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PMC10431037
core_pubmed_pmc
Population pharmacokinetics of atacicept in systemic lupus erythematosus: An analysis of three clinical trials
Population pharmacokinetics of atacicept in systemic lupus erythematosus: An analysis of three clinical trials Abstract Abstract B cell stimulating factor (BLyS) and a proliferation‐inducing ligand (APRIL) are targets for novel treatments in patients with systemic lupus erythematosus (SLE). Atacicept is a recombinant, ...
PMC8146505
core_pubmed_pmc
Enantioselective Interactions of Anti-Infective 8-Aminoquinoline Therapeutics with Human Monoamine Oxidases A and B †
Enantioselective Interactions of Anti-Infective 8-Aminoquinoline Therapeutics with Human Monoamine Oxidases A and B † Abstract 8-Aminoquinolines (8-AQs) are an important class of anti-infective therapeutics. The monoamine oxidases (MAOs) play a key role in metabolism of 8-AQs. A major role for MAO-A in metabolism of pr...
PMC8079976
core_pubmed_pmc
Influence of ABCB1 Gene Polymorphism on Rivaroxaban Blood Concentration and Hemorrhagic Events in Patients With Atrial Fibrillation
Influence of ABCB1 Gene Polymorphism on Rivaroxaban Blood Concentration and Hemorrhagic Events in Patients With Atrial Fibrillation Abstract Background and Objectives: Genetic data on the pharmacokinetics of rivaroxaban and identification of factors that affect its biotransformation, distribution, and excretion will al...
PMC3829570
core_pubmed_pmc
Incorporating New Technologies Into Toxicity Testing and Risk Assessment: Moving From 21st Century Vision to a Data-Driven Framework
Incorporating New Technologies Into Toxicity Testing and Risk Assessment: Moving From 21st Century Vision to a Data-Driven Framework Abstract Abstract Based on existing data and previous work, a series of studies is proposed as a basis toward a pragmatic early step in transforming toxicity testing. These studies were a...
PMC4186727
core_pubmed_pmc
Pharmacokinetics of olanzapine long-acting injection: the clinical perspective
Pharmacokinetics of olanzapine long-acting injection: the clinical perspective Abstract Olanzapine long-acting injection (OLAI) is a sustained-release depot antipsychotic for the treatment of schizophrenia in adults. Our objective was to explain the pharmacokinetics of OLAI to provide clinical insight. Simulation model...
PMC9474474
core_pubmed_pmc
Determination of pharmacokinetics and tissue distribution of a novel lutetium-labeled PSMA-targeted ligand, 177 Lu-DOTA-PSMA-GUL, in rats by using LC–MS/MS
Determination of pharmacokinetics and tissue distribution of a novel lutetium-labeled PSMA-targeted ligand, 177 Lu-DOTA-PSMA-GUL, in rats by using LC–MS/MS Abstract Abstract Prostate specific membrane antigen (PSMA) is known to be overexpressed in prostate cancer cells, providing as a diagnostic and therapeutic target ...
PMC12001275
core_pubmed_pmc
Comparing Scientific Machine Learning With Population Pharmacokinetic and Classical Machine Learning Approaches for Prediction of Drug Concentrations
Comparing Scientific Machine Learning With Population Pharmacokinetic and Classical Machine Learning Approaches for Prediction of Drug Concentrations Abstract ABSTRACT A variety of classical machine learning (ML) approaches has been developed over the past decade aiming to individualize drug dosages based on measured p...
PMC5117905
core_pubmed_pmc
A prospective, observational study comparing the PK/PD relationships of generic Meropenem (Mercide ® ) to the innovator brand in critically ill patients
A prospective, observational study comparing the PK/PD relationships of generic Meropenem (Mercide ® ) to the innovator brand in critically ill patients Abstract Introduction Clinicians’ skepticism, fueled by evidence of inferiority of some multisource generic antimicrobial products, results in the underutilization of ...
PMC3603473
core_pubmed_pmc
Bridging Clinical Outcomes of Canakinumab Treatment in Patients With Rheumatoid Arthritis With a Population Model of IL-1β Kinetics
Bridging Clinical Outcomes of Canakinumab Treatment in Patients With Rheumatoid Arthritis With a Population Model of IL-1β Kinetics Abstract Canakinumab, an anti-interleukin-1β (IL-1β) monoclonal antibody, is approved for cryopyrin-associated periodic syndromes and is under investigation for the management of other inf...
PMC7918738
core_pubmed_pmc
Microtubule Destabilizing Sulfonamides as an Alternative to Taxane-Based Chemotherapy
Microtubule Destabilizing Sulfonamides as an Alternative to Taxane-Based Chemotherapy Abstract Pan-Gyn cancers entail 1 in 5 cancer cases worldwide, breast cancer being the most commonly diagnosed and responsible for most cancer deaths in women. The high incidence and mortality of these malignancies, together with the ...
PMC6709486
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Drug Interaction Potential of SPR741, an Intravenous Potentiator, after Single and Multiple Ascending Doses and When Combined with β-Lactam Antibiotics in Healthy Subjects
Safety, Tolerability, Pharmacokinetics, and Drug Interaction Potential of SPR741, an Intravenous Potentiator, after Single and Multiple Ascending Doses and When Combined with β-Lactam Antibiotics in Healthy Subjects Abstract SPR741 is a novel polymyxin B derivative, with minimal intrinsic antibacterial activity and red...
PMC2820465
core_pubmed_pmc
A phase 1 study evaluating the pharmacokinetics, safety and tolerability of repeat dosing with a human IL-13 antibody (CAT-354) in subjects with asthma
A phase 1 study evaluating the pharmacokinetics, safety and tolerability of repeat dosing with a human IL-13 antibody (CAT-354) in subjects with asthma Abstract Background IL-13 has been implicated in the development of airway inflammation and hyperresponsiveness. This study investigated the multiple-dose pharmacokinet...
PMC12327169
core_pubmed_pmc
Modeling Antibody Kinetics Post‐mRNA Booster Vaccination and Protection Durations Against SARS‐CoV‐2 Infection
Modeling Antibody Kinetics Post‐mRNA Booster Vaccination and Protection Durations Against SARS‐CoV‐2 Infection Abstract ABSTRACT Understanding the dynamics of SARS‐CoV‐2 antibody levels post‐booster vaccination is important to inform their durations of protection. Longitudinal antibody data was collected on the day of ...
