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PMC6058676 | core_pubmed_pmc | Developments in drug delivery of bioactive alkaloids derived from traditional Chinese medicine | Developments in drug delivery of bioactive alkaloids derived from traditional Chinese medicine Abstract Abstract The bioactive alkaloids (e.g. vincristine, hydroxycamptothecin, ligustrazine, and so on) from traditional Chinese medicine (TCM) have exerted potent efficacies (e.g. anti-tumor, anti-inflammation, immunosupp... |
PMC10022732 | core_pubmed_pmc | Practice of CYP450 genotyping and phenotyping in children in a real-life setting | Practice of CYP450 genotyping and phenotyping in children in a real-life setting Abstract Pharmacokinetics varies widely between children. Many factors play an important role in this variability, such as ontogeny, pharmacogenetics, gender, comorbidities, and drug-drug interactions. Significant work has already been don... |
PMC10134273 | core_pubmed_pmc | Phase 1 dose escalation study of FGFR4 inhibitor in combination with pembrolizumab in advanced solid tumors patients | Phase 1 dose escalation study of FGFR4 inhibitor in combination with pembrolizumab in advanced solid tumors patients Abstract Abstract Objective Inhibition of fibroblast growth factor (FGF) 19‐FGF Receptor 4 (FGFR4) signaling demonstrates potent anticancer activity. EVER4010001 is a highly selective FGFR4 inhibitor and... |
PMC12105008 | core_pubmed_pmc | Species-Dependent Metabolism of a Covalent nsP2 Protease Inhibitor with In Vivo Antialphaviral Activity | Species-Dependent Metabolism of a Covalent nsP2 Protease Inhibitor with In Vivo Antialphaviral Activity Abstract Abstract RA-0002034 ( 1 ) is a potent covalent inhibitor targeting the nsP2 cysteine protease. The species-dependent pharmacokinetics and metabolism of 1 were investigated to evaluate its therapeutic potenti... |
PMC9672991 | core_pubmed_pmc | Quantification of clofarabine in urine and plasma by LC-MS/MS: suitable for PK study and TDM in pediatric patients with relapsed or refractory ALL | Quantification of clofarabine in urine and plasma by LC-MS/MS: suitable for PK study and TDM in pediatric patients with relapsed or refractory ALL Abstract Clofarabine is approved for the treatment of relapsed or refractory acute lymphoblastic leukemia (ALL) in pediatric patients aged 1 to 21 years. Its pharmacokinetic... |
PMC11609057 | core_pubmed_pmc | Effect of Itraconazole, a CYP3A4 Inhibitor, and Rifampin, a CYP3A4 Inducer, on the Pharmacokinetics of Vatiquinone | Effect of Itraconazole, a CYP3A4 Inhibitor, and Rifampin, a CYP3A4 Inducer, on the Pharmacokinetics of Vatiquinone Abstract Abstract Vatiquinone is a small molecule inhibitor of 15‐lipoxygenase in development for patients with Friedreich's ataxia. The objective of this analysis was to determine the effect of a cytochro... |
PMC2837574 | core_pubmed_pmc | Methotrexate area under the curve is an important outcome predictor in patients with primary CNS lymphoma: A pharmacokinetic–pharmacodynamic analysis from the IELSG no. 20 trial | Methotrexate area under the curve is an important outcome predictor in patients with primary CNS lymphoma: A pharmacokinetic–pharmacodynamic analysis from the IELSG no. 20 trial Abstract Background: This analysis was initiated to define the predictive value of the area under the curve of high-dose methotrexate (AUC HD-... |
PMC9401497 | core_pubmed_pmc | Pharmacodynamic Biomarkers Predictive of Survival Benefit with Lenvatinib in Unresectable Hepatocellular Carcinoma: From the Phase III REFLECT Study | Pharmacodynamic Biomarkers Predictive of Survival Benefit with Lenvatinib in Unresectable Hepatocellular Carcinoma: From the Phase III REFLECT Study Abstract Abstract Purpose: In REFLECT, lenvatinib demonstrated an effect on overall survival (OS) by confirmation of noninferiority to sorafenib in unresectable hepatocell... |
PMC11074276 | core_pubmed_pmc | Targeted delivery of the probiotic Saccharomyces boulardii to the extracellular matrix enhances gut residence time and recovery in murine colitis | Targeted delivery of the probiotic Saccharomyces boulardii to the extracellular matrix enhances gut residence time and recovery in murine colitis Abstract Probiotic and engineered microbe-based therapeutics are an emerging class of pharmaceutical agents. They represent a promising strategy for treating various chronic ... |
PMC9361274 | core_pubmed_pmc | Placebo: a brief updated review | Placebo: a brief updated review Abstract Our aims were to provide updated information on placebo/nocebo effect and the potential use of placebo in clinical practice. This article can only provide a rough overview on the placebo and nocebo effect and is intended to serve as a starting point for the reader to go deeper i... |
PMC10135070 | core_pubmed_pmc | Physiologically-Based Pharmacokinetic Modelling to Predict the Pharmacokinetics and Pharmacodynamics of Linezolid in Adults and Children with Tuberculous Meningitis | Physiologically-Based Pharmacokinetic Modelling to Predict the Pharmacokinetics and Pharmacodynamics of Linezolid in Adults and Children with Tuberculous Meningitis Abstract Abstract Linezolid is used off-label for treatment of central nervous system infections. However, its pharmacokinetics and target attainment in cr... |
