id stringlengths 9 11 | source stringclasses 1
value | title stringlengths 15 560 | text stringlengths 2k 153k |
|---|---|---|---|
PMC10141594 | core_pubmed_pmc | Kinase-Modulated Bioluminescent Indicators Enable Noninvasive Imaging of Drug Activity in the Brain | Kinase-Modulated Bioluminescent Indicators Enable Noninvasive Imaging of Drug Activity in the Brain Abstract Aberrant kinase activity contributes to the pathogenesis of brain cancers, neurodegeneration, and neuropsychiatric diseases, but identifying kinase inhibitors that function in the brain is challenging. Drug leve... |
PMC9909725 | core_pubmed_pmc | Role of in vitro two-dimensional (2D) and three-dimensional (3D) cell culture systems for ADME-Tox screening in drug discovery and development: a comprehensive review | Role of in vitro two-dimensional (2D) and three-dimensional (3D) cell culture systems for ADME-Tox screening in drug discovery and development: a comprehensive review Abstract Drug discovery and development have become a very time-consuming and expensive process. Preclinical animal models have become the gold standard ... |
PMC6150296 | core_pubmed_pmc | Influence of Shenxiong Glucose Injection on the Activities of Six CYP Isozymes and Metabolism of Warfarin in Rats Assessed Using Probe Cocktail and Pharmacokinetic Approaches | Influence of Shenxiong Glucose Injection on the Activities of Six CYP Isozymes and Metabolism of Warfarin in Rats Assessed Using Probe Cocktail and Pharmacokinetic Approaches Abstract Abstract Shenxiong glucose injection (SGI), a traditional Chinese medicine (TCM) preparation, has been widely used for the treatment of ... |
PMC8060183 | core_pubmed_pmc | Improved numerical stability for the bounded integer model | Improved numerical stability for the bounded integer model Abstract Abstract This article highlights some numerical challenges when implementing the bounded integer model for composite score modeling and suggests an improved implementation. The improvement is based on an approximation of the logarithm of the error func... |
PMC8691714 | core_pubmed_pmc | Intentional Modulation of Ibrutinib Pharmacokinetics through CYP3A Inhibition | Intentional Modulation of Ibrutinib Pharmacokinetics through CYP3A Inhibition Abstract Ibrutinib (Imbruvica; PCI-32765) is an orally administered inhibitor of Bruton's tyrosine kinase that has transformed the treatment of B-cell malignancies. However, ibrutinib has very low oral bioavailability that contributes to sign... |
PMC10654271 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of Same-Knee Intra-Articular Injection of Corticosteroid and Lorecivivint Within 7 Days: An Open-Label, Randomized, Parallel-Arm Study | Safety, Tolerability, and Pharmacokinetics of Same-Knee Intra-Articular Injection of Corticosteroid and Lorecivivint Within 7 Days: An Open-Label, Randomized, Parallel-Arm Study Abstract Abstract Introduction Knee osteoarthritis (OA) is a common painful disorder. Intra-articular (IA) corticosteroid injections are frequ... |
PMC4917808 | core_pubmed_pmc | Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects | Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects Abstract Aims Free fatty acids (FFA) can act as direct signalling molecules through activation of several membrane‐bound G‐protein coupled receptors. The FFA2 receptor (known as GPR43) is activate... |
PMC3733800 | core_pubmed_pmc | Reticulocyte dynamic and hemoglobin variability in hemodialysis patients treated with Darbepoetin alfa and C.E.R.A.: a randomized controlled trial | Reticulocyte dynamic and hemoglobin variability in hemodialysis patients treated with Darbepoetin alfa and C.E.R.A.: a randomized controlled trial Abstract Background In a simulation based on a pharmacokinetic model we demonstrated that increasing the erythropoiesis stimulating agents (ESAs) half-life or shortening the... |
PMC10851633 | core_pubmed_pmc | Psychological and physiological effects of extended DMT | Psychological and physiological effects of extended DMT Abstract N,N-Dimethyltryptamine (DMT) is a serotonergic psychedelic that induces a rapid and transient altered state of consciousness when inhaled or injected via bolus administration. Its marked and novel subjective effects make DMT a powerful tool for the neuros... |
PMC4728823 | core_pubmed_pmc | Population pharmacokinetics and optimization of the dosing regimen of digoxin in adult patients | Population pharmacokinetics and optimization of the dosing regimen of digoxin in adult patients Abstract Background This study aimed to evaluate the population pharmacokinetics of digoxin in Japanese patients and establish a dosage regimen based on the pharmacokinetic data. Methods We analyzed 287 serum digoxin samples... |
PMC12263732 | core_pubmed_pmc | Pharmacokinetics of Binimetinib in Participants with Hepatic Impairment | Pharmacokinetics of Binimetinib in Participants with Hepatic Impairment Abstract Background and Objective Binimetinib is approved for multiple indications at a therapeutic dose of 45 mg twice a day (BID), in combination with encorafenib. A clinical hepatic impairment (HI) study was designed to evaluate the pharmacokine... |
PMC10056037 | core_pubmed_pmc | Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy | Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy Abstract Abstract To date, the ophthalmic application of liquid crystalline nanostructures (LCNs) has not been thoroughly reconnoitered, yet they have been extensively used. LCNs are primarily made up of glyceryl monooleate (GMO)... |
PMC7293536 | core_pubmed_pmc | Eudragit ® -S100 Coated PLGA Nanoparticles for Colon Targeting of Etoricoxib: Optimization and Pharmacokinetic Assessments in Healthy Human Volunteers | Eudragit ® -S100 Coated PLGA Nanoparticles for Colon Targeting of Etoricoxib: Optimization and Pharmacokinetic Assessments in Healthy Human Volunteers Abstract Aim Etoricoxib is a selective inhibitor of COX-2 enzyme. It is proposed as a potent anti-inflammatory drug intended for the control of irritable bowel syndrome.... |