PMC5866904
core_pubmed_pmc
Assessment of Liver Function Using Pharmacokinetic Parameters of Gd-EOB-DTPA: Experimental Study in Rat Hepatectomy Model
Assessment of Liver Function Using Pharmacokinetic Parameters of Gd-EOB-DTPA: Experimental Study in Rat Hepatectomy Model Abstract Objectives To determine whether the pharmacokinetic parameters of Gd-EOB-DTPA can identify the difference in liver function in a rat hepatectomy model. Methods A total of 56 eight-week-old ...
PMC11353013
core_pubmed_pmc
Computational Modeling of Drug Response Identifies Mutant-Specific Constraints for Dosing panRAF and MEK Inhibitors in Melanoma
Computational Modeling of Drug Response Identifies Mutant-Specific Constraints for Dosing panRAF and MEK Inhibitors in Melanoma Abstract Simple Summary Combining drugs is crucial for enhancing anti-cancer responses. However, the potential of pre-clinical data in identifying suitable combinations and dosage is often und...
PMC11176903
core_pubmed_pmc
A Gastroenterologist's guide to drug interactions of small molecules for inflammatory bowel disease
A Gastroenterologist's guide to drug interactions of small molecules for inflammatory bowel disease Abstract Abstract Small molecule drugs are becoming increasingly used in the treatment of inflammatory bowel diseases (IBD). However, unlike monoclonal antibody drugs, which have few interactions with other medications, ...
PMC6430597
core_pubmed_pmc
An experimental randomized study on the analgesic effects of pharmaceutical-grade cannabis in chronic pain patients with fibromyalgia
An experimental randomized study on the analgesic effects of pharmaceutical-grade cannabis in chronic pain patients with fibromyalgia Abstract Supplemental Digital Content is Available in the Text. This experimental highly controlled trial in 20 patients with fibromyalgia shows that the cannabinoid THC, but not CBD, is...
PMC11628858
core_pubmed_pmc
Nonalcoholic steatohepatitis increases plasma retention of sorafenib-glucuronide in a mouse model by altering hepatocyte hopping
Nonalcoholic steatohepatitis increases plasma retention of sorafenib-glucuronide in a mouse model by altering hepatocyte hopping Abstract Hepatocyte hopping is the hepatocyte-to-sinusoid-to-hepatocyte shuttling that increases the efficiency of hepatic elimination of xenobiotics. This phenomenon is mediated via efflux o...
PMC7779619
core_pubmed_pmc
Zonisamide for the Treatment of Parkinson Disease: A Current Update
Zonisamide for the Treatment of Parkinson Disease: A Current Update Abstract Abstract Zonisamide has been used as an add-on treatment in order to overcome the deficiencies of the general therapies currently used to resolve the motor complications and non-motor symptoms of Parkinson disease. Various trials have been des...
PMC3784056
core_pubmed_pmc
Use of Nicotinamide to Treat Hyperphosphatemia in Dialysis Patients
Use of Nicotinamide to Treat Hyperphosphatemia in Dialysis Patients Abstract Abstract Hyperphosphatemia in chronic kidney disease (CKD) has been associated with elevated cardiovascular morbidity and mortality. Serum phosphate control remains a cornerstone of the clinical management of patients with CKD, in order to bot...
PMC10653719
core_pubmed_pmc
High-Evidence, Actionable Phenotype Gene Distribution in a Multispecialty, Tertiary Care Clinic: Potentially Actionable Genes and a Referring Department Profile
High-Evidence, Actionable Phenotype Gene Distribution in a Multispecialty, Tertiary Care Clinic: Potentially Actionable Genes and a Referring Department Profile Abstract Abstract Background There has been a trend in recent years toward individualized medicine. Pharmacogenomics (PGx) is the use of patient-specific genet...
PMC8247418
core_pubmed_pmc
Effect of Food Intake on the Pharmacokinetics of the Selective Progesterone Receptor Modulator Vilaprisan: A Randomized Clinical Study in Healthy Postmenopausal Women
Effect of Food Intake on the Pharmacokinetics of the Selective Progesterone Receptor Modulator Vilaprisan: A Randomized Clinical Study in Healthy Postmenopausal Women Abstract Abstract This exploratory, open‐label, randomized, 3‐period crossover study in 12 healthy postmenopausal women investigated the effects of food ...
PMC7515941
core_pubmed_pmc
An evaluation of overall survival in patients with newly diagnosed acute myeloid leukemia and the relationship with glasdegib treatment and exposure
An evaluation of overall survival in patients with newly diagnosed acute myeloid leukemia and the relationship with glasdegib treatment and exposure Abstract Abstract Purpose Glasdegib, an oral inhibitor of the Hedgehog signaling pathway, is approved in the United States in combination with low-dose cytarabine (LDAC) t...
PMC8026752
core_pubmed_pmc
Polymer stealthing and mucin-1 retargeting for enhanced pharmacokinetics of an oncolytic vaccinia virus
Polymer stealthing and mucin-1 retargeting for enhanced pharmacokinetics of an oncolytic vaccinia virus Abstract Abstract Vaccinia virus (VV) is a powerful tool for cancer treatment with the potential for tumor tropism, efficient cell-to-cell spread, rapid replication in cancer cells, and stimulation of anti-tumor immu...
PMC7448997
core_pubmed_pmc
Effects of ∆ 9 -tetrahydrocannabinol on aversive memories and anxiety: a review from human studies
Effects of ∆ 9 -tetrahydrocannabinol on aversive memories and anxiety: a review from human studies Abstract Abstract Background Posttraumatic stress disorder (PTSD) may stem from the formation of aberrant and enduring aversive memories. Some PTSD patients have recreationally used Cannabis , probably aiming at relieving...
PMC10982469
core_pubmed_pmc
Physicochemical properties, pharmacokinetic studies, DFT approach, and antioxidant activity of nitro and chloro indolinone derivatives
Physicochemical properties, pharmacokinetic studies, DFT approach, and antioxidant activity of nitro and chloro indolinone derivatives Abstract The process of developing of new drugs is greatly hampered by their inadequate physicochemical, pharmacokinetic, and intrinsic characteristics. In this regard, the selected chl...
