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PMC10666448 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics and effects of diet on AD16, a novel neuroinflammatory inhibitor for Alzheimer’s disease: a randomized phase 1 study | Safety, tolerability, pharmacokinetics and effects of diet on AD16, a novel neuroinflammatory inhibitor for Alzheimer’s disease: a randomized phase 1 study Abstract Background AD16 is a Class 1.1 new drug candidate for Alzheimer’s disease (AD), which has demonstrated potential benefits in AD by reducing neuroinflammati... |
PMC9220111 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Colistin Methanesulfonate in Healthy Chinese Subjects after Multi-Dose Regimen | Pharmacokinetics and Pharmacodynamics of Colistin Methanesulfonate in Healthy Chinese Subjects after Multi-Dose Regimen Abstract Colistin methanesulfonate (CMS) is an important treatment option for infections caused by carbapenem-resistant Gram-negative organisms (CROs). This study evaluated the pharmacokinetic/pharmac... |
PMC9211429 | core_pubmed_pmc | The Effect of Rifampicin on Darunavir, Ritonavir, and Dolutegravir Exposure within Peripheral Blood Mononuclear Cells: a Dose Escalation Study | The Effect of Rifampicin on Darunavir, Ritonavir, and Dolutegravir Exposure within Peripheral Blood Mononuclear Cells: a Dose Escalation Study Abstract ABSTRACT Ritonavir-boosted darunavir (DRV/r) and dolutegravir (DTG) are affected by induction of metabolizing enzymes and efflux transporters caused by rifampicin (RIF)... |
PMC8361743 | core_pubmed_pmc | Terminal half‐life of FVIII and FIX according to age, blood group and concentrate type: Data from the WAPPS database | Terminal half‐life of FVIII and FIX according to age, blood group and concentrate type: Data from the WAPPS database Abstract Abstract Background Real‐life data on pharmacokinetics of factor (F) VIII/IX concentrates, especially extended half‐life (EHL), concentrates in large cohorts of persons with hemophilia are curre... |
PMC12654086 | core_pubmed_pmc | Assessing the Influence of Proton Pump Inhibitors on Clinical Outcomes in Hormone Receptor-Positive Metastatic Breast Cancer Patients Receiving CDK4/6 Inhibitors: Evidence from a Ribociclib-Dominant Cohort | Assessing the Influence of Proton Pump Inhibitors on Clinical Outcomes in Hormone Receptor-Positive Metastatic Breast Cancer Patients Receiving CDK4/6 Inhibitors: Evidence from a Ribociclib-Dominant Cohort Abstract Background and Objectives : Endocrine therapy combined with CDK4/6 inhibitors are widely recognized as th... |
PMC11751299 | core_pubmed_pmc | Pharmacodynamics of interspecies interactions in polymicrobial infections | Pharmacodynamics of interspecies interactions in polymicrobial infections Abstract The pharmacodynamic response of bacterial pathogens to antibiotics can be influenced by interactions with other bacterial species in polymicrobial infections (PMIs). Understanding the complex eco-evolutionary dynamics of PMIs and their i... |
PMC10221165 | core_pubmed_pmc | Chemical Analysis and Molecular Modelling of Cyclodextrin-Formulated Propofol and Its Sodium Salt to Improve Drug Solubility, Stability and Pharmacokinetics (Cytogenotoxicity) | Chemical Analysis and Molecular Modelling of Cyclodextrin-Formulated Propofol and Its Sodium Salt to Improve Drug Solubility, Stability and Pharmacokinetics (Cytogenotoxicity) Abstract Abstract Propofol is a widely used general anesthetic in clinical practice, but its use is limited by its water-insoluble nature and as... |
PMC4836284 | core_pubmed_pmc | Inducible T-cell co-stimulator ligand (ICOSL) blockade leads to selective inhibition of anti-KLH IgG responses in subjects with systemic lupus erythematosus | Inducible T-cell co-stimulator ligand (ICOSL) blockade leads to selective inhibition of anti-KLH IgG responses in subjects with systemic lupus erythematosus Abstract Objectives To evaluate the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of single-dose and multiple-dose administration of AMG 55... |
PMC5807833 | core_pubmed_pmc | Prediction of Methionine and Homocysteine levels in Zucker diabetic fatty (ZDF) rats as a T2DM animal model after consumption of a Methionine-rich diet | Prediction of Methionine and Homocysteine levels in Zucker diabetic fatty (ZDF) rats as a T2DM animal model after consumption of a Methionine-rich diet Abstract Abstract Background Although alterations in the methionine metabolism cycle (MMC) have been associated with vascular complications of diabetes, there have not ... |
PMC10729150 | core_pubmed_pmc | XTX101, a tumor-activated, Fc-enhanced anti-CTLA-4 monoclonal antibody, demonstrates tumor-growth inhibition and tumor-selective pharmacodynamics in mouse models of cancer | XTX101, a tumor-activated, Fc-enhanced anti-CTLA-4 monoclonal antibody, demonstrates tumor-growth inhibition and tumor-selective pharmacodynamics in mouse models of cancer Abstract Abstract Introduction The clinical benefit of the anti-CTLA-4 monoclonal antibody (mAb) ipilimumab has been well established but limited by... |
PMC8137807 | core_pubmed_pmc | A first‐in‐human oral dose study of mesdopetam (IRL790) to assess its safety, tolerability, and pharmacokinetics in healthy male volunteers | A first‐in‐human oral dose study of mesdopetam (IRL790) to assess its safety, tolerability, and pharmacokinetics in healthy male volunteers Abstract Abstract The management of Parkinson's disease (PD) is frequently compromised by complications induced by dopaminergic treatment such as involuntary movements (dyskinesias... |
PMC9056642 | core_pubmed_pmc | Assessment of a developed HPLC-MS/MS approach for determining plasma eupatorin in rats and its application in pharmacokinetics analysis | Assessment of a developed HPLC-MS/MS approach for determining plasma eupatorin in rats and its application in pharmacokinetics analysis Abstract Abstract Eupatorin, a bioactive compound extracted from Java tea ( Orthosiphon stamineus ), possesses potent anti-cancer, anti-inflammatory and vasodilation activities. To dat... |