PMC10511078 | core_pubmed_pmc | Peri-operative pharmacokinetics of cefazolin prophylaxis during valve replacement surgery | Peri-operative pharmacokinetics of cefazolin prophylaxis during valve replacement surgery Abstract Objective There is little prospective data to guide effective dosing for antibiotic prophylaxis during surgery requiring cardiopulmonary bypass (CPB). We aim to describe the effects of CPB on the population pharmacokineti... |
PMC4657463 | core_pubmed_pmc | An open-label clinical trial of the effects of age and gender on the pharmacodynamics, pharmacokinetics and safety of the ghrelin receptor agonist anamorelin | An open-label clinical trial of the effects of age and gender on the pharmacodynamics, pharmacokinetics and safety of the ghrelin receptor agonist anamorelin Abstract Purpose To assess the effect of age and gender on the pharmacokinetics (PK) of the ghrelin receptor agonist anamorelin. Methods Three demographic cohorts... |
PMC11606118 | core_pubmed_pmc | The first-in-class bispecific antibody IBI318 (LY3434172) targeting PD-1 and PD-L1 in patients with advanced tumors: a phase Ia/Ib study | The first-in-class bispecific antibody IBI318 (LY3434172) targeting PD-1 and PD-L1 in patients with advanced tumors: a phase Ia/Ib study Abstract Background There is an unmet clinical need to enhance the response rate and safety of anti-PD-1/PD-L1-based cancer immunotherapy (IO). Herein, we presented the clinical study... |
PMC7028061 | core_pubmed_pmc | Population Pharmacokinetics of Paliperidone Palmitate (Once‐Monthly Formulation) in Japanese, Korean, and Taiwanese Patients With Schizophrenia | Population Pharmacokinetics of Paliperidone Palmitate (Once‐Monthly Formulation) in Japanese, Korean, and Taiwanese Patients With Schizophrenia Abstract Abstract The paliperidone pharmacokinetics after intramuscular administration of once‐monthly paliperidone palmitate in Japanese patients were studied in 3 phase 1 stu... |
PMC11910153 | core_pubmed_pmc | A systematic review of fluralaner as a treatment for ectoparasitic infections in mammalian species | A systematic review of fluralaner as a treatment for ectoparasitic infections in mammalian species Abstract Fluralaner (Bravecto™) is a novel isoxazoline ectoparasiticide used for controlling ectoparasites of domestic mammals and is increasingly being used on wildlife. The aim of this systematic review was to evaluate ... |
PMC3619253 | core_pubmed_pmc | In vivo RAF signal transduction as a potential biomarker for sorafenib efficacy in patients with neuroendocrine tumours | In vivo RAF signal transduction as a potential biomarker for sorafenib efficacy in patients with neuroendocrine tumours Abstract Abstract Background: Targeted therapies elicit anticancer activity by exerting pharmacodynamic effects on specific molecular targets. Currently, there is limited use of pharmacodynamic assess... |
PMC5365648 | core_pubmed_pmc | Pharmacokinetics of the Novel Echinocandin CD101 in Multiple Animal Species | Pharmacokinetics of the Novel Echinocandin CD101 in Multiple Animal Species Abstract ABSTRACT CD101 is a novel semisynthetic echinocandin with antifungal activity against Candida and Aspergillus spp. The pharmacokinetics (PK) of CD101 administered intravenously to mice, rats, dogs, cynomolgus monkeys, and chimpanzees a... |
PMC6270787 | core_pubmed_pmc | Pharmacokinetics, Tissue Distribution, Excretion and Plasma Protein Binding Studies of Wogonin in Rats | Pharmacokinetics, Tissue Distribution, Excretion and Plasma Protein Binding Studies of Wogonin in Rats Abstract Abstract Wogonin is a natural anticancer candidate. The purpose of this study was to explore the pharmacokinetic profiles, tissue distribution, excretion and plasma protein binding of wogonin in Sprague—Dawle... |
PMC9197532 | core_pubmed_pmc | Model‐informed drug development of voxelotor in sickle cell disease: Exposure‐response analysis to support dosing and confirm mechanism of action | Model‐informed drug development of voxelotor in sickle cell disease: Exposure‐response analysis to support dosing and confirm mechanism of action Abstract Abstract Sickle cell disease (SCD) is characterized by the production of sickle hemoglobin (HbS), which when deoxygenated, polymerizes leading to red blood cell dama... |
PMC9781892 | core_pubmed_pmc | Impact of N-Linked Glycosylation on Therapeutic Proteins | Impact of N-Linked Glycosylation on Therapeutic Proteins Abstract Therapeutic proteins have unique advantages over small-molecule drugs in the treatment of various diseases, such as higher target specificity, stronger pharmacological efficacy and relatively low side effects. These advantages make them increasingly valu... |
PMC12816373 | core_pubmed_pmc | Progress of coproporphyrin as an endogenous biomarker for transporter-mediated drug-drug interactions | Progress of coproporphyrin as an endogenous biomarker for transporter-mediated drug-drug interactions Abstract Abstract Drug-drug interactions (DDIs) can present challenges in both the development of new drugs and clinical practice. Transporters play a pivotal role in the pharmacokinetics, safety, and efficacy of combi... |
PMC11875335 | core_pubmed_pmc | Pharmacometabolomics in TB meningitis—Understanding the pharmacokinetic, metabolic, and immune factors associated with anti-TB drug concentrations in cerebrospinal fluid | Pharmacometabolomics in TB meningitis—Understanding the pharmacokinetic, metabolic, and immune factors associated with anti-TB drug concentrations in cerebrospinal fluid Abstract Abstract Poor penetration of many anti-tuberculosis (TB) antibiotics into the central nervous system (CNS) is thought to be a major driver of... |
PMC12494972 | core_pubmed_pmc | Exploring Nigella Sativa’s medicinal capacity against skin cancer pathways using network pharmacology and molecular docking | Exploring Nigella Sativa’s medicinal capacity against skin cancer pathways using network pharmacology and molecular docking Abstract Skin cancer is a growing global health concern, marked by high incidence and significant mortality, particularly in aggressive melanoma subtypes. In this study, we employed an integrative... |
