famotidine or Pantoprazole | No Pharmacokinetic Interaction Between the Hepatitis C Virus Inhibitors Elbasvir/Grazoprevir and Famotidine or Pantoprazole Abstract Abstract Use of agents to suppress gastric acid secretion is common among patients with hepatitis C virus (HCV) infection. The aims of this open‐label, three‐period, fixed‐sequence study ... |
PMC6510909 | core_pubmed_pmc | Phase 1 dose-escalation study of momelotinib, a Janus kinase 1/2 inhibitor, combined with gemcitabine and nab-paclitaxel in patients with previously untreated metastatic pancreatic ductal adenocarcinoma | Phase 1 dose-escalation study of momelotinib, a Janus kinase 1/2 inhibitor, combined with gemcitabine and nab-paclitaxel in patients with previously untreated metastatic pancreatic ductal adenocarcinoma Abstract Summary Purpose Preclinical evidence suggests the importance of Janus activating kinase (JAK) and TANK-bindi... |
PMC3260990 | core_pubmed_pmc | Smoking Cessation Pharmacogenetics: Analysis of Varenicline and Bupropion in Placebo-Controlled Clinical Trials | Smoking Cessation Pharmacogenetics: Analysis of Varenicline and Bupropion in Placebo-Controlled Clinical Trials Abstract Despite effective therapies for smoking cessation, most smokers find quitting difficult and most successful quitters relapse. Considerable evidence supports a genetic risk for nicotine dependence; ho... |
PMC4669083 | core_pubmed_pmc | Pharmacokinetic Study of Adjuvant Gemcitabine Therapy for Biliary Tract Cancer following Major Hepatectomy (KHBO1101) | Pharmacokinetic Study of Adjuvant Gemcitabine Therapy for Biliary Tract Cancer following Major Hepatectomy (KHBO1101) Abstract Background Biliary tract cancer (BTC) patients who have undergone surgical resection with major hepatectomy cannot tolerate the standard gemcitabine regimen (1,000 mg/m 2 on days 1, 8, and 15 e... |
PMC4775937 | core_pubmed_pmc | Combination Effects of Antimicrobial Peptides | Combination Effects of Antimicrobial Peptides Abstract Abstract Antimicrobial peptides (AMPs) are ancient and conserved across the tree of life. Their efficacy over evolutionary time has been largely attributed to their mechanisms of killing. Yet, the understanding of their pharmacodynamics both in vivo and in vitro is... |
PMC10691362 | core_pubmed_pmc | Comparison of pharmacokinetics and safety between CE-fosphenytoin sodium, fosphenytoin sodium, and phenytoin sodium after intravenous and intramuscular administration in healthy volunteers | Comparison of pharmacokinetics and safety between CE-fosphenytoin sodium, fosphenytoin sodium, and phenytoin sodium after intravenous and intramuscular administration in healthy volunteers Abstract Background: Captisol ® -enabled-fosphenytoin sodium (CE-fosphenytoin sodium) injection is a modified formulation of fosphe... |
PMC12175989 | core_pubmed_pmc | In Vivo Visualization and Quantification of Brain Heat Shock Protein 90 with [ 11 C]HSP990 in Healthy Aging and Neurodegeneration | In Vivo Visualization and Quantification of Brain Heat Shock Protein 90 with [ 11 C]HSP990 in Healthy Aging and Neurodegeneration Abstract Heat shock protein 90 (Hsp90) is essential for maintaining cellular proteostasis and may play an important role in the development of neurodegenerative proteinopathies. Therefore, w... |
PMC8458898 | core_pubmed_pmc | Novel Methods and Approaches for Safety Evaluation of Nanoparticle Formulations: A Focus Towards In Vitro Models and Adverse Outcome Pathways | Novel Methods and Approaches for Safety Evaluation of Nanoparticle Formulations: A Focus Towards In Vitro Models and Adverse Outcome Pathways Abstract Nanotoxicology is an emerging field employed in the assessment of unintentional hazardous effects produced by nanoparticles (NPs) impacting human health and the environm... |
PMC11617642 | core_pubmed_pmc | Improving CYP2C19 phenotyping using stereoselective omeprazole and 5‐hydroxy‐omeprazole metabolic ratios | Improving CYP2C19 phenotyping using stereoselective omeprazole and 5‐hydroxy‐omeprazole metabolic ratios Abstract Abstract Omeprazole (OME) is a CYP2C19 phenotyping probe, marketed as a racemic (S) / (R) mixture or as an S‐enantiomer. Both CYP2C19 and CYP3A4 enzymes mediate (R)‐OME hydroxylation to (R)‐5‐hydroxyomepraz... |
