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PMC9439977
core_pubmed_pmc
Insulin Glargine 300 U/mL Therapy in Children and Adolescents with Type 1 Diabetes
Insulin Glargine 300 U/mL Therapy in Children and Adolescents with Type 1 Diabetes Abstract The pharmacokinetic and pharmacodynamic properties of the second-generation basal insulin glargine 300 Units/mL (Gla-300) may be of benefit in the treatment of type 1 diabetes mellitus (T1DM). Gla-300 provides a stable and susta...
PMC7550323
core_pubmed_pmc
Pharmacokinetic Profile of Gilteritinib: A Novel FLT-3 Tyrosine Kinase Inhibitor
Pharmacokinetic Profile of Gilteritinib: A Novel FLT-3 Tyrosine Kinase Inhibitor Abstract Abstract Background and Objective Gilteritinib is a novel, highly selective tyrosine kinase inhibitor approved in the USA, Canada, Europe, Brazil, Korea, and Japan for the treatment of FLT3 mutation-positive acute myeloid leukemia...
PMC9515952
core_pubmed_pmc
Tentative exploration of pharmacodynamic substances: Pharmacological effects, chemical compositions, and multi-components pharmacokinetic characteristics of ESZWD in CHF-HKYd rats
Tentative exploration of pharmacodynamic substances: Pharmacological effects, chemical compositions, and multi-components pharmacokinetic characteristics of ESZWD in CHF-HKYd rats Abstract Abstract The chemical components of Xin'an famous prescription Ershen Zhenwu Decoction (ESZWD) are still unclear. The results showe...
PMC10267849
core_pubmed_pmc
Association of Intraoperative Opioid Administration With Postoperative Pain and Opioid Use
Association of Intraoperative Opioid Administration With Postoperative Pain and Opioid Use Abstract Key Points Question What is the association between intraoperative opioid administration and postoperative pain and opioid use? Findings In this cohort study of 61 249 individuals undergoing surgery, greater intraoperati...
PMC8067632
core_pubmed_pmc
Assessment and Development of the Antifungal Agent Caspofungin for Aerosolized Pulmonary Delivery
Assessment and Development of the Antifungal Agent Caspofungin for Aerosolized Pulmonary Delivery Abstract Invasive Pulmonary Aspergillosis (IPA) and Pneumocystis jiroveci Pneumonia (PCP) are serious fungal pulmonary diseases for immunocompromised patients. The brand name drug CANCIDAS ® (Caspofungin acetate for inject...
PMC12467464
core_pubmed_pmc
Letrozole at the Crossroads of Efficacy and Fetal Safety in Ovulation Induction: A Narrative Review
Letrozole at the Crossroads of Efficacy and Fetal Safety in Ovulation Induction: A Narrative Review Abstract Abstract Letrozole, a third-generation aromatase inhibitor initially developed for breast cancer, has become the preferred first-line agent for ovulation induction (OI), particularly in women with polycystic ova...
PMC4243296
core_pubmed_pmc
Efficacy and safety of pateclizumab (anti-lymphotoxin-α) compared to adalimumab in rheumatoid arthritis: a head-to-head phase 2 randomized controlled study (The ALTARA Study)
Efficacy and safety of pateclizumab (anti-lymphotoxin-α) compared to adalimumab in rheumatoid arthritis: a head-to-head phase 2 randomized controlled study (The ALTARA Study) Abstract Introduction Tumor necrosis factor (TNF) and, possibly, lymphotoxin alpha (LTα) signaling contribute to inflammation and rheumatoid arth...
PMC12927388
core_pubmed_pmc
First-in-human phase 1 dose-escalation study of W0180, an anti-VISTA monoclonal antibody, with and without pembrolizumab in patients with locally advanced or metastatic solid tumours
First-in-human phase 1 dose-escalation study of W0180, an anti-VISTA monoclonal antibody, with and without pembrolizumab in patients with locally advanced or metastatic solid tumours Abstract Abstract Objective W0180 is a humanised IgG1κ antagonistic monoclonal antibody against the V domain-containing immunoglobulin su...
PMC11725995
core_pubmed_pmc
Effects of multiple‐dose administration of zavegepant nasal spray on the single‐dose pharmacokinetics of ethinyl estradiol‐levonorgestrel
Effects of multiple‐dose administration of zavegepant nasal spray on the single‐dose pharmacokinetics of ethinyl estradiol‐levonorgestrel Abstract Abstract Objective The potential for drug–drug interaction of multiple‐dose intranasal zavegepant on the single‐dose oral contraceptive ethinyl estradiol and levonorgestrel ...
PMC8086025
core_pubmed_pmc
A benzopyran with antiarrhythmic activity is an inhibitor of Kir3.1-containing potassium channels
A benzopyran with antiarrhythmic activity is an inhibitor of Kir3.1-containing potassium channels Abstract Atrial fibrillation (AF) is the most commonly diagnosed cardiac arrhythmia and is associated with increased morbidity and mortality. Currently approved AF antiarrhythmic drugs have limited efficacy and/or carry th...
PMC4532344
core_pubmed_pmc
Randomized, open-label, blinded-endpoint, crossover, single-dose study to compare the pharmacodynamics of torasemide-PR 10 mg, torasemide-IR 10 mg, and furosemide-IR 40 mg, in patients with chronic heart failure
Randomized, open-label, blinded-endpoint, crossover, single-dose study to compare the pharmacodynamics of torasemide-PR 10 mg, torasemide-IR 10 mg, and furosemide-IR 40 mg, in patients with chronic heart failure Abstract Abstract Purpose Diuretics are the primary treatment for the management of chronic heart failure (H...
PMC8955144
core_pubmed_pmc
Development and Evaluation of Nanoparticles-in-Film Technology to Achieve Extended In Vivo Exposure of MK-2048 for HIV Prevention
Development and Evaluation of Nanoparticles-in-Film Technology to Achieve Extended In Vivo Exposure of MK-2048 for HIV Prevention Abstract MK-2048 is a second-generation integrase inhibitor active against HIV, which has been applied vaginally using ring formulations. In this work, a nanoparticle-in-film technology was ...
