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PMC8799535
core_pubmed_pmc
Pharmacology Versus Convenience: A Benefit/Risk Analysis of Regular Maintenance Versus Infrequent or As-Needed Inhaled Corticosteroid Use in Mild Asthma
Pharmacology Versus Convenience: A Benefit/Risk Analysis of Regular Maintenance Versus Infrequent or As-Needed Inhaled Corticosteroid Use in Mild Asthma Abstract Introduction This study compared the bronchoprotective and benefit/risk profiles of various inhaled corticosteroid (ICS) dosing regimens in mild asthma. Metho...
PMC9372424
core_pubmed_pmc
Influence of hepatic impairment on the pharmacokinetics and pharmacodynamics of the P2Y12 receptor antagonist selatogrel
Influence of hepatic impairment on the pharmacokinetics and pharmacodynamics of the P2Y12 receptor antagonist selatogrel Abstract Abstract Selatogrel is a potent and selective reversible P2Y12 receptor antagonist in development for early treatment of acute myocardial infarction via subcutaneous (s.c.) self‐injection. S...
PMC10289236
core_pubmed_pmc
Haptoglobin Treatment for Aneurysmal Subarachnoid Hemorrhage: Review and Expert Consensus on Clinical Translation
Haptoglobin Treatment for Aneurysmal Subarachnoid Hemorrhage: Review and Expert Consensus on Clinical Translation Abstract Aneurysmal subarachnoid hemorrhage (aSAH) is a devastating form of stroke frequently affecting young to middle-aged adults, with an unmet need to improve outcome. This special report focusses on th...
PMC6445238
core_pubmed_pmc
A first-in-human study to investigate the safety, tolerability, pharmacokinetics, and pharmacodynamics of KM-819 (FAS-associated factor 1 inhibitor), a drug for Parkinson’s disease, in healthy volunteers
A first-in-human study to investigate the safety, tolerability, pharmacokinetics, and pharmacodynamics of KM-819 (FAS-associated factor 1 inhibitor), a drug for Parkinson’s disease, in healthy volunteers Abstract Abstract Background KM-819 is a novel FAS-associated factor 1 (FAF1) inhibitor, and a neuroprotective agent...
PMC11976879
core_pubmed_pmc
Safety, Tolerability and Pharmacokinetics of Sodium Tungstate (OXO-001) in Healthy Female Volunteers of Childbearing Age: A Randomized, Double-Blind, Dose-Finding, and Placebo-Controlled Phase I Study
Safety, Tolerability and Pharmacokinetics of Sodium Tungstate (OXO-001) in Healthy Female Volunteers of Childbearing Age: A Randomized, Double-Blind, Dose-Finding, and Placebo-Controlled Phase I Study Abstract Abstract Background: Phase I study to assess the effects of single oral doses of 100, 200, and 300 mg/day of s...
PMC4759723
core_pubmed_pmc
Pharmacokinetics of oral and intravenous melatonin in healthy volunteers
Pharmacokinetics of oral and intravenous melatonin in healthy volunteers Abstract Abstract Background The aim was to investigate the pharmacokinetics of oral and iv melatonin in healthy volunteers. Methods The study was performed as a cohort crossover study. The volunteers received either 10 mg oral melatonin or 10 mg ...
PMC6606601
core_pubmed_pmc
Nasal delivery of donepezil HCl-loaded hydrogels for the treatment of Alzheimer’s disease
Nasal delivery of donepezil HCl-loaded hydrogels for the treatment of Alzheimer’s disease Abstract Abstract This study aims to prepare, characterize and evaluate the pharmacokinetics of liposomal donepezil HCl (LDH) dispersed into thiolated chitosan hydrogel (TCH) in rabbits. Various hydrogels including TCH were prepar...
PMC8200773
core_pubmed_pmc
A Comprehensive Review of the Chemistry, Pharmacokinetics, Pharmacology, Clinical Applications, Adverse Events, and Quality Control of Indigo Naturalis
A Comprehensive Review of the Chemistry, Pharmacokinetics, Pharmacology, Clinical Applications, Adverse Events, and Quality Control of Indigo Naturalis Abstract Abstract Indigo naturalis (IN), which is derived from indigo plants such as Strobilanthes cusia (Nees) Kuntze, Persicaria tinctoria (Aiton) Spach, and Isatis t...
PMC3141322
core_pubmed_pmc
Evidence of a pharmacodynamic EEG profile in rats following clonidine administration using a nonlinear analysis
Evidence of a pharmacodynamic EEG profile in rats following clonidine administration using a nonlinear analysis Abstract Abstract Background Changes caused by clonidine in rodent electroencephalograms (EEG) have been reported with some inconsistency. For this reason, a pre-clinical study was conducted in order to confi...
PMC11652867
core_pubmed_pmc
Stability of the thromboxane B 2 biomarker of low-dose aspirin pharmacodynamics in human whole blood and in long-term stored serum samples
Stability of the thromboxane B 2 biomarker of low-dose aspirin pharmacodynamics in human whole blood and in long-term stored serum samples Abstract Abstract Background Serum thromboxane B 2 (sTXB 2 ) is a validated biomarker of low-dose aspirin pharmacodynamics. In the original method, nonanticoagulated blood samples m...
PMC9864825
core_pubmed_pmc
In Silico Mining of Natural Products Atlas (NPAtlas) Database for Identifying Effective Bcl-2 Inhibitors: Molecular Docking, Molecular Dynamics, and Pharmacokinetics Characteristics
In Silico Mining of Natural Products Atlas (NPAtlas) Database for Identifying Effective Bcl-2 Inhibitors: Molecular Docking, Molecular Dynamics, and Pharmacokinetics Characteristics Abstract The Bcl-2 protein has a vital function in controlling the programmed cell doom of mitochondria. If programmed cell death signals ...
PMC12341389
core_pubmed_pmc
Are plasma drug concentrations still necessary? Rethinking the pharmacokinetic link in dose–response relationships
Are plasma drug concentrations still necessary? Rethinking the pharmacokinetic link in dose–response relationships Abstract Plasma drug concentrations have historically played a central role in pharmacology, serving as a measurable intermediary between administered dose and clinical response. This model, linking Dose, ...
