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PMC10926075
core_pubmed_pmc
Exploring antioxidative, cytotoxic and neuropharmacological insights into Bixa orellana leaves: Experimental and in silico approaches
Exploring antioxidative, cytotoxic and neuropharmacological insights into Bixa orellana leaves: Experimental and in silico approaches Abstract Background Study The aim of this research was to examine possible antioxidant, cytotoxic and neurological activity of methanol and n-hexane extracts of Bixa orellana leaves. Add...
PMC3967145
core_pubmed_pmc
Pediatric Dosing and Body Size in Biotherapeutics
Pediatric Dosing and Body Size in Biotherapeutics Abstract Abstract Although pediatric doses for biotherapeutics are often based on patients' body weight (mg/kg) or body surface area (mg/m 2 ), linear body size dose adjustment is highly empirical. Growth and maturity are also important factors that affect the absorptio...
PMC5096055
core_pubmed_pmc
CD101: a novel long‐acting echinocandin
CD101: a novel long‐acting echinocandin Abstract Summary CD101 is a novel echinocandin drug being developed to treat severe fungal infections including invasive candidiasis. We have performed a series of studies to evaluate the antifungal properties of CD101 against both echinocandin‐susceptible and ‐resistant Candida ...
PMC6099803
core_pubmed_pmc
Stereoselective and Simultaneous Analysis of Ginsenosides from Ginseng Berry Extract in Rat Plasma by UPLC-MS/MS: Application to a Pharmacokinetic Study of Ginseng Berry Extract
Stereoselective and Simultaneous Analysis of Ginsenosides from Ginseng Berry Extract in Rat Plasma by UPLC-MS/MS: Application to a Pharmacokinetic Study of Ginseng Berry Extract Abstract The role of ginseng berry extract (GBE) has been attributed to its anti-hyperglycemic effect in humans. However, the pharmacokinetic ...
PMC10582846
core_pubmed_pmc
Repurposing the FDA-approved anthelmintic pyrvinium pamoate for pancreatic cancer treatment: study protocol for a phase I clinical trial in early-stage pancreatic ductal adenocarcinoma
Repurposing the FDA-approved anthelmintic pyrvinium pamoate for pancreatic cancer treatment: study protocol for a phase I clinical trial in early-stage pancreatic ductal adenocarcinoma Abstract Background Recent reports of the utilisation of pyrvinium pamoate (PP), an FDA-approved anti-helminth, have shown that it inhi...
PMC3025326
core_pubmed_pmc
Determination of ciprofloxacin in human plasma using high-performance liquid chromatography coupled with fluorescence detection: Application to a population pharmacokinetics study in children with severe malnutrition
Determination of ciprofloxacin in human plasma using high-performance liquid chromatography coupled with fluorescence detection: Application to a population pharmacokinetics study in children with severe malnutrition Abstract Clinical pharmacokinetic studies of ciprofloxacin require accurate and precise measurement of ...
PMC4924246
core_pubmed_pmc
New insights into the pharmacokinetics and pharmacodynamics of natalizumab treatment for patients with multiple sclerosis, obtained from clinical and in vitro studies
New insights into the pharmacokinetics and pharmacodynamics of natalizumab treatment for patients with multiple sclerosis, obtained from clinical and in vitro studies Abstract Abstract Background The monoclonal antibody natalizumab (NAT) inhibits the migration of lymphocytes throughout the blood–brain barrier by blocki...
PMC6555163
core_pubmed_pmc
Deciphering pharmacokinetics and pharmacodynamics of fosfomycin
Deciphering pharmacokinetics and pharmacodynamics of fosfomycin Abstract Abstract Fosfomycin, a low molecular weight and hydrophilic drug with negligible protein binding, is eliminated almost exclusively by glomerular filtration, whose clearance is subject to patient renal function. The volume of distribution approxima...
PMC7841500
core_pubmed_pmc
Pharmacokinetics and predicted neutralisation coverage of VRC01 in HIV-uninfected participants of the Antibody Mediated Prevention (AMP) trials
Pharmacokinetics and predicted neutralisation coverage of VRC01 in HIV-uninfected participants of the Antibody Mediated Prevention (AMP) trials Abstract Abstract The phase 2b AMP trials are testing whether the broadly neutralising antibody VRC01 prevents HIV-1 infection in two cohorts: women in sub-Saharan Africa, and ...
PMC10447587
core_pubmed_pmc
Single-dose pharmacokinetics and lung function of nebulized niclosamide ethanolamine in sheep
Single-dose pharmacokinetics and lung function of nebulized niclosamide ethanolamine in sheep Abstract Purpose Niclosamide is approved as an oral anthelminthic, but its low oral bioavailability hinders its medical use requiring high drug exposure outside the gastrointestinal tract. An optimized solution of niclosamide ...
PMC6058499
core_pubmed_pmc
The paradigm shift for drug delivery systems for oral and maxillofacial implants
The paradigm shift for drug delivery systems for oral and maxillofacial implants Abstract Abstract Along with the development of nanotechnological strategies for biomaterials associated with the prevention of infections, a myriad of clinically unproven techniques have been described to date. In this work, the aim was t...
PMC4251300
core_pubmed_pmc
Systemic pharmacokinetics following intravitreal injections of ranibizumab, bevacizumab or aflibercept in patients with neovascular AMD
Systemic pharmacokinetics following intravitreal injections of ranibizumab, bevacizumab or aflibercept in patients with neovascular AMD Abstract Background Data comparing systemic exposure and systemic vascular endothelial growth factor (VEGF) suppression of ranibizumab, bevacizumab and aflibercept following intravitre...
PMC5744427
core_pubmed_pmc
An Integrated Computational Approach for Plant-Based Protein Tyrosine Phosphatase Non-Receptor Type 1 Inhibitors
An Integrated Computational Approach for Plant-Based Protein Tyrosine Phosphatase Non-Receptor Type 1 Inhibitors Abstract Abstract Background: Protein tyrosine phosphatase non-receptor type 1 is a therapeutic target for the type 2 diabetes mellitus. According to the International Diabetes Federation 2015 report, one ou...
