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PMC3334750
core_pubmed_pmc
Antibiotics in critically ill patients: a systematic review of the pharmacokinetics of β-lactams
Antibiotics in critically ill patients: a systematic review of the pharmacokinetics of β-lactams Abstract Introduction Several reports have shown marked heterogeneity of antibiotic pharmacokinetics (PK) in patients admitted to ICUs, which might potentially affect outcomes. Therefore, the pharmacodynamic (PD) parameter ...
PMC10557102
core_pubmed_pmc
Effect of nivasorexant ( ACT ‐539313), a selective orexin‐1‐receptor antagonist, on multiple cytochrome P450 probe substrates in vitro and in vivo using a cocktail approach in healthy subjects
Effect of nivasorexant ( ACT ‐539313), a selective orexin‐1‐receptor antagonist, on multiple cytochrome P450 probe substrates in vitro and in vivo using a cocktail approach in healthy subjects Abstract Abstract Nivasorexant, a selective orexin‐1‐receptor antagonist, has recently been assessed in the treatment of humans...
PMC9352398
core_pubmed_pmc
Ceftazidime-avibactam based combinations against carbapenemase producing Klebsiella pneumoniae harboring hypervirulence plasmids
Ceftazidime-avibactam based combinations against carbapenemase producing Klebsiella pneumoniae harboring hypervirulence plasmids Abstract Abstract The combination of carbapenem resistance and hypervirulence in Klebsiella pneumoniae is an emerging and urgent threat due to its potential to resist common antibiotics and c...
PMC12817472
core_pubmed_pmc
Efavirenz and CYP2C9 Genetic Polymorphisms Reduce CYP2C9 Activity in Healthy Participants
Efavirenz and CYP2C9 Genetic Polymorphisms Reduce CYP2C9 Activity in Healthy Participants Abstract ABSTRACT Efavirenz's effects on cytochrome P450 2C9 (CYP2C9) activity have not been formally characterized in vivo. We conducted the first clinical drug–drug interaction (DDI) study to test the effect of chronic efavirenz...
PMC12066422
core_pubmed_pmc
Prediction of pharmacokinetic/pharmacodynamic properties of aldosterone synthase inhibitors at drug discovery stage using an artificial intelligence-physiologically based pharmacokinetic model
Prediction of pharmacokinetic/pharmacodynamic properties of aldosterone synthase inhibitors at drug discovery stage using an artificial intelligence-physiologically based pharmacokinetic model Abstract The objective of this study is to develop an artificial intelligence-physiologically based pharmacokinetic (AI-PBPK) m...
PMC12406673
core_pubmed_pmc
Clinical pharmacokinetics of metronidazole: a systematic review and meta-analysis
Clinical pharmacokinetics of metronidazole: a systematic review and meta-analysis Abstract ABSTRACT Metronidazole (MTZ) is used in various clinical settings; however, its pharmacokinetics may vary across patient populations due to physiological and pathological differences. Understanding these variations is important f...
PMC5355322
core_pubmed_pmc
Enhancement of the bioavailability of a novel anticancer compound (acetyltanshinone IIA) by encapsulation within mPEG-PLGA nanoparticles: a study of formulation optimization, toxicity, and pharmacokinetics
Enhancement of the bioavailability of a novel anticancer compound (acetyltanshinone IIA) by encapsulation within mPEG-PLGA nanoparticles: a study of formulation optimization, toxicity, and pharmacokinetics Abstract The Poly (ethylene glycol) methyl ether-block-poly (lactide-co-glycolide) (mPEG-PLGA) nanoparticles carry...
PMC10196428
core_pubmed_pmc
Regulatory utility of physiologically‐based pharmacokinetic modeling to support alternative bioequivalence approaches and risk assessment: A workshop summary report
Regulatory utility of physiologically‐based pharmacokinetic modeling to support alternative bioequivalence approaches and risk assessment: A workshop summary report Abstract Abstract This report summarizes the proceedings for day 2 sessions 1 and 3 of the 2‐day public workshop entitled “Regulatory Utility of Mechanisti...
PMC9497196
core_pubmed_pmc
Detection of Experimental Colorectal Peritoneal Metastases by a Novel PDGFRβ-Targeting Nanobody
Detection of Experimental Colorectal Peritoneal Metastases by a Novel PDGFRβ-Targeting Nanobody Abstract Abstract Simple Summary Colorectal cancer can metastasize to multiple distant sites. Metastases growing within the peritoneal cavity cause a high degree of morbidity and are associated with very poor survival. Moreo...
PMC7261296
core_pubmed_pmc
Low Blood Glucose Index and Hypoglycaemia Risk: Insulin Glargine 300 U/mL Versus Insulin Glargine 100 U/mL in Type 2 Diabetes
Low Blood Glucose Index and Hypoglycaemia Risk: Insulin Glargine 300 U/mL Versus Insulin Glargine 100 U/mL in Type 2 Diabetes Abstract Abstract Introduction We examined differences in hypoglycaemia risk between insulin glargine 300 U/mL (Gla-300) and insulin glargine 100 U/mL (Gla-100) in individuals with type 2 diabet...
PMC7179275
core_pubmed_pmc
Extension of Pharmacokinetic/Pharmacodynamic Time-Kill Studies To Include Lipopolysaccharide/Endotoxin Release from Escherichia coli Exposed to Cefuroxime
Extension of Pharmacokinetic/Pharmacodynamic Time-Kill Studies To Include Lipopolysaccharide/Endotoxin Release from Escherichia coli Exposed to Cefuroxime Abstract The release of inflammatory bacterial products, such as lipopolysaccharide (LPS)/endotoxin, may be increased upon the administration of antibiotics. An impr...
PMC8961622
core_pubmed_pmc
Inhaled remdesivir reduces viral burden in a nonhuman primate model of SARS-CoV-2 infection
Inhaled remdesivir reduces viral burden in a nonhuman primate model of SARS-CoV-2 infection Abstract Remdesivir (RDV) is a nucleotide analog prodrug with demonstrated clinical benefit in patients with coronavirus disease 2019 (COVID-19). In October 2020, the US FDA approved intravenous (IV) RDV as the first treatment f...