PMC6024869
core_pubmed_pmc
Greenshell™ Mussels: A Review of Veterinary Trials and Future Research Directions
Greenshell™ Mussels: A Review of Veterinary Trials and Future Research Directions Abstract Abstract The therapeutic benefits of Greenshell™ mussel (GSM; Perna canaliculus ) preparations have been studied using in vitro test systems, animal models, and human clinical trials focusing mainly on anti-inflammatory and anti-...
PMC11667254
core_pubmed_pmc
Efficacy and safety of rivaroxaban in preventing venous thromboembolism in postoperative patients with gynecological malignancies: protocol for a randomised controlled open-label trial (G-alfalfa trial)
Efficacy and safety of rivaroxaban in preventing venous thromboembolism in postoperative patients with gynecological malignancies: protocol for a randomised controlled open-label trial (G-alfalfa trial) Abstract Abstract Introduction Compared with the guideline-recommended use of low-molecular weight heparin (LMWH) for...
PMC12462173
core_pubmed_pmc
Evaluation of in vitro drug-drug interactions of ivermectin and antimalarial compounds
Evaluation of in vitro drug-drug interactions of ivermectin and antimalarial compounds Abstract Abstract Background Ivermectin is lethal to Anopheles mosquitoes and a novel approach to malaria transmission control. Ivermectin could be co-administered with antimalarial drugs in mass drug administration, seasonal malaria...
PMC10967354
core_pubmed_pmc
Tramadol and M1 Bioavailability Induced by Metamizole Co-Administration in Donkeys ( Equus asinus )
Tramadol and M1 Bioavailability Induced by Metamizole Co-Administration in Donkeys ( Equus asinus ) Abstract Abstract Simple Summary The combination of an opioid compound with a nonsteroidal anti-inflammatory drug can lead to additive or enhanced effects while minimizing adverse reactions. Recently, we reported the pha...
PMC7868548
core_pubmed_pmc
A Phase I Clinical Study Comparing the Tolerance, Immunogenicity, and Pharmacokinetics of Proposed Biosimilar BAT1806 and Reference Tocilizumab in Healthy Chinese Men
A Phase I Clinical Study Comparing the Tolerance, Immunogenicity, and Pharmacokinetics of Proposed Biosimilar BAT1806 and Reference Tocilizumab in Healthy Chinese Men Abstract Abstract Objective: The study aimed to explore the bioequivalence of a proposed biosimilar BAT1806 to its reference products marketed in the EU ...
PMC11645281
core_pubmed_pmc
Safety and antiviral effect of a triple combination of HIV-1 broadly neutralizing antibodies: a phase 1/2a trial
Safety and antiviral effect of a triple combination of HIV-1 broadly neutralizing antibodies: a phase 1/2a trial Abstract Abstract Human immunodeficiency virus type 1 (HIV-1)-specific broadly neutralizing monoclonal antibodies (bNAbs) have to date shown transient viral suppression when administered as monotherapy or as...
PMC7170367
core_pubmed_pmc
Influence of astragaloside IV on pharmacokinetics of triptolide in rats and its potential mechanism
Influence of astragaloside IV on pharmacokinetics of triptolide in rats and its potential mechanism Abstract Abstract Context It is common to combine two or more drugs in clinics in China. Triptolide (TP) has been used primarily for the treatment of inflammatory and autoimmune diseases. Astragaloside IV (AS-IV) has bee...
PMC5717323
core_pubmed_pmc
Interaction of Antibiotics with Innate Host Defense Factors against Salmonella enterica Serotype Newport
Interaction of Antibiotics with Innate Host Defense Factors against Salmonella enterica Serotype Newport Abstract It is becoming increasingly understood that the current paradigms of in vitro antimicrobial susceptibility testing may have significant shortcomings in predicting activity in vivo . This study evaluated the...
PMC6997415
core_pubmed_pmc
CYP2C19*2 Polymorphism Is Associated with Impaired Oral Clearance of Gliclazide in Healthy Chinese
CYP2C19*2 Polymorphism Is Associated with Impaired Oral Clearance of Gliclazide in Healthy Chinese Abstract Abstract Background Previous studies suggest gliclazide is metabolised primarily by CYP2C19 rather than CYP2C9, unlike other sulphonylureas. CYP2C19 *2 and *3 polymorphisms are more common in Asians. Methods We i...
PMC10458796
core_pubmed_pmc
Mannose-Functionalized Isoniazid-Loaded Nanostructured Lipid Carriers for Pulmonary Delivery: In Vitro Prospects and In Vivo Therapeutic Efficacy Assessment
Mannose-Functionalized Isoniazid-Loaded Nanostructured Lipid Carriers for Pulmonary Delivery: In Vitro Prospects and In Vivo Therapeutic Efficacy Assessment Abstract Resistance to isoniazid (INH) is common and increases the possibility of acquiring multidrug-resistant tuberculosis. For this study, isoniazid-loaded nano...
PMC10087074
core_pubmed_pmc
PK/PD analysis of trazodone and gabapentin in neuropathic pain rodent models: Translational PK‐PD modeling from nonclinical to clinical development
PK/PD analysis of trazodone and gabapentin in neuropathic pain rodent models: Translational PK‐PD modeling from nonclinical to clinical development Abstract Abstract A pharmacokinetic/pharmacodynamic (PK/PD) model was developed to describe the time course of writhings after intraperitoneal injection of acetic acid in m...
PMC12411014
core_pubmed_pmc
Phytochemicals in Bone Therapy: Exploring Natural Alternatives for Bone Health
Phytochemicals in Bone Therapy: Exploring Natural Alternatives for Bone Health Abstract Abstract Bone diseases such as osteoporosis and osteoarthritis are increasingly prevalent, particularly in aging populations. While conventional treatments, including synthetic drugs and mineral supplements, are effective yet often ...