PMC7002565
core_pubmed_pmc
Implementation of a Physiologically Based Pharmacokinetic Modeling Approach to Guide Optimal Dosing Regimens for Imatinib and Potential Drug Interactions in Paediatrics
Implementation of a Physiologically Based Pharmacokinetic Modeling Approach to Guide Optimal Dosing Regimens for Imatinib and Potential Drug Interactions in Paediatrics Abstract Long-term use of imatinib is effective and well-tolerated in children with chronic myeloid leukaemia (CML) yet defining an optimal dosing regi...
PMC8613993
core_pubmed_pmc
The impact of early target attainment of vancomycin in critically ill patients with confirmed Gram-positive infection: A retrospective cohort study
The impact of early target attainment of vancomycin in critically ill patients with confirmed Gram-positive infection: A retrospective cohort study Abstract Background Vancomycin is a commonly used antibiotic in critically ill patients for various indications. Critical illness imposes pharmacokinetic-pharmacodynamics c...
PMC5547068
core_pubmed_pmc
Clinical dosage of meclozine promotes longitudinal bone growth, bone volume, and trabecular bone quality in transgenic mice with achondroplasia
Clinical dosage of meclozine promotes longitudinal bone growth, bone volume, and trabecular bone quality in transgenic mice with achondroplasia Abstract Abstract Achondroplasia (ACH) is the most common short-limbed skeletal dysplasia caused by gain-of-function mutations in the fibroblast growth factor receptor 3 (FGFR3...
PMC12013231
core_pubmed_pmc
Apixaban Failure in A Post-Bariatric Surgery Female Patient with Thoracic Aortic Thrombus Secondary to Covid-19
Apixaban Failure in A Post-Bariatric Surgery Female Patient with Thoracic Aortic Thrombus Secondary to Covid-19 Abstract Abstract A floating thrombus in the thoracic aorta represents a rare vascular condition frequently associated with morbidity and mortality. There is no standardised management approach, but options p...
PMC10186379
core_pubmed_pmc
Pharmacokinetics and Tissue Distribution of Nasal Spray of a Novel Muscarinic Receptor Blocker, 101BHG-D01, in Dogs and Rats
Pharmacokinetics and Tissue Distribution of Nasal Spray of a Novel Muscarinic Receptor Blocker, 101BHG-D01, in Dogs and Rats Abstract Background 101BHG-D01 is a novel selective anti-muscarinic (M) 3 receptor-blocking drug. 101BHG-D01 nasal spray is intended to be used to relieve sneezing and runny nose symptoms caused ...
PMC10804867
core_pubmed_pmc
Adherence to Background Antipsychotic and Pimavanserin in Patients with Schizophrenia: Post Hoc Analyses from the ENHANCE and ADVANCE Studies
Adherence to Background Antipsychotic and Pimavanserin in Patients with Schizophrenia: Post Hoc Analyses from the ENHANCE and ADVANCE Studies Abstract Background In patients with schizophrenia, study design to optimize adherence and objective measurement of adherence is critical for interpreting results. Two randomized...
PMC12133530
core_pubmed_pmc
Serum retinol binding protein as a novel marker for clearance and dosage optimization: pharmacokinetics study of voriconazole in a cirrhosis population
Serum retinol binding protein as a novel marker for clearance and dosage optimization: pharmacokinetics study of voriconazole in a cirrhosis population Abstract Background and Objective Voriconazole (VRC) exhibits nonlinear pharmacokinetic (PK) characteristics and a narrow therapeutic window. Consequently, standardized...
PMC10147685
core_pubmed_pmc
Safety, tolerability, and pharmacokinetics of Aurora kinase B inhibitor AZD2811: a phase 1 dose-finding study in patients with advanced solid tumours
Safety, tolerability, and pharmacokinetics of Aurora kinase B inhibitor AZD2811: a phase 1 dose-finding study in patients with advanced solid tumours Abstract Background AZD2811 is a potent, selective Aurora kinase B inhibitor. We report the dose-escalation phase of a first-in-human study assessing nanoparticle-encapsu...
PMC12025772
core_pubmed_pmc
Retrospective Review of Intra-Cerebrospinal Fluid (CSF) Drug Delivery in CNS Malignancies: Safety, Clinical Efficacy and Pharmacokinetic Profiles of Intracerebroventricular (ICV), Lumbar Intrathecal (LIT), and Intra-Cisterna Magna (ICM) Injections
Retrospective Review of Intra-Cerebrospinal Fluid (CSF) Drug Delivery in CNS Malignancies: Safety, Clinical Efficacy and Pharmacokinetic Profiles of Intracerebroventricular (ICV), Lumbar Intrathecal (LIT), and Intra-Cisterna Magna (ICM) Injections Abstract Simple Summary Intra-cerebrospinal fluid (CSF) drug delivery is...
PMC9469701
core_pubmed_pmc
Flexible and efficient Bayesian pharmacometrics modeling using Stan and Torsten, Part I
Flexible and efficient Bayesian pharmacometrics modeling using Stan and Torsten, Part I Abstract Abstract Stan is an open‐source probabilistic programing language, primarily designed to do Bayesian data analysis. Its main inference algorithm is an adaptive Hamiltonian Monte Carlo sampler, supported by state‐of‐the‐art ...
PMC6153844
core_pubmed_pmc
Population Pharmacokinetics of the Antimalarial Amodiaquine: a Pooled Analysis To Optimize Dosing
Population Pharmacokinetics of the Antimalarial Amodiaquine: a Pooled Analysis To Optimize Dosing Abstract Amodiaquine plus artesunate is the recommended antimalarial treatment in many countries where malaria is endemic. However, pediatric doses are largely based on a linear extrapolation from adult doses. KEYWORDS: NO...
PMC3528070
core_pubmed_pmc
Comparative pharmacokinetic study of two mycophenolate mofetil formulations in stable kidney transplant recipients
Comparative pharmacokinetic study of two mycophenolate mofetil formulations in stable kidney transplant recipients Abstract Summary We compared steady-state pharmacokinetics of mycophenolate mofetil (MMF) – Myfenax® (Teva) and CellCept® (Roche) – in stable kidney transplant recipients (KTRs). This was an international,...