PMC3587987
core_pubmed_pmc
Regulation of Erythropoietin Receptor Activity in Endothelial Cells by Different Erythropoietin (EPO) Derivatives: An in Vitro Study
Regulation of Erythropoietin Receptor Activity in Endothelial Cells by Different Erythropoietin (EPO) Derivatives: An in Vitro Study Abstract Abstract In endothelial cells, erythropoietin receptors (EPORs) mediate the protective, proliferative and angiogenic effects of EPO and its analogues, which act as EPOR agonists....
PMC4676304
core_pubmed_pmc
Bioequivalence of oral and intravenous carbamazepine formulations in adult patients with epilepsy
Bioequivalence of oral and intravenous carbamazepine formulations in adult patients with epilepsy Abstract Abstract Objective To evaluate the safety, tolerability, and comparative pharmacokinetics (PK) of intravenous and oral carbamazepine. Methods In this phase 1, open-label study, adult patients with epilepsy on a st...
PMC10418331
core_pubmed_pmc
Development and In Vitro–In Vivo Correlation Evaluation of IMM-H014 Extended-Release Tablets for the Treatment of Fatty Liver Disease
Development and In Vitro–In Vivo Correlation Evaluation of IMM-H014 Extended-Release Tablets for the Treatment of Fatty Liver Disease Abstract Abstract This study aimed to develop extended-release tablets containing 25 mg IMM-H014, an original drug formulated by a direct powder pressing method based on pharmaceutical-g...
PMC8671955
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Determinations of Iron-tannic Molecular Nanoparticles with its Implication in MR Imaging and Enhancement of Liver Clearance
Pharmacokinetic/Pharmacodynamic Determinations of Iron-tannic Molecular Nanoparticles with its Implication in MR Imaging and Enhancement of Liver Clearance Abstract Abstract Assessment and enhancement of liver clearance are promising strategies for protection of liver from various liver diseases. Iron-tannic nanopartic...
PMC12868915
core_pubmed_pmc
The Effect of Ecopipam on the Pharmacokinetics of Concomitant Medications
The Effect of Ecopipam on the Pharmacokinetics of Concomitant Medications Abstract ABSTRACT Ecopipam is a first‐in‐class dopamine D1 receptor antagonist under investigation for the treatment of Tourette syndrome. This open‐label, fixed‐sequence, three‐cohort study evaluated whether ecopipam induces or inhibits cytochro...
PMC9692377
core_pubmed_pmc
Mucolytic and Antioxidant Properties of Carbocysteine as a Strategy in COVID-19 Therapy
Mucolytic and Antioxidant Properties of Carbocysteine as a Strategy in COVID-19 Therapy Abstract Abstract SARS-CoV-2 infection leads to a heterogenous spectrum of clinical conditions ranging from self-limiting upper airway infection to severe respiratory failure. Carbocysteine is a thioether mucolytic with antioxidant ...
PMC9636110
core_pubmed_pmc
Glycerosomal thermosensitive in situ gel of duloxetine HCl as a novel nanoplatform for rectal delivery: in vitro optimization and in vivo appraisal
Glycerosomal thermosensitive in situ gel of duloxetine HCl as a novel nanoplatform for rectal delivery: in vitro optimization and in vivo appraisal Abstract Duloxetine HCl (DXH) is a reuptake inhibitor of serotonin and norepinephrine used to treat the major depressive disorder. Following its extensive hepatic metabolis...
PMC9541024
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic modeling of ketoprofen and flunixin at piglet castration and tail‐docking
Pharmacokinetic/pharmacodynamic modeling of ketoprofen and flunixin at piglet castration and tail‐docking Abstract Abstract This study performed population‐pharmacokinetic/pharmacodynamic (pop‐PK/PD) modeling of ketoprofen and flunixin in piglets undergoing routine castration and tail‐docking, utilizing previously publ...
PMC10985247
core_pubmed_pmc
Case report: Avoiding intolerance to antipsychotics through a personalized treatment approach based on pharmacogenetics
Case report: Avoiding intolerance to antipsychotics through a personalized treatment approach based on pharmacogenetics Abstract Introduction The standard approach to treatment in psychiatry is known as “treatment as usual” (TAU), in which the same types of treatment are administered to a group of patients. TAU often r...
PMC12030250
core_pubmed_pmc
Comprehensive Phytochemical, Antioxidant, and Antibacterial Analysis of Vitex agnus-castus L. Essential Oil (VACEO): Insights from ADMET and Molecular Docking Studies
Comprehensive Phytochemical, Antioxidant, and Antibacterial Analysis of Vitex agnus-castus L. Essential Oil (VACEO): Insights from ADMET and Molecular Docking Studies Abstract Abstract Background/Objectives: The phytochemical composition, antioxidant, and antibacterial properties of Vitex agnus-castus L. essential oil ...
PMC11201171
core_pubmed_pmc
Antibiotic Treatment of Carbapenem-Resistant Acinetobacter baumannii Infections in View of the Newly Developed β-Lactams: A Narrative Review of the Existing Evidence
Antibiotic Treatment of Carbapenem-Resistant Acinetobacter baumannii Infections in View of the Newly Developed β-Lactams: A Narrative Review of the Existing Evidence Abstract It is estimated that antimicrobial resistance (AMR) is responsible for nearly 5 million human deaths worldwide each year and will reach 10 millio...
PMC10295334
core_pubmed_pmc
Altered Pharmacokinetics Parameters of Vancomycin in Patients with Hematological Malignancy with Febrile Neutropenia, a Bayesian Software Estimation
Altered Pharmacokinetics Parameters of Vancomycin in Patients with Hematological Malignancy with Febrile Neutropenia, a Bayesian Software Estimation Abstract The pharmacokinetics of vancomycin vary significantly between specific groups of patients, such as critically ill patients and patients with hematological maligna...