PMC8332571 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Profiles of Ethinylestradiol/Norgestimate Combination or Norethindrone upon Coadministration with Elagolix 150 mg Once Daily in Healthy Premenopausal Women | Pharmacokinetic and Pharmacodynamic Profiles of Ethinylestradiol/Norgestimate Combination or Norethindrone upon Coadministration with Elagolix 150 mg Once Daily in Healthy Premenopausal Women Abstract Abstract Background Two pharmacokinetic/pharmacodynamic studies were conducted to evaluate the potential drug–drug inte... |
PMC4268911 | core_pubmed_pmc | Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel | Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel Abstract Low-molecular-weight heparin (LMWH)–stearylamine (SA) conjugates (LHSA)-based self-assembled nanoparticles were prepared for intravenous delive... |
PMC12313752 | core_pubmed_pmc | Multiple Switches Between Adalimumab-fkjp and Reference Adalimumab in Moderate-to-Severe Chronic Plaque Psoriasis: A Multicenter, Double-Blind, Parallel Group, Randomized Clinical Trial for Interchangeability | Multiple Switches Between Adalimumab-fkjp and Reference Adalimumab in Moderate-to-Severe Chronic Plaque Psoriasis: A Multicenter, Double-Blind, Parallel Group, Randomized Clinical Trial for Interchangeability Abstract Abstract Introduction This study was conducted to fulfill the FDA requirement for the designation of a... |
PMC11597831 | core_pubmed_pmc | Design of Nanocrystalline Suspension of Dutasteride for Intramuscular Prolonged Delivery | Design of Nanocrystalline Suspension of Dutasteride for Intramuscular Prolonged Delivery Abstract Abstract The aim of the study is to formulate an injectable nanocrystalline suspension (NS) of dutasteride (DTS), a hydrophobic 5α-reductase inhibitor used to treat benign prostatic hyperplasia and scalp hair loss, for par... |
PMC11481319 | core_pubmed_pmc | Activity of polymyxin B combined with cefepime-avibactam against the biofilms of polymyxin B-resistant Pseudomonas aeruginosa and Klebsiella pneumoniae in in vitro and in vivo models | Activity of polymyxin B combined with cefepime-avibactam against the biofilms of polymyxin B-resistant Pseudomonas aeruginosa and Klebsiella pneumoniae in in vitro and in vivo models Abstract Bacterial biofilms, often forming on medical devices, can lead to treatment failure due to their increased antimicrobial resista... |
PMC10864925 | core_pubmed_pmc | Use of physiologically‐based pharmacokinetic modeling to understand the effect of omeprazole administration on the pharmacokinetics of oral extended‐release nifedipine | Use of physiologically‐based pharmacokinetic modeling to understand the effect of omeprazole administration on the pharmacokinetics of oral extended‐release nifedipine Abstract Abstract Proton pump inhibitors (PPIs) can affect the release of drugs from their dosage forms in vivo by elevating the gastric pH. Our recent ... |
PMC6475100 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of the novel Nrf2 activator omaveloxolone in primates | Pharmacokinetics and pharmacodynamics of the novel Nrf2 activator omaveloxolone in primates Abstract Abstract Background Omaveloxolone is a synthetic oleanane triterpenoid that pharmacologically activates Nrf2, a master transcription factor that regulates genes with antioxidative, anti-inflammatory, and mitochondrial b... |
PMC2939650 | core_pubmed_pmc | In vivo quantification of formulated and chemically modified small interfering RNA by heating-in-Triton quantitative reverse transcription polymerase chain reaction (HIT qRT-PCR) | In vivo quantification of formulated and chemically modified small interfering RNA by heating-in-Triton quantitative reverse transcription polymerase chain reaction (HIT qRT-PCR) Abstract Background While increasing numbers of small interfering RNA (siRNA) therapeutics enter into clinical trials, the quantification of ... |
PMC3386599 | core_pubmed_pmc | Using Physiologically-Based Pharmacokinetic Models to Incorporate Chemical and Non-Chemical Stressors into Cumulative Risk Assessment: A Case Study of Pesticide Exposures | Using Physiologically-Based Pharmacokinetic Models to Incorporate Chemical and Non-Chemical Stressors into Cumulative Risk Assessment: A Case Study of Pesticide Exposures Abstract Cumulative risk assessment has been proposed as an approach to evaluate the health risks associated with simultaneous exposure to multiple c... |