PMC7993277
core_pubmed_pmc
Retrospective Analysis Using Pharmacokinetic/Pharmacodynamic Modeling and Simulation Offers Improvements in Efficiency of the Design of Volunteer Infection Studies for Antimalarial Drug Development
Retrospective Analysis Using Pharmacokinetic/Pharmacodynamic Modeling and Simulation Offers Improvements in Efficiency of the Design of Volunteer Infection Studies for Antimalarial Drug Development Abstract Volunteer infection studies using the induced blood stage malaria (IBSM) model have been shown to facilitate anti...
PMC12261486
core_pubmed_pmc
ADME-drug-likeness: enriching molecular foundation models via pharmacokinetics-guided multi-task learning for drug-likeness prediction
ADME-drug-likeness: enriching molecular foundation models via pharmacokinetics-guided multi-task learning for drug-likeness prediction Abstract Abstract Summary Recent breakthroughs in AI-driven generative models enable the rapid design of extensive molecular libraries, creating an urgent need for fast and accurate dru...
PMC4629105
core_pubmed_pmc
Pharmacokinetic aspects and in vitro – in vivo correlation potential for lipid-based formulations
Pharmacokinetic aspects and in vitro – in vivo correlation potential for lipid-based formulations Abstract Abstract Lipid-based formulations have been an attractive choice among novel drug delivery systems for enhancing the solubility and bioavailability of poorly soluble drugs due to their ability to keep the drug in ...
PMC3261206
core_pubmed_pmc
Rapid Evaluation in Whole Blood Culture of Regimens for XDR-TB Containing PNU-100480 (Sutezolid), TMC207, PA-824, SQ109, and Pyrazinamide
Rapid Evaluation in Whole Blood Culture of Regimens for XDR-TB Containing PNU-100480 (Sutezolid), TMC207, PA-824, SQ109, and Pyrazinamide Abstract Abstract There presently is no rapid method to assess the bactericidal activity of new regimens for tuberculosis. This study examined PNU-100480, TMC207, PA-824, SQ109, and ...
PMC9651896
core_pubmed_pmc
Pharmacokinetics, Bioequivalence and Safety of Cloperastine in Chinese Healthy Subjects Under Fasting and Postprandial Conditions
Pharmacokinetics, Bioequivalence and Safety of Cloperastine in Chinese Healthy Subjects Under Fasting and Postprandial Conditions Abstract Abstract Background Cloperastine is a pivotal antibechic widely prescribed to treat cough caused by respiratory diseases. The present trial evaluated the pharmacokinetics (PK), bioe...
PMC8042570
core_pubmed_pmc
In silico approach for identifying natural lead molecules against SARS-COV-2
In silico approach for identifying natural lead molecules against SARS-COV-2 Abstract The life challenging COVID-19 disease caused by the SARS-CoV-2 virus has greatly impacted smooth survival worldwide since its discovery in December 2019. Currently, it is one of the major threats to humanity. Moreover, any specific dr...
PMC4158172
core_pubmed_pmc
Effects of enzyme inducers efavirenz and tipranavir/ritonavir on the pharmacokinetics of the HIV integrase inhibitor dolutegravir
Effects of enzyme inducers efavirenz and tipranavir/ritonavir on the pharmacokinetics of the HIV integrase inhibitor dolutegravir Abstract Purpose Dolutegravir (DTG) is an unboosted, integrase inhibitor for the treatment of HIV infection. Two studies evaluated the effects of efavirenz (EFV) and tipranavir/ritonavir (TP...
PMC4592230
core_pubmed_pmc
A Fab-Selective Immunoglobulin-Binding Domain from Streptococcal Protein G with Improved Half-Life Extension Properties
A Fab-Selective Immunoglobulin-Binding Domain from Streptococcal Protein G with Improved Half-Life Extension Properties Abstract Background Half-life extension strategies have gained increasing interest to improve the pharmacokinetic and pharmacodynamic properties of protein therapeutics. Recently, we established an im...
PMC6156733
core_pubmed_pmc
Randomized study of the safety and pharmacodynamics of inhaled interleukin-13 monoclonal antibody fragment VR942
Randomized study of the safety and pharmacodynamics of inhaled interleukin-13 monoclonal antibody fragment VR942 Abstract Abstract Background Interleukin-13 (IL-13) is a key mediator of T-helper-cell-type-2 (Th-2)-driven asthma, the inhibition of which may improve treatment outcomes. We examined the safety, pharmacokin...
PMC9681820
core_pubmed_pmc
A PDE10A inhibitor CPL500036 is a novel agent modulating striatal function devoid of most neuroleptic side-effects
A PDE10A inhibitor CPL500036 is a novel agent modulating striatal function devoid of most neuroleptic side-effects Abstract Abstract Background: Phosphodiesterase 10A (PDE10A) is expressed almost exclusively in the striatum and its inhibition is suggested to offer potential treatment in disorders associated with basal ...
PMC5614923
core_pubmed_pmc
microRNAs Make the Call in Cancer Personalized Medicine
microRNAs Make the Call in Cancer Personalized Medicine Abstract Since their discovery and the advent of RNA interference, microRNAs have drawn enormous attention because of their ubiquitous involvement in cellular pathways from life to death, from metabolism to communication. It is also widely accepted that they posse...
PMC12059905
core_pubmed_pmc
Recent Advances in Therapeutic Peptides: Innovations and Applications in Treating Infections and Diseases
Recent Advances in Therapeutic Peptides: Innovations and Applications in Treating Infections and Diseases Abstract Peptides have become a powerful frontier in modern medicine, offering a promising therapeutic solution for various diseases and advancing rapidly in pharmaceutical development. These small amino acid chain...
PMC10623729
core_pubmed_pmc
nlive: an R package to facilitate the application of the sigmoidal and random changepoint mixed models
nlive: an R package to facilitate the application of the sigmoidal and random changepoint mixed models Abstract Abstract Background The use of mixed effect models with a specific functional form such as the Sigmoidal Mixed Model and the Piecewise Mixed Model (or Changepoint Mixed Model) with abrupt or smooth random cha...