PMC11743273
core_pubmed_pmc
Liquid chromatography-tandem mass spectrometry for the quantification of ripretinib and its metabolites DP-5439 in human plasma
Liquid chromatography-tandem mass spectrometry for the quantification of ripretinib and its metabolites DP-5439 in human plasma Abstract Abstract Background Ripretinib, a broad-spectrum tyrosine kinase inhibitor, has been approved for the treatment of advanced gastrointestinal stromal tumors in adult patients. Clinical...
PMC11263531
core_pubmed_pmc
Relative Bioavailability Study of Midazolam Intramuscularly Administered with the Needle-Free Auto-Injector ZENEO ® in Healthy Adults
Relative Bioavailability Study of Midazolam Intramuscularly Administered with the Needle-Free Auto-Injector ZENEO ® in Healthy Adults Abstract Introduction Intramuscular (IM) midazolam is indicated for the treatment of status epilepticus. Administration must be efficient to rapidly terminate prolonged seizures and prev...
PMC8586755
core_pubmed_pmc
Dose selection and tolerability of anticancer agents evaluated by the European Medicines Agency in the period 2015-2020
Dose selection and tolerability of anticancer agents evaluated by the European Medicines Agency in the period 2015-2020 Abstract Abstract Background Novel anticancer agents are initially evaluated in a palliative setting in phase I studies. The benefit–risk applying the selected dose from these phase I studies can be c...
PMC9893889
core_pubmed_pmc
Tumor growth inhibition modeling to support the starting dose for dacomitinib
Tumor growth inhibition modeling to support the starting dose for dacomitinib Abstract Abstract Dacomitinib is a second‐generation, irreversible EGFR tyrosine kinase inhibitor for first‐line treatment of patients with metastatic non‐small cell lung cancer and EGFR‐activating mutations. A high rate of dose reductions in...
PMC8161888
core_pubmed_pmc
Augmented renal clearance: a retrospective, cohort study of urinary creatinine clearance in critically ill patients in the United Kingdom
Augmented renal clearance: a retrospective, cohort study of urinary creatinine clearance in critically ill patients in the United Kingdom Abstract Abstract Objective Augmented renal clearance (ARC) is associated with sub-therapeutic antibiotic, anti-epileptic, and anticoagulant serum concentrations leading to adverse p...
PMC11578130
core_pubmed_pmc
Development of breakthrough bleeding model of combined‐oral contraceptives utilizing model‐based meta‐analysis
Development of breakthrough bleeding model of combined‐oral contraceptives utilizing model‐based meta‐analysis Abstract Abstract Breakthrough bleeding (BTB) is a common side effect of hormonal contraception and is thought to impact adherence to combined oral contraceptives (COCs) but respective dose–response relationsh...
PMC5557574
core_pubmed_pmc
Selepressin, a novel selective vasopressin V 1A agonist, is an effective substitute for norepinephrine in a phase IIa randomized, placebo-controlled trial in septic shock patients
Selepressin, a novel selective vasopressin V 1A agonist, is an effective substitute for norepinephrine in a phase IIa randomized, placebo-controlled trial in septic shock patients Abstract Abstract Background Vasopressin is widely used for vasopressor support in septic shock patients, but experimental evidence suggests...
PMC12855707
core_pubmed_pmc
Continuous Infusion of Aztreonam–Avibactam After High Loading Dose for an Infection Caused by an OXA-48- and NDM-1-Co-producing ST147 Klebsiella pneumoniae
Continuous Infusion of Aztreonam–Avibactam After High Loading Dose for an Infection Caused by an OXA-48- and NDM-1-Co-producing ST147 Klebsiella pneumoniae Abstract Abstract Introduction Infections caused by metallo-β-lactamase-producing Enterobacterales offer limited therapeutic options. Aztreonam–avibactam (ATM-AVI) ...
PMC7491979
core_pubmed_pmc
Neutropenia and survival outcomes in metastatic colorectal cancer patients treated with trifluridine/tipiracil in the RECOURSE and J003 trials
Neutropenia and survival outcomes in metastatic colorectal cancer patients treated with trifluridine/tipiracil in the RECOURSE and J003 trials Abstract Background: The phase II J003 ( N = 169) and phase III RECOURSE ( N = 800) trials demonstrated a significant improvement in survival with trifluridine (FTD)/tipiracil (...
PMC11985623
core_pubmed_pmc
Integrating LC–MS/MS and In Silico Methods to Uncover Bioactive Compounds with Lipase Inhibitory Potential in the Antarctic Moss Warnstorfia fontinaliopsis
Integrating LC–MS/MS and In Silico Methods to Uncover Bioactive Compounds with Lipase Inhibitory Potential in the Antarctic Moss Warnstorfia fontinaliopsis Abstract Abstract Antarctic organisms are known for producing unique secondary metabolites, and this study specifically focuses on the less-explored metabolites of ...
PMC9109935
core_pubmed_pmc
Preparation, in vitro and in vivo Evaluation of Thermosensitive in situ Gel Loaded with Ibuprofen-Solid Lipid Nanoparticles for Rectal Delivery
Preparation, in vitro and in vivo Evaluation of Thermosensitive in situ Gel Loaded with Ibuprofen-Solid Lipid Nanoparticles for Rectal Delivery Abstract Abstract Background Ibuprofen (IBU), a nonsteroidal anti-inflammatory drug, shows poor gastrointestinal absorption due to its low solubility, which limits its clinical...
PMC6864547
core_pubmed_pmc
Multimerization through Pegylation Improves Pharmacokinetic Properties of scFv Fragments of GD2-Specific Antibodies
Multimerization through Pegylation Improves Pharmacokinetic Properties of scFv Fragments of GD2-Specific Antibodies Abstract Abstract Antigen-binding fragments of antibodies specific to the tumor-associated ganglioside GD2 are well poised to play a substantial role in modern GD2-targeted cancer therapies, however, rapi...