PMC5345986 | core_pubmed_pmc | New developments in the management of partial-onset epilepsy: role of brivaracetam | New developments in the management of partial-onset epilepsy: role of brivaracetam Abstract Currently, a number of novel anticonvulsant drugs, the so-called third generation, are in various stages of development. Several of them are already available or in ongoing clinical trials. These new compounds should take advant... |
PMC3970305 | core_pubmed_pmc | Underestimation of the Calculated Area Under the Concentration-Time Curve Based on Serum Creatinine for Vancomycin Dosing | Underestimation of the Calculated Area Under the Concentration-Time Curve Based on Serum Creatinine for Vancomycin Dosing Abstract Background The ratio of the steady-state 24-hour area under the concentration-time curve (ssAUC 24 ) to the MIC (AUC 24 /MIC) for vancomycin has been recommended as the preferred pharmacody... |
PMC3603474 | core_pubmed_pmc | Modeling Interindividual Variability in Physiologically Based Pharmacokinetics and Its Link to Mechanistic Covariate Modeling | Modeling Interindividual Variability in Physiologically Based Pharmacokinetics and Its Link to Mechanistic Covariate Modeling Abstract Covariate modeling is a key step in the analysis of clinical data and is essential for establishing dosing recommendations for specific populations, e.g., in obese individuals and child... |
PMC12486194 | core_pubmed_pmc | Pharmacokinetics, Safety, and Skin Irritation and Sensitization Potential of Clascoterone Cream in Early‐Phase Clinical Study Participants | Pharmacokinetics, Safety, and Skin Irritation and Sensitization Potential of Clascoterone Cream in Early‐Phase Clinical Study Participants Abstract Abstract Clascoterone is an androgen receptor inhibitor approved for the treatment of acne vulgaris in patients 12 years of age and older. Here, we report results of 5 phas... |
PMC4823323 | core_pubmed_pmc | Development of Human Membrane Transporters: Drug Disposition and Pharmacogenetics | Development of Human Membrane Transporters: Drug Disposition and Pharmacogenetics Abstract Abstract Membrane transporters play an essential role in the transport of endogenous and exogenous compounds, and consequently they mediate the uptake, distribution, and excretion of many drugs. The clinical relevance of transpor... |
PMC6479388 | core_pubmed_pmc | Quantitative Analysis of Tozadenant Using Liquid Chromatography-Mass Spectrometric Method in Rat Plasma and Its Human Pharmacokinetics Prediction Using Physiologically Based Pharmacokinetic Modeling | Quantitative Analysis of Tozadenant Using Liquid Chromatography-Mass Spectrometric Method in Rat Plasma and Its Human Pharmacokinetics Prediction Using Physiologically Based Pharmacokinetic Modeling Abstract Abstract Tozadenant is one of the selective adenosine A2a receptor antagonists with a potential to be a new Park... |
PMC11366868 | core_pubmed_pmc | Evaluation of sunobinop for next-day residual effects in healthy participants | Evaluation of sunobinop for next-day residual effects in healthy participants Abstract Sunobinop is a novel, potent, selective partial agonist at nociceptin/orphanin FQ peptide (NOP) receptors. The primary objective of this randomized, double-blind, placebo-controlled study was to assess the next-day residual effects o... |
PMC9290801 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug‐Drug Interactions and Pediatric Dose Regimens | Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug‐Drug Interactions and Pediatric Dose Regimens Abstract Abstract Selumetinib (ARRY‐142886), an oral, potent and highly selective allosteric mitogen‐activated protein kinase kinase 1/2 inhibitor, is approved by the US Food and Drug Administra... |
PMC11625063 | core_pubmed_pmc | Clinical research progress of fruquintinib in the treatment of malignant tumors | Clinical research progress of fruquintinib in the treatment of malignant tumors Abstract Abstract Malignant tumors represent an important cause of mortality within the global population. Tumor angiogenesis, recognized as one of the key hallmarks of malignant tumors, is crucial for supplying essential nutrients and oxyg... |
PMC6329051 | core_pubmed_pmc | Clazakizumab in late antibody-mediated rejection: study protocol of a randomized controlled pilot trial | Clazakizumab in late antibody-mediated rejection: study protocol of a randomized controlled pilot trial Abstract Background Late antibody-mediated rejection (ABMR) triggered by donor-specific antibodies (DSA) is a cardinal cause of kidney allograft dysfunction and loss. Diagnostic criteria for this rejection type are w... |
PMC5700771 | core_pubmed_pmc | Assessment of a statistical AIF extraction method for dynamic PET studies with 15 O water and 18 F fluorodeoxyglucose in locally advanced breast cancer patients | Assessment of a statistical AIF extraction method for dynamic PET studies with 15 O water and 18 F fluorodeoxyglucose in locally advanced breast cancer patients Abstract Abstract. Blood flow-metabolism mismatch from dynamic positron emission tomography (PET) studies with O 15 -labeled water ( H 2 O ) and F 18 -labeled ... |
PMC6535670 | core_pubmed_pmc | Bioequivalence of paclitaxel protein-bound particles in patients with breast cancer: determining total and unbound paclitaxel in plasma by rapid equilibrium dialysis and liquid chromatography–tandem mass spectrometry | Bioequivalence of paclitaxel protein-bound particles in patients with breast cancer: determining total and unbound paclitaxel in plasma by rapid equilibrium dialysis and liquid chromatography–tandem mass spectrometry Abstract Abstract Background and objective: Paclitaxel protein-bound particles for injectable suspensio... |
PMC6519384 | core_pubmed_pmc | Accurate measurement of androgen after androgen esters: problems created by ex vivo esterase effects and LC‐MS/MS interference | Accurate measurement of androgen after androgen esters: problems created by ex vivo esterase effects and LC‐MS/MS interference Abstract Abstract Background Ex vivo androgen prodrug conversion by blood esterases after oral androgen ester administration may result in an overestimation of the measured blood androgens. Obj... |
