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PMC5843799
core_pubmed_pmc
Strategic establishment of an International Pharmacology Specialty Laboratory in a resource-limited setting
Strategic establishment of an International Pharmacology Specialty Laboratory in a resource-limited setting Abstract Background A growing number of drug development studies that include pharmacokinetic evaluations are conducted in regions lacking a specialised pharmacology laboratory. This necessitated the development ...
PMC8742648
core_pubmed_pmc
Upadacitinib pharmacokinetics and exposure‐response analyses of efficacy and safety in psoriatic arthritis patients – Analyses of phase III clinical trials
Upadacitinib pharmacokinetics and exposure‐response analyses of efficacy and safety in psoriatic arthritis patients – Analyses of phase III clinical trials Abstract Abstract Upadacitinib is an oral Janus kinase inhibitor approved for the treatment of rheumatoid arthritis (RA) and recently approved by the European Medic...
PMC10930352
core_pubmed_pmc
Therapeutic Drug Monitoring to Optimize Risperidone Treatment in Children with Autism Spectrum Disorder
Therapeutic Drug Monitoring to Optimize Risperidone Treatment in Children with Autism Spectrum Disorder Abstract Background: Risperidone is an atypical antipsychotic drug used to treat irritability and aggression in children and adolescents with autism spectrum disorder. In an earlier study, the sum trough concentratio...
PMC10843628
core_pubmed_pmc
Population pharmacokinetics of methotrexate and 7-hydroxymethotrexate and delayed excretion in infants and young children with brain tumor *
Population pharmacokinetics of methotrexate and 7-hydroxymethotrexate and delayed excretion in infants and young children with brain tumor * Abstract Purpose: The objectives of this study were to develop a population pharmacokinetic model of methotrexate (MTX) and its primary metabolite 7-hydroxymethotrexate (7OHMTX) i...
PMC6831456
core_pubmed_pmc
Recent advances and challenges of repurposing nanoparticle-based drug delivery systems to enhance cancer immunotherapy
Recent advances and challenges of repurposing nanoparticle-based drug delivery systems to enhance cancer immunotherapy Abstract Cancer immunotherapy is an attractive treatment option under clinical settings. However, the major challenges of immunotherapy include limited patient response, limited tumor specificity, immu...
PMC12394691
core_pubmed_pmc
PopPK modeling supports BW band dosing of lacosamide for pediatric epilepsy
PopPK modeling supports BW band dosing of lacosamide for pediatric epilepsy Abstract Abstract Personalized precision dosing remains an unmet clinical need. This study used population pharmacokinetic (PopPK) modeling to evaluate transitioning lacosamide (LCM) in children with epilepsy from body weight (BW)-based (mg/kg)...
PMC10635338
core_pubmed_pmc
Using Prior Knowledge on Systems Through PBPK to Gain Further Insight into Routine Clinical Data on Trough Concentrations: The Case of Tacrolimus in Chronic Kidney Disease
Using Prior Knowledge on Systems Through PBPK to Gain Further Insight into Routine Clinical Data on Trough Concentrations: The Case of Tacrolimus in Chronic Kidney Disease Abstract Supplemental Digital Content is Available in the Text. Background: Routine therapeutic drug monitoring (TDM) relies heavily on measuring tr...
PMC12388016
core_pubmed_pmc
Comparative Study Between the Short-Term Effects of Replacement Therapy with Liquid and Tablet Formulations of Levothyroxine on Insulin Resistance Markers in Recently Thyroidectomized Female Patients
Comparative Study Between the Short-Term Effects of Replacement Therapy with Liquid and Tablet Formulations of Levothyroxine on Insulin Resistance Markers in Recently Thyroidectomized Female Patients Abstract Background/Objectives : Levothyroxine (L-T4) replacement therapy is essential following total thyroidectomy. Wh...
PMC12909347
core_pubmed_pmc
Disconnect between in vitro and in vivo efficacy of the MPS1 inhibitor NTRC 0066-0 against glioblastoma
Disconnect between in vitro and in vivo efficacy of the MPS1 inhibitor NTRC 0066-0 against glioblastoma Abstract Abstract Purpose Glioblastoma (GBM) is the most common adult primary brain tumor for which new therapeutic strategies are desperately needed. Monopolar spindle 1 (MPS1) is a mitotic kinase that plays a pivot...
PMC9506126
core_pubmed_pmc
Development and Evaluation of a Physiologically Based Pharmacokinetic Model for Predicting Haloperidol Exposure in Healthy and Disease Populations
Development and Evaluation of a Physiologically Based Pharmacokinetic Model for Predicting Haloperidol Exposure in Healthy and Disease Populations Abstract Abstract The physiologically based pharmacokinetic (PBPK) approach can be used to develop mathematical models for predicting the absorption, distribution, metabolis...
PMC9780293
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of anti-tuberculosis drugs: An evaluation of in vitro , in vivo methodologies and human studies
Pharmacokinetics and pharmacodynamics of anti-tuberculosis drugs: An evaluation of in vitro , in vivo methodologies and human studies Abstract Abstract There has been an increased interest in pharmacokinetics and pharmacodynamics (PKPD) of anti-tuberculosis drugs. A better understanding of the relationship between drug...
PMC3910010
core_pubmed_pmc
Scale Reduction of a Systems Coagulation Model With an Application to Modeling Pharmacokinetic–Pharmacodynamic Data
Scale Reduction of a Systems Coagulation Model With an Application to Modeling Pharmacokinetic–Pharmacodynamic Data Abstract Bridging systems biology and pharmacokinetics–pharmacodynamics has resulted in models that are highly complex and complicated. They usually contain large numbers of states and parameters and desc...
PMC11219779
core_pubmed_pmc
Identifying Bayesian optimal experiments for uncertain biochemical pathway models
Identifying Bayesian optimal experiments for uncertain biochemical pathway models Abstract Pharmacodynamic (PD) models are mathematical models of cellular reaction networks that include drug mechanisms of action. These models are useful for studying predictive therapeutic outcomes of novel drug therapies in silico. How...