PMC11349424
core_pubmed_pmc
Pharmacokinetics of Edoxaban 15 mg in Very Elderly Patients with Nonvalvular Atrial Fibrillation: A Subanalysis of the ELDERCARE-AF Study
Pharmacokinetics of Edoxaban 15 mg in Very Elderly Patients with Nonvalvular Atrial Fibrillation: A Subanalysis of the ELDERCARE-AF Study Statistical Analysis Statistical Analysis The PK analysis set consisted of all patients randomly assigned to receive edoxaban without major protocol deviations affecting PK and with ...
PMC12252343
core_pubmed_pmc
Dietary Carnosine Supplementation in Healthy Human Volunteers: A Safety, Tolerability, Plasma and Brain Concentration Study
Dietary Carnosine Supplementation in Healthy Human Volunteers: A Safety, Tolerability, Plasma and Brain Concentration Study Abstract Background: Carnosine is a multimodal pleotropic endogenous molecule that exhibits properties that make it a compelling therapeutic agent for further evaluation in a number of diseases. H...
PMC7025654
core_pubmed_pmc
Pharmacokinetics and Tolerability of Single and Multiple Intravenous Doses of Cefotetan Disodium in Healthy Chinese Volunteers
Pharmacokinetics and Tolerability of Single and Multiple Intravenous Doses of Cefotetan Disodium in Healthy Chinese Volunteers Abstract Background Cefotetan is highly stable to penicillinase and cephalosporin produced by gram-negative bacteria, and it has strong antimicrobial activity against most gram-negative bacteri...
PMC3961628
core_pubmed_pmc
Effect of Activated Charcoal on Apixaban Pharmacokinetics in Healthy Subjects
Effect of Activated Charcoal on Apixaban Pharmacokinetics in Healthy Subjects Abstract Background Activated charcoal is commonly used to manage overdose or accidental ingestion of medicines. This study evaluated the effect of activated charcoal on apixaban exposure in human subjects. Methods This was an open-label, thr...
PMC12489817
core_pubmed_pmc
Nosocomial and Ventilator-associated Pneumonia
Nosocomial and Ventilator-associated Pneumonia Abstract Abstract Nosocomial pneumonia (NP), including its subtype ventilator-associated pneumonia (VAP), represents a major cause of morbidity, mortality, and increased healthcare utilization in hospitalized patients, particularly in intensive care settings. This comprehe...
PMC7066296
core_pubmed_pmc
A clinical pharmacology study of the novel, selective urate reabsorption inhibitor dotinurad in outpatients
A clinical pharmacology study of the novel, selective urate reabsorption inhibitor dotinurad in outpatients Abstract Background Dotinurad is a novel, selective urate reabsorption inhibitor (SURI), which reduces serum uric acid levels by selective inhibition of the urate transporter 1 (URAT1). The Japanese guideline for...
PMC11533099
core_pubmed_pmc
Recommendation of mavacamten posology by model‐based analyses in adults with obstructive hypertrophic cardiomyopathy
Recommendation of mavacamten posology by model‐based analyses in adults with obstructive hypertrophic cardiomyopathy Abstract Abstract Mavacamten is the first cardiac myosin inhibitor approved by the US Food and Drug Administration for the treatment of adults with symptomatic obstructive hypertrophic cardiomyopathy (HC...
PMC3910015
core_pubmed_pmc
Incorporating Target Shedding Into a Minimal PBPK–TMDD Model for Monoclonal Antibodies
Incorporating Target Shedding Into a Minimal PBPK–TMDD Model for Monoclonal Antibodies Abstract Shedding of a pharmacological target from cells, giving rise to a soluble target that can also bind therapeutic proteins, is a common phenomenon. In this study, a minimal physiologically based pharmacokinetic model was used ...
PMC6161324
core_pubmed_pmc
Pharmacokinetics of Salmeterol and Fluticasone Propionate Delivered in Combination via Easyhaler and Diskus Dry Powder Inhalers in Healthy Subjects
Pharmacokinetics of Salmeterol and Fluticasone Propionate Delivered in Combination via Easyhaler and Diskus Dry Powder Inhalers in Healthy Subjects Abstract Abstract Background: Easyhaler ® dry powder inhaler (DPI) containing salmeterol and fluticasone propionate was developed for the treatment of asthma and chronic ob...
PMC8856936
core_pubmed_pmc
Plasma neurofilament light, glial fibrillary acidic protein and lysosphingolipid biomarkers for pharmacodynamics and disease monitoring of GM2 and GM1 gangliosidoses patients
Plasma neurofilament light, glial fibrillary acidic protein and lysosphingolipid biomarkers for pharmacodynamics and disease monitoring of GM2 and GM1 gangliosidoses patients Abstract Abstract GM2 and GM1 gangliosidoses are genetic, neurodegenerative lysosomal sphingolipid storage disorders. The earlier the age of onse...
PMC12072619
core_pubmed_pmc
Challenges and Opportunities of Direct Oral Anticoagulant (DOAC) Therapy in Complex Clinical Scenarios: A Comprehensive Review and Practical Guide
Challenges and Opportunities of Direct Oral Anticoagulant (DOAC) Therapy in Complex Clinical Scenarios: A Comprehensive Review and Practical Guide Abstract Direct oral anticoagulants (DOACs) have emerged as a preferred alternative to vitamin K antagonists (VKAs) for the prevention and treatment of thromboembolic disord...
PMC9492925
core_pubmed_pmc
Effects of ilaprazole on the steady-state pharmacodynamics of clopidogrel in healthy volunteers: An open-label randomized crossover study
Effects of ilaprazole on the steady-state pharmacodynamics of clopidogrel in healthy volunteers: An open-label randomized crossover study Abstract Abstract Background: Previous studies have suggested that proton pump inhibitors could impair the antiplatelet effect of clopidogrel. It is uncertain whether ilaprazole affe...