PMC12057361 | core_pubmed_pmc | Bedaquiline does not enhance a clofazimine-azithromycin-ethambutol regimen against Mycobacterium avium in the hollow-fiber system | Bedaquiline does not enhance a clofazimine-azithromycin-ethambutol regimen against Mycobacterium avium in the hollow-fiber system Abstract ABSTRACT Bedaquiline has been proposed as a second-line drug to treat pulmonary disease caused by Mycobacterium avium complex. Based on in vitro synergy and interactions, a logical ... |
PMC11808267 | core_pubmed_pmc | Anxiolytic Efficacy of Indirubin: In Vivo Approach Along with Receptor Binding Profiling and Molecular Interaction with GABAergic Pathways | Anxiolytic Efficacy of Indirubin: In Vivo Approach Along with Receptor Binding Profiling and Molecular Interaction with GABAergic Pathways Abstract Abstract Anxiety is a natural response to stress, characterized by feelings of worry, fear, or unease. The current research was conducted to investigate the anxiolytic effe... |
PMC8035703 | core_pubmed_pmc | Effect of Synchronous Versus Sequential Regimens on the Pharmacokinetics and Biodistribution of Regorafenib with Irradiation | Effect of Synchronous Versus Sequential Regimens on the Pharmacokinetics and Biodistribution of Regorafenib with Irradiation Abstract Abstract This study was performed to evaluate the interaction between conventional or high-dose radiotherapy (RT) and the pharmacokinetics (PK) of regorafenib in concurrent or sequential... |
PMC4989998 | core_pubmed_pmc | The pharmacokinetics and toxicity of morning vs. evening tobramycin dosing for pulmonary exacerbations of cystic fibrosis: A randomised comparison | The pharmacokinetics and toxicity of morning vs. evening tobramycin dosing for pulmonary exacerbations of cystic fibrosis: A randomised comparison Abstract Background Circadian variation in renal toxicity of aminoglycosides has been demonstrated in animal and human studies. People with CF are frequently prescribed amin... |
PMC11242460 | core_pubmed_pmc | Low-dose aspirin for the prevention of atherosclerotic cardiovascular disease | Low-dose aspirin for the prevention of atherosclerotic cardiovascular disease Abstract Abstract During the past 30 years, several developments have occurred in the antiplatelet field, including the role of aspirin in primary prevention of atherosclerotic cardiovascular disease. There have been several attempts to devel... |
PMC6790397 | core_pubmed_pmc | Association Between Estimated Pharmacokinetic/Pharmacodynamic Predictions of Efficacy and Observed Clinical Outcomes in Obese and Nonobese Patients With Enterobacteriaceae Bloodstream Infections | Association Between Estimated Pharmacokinetic/Pharmacodynamic Predictions of Efficacy and Observed Clinical Outcomes in Obese and Nonobese Patients With Enterobacteriaceae Bloodstream Infections Abstract Abstract Background Evidence on pharmacokinetic/pharmacodynamic (PK/PD) alterations and clinical outcomes in obese p... |
PMC6834656 | core_pubmed_pmc | From Petri Dish to Patient: Bioavailability Estimation and Mechanism of Action for Antimicrobial and Immunomodulatory Natural Products | From Petri Dish to Patient: Bioavailability Estimation and Mechanism of Action for Antimicrobial and Immunomodulatory Natural Products Abstract The new era of multidrug resistance of pathogens against frontline antibiotics has compromised the immense therapeutic gains of the ‘golden age,’ stimulating a resurgence in an... |
PMC9035351 | core_pubmed_pmc | Voclosporin: a novel calcineurin inhibitor with no impact on mycophenolic acid levels in patients with SLE | Voclosporin: a novel calcineurin inhibitor with no impact on mycophenolic acid levels in patients with SLE Abstract Abstract Background An open-label phase 1 study was conducted to evaluate the effect of voclosporin following dosing with mycophenolate mofetil (MMF) on blood levels of mycophenolic acid (MPA, the active ... |
PMC12258420 | core_pubmed_pmc | Multivariate Adjustments for Average Equivalence Testing | Multivariate Adjustments for Average Equivalence Testing Abstract ABSTRACT Multivariate (average) equivalence testing is widely used to assess whether the means of two conditions of interest are “equivalent” for different outcomes simultaneously. In pharmacological research for example, many regulatory agencies require... |
PMC5397562 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of Benralizumab in Healthy Volunteers and Patients With Asthma | Population Pharmacokinetics and Pharmacodynamics of Benralizumab in Healthy Volunteers and Patients With Asthma Abstract Benralizumab is a humanized, afucosylated, anti‐interleukin‐5 receptor α, immunoglobulin G (IgG) 1 κ monoclonal antibody. We developed a population pharmacokinetic (PK)/pharmacodynamic (PD) model for... |
PMC2952487 | core_pubmed_pmc | Resistance and the management of complicated skin and skin structure infections: the role of ceftobiprole | Resistance and the management of complicated skin and skin structure infections: the role of ceftobiprole Abstract Antimicrobial resistant bacteria are an increasing concern due to the resulting increase in morbidity, mortality, and health-care costs associated with the administration of inadequate or delayed antimicro... |
PMC4835124 | core_pubmed_pmc | Pharmacokinetics of the evogliptin/metformin extended-release (5/1,000 mg) fixed-dose combination formulation compared to the corresponding loose combination, and food effect in healthy subjects | Pharmacokinetics of the evogliptin/metformin extended-release (5/1,000 mg) fixed-dose combination formulation compared to the corresponding loose combination, and food effect in healthy subjects Abstract A new fixed-dose combination formulation of evogliptin 5 mg and metformin extended-release (XR) 1,000 mg (FDC_EVO5/M... |
