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PMC10403107 | core_pubmed_pmc | Testing the mutant selection window hypothesis with meropenem: In vitro model study with OXA-48-producing Klebsiella pneumoniae | Testing the mutant selection window hypothesis with meropenem: In vitro model study with OXA-48-producing Klebsiella pneumoniae Abstract Abstract OXA-48 carbapenemases are frequently expressed by Klebsiella pneumoniae clinical isolates; they decrease the effectiveness of carbapenem therapy, particularly with meropenem.... |
PMC3273701 | core_pubmed_pmc | An Overview of the CNS-Pharmacodynamic Profiles of Nonselective and Selective GABA Agonists | An Overview of the CNS-Pharmacodynamic Profiles of Nonselective and Selective GABA Agonists Abstract Various α 2,3 subtype selective partial GABA-A agonists are in development to treat anxiety disorders. These compounds are expected to be anxiolytic with fewer undesirable side effects, compared to nonselective GABA-A a... |
PMC5494168 | core_pubmed_pmc | The influence of storage time and temperature on propofol concentrations in canine blood and plasma | The influence of storage time and temperature on propofol concentrations in canine blood and plasma Abstract Propofol is an intravenous anesthetic commonly used due to its favorable pharmacokinetic and pharmacodynamic profile. There are discrepancies in the literature about the most appropriate sample for determining p... |
PMC10237355 | core_pubmed_pmc | A review of nanomaterials from synthetic and natural molecules for prospective breast cancer nanotherapy | A review of nanomaterials from synthetic and natural molecules for prospective breast cancer nanotherapy Abstract Abstract Breast cancer being one of the most frequent cancers in women accounts for almost a quarter of all cancer cases. Early and late-stage breast cancer outcomes have improved dramatically, with conside... |
PMC11626171 | core_pubmed_pmc | Nebulized vasopressin penetrates CSF and improves social cognition without inducing aggression in a rhesus monkey model of autism | Nebulized vasopressin penetrates CSF and improves social cognition without inducing aggression in a rhesus monkey model of autism Abstract Significance Low vasopressin level in cerebrospinal fluid (CSF) is an indicator of social impairment in low-social monkeys and autistic children. This evidence suggests vasopressin ... |
PMC10780562 | core_pubmed_pmc | Tissue Distribution, Pharmacokinetics, and Effect of Hematological and Biochemical Parameters of Acute Intravenous Administration of Silver Nanoparticles in Rats | Tissue Distribution, Pharmacokinetics, and Effect of Hematological and Biochemical Parameters of Acute Intravenous Administration of Silver Nanoparticles in Rats Abstract Abstract The widespread biomedical and commercial applications of silver nanoparticles (AgNPs) have increased their potential for human and environme... |
PMC7809782 | core_pubmed_pmc | ODYSSEY clinical trial design: a randomised global study to evaluate the efficacy and safety of dolutegravir-based antiretroviral therapy in HIV-positive children, with nested pharmacokinetic sub-studies to evaluate pragmatic WHO-weight-band based dolutegravir dosing | ODYSSEY clinical trial design: a randomised global study to evaluate the efficacy and safety of dolutegravir-based antiretroviral therapy in HIV-positive children, with nested pharmacokinetic sub-studies to evaluate pragmatic WHO-weight-band based dolutegravir dosing Abstract Background Dolutegravir (DTG)-based antiret... |
PMC5069578 | core_pubmed_pmc | The Effect of a High‐Fat Meal on the Pharmacokinetics of Ixazomib, an Oral Proteasome Inhibitor, in Patients With Advanced Solid Tumors or Lymphoma | The Effect of a High‐Fat Meal on the Pharmacokinetics of Ixazomib, an Oral Proteasome Inhibitor, in Patients With Advanced Solid Tumors or Lymphoma Abstract Abstract Ixazomib is the first oral proteasome inhibitor to be investigated in the clinic. This clinical study assessed whether the pharmacokinetics of ixazomib wo... |
PMC6444836 | core_pubmed_pmc | Population pharmacokinetics of primaquine and the effect of hepatic and renal dysfunction: An exploratory approach | Population pharmacokinetics of primaquine and the effect of hepatic and renal dysfunction: An exploratory approach Abstract Abstract OBJECTIVES: We attempted to develop a population pharmacokinetic model for primaquine (PQ) and evaluate the effect of renal and hepatic dysfunction on PQ pharmacokinetics. MATERIALS AND M... |
PMC12107360 | core_pubmed_pmc | Development and validation of BCG vaccine‐induced novel granulomatous liver injury preclinical animal model | Development and validation of BCG vaccine‐induced novel granulomatous liver injury preclinical animal model Abstract Abstract Background Developing a granulomatous liver injury preclinical model may pave the way to understanding hepatic‐TB (tuberculosis) and autoimmune granulomatous liver diseases. Antitubercular (ATT)... |
PMC11128094 | core_pubmed_pmc | Bayesian modelling of time series data (BayModTS)—a FAIR workflow to process sparse and highly variable data | Bayesian modelling of time series data (BayModTS)—a FAIR workflow to process sparse and highly variable data Abstract Abstract Motivation Systems biology aims to better understand living systems through mathematical modelling of experimental and clinical data. A pervasive challenge in quantitative dynamical modelling i... |
PMC4917805 | core_pubmed_pmc | The impact of genetic polymorphisms on the pharmacokinetics of efavirenz in African children | The impact of genetic polymorphisms on the pharmacokinetics of efavirenz in African children Abstract Abstract Aims Using a model‐based approach, the efavirenz steady‐state pharmacokinetics in African children is characterized, quantifying demographic and genotypic effects on the drug's disposition. Simulations are als... |
