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PMC11379657 | core_pubmed_pmc | Model-informed drug development of envafolimab, a subcutaneously injectable PD-L1 antibody, in patients with advanced solid tumors | Model-informed drug development of envafolimab, a subcutaneously injectable PD-L1 antibody, in patients with advanced solid tumors Abstract Abstract Background and Objectives Envafolimab is the first and only globally approved subcutaneously injectable PD-L1 antibody for the treatment of instability-high (MSI-H) or DNA... |
PMC4896111 | core_pubmed_pmc | Relationship between Cefquinome PK/PD Parameters and Emergence of Resistance of Staphylococcus aureus in Rabbit Tissue-Cage Infection Model | Relationship between Cefquinome PK/PD Parameters and Emergence of Resistance of Staphylococcus aureus in Rabbit Tissue-Cage Infection Model Abstract In order to explore the relationship between different antibiotic dosing regimens and selective enrichment of resistant strains, tissue-cage infection model was establishe... |
PMC4365277 | core_pubmed_pmc | Preclinical pharmacokinetics, pharmacodynamics, and efficacy of RG7116: a novel humanized, glycoengineered anti-HER3 antibody | Preclinical pharmacokinetics, pharmacodynamics, and efficacy of RG7116: a novel humanized, glycoengineered anti-HER3 antibody Abstract Purpose RG7116 is a novel anti-HER3 therapeutic antibody that inhibits HER3 signalling and induces antibody-dependent cellular cytotoxicity of tumor cells due to a glycoengineered antib... |
PMC7084906 | core_pubmed_pmc | Application of an Inter-Species Extrapolation Method for the Prediction of Drug Interactions between Propolis and Duloxetine in Humans | Application of an Inter-Species Extrapolation Method for the Prediction of Drug Interactions between Propolis and Duloxetine in Humans Abstract Abstract Duloxetine (DLX) is a potent drug investigated for the treatment of depression and urinary incontinence. DLX is extensively metabolized in the liver by two P450 isozym... |
PMC12081501 | core_pubmed_pmc | Minimal Physiologically-Based Pharmacokinetic Modeling of Atenolol and Metoprolol Absorption in Malnourished Rats | Minimal Physiologically-Based Pharmacokinetic Modeling of Atenolol and Metoprolol Absorption in Malnourished Rats Abstract Abstract Background and Objective The pharmacokinetics of drugs can be altered by pathophysiological changes in the body that result from malnutrition. The objective of this study was to evaluate t... |
PMC8752104 | core_pubmed_pmc | Population pharmacokinetics and standard uptake value ratio of aducanumab, an amyloid plaque–removing agent, in patients with Alzheimer’s disease | Population pharmacokinetics and standard uptake value ratio of aducanumab, an amyloid plaque–removing agent, in patients with Alzheimer’s disease Abstract Abstract Aducanumab is a human immunoglobulin G1 anti‐amyloid beta (Aβ) antibody currently being evaluated for potential treatment of patients with early Alzheimer’s... |
PMC6320938 | core_pubmed_pmc | UPLC-MS/MS of Atractylenolide I, Atractylenolide II, Atractylenolide III, and Atractyloside A in Rat Plasma after Oral Administration of Raw and Wheat Bran-Processed Atractylodis Rhizoma | UPLC-MS/MS of Atractylenolide I, Atractylenolide II, Atractylenolide III, and Atractyloside A in Rat Plasma after Oral Administration of Raw and Wheat Bran-Processed Atractylodis Rhizoma Abstract Abstract Atractylodis Rhizoma is the dried rhizome of Atractylodes lancea (Thunb.) DC. or Atractylodes chinensis (DC.) Koidz... |
PMC9944701 | core_pubmed_pmc | In Silico Dosimetry Study of Tc99m-Tetrofosmin in Children Using a Novel PBPK Model in Humans Built from SPECT Imaging Data | In Silico Dosimetry Study of Tc99m-Tetrofosmin in Children Using a Novel PBPK Model in Humans Built from SPECT Imaging Data Abstract Purpose The aim of this work is to develop a Physiologically Based Pharmacokinetic model (PBPK) for the radiopharmaceutical Tc99m-Tetrofosmin in humans, from literature SPECT imaging data... |
PMC4480820 | core_pubmed_pmc | Modafinil and its metabolites enhance the anticonvulsant action of classical antiepileptic drugs in the mouse maximal electroshock-induced seizure model | Modafinil and its metabolites enhance the anticonvulsant action of classical antiepileptic drugs in the mouse maximal electroshock-induced seizure model Abstract Abstract Rationale Seizures occur when the excitability of brain circuits is not sufficiently restrained by inhibitory mechanisms. Although modafinil is repor... |
PMC11352548 | core_pubmed_pmc | Radioimmunotheragnosis in Cancer Research | Radioimmunotheragnosis in Cancer Research Abstract Abstract Simple Summary ImmunoPET involves tagging an antibody (a protein that targets cancer cells) with a radioactive substance that can be seen by imaging. This could non-invasively visualize where cancer is and how much of the target antigen is present, helping dec... |
PMC10493267 | core_pubmed_pmc | Establishment of a sensitive UPLC-MS/MS method to quantify safinamide in rat plasma | Establishment of a sensitive UPLC-MS/MS method to quantify safinamide in rat plasma Abstract A fast, simple, and sensitive ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was established for the quantification of safinamide in rat plasma. Plasma samples were treated with acetonitril... |
PMC4488889 | core_pubmed_pmc | Incidence of cardiovascular events and gastrointestinal bleeding in patients receiving clopidogrel with and without proton pump inhibitors: an updated meta-analysis | Incidence of cardiovascular events and gastrointestinal bleeding in patients receiving clopidogrel with and without proton pump inhibitors: an updated meta-analysis Abstract Abstract Background Dual antiplatelet therapy is the standard of care after coronary stent placement but increases the bleeding risk. The effects ... |
