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PMC8107167
core_pubmed_pmc
An Open-Label Tolerability and Actual-Use Human Factors Study of Etrolizumab Autoinjector in Healthy Volunteers
An Open-Label Tolerability and Actual-Use Human Factors Study of Etrolizumab Autoinjector in Healthy Volunteers Abstract Abstract Introduction Etrolizumab is a novel, dual-action, anti-β7 integrin antibody in development for patients with moderate to severe ulcerative colitis or Crohn’s disease. Phase 3 studies use a p...
PMC7452927
core_pubmed_pmc
Item Response Theory Modeling of the International Prostate Symptom Score in Patients with Lower Urinary Tract Symptoms Associated with Benign Prostatic Hyperplasia
Item Response Theory Modeling of the International Prostate Symptom Score in Patients with Lower Urinary Tract Symptoms Associated with Benign Prostatic Hyperplasia Abstract Item response theory (IRT) was used to characterize the time course of lower urinary tract symptoms due to benign prostatic hyperplasia (BPH-LUTS)...
PMC12131725
core_pubmed_pmc
Population pharmacokinetics of vancomycin in non-extremely preterm neonates based on real-world studies: influence of daily fluid input and diuretics
Population pharmacokinetics of vancomycin in non-extremely preterm neonates based on real-world studies: influence of daily fluid input and diuretics Abstract ABSTRACT This study aimed to develop a population pharmacokinetics (PPK) model for vancomycin in non-extremely preterm neonates hospitalized in the neonatal inte...
PMC9924065
core_pubmed_pmc
Development of a population pharmacokinetics and pharmacodynamics model of glucarpidase rescue treatment after high-dose methotrexate therapy
Development of a population pharmacokinetics and pharmacodynamics model of glucarpidase rescue treatment after high-dose methotrexate therapy Abstract Introduction Glucarpidase (CPG2) reduces the lethal toxicity of methotrexate (MTX) by rapid degradation. Methods In this study, a CPG2 population pharmacokinetics (popPK...
PMC3147227
core_pubmed_pmc
Mavrilimumab, a human monoclonal antibody targeting GM-CSF receptor-α, in subjects with rheumatoid arthritis: a randomised, double-blind, placebo-controlled, phase I, first-in-human study
Mavrilimumab, a human monoclonal antibody targeting GM-CSF receptor-α, in subjects with rheumatoid arthritis: a randomised, double-blind, placebo-controlled, phase I, first-in-human study Abstract Objective To evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic profiles of mavrilimumab, a human monoc...
PMC12779737
core_pubmed_pmc
Safety and pharmacokinetics of teplizumab in children less than 8 years of age with stage 2 type 1 diabetes
Safety and pharmacokinetics of teplizumab in children less than 8 years of age with stage 2 type 1 diabetes Abstract Abstract Aims/hypothesis Teplizumab is approved in the USA and seven other countries to delay stage 3 type 1 diabetes onset in individuals ≥8 years of age with stage 2 type 1 diabetes. As part of a US Fo...
PMC11992664
core_pubmed_pmc
Adaptive dosing of high‐dose busulfan in real‐world adult patients undergoing haematopoietic cell transplant conditioning
Adaptive dosing of high‐dose busulfan in real‐world adult patients undergoing haematopoietic cell transplant conditioning Abstract Abstract Aim To evaluate the effectiveness of a Bayesian adaptive dosing strategy in achieving target busulfan exposure in adult patients undergoing haematopoietic cell transplantation (HCT...
PMC10535763
core_pubmed_pmc
Development of a Physiologically Based Pharmacokinetic Model for Nitrofurantoin in Rabbits, Rats, and Humans
Development of a Physiologically Based Pharmacokinetic Model for Nitrofurantoin in Rabbits, Rats, and Humans Abstract Abstract Nitrofurantoin (NFT) is a commonly used antibiotic for the treatment of urinary tract infections that can cause liver toxicity. Despite reports of hepatic adverse events associated with NFT exp...
PMC3504364
core_pubmed_pmc
Impact of genetic polymorphisms on chemotherapy toxicity in childhood acute lymphoblastic leukemia
Impact of genetic polymorphisms on chemotherapy toxicity in childhood acute lymphoblastic leukemia Abstract Abstract The efficacy of chemotherapy in pediatric acute lymphoblastic leukemia (ALL) patients has significantly increased in the last 20 years; as a result, the focus of research is slowly shifting from trying t...
PMC10936618
core_pubmed_pmc
Application of quantitative protein mass spectrometric data in the early predictive analysis of membrane-bound target engagement by monoclonal antibodies
Application of quantitative protein mass spectrometric data in the early predictive analysis of membrane-bound target engagement by monoclonal antibodies Abstract ABSTRACT Model-informed drug discovery advocates the use of mathematical modeling and simulation for improved efficacy in drug discovery. In the case of mono...
PMC8587851
core_pubmed_pmc
Validation of the Antioxidant and Enzyme Inhibitory Potential of Selected Triterpenes Using In Vitro and In Silico Studies, and the Evaluation of Their ADMET Properties
Validation of the Antioxidant and Enzyme Inhibitory Potential of Selected Triterpenes Using In Vitro and In Silico Studies, and the Evaluation of Their ADMET Properties Abstract The antioxidant and enzyme inhibitory potential of fifteen cycloartane-type triterpenes’ potentials were investigated using different assays. ...
PMC12319571
core_pubmed_pmc
Phloridzin as a Nutraceutical for Cancer Prevention and Therapy: A Comprehensive Review of Its Mechanisms, Bioavailability Challenges and Future Applications
Phloridzin as a Nutraceutical for Cancer Prevention and Therapy: A Comprehensive Review of Its Mechanisms, Bioavailability Challenges and Future Applications Abstract ABSTRACT The global rise in cancer incidence has driven the search for safer, more effective therapies, with natural compounds gaining increasing attenti...
PMC5354820
core_pubmed_pmc
Novel PARP1/2 inhibitor mefuparib hydrochloride elicits potent in vitro and in vivo anticancer activity, characteristic of high tissue distribution
Novel PARP1/2 inhibitor mefuparib hydrochloride elicits potent in vitro and in vivo anticancer activity, characteristic of high tissue distribution Abstract Abstract The approval of poly(ADP-ribose) polymerase (PARP) inhibitor AZD2281 in 2014 marked the successful establishment of the therapeutic strategy targeting hom...