PMC8286575 | core_pubmed_pmc | Biomimetic recombinant of red blood cell membranes for improved photothermal therapy | Biomimetic recombinant of red blood cell membranes for improved photothermal therapy Abstract Background RBC membrane derived nanoparticles (NPs) represent an emerging platform with prolonged circulation capacity for the delivery of active substances. For functionalize derived RBCs NPs, various strategies, such as biom... |
PMC11067167 | core_pubmed_pmc | Quantitative investigation of drug-drug interaction between bergenin and vilazodone in rats through UPLC-MS/MS assay | Quantitative investigation of drug-drug interaction between bergenin and vilazodone in rats through UPLC-MS/MS assay Abstract Abstract In this study, we firstly established and verified a method by ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) for the analysis of vilazodone and its metab... |
PMC5307914 | core_pubmed_pmc | Comparative Pharmacokinetic Profiles of Three Protoberberine-type Alkaloids from Raw and Bile-processed Rhizoma coptidis in Heat Syndrome Rats | Comparative Pharmacokinetic Profiles of Three Protoberberine-type Alkaloids from Raw and Bile-processed Rhizoma coptidis in Heat Syndrome Rats Abstract Abstract Background: The Bile-processed Rhizoma coptidis (BRC), which has a colder drug property than Rhizoma coptidis (RC), is widely used for the treatment of heat sy... |
PMC12001273 | core_pubmed_pmc | PBPK ‐Led Assessment of Antimalarial Drug Concentrations in Breastmilk: A Strategy for Optimal Use of Prediction Methods to Guide Decision Making in an Understudied Population | PBPK ‐Led Assessment of Antimalarial Drug Concentrations in Breastmilk: A Strategy for Optimal Use of Prediction Methods to Guide Decision Making in an Understudied Population Abstract ABSTRACT Treatment of breastfeeding mothers with malaria is challenging due to the lack of information describing drug exposure in milk... |
PMC11980851 | core_pubmed_pmc | Preclinical evaluation of AGT mRNA replacement therapy for primary hyperoxaluria type I disease | Preclinical evaluation of AGT mRNA replacement therapy for primary hyperoxaluria type I disease Abstract Primary hyperoxaluria type 1 (PH1) is a rare inherited liver disorder caused by alanine glyoxylate aminotransferase (AGT) dysfunction, leading to accumulation of glyoxylate which is then converted into oxalate. Exce... |
PMC7365463 | core_pubmed_pmc | Oxfendazole mediates macrofilaricidal efficacy against the filarial nematode Litomosoides sigmodontis in vivo and inhibits Onchocerca spec . motility in vitro | Oxfendazole mediates macrofilaricidal efficacy against the filarial nematode Litomosoides sigmodontis in vivo and inhibits Onchocerca spec . motility in vitro Abstract A major impediment to eliminate lymphatic filariasis and onchocerciasis is the lack of effective short-course macrofilaricidal drugs or regimens that ar... |
PMC11296516 | core_pubmed_pmc | Revealing Changes in Celecoxib Nanostructured Lipid Carrier’s Bioavailability Using Hyaluronic Acid as an Enhancer by HPLC-MS/MS | Revealing Changes in Celecoxib Nanostructured Lipid Carrier’s Bioavailability Using Hyaluronic Acid as an Enhancer by HPLC-MS/MS Abstract Purpose Oral drug administration is the most common and convenient route, offering good patient compliance but drug solubility limits oral applications. Celecoxib, an insoluble drug,... |
PMC8537267 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Model of Neutropenia in Real-Life Palbociclib-Treated Patients | Pharmacokinetic/Pharmacodynamic Model of Neutropenia in Real-Life Palbociclib-Treated Patients Abstract Palbociclib is an oral CDK4/6 inhibitor indicated in HR+/HER2- advanced or metastatic breast cancer in combination with hormonotherapy. Its main toxicity is neutropenia. The aim of our study was to describe the kinet... |
PMC11160854 | core_pubmed_pmc | Clinical Predictors of 3-Months Isoniazid Rifapentine (3HP) - Related Adverse Drug Reactions (ADR) During Tuberculosis Preventive Therapy. (PAnDoRA-3HP study): An Observational Study Protocol | Clinical Predictors of 3-Months Isoniazid Rifapentine (3HP) - Related Adverse Drug Reactions (ADR) During Tuberculosis Preventive Therapy. (PAnDoRA-3HP study): An Observational Study Protocol Abstract Introduction Tuberculosis (TB) is the leading infectious cause of death globally. Despite WHO recommendations for Tuber... |
PMC10949085 | core_pubmed_pmc | A phase Ib study evaluating the recommended phase II dose, safety, tolerability, and efficacy of mivavotinib in combination with nivolumab in advanced solid tumors | A phase Ib study evaluating the recommended phase II dose, safety, tolerability, and efficacy of mivavotinib in combination with nivolumab in advanced solid tumors Abstract Abstract Mivavotinib (TAK‐659/CB‐659), a dual SYK/FLT3 inhibitor, reduced immunosuppressive immune cell populations and suppressed tumor growth in ... |
PMC6288157 | core_pubmed_pmc | A phase Ib dose-escalation and expansion study of the oral MEK inhibitor pimasertib and PI3K/MTOR inhibitor voxtalisib in patients with advanced solid tumours | A phase Ib dose-escalation and expansion study of the oral MEK inhibitor pimasertib and PI3K/MTOR inhibitor voxtalisib in patients with advanced solid tumours Abstract Abstract Background This phase Ib study evaluated the safety, maximum-tolerated dose (MTD), pharmacokinetics, pharmacodynamics, and preliminary efficacy... |
PMC12141673 | core_pubmed_pmc | A PBPK modeling approach for personalized dose optimization of nicardipine in renal and hepatic dysfunction | A PBPK modeling approach for personalized dose optimization of nicardipine in renal and hepatic dysfunction Abstract Abstract Nicardipine is a calcium channel blocker employed to manage hypertension and angina. It is primarily metabolized in the liver; therefore, hepatic impairment patients may experience drug accumula... |