PMC8450222
core_pubmed_pmc
In-silico design and ADMET predictions of some new imidazo[1,2-a]pyridine-3-carboxamides (IPAs) as anti-tubercular agents
In-silico design and ADMET predictions of some new imidazo[1,2-a]pyridine-3-carboxamides (IPAs) as anti-tubercular agents Abstract Abstract Tuberculosis (TB) is one of the leading infectious diseases worldwide even with the ravaging COVID-19 pandemic in recent times. This mandated further search and exploration of more...
PMC11289514
core_pubmed_pmc
Impact of lactoferrin supplementation on cotrimoxazole pharmacokinetics: A preliminary clinical investigation
Impact of lactoferrin supplementation on cotrimoxazole pharmacokinetics: A preliminary clinical investigation Abstract Abstract Background and purpose Cotrimoxazole, a commonly prescribed antibiotic, has substantial resistance, especially in Indonesia, with its uropathogenic resistance reaching 67% in 2017. Although co...
PMC8600502
core_pubmed_pmc
Affinity Capillary Electrophoresis–Mass Spectrometry as a Tool to Unravel Proteoform-Specific Antibody–Receptor Interactions
Affinity Capillary Electrophoresis–Mass Spectrometry as a Tool to Unravel Proteoform-Specific Antibody–Receptor Interactions Abstract Monoclonal antibody (mAb) pharmaceuticals consist of a plethora of different proteoforms with different functional characteristics, including pharmacokinetics and pharmacodynamics, requi...
PMC12661425
core_pubmed_pmc
Anti-lung cancer therapy using nano-assembly particles of traditional Chinese Medicine formula
Anti-lung cancer therapy using nano-assembly particles of traditional Chinese Medicine formula Abstract Nano-assembly particles (NAPs) isolated from Traditional Chinese Medicine (TCM) formulations retain a better multi-component overall effect than isolated single active ingredient, which gradually emerging as a transf...
PMC11756928
core_pubmed_pmc
Comparison of etonogestrel bioanalytical assay results in plasma and serum within and across laboratories
Comparison of etonogestrel bioanalytical assay results in plasma and serum within and across laboratories Abstract Abstract Objectives: To compare performance characteristics of etonogestrel bioanalytical assays across laboratories. Study design: We conducted a blinded, six laboratory study: five academic laboratories ...
PMC10144708
core_pubmed_pmc
In Vitro and In Vivo Characterization of the Transdermal Gel Formulation of Desloratadine for Prevention of Obesity and Metabolic Syndrome
In Vitro and In Vivo Characterization of the Transdermal Gel Formulation of Desloratadine for Prevention of Obesity and Metabolic Syndrome Abstract Abstract Chronic use of antihistamines can induce abnormalities in lipid absorption with potential excessive accumulation of lipids in the mesentery that can lead to the de...
PMC3107238
core_pubmed_pmc
Tumor Endothelium Marker-8 Based Decoys Exhibit Superiority over Capillary Morphogenesis Protein-2 Based Decoys as Anthrax Toxin Inhibitors
Tumor Endothelium Marker-8 Based Decoys Exhibit Superiority over Capillary Morphogenesis Protein-2 Based Decoys as Anthrax Toxin Inhibitors Abstract Anthrax toxin is the major virulence factor produced by Bacillus anthracis . The toxin consists of three protein subunits: protective antigen (PA), lethal factor, and edem...
PMC5061793
core_pubmed_pmc
First‐in‐human study assessing safety, tolerability and pharmacokinetics of BI 409306, a selective phosphodiesterase 9A inhibitor, in healthy males
First‐in‐human study assessing safety, tolerability and pharmacokinetics of BI 409306, a selective phosphodiesterase 9A inhibitor, in healthy males Abstract Abstract Aims The aim of the present study was to investigate the safety, tolerability, dose proportionality and relative bioavailability of tablet and oral soluti...
PMC7600566
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling of Transdermal Selegiline and Its Metabolites for the Evaluation of Disposition Differences between Healthy and Special Populations
Physiologically Based Pharmacokinetic Modeling of Transdermal Selegiline and Its Metabolites for the Evaluation of Disposition Differences between Healthy and Special Populations Abstract A physiologically based pharmacokinetic (PBPK) model of selegiline (SEL), and its metabolites, was developed in silico to evaluate t...
PMC12355019
core_pubmed_pmc
Absolute Oral Bioavailability and Bioequivalence of LSD Base and Tartrate in a Double‐Blind, Placebo‐Controlled, Crossover Study
Absolute Oral Bioavailability and Bioequivalence of LSD Base and Tartrate in a Double‐Blind, Placebo‐Controlled, Crossover Study Abstract Lysergic acid diethylamide (LSD) is currently being investigated as a potential treatment for psychiatric and neurological disorders. Different LSD formulations (base or tartrate, or...
PMC8300739
core_pubmed_pmc
Pharmacokinetics of Non-β-Lactam β-Lactamase Inhibitors
Pharmacokinetics of Non-β-Lactam β-Lactamase Inhibitors Abstract The growing emergence of drug-resistant bacterial strains is an issue to treat severe infections, and many efforts have identified new pharmacological agents. The inhibitors of β-lactamases (BLI) have gained a prominent role in the safeguard of beta-lacta...
PMC12202196
core_pubmed_pmc
Population Pharmacokinetics of Fruquintinib, a Selective Oral Inhibitor of VEGFR ‐1, ‐2, and ‐3, in Patients with Refractory Metastatic Colorectal Cancer
Population Pharmacokinetics of Fruquintinib, a Selective Oral Inhibitor of VEGFR ‐1, ‐2, and ‐3, in Patients with Refractory Metastatic Colorectal Cancer Abstract Abstract Fruquintinib is a selective, oral tyrosine kinase inhibitor of all three vascular endothelial growth factor receptors 1, 2, and 3, which is approved...
PMC9734226
core_pubmed_pmc
The Pharmacokinetics and Safety of Tucatinib in Volunteers with Hepatic Impairment
The Pharmacokinetics and Safety of Tucatinib in Volunteers with Hepatic Impairment Abstract Abstract Background and Objective Tucatinib, a highly selective tyrosine kinase inhibitor of the human epidermal growth factor receptor 2 (HER2) approved for HER2-positive metastatic breast cancer, is cleared by hepatic metaboli...