PMC12597969
core_pubmed_pmc
Predicting the Pharmacokinetics of T‐Cell Engagers as a Function of Target‐Mediated Drug Disposition
Predicting the Pharmacokinetics of T‐Cell Engagers as a Function of Target‐Mediated Drug Disposition Abstract ABSTRACT T‐Cell Engagers (TCEs) are biological multi‐specific molecules designed to co‐engage targets on T cells and on a target cell for destruction. Molecular formats are typically derived from IgG monoclonal...
PMC10014685
core_pubmed_pmc
Pharmacokinetics, safety and tolerability of valbenazine in Korean CYP2D6 normal and intermediate metabolizers
Pharmacokinetics, safety and tolerability of valbenazine in Korean CYP2D6 normal and intermediate metabolizers Abstract Abstract Valbenazine is a selective vesicular monoamine transporter 2 (VMAT2) inhibitor approved for tardive dyskinesia treatment by the US Food and Drug Administration; its major active metabolite (N...
PMC6827099
core_pubmed_pmc
Folate Receptor-Targeted Albumin Nanoparticles Based on Microfluidic Technology to Deliver Cabazitaxel
Folate Receptor-Targeted Albumin Nanoparticles Based on Microfluidic Technology to Deliver Cabazitaxel Abstract Abstract Microfluidic technology (MF) has improved the formulation of nanoparticles (NPs) by achieving uniform particle size distribution, controllable particle size, and consistency. Moreover, because liquid...
PMC9570165
core_pubmed_pmc
A Physiologically Based Pharmacokinetic Model to Predict the Impact of Metabolic Changes Associated with Metabolic Associated Fatty Liver Disease on Drug Exposure
A Physiologically Based Pharmacokinetic Model to Predict the Impact of Metabolic Changes Associated with Metabolic Associated Fatty Liver Disease on Drug Exposure Abstract Abstract Metabolic associated fatty liver disease (MAFLD) is the most common chronic liver disease, with an estimated prevalence of between 20 and 3...
PMC10962466
core_pubmed_pmc
Tizanidine: Advances in Pharmacology & Therapeutics and Drug Formulations
Tizanidine: Advances in Pharmacology & Therapeutics and Drug Formulations Abstract Background Skeletal muscle relaxants (SMRs) are widely used in treating musculoskeletal conditions. All SMRs, with the exception of baclofen and tizanidine, are on the list of 2023 American Geriatrics Society Beers Criteria ® for potenti...
PMC4564386
core_pubmed_pmc
Effects of humeral intraosseous versus intravenous epinephrine on pharmacokinetics and return of spontaneous circulation in a porcine cardiac arrest model: A randomized control trial
Effects of humeral intraosseous versus intravenous epinephrine on pharmacokinetics and return of spontaneous circulation in a porcine cardiac arrest model: A randomized control trial Abstract Abstract Cardiopulmonary Resuscitation (CPR), defibrillation, and epinephrine administration are pillars of advanced cardiac lif...
PMC9964073
core_pubmed_pmc
Celecoxib Nanoformulations with Enhanced Solubility, Dissolution Rate, and Oral Bioavailability: Experimental Approaches over In Vitro/In Vivo Evaluation
Celecoxib Nanoformulations with Enhanced Solubility, Dissolution Rate, and Oral Bioavailability: Experimental Approaches over In Vitro/In Vivo Evaluation Abstract Abstract Celecoxib (CXB) is a Biopharmaceutical Classification System (BCS) Class II molecule with high permeability that is practically insoluble in water. ...
PMC11531807
core_pubmed_pmc
Pharmacokinetics of ceftriaxone, gentamicin, meropenem and vancomycin in liver cirrhosis: a systematic review
Pharmacokinetics of ceftriaxone, gentamicin, meropenem and vancomycin in liver cirrhosis: a systematic review Abstract Abstract Objectives Patients with liver cirrhosis are prone to develop severe bacterial infections. Pharmacokinetics (PK) of antibiotics in cirrhosis are potentially affected by impaired biotransformat...
PMC12318716
core_pubmed_pmc
MiR-132 inhibition improves myocardial strain in a large animal model of chronic left ventricular adverse remodelling
MiR-132 inhibition improves myocardial strain in a large animal model of chronic left ventricular adverse remodelling Abstract Abstract Aims Cardiac miR-132 has been proposed as a target for heart failure (HF) therapy. CDR132L, a rationally designed synthetic oligonucleotide inhibitor of miR-132 has proved pre-clinical...
PMC6278122
core_pubmed_pmc
Exploratory evaluation of pharmacodynamics, pharmacokinetics and safety of rivaroxaban in children and adolescents: an EINSTEIN-Jr phase I study
Exploratory evaluation of pharmacodynamics, pharmacokinetics and safety of rivaroxaban in children and adolescents: an EINSTEIN-Jr phase I study Abstract Abstract Background The EINSTEIN-Jr program will evaluate rivaroxaban for the treatment of venous thromboembolism (VTE) in children, targeting exposures similar to th...
PMC7413516
core_pubmed_pmc
Antidepressant-like activity and safety profile evaluation of 1 H -imidazo[2,1- f ]purine-2,4(3H,8H)-dione derivatives as 5-HT 1A receptor partial agonists
Antidepressant-like activity and safety profile evaluation of 1 H -imidazo[2,1- f ]purine-2,4(3H,8H)-dione derivatives as 5-HT 1A receptor partial agonists Abstract Abstract Current antidepressant therapy has several disadvantages related to the properties of antidepressants. Considering their unfavourable features, th...
PMC11226858
core_pubmed_pmc
The Role of Pharmacogenomics Studies for Precision Medicine Among Ethiopian Patients and Their Clinical Implications: A Scoping Review
The Role of Pharmacogenomics Studies for Precision Medicine Among Ethiopian Patients and Their Clinical Implications: A Scoping Review Abstract Abstract Background Pharmacogenomics research is currently revolutionizing treatment optimization by discovering molecular markers. Medicines are the cornerstone of treatment f...