PMC7187253 | core_pubmed_pmc | A Thorough QT Study to Evaluate the Effects of a Supratherapeutic Dose of Sertraline on Cardiac Repolarization in Healthy Subjects | A Thorough QT Study to Evaluate the Effects of a Supratherapeutic Dose of Sertraline on Cardiac Repolarization in Healthy Subjects Abstract Abstract The effect of steady‐state supratherapeutic sertraline (Zoloft) on QT interval was assessed in a single‐center, randomized, 3‐way crossover, double‐blind, placebo‐ and mox... |
PMC12378131 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling-Based Evaluation of Current Carbamazepine and Valproic Acid Dosing Guidelines for Pediatric Epilepsy Treatment | Physiologically Based Pharmacokinetic Modeling-Based Evaluation of Current Carbamazepine and Valproic Acid Dosing Guidelines for Pediatric Epilepsy Treatment Abstract Background Carbamazepine and valproic acid (VPA) are long-standing treatments for epilepsy in children. Interestingly, they display unique drug dispositi... |
PMC7517894 | core_pubmed_pmc | Computational Approaches in Preclinical Studies on Drug Discovery and Development | Computational Approaches in Preclinical Studies on Drug Discovery and Development Abstract Because undesirable pharmacokinetics and toxicity are significant reasons for the failure of drug development in the costly late stage, it has been widely recognized that drug ADMET properties should be considered as early as pos... |
PMC3888848 | core_pubmed_pmc | The efficacy of the time-scheduled decremental continuous infusion of fentanyl for postoperative patient-controlled analgesia after total intravenous anesthesia | The efficacy of the time-scheduled decremental continuous infusion of fentanyl for postoperative patient-controlled analgesia after total intravenous anesthesia Abstract Background Intravenous fentanyl has been used for acute postoperative pain management, but has not always provided reliable adequate analgesia, includ... |
PMC6868133 | core_pubmed_pmc | Pharmacokinetics of Exenatide in nonhuman primates following its administration in the form of sustained-release PT320 and Bydureon | Pharmacokinetics of Exenatide in nonhuman primates following its administration in the form of sustained-release PT320 and Bydureon Abstract The time-dependent (30 min - day 84) plasma profile of PT320, a sustained-release (SR)-Exenatide formulation under clinical development for treatment of neurodegenerative disorder... |
PMC6100475 | core_pubmed_pmc | Development and Validation of a HPLC-MS/MS Method for Simultaneous Determination of Twelve Bioactive Compounds in Epimedium : Application to a Pharmacokinetic Study in Rats | Development and Validation of a HPLC-MS/MS Method for Simultaneous Determination of Twelve Bioactive Compounds in Epimedium : Application to a Pharmacokinetic Study in Rats Abstract Abstract A rapid and reliable HPLC-MS/MS method has been developed and validated for the simultaneous quantification of twelve bioactive c... |
PMC11391713 | core_pubmed_pmc | Pharmacological and physiological effects of cannabidiol: a dose escalation, placebo washout study protocol | Pharmacological and physiological effects of cannabidiol: a dose escalation, placebo washout study protocol Abstract Abstract Background Cannabinoids such as cannabidiol (CBD) exhibit anti-inflammatory properties and have the potential to act as a therapeutic following mild traumatic brain injury. There is limited evid... |
PMC6162236 | core_pubmed_pmc | Safety, anti-tumour activity, and pharmacokinetics of fixed-dose SHR-1210, an anti-PD-1 antibody in advanced solid tumours: a dose-escalation, phase 1 study | Safety, anti-tumour activity, and pharmacokinetics of fixed-dose SHR-1210, an anti-PD-1 antibody in advanced solid tumours: a dose-escalation, phase 1 study Abstract Abstract Background To assess the safety profile, pharmacokinetics, pharmacodynamics and preliminary antitumour activity of fixed-dose SHR-1210, a novel a... |
PMC8329375 | core_pubmed_pmc | Case Report: Predicting the Range of Lamotrigine Concentration Using Pharmacokinetic Models Based on Monte Carlo Simulation: A Case Study of Antiepileptic Drug-Related Leukopenia | Case Report: Predicting the Range of Lamotrigine Concentration Using Pharmacokinetic Models Based on Monte Carlo Simulation: A Case Study of Antiepileptic Drug-Related Leukopenia Abstract Lamotrigine (LTG), a wide-spectrum antiepileptic drug, is frequently associated with cutaneous side-effects, whereas hematological s... |
PMC11216006 | core_pubmed_pmc | Icanbelimod (CBP-307), a next-generation Sphingosine-1-phosphate receptor modulator, in healthy men: pharmacokinetics, pharmacodynamics, safety, and tolerability in a randomized trial in Australia | Icanbelimod (CBP-307), a next-generation Sphingosine-1-phosphate receptor modulator, in healthy men: pharmacokinetics, pharmacodynamics, safety, and tolerability in a randomized trial in Australia Abstract Abstract Background Icanbelimod (formerly CBP-307) is a next-generation S1PR modulator, targeting S1PR 1 . In this... |
PMC9961156 | core_pubmed_pmc | Virtual Clinical Trials Guided Design of an Age-Appropriate Formulation and Dosing Strategy of Nifedipine for Paediatric Use | Virtual Clinical Trials Guided Design of an Age-Appropriate Formulation and Dosing Strategy of Nifedipine for Paediatric Use Abstract The rapid onset of action of nifedipine causes a precipitous reduction in blood pressure leading to adverse effects associated with reflex sympathetic nervous system (SNS) activation, in... |
PMC3346058 | core_pubmed_pmc | Critical appraisal of lurasidone in the management of schizophrenia | Critical appraisal of lurasidone in the management of schizophrenia Abstract Abstract Lurasidone is a new atypical antipsychotic in the benzoisothiazoles class of chemicals. Like most second-generation antipsychotics it is a full antagonist at dopamine D 2 and serotonin 5-HT 2A receptors, and is a partial agonist at 5-... |
PMC6068194 | core_pubmed_pmc | Neoadjuvant PF-05280014 (a potential trastuzumab biosimilar) versus trastuzumab for operable HER2+ breast cancer | Neoadjuvant PF-05280014 (a potential trastuzumab biosimilar) versus trastuzumab for operable HER2+ breast cancer Abstract Abstract Background This randomised, double-blind study compared pharmacokinetics, efficacy, safety and immunogenicity of PF-05280014 (potential trastuzumab biosimilar) and trastuzumab reference pro... |