PMC4133599 | core_pubmed_pmc | Effect of gastrointestinal resection on sunitinib exposure in patients with GIST | Effect of gastrointestinal resection on sunitinib exposure in patients with GIST Abstract Background GIST patients often undergo GI-surgery. Previous studies have shown that imatinib and nilotinib exposures were decreased in GIST patients with prior major gastrectomy. We investigated whether major gastrectomy influence... |
PMC10904617 | core_pubmed_pmc | Predicting pharmacodynamic effects through early drug discovery with artificial intelligence-physiologically based pharmacokinetic (AI-PBPK) modelling | Predicting pharmacodynamic effects through early drug discovery with artificial intelligence-physiologically based pharmacokinetic (AI-PBPK) modelling Abstract A mechanism-based pharmacokinetic/pharmacodynamic (PK/PD) model links the concentration-time profile of a drug with its therapeutic effects based on the underly... |
PMC11736911 | core_pubmed_pmc | Optimal dose of mivacurium for laser-assisted laryngeal microsurgery: a pharmacokinetic study using closed-loop target-controlled infusion | Optimal dose of mivacurium for laser-assisted laryngeal microsurgery: a pharmacokinetic study using closed-loop target-controlled infusion Abstract Abstract Purpose Mivacurium is a short-acting, non-depolarising neuromuscular blocking agent that provides adequate vocal cord myorelaxation during transoral laser microsur... |
PMC9549737 | core_pubmed_pmc | In vitro activity of lactone ketolide nafithromycin (WCK 4873) against Streptococcus pneumoniae isolates enriched with macrolide-resistance phenotype collected from mainland China | In vitro activity of lactone ketolide nafithromycin (WCK 4873) against Streptococcus pneumoniae isolates enriched with macrolide-resistance phenotype collected from mainland China Abstract Abstract Background Widespread MDR Streptococcus pneumoniae in China translates clinically into a substantial pneumococcal disease ... |
PMC11645972 | core_pubmed_pmc | Use of dexmedetomidine during mechanical ventilation in extremely preterm and extremely low birth weight neonates receiving morphine: A single‐center retrospective study | Use of dexmedetomidine during mechanical ventilation in extremely preterm and extremely low birth weight neonates receiving morphine: A single‐center retrospective study Abstract Abstract Analgesia and sedation are often provided during mechanical ventilation in extremely preterm neonates. Opioids and benzodiazepines a... |
PMC11026178 | core_pubmed_pmc | Amiodarone and Dronedarone Causes Liver Injury with Distinctly Different Clinical Presentations | Amiodarone and Dronedarone Causes Liver Injury with Distinctly Different Clinical Presentations Abstract Abstract Objective To describe hepatotoxicity due to amiodarone and dronedarone from the DILIN and the US FDA’s surveillance database. Methods Hepatotoxicity due to amiodarone and dronedarone enrolled in the U.S. Dr... |
PMC6493276 | core_pubmed_pmc | Quantification of 1D, a novel derivative of curcumin with potential antitumor activity, in rat plasma by liquid chromatography-tandem mass spectrometry: application to a pharmacokinetic study in rats | Quantification of 1D, a novel derivative of curcumin with potential antitumor activity, in rat plasma by liquid chromatography-tandem mass spectrometry: application to a pharmacokinetic study in rats Abstract Abstract Context: 1 D is a novel derivative of curcumin and shows very promising antitumor activities in variou... |
PMC10695100 | core_pubmed_pmc | Phase Ib Trial of Phenformin in Patients with V600-mutated Melanoma Receiving Dabrafenib and Trametinib | Phase Ib Trial of Phenformin in Patients with V600-mutated Melanoma Receiving Dabrafenib and Trametinib Abstract Abstract Purpose: Preclinical studies show that activation of AMP kinase by phenformin can augment the cytotoxic effect and RAF inhibitors in BRAF V600-mutated melanoma. We conducted a phase Ib dose-escalati... |
PMC8821167 | core_pubmed_pmc | Dopamine Receptor Partial Agonists: Do They Differ in Their Clinical Efficacy? | Dopamine Receptor Partial Agonists: Do They Differ in Their Clinical Efficacy? Abstract Dopamine receptor partial agonists (DRPAs; aripiprazole, brexpiprazole, and cariprazine) constitute a novel class of antipsychotics. Although they share a similar mechanism of action, DRPAs differ in their pharmacodynamics, pharmaco... |
PMC7838596 | core_pubmed_pmc | Determination and Pharmacokinetic Profiles of Four Active Components From Scrophularia ningpoensis Hemsl. in Rats | Determination and Pharmacokinetic Profiles of Four Active Components From Scrophularia ningpoensis Hemsl. in Rats Abstract Abstract Acteoside, angoroside C, harpagoside, and cinnamic acid, which are the main bioactive ingredients of Scrophularia ningpoensis Hemsl. , have wide clinical use with various biological effect... |
PMC3224552 | core_pubmed_pmc | Current european regulatory perspectives on insulin analogues | Current european regulatory perspectives on insulin analogues Abstract Insulin analogues are increasingly considered as an alternative to human insulin in the therapy of diabetes mellitus. Insulin analogues (IAs) are chemically different from human insulin and may have different pharmacokinetic or pharmacodynamic prope... |