PMC9058874
core_pubmed_pmc
Mechanisms of Reduced Susceptibility to Cefiderocol Among Isolates from the CREDIBLE-CR and APEKS-NP Clinical Trials
Mechanisms of Reduced Susceptibility to Cefiderocol Among Isolates from the CREDIBLE-CR and APEKS-NP Clinical Trials Abstract Abstract The objective of this study was to characterize isolates with reduced susceptibility to cefiderocol in patients receiving cefiderocol for nosocomial pneumonia or carbapenem-resistant in...
PMC4896039
core_pubmed_pmc
Incorporating pharmacodynamic considerations into caffeine therapeutic drug monitoring in preterm neonates
Incorporating pharmacodynamic considerations into caffeine therapeutic drug monitoring in preterm neonates Abstract Background This study sought to assess the pharmacokinetic and pharmacodynamic relationships of caffeine citrate therapy in preterm neonates who had therapeutic drug monitoring (TDM) in the post-extubatio...
PMC12614971
core_pubmed_pmc
Deriving Dosages for Levofloxacin Tuberculosis Preventive Treatment for Young People Exposed to Rifampicin-Resistant Tuberculosis
Deriving Dosages for Levofloxacin Tuberculosis Preventive Treatment for Young People Exposed to Rifampicin-Resistant Tuberculosis Abstract Abstract Background Tuberculosis (TB) is the leading single bacterial cause of death worldwide. In 2023, approximately 400 000 people developed multidrug- and rifampicin-resistant T...
PMC12479079
core_pubmed_pmc
Quantitative Train-of-Four Monitoring Using the TetraGraph™ to Evaluate Rocuronium Requirements During Renal Transplantation in a Pediatric Patient
Quantitative Train-of-Four Monitoring Using the TetraGraph™ to Evaluate Rocuronium Requirements During Renal Transplantation in a Pediatric Patient Abstract Abstract The pharmacokinetics of neuromuscular blocking agents (NMBAs) may be altered in patients with renal insufficiency or failure, including alterations in the...
PMC5508362
core_pubmed_pmc
Pharmacokinetics and Relative Bioavailability of Orally Administered Innovator‐Formulated Itraconazole Capsules and Solution in Healthy Dogs
Pharmacokinetics and Relative Bioavailability of Orally Administered Innovator‐Formulated Itraconazole Capsules and Solution in Healthy Dogs Abstract Abstract Background Itraconazole is commonly used for treatment of systemic and cutaneous mycoses in veterinary medicine. Two formulations, capsule and solution, are used...
PMC5108428
core_pubmed_pmc
Impact of Increased Gastric pH on the Pharmacokinetics of Evacetrapib in Healthy Subjects
Impact of Increased Gastric pH on the Pharmacokinetics of Evacetrapib in Healthy Subjects Abstract Study Objective To examine the effect of increased gastric pH on exposure to evacetrapib, a cholesteryl ester transfer protein inhibitor evaluated for the treatment of atherosclerotic heart disease. Design Open‐label, two...
PMC2809740
core_pubmed_pmc
Postcoital Bioavailability and Antiviral Activity of 0.5% PRO 2000 Gel: Implications for Future Microbicide Clinical Trials
Postcoital Bioavailability and Antiviral Activity of 0.5% PRO 2000 Gel: Implications for Future Microbicide Clinical Trials Abstract Abstract Background The pharmacokinetics and pharmacodynamics of vaginal microbicides are typically assessed among sexually abstinent women. However, the physical act of sex may modulate ...
PMC9502522
core_pubmed_pmc
Acyldepsipeptide Analogues: A Future Generation Antibiotics for Tuberculosis Treatment
Acyldepsipeptide Analogues: A Future Generation Antibiotics for Tuberculosis Treatment Abstract Acyldepsipeptides (ADEPs) are a new class of emerging antimicrobial peptides (AMPs), which are currently explored for treatment of pathogenic infections, including tuberculosis (TB). These cyclic hydrophobic peptides have a ...
PMC3286478
core_pubmed_pmc
HemaMax™, a Recombinant Human Interleukin-12, Is a Potent Mitigator of Acute Radiation Injury in Mice and Non-Human Primates
HemaMax™, a Recombinant Human Interleukin-12, Is a Potent Mitigator of Acute Radiation Injury in Mice and Non-Human Primates Abstract Abstract HemaMax, a recombinant human interleukin-12 (IL-12), is under development to address an unmet medical need for effective treatments against acute radiation syndrome due to radio...
PMC10581956
core_pubmed_pmc
Do the Outcomes of Clinical Efficacy Trials Matter in Regulatory Decision-Making for Biosimilars?
Do the Outcomes of Clinical Efficacy Trials Matter in Regulatory Decision-Making for Biosimilars? Abstract Abstract Background There is an increasing body of evidence supporting a more flexible approach in clinical data requirements for the approval of more complex biosimilar substances such as monoclonal antibodies (m...
PMC7780923
core_pubmed_pmc
Review of Questions Concerning Clinical Drug Interactions in ADHD Treatment From Physicians in Norway
Review of Questions Concerning Clinical Drug Interactions in ADHD Treatment From Physicians in Norway Abstract Abstract Pharmacological treatment of attention deficit hyperactivity disorder (ADHD) is challenging due to a wide age span among patients, risk of reduced adherence, and comorbidities like psychiatric disorde...
PMC7865387
core_pubmed_pmc
Artemether-Loaded Zein Nanoparticles: An Innovative Intravenous Dosage Form for the Management of Severe Malaria
Artemether-Loaded Zein Nanoparticles: An Innovative Intravenous Dosage Form for the Management of Severe Malaria Abstract Abstract Artemether, an artemisinin derivative, is used in the management of life-threatening severe malaria. This study aimed to develop an intravenous dosage form of artemether using nanotechnolog...