PMC7385321 | core_pubmed_pmc | Orally Administered Koumine Persists Longer in the Plasma of Aged Rats Than That of Adult Rats as Assessed by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry | Orally Administered Koumine Persists Longer in the Plasma of Aged Rats Than That of Adult Rats as Assessed by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry Abstract Abstract Aging leads to changes in nearly all pharmacokinetic phases. Koumine (KM), an alkaloid derived from Gelsemium elegans Benth., i... |
PMC9759297 | core_pubmed_pmc | Overview of Drug-Drug Interactions Between Ritonavir-Boosted Nirmatrelvir (Paxlovid) and Targeted Therapy and Supportive Care for Lung Cancer | Overview of Drug-Drug Interactions Between Ritonavir-Boosted Nirmatrelvir (Paxlovid) and Targeted Therapy and Supportive Care for Lung Cancer Abstract Introduction Oral administration of ritonavir-boosted nirmatrelvir (Paxlovid) was found to be promising in the treatment of coronavirus disease 2019. The active antivira... |
PMC9457984 | core_pubmed_pmc | Nanocrystal Suspensions for Enhancing the Oral Absorption of Albendazole | Nanocrystal Suspensions for Enhancing the Oral Absorption of Albendazole Abstract Abstract Albendazole (ABZ), an effective benzimidazole antiparasitic drug is limited by its poor solubility and oral bioavailability. In order to overcome its disadvantages, ABZ nanocrystals were prepared using a novel bottom-up method ba... |
PMC5762974 | core_pubmed_pmc | NPT-IIb Inhibition Does Not Improve Hyperphosphatemia in CKD | NPT-IIb Inhibition Does Not Improve Hyperphosphatemia in CKD Abstract Introduction Serum phosphate levels are insufficiently controlled in many patients with end-stage renal disease (ESRD), and novel therapeutic strategies are needed. Blocking intestinal phosphate absorption mediated by sodium-dependent phosphate co-tr... |
PMC11251383 | core_pubmed_pmc | Case report of pharmacokinetic analysis of continuous intravenous infusion of fentanyl in a patient with severe burn: burn shock stage complicates pain management | Case report of pharmacokinetic analysis of continuous intravenous infusion of fentanyl in a patient with severe burn: burn shock stage complicates pain management Abstract Abstract Background Fentanyl is widely used as an analgesic and sedative for patients with severe burn injuries in intensive care units. However, ph... |
PMC7778363 | core_pubmed_pmc | Inhaled tigecycline is effective against Mycobacterium abscessus in vitro and in vivo | Inhaled tigecycline is effective against Mycobacterium abscessus in vitro and in vivo Abstract Abstract Background Mycobacterium abscessus causes chronic pulmonary infections. Owing to its resistance to most classes of antibiotics, treatment is complex and cure rates are only 45%. Tigecycline is active against M. absce... |
PMC3419763 | core_pubmed_pmc | A Simple Dosing Scheme for Intravenous Busulfan Based on Retrospective Population Pharmacokinetic Analysis in Korean Patients | A Simple Dosing Scheme for Intravenous Busulfan Based on Retrospective Population Pharmacokinetic Analysis in Korean Patients Abstract Abstract Busulfan is an antineoplastic agent with a narrow therapeutic window. A post-hoc population pharmacokinetic analysis of a prospective randomized trial for comparison of four-ti... |
PMC8228864 | core_pubmed_pmc | Model-Informed Optimization of a Pediatric Clinical Pharmacokinetic Trial of a New Spironolactone Liquid Formulation | Model-Informed Optimization of a Pediatric Clinical Pharmacokinetic Trial of a New Spironolactone Liquid Formulation Abstract Quantitative pharmacology brings important advantages in the design and conduct of pediatric clinical trials. Herein, we demonstrate the application of a model-based approach to select doses and... |
PMC6994827 | core_pubmed_pmc | Developing an animal model to detect drug–drug interactions impacting drug-induced respiratory depression ⋆ | Developing an animal model to detect drug–drug interactions impacting drug-induced respiratory depression ⋆ Abstract Highlights • A model to assess drug interaction effects on drug induced respiratory depression. • Plasma oxycodone level AUC was 113 % higher when the two drugs were co-administered. • Diazepam showed sy... |
PMC10604233 | core_pubmed_pmc | In Silico Approaches to Developing Novel Glycogen Synthase Kinase 3β (GSK-3β) | In Silico Approaches to Developing Novel Glycogen Synthase Kinase 3β (GSK-3β) Abstract Abstract Alzheimer’s disease (AD) is caused by plaque agglomeration and entanglement in several areas of the neural cells, which leads to apoptosis. The main etiology of AD is senile dementia, which is linked to amyloid-beta (Aβ) der... |
PMC11083391 | core_pubmed_pmc | Insights into Inhalation Drug Disposition: The Roles of Pulmonary Drug-Metabolizing Enzymes and Transporters | Insights into Inhalation Drug Disposition: The Roles of Pulmonary Drug-Metabolizing Enzymes and Transporters Abstract The past five decades have witnessed remarkable advancements in the field of inhaled medicines targeting the lungs for respiratory disease treatment. As a non-invasive drug delivery route, inhalation th... |
PMC12522909 | core_pubmed_pmc | Optimal antibiotic use in the intensive care unit | Optimal antibiotic use in the intensive care unit Abstract Abstract Background Antibiotic resistance has emerged as one of the most important factors influencing the outcomes of patients with life-threatening infections in the ICU. The increasing prevalence of antibiotic-resistant infections globally highlights the imp... |
PMC4518424 | core_pubmed_pmc | Detection of antidiabetic activity by crude paratoid gland secretions from common Indian toad (bufomelano stictus) | Detection of antidiabetic activity by crude paratoid gland secretions from common Indian toad (bufomelano stictus) Abstract Abstract Background: Amphibians have provided a remarkable array of biological active compounds, which are secreted from socalled granular skin glands which serve to protect the amphibians from pr... |