PMC12402305
core_pubmed_pmc
Leveraging quantitative systems pharmacology modeling for elranatamab regimen optimization in relapsed or refractory multiple myeloma
Leveraging quantitative systems pharmacology modeling for elranatamab regimen optimization in relapsed or refractory multiple myeloma Abstract Abstract Elranatamab, an approved bispecific antibody (BsAb) for relapsed/refractory multiple myeloma, forms an immune synapse between the T-cell CD3 marker and B-cell maturatio...
PMC7370567
core_pubmed_pmc
Interaction Between Low-Dose Aspirin and Nonsteroidal Anti-Inflammatory Drugs Can Compromise Aspirin’s Efficacy in Preventing Venous Thrombosis Following Total Joint Arthroplasty
Interaction Between Low-Dose Aspirin and Nonsteroidal Anti-Inflammatory Drugs Can Compromise Aspirin’s Efficacy in Preventing Venous Thrombosis Following Total Joint Arthroplasty Abstract Total joint arthroplasty is a rapid recovery procedure with patients optimized quickly in preparation for discharge. Two significant...
PMC5784556
core_pubmed_pmc
Brivaracetam: a novel antiepileptic drug for focal-onset seizures
Brivaracetam: a novel antiepileptic drug for focal-onset seizures Abstract Abstract Brivaracetam (BRV), the n -propyl analogue of levetiracetam (LEV), is the latest antiepileptic drug (AED) to be licensed in Europe and the USA for the adjunctive treatment of focal-onset seizures with or without secondary generalization...
PMC12133543
core_pubmed_pmc
Case Report: Pharmacokinetics of ceftazidime and avibactam during and after CRRT in an elderly patient and their associations with CNS adverse effects
Case Report: Pharmacokinetics of ceftazidime and avibactam during and after CRRT in an elderly patient and their associations with CNS adverse effects Abstract Ceftazidime/avibactam is effective for treating infections caused by multidrug-resistant gram-negative bacteria and is widely used. The pharmacokinetic data of ...
PMC8685423
core_pubmed_pmc
Pharmacokinetic Evaluation of Eltrombopag in ITP Pediatric Patients
Pharmacokinetic Evaluation of Eltrombopag in ITP Pediatric Patients Abstract Background: Eltrombopag (EPAG) is an oral thrombopoietin receptor agonist, approved for refractory primary immune thrombocytopenia (ITP) in pediatric patients. In two pediatric RCTs, EPAG led to an improvement of platelet counts and a reductio...
PMC9544664
core_pubmed_pmc
Characterisation of individual ferritin response in patients receiving chelation therapy
Characterisation of individual ferritin response in patients receiving chelation therapy Abstract Abstract Aims To develop a drug–disease model describing iron overload and its effect on ferritin response in patients affected by transfusion‐dependent haemoglobinopathies and investigate the contribution of interindividu...
PMC10147791
core_pubmed_pmc
Nedosiran in primary hyperoxaluria subtype 3: results from a phase I, single-dose study (PHYOX4)
Nedosiran in primary hyperoxaluria subtype 3: results from a phase I, single-dose study (PHYOX4) Abstract Abstract Nedosiran is an N -acetyl-D-galactosamine (GalNAc)–conjugated RNA interference agent targeting hepatic lactate dehydrogenase (encoded by the LDHA gene), the putative enzyme mediating the final step of oxal...
PMC6960222
core_pubmed_pmc
Benzodiazepines and Related Drugs as a Risk Factor in Alzheimer's Disease Dementia
Benzodiazepines and Related Drugs as a Risk Factor in Alzheimer's Disease Dementia Abstract Benzodiazepines (BZDs) and Z-drugs are compounds widely prescribed in medical practice due to their anxiolytic, hypnotic, and muscle relaxant properties. Yet, their chronic use is associated with cases of abuse, dependence, and ...
PMC11984981
core_pubmed_pmc
A simulation-based framework for modeling and prediction of personalized blood pressure trajectories in hypertensive patients after antihypertensive treatment
A simulation-based framework for modeling and prediction of personalized blood pressure trajectories in hypertensive patients after antihypertensive treatment Abstract Hypertension, a leading global cause of death, poses challenges in stabilizing blood pressure within target values despite various therapeutic options, ...
PMC10135424
core_pubmed_pmc
Clinical Outcomes With Extended Versus Intermittent Infusion of Anti-Pseudomonal Beta-Lactams in Patients With Gram-Negative Bacteremia
Clinical Outcomes With Extended Versus Intermittent Infusion of Anti-Pseudomonal Beta-Lactams in Patients With Gram-Negative Bacteremia Abstract Abstract Background Administration of doses via an extended infusion (EI) is an important strategy to optimize beta-lactams. Available data on the impact of EI on outcomes lar...
PMC7900506
core_pubmed_pmc
Antinociceptive Effects of Sinomenine Combined With Ligustrazine or Paracetamol in Animal Models of Incisional and Inflammatory Pain
Antinociceptive Effects of Sinomenine Combined With Ligustrazine or Paracetamol in Animal Models of Incisional and Inflammatory Pain Abstract Abstract The management of postoperative and inflammatory pain has been a pressing challenge in clinical settings. Sinomenine (SN) is a morphinan derived alkaloid with remarkable...
PMC11345372
core_pubmed_pmc
A phase I trial of LHC165 single agent and in combination with spartalizumab in patients with advanced solid malignancies
A phase I trial of LHC165 single agent and in combination with spartalizumab in patients with advanced solid malignancies Abstract Abstract Background LHC165 is a Toll-like receptor (TLR)-7 agonist that generates an effective tumor antigen-specific T-cell adaptive immune response as well as durable antitumor responses....
PMC8489053
core_pubmed_pmc
Practical identifiability in the frame of nonlinear mixed effects models: the example of the in vitro erythropoiesis
Practical identifiability in the frame of nonlinear mixed effects models: the example of the in vitro erythropoiesis Abstract Background Nonlinear mixed effects models provide a way to mathematically describe experimental data involving a lot of inter-individual heterogeneity. In order to assess their practical identif...