PMC12072234 | core_pubmed_pmc | Toward Precision Dosing of Lamotrigine During Pregnancy: Physiologically Based Pharmacokinetic Modeling and Simulation | Toward Precision Dosing of Lamotrigine During Pregnancy: Physiologically Based Pharmacokinetic Modeling and Simulation Abstract ABSTRACT Lamotrigine is a commonly used anti‐seizure medication in pregnant women. However, its pharmacokinetics (PK) during pregnancy markedly change, increasing the frequency of seizures and... |
PMC3674326 | core_pubmed_pmc | White Paper: Landscape on Technical and Conceptual Requirements and Competence Framework in Drug/Disease Modeling and Simulation | White Paper: Landscape on Technical and Conceptual Requirements and Competence Framework in Drug/Disease Modeling and Simulation Abstract Pharmaceutical sciences experts and regulators acknowledge that pharmaceutical development as well as drug usage requires more than scientific advancements to cope with current attri... |
PMC12592087 | core_pubmed_pmc | Therapeutic challenges in managing Stenotrophomonas maltophilia bloodstream infection in a renal dysfunction patient: a case study and literature review | Therapeutic challenges in managing Stenotrophomonas maltophilia bloodstream infection in a renal dysfunction patient: a case study and literature review Abstract Background The overall infection rate of Stenotrophomonas maltophilia has markedly increased over the past two decades, with its bloodstream infections being ... |
PMC12435493 | core_pubmed_pmc | Safety, Pharmacokinetics, and Pharmacodynamics of BI 1595043, a Selective Vanin Inhibitor, in Phase 1 Clinical Trials Involving Healthy Volunteers | Safety, Pharmacokinetics, and Pharmacodynamics of BI 1595043, a Selective Vanin Inhibitor, in Phase 1 Clinical Trials Involving Healthy Volunteers Abstract ABSTRACT BI 1595043 is an oral vanin‐1 and vanin‐2 inhibitor, which demonstrated promising effects on epithelial cell protection and reduction of inflammatory media... |
PMC12767178 | core_pubmed_pmc | Engineering a drug-inducible pyroptosis platform enables precise tumor suppression in colorectal cancer | Engineering a drug-inducible pyroptosis platform enables precise tumor suppression in colorectal cancer Abstract Colorectal cancer remains a leading cause of cancer-related mortality, with long-term survival rates hindered by chemoresistance and an immunosuppressive tumor microenvironment. Gene-based therapies offer hi... |
PMC8596620 | core_pubmed_pmc | Population pharmacokinetics and genetics of oral meltdose tacrolimus (Envarsus) in stable adult liver transplant recipients | Population pharmacokinetics and genetics of oral meltdose tacrolimus (Envarsus) in stable adult liver transplant recipients Abstract Aims Meltdose tacrolimus (Envarsus) is marketed as a formulation with a more consistent exposure. Due to the narrow therapeutic window, therapeutic drug monitoring is essential to maintai... |
PMC8246536 | core_pubmed_pmc | Dosing of factor VIII concentrate by ideal body weight is more accurate in overweight and obese haemophilia A patients | Dosing of factor VIII concentrate by ideal body weight is more accurate in overweight and obese haemophilia A patients Abstract Aims Under‐ and, especially, overdosing of replacement therapy in haemophilia A patients may be prevented by application of other morphometric variables than body weight (BW) to dose factor VI... |
PMC12886916 | core_pubmed_pmc | A one compartment model to assess skin lightening rate of cosmetic formulae in UV induced clinical studies | A one compartment model to assess skin lightening rate of cosmetic formulae in UV induced clinical studies Abstract Abstract Ultraviolet-induced skin darkening is often used as a clinical model to assess the efficacy of active ingredients aimed at modulating skin pigmentation ; targeting pigmentary skin disorders. Stud... |
PMC6037268 | core_pubmed_pmc | Pharmacokinetics of placental protein 13 after intravenous and subcutaneous administration in rabbits | Pharmacokinetics of placental protein 13 after intravenous and subcutaneous administration in rabbits Abstract Introduction Human placental protein 13 (PP13) is a galectin predominantly expressed by the placenta. Low serum concentrations of PP13 in early pregnancy indicate a higher risk of developing preeclampsia. Meth... |
PMC10202413 | core_pubmed_pmc | The First-in-Human Whole-Body Dynamic Pharmacokinetics Study of Aptamer | The First-in-Human Whole-Body Dynamic Pharmacokinetics Study of Aptamer Abstract Serving as targeting ligands, aptamers have shown promise in precision medicine. However, the lack of knowledge of the biosafety and metabolism patterns in the human body largely impeded aptamers’ clinical translation. To bridge this gap, ... |
PMC9636542 | core_pubmed_pmc | Acute liver failure associated with lamotrigine in children with epilepsy: A report of two cases and thoughts on pharmacogenomics | Acute liver failure associated with lamotrigine in children with epilepsy: A report of two cases and thoughts on pharmacogenomics Abstract Highlights • We describe two cases of pediatric acute liver failure after LTG administration in children with epilepsy. • Higher dose, rapid titration, and in combination with valpr... |
PMC5612971 | core_pubmed_pmc | Comparative population pharmacokinetics and absolute oral bioavailability of COX-2 selective inhibitors celecoxib, mavacoxib and meloxicam in cockatiels ( Nymphicus hollandicus ) | Comparative population pharmacokinetics and absolute oral bioavailability of COX-2 selective inhibitors celecoxib, mavacoxib and meloxicam in cockatiels ( Nymphicus hollandicus ) Abstract Selective COX-2 inhibitors are non-steroidal anti-inflammatory drugs which directly target cyclooxygenase-2 (COX-2), an enzyme mainl... |
PMC8602176 | core_pubmed_pmc | Novel Quantification of Extracellular Vesicles with Unaltered Surface Membranes Using an Internalized Oligonucleotide Tracer and Applied Pharmacokinetic Multiple Compartment Modeling | Novel Quantification of Extracellular Vesicles with Unaltered Surface Membranes Using an Internalized Oligonucleotide Tracer and Applied Pharmacokinetic Multiple Compartment Modeling Abstract Abstract Purpose We developed an accessible method for labeling small extracellular vesicles (sEVs) without disrupting endogenou... |