PMC10196403
core_pubmed_pmc
Mechanistic modeling of drug products applied to the skin: A workshop summary report
Mechanistic modeling of drug products applied to the skin: A workshop summary report Abstract Abstract The development of a generic drug product involves demonstrating that there is no significant difference in the rate and extent to which the active ingredient becomes available at the site of action, relative to the r...
PMC5874536
core_pubmed_pmc
Effect of Apium graveolens Extract Administration on the Pharmacokinetics of Captopril in the Plasma of Rats
Effect of Apium graveolens Extract Administration on the Pharmacokinetics of Captopril in the Plasma of Rats Abstract Abstract Apium graveolens (celery) is an edible and traditionally medicinal plant that is used worldwide, among others for the treatment of hypertension. Combining celery with antihypertensive drugs can...
PMC3094355
core_pubmed_pmc
Artesunate Dose Escalation for the Treatment of Uncomplicated Malaria in a Region of Reported Artemisinin Resistance: A Randomized Clinical Trial
Artesunate Dose Escalation for the Treatment of Uncomplicated Malaria in a Region of Reported Artemisinin Resistance: A Randomized Clinical Trial Abstract Abstract Background The emergence of artemisinin resistance has raised concerns that the most potent antimalarial drug may be under threat. The currently recommended...
PMC7200804
core_pubmed_pmc
Predictive engines based on pharmacokinetics modelling for tacrolimus personalized dosage in paediatric renal transplant patients
Predictive engines based on pharmacokinetics modelling for tacrolimus personalized dosage in paediatric renal transplant patients Abstract The development of predictive engines based on pharmacokinetic-physiological mathematical models for personalised dosage recommendations is an immature field. Nevertheless, these mo...
PMC10006082
core_pubmed_pmc
Efficacy of ceftazidime in a murine model following a lethal aerosol exposure to Burkholderia pseudomallei
Efficacy of ceftazidime in a murine model following a lethal aerosol exposure to Burkholderia pseudomallei Abstract Abstract Melioidosis is an endemic disease in numerous tropical regions. Additionally, the bacterium that causes melioidosis, Burkholderia pseudomallei , has potential to be used as a biological weapon. T...
PMC6355468
core_pubmed_pmc
Assay development for determination of DZ2002, a new reversible SAHH inhibitor, and its acid metabolite DZA in blood and application to rat pharmacokinetic study
Assay development for determination of DZ2002, a new reversible SAHH inhibitor, and its acid metabolite DZA in blood and application to rat pharmacokinetic study Abstract Abstract Methyl ( S )-4-(6-amino-9 H -purin-9-yl)-2-hydroxybutanoate (DZ2002) is a potent reversible inhibitor of S -adenosyl-L-homocysteine hydrolas...
PMC9263650
core_pubmed_pmc
Gut microbiota and host Cyp450s co-contribute to pharmacokinetic variability in mice with non-alcoholic steatohepatitis: Effects vary from drug to drug
Gut microbiota and host Cyp450s co-contribute to pharmacokinetic variability in mice with non-alcoholic steatohepatitis: Effects vary from drug to drug Abstract Highlights • Drugs’ pharmacokinetics were changed in NASH disease. • A systematical research on cocktail drugs in NASH. • Gut microbiota can bio-transform some...
PMC6466473
core_pubmed_pmc
Pathway-Based Analysis of the Liver Response to Intravenous Methylprednisolone Administration in Rats: Acute Versus Chronic Dosing
Pathway-Based Analysis of the Liver Response to Intravenous Methylprednisolone Administration in Rats: Acute Versus Chronic Dosing Abstract Pharmacological time-series data, from comparative dosing studies, are critical to characterizing drug effects. Reconciling the data from multiple studies is inevitably difficult; ...
PMC11698622
core_pubmed_pmc
Exploring the therapeutic potential of Asparagus africanus in polycystic ovarian syndrome: a computational analysis
Exploring the therapeutic potential of Asparagus africanus in polycystic ovarian syndrome: a computational analysis Abstract Abstract PCOS is a multifaceted condition characterized by ovarian abnormalities, metabolic disorders, anovulation, and hormonal imbalances. In response to the growing demand for treatments with ...
PMC9081329
core_pubmed_pmc
Pharmacokinetics, Mass Balance, Excretion, and Tissue Distribution of Plasmalogen Precursor PPI-1011
Pharmacokinetics, Mass Balance, Excretion, and Tissue Distribution of Plasmalogen Precursor PPI-1011 Abstract Abstract PPI-1011 is a synthetic plasmalogen precursor in development as a treatment for multiple plasmalogen-deficiency disorders. Previous work has demonstrated the ability of PPI-1011 to augment plasmalogens...
PMC4120017
core_pubmed_pmc
Kinetic Interpretation of the Importance of OATP1B3 and MRP2 in Docetaxel-Induced Hematopoietic Toxicity
Kinetic Interpretation of the Importance of OATP1B3 and MRP2 in Docetaxel-Induced Hematopoietic Toxicity Abstract Neutropenia is a lethal dose-limiting toxicity of docetaxel. Our previous report indicated that the prevalence of severe docetaxel-induced neutropenia is significantly associated with genetic polymorphisms ...
PMC9947705
core_pubmed_pmc
Effectiveness, safety and pharmacokinetics of Polo-like kinase 1 inhibitors in tumor therapy: A systematic review and meta-analysis
Effectiveness, safety and pharmacokinetics of Polo-like kinase 1 inhibitors in tumor therapy: A systematic review and meta-analysis Abstract Objective To provide a systematic review of existing meta-analysis on the efficacy, safety and pharmacokinetics of the novel Polo-like kinase-1 (Plk1) inhibitors in various tumor ...
PMC12046398
core_pubmed_pmc
Ceftazidime-avibactam plus aztreonam cocktail for the treatment of VIM-producing Pseudomonas aeruginosa infections: good enough to have another?