PMC12869905
core_pubmed_pmc
Protocol for a phase 2, partially blinded, randomized trial assessing the safety and efficacy of sorfequiline or bedaquiline in combination with pretomanid and linezolid in adult participants with newly diagnosed, drug-sensitive, smear-positive pulmonary tuberculosis (NC-009)
Protocol for a phase 2, partially blinded, randomized trial assessing the safety and efficacy of sorfequiline or bedaquiline in combination with pretomanid and linezolid in adult participants with newly diagnosed, drug-sensitive, smear-positive pulmonary tuberculosis (NC-009) Abstract Abstract Introduction In 2023, tub...
PMC8583966
core_pubmed_pmc
Proteasome Inhibitors and Their Pharmacokinetics, Pharmacodynamics, and Metabolism
Proteasome Inhibitors and Their Pharmacokinetics, Pharmacodynamics, and Metabolism Abstract Abstract The proteasome is responsible for mediating intracellular protein degradation and regulating cellular function with impact on tumor and immune effector cell biology. The proteasome is found predominantly in two forms, t...
PMC3876561
core_pubmed_pmc
A Rapid, Simple, Liquid Chromatographic-Electrospray Ionization, Ion Trap Mass Spectrometry Method for the Determination of Finasteride in Human Plasma and its Application to Pharmacokinetic Study
A Rapid, Simple, Liquid Chromatographic-Electrospray Ionization, Ion Trap Mass Spectrometry Method for the Determination of Finasteride in Human Plasma and its Application to Pharmacokinetic Study Abstract Abstract A fast, accurate, sensitive, selective and reliable method using reversed-phase high performance liquid c...
PMC9227284
core_pubmed_pmc
Analysis of Pros and Cons in Using [ 68 Ga]Ga-PSMA-11 and [ 18 F]PSMA-1007: Production, Costs, and PET/CT Applications in Patients with Prostate Cancer
Analysis of Pros and Cons in Using [ 68 Ga]Ga-PSMA-11 and [ 18 F]PSMA-1007: Production, Costs, and PET/CT Applications in Patients with Prostate Cancer Abstract The aim of this work is to compare [ 68 Ga]Ga-PSMA-11 and [ 18 F]PSMA-1007 PET/CT as imaging agents in patients with prostate cancer (PCa). Comparisons were ma...
PMC7422009
core_pubmed_pmc
A Review of the Botany, Traditional Use, Phytochemistry, Analytical Methods, Pharmacological Effects, and Toxicity of Angelicae Pubescentis Radix
A Review of the Botany, Traditional Use, Phytochemistry, Analytical Methods, Pharmacological Effects, and Toxicity of Angelicae Pubescentis Radix Abstract Angelicae Pubescentis Radix (AP), as a traditional Chinese medicine (TCM), has been used for thousands of years in China. In this paper, the botany, traditional use,...
PMC4622569
core_pubmed_pmc
A novel approach to investigate the effect of methionine oxidation on pharmacokinetic properties of therapeutic antibodies
A novel approach to investigate the effect of methionine oxidation on pharmacokinetic properties of therapeutic antibodies Abstract Preserving the chemical and structural integrity of therapeutic antibodies during manufacturing and storage is a major challenge during pharmaceutical development. Oxidation of Fc methioni...
PMC5510450
core_pubmed_pmc
Comparative pharmacology of a new recombinant FSH expressed by a human cell line
Comparative pharmacology of a new recombinant FSH expressed by a human cell line Abstract Abstract Recombinant FSH proteins are important therapeutic agents for the treatment of infertility, including follitropin alfa expressed in Chinese Hamster Ovary (CHO) cells and, more recently, follitropin delta expressed in the ...
PMC9855849
core_pubmed_pmc
Development of Lanzyme as the Potential Enzyme Replacement Therapy Drug for Fabry Disease
Development of Lanzyme as the Potential Enzyme Replacement Therapy Drug for Fabry Disease Abstract Abstract Fabry disease (FD) is a progressive multisystemic disease characterized by lysosomal enzyme deficiency. Enzyme replacement therapy (ERT) is one of the most significant advancements and breakthroughs in treating F...
PMC9805947
core_pubmed_pmc
A highly efficient protein corona-based proteomic analysis strategy for the discovery of pharmacodynamic biomarkers
A highly efficient protein corona-based proteomic analysis strategy for the discovery of pharmacodynamic biomarkers Abstract Abstract The composition of serum is extremely complex, which complicates the discovery of new pharmacodynamic biomarkers via serum proteome for disease prediction and diagnosis. Recently, nanopa...
PMC10133546
core_pubmed_pmc
Simultaneous determination of multiple components in rat plasma by UHPLC-sMRM for pharmacokinetic studies after oral administration of Qingjin Yiqi Granules
Simultaneous determination of multiple components in rat plasma by UHPLC-sMRM for pharmacokinetic studies after oral administration of Qingjin Yiqi Granules Abstract Abstract As a Traditional Chinese Medicine prescription, Qingjin Yiqi Granules (QJYQ) provides an effective treatment for patients recovering from COVID-1...
PMC9495066
core_pubmed_pmc
Tissue Penetration of Antimicrobials in Intensive Care Unit Patients: A Systematic Review—Part II
Tissue Penetration of Antimicrobials in Intensive Care Unit Patients: A Systematic Review—Part II Abstract In patients that are admitted to intensive care units (ICUs), the clinical outcome of severe infections depends on several factors, as well as the early administration of chemotherapies and comorbidities. Antimicr...
PMC4454784
core_pubmed_pmc
Successful pregnancy outcome in paroxysmal nocturnal hemoglobinuria (PNH) following escalated eculizumab dosing to control breakthrough hemolysis
Successful pregnancy outcome in paroxysmal nocturnal hemoglobinuria (PNH) following escalated eculizumab dosing to control breakthrough hemolysis Abstract Pregnancy in women with paroxysmal nocturnal hemoglobinuria (PNH) is associated with increased maternal and fetal morbidity and mortality. There is limited published...
PMC10053857
core_pubmed_pmc
Analysis of NSAIDs in Rat Plasma Using 3D-Printed Sorbents by LC-MS/MS: An Approach to Pre-Clinical Pharmacokinetic Studies
Analysis of NSAIDs in Rat Plasma Using 3D-Printed Sorbents by LC-MS/MS: An Approach to Pre-Clinical Pharmacokinetic Studies Abstract Analytical sample preparation techniques are essential for assessing chemicals in various biological matrices. The development of extraction techniques is a modern trend in the bioanalyti...