PMC9738279
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Dosing Considerations of Novel β-Lactams and β-Lactam/β-Lactamase Inhibitors in Critically Ill Adult Patients: Focus on Obesity, Augmented Renal Clearance, Renal Replacement Therapies, and Extracorporeal Membrane Oxygenation
Pharmacokinetics, Pharmacodynamics, and Dosing Considerations of Novel β-Lactams and β-Lactam/β-Lactamase Inhibitors in Critically Ill Adult Patients: Focus on Obesity, Augmented Renal Clearance, Renal Replacement Therapies, and Extracorporeal Membrane Oxygenation Abstract Abstract Objective: Dose optimization of novel...
PMC11494486
core_pubmed_pmc
Elucidation of DPP‐4 involvement in systemic distribution and renal reabsorption of linagliptin by PBPK modeling with a cluster Gauss–Newton method
Elucidation of DPP‐4 involvement in systemic distribution and renal reabsorption of linagliptin by PBPK modeling with a cluster Gauss–Newton method Abstract Abstract The dipeptidyl peptidase‐4 (DPP‐4) inhibitor linagliptin (LNG) exhibits target‐mediated drug disposition (TMDD) in clinical settings, characterized by sat...
PMC6422836
core_pubmed_pmc
Phase 2 clinical trial of PBI-4050 in patients with idiopathic pulmonary fibrosis
Phase 2 clinical trial of PBI-4050 in patients with idiopathic pulmonary fibrosis Abstract PBI-4050 is a novel orally active small-molecule compound with demonstrated anti-fibrotic activity in several models of fibrosis, including lung fibrosis. We present results from our first clinical study of PBI-4050 in patients w...
PMC9209747
core_pubmed_pmc
Wee1 kinase inhibitor adavosertib with radiation in newly diagnosed diffuse intrinsic pontine glioma: A Children’s Oncology Group phase I consortium study
Wee1 kinase inhibitor adavosertib with radiation in newly diagnosed diffuse intrinsic pontine glioma: A Children’s Oncology Group phase I consortium study Abstract Abstract Background Children with diffuse intrinsic pontine gliomas (DIPG) have a dismal prognosis. Adavosertib (AZD1775) is an orally available, blood-brai...
PMC11192828
core_pubmed_pmc
Population Pharmacokinetics of Adalimumab in Juvenile Idiopathic Arthritis Patients: A Retrospective Cohort Study Using Clinical Care Data
Population Pharmacokinetics of Adalimumab in Juvenile Idiopathic Arthritis Patients: A Retrospective Cohort Study Using Clinical Care Data Abstract Abstract Background and Objective Juvenile idiopathic arthritis (JIA) is a chronic autoimmune disorder that primarily affects the joints in children. Notably, it is known t...
PMC11844388
core_pubmed_pmc
Cethromycin Pharmacokinetics and Pharmacodynamics for Single Dose Cure of Plasmodium berghei Liver Stages
Cethromycin Pharmacokinetics and Pharmacodynamics for Single Dose Cure of Plasmodium berghei Liver Stages Abstract Abstract Cethromycin combines a quinoline nucleus and a macrolide for broad spectrum antibacterial and antiprotozoan activity. Here we characterized the murine pharmacokinetics and Plasmodium berghei lifec...
PMC7911305
core_pubmed_pmc
Efficacy of Providing the PI3K p110α Inhibitor BYL719 (Alpelisib) to Middle-Aged Mice in Their Diet
Efficacy of Providing the PI3K p110α Inhibitor BYL719 (Alpelisib) to Middle-Aged Mice in Their Diet Abstract Abstract BYL719 (alpelisib) is a small molecule inhibitor of PI3K p110α developed for cancer therapy. Targeted suppression of PI3K has led to lifespan extension in rodents and model organisms. If PI3K inhibitors...
PMC9998255
core_pubmed_pmc
Anti-fibrotic effect of aurocyanide, the active metabolite of auranofin
Anti-fibrotic effect of aurocyanide, the active metabolite of auranofin Abstract Abstract Drug repositioning has gained significant attention over the past several years. The anti-rheumatoid arthritis drug auranofin has been investigated for the treatment of other diseases, including liver fibrosis. Because auranofin i...
PMC7497683
core_pubmed_pmc
Phase I study of metformin in combination with carboplatin/paclitaxel chemotherapy in patients with advanced epithelial ovarian cancer
Phase I study of metformin in combination with carboplatin/paclitaxel chemotherapy in patients with advanced epithelial ovarian cancer Abstract Summary Background Metformin use is associated with reduced cancer risk in epidemiological studies and has preclinical anti-cancer activity in ovarian cancer models. The primar...
PMC3988383
core_pubmed_pmc
The effect of transdermal scopolamine for the prevention of postoperative nausea and vomiting
The effect of transdermal scopolamine for the prevention of postoperative nausea and vomiting Abstract Abstract Postoperative nausea and vomiting (PONV) is one of the most common and undesirable complaints recorded in as many as 70–80% of high-risk surgical patients. The current prophylactic therapy recommendations for...
PMC10853358
core_pubmed_pmc
Are novel oral oncolytics underdosed in obese patients?
Are novel oral oncolytics underdosed in obese patients? Abstract Purpose Data on the effects of obesity on drug exposure of oral targeted oncolytics is scarce. Therefore, the aim of this study was to investigate the influence of body weight and body mass index (BMI) on trough levels of oral oncolytics with an exposure–...
PMC8466444
core_pubmed_pmc
Pharmacist-Led Medication Evaluation Considering Pharmacogenomics and Drug-Induced Phenoconversion in the Treatment of Multiple Comorbidities: A Case Report
Pharmacist-Led Medication Evaluation Considering Pharmacogenomics and Drug-Induced Phenoconversion in the Treatment of Multiple Comorbidities: A Case Report Abstract Pharmacogenomic (PGx) information can guide drug and dose selection, optimize therapy outcomes, and/or decrease the risk of adverse drug events (ADEs). Th...
PMC11540769
core_pubmed_pmc
Pharmacokinetics study of atracurium, dexmedetomidine, midazolam and 1-hydroxymidazolam in patients undergoing acute aortic dissection surgery
Pharmacokinetics study of atracurium, dexmedetomidine, midazolam and 1-hydroxymidazolam in patients undergoing acute aortic dissection surgery Abstract Objective An UPLC-MS/MS method was developed and validated for simultaneous determination of atracurium (ATC), dexmedetomidine (DEX), midazolam (MDZ) and 1-hydroxymidaz...