PMC8720797
core_pubmed_pmc
Pharmacokinetic profile of sildenafil citrate in healthy Middle Eastern Males: Comparison with other ethnicities
Pharmacokinetic profile of sildenafil citrate in healthy Middle Eastern Males: Comparison with other ethnicities Abstract Abstract Aim 1) To investigate the pharmacokinetic profile of sildenafil citrate in Middle Eastern males and, 2) To highlight the impact of ethnicity on its pharmacokinetics parameters through compa...
PMC12044999
core_pubmed_pmc
Improved pharmacotherapy after revised dosing regimens of two slow-release formulations of benzylpenicillin in an Actinobacillus pleuropneumoniae infection model in pigs
Improved pharmacotherapy after revised dosing regimens of two slow-release formulations of benzylpenicillin in an Actinobacillus pleuropneumoniae infection model in pigs Abstract Background Actinobacillus pleuropneumoniae (APP) is a Gram-negative bacterium that causes respiratory disease in pigs, resulting in significa...
PMC12844775
core_pubmed_pmc
Combining Fluorescence and Magnetic Resonance Imaging in Drug Discovery—A Review
Combining Fluorescence and Magnetic Resonance Imaging in Drug Discovery—A Review Abstract Abstract Drug discovery is a complex and multi-stage process that requires advanced analytical technologies capable of accelerating preclinical evaluation and improving the precision of therapeutic design. The combination of fluor...
PMC9500665
core_pubmed_pmc
Optimization of the Pharmacokinetic Profile of [ 99m Tc]Tc-N 4 -Bombesin Derivatives by Modification of the Pharmacophoric Gln-Trp Sequence
Optimization of the Pharmacokinetic Profile of [ 99m Tc]Tc-N 4 -Bombesin Derivatives by Modification of the Pharmacophoric Gln-Trp Sequence Abstract Abstract Current radiolabeled gastrin-releasing peptide receptor (GRPR) ligands usually suffer from high accumulation in GRPR-positive organs (pancreas, stomach), limiting...
PMC5784607
core_pubmed_pmc
Deleterious genetic variants in ciliopathy genes increase risk of ritodrine-induced cardiac and pulmonary side effects
Deleterious genetic variants in ciliopathy genes increase risk of ritodrine-induced cardiac and pulmonary side effects Abstract Background Ritodrine is a commonly used tocolytic to prevent preterm labour. However, it can cause unexpected serious adverse reactions, such as pulmonary oedema, pulmonary congestion, and tac...
PMC9290342
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Repository Corticotropin Injection Compared With Synthetic ACTH 1‐24 Depot and Methylprednisolone in Healthy Subjects
Pharmacokinetics and Pharmacodynamics of Repository Corticotropin Injection Compared With Synthetic ACTH 1‐24 Depot and Methylprednisolone in Healthy Subjects Abstract Abstract Repository corticotropin injection (RCI; Acthar Gel) is a naturally sourced complex mixture of adrenocorticotropic hormone (ACTH) analogs and o...
PMC9476744
core_pubmed_pmc
Sesquiterpene lactones of Aucklandia lappa : Pharmacology, pharmacokinetics, toxicity, and structure–activity relationship
Sesquiterpene lactones of Aucklandia lappa : Pharmacology, pharmacokinetics, toxicity, and structure–activity relationship Abstract Abstract The medicinal part of Aucklandia lappa (Asteraceae) is its dried root, which is one of the commonly used Chinese medicinal materials. Here we reviewed sesquiterpene lactones isola...
PMC6256812
core_pubmed_pmc
Microbiological Analysis from a Phase 2 Randomized Study in Adults Evaluating Single Oral Doses of Gepotidacin in the Treatment of Uncomplicated Urogenital Gonorrhea Caused by Neisseria gonorrhoeae
Microbiological Analysis from a Phase 2 Randomized Study in Adults Evaluating Single Oral Doses of Gepotidacin in the Treatment of Uncomplicated Urogenital Gonorrhea Caused by Neisseria gonorrhoeae Abstract We evaluated microbiological correlates for the successful treatment of Neisseria gonorrhoeae isolates from a pha...
PMC6590357
core_pubmed_pmc
Physiologically Based Modeling Approach to Predict Dopamine D2 Receptor Occupancy of Antipsychotics in Brain: Translation From Rat to Human
Physiologically Based Modeling Approach to Predict Dopamine D2 Receptor Occupancy of Antipsychotics in Brain: Translation From Rat to Human Abstract Abstract Receptor occupancy (RO) is a translational biomarker for assessing drug efficacy and safety. We aimed to apply a physiologically based pharmacokinetic (PBPK) mode...
PMC10459442
core_pubmed_pmc
Translation of Monoclonal Antibodies Pharmacokinetics from Animal to Human Using Physiologically Based Modeling in Open Systems Pharmacology (OSP) Suite: A Retrospective Analysis of Bevacizumab
Translation of Monoclonal Antibodies Pharmacokinetics from Animal to Human Using Physiologically Based Modeling in Open Systems Pharmacology (OSP) Suite: A Retrospective Analysis of Bevacizumab Abstract Interspecies translation of monoclonal antibodies (mAbs) pharmacokinetics (PK) in presence of target-mediated drug di...
PMC7558535
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In Vitro Metabolism of DWP16001, a Novel Sodium-Glucose Cotransporter 2 Inhibitor, in Human and Animal Hepatocytes
In Vitro Metabolism of DWP16001, a Novel Sodium-Glucose Cotransporter 2 Inhibitor, in Human and Animal Hepatocytes Abstract DWP16001 is currently in a phase 2 clinical trial as a novel anti-diabetes drug for the treatment of type 2 diabetes by selective inhibition of sodium-glucose cotransporter 2. This in vitro study ...
PMC11676204
core_pubmed_pmc
Molecular Docking and Antihypertensive Activity of Eupalitin 3-O-β-D-galactopyranoside Isolated from Boerhavia diffusa Linn
Molecular Docking and Antihypertensive Activity of Eupalitin 3-O-β-D-galactopyranoside Isolated from Boerhavia diffusa Linn Abstract Background: Angiotensin-converting enzyme (ACE) is a key regulator of blood pressure, and ACE inhibition is an essential part of the treatment of hypertension. We used a molecular docking...
PMC3059462
core_pubmed_pmc
Whole plant extracts versus single compounds for the treatment of malaria: synergy and positive interactions
Whole plant extracts versus single compounds for the treatment of malaria: synergy and positive interactions Abstract Background In traditional medicine whole plants or mixtures of plants are used rather than isolated compounds. There is evidence that crude plant extracts often have greater in vitro or/and in vivo anti...
PMC12944649
core_pubmed_pmc
Cefepime and New Cefepime/Beta-Lactamase Inhibitor Combination for the Treatment of Gram-Negative Bacteria: Chemical Structure and Mechanism of Action, Microbiological Target, Clinical Use and PK/PD Characteristics
Cefepime and New Cefepime/Beta-Lactamase Inhibitor Combination for the Treatment of Gram-Negative Bacteria: Chemical Structure and Mechanism of Action, Microbiological Target, Clinical Use and PK/PD Characteristics Abstract The global spread of multidrug-resistant (MDR) Gram-negative bacteria, particularly extended-spe...
PMC8025906
core_pubmed_pmc
Understanding Carrier Performance in Low-Dose Dry Powder Inhalation: An In Vitro–In Silico Approach
Understanding Carrier Performance in Low-Dose Dry Powder Inhalation: An In Vitro–In Silico Approach Abstract The use of physiologically based pharmacokinetic (PBPK) models to support drug product development has become increasingly popular. The in vitro characterization of the materials of the formulation provides valu...
PMC5685476
core_pubmed_pmc
Safety, pharmacokinetics, and immunological activities of multiple intravenous or subcutaneous doses of an anti-HIV monoclonal antibody, VRC01, administered to HIV-uninfected adults: Results of a phase 1 randomized trial
Safety, pharmacokinetics, and immunological activities of multiple intravenous or subcutaneous doses of an anti-HIV monoclonal antibody, VRC01, administered to HIV-uninfected adults: Results of a phase 1 randomized trial Abstract Background VRC01 is an HIV-1 CD4 binding site broadly neutralizing antibody (bnAb) that is...
PMC12127635
core_pubmed_pmc
Population pharmacokinetics of high-dose methotrexate in patients with primary central nervous system lymphoma
Population pharmacokinetics of high-dose methotrexate in patients with primary central nervous system lymphoma Abstract Objective Methotrexate (MTX) serves as a cornerstone therapy for primary central nervous system lymphoma (PCNSL). However, the considerable intra- and inter-individual variability in its pharmacokinet...
PMC6260160
core_pubmed_pmc
Optimizing the Design and Analysis of Clinical Trials for Antibacterials Against Multidrug-resistant Organisms: A White Paper From COMBACTE’s STAT-Net
Optimizing the Design and Analysis of Clinical Trials for Antibacterials Against Multidrug-resistant Organisms: A White Paper From COMBACTE’s STAT-Net Abstract Abstract Innovations are urgently required for clinical development of antibacterials against multidrug-resistant organisms. Therefore, a European, public-priva...
PMC11011928
core_pubmed_pmc
Unified Methodology for the Primary Preclinical In Vivo Screening of New Anticoagulant Pharmaceutical Agents from Hematophagous Organisms
Unified Methodology for the Primary Preclinical In Vivo Screening of New Anticoagulant Pharmaceutical Agents from Hematophagous Organisms Abstract Abstract The development of novel anticoagulants requires a comprehensive investigational approach that is capable of characterizing different aspects of antithrombotic acti...
PMC8958266
core_pubmed_pmc
Chromosomal Region 11p14.1 is Associated with Pharmacokinetics and Pharmacodynamics of Bisoprolol
Chromosomal Region 11p14.1 is Associated with Pharmacokinetics and Pharmacodynamics of Bisoprolol Abstract Abstract Purpose Bisoprolol is a widely used beta-blocker in patients with cardiovascular diseases. As with other beta-blockers, there is variability in response to bisoprolol, but the underlying reasons for this ...
PMC12049132
core_pubmed_pmc
Drug Interactions of Imperatorin and Curcumin on Macitentan in vitro and in vivo
Drug Interactions of Imperatorin and Curcumin on Macitentan in vitro and in vivo Abstract Abstract Purpose The purpose of this study was to establish an in vitro incubation system and an in vivo model to investigate the potential kinetic interactions of macitentan with imperatorin and curcumin, and to validate the pote...
PMC10353356
core_pubmed_pmc
Using Dynamic Oral Dosing of Rifapentine and Rifabutin to Simulate Exposure Profiles of Long-Acting Formulations in a Mouse Model of Tuberculosis Preventive Therapy
Using Dynamic Oral Dosing of Rifapentine and Rifabutin to Simulate Exposure Profiles of Long-Acting Formulations in a Mouse Model of Tuberculosis Preventive Therapy Abstract ABSTRACT Administration of tuberculosis preventive therapy (TPT) to individuals with latent tuberculosis infection is an important facet of global...
PMC12449878
core_pubmed_pmc
Population Pharmacokinetic/Pharmacodynamic Modeling of Tacrolimus in Renal Transplant Recipients: Impact of CYP3A5 Genotype and Wuzhi Capsule Co-Medication
Population Pharmacokinetic/Pharmacodynamic Modeling of Tacrolimus in Renal Transplant Recipients: Impact of CYP3A5 Genotype and Wuzhi Capsule Co-Medication Abstract Abstract Object Tacrolimus is a crucial immunosuppressant used to prevent renal transplant rejection. While, long-term application of tacrolimus can lead t...
PMC5237699
core_pubmed_pmc
Understanding and applying pharmacometric modelling and simulation in clinical practice and research
Understanding and applying pharmacometric modelling and simulation in clinical practice and research Abstract Abstract Understanding the dose–concentration–effect relationship is a fundamental component of clinical pharmacology. Interpreting data arising from observations of this relationship requires the use of mathem...
PMC4293289
core_pubmed_pmc
Solid lipid nanoparticles loaded with iron to overcome barriers for treatment of iron deficiency anemia
Solid lipid nanoparticles loaded with iron to overcome barriers for treatment of iron deficiency anemia Abstract According to the World Health Organization, 46% of the world’s children suffer from anemia, which is usually treated with iron supplements such as ferrous sulfate. The aim of this study was to prepare iron a...