Ceftazidime-avibactam plus aztreonam cocktail for the treatment of VIM-producing Pseudomonas aeruginosa infections: good enough to have another? Abstract Abstract Background Few active antibiotic options are available to treat MBL-producing Pseudomonas aeruginosa infections, and some of these options are either poorly ...
PMC7324303
core_pubmed_pmc
Simulation as a Tool to Illustrate Clinical Pharmacology Concepts to Healthcare Program Learners
Simulation as a Tool to Illustrate Clinical Pharmacology Concepts to Healthcare Program Learners Abstract Purpose of Review This article provides an overview of simulation as an effective and evolving tool for teaching clinical pharmacology within the health professions. Further, opportunities for positioning this meth...
PMC9932581
core_pubmed_pmc
Exposure-Response Analyses of Tremelimumab Monotherapy or in Combination with Durvalumab in Patients with Unresectable Hepatocellular Carcinoma
Exposure-Response Analyses of Tremelimumab Monotherapy or in Combination with Durvalumab in Patients with Unresectable Hepatocellular Carcinoma Abstract Abstract Purpose: A novel single-dose regimen of 300 mg tremelimumab in combination with durvalumab [Single Tremelimumab Regular Interval Durvalumab (STRIDE)] has demo...
PMC7700087
core_pubmed_pmc
Population Pharmacokinetics of Tapentadol in Children from Birth to <18 Years Old
Population Pharmacokinetics of Tapentadol in Children from Birth to <18 Years Old Abstract Objective The main aim of this analysis was to characterize the pharmacokinetics (PK) of tapentadol in pediatric patients from birth to <18 years old who experience acute pain, requiring treatment with an opioid analgesic. Patien...
PMC9865702
core_pubmed_pmc
Nanovesicles as Vanillin Carriers for Antimicrobial Applications
Nanovesicles as Vanillin Carriers for Antimicrobial Applications Abstract Vanillin is a natural compound easily extracted from plants. It has neuroprotective, anti-carcinogenic, antioxidant, antimicrobial, and anti-biofilm properties. It also presents high volatility, high hydrophilicity, and low bioavailability. Nanom...
PMC12843228
core_pubmed_pmc
Medicinal Plants and Phytochemicals in Cardioprotection—Mechanistic Pathways and Translational Roadmap
Medicinal Plants and Phytochemicals in Cardioprotection—Mechanistic Pathways and Translational Roadmap Abstract Abstract Despite major advances in guideline-directed cardiovascular therapy, residual cardiovascular risk persists, partly driven by oxidative stress, chronic inflammation, endothelial dysfunction, and mitoc...
PMC7517983
core_pubmed_pmc
Comparison study of different indoleamine-2,3 dioxygenase inhibitors from the perspective of pharmacodynamic effects
Comparison study of different indoleamine-2,3 dioxygenase inhibitors from the perspective of pharmacodynamic effects Abstract Introduction: Indoleamine 2,3-dioxygenase (IDO) was a potential tumor immunotherapy target. IDO inhibitors showed inconsistent results in clinical trials, but no preclinical comparative study wa...
PMC11161965
core_pubmed_pmc
Intra-abdominal infections survival guide: a position statement by the Global Alliance For Infections In Surgery
Intra-abdominal infections survival guide: a position statement by the Global Alliance For Infections In Surgery Abstract Abstract Intra-abdominal infections (IAIs) are an important cause of morbidity and mortality in hospital settings worldwide. The cornerstones of IAI management include rapid, accurate diagnostics; t...
PMC6110295
core_pubmed_pmc
Spotlight on lorlatinib and its potential in the treatment of NSCLC: the evidence to date
Spotlight on lorlatinib and its potential in the treatment of NSCLC: the evidence to date Abstract The identification of anaplastic lymphoma kinase ( ALK ), an oncogenetic driver mutation, in lung cancer has paved the way for a new era in the treatment of non-small cell lung cancer (NSCLC). Targeting ALK using tyrosine...
PMC11868009
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Properties of Once-Weekly Insulin Efsitora Alfa in Japanese Patients with Type 2 Diabetes
Pharmacokinetic and Pharmacodynamic Properties of Once-Weekly Insulin Efsitora Alfa in Japanese Patients with Type 2 Diabetes Abstract Abstract Introduction This analysis aimed to assess the safety and tolerability of insulin efsitora alfa (efsitora, basal insulin Fc, LY3209590) and characterize the pharmacokinetic and...
PMC9072418
core_pubmed_pmc
Population pharmacokinetic analysis of sildenafil in term and preterm infants with pulmonary arterial hypertension
Population pharmacokinetic analysis of sildenafil in term and preterm infants with pulmonary arterial hypertension Abstract Sildenafil is widely used off-label in pediatric patients with pulmonary arterial hypertension (PAH). This study was conducted to characterize the pharmacokinetics (PK) of sildenafil in term and p...
PMC6032166
core_pubmed_pmc
Natural Products for Drug Discovery in the 21st Century: Innovations for Novel Drug Discovery
Natural Products for Drug Discovery in the 21st Century: Innovations for Novel Drug Discovery Abstract Abstract The therapeutic properties of plants have been recognised since time immemorial. Many pathological conditions have been treated using plant-derived medicines. These medicines are used as concoctions or concen...
PMC12577477
core_pubmed_pmc
A Comprehensive Analysis of Teicoplanin Population Pharmacokinetic Models in Pediatric Populations: Age-Dependent Variability and Implications for Dose Optimization
A Comprehensive Analysis of Teicoplanin Population Pharmacokinetic Models in Pediatric Populations: Age-Dependent Variability and Implications for Dose Optimization Abstract Purpose Teicoplanin (TEC) is widely used for treating invasive infections caused by Gram-positive bacteria. Due to its high pharmacokinetic variab...