PMC12736256
core_pubmed_pmc
The Impact of Maternal BMI on the Efficacy and Safety of Oral Misoprostol for Labor Induction
The Impact of Maternal BMI on the Efficacy and Safety of Oral Misoprostol for Labor Induction Abstract Background : Maternal obesity may influence the efficacy and course of induction of labor (IoL). Misoprostol, a prostaglandin E1 analogue, is widely used for cervical ripening, but evidence regarding its effectiveness...
PMC7499073
core_pubmed_pmc
Synthesis, characterization and computational study on potential inhibitory action of novel azo imidazole derivatives against COVID-19 main protease (M pro : 6LU7)
Synthesis, characterization and computational study on potential inhibitory action of novel azo imidazole derivatives against COVID-19 main protease (M pro : 6LU7) Abstract Highlights • Six azo imidazole derivatives have been synthesized and characterized by spectroscopic and analytical tools. • Inhibitory potential ag...
PMC9935805
core_pubmed_pmc
Molecular Modeling Identification of Key Secondary Metabolites from Xylopia aethiopica as Promising Therapeutics Targeting Essential Measles Viral Proteins
Molecular Modeling Identification of Key Secondary Metabolites from Xylopia aethiopica as Promising Therapeutics Targeting Essential Measles Viral Proteins Abstract This study computationally screened three key compounds (vanillin (VAN), oxophoebine (OPB), and dihydrochalcone (DHC)) derived from Xylopia aethiopica (Gui...
PMC11198855
core_pubmed_pmc
Computational evaluation of efflux pump homologues and lignans as potent inhibitors against multidrug-resistant Salmonella typhi
Computational evaluation of efflux pump homologues and lignans as potent inhibitors against multidrug-resistant Salmonella typhi Abstract Typhoid fever, caused by Salmonella enterica serovar typhi , presents a substantial global health threat, particularly in regions with limited healthcare infrastructure. The rise of ...
PMC12037592
core_pubmed_pmc
Carbapenem treatment options for metallo-beta-lactamase: drug screening and dose optimization of meropenem-based combinations against NDM- or IMP-producing Klebsiella pneumoniae
Carbapenem treatment options for metallo-beta-lactamase: drug screening and dose optimization of meropenem-based combinations against NDM- or IMP-producing Klebsiella pneumoniae Abstract Abstract Background The global dissemination of carbapenemase-producing Klebsiella pneumoniae (CPKP) has been occurring at an alarmin...
PMC10527716
core_pubmed_pmc
Therapeutic Oligonucleotides: An Outlook on Chemical Strategies to Improve Endosomal Trafficking
Therapeutic Oligonucleotides: An Outlook on Chemical Strategies to Improve Endosomal Trafficking Abstract Abstract The potential of oligonucleotide therapeutics is undeniable as more than 15 drugs have been approved to treat various diseases in the liver, central nervous system (CNS), and muscles. However, achieving ef...
PMC9049505
core_pubmed_pmc
Drug therapy problems and predicting factors among ambulatory epileptic patients in Jimma Medical Center, Southwest Ethiopia
Drug therapy problems and predicting factors among ambulatory epileptic patients in Jimma Medical Center, Southwest Ethiopia Abstract Abstract Background The care of epileptic patients is complicated by the cognitive adverse effect of the drug, disease, pharmacokinetics, and pharmacodynamics properties of antiepileptic...
PMC7894442
core_pubmed_pmc
Pharmacokinetics and efficacy of a ketorolac-loaded ocular coil in New Zealand white rabbits
Pharmacokinetics and efficacy of a ketorolac-loaded ocular coil in New Zealand white rabbits Abstract Abstract Eye drops are considered standard practice for the delivery of ocular drugs. However, low patient compliance and low drug levels compromise its effectiveness. Our group developed a ketorolac-loaded ocular coil...
PMC11965789
core_pubmed_pmc
Rapid Differentiation of False Positives of Galactomannan Related to Contaminated Intravenous Fluids via a Pharmacokinetics Model and Innovative Web-Based Tool
Rapid Differentiation of False Positives of Galactomannan Related to Contaminated Intravenous Fluids via a Pharmacokinetics Model and Innovative Web-Based Tool Abstract Abstract This study developed a pharmacokinetic model and web-based tool to distinguish true invasive aspergillosis from false positives caused by cont...
PMC10715703
core_pubmed_pmc
A study of the pharmacokinetics, safety, and efficacy of bictegravir/emtricitabine/tenofovir alafenamide in virologically suppressed pregnant women with HIV
A study of the pharmacokinetics, safety, and efficacy of bictegravir/emtricitabine/tenofovir alafenamide in virologically suppressed pregnant women with HIV Abstract Abstract Objective: The objective of this study was to assess the pharmacokinetics, safety, and efficacy and confirm the dose of once-daily bictegravir/em...
PMC7961380
core_pubmed_pmc
A Systematic Study of the In Vitro Pharmacokinetics and Estimated Human In Vivo Clearance of Indole and Indazole-3-Carboxamide Synthetic Cannabinoid Receptor Agonists Detected on the Illicit Drug Market
A Systematic Study of the In Vitro Pharmacokinetics and Estimated Human In Vivo Clearance of Indole and Indazole-3-Carboxamide Synthetic Cannabinoid Receptor Agonists Detected on the Illicit Drug Market Abstract Abstract In vitro pharmacokinetic studies were conducted on enantiomer pairs of twelve valinate or tert -leu...
PMC9231005
core_pubmed_pmc
Pharmacokinetic Modeling of Hydrocortisone by Including Protein Binding to Corticosteroid-Binding Globulin
Pharmacokinetic Modeling of Hydrocortisone by Including Protein Binding to Corticosteroid-Binding Globulin Abstract Background: Patients with adrenal insufficiency are treated with oral hydrocortisone (HC) to compensate for the loss of endogenous cortisol production. Intrinsic imperfections of cortisol replacement stra...
PMC8585829
core_pubmed_pmc
Analgesic effect of oral ibuprofen 400, 600, and 800 mg; paracetamol 500 and 1000 mg; and paracetamol 1000 mg plus 60 mg codeine in acute postoperative pain: a single-dose, randomized, placebo-controlled, and double-blind study
Analgesic effect of oral ibuprofen 400, 600, and 800 mg; paracetamol 500 and 1000 mg; and paracetamol 1000 mg plus 60 mg codeine in acute postoperative pain: a single-dose, randomized, placebo-controlled, and double-blind study Abstract Purpose Effect size estimates of analgesic drugs can be misleading. Ibuprofen (400 ...
PMC12433209
core_pubmed_pmc
Shatai Heji Mitigates Sjögren Disease-Induced Xerostomia by Regulating AQP5, NF-κB, and p38 MAPK Signaling Pathwaysaff
Shatai Heji Mitigates Sjögren Disease-Induced Xerostomia by Regulating AQP5, NF-κB, and p38 MAPK Signaling Pathwaysaff Abstract Abstract Introduction Xerostomia, commonly caused by Sjögren disease (SjD) or head and neck radiotherapy, significantly impairs patients’ quality of life, yet effective treatments remain limit...
PMC5481453
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic modeling of cyadox against Clostridium perfringens in swine
Pharmacokinetic and pharmacodynamic modeling of cyadox against Clostridium perfringens in swine Abstract Abstract The purpose of this study was to evaluate the activity of cyadox against Clostridium perfringens in swine and optimize the dosage regimen using ex vivo pharmacokinetic-pharmacodynamic (PK-PD) modeling. Afte...
PMC11515656
core_pubmed_pmc
Preclinical and first-in-human evaluation of AL002, a novel TREM2 agonistic antibody for Alzheimer’s disease
Preclinical and first-in-human evaluation of AL002, a novel TREM2 agonistic antibody for Alzheimer’s disease Abstract Abstract Background Variants of the gene triggering receptor expressed on myeloid cells-2 (TREM2) increase the risk of Alzheimer’s disease (AD) and other neurodegenerative disorders. Signaling by TREM2,...
PMC9286718
core_pubmed_pmc
Quantitative systems pharmacology modeling provides insight into inter‐mouse variability of Anti‐CTLA4 response
Quantitative systems pharmacology modeling provides insight into inter‐mouse variability of Anti‐CTLA4 response Abstract Abstract Clinical responses of immuno‐oncology therapies are highly variable among patients. Similar response variability has been observed in syngeneic mouse models. Understanding of the variability...
PMC7032255
core_pubmed_pmc
PEPT1-mediated prodrug strategy for oral delivery of peramivir
PEPT1-mediated prodrug strategy for oral delivery of peramivir Abstract Abstract Peramivir was a novel and highly potent neuraminidase (NA) inhibitor for the treatment of influenza A and B. However, it exhibited a very low oral bioavailability (only 3%) due to the high polarity (log P of −1.4) and the low membrane perm...
PMC12190963
core_pubmed_pmc
Drug-Coated Balloon PCI in Different Plaque Morphologies: A Narrative Review
Drug-Coated Balloon PCI in Different Plaque Morphologies: A Narrative Review Abstract The evolution of percutaneous coronary intervention (PCI) has led to significant advances in drug-coated balloon (DCB) technology, offering a stent-free alternative for treating coronary artery disease. While paclitaxel-coated balloon...
PMC9167418
core_pubmed_pmc
Evaluation of the Effect of Food on the Pharmacokinetics of SHR6390, An Oral CDK4/6 Inhibitor, in Healthy Volunteers
Evaluation of the Effect of Food on the Pharmacokinetics of SHR6390, An Oral CDK4/6 Inhibitor, in Healthy Volunteers Abstract Abstract Background and Introduction SHR6390 is a new developed highly effective and selective small-molecule oral CDK4/6 inhibitor. We aimed to evaluate the effect of food on the pharmacokineti...
PMC11843613
core_pubmed_pmc
Further Optimization of the mGlu 1 PAM VU6024578/BI02982816: Discovery and Characterization of VU6033685
Further Optimization of the mGlu 1 PAM VU6024578/BI02982816: Discovery and Characterization of VU6033685 Abstract Abstract Herein, we report the further chemical optimization of the metabotropic glutamate receptor subtype 1 (mGlu 1 ) positive allosteric modulator (PAM) VU6024578/BI02982816 and the discovery of VU603368...
PMC7855969
core_pubmed_pmc
Single Dose Study Assessing the Pharmacokinetic and Metabolic Profile of Alverine Citrate in Healthy Volunteers
Single Dose Study Assessing the Pharmacokinetic and Metabolic Profile of Alverine Citrate in Healthy Volunteers Abstract Alverine citrate is a spasmolytic commonly prescribed in conditions such as irritable bowel syndrome, painful diverticular disease of the colon, and primary dysmenorrhea. While clinical efficacy data...
PMC10892872
core_pubmed_pmc
Interspecies Brain PBPK Modeling Platform to Predict Passive Transport through the Blood–Brain Barrier and Assess Target Site Disposition
Interspecies Brain PBPK Modeling Platform to Predict Passive Transport through the Blood–Brain Barrier and Assess Target Site Disposition Abstract Abstract The high failure rate of central nervous system (CNS) drugs is partly associated with an insufficient understanding of target site exposure. Blood–brain barrier (BB...
PMC12801895
core_pubmed_pmc
Machine learning to predict food effects during drug development: a comprehensive review
Machine learning to predict food effects during drug development: a comprehensive review Abstract Abstract Drug absorption can be altered due to the consumption of food, impacting the efficacy and safety of the drug administered, and predicting food effects (FE) can be quite complex. Traditional methods, including in v...
PMC12946594
core_pubmed_pmc
Effects of High‐ and Low‐Fat Meals on the Bioavailability and Pharmacokinetics of Votoplam, a HTT Gene Splicing Modifier
Effects of High‐ and Low‐Fat Meals on the Bioavailability and Pharmacokinetics of Votoplam, a HTT Gene Splicing Modifier Abstract Abstract Votoplam is a novel, orally bioavailable, small molecule HTT gene splicing modifier that is being developed for the treatment of Huntington's disease. This was a single dose, open‐l...
PMC5950942
core_pubmed_pmc
The Effect of Undaria pinnatifida Fucoidan on the Pharmacokinetics of Letrozole and Tamoxifen in Patients With Breast Cancer
The Effect of Undaria pinnatifida Fucoidan on the Pharmacokinetics of Letrozole and Tamoxifen in Patients With Breast Cancer Abstract Background: Although the use of complementary and alternative medicines is widespread in cancer patients, clinical evidence of their benefits is sparse. Furthermore, while they are often...
PMC5573753
core_pubmed_pmc
A review of oral cannabinoids and medical marijuana for the treatment of chemotherapy-induced nausea and vomiting: a focus on pharmacokinetic variability and pharmacodynamics
A review of oral cannabinoids and medical marijuana for the treatment of chemotherapy-induced nausea and vomiting: a focus on pharmacokinetic variability and pharmacodynamics Abstract Abstract Purpose Oral cannabinoids (i.e., dronabinol, nabilone) containing the active component of marijuana, delta(Δ)9-tetrahydrocannab...
PMC12338012
core_pubmed_pmc
A Phase 1, Double‐Blind, Placebo‐Controlled Trial of Sevasemten (EDG‐5506), a Selective Modulator of Fast Skeletal Muscle Contraction, in Healthy Volunteers and Adults With Becker Muscular Dystrophy
A Phase 1, Double‐Blind, Placebo‐Controlled Trial of Sevasemten (EDG‐5506), a Selective Modulator of Fast Skeletal Muscle Contraction, in Healthy Volunteers and Adults With Becker Muscular Dystrophy Abstract ABSTRACT Introduction/Aims Sevasemten (EDG‐5506) is an orally administered, investigational small molecule that ...
PMC3409546
core_pubmed_pmc
Doripenem Dosing Recommendations for Critically Ill Patients Receiving Continuous Renal Replacement Therapy
Doripenem Dosing Recommendations for Critically Ill Patients Receiving Continuous Renal Replacement Therapy Abstract Abstract Doripenem dosing regimens for patients receiving continuous venovenous hemofiltration (CVVH) and continuous venovenous hemodiafiltration (CVVHDF) were devised based on an established efficacy cr...
PMC6153434
core_pubmed_pmc
Bystander Effects of Hypoxia-Activated Prodrugs: Agent-Based Modeling Using Three Dimensional Cell Cultures
Bystander Effects of Hypoxia-Activated Prodrugs: Agent-Based Modeling Using Three Dimensional Cell Cultures Abstract Intra-tumor heterogeneity represents a major barrier to anti-cancer therapies. One strategy to minimize this limitation relies on bystander effects via diffusion of cytotoxins from targeted cells. Hypoxi...
PMC11667036
core_pubmed_pmc
In vivo pharmacokinetic and pharmacodynamic study and cutoff of florfenicol against Riemerella anatipestifer in ducks
In vivo pharmacokinetic and pharmacodynamic study and cutoff of florfenicol against Riemerella anatipestifer in ducks Abstract Abstract Riemerella anatipestifer causes serious infections, characterized by septicemia and serositis, in ducks and geese. R. anatipestifer is mainly controlled through antimicrobial chemother...
PMC8890714
core_pubmed_pmc
Clinically translatable cytokine delivery platform for eradication of intraperitoneal tumors
Clinically translatable cytokine delivery platform for eradication of intraperitoneal tumors Abstract Abstract Proinflammatory cytokines have been approved by the Food and Drug Administration for the treatment of metastatic melanoma and renal carcinoma. However, effective cytokine therapy requires high-dose infusions t...
PMC11609056
core_pubmed_pmc
Population Pharmacokinetics Modeling and Simulation of Deutenzalutamide, A Novel Androgen Receptor Antagonist, in Patients With Metastatic Castration‐Resistant Prostate Cancer
Population Pharmacokinetics Modeling and Simulation of Deutenzalutamide, A Novel Androgen Receptor Antagonist, in Patients With Metastatic Castration‐Resistant Prostate Cancer Abstract Abstract Deutenzalutamide is a new molecular entity androgen receptor antagonist. The primary aim of this study was to develop a popula...
PMC11921678
core_pubmed_pmc
ADME gene-driven prognostic model for bladder cancer: a breakthrough in predicting survival and personalized treatment
ADME gene-driven prognostic model for bladder cancer: a breakthrough in predicting survival and personalized treatment Abstract Abstract Background Genes that participate in the absorption, distribution, metabolism, excretion (ADME) processes occupy a central role in pharmacokinetics. Meanwhile, variability in clinical...
PMC6591842
core_pubmed_pmc
Determination and pharmacokinetics study of oxyclozanide suspension in cattle by LC-MS/MS
Determination and pharmacokinetics study of oxyclozanide suspension in cattle by LC-MS/MS Abstract Background Oxyclozanide is an anthelmintic drug that is widely used to treat fasciolosis . However, the pharmacokinetics of oxyclozanide in cattle are not yet clearly understood. The present study was designed to develop ...
PMC11125810
core_pubmed_pmc
Poly(acrylic acid)/Poly(vinyl alcohol) Microarray Patches for Continuous Transdermal Delivery of Levodopa and Carbidopa: In Vitro and In Vivo Studies
Poly(acrylic acid)/Poly(vinyl alcohol) Microarray Patches for Continuous Transdermal Delivery of Levodopa and Carbidopa: In Vitro and In Vivo Studies Abstract Levodopa (LD) has been the most efficacious medication and the gold standard therapy for Parkinson’s disease (PD) for decades. However, its long-term administrat...
PMC10456269
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Drug–Drug Interactions: Research Methods and Applications
Pharmacokinetic and Pharmacodynamic Drug–Drug Interactions: Research Methods and Applications Abstract Because of the high research and development cost of new drugs, the long development process of new drugs, and the high failure rate at later stages, combining past drugs has gradually become a more economical and att...
PMC9249715
core_pubmed_pmc
Pooled Population Pharmacokinetic Analysis for Exploring Ciprofloxacin Pharmacokinetic Variability in Intensive Care Patients
Pooled Population Pharmacokinetic Analysis for Exploring Ciprofloxacin Pharmacokinetic Variability in Intensive Care Patients Abstract Background and Objective Previous pharmacokinetic (PK) studies of ciprofloxacin in intensive care (ICU) patients have shown large differences in estimated PK parameters, suggesting that...
PMC12703252
core_pubmed_pmc
Clinical results of an HBV-specific T-cell receptor-T-cell therapy (SCG101) in patients with HBV-related hepatocellular carcinoma treated in an investigator-initiated, interventional trial
Clinical results of an HBV-specific T-cell receptor-T-cell therapy (SCG101) in patients with HBV-related hepatocellular carcinoma treated in an investigator-initiated, interventional trial Abstract Abstract Background SCG101 is an autologous T-cell therapy specifically targeting hepatitis B virus (HBV) using a natural,...
PMC7023162
core_pubmed_pmc
Challenges and Opportunities in Preclinical Research of Synthetic Cannabinoids for Pain Therapy
Challenges and Opportunities in Preclinical Research of Synthetic Cannabinoids for Pain Therapy Abstract Abstract Cannabis has been used in pain management since 2900 BC. In the 20th century, synthetic cannabinoids began to emerge, thus opening the way for improved efficacy. The search for new forms of synthetic cannab...
PMC7965837
core_pubmed_pmc
Pretomanid dose selection for pulmonary tuberculosis: An application of multi‐objective optimization to dosage regimen design
Pretomanid dose selection for pulmonary tuberculosis: An application of multi‐objective optimization to dosage regimen design Abstract Abstract Clinical development of combination chemotherapies for tuberculosis (TB) is complicated by partial or restricted phase II dose‐finding. Barriers include a propensity for drug r...
PMC10427541
core_pubmed_pmc
In vitro activity of aztreonam–avibactam against Enterobacterales isolates collected in Latin America, Africa/Middle East, Asia, and Eurasia for the ATLAS Global Surveillance Program in 2019–2021
In vitro activity of aztreonam–avibactam against Enterobacterales isolates collected in Latin America, Africa/Middle East, Asia, and Eurasia for the ATLAS Global Surveillance Program in 2019–2021 Abstract This study aimed to report reference method antimicrobial susceptibility results for 24,937 recent (2019–2021) clin...
PMC12736829
core_pubmed_pmc
Advances in Drug Delivery Science for Diacerein: Strategies to Enhance Solubility, Bioavailability, and Pharmacokinetic Performance
Advances in Drug Delivery Science for Diacerein: Strategies to Enhance Solubility, Bioavailability, and Pharmacokinetic Performance Abstract Diacerein is known as a disease-modifying anti-inflammatory drug, primarily used for the treatment of osteoarthritis. Despite its therapeutic potential, the clinical use of diacer...
PMC7481307
core_pubmed_pmc
Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) with OT-82 induces DNA damage, cell death, and suppression of tumor growth in preclinical models of Ewing sarcoma
Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) with OT-82 induces DNA damage, cell death, and suppression of tumor growth in preclinical models of Ewing sarcoma Abstract Abstract NAMPT mediates the rate-limiting step of the NAD salvage pathway, which maintains cellular bioenergetics and provides a necessa...
PMC8370193
core_pubmed_pmc
Pharmacokinetics and Bioequivalence of Isavuconazole Administered as Isavuconazonium Sulfate Intravenous Solution via Nasogastric Tube or Orally in Healthy Subjects
Pharmacokinetics and Bioequivalence of Isavuconazole Administered as Isavuconazonium Sulfate Intravenous Solution via Nasogastric Tube or Orally in Healthy Subjects Abstract ABSTRACT For critically ill patients with invasive fungal infections, a nasogastric (NG) tube can be an alternative route for administration of is...
PMC5178048
core_pubmed_pmc
Opinion of stakeholders on existing curriculum for postgraduate (MD) course in Pharmacology: A survey
Opinion of stakeholders on existing curriculum for postgraduate (MD) course in Pharmacology: A survey Abstract Objectives: To survey the opinion about various curricular components of Doctor of Medicine (MD) pharmacology curriculum in India by stakeholders, including faculty and students. Materials and Methods: An onli...
PMC6240080
core_pubmed_pmc
Mechanistic Interaction Study of Bromo-Noscapine with Bovine Serum Albumin employing Spectroscopic and Chemoinformatics Approaches
Mechanistic Interaction Study of Bromo-Noscapine with Bovine Serum Albumin employing Spectroscopic and Chemoinformatics Approaches Abstract Abstract Bromo-Noscapine (BrNs) is a tubulin-binding cytotoxic agent with significant activity against breast and lung cancer. The mechanistic interaction insight into the binding ...
PMC12024021
core_pubmed_pmc
Do Critically Ill Patients Undergoing Continuous Renal Replacement Therapy Require Ceftaroline Dosage Adjustments? Ceftaroline PopPK Model and Dosage Simulations with the Probability of Target Attainment Analysis Based on Retrospective Data †
Do Critically Ill Patients Undergoing Continuous Renal Replacement Therapy Require Ceftaroline Dosage Adjustments? Ceftaroline PopPK Model and Dosage Simulations with the Probability of Target Attainment Analysis Based on Retrospective Data † Abstract Abstract Objectives : We aimed to develop a population pharmacokinet...
PMC3398252
core_pubmed_pmc
Dissolution and pharmacokinetics of a novel micronized aspirin formulation
Dissolution and pharmacokinetics of a novel micronized aspirin formulation Abstract Abstract Aspirin (acetylsalicylic acid, ASA) has been used as an analgesic, antipyretic and antiinflammatory drug for many years. A new 500 mg aspirin tablet formulation containing micronized active ingredient and an effervescent compon...
PMC8045405
core_pubmed_pmc
Phase I dose-escalation oncology trials with sequential multiple schedules
Phase I dose-escalation oncology trials with sequential multiple schedules Abstract Background Conventional methods for phase I dose-escalation trials in oncology are based on a single treatment schedule only. More recently, however, multiple schedules are more frequently investigated in the same trial. Methods Here, w...