PMC8364917
core_pubmed_pmc
Generation and Characterization of Torudokimab (LY3375880): A Monoclonal Antibody That Neutralizes Interleukin-33
Generation and Characterization of Torudokimab (LY3375880): A Monoclonal Antibody That Neutralizes Interleukin-33 Abstract Background Interleukin-33 (IL-33) is an alarmin that is released following cellular damage, mechanical injury, or necrosis. It is a member of the IL-1 family and binds to a heterodimer receptor con...
PMC8861237
core_pubmed_pmc
Pharmacokinetics, Safety, and Tolerability of a Medicinal Cannabis Formulation in Patients with Chronic Non-cancer Pain on Long-Term High Dose Opioid Analgesia: A Pilot Study
Pharmacokinetics, Safety, and Tolerability of a Medicinal Cannabis Formulation in Patients with Chronic Non-cancer Pain on Long-Term High Dose Opioid Analgesia: A Pilot Study Abstract Abstract Introduction This phase I open-label study examined pharmacokinetics, safety, and tolerability of escalating doses of a novel c...
PMC5055913
core_pubmed_pmc
Effect of Oral Coadministration of Ascorbic Acid with Ling Zhi Preparation on Pharmacokinetics of Ganoderic Acid A in Healthy Male Subjects: A Randomized Crossover Study
Effect of Oral Coadministration of Ascorbic Acid with Ling Zhi Preparation on Pharmacokinetics of Ganoderic Acid A in Healthy Male Subjects: A Randomized Crossover Study Abstract Abstract The objective of this randomized, open-label, single-dose, two-phase crossover study was to determine the effect of ascorbic acid on...
PMC7301706
core_pubmed_pmc
Effects of curcumin on the pharmacokinetics of amlodipine in rats and its potential mechanism
Effects of curcumin on the pharmacokinetics of amlodipine in rats and its potential mechanism Abstract Abstract Context Hyperlipidaemia and hypertension are often treated together with curcumin and amlodipine. It is necessary to investigate the drug-drug interaction between curcumin and amlodipine. Objective The intera...
PMC12546590
core_pubmed_pmc
Evaluation of cationic peptide-based nanogels as delivery systems for negatively charged molecules: a formulative study
Evaluation of cationic peptide-based nanogels as delivery systems for negatively charged molecules: a formulative study Abstract Abstract Peptide-based nanogels (NGs) represent a cutting-edge class of nanoscale drug delivery systems. Due to their structural properties, NGs platforms can encapsulate and protect therapeu...
PMC9697941
core_pubmed_pmc
Safety, Tolerability, and Serum/Tear Pharmacokinetics of Human Recombinant Epidermal Growth Factor Eyedrops in Healthy Subjects
Safety, Tolerability, and Serum/Tear Pharmacokinetics of Human Recombinant Epidermal Growth Factor Eyedrops in Healthy Subjects Abstract The purpose of this study was to evaluate the safety, tolerability, and pharmacokinetics (PKs) of rhEGF eyedrops after the administration of single and multiple doses in healthy subje...
PMC11927236
core_pubmed_pmc
Doxorubicin PK/PD modeling in multiple myeloma: towards in silico trials
Doxorubicin PK/PD modeling in multiple myeloma: towards in silico trials Abstract Doxorubicin (DOXO) is a well-known chemotherapy drug, which is widely used in the treatment of Multiple Myeloma (MM), a treatable but not curable type of blood cancer. Here, we propose a pharmacokinetics and pharmacodynamics (PK/PD) simul...
PMC12150788
core_pubmed_pmc
Pharmacokinetics, Safety and Antiviral Activity of Rilpivirine in Antiretroviral-naïve Children With HIV ≥6 to <12 Years Old: Week 48 and Final Analysis of Cohort 2 From the Open-label, Phase 2 PAINT Study
Pharmacokinetics, Safety and Antiviral Activity of Rilpivirine in Antiretroviral-naïve Children With HIV ≥6 to <12 Years Old: Week 48 and Final Analysis of Cohort 2 From the Open-label, Phase 2 PAINT Study Abstract Abstract Background: Rilpivirine has shown adequate antiviral activity, consistent pharmacokinetics and s...
PMC11946087
core_pubmed_pmc
Niosomes as Vesicular Nanocarriers in Cosmetics: Characterisation, Development and Efficacy
Niosomes as Vesicular Nanocarriers in Cosmetics: Characterisation, Development and Efficacy Abstract Abstract In an era of significant developments in cosmetic chemistry and growing demand for efficacious skincare products, the efficient delivery of active molecules has been a challenge in formulations of cosmetics. In...
PMC3499341
core_pubmed_pmc
Pharmacokinetics of engineered human monomeric and dimeric CH2 domains
Pharmacokinetics of engineered human monomeric and dimeric CH2 domains Abstract Therapeutic monoclonal antibodies have several advantages over small molecule drugs and small proteins and peptides, including a long serum half-life. The long serum half-life of IgG is due, in part, to its molecular weight (150kDa) and its...
PMC9923107
core_pubmed_pmc
Evaluation of the mutant selection window of danofloxacin against Actinobacillus pleuropneumoniae in an in vitro dynamic model
Evaluation of the mutant selection window of danofloxacin against Actinobacillus pleuropneumoniae in an in vitro dynamic model Abstract Abstract Introduction The rapid emergence and widespread spread of multidrug-resistant bacteria is a serious threat to the health of humans and animals. The pharmacokinetic/pharmacodyn...
PMC9931020
core_pubmed_pmc
Pharmacokinetics of panduratin A following oral administration of a Boesenbergia pandurata extract to rats
Pharmacokinetics of panduratin A following oral administration of a Boesenbergia pandurata extract to rats Abstract Boesenbergia pandurata and its major active ingredient, panduratin A (PAN), exhibit antibacterial, anti-oxidant, anti-inflammatory, and anti-obesity effects. We explored the time course of the plasma and ...