PMC7580200
core_pubmed_pmc
A Phase I, Randomized, Single-Dose Study to Evaluate the Biosimilarity of QL1206 to Denosumab Among Chinese Healthy Subjects
A Phase I, Randomized, Single-Dose Study to Evaluate the Biosimilarity of QL1206 to Denosumab Among Chinese Healthy Subjects Abstract Objective This study was conducted to explore the tolerance, variability, pharmacokinetics (PK), and pharmacodynamics (PD) of denosumab biosimilar (QL1206) in healthy Chinese subjects. M...
PMC12057627
core_pubmed_pmc
Prediction of High-Dose Methotrexate Blood Concentration in Osteosarcoma Patients Using Machine Learning
Prediction of High-Dose Methotrexate Blood Concentration in Osteosarcoma Patients Using Machine Learning Abstract Abstract Introduction High-dose methotrexate is a typical chemotherapy that is widely used in the treatment of osteosarcoma. However, the unique dose-response relationship of methotrexate makes its treatmen...
PMC7492636
core_pubmed_pmc
Virtual Lobule Models Are the Key for Multiscale Biomechanical and Pharmacological Modeling for the Liver
Virtual Lobule Models Are the Key for Multiscale Biomechanical and Pharmacological Modeling for the Liver Modeling Multi-Dimensional Models for Hepatic Circulation Different mathematical/computational techniques are used for modeling the hepatic blood flow. When subject-specific vascular information are essential, for ...
PMC4065283
core_pubmed_pmc
The SGLT2 Inhibitor Empagliflozin for the Treatment of Type 2 Diabetes Mellitus: a Bench to Bedside Review
The SGLT2 Inhibitor Empagliflozin for the Treatment of Type 2 Diabetes Mellitus: a Bench to Bedside Review Abstract Introduction The treatment of type 2 diabetes mellitus (T2DM) continues to pose challenges for clinicians and patients. The dramatic rise in T2DM prevalence, which has paralleled the rise in obesity, has ...
PMC8827224
core_pubmed_pmc
Current State and Principles of Basal Insulin Therapy in Type 2 Diabetes
Current State and Principles of Basal Insulin Therapy in Type 2 Diabetes Abstract Treatment with basal insulins is a fundamental part of management in many patients with type 2 diabetes mellitus. Multiple management schemes may be indicated in these individuals, for example, the use of oral antihyperglycemic agents wit...
PMC5723698
core_pubmed_pmc
Modeling of prolactin response following dopamine D 2 receptor antagonists in rats: can it be translated to clinical dosing?
Modeling of prolactin response following dopamine D 2 receptor antagonists in rats: can it be translated to clinical dosing? Abstract Abstract Prolactin release is a side effect of antipsychotic therapy with dopamine antagonists, observed in rats as well as humans. We examined whether two semimechanistic models could d...
PMC11962723
core_pubmed_pmc
Development and validation of the HPLC–MS/MS method and its application to the pharmacokinetic study for the Mongolian drug Sendeng-4 in rat blood plasma
Development and validation of the HPLC–MS/MS method and its application to the pharmacokinetic study for the Mongolian drug Sendeng-4 in rat blood plasma Abstract Abstract Abstract Sendeng-4 is a Mongolian drug. The Mongolian people have been using it to treat rheumatoid arthritis. At present, an increasing number of H...
PMC9931972
core_pubmed_pmc
Single-Dose Pharmacokinetics and Metabolism of the Oral Decongestant Phenylephrine HCl in Children and Adolescents
Single-Dose Pharmacokinetics and Metabolism of the Oral Decongestant Phenylephrine HCl in Children and Adolescents Abstract Introduction Pediatric data for phenylephrine, a decongestant used in cold medicines, are limited. This study characterized the pharmacokinetics and metabolism of phenylephrine HCl in children age...
PMC8300652
core_pubmed_pmc
Synergistic Meropenem/Vaborbactam Plus Fosfomycin Treatment of KPC Producing K. pneumoniae Septic Thrombosis Unresponsive to Ceftazidime/Avibactam: From the Bench to the Bedside
Synergistic Meropenem/Vaborbactam Plus Fosfomycin Treatment of KPC Producing K. pneumoniae Septic Thrombosis Unresponsive to Ceftazidime/Avibactam: From the Bench to the Bedside Abstract Abstract Gram-negative bacilli septic thrombosis (GNB-ST) represents a subtle and often misleading condition, potentially fatal if no...
PMC5849680
core_pubmed_pmc
Use of quercetin in animal feed: effects on the P-gp expression and pharmacokinetics of orally administrated enrofloxacin in chicken
Use of quercetin in animal feed: effects on the P-gp expression and pharmacokinetics of orally administrated enrofloxacin in chicken Abstract Abstract Modulation of P-glycoprotein (P-gp, encoded by Mdr1) by xenobiotics plays central role in pharmacokinetics of various drugs. Quercetin has a potential to modulate P-gp i...
PMC7037984
core_pubmed_pmc
Comprehensive Investigation of Moringa oleifera from Different Regions by Simultaneous Determination of 11 Polyphenols Using UPLC-ESI-MS/MS
Comprehensive Investigation of Moringa oleifera from Different Regions by Simultaneous Determination of 11 Polyphenols Using UPLC-ESI-MS/MS Abstract In this study, we develop and validate a simultaneous quantification of polyphenols method based on an ultra-performance liquid chromatography-electrospray ionization-tand...
PMC7927064
core_pubmed_pmc
Shared IVIVR for Five Commercial Enabling Formulations Using the BiPHa+ Biphasic Dissolution Assay
Shared IVIVR for Five Commercial Enabling Formulations Using the BiPHa+ Biphasic Dissolution Assay Abstract The present study intended to confirm the in vivo relevance of the BiPHa+ biphasic dissolution assay using a single set of assay parameters. Herein, we evaluated five commercial drug products formulated by variou...
PMC5591798
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Lysergic Acid Diethylamide in Healthy Subjects
Pharmacokinetics and Pharmacodynamics of Lysergic Acid Diethylamide in Healthy Subjects Abstract Abstract Background and Objective Lysergic acid diethylamide (LSD) is used recreationally and in clinical research. The aim of the present study was to characterize the pharmacokinetics and exposure–response relationship of...