PMC12641129 | core_pubmed_pmc | Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Tunisia: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints | Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Tunisia: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints Abstract Abstract Objectives To determine the antibiotic susceptibility of community-acquired respiratory tract infection (CA-RTI) isolates of St... |
PMC12343485 | core_pubmed_pmc | Pharmacokinetics of levosimendan in critically Ill children on extracorporeal membrane oxygenation: a prospective observational study | Pharmacokinetics of levosimendan in critically Ill children on extracorporeal membrane oxygenation: a prospective observational study Abstract Abstract Background Levosimendan is used off-label in pediatrics and pharmacokinetic (PK) data in this population are scarce. The only study in critically ill patients on extrac... |
PMC12736914 | core_pubmed_pmc | Silymarin and Silybin: Rejuvenating Traditional Remedies with Modern Delivery Strategies | Silymarin and Silybin: Rejuvenating Traditional Remedies with Modern Delivery Strategies Abstract Silymarin, a polyphenolic flavonolignan complex extracted from Silybum marianum (milk thistle), has long been recognized for its hepatoprotective, antioxidant, anti-inflammatory, and anticancer properties. Among its consti... |
PMC8532953 | core_pubmed_pmc | Pharmacokinetics of Antibiotics in Pediatric Intensive Care: Fostering Variability to Attain Precision Medicine | Pharmacokinetics of Antibiotics in Pediatric Intensive Care: Fostering Variability to Attain Precision Medicine Abstract Abstract Children show important developmental and maturational changes, which may contribute greatly to pharmacokinetic (PK) variability observed in pediatric patients. These PK alterations are furt... |
PMC10827856 | core_pubmed_pmc | CHronic hypERtension and L-citRulline studY (CHERRY): an Early-Phase Randomised Controlled Trial in Pregnancy | CHronic hypERtension and L-citRulline studY (CHERRY): an Early-Phase Randomised Controlled Trial in Pregnancy Abstract Oral supplementation with L-citrulline, which is sequentially converted to L-arginine then nitric oxide, improves vascular biomarkers and reduces blood pressure in non-pregnant, hypertensive human coho... |
PMC5142404 | core_pubmed_pmc | Elimination of N-glycosylation by site mutation further prolongs the half-life of IFN-α/Fc fusion proteins expressed in Pichia pastoris | Elimination of N-glycosylation by site mutation further prolongs the half-life of IFN-α/Fc fusion proteins expressed in Pichia pastoris Abstract Abstract Background Interferon (IFN)-α has been commonly used as an antiviral drug worldwide; however, its short half-life in circulation due to its low molecular weight and s... |
PMC12655213 | core_pubmed_pmc | Generating and Modeling Virtual Patient Data from Published Population Pharmacokinetic Analyses: A Vancomycin Case Study | Generating and Modeling Virtual Patient Data from Published Population Pharmacokinetic Analyses: A Vancomycin Case Study Abstract Abstract Background/Objectives : In recent years, clinical pharmacometrics has become vital for drug development and clinical practice, particularly for predicting drug efficacy and safety. ... |
PMC12386793 | core_pubmed_pmc | Computational Profiling of Monoterpenoid Phytochemicals: Insights for Medicinal Chemistry and Drug Design Strategies | Computational Profiling of Monoterpenoid Phytochemicals: Insights for Medicinal Chemistry and Drug Design Strategies Abstract Abstract Monoterpenoids are a structurally diverse class of natural products with a long-standing history of therapeutic use. Despite their promising bioactivities, their clinical development ha... |
PMC7534330 | core_pubmed_pmc | UHPLC-MS/MS method for pharmacokinetic and bioavailability determination of five bioactive components in raw and various processed products of Polygala tenuifolia in rat plasma | UHPLC-MS/MS method for pharmacokinetic and bioavailability determination of five bioactive components in raw and various processed products of Polygala tenuifolia in rat plasma Abstract Abstract Context Sibiricose A5 (A5), sibiricose A6 (A6), 3,6′-disinapoyl sucrose (DSS), tenuifoliside A (TFSA) and 3,4,5-trimethoxycin... |
PMC5824709 | core_pubmed_pmc | Metabolite profiling with HPLC-ICP-MS as a tool for in vivo characterization of imaging probes | Metabolite profiling with HPLC-ICP-MS as a tool for in vivo characterization of imaging probes Abstract Abstract Background Current analytical methods for characterizing pharmacokinetic and metabolic properties of positron emission tomography (PET) and single photon emission computed tomography (SPECT) probes are limit... |