PMC9460261 | core_pubmed_pmc | Need for a Standardized Translational Drug Development Platform: Lessons Learned from the Repurposing of Drugs for COVID-19 | Need for a Standardized Translational Drug Development Platform: Lessons Learned from the Repurposing of Drugs for COVID-19 Abstract In the absence of drugs to treat or prevent COVID-19, drug repurposing can be a valuable strategy. Despite a substantial number of clinical trials, drug repurposing did not deliver on its... |
PMC6267815 | core_pubmed_pmc | In vivo pharmacokinetic/Pharmacodynamic modeling of Enrofloxacin against Escherichia coli in broiler chickens | In vivo pharmacokinetic/Pharmacodynamic modeling of Enrofloxacin against Escherichia coli in broiler chickens Abstract Abstract Background Systemic Escherichia coli infections cause early mortality of commercial broiler chickens. Although enrofloxacin has long been used in poultry, the in vivo pharmacokinetic/pharmacod... |
PMC5452173 | core_pubmed_pmc | Distribution of Constituents and Metabolites of Maritime Pine Bark Extract (Pycnogenol ® ) into Serum, Blood Cells, and Synovial Fluid of Patients with Severe Osteoarthritis: A Randomized Controlled Trial | Distribution of Constituents and Metabolites of Maritime Pine Bark Extract (Pycnogenol ® ) into Serum, Blood Cells, and Synovial Fluid of Patients with Severe Osteoarthritis: A Randomized Controlled Trial Abstract Abstract The present randomized controlled study aimed to investigate the in vivo distribution of constitu... |
PMC12008688 | core_pubmed_pmc | Phase 1 study of quercetin, a natural antioxidant for children and young adults with Fanconi anemia | Phase 1 study of quercetin, a natural antioxidant for children and young adults with Fanconi anemia Abstract Key Points • In this dose-finding phase 1 study, quercetin, a natural antioxidant was found to be safe and well tolerated in patients with FA. • ROS levels decreased in the blood, and hematological responses wer... |
PMC10525625 | core_pubmed_pmc | Dosing Optimization of Posaconazole in Lung-Transplant Recipients Based on Population Pharmacokinetic Model | Dosing Optimization of Posaconazole in Lung-Transplant Recipients Based on Population Pharmacokinetic Model Abstract Abstract Although posaconazole tablets show relatively low variability in pharmacokinetics (PK), the proportion of patients achieving the PK/PD target at the approved uniform dose for both prophylaxis an... |
PMC7236770 | core_pubmed_pmc | Precision Dosing of Doxapram in Preterm Infants Using Continuous Pharmacodynamic Data and Model-Based Pharmacokinetics: An Illustrative Case Series | Precision Dosing of Doxapram in Preterm Infants Using Continuous Pharmacodynamic Data and Model-Based Pharmacokinetics: An Illustrative Case Series Abstract Abstract Introduction Current drug dosing in preterm infants is standardized, mostly based on bodyweight. Still, covariates such as gestational and postnatal age m... |
PMC12787225 | core_pubmed_pmc | Geraniin Mitigates Neuropathic Pain Through Antioxidant, Anti-Inflammatory, and Nitric Oxide Modulation in a Rat Model of Chronic Constriction Injury | Geraniin Mitigates Neuropathic Pain Through Antioxidant, Anti-Inflammatory, and Nitric Oxide Modulation in a Rat Model of Chronic Constriction Injury Abstract Abstract Neuropathic pain (NPP) remains therapeutically challenging, with oxidative/nitrosative stress and neuroinflammation—amplified by nitric oxide (NO)—as ke... |
PMC10824522 | core_pubmed_pmc | Pharmacokinetic Variability of Oral Cannabidiol and Its Major Metabolites after Short-Term High-Dose Exposure in Healthy Subjects | Pharmacokinetic Variability of Oral Cannabidiol and Its Major Metabolites after Short-Term High-Dose Exposure in Healthy Subjects Abstract Abstract Introduction Cannabidiol (CBD) is a widely utilized nonpsychoactive cannabinoid available as a prescriptive drug treatment and over-the-counter supplement. In humans, CBD i... |
PMC9087830 | core_pubmed_pmc | Anti-infective Medicines Use in Children and Neonates With Pre-existing Kidney Dysfunction: A Systematic Review | Anti-infective Medicines Use in Children and Neonates With Pre-existing Kidney Dysfunction: A Systematic Review Abstract Abstract Background Dosing recommendations for anti-infective medicines in children with pre-existing kidney dysfunction are derived from adult pharmacokinetics studies and adjusted to kidney functio... |
PMC6056758 | core_pubmed_pmc | Precision Medicine with Imprecise Therapy: Computational Modeling for Chemotherapy in Breast Cancer 1 | Precision Medicine with Imprecise Therapy: Computational Modeling for Chemotherapy in Breast Cancer 1 Abstract Medical oncology is in need of a mathematical modeling toolkit that can leverage clinically-available measurements to optimize treatment selection and schedules for patients. Just as the therapeutic choice has... |
PMC3017105 | core_pubmed_pmc | A Novel Approach to Pharmacodynamic Assessment of Antimicrobial Agents: New Insights to Dosing Regimen Design | A Novel Approach to Pharmacodynamic Assessment of Antimicrobial Agents: New Insights to Dosing Regimen Design Abstract Abstract Pharmacodynamic modeling has been increasingly used as a decision support tool to guide dosing regimen selection, both in the drug development and clinical settings. Killing by antimicrobial a... |