PMC8740502
core_pubmed_pmc
Individual Pharmacotherapy Management (IPM) - I: a group-matched retrospective controlled clinical study on prevention of complicating delirium in the elderly trauma patients and identification of associated factors
Individual Pharmacotherapy Management (IPM) - I: a group-matched retrospective controlled clinical study on prevention of complicating delirium in the elderly trauma patients and identification of associated factors Abstract Background Delirium is one of the most frequent complications in hospitalized elderly patients ...
PMC9457551
core_pubmed_pmc
Anticancer Drugs: Recent Strategies to Improve Stability Profile, Pharmacokinetic and Pharmacodynamic Properties
Anticancer Drugs: Recent Strategies to Improve Stability Profile, Pharmacokinetic and Pharmacodynamic Properties Abstract In past decades, anticancer research has led to remarkable results despite many of the approved drugs still being characterized by high systemic toxicity mainly due to the lack of tumor selectivity ...
PMC3762314
core_pubmed_pmc
Pharmacokinetics of Uridine Following Ocular, Oral and Intravenous Administration in Rabbits
Pharmacokinetics of Uridine Following Ocular, Oral and Intravenous Administration in Rabbits Abstract The pyrimidine nucleoside uridine has recently been reported to have a protective effect on cultured human corneal epithelial cells, in an animal model of dry eye and in patients. In this study, we investigate the phar...
PMC9229108
core_pubmed_pmc
Seafood Paramyosins as Sources of Anti-Angiotensin-Converting-Enzyme and Anti-Dipeptidyl-Peptidase Peptides after Gastrointestinal Digestion: A Cheminformatic Investigation
Seafood Paramyosins as Sources of Anti-Angiotensin-Converting-Enzyme and Anti-Dipeptidyl-Peptidase Peptides after Gastrointestinal Digestion: A Cheminformatic Investigation Abstract Abstract Paramyosins, muscle proteins occurring exclusively in invertebrates, are abundant in seafoods. The potential of seafood paramyosi...
PMC12477080
core_pubmed_pmc
Polychlorinated biphenyls (PCBs) interact with drug metabolism in vivo
Polychlorinated biphenyls (PCBs) interact with drug metabolism in vivo Abstract Abstract Polychlorinated biphenyls (PCBs) are widespread environmental contaminants that interfere with xenobiotic metabolism, primarily by modulating cytochrome P450 (CYP) enzymes. However, their pharmacokinetic consequences in exposed ind...
PMC12738446
core_pubmed_pmc
AI-powered in silico twins: redefining precision medicine through simulation, personalization, and predictive healthcare
AI-powered in silico twins: redefining precision medicine through simulation, personalization, and predictive healthcare Abstract In silico twins (ISTs) are emerging as a transformative paradigm in precision medicine, offering dynamic, high-fidelity representations of individual patients through real-time integration o...
PMC8728677
core_pubmed_pmc
Absence of exaggerated pharmacology by recombinant ADAMTS13 in the rat and monkey
Absence of exaggerated pharmacology by recombinant ADAMTS13 in the rat and monkey Abstract Insufficiency of ADAMTS13 (a disintegrin and metalloprotease with thrombospondin motif repeats-13) is the cause of thrombotic thrombocytopenic purpura (TTP) and contributes in microangiopathy in sickle cell disease (SCD). Recombi...
PMC11378297
core_pubmed_pmc
Discovery and Profiling of New Multimodal Phenylglycinamide Derivatives as Potent Antiseizure and Antinociceptive Drug Candidates
Discovery and Profiling of New Multimodal Phenylglycinamide Derivatives as Potent Antiseizure and Antinociceptive Drug Candidates Abstract We developed a focused series of original phenyl-glycinamide derivatives which showed potent activity across in vivo mouse seizure models, namely, maximal electroshock (MES) and 6 H...
PMC4773999
core_pubmed_pmc
SaMpling Antibiotics in Renal Replacement Therapy (SMARRT): an observational pharmacokinetic study in critically ill patients
SaMpling Antibiotics in Renal Replacement Therapy (SMARRT): an observational pharmacokinetic study in critically ill patients Abstract Abstract Background Optimal antibiotic dosing is key to maximising patient survival, and minimising the emergence of bacterial resistance. Evidence-based antibiotic dosing guidelines fo...
PMC3787017
core_pubmed_pmc
Relative Contributions of Norepinephrine and Serotonin Transporters to Antinociceptive Synergy between Monoamine Reuptake Inhibitors and Morphine in the Rat Formalin Model
Relative Contributions of Norepinephrine and Serotonin Transporters to Antinociceptive Synergy between Monoamine Reuptake Inhibitors and Morphine in the Rat Formalin Model Abstract Multimodal analgesia is designed to optimize pain relief by coadministering drugs with distinct mechanisms of action or by combining multip...
PMC12670153
core_pubmed_pmc
Piperacillin dosing in pediatric patients and augmented renal clearance: are current guidelines sufficient to achieve therapeutic concentration coverage?
Piperacillin dosing in pediatric patients and augmented renal clearance: are current guidelines sufficient to achieve therapeutic concentration coverage? Abstract Abstract Background Appropriate dosing of piperacillin/tazobactam is crucial for hospitalized children and might be a challenge in case of augmented renal cl...
PMC12292318
core_pubmed_pmc
The Impact of PET Imaging on Translational Medicine: Insights from Large-Animal Disease Models
The Impact of PET Imaging on Translational Medicine: Insights from Large-Animal Disease Models Abstract Large-animal models are playing a pivotal role in bridging the translational research gap. Positron emission tomography (PET) imaging is preferred in disease research involving large-animal models. Its ability to non...
PMC7318178
core_pubmed_pmc
Bioavailability of Triprolidine as a Single Agent or in Combination With Pseudoephedrine: A Randomized, Open‐Label Crossover Study in Healthy Volunteers
Bioavailability of Triprolidine as a Single Agent or in Combination With Pseudoephedrine: A Randomized, Open‐Label Crossover Study in Healthy Volunteers Abstract Abstract Antihistamines have been in clinical use for more than 70 years to treat allergic and nonallergic symptoms including relief from cold and flu symptom...