PMC8598307
core_pubmed_pmc
Optimal dose and safety of molnupiravir in patients with early SARS-CoV-2: a phase 1, open-label, dose-escalating, randomised controlled study
Optimal dose and safety of molnupiravir in patients with early SARS-CoV-2: a phase 1, open-label, dose-escalating, randomised controlled study Abstract Synopsis Objectives AGILE is a phase Ib/IIa platform for rapidly evaluating COVID-19 treatments. In this trial ( NCT04746183 ) we evaluated the safety and optimal dose ...
PMC8615109
core_pubmed_pmc
Assessment of Micafungin Dosage Regimens in Patients with Cancer Using Pharmacokinetic/Pharmacodynamic Modeling and Monte Carlo Simulation
Assessment of Micafungin Dosage Regimens in Patients with Cancer Using Pharmacokinetic/Pharmacodynamic Modeling and Monte Carlo Simulation Abstract Micafungin is widely used for invasive candidiasis, especially in critically ill patients and those with cancer, and for empirical antifungal therapy in patients with neutr...
PMC10034131
core_pubmed_pmc
Pharmacokinetics and tissue distribution of bleomycin-induced idiopathic pulmonary fibrosis rats treated with cryptotanshinone
Pharmacokinetics and tissue distribution of bleomycin-induced idiopathic pulmonary fibrosis rats treated with cryptotanshinone Abstract Abstract Introduction: Cryptotanshinone(CTS), a compound derived from the root of Salvia miltiorrhiza , has been linked to various of diseases, particularly pulmonary fibrosis. In the ...
PMC5412923
core_pubmed_pmc
Developing a Bayesian adaptive design for a phase I clinical trial: a case study for a novel HIV treatment
Developing a Bayesian adaptive design for a phase I clinical trial: a case study for a novel HIV treatment Abstract Abstract The design of phase I studies is often challenging, because of limited evidence to inform study protocols. Adaptive designs are now well established in cancer but much less so in other clinical a...
PMC11671680
core_pubmed_pmc
Population pharmacokinetics of iruplinalkib in healthy volunteers and patients with solid tumors
Population pharmacokinetics of iruplinalkib in healthy volunteers and patients with solid tumors Abstract Abstract Iruplinalkib (WX‐0593), a selective oral ALK/ROS1 tyrosine kinase inhibitor, was approved in China as first‐line therapy for ALK ‐positive non‐small‐cell lung cancer (NSCLC) and for the treatment of locall...
PMC5064974
core_pubmed_pmc
Pharmacokinetics (PK), pharmacodynamics (PD), and PK-PD integration of ceftiofur after a single intravenous, subcutaneous and subcutaneous-LA administration in lactating goats
Pharmacokinetics (PK), pharmacodynamics (PD), and PK-PD integration of ceftiofur after a single intravenous, subcutaneous and subcutaneous-LA administration in lactating goats Abstract Abstract Background Bacterial pneumonia in goats is usually caused by Mannheimia haemolytica and Pasteurella multocida. Another importa...
PMC12810753
core_pubmed_pmc
Pharmacodynamic evidence for tedizolid use in Mycobacterium avium lung disease
Pharmacodynamic evidence for tedizolid use in Mycobacterium avium lung disease Abstract SUMMARY OBJECTIVE On guideline-based therapy for Mycobacterium avium complex (MAC) lung disease (LD), ∼50%–60% of patients suffer recalcitrant disease. Tedizolid is a promising agent based on the intracellular hollow fibre model of ...
PMC11216685
core_pubmed_pmc
Phage therapy: breathing new tactics into lower respiratory tract infection treatments
Phage therapy: breathing new tactics into lower respiratory tract infection treatments Abstract Lower respiratory tract infections (LRTIs) present a significant global health burden, exacerbated by the rise in antimicrobial resistance (AMR). The persistence and evolution of multidrug-resistant bacteria intensifies the ...
PMC3471604
core_pubmed_pmc
In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration
In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration Abstract Abstract Background Curcumin has a variety of pharmacological effects. However, poor water solubility and low oral bioavailability limit its clinical utility. A delivery system for nanostr...
PMC7729387
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic analysis of baloxavir marboxil, a novel cap-dependent endonuclease inhibitor, in a murine model of influenza virus infection
Pharmacokinetic and pharmacodynamic analysis of baloxavir marboxil, a novel cap-dependent endonuclease inhibitor, in a murine model of influenza virus infection Abstract Abstract Background Baloxavir acid, the active form of the orally available prodrug baloxavir marboxil, is a novel cap-dependent endonuclease inhibito...
PMC9145815
core_pubmed_pmc
Ciprofloxacin in Patients Undergoing Extracorporeal Membrane Oxygenation (ECMO): A Population Pharmacokinetic Study
Ciprofloxacin in Patients Undergoing Extracorporeal Membrane Oxygenation (ECMO): A Population Pharmacokinetic Study Abstract Abstract Extracorporeal membrane oxygenation (ECMO) is utilized to temporarily sustain respiratory and/or cardiac function in critically ill patients. Ciprofloxacin is used to treat nosocomial in...
PMC12603840
core_pubmed_pmc
Body mass index mediates the association between heavy metal exposure and overactive bladder risk: insights from a nationally representative cross-sectional study using explainable machine learning
Body mass index mediates the association between heavy metal exposure and overactive bladder risk: insights from a nationally representative cross-sectional study using explainable machine learning Abstract Abstract Background While environmental heavy metal exposure has been linked to various metabolic disorders, its ...
PMC8955109
core_pubmed_pmc
Pharmacokinetic Variability in Pre-Clinical Studies: Sample Study with Abiraterone in Rats and Implications for Short-Term Comparative Pharmacokinetic Study Designs
Pharmacokinetic Variability in Pre-Clinical Studies: Sample Study with Abiraterone in Rats and Implications for Short-Term Comparative Pharmacokinetic Study Designs Abstract One of the major concerns for all in vivo experiments is intra- and inter-subject variability, which can be a great source of inaccuracy. The aim ...