PMC6263297 | core_pubmed_pmc | Pharmacokinetics of single- and multiple-dose roflumilast: an open-label, three-way crossover study in healthy Chinese volunteers | Pharmacokinetics of single- and multiple-dose roflumilast: an open-label, three-way crossover study in healthy Chinese volunteers Abstract Purpose To determine the pharmacokinetic properties of the common tablet of roflumilast administered in single and multiple oral doses in Chinese subjects. Subjects and methods Both... |
PMC9251370 | core_pubmed_pmc | Utilization of Pharmacokinetic/Pharmacodynamic Modeling in Pharmacoepidemiological Studies: A Systematic Review on Antiarrhythmic and Glucose-Lowering Medicines | Utilization of Pharmacokinetic/Pharmacodynamic Modeling in Pharmacoepidemiological Studies: A Systematic Review on Antiarrhythmic and Glucose-Lowering Medicines Abstract Introduction: In human pharmacology, there are two important scientific branches: clinical pharmacology and pharmacoepidemiology. Pharmacokinetic/phar... |
PMC9925637 | core_pubmed_pmc | Bloodstream Infection Due to a VIM-Metallo-β-Lactamase-Producing Klebsiella pneumoniae Treated with Cefiderocol in a Preterm Newborn | Bloodstream Infection Due to a VIM-Metallo-β-Lactamase-Producing Klebsiella pneumoniae Treated with Cefiderocol in a Preterm Newborn Abstract Abstract Background The prevalence of certain multidrug-resistant organisms (MDROs), especially Gram-negative bacteria, is dramatically increasing in patient care settings, inclu... |
PMC12671115 | core_pubmed_pmc | Effect of pH on antimicrobial activity of delafloxacin against Escherichia coli isogenic strains carrying diverse chromosomal and plasmid-mediated fluoroquinolone resistance mechanisms | Effect of pH on antimicrobial activity of delafloxacin against Escherichia coli isogenic strains carrying diverse chromosomal and plasmid-mediated fluoroquinolone resistance mechanisms Abstract ABSTRACT The aim of this study is to evaluate the pH-dependent antimicrobial activities of delafloxacin against isogenic Esche... |
PMC7689702 | core_pubmed_pmc | Pharmacokinetic/pharmacodynamics variability of echinocandins in critically ill patients: A systematic review and meta‐analysis | Pharmacokinetic/pharmacodynamics variability of echinocandins in critically ill patients: A systematic review and meta‐analysis Abstract Abstract What is known and objective Anidulafungin, caspofungin and micafungin are three widely used echinocandin drugs licensed for the treatment of invasive fungal infections, and t... |
PMC12450495 | core_pubmed_pmc | A Case Series and Review of Hydroxychloroquine Toxicity and Monitoring: How Do We Dose Hydroxychloroquine? | A Case Series and Review of Hydroxychloroquine Toxicity and Monitoring: How Do We Dose Hydroxychloroquine? Abstract Hydroxychloroquine (HCQ) is an anti-malarial drug safely used in rheumatologic conditions with its various mechanisms on immunomodulation aside from its impact on cardiovascular health. However, multiple ... |
PMC8961338 | core_pubmed_pmc | Antipsychotic medication for women with schizophrenia spectrum disorders | Antipsychotic medication for women with schizophrenia spectrum disorders Abstract Abstract There are significant differences between men and women in the efficacy and tolerability of antipsychotic drugs. Here, we provide a comprehensive overview of what is currently known about the pharmacokinetics and pharmacodynamics... |
PMC12542493 | core_pubmed_pmc | The role of ABCB1 and CES1 genotypes on the efficacy and safety of dabigatran: a systematic review and meta-analysis | The role of ABCB1 and CES1 genotypes on the efficacy and safety of dabigatran: a systematic review and meta-analysis Abstract Introduction : Dabigatran is a direct oral anticoagulant associated with a high incidence of gastrointestinal bleeding, which presents a significant clinical concern. Genetic polymorphisms in th... |
PMC5363806 | core_pubmed_pmc | Multi-scale model of drug induced adaptive resistance of Gram-negative bacteria to polymyxin B | Multi-scale model of drug induced adaptive resistance of Gram-negative bacteria to polymyxin B Abstract Abstract The purpose of this report is to apply multi-scale modeling using the theory of physiologically structured populations (PSP) to develop a mathematical model for antimicrobial resistance based on a heterogene... |