PMC12631143 | core_pubmed_pmc | Low-dose methotrexate adverse reaction risk in renal impairment: pharmacovigilance and physiological pharmacokinetic model assessment | Low-dose methotrexate adverse reaction risk in renal impairment: pharmacovigilance and physiological pharmacokinetic model assessment Abstract Abstract Objective Low-dose methotrexate (LD-MTX), a treatment regimen involving weekly doses ≤20 mg, is widely used in rheumatoid arthritis. Methotrexate (MTX) is primarily exc... |
PMC11982668 | core_pubmed_pmc | Postmortem distribution of MDPHP in a fatal intoxication case | Postmortem distribution of MDPHP in a fatal intoxication case Abstract Abstract The synthetic cathinone (SC) 3,4-methylenedioxy-α-pyrrolidinohexanophenone (MDPHP) is structurally correlated to the 3,4-methylenedioxypyrovalerone (MDPV). In recent years, the number of intoxication cases has increased even if little is kn... |
PMC12104081 | core_pubmed_pmc | Osmotic laxatives do not alter dabigatran plasma concentration in healthy volunteers – a randomized, controlled, cross-over trial | Osmotic laxatives do not alter dabigatran plasma concentration in healthy volunteers – a randomized, controlled, cross-over trial Abstract Background Laxatives are among the most commonly used pharmacological agents worldwide. Available data indicate a significant potential for clinically relevant drug-drug interaction... |
PMC3978216 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Gliclazide from Immediate and Modified Release Formulation Tablets in Rats | Pharmacokinetics and Pharmacodynamics of Gliclazide from Immediate and Modified Release Formulation Tablets in Rats Abstract Abstract The objective of the study was to compare pharmacokinetic and pharmacodynamic parameters of gliclazide after administration of immediate (IR) and modified release (MR) tablets. The exper... |
PMC12018915 | core_pubmed_pmc | Sorption and release of small molecules in PDMS and COC for Organs on chip | Sorption and release of small molecules in PDMS and COC for Organs on chip Abstract Accurate risk assessment in drug development is crucial, as conventional in vitro and in vivo models often fail to predict human-specific responses. Organs on chips offer a promising alternative, but widespread use of polydimethylsiloxa... |
PMC11154707 | core_pubmed_pmc | Polymer-based antibody mimetics (iBodies) target human PD-L1 and function as a potent immune checkpoint blocker | Polymer-based antibody mimetics (iBodies) target human PD-L1 and function as a potent immune checkpoint blocker Abstract Abstract Immune checkpoint blockade (ICB) using monoclonal antibodies against programmed cell death protein 1 (PD-1) or programmed death-ligand 1 (PD-L1) is the treatment of choice for cancer immunot... |
PMC9637074 | core_pubmed_pmc | Characterization of exposure–response relationships of ipatasertib in patients with metastatic castration-resistant prostate cancer in the IPATential150 study | Characterization of exposure–response relationships of ipatasertib in patients with metastatic castration-resistant prostate cancer in the IPATential150 study Abstract Purpose The exposure–response relationships for efficacy and safety of ipatasertib, a selective AKT kinase inhibitor, were characterized using data coll... |
PMC3763640 | core_pubmed_pmc | Effect of Co-Administration of Rivaroxaban and Clopidogrel on Bleeding Time, Pharmacodynamics and Pharmacokinetics: A Phase I Study | Effect of Co-Administration of Rivaroxaban and Clopidogrel on Bleeding Time, Pharmacodynamics and Pharmacokinetics: A Phase I Study Abstract Dual antiplatelet therapy with acetylsalicylic acid and a thienopyridine, such as clopidogrel, is effective for the secondary prevention of cardiovascular events in patients with ... |
PMC9559057 | core_pubmed_pmc | Safety, pharmacokinetics and pharmacodynamics of a novel γ-aminobutyric acid (GABA) receptor potentiator, HSK3486, in Chinese patients with hepatic impairment | Safety, pharmacokinetics and pharmacodynamics of a novel γ-aminobutyric acid (GABA) receptor potentiator, HSK3486, in Chinese patients with hepatic impairment Abstract Abstract Background The primary objective of this study was to investigate if hepatic impairment alters the safety, pharma c okinetics, and pharmacodyna... |
PMC6823368 | core_pubmed_pmc | Lack of effect of Imrecoxib, an innovative and moderate COX-2 inhibitor, on pharmacokinetics and pharmacodynamics of warfarin in healthy volunteers | Lack of effect of Imrecoxib, an innovative and moderate COX-2 inhibitor, on pharmacokinetics and pharmacodynamics of warfarin in healthy volunteers Abstract Imrecoxib is a registered treatment for osteoarthritis pain symptoms in China. This study aims to assess the effect of imrecoxib on the pharmacodynamics and pharma... |
PMC5913258 | core_pubmed_pmc | Mousetap, a Novel Technique to Collect Uncontaminated Vitreous or Aqueous and Expand Usefulness of Mouse Models | Mousetap, a Novel Technique to Collect Uncontaminated Vitreous or Aqueous and Expand Usefulness of Mouse Models Abstract Abstract Vitreous or aqueous humour taps are widely used in patients or large animals with retinal diseases to monitor disease biomarkers, search for novel biomarkers, assess the integrity of the blo... |
PMC9931184 | core_pubmed_pmc | Association of Higher Ocrelizumab Exposure With Reduced Disability Progression in Multiple Sclerosis | Association of Higher Ocrelizumab Exposure With Reduced Disability Progression in Multiple Sclerosis Abstract Abstract Background and Objectives Ocrelizumab improved clinical and MRI measures of disease activity and progression in three phase 3 multiple sclerosis (MS) studies. Post hoc analyses demonstrated a correlati... |