PMC8416862
core_pubmed_pmc
Effect of Oral Semaglutide on the Pharmacokinetics of Levonorgestrel and Ethinylestradiol in Healthy Postmenopausal Women and Furosemide and Rosuvastatin in Healthy Subjects
Effect of Oral Semaglutide on the Pharmacokinetics of Levonorgestrel and Ethinylestradiol in Healthy Postmenopausal Women and Furosemide and Rosuvastatin in Healthy Subjects Abstract Background The first oral glucagon-like peptide-1 receptor agonist (GLP-1RA) comprises semaglutide co-formulated with the absorption enha...
PMC6618047
core_pubmed_pmc
Effect of Food on the Pharmacokinetics of Ertugliflozin and Its Fixed‐Dose Combinations Ertugliflozin/Sitagliptin and Ertugliflozin/Metformin
Effect of Food on the Pharmacokinetics of Ertugliflozin and Its Fixed‐Dose Combinations Ertugliflozin/Sitagliptin and Ertugliflozin/Metformin Abstract Abstract Ertugliflozin, an inhibitor of sodium‐glucose cotransporter 2, is approved in the United States and European Union for the treatment of type 2 diabetes in adult...
PMC8980709
core_pubmed_pmc
Understanding Pharmaco-Epigenomic Response of Antipsychotic Drugs Using Genome-Wide MicroRNA Expression Profile in Liver Cell Line
Understanding Pharmaco-Epigenomic Response of Antipsychotic Drugs Using Genome-Wide MicroRNA Expression Profile in Liver Cell Line Abstract Interindividual variability in drug response is a major concern among patients undergoing antipsychotic drug treatment. Apart from genetic and physiological factors, this variabili...
PMC9783783
core_pubmed_pmc
Effects of Isosakuranetin on Pharmacokinetic Changes of Tofacitinib in Rats with N -Dimethylnitrosamine-Induced Liver Cirrhosis
Effects of Isosakuranetin on Pharmacokinetic Changes of Tofacitinib in Rats with N -Dimethylnitrosamine-Induced Liver Cirrhosis Abstract Tofacitinib, a Janus kinase 1 and 3 inhibitor, is used to treat rheumatoid arthritis. It is mainly metabolized by the cytochromes p450 (CYP) 3A1/2 and CYP2C11 in the liver. Chronic in...
PMC12041135
core_pubmed_pmc
Leveraging Clinical Data to Enhance the Performance Evaluation of Ceftriaxone Population Pharmacokinetic Models in Children
Leveraging Clinical Data to Enhance the Performance Evaluation of Ceftriaxone Population Pharmacokinetic Models in Children Abstract Abstract Introduction Sepsis affects approximately 8% of pediatric intensive care unit (PICU) admissions in high-income countries. Ceftriaxone, a broad-spectrum beta-lactam antibiotic, is...
PMC10051811
core_pubmed_pmc
Plasma and Cerebrospinal Fluid Concentrations of Micafungin Administered at High Doses in Critically Ill Infants with Systemic Candidiasis: A Pooled Analysis of Two Studies
Plasma and Cerebrospinal Fluid Concentrations of Micafungin Administered at High Doses in Critically Ill Infants with Systemic Candidiasis: A Pooled Analysis of Two Studies Abstract Background : Neonates may require higher doses of micafungin than adults to reach the therapeutic effect for increased plasma clearance. O...
PMC8862763
core_pubmed_pmc
Perioperative Low Dose Dexmedetomidine and Its Effect on the Visibility of the Surgical Field for Middle Ear Microsurgery: A Randomised Controlled Trial
Perioperative Low Dose Dexmedetomidine and Its Effect on the Visibility of the Surgical Field for Middle Ear Microsurgery: A Randomised Controlled Trial Abstract Abstract Background and Purpose: There are many benefits of administering dexmedetomidine perioperatively. The pharmacokinetics (PK) and pharmacodynamics (PD)...
PMC7914087
core_pubmed_pmc
Preclinical Evaluation of Safety, Pharmacokinetics, Efficacy, and Mechanism of Radioprotective Agent HL-003
Preclinical Evaluation of Safety, Pharmacokinetics, Efficacy, and Mechanism of Radioprotective Agent HL-003 Abstract Abstract Amifostine is a radioprotector with high efficacy but poor safety, short half-life, no oral formulation, and poor compliance, which limits its application. With the increasing risk of exposure t...
PMC10943176
core_pubmed_pmc
Preclinical metabolism and the disposition of vornorexant/TS‐142, a novel dual orexin 1/2 receptor antagonist for the treatment of insomnia
Preclinical metabolism and the disposition of vornorexant/TS‐142, a novel dual orexin 1/2 receptor antagonist for the treatment of insomnia Abstract Abstract We investigated the metabolism and disposition of vornorexant, a novel dual orexin receptor antagonist, in rats and dogs, and clarified in vitro metabolite profil...
PMC4150275
core_pubmed_pmc
Phase I study and preclinical efficacy evaluation of the mTOR inhibitor sirolimus plus gemcitabine in patients with advanced solid tumours
Phase I study and preclinical efficacy evaluation of the mTOR inhibitor sirolimus plus gemcitabine in patients with advanced solid tumours Abstract Abstract Background: We conducted a phase I study in patients with advanced solid tumours to identify the recommended dose, assess pharmacokinetics (PK), pharmacodynamic ac...
PMC12863543
core_pubmed_pmc
In-silico identification of anti-cholera phytochemicals from Indian medicinal plants
In-silico identification of anti-cholera phytochemicals from Indian medicinal plants Abstract Cholera is a severe diarrheal disease caused by ingestion of food or water contaminated with pathogenic Vibrio cholerae . Treatment for cholera includes rehydration therapy and antibiotics to avert death and reduce bacterial b...
PMC10149412
core_pubmed_pmc
Current microfluidic platforms for reverse engineering of cornea
Current microfluidic platforms for reverse engineering of cornea Abstract According to the World Health Organization, corneal blindness constitutes 5.1% of global blindness population. Surgical outcomes have been improved significantly in the treatment of corneal blindness. However, corneal transplantation is limited b...
PMC9283739
core_pubmed_pmc
Dexamethasone exposure in normal‐weight and obese hospitalized COVID ‐19 patients: An observational exploratory trial
Dexamethasone exposure in normal‐weight and obese hospitalized COVID ‐19 patients: An observational exploratory trial Abstract Abstract During the latest pandemic, the RECOVERY study showed the benefits of dexamethasone (DEX) use in COVID‐19 patients. Obesity has been proven to be an independent risk factor for severe ...
PMC7343737
core_pubmed_pmc
In vitro and In vivo Assessment of Suitable Reference Region and Kinetic Modelling for the mGluR1 Radioligand [ 11 C]ITDM in Mice
In vitro and In vivo Assessment of Suitable Reference Region and Kinetic Modelling for the mGluR1 Radioligand [ 11 C]ITDM in Mice Abstract Abstract Purpose This study aimed at investigating binding specificity, suitability of reference region-based kinetic modelling, and pharmacokinetics of the metabotropic glutamate r...
PMC6497849
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic study of posaconazole delayed-release tablet in a patient with coexisting invasive aspergillosis and mucormycosis
Pharmacokinetic/pharmacodynamic study of posaconazole delayed-release tablet in a patient with coexisting invasive aspergillosis and mucormycosis Abstract Abstract Limited information exists regarding the optimal dose of posaconazole delayed-release tablet for the treatment of invasive mold infection. Here, we report t...
PMC10832600
core_pubmed_pmc
Effect of albumin substitution on pharmacokinetics of piperacillin/tazobactam in patients with severe burn injury admitted to the ICU
Effect of albumin substitution on pharmacokinetics of piperacillin/tazobactam in patients with severe burn injury admitted to the ICU Abstract Abstract Background Pathophysiological changes in severely burned patients alter the pharmacokinetics (PK) of anti-infective agents, potentially leading to subtherapeutic concen...
PMC10610256
core_pubmed_pmc
Development and Preclinical Evaluation of [ 68 Ga]BMSH as a New Potent Positron Emission Tomography Tracer for Imaging Programmed Death-Ligand 1 Expression
Development and Preclinical Evaluation of [ 68 Ga]BMSH as a New Potent Positron Emission Tomography Tracer for Imaging Programmed Death-Ligand 1 Expression Abstract Abstract Immunotherapy targeting the programmed death-ligand 1 (PD-L1)/programmed cell death protein 1 (PD-1) pathway has shown remarkable efficacy against...
PMC11533096
core_pubmed_pmc
Characterization of mavacamten pharmacokinetics in patients with hypertrophic cardiomyopathy to inform dose titration
Characterization of mavacamten pharmacokinetics in patients with hypertrophic cardiomyopathy to inform dose titration Abstract Abstract Mavacamten is a selective, allosteric, reversible cardiac myosin inhibitor that has been developed for the treatment of adults with symptomatic obstructive hypertrophic cardiomyopathy ...
PMC7106981
core_pubmed_pmc
Understanding the Role of Comparative Clinical Studies in the Development of Oncology Biosimilars
Understanding the Role of Comparative Clinical Studies in the Development of Oncology Biosimilars Abstract Abstract Biosimilars have the potential to broaden patient access to biologics and provide cost savings for health care systems. During the development of a biosimilar, data that directly compare the proposed bios...
PMC3608328
core_pubmed_pmc
Development and validation of ultra-performance liquid chromatographic method with tandem mass spectrometry for determination of lenalidomide in rabbit and human plasma
Development and validation of ultra-performance liquid chromatographic method with tandem mass spectrometry for determination of lenalidomide in rabbit and human plasma Abstract Abstract Background Lenalidomide (LND) is a potent novel thalidomide analog which demonstrated remarkable clinical activity in treatment of mu...
PMC6996485
core_pubmed_pmc
Comparative Pharmacokinetics, Bioequivalence and Safety Study of Two Recombinant Human Chorionic Gonadotropin Injections in Healthy Chinese Subjects
Comparative Pharmacokinetics, Bioequivalence and Safety Study of Two Recombinant Human Chorionic Gonadotropin Injections in Healthy Chinese Subjects Abstract Abstract Objective To evaluate the pharmacokinetics (PK), bioequivalence and safety profile of the recombinant human chorionic gonadotropin (r-hCG) injection form...
PMC4392787
core_pubmed_pmc
Pharmacokinetics of nalbuphine hydrochloride extended release tablets in hemodialysis patients with exploratory effect on pruritus
Pharmacokinetics of nalbuphine hydrochloride extended release tablets in hemodialysis patients with exploratory effect on pruritus Abstract Abstract Background Uremic pruritus is a common and deleterious condition among hemodialysis (HD) patients. Central gating of μ/κ opiate circuitry plays an important role in mediat...
PMC8849072
core_pubmed_pmc
Sudapyridine (WX-081), a Novel Compound against Mycobacterium tuberculosis
Sudapyridine (WX-081), a Novel Compound against Mycobacterium tuberculosis Abstract ABSTRACT Bedaquiline (BDQ) was historically listed by the World Health Organization (WHO) in 2018 as the preferred option for rifampin-resistant tuberculosis (RR-TB) and multidrug-resistant tuberculosis (MDR-TB). However, when there is ...
PMC11768268
core_pubmed_pmc
Gestational Diabetes Mellitus Does Not Change the Pharmacokinetics and Transplacental Distribution of Fluoxetine and Norfluoxetine Enantiomers
Gestational Diabetes Mellitus Does Not Change the Pharmacokinetics and Transplacental Distribution of Fluoxetine and Norfluoxetine Enantiomers Abstract Background/Objectives : Fluoxetine (FLX) is the inhibitor of serotonin reuptake most prescribed in pregnant women with depression. This study evaluates the influence of...