PMC12007268 | core_pubmed_pmc | Engineering FcRn binding kinetics dramatically extends antibody serum half-life and enhances therapeutic potential | Engineering FcRn binding kinetics dramatically extends antibody serum half-life and enhances therapeutic potential Abstract Abstract Background Optimizing the IgG Fc domain for neonatal Fc receptor (FcRn) binding is crucial for enhancing antibody pharmacokinetics. The prolonged serum half-life of IgG antibody is govern... |
PMC12084251 | core_pubmed_pmc | Molecular pathways of ketamine: A systematic review of immediate and sustained effects on PTSD | Molecular pathways of ketamine: A systematic review of immediate and sustained effects on PTSD Abstract Abstract Rationale Existing studies predominantly focus on the molecular and neurobiological mechanisms underlying Ketamine’s acute treatment effects on post-traumatic stress disorder (PTSD). This emphasis has largel... |
PMC5028982 | core_pubmed_pmc | Failure of dihydroartemisinin plus piperaquine treatment of falciparum malaria by under-dosing in an overweight patient | Failure of dihydroartemisinin plus piperaquine treatment of falciparum malaria by under-dosing in an overweight patient Abstract Background Artemisinin-based combination therapy (ACT) introduced in the mid-1990s has been recommended since 2005 by the World Health Organization as first-line treatment against Plasmodium ... |
PMC6161292 | core_pubmed_pmc | A Sensitive Liquid Chromatography-Tandem Mass Spectrometry Method for the Determination of Nimbolide in Mouse Serum: Application to a Preclinical Pharmacokinetics Study | A Sensitive Liquid Chromatography-Tandem Mass Spectrometry Method for the Determination of Nimbolide in Mouse Serum: Application to a Preclinical Pharmacokinetics Study Abstract Abstract A sensitive and robust liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed and validated for the determin... |
PMC10347058 | core_pubmed_pmc | Ribociclib Hybrid Lipid–Polymer Nanoparticle Preparation and Characterization for Cancer Treatment | Ribociclib Hybrid Lipid–Polymer Nanoparticle Preparation and Characterization for Cancer Treatment Abstract Abstract Ribociclib is a newly approved orally administered drug for breast cancer. This study aimed to prepare, characterize, and evaluate hybrid lipid–polymer nanoparticles (PLNs) of ribociclib to enhance its i... |
PMC12823318 | core_pubmed_pmc | Pharmacometric‐Based Evaluation of Salmeterol and Its Metabolite α‐Hydroxysalmeterol in Plasma and Urine: Practical Implications for Doping Control | Pharmacometric‐Based Evaluation of Salmeterol and Its Metabolite α‐Hydroxysalmeterol in Plasma and Urine: Practical Implications for Doping Control Abstract ABSTRACT Salmeterol is a commonly used β 2 ‐agonist included on the List of Prohibited Substances and Methods published by the World Anti‐Doping Agency (WADA). We ... |
PMC6658826 | core_pubmed_pmc | Bioequivalence Study of 100-mg Cilostazol Tablets in Healthy Thai Adult Volunteers | Bioequivalence Study of 100-mg Cilostazol Tablets in Healthy Thai Adult Volunteers Abstract Highlights • Cilostazol is used in practice for the management of peripheral arterial disease. • A generic formulation of cilostazol was compared (C max , AUC, T max ) with the brand-name product. • No statistically significant ... |
PMC10442685 | core_pubmed_pmc | Simultaneous Assessment of Serum Levels and Pharmacologic Effects of Cannabinoids on Endocannabinoids and N -Acylethanolamines by Liquid Chromatography–Tandem Mass Spectrometry | Simultaneous Assessment of Serum Levels and Pharmacologic Effects of Cannabinoids on Endocannabinoids and N -Acylethanolamines by Liquid Chromatography–Tandem Mass Spectrometry Abstract Abstract Introduction: The primary compounds of Cannabis sativa , delta-9-tetrahydrocannabinol (Δ 9 -THC) and cannabidiol (CBD), infli... |
PMC9297990 | core_pubmed_pmc | Prediction of Moxifloxacin Concentrations in Tuberculosis Patient Populations by Physiologically Based Pharmacokinetic Modeling | Prediction of Moxifloxacin Concentrations in Tuberculosis Patient Populations by Physiologically Based Pharmacokinetic Modeling Abstract Abstract Moxifloxacin has an important role in the treatment of tuberculosis (TB). Unfortunately, coadministration with the cornerstone TB drug rifampicin results in suboptimal plasma... |
PMC5732638 | core_pubmed_pmc | Concomitant medication polypharmacy, interactions and imperfect adherence are common in Australian adults on suppressive antiretroviral therapy | Concomitant medication polypharmacy, interactions and imperfect adherence are common in Australian adults on suppressive antiretroviral therapy Abstract Abstract Objectives: We quantified concomitant medication polypharmacy, pharmacokinetic and pharmacodynamic interactions, adverse effects and adherence in Australian a... |
PMC10546659 | core_pubmed_pmc | Critical appraisal beyond clinical guidelines for intraabdominal candidiasis | Critical appraisal beyond clinical guidelines for intraabdominal candidiasis Abstract Background Regardless of the available antifungals, intraabdominal candidiasis (IAC) mortality continues to be high and represents a challenge for clinicians. Main body This opinion paper discusses alternative antifungal options for t... |
PMC3491670 | core_pubmed_pmc | Systematic review: cardiovascular safety profile of 5-HT 4 agonists developed for gastrointestinal disorders | Systematic review: cardiovascular safety profile of 5-HT 4 agonists developed for gastrointestinal disorders Abstract Summary Background The nonselective 5-HT 4 receptor agonists, cisapride and tegaserod have been associated with cardiovascular adverse events (AEs). Aim To perform a systematic review of the safety prof... |