PMC11934034 | core_pubmed_pmc | Cortistatin and plakinamine steroidal alkaloids from the marine sponges of the genus Corticium : insights into their chemistry, pharmacology, pharmacokinetics and structure activity relationships (SARs) † | Cortistatin and plakinamine steroidal alkaloids from the marine sponges of the genus Corticium : insights into their chemistry, pharmacology, pharmacokinetics and structure activity relationships (SARs) † Abstract Cortistatins and plakinamines represent a unique class of marine-derived steroidal alkaloids, renowned for... |
PMC6310869 | core_pubmed_pmc | A Novel PBPK Modeling Approach to Assess Cytochrome P450 Mediated Drug‐Drug Interaction Potential of the Cytotoxic Prodrug Evofosfamide | A Novel PBPK Modeling Approach to Assess Cytochrome P450 Mediated Drug‐Drug Interaction Potential of the Cytotoxic Prodrug Evofosfamide Abstract Evofosfamide is a cytotoxic small‐molecule prodrug preferentially activated under hypoxic conditions. The cytotoxicity of evofosfamide impacted the generation of in vitro drug... |
PMC11110461 | core_pubmed_pmc | Italian Association of Hospital Cardiologists Position Paper ‘Gender discrepancy: time to implement gender-based clinical management’ | Italian Association of Hospital Cardiologists Position Paper ‘Gender discrepancy: time to implement gender-based clinical management’ Abstract Abstract It has been well assessed that women have been widely under-represented in cardiovascular clinical trials. Moreover, a significant discrepancy in pharmacological and in... |
PMC5008412 | core_pubmed_pmc | A phase I study of indoximod in patients with advanced malignancies | A phase I study of indoximod in patients with advanced malignancies Abstract Purpose Indoximod is an oral inhibitor of the indoleamine 2,3-dioxygenase pathway, which causes tumor-mediated immunosuppression. Primary endpoints were maximum tolerated dose (MTD) and toxicity for indoximod in patients with advanced solid tu... |
PMC5818879 | core_pubmed_pmc | Poly(lactic- co -glycolic acid)-loaded nanoparticles of betulinic acid for improved treatment of hepatic cancer: characterization, in vitro and in vivo evaluations | Poly(lactic- co -glycolic acid)-loaded nanoparticles of betulinic acid for improved treatment of hepatic cancer: characterization, in vitro and in vivo evaluations Abstract Abstract Purpose The application of betulinic acid (B), a potent antineoplastic agent, is limited due to poor bioavailability, short plasma half-li... |
PMC5514613 | core_pubmed_pmc | The 10-D assessment and evidence-based medicine tool for authors and peer reviewers in clinical pharmacology | The 10-D assessment and evidence-based medicine tool for authors and peer reviewers in clinical pharmacology Abstract Background: Peer reviewers and authors of clinical pharmacology manuscripts need to meet the standards for Evidence-Based Medicine (EBM) and Good Publication Practices (GPP), and editors of clinical pha... |
PMC9328374 | core_pubmed_pmc | Impact of enantiomer‐specific changes in pharmacokinetics between infants and adults on the target concentration of racemic ketorolac: A pooled analysis | Impact of enantiomer‐specific changes in pharmacokinetics between infants and adults on the target concentration of racemic ketorolac: A pooled analysis Abstract Abstract Aims Ketorolac is a nonsteroidal anti‐inflammatory racemic drug with analgesic effects only attributed to its S‐enantiomer. The aim of this study is ... |
PMC5069726 | core_pubmed_pmc | A Randomized Phase 1 Dose Escalation Study to Evaluate Safety, Tolerability, and Pharmacokinetics of Trabodenoson in Healthy Adult Volunteers | A Randomized Phase 1 Dose Escalation Study to Evaluate Safety, Tolerability, and Pharmacokinetics of Trabodenoson in Healthy Adult Volunteers Abstract Abstract Purpose: To investigate the safety, tolerability, and pharmacokinetics of trabodenoson, a highly selective adenosine mimetic targeting the adenosine A 1 recepto... |
PMC4418000 | core_pubmed_pmc | Assessment of Physicochemical Properties of Rituximab Related to Its Immunomodulatory Activity | Assessment of Physicochemical Properties of Rituximab Related to Its Immunomodulatory Activity Abstract Abstract Rituximab is a chimeric monoclonal antibody employed for the treatment of CD20-positive B-cell non-Hodgkin's lymphoma, chronic lymphocytic leukemia, rheumatoid arthritis, granulomatosis with polyangiitis and... |
PMC12497951 | core_pubmed_pmc | Phase 1 Evaluation of VH4524184, a Third-Generation Integrase Strand Transfer Inhibitor With an Enhanced Resistance Profile | Phase 1 Evaluation of VH4524184, a Third-Generation Integrase Strand Transfer Inhibitor With an Enhanced Resistance Profile Abstract Abstract Background Integrase strand transfer inhibitors (INSTIs) have been fundamental to human immunodeficiency virus type 1 (HIV-1) treatment for over 15 years. VH4524184 (VH-184) is a... |
PMC4819841 | core_pubmed_pmc | Pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule | Pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule Abstract Abstract Objective To evaluate the bioavailability and safety of a novel vaginal capsule containing solubilized bioidentical 17β-estradiol for vulvar and vaginal atrophy and compare its pharmacokinetics with that of an ... |