PMC8923731
core_pubmed_pmc
Increasing application of pediatric physiologically based pharmacokinetic models across academic and industry organizations
Increasing application of pediatric physiologically based pharmacokinetic models across academic and industry organizations Abstract Abstract There has been a significant increase in the use of physiologically based pharmacokinetic (PBPK) models during the past 20 years, especially for pediatrics. The aim of this study...
PMC5872895
core_pubmed_pmc
Comparison of Three Different Concentrations of Levobupivacaine for Epidural Labor Analgesia: Clinical Effect and Pharmacokinetic Profile
Comparison of Three Different Concentrations of Levobupivacaine for Epidural Labor Analgesia: Clinical Effect and Pharmacokinetic Profile Abstract Background: The aim is to compare the clinical effect of three different concentrations of levobupivacaine (0.25%, 0.125%, and 0.0625%) on the sensory and motor block charac...
PMC12178312
core_pubmed_pmc
Pharmacokinetics and Tissue Distribution of Palmatine after Single Intramuscular Injection in Partridge Shank Chickens
Pharmacokinetics and Tissue Distribution of Palmatine after Single Intramuscular Injection in Partridge Shank Chickens Abstract ABSTRACT Palmatine is an isoquinoline alkaloid isolated from many medicinal plants with diverse pharmacological activities, with potential for the treatment of chronic metabolic disorders and ...
PMC7993265
core_pubmed_pmc
YH12852, a Potent and Selective Receptor Agonist of 5‐hydroxytryptamine, Increased Gastrointestinal Motility in Healthy Volunteers and Patients With Functional Constipation
YH12852, a Potent and Selective Receptor Agonist of 5‐hydroxytryptamine, Increased Gastrointestinal Motility in Healthy Volunteers and Patients With Functional Constipation Abstract Abstract Gastrointestinal (GI) motility disorders are common, decreases quality of life, and imposes a substantial economic burden. YH1285...
PMC6820598
core_pubmed_pmc
Routine clinical care data for population pharmacokinetic modeling: the case for Fanhdi/Alphanate in hemophilia A patients
Routine clinical care data for population pharmacokinetic modeling: the case for Fanhdi/Alphanate in hemophilia A patients Abstract Abstract Fanhdi/Alphanate is a plasma derived factor VIII concentrate used for treating hemophilia A, for which there has not been any dedicated model describing its pharmacokinetics (PK)....
PMC6273400
core_pubmed_pmc
Enhancement of Exposure and Reduction of Elimination for Paeoniflorin or Albiflorin via Co-Administration with Total Peony Glucosides and Hypoxic Pharmacokinetics Comparison
Enhancement of Exposure and Reduction of Elimination for Paeoniflorin or Albiflorin via Co-Administration with Total Peony Glucosides and Hypoxic Pharmacokinetics Comparison Abstract There is evidence suggesting that herbal extracts demonstrate greater bioactivities than their isolated constituents at an equivalent dos...
PMC3456924
core_pubmed_pmc
Single-dose pharmacokinetic and toxicity analysis of pyrrole–imidazole polyamides in mice
Single-dose pharmacokinetic and toxicity analysis of pyrrole–imidazole polyamides in mice Abstract Purpose Pyrrole–imidazole (Py-Im) polyamides are programmable, sequence-specific DNA minor groove–binding ligands. Previous work in cell culture has shown that various polyamides can be used to modulate the transcriptiona...
PMC11945243
core_pubmed_pmc
Assessing Drug–Drug Interaction and Food Effect for BCS Class 2 Compound BI 730357 (Retinoic Acid-Related Orphan Receptor Gamma Antagonist, Bevurogant) Using a Physiology-Based Pharmacokinetics Modeling (PBPK) Approach with Semi-Mechanistic Absorption
Assessing Drug–Drug Interaction and Food Effect for BCS Class 2 Compound BI 730357 (Retinoic Acid-Related Orphan Receptor Gamma Antagonist, Bevurogant) Using a Physiology-Based Pharmacokinetics Modeling (PBPK) Approach with Semi-Mechanistic Absorption Abstract Abstract Background : The drug candidate BI 730357 is a Bio...
PMC7653926
core_pubmed_pmc
Comparative proteomic analysis of serum from nonhuman primates administered BIO 300: a promising radiation countermeasure
Comparative proteomic analysis of serum from nonhuman primates administered BIO 300: a promising radiation countermeasure Abstract Hematopoietic acute radiation syndrome (H-ARS) and delayed effects of acute radiation exposure (DEARE) are detrimental health effects that occur after exposure to high doses of ionizing rad...
PMC12041905
core_pubmed_pmc
Development of a Rapid LC‐MS/MS Method and Its Application for the Pharmacokinetic Analysis of Pacritinib in Rats
Development of a Rapid LC‐MS/MS Method and Its Application for the Pharmacokinetic Analysis of Pacritinib in Rats Abstract ABSTRACT Pacritinib is a novel medication with certain limitations and unknowns in therapeutic applications. Due to the increased frequency of side effects such as fungal infections, nausea, and vo...
PMC12547357
core_pubmed_pmc
A Comparison of AI and Population PK Models to Predict the Concentrations of Antiepileptic Drugs Using Therapeutic Drug Monitoring Records
A Comparison of AI and Population PK Models to Predict the Concentrations of Antiepileptic Drugs Using Therapeutic Drug Monitoring Records Abstract ABSTRACT Population pharmacokinetic (PK) models are commonly used to predict drug concentrations, but artificial intelligence (AI) models have gained interest due to their ...
PMC11499533
core_pubmed_pmc
Efficacy and safety of candidate biosimilar CT-P41 versus reference denosumab: a double-blind, randomized, active-controlled, Phase 3 trial in postmenopausal women with osteoporosis
Efficacy and safety of candidate biosimilar CT-P41 versus reference denosumab: a double-blind, randomized, active-controlled, Phase 3 trial in postmenopausal women with osteoporosis Abstract Abstract Summary This 78-week (18-month) study conducted in 479 postmenopausal women with osteoporosis evaluated the efficacy, ph...
PMC4773674
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic properties of insulin degludec in Japanese patients with type 1 diabetes mellitus reflect similarities with Caucasian patients
Pharmacokinetic and pharmacodynamic properties of insulin degludec in Japanese patients with type 1 diabetes mellitus reflect similarities with Caucasian patients Abstract Abstract Introduction The present study aimed to evaluate the pharmacokinetic and pharmacodynamic properties of insulin degludec ( ID eg) in Japanes...
PMC5369873
core_pubmed_pmc
Beta‐blockers for hypertension
Beta‐blockers for hypertension Abstract Abstract Background Beta‐blockers refer to a mixed group of drugs with diverse pharmacodynamic and pharmacokinetic properties. They have shown long‐term beneficial effects on mortality and cardiovascular disease (CVD) when used in people with heart failure or acute myocardial inf...
PMC6485091
core_pubmed_pmc
Drug related problems in the neonatal intensive care unit: incidence, characterization and clinical relevance
Drug related problems in the neonatal intensive care unit: incidence, characterization and clinical relevance Abstract Background Any event involving drug therapy that may interfere in a patient’s desired clinical outcome is called a drug related problem (DRP). DRP are very common in intensive therapy, however, little ...
PMC9862597
core_pubmed_pmc
Anti-Colorectal Cancer Effects of a Novel Camptothecin Derivative PCC0208037 In Vitro and In Vivo
Anti-Colorectal Cancer Effects of a Novel Camptothecin Derivative PCC0208037 In Vitro and In Vivo Abstract Abstract Colorectal cancer is one of the most common malignancies, and the topoisomerase inhibitor irinotecan (CPT-11)-based chemotherapeutic regimen is currently the first-line treatment with impressive therapeut...
PMC6326087
core_pubmed_pmc
Clinical Pharmacokinetics and Dose Recommendations for Posaconazole in Infants and Children
Clinical Pharmacokinetics and Dose Recommendations for Posaconazole in Infants and Children Abstract Abstract Objectives The objectives of this study were to investigate the population pharmacokinetics of posaconazole in immunocompromised children, evaluate the influence of patient characteristics on posaconazole expos...
PMC6518930
core_pubmed_pmc
Population Pharmacokinetic Modeling to Evaluate Standard Magnesium Sulfate Treatments and Alternative Dosing Regimens for Women With Preeclampsia
Population Pharmacokinetic Modeling to Evaluate Standard Magnesium Sulfate Treatments and Alternative Dosing Regimens for Women With Preeclampsia Abstract Abstract Magnesium sulfate is the standard therapy for prevention and treatment of eclampsia. Two standard dosing regimens require either continuous intravenous infu...
PMC12351152
core_pubmed_pmc
No Impact of Vancomycin MIC, AUC, or AUC/MIC in Enterococcus faecium Bacteremia
No Impact of Vancomycin MIC, AUC, or AUC/MIC in Enterococcus faecium Bacteremia Abstract ABSTRACT Background There is no clear pharmacokinetic and pharmacodynamic (PK/PD) target during vancomycin‐susceptible Enterococcus faecium bacteremia (EFB). Objectives To investigate whether in‐hospital mortality was associated wi...
PMC12602992
core_pubmed_pmc
Gender‐Affirming Hormone Therapy: Pharmacokinetic Considerations for Oncology in Transgender Patients
Gender‐Affirming Hormone Therapy: Pharmacokinetic Considerations for Oncology in Transgender Patients Abstract ABSTRACT Gender‐Affirming Hormone Therapy (GAHT) is a cornerstone of transgender care which induces profound physiological changes and significantly impacts pharmacokinetics and drug dosing strategies. This na...
PMC3476920
core_pubmed_pmc
Remogliflozin Etabonate, a Selective Inhibitor of the Sodium-Glucose Transporter 2, Improves Serum Glucose Profiles in Type 1 Diabetes
Remogliflozin Etabonate, a Selective Inhibitor of the Sodium-Glucose Transporter 2, Improves Serum Glucose Profiles in Type 1 Diabetes Abstract Abstract OBJECTIVE Remogliflozin etabonate (RE), an inhibitor of the sodium-glucose transporter 2, improves glucose profiles in type 2 diabetes. This study assessed safety, tol...
PMC8954907
core_pubmed_pmc
Theoretical Model and Actual Characteristics of Air Pollution Affecting Health Cost: A Review
Theoretical Model and Actual Characteristics of Air Pollution Affecting Health Cost: A Review Abstract Abstract Background: The impact of environmental pollution (such as air pollution) on health costs has received a great deal of global attention in the last 20 years. Methods: This review aims to summarize the theoret...
PMC7042003
core_pubmed_pmc
Pharmacokinetic characteristics of fluticasone, salmeterol and tiotropium after concurrent inhalation
Pharmacokinetic characteristics of fluticasone, salmeterol and tiotropium after concurrent inhalation Abstract Abstract Chronic obstructive pulmonary disease (COPD) is a type of progressive, obstructive lung disease characterized by long-term poor airflow. The symptoms of COPD may be relieved and its progression delaye...
PMC4761019
core_pubmed_pmc
Physiologically Based Modelling of Darunavir/Ritonavir Pharmacokinetics During Pregnancy
Physiologically Based Modelling of Darunavir/Ritonavir Pharmacokinetics During Pregnancy Abstract Abstract Pregnant women are usually excluded from clinical trials. Physiologically based pharmacokinetic (PBPK) modelling may provide a method to predict pharmacokinetics in pregnant women, without the need to perform exte...
PMC7525157
core_pubmed_pmc
Commentary: Recommendation of Antimicrobial Dosing Optimization During Continuous Renal Replacement Therapy
Commentary: Recommendation of Antimicrobial Dosing Optimization During Continuous Renal Replacement Therapy Modeling Consider Therapeutic Drug Monitoring (TDM) and PK-PD Models Regarding inter/intra-individual variability, individualized PK-PD targets and dosing are required ( Goldstein and Nolin, 2014 ; Roberts and Ro...