PMC6682857
core_pubmed_pmc
Pharmacokinetic and exposure–response analysis of pertuzumab in patients with HER2-positive metastatic gastric or gastroesophageal junction cancer
Pharmacokinetic and exposure–response analysis of pertuzumab in patients with HER2-positive metastatic gastric or gastroesophageal junction cancer Abstract Purpose To characterize the pharmacokinetics (PK) of pertuzumab and trastuzumab in patients with HER2-positive metastatic gastric or gastroesophageal junction cance...
PMC12108214
core_pubmed_pmc
Navigating Vancomycin and Acute Kidney Injury: AUC- vs. Trough-Guided Monitoring in Initial and Steady-State Therapy
Navigating Vancomycin and Acute Kidney Injury: AUC- vs. Trough-Guided Monitoring in Initial and Steady-State Therapy Abstract Background/Objectives : Vancomycin, a glycopeptide antibiotic used for gram-positive infections, is associated with acute kidney injury (AKI). Therapeutic drug monitoring (TDM) is recommended to...
PMC12350473
core_pubmed_pmc
Pharmacokinetics and brain tissue distribution of Gastrodia elata extract in normal and cerebral ischemic rats: a comparative study
Pharmacokinetics and brain tissue distribution of Gastrodia elata extract in normal and cerebral ischemic rats: a comparative study Abstract Objective This study systematically investigated the pharmacokinetic characteristics, cerebral distribution, and metabolic transformation of Gastrodia elata components in both hea...
PMC11592097
core_pubmed_pmc
Recent Updates of PET in Lymphoma: FDG and Beyond
Recent Updates of PET in Lymphoma: FDG and Beyond Abstract Abstract Lymphoma is one of the most common cancers worldwide, categorized into Hodgkin lymphoma and non-Hodgkin lymphoma. 18 F-fluorodeoxyglucose positron emission tomography (FDG PET) has become an essential imaging tool for evaluating patients with lymphoma ...
PMC5702381
core_pubmed_pmc
Pharmacokinetic Evaluation of the Interactions of Amenamevir (ASP2151) with Ketoconazole, Rifampicin, Midazolam, and Warfarin in Healthy Adults
Pharmacokinetic Evaluation of the Interactions of Amenamevir (ASP2151) with Ketoconazole, Rifampicin, Midazolam, and Warfarin in Healthy Adults Abstract Abstract Introduction Amenamevir is a nonnucleoside antiherpes virus compound available for treating herpes zoster infections. Four studies aimed to determine any pote...
PMC3642742
core_pubmed_pmc
Anesthetic drug development: Novel drugs and new approaches
Anesthetic drug development: Novel drugs and new approaches Abstract Abstract The ideal sedative–hypnotic drug would be a rapidly titratable intravenous agent with a high therapeutic index and minimal side effects. The current efforts to develop such agents are primarily focused on modifying the structures of existing ...
PMC12580768
core_pubmed_pmc
Izalontamab (SI-B001), a Novel EGFRxHER3 Bispecific Antibody in Patients with Locally Advanced or Metastatic Epithelial Tumor: Results from First-in-Human Phase I/Ib Study
Izalontamab (SI-B001), a Novel EGFRxHER3 Bispecific Antibody in Patients with Locally Advanced or Metastatic Epithelial Tumor: Results from First-in-Human Phase I/Ib Study Abstract Abstract Purpose: Izalontamab (SI-B001) is a novel EGFR×HER3 bispecific antibody. This first-in-human phase I study presents the safety and...
PMC4122185
core_pubmed_pmc
Novel artificial cell microencapsulation of a complex gliclazide-deoxycholic bile acid formulation: a characterization study
Novel artificial cell microencapsulation of a complex gliclazide-deoxycholic bile acid formulation: a characterization study Abstract Abstract Gliclazide (G) is an antidiabetic drug commonly used in type 2 diabetes. It has extrapancreatic hypoglycemic effects, which makes it a good candidate in type 1 diabetes (T1D). I...
PMC10760220
core_pubmed_pmc
Computational identification of potential modulators of heme-regulated inhibitor (HRI) for pharmacological intervention against sickle cell disease
Computational identification of potential modulators of heme-regulated inhibitor (HRI) for pharmacological intervention against sickle cell disease Abstract Abstract Background Sickle cell disease (SCD) poses a significant health challenge and therapeutic approaches often target fetal hemoglobin (HbF) to ameliorate sym...
PMC4068454
core_pubmed_pmc
Pharmacokinetic Interactions between Primaquine and Chloroquine
Pharmacokinetic Interactions between Primaquine and Chloroquine Abstract Abstract Chloroquine combined with primaquine has been the standard radical curative regimen for Plasmodium vivax and Plasmodium ovale malaria for over half a century. In an open-label crossover pharmacokinetic study, 16 healthy volunteers (4 male...
PMC9786617
core_pubmed_pmc
Time to Rethink the Current Paradigm for Assessing Kidney Function in Drug Development and Beyond
Time to Rethink the Current Paradigm for Assessing Kidney Function in Drug Development and Beyond Abstract Abstract Chronic kidney disease (CKD) is an important health issue that affects ~ 9.1% of the world adult population. Serum creatinine is the most commonly used biomarker for assessing kidney function and is utili...
PMC7588843
core_pubmed_pmc
Azacarbazole n-3 and n-6 polyunsaturated fatty acids ethyl esters nanoemulsion with enhanced efficacy against Plasmodium falciparum
Azacarbazole n-3 and n-6 polyunsaturated fatty acids ethyl esters nanoemulsion with enhanced efficacy against Plasmodium falciparum Abstract Alternative therapies are necessary for the treatment of malaria due to emerging drug resistance. However, many promising antimalarial compounds have poor water solubility and suf...
PMC4263903
core_pubmed_pmc
Is Dosing of Therapeutic Immunoglobulins Optimal? A Review of a Three-Decade Long Debate in Europe
Is Dosing of Therapeutic Immunoglobulins Optimal? A Review of a Three-Decade Long Debate in Europe Abstract The consumption of immunoglobulins (Ig) is increasing due to better recognition of antibody deficiencies, an aging population, and new indications. This review aims to examine the various dosing regimens and rese...