PMC5705693 | core_pubmed_pmc | The antiviral effects of RSV fusion inhibitor, MDT ‐637, on clinical isolates, vs its achievable concentrations in the human respiratory tract and comparison to ribavirin | The antiviral effects of RSV fusion inhibitor, MDT ‐637, on clinical isolates, vs its achievable concentrations in the human respiratory tract and comparison to ribavirin Abstract Background Respiratory syncytial virus ( RSV ) viral load and disease severity associate, and the timing of viral load and disease run in pa... |
PMC8880887 | core_pubmed_pmc | Preparation and evaluation of bilayer-core osmotic pump tablets contained topiramate | Preparation and evaluation of bilayer-core osmotic pump tablets contained topiramate Abstract Abstract Topiramate (TPM) was an antiepileptic agent commonly used in clinical. Studies showed that an oral preparation of TPM with extended-release manner could bring some benefits for epileptics. In this paper, controlled re... |
PMC11678041 | core_pubmed_pmc | Evaluation of the Drug–Drug Interaction Potential of Cannabidiol Against UGT2B7-Mediated Morphine Metabolism Using Physiologically Based Pharmacokinetic Modeling | Evaluation of the Drug–Drug Interaction Potential of Cannabidiol Against UGT2B7-Mediated Morphine Metabolism Using Physiologically Based Pharmacokinetic Modeling Abstract Background: Morphine is a commonly prescribed opioid analgesic used to treat chronic pain. Morphine undergoes glucuronidation by UDP-glucuronosyltran... |
PMC5312529 | core_pubmed_pmc | A phase II study to evaluate LY2603618 in combination with gemcitabine in pancreatic cancer patients | A phase II study to evaluate LY2603618 in combination with gemcitabine in pancreatic cancer patients Abstract Abstract Background The aim of this study was to determine whether checkpoint kinase 1 inihibitor (CHK1), LY2603618, and gemcitabine prolong overall survival (OS) compared to gemcitabine alone in patients with ... |
PMC6585085 | core_pubmed_pmc | Disposition and effect of intra-articularly administered dexamethasone on lipopolysaccharide induced equine synovitis | Disposition and effect of intra-articularly administered dexamethasone on lipopolysaccharide induced equine synovitis Abstract Background Dexamethasone is used for the intra-articular route of administration in management of aseptic arthritis in horses. Despite its widespread use there is very little quantitative data ... |
PMC9764998 | core_pubmed_pmc | Pharmacokinetic-Pharmacodynamic Target Attainment Analyses as Support for Meropenem-Vaborbactam Dosing Regimens and Susceptibility Breakpoints | Pharmacokinetic-Pharmacodynamic Target Attainment Analyses as Support for Meropenem-Vaborbactam Dosing Regimens and Susceptibility Breakpoints Abstract ABSTRACT Meropenem-vaborbactam is a fixed-dose beta-lactam/beta-lactamase inhibitor with potent in vitro and in vivo activity against Klebsiella pneumoniae carbapenemas... |
PMC4955053 | core_pubmed_pmc | Pharmacokinetic Behaviors of Intravenously Administered siRNA in Glandular Tissues | Pharmacokinetic Behaviors of Intravenously Administered siRNA in Glandular Tissues Abstract The pharmacokinetics of small interfering RNAs (siRNAs) is a pivotal issue for siRNA-based drug development. In this study, we comprehensively investigated the behavior of siRNAs in vivo in various tissues and demonstrated that ... |
PMC6071752 | core_pubmed_pmc | A Novel Method for the Development of Environmental Public Health Indicators and Benchmark Dose Estimation Using a Health-Based End Point for Chlorpyrifos | A Novel Method for the Development of Environmental Public Health Indicators and Benchmark Dose Estimation Using a Health-Based End Point for Chlorpyrifos Abstract Background: Organophosphorus (OP) compounds are the most widely used group of insecticides in the world. Risk assessments for these chemicals have focused p... |
PMC8597046 | core_pubmed_pmc | Use of Mixture Dosing and Nonlinear Mixed Effect Modeling of Eight Environmental Contaminants in Rabbits to Improve Extrapolation Value of Toxicokinetic Data | Use of Mixture Dosing and Nonlinear Mixed Effect Modeling of Eight Environmental Contaminants in Rabbits to Improve Extrapolation Value of Toxicokinetic Data Abstract Abstract Background: Although in vivo studies of internal exposure to hazardous substances have been carried out for many years, there is room for progre... |
PMC9588929 | core_pubmed_pmc | Use of modeling and simulation to predict the influence of triazole antifungal agents on the pharmacokinetics of zanubrutinib and acalabrutinib | Use of modeling and simulation to predict the influence of triazole antifungal agents on the pharmacokinetics of zanubrutinib and acalabrutinib Abstract Abstract Background: Bruton’s tyrosine kinase (BTK) inhibitors are commonly used in the targeted therapy of B-cell malignancies. It is reported that myelosuppression a... |
PMC7364195 | core_pubmed_pmc | Pharmacokinetic Effects of l -Tetrahydropalmatine on Ketamine in Rat Plasma by Ultraperformance Liquid Chromatography Tandem Mass Spectrometry | Pharmacokinetic Effects of l -Tetrahydropalmatine on Ketamine in Rat Plasma by Ultraperformance Liquid Chromatography Tandem Mass Spectrometry Abstract Abstract Male Sprague-Dawley rats ( n = 18) were randomly divided into three groups: a saline group (20 mL/kg by gavage), a ketamine (KET) group (100 mg/kg by gavage), ... |
PMC5225209 | core_pubmed_pmc | First-dose and steady-state pharmacokinetics of orally administered crizotinib in children with solid tumors: a report on ADVL0912 from the Children’s Oncology Group Phase 1/Pilot Consortium | First-dose and steady-state pharmacokinetics of orally administered crizotinib in children with solid tumors: a report on ADVL0912 from the Children’s Oncology Group Phase 1/Pilot Consortium Abstract Purpose Characterize the pharmacokinetics of oral crizotinib in children with cancer. Methods Sixty-four children with s... |
PMC9921379 | core_pubmed_pmc | Tailoring of Novel Bile Salt Stabilized Vesicles for Enhanced Transdermal Delivery of Simvastatin: A New Therapeutic Approach against Inflammation | Tailoring of Novel Bile Salt Stabilized Vesicles for Enhanced Transdermal Delivery of Simvastatin: A New Therapeutic Approach against Inflammation Abstract Abstract Simvastatin (SMV), a cholesterol-lowering agent, has antioxidant and anti-inflammatory effects. Nevertheless, the oral use of SMV is linked with poor syste... |
PMC2850127 | core_pubmed_pmc | Duration of Suppression of Adrenal Steroids after Glucocorticoid Administration | Duration of Suppression of Adrenal Steroids after Glucocorticoid Administration Abstract Hydrocortisone has long been the treatment of choice for congenital adrenal hyperplasia (CAH). However, treatment with this medication remains problematic. Patients with 21-hydroxylase deficiency CAH have significant diurnal variat... |
PMC7158205 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Intensive Antituberculosis Treatment of Tuberculous Meningitis | Pharmacokinetics and Pharmacodynamics of Intensive Antituberculosis Treatment of Tuberculous Meningitis Abstract Abstract The most effective antituberculosis drug treatment regimen for tuberculous meningitis is uncertain. We conducted a randomized controlled trial comparing standard treatment with a regimen intensified... |
PMC6713146 | core_pubmed_pmc | Intraocular administration of tetramethylpyrazine hydrochloride to rats: a direct delivery pathway for brain targeting? | Intraocular administration of tetramethylpyrazine hydrochloride to rats: a direct delivery pathway for brain targeting? Abstract Abstract The purpose of this study was to compare the pharmacokinetic profile of tetramethylpyrazine hydrochloride (TMPH) in rat plasma and tissues following intravenous (iv), intragastric (i... |
PMC6364906 | core_pubmed_pmc | Nontherapeutic equivalence of a generic product of imipenem-cilastatin is caused more by chemical instability of the active pharmaceutical ingredient (imipenem) than by its substandard amount of cilastatin | Nontherapeutic equivalence of a generic product of imipenem-cilastatin is caused more by chemical instability of the active pharmaceutical ingredient (imipenem) than by its substandard amount of cilastatin Abstract Background We demonstrated therapeutic nonequivalence of “bioequivalent” generics for meropenem, but ther... |
PMC8048880 | core_pubmed_pmc | Model‐Informed Drug Development for Antimicrobials: Translational PK and PK/PD Modeling to Predict an Efficacious Human Dose for Apramycin | Model‐Informed Drug Development for Antimicrobials: Translational PK and PK/PD Modeling to Predict an Efficacious Human Dose for Apramycin Abstract Abstract Apramycin represents a subclass of aminoglycoside antibiotics that has been shown to evade almost all mechanisms of clinically relevant aminoglycoside resistance. ... |
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