PMC9496228
core_pubmed_pmc
Plasma Clearance of Intravenously Infused Adrenomedullin in Rats with Acute Renal Failure
Plasma Clearance of Intravenously Infused Adrenomedullin in Rats with Acute Renal Failure Abstract Abstract Plasma adrenomedullin concentrations are reportedly elevated in patients with renal failure; however, the underlying mechanism is unclear. In this study, we investigated the plasma clearance of synthetic human ad...
PMC11465586
core_pubmed_pmc
Determination of the extremolyte ectoine in plasma and a pharmacokinetic study in rats by a validated and BAGI-evaluated UPLC-MS/MS method
Determination of the extremolyte ectoine in plasma and a pharmacokinetic study in rats by a validated and BAGI-evaluated UPLC-MS/MS method Abstract Abstract Ectoine (ECT) has recently gained considerable interest in the healthcare sector due to its promising therapeutic benefits in a variety of human disorders. This re...
PMC4488827
core_pubmed_pmc
Pharmacokinetics and Toxicity of Sodium Selenite in the Treatment of Patients with Carcinoma in a Phase I Clinical Trial: The SECAR Study
Pharmacokinetics and Toxicity of Sodium Selenite in the Treatment of Patients with Carcinoma in a Phase I Clinical Trial: The SECAR Study Abstract Abstract Background: Sodium selenite at high dose exerts antitumor effects and increases efficacy of cytostatic drugs in multiple preclinical malignancy models. We assessed ...
PMC11015072
core_pubmed_pmc
Simulation‐based evaluation of personalized dosing approaches for anti‐FGFR/KLB bispecific antibody fazpilodemab
Simulation‐based evaluation of personalized dosing approaches for anti‐FGFR/KLB bispecific antibody fazpilodemab Abstract Abstract Personalized dosing approaches play important roles in clinical practices to improve benefit: risk profiles. Whereas this is also important for drug development, especially in the context o...
PMC6130670
core_pubmed_pmc
Determination of cepharanthine in rat plasma by LC–MS/MS and its application to a pharmacokinetic study
Determination of cepharanthine in rat plasma by LC–MS/MS and its application to a pharmacokinetic study Abstract Abstract Context: Cepharanthine (CPA) has been reported to possess a wide range of pharmacological activities. Objective: This study investigates the pharmacokinetic characteristics after oral or intravenous...
PMC4463677
core_pubmed_pmc
Preparation and in Vivo Evaluation of a Dutasteride-Loaded Solid-Supersaturatable Self-Microemulsifying Drug Delivery System
Preparation and in Vivo Evaluation of a Dutasteride-Loaded Solid-Supersaturatable Self-Microemulsifying Drug Delivery System Abstract The purpose of this study was to prepare a dutasteride-loaded solid-supersaturatable self-microemulsifying drug delivery system (SMEDDS) using hydrophilic additives with high oral bioava...
PMC11682675
core_pubmed_pmc
Pharmacokinetic Changes and Influencing Factors of Polymyxin B in Different ECMO Modes
Pharmacokinetic Changes and Influencing Factors of Polymyxin B in Different ECMO Modes Abstract Purpose With the development of extracorporeal membrane oxygenation (ECMO) technology, the duration of ECMO support has gradually increased, leading to an increased risk of ECMO-related bacterial resistance. Polymyxin B (PMB...
PMC6734274
core_pubmed_pmc
Study protocols of three parallel phase 1 trials combining radical radiotherapy with the PARP inhibitor olaparib
Study protocols of three parallel phase 1 trials combining radical radiotherapy with the PARP inhibitor olaparib Abstract Abstract Background Poly (ADP-ribose) Polymerase (PARP) inhibitors are promising novel radiosensitisers. Pre-clinical models have demonstrated potent and tumour-specific radiosensitisation by PARP i...
PMC8773303
core_pubmed_pmc
An Evidence-Based Multidisciplinary Approach Focused on Creating Algorithms for Targeted Therapy of Infection-Related Ventilator-Associated Complications (IVACs) Caused by Pseudomonas aeruginosa and Acinetobacter baumannii in Critically Ill Adult Patients
An Evidence-Based Multidisciplinary Approach Focused on Creating Algorithms for Targeted Therapy of Infection-Related Ventilator-Associated Complications (IVACs) Caused by Pseudomonas aeruginosa and Acinetobacter baumannii in Critically Ill Adult Patients Abstract (1) Background: To develop evidence-based algorithms fo...
PMC4394619
core_pubmed_pmc
Systems Pharmacology Approach Toward the Design of Inhaled Formulations of Rifampicin and Isoniazid for Treatment of Tuberculosis
Systems Pharmacology Approach Toward the Design of Inhaled Formulations of Rifampicin and Isoniazid for Treatment of Tuberculosis Abstract Conventional oral therapies for the treatment of tuberculosis are limited by poor antibiotic distribution in granulomas, which contributes to lengthy treatment regimens and inadequa...
PMC6016700
core_pubmed_pmc
Pharmacological properties of betrixaban
Pharmacological properties of betrixaban Abstract Abstract Venous thromboembolism (VTE) in acute medically ill patients is a leading cause of in-hospital morbidity and mortality. A majority of these VTE events occur post-discharge, and patients remain at increased VTE risk for up to 3 months post-discharge. Recent clin...
PMC10787215
core_pubmed_pmc
Population pharmacokinetic‐pharmacodynamic modeling of clopidogrel for dose regimen optimization based on CYP2C19 phenotypes: A proof of concept study
Population pharmacokinetic‐pharmacodynamic modeling of clopidogrel for dose regimen optimization based on CYP2C19 phenotypes: A proof of concept study Abstract Abstract Clopidogrel is an antiplatelet drug used to reduce the risk of acute coronary syndrome and stroke. It is converted by CYP2C19 to its active metabolite;...
PMC11939159
core_pubmed_pmc
Pharmacokinetics of Doxycycline in Alpacas After Intravenous and Subcutaneous Administration
Pharmacokinetics of Doxycycline in Alpacas After Intravenous and Subcutaneous Administration Abstract Abstract Background/Objectives : Doxycycline, a tetracycline-class antibiotic, is commonly used across various species to treat infections caused by susceptible bacteria. However, pharmacokinetic data on its use in alp...