PMC8604216
core_pubmed_pmc
Evaluation of moxifloxacin in canine and non‐human primate telemetry assays: Comparison of QTc interval prolongation by timepoint and concentration‐QTc analysis
Evaluation of moxifloxacin in canine and non‐human primate telemetry assays: Comparison of QTc interval prolongation by timepoint and concentration‐QTc analysis Abstract Abstract The in vivo correct QT (QTc) assay is used by the pharmaceutical industry to characterize the potential for delayed ventricular repolarizatio...
PMC6834678
core_pubmed_pmc
An engineered human Fc domain that behaves like a pH-toggle switch for ultra-long circulation persistence
An engineered human Fc domain that behaves like a pH-toggle switch for ultra-long circulation persistence Abstract Abstract The pharmacokinetic properties of antibodies are largely dictated by the pH-dependent binding of the IgG fragment crystallizable (Fc) domain to the human neonatal Fc receptor (hFcRn). Engineered F...
PMC4648050
core_pubmed_pmc
Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library
Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library Abstract Abstract A screen of a focused kinase inhibitor library against Trypanosoma brucei rhodesiense led to the identification of seven series, totaling 121 compounds, which showed >50 % inhibition at 5 μ m . Sc...
PMC4784132
core_pubmed_pmc
Pharmacodynamic and pharmacokinetic interaction of Panchagavya Ghrita with phenytoin and carbamazepine in maximal electroshock induced seizures in rats
Pharmacodynamic and pharmacokinetic interaction of Panchagavya Ghrita with phenytoin and carbamazepine in maximal electroshock induced seizures in rats Abstract Introduction: Traditionally, Panchagavya Ghrita (PG) has been used for the management of epilepsy, anxiety, fever and jaundice. It consists of five components ...
PMC12733353
core_pubmed_pmc
Gut Microbiota in the Regulation of Intestinal Drug Transporters: Molecular Mechanisms and Pharmacokinetic Implications
Gut Microbiota in the Regulation of Intestinal Drug Transporters: Molecular Mechanisms and Pharmacokinetic Implications Abstract Abstract Gut microbiota, through both its species composition and its metabolites, impacts expression and activity of intestinal drug transporters. This phenomenon directly affects absorption...
PMC10056758
core_pubmed_pmc
pH-Responsive and Mucoadhesive Nanoparticles for Enhanced Oral Insulin Delivery: The Effect of Hyaluronic Acid with Different Molecular Weights
pH-Responsive and Mucoadhesive Nanoparticles for Enhanced Oral Insulin Delivery: The Effect of Hyaluronic Acid with Different Molecular Weights Abstract Abstract Drug degradation at low pH and rapid clearance from intestinal absorption sites are the main factors limiting the development of oral macromolecular delivery ...
PMC10417386
core_pubmed_pmc
The Use of Parenteral Opioids in Cancer Pain Management
The Use of Parenteral Opioids in Cancer Pain Management Abstract Abstract Simple Summary There are some clinical circumstances that require the parenteral administration of opioids, as an alternative to the oral route. A parenteral route of administration is often indicated in patients with severe pain intensity requir...
PMC8585766
core_pubmed_pmc
Limitations of Antibiotic MIC-Based PK-PD Metrics: Looking Back to Move Forward
Limitations of Antibiotic MIC-Based PK-PD Metrics: Looking Back to Move Forward Abstract Within a few years after the first successful clinical use of penicillin, investigations were conducted in animal infection models to explore a range of factors that were considered likely to influence the antibacterial response to...
PMC10431043
core_pubmed_pmc
Physiologically‐based pharmacokinetic pharmacodynamic parent‐metabolite model of edoxaban to predict drug–drug‐disease interactions: M4 contribution
Physiologically‐based pharmacokinetic pharmacodynamic parent‐metabolite model of edoxaban to predict drug–drug‐disease interactions: M4 contribution Abstract Abstract This study aimed to develop a physiologically‐based pharmacokinetic pharmacodynamic (PBPK/PD) parent‐metabolite model of edoxaban, an oral anticoagulant ...
PMC10766057
core_pubmed_pmc
Predictability of human exposure by human‐CYP3A4‐transgenic mouse models: A meta‐analysis
Predictability of human exposure by human‐CYP3A4‐transgenic mouse models: A meta‐analysis Abstract Abstract First‐in‐human dose predictions are primarily based on no‐observed‐adverse‐effect levels in animal studies. Predictions from these animal models are only as effective as their ability to predict human results. To...
PMC11904003
core_pubmed_pmc
Recent insights on phage therapy against multidrug-resistant Acinetobacter baumannii
Recent insights on phage therapy against multidrug-resistant Acinetobacter baumannii Abstract Abstract Acinetobacter baumannii is a prevalent clinical pathogen commonly found to be multidrug-resistant (MDR), causing serious to life-threatening infections, particularly hospital-acquired infections with limited therapeut...
PMC10788265
core_pubmed_pmc
Effects of chitooligosaccharide on the in vitro antibacterial activity against avian Escherichia coli and the pharmacokinetics of florfenicol in healthy chickens
Effects of chitooligosaccharide on the in vitro antibacterial activity against avian Escherichia coli and the pharmacokinetics of florfenicol in healthy chickens Abstract This study investigates the combined effects of chitooligosaccharide ( COS ) and florfenicol ( FLO ) on the inhibition of Escherichia coli in vitro, ...
PMC10144785
core_pubmed_pmc
Pharmacokinetics, Milk Residues, and Toxicological Evaluation of a Single High Dose of Meloxicam Administered at 30 mg/kg per os to Lactating Dairy Cattle
Pharmacokinetics, Milk Residues, and Toxicological Evaluation of a Single High Dose of Meloxicam Administered at 30 mg/kg per os to Lactating Dairy Cattle Abstract Simple Summary Pain control is a major concern for cattle producers, consumers, and veterinarians. There are currently no analgesic drugs labeled for pain c...