PMC6437540
core_pubmed_pmc
A Population Pharmacokinetic Analysis Shows that Arylacetamide Deacetylase (AADAC) Gene Polymorphism and HIV Infection Affect the Exposure of Rifapentine
A Population Pharmacokinetic Analysis Shows that Arylacetamide Deacetylase (AADAC) Gene Polymorphism and HIV Infection Affect the Exposure of Rifapentine Abstract Rifapentine is a rifamycin used to treat tuberculosis. As is the case for rifampin, plasma exposures of rifapentine are associated with the treatment respons...
PMC8212739
core_pubmed_pmc
Characterizing the reproducibility in using a liver microphysiological system for assaying drug toxicity, metabolism, and accumulation
Characterizing the reproducibility in using a liver microphysiological system for assaying drug toxicity, metabolism, and accumulation Abstract Abstract Abstract Liver microphysiological systems (MPSs) are promising models for predicting hepatic drug effects. Yet, after a decade since their introduction, MPSs are not r...
PMC11249067
core_pubmed_pmc
Clinical Toxicology of OTC Cough and Cold Pediatric Medications: A Narrative Review
Clinical Toxicology of OTC Cough and Cold Pediatric Medications: A Narrative Review Abstract Abstract Cough and cold symptoms (CCS) are common pediatric conditions often treated with over-the-counter (OTC) medications. However, the available knowledge regarding the safety and toxicity of these medications in children i...
PMC8604244
core_pubmed_pmc
Effects of sedative psychotropic drugs combined with oxycodone on respiratory depression in the rat
Effects of sedative psychotropic drugs combined with oxycodone on respiratory depression in the rat Abstract Abstract Following a decision to require label warnings for concurrent use of opioids and benzodiazepines and increased risk of respiratory depression and death, the US Food and Drug Administratioin (FDA) recogn...
PMC8196716
core_pubmed_pmc
Phase 1 pharmacokinetics and safety study of extended duration dapivirine vaginal rings in the United States
Phase 1 pharmacokinetics and safety study of extended duration dapivirine vaginal rings in the United States Abstract Abstract Introduction Vaginal rings are a promising approach to provide a woman‐centred, long‐acting HIV prevention strategy. Prior trials of a 25 mg dapivirine (DPV) ring have shown a favourable safety...
PMC10107174
core_pubmed_pmc
A randomized, open‐label, two‐treatment crossover study to evaluate the effect of food on the pharmacokinetics of diazepam nasal spray in healthy adults
A randomized, open‐label, two‐treatment crossover study to evaluate the effect of food on the pharmacokinetics of diazepam nasal spray in healthy adults Abstract Abstract Objective The pharmacokinetics of oral diazepam are affected by food, but food‐effect studies have not been conducted for diazepam nasal spray becaus...
PMC6630667
core_pubmed_pmc
Novel Population Pharmacokinetic Approach to Explain the Differences between Cystic Fibrosis Patients and Healthy Volunteers via Protein Binding
Novel Population Pharmacokinetic Approach to Explain the Differences between Cystic Fibrosis Patients and Healthy Volunteers via Protein Binding Abstract Abstract The pharmacokinetics in patients with cystic fibrosis (CF) has long been thought to differ considerably from that in healthy volunteers. For highly protein b...
PMC12479679
core_pubmed_pmc
The Influence of Patient Factors on the Population Pharmacokinetics of Colchicine: Implications for Safe and Effective Dosing
The Influence of Patient Factors on the Population Pharmacokinetics of Colchicine: Implications for Safe and Effective Dosing Abstract Background and Objectives The factors that predict colchicine plasma concentrations and the impact on safety and efficacy are under-researched. We aimed to determine the probability of ...
PMC6341123
core_pubmed_pmc
Genotoxicity and pharmacokinetic characterization of Cereus jamacaru ethanolic extract in rats
Genotoxicity and pharmacokinetic characterization of Cereus jamacaru ethanolic extract in rats Abstract The effect of Cereus jamacaru ethanolic extract in rats was analyzed using genotoxicity assays and liver ABCB1 and CYP2D4 gene expression. The lyophilized extract of C. jamacaru cladodes was analyzed with LC–MS/MS. M...
PMC5615155
core_pubmed_pmc
Toxicological evaluation of the flavour ingredient N -(1-((4-amino-2,2-dioxido-1 H -benzo[ c ][1,2,6]thiadiazin-5-yl)oxy)-2-methylpropan-2-yl)-2,6-dimethylisonicotinamide (S2218)
Toxicological evaluation of the flavour ingredient N -(1-((4-amino-2,2-dioxido-1 H -benzo[ c ][1,2,6]thiadiazin-5-yl)oxy)-2-methylpropan-2-yl)-2,6-dimethylisonicotinamide (S2218) Abstract Highlights • A toxicological evaluation of S2218 was completed for the purpose of assessing its safety for use in food and beverage ...
PMC7164403
core_pubmed_pmc
Intranasal epinephrine in dogs: Pharmacokinetic and heart rate effects
Intranasal epinephrine in dogs: Pharmacokinetic and heart rate effects Abstract Abstract Epinephrine is the standard of care for the treatment of severe allergy and anaphylaxis. Epinephrine is most often administered through the intramuscular (IM) route via autoinjector. The current study aimed to evaluate an alternati...
PMC4243872
core_pubmed_pmc
Monitoring vigabatrin in head injury patients by cerebral microdialysis: obtaining pharmacokinetic measurements in a neurocritical care setting
Monitoring vigabatrin in head injury patients by cerebral microdialysis: obtaining pharmacokinetic measurements in a neurocritical care setting Abstract Abstract Aims The aims were to determine blood–brain barrier penetration and brain extracellular pharmacokinetics for the anticonvulsant vigabatrin (VGB; γ-vinyl-γ-ami...
PMC4291381
core_pubmed_pmc
Pharmacokinetic Interactions between Primaquine and Pyronaridine-Artesunate in Healthy Adult Thai Subjects
Pharmacokinetic Interactions between Primaquine and Pyronaridine-Artesunate in Healthy Adult Thai Subjects Abstract Pyronaridine-artesunate is a newly introduced artemisinin-based combination treatment which may be deployed together with primaquine. A single-dose, randomized, three-sequence crossover study was conducte...
PMC10684614
core_pubmed_pmc
High Variability in Isavuconazole Unbound Fraction in Clinical Practice: A Call to Reconsider Pharmacokinetic/Pharmacodynamic Targets and Breakpoints
High Variability in Isavuconazole Unbound Fraction in Clinical Practice: A Call to Reconsider Pharmacokinetic/Pharmacodynamic Targets and Breakpoints Abstract Isavuconazole exposure–response relationships have been studied with a focus on total rather than unbound exposure, assuming a constant unbound fraction of 1%. W...
PMC7174946
core_pubmed_pmc
RNA-Seq Analysis of the Liver Transcriptome Reveals the Networks Regulating Treatment of Sitagliptin Phosphate plus Fuzhujiangtang Granule in the Zucker Diabetic Fatty Rats
RNA-Seq Analysis of the Liver Transcriptome Reveals the Networks Regulating Treatment of Sitagliptin Phosphate plus Fuzhujiangtang Granule in the Zucker Diabetic Fatty Rats Abstract Abstract Diabetes is one of the most serious chronic diseases. Numerous drugs including oral agents and traditional Chinese medicines, suc...
PMC4885489
core_pubmed_pmc
Prediction of Drug-Drug Interactions Arising from CYP3A induction Using a Physiologically Based Dynamic Model
Prediction of Drug-Drug Interactions Arising from CYP3A induction Using a Physiologically Based Dynamic Model Abstract Abstract Using physiologically based pharmacokinetic modeling, we predicted the magnitude of drug-drug interactions (DDIs) for studies with rifampicin and seven CYP3A4 probe substrates administered i.v...
PMC8199682
core_pubmed_pmc
Population Pharmacokinetics of Oxycodone and Metabolites in Patients with Cancer-Related Pain
Population Pharmacokinetics of Oxycodone and Metabolites in Patients with Cancer-Related Pain Abstract Abstract Simple Summary Patients with moderate to severe cancer-related pain are frequently treated with oxycodone, a strong-acting opioid. However, treatment with oxycodone does not always lead to sufficient analgesi...
PMC9338916
core_pubmed_pmc
Exploring Inductive Linearization for simulation and estimation with an application to the Michaelis–Menten model
Exploring Inductive Linearization for simulation and estimation with an application to the Michaelis–Menten model Abstract Nonlinear ordinary differential equations (ODEs) are common in pharmacokinetic–pharmacodynamic systems. Although their exact solutions cannot generally be determined via algebraic methods, their ra...
PMC11682956
core_pubmed_pmc
Population pharmacokinetic and pharmacodynamic model guided weight-tiered dose of AST-001 in pediatric patients with autism spectrum disorder
Population pharmacokinetic and pharmacodynamic model guided weight-tiered dose of AST-001 in pediatric patients with autism spectrum disorder Abstract Abstract AST-001, a novel syrup formulation of L-serine, was developed for the treatment of autism spectrum disorders (ASD) in pediatric patients. This study aimed to es...
PMC7543161
core_pubmed_pmc
Statin-Induced Rhabdomyolysis Due to Pharmacokinetic Changes From Biliary Obstruction in a Patient With Metastatic Prostate Cancer
Statin-Induced Rhabdomyolysis Due to Pharmacokinetic Changes From Biliary Obstruction in a Patient With Metastatic Prostate Cancer Abstract Abstract Statins work synergistically with androgen receptor blockers and androgen biosynthesis inhibitors, improving survival in patients with metastatic castration resistant pros...
PMC11617995
core_pubmed_pmc
Biopharmaceutical and pharmacokinetic attributes to drive nanoformulations of small molecule tyrosine kinase inhibitors
Biopharmaceutical and pharmacokinetic attributes to drive nanoformulations of small molecule tyrosine kinase inhibitors Abstract Buoyed by the discovery of small-molecule tyrosine kinase inhibitors (smTKIs), significant impact has been made in cancer chemotherapeutics. However, some of these agents still encounter off-...
PMC11203737
core_pubmed_pmc
Impact of CYP3A5 Polymorphisms on Pediatric Asthma Outcomes
Impact of CYP3A5 Polymorphisms on Pediatric Asthma Outcomes Abstract Abstract Genetic variation among inhaled corticosteroid (ICS)-metabolizing enzymes may affect asthma control, but evidence is limited. This study tested the hypothesis that single-nucleotide polymorphisms (SNPs) in Cytochrome P450 3A5 (CYP3A5) would a...
PMC10515382
core_pubmed_pmc
Aminochalcones Attenuate Neuronal Cell Death under Oxidative Damage via Sirtuin 1 Activity
Aminochalcones Attenuate Neuronal Cell Death under Oxidative Damage via Sirtuin 1 Activity Abstract Abstract Encouraged by the lack of effective treatments and the dramatic growth in the global prevalence of neurodegenerative diseases along with various pharmacological properties of chalcone pharmacophores, this study ...
PMC9010277
core_pubmed_pmc
Single‐dose of LC51‐0255, a selective S1P 1 receptor modulator, showed dose‐dependent and reversible reduction of absolute lymphocyte count in humans
Single‐dose of LC51‐0255, a selective S1P 1 receptor modulator, showed dose‐dependent and reversible reduction of absolute lymphocyte count in humans Abstract Abstract Reducing the peripheral absolute lymphocyte count (ALC) is a promising therapeutic approach in treating autoimmune diseases. LC51‐0255 is a sphingosine‐...
PMC10977428
core_pubmed_pmc
A Phase I, Randomized, SAD, MAD, and PK Study of Risvodetinib in Older Adults and Parkinson’s Disease
A Phase I, Randomized, SAD, MAD, and PK Study of Risvodetinib in Older Adults and Parkinson’s Disease Abstract Abstract Background: Pre-clinical studies suggest that c-Abl activation may play an important role in the etiology of Parkinson’s disease, making c-Abl an important target to evaluate for potential disease-mod...