PMC10101132
core_pubmed_pmc
Limited sampling strategies for individualized BAX 855 prophylaxis in severe hemophilia A: in silico evaluation
Limited sampling strategies for individualized BAX 855 prophylaxis in severe hemophilia A: in silico evaluation Abstract Objective Limited sampling strategies (LSS) lower the burden of pharmacokinetic (PK)-guided dosing, but an extensive evaluation of LSS for BAX 855 (Adynovi) is currently lacking. This study aimed to ...
PMC6514017
core_pubmed_pmc
An Update of Current Cannabis-Based Pharmaceuticals in Pain Medicine
An Update of Current Cannabis-Based Pharmaceuticals in Pain Medicine Abstract Cannabis users have long reported therapeutic properties of the plant for a variety of conditions, some of which include nausea, emesis, seizures, cancer, neurogenic diseases and pain control. Research has elucidated many cannabinoid pharmaco...
PMC6510802
core_pubmed_pmc
Pharmacodynamics of evocalcet for secondary hyperparathyroidism in Japanese hemodialysis patients
Pharmacodynamics of evocalcet for secondary hyperparathyroidism in Japanese hemodialysis patients Abstract Background This study investigated the pharmacokinetics, pharmacodynamics, and safety of multiple doses of evocalcet in Japanese secondary hyperparathyroidism (SHPT) patients receiving hemodialysis. Methods In thi...
PMC4302705
core_pubmed_pmc
An open-label, randomized bioavailability study with alternative methods of administration of crushed ticagrelor tablets in healthy volunteers
An open-label, randomized bioavailability study with alternative methods of administration of crushed ticagrelor tablets in healthy volunteers Abstract Abstract Objective: To compare the bioavailability and safety profile of crushed ticagrelor tablets suspended in water and administered orally or via nasogastric tube, ...
PMC7488005
core_pubmed_pmc
Navafenterol (AZD8871) in healthy volunteers: safety, tolerability and pharmacokinetics of multiple ascending doses of this novel inhaled, long-acting, dual-pharmacology bronchodilator, in two phase I, randomised, single-blind, placebo-controlled studies
Navafenterol (AZD8871) in healthy volunteers: safety, tolerability and pharmacokinetics of multiple ascending doses of this novel inhaled, long-acting, dual-pharmacology bronchodilator, in two phase I, randomised, single-blind, placebo-controlled studies Abstract Abstract Background Navafenterol (AZD8871) is a novel, l...
PMC8520146
core_pubmed_pmc
Clinical pharmacology of tramadol and tapentadol, and their therapeutic efficacy in different models of acute and chronic pain in dogs and cats
Clinical pharmacology of tramadol and tapentadol, and their therapeutic efficacy in different models of acute and chronic pain in dogs and cats Abstract Opioids are considered the gold standard to manage acute or chronic or mild to severe pain. Tramadol is a widely prescribed analgesic drug for dogs and cats; it has a ...
PMC7823995
core_pubmed_pmc
Role and Interpretation of Antifungal Susceptibility Testing for the Management of Invasive Fungal Infections
Role and Interpretation of Antifungal Susceptibility Testing for the Management of Invasive Fungal Infections Abstract Abstract Invasive fungal infections (IFIs) are associated with high mortality rates and timely appropriate antifungal therapy is essential for good outcomes. Emerging antifungal resistance among Candid...
PMC6985981
core_pubmed_pmc
Clinical Evaluation of Risankizumab-rzaa in the Treatment of Plaque Psoriasis
Clinical Evaluation of Risankizumab-rzaa in the Treatment of Plaque Psoriasis Abstract Abstract Risankizumab-rzaa (Skyrizi ® ; AbbVie) is a humanized IgG monoclonal antibody directed against interleukin-23p19 (IL-23p19) indicated for the treatment of moderate-to-severe psoriasis in adults who are candidates for systemi...
PMC11738770
core_pubmed_pmc
Evaluating the pharmacokinetics and safety of blonanserin tablets and Lonasen ® : a randomized, open-label, two-period, two-sequence, self-crossover phase I clinical trial
Evaluating the pharmacokinetics and safety of blonanserin tablets and Lonasen ® : a randomized, open-label, two-period, two-sequence, self-crossover phase I clinical trial Abstract Objective This study evaluated the pharmacokinetic and safety profiles of generic and original blonanserin tablets under fasting and postpr...
PMC9229812
core_pubmed_pmc
Quantitative Biodistribution and Pharmacokinetics Study of GMP-Grade Exosomes Labeled with 89 Zr Radioisotope in Mice and Rats
Quantitative Biodistribution and Pharmacokinetics Study of GMP-Grade Exosomes Labeled with 89 Zr Radioisotope in Mice and Rats Abstract Abstract For the successful clinical advancement of exosome therapeutics, the biodistribution and pharmacokinetic profile of exogenous exosomes in various animal models must be determi...
PMC12343327
core_pubmed_pmc
Skimmianine Attenuates Osteoclast Activity by Suppressing ERp57‐Driven Calcium Oscillations/Calcineurin/Nfatc1 Signalling in Postmenopausal Osteoporosis
Skimmianine Attenuates Osteoclast Activity by Suppressing ERp57‐Driven Calcium Oscillations/Calcineurin/Nfatc1 Signalling in Postmenopausal Osteoporosis Abstract ABSTRACT Postmenopausal osteoporosis is primarily attributed to the hyperactivation of osteoclast‐induced bone resorption. The differentiation and function of...
PMC6388052
core_pubmed_pmc
Microdialysis in awake macaque monkeys for central nervous system pharmacokinetics
Microdialysis in awake macaque monkeys for central nervous system pharmacokinetics Abstract Abstract Background The brain bioavailability of novel small molecules developed to address central nervous system disease is classically documented through ex vivo or in vivo analyses conducted in rodent models. Data acquired i...
PMC6482278
core_pubmed_pmc
Modeling Exposure‐Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib
Modeling Exposure‐Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib Abstract Abstract Models were developed to characterize the relationship between afatinib exposure and diarrhea and rash/acne adverse event (AE) trajectories, and their predictive ability was assessed. Based on pooled data from seve...