PMC12464645
core_pubmed_pmc
Population pharmacokinetic modelling of prednisolone in systemic lupus erythematosus patients: Analysis of exposure and disease activity
Population pharmacokinetic modelling of prednisolone in systemic lupus erythematosus patients: Analysis of exposure and disease activity Abstract Abstract Aims Prednisone is a widely used glucocorticoid in the treatment of lupus, although its dosing is often determined empirically. Prednisolone, the active metabolite o...
PMC11315817
core_pubmed_pmc
Pharmacokinetics and Bioequivalence of Two Formulations of Azithromycin Tablets: A Randomized, Single-Dose, Three-Period, Crossover Study in Healthy Chinese Volunteers Under Fasting and Fed Conditions
Pharmacokinetics and Bioequivalence of Two Formulations of Azithromycin Tablets: A Randomized, Single-Dose, Three-Period, Crossover Study in Healthy Chinese Volunteers Under Fasting and Fed Conditions Abstract Abstract Background and Objective Azithromycin is the first azalide antibiotic that is related to the macrolid...
PMC10122588
core_pubmed_pmc
A Systematic Review of Weight-Based Metoprolol for Acute Atrial Fibrillation with Rapid Ventricular Rate
A Systematic Review of Weight-Based Metoprolol for Acute Atrial Fibrillation with Rapid Ventricular Rate Abstract Abstract Atrial fibrillation (AF) is the most common cardiac arrhythmia encountered in the emergency department (ED) and when patients present in acute AF with rapid ventricular rate (RVR), it can result in...
PMC8226678
core_pubmed_pmc
Broad-Spectrum Anticancer Activity and Pharmacokinetic Properties of a Prenyloxy-Substituted Indeno[1,2- b ]indole Derivative, Discovered as CK2 Inhibitor
Broad-Spectrum Anticancer Activity and Pharmacokinetic Properties of a Prenyloxy-Substituted Indeno[1,2- b ]indole Derivative, Discovered as CK2 Inhibitor Abstract Abstract Protein kinase CK2 is involved in regulating cellular processes, such as cell cycle, proliferation, migration, and apoptosis, making it an attracti...
PMC12472680
core_pubmed_pmc
The Efficacy of Melatonergic Receptor Agonists Used in Clinical Practice in Insomnia Treatment: Melatonin, Tasimelteon, Ramelteon, Agomelatine, and Selected Herbs
The Efficacy of Melatonergic Receptor Agonists Used in Clinical Practice in Insomnia Treatment: Melatonin, Tasimelteon, Ramelteon, Agomelatine, and Selected Herbs Abstract Abstract Insomnia is a common and complex disorder, rooted in the dysregulation of circadian rhythms, impaired neurotransmitter function, and distur...
PMC11996768
core_pubmed_pmc
Clopidogrel transfer into human milk: case series – a contribution from the ConcePTION project
Clopidogrel transfer into human milk: case series – a contribution from the ConcePTION project Abstract Abstract Introduction Implementation of breastfeeding recommendations is hampered by–among others–lacking information regarding medicine safety during breastfeeding. This article describes the clinical and pharmacoki...
PMC11892681
core_pubmed_pmc
Use of metabolic imaging to monitor heterogeneity of tumour response following therapeutic mTORC1/2 pathway inhibition
Use of metabolic imaging to monitor heterogeneity of tumour response following therapeutic mTORC1/2 pathway inhibition Abstract ABSTRACT The PI3K–mTOR–AKT pathway regulates tumour proliferation, gene expression and metabolism, but pathway inhibition induces heterogeneous feedback reactivation, limiting anti-tumour resp...
PMC9292832
core_pubmed_pmc
Abacavir pharmacokinetics in African children living with HIV: A pooled analysis describing the effects of age, malnutrition and common concomitant medications
Abacavir pharmacokinetics in African children living with HIV: A pooled analysis describing the effects of age, malnutrition and common concomitant medications Abstract Aims Abacavir is part of WHO‐recommended regimens to treat HIV in children under 15 years of age. In a pooled analysis across four studies, we describe...
PMC9774462
core_pubmed_pmc
Antibiotic Therapy in the Critically Ill with Acute Renal Failure and Renal Replacement Therapy: A Narrative Review
Antibiotic Therapy in the Critically Ill with Acute Renal Failure and Renal Replacement Therapy: A Narrative Review Abstract Abstract The outcome for critically ill patients is burdened by a double mortality rate and a longer hospital stay in the case of sepsis or septic shock. The adequate use of antibiotics may impac...
PMC9631830
core_pubmed_pmc
Closed-loop control of continuous piperacillin delivery: An in silico study
Closed-loop control of continuous piperacillin delivery: An in silico study Abstract Background and objective: Sub-therapeutic dosing of piperacillin-tazobactam in critically-ill patients is associated with poor clinical outcomes and may promote the emergence of drug-resistant infections. In this paper, an in silico in...
PMC4424595
core_pubmed_pmc
Influence of Morphine on Pharmacokinetics and Pharmacodynamics of Ticagrelor in Patients with Acute Myocardial Infarction (IMPRESSION): study protocol for a randomized controlled trial
Influence of Morphine on Pharmacokinetics and Pharmacodynamics of Ticagrelor in Patients with Acute Myocardial Infarction (IMPRESSION): study protocol for a randomized controlled trial Abstract Background Ticagrelor is an oral platelet P2Y12 receptor antagonist which is recommended for patients suffering from myocardia...
PMC12598903
core_pubmed_pmc
Pharmacokinetics of Intravenous and Transdermal Flunixin Meglumine in Wool and Hair Sheep ( Ovis aries )
Pharmacokinetics of Intravenous and Transdermal Flunixin Meglumine in Wool and Hair Sheep ( Ovis aries ) Abstract ABSTRACT The objective of the study was to evaluate the pharmacokinetics of flunixin meglumine of intravenous (IV) and transdermal (TD) flunixin meglumine administration on different coat types (wool vs. ha...