PMC8667269 | core_pubmed_pmc | Statin Therapy in Very Old Patients: Lights and Shadows | Statin Therapy in Very Old Patients: Lights and Shadows Abstract Atherosclerotic cardiovascular diseases (ASCVD) are the leading cause of death worldwide. High levels of total cholesterol—and of low-density lipoprotein cholesterol in particular—are one of the main risk factors associated with ASCVD. Statins are first-l... |
PMC9736746 | core_pubmed_pmc | Lack of Effect of Cenerimod, a Selective S1P 1 Receptor Modulator, on the Pharmacokinetics of a Combined Oral Contraceptive | Lack of Effect of Cenerimod, a Selective S1P 1 Receptor Modulator, on the Pharmacokinetics of a Combined Oral Contraceptive Abstract Abstract Cenerimod, a sphingosine-1-phosphate 1 receptor modulator, is in development for the treatment of systemic lupus erythematosus, a disease mainly affecting women of childbearing p... |
PMC7569237 | core_pubmed_pmc | BPRDP056, a novel small molecule drug conjugate specifically targeting phosphatidylserine for cancer therapy | BPRDP056, a novel small molecule drug conjugate specifically targeting phosphatidylserine for cancer therapy Abstract Abstract Zinc(II)-dipicolylamine (Zn-DPA) has been shown to specifically identify and bind to phosphatidylserine (PS), which exists in bulk in the tumor microenvironment. BPRDP056, a Zn-DPA-SN38 conjuga... |
PMC5021919 | core_pubmed_pmc | Improved bioavailability of timolol maleate via transdermal transfersomal gel: Statistical optimization, characterization, and pharmacokinetic assessment | Improved bioavailability of timolol maleate via transdermal transfersomal gel: Statistical optimization, characterization, and pharmacokinetic assessment Abstract Timolol maleate (TiM), a nonselective β-adrenergic blocker, is a potent highly effective agent for management of hypertension. The drug suffers from extensiv... |
PMC9010268 | core_pubmed_pmc | Pediatric growth patterns in youth‐onset type 2 diabetes mellitus: Implications for physiologically‐based pharmacokinetic models | Pediatric growth patterns in youth‐onset type 2 diabetes mellitus: Implications for physiologically‐based pharmacokinetic models Abstract Abstract An accurate understanding of the changes in height and weight of children with age is critical to the development of models predicting drug concentrations in children (i.e.,... |
PMC12697044 | core_pubmed_pmc | Evaluation of Efficacy and Review of Side Effect Profile in Epilepsy Patients Treated with Extended-Release Levetiracetam | Evaluation of Efficacy and Review of Side Effect Profile in Epilepsy Patients Treated with Extended-Release Levetiracetam Abstract ABSTRACT Background and Objective: Extended-release levetiracetam offers pharmacokinetic advantages over immediate-release formulations, including stable plasma concentrations and once-dail... |
PMC9031635 | core_pubmed_pmc | Simultaneous Quantification and Pharmacokinetic Characterization of Doxapram and 2-Ketodoxapram in Porcine Plasma and Brain Tissue | Simultaneous Quantification and Pharmacokinetic Characterization of Doxapram and 2-Ketodoxapram in Porcine Plasma and Brain Tissue Abstract Atrial fibrillation (AF) is an arrhythmia associated with an increased stroke risk and mortality rate. Current treatment options leave unmet needs in AF therapy. Recently, doxapram... |
PMC12736208 | core_pubmed_pmc | A Multi-Omics Study Reveals the Active Components and Therapeutic Mechanism of Erhuang Quzhi Formula for Non-Alcoholic Fatty Liver Disease | A Multi-Omics Study Reveals the Active Components and Therapeutic Mechanism of Erhuang Quzhi Formula for Non-Alcoholic Fatty Liver Disease Abstract Objectives : Erhuang Quzhi Formula (EQF) has been used for the treatment of non-alcoholic fatty liver disease (NAFLD). However, its active components and mechanistic basis ... |
PMC12158843 | core_pubmed_pmc | Pharmacokinetics and Lung Deposition After Administration of Inhaled Mosliciguat (BAY 1237592): Results from Randomized Phase I Studies in Healthy Men | Pharmacokinetics and Lung Deposition After Administration of Inhaled Mosliciguat (BAY 1237592): Results from Randomized Phase I Studies in Healthy Men Abstract Background and Objective Mosliciguat is the first soluble guanylate cyclase activator designed for dry powder inhalation. It is currently under development for ... |
PMC6321252 | core_pubmed_pmc | Enhancement of Berberine Hypoglycemic Activity by Oligomeric Proanthocyanidins | Enhancement of Berberine Hypoglycemic Activity by Oligomeric Proanthocyanidins Abstract Abstract This study investigated the possible enhancement of berberine’s (BB) hypoglycemic activity by oligomeric proanthocyanidins (OPCs) and its underlying mechanism. The hypoglycemic activity of the studied compounds was evaluate... |
PMC10573769 | core_pubmed_pmc | Pharmacokinetic Model-Based Control across the Blood–Brain Barrier for Circadian Entrainment | Pharmacokinetic Model-Based Control across the Blood–Brain Barrier for Circadian Entrainment Abstract Abstract The ability to shift circadian phase in vivo has the potential to offer substantial health benefits. However, the blood–brain barrier prevents the absorption of the majority of large and many small molecules, ... |
PMC9164301 | core_pubmed_pmc | Improving Therapy of Pharmacoresistant Epilepsies: The Role of Fenfluramine | Improving Therapy of Pharmacoresistant Epilepsies: The Role of Fenfluramine Abstract Abstract Epilepsy is among the most common neurological chronic disorders, with a prevalence of 0.5–1%. Despite the introduction of new antiepileptic drugs during recent years, about one third of the epileptic population remain drug-re... |
PMC7204809 | core_pubmed_pmc | ALKS 4230: a novel engineered IL-2 fusion protein with an improved cellular selectivity profile for cancer immunotherapy | ALKS 4230: a novel engineered IL-2 fusion protein with an improved cellular selectivity profile for cancer immunotherapy Abstract Background Interleukin-2 (IL-2) plays a pivotal role in immune homeostasis due to its ability to stimulate numerous lymphocyte subsets including natural killer (NK) cells, effector CD4 + and... |
PMC11893723 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of SC1011 (Sufenidone), a Novel Antifibrotic Small Molecule, in Phase 1 Studies in Healthy Subjects | Safety, Tolerability, and Pharmacokinetics of SC1011 (Sufenidone), a Novel Antifibrotic Small Molecule, in Phase 1 Studies in Healthy Subjects Abstract ABSTRACT SC1011 (sufenidone) is a novel pyridone derivative with therapeutic potential for idiopathic pulmonary fibrosis (IPF). Two Phase 1 studies evaluated the safety... |
PMC10520058 | core_pubmed_pmc | Association between SLCO1B1 genetic polymorphisms and bleeding risk in patients treated with edoxaban | Association between SLCO1B1 genetic polymorphisms and bleeding risk in patients treated with edoxaban Abstract Since SLCO1B1 encodes the uptake transporter OATP1B1, which can influence the pharmacokinetic and pharmacodynamic profiles of edoxaban, polymorphisms in SLCO1B1 may affect the edoxaban response. This study aim... |
PMC2939854 | core_pubmed_pmc | Novel GLP-1 Fusion Chimera as Potent Long Acting GLP-1 Receptor Agonist | Novel GLP-1 Fusion Chimera as Potent Long Acting GLP-1 Receptor Agonist Abstract GLP-1 has a variety of anti-diabetic effects. However, native GLP-1 is not suitable for therapy of diabetes due to its short half-life (t1/2<2 min). To circumvent this, we developed a long-lasting GLP-1 receptor agonist by the fusion of GL... |
PMC12446568 | core_pubmed_pmc | Utilization of Machine Learning Approaches for Drug Clearance Prediction and Population Pharmacokinetic Covariate Analysis | Utilization of Machine Learning Approaches for Drug Clearance Prediction and Population Pharmacokinetic Covariate Analysis Abstract ABSTRACT Population pharmacokinetic (popPK) analysis is routinely used to evaluate drug clearance and covariate effects on pharmacokinetic parameters to support dosing recommendations. Whi... |
PMC4821377 | core_pubmed_pmc | A novel tetrandrine-loaded chitosan microsphere: characterization and in vivo evaluation | A novel tetrandrine-loaded chitosan microsphere: characterization and in vivo evaluation Abstract In this study, novel tetrandrine-loaded chitosan microspheres were prepared by the emulsion cross-linking method. The systems were then characterized for physicochemical properties and in vitro drug release. In addition, t... |
PMC9400904 | core_pubmed_pmc | Regio‐ and Stereoselective Epoxidation and Acidic Epoxide Opening of Antibacterial and Antiplasmodial Chlorotonils Yield Highly Potent Derivatives | Regio‐ and Stereoselective Epoxidation and Acidic Epoxide Opening of Antibacterial and Antiplasmodial Chlorotonils Yield Highly Potent Derivatives Abstract Abstract The rise of antimicrobial resistance poses a severe threat to public health. The natural product chlorotonil was identified as a new antibiotic targeting m... |
PMC12702926 | core_pubmed_pmc | Deep learning-guided discovery of selective JAK2-JH2 allosteric inhibitors: integration of MLP predictive modeling, BREED-based library design, and computational validation | Deep learning-guided discovery of selective JAK2-JH2 allosteric inhibitors: integration of MLP predictive modeling, BREED-based library design, and computational validation Abstract Abstract The JAK2 pseudokinase domain (JH2) is an important therapeutic target in hematologic and oncologic diseases, motivating the searc... |
PMC6161803 | core_pubmed_pmc | The importance of clinical pharmacokinetic–pharmacodynamic studies in unraveling the determinants of early and late tuberculosis outcomes | The importance of clinical pharmacokinetic–pharmacodynamic studies in unraveling the determinants of early and late tuberculosis outcomes Abstract Abstract Tuberculosis remains a major infectious cause of morbidity and mortality worldwide. Current antibiotic regimens, constructed prior to the development of modern phar... |
PMC9147984 | core_pubmed_pmc | The Role of Atropine in Preventing Myopia Progression: An Update | The Role of Atropine in Preventing Myopia Progression: An Update Abstract Abstract Several approaches have been investigated for preventing myopia progression in children and teenagers. Among them, topical atropine has shown promising results and it is being adopted in clinical practice more and more frequently. Howeve... |
PMC11206683 | core_pubmed_pmc | Scaffold-Hopping Strategies in Aurone Optimization: A Comprehensive Review of Synthetic Procedures and Biological Activities of Nitrogen and Sulfur Analogues | Scaffold-Hopping Strategies in Aurone Optimization: A Comprehensive Review of Synthetic Procedures and Biological Activities of Nitrogen and Sulfur Analogues Abstract Aurones, particular polyphenolic compounds belonging to the class of minor flavonoids and overlooked for a long time, have gained significative attention... |
PMC12886976 | core_pubmed_pmc | Long-term in vivo pharmacokinetics of dexamethasone-loaded cochlear implant electrode carrier dummies with optimized release profiles | Long-term in vivo pharmacokinetics of dexamethasone-loaded cochlear implant electrode carrier dummies with optimized release profiles Abstract Abstract Cochlear implants (CIs) are the primary treatment for severe hearing loss. However, despite advances in electrode materials, implantation remains invasive and can cause... |
PMC10568112 | core_pubmed_pmc | Gut microbiota-based pharmacokinetic-pharmacodynamic study and molecular mechanism of specnuezhenide in the treatment of colorectal cancer targeting carboxylesterase | Gut microbiota-based pharmacokinetic-pharmacodynamic study and molecular mechanism of specnuezhenide in the treatment of colorectal cancer targeting carboxylesterase Abstract Abstract Specnuezhenide (SNZ) is among the main components of Fructus Ligustri Lucidi, which has anti-inflammation, anti-oxidation, and anti-tumo... |