PMC9419134 | core_pubmed_pmc | Safety, Tolerability and Pharmacokinetics of Icapamespib, a Selective Epichaperome Inhibitor, in Healthy Adults | Safety, Tolerability and Pharmacokinetics of Icapamespib, a Selective Epichaperome Inhibitor, in Healthy Adults Abstract Abstract Background Neurodegenerative diseases are devastating conditions that most commonly affect individuals 65 years and older. Currently there are no effective treatments or cures for neurodegen... |
PMC8784755 | core_pubmed_pmc | Precision Cardio-Oncology: Use of Mechanistic Pharmacokinetic and Pharmacodynamic Modeling to Predict Cardiotoxicities of Anti-Cancer Drugs | Precision Cardio-Oncology: Use of Mechanistic Pharmacokinetic and Pharmacodynamic Modeling to Predict Cardiotoxicities of Anti-Cancer Drugs Abstract Abstract The cardiotoxicity of anti-cancer drugs presents as a challenge to both clinicians and patients. Significant advances in cancer treatments have improved patient s... |
PMC9633720 | core_pubmed_pmc | Population pharmacokinetics of ethambutol in African children: a pooled analysis | Population pharmacokinetics of ethambutol in African children: a pooled analysis Abstract Abstract Objectives Ethambutol protects against the development of resistance to co-administered drugs in the intensive phase of first-line anti-TB treatment in children. It is especially relevant in settings with a high prevalenc... |
PMC4709704 | core_pubmed_pmc | Pharmacokinetic profile evaluation of di-μ-hydroxo-bis(quercetinatooxovanadium(IV)) complex | Pharmacokinetic profile evaluation of di-μ-hydroxo-bis(quercetinatooxovanadium(IV)) complex Abstract Abstract The present study was designed to evaluate the pharmacokinetic (PK) properties of di-μ-hydroxo-bis(quercetinatooxovanadium(IV) (HOBQOV) complex, with hypoglycemic and hypolipidemic properties, in rats after a s... |
PMC3858267 | core_pubmed_pmc | The Enhanced In Vivo Activity of the Combination of a MEK and a PI3K Inhibitor Correlates with [ 18 F]-FLT PET in Human Colorectal Cancer Xenograft Tumour-Bearing Mice | The Enhanced In Vivo Activity of the Combination of a MEK and a PI3K Inhibitor Correlates with [ 18 F]-FLT PET in Human Colorectal Cancer Xenograft Tumour-Bearing Mice Abstract Abstract Combined targeting of the MAPK and PI3K signalling pathways in cancer may be necessary for optimal therapeutic activity. To support cl... |
PMC6861867 | core_pubmed_pmc | Population pharmacokinetics of tacrolimus in pediatric patients with systemic-onset juvenile idiopathic arthritis: Initial dosage recommendations | Population pharmacokinetics of tacrolimus in pediatric patients with systemic-onset juvenile idiopathic arthritis: Initial dosage recommendations Abstract Abstract Pediatric patients with systemic-onset juvenile idiopathic arthritis (SOJIA) may be treated with tacrolimus. However, the therapeutic range for tacrolimus i... |
PMC12890627 | core_pubmed_pmc | Apigenin ameliorates postoperative inflammation and accelerates wound healing in a rat model of perianal abscess by targeting the JAK1/STAT3 pathway in macrophages | Apigenin ameliorates postoperative inflammation and accelerates wound healing in a rat model of perianal abscess by targeting the JAK1/STAT3 pathway in macrophages Abstract Abstract Background Excessive inflammation mediated by macrophages impedes wound healing following surgical drainage of perianal abscess, a common ... |
PMC6266420 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, and safety of bococizumab, a monoclonal antibody against proprotein convertase subtilisin/kexin type 9, in healthy subjects when administered in co‐mixture with recombinant human hyaluronidase: A phase 1 randomized trial | Pharmacokinetics, pharmacodynamics, and safety of bococizumab, a monoclonal antibody against proprotein convertase subtilisin/kexin type 9, in healthy subjects when administered in co‐mixture with recombinant human hyaluronidase: A phase 1 randomized trial Abstract Abstract Aim Prior to the discontinuation of bococizum... |
PMC10809820 | core_pubmed_pmc | The multiple uses of azelaic acid in dermatology: mechanism of action, preparations, and potential therapeutic applications | The multiple uses of azelaic acid in dermatology: mechanism of action, preparations, and potential therapeutic applications Abstract Azelaic acid (AZA) is a naturally occurring saturated dicarboxylic acid whose topical application has found multiple uses in dermatology. Its anti-inflammatory, antioxidant and antimicrob... |
PMC12104674 | core_pubmed_pmc | Evaluation of the pharmacokinetic interactions of montmorillonite powder or loperamide on pyrotinib in healthy volunteers | Evaluation of the pharmacokinetic interactions of montmorillonite powder or loperamide on pyrotinib in healthy volunteers Abstract Abstract Aims To investigate the potential pharmacokinetic interactions of montmorillonite powder or loperamide on pyrotinib. Methods This study was a single-center, open-label, single-dose... |
PMC3900379 | core_pubmed_pmc | Modeling Within-Host Effects of Drugs on Plasmodium falciparum Transmission and Prospects for Malaria Elimination | Modeling Within-Host Effects of Drugs on Plasmodium falciparum Transmission and Prospects for Malaria Elimination Abstract Abstract Achieving a theoretical foundation for malaria elimination will require a detailed understanding of the quantitative relationships between patient treatment-seeking behavior, treatment cov... |