PMC9743388 | core_pubmed_pmc | Study protocol for controlled human infection for penicillin G against Streptococcus pyogenes : a double-blinded, placebo-controlled, randomised trial to determine the minimum concentration required to prevent experimental pharyngitis (the CHIPS trial) | Study protocol for controlled human infection for penicillin G against Streptococcus pyogenes : a double-blinded, placebo-controlled, randomised trial to determine the minimum concentration required to prevent experimental pharyngitis (the CHIPS trial) Abstract Abstract Introduction Regular intramuscular benzathine pen... |
PMC9561237 | core_pubmed_pmc | Atovaquone for treatment of COVID-19: A prospective randomized, double-blind, placebo-controlled clinical trial | Atovaquone for treatment of COVID-19: A prospective randomized, double-blind, placebo-controlled clinical trial Abstract Abstract Background: An in silico screen was performed to identify FDA approved drugs that inhibit SARS-CoV-2 main protease (M pro ), followed by in vitro viral replication assays, and in vivo pharma... |
PMC10345482 | core_pubmed_pmc | Modeling the Impact of a Highly Potent Plasmodium falciparum Transmission-Blocking Monoclonal Antibody in Areas of Seasonal Malaria Transmission | Modeling the Impact of a Highly Potent Plasmodium falciparum Transmission-Blocking Monoclonal Antibody in Areas of Seasonal Malaria Transmission Abstract Abstract Transmission-blocking interventions can play an important role in combating malaria worldwide. Recently, a highly potent Plasmodium falciparum transmission-b... |
PMC11025614 | core_pubmed_pmc | Coadministration of fluconazole to boost subtherapeutic sirolimus concentrations: A case report | Coadministration of fluconazole to boost subtherapeutic sirolimus concentrations: A case report Abstract Abstract Individual sirolimus whole blood concentrations are highly variable, critically influenced by the concomitant use of cytochrome P450 (CYP) 3A inducers or inhibitors, and also modulated by food. Therapeutic ... |
PMC3717151 | core_pubmed_pmc | Population Pharmacokinetics of Dexmedetomidine in Critically Ill Patients | Population Pharmacokinetics of Dexmedetomidine in Critically Ill Patients Abstract Background and Objectives Although the pharmacokinetics of dexmedetomidine in healthy volunteers have been studied, there are limited data about the pharmacokinetics of long-term administration of dexmedetomidine in critically ill patien... |
PMC8004874 | core_pubmed_pmc | The Evolving Role of Microsampling in Therapeutic Drug Monitoring of Monoclonal Antibodies in Inflammatory Diseases | The Evolving Role of Microsampling in Therapeutic Drug Monitoring of Monoclonal Antibodies in Inflammatory Diseases Abstract Abstract Monoclonal antibodies (mAbs) have been extensively developed over the past few years, for the treatment of various inflammatory diseases. They are large molecules characterized by comple... |
PMC8053786 | core_pubmed_pmc | An Ensemble Model for Prediction of Vancomycin Trough Concentrations in Pediatric Patients | An Ensemble Model for Prediction of Vancomycin Trough Concentrations in Pediatric Patients Abstract Abstract Purpose This study aimed to establish an optimal model to predict vancomycin trough concentrations by using machine learning. Patients and Methods We enrolled 407 pediatric patients (age < 18 years) who received... |
PMC6838174 | core_pubmed_pmc | Gut Microbiota-Mediated Drug-Drug Interaction between Amoxicillin and Aspirin | Gut Microbiota-Mediated Drug-Drug Interaction between Amoxicillin and Aspirin Abstract The effects of antibiotics on the intestinal flora can create potential drug-drug interactions. The combination of amoxicillin and aspirin is high and there is a high probability of interaction. We used 16S rRNA, incubation experimen... |
PMC8280020 | core_pubmed_pmc | Phase 1 cohort expansion study of LY3023414, a dual PI3K/mTOR inhibitor, in patients with advanced mesothelioma | Phase 1 cohort expansion study of LY3023414, a dual PI3K/mTOR inhibitor, in patients with advanced mesothelioma Abstract Summary BACKGROUND LY3023414 is a selective, ATP competitive inhibitor of class I PI3K isoforms, mTORC1/2 and DNA-PK. A Phase 1 dose escalation, 200 mg twice daily (BID) of LY3023414 was the determin... |
PMC12708835 | core_pubmed_pmc | Acute effects of MDMA, MDA, lysine-MDMA, and lysine-MDA in a randomized, double-blind, placebo-controlled, crossover trial in healthy participants | Acute effects of MDMA, MDA, lysine-MDMA, and lysine-MDA in a randomized, double-blind, placebo-controlled, crossover trial in healthy participants Abstract 3,4-Methylenedioxymethamphetamine (MDMA) is used recreationally, as a research tool, and in MDMA-assisted therapy in patients with posttraumatic stress disorder. 3,... |
PMC12065284 | core_pubmed_pmc | A randomized, open-label, multi-center, active-controlled phase II study comparing abiraterone acetate tablets (II), an improved formulation, versus originator abiraterone acetate in patients with metastatic castration-resistant prostate cancer | A randomized, open-label, multi-center, active-controlled phase II study comparing abiraterone acetate tablets (II), an improved formulation, versus originator abiraterone acetate in patients with metastatic castration-resistant prostate cancer Abstract Background Abiraterone is a 17α-hydroxylase/C17-20 lyase inhibitor... |
PMC7955945 | core_pubmed_pmc | Evaluation of flavonoids as 2019-nCoV cell entry inhibitor through molecular docking and pharmacological analysis | Evaluation of flavonoids as 2019-nCoV cell entry inhibitor through molecular docking and pharmacological analysis Abstract Abstract The outbreak of Coronavirus Disease 2019 (COVID-19) has been declared as a Public Health Emergency of International Concern (PHEIC) by the World Health Organization (WHO), which is being r... |
PMC11903593 | core_pubmed_pmc | RETRACTED ARTICLE: New recommendations for reversal of high-dose methotrexate cytotoxicity with folinic acid | RETRACTED ARTICLE: New recommendations for reversal of high-dose methotrexate cytotoxicity with folinic acid Abstract Abstract Purpose Folinic acid (FA) rescue protocols to counter the adverse effects of high-dose methotrexate (HDMTX) vary widely, and the risk of over-rescue and potential adverse effects of excessive F... |