PMC7785882 | core_pubmed_pmc | Characteristics of Medical Products Comprising Human Cells, Genes, or Tissues Developed in Japan and the European Union Compared via Public Assessment Reports | Characteristics of Medical Products Comprising Human Cells, Genes, or Tissues Developed in Japan and the European Union Compared via Public Assessment Reports Abstract Abstract Medical products comprising human cells, genes, and tissues have been developed for clinical applications worldwide, and their developmental en... |
PMC10671963 | core_pubmed_pmc | Oral Bioavailability and Pharmacokinetics of Sildenafil Orally Disintegrating Tablets under Various Gastric pH Levels Following Administration of Omeprazole in Rats | Oral Bioavailability and Pharmacokinetics of Sildenafil Orally Disintegrating Tablets under Various Gastric pH Levels Following Administration of Omeprazole in Rats Abstract Abstract Sildenafil citrate, an oral drug used to treat erectile dysfunction, has low water solubility and oral bioavailability. The solubility is... |
PMC5762444 | core_pubmed_pmc | Determination of torasemide in human plasma and its bioequivalence study by high-performance liquid chromatography with electrospray ionization tandem mass spectrometry ☆ | Determination of torasemide in human plasma and its bioequivalence study by high-performance liquid chromatography with electrospray ionization tandem mass spectrometry ☆ Abstract A sensitive and selective method using high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry ... |
PMC9381895 | core_pubmed_pmc | Model‐informed bridging of rivaroxaban doses for thromboprophylaxis in pediatric patients aged 9 years and older with congenital heart disease | Model‐informed bridging of rivaroxaban doses for thromboprophylaxis in pediatric patients aged 9 years and older with congenital heart disease Abstract Abstract Rivaroxaban is approved in various regions for the treatment of acute venous thromboembolism (VTE) in children aged between 0 and 18 years and was recently inv... |
PMC7736590 | core_pubmed_pmc | C-demethylation and 1, 2-amino shift in (E)-2-(1-(3-aminophenyl) ethylidene)hydrazinecarboxamide to (E)-2-(2-aminobenzylidene)hydrazinecarboxamide and their applications | C-demethylation and 1, 2-amino shift in (E)-2-(1-(3-aminophenyl) ethylidene)hydrazinecarboxamide to (E)-2-(2-aminobenzylidene)hydrazinecarboxamide and their applications Abstract A Novel (E)-2-(1-(3-aminophenyl)ethylidene)hydrazinecarboxamide 1 was synthesized by traditional method and converted to (E)-2-(2-aminobenzyl... |
PMC12242177 | core_pubmed_pmc | Editorial: Application of PKPD modeling in drug discovery and development | Editorial: Application of PKPD modeling in drug discovery and development Modeling Accelerating clinical development with model-informed strategies The COVID-19 pandemic underscored the need for rapid clinical development, a challenge addressed through model-informed drug development (MIDD). The leritrelvir study demon... |
PMC8954677 | core_pubmed_pmc | Poly (Lactic-Co-Glycolic) Acid–Poly (Vinyl Pyrrolidone) Hybrid Nanoparticles to Improve the Efficiency of Oral Delivery of β-Carotene | Poly (Lactic-Co-Glycolic) Acid–Poly (Vinyl Pyrrolidone) Hybrid Nanoparticles to Improve the Efficiency of Oral Delivery of β-Carotene Abstract The aim of this study was to develop a nanoparticle formulation made of poly (vinyl pyrrolidone) (PVP) and poly (lactic-co-glycolic) acid (PLGA) for the oral delivery of β-carot... |
PMC12899999 | core_pubmed_pmc | Anti-Inflammatory Effects of Bisacurone Isolated from Curcuma longa (Ryudai Gold): An In Vivo and In Silico Study | Anti-Inflammatory Effects of Bisacurone Isolated from Curcuma longa (Ryudai Gold): An In Vivo and In Silico Study Abstract Bisacurone is a sesquiterpenoid constituent of Curcuma longa that has received considerably less attention than curcuminoids despite emerging evidence of its biological activity. In this study, the... |
PMC4661432 | core_pubmed_pmc | Pharmacokinetics and Dosimetry Studies for Optimization of Pretargeted Radioimmunotherapy in CEA-Expressing Advanced Lung Cancer Patients | Pharmacokinetics and Dosimetry Studies for Optimization of Pretargeted Radioimmunotherapy in CEA-Expressing Advanced Lung Cancer Patients Abstract Abstract Objectives A phase I pretargeted radioimmunotherapy trial (EudractCT 200800603096) was designed in patients with metastatic lung cancer expressing carcinoembryonic ... |
PMC4229181 | core_pubmed_pmc | Vancomycin Dosing in Neutropenic Patients | Vancomycin Dosing in Neutropenic Patients Abstract Background To compare vancomycin pharmacokinetic parameters in patients with and without neutropenia. Methods Patients ≥18 years admitted on general wards were included. Routinely vancomycin trough and peak plasma concentrations were measured with a fluorescence polari... |
PMC10558021 | core_pubmed_pmc | Post-Transplant Cyclophosphamide for the Prevention of Graft-vs.-Host Disease in Allogeneic Hematopoietic Cell Transplantation: A Guide to Management for the Advanced Practitioner | Post-Transplant Cyclophosphamide for the Prevention of Graft-vs.-Host Disease in Allogeneic Hematopoietic Cell Transplantation: A Guide to Management for the Advanced Practitioner Abstract Abstract Cyclophosphamide remains a critical component to haploidentical transplant conditioning regimens. Post-transplant cyclopho... |
PMC9547507 | core_pubmed_pmc | Pharmacokinetic Analysis and In Vitro Synergy Evaluation of Cefiderocol, Sulbactam, and Tigecycline in an Extensively Drug-Resistant Acinetobacter baumannii Pneumonia Patient Receiving Continuous Venovenous Hemodiafiltration | Pharmacokinetic Analysis and In Vitro Synergy Evaluation of Cefiderocol, Sulbactam, and Tigecycline in an Extensively Drug-Resistant Acinetobacter baumannii Pneumonia Patient Receiving Continuous Venovenous Hemodiafiltration Abstract Abstract Antimicrobial treatments for extensively drug-resistant Acinetobacter baumann... |
PMC12053642 | core_pubmed_pmc | Oral PRI-002 treatment in patients with MCI or mild AD: a randomized, double-blind phase 1b trial | Oral PRI-002 treatment in patients with MCI or mild AD: a randomized, double-blind phase 1b trial Abstract Abstract Self-replicating amyloid beta (Aβ) oligomers are considered as one of the major drivers for disrupted synaptic function and plasticity, leading to impaired neuronal viability and progression of Alzheimer’... |
PMC6335810 | core_pubmed_pmc | MITK-ModelFit: A generic open-source framework for model fits and their exploration in medical imaging – design, implementation and application on the example of DCE-MRI | MITK-ModelFit: A generic open-source framework for model fits and their exploration in medical imaging – design, implementation and application on the example of DCE-MRI Abstract Background Many medical imaging techniques utilize fitting approaches for quantitative parameter estimation and analysis. Common examples are... |
PMC4948680 | core_pubmed_pmc | Preclinical pharmacokinetics, biodistribution, radiation dosimetry and toxicity studies required for regulatory approval of a phase I clinical trial with 111 In-CP04 in medullary thyroid carcinoma patients | Preclinical pharmacokinetics, biodistribution, radiation dosimetry and toxicity studies required for regulatory approval of a phase I clinical trial with 111 In-CP04 in medullary thyroid carcinoma patients Abstract Abstract Introduction From a series of radiolabelled cholecystokinin (CCK) and gastrin analogues, 111 In-... |
PMC8112767 | core_pubmed_pmc | Pharmacokinetics of Supplemental Omega-3 Fatty Acids Esterified in Monoglycerides, Ethyl Esters, or Triglycerides in Adults in a Randomized Crossover Trial | Pharmacokinetics of Supplemental Omega-3 Fatty Acids Esterified in Monoglycerides, Ethyl Esters, or Triglycerides in Adults in a Randomized Crossover Trial Abstract ABSTRACT Background Omega-3 (n–3) fatty acid (FA) supplements increase blood concentrations of EPA and DHA. Most of the supplements on the market are ester... |
PMC7863331 | core_pubmed_pmc | An innovative pharmacology curriculum for medical students: promoting higher order cognition, learner-centered coaching, and constructive feedback through a social pedagogy framework | An innovative pharmacology curriculum for medical students: promoting higher order cognition, learner-centered coaching, and constructive feedback through a social pedagogy framework Abstract Background Ongoing developments in medical education recognize the move to curricula that support self-regulated learning proces... |
PMC12652146 | core_pubmed_pmc | Synergistic Effect Evaluation and Mechanism Investigation of Vitamin B6 and B12 in Models of Neuroinflammation | Synergistic Effect Evaluation and Mechanism Investigation of Vitamin B6 and B12 in Models of Neuroinflammation Abstract Abstract Neurological damage, a debilitating condition closely associated with chronic neuroinflammation, currently lacks disease-modifying treatments, with management limited to symptomatic relief. V... |
PMC10411801 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, and safety of prandial oral insulin (N11005) in healthy subjects | Pharmacokinetics, pharmacodynamics, and safety of prandial oral insulin (N11005) in healthy subjects Abstract Abstract Aims To verify whether the oral insulin N11005 is administered as a prandial insulin by assessing the pharmacokinetics (PK), pharmacodynamics (PD), and safety profiles of N11005 with a short-acting bio... |
PMC4561054 | core_pubmed_pmc | Evaluation of the Pharmacokinetics and Renal Excretion of Simeprevir in Subjects with Renal Impairment | Evaluation of the Pharmacokinetics and Renal Excretion of Simeprevir in Subjects with Renal Impairment Abstract Background Simeprevir is a N3/4 protease inhibitor approved for the treatment of hepatitis C virus (HCV) infection. HCV prevalence is higher in patients with chronic kidney disease compared with the general p... |
PMC8416858 | core_pubmed_pmc | Clinical Pharmacokinetics of Triazoles in Pediatric Patients | Clinical Pharmacokinetics of Triazoles in Pediatric Patients Abstract Abstract Triazoles represent an important class of antifungal drugs in the prophylaxis and treatment of invasive fungal disease in pediatric patients. Understanding the pharmacokinetics of triazoles in children is crucial to providing optimal care fo... |
PMC11297282 | core_pubmed_pmc | Evaluation of intra‐ and inter‐individual variations in plasma belimumab concentrations in adult patients with systemic lupus erythematosus | Evaluation of intra‐ and inter‐individual variations in plasma belimumab concentrations in adult patients with systemic lupus erythematosus Abstract Abstract In this study, plasma belimumab concentrations were measured over the course of treatment in systemic lupus erythematosus (SLE) patients on belimumab therapy, and... |
PMC12301248 | core_pubmed_pmc | Pharmacokinetic Profile of Isoniazid and Acetylator Status in Patients with Systemic Lupus Erythematosus: Implications for Tuberculosis Prevention Therapy in Indonesia | Pharmacokinetic Profile of Isoniazid and Acetylator Status in Patients with Systemic Lupus Erythematosus: Implications for Tuberculosis Prevention Therapy in Indonesia Abstract Introduction Systemic Lupus Erythematosus (SLE) is a chronic autoimmune inflammatory disease with a high risk of tuberculosis (TB) infection, e... |
PMC11579194 | core_pubmed_pmc | Generation of realistic virtual adult populations using a model-based copula approach | Generation of realistic virtual adult populations using a model-based copula approach Abstract Incorporating realistic sets of patient-associated covariates, i.e., virtual populations, in pharmacometric simulation workflows is essential to obtain realistic model predictions. Current covariate simulation strategies ofte... |
PMC11962376 | core_pubmed_pmc | Relationship between posaconazole concentrations and clinical outcomes in paediatric cancer and haematopoietic stem cell transplant recipients | Relationship between posaconazole concentrations and clinical outcomes in paediatric cancer and haematopoietic stem cell transplant recipients Abstract Abstract Background Posaconazole is used to prevent and treat invasive fungal infections (IFIs) in immunocompromised children, including those undergoing cancer treatme... |
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