PMC3267521 | core_pubmed_pmc | Insulin detemir for the treatment of obese patients with type 2 diabetes | Insulin detemir for the treatment of obese patients with type 2 diabetes Abstract The risk for developing type 2 diabetes (T2DM) is greater among obese individuals. Following onset of the disease, patients with T2DM become more likely to be afflicted with diabetic micro- and macrovascular complications. Decreasing body... |
PMC12941667 | core_pubmed_pmc | Clinical Application of Microvolume LC–MS/MS for Therapeutic Drug Monitoring of Immunosuppressants in Solid-Organ Transplant Recipients | Clinical Application of Microvolume LC–MS/MS for Therapeutic Drug Monitoring of Immunosuppressants in Solid-Organ Transplant Recipients Abstract Abstract Background/Objectives: Therapeutic drug monitoring (TDM) is essential for optimizing immunosuppressive therapy in solid-organ transplant recipients by maintaining eff... |
PMC9294864 | core_pubmed_pmc | Approaches to accelerating the study of new antiretrovirals in pregnancy | Approaches to accelerating the study of new antiretrovirals in pregnancy Abstract Abstract Introduction Women who are pregnant or who could become pregnant experience delayed access to or underinformed use of important new antiretroviral (ARV) drugs because of traditional drug development processes that ostensibly aim ... |
PMC10985027 | core_pubmed_pmc | Construction and characterization of a humanized SLCO1B1 rat model with its application in evaluating the uptake of different statins | Construction and characterization of a humanized SLCO1B1 rat model with its application in evaluating the uptake of different statins Abstract Abstract Organic anion-transporting polypeptides 1B1 (OATP1B1) plays a crucial role in the transport of statins. However, there are too few animal models related to OATP1B1, esp... |
PMC6082003 | core_pubmed_pmc | Pharmacokinetics and Oxidation Parameters in Volunteers Supplemented with Microencapsulated Docosahexaenoic Acid | Pharmacokinetics and Oxidation Parameters in Volunteers Supplemented with Microencapsulated Docosahexaenoic Acid Abstract Abstract Context: Docosahexaenoic acid (DHA) is an omega-3 fatty acid essential for cardiovascular health, brain development, and reproductive function. Due to hydrophobicity and low DHA bioavailabi... |
PMC6252322 | core_pubmed_pmc | Population Pharmacokinetic/Pharmacodynamic Model-Guided Dosing Optimization of a Novel Sedative HR7056 in Chinese Healthy Subjects | Population Pharmacokinetic/Pharmacodynamic Model-Guided Dosing Optimization of a Novel Sedative HR7056 in Chinese Healthy Subjects Abstract HR7056 is a new benzodiazepine, showing more faster acting onset and recovery than currently available short-acting sedatives. To avoid inadequate anesthesia and predict return of ... |
PMC12339985 | core_pubmed_pmc | In Silico discovery of novel androgen receptor inhibitors for prostate cancer therapy using virtual screening, molecular docking, and molecular dynamics simulations | In Silico discovery of novel androgen receptor inhibitors for prostate cancer therapy using virtual screening, molecular docking, and molecular dynamics simulations Abstract This study employs an integrated computational approach to identify novel androgen receptor (AR) inhibitors, a key target in prostate cancer (PC) ... |
PMC8938336 | core_pubmed_pmc | Structure-based screening of natural product libraries in search of potential antiviral drug-leads as first-line treatment to COVID-19 infection | Structure-based screening of natural product libraries in search of potential antiviral drug-leads as first-line treatment to COVID-19 infection Abstract The study focuses on identifying and screening natural products (NPs) based on their structural similarities with chemical drugs followed by their possible use in fir... |
PMC8231812 | core_pubmed_pmc | Antimicrobial, Antioxidant, Anti-Acetylcholinesterase, Antidiabetic, and Pharmacokinetic Properties of Carum carvi L. and Coriandrum sativum L. Essential Oils Alone and in Combination | Antimicrobial, Antioxidant, Anti-Acetylcholinesterase, Antidiabetic, and Pharmacokinetic Properties of Carum carvi L. and Coriandrum sativum L. Essential Oils Alone and in Combination Abstract Abstract Herbs and spices have been used since antiquity for their nutritional and health properties, as well as in traditional... |
PMC11791192 | core_pubmed_pmc | Personalized metronomic radiopharmaceutical therapy through injection profile optimization via physiologically based pharmacokinetic (PBPK) modeling | Personalized metronomic radiopharmaceutical therapy through injection profile optimization via physiologically based pharmacokinetic (PBPK) modeling Abstract Each treatment cycle of radiopharmaceutical therapy (RPT) is administered as a single dose. We aimed to investigate a personalized metronomic RPT paradigm, employ... |
PMC8995034 | core_pubmed_pmc | Therapeutic treatment with an oral prodrug of the remdesivir parental nucleoside is protective against SARS-CoV-2 pathogenesis in mice | Therapeutic treatment with an oral prodrug of the remdesivir parental nucleoside is protective against SARS-CoV-2 pathogenesis in mice Abstract Abstract The coronavirus disease 2019 (COVID-19) pandemic remains uncontrolled despite the rapid rollout of safe and effective severe acute respiratory syndrome coronavirus 2 (... |
PMC11557512 | core_pubmed_pmc | Concentration‐QTcF analysis of quizartinib in patients with newly diagnosed FLT3‐internal‐tandem‐duplication‐positive acute myeloid leukemia | Concentration‐QTcF analysis of quizartinib in patients with newly diagnosed FLT3‐internal‐tandem‐duplication‐positive acute myeloid leukemia Abstract Abstract Quizartinib prolongs QT interval through inhibition of the slow delayed rectifier potassium current (I Ks ). We used non‐linear mixed‐effects modeling to explore... |
PMC7248203 | core_pubmed_pmc | Validation of a Double-Sandwich Enzyme-Linked Immunoassay for Pharmacokinetic Study of an rh-aFGF Hydrogel in Rat Skin and Serum | Validation of a Double-Sandwich Enzyme-Linked Immunoassay for Pharmacokinetic Study of an rh-aFGF Hydrogel in Rat Skin and Serum Abstract Abstract In this study, we validated a double-sandwich enzyme-linked immunosorbent assay (ELISA) to investigate the pharmacokinetics of a recombinant human acidic fibroblast growth f... |
PMC9178791 | core_pubmed_pmc | Temporin B Forms Hetero-Oligomers with Temporin L, Modifies Its Membrane Activity, and Increases the Cooperativity of Its Antibacterial Pharmacodynamic Profile | Temporin B Forms Hetero-Oligomers with Temporin L, Modifies Its Membrane Activity, and Increases the Cooperativity of Its Antibacterial Pharmacodynamic Profile Abstract Abstract The pharmacodynamic profile of antimicrobial peptides (AMPs) and their in vivo synergy are two factors that are thought to restrict resistance... |
PMC6201795 | core_pubmed_pmc | A first-in-human, randomized, double-blind, placebo-controlled, single and multiple ascending oral dose study to assess the safety, tolerability, and pharmacokinetics of BZF961 with and without ritonavir in healthy adult volunteers | A first-in-human, randomized, double-blind, placebo-controlled, single and multiple ascending oral dose study to assess the safety, tolerability, and pharmacokinetics of BZF961 with and without ritonavir in healthy adult volunteers Abstract Abstract Objective: Infection with hepatitis C virus is the leading indication ... |
PMC6767429 | core_pubmed_pmc | Safety, Pharmacokinetics, and Pharmacodynamics of the Autotaxin Inhibitor GLPG1690 in Healthy Subjects: Phase 1 Randomized Trials | Safety, Pharmacokinetics, and Pharmacodynamics of the Autotaxin Inhibitor GLPG1690 in Healthy Subjects: Phase 1 Randomized Trials Abstract Abstract GLPG1690 is a novel autotaxin inhibitor in development for the treatment of idiopathic pulmonary fibrosis (IPF). We report phase 1 studies investigating the safety, tolerab... |
PMC7412782 | core_pubmed_pmc | Bismuth chelate as a contrast agent for X-ray computed tomography | Bismuth chelate as a contrast agent for X-ray computed tomography Abstract Abstract Backgrounds Due to the unexpected side effects of the iodinated contrast agents, novel contrast agents for X-ray computed tomography (CT) imaging are urgently needed. Nanoparticles made by heavy metal elements are often employed, such a... |
PMC10272307 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling for development and applications of a virtual celiac disease population using felodipine as a model drug | Physiologically based pharmacokinetic modeling for development and applications of a virtual celiac disease population using felodipine as a model drug Abstract Abstract In celiac disease (CeD), gastrointestinal CYP3A4 abundance and morphology is affected by the severity of disease. Therefore, exposure to CYP3A4 substr... |
PMC10349185 | core_pubmed_pmc | Model‐based approach to identify predictors of paclitaxel‐induced myelosuppression in “real‐world” administration | Model‐based approach to identify predictors of paclitaxel‐induced myelosuppression in “real‐world” administration Abstract Abstract Taxanes are currently the most frequently used chemotherapeutic agents in cancer care, where real‐world use has focused on minimizing adverse events and standardizing the delivery. Myelosu... |
PMC6114106 | core_pubmed_pmc | In vitro and in vivo pharmacodynamics of three novel antileishmanial lead series | In vitro and in vivo pharmacodynamics of three novel antileishmanial lead series Abstract Objectives Three new chemical series (bicyclic nitroimidazoles, aminopyrazoles and oxaboroles) were selected by Drugs for Neglected Diseases initiative as potential new drug leads for leishmaniasis. Pharmacodynamics studies includ... |
PMC10984015 | core_pubmed_pmc | Dynamic PET Reveals Compartmentalized Brain and Lung Tissue Antibiotic Exposures | Dynamic PET Reveals Compartmentalized Brain and Lung Tissue Antibiotic Exposures Abstract Abstract Tuberculosis (TB) remains a leading cause of death, but antibiotic treatments for tuberculous meningitis, the deadliest form of TB, are based on those developed for pulmonary TB and not optimized for brain penetration. He... |
PMC6008465 | core_pubmed_pmc | Safety, pharmacokinetics, and preliminary efficacy of E6201 in patients with advanced solid tumours, including melanoma: results of a phase 1 study | Safety, pharmacokinetics, and preliminary efficacy of E6201 in patients with advanced solid tumours, including melanoma: results of a phase 1 study Abstract Background This phase 1 first-in-human study aimed to determine the maximum-tolerated dose (MTD), dose-limiting toxicities, and safety of E6201, and to establish r... |
PMC12217483 | core_pubmed_pmc | Synergistic combination of next-generation polymyxin MRX-8 and meropenem against carbapenem-resistant A. baumannii | Synergistic combination of next-generation polymyxin MRX-8 and meropenem against carbapenem-resistant A. baumannii Abstract ABSTRACT MRX-8 is a new next-generation polymyxin with potent antibacterial activity against carbapenem-resistant Acinetobacter baumannii (CRAB). This study evaluated the MRX-8 and meropenem combi... |
PMC4263154 | core_pubmed_pmc | Investigation of Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single and Multiple Doses of a Long-Acting α-MSH Analog in Healthy Overweight and Obese Subjects | Investigation of Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single and Multiple Doses of a Long-Acting α-MSH Analog in Healthy Overweight and Obese Subjects Abstract MC4-NN2-0453 is a novel, long-acting, selective, melanocortin-4-receptor agonist developed for treatment of obesity. This first-human... |
PMC6981711 | core_pubmed_pmc | Insight into the Molecular Interaction of Cloxyquin (5-chloro-8-hydroxyquinoline) with Bovine Serum Albumin: Biophysical Analysis and Computational Simulation | Insight into the Molecular Interaction of Cloxyquin (5-chloro-8-hydroxyquinoline) with Bovine Serum Albumin: Biophysical Analysis and Computational Simulation Abstract Cloxyquin is a potential therapeutic compound possessing various bioactivities, especially antibacterial, antifungal, cardioprotective, and pain relief ... |
PMC3410379 | core_pubmed_pmc | The role of regulated clinical trials in the development of bacteriophage therapeutics | The role of regulated clinical trials in the development of bacteriophage therapeutics Abstract Antibiotic resistance is now recognized as a major, global threat to human health and the need for the development of novel antibacterial therapies has become urgent. Lytic bacteriophages (phages) targeting individual bacter... |
PMC10894245 | core_pubmed_pmc | Neurophysiological evidence that frontoparietal connectivity and GABA-A receptor changes underpin the antidepressant response to ketamine | Neurophysiological evidence that frontoparietal connectivity and GABA-A receptor changes underpin the antidepressant response to ketamine Abstract Revealing the acute cortical pharmacodynamics of an antidepressant dose of ketamine in humans with depression is key to determining the specific mechanism(s) of action for a... |
PMC5380267 | core_pubmed_pmc | Influence of cyclosporine and everolimus on the main mycophenolate mofetil pharmacokinetic parameters | Influence of cyclosporine and everolimus on the main mycophenolate mofetil pharmacokinetic parameters Abstract Abstract The objective of the present study was to assess the effect of cyclosporine (CsA) on the pharmacokinetic parameters of mycophenolic acid (MPA), an active mycophenolate mofetil (MMF) metabolite, and to... |
PMC10374488 | core_pubmed_pmc | Implementation of non-linear mixed effects models defined by fractional differential equations | Implementation of non-linear mixed effects models defined by fractional differential equations Abstract Abstract Fractional differential equations (FDEs), i.e. differential equations with derivatives of non-integer order, can describe certain experimental datasets more accurately than classic models and have found appl... |
PMC9495226 | core_pubmed_pmc | Use of Antibiotics in Preterm Newborns | Use of Antibiotics in Preterm Newborns Abstract Due to complex maturational and physiological changes that characterize neonates and affect their response to pharmacological treatments, neonatal pharmacology is different from children and adults and deserves particular attention. Although preterms are usually considere... |
PMC11720353 | core_pubmed_pmc | Clove Essential Oil as a Source of Antitumoral Compounds Capable of Crossing the Blood–Brain Barrier: A Focus on the Effects of β-Caryophyllene and Eugenol in a Glioblastoma Cell Line | Clove Essential Oil as a Source of Antitumoral Compounds Capable of Crossing the Blood–Brain Barrier: A Focus on the Effects of β-Caryophyllene and Eugenol in a Glioblastoma Cell Line Abstract This study aimed to investigate β-Caryophyllene (BCA) pharmacokinetics as well as the potential antitumor activity and mechanis... |
PMC10720006 | core_pubmed_pmc | Promising 8-Aminoquinoline-Based Metal Complexes in the Modulation of SIRT1/3-FOXO3a Axis against Oxidative Damage-Induced Preclinical Neurons | Promising 8-Aminoquinoline-Based Metal Complexes in the Modulation of SIRT1/3-FOXO3a Axis against Oxidative Damage-Induced Preclinical Neurons Abstract The discovery of novel bioactive molecules as potential multifunctional neuroprotective agents has clinically drawn continual interest due to devastating oxidative dama... |
PMC9412689 | core_pubmed_pmc | Lipomics: A Potential Carrier for the Intravenous Delivery of Lipophilic and Hydrophilic Drugs | Lipomics: A Potential Carrier for the Intravenous Delivery of Lipophilic and Hydrophilic Drugs Abstract In the present work, we propose the development of a novel carrier that does not need organic solvents for its preparation and with the potential for the intravenous delivery of lipophilic and hydrophilic drugs. Name... |
PMC12944227 | core_pubmed_pmc | Pharmacogenomics of Antineoplastic Therapy in Children: Genetic Determinants of Toxicity and Efficacy | Pharmacogenomics of Antineoplastic Therapy in Children: Genetic Determinants of Toxicity and Efficacy Abstract Abstract Over the past decades, remarkable progress in multimodal therapy has significantly improved survival outcomes for children with cancer. Yet, considerable variability in treatment response and toxicity... |
PMC8402096 | core_pubmed_pmc | Just a Reflection: Does Drug Repurposing Perpetuate Sex-Gender Bias in the Safety Profile? | Just a Reflection: Does Drug Repurposing Perpetuate Sex-Gender Bias in the Safety Profile? Abstract Abstract Vaccines constitute a strategy to reduce the burden of COVID-19, but the treatment of COVID-19 is still a challenge. The lack of approved drugs for severe COVID-19 makes repurposing or repositioning of approved ... |
PMC6916612 | core_pubmed_pmc | Exposure and response analysis of aleglitazar on cardiovascular risk markers and safety outcomes: An analysis of the AleCardio trial | Exposure and response analysis of aleglitazar on cardiovascular risk markers and safety outcomes: An analysis of the AleCardio trial Abstract Abstract Aims The AleCardio trial aimed to characterize the efficacy and safety of peroxisome proliferator‐activated receptor‐αγ agonist aleglitazar in patients with type 2 diabe... |
PMC10761262 | core_pubmed_pmc | A new PK/PD target for assessing efficacy of micafungin against Candida parapsilosis | A new PK/PD target for assessing efficacy of micafungin against Candida parapsilosis Abstract Abstract Background Pharmacokinetic/pharmacodynamic (PK/PD) targets of echinocandins failed to support current clinical breakpoints of Candida parapsilosis as the PTA is low for susceptible isolates despite the good clinical e... |
PMC10384042 | core_pubmed_pmc | Modeling and Simulation as a Tool to Assess Voriconazole Exposure in the Central Nervous System | Modeling and Simulation as a Tool to Assess Voriconazole Exposure in the Central Nervous System Abstract Voriconazole is a triazole antifungal used empirically for the treatment of complicated meningitis associated with Cryptococcus neoformans . Biopsy studies show that the drug exhibits adequate brain penetration alth... |
PMC6440567 | core_pubmed_pmc | Ceftazidime‐Avibactam Population Pharmacokinetic Modeling and Pharmacodynamic Target Attainment Across Adult Indications and Patient Subgroups | Ceftazidime‐Avibactam Population Pharmacokinetic Modeling and Pharmacodynamic Target Attainment Across Adult Indications and Patient Subgroups Abstract Ceftazidime‐avibactam is a novel β‐lactam/β‐lactamase inhibitor combination for the treatment of serious infections caused by resistant gram‐negative pathogens. Populat... |
PMC5784002 | core_pubmed_pmc | Clinical Pharmacokinetics of Systemically Administered Antileishmanial Drugs | Clinical Pharmacokinetics of Systemically Administered Antileishmanial Drugs Abstract Abstract This review describes the pharmacokinetic properties of the systemically administered antileishmanial drugs pentavalent antimony, paromomycin, pentamidine, miltefosine and amphotericin B (AMB), including their absorption, dis... |
PMC6405003 | core_pubmed_pmc | Intraperitoneal aerosolization of albumin-stabilized paclitaxel nanoparticles (Abraxane™) for peritoneal carcinomatosis – a phase I first-in-human study | Intraperitoneal aerosolization of albumin-stabilized paclitaxel nanoparticles (Abraxane™) for peritoneal carcinomatosis – a phase I first-in-human study Abstract Abstract Background Nanoparticles hold considerable promise for aerosol-based intraperitoneal delivery in patients with carcinomatosis. Recently, results from... |
PMC6624454 | core_pubmed_pmc | Pharmacokinetic variability of beta‐adrenergic blocking agents used in cardiology | Pharmacokinetic variability of beta‐adrenergic blocking agents used in cardiology Abstract Abstract The aim of this study was to evaluate the pharmacokinetic variability of beta‐adrenergic blocking agents used in cardiology by reviewing single‐dose and steady‐state pharmacokinetic studies from the literature. PubMed wa... |
PMC6587782 | core_pubmed_pmc | Moderate Renal Impairment Does Not Impact the Ability of CSL112 (Apolipoprotein A‐I [Human]) to Enhance Cholesterol Efflux Capacity | Moderate Renal Impairment Does Not Impact the Ability of CSL112 (Apolipoprotein A‐I [Human]) to Enhance Cholesterol Efflux Capacity Abstract Abstract CSL112 (apolipoprotein A‐I [human]) is a novel intravenous formulation of plasma‐derived apolipoprotein A‐I (apoA‐I) that enhances cholesterol efflux capacity. Renal impa... |
PMC7817199 | core_pubmed_pmc | Pharmacokinetic modeling reveals parameters that govern tumor targeting and delivery by a pH-Low Insertion Peptide (pHLIP) | Pharmacokinetic modeling reveals parameters that govern tumor targeting and delivery by a pH-Low Insertion Peptide (pHLIP) Abstract Significance Tumors exhibit an acidic extracellular microenvironment that is accentuated at cell surfaces. As a result, they can be targeted by a pH-Low Insertion Peptide (pHLIP), an acid-... |
PMC4761233 | core_pubmed_pmc | Application of a Physiologically Based Pharmacokinetic Model to Study Theophylline Metabolism and Its Interactions With Ciprofloxacin and Caffeine | Application of a Physiologically Based Pharmacokinetic Model to Study Theophylline Metabolism and Its Interactions With Ciprofloxacin and Caffeine Abstract Theophylline is a commonly used bronchodilator. However, due to its narrow therapeutic range, moderate elevation of serum concentration can result in adverse drug r... |
PMC4129431 | core_pubmed_pmc | Is the standard dose of amoxicillin-clavulanic acid sufficient? | Is the standard dose of amoxicillin-clavulanic acid sufficient? Abstract Background The pharmacodynamic (PD) efficacy target of amoxicillin is 40% time above the minimal inhibition concentration (40%T > MIC). Recent studies of other antibiotics have shown that PD-efficacy targets are not always reached. The aim of this... |
PMC6281656 | core_pubmed_pmc | Lecithin-Stabilized Polymeric Micelles (L sb PMs) for Delivering Quercetin: Pharmacokinetic Studies and Therapeutic Effects of Quercetin Alone and in Combination with Doxorubicin | Lecithin-Stabilized Polymeric Micelles (L sb PMs) for Delivering Quercetin: Pharmacokinetic Studies and Therapeutic Effects of Quercetin Alone and in Combination with Doxorubicin Abstract In this study, lecithin-stabilized polymeric micelles (L sb PMs) were prepared to load quercetin (QUE) in order to improve its bioav... |
PMC12035729 | core_pubmed_pmc | Bioequivalence and safety assessment of sorafenib tosylate tablets in healthy Chinese subjects under fasting conditions | Bioequivalence and safety assessment of sorafenib tosylate tablets in healthy Chinese subjects under fasting conditions Abstract Objective This study aimed to assess the bioequivalence and safety of two formulations of sorafenib in healthy Chinese subjects under fasting conditions. Methods A single-center, randomized, ... |
PMC6977018 | core_pubmed_pmc | Noninvasive and real-time pharmacokinetics imaging of polymeric nanoagents in the thoracoepigastric vein networks of living mice | Noninvasive and real-time pharmacokinetics imaging of polymeric nanoagents in the thoracoepigastric vein networks of living mice Abstract Abstract. Noninvasive and real-time visualization of the thoracoepigastric veins (TVs) of living mice was demonstrated by using two-photon excitation (TPE) optical imaging with a Eu-... |
PMC8813707 | core_pubmed_pmc | Pharmacokinetics and Exposure–Response of Vosoritide in Children with Achondroplasia | Pharmacokinetics and Exposure–Response of Vosoritide in Children with Achondroplasia Abstract Abstract Background and Objective Vosoritide, an analog of C-type natriuretic peptide, has been developed for the treatment of children with achondroplasia. The pharmacokinetics of vosoritide and relationships between plasma e... |
PMC11313540 | core_pubmed_pmc | The Effect of Thickened Water on Ciprofloxacin Pharmacokinetics: A Comparative Study in Adult Males | The Effect of Thickened Water on Ciprofloxacin Pharmacokinetics: A Comparative Study in Adult Males Abstract Abstract Background/Objectives : The use of food thickeners with ciprofloxacin tablets may result in a gelatinous appearance and experience delayed dissolution, which presents a challenge for the drug’s efficacy... |
PMC11253049 | core_pubmed_pmc | Generation of anti-SN38 antibody for loading efficacy and therapeutic monitoring of SN38-containing therapeutics | Generation of anti-SN38 antibody for loading efficacy and therapeutic monitoring of SN38-containing therapeutics Abstract SN38, one of the most potent anti-tumor analogues of the camptothecins (CPTs), has limitations in its direct formulation as an anticancer agent due to its super toxicity and poor solubility in water... |
PMC12195666 | core_pubmed_pmc | Harnessing the Therapeutic Potential of Pomegranate Peel-Derived Bioactive Compounds in Pancreatic Cancer: A Computational Approach | Harnessing the Therapeutic Potential of Pomegranate Peel-Derived Bioactive Compounds in Pancreatic Cancer: A Computational Approach Abstract Abstract Background/Objectives : Pomegranate (Punica granatum) peel, often discarded as waste, contains abundant bioactive compounds such as polyphenols, vitamins, flavonoids, tan... |
PMC8302467 | core_pubmed_pmc | Quantitative HPLC-MS/MS determination of Nuc, the active metabolite of remdesivir, and its pharmacokinetics in rat | Quantitative HPLC-MS/MS determination of Nuc, the active metabolite of remdesivir, and its pharmacokinetics in rat Abstract Remdesivir is a nucleotide analog prodrug that has received much attention since the outbreak of the COVID-19 pandemic in December 2019. GS-441524 (Nuc) is the active metabolite of remdesivir and ... |
PMC11365720 | core_pubmed_pmc | Flecainide Toxicity From Clinical Pharmacology Perspectives | Flecainide Toxicity From Clinical Pharmacology Perspectives Abstract Abstract We report a case comparing the measured half-life of flecainide with the half-life stated on the label. An 84-year-old woman presented with symptoms of anorexia and exertional dyspnea. She had undergone mitral and aortic valve replacements an... |
PMC8129133 | core_pubmed_pmc | Polymer-free corticosteroid dimer implants for controlled and sustained drug delivery | Polymer-free corticosteroid dimer implants for controlled and sustained drug delivery Abstract Polymeric drug carriers are widely used for providing temporal and/or spatial control of drug delivery, with corticosteroids being one class of drugs that have benefitted from their use for the treatment of inflammatory-media... |
PMC7496950 | core_pubmed_pmc | Handling and performance characteristics of a new small caliber radiopaque embolic microsphere | Handling and performance characteristics of a new small caliber radiopaque embolic microsphere Abstract Abstract The in vitro and in vivo handling and performance characteristics of a small caliber radiopaque embolic microsphere, 40–90 μm DC Bead LUMI™ (LUMI40‐90), were studied. Microsphere drug loading and elution and... |
PMC7032150 | core_pubmed_pmc | Virtual population pharmacokinetic using physiologically based pharmacokinetic model for evaluating bioequivalence of oral lacidipine formulations in dogs | Virtual population pharmacokinetic using physiologically based pharmacokinetic model for evaluating bioequivalence of oral lacidipine formulations in dogs Abstract The aim of the present study was to investigate virtual population pharmacokinetic using physiologically based pharmacokinetic (PBPK) model for evaluating b... |
PMC9320654 | core_pubmed_pmc | Study on In Vitro Metabolism and In Vivo Pharmacokinetics of Beauvericin | Study on In Vitro Metabolism and In Vivo Pharmacokinetics of Beauvericin Abstract Beauvericin (BEA) is a well-known mycotoxin produced by many fungi, including Beaveria bassiana . The purpose of this study was to evaluate the in vitro distribution and metabolism characteristics as well as the in vivo pharmacokinetic (P... |
PMC6947033 | core_pubmed_pmc | Development of Prodrugs for PDT-Based Combination Therapy Using a Singlet-Oxygen-Sensitive Linker and Quantitative Systems Pharmacology | Development of Prodrugs for PDT-Based Combination Therapy Using a Singlet-Oxygen-Sensitive Linker and Quantitative Systems Pharmacology Abstract Photodynamic therapy (PDT) has become an effective treatment for certain types of solid tumors. The combination of PDT with other therapies has been extensively investigated i... |
PMC7384084 | core_pubmed_pmc | Pharmacokinetics of Gepotidacin in Renal Impairment | Pharmacokinetics of Gepotidacin in Renal Impairment Abstract Abstract Gepotidacin is a novel triazaacenaphthylene bacterial topoisomerase inhibitor. In this phase 1, nonrandomized, open‐label, parallel‐group, multicenter, multipart study, the pharmacokinetics, safety, and tolerability of a single intravenous (IV) dose ... |
PMC9673935 | core_pubmed_pmc | Dose Adjustment of Poly (ADP‑Ribose) Polymerase Inhibitors in Patients with Hepatic or Renal Impairment | Dose Adjustment of Poly (ADP‑Ribose) Polymerase Inhibitors in Patients with Hepatic or Renal Impairment Abstract Abstract Poly (ADP-ribose) polymerase (PARP) inhibitors are small-molecule inhibitors of PARP enzymes (including PARP1, PARP2, and PARP3) that exhibit activity against tumor cells with defects in DNA repair.... |
PMC8218669 | core_pubmed_pmc | Randomized, Double-Blind, Placebo- and Positive-Controlled Crossover Study of the Effects of Tebipenem Pivoxil Hydrobromide on QT/QTc Intervals in Healthy Subjects | Randomized, Double-Blind, Placebo- and Positive-Controlled Crossover Study of the Effects of Tebipenem Pivoxil Hydrobromide on QT/QTc Intervals in Healthy Subjects Abstract ABSTRACT Tebipenem pivoxil hydrobromide (TBP-PI-HBr) is an orally available prodrug of tebipenem (TBP), a carbapenem with in vitro activity against... |
PMC10196429 | core_pubmed_pmc | Biased computation of probability of target attainment for antimicrobial drugs | Biased computation of probability of target attainment for antimicrobial drugs Abstract Abstract The medical literature is replete with articles in which there is confusion between “free concentration” and “unbound fraction” ( f u ), which is the ratio of free to total plasma concentration. The lack of clarity in disti... |
PMC10812599 | core_pubmed_pmc | A Review of the Clinical Utilization of Oral Antibacterial Therapy in the Treatment of Bone Infections in Adults | A Review of the Clinical Utilization of Oral Antibacterial Therapy in the Treatment of Bone Infections in Adults Abstract Abstract Chronic osteomyelitis in adults is managed with prolonged courses of intravenous antibiotics in conjunction with surgical debridement of necrotic bone. Over the past 40 years, there has bee... |
PMC7376291 | core_pubmed_pmc | Population Pharmacodynamic Model of Neutrophil Margination and Tolerance to Describe Effect of Sarilumab on Absolute Neutrophil Count in Patients with Rheumatoid Arthritis | Population Pharmacodynamic Model of Neutrophil Margination and Tolerance to Describe Effect of Sarilumab on Absolute Neutrophil Count in Patients with Rheumatoid Arthritis Abstract Evidence suggests that effects of interleukin‐6 pathway inhibitors sarilumab, tocilizumab, and sirukumab on absolute neutrophil count (ANC)... |
PMC11022745 | core_pubmed_pmc | Nanotherapeutics for Alleviating Anesthesia‐Associated Complications | Nanotherapeutics for Alleviating Anesthesia‐Associated Complications Abstract Abstract Current management of anesthesia‐associated complications falls short in terms of both efficacy and safety. Nanomaterials with versatile properties and unique nano‐bio interactions hold substantial promise as therapeutics for address... |
PMC11915130 | core_pubmed_pmc | The importance of getting the dose right in the treatment of tuberculosis | The importance of getting the dose right in the treatment of tuberculosis Abstract Prescribing the optimal combination of anti-tuberculosis drugs at the right dose is a fundamental step to achieve successful treatment outcomes. To aid the decision, clinicians should consider multiple factors, such as body weight, age, ... |
PMC11494917 | core_pubmed_pmc | Simulation‐based evaluation of the Pharmpy Automatic Model Development tool for population pharmacokinetic modeling in early clinical drug development | Simulation‐based evaluation of the Pharmpy Automatic Model Development tool for population pharmacokinetic modeling in early clinical drug development Abstract Abstract The Pharmpy Automatic Model Development (AMD) tool automates the building of population pharmacokinetic (popPK) models by utilizing a systematic stepwi... |
PMC4937663 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics and pharmacodynamics of belimumab in Japanese patients with mild-to-moderate systemic lupus erythematosus | Safety, tolerability, pharmacokinetics and pharmacodynamics of belimumab in Japanese patients with mild-to-moderate systemic lupus erythematosus Abstract Abstract Objectives Belimumab, an anti-B lymphocyte stimulator (BLyS) human monoclonal antibody, was approved in the United States, Canada and European Union for the ... |
PMC8697188 | core_pubmed_pmc | A reduction-responsive drug delivery with improved stability: disulfide crosslinked micelles of small amiphiphilic molecules † | A reduction-responsive drug delivery with improved stability: disulfide crosslinked micelles of small amiphiphilic molecules † Abstract Micelles self-assembled from small amphiphilic molecules are unstable in biological fluids, and thus are poor drug carriers. In contrast, amphiphilic polymer micelles can encapsulate h... |
PMC4453594 | core_pubmed_pmc | A phase I trial of vertical inhibition of IGF signalling using cixutumumab, an anti-IGF-1R antibody, and selumetinib, an MEK 1/2 inhibitor, in advanced solid tumours | A phase I trial of vertical inhibition of IGF signalling using cixutumumab, an anti-IGF-1R antibody, and selumetinib, an MEK 1/2 inhibitor, in advanced solid tumours Abstract Abstract Background: We completed a phase I clinical trial to test the safety and toxicity of combined treatment with cixutumumab (anti-IGF-1R an... |
PMC8397669 | core_pubmed_pmc | The Challenging Pharmacokinetics of Mitotane: An Old Drug in Need of New Packaging | The Challenging Pharmacokinetics of Mitotane: An Old Drug in Need of New Packaging Abstract Abstract Adrenocortical carcinoma (ACC) is a malignant tumor originating from the adrenal gland cortex with a heterogeneous but overall dismal prognosis in advanced stages. For more than 50 years, mitotane has remained a corners... |
PMC10349196 | core_pubmed_pmc | Synthetic Model Combination: A new machine‐learning method for pharmacometric model ensembling | Synthetic Model Combination: A new machine‐learning method for pharmacometric model ensembling Abstract Abstract When aiming to make predictions over targets in the pharmacological setting, a data‐focused approach aims to learn models based on a collection of labeled examples. Unfortunately, data sharing is not always ... |
PMC10220925 | core_pubmed_pmc | Optimizing Vancomycin Therapy in Critically Ill Children: A Population Pharmacokinetics Study to Inform Vancomycin Area under the Curve Estimation Using Novel Biomarkers | Optimizing Vancomycin Therapy in Critically Ill Children: A Population Pharmacokinetics Study to Inform Vancomycin Area under the Curve Estimation Using Novel Biomarkers Abstract Abstract Area under the curve (AUC)-directed vancomycin therapy is recommended, but Bayesian AUC estimation in critically ill children is dif... |
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