PMC11078285
core_pubmed_pmc
Predictive Performance of a Gentamicin Pharmacokinetic Model in Term Neonates with Perinatal Asphyxia Undergoing Controlled Therapeutic Hypothermia
Predictive Performance of a Gentamicin Pharmacokinetic Model in Term Neonates with Perinatal Asphyxia Undergoing Controlled Therapeutic Hypothermia Abstract Supplemental Digital Content is Available in the Text. Background: Model validation procedures are crucial when population pharmacokinetic (PK) models are used to ...
PMC11685127
core_pubmed_pmc
Pharmacokinetic/pharma-codynamic study of pralurbactam (FL058) combined with meropenem in a neutropenic murine thigh infection model
Pharmacokinetic/pharma-codynamic study of pralurbactam (FL058) combined with meropenem in a neutropenic murine thigh infection model Abstract Introduction Pralurbactam (FL058) is a novel β-lactamase inhibitor with good inhibitory activity on class A, C, and D β-lactamases. This study aimed to evaluate the pharmacokinet...
PMC11724149
core_pubmed_pmc
New Insights Into Hepatic Impairment (HI) Trials
New Insights Into Hepatic Impairment (HI) Trials Abstract ABSTRACT Hepatic impairment (HI) trials are traditionally part of the clinical pharmacology development to assess the need for dose adaptation in people with impaired metabolic capacity due to their diseased liver. This review aimed at looking into the data from...
PMC12314832
core_pubmed_pmc
Efficacy and safety of oral amantadine in Parkinson’s disease with dyskinesia and motor fluctuations: a systematic review and meta-analysis of randomised controlled trials
Efficacy and safety of oral amantadine in Parkinson’s disease with dyskinesia and motor fluctuations: a systematic review and meta-analysis of randomised controlled trials Abstract Abstract Background Oral amantadine is available in three formulations with distinct pharmacokinetics: immediate-release (IR), delayed-rele...
PMC3317729
core_pubmed_pmc
Pharmacokinetic Comparison of Ferulic Acid in Normal and Blood Deficiency Rats after Oral Administration of Angelica sinensis , Ligusticum chuanxiong and Their Combination
Pharmacokinetic Comparison of Ferulic Acid in Normal and Blood Deficiency Rats after Oral Administration of Angelica sinensis , Ligusticum chuanxiong and Their Combination Abstract Abstract Radix Angelica Sinensis (RAS) and Rhizome Ligusticum (RLC) combination is a popular herb pair commonly used in clinics for treatme...
PMC12480005
core_pubmed_pmc
Interleukin-12 anchored drug conjugate (tolododekin alfa) in patients with advanced solid tumors: first-in-human Phase 1 trial
Interleukin-12 anchored drug conjugate (tolododekin alfa) in patients with advanced solid tumors: first-in-human Phase 1 trial Abstract Abstract Anchored immunotherapy is a novel approach for retaining drugs within the tumour microenvironment. Tolododekin alfa is a first-in-class anchored Interleukin 12 (IL-12) linked ...
PMC6312611
core_pubmed_pmc
Pharmacokinetics of Eight Flavonoids in Rats Assayed by UPLC-MS/MS after Oral Administration of Drynariae rhizoma Extract
Pharmacokinetics of Eight Flavonoids in Rats Assayed by UPLC-MS/MS after Oral Administration of Drynariae rhizoma Extract Abstract As a traditional Chinese medicine, Drynariae rhizoma (Kunze ex Mett.) J. Sm. has been used to treat osteoporosis and bone resorption for 2500 years. Based on the previous study and literatu...
PMC9532340
core_pubmed_pmc
Analysis of the uncharted, druglike property space by self-organizing maps
Analysis of the uncharted, druglike property space by self-organizing maps Abstract Abstract Physicochemical properties are fundamental to predict the pharmacokinetic and pharmacodynamic behavior of drug candidates. Easily calculated descriptors such as molecular weight and logP have been found to correlate with the su...
PMC6848905
core_pubmed_pmc
Vancomycin is commonly under‐dosed in critically ill children and neonates
Vancomycin is commonly under‐dosed in critically ill children and neonates Abstract Abstract Aims Vancomycin is frequently used in critically ill children in whom the drug pharmacokinetics are significantly altered as a result of changes in renal clearance and volume of distribution. Therapeutic drug monitoring (TDM) i...
PMC9298414
core_pubmed_pmc
Single‐ and multiple‐dose safety, tolerability, pharmacokinetic, and pharmacodynamic profiles of ASP0367 , or bocidelpar sulfate, a novel modulator of peroxisome proliferator‐activated receptor delta in healthy adults: Results from a phase 1 study
Single‐ and multiple‐dose safety, tolerability, pharmacokinetic, and pharmacodynamic profiles of ASP0367 , or bocidelpar sulfate, a novel modulator of peroxisome proliferator‐activated receptor delta in healthy adults: Results from a phase 1 study Abstract Abstract Introduction/Aims ASP0367, or bocidelpar sulfate, is a...
PMC7677276
core_pubmed_pmc
Ocular Physiologically Based Pharmacokinetic Modeling for Ointment Formulations
Ocular Physiologically Based Pharmacokinetic Modeling for Ointment Formulations Abstract Purpose The purpose of this study is to show how the Ocular Compartmental Absorption & Transit (OCAT™) model in GastroPlus ® can be used to characterize ocular drug pharmacokinetic performance in rabbits for ointment formulations. ...
PMC9402896
core_pubmed_pmc
S -Ketamine oral thin film—Part 2: Population pharmacodynamics of S -ketamine, S -norketamine and S -hydroxynorketamine
S -Ketamine oral thin film—Part 2: Population pharmacodynamics of S -ketamine, S -norketamine and S -hydroxynorketamine Abstract Abstract Ketamine is a versatile drug used for many indications and is administered via various routes. Here, we report on the pharmacodynamics of sublingual and buccal fast-dissolving oral-t...