PMC9075737
core_pubmed_pmc
Benefits of Curcumin in the Vasculature: A Therapeutic Candidate for Vascular Remodeling in Arterial Hypertension and Pulmonary Arterial Hypertension?
Benefits of Curcumin in the Vasculature: A Therapeutic Candidate for Vascular Remodeling in Arterial Hypertension and Pulmonary Arterial Hypertension? Abstract Abstract Growing evidence suggests that hypertension is one of the leading causes of cardiovascular morbidity and mortality since uncontrolled high blood pressu...
PMC9006295
core_pubmed_pmc
Optimal fludarabine lymphodepletion is associated with improved outcomes after CAR T-cell therapy
Optimal fludarabine lymphodepletion is associated with improved outcomes after CAR T-cell therapy Abstract Key Points Optimal fludarabine exposure in those with relapsed/refractory B-cell ALL receiving CD19-specific CAR T-cell therapy was AUC ≥13.8 mg × h/L. Suboptimal exposure led to a 2.5-fold higher risk of relapse ...
PMC4910209
core_pubmed_pmc
A randomized, double-blind, placebo controlled safety, tolerability, and pharmacokinetic dose escalation study of a gentamicin vancomycin gel in patients undergoing colorectal surgery
A randomized, double-blind, placebo controlled safety, tolerability, and pharmacokinetic dose escalation study of a gentamicin vancomycin gel in patients undergoing colorectal surgery Abstract Abstract Background Despite numerous interventions promulgated by the Surgical Care Improve Project (SCIP) and other organizati...
PMC12445128
core_pubmed_pmc
Bridging Pharmacokinetics and Pharmacodynamics: A PBPK/PD Model‐Based Approach for Deferasirox Dosing in Transfusion‐Dependent Thalassemia
Bridging Pharmacokinetics and Pharmacodynamics: A PBPK/PD Model‐Based Approach for Deferasirox Dosing in Transfusion‐Dependent Thalassemia Abstract ABSTRACT Patients with transfusion‐dependent thalassemia (TDT) require lifelong blood transfusions, resulting in excessive iron accumulation and necessitating effective che...
PMC12673595
core_pubmed_pmc
Noninvasive Evaluation of Trop2 Expression Using 64 Cu-NOTA-Trodelvy-F(ab’) 2 in Gastric and Pancreatic Cancer
Noninvasive Evaluation of Trop2 Expression Using 64 Cu-NOTA-Trodelvy-F(ab’) 2 in Gastric and Pancreatic Cancer Abstract Abstract This study aimed to develop and evaluate a 64 Cu-labeled NOTA-conjugated F­(ab’) 2 fragment of Trodelvy for ImmunoPET imaging of Trop2 expression in gastric and pancreatic cancer models. Trod...
PMC8712509
core_pubmed_pmc
In vitro and in vivo Evaluation of a Novel Estrogen-Targeted PEGylated Oxaliplatin Liposome for Gastric Cancer
In vitro and in vivo Evaluation of a Novel Estrogen-Targeted PEGylated Oxaliplatin Liposome for Gastric Cancer Abstract Abstract Background Chemotherapy is still the main first-line treatment for advanced metastatic gastric cancer, but it has the limitations of serious side effects and drug resistance. Conventional lip...
PMC5089741
core_pubmed_pmc
Pregnancy-Associated Changes in Pharmacokinetics: A Systematic Review
Pregnancy-Associated Changes in Pharmacokinetics: A Systematic Review Abstract Background Women are commonly prescribed a variety of medications during pregnancy. As most organ systems are affected by the substantial anatomical and physiological changes that occur during pregnancy, it is expected that pharmacokinetics ...
PMC10349187
core_pubmed_pmc
Physiologically based pharmacokinetic modeling of levetiracetam to predict the exposure in hepatic and renal impairment and elderly populations
Physiologically based pharmacokinetic modeling of levetiracetam to predict the exposure in hepatic and renal impairment and elderly populations Abstract Abstract Levetiracetam (LEV) is an anti‐epileptic drug approved for use in various populations. The pharmacokinetic (PK) behavior of LEV may be altered in the elderly ...
PMC12398828
core_pubmed_pmc
Optimizing phage therapy for Salmonella Pullorum: dosage, timing, and pharmacokinetics define treatment efficacy in SPF chickens
Optimizing phage therapy for Salmonella Pullorum: dosage, timing, and pharmacokinetics define treatment efficacy in SPF chickens Abstract Phage therapy has emerged as a highly effective antibiotic alternative for treating Salmonella infections; however, research into how phage dosage, administration timing, and frequen...
PMC11424055
core_pubmed_pmc
Comparative performance of pharmacogenetics-based warfarin dosing algorithms in Chinese population: use of a pharmacokinetic/pharmacodynamic model to explore dosing regimen through clinical trial simulation
Comparative performance of pharmacogenetics-based warfarin dosing algorithms in Chinese population: use of a pharmacokinetic/pharmacodynamic model to explore dosing regimen through clinical trial simulation Abstract Objective Warfarin has a narrow therapeutic window and large variability in dosing that are affected by ...
PMC5052446
core_pubmed_pmc
Effect of Red Ginseng on cytochrome P450 and P-glycoprotein activities in healthy volunteers
Effect of Red Ginseng on cytochrome P450 and P-glycoprotein activities in healthy volunteers Abstract Abstract Background We evaluated the drug interaction profile of Red Ginseng (RG) with respect to the activities of major cytochrome P450 (CYP) enzymes and the drug transporter P-glycoprotein (P-gp) in healthy Korean v...
PMC10875631
core_pubmed_pmc
Effective γδ T‐cell clinical therapies: current limitations and future perspectives for cancer immunotherapy
Effective γδ T‐cell clinical therapies: current limitations and future perspectives for cancer immunotherapy Abstract Abstract γδ T cells are a unique subset of T lymphocytes, exhibiting features of both innate and adaptive immune cells and are involved with cancer immunosurveillance. They present an attractive alterna...