PMC7248759
core_pubmed_pmc
Isofraxidin: Synthesis, Biosynthesis, Isolation, Pharmacokinetic and Pharmacological Properties
Isofraxidin: Synthesis, Biosynthesis, Isolation, Pharmacokinetic and Pharmacological Properties Abstract Abstract Isofraxidin (7-hydroxy-6, 8-dimethoxy coumarin) (IF) is a hydroxy coumarin with several biological and pharmacological activities. The plant kingdom is of the most prominent sources of IF, which, among them...
PMC12958372
core_pubmed_pmc
Evexomostat (SDX-7320), a methionine aminopeptidase type 2 inhibitor, stimulates weight loss and inhibits obesity-accelerated tumor growth
Evexomostat (SDX-7320), a methionine aminopeptidase type 2 inhibitor, stimulates weight loss and inhibits obesity-accelerated tumor growth Abstract Obesity and diabetes are associated with worse prognosis for numerous malignancies. Both insulin resistance and altered levels of adipokines may explain the link between ob...
PMC12834370
core_pubmed_pmc
Mangiferin in human disease: Multifaceted mechanisms and applications (Review)
Mangiferin in human disease: Multifaceted mechanisms and applications (Review) Abstract Mangiferin (MGF) is a natural C-glucosyl xanthone with multitarget activity relevant to metabolic, inflammatory and cancer diseases. Notably, MGF modulates AMP-activated protein kinase, NF-κB, PI3K/AKT and MAPK signaling; through th...
PMC8621373
core_pubmed_pmc
New Bioactive Fused Triazolothiadiazoles as Bcl-2-Targeted Anticancer Agents
New Bioactive Fused Triazolothiadiazoles as Bcl-2-Targeted Anticancer Agents Abstract Abstract A series of 3-(6-substituted phenyl--triazolo[3,4-b]--thiadiazol-3-yl)-1H-indoles ( 5a – l ) were designed, synthesized and evaluated for anti-apoptotic Bcl-2-inhibitory activity. Synthesis of the target compounds was readily...
PMC10892660
core_pubmed_pmc
Physiologically Based Pharmacokinetic (PBPK) Modeling to Predict CYP3A-Mediated Drug Interaction between Saxagliptin and Nicardipine: Bridging Rat-to-Human Extrapolation
Physiologically Based Pharmacokinetic (PBPK) Modeling to Predict CYP3A-Mediated Drug Interaction between Saxagliptin and Nicardipine: Bridging Rat-to-Human Extrapolation Abstract The aim of this study was to predict the cytochrome P450 3A (CYP3A)-mediated drug–drug interactions (DDIs) between saxagliptin and nicardipin...
PMC10501372
core_pubmed_pmc
Effect of apatinib on the pharmacokinetics of tramadol and O-desmethyltramadol in rats
Effect of apatinib on the pharmacokinetics of tramadol and O-desmethyltramadol in rats Abstract Abstract Since the combination of anticancer drugs and opioids is very common, apatinib and tramadol are likely to be used in combination clinically. This study evaluated the effects of apatinib on the pharmacokinetics of tr...
PMC9687418
core_pubmed_pmc
Individualization of Mycophenolic Acid Therapy through Pharmacogenetic, Pharmacokinetic and Pharmacodynamic Testing
Individualization of Mycophenolic Acid Therapy through Pharmacogenetic, Pharmacokinetic and Pharmacodynamic Testing Abstract Mycophenolic acid (MPA) is a widely used immunosuppressive agent and exerts its effect by inhibiting inosine 5′-monophosphate dehydrogenase (IMPDH), the main regulating enzyme of purine metabolis...
PMC11899301
core_pubmed_pmc
Green Tea: Current Knowledge and Issues
Green Tea: Current Knowledge and Issues Abstract Abstract Green tea possesses antioxidant, anti-inflammatory, anticancer, and antimicrobial activities, reduces body weight, and slows down aging. These effects are primarily attributed to catechins contained in green tea leaves, particularly epigallocatechin-3-gallate. H...
PMC11876727
core_pubmed_pmc
An International Study of Factors Affecting Variability of Dosimetry Calculations, Part 4: Impact of Fitting Functions in Estimated Absorbed Doses
An International Study of Factors Affecting Variability of Dosimetry Calculations, Part 4: Impact of Fitting Functions in Estimated Absorbed Doses Abstract Individualized radiopharmaceutical therapies guided by patient-specific absorbed dose (AD) assessments using nuclear medicine imaging have the potential to improve ...
PMC5548818
core_pubmed_pmc
Efficacy, Safety and Pharmacokinetics of Up to Two Courses of the Rituximab Biosimilar CT-P10 Versus Innovator Rituximab in Patients with Rheumatoid Arthritis: Results up to Week 72 of a Phase I Randomized Controlled Trial
Efficacy, Safety and Pharmacokinetics of Up to Two Courses of the Rituximab Biosimilar CT-P10 Versus Innovator Rituximab in Patients with Rheumatoid Arthritis: Results up to Week 72 of a Phase I Randomized Controlled Trial Abstract Background CT-P10 is a biosimilar of innovator rituximab (RTX), a biological therapy use...
PMC11243602
core_pubmed_pmc
Colistin: Lights and Shadows of an Older Antibiotic
Colistin: Lights and Shadows of an Older Antibiotic Abstract The emergence of antimicrobial resistance represents a serious threat to public health and for infections due to multidrug-resistant (MDR) microorganisms, representing one of the most important causes of death worldwide. The renewal of old antimicrobials, suc...
PMC8742645
core_pubmed_pmc
Novel Bruton’s Tyrosine Kinase inhibitor remibrutinib: Drug‐drug interaction potential as a victim of CYP3A4 inhibitors based on clinical data and PBPK modeling
Novel Bruton’s Tyrosine Kinase inhibitor remibrutinib: Drug‐drug interaction potential as a victim of CYP3A4 inhibitors based on clinical data and PBPK modeling Abstract Abstract Remibrutinib, a novel oral Bruton’s Tyrosine Kinase inhibitor (BTKi) is highly selective for BTK, potentially mitigating the side effects of ...