PMC5598882 | core_pubmed_pmc | Ciprofloxacin Pharmacokinetics in Clinical Canine Patients | Ciprofloxacin Pharmacokinetics in Clinical Canine Patients Abstract Background Ciprofloxacin generic tablets approved for human use frequently are administered to dogs for treatment of bacterial infections because they are inexpensive and readily available. However, previous work indicated low and variable oral absorpt... |
PMC12044325 | core_pubmed_pmc | A Phase 1 Randomized Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single Escalating Oral Doses of Dordaviprone and the Effects of Food on the Bioavailability of Dordaviprone in Healthy Adult Subjects | A Phase 1 Randomized Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single Escalating Oral Doses of Dordaviprone and the Effects of Food on the Bioavailability of Dordaviprone in Healthy Adult Subjects Abstract Abstract Dordaviprone (ONC201) is a novel, small molecule imipridone with antitumor effe... |
PMC8550843 | core_pubmed_pmc | Formulation, Optimization, In Vitro and In Vivo Evaluation of Saxagliptin-Loaded Lipospheres for an Improved Pharmacokinetic Behavior | Formulation, Optimization, In Vitro and In Vivo Evaluation of Saxagliptin-Loaded Lipospheres for an Improved Pharmacokinetic Behavior Abstract The development and optimization of controlled release lipospheres (LS) from safe biocompatible behenic acid (BA) was performed for not only enhancing patient's compliance again... |
PMC12484417 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling to Predict Nicotine Pharmacokinetics of Nicotine Pouches Under Naturalistic Use Conditions | Physiologically Based Pharmacokinetic Modeling to Predict Nicotine Pharmacokinetics of Nicotine Pouches Under Naturalistic Use Conditions Abstract Abstract Adult users of traditional tobacco products like combustible cigarettes (CC) or moist smokeless tobacco (MST) products can reduce exposure to toxicants by switching... |
PMC4505830 | core_pubmed_pmc | Semiphysiologically Based Pharmacokinetic Model of Leflunomide Disposition in Rheumatoid Arthritis Patients | Semiphysiologically Based Pharmacokinetic Model of Leflunomide Disposition in Rheumatoid Arthritis Patients Abstract Abstract A semiphysiologically based pharmacokinetic (semi-PBPK) population model was used to evaluate the influence of enterohepatic recycling and protein binding, as well as the effect of genetic varia... |
PMC10136941 | core_pubmed_pmc | Perioperative Acetaminophen Dosing in Obese Children | Perioperative Acetaminophen Dosing in Obese Children Abstract Abstract Acetaminophen is a commonly used perioperative analgesic drug in children. The use of a preoperative loading dose achieves a target concentration of 10 mg/L associated with a target analgesic effect that is 2.6 pain units (visual analogue scale 1–10... |
PMC11594466 | core_pubmed_pmc | Factors Associated with the Practice of Assessing Drug–Drug Interactions Among Pharmacists in Saudi Arabia | Factors Associated with the Practice of Assessing Drug–Drug Interactions Among Pharmacists in Saudi Arabia Abstract Background: Drug–drug interactions (DDIs) occur when two or more drugs are administered concomitantly, changing the pharmacokinetics or pharmacodynamics of a drug’s characteristics. Despite the advances i... |
PMC9841522 | core_pubmed_pmc | The Identification of Potent, Selective, and Brain Penetrant PI5P4Kγ Inhibitors as In Vivo-Ready Tool Molecules | The Identification of Potent, Selective, and Brain Penetrant PI5P4Kγ Inhibitors as In Vivo-Ready Tool Molecules Abstract Abstract Owing to their central role in regulating cell signaling pathways, the phosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks) are attractive therapeutic targets in diseases such as cancer, neu... |
PMC9803160 | core_pubmed_pmc | Dual effects of NV-CoV-2 biomimetic polymer: An antiviral regimen against COVID-19 | Dual effects of NV-CoV-2 biomimetic polymer: An antiviral regimen against COVID-19 Abstract Remdesivir (RDV) is the only antiviral drug approved for COVID-19 therapy by the FDA. Another drug LAGEVRIO™ (molnupiravir) though has not been approved yet by FDA but has been authorized on December 23, 2021, for emergency use ... |
PMC10703341 | core_pubmed_pmc | Analgesia and sedation strategies in neonates undergoing whole-body therapeutic hypothermia: A scoping review | Analgesia and sedation strategies in neonates undergoing whole-body therapeutic hypothermia: A scoping review Abstract Abstract Background Therapeutic hypothermia (TH) is a widely practiced neuroprotective strategy for neonates with hypoxic-ischemic encephalopathy. Induced hypothermia is associated with shivering, cold... |
PMC9635907 | core_pubmed_pmc | Quantitation of mycophenolic acid and metabolites by UPLC-MS/MS in renal transplant patients | Quantitation of mycophenolic acid and metabolites by UPLC-MS/MS in renal transplant patients Abstract Mycophenolate mofetil (MMF) and enteric-coated mycophenolate sodium (EC-MPS), specific inhibitors of lymphocyte proliferation, are commonly used as adjuvant therapy with calcineurin inhibitor agents after kidney transp... |