PMC12167508 | core_pubmed_pmc | Pharmacokinetic Properties and Therapeutic Effectiveness of Remimazolam in ICU Patients With Mechanical Ventilation: A Preliminary Study | Pharmacokinetic Properties and Therapeutic Effectiveness of Remimazolam in ICU Patients With Mechanical Ventilation: A Preliminary Study Abstract ABSTRACT The pharmacokinetic (PK) profile of remimazolam, a ultra‐short‐acting benzodiazepine, has been investigated for procedural sedation and anesthesia, but its pharmacok... |
PMC7561547 | core_pubmed_pmc | Population pharmacokinetic analysis of phase 1 bemarituzumab data to support phase 2 gastroesophageal adenocarcinoma FIGHT trial | Population pharmacokinetic analysis of phase 1 bemarituzumab data to support phase 2 gastroesophageal adenocarcinoma FIGHT trial Abstract Purpose To report population pharmacokinetic (PK) analysis of the phase 1 study (FPA144-001, NCT02318329 ) and to select a clinical dose and schedule that will achieve an empirical t... |
PMC8078916 | core_pubmed_pmc | Disease-drug and drug-drug interaction in COVID-19: Risk and assessment | Disease-drug and drug-drug interaction in COVID-19: Risk and assessment Abstract COVID-19 is announced as a global pandemic in 2020. Its mortality and morbidity rate are rapidly increasing, with limited medications. The emergent outbreak of COVID-19 prompted by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-... |
PMC12146887 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics with Enterohepatic Recirculation of Co-Medication of Rosuvastatin and Ezetimibe | Population Pharmacokinetics and Pharmacodynamics with Enterohepatic Recirculation of Co-Medication of Rosuvastatin and Ezetimibe Abstract Abstract Objective Combination therapy with rosuvastatin and ezetimibe is generally administered to patients with high cardiovascular risk. The objective of this study was to develop... |
PMC10711044 | core_pubmed_pmc | The effect of insulin analogs in people with type 1 diabetes at increased risk of severe hypoglycemia | The effect of insulin analogs in people with type 1 diabetes at increased risk of severe hypoglycemia Abstract Abstract Type 1 diabetes is characterized by insulin deficiency, and treatment is to supply insulin mimicking the physiological endogenous insulin secretion. Since its discovery, insulin therapy has evolved, a... |
PMC7536589 | core_pubmed_pmc | Safety, Antitumor Activity, and Pharmacokinetics of Toripalimab, a Programmed Cell Death 1 Inhibitor, in Patients With Advanced Non–Small Cell Lung Cancer | Safety, Antitumor Activity, and Pharmacokinetics of Toripalimab, a Programmed Cell Death 1 Inhibitor, in Patients With Advanced Non–Small Cell Lung Cancer Abstract Key Points Question What is the performance of toripalimab, a programmed cell death 1 (PD-1) antibody, and JS311, a novel PD ligand 1 (PD-L1) immunohistoche... |
PMC8408068 | core_pubmed_pmc | Absolute and Dose-Adjusted Serum Concentrations of Clozapine in Patients Switching vs. Maintaining Treatment: An Observational Study of 1979 Patients | Absolute and Dose-Adjusted Serum Concentrations of Clozapine in Patients Switching vs. Maintaining Treatment: An Observational Study of 1979 Patients Abstract Background Clozapine is an effective drug for the management of schizophrenia that has not responded to other agents, but some patients experience insufficient o... |
PMC6390162 | core_pubmed_pmc | Allele Frequency of SLC22A1 Met420del Metformin Main Transporter Encoding Gene among Javanese-Indonesian Population | Allele Frequency of SLC22A1 Met420del Metformin Main Transporter Encoding Gene among Javanese-Indonesian Population Abstract BACKGROUND: Genetic variation in the genes that encode metformin transporters has been proven to cause pharmacokinetic variability and various glycemic response to metformin. Organic Cation Trans... |
PMC6447767 | core_pubmed_pmc | Simultaneous determination of the potent anti-tuberculosis regimen—Pyrazinamide, ethambutol, protionamide, clofazimine in beagle dog plasma using LC–MS/MS method coupled with 96-well format plate | Simultaneous determination of the potent anti-tuberculosis regimen—Pyrazinamide, ethambutol, protionamide, clofazimine in beagle dog plasma using LC–MS/MS method coupled with 96-well format plate Abstract Highlights • LC–MS/MS method for determination of Pyrazinamide, Ethambutol, Protionamide and Clofazimine in Beagle ... |
PMC11757102 | core_pubmed_pmc | Amphotericin B tissue penetration and pharmacokinetics in healthy and Candida albicans -infected rats: insights from microdialysis and population modeling | Amphotericin B tissue penetration and pharmacokinetics in healthy and Candida albicans -infected rats: insights from microdialysis and population modeling Abstract Introduction This study evaluated the relationship between total plasma and free kidney concentrations of amphotericin B (AmB) in healthy and C. albicans -i... |
PMC11040693 | core_pubmed_pmc | Clinical pharmacology and tolerability of REC‐994, a redox‐cycling nitroxide compound, in randomized phase 1 dose‐finding studies | Clinical pharmacology and tolerability of REC‐994, a redox‐cycling nitroxide compound, in randomized phase 1 dose‐finding studies Abstract Abstract Cerebral cavernous malformation (CCM) has variable clinical symptoms, including potentially fatal hemorrhagic stroke. Treatment options are very limited, presenting a large... |
PMC10884144 | core_pubmed_pmc | Characterization of anti-drug antibody dynamics using a bivariate mixed hidden-markov model by nonlinear-mixed effects approach | Characterization of anti-drug antibody dynamics using a bivariate mixed hidden-markov model by nonlinear-mixed effects approach Abstract Biological therapies may act as immunogenic triggers leading to the formation of anti-drug antibodies (ADAs). Population pharmacokinetic (PK) models can be used to characterize the re... |
PMC6163764 | core_pubmed_pmc | Interprofessional Pharmacokinetics Simulation: Pharmacy and Nursing Students’ Perceptions | Interprofessional Pharmacokinetics Simulation: Pharmacy and Nursing Students’ Perceptions Abstract Interprofessional practice between pharmacists and nurses can involve pharmacokinetic dosing of medications in a hospital setting. This study describes student perceptions of an interprofessional collaboration pharmacokin... |