PMC5942357
core_pubmed_pmc
Safety, tolerability and pharmacokinetics of GSK3008348, a novel integrin αvβ6 inhibitor, in healthy participants
Safety, tolerability and pharmacokinetics of GSK3008348, a novel integrin αvβ6 inhibitor, in healthy participants Abstract Abstract Purpose Inhaled drug delivery is an attractive route by which to deliver drugs to lungs of patients with idiopathic pulmonary fibrosis (IPF). GSK3008348 is a potent and selective small mol...
PMC6132363
core_pubmed_pmc
Population Pharmacokinetic and Exposure–dizziness Modeling for a Metabotropic Glutamate Receptor Subtype 5 Negative Allosteric Modulator in Major Depressive Disorder Patients
Population Pharmacokinetic and Exposure–dizziness Modeling for a Metabotropic Glutamate Receptor Subtype 5 Negative Allosteric Modulator in Major Depressive Disorder Patients Abstract Abstract Dizziness, the most frequently observed adverse event in patients with major depressive disorder, was observed with basimgluran...
PMC11481079
core_pubmed_pmc
Cell‐Derived Vesicles for Nanoparticles' Coating: Biomimetic Approaches for Enhanced Blood Circulation and Cancer Therapy
Cell‐Derived Vesicles for Nanoparticles' Coating: Biomimetic Approaches for Enhanced Blood Circulation and Cancer Therapy Abstract Abstract Cancer nanomedicines are designed to encapsulate different therapeutic agents, prevent their premature release, and deliver them specifically to cancer cells, due to their ability ...
PMC12214881
core_pubmed_pmc
A Pharmacokinetic and Pharmacodynamic Model of an IL-12 Anchored-Drug Conjugate for the Treatment of Solid Tumors
A Pharmacokinetic and Pharmacodynamic Model of an IL-12 Anchored-Drug Conjugate for the Treatment of Solid Tumors Abstract Abstract IL-12 mediates innate and adaptive immune responses and has demonstrated therapeutic antitumor activity, but clinical development has been hindered by a narrow therapeutic window. We gener...
PMC3897005
core_pubmed_pmc
Evaluation of Phyllanthus emblica extract on cold pressor induced cardiovascular changes in healthy human subjects
Evaluation of Phyllanthus emblica extract on cold pressor induced cardiovascular changes in healthy human subjects Abstract Background: Acute and chronic stress is a risk factor for the development and progression of coronary artery disease. Increased arterial stiffness is an independent marker for cardiovascular disea...
PMC4529450
core_pubmed_pmc
Demonstration of the reproducibility of free-breathing diffusion-weighted MRI and dynamic contrast enhanced MRI in children with solid tumours: a pilot study
Demonstration of the reproducibility of free-breathing diffusion-weighted MRI and dynamic contrast enhanced MRI in children with solid tumours: a pilot study Abstract Objectives The objectives are to examine the reproducibility of functional MR imaging in children with solid tumours using quantitative parameters derive...
PMC7021845
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics and Safety of Belimumab in Chinese Patients with Systemic Lupus Erythematosus: A Phase I, Open-Label Study
Pharmacokinetics, Pharmacodynamics and Safety of Belimumab in Chinese Patients with Systemic Lupus Erythematosus: A Phase I, Open-Label Study Abstract Abstract Introduction The B cell survival factor B lymphocyte stimulator (BLyS) is elevated in patients with systemic lupus erythematosus (SLE) and associated with disea...
PMC4982891
core_pubmed_pmc
Benefit–Risk Assessment of Fish Oil in Preventing Cardiovascular Disease
Benefit–Risk Assessment of Fish Oil in Preventing Cardiovascular Disease Abstract Abstract Cardiovascular disease (CVD) is a preventable disease, which combines two general processes: chronic vascular inflammation and acute thrombosis. Both are amplified with positive feedback signals by n-6 eicosanoids derived from fo...
PMC7029744
core_pubmed_pmc
A Relative Bioavailability Study of Two Misoprostol Formulations Following a Single Oral or Sublingual Administration
A Relative Bioavailability Study of Two Misoprostol Formulations Following a Single Oral or Sublingual Administration Abstract Introduction Misoprostol (Cytotec) was primarily made for treating gastric ulcers. However today it is mostly used for abortion, treating postpartum hemorrhage, and for induction of labor. The ...
PMC8921477
core_pubmed_pmc
Combined Effects of Temperature and Salinity on the Pharmacokinetics of Florfenicol in Nile Tilapia ( Oreochromis niloticus ) Reared in Brackish Water
Combined Effects of Temperature and Salinity on the Pharmacokinetics of Florfenicol in Nile Tilapia ( Oreochromis niloticus ) Reared in Brackish Water Abstract Abstract Prudent antimicrobial use requires knowledge of pharmacokinetics (PK) in a specific fish species which in turn depends on water temperature and salinit...
PMC12571116
core_pubmed_pmc
Low-Dose Trimethoprim-Sulfamethoxazole Prophylaxis for Pneumocystis jirovecii Pneumonia in a Critically Ill Patient with HIV/TB Coinfection: Pharmacokinetics and Clinical Outcomes
Low-Dose Trimethoprim-Sulfamethoxazole Prophylaxis for Pneumocystis jirovecii Pneumonia in a Critically Ill Patient with HIV/TB Coinfection: Pharmacokinetics and Clinical Outcomes Abstract Abstract Background Pneumocystis jirovecii pneumonia (PJP) is a life-threatening opportunistic infection disease in immunocompromis...