PMC5340839 | core_pubmed_pmc | A Review of Insulin Degludec/Insulin Aspart: Pharmacokinetic and Pharmacodynamic Properties and Their Implications in Clinical Use | A Review of Insulin Degludec/Insulin Aspart: Pharmacokinetic and Pharmacodynamic Properties and Their Implications in Clinical Use Abstract Insulin degludec/insulin aspart (IDegAsp; 70 % IDeg and 30 % IAsp) is a soluble combination of two individual insulin analogues in one product, designed to provide mealtime glycaem... |
PMC12439276 | core_pubmed_pmc | Impact of Mechanistic Modeling and Simulation Methodologies on Product‐Specific Guidance Development for Non‐Orally Administered Drug Products | Impact of Mechanistic Modeling and Simulation Methodologies on Product‐Specific Guidance Development for Non‐Orally Administered Drug Products Abstract ABSTRACT The U.S. Food and Drug Administration (FDA) publishes product‐specific guidances (PSGs), with bioequivalence (BE) recommendations for prospective generics. Dev... |
PMC12339515 | core_pubmed_pmc | Sweroside: unveiling broad therapeutic potential—from mechanistic insights to clinical potential | Sweroside: unveiling broad therapeutic potential—from mechanistic insights to clinical potential Abstract Background Sweroside, a secoiridoid glycoside abundantly present in medicinal plants, has garnered significant attention due to its diverse bioactivities, including anti-inflammatory, antioxidant, hepatoprotective,... |
PMC9994762 | core_pubmed_pmc | Sloppiness: Fundamental study, new formalism and its application in model assessment | Sloppiness: Fundamental study, new formalism and its application in model assessment Abstract Abstract Computational modelling of biological processes poses multiple challenges in each stage of the modelling exercise. Some significant challenges include identifiability, precisely estimating parameters from limited data... |
PMC8411896 | core_pubmed_pmc | Increased bactericidal activity but dose-limiting intolerability at 50 mg·kg −1 rifampicin | Increased bactericidal activity but dose-limiting intolerability at 50 mg·kg −1 rifampicin Abstract Background Accumulating data indicate that higher rifampicin doses are more effective and shorten tuberculosis (TB) treatment duration. This study evaluated the safety, tolerability, pharmacokinetics, and 7- and 14-day e... |
PMC9652254 | core_pubmed_pmc | Clinical Pharmacokinetics and Pharmacodynamics of Rucaparib | Clinical Pharmacokinetics and Pharmacodynamics of Rucaparib Abstract Abstract Rucaparib is an oral small-molecule poly(ADP-ribose) polymerase inhibitor indicated for patients with recurrent ovarian cancer in the maintenance and treatment settings and for patients with metastatic castration-resistant prostate cancer ass... |
PMC6042703 | core_pubmed_pmc | In healthy volunteers, taking flucloxacillin with food does not compromise effective plasma concentrations in most circumstances | In healthy volunteers, taking flucloxacillin with food does not compromise effective plasma concentrations in most circumstances Abstract It is usually recommended that flucloxacillin is given on an empty stomach. The aim of this study was to compare total and free flucloxacillin concentrations after oral flucloxacilli... |
PMC8460034 | core_pubmed_pmc | A randomized phase I study comparing the pharmacokinetics of a bevacizumab (HD204) biosimilar to European Union- and United States of America-sourced bevacizumab | A randomized phase I study comparing the pharmacokinetics of a bevacizumab (HD204) biosimilar to European Union- and United States of America-sourced bevacizumab Abstract Abstract Purpose This first-in-human study was designed to evaluate the pharmacokinetic (PK) equivalence between HD204 and the European Union (EU)-so... |
PMC8183294 | core_pubmed_pmc | Prospective real-world study on the pharmacokinetics of pembrolizumab in patients with solid tumors | Prospective real-world study on the pharmacokinetics of pembrolizumab in patients with solid tumors Abstract Background Dosing schemes of pembrolizumab (anti-programmed cell death protein 1 monoclonal antibody) are solely based on pharmacokinetic (PK) modelling derived from phase I–III trials. The current study aimed t... |
PMC11488834 | core_pubmed_pmc | Rivaroxaban for Thromboembolism Prophylaxis in Patients with Nephrotic Syndrome: A Single-Arm, Prospective Study | Rivaroxaban for Thromboembolism Prophylaxis in Patients with Nephrotic Syndrome: A Single-Arm, Prospective Study Abstract Abstract Introduction Thromboembolism is a recognized complication of nephrotic syndrome (NS). Evidence supporting the use of rivaroxaban to prevent NS-related thrombosis is limited and controversia... |
PMC11441728 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of the Novel Tetrameric, High-Relaxivity, Macrocyclic Gadolinium-Based Contrast Agent Gadoquatrane in Healthy Adults | Pharmacokinetics, Safety, and Tolerability of the Novel Tetrameric, High-Relaxivity, Macrocyclic Gadolinium-Based Contrast Agent Gadoquatrane in Healthy Adults Abstract Abstract Objectives Gadolinium (Gd)–based contrast agents are well established in clinical routine and have been proven safe and effective. However, th... |
PMC9632963 | core_pubmed_pmc | Preclinical characterization and phase I clinical trial of CT053PTSA targets MET, AXL, and VEGFR2 in patients with advanced solid tumors | Preclinical characterization and phase I clinical trial of CT053PTSA targets MET, AXL, and VEGFR2 in patients with advanced solid tumors Abstract Background CT053PTSA is a novel tyrosine kinase inhibitor that targets MET, AXL, VEGFR2, