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PMC3405214 | core_pubmed_pmc | Phase I study of TAS-102 treatment in Japanese patients with advanced solid tumours | Phase I study of TAS-102 treatment in Japanese patients with advanced solid tumours Abstract Abstract Background: TAS-102 consists of α, α, α-trifluorothymidine (TFT) and an inhibitor of thymidine phosphorylase (TPI). We conducted a dose-escalation phase I study in Japanese patients with advanced solid tumours. Methods... |
PMC12462925 | core_pubmed_pmc | Remodeling the Physicochemical and Pharmacokinetic Properties of PROTAC via Lipid Nanodisks for Cancer Therapy | Remodeling the Physicochemical and Pharmacokinetic Properties of PROTAC via Lipid Nanodisks for Cancer Therapy Abstract Abstract Proteolysis targeting chimera (PROTAC), as an emerging approach for target protein degradation based on the intracellular ubiquitin‐protease system, is characterized by catalytic and reusabil... |
PMC7179644 | core_pubmed_pmc | Drug Effect of Clofazimine on Persisters Explains an Unexpected Increase in Bacterial Load in Patients | Drug Effect of Clofazimine on Persisters Explains an Unexpected Increase in Bacterial Load in Patients Abstract Antituberculosis (anti-TB) drug development is dependent on informative trials to secure the development of new antibiotics and combination regimens. Clofazimine (CLO) and pyrazinamide (PZA) are important com... |
PMC10173800 | core_pubmed_pmc | Acacetin-loaded microemulsion for transdermal delivery: preparation, optimization and evaluation | Acacetin-loaded microemulsion for transdermal delivery: preparation, optimization and evaluation Abstract Abstract Context Acacetin is reported as a potential drug candidate for the treatment of atrial fibrillation. However, clinical applications are limited by poor water solubility, limited ethanol solubility, and ext... |
PMC10046771 | core_pubmed_pmc | Brexpiprazole—Pharmacologic Properties and Use in Schizophrenia and Mood Disorders | Brexpiprazole—Pharmacologic Properties and Use in Schizophrenia and Mood Disorders Abstract Abstract In 2002, the first III generation antipsychotic drug was registered—aripiprazole. Its partial dopaminergic agonism underlies its unique mechanism of action and the potentially beneficial influence on the positive, negat... |
PMC3752965 | core_pubmed_pmc | Pharmacodynamic characteristics of lixisenatide once daily versus liraglutide once daily in patients with type 2 diabetes insufficiently controlled on metformin | Pharmacodynamic characteristics of lixisenatide once daily versus liraglutide once daily in patients with type 2 diabetes insufficiently controlled on metformin Abstract Aim Assess the pharmacodynamics of lixisenatide once daily (QD) versus liraglutide QD in type 2 diabetes insufficiently controlled on metformin. Metho... |
PMC12481941 | core_pubmed_pmc | Evaluation of Potential Inhibitors of Zika Virus Envelope Protein Through Molecular Docking and Molecular Dynamics Simulation | Evaluation of Potential Inhibitors of Zika Virus Envelope Protein Through Molecular Docking and Molecular Dynamics Simulation Abstract Highlights • An integrated in silico approach was used to identify flavonoid-based compounds as potential inhibitors of the Zika virus (ZIKV) envelope protein. • Molecular docking revea... |
PMC12376358 | core_pubmed_pmc | Physiologically based pharmacokinetic modelling to predict artemether and lumefantrine exposure in neonates weighing less than 5 kg treated with artemether–lumefantrine to supplement the clinical data from the CALINA study | Physiologically based pharmacokinetic modelling to predict artemether and lumefantrine exposure in neonates weighing less than 5 kg treated with artemether–lumefantrine to supplement the clinical data from the CALINA study Abstract Abstract Background Evidence-based recommendations for malaria treatment in patients wei... |
PMC10696427 | core_pubmed_pmc | Differential Effect of Fixed Ratio Magnitude on the Rate of Lever-Pressing and Interinjection Intervals of Cocaine Self-Administration in Rats | Differential Effect of Fixed Ratio Magnitude on the Rate of Lever-Pressing and Interinjection Intervals of Cocaine Self-Administration in Rats Abstract Background Many features of self-administration behavior may be explained by reference to the properties of schedules of reinforcement. Schedules alter the probability ... |
PMC3730309 | core_pubmed_pmc | Vitamin D: Pharmacokinetics and Safety When Used in Conjunction with the Pharmaceutical Drugs Used in Cancer Patients: A Systematic Review | Vitamin D: Pharmacokinetics and Safety When Used in Conjunction with the Pharmaceutical Drugs Used in Cancer Patients: A Systematic Review Abstract Abstract Vitamin D has reported anti-cancer and anti-inflammatory properties modulated through gene transcription and non-genomic signaling cascades. The purpose of this re... |
PMC10812538 | core_pubmed_pmc | Assessment of the Pharmacokinetics and Pharmacodynamics of Injectable Lidocaine and a Lidocaine-Impregnated Latex Band for Castration and Tail Docking in Lambs | Assessment of the Pharmacokinetics and Pharmacodynamics of Injectable Lidocaine and a Lidocaine-Impregnated Latex Band for Castration and Tail Docking in Lambs Abstract Simple Summary Tail docking and castration in lambs are common husbandry practices, both of which cause pain and discomfort, for which many industries ... |
PMC10912895 | core_pubmed_pmc | Cerasome Versus Liposome: A Comparative Pharmacokinetic Analysis Following Intravenous Administration into Rats | Cerasome Versus Liposome: A Comparative Pharmacokinetic Analysis Following Intravenous Administration into Rats Abstract Background Cerasomes, due to their external siloxane network, demonstrate markedly higher physicochemical stability and, therefore, easier handling and storage than liposomes. Objectives The main obj... |
PMC11217561 | core_pubmed_pmc | Drug–drug interaction and initial dosage optimization of aripiprazole in patients with schizophrenia based on population pharmacokinetics | Drug–drug interaction and initial dosage optimization of aripiprazole in patients with schizophrenia based on population pharmacokinetics Abstract Background The present study aimed to investigate the drug–drug interaction and initial dosage optimization of aripiprazole in patients with schizophrenia based on populatio... |
PMC10744289 | core_pubmed_pmc | De Novo Potent Peptide Nucleic Acid Antisense Oligomer Inhibitors Targeting SARS-CoV-2 RNA-Dependent RNA Polymerase via Structure-Guided Drug Design | De Novo Potent Peptide Nucleic Acid Antisense Oligomer Inhibitors Targeting SARS-CoV-2 RNA-Dependent RNA Polymerase via Structure-Guided Drug Design Abstract Abstract Global reports of novel SARS-CoV-2 variants and recurrence cases continue despite substantial vaccination campaigns, raising severe concerns about COVID-... |
PMC6331900 | core_pubmed_pmc | Heterocyclic Anticancer Compounds: Recent Advances and the Paradigm Shift towards the Use of Nanomedicine’s Tool Box | Heterocyclic Anticancer Compounds: Recent Advances and the Paradigm Shift towards the Use of Nanomedicine’s Tool Box Abstract Abstract The majority of heterocycle compounds and typically common heterocycle fragments present in most pharmaceuticals currently marketed, alongside with their intrinsic versatility and uniqu... |
PMC9592662 | core_pubmed_pmc | Intravenous Golimumab in Patients with Polyarticular Juvenile Idiopathic Arthritis and Juvenile Psoriatic Arthritis and Subcutaneous Ustekinumab in Patients with Juvenile Psoriatic Arthritis: Extrapolation of Data from Studies in Adults and Adjacent Pediatric Populations | Intravenous Golimumab in Patients with Polyarticular Juvenile Idiopathic Arthritis and Juvenile Psoriatic Arthritis and Subcutaneous Ustekinumab in Patients with Juvenile Psoriatic Arthritis: Extrapolation of Data from Studies in Adults and Adjacent Pediatric Populations Abstract Abstract Objectives To describe the ext... |
PMC12481409 | core_pubmed_pmc | Therapeutic inhibition of USP7 promotes antitumor immune responses | Therapeutic inhibition of USP7 promotes antitumor immune responses Abstract Abstract Background Ubiquitin-specific peptidase 7 (USP7) is a deubiquitinating enzyme that removes ubiquitin from specific protein substrates to modify their degradation rates thereby regulating crucial cellular processes integral to cancer. C... |
PMC4462369 | core_pubmed_pmc | Carboplatin-induced severe hypersensitivity reaction: Role of IgE-dependent basophil activation and FcεRI | Carboplatin-induced severe hypersensitivity reaction: Role of IgE-dependent basophil activation and FcεRI Abstract Basophil activation was observed in patients with a history of carboplatin-induced severe hypersensitivity reaction (HR). However, the precise mechanism by which carboplatin induces basophil activation and... |
PMC12539420 | core_pubmed_pmc | Cardiac Myosin Inhibitors in Hypertrophic Cardiomyopathy: Clinical Advances and Therapeutic Prospects | Cardiac Myosin Inhibitors in Hypertrophic Cardiomyopathy: Clinical Advances and Therapeutic Prospects Abstract Abstract Hypertrophic cardiomyopathy (HCM) is a common inherited disease with substantial residual morbidity despite established pharmacological and surgical therapies. We conducted a narrative review of the c... |
PMC12932482 | core_pubmed_pmc | Regional absorption of talinolol mediated by intestinal transporters: insights from PBPK modeling analysis | Regional absorption of talinolol mediated by intestinal transporters: insights from PBPK modeling analysis Abstract Intestinal transporters play a pivotal role in oral absorption dynamics to shape the plasma or blood concentration-time curves of drugs, influencing interindividual pharmacokinetic (PK) variability and dr... |
PMC12521069 | core_pubmed_pmc | A Case Study of Model‐Informed Drug Development of a Novel PCSK9 Antisense Oligonucleotide. Part 2: Phase 2 to Phase 3 | A Case Study of Model‐Informed Drug Development of a Novel PCSK9 Antisense Oligonucleotide. Part 2: Phase 2 to Phase 3 Abstract ABSTRACT In this second part of a case study on the practical use of model‐informed drug development (MIDD), we describe the clinical development of AZD8233, a novel proprotein convertase subt... |
PMC6452577 | core_pubmed_pmc | Abuse potential of mirogabalin in recreational polydrug users | Abuse potential of mirogabalin in recreational polydrug users Abstract Mirogabalin is a selective calcium channel α 2 δ subunit ligand being developed to treat neuropathic pain. In accordance with US Food and Drug Administration (FDA) guidance, the human abuse potential of mirogabalin (15–105 mg) was examined, relative... |
PMC12399940 | core_pubmed_pmc | Evorpacept plus rituximab for the treatment of relapsed or refractory non-Hodgkin lymphoma: results from the phase I ASPEN-01 study | Evorpacept plus rituximab for the treatment of relapsed or refractory non-Hodgkin lymphoma: results from the phase I ASPEN-01 study Abstract CD47 overexpression has been associated with tumor cell survival. We present the safety, pharmacokinetics, pharmacodynamics, and preliminary anti-tumor activity of evorpacept, a n... |
PMC5322902 | core_pubmed_pmc | Effects of vasoactive drugs on crystalloid fluid kinetics in septic sheep | Effects of vasoactive drugs on crystalloid fluid kinetics in septic sheep Abstract Purpose Crystalloid fluid and vasoactive drugs are used in the early treatment of sepsis. The purpose of the present study was to examine how these drugs alter plasma volume expansion, peripheral edema, and urinary excretion. Methods Twe... |
PMC8376129 | core_pubmed_pmc | Prediction of drug concentrations in milk during breastfeeding, integrating predictive algorithms within a physiologically‐based pharmacokinetic model | Prediction of drug concentrations in milk during breastfeeding, integrating predictive algorithms within a physiologically‐based pharmacokinetic model Abstract Abstract There is a risk of exposure to drugs in neonates during the lactation period due to maternal drug intake. The ability to predict drugs of potential haz... |
PMC12823302 | core_pubmed_pmc | Characterizing Apixaban Pharmacokinetics Through Physiologically‐Based Pharmacokinetic Modeling: Critical Role of Biliary Secretion and Enterohepatic Circulation in Humans | Characterizing Apixaban Pharmacokinetics Through Physiologically‐Based Pharmacokinetic Modeling: Critical Role of Biliary Secretion and Enterohepatic Circulation in Humans Abstract ABSTRACT Apixaban, a factor Xa inhibitor, is a direct oral anticoagulant with a well‐balanced elimination; it is eliminated evenly via fece... |
PMC12061680 | core_pubmed_pmc | Fortified Withaferin A accelerates the transition from fibrovascular to bone remodeling phase during endochondral bone formation to promote ossification | Fortified Withaferin A accelerates the transition from fibrovascular to bone remodeling phase during endochondral bone formation to promote ossification Abstract Abstract Introduction This study shows that Fortified Withaferin A (FWA, 10% w/w) accelerates bone healing, advancing from the fibrovascular to bone remodelin... |
PMC9407039 | core_pubmed_pmc | QbD-based rivastigmine tartrate-loaded solid lipid nanoparticles for enhanced intranasal delivery to the brain for Alzheimer's therapeutics | QbD-based rivastigmine tartrate-loaded solid lipid nanoparticles for enhanced intranasal delivery to the brain for Alzheimer's therapeutics Abstract Alzheimer's disease (AD) is a neurodegenerative disease that affects a wide range of populations and is the primary cause of death in various countries. The treatment of A... |
PMC12483463 | core_pubmed_pmc | In silico evaluation of vitamin D3 as a dual inhibitor of CDK2 and Bcl-2 in colorectal cancer | In silico evaluation of vitamin D3 as a dual inhibitor of CDK2 and Bcl-2 in colorectal cancer Abstract Background: The potential anticancer properties of vitamin D3 (cholecalciferol) have garnered growing interest. Epidemiological and preclinical studies suggest an inverse correlation between vitamin D3 levels and CRC ... |
PMC9500076 | core_pubmed_pmc | A report on the potential of Rac1/pSTAT3 protein levels in T lymphocytes to assess the pharmacodynamic effect of thiopurine therapy in Inflammatory Bowel Disease patients | A report on the potential of Rac1/pSTAT3 protein levels in T lymphocytes to assess the pharmacodynamic effect of thiopurine therapy in Inflammatory Bowel Disease patients Abstract Abstract The thiopurine derivatives azathioprine (AZA), mercaptopurine (MP) and tioguanine (TG) remain standard treatment of inflammatory bo... |
PMC8301548 | core_pubmed_pmc | Oxypurinol pharmacokinetics and pharmacodynamics in healthy volunteers: Influence of BCRP Q141K polymorphism and patient characteristics | Oxypurinol pharmacokinetics and pharmacodynamics in healthy volunteers: Influence of BCRP Q141K polymorphism and patient characteristics Abstract Abstract The missense variant, breast cancer resistance protein (BCRP) p.Q141K, which encodes a reduced function BCRP, has been linked to poor response to allopurinol. Using ... |
PMC6868795 | core_pubmed_pmc | Enhanced renal clearance and impact on vancomycin pharmacokinetic parameters in patients with hemorrhagic stroke | Enhanced renal clearance and impact on vancomycin pharmacokinetic parameters in patients with hemorrhagic stroke Abstract Abstract Background The majority of patients with hemorrhagic stroke experience enhanced renal clearance or augmented renal clearance (ARC). The purpose of this study was to determine the impact of ... |
PMC10614045 | core_pubmed_pmc | A systems approach reveals species differences in hepatic stress response capacity | A systems approach reveals species differences in hepatic stress response capacity Abstract Abstract To minimize the occurrence of unexpected toxicities in early phase preclinical studies of new drugs, it is vital to understand fundamental similarities and differences between preclinical species and humans. Species dif... |
PMC10674081 | core_pubmed_pmc | Sex Differences in Plasma, Adipose Tissue, and Central Accumulation of Cannabinoids, and Behavioral Effects of Oral Cannabis Consumption in Male and Female C57BL/6 Mice | Sex Differences in Plasma, Adipose Tissue, and Central Accumulation of Cannabinoids, and Behavioral Effects of Oral Cannabis Consumption in Male and Female C57BL/6 Mice Abstract Abstract Background Cannabis edibles are an increasingly popular form of cannabis consumption. Oral consumption of cannabis has distinct physi... |
PMC4694668 | core_pubmed_pmc | Pharmacokinetics and safety of posaconazole delayed-release tablets for invasive fungal infections | Pharmacokinetics and safety of posaconazole delayed-release tablets for invasive fungal infections Abstract Posaconazole is a broad-spectrum triazole antifungal agent with potent activity against various pathogenic fungi, including yeast and moulds. Clinical studies have demonstrated that this agent is efficacious as p... |
PMC12131839 | core_pubmed_pmc | Population pharmacokinetics and pharmacogenomics of edoxaban in Japanese adults with atrial fibrillation | Population pharmacokinetics and pharmacogenomics of edoxaban in Japanese adults with atrial fibrillation Abstract Background Edoxaban is used as an anti-coagulant to prevent cardioembolic infarction, deep vein thrombosis, and pulmonary embolism. Edoxaban pharmacokinetics have been reported to be affected by several fac... |
PMC3407359 | core_pubmed_pmc | The role of genetics in drug dosing | The role of genetics in drug dosing Abstract Renal transplantation is the optimal form of renal replacement therapy (RRT) for the majority of patients. Both short- and long-term graft rejection are well recognized complications following transplantation, and optimal immunosuppression is often difficult to achieve. Phar... |
PMC10536648 | core_pubmed_pmc | Investigating Tacrolimus Disposition in Paediatric Patients with a Physiologically Based Pharmacokinetic Model Incorporating CYP3A4 Ontogeny, Mechanistic Absorption and Red Blood Cell Binding | Investigating Tacrolimus Disposition in Paediatric Patients with a Physiologically Based Pharmacokinetic Model Incorporating CYP3A4 Ontogeny, Mechanistic Absorption and Red Blood Cell Binding Abstract Abstract Tacrolimus is a crucial immunosuppressant for organ transplant patients, requiring therapeutic drug monitoring... |
PMC11609058 | core_pubmed_pmc | Relative Bioavailability Studies With Mitapivat: Formulation and Food Effect Assessments in Healthy Subjects | Relative Bioavailability Studies With Mitapivat: Formulation and Food Effect Assessments in Healthy Subjects Abstract Abstract Pyruvate kinase (PK) deficiency is a rare, hereditary, hemolytic anemia caused by mutations in the PKLR gene encoding the PK enzyme. Mitapivat (previously designated AG‐348) is a first‐in‐class... |
PMC3489553 | core_pubmed_pmc | Pharmacokinetics and modeling of immune cell trafficking: quantifying differential influences of target tissues versus lymphocytes in SJL and lipopolysaccharide-treated mice | Pharmacokinetics and modeling of immune cell trafficking: quantifying differential influences of target tissues versus lymphocytes in SJL and lipopolysaccharide-treated mice Abstract Background Immune cell trafficking into the CNS and other tissues plays important roles in health and disease. Rapid quantitative methods... |
PMC4887041 | core_pubmed_pmc | Critical appraisal of 3-monthly paliperidone depot injections in the treatment of schizophrenia | Critical appraisal of 3-monthly paliperidone depot injections in the treatment of schizophrenia Abstract Abstract Aims Three-monthly injections of paliperidone palmitate (PP-3M) represent a new and recently introduced long-acting antipsychotic therapeutic option. This review focuses on available data relating to the ef... |
PMC7314794 | core_pubmed_pmc | Durable protection against repeated penile exposures to simian-human immunodeficiency virus by broadly neutralizing antibodies | Durable protection against repeated penile exposures to simian-human immunodeficiency virus by broadly neutralizing antibodies Abstract Penile acquisition of HIV accounts for most infections among men globally. Nevertheless, candidate HIV interventions for men advance to clinical trials without preclinical efficacy dat... |
PMC9322739 | core_pubmed_pmc | Feasibility Studies of Nebulized SARS-CoV-2 Neutralizing Antibody in Mice and Cynomolgus Monkeys | Feasibility Studies of Nebulized SARS-CoV-2 Neutralizing Antibody in Mice and Cynomolgus Monkeys Abstract Purpose Neutralizing antibodies, administrated through intravenous infusion, have shown to be highly efficacious in treating mild and moderate COVID-19 caused by SARS-CoV-2 infection in the lung. However, antibodie... |
PMC10575168 | core_pubmed_pmc | Impedimetric DNA Sensors for Epirubicin Detection Based on Polythionine Films Electropolymerized from Deep Eutectic Solvent | Impedimetric DNA Sensors for Epirubicin Detection Based on Polythionine Films Electropolymerized from Deep Eutectic Solvent Abstract An electrochemically active polymer, polythionine (PTN), was synthesized in natural deep eutectic solvent (NADES) via multiple potential scans and characterized using cyclic voltammetry a... |
PMC9298354 | core_pubmed_pmc | F9 missense mutations impairing factor IX activation are associated with pleiotropic plasma phenotypes | F9 missense mutations impairing factor IX activation are associated with pleiotropic plasma phenotypes Abstract Abstract Background Circulating dysfunctional factor IX (FIX) might modulate distribution of infused FIX in hemophilia B (HB) patients. Recurrent substitutions at FIX activation sites (R191‐R226, >300 patient... |
PMC12327396 | core_pubmed_pmc | Plasma pharmacokinetics, milk residue depletion profile, and milk withdrawal interval estimation following multiple-dose oral administration of meloxicam to lactating dairy goats | Plasma pharmacokinetics, milk residue depletion profile, and milk withdrawal interval estimation following multiple-dose oral administration of meloxicam to lactating dairy goats Abstract Abstract Introduction Meloxicam is frequently administered orally to lactating dairy goats in an extra-label manner. However, since ... |
PMC7118210 | core_pubmed_pmc | Pharmacokinetics and Metabolism of Naringin and Active Metabolite Naringenin in Rats, Dogs, Humans, and the Differences Between Species | Pharmacokinetics and Metabolism of Naringin and Active Metabolite Naringenin in Rats, Dogs, Humans, and the Differences Between Species Abstract Abstract Background Pharmacokinetics provides a scientific basis for drug product design, dosage regimen planning, understanding the body's action on the drug, and relating th... |
PMC7877859 | core_pubmed_pmc | Model Informed Dosing Regimen and Phase I Results of the Anti‐PD‐1 Antibody Budigalimab (ABBV‐181) | Model Informed Dosing Regimen and Phase I Results of the Anti‐PD‐1 Antibody Budigalimab (ABBV‐181) Abstract Budigalimab is a humanized, recombinant, Fc mutated IgG1 monoclonal antibody targeting programmed cell death 1 (PD‐1) receptor, currently in phase I clinical trials. The safety, efficacy, pharmacokinetics (PKs), ... |
PMC8338929 | core_pubmed_pmc | Acetylation turns leucine into a drug by membrane transporter switching | Acetylation turns leucine into a drug by membrane transporter switching Abstract Abstract Small changes to molecules can have profound effects on their pharmacological activity as exemplified by the addition of the two-carbon acetyl group to make drugs more effective by enhancing their pharmacokinetic or pharmacodynami... |
PMC7680462 | core_pubmed_pmc | An Appraisal of the Pharmacokinetic and Pharmacodynamic Properties of Meropenem-Vaborbactam | An Appraisal of the Pharmacokinetic and Pharmacodynamic Properties of Meropenem-Vaborbactam Abstract Abstract Carbapenem-resistant gram-negative pathogens remain an urgent public health threat, and safe, effective treatment options are limited. Although several agents are now available to combat these infections, merop... |
PMC4019894 | core_pubmed_pmc | Recombinant interleukin-21 plus sorafenib for metastatic renal cell carcinoma: a phase 1/2 study | Recombinant interleukin-21 plus sorafenib for metastatic renal cell carcinoma: a phase 1/2 study Abstract Background Despite the positive impact of targeted therapies on metastatic renal cell carcinoma (mRCC), durable responses are infrequent and an unmet need exists for novel therapies with distinct mechanisms of acti... |
PMC9898357 | core_pubmed_pmc | Evaluation of Neonatal and Paediatric Vancomycin Pharmacokinetic Models and the Impact of Maturation and Serum Creatinine Covariates in a Large Multicentre Data Set | Evaluation of Neonatal and Paediatric Vancomycin Pharmacokinetic Models and the Impact of Maturation and Serum Creatinine Covariates in a Large Multicentre Data Set Abstract Background and Objective Infants and neonates present a clinical challenge for dosing drugs with high interindividual variability due to these pat... |
PMC11196376 | core_pubmed_pmc | A first‐in‐human, single and multiple dose study of lunsekimig, a novel anti‐TSLP/anti‐IL‐13 NANOBODY® compound, in healthy volunteers | A first‐in‐human, single and multiple dose study of lunsekimig, a novel anti‐TSLP/anti‐IL‐13 NANOBODY® compound, in healthy volunteers Abstract Abstract Lunsekimig is a novel, bispecific NANOBODY® molecule that inhibits both thymic stromal lymphopoietin (TSLP) and interleukin (IL)‐13, two key mediators of asthma pathop... |
PMC8566392 | core_pubmed_pmc | Pharmacokinetic studies of [ 68 Ga]Ga-PSMA-11 in patients with biochemical recurrence of prostate cancer: detection, differences in temporal distribution and kinetic modelling by tissue type | Pharmacokinetic studies of [ 68 Ga]Ga-PSMA-11 in patients with biochemical recurrence of prostate cancer: detection, differences in temporal distribution and kinetic modelling by tissue type Abstract Purpose [ 68 Ga]Ga-PSMA-11 is a promising radiopharmaceutical for detecting tumour lesions in prostate cancer, but knowl... |
PMC3334808 | core_pubmed_pmc | Pharmacokinetics of prolonged infusion of high-dose dexmedetomidine in critically ill patients | Pharmacokinetics of prolonged infusion of high-dose dexmedetomidine in critically ill patients Abstract Introduction Only limited information exists on the pharmacokinetics of prolonged (> 24 hours) and high-dose dexmedetomidine infusions in critically ill patients. The aim of this study was to characterize the pharmac... |
PMC12098654 | core_pubmed_pmc | First-in-human dosimetry and safety evaluation of 68 Ga-αMSH derivative for PET imaging of melanoma | First-in-human dosimetry and safety evaluation of 68 Ga-αMSH derivative for PET imaging of melanoma Abstract Abstract Melanoma remains one of the leading causes of cancer-related mortality worldwide, necessitating advanced imaging techniques for early and accurate detection. This study assesses the dosimetry, safety, a... |
PMC8329483 | core_pubmed_pmc | Remimazolam: Non-Clinical and Clinical Profile of a New Sedative/Anesthetic Agent | Remimazolam: Non-Clinical and Clinical Profile of a New Sedative/Anesthetic Agent Abstract Abstract A program to identify novel intravenous sedatives with a short and predictable duration of action was initiated in the late 1990’s by Glaxo Wellcome. The program focussed on the identification of ester-based benzodiazepi... |
PMC6019254 | core_pubmed_pmc | Optimal dynamic regimens with artificial intelligence: The case of temozolomide | Optimal dynamic regimens with artificial intelligence: The case of temozolomide Abstract We determine an optimal protocol for temozolomide using population variability and dynamic optimization techniques inspired by artificial intelligence. We use a Pharmacokinetics/Pharmacodynamics (PK/PD) model based on Faivre and co... |
PMC5114203 | core_pubmed_pmc | Bioequivalence and Pharmacokinetic Evaluation Study of Acetaminophen vs. Acetaminophen Plus Caffeine Tablets in Healthy Mexican Volunteers | Bioequivalence and Pharmacokinetic Evaluation Study of Acetaminophen vs. Acetaminophen Plus Caffeine Tablets in Healthy Mexican Volunteers Abstract Objective The aim of this clinical trial was to establish the bioequivalence of two tablets containing acetaminophen 650 mg (reference) and acetaminophen 650 mg plus caffei... |
PMC12567248 | core_pubmed_pmc | MIL-100(Fe)-Enabled Oral Delivery of Syringic Acid with Enhanced Pharmacokinetics | MIL-100(Fe)-Enabled Oral Delivery of Syringic Acid with Enhanced Pharmacokinetics Abstract Abstract Background/Objectives: Plant-derived bioactive compounds like syringic acid, a phenolic acid from the shikimic acid pathway, have shown potential against chronic diseases, including diabetes, cardiovascular disorders, ca... |
PMC4620676 | core_pubmed_pmc | Bovine Serum Albumin Interactions with Metal Complexes | Bovine Serum Albumin Interactions with Metal Complexes Abstract Abstract The continuous search for new molecules with therapeutic abilities has led to the synthesis and characterization of a large number of metal complexes, proven to exhibit potential as pharmacological agents through their antibacterial, antiviral, an... |
PMC5448051 | core_pubmed_pmc | Radix Bupleuri : A Review of Traditional Uses, Botany, Phytochemistry, Pharmacology, and Toxicology | Radix Bupleuri : A Review of Traditional Uses, Botany, Phytochemistry, Pharmacology, and Toxicology Abstract Abstract Radix Bupleuri (Chaihu) has been used as a traditional medicine for more than 2000 years in China, Japan, Korea, and other Asian countries. Phytochemical studies demonstrated that this plant contains es... |
PMC8236452 | core_pubmed_pmc | Pharmacokinetics and safety of rucaparib in patients with advanced solid tumors and hepatic impairment | Pharmacokinetics and safety of rucaparib in patients with advanced solid tumors and hepatic impairment Abstract Abstract Purpose The poly(ADP-ribose) polymerase inhibitor rucaparib is approved for the treatment of patients with recurrent ovarian and metastatic castration-resistant prostate cancer; however, limited data... |
PMC11611764 | core_pubmed_pmc | Population pharmacokinetic model of ABL001/CTX‐009 (anti‐VEGF/DLL4) in adult cancer patients with solid tumor | Population pharmacokinetic model of ABL001/CTX‐009 (anti‐VEGF/DLL4) in adult cancer patients with solid tumor Abstract Abstract ABL001/CTX‐009 is a bispecific antibody targeting delta‐like ligand‐4 and vascular endothelial growth factor A. In this study, we developed a population pharmacokinetic (PK) model of ABL001/CT... |
PMC6373393 | core_pubmed_pmc | The Clinical Pharmacology of Cladribine Tablets for the Treatment of Relapsing Multiple Sclerosis | The Clinical Pharmacology of Cladribine Tablets for the Treatment of Relapsing Multiple Sclerosis Abstract Cladribine Tablets (MAVENCLAD ® ) are used to treat relapsing multiple sclerosis (MS). The recommended dose is 3.5 mg/kg, consisting of 2 annual courses, each comprising 2 treatment weeks 1 month apart. We reviewe... |
PMC8484122 | core_pubmed_pmc | Safety and Efficacy of GFB-887, a TRPC5 Channel Inhibitor, in Patients With Focal Segmental Glomerulosclerosis, Treatment-Resistant Minimal Change Disease, or Diabetic Nephropathy: TRACTION-2 Trial Design | Safety and Efficacy of GFB-887, a TRPC5 Channel Inhibitor, in Patients With Focal Segmental Glomerulosclerosis, Treatment-Resistant Minimal Change Disease, or Diabetic Nephropathy: TRACTION-2 Trial Design Abstract Abstract Introduction A critical unmet need exists for precision therapies for chronic kidney disease. GFB... |
PMC12499247 | core_pubmed_pmc | A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Efficacy of QP002 for the Treatment of Post-Operative Pain After Tension-Free Repair of Open Unilateral Inguinal Hernia | A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Efficacy of QP002 for the Treatment of Post-Operative Pain After Tension-Free Repair of Open Unilateral Inguinal Hernia Abstract Background QP002 Long-acting local anaesthetic with bupivacaine and low-dose meloxicam as active ingredients for po... |
PMC7221868 | core_pubmed_pmc | Development and Validation of Liquid Chromatography-Tandem Mass Spectrometry Method for Pharmacokinetic Evaluation of 7β-(3-Ethyl-cis-crotonoyloxy)-1α-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranon in Rats | Development and Validation of Liquid Chromatography-Tandem Mass Spectrometry Method for Pharmacokinetic Evaluation of 7β-(3-Ethyl-cis-crotonoyloxy)-1α-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranon in Rats Abstract Abstract Recently, potent neuroprotective and anti-diabetic effects of 7 β -(3-Ethyl-cis-crotonoyloxy... |
PMC3040610 | core_pubmed_pmc | Intrinsic Human Elimination Half-Lives of Polychlorinated Biphenyls Derived from the Temporal Evolution of Cross-Sectional Biomonitoring Data from the United Kingdom | Intrinsic Human Elimination Half-Lives of Polychlorinated Biphenyls Derived from the Temporal Evolution of Cross-Sectional Biomonitoring Data from the United Kingdom Abstract Background Most empirical estimates of human elimination kinetics for persistent chemicals reflect apparent elimination half-lives that represent... |
PMC6273185 | core_pubmed_pmc | Pharmacokinetics of Maleic Acid as a Food Adulterant Determined by Microdialysis in Rat Blood and Kidney Cortex | Pharmacokinetics of Maleic Acid as a Food Adulterant Determined by Microdialysis in Rat Blood and Kidney Cortex Abstract Abstract Maleic acid has been shown to be used as a food adulterant in the production of modified starch by the Taiwan Food and Drug Administration. Due to the potential toxicity of maleic acid to th... |
PMC6900561 | core_pubmed_pmc | Current trends in drug metabolism and pharmacokinetics | Current trends in drug metabolism and pharmacokinetics Abstract Abstract Pharmacokinetics (PK) is the study of the absorption, distribution, metabolism, and excretion (ADME) processes of a drug. Understanding PK properties is essential for drug development and precision medication. In this review we provided an overvie... |
PMC10044180 | core_pubmed_pmc | Challenges of Colistin Use in ICU and Therapeutic Drug Monitoring: A Literature Review | Challenges of Colistin Use in ICU and Therapeutic Drug Monitoring: A Literature Review Abstract Abstract The emerging resistance of Gram-negative bacteria is a growing problem worldwide. Together with the financial cost, limited efficacy, and local unavailability of newer antibiotics or their combinations, it has led t... |
PMC12511262 | core_pubmed_pmc | Validation of pharmacokinetic model for quizartinib quantified by UPLC-MS/MS in patients with FLT3-ITD negative newly diagnosed acute myeloid leukemia | Validation of pharmacokinetic model for quizartinib quantified by UPLC-MS/MS in patients with FLT3-ITD negative newly diagnosed acute myeloid leukemia Abstract Abstract Purpose Quizartinib pharmacokinetics in FLT3-ITD negative acute myeloid leukemia (AML) remain largely unexplored. This study aims to validate a populat... |
PMC3565294 | core_pubmed_pmc | Pharmacokinetics of Dibutyl Phthalate (DBP) in the Rat Determined by UPLC-MS/MS | Pharmacokinetics of Dibutyl Phthalate (DBP) in the Rat Determined by UPLC-MS/MS Abstract Abstract Dibutyl phthalate (DBP) is commonly used to increase the flexibility of plastics in industrial products. However, several plasticizers have been illegally used as clouding agents to increase dispersion of aqueous matrix in... |
PMC5125998 | core_pubmed_pmc | The pharmacokinetics of vancomycin during the initial loading dose in patients with septic shock | The pharmacokinetics of vancomycin during the initial loading dose in patients with septic shock Abstract Objective To characterize the pharmacokinetics (PK) of vancomycin in patients in the initial phase of septic shock. Methods Twelve patients with septic shock received an intravenous infusion of vancomycin 30 mg/kg ... |
PMC9944674 | core_pubmed_pmc | Clinical Ocular Exposure Extrapolation for Ophthalmic Solutions Using PBPK Modeling and Simulation | Clinical Ocular Exposure Extrapolation for Ophthalmic Solutions Using PBPK Modeling and Simulation Abstract Abstract Background The development of generic ophthalmic drug products is challenging due to the complexity of the ocular system, and a lack of sensitive testing to evaluate the interplay of physiology with opht... |
PMC9087007 | core_pubmed_pmc | Physiologically‐Based Pharmacokinetic‐Led Guidance for Patients With Cystic Fibrosis Taking Elexacaftor‐Tezacaftor‐Ivacaftor With Nirmatrelvir‐Ritonavir for the Treatment of COVID‐19 | Physiologically‐Based Pharmacokinetic‐Led Guidance for Patients With Cystic Fibrosis Taking Elexacaftor‐Tezacaftor‐Ivacaftor With Nirmatrelvir‐Ritonavir for the Treatment of COVID‐19 Abstract Abstract Cystic fibrosis transmembrane conductance regulator (CFTR) modulating therapies, including elexacaftor‐tezacaftor‐ivaca... |
PMC11109088 | core_pubmed_pmc | Magnetic resonance imaging of tumor response to stroma-modifying pegvorhyaluronidase alpha (PEGPH20) therapy in early-phase clinical trials | Magnetic resonance imaging of tumor response to stroma-modifying pegvorhyaluronidase alpha (PEGPH20) therapy in early-phase clinical trials Abstract Abstract Pre-clinical and clinical studies have shown that PEGPH20 depletes intratumoral hyaluronic acid (HA), which is linked to high interstitial fluid pressures and poo... |
PMC3617031 | core_pubmed_pmc | The Pharmaco –, Population and Evolutionary Dynamics of Multi-drug Therapy: Experiments with S. aureus and E. coli and Computer Simulations | The Pharmaco –, Population and Evolutionary Dynamics of Multi-drug Therapy: Experiments with S. aureus and E. coli and Computer Simulations Abstract There are both pharmacodynamic and evolutionary reasons to use multiple rather than single antibiotics to treat bacterial infections; in combination antibiotics can be mor... |
PMC9421327 | core_pubmed_pmc | Agrimonia pilosa Ledeb.: A review of its traditional uses, botany, phytochemistry, pharmacology, and toxicology | Agrimonia pilosa Ledeb.: A review of its traditional uses, botany, phytochemistry, pharmacology, and toxicology Abstract Ethnopharmacological relevance Agrimonia pilosa Ledeb. is the dried above-ground part of dragon's tooth grass, a plant of the Rosaceae family, which is widely distributed in China, Korea, and Japan. ... |
PMC5660009 | core_pubmed_pmc | Safety, pharmacokinetics, metabolism and radiation dosimetry of 18 F-tetrafluoroborate ( 18 F-TFB) in healthy human subjects | Safety, pharmacokinetics, metabolism and radiation dosimetry of 18 F-tetrafluoroborate ( 18 F-TFB) in healthy human subjects Abstract Background 18 F-Tetrafluoroborate ( 18 F-TFB) is a promising iodide analog for PET imaging of thyroid cancer and sodium/iodide symporter (NIS) reporter activity in viral therapy applicat... |
PMC11839030 | core_pubmed_pmc | Whole-body Bacteriophage Distribution Characterized by a Physiologically based Pharmacokinetic Model | Whole-body Bacteriophage Distribution Characterized by a Physiologically based Pharmacokinetic Model Abstract Abstract In 2019 there were over 2.8 million cases of antibiotic-resistant bacterial infection in the US with gram negative organisms having up to a 6% rate of mortality. Bacteriophage (phage) therapy holds gre... |
PMC8536600 | core_pubmed_pmc | Ruxolitinib exposure in patients with acute and chronic graft versus host disease in routine clinical practice—a prospective single-center trial | Ruxolitinib exposure in patients with acute and chronic graft versus host disease in routine clinical practice—a prospective single-center trial Abstract Purpose Knowledge on Ruxolitinib exposure in patients with graft versus host disease (GvHD) is scarce. The purpose of this prospective study was to analyze Ruxolitini... |
PMC7033341 | core_pubmed_pmc | Ginsenoside Rb1 exerts neuroprotective effects through regulation of Lactobacillus helveticus abundance and GABA A receptor expression | Ginsenoside Rb1 exerts neuroprotective effects through regulation of Lactobacillus helveticus abundance and GABA A receptor expression Abstract Background Ginsenoside Rb1 (Rb1), one of the most abundant protopanaxadiol-type ginsenosides, exerts excellent neuroprotective effects even though it has low intracephalic expo... |
PMC11441388 | core_pubmed_pmc | Mass balance and pharmacokinetic characterization of zavegepant in healthy male subjects | Mass balance and pharmacokinetic characterization of zavegepant in healthy male subjects Abstract Abstract Zavegepant, a high‐affinity, selective, small‐molecule calcitonin gene‐related peptide receptor antagonist, is approved as a nasal spray for acute treatment of migraine in adults. This phase I, open‐label, single‐... |
PMC9804084 | core_pubmed_pmc | Multiple drug transporters contribute to the brain transfer of levofloxacin | Multiple drug transporters contribute to the brain transfer of levofloxacin Abstract Abstract Aims The aim of this study was to assess the influence of the major transporters at blood–brain barrier and blood–cerebrospinal fluid barrier on levofloxacin (LVFX) pharmacokinetics in rat. To explore the different effects of ... |
PMC10431683 | core_pubmed_pmc | A physiologically based pharmacokinetic model to optimize the dosage regimen and withdrawal time of cefquinome in pigs | A physiologically based pharmacokinetic model to optimize the dosage regimen and withdrawal time of cefquinome in pigs Abstract Abstract Cefquinome is widely used to treat respiratory tract diseases of swine. While extra-label dosages of cefquinome could improve clinical efficacy, they might lead to excessively high re... |
PMC6373243 | core_pubmed_pmc | Effects of rolapitant administered orally on the pharmacokinetics of dextromethorphan (CYP2D6), tolbutamide (CYP2C9), omeprazole (CYP2C19), efavirenz (CYP2B6), and repaglinide (CYP2C8) in healthy subjects | Effects of rolapitant administered orally on the pharmacokinetics of dextromethorphan (CYP2D6), tolbutamide (CYP2C9), omeprazole (CYP2C19), efavirenz (CYP2B6), and repaglinide (CYP2C8) in healthy subjects Abstract Purpose Rolapitant is a neurokinin-1 receptor antagonist indicated in combination with other antiemetic ag... |
PMC5554537 | core_pubmed_pmc | Reductive Metabolism Influences the Toxicity and Pharmacokinetics of the Hypoxia-Targeted Benzotriazine Di-Oxide Anticancer Agent SN30000 in Mice | Reductive Metabolism Influences the Toxicity and Pharmacokinetics of the Hypoxia-Targeted Benzotriazine Di-Oxide Anticancer Agent SN30000 in Mice Abstract Abstract 3-(3-Morpholinopropyl)-7,8-dihydro-6 H -indeno[5,6- e ]triazine 1,4-dioxide (SN30- 000), an analog of the well-studied bioreductive prodrug tirapazamine (TP... |
PMC9864514 | core_pubmed_pmc | Evaluation of the Local Anesthetic Activity, Acute Toxicity, and Structure–Toxicity Relationship in Series of Synthesized 1-Aryltetrahydroisoquinoline Alkaloid Derivatives In Vivo and In Silico | Evaluation of the Local Anesthetic Activity, Acute Toxicity, and Structure–Toxicity Relationship in Series of Synthesized 1-Aryltetrahydroisoquinoline Alkaloid Derivatives In Vivo and In Silico Abstract Isoquinoline alkaloids constitute one of the most common classes of alkaloids that have shown a pronounced role in cu... |
PMC9338137 | core_pubmed_pmc | Factors affecting inter-individual variability in endoxifen concentrations in patients with breast cancer: results from the prospective TOTAM trial | Factors affecting inter-individual variability in endoxifen concentrations in patients with breast cancer: results from the prospective TOTAM trial Abstract Abstract Introduction Endoxifen—the principal metabolite of tamoxifen—is subject to a high inter-individual variability in serum concentration. Numerous attempts h... |
PMC11089204 | core_pubmed_pmc | In vitro and in vivo metabolism of psilocybin’s active metabolite psilocin | In vitro and in vivo metabolism of psilocybin’s active metabolite psilocin Abstract Abstract In vivo , psilocybin is rapidly dephosphorylated to psilocin which induces psychedelic effects by interacting with the 5-HT 2A receptor. Psilocin primarily undergoes glucuronidation or conversion to 4-hydroxyindole-3-acetic aci... |
PMC4490036 | core_pubmed_pmc | Targeting the interleukin-11 receptor α in metastatic prostate cancer: A first-in-man study | Targeting the interleukin-11 receptor α in metastatic prostate cancer: A first-in-man study Abstract Abstract BACKGROUND Receptors in tumor blood vessels are attractive targets for ligand-directed drug discovery and development. The authors have worked systematically to map human endothelial receptors (“vascular zip co... |
PMC8794956 | core_pubmed_pmc | Electroencephalographic Evidence for Individual Neural Inertia in Mice That Decreases With Time | Electroencephalographic Evidence for Individual Neural Inertia in Mice That Decreases With Time Abstract Previous studies have demonstrated that the brain has an intrinsic resistance to changes in arousal state. This resistance is most easily measured at the population level in the setting of general anesthesia and has... |
PMC8278733 | core_pubmed_pmc | Scintigraphic tracking of 99m Technetium-labelled equine peripheral blood-derived mesenchymal stem cells after intravenous, intramuscular, and subcutaneous injection in healthy dogs | Scintigraphic tracking of 99m Technetium-labelled equine peripheral blood-derived mesenchymal stem cells after intravenous, intramuscular, and subcutaneous injection in healthy dogs Abstract Background Mesenchymal stem cell treatments in dogs have been investigated as a potential innovative alternative to current conve... |
PMC7828520 | core_pubmed_pmc | Disposition of Phytocannabinoids, Their Acidic Precursors and Their Metabolites in Biological Matrices of Healthy Individuals Treated with Vaporized Medical Cannabis | Disposition of Phytocannabinoids, Their Acidic Precursors and Their Metabolites in Biological Matrices of Healthy Individuals Treated with Vaporized Medical Cannabis Abstract Inhalation by vaporization is a useful application mode for medical cannabis. In this study, we present the disposition of Δ9-tetrahydrocannabino... |
PMC12479633 | core_pubmed_pmc | A Phase IIa, Single-Blind, Placebo-Controlled, Parallel-Group Study to Assess Safety, Tolerability, and Pharmacokinetics/Pharmacodynamics of Brensocatib in Adults with Cystic Fibrosis | A Phase IIa, Single-Blind, Placebo-Controlled, Parallel-Group Study to Assess Safety, Tolerability, and Pharmacokinetics/Pharmacodynamics of Brensocatib in Adults with Cystic Fibrosis Abstract Background and Objectives Brensocatib, an oral, competitive, and reversible inhibitor of dipeptidyl peptidase 1 (DPP1), reduces... |
PMC4366075 | core_pubmed_pmc | First Administration of the Fc-Attenuated Anti-β Amyloid Antibody GSK933776 to Patients with Mild Alzheimer’s Disease: A Randomized, Placebo-Controlled Study | First Administration of the Fc-Attenuated Anti-β Amyloid Antibody GSK933776 to Patients with Mild Alzheimer’s Disease: A Randomized, Placebo-Controlled Study Abstract Abstract Objective To assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of the Fc-inactivated anti-β amyloid (Aβ) monoclonal antibo... |
PMC3714492 | core_pubmed_pmc | Randomized Assessment of Ticagrelor Versus Prasugrel Antiplatelet Effects in Patients With Diabetes | Randomized Assessment of Ticagrelor Versus Prasugrel Antiplatelet Effects in Patients With Diabetes Abstract OBJECTIVE It has been postulated that prasugrel might be the preferred treatment option in diabetes mellitus (DM) patients with acute coronary syndrome (ACS) undergoing percutaneous coronary intervention (PCI). ... |
PMC7886742 | core_pubmed_pmc | Pharmacokinetics of Coadministered Viloxazine Extended-Release (SPN-812) and Methylphenidate in Healthy Adults | Pharmacokinetics of Coadministered Viloxazine Extended-Release (SPN-812) and Methylphenidate in Healthy Adults Abstract Background and Objectives Viloxazine extended-release (viloxazine ER, SPN-812) is a novel non-stimulant with activity at serotonin receptors and the norepinephrine transporter, which is under investig... |
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