PMC8657982 | core_pubmed_pmc | Overlap and Specificity in the Substrate Spectra of Human Monoamine Transporters and Organic Cation Transporters 1, 2, and 3 | Overlap and Specificity in the Substrate Spectra of Human Monoamine Transporters and Organic Cation Transporters 1, 2, and 3 Abstract Abstract Human monoamine transporters (MATs) are cation transporters critically involved in neuronal signal transmission. While inhibitors of MATs have been intensively studied, their su... |
PMC5461651 | core_pubmed_pmc | Absorption, distribution, metabolism, and excretion of [ 14 C]‐dasotraline in humans | Absorption, distribution, metabolism, and excretion of [ 14 C]‐dasotraline in humans Abstract Abstract Dasotraline is a dopamine and norepinephrine reuptake inhibitor, and the early clinical trials show a slow absorption and long elimination half‐life. To investigate the absorption, distribution, metabolism, and excret... |
PMC6113880 | core_pubmed_pmc | High dose oral and intravenous rifampicin for improved survival from adult tuberculous meningitis: a phase II open-label randomised controlled trial (the RifT study) | High dose oral and intravenous rifampicin for improved survival from adult tuberculous meningitis: a phase II open-label randomised controlled trial (the RifT study) Abstract Abstract Background : Tuberculous meningitis (TBM) has 44% (95%CI 35-52%) in-hospital mortality with standard therapy in Uganda. Rifampicin, the ... |
PMC5712048 | core_pubmed_pmc | Dataset for Phase I randomized clinical trial for safety and tolerability of GET 73 in single and repeated ascending doses including preliminary pharmacokinetic parameters | Dataset for Phase I randomized clinical trial for safety and tolerability of GET 73 in single and repeated ascending doses including preliminary pharmacokinetic parameters Abstract The data in this article outline the methods used for the administration of GET 73 in the first time-in-human manuscript entitled “Phase I ... |
PMC10293504 | core_pubmed_pmc | A Phase I Study to Investigate the Safety, Tolerability and Pharmacokinetics of Napabucasin Combined with Sorafenib in Japanese Patients with Unresectable Hepatocellular Carcinoma | A Phase I Study to Investigate the Safety, Tolerability and Pharmacokinetics of Napabucasin Combined with Sorafenib in Japanese Patients with Unresectable Hepatocellular Carcinoma Abstract Background and Objective For patients with advanced hepatocellular carcinoma (HCC), the standard of care for many years has been so... |
PMC9926068 | core_pubmed_pmc | Selective Inhibition of the MK2 Pathway: Data From a Phase IIa Randomized Clinical Trial in Rheumatoid Arthritis | Selective Inhibition of the MK2 Pathway: Data From a Phase IIa Randomized Clinical Trial in Rheumatoid Arthritis Abstract Objective The study objective was to evaluate the safety, tolerability, pharmacodynamics, and preliminary efficacy of ATI‐450 with methotrexate in patients with rheumatoid arthritis (RA). Methods A ... |
PMC7534724 | core_pubmed_pmc | Randomised multicentre clinical trial to evaluate voriconazole pre-emptive genotyping strategy in patients with risk of aspergillosis: vorigenipharm study protocol | Randomised multicentre clinical trial to evaluate voriconazole pre-emptive genotyping strategy in patients with risk of aspergillosis: vorigenipharm study protocol Abstract Abstract Introduction Invasive aspergillosis is the most important cause of morbidity and mortality in patients with haematological diseases. At pr... |
PMC4909763 | core_pubmed_pmc | Transient Expression of Tetrameric Recombinant Human Butyrylcholinesterase in Nicotiana benthamiana | Transient Expression of Tetrameric Recombinant Human Butyrylcholinesterase in Nicotiana benthamiana Abstract To optimize the expression, extraction and purification of plant-derived tetrameric recombinant human butyrylcholinesterase (prBChE), we describe the development and use of plant viral amplicon-based gene expres... |
PMC5618418 | core_pubmed_pmc | Pharmacokinetics of Jaspine B and Enhancement of Intestinal Absorption of Jaspine B in the Presence of Bile Acid in Rats | Pharmacokinetics of Jaspine B and Enhancement of Intestinal Absorption of Jaspine B in the Presence of Bile Acid in Rats Abstract We aimed to investigate the pharmacokinetics and the underlying mechanisms of the intestinal absorption, distribution, metabolism, and excretion of Jaspine B in rats. The oral bioavailabilit... |
PMC10121149 | core_pubmed_pmc | Efficacy of cefiderocol- vs colistin-containing regimen for treatment of bacteraemic ventilator-associated pneumonia caused by carbapenem-resistant Acinetobacter baumannii in patients with COVID-19 | Efficacy of cefiderocol- vs colistin-containing regimen for treatment of bacteraemic ventilator-associated pneumonia caused by carbapenem-resistant Acinetobacter baumannii in patients with COVID-19 Abstract Abstract Introduction Ventilator-associated pneumonia (VAP) caused by carbapenem-resistant Acinetobacter baumanni... |
PMC10537372 | core_pubmed_pmc | Nanomaterial-Based Drug Delivery Systems for Pain Treatment and Relief: From the Delivery of a Single Drug to Co-Delivery of Multiple Therapeutics | Nanomaterial-Based Drug Delivery Systems for Pain Treatment and Relief: From the Delivery of a Single Drug to Co-Delivery of Multiple Therapeutics Abstract Abstract The use of nanomaterials in drug delivery systems for pain treatment is becoming increasingly common. This review aims to summarize how nanomaterial-based ... |
PMC9576902 | core_pubmed_pmc | Farnesoid X receptor agonist tropifexor attenuates cholestasis in a randomised trial in patients with primary biliary cholangitis | Farnesoid X receptor agonist tropifexor attenuates cholestasis in a randomised trial in patients with primary biliary cholangitis Abstract Background & Aims The safety, tolerability, and efficacy of the non-bile acid farnesoid X receptor agonist tropifexor were evaluated in a phase II, double-blind, placebo-controlled ... |
PMC4809455 | core_pubmed_pmc | PBPK-Based Probabilistic Risk Assessment for Total Chlorotriazines in Drinking Water | PBPK-Based Probabilistic Risk Assessment for Total Chlorotriazines in Drinking Water Abstract Abstract The risk of human exposure to total chlorotriazines (TCT) in drinking water was evaluated using a physiologically based pharmacokinetic (PBPK) model. Daily TCT (atrazine, deethylatrazine, deisopropylatrazine, and diam... |
PMC12354894 | core_pubmed_pmc | Novel environmental and sustainable approach for concurrent assay of antineoplastics in VMP regimen with a comprehensive Pharmacokinetic study | Novel environmental and sustainable approach for concurrent assay of antineoplastics in VMP regimen with a comprehensive Pharmacokinetic study Abstract Abstract Multiple myeloma (MM) is a blood cancer that, unfortunately, has a high morbidity and mortality rate. The VMP regimen, which includes bortezomib (BOR), melphal... |
PMC12944364 | core_pubmed_pmc | Dried Blood Spot for CXCL-10 and Tacrolimus: Integrated Non-Invasive Monitoring to Guide Personalized Treatment in Adult Kidney Transplant Recipients | Dried Blood Spot for CXCL-10 and Tacrolimus: Integrated Non-Invasive Monitoring to Guide Personalized Treatment in Adult Kidney Transplant Recipients Abstract Background/objectives: Kidney transplant recipients require lifelong immunosuppression and monitoring to prevent rejection, infection, and graft dysfunction. Cur... |
PMC5563346 | core_pubmed_pmc | Remarkable Pharmacokinetics of Monoclonal Antibodies: A Quest for an Explanation | Remarkable Pharmacokinetics of Monoclonal Antibodies: A Quest for an Explanation Abstract Monoclonal antibodies (MAbs) usually display slow and limited distribution with combined linear and non-linear elimination mechanisms. While studying individual pharmacokinetic profiles, it was noticed that MAb plasma concentratio... |
PMC5616206 | core_pubmed_pmc | Toxicological evaluation and metabolism of two N -alkyl benzamide umami flavour compounds: N -(heptan-4-yl)benzo[d][1,3]dioxole-5-carboxamide and ( R )- N -(1-methoxy-4-methylpentan-2-yl)-3,4-dimethylbenzamide | Toxicological evaluation and metabolism of two N -alkyl benzamide umami flavour compounds: N -(heptan-4-yl)benzo[d][1,3]dioxole-5-carboxamide and ( R )- N -(1-methoxy-4-methylpentan-2-yl)-3,4-dimethylbenzamide Abstract Abstract Toxicological evaluations of two N -alkyl benzamide umami flavour compounds, N -(heptan-4-yl... |
PMC11542112 | core_pubmed_pmc | SCALA: a randomized phase I trial comparing subcutaneous and intravenous alemtuzumab in patients with progressive multiple sclerosis | SCALA: a randomized phase I trial comparing subcutaneous and intravenous alemtuzumab in patients with progressive multiple sclerosis Abstract Background: Alemtuzumab is administered intravenously (IV) for relapsing-remitting multiple sclerosis (RRMS), with limited studies of subcutaneous (SC) treatment. Objectives: We ... |
PMC6851657 | core_pubmed_pmc | Prediction of the Impact of Cytochrome P450 2C9 Genotypes on the Drug–Drug Interaction Potential of Siponimod With Physiologically‐Based Pharmacokinetic Modeling: A Comprehensive Approach for Drug Label Recommendations | Prediction of the Impact of Cytochrome P450 2C9 Genotypes on the Drug–Drug Interaction Potential of Siponimod With Physiologically‐Based Pharmacokinetic Modeling: A Comprehensive Approach for Drug Label Recommendations Abstract We predicted the drug–drug interaction ( DDI ) potential of siponimod in presence of cytochr... |
PMC12888238 | core_pubmed_pmc | Proteolysis-targeting Chimera efficacy prediction using a deep-learning–QSP model | Proteolysis-targeting Chimera efficacy prediction using a deep-learning–QSP model Abstract Abstract This study presents an integrated computational modeling framework combining deep learning and Quantitative Systems Pharmacology (QSP) to predict the efficacy of PROTAC (PROteolysis Targeting Chimera) molecules. PROTACs ... |
PMC9699427 | core_pubmed_pmc | Structure-Based Discovery and Characterization of a Preclinical Drug Candidate for the Treatment of HIV-1 Infection | Structure-Based Discovery and Characterization of a Preclinical Drug Candidate for the Treatment of HIV-1 Infection Abstract HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) area key component of the current HIV-1 combination drug regimens. Although they exhibit potent anti-HIV-1 activity and modest toxic... |
PMC11254595 | core_pubmed_pmc | The mysteries of pharmacokinetics and in vivo metabolism of Oroxylum indicum (L.) Kurz: A new perspective from MSOP method | The mysteries of pharmacokinetics and in vivo metabolism of Oroxylum indicum (L.) Kurz: A new perspective from MSOP method Abstract The pharmacological effects of flavonoids in Oroxylum indicum (L.) Kurz against inflammation, bacterial, and oxidation have been well-documented. Additionally, it is commonly consumed as t... |
PMC8602162 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Rosuvastatin to Predict Transporter-Mediated Drug-Drug Interactions | Physiologically Based Pharmacokinetic Modeling of Rosuvastatin to Predict Transporter-Mediated Drug-Drug Interactions Abstract Abstract Purpose To build a physiologically based pharmacokinetic (PBPK) model of the clinical OATP1B1/OATP1B3/BCRP victim drug rosuvastatin for the investigation and prediction of its transpor... |
PMC6554958 | core_pubmed_pmc | Therapeutic drug monitoring-based dose optimisation of piperacillin/tazobactam to improve outcome in patients with sepsis (TARGET): a prospective, multi-centre, randomised controlled trial | Therapeutic drug monitoring-based dose optimisation of piperacillin/tazobactam to improve outcome in patients with sepsis (TARGET): a prospective, multi-centre, randomised controlled trial Abstract Abstract Background Sepsis is a life-threatening organ dysfunction caused by a dysregulated host response to infection wit... |
Subsets and Splits
No community queries yet
The top public SQL queries from the community will appear here once available.