PMC5516171
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of ARC‐520 Injection, an RNA Interference‐Based Therapeutic for the Treatment of Chronic Hepatitis B Virus Infection, in Healthy Volunteers
Safety, Tolerability, and Pharmacokinetics of ARC‐520 Injection, an RNA Interference‐Based Therapeutic for the Treatment of Chronic Hepatitis B Virus Infection, in Healthy Volunteers Abstract Abstract ARC‐520 Injection, an RNA interference drug for the treatment of hepatitis B that targets cccDNA‐derived viral mRNA tra...
PMC12648153
core_pubmed_pmc
Phase I/II Study of AXL-Specific Antibody–Drug Conjugate Enapotamab Vedotin in Patients with Advanced Solid Tumors
Phase I/II Study of AXL-Specific Antibody–Drug Conjugate Enapotamab Vedotin in Patients with Advanced Solid Tumors Abstract Abstract Purpose: AXL, a receptor tyrosine kinase related to oncogenic processes, is aberrantly expressed in various cancers and associated with treatment resistance. Enapotamab vedotin (EnaV), a ...
PMC4458612
core_pubmed_pmc
A prospective study of adverse drug reactions to antiepileptic drugs in children
A prospective study of adverse drug reactions to antiepileptic drugs in children Abstract Abstract Objectives To prospectively determine the nature and rate of adverse drug reactions (ADRs) in children on antiepileptic drugs (AEDs) and to prospectively evaluate the effect of AEDs on behaviour. Setting A single centre p...
PMC12655449
core_pubmed_pmc
Development and Characterization of EGCG-Loaded TPGS/Poloxamer 407 Micelles with Evaluation of In Vitro Drug Release and In Vivo Pharmacokinetics and Tolerability Observations Following Oral Administration
Development and Characterization of EGCG-Loaded TPGS/Poloxamer 407 Micelles with Evaluation of In Vitro Drug Release and In Vivo Pharmacokinetics and Tolerability Observations Following Oral Administration Abstract Background : Epigallocatechin-3-gallate (EGCG), a potent green tea polyphenol, possesses significant ther...
PMC12167920
core_pubmed_pmc
A Multiple Imputation Workflow for Handling Missing Covariate Data in Pharmacometrics Modeling
A Multiple Imputation Workflow for Handling Missing Covariate Data in Pharmacometrics Modeling Abstract ABSTRACT Covariate missingness is a prevalent issue in pharmacometrics modeling. Incorrect handling of missing covariates can lead to biased parameter estimates, adversely affecting clinical practice and drug develop...
PMC10815823
core_pubmed_pmc
SLCO1B1 Genetic Variation Influence on Atorvastatin Systemic Exposure in Pediatric Hypercholesterolemia
SLCO1B1 Genetic Variation Influence on Atorvastatin Systemic Exposure in Pediatric Hypercholesterolemia Abstract Abstract This clinical study examined the influence of SLCO1B1 c.521T>C (rs4149056) on plasma atorvastatin concentrations in pediatric hypercholesterolemia. The participants (8–21 years), including heterozyg...
PMC12129586
core_pubmed_pmc
Activity of rezafungin against Candida auris
Activity of rezafungin against Candida auris Abstract Abstract The increasing prevalence of candidemia and invasive candidiasis infections caused by Candida auris represents a global health risk. Such infections are difficult to treat as they are often multidrug-resistant and are linked to high rates of mortality. Reza...
PMC9778508
core_pubmed_pmc
The Influence of Structural Variants of the CES1 Gene on the Pharmacokinetics of Enalapril, Presumably Due to Linkage Disequilibrium with the Intronic rs2244613
The Influence of Structural Variants of the CES1 Gene on the Pharmacokinetics of Enalapril, Presumably Due to Linkage Disequilibrium with the Intronic rs2244613 Abstract Variants in the CES1 gene encoding carboxylesterase 1 may affect the metabolism of enalapril to the active metabolite enalaprilat. It was shown that t...
PMC12131858
core_pubmed_pmc
A freely accessible, adaptable hollow-fiber setup to reproduce first-order absorption: illustration with linezolid cerebrospinal fluid pharmacokinetic data
A freely accessible, adaptable hollow-fiber setup to reproduce first-order absorption: illustration with linezolid cerebrospinal fluid pharmacokinetic data Abstract ABSTRACT The main objective of this study was to validate an algorithm and experimental setup to simulate first-order absorption pharmacokinetic profiles w...
PMC11052825
core_pubmed_pmc
Clinical Evaluation of the Effect of Encorafenib on Bupropion, Rosuvastatin, and Coproporphyrin I and Considerations for Statin Coadministration
Clinical Evaluation of the Effect of Encorafenib on Bupropion, Rosuvastatin, and Coproporphyrin I and Considerations for Statin Coadministration Abstract Abstract Background and Objectives Encorafenib is a kinase inhibitor indicated for the treatment of patients with unresectable or metastatic melanoma or metastatic co...
PMC10719564
core_pubmed_pmc
Voclosporin and the Antiviral Effect Against SARS-CoV-2 in Immunocompromised Kidney Patients
Voclosporin and the Antiviral Effect Against SARS-CoV-2 in Immunocompromised Kidney Patients Abstract Abstract Introduction Immunocompromised kidney patients are at increased risk of prolonged SARS-CoV-2 infection and related complications. Preclinical evidence demonstrates a more potent inhibitory effect of voclospori...
PMC6321130
core_pubmed_pmc
A Review on Liquid Chromatography-Tandem Mass Spectrometry Methods for Rapid Quantification of Oncology Drugs
A Review on Liquid Chromatography-Tandem Mass Spectrometry Methods for Rapid Quantification of Oncology Drugs Abstract In the last decade, the tremendous improvement in the sensitivity and also affordability of liquid chromatography-tandem mass spectrometry (LC-MS/MS) has revolutionized its application in pharmaceutica...
PMC12777555
core_pubmed_pmc
Ceftobiprole alone versus ampicillin-ceftriaxone against borderline-penicillin-resistant, ampicillin-susceptible, and vancomycin-resistant Enterococcus faecalis isolates
Ceftobiprole alone versus ampicillin-ceftriaxone against borderline-penicillin-resistant, ampicillin-susceptible, and vancomycin-resistant Enterococcus faecalis isolates Abstract ABSTRACT Despite the use of recommended treatments against Enterococcus faecalis infective endocarditis, mortality rates remain at 30%. Penic...