PMC10613910
core_pubmed_pmc
Exploring pharmacokinetics of talazoparib in ABCB1/ABCG2-deficient mice using a novel UHPLC-MS/MS method
Exploring pharmacokinetics of talazoparib in ABCB1/ABCG2-deficient mice using a novel UHPLC-MS/MS method Abstract A rapid, sensitive, and simple UHPLC-MS/MS method for the determination of the PARP inhibitor talazoparib in mouse plasma was developed and validated using [ 13 C, 2 H 4 ]-talazoparib as an internal standar...
PMC11558173
core_pubmed_pmc
Combined Nabpaclitaxel pressurized intraPeritoneal aerosol chemotherapy with systemic Nabpaclitaxel-Gemcitabine chemotherapy for pancreatic cancer peritoneal metastases: protocol of single-arm, open-label, phase II trial (Nab-PIPAC trial)
Combined Nabpaclitaxel pressurized intraPeritoneal aerosol chemotherapy with systemic Nabpaclitaxel-Gemcitabine chemotherapy for pancreatic cancer peritoneal metastases: protocol of single-arm, open-label, phase II trial (Nab-PIPAC trial) Abstract Abstract Objectives Current therapies show limited efficacy against peri...
PMC10860498
core_pubmed_pmc
Clozapine-Induced Severe Toxicity: Exploring the Pharmacokinetic Profile of Clozapine and Its Significance in Hemodynamic Instability – A Case Report
Clozapine-Induced Severe Toxicity: Exploring the Pharmacokinetic Profile of Clozapine and Its Significance in Hemodynamic Instability – A Case Report Abstract Abstract Hemodynamic instability in patients with clozapine intoxication can indirectly reflect the serum concentration of clozapine.We have described a case of ...
PMC3244639
core_pubmed_pmc
An investigation of the safety and pharmacokinetics of the novel TRPV1 antagonist XEN-D0501 in healthy subjects
An investigation of the safety and pharmacokinetics of the novel TRPV1 antagonist XEN-D0501 in healthy subjects Abstract Abstract AIMS XEN-D0501, a novel TRPV1 antagonist, is being developed to treat overactive bladder. This study investigated the safety and pharmacokinetics of repeat-dose XEN-D0501 in healthy subjects...
PMC9031623
core_pubmed_pmc
Macrolide Treatment Failure due to Drug–Drug Interactions: Real-World Evidence to Evaluate a Pharmacological Hypothesis
Macrolide Treatment Failure due to Drug–Drug Interactions: Real-World Evidence to Evaluate a Pharmacological Hypothesis Abstract Abstract Macrolide antibiotics have received criticism concerning their use and risk of treatment failure. Nevertheless, they are an important class of antibiotics and are frequently used in ...
PMC5561377
core_pubmed_pmc
A randomised, double-blind trial to demonstrate bioequivalence of GP2013 and reference rituximab combined with methotrexate in patients with active rheumatoid arthritis
A randomised, double-blind trial to demonstrate bioequivalence of GP2013 and reference rituximab combined with methotrexate in patients with active rheumatoid arthritis Abstract Objectives The aim of this report is to demonstrate pharmacokinetic (PK) and pharmacodynamic (PD) equivalence as well as similar efficacy, saf...
PMC4061120
core_pubmed_pmc
Identification of longitudinally dynamic biomarkers in Alzheimer’s disease cerebrospinal fluid by targeted proteomics
Identification of longitudinally dynamic biomarkers in Alzheimer’s disease cerebrospinal fluid by targeted proteomics Abstract Background Alzheimer’s disease (AD) is the leading cause of dementia affecting greater than 26 million people worldwide. Although cerebrospinal fluid (CSF) levels of Aβ 42 , tau, and p-tau 181 ...
PMC6008768
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modelling with Dynamic PET Data to Study the In Vivo Effects of Transporter Inhibition on Hepatobiliary Clearance in Mice
Physiologically Based Pharmacokinetic Modelling with Dynamic PET Data to Study the In Vivo Effects of Transporter Inhibition on Hepatobiliary Clearance in Mice Abstract Abstract Physiologically based pharmacokinetic modelling (PBPK) is a powerful tool to predict in vivo pharmacokinetics based on physiological parameter...
PMC12943871
core_pubmed_pmc
Combined Intraperitoneal and Systemic Chemotherapy for Peritoneal Metastases: Drug Delivery Concepts, Pharmacokinetics, and Clinical Applications: A Narrative Review
Combined Intraperitoneal and Systemic Chemotherapy for Peritoneal Metastases: Drug Delivery Concepts, Pharmacokinetics, and Clinical Applications: A Narrative Review Abstract Abstract Background/Objectives: Peritoneal metastases (PMs) remain difficult to treat because the peritoneum–plasma barrier limits drug penetrati...
PMC4861375
core_pubmed_pmc
Targeting Prolactin Receptor (PRLR) Signaling in PRLR-Positive Breast and Prostate Cancer
Targeting Prolactin Receptor (PRLR) Signaling in PRLR-Positive Breast and Prostate Cancer Abstract In this issue of The Oncologist , Agarwal et al. report negative results from a phase I trial of LFA102. Although “negative” in terms of antitumor activity, the study provides useful pharmacokinetic and pharmacodynamic in...
PMC3509542
core_pubmed_pmc
The Effect of Glycyrrhetinic Acid on Pharmacokinetics of Cortisone and Its Metabolite Cortisol in Rats
The Effect of Glycyrrhetinic Acid on Pharmacokinetics of Cortisone and Its Metabolite Cortisol in Rats Abstract The purpose of this paper is to study pharmacokinetics of cortisone (E) and its metabolite cortisol (F) in rats after administration of glycyrrhetinic acid (GA) and cortisone. Healthy male SD rats were random...
PMC12198556
core_pubmed_pmc
Unexpected voriconazole toxicity due to nirmatrelvir/ritonavir: a case report on drug-drug interaction and the role of therapeutic drug monitoring
Unexpected voriconazole toxicity due to nirmatrelvir/ritonavir: a case report on drug-drug interaction and the role of therapeutic drug monitoring Abstract Voriconazole is a triazole antifungal used for invasive fungal infections, particularly invasive aspergillosis. Its metabolism is primarily mediated by CYP2C19, wit...