PMC6059009
core_pubmed_pmc
Subcutaneous Furosemide in Heart Failure
Subcutaneous Furosemide in Heart Failure Abstract Highlights • Parenteral diuretics form the cornerstone of treatment of fluid overload in heart failure. The alkaline pH of furosemide USP precludes SC administration. • A novel buffered formulation of furosemide (pH 7.4) was developed for SC infusion using a wearable pa...
PMC10876507
core_pubmed_pmc
Chelator impact: investigating the pharmacokinetic behavior of copper-64 labeled PD-L1 radioligands
Chelator impact: investigating the pharmacokinetic behavior of copper-64 labeled PD-L1 radioligands Abstract Background Programmed cell death ligand 1 (PD-L1) plays a critical role in the tumor microenvironment and overexpression in several solid cancers has been reported. This was associated with a downregulation of t...
PMC12505756
core_pubmed_pmc
Association of CYP3A5 rs15524 and CYP3A7 rs776744 polymorphisms on tac IPV and clinical outcomes in early post-heart transplantation
Association of CYP3A5 rs15524 and CYP3A7 rs776744 polymorphisms on tac IPV and clinical outcomes in early post-heart transplantation Abstract Background The intrapatient variability (IPV) of tacrolimus (Tac) has gradually become a new index for the prognosis of organ transplantation. The gene polymorphism is involved i...
PMC3782673
core_pubmed_pmc
What Is the Most Effective Drug Delivery System for Cisplatin during the Treatment of Hepatic Tumors with Single-Session Transcatheter Chemotherapy? A Pilot Study
What Is the Most Effective Drug Delivery System for Cisplatin during the Treatment of Hepatic Tumors with Single-Session Transcatheter Chemotherapy? A Pilot Study Abstract Abstract Background/Aims The aim of this study was to determine the pharmacodynamics of cisplatin following three different treatment procedures for...
PMC12492365
core_pubmed_pmc
Drug Interaction of Dasatinib with Thymoquinone: A Pharmacokinetic Study in Rats
Drug Interaction of Dasatinib with Thymoquinone: A Pharmacokinetic Study in Rats Abstract Dasatinib (DAS), a multi-kinase inhibitor targeting Src and BCR-ABL families, is approved for Ph+ acute lymphoblastic leukemia (ALL) and chronic lymphocytic leukemia (CML). Its metabolism by CYP3A4 and transported by efflux pump P...
PMC9780873
core_pubmed_pmc
Analysis of Time-Dependent Pharmacokinetics Using In Vitro–In Vivo Extrapolation and Physiologically Based Pharmacokinetic Modeling
Analysis of Time-Dependent Pharmacokinetics Using In Vitro–In Vivo Extrapolation and Physiologically Based Pharmacokinetic Modeling Abstract SCR430, a sorafenib derivative, is an investigational drug exhibiting anti-tumor action. This study aimed to have a mechanistic understanding of SCR430’s time-dependent pharmacoki...
PMC7590375
core_pubmed_pmc
Phase Ib study of anti-CSF-1R antibody emactuzumab in combination with CD40 agonist selicrelumab in advanced solid tumor patients
Phase Ib study of anti-CSF-1R antibody emactuzumab in combination with CD40 agonist selicrelumab in advanced solid tumor patients Abstract Abstract Background This phase Ib study evaluated the safety, clinical activity, pharmacokinetics, and pharmacodynamics (PD) of emactuzumab (anti-colony stimulating factor 1 recepto...
PMC4749089
core_pubmed_pmc
Phosphate binders for the treatment of chronic kidney disease: role of iron oxyhydroxide
Phosphate binders for the treatment of chronic kidney disease: role of iron oxyhydroxide Abstract Chronic kidney disease-mineral bone disorder is frequent in patients with renal failure. It is characterized by abnormalities in mineral and bone metabolism with resulting hyperphosphatemia, low serum vitamin D, secondary ...
PMC4930485
core_pubmed_pmc
Once-daily delayed-release metformin lowers plasma glucose and enhances fasting and postprandial GLP-1 and PYY: results from two randomised trials
Once-daily delayed-release metformin lowers plasma glucose and enhances fasting and postprandial GLP-1 and PYY: results from two randomised trials Abstract Abstract Aims/hypothesis Delayed-release metformin (Metformin DR) was developed to maximise gut-based mechanisms of metformin action by targeting the drug to the il...
PMC8848942
core_pubmed_pmc
The INVENT COVID trial: a structured protocol for a randomized controlled trial investigating the efficacy and safety of intravenous imatinib mesylate (Impentri®) in subjects with acute respiratory distress syndrome induced by COVID-19
The INVENT COVID trial: a structured protocol for a randomized controlled trial investigating the efficacy and safety of intravenous imatinib mesylate (Impentri®) in subjects with acute respiratory distress syndrome induced by COVID-19 Abstract Abstract Background The coronavirus disease 2019 (COVID-19) pandemic has le...
PMC11179666
core_pubmed_pmc
Nose-to-Brain Drug Delivery and Physico-Chemical Properties of Nanosystems: Analysis and Correlation Studies of Data from Scientific Literature
Nose-to-Brain Drug Delivery and Physico-Chemical Properties of Nanosystems: Analysis and Correlation Studies of Data from Scientific Literature Abstract Background In the last few decades, nose-to-brain delivery has been investigated as an alternative route to deliver molecules to the Central Nervous System (CNS), bypa...
PMC6161083
core_pubmed_pmc
Beneficial Pharmacokinetic Drug Interactions: A Tool to Improve the Bioavailability of Poorly Permeable Drugs
Beneficial Pharmacokinetic Drug Interactions: A Tool to Improve the Bioavailability of Poorly Permeable Drugs Abstract Simultaneous oral intake of herbs, supplements, foods and drugs with other drug(s) may result in pharmacokinetic or pharmacodynamic interactions with the latter. Although these interactions are often a...
PMC10499425
core_pubmed_pmc
Variant‐based heritability assessment of dexmedetomidine and fentanyl clearance in pediatric patients
Variant‐based heritability assessment of dexmedetomidine and fentanyl clearance in pediatric patients Abstract Abstract Despite complex pathways of drug disposition, clinical pharmacogenetic predictors currently rely on only a few high effect variants. Quantification of the polygenic contribution to variability in drug...