PMC2958909 | core_pubmed_pmc | S110, a novel decitabine dinucleotide, increases fetal hemoglobin levels in baboons ( P. anubis ) | S110, a novel decitabine dinucleotide, increases fetal hemoglobin levels in baboons ( P. anubis ) Abstract Background S110 is a novel dinucleoside analog that could have advantages over existing DNA methyltransferase (DNMT) inhibitors such as decitabine. A potential therapeutic role for S110 is to increase fetal hemogl... |
PMC11999743 | core_pubmed_pmc | Quantitative Analysis of Muscarinic Antagonist Atropine and Tiotropium in Microvolume Plasma Using Liquid Chromatography–Mass Spectrometry: Application for Pharmacokinetic Studies | Quantitative Analysis of Muscarinic Antagonist Atropine and Tiotropium in Microvolume Plasma Using Liquid Chromatography–Mass Spectrometry: Application for Pharmacokinetic Studies Abstract Abstract Despite the availability of current resources, the development of medical countermeasures remains crucial in combatting th... |
PMC7867544 | core_pubmed_pmc | Bleeding and thromboembolism due to drug-drug interactions with non-vitamin K antagonist oral anticoagulants—a Swedish, register-based cohort study in atrial fibrillation outpatients | Bleeding and thromboembolism due to drug-drug interactions with non-vitamin K antagonist oral anticoagulants—a Swedish, register-based cohort study in atrial fibrillation outpatients Abstract Purpose To study the association between interacting drugs and bleeding or thromboembolism in atrial fibrillation outpatients tr... |
PMC12823615 | core_pubmed_pmc | Anticancer potential of Dendrocnide meyeniana through phytochemical profiling, ADMET analysis, molecular docking, and in silico cytotoxicity evaluation | Anticancer potential of Dendrocnide meyeniana through phytochemical profiling, ADMET analysis, molecular docking, and in silico cytotoxicity evaluation Abstract Phytochemicals are widely explored for cancer therapeutics due to their structural diversity and broad pharmacological activities. This study investigated the ... |
PMC10484477 | core_pubmed_pmc | Phenylbutazone concentrations in synovial fluid following administration via intravenous regional limb perfusion in the forelimbs of six adult horses | Phenylbutazone concentrations in synovial fluid following administration via intravenous regional limb perfusion in the forelimbs of six adult horses Abstract Abstract Background Pain management is critical to equine welfare with non-steroidal anti-inflammatory drugs (NSAID) commonly used in horses. However, systemic N... |
PMC5854640 | core_pubmed_pmc | Evaluation of 25% Poloxamer As a Slow Release Carrier for Morphine in a Rat Model | Evaluation of 25% Poloxamer As a Slow Release Carrier for Morphine in a Rat Model Abstract Abstract The objectives of this study were to evaluate poloxamer as a slow release carrier for morphine (M) and potential tissue irritation after subcutaneous poloxamer–morphine (PM) injection in a rat model. Based on the result ... |
PMC5306247 | core_pubmed_pmc | Impact of CYP3A4*1G Allele on Clinical Pharmacokinetics and Pharmacodynamics of Clopidogrel | Impact of CYP3A4*1G Allele on Clinical Pharmacokinetics and Pharmacodynamics of Clopidogrel Abstract Background and Objectives Resistance to the antiplatelet treatment with clopidogrel has both genetic and non-genetic causes. Polymorphic variants of cytochrome P450 3A4 isoenzyme involved in the bioactivation of clopido... |
PMC9243314 | core_pubmed_pmc | The Correlation Between Busulfan Exposure and Clinical Outcomes in Chinese Pediatric Patients: A Population Pharmacokinetic Study | The Correlation Between Busulfan Exposure and Clinical Outcomes in Chinese Pediatric Patients: A Population Pharmacokinetic Study Abstract Abstract Aims: The aims of the study were to 1) establish a population pharmacokinetic (Pop-PK) model for busulfan in Chinese pediatric patients undergoing hematopoietic stem cell t... |
PMC6172054 | core_pubmed_pmc | Weekly carfilzomib and dexamethasone in Japanese patients with relapsed or refractory multiple myeloma: A phase 1 and PK/PD trial | Weekly carfilzomib and dexamethasone in Japanese patients with relapsed or refractory multiple myeloma: A phase 1 and PK/PD trial Abstract Abstract This open‐label multicenter phase 1 study evaluated the safety, tolerability, efficacy, pharmacokinetics and pharmacodynamics of weekly carfilzomib and dexamethasone (Cd) i... |
PMC4139342 | core_pubmed_pmc | Pharmacokinetics-Pharmacodynamics Analysis of Bicyclic 4-Nitroimidazole Analogs in a Murine Model of Tuberculosis | Pharmacokinetics-Pharmacodynamics Analysis of Bicyclic 4-Nitroimidazole Analogs in a Murine Model of Tuberculosis Abstract PA-824 is a bicyclic 4-nitroimidazole, currently in phase II clinical trials for the treatment of tuberculosis. Dose fractionation pharmacokinetic-pharmacodynamic studies in mice indicated that the... |
PMC6203217 | core_pubmed_pmc | Recent advances in methodology for clinical trials in small populations: the InSPiRe project | Recent advances in methodology for clinical trials in small populations: the InSPiRe project Abstract Where there are a limited number of patients, such as in a rare disease, clinical trials in these small populations present several challenges, including statistical issues. This led to an EU FP7 call for proposals in ... |
PMC10252037 | core_pubmed_pmc | Cardiorespiratory and Neuroprotective Effects of Caffeine in Neonate Animal Models | Cardiorespiratory and Neuroprotective Effects of Caffeine in Neonate Animal Models Abstract Abstract Simple Summary Caffeine is a stimulant used in humans and animals to improve newborns’ respiratory and neurological responses. The use of caffeine after birth could increase neonate survival. However, due to the immatur... |