PMC6458983
core_pubmed_pmc
Gefitinib exposure and occurrence of interstitial lung disease in Japanese patients with non-small-cell lung cancer
Gefitinib exposure and occurrence of interstitial lung disease in Japanese patients with non-small-cell lung cancer Abstract Abstract Purpose A prospective, multicenter, large-scale cohort with a nested case–control study ( NCT00252759 ) was conducted to identify and quantify risk factors for interstitial lung disease ...
PMC6753944
core_pubmed_pmc
Variability in the Analgesic Response to Ibuprofen Is Associated With Cyclooxygenase Activation in Inflammatory Pain
Variability in the Analgesic Response to Ibuprofen Is Associated With Cyclooxygenase Activation in Inflammatory Pain Abstract The mechanisms underlying interindividual variability in analgesic efficacy of nonsteroidal anti‐inflammatory drugs (NSAIDs) are not well understood. Therefore, we performed pain phenotyping, fu...
PMC8899577
core_pubmed_pmc
Targeting the anti-apoptotic Bcl-2 family proteins: machine learning virtual screening and biological evaluation of new small molecules
Targeting the anti-apoptotic Bcl-2 family proteins: machine learning virtual screening and biological evaluation of new small molecules Abstract Abstract Bcl-2 family anti-apoptotic proteins are overexpressed in several hematological and solid tumors, and contribute to tumor formation, progression, and resistance to th...
PMC12443659
core_pubmed_pmc
Targeting Acute Myeloid Leukemia with 1,2,4-triazolo[4,3-b]pyridazine derivatives: a molecular docking, dynamics, and ADMET approach
Targeting Acute Myeloid Leukemia with 1,2,4-triazolo[4,3-b]pyridazine derivatives: a molecular docking, dynamics, and ADMET approach Abstract Abstract Acute Myeloid Leukemia (AML) remains a critical therapeutic challenge, warranting the development of novel inhibitors targeting essential survival proteins such as Myelo...
PMC11494844
core_pubmed_pmc
A fully automatic tool for development of population pharmacokinetic models
A fully automatic tool for development of population pharmacokinetic models Abstract Abstract Population pharmacokinetic (PK) models are widely used to inform drug development by pharmaceutical companies and facilitate drug evaluation by regulatory agencies. Developing a population PK model is a multi‐step, challenging...
PMC12587624
core_pubmed_pmc
Molecular and pharmacodynamic insights into β-lactam therapy for high-inoculum Enterobacter cloacae complex infections
Molecular and pharmacodynamic insights into β-lactam therapy for high-inoculum Enterobacter cloacae complex infections Abstract ABSTRACT High-inoculum Enterobacter cloacae complex (ECC) infections challenge β-lactam therapy due to β-lactamase-mediated resistance and the inoculum effect, where high bacterial densities a...
PMC11530130
core_pubmed_pmc
Peripherally restricted PICK1 inhibitor mPD5 ameliorates pain behaviors in murine inflammatory and neuropathic pain models
Peripherally restricted PICK1 inhibitor mPD5 ameliorates pain behaviors in murine inflammatory and neuropathic pain models Abstract Abstract Chronic pain is a complex, debilitating, and escalating health problem worldwide, impacting 1 in 5 adults. Current treatment is compromised by dose-limiting side effects, includin...
PMC5487756
core_pubmed_pmc
Evaluation of the Safety, Tolerability, and Pharmacokinetics of Gammaplex ® 10% Versus Gammaplex ® 5% in Subjects with Primary Immunodeficiency
Evaluation of the Safety, Tolerability, and Pharmacokinetics of Gammaplex ® 10% Versus Gammaplex ® 5% in Subjects with Primary Immunodeficiency Abstract Purpose This phase 3, multicenter, open-label, randomized, two-period, crossover bioequivalence trial evaluated the safety, tolerability, and pharmacokinetics of intra...
PMC7760391
core_pubmed_pmc
Quantification of Drugs in Distinctly Separated Ocular Substructures of Albino and Pigmented Rats
Quantification of Drugs in Distinctly Separated Ocular Substructures of Albino and Pigmented Rats Abstract The rat is a commonly used species in ocular drug research. Detailed methods of separating rat ocular tissues have not been described in literature. To understand the intraocular drug distribution, we developed a ...
PMC4465017
core_pubmed_pmc
Use of low-dose oral theophylline as an adjunct to inhaled corticosteroids in preventing exacerbations of chronic obstructive pulmonary disease: study protocol for a randomised controlled trial
Use of low-dose oral theophylline as an adjunct to inhaled corticosteroids in preventing exacerbations of chronic obstructive pulmonary disease: study protocol for a randomised controlled trial Abstract Abstract Background Chronic obstructive pulmonary disease (COPD) is associated with high morbidity, mortality, and he...
PMC6017867
core_pubmed_pmc
Chemoresistance to Cancer Treatment: Benzo-α-Pyrene as Friend or Foe?
Chemoresistance to Cancer Treatment: Benzo-α-Pyrene as Friend or Foe? Abstract Abstract Background: Environmental pollution such as exposure to pro-carcinogens including benzo-α-pyrene is becoming a major problem globally. Moreover, the effects of benzo-α-pyrene (BaP) on drug pharmacokinetics, pharmacodynamics, and dru...
PMC7909566
core_pubmed_pmc
Improving Breviscapine Oral Bioavailability by Preparing Nanosuspensions, Liposomes and Phospholipid Complexes
Improving Breviscapine Oral Bioavailability by Preparing Nanosuspensions, Liposomes and Phospholipid Complexes Abstract Abstract Breviscapine (BVP), a flavonoid compound, is widely used in the treatment of cardiovascular and cerebrovascular diseases; however, the low oral bioavailability and short half-life properties ...
PMC12162920
core_pubmed_pmc
Lipid-lowering statins and polyphenol-based supplementation: a scoping review on drug-food interaction potential
Lipid-lowering statins and polyphenol-based supplementation: a scoping review on drug-food interaction potential Abstract Abstract Background Lifestyle modifications, particularly the adoption of healthy dietary patterns such as the Mediterranean Diet (MedDiet), are foundational in any treatment plan, including for pat...