PMC12945055
core_pubmed_pmc
Detection of Mycotoxins in Fallow Deer Milk and Feces: Evidence of Climate-Driven Contamination in a Comparative Study of Two Weather-Divergent Years in Hungary
Detection of Mycotoxins in Fallow Deer Milk and Feces: Evidence of Climate-Driven Contamination in a Comparative Study of Two Weather-Divergent Years in Hungary Abstract Abstract Extreme weather impacts the ecological niches of fungi, altering mycotoxin risks in wildlife. We analyzed mycotoxin carry-over into European ...
PMC8791303
core_pubmed_pmc
Nanoparticles in Combating Neuronal Dysregulated Signaling Pathways: Recent Approaches to the Nanoformulations of Phytochemicals and Synthetic Drugs Against Neurodegenerative Diseases
Nanoparticles in Combating Neuronal Dysregulated Signaling Pathways: Recent Approaches to the Nanoformulations of Phytochemicals and Synthetic Drugs Against Neurodegenerative Diseases Abstract Abstract As the worldwide average life expectancy has grown, the prevalence of age-related neurodegenerative diseases (NDDs) ha...
PMC5324677
core_pubmed_pmc
Pharmacokinetics of Ferric Pyrophosphate Citrate, a Novel Iron Salt, Administered Intravenously to Healthy Volunteers
Pharmacokinetics of Ferric Pyrophosphate Citrate, a Novel Iron Salt, Administered Intravenously to Healthy Volunteers Abstract Abstract Ferric pyrophosphate citrate (Triferic) is a water‐soluble iron salt that is administered via dialysate to maintain iron balance and hemoglobin in hemodialysis patients. This double‐bl...
PMC12034272
core_pubmed_pmc
Development and Validation of a Population Pharmacokinetics Model of Perampanel for Pediatric Epilepsy Patients for Optimized Dosing
Development and Validation of a Population Pharmacokinetics Model of Perampanel for Pediatric Epilepsy Patients for Optimized Dosing Abstract Background Perampanel exhibits substantial interindividual variability, and pharmacokinetic data in pediatric patients are scarce. The aim of this study was to develop a populati...
PMC11476299
core_pubmed_pmc
PLK1 Inhibitor Onvansertib Enhances the Efficacy of Alpelisib in PIK3CA -Mutated HR-Positive Breast Cancer Resistant to Palbociclib and Endocrine Therapy: Preclinical Insights
PLK1 Inhibitor Onvansertib Enhances the Efficacy of Alpelisib in PIK3CA -Mutated HR-Positive Breast Cancer Resistant to Palbociclib and Endocrine Therapy: Preclinical Insights Abstract Abstract Simple Summary Patients with hormone receptor-positive (HR+)/HER2-negative metastatic breast cancer who have PIK3CA mutations ...
PMC8944760
core_pubmed_pmc
HR-LC-ESI-Orbitrap-MS-Based Metabolic Profiling Coupled with Chemometrics for the Discrimination of Different Echinops spinosus Organs and Evaluation of Their Antioxidant Activity
HR-LC-ESI-Orbitrap-MS-Based Metabolic Profiling Coupled with Chemometrics for the Discrimination of Different Echinops spinosus Organs and Evaluation of Their Antioxidant Activity Abstract This study aimed to assess and correlate the phenolic content and the antioxidant activity of the methanol extracts of the stems, r...
PMC10512707
core_pubmed_pmc
Pharmacokinetics and safety of highly variable valsartan in single-pill combination with amlodipine versus its generic formulation: a randomized, three-cycle, three-sequence, partially replicated crossover phase I bioequivalence clinical trial
Pharmacokinetics and safety of highly variable valsartan in single-pill combination with amlodipine versus its generic formulation: a randomized, three-cycle, three-sequence, partially replicated crossover phase I bioequivalence clinical trial Abstract Valsartan/amlodipine (I) is a single-pill combination (SPC) of an a...
PMC11061577
core_pubmed_pmc
Pharmacokinetics/pharmacodynamics cut-off determination for fosfomycin using Monte Carlo simulation in healthy horses
Pharmacokinetics/pharmacodynamics cut-off determination for fosfomycin using Monte Carlo simulation in healthy horses Abstract Abstract Fosfomycin (FOM) is an approved veterinary medicinal product for large animals in Japan, but Clinical breakpoint (CBP) for antimicrobial susceptibility test (AST) is not defined for an...
PMC10772058
core_pubmed_pmc
Phage-host-immune system dynamics in bacteriophage therapy: basic principles and mathematical models
Phage-host-immune system dynamics in bacteriophage therapy: basic principles and mathematical models Abstract Abstract Phage therapy is progressively being recognized as a viable alternative to conventional antibiotic treatments, particularly in the context of multi-drug resistant bacterial challenges. However, the int...
PMC10779243
core_pubmed_pmc
HSA-ZW800-PEG for Enhanced Optophysical Stability and Tumor Targeting
HSA-ZW800-PEG for Enhanced Optophysical Stability and Tumor Targeting Abstract Abstract Small molecule fluorophores often face challenges such as short blood half-life, limited physicochemical and optical stability, and poor pharmacokinetics. To overcome these limitations, we conjugated the zwitterionic near-infrared f...
PMC9055195
core_pubmed_pmc
Safety of direct acting antiviral treatment for hepatitis C in oncologic setting: A clinical experience and a literature review
Safety of direct acting antiviral treatment for hepatitis C in oncologic setting: A clinical experience and a literature review Abstract With a globally estimated 58 million people affected by, chronic hepatitis C virus (HCV) infection still represents a hard challenge for scientific community. A chronic course can occ...
PMC9133758
core_pubmed_pmc
The effect of sickle cell genotype on the pharmacokinetic properties of artemether-lumefantrine in Tanzanian children
The effect of sickle cell genotype on the pharmacokinetic properties of artemether-lumefantrine in Tanzanian children Abstract Abstract Since there are inconsistent data relating to the effect of haemoglobinopathies on disposition of artemisinin antimalarial combination therapy, and none in sickle cell trait (SCT) or s...
PMC7683353
core_pubmed_pmc
Optimal Empiric Treatment for Klebsiella pneumoniae Infections in Short-Stay ICU Patients During Continuous Renal Replacement Therapy: Results from a Population Pharmacokinetic/Pharmacodynamic Analysis
Optimal Empiric Treatment for Klebsiella pneumoniae Infections in Short-Stay ICU Patients During Continuous Renal Replacement Therapy: Results from a Population Pharmacokinetic/Pharmacodynamic Analysis Abstract Abstract Objective There is a paucity of published data to evaluate the efficacy and safety of imipenem (IPM)...
PMC5209410
core_pubmed_pmc
Concentration of Donepezil in the Cerebrospinal Fluid of AD Patients: Evaluation of Dosage Sufficiency in Standard Treatment Strategy
Concentration of Donepezil in the Cerebrospinal Fluid of AD Patients: Evaluation of Dosage Sufficiency in Standard Treatment Strategy Abstract Abstract Although some studies have described the pharmacokinetics and pharmacodynamics of donepezil in the peripheral compartment, studies focused on drug transport across the ...
PMC6861098
core_pubmed_pmc
First use of cenerimod, a selective S1P 1 receptor modulator, for the treatment of SLE: a double-blind, randomised, placebo-controlled, proof-of-concept study
First use of cenerimod, a selective S1P 1 receptor modulator, for the treatment of SLE: a double-blind, randomised, placebo-controlled, proof-of-concept study Abstract Objective To investigate the pharmacodynamics, pharmacokinetics and safety of cenerimod—a potent, oral, selective sphingosine 1-phosphate 1 receptor mod...
PMC4634831
core_pubmed_pmc
Managing gastroesophageal reflux disease – comparative efficacy and outcomes of dexlansoprazole MR
Managing gastroesophageal reflux disease – comparative efficacy and outcomes of dexlansoprazole MR Abstract Abstract The management of gastroesophageal reflux disease (GERD) has been revolutionized with the development of proton pump inhibitors (PPIs). Unfortunately, due to the inherent pharmacokinetic and pharmacodyna...
PMC5776115
core_pubmed_pmc
PK-PD Integration Modeling and Cutoff Value of Florfenicol against Streptococcus suis in Pigs
PK-PD Integration Modeling and Cutoff Value of Florfenicol against Streptococcus suis in Pigs Abstract The aims of the present study were to establish optimal doses and provide an alternate CO PD for florfenicol against Streptococcus suis based on pharmacokinetic-pharmacodynamic integration modeling. The recommended do...
PMC10181972
core_pubmed_pmc
Neither Gastric Bypass Surgery Nor Diet-Induced Weight-Loss Affect OATP1B1 Activity as Measured by Rosuvastatin Oral Clearance
Neither Gastric Bypass Surgery Nor Diet-Induced Weight-Loss Affect OATP1B1 Activity as Measured by Rosuvastatin Oral Clearance Abstract Abstract Introduction Rosuvastatin pharmacokinetics is mainly dependent on the activity of hepatic uptake transporter OATP1B1. In this study, we aimed to investigate and disentangle th...
PMC5423501
core_pubmed_pmc
A Phase Ib Study of Sorafenib (BAY 43‐9006) in Patients with Kaposi Sarcoma
A Phase Ib Study of Sorafenib (BAY 43‐9006) in Patients with Kaposi Sarcoma Abstract Abstract Lessons Learned. Oral targeted agents are desirable for treatment of Kaposi sarcoma (KS); however, in patients with HIV, drug–drug interactions must be considered. In this study to treat KS, sorafenib was poorly tolerated at d...
PMC8448162
core_pubmed_pmc
Single- and Multiple-Ascending-Dose Study of the Safety, Tolerability, and Pharmacokinetics of the Polymyxin Derivative SPR206
Single- and Multiple-Ascending-Dose Study of the Safety, Tolerability, and Pharmacokinetics of the Polymyxin Derivative SPR206 Abstract ABSTRACT Carbapenem-resistant Acinetobacter baumannii and Enterobacterales are identified as urgent threats, and multidrug-resistant (MDR) Pseudomonas aeruginosa and extended-spectrum ...
PMC12415978
core_pubmed_pmc
Species-specific gene expression manipulation in humanized livers of chimeric mice via siRNA-encapsulated lipid nanoparticle treatment
Species-specific gene expression manipulation in humanized livers of chimeric mice via siRNA-encapsulated lipid nanoparticle treatment Abstract Liver-humanized chimeric mice (PXB-mice) are widely utilized for predicting human pharmacokinetics (PK) and as human disease models. However, residual metabolic activity of mou...
PMC12214119
core_pubmed_pmc
Advancing hepatotoxicity assessment: current advances and future directions
Advancing hepatotoxicity assessment: current advances and future directions Abstract During drug development, it is crucial to ensure that a drug exhibits effective activity in its target cells and organs. However, regardless of its effectiveness, a drug cannot be administered to patients if it exhibits toxicity in viv...
PMC8590460
core_pubmed_pmc
The Anti-Inflammation and Anti-Nociception Effect of Ketoprofen in Rats Could Be Strengthened Through Co-Delivery of a H 2 S Donor, S-Propargyl-Cysteine
The Anti-Inflammation and Anti-Nociception Effect of Ketoprofen in Rats Could Be Strengthened Through Co-Delivery of a H 2 S Donor, S-Propargyl-Cysteine Abstract Abstract Purpose Ketoprofen (KETO) is a traditional non-steroidal anti-inflammatory drug (NSAIDs) with good analgesic and antipyretic effects. However, as NAS...
PMC9650305
core_pubmed_pmc
Population pharmacokinetic analysis for dabigatran etexilate in Chinese patients with non-valvular atrial fibrillation
Population pharmacokinetic analysis for dabigatran etexilate in Chinese patients with non-valvular atrial fibrillation Abstract Abstract We aimed to develop a pharmacokinetic (PK) and pharmacodynamic (PD) model from healthy Chinese subjects and real-world non-valvular atrial fibrillation (NVAF) patients. We also invest...
PMC8399464
core_pubmed_pmc
Long-Acting Risperidone Dual Control System: Preparation, Characterization and Evaluation In Vitro and In Vivo
Long-Acting Risperidone Dual Control System: Preparation, Characterization and Evaluation In Vitro and In Vivo Abstract Abstract Schizophrenia, a psychiatric disorder, requires long-term treatment; however, large fluctuations in blood drug concentration increase the risk of adverse reactions. We prepared a long-term ri...
PMC7653950
core_pubmed_pmc
Modelling of combination therapy using implantable anticancer drug delivery with thermal ablation in solid tumor
Modelling of combination therapy using implantable anticancer drug delivery with thermal ablation in solid tumor Abstract Local implantable drug delivery system (IDDS) can be used as an effective adjunctive therapy for solid tumor following thermal ablation for destroying the residual cancer cells and preventing the tu...
PMC4077389
core_pubmed_pmc
Novel nanocrystal formulation of megestrol acetate has improved bioavailability compared with the conventional micronized formulation in the fasting state
Novel nanocrystal formulation of megestrol acetate has improved bioavailability compared with the conventional micronized formulation in the fasting state Abstract Background Megestrol acetate is an effective treatment for improving appetite and increasing body weight in patients with cancer-associated anorexia. Howeve...
PMC4126480
core_pubmed_pmc
Evaluation of drug interaction potential of Labisia pumila (Kacip Fatimah) and its constituents
Evaluation of drug interaction potential of Labisia pumila (Kacip Fatimah) and its constituents Abstract Labisia pumila (Kacip Fatimah) is a popular herb in Malaysia that has been traditionally used in a number of women’s health applications such as to improve libido, relieve postmenopausal symptoms, and to facilitate ...
PMC9298787
core_pubmed_pmc
Phase I clinical trial of HC‐1119 soft capsule in Chinese healthy adult male subjects: Pharmacokinetics and safety of single‐dose proportionality and effects of food
Phase I clinical trial of HC‐1119 soft capsule in Chinese healthy adult male subjects: Pharmacokinetics and safety of single‐dose proportionality and effects of food Abstract Abstract Background Preclinical studies showed that HC‐1119, a deuterated version of enzalutamide, could competitively inhibit androgen binding t...
PMC12307181
core_pubmed_pmc
Development and evaluation of mPEG-PLLA polymeric micelles encapsulating enrofloxacin for enhanced solubility, bioavailability, and antibacterial performance
Development and evaluation of mPEG-PLLA polymeric micelles encapsulating enrofloxacin for enhanced solubility, bioavailability, and antibacterial performance Abstract Abstract The aim of this study was to prepare polymeric micelles composed of enrofloxacin (ENR) and methoxy poly (ethylene glycol)-poly(lactide) (mPEG-PL...
PMC8359850
core_pubmed_pmc
Modeling Complex Pharmacokinetics of Long‐Acting Injectable Products Using Convolution‐Based Models With Nonparametric Input Functions
Modeling Complex Pharmacokinetics of Long‐Acting Injectable Products Using Convolution‐Based Models With Nonparametric Input Functions Abstract Abstract The interest in the development and the therapeutic use of long‐acting injectable (LAI) products for chronic or long‐term treatments has grown exponentially. The compl...
PMC6398530
core_pubmed_pmc
A comprehensive approach to the molecular determinants of lifespan using a Boolean model of geroconversion
A comprehensive approach to the molecular determinants of lifespan using a Boolean model of geroconversion Abstract Summary Altered molecular responses to insulin and growth factors ( GF ) are responsible for late‐life shortening diseases such as type‐2 diabetes mellitus (T2 DM ) and cancers. We have built a network of...
PMC12263763
core_pubmed_pmc
Population Pharmacokinetics Model of Thioguanine in Patients with Inflammatory Bowel Disease
Population Pharmacokinetics Model of Thioguanine in Patients with Inflammatory Bowel Disease Abstract Abstract Background Thioguanine (TG) has recently been rediscovered as an immunosuppressive agent in the treatment of inflammatory bowel disease (IBD). This prodrug is directly converted into its active metabolites, 6-...
PMC12736095
core_pubmed_pmc
Safety, Pharmacokinetics, and Bioequivalence Characterization of Two Different Strengths of Mesalazine Gastro-Resistant Tablets
Safety, Pharmacokinetics, and Bioequivalence Characterization of Two Different Strengths of Mesalazine Gastro-Resistant Tablets Abstract Background/Objectives : Ulcerative colitis (UC), a chronic inflammatory bowel disease, affects approximately 5 million individuals worldwide, exerting a considerable influence on glob...
PMC3662125
core_pubmed_pmc
Cultural Aspects of Major Mental Disorders: A Critical Review from an Indian Perspective
Cultural Aspects of Major Mental Disorders: A Critical Review from an Indian Perspective Abstract Abstract Major mental disorders such as schizophrenia and affective disorders are highly disabling illnesses. The cultural factors that influence the diagnosis and treatment of these disorders are of paramount clinical sig...
PMC12559477
core_pubmed_pmc
Nonclinical safety evaluation and pharmacokinetics of Ab612, a novel anti-L1CAM (CD171) therapeutic antibody candidate against solid cancer
Nonclinical safety evaluation and pharmacokinetics of Ab612, a novel anti-L1CAM (CD171) therapeutic antibody candidate against solid cancer Abstract L1 cell adhesion molecule (L1CAM, CD171) is a transmembrane glycoprotein important for nervous system development. Conversely, L1CAM is overexpressed in many human solid t...
PMC9020499
core_pubmed_pmc
Management of drug-drug interactions with nirmatrelvir/ritonavir in patients treated for Covid-19: Guidelines from the French Society of Pharmacology and Therapeutics (SFPT)
Management of drug-drug interactions with nirmatrelvir/ritonavir in patients treated for Covid-19: Guidelines from the French Society of Pharmacology and Therapeutics (SFPT) Abstract Abstract Objectives Nirmatrelvir in association with ritonavir (PAXLOVID™, Pfizer) is an antiviral agent targeting the 3-chymotrypsin–lik...
PMC12504911
core_pubmed_pmc
The Cardiac Sodium Channel Safety Profile of Cenobamate at Therapeutic Concentrations: In Vitro Analyses
The Cardiac Sodium Channel Safety Profile of Cenobamate at Therapeutic Concentrations: In Vitro Analyses Abstract ABSTRACT The US Food and Drug Administration (FDA) issued a Drug Safety Communication for the antiseizure drug lamotrigine (Lamictal), warning of the risk of QRS prolongation and cardiac arrhythmias. The FD...
PMC4813608
core_pubmed_pmc
Preclinical safety, pharmacokinetics, pharmacodynamics, and biodistribution studies with Ad35K++ protein: a novel rituximab cotherapeutic
Preclinical safety, pharmacokinetics, pharmacodynamics, and biodistribution studies with Ad35K++ protein: a novel rituximab cotherapeutic Abstract Abstract Rituximab is a mouse/human chimeric monoclonal antibody targeted toward CD20. It is efficient as first-line therapy of CD20-positive B-cell malignancies. However, a...
PMC12683255
core_pubmed_pmc
Dose Optimization of Rivaroxaban in Elderly Chinese Patients with Non-Valvular Atrial Fibrillation: Analysis of Populations Pharmacokinetics and Exposure-Response Relationships
Dose Optimization of Rivaroxaban in Elderly Chinese Patients with Non-Valvular Atrial Fibrillation: Analysis of Populations Pharmacokinetics and Exposure-Response Relationships Abstract Purpose This study aimed to develop a population pharmacokinetic (PopPK) model in elderly Chinese patient with NVAF, characterize the ...
PMC11445516
core_pubmed_pmc
Sol-moiety: Discovery of a water-soluble prodrug technology for enhanced oral bioavailability of insoluble therapeutics
Sol-moiety: Discovery of a water-soluble prodrug technology for enhanced oral bioavailability of insoluble therapeutics Abstract Though conceptually attractive, the use of water-soluble prodrug technology to enhance oral bioavailability of highly insoluble small molecule therapeutics has not been widely adopted. In lar...
PMC9966833
core_pubmed_pmc
Risk Factors for Rivaroxaban-Related Bleeding Events—Possible Role of Pharmacogenetics: Case Series
Risk Factors for Rivaroxaban-Related Bleeding Events—Possible Role of Pharmacogenetics: Case Series Abstract Abstract Non-vitamin K antagonist oral anticoagulants’ interindividual trough concentration variability affects efficacy and safety, especially in bleeding events. Rivaroxaban is metabolised via CYP3A4/5-, CYP2J...
PMC12634627
core_pubmed_pmc
Safety and adverse events associated with dexmedetomidine for sedation in adult ICU patients: a systematic review and meta-analysis
Safety and adverse events associated with dexmedetomidine for sedation in adult ICU patients: a systematic review and meta-analysis Abstract Background Dexmedetomidine (DEX) is increasingly used for sedation in critically ill adults due to its favorable pharmacokinetic profile and potential benefits over traditional se...
PMC9783864
core_pubmed_pmc
Impact of Cabozantinib Exposure on Proteinuria and Muscle Toxicity in Patients with Unresectable Hepatocellular Carcinoma
Impact of Cabozantinib Exposure on Proteinuria and Muscle Toxicity in Patients with Unresectable Hepatocellular Carcinoma Abstract Abstract This prospective study investigated the impact of cabozantinib exposure on proteinuria and muscle toxicity, in a cohort of 14 Japanese patients with unresectable hepatocellular car...
PMC4463967
core_pubmed_pmc
Cytochrome P450 enzyme mediated herbal drug interactions (Part 1)
Cytochrome P450 enzyme mediated herbal drug interactions (Part 1) Abstract Abstract It is well recognized that herbal supplements or herbal medicines are now commonly used. As many patients taking prescription medications are concomitantly using herbal supplements, there is considerable risk for adverse herbal drug int...
PMC8335694
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic studies of CD19 CAR T cell in human leukaemic xenograft models with dual‐modality imaging
Pharmacokinetic and pharmacodynamic studies of CD19 CAR T cell in human leukaemic xenograft models with dual‐modality imaging Abstract Abstract In recent years, chimeric antigen receptor T (CAR T)‐cell therapy has shown great potential in treating haematologic disease, but no breakthrough has been achieved in solid tum...
PMC11646929
core_pubmed_pmc
Population pharmacokinetics of selexipag for dose selection and confirmation in pediatric patients with pulmonary arterial hypertension
Population pharmacokinetics of selexipag for dose selection and confirmation in pediatric patients with pulmonary arterial hypertension Abstract Abstract Selexipag is an oral selective prostacyclin receptor agonist approved for the treatment of pulmonary arterial hypertension (PAH) in adults. To date, no treatment targ...
PMC6547164
core_pubmed_pmc
Receptor-Enriched Analysis of functional connectivity by targets (REACT): A novel, multimodal analytical approach informed by PET to study the pharmacodynamic response of the brain under MDMA
Receptor-Enriched Analysis of functional connectivity by targets (REACT): A novel, multimodal analytical approach informed by PET to study the pharmacodynamic response of the brain under MDMA Abstract Abstract One of the main limitations of pharmacological fMRI is its inability to provide a molecular insight into the m...
PMC11739781
core_pubmed_pmc
Clinical Pharmacology of Cytokine Release Syndrome with T-Cell–Engaging Bispecific Antibodies: Current Insights and Drug Development Strategies
Clinical Pharmacology of Cytokine Release Syndrome with T-Cell–Engaging Bispecific Antibodies: Current Insights and Drug Development Strategies Abstract Abstract Cytokine release syndrome (CRS) is a common acute toxicity in T-cell therapies, including T-cell–engaging bispecific antibodies (T-BiSp). Effective CRS manage...
PMC11846858
core_pubmed_pmc
Macrocarpal I induces immunogenic cell death and synergizes with immune checkpoint inhibition by targeting tubulin and PARP1 in colorectal cancer
Macrocarpal I induces immunogenic cell death and synergizes with immune checkpoint inhibition by targeting tubulin and PARP1 in colorectal cancer Abstract Colorectal cancer (CRC) presents an obstacle to immunotherapy, primarily because most cases are microsatellite stable (MSS) tumors, which are often described as “col...