PMC12712847 | core_pubmed_pmc | Pyrazoline B Induces Oxidative Stress Mediated Toxicity, Cell Cycle Arrest, and Caspase-Independent Apoptosis in BT-474 Human Breast Cancer Cells | Pyrazoline B Induces Oxidative Stress Mediated Toxicity, Cell Cycle Arrest, and Caspase-Independent Apoptosis in BT-474 Human Breast Cancer Cells Abstract Abstract Introduction Luminal subtype B breast cancer represents a clinically challenging subtype, accounting for nearly 40% of all breast cancers. However, clinical... |
PMC6477588 | core_pubmed_pmc | Pharmacokinetic Profile of Inhaled Submicron Particle Paclitaxel (NanoPac ® ) in a Rodent Model | Pharmacokinetic Profile of Inhaled Submicron Particle Paclitaxel (NanoPac ® ) in a Rodent Model Abstract Abstract Background: Inhaled chemotherapeutics may enhance pulmonary drug exposure to malignant lesions in the lung without substantially contributing to systemic toxicities. The pharmacokinetic profile of inhaled s... |
PMC12518218 | core_pubmed_pmc | Application of population pharmacokinetic modeling of SVG-101 to evaluate proper dose selection | Application of population pharmacokinetic modeling of SVG-101 to evaluate proper dose selection Abstract Everolimus, an inhibitor of the mammalian target of the rapamycin signaling pathway, is used to treat tuberous sclerosis complex (TSC), certain cancers, and organ transplantation. Although a dispersible formulation ... |
PMC8674128 | core_pubmed_pmc | Tritiation of aryl thianthrenium salts with a molecular palladium catalyst | Tritiation of aryl thianthrenium salts with a molecular palladium catalyst Abstract Tritium labelling is a critical tool for investigating the pharmacokinetic and pharmacodynamic properties of drugs, autoradiography, receptor binding and receptor occupancy studies 1 . Tritium gas is the preferred source of tritium for ... |
PMC11235607 | core_pubmed_pmc | Dopamine agonist serum concentrations and impulse control disorders in Parkinson's disease | Dopamine agonist serum concentrations and impulse control disorders in Parkinson's disease Abstract Abstract Background and purpose Impulse control disorders (ICDs) are common among Parkinson's disease patients using dopamine agonists. We wanted to determine whether ICD patients have higher dopamine agonist serum conce... |
PMC9536713 | core_pubmed_pmc | Synthesis and Preclinical Evaluation of 177 Lu-Labeled Radiohybrid PSMA Ligands for Endoradiotherapy of Prostate Cancer | Synthesis and Preclinical Evaluation of 177 Lu-Labeled Radiohybrid PSMA Ligands for Endoradiotherapy of Prostate Cancer Abstract The prostate-specific membrane antigen (PSMA)–targeted radiohybrid (rh) ligand [ 177 Lu]Lu-rhPSMA-7.3 has recently been assessed in a pretherapeutic dosimetry study on prostate cancer patient... |
PMC2994065 | core_pubmed_pmc | Effects of Flos carthami on CYP2D6 and on the Pharmacokinetics of Metoprolol in Rats | Effects of Flos carthami on CYP2D6 and on the Pharmacokinetics of Metoprolol in Rats Abstract Flos carthami is a traditional Chinese herbal medicine. Clinically, the Flos carthami Injection has been used concomitantly with other Western drugs and may be used concomitantly with β -blockers, such as metoprolol, to treat ... |
PMC9618533 | core_pubmed_pmc | Apixaban Use in Obese Patients: A Review of the Pharmacokinetic, Interventional, and Observational Study Data | Apixaban Use in Obese Patients: A Review of the Pharmacokinetic, Interventional, and Observational Study Data Abstract Abstract Relatively little is known about the influence of extreme body weight on the pharmacokinetics (PK), pharmacodynamics (PD), efficacy, and safety of drugs used in many disease states. While dire... |
PMC12417622 | core_pubmed_pmc | Contribution of Organic Anion Transporter 3 in Delayed Elimination of Methotrexate by Concomitant Administration of Febuxostat | Contribution of Organic Anion Transporter 3 in Delayed Elimination of Methotrexate by Concomitant Administration of Febuxostat Abstract ABSTRACT Methotrexate is an antifolate agent used for the treatment of various malignancies and is mainly secreted via human organic anion transporter 3 (hOAT3) in the proximal tubular... |
PMC7477545 | core_pubmed_pmc | Translational evaluation of novel selective orexin-1 receptor antagonist JNJ-61393215 in an experimental model for panic in rodents and humans | Translational evaluation of novel selective orexin-1 receptor antagonist JNJ-61393215 in an experimental model for panic in rodents and humans Abstract Abstract Orexin neurons originating in the perifornical and lateral hypothalamic area project to anxiety- and panic-associated neural circuitry, and are highly reactive... |
PMC7379668 | core_pubmed_pmc | Application of different pharmacokinetic models to describe and predict pharmacokinetics of voriconazole in magellanic penguins following oral administration | Application of different pharmacokinetic models to describe and predict pharmacokinetics of voriconazole in magellanic penguins following oral administration Abstract Abstract Aspergillosis is a condition causing serious morbidity and mortality in captive penguins and other bird species. It can be treated with antifung... |
PMC7754409 | core_pubmed_pmc | Discordance Between Child‐Pugh and National Cancer Institute Classifications for Hepatic Dysfunction: Implications on Dosing Recommendations for Oncology Compounds | Discordance Between Child‐Pugh and National Cancer Institute Classifications for Hepatic Dysfunction: Implications on Dosing Recommendations for Oncology Compounds Abstract Abstract Guidance from the U.S. Food and Drug Administration (FDA) and the European Medicines Agency recommends using Child‐Pugh classification for... |
PMC12389747 | core_pubmed_pmc | Harnessing the Loop: The Perspective of Circular RNA in Modern Therapeutics | Harnessing the Loop: The Perspective of Circular RNA in Modern Therapeutics Abstract Circular RNAs (circRNAs) have emerged as a transformative class of RNA therapeutics, distinguished by their closed-loop structure conferring nuclease resistance, reduced immunogenicity, and sustained translational activity. While chall... |
PMC5306477 | core_pubmed_pmc | Population pharmacokinetics of exenatide | Population pharmacokinetics of exenatide Abstract Abstract Aim The aim of the present analysis was to develop a core population pharmacokinetic model for the pharmacokinetic properties of immediate‐release (IR) exenatide, which can be used in subsequent analyses of novel sustained‐release formulations. Methods Data fro... |
PMC3586162 | core_pubmed_pmc | Phase I Clinical Study of Edaravone in Healthy Chinese Volunteers | Phase I Clinical Study of Edaravone in Healthy Chinese Volunteers Abstract Abstract Objective The objective of this study was to investigate the safety and pharmacokinetics of edaravone administered by single or successive intravenous infusions in healthy Chinese volunteers. Methods A total of 30 subjects (15 males and... |
PMC8067051 | core_pubmed_pmc | Sirolimus Pharmacokinetics Variability Points to the Relevance of Therapeutic Drug Monitoring in Pediatric Oncology | Sirolimus Pharmacokinetics Variability Points to the Relevance of Therapeutic Drug Monitoring in Pediatric Oncology Abstract Abstract Sirolimus is widely used in transplantation, where its therapeutic drug monitoring (TDM) is well established. Evidence of a crucial role for sirolimus in the PI3K/AkT/mTor pathway has st... |
PMC11249824 | core_pubmed_pmc | The effect of itraconazole, a strong CYP3A4 inhibitor, on the pharmacokinetics of the first‐in‐class ACKR3 / CXCR7 antagonist, ACT ‐1004‐1239 | The effect of itraconazole, a strong CYP3A4 inhibitor, on the pharmacokinetics of the first‐in‐class ACKR3 / CXCR7 antagonist, ACT ‐1004‐1239 Abstract Abstract Cytochrome P450 (CYP) 3A4 is an enzyme involved in the metabolism of many drugs that are currently on the market and is therefore a key player in drug–drug inte... |
PMC10087001 | core_pubmed_pmc | Population Pharmacokinetics of Patritumab Deruxtecan in Patients With Solid Tumors | Population Pharmacokinetics of Patritumab Deruxtecan in Patients With Solid Tumors Abstract Abstract Patritumab deruxtecan is an antibody–drug conjugate consisting of a fully human monoclonal antibody against human epidermal growth factor receptor 3 (HER3) attached to a topoisomerase I inhibitor payload via a tetrapept... |
PMC7835591 | core_pubmed_pmc | Ligand conjugated antisense oligonucleotide for the treatment of transthyretin amyloidosis: preclinical and phase 1 data | Ligand conjugated antisense oligonucleotide for the treatment of transthyretin amyloidosis: preclinical and phase 1 data Abstract Abstract Aims Amyloidogenic transthyretin (ATTR) amyloidosis is a fatal disease characterized by progressive cardiomyopathy and/or polyneuropathy. AKCEA‐TTR‐L Rx (ION‐682884) is a ligand‐con... |
PMC6753841 | core_pubmed_pmc | Δ 9 -Tetrahydrocannabinol Derivative-Loaded Nanoformulation Lowers Intraocular Pressure in Normotensive Rabbits | Δ 9 -Tetrahydrocannabinol Derivative-Loaded Nanoformulation Lowers Intraocular Pressure in Normotensive Rabbits Abstract Abstract Purpose Δ 9 -Tetrahydrocannabinol-valine-hemisuccinate, a hydrophilic prodrug of Δ 9 -tetrahydrocannabinol, synthesized with the aim of improving the ocular bioavailability of the parent mol... |
PMC5709452 | core_pubmed_pmc | The Influence of Hepatic and Renal Impairment on the Pharmacokinetics of a Treatment for Herpes Zoster, Amenamevir (ASP2151): Phase 1, Open-Label, Single-Dose, Parallel-Group Studies | The Influence of Hepatic and Renal Impairment on the Pharmacokinetics of a Treatment for Herpes Zoster, Amenamevir (ASP2151): Phase 1, Open-Label, Single-Dose, Parallel-Group Studies Abstract Introduction Amenamevir (ASP2151) is a nonnucleoside human herpesvirus helicase-primase inhibitor that was approved in Japan for... |
PMC8700130 | core_pubmed_pmc | Exploring the Binding Pattern of Geraniol with Acetylcholinesterase through In Silico Docking, Molecular Dynamics Simulation, and In Vitro Enzyme Inhibition Kinetics Studies | Exploring the Binding Pattern of Geraniol with Acetylcholinesterase through In Silico Docking, Molecular Dynamics Simulation, and In Vitro Enzyme Inhibition Kinetics Studies Abstract Acetylcholinesterase (AChE) inhibition is a key element in enhancing cholinergic transmission and subsequently relieving major symptoms o... |
PMC7444762 | core_pubmed_pmc | Phase I study of imalumab (BAX69), a fully human recombinant antioxidized macrophage migration inhibitory factor antibody in advanced solid tumours | Phase I study of imalumab (BAX69), a fully human recombinant antioxidized macrophage migration inhibitory factor antibody in advanced solid tumours Abstract Aim Preclinical evidence suggests that oxidized macrophage migration inhibitory factor (oxMIF) may be involved in carcinogenesis. This phase 1 study ( NCT01765790 ... |
PMC12208120 | core_pubmed_pmc | Clinical Use of Fospropofol Disodium: Evaluation of Pharmacology, Safety, and Efficacy | Clinical Use of Fospropofol Disodium: Evaluation of Pharmacology, Safety, and Efficacy Abstract Abstract Fospropofol disodium (FD) is a safe and effective alternative to propofol, as it avoids injection pain, severe hypotension, significant respiratory depression, and allergic reactions during intravenous anesthesia in... |
PMC12811002 | core_pubmed_pmc | Pharmacological MRI : Utility in Understanding Drug Mechanisms in Psychiatric Disorders | Pharmacological MRI : Utility in Understanding Drug Mechanisms in Psychiatric Disorders Abstract ABSTRACT Pharmacological MRI (pharmaMRI) has emerged as a powerful tool to study how psychoactive drugs affect brain function and to uncover mechanisms of drug action in psychiatric disorders. This review provides an overvi... |
PMC3877914 | core_pubmed_pmc | Pharmacokinetics and Bioavailability of Plant Lignan 7-Hydroxymatairesinol and Effects on Serum Enterolactone and Clinical Symptoms in Postmenopausal Women: A Single-Blinded, Parallel, Dose-Comparison Study | Pharmacokinetics and Bioavailability of Plant Lignan 7-Hydroxymatairesinol and Effects on Serum Enterolactone and Clinical Symptoms in Postmenopausal Women: A Single-Blinded, Parallel, Dose-Comparison Study Abstract Objective 7-Hydroxymaitairesinol (7-HMR) is a naturally occurring plant lignan found in whole grains and... |
PMC3262389 | core_pubmed_pmc | Detemir as a once-daily basal insulin in type 2 diabetes | Detemir as a once-daily basal insulin in type 2 diabetes Abstract Background Insulin detemir, a long-acting basal insulin analog, is labeled for once-daily or twice-daily dosing in patients with type 1 (T1DM) or type 2 (T2DM) diabetes mellitus. Protocols for some earlier clinical studies of detemir evaluated twice-dail... |
PMC3282081 | core_pubmed_pmc | A Modular Strategy to Prepare Multivalent Inhibitors of Prostate-Specific Membrane Antigen (PSMA) | A Modular Strategy to Prepare Multivalent Inhibitors of Prostate-Specific Membrane Antigen (PSMA) Abstract Abstract We have developed a modular scaffold for preparing high-affinity, homo-multivalent inhibitors of the prostate-specific membrane antigen (PSMA) for imaging and therapy of prostate cancer (PCa). Our system ... |
PMC8308800 | core_pubmed_pmc | ADME and Pharmacokinetic Properties of Remdesivir: Its Drug Interaction Potential | ADME and Pharmacokinetic Properties of Remdesivir: Its Drug Interaction Potential Abstract Abstract On 11 March 2020, the World Health Organization (WHO) classified the Coronavirus Disease 2019 (COVID-19) as a global pandemic, which tested healthcare systems, administrations, and treatment ingenuity across the world. C... |
PMC12167917 | core_pubmed_pmc | Development of a Joint Tumor Size–Overall Survival Modeling and Simulation Framework Supporting Oncology Development Decision‐Making | Development of a Joint Tumor Size–Overall Survival Modeling and Simulation Framework Supporting Oncology Development Decision‐Making Abstract ABSTRACT Tumor size–overall survival (TS‐OS) models can support decision‐making in oncology drug development by predicting long‐term OS based on TS data from early data cuts and ... |
PMC12237026 | core_pubmed_pmc | Influence of bodyweight on prednisolone pharmacokinetics in dogs | Influence of bodyweight on prednisolone pharmacokinetics in dogs Abstract Background Larger dogs may be at greater risk of prednisolone side effects, yet there is limited research about how bodyweight affects prednisolone pharmacokinetics in dogs. Hypothesis/objectives To describe the relationship between prednisolone ... |
PMC3644400 | core_pubmed_pmc | Phase I study of pulsatile 3-day administration of afatinib (BIBW 2992) in combination with docetaxel in advanced solid tumors | Phase I study of pulsatile 3-day administration of afatinib (BIBW 2992) in combination with docetaxel in advanced solid tumors Abstract Summary Background A phase I study to assess the maximum tolerated dose (MTD) of a short course of afatinib in combination with docetaxel for the treatment of solid tumors. Methods Pat... |
PMC10986017 | core_pubmed_pmc | A phase I open-label, dose-escalation study of NUC-3373, a targeted thymidylate synthase inhibitor, in patients with advanced cancer (NuTide:301) | A phase I open-label, dose-escalation study of NUC-3373, a targeted thymidylate synthase inhibitor, in patients with advanced cancer (NuTide:301) Abstract Abstract Purpose 5-fluorouracil (5-FU) is inefficiently converted to the active anti-cancer metabolite, fluorodeoxyuridine-monophosphate (FUDR-MP), is associated wit... |
PMC8274831 | core_pubmed_pmc | Study on the Effect of Antiplatelet and Gastric Mucosal Protection of Traditional Chinese Medicine Invigorating Qi and Hemostasis | Study on the Effect of Antiplatelet and Gastric Mucosal Protection of Traditional Chinese Medicine Invigorating Qi and Hemostasis Abstract Background To investigate the effects of Chinese herbal medicine in tonifying qi and attaining hemostasis caused by the metabolism of the drug clopidogrel and as a result of platele... |
PMC6438701 | core_pubmed_pmc | Mechanistic interaction study of 5,6-Dichloro-2-[2-(pyridin-2-yl)ethyl]isoindoline-1,3-dione with bovine serum albumin by spectroscopic and molecular docking approaches | Mechanistic interaction study of 5,6-Dichloro-2-[2-(pyridin-2-yl)ethyl]isoindoline-1,3-dione with bovine serum albumin by spectroscopic and molecular docking approaches Abstract Abstract A synthesized and promising biologically hypoglycemic compound 5,6-Dichloro-2-[2-(pyridin-2-yl)ethyl]isoindoline-1,3-dione ( 5e ) was... |
PMC6519044 | core_pubmed_pmc | Pharmacogenomics of Vincristine‐Induced Peripheral Neuropathy Implicates Pharmacokinetic and Inherited Neuropathy Genes | Pharmacogenomics of Vincristine‐Induced Peripheral Neuropathy Implicates Pharmacokinetic and Inherited Neuropathy Genes Abstract Vincristine is an effective chemotherapeutic drug for various cancers, including acute lymphoblastic leukemia ( ALL ). Unfortunately, clinical utility is restricted by dose‐limiting vincristi... |
PMC4788712 | core_pubmed_pmc | Intracellular pharmacokinetic study of zidovudine and its phosphorylated metabolites | Intracellular pharmacokinetic study of zidovudine and its phosphorylated metabolites Abstract Zidovudine (AZT), the first drug approved by the US Food and Drug Administration for the treatment of human immunodeficiency virus (HIV) infection, is metabolized in the host cells to 5′-AZT triphosphate (AZT-TP) which inhibit... |
PMC11678589 | core_pubmed_pmc | Nanomedicine in Ophthalmology: From Bench to Bedside | Nanomedicine in Ophthalmology: From Bench to Bedside Abstract Abstract Ocular diseases such as cataract, refractive error, age-related macular degeneration, glaucoma, and diabetic retinopathy significantly impact vision and quality of life worldwide. Despite advances in conventional treatments, challenges like limited ... |
PMC6078957 | core_pubmed_pmc | Metabolism of ticagrelor in patients with acute coronary syndromes | Metabolism of ticagrelor in patients with acute coronary syndromes Abstract Abstract Ticagrelor is a state-of-the-art antiplatelet agent used for the treatment of patients with acute coronary syndromes (ACS). Unlike remaining oral P2Y12 receptor inhibitors ticagrelor does not require metabolic activation to exert its a... |
PMC10741196 | core_pubmed_pmc | Which Are the Best Regimens of Broad-Spectrum Beta-Lactam Antibiotics in Burn Patients? A Systematic Review of Evidence from Pharmacology Studies | Which Are the Best Regimens of Broad-Spectrum Beta-Lactam Antibiotics in Burn Patients? A Systematic Review of Evidence from Pharmacology Studies Abstract Background: Burn injury causes profound pathophysiological changes in the pharmacokinetic/pharmacodynamic (PK/PD) properties of antibiotics. Infections are among the... |
PMC6250289 | core_pubmed_pmc | Individualized Medication of Voriconazole: A Practice Guideline of the Division of Therapeutic Drug Monitoring, Chinese Pharmacological Society | Individualized Medication of Voriconazole: A Practice Guideline of the Division of Therapeutic Drug Monitoring, Chinese Pharmacological Society Abstract Supplemental Digital Content is Available in the Text. Key Words: guideline, voriconazole, individualized medication, GRADE Abstract Background: Voriconazole (VRZ) is ... |
PMC9005427 | core_pubmed_pmc | The effect of BI 409306 on heart rate in healthy volunteers: a randomised, double-blind, placebo-controlled, crossover study | The effect of BI 409306 on heart rate in healthy volunteers: a randomised, double-blind, placebo-controlled, crossover study Abstract Abstract Purpose The potent, selective phosphodiesterase-9A inhibitor BI 409306 may be beneficial for patients with attenuated psychosis syndrome and could prevent relapse in patients wi... |
PMC12220319 | core_pubmed_pmc | Single low dose primaquine to block the transmission of Plasmodium falciparum —proposed stand-alone and ACT-adapted regimens | Single low dose primaquine to block the transmission of Plasmodium falciparum —proposed stand-alone and ACT-adapted regimens Abstract Abstract Background Despite the 2012 WHO recommendation to add single low dose primaquine (SLDPQ, 0.25 mg/kg body weight) to artemisinin-based combination treatments (ACTs) for blocking ... |
PMC6296667 | core_pubmed_pmc | Exploring the insulin secretory properties of the PGD 2 -GPR44/DP2 axis in vitro and in a randomized phase-1 trial of type 2 diabetes patients | Exploring the insulin secretory properties of the PGD 2 -GPR44/DP2 axis in vitro and in a randomized phase-1 trial of type 2 diabetes patients Abstract Aims/Hypothesis GPR44 ( DP2 , PTGDR2 , CRTh2 ) is the receptor for the pro-inflammatory mediator prostaglandin D 2 (PGD 2 ) and it is enriched in human islets. In roden... |
PMC2868996 | core_pubmed_pmc | Pharmacokinetics of gemcitabine in non-small-cell lung cancer patients: impact of the 79A>C cytidine deaminase polymorphism | Pharmacokinetics of gemcitabine in non-small-cell lung cancer patients: impact of the 79A>C cytidine deaminase polymorphism Abstract Abstract Objective To study the impact of the 79A>C polymorphism in the cytidine deaminase (CDA) gene on the pharmacokinetics of gemcitabine and its metabolite 2′,2′-difluorodeoxyuridine ... |
PMC10786964 | core_pubmed_pmc | How to Dose Vancomycin in Overweight and Obese Patients with Varying Renal (Dys)function in the Novel Era of AUC 400–600 mg·h/L-Targeted Dosing | How to Dose Vancomycin in Overweight and Obese Patients with Varying Renal (Dys)function in the Novel Era of AUC 400–600 mg·h/L-Targeted Dosing Abstract Abstract Background and Objective The latest vancomycin guideline recommends area under the curve (AUC)-targeted dosing and monitoring for efficacy and safety. However... |
PMC3828006 | core_pubmed_pmc | Assessment of Maraviroc Exposure–Response Relationship at 48 Weeks in Treatment-Experienced HIV-1–Infected Patients in the MOTIVATE Studies | Assessment of Maraviroc Exposure–Response Relationship at 48 Weeks in Treatment-Experienced HIV-1–Infected Patients in the MOTIVATE Studies Abstract Efficacy exposure–response relationships of the CCR5 antagonist maraviroc were evaluated across two phase III clinical trials. This post-hoc analysis used 48-week efficacy... |
PMC6593826 | core_pubmed_pmc | Metabolism, Excretion, and Pharmacokinetics of [ 14 C]‐Cefiderocol (S‐649266), a Siderophore Cephalosporin, in Healthy Subjects Following Intravenous Administration | Metabolism, Excretion, and Pharmacokinetics of [ 14 C]‐Cefiderocol (S‐649266), a Siderophore Cephalosporin, in Healthy Subjects Following Intravenous Administration Abstract Abstract The objectives of this study were to characterize the concentration‐time profiles of total radioactivity equivalent and unchanged cefider... |
PMC6900889 | core_pubmed_pmc | Steady-state Pharmacokinetics of Vancomycin in Children Admitted to Pediatric Intensive Care Unit of a Tertiary Referral Center | Steady-state Pharmacokinetics of Vancomycin in Children Admitted to Pediatric Intensive Care Unit of a Tertiary Referral Center Abstract ABSTRACT Aims and objectives Vancomycin is a drug of choice for various gram-positive bacterial (GPB) infections and is largely prescribed to pediatric intensive care unit (PICU) pati... |
PMC5903260 | core_pubmed_pmc | Topical administration of regorafenib eye drops: phase I dose‐escalation study in healthy volunteers | Topical administration of regorafenib eye drops: phase I dose‐escalation study in healthy volunteers Abstract Abstract Aim Regorafenib is a multikinase inhibitor under investigation for use in neovascular age‐related macular degeneration. In this phase I study, regorafenib eye drops were administered to healthy volunte... |
PMC9298258 | core_pubmed_pmc | Semi‐Mechanistic PK/PD Modeling and Simulation of Irreversible BTK Inhibition to Support Dose Selection of Tirabrutinib in Subjects with RA | Semi‐Mechanistic PK/PD Modeling and Simulation of Irreversible BTK Inhibition to Support Dose Selection of Tirabrutinib in Subjects with RA Abstract Abstract Tirabrutinib is an irreversible, small‐molecule Bruton’s tyrosine kinase (BTK) inhibitor, which was approved in Japan (VELEXBRU) to treat B‐cell malignancies and ... |
PMC9879930 | core_pubmed_pmc | Effect of pharmacogenetic variations on praziquantel plasma concentration and safety outcomes among school children in Rwanda | Effect of pharmacogenetic variations on praziquantel plasma concentration and safety outcomes among school children in Rwanda Abstract School-based mass drug administration (MDA) of Praziquantel (PZQ) is the global intervention strategy for elimination of schistosomiasis. Genetic variations in drug metabolizing enzymes... |
PMC7400317 | core_pubmed_pmc | Oxytetracycline Pharmacokinetics After Intramuscular Administration in Cows with Clinical Metritis Associated with Trueperella Pyogenes Infection | Oxytetracycline Pharmacokinetics After Intramuscular Administration in Cows with Clinical Metritis Associated with Trueperella Pyogenes Infection Abstract Systemic therapy with oxytetracycline is often used for treatment of clinical metritis although data about its penetration into the uterus and uterine secretion are ... |
PMC7518421 | core_pubmed_pmc | Phase I clinical trial repurposing all-trans retinoic acid as a stromal targeting agent for pancreatic cancer | Phase I clinical trial repurposing all-trans retinoic acid as a stromal targeting agent for pancreatic cancer Abstract Pre-clinical models have shown that targeting pancreatic stellate cells with all-trans-retinoic-acid (ATRA) reprograms pancreatic stroma to suppress pancreatic ductal adenocarcinoma (PDAC) growth. Here... |
PMC10556534 | core_pubmed_pmc | Optimizing tylosin dosage for co-infection of Actinobacillus pleuropneumoniae and Pasteurella multocida in pigs using pharmacokinetic/pharmacodynamic modeling | Optimizing tylosin dosage for co-infection of Actinobacillus pleuropneumoniae and Pasteurella multocida in pigs using pharmacokinetic/pharmacodynamic modeling Abstract Abstract Formulating a therapeutic strategy that can effectively combat concurrent infections of Actinobacillus pleuropneumoniae ( A. pleuropneumoniae )... |
PMC7179450 | core_pubmed_pmc | Primary Human Hepatocytes, But not HepG2 or Balb/c 3T3 Cells, Efficiently Metabolize Salinomycin and Are Resistant to Its Cytotoxicity | Primary Human Hepatocytes, But not HepG2 or Balb/c 3T3 Cells, Efficiently Metabolize Salinomycin and Are Resistant to Its Cytotoxicity Abstract Abstract Salinomycin is a polyether antibiotic showing anticancer activity. There are many reports of its toxicity to animals but little is known about the potential adverse ef... |
PMC8532626 | core_pubmed_pmc | Beta-Lactams Dosing in Critically Ill Patients with Gram-Negative Bacterial Infections: A PK/PD Approach | Beta-Lactams Dosing in Critically Ill Patients with Gram-Negative Bacterial Infections: A PK/PD Approach Abstract Abstract Beta-lactam antibiotics are often the backbone of treatment for Gram-negative infections in the critically ill. Beta-lactams exhibit time-dependent killing, and their efficacy depends on the percen... |
PMC11625073 | core_pubmed_pmc | Exposure-response relationships of venetoclax in combination with carfilzomib and dexamethasone in relapsed/refractory t(11;14) multiple myeloma patients | Exposure-response relationships of venetoclax in combination with carfilzomib and dexamethasone in relapsed/refractory t(11;14) multiple myeloma patients Abstract Abstract Venetoclax is a first in class BCL-2 inhibitor, currently under investigation for the treatment of t(11;14) multiple myeloma (MM). The objective of ... |
PMC10433423 | core_pubmed_pmc | The pharmacokinetic–pharmacodynamic modelling framework as a tool to predict drug resistance evolution | The pharmacokinetic–pharmacodynamic modelling framework as a tool to predict drug resistance evolution Abstract Abstract Pharmacokinetic–pharmacodynamic (PKPD) models, which describe how drug concentrations change over time and how that affects pathogen growth, have proven highly valuable in designing optimal drug trea... |
PMC9878670 | core_pubmed_pmc | Rapid In Vitro Quantification of a Sensitized Gadolinium Chelate via Photoinduced Triplet Harvesting | Rapid In Vitro Quantification of a Sensitized Gadolinium Chelate via Photoinduced Triplet Harvesting Abstract Abstract Gadolinium (Gd) based contrast agents (GBCAs) are widely used in magnetic resonance imaging (MRI) and are paramount to cancer diagnostics and tumor pharmacokinetic analysis. Accurate quantification of ... |
PMC5598146 | core_pubmed_pmc | Toxicological evaluation of the flavour ingredient 4-amino-5-(3-(isopropylamino)-2,2-dimethyl-3-oxopropoxy)-2-methylquinoline-3-carboxylic acid | Toxicological evaluation of the flavour ingredient 4-amino-5-(3-(isopropylamino)-2,2-dimethyl-3-oxopropoxy)-2-methylquinoline-3-carboxylic acid Abstract Abstract A toxicological evaluation of 4-amino-5-(3-(isopropylamino)-2,2-dimethyl-3-oxopropoxy)-2-methylquinoline-3-carboxylic acid(S9632; CAS 1359963-68-0), a flavour... |
PMC3252270 | core_pubmed_pmc | A Viral Dynamic Model for Treatment Regimens with Direct-acting Antivirals for Chronic Hepatitis C Infection | A Viral Dynamic Model for Treatment Regimens with Direct-acting Antivirals for Chronic Hepatitis C Infection Abstract Abstract We propose an integrative, mechanistic model that integrates in vitro virology data, pharmacokinetics, and viral response to a combination regimen of a direct-acting antiviral (telaprevir, an H... |
PMC10052254 | core_pubmed_pmc | Target-specificity of different amyrin subunits in impeding HCV influx mechanism inside the human cells considering the quantum tunnel profiles and molecular strings of the CD81 receptor: a combined in silico and in vivo study | Target-specificity of different amyrin subunits in impeding HCV influx mechanism inside the human cells considering the quantum tunnel profiles and molecular strings of the CD81 receptor: a combined in silico and in vivo study Abstract Abstract HCV is a hepatotropic RNA virus recognized for its frequent virulence and f... |
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