PMC7023730
core_pubmed_pmc
A bioanalytical UHPLC based method used for the quantification of Thymoquinone-loaded-PLGA-nanoparticles in the treatment of epilepsy
A bioanalytical UHPLC based method used for the quantification of Thymoquinone-loaded-PLGA-nanoparticles in the treatment of epilepsy Abstract To formulate a nanoformulation (PLGA-NPs) and to improve brain bioavailability for thymoquinone (THQ) through intranasal (i.n.) drug delivery, using a newly UHPLC-PDA developed ...
PMC6601565
core_pubmed_pmc
Redirected optimized cell killing (ROCK®): A highly versatile multispecific fit-for-purpose antibody platform for engaging innate immunity
Redirected optimized cell killing (ROCK®): A highly versatile multispecific fit-for-purpose antibody platform for engaging innate immunity Abstract ABSTRACT Redirection of immune cells to efficiently eliminate tumor cells holds great promise. Natural killer cells (NK), macrophages, or T cells are specifically engaged w...
PMC7938517
core_pubmed_pmc
The pharmacokinetics of epinephrine/adrenaline autoinjectors
The pharmacokinetics of epinephrine/adrenaline autoinjectors Abstract Background For a century, epinephrine has been the drug of choice for acute treatment of systemic allergic reactions/anaphylaxis. For 40 years, autoinjectors have been used for the treatment of anaphylaxis. Over the last 20 years, intramuscular epine...
PMC12823057
core_pubmed_pmc
Unveiling sex differences in pancreatic ductal adenocarcinoma: Current evidence and future directions (Review)
Unveiling sex differences in pancreatic ductal adenocarcinoma: Current evidence and future directions (Review) Abstract Abstract Pancreatic ductal adenocarcinoma (PDAC) is the seventh leading cause of cancer-related death worldwide in both men and women. While sex-specific differences are increasingly recognized as cri...
PMC4970833
core_pubmed_pmc
Effect of food on the pharmacokinetics of TAS ‐102 and its efficacy and safety in patients with advanced solid tumors
Effect of food on the pharmacokinetics of TAS ‐102 and its efficacy and safety in patients with advanced solid tumors Abstract TAS ‐102, a novel oral antitumor agent, consists of trifluridine and tipiracil hydrochloride (molar ratio, 1:0.5). We investigated the effects of food on trifluridine and tipiracil hydrochlorid...
PMC7282146
core_pubmed_pmc
Initial dosage optimization of ciclosporin in pediatric Chinese patients who underwent bone marrow transplants based on population pharmacokinetics
Initial dosage optimization of ciclosporin in pediatric Chinese patients who underwent bone marrow transplants based on population pharmacokinetics Abstract Abstract Bone marrow transplants (BMT) are an established therapeutic strategy for patients with severe aplastic anemia, acute lymphoblastic leukemia, acute myeloi...
PMC9894996
core_pubmed_pmc
A PBPK model to evaluate zebrafish eleutheroembryos’ actual exposure: bisphenol A and analogs’ (AF, F, and S) case studies
A PBPK model to evaluate zebrafish eleutheroembryos’ actual exposure: bisphenol A and analogs’ (AF, F, and S) case studies Abstract Abstract The zebrafish eleutheroembryo model is increasingly used to assess the toxicity and developmental adverse effects of xenobiotics. However, the actual exposure is seldom measured (...
PMC6818770
core_pubmed_pmc
Sustained activity of novel THIOMAB antibody-antibiotic conjugate against Staphylococcus aureus in a mouse model: Longitudinal pharmacodynamic assessment by bioluminescence imaging
Sustained activity of novel THIOMAB antibody-antibiotic conjugate against Staphylococcus aureus in a mouse model: Longitudinal pharmacodynamic assessment by bioluminescence imaging Abstract Abstract Staphylococcus aureus ( S . aureus ) infections are a leading cause of death by an infectious agent. Survival within host...
PMC9315563
core_pubmed_pmc
Physiology-Based Pharmacokinetic Study on 18β-Glycyrrhetic Acid Mono-Glucuronide (GAMG) Prior to Glycyrrhizin in Rats
Physiology-Based Pharmacokinetic Study on 18β-Glycyrrhetic Acid Mono-Glucuronide (GAMG) Prior to Glycyrrhizin in Rats Abstract Abstract To understand that 18β-Glycyrrhetic acid 3-O-mono- β -D-glucuronide (GAMG) showed better pharmacological activity and drug-like properties than 18β-Glycyrrhizin (GL); a rapid and sensi...
PMC9574729
core_pubmed_pmc
Machine learning‐guided covariate selection for time‐to‐event models developed from a small sample of real‐world patients receiving bevacizumab treatment
Machine learning‐guided covariate selection for time‐to‐event models developed from a small sample of real‐world patients receiving bevacizumab treatment Abstract Abstract Therapeutic outcomes in patients with metastatic colorectal cancer (mCRC) receiving bevacizumab treatment are highly variable, and a reliable predic...
PMC8568457
core_pubmed_pmc
Human Sirtuin Regulators: The “Success” Stories
Human Sirtuin Regulators: The “Success” Stories Abstract The human sirtuins are a group of NAD + -dependent protein deacylases. They “erase” acyl modifications from lysine residues in various cellular targets including histones, transcription factors, and metabolic enzymes. Through these far-reaching activities, sirtui...
PMC5754001
core_pubmed_pmc
Quantitative systems toxicology
Quantitative systems toxicology Abstract The overarching goal of modern drug development is to optimize therapeutic benefits while minimizing adverse effects. However, inadequate efficacy and safety concerns remain to be the major causes of drug attrition in clinical development. For the past 80 years, toxicity testing...
PMC10847293
core_pubmed_pmc
Progress of Ginsenoside Rb1 in neurological disorders
Progress of Ginsenoside Rb1 in neurological disorders Abstract Abstract Ginseng is frequently used in traditional Chinese medicine to treat neurological disorders. The primary active component of ginseng is ginsenoside, which has been classified into more than 110 types based on their chemical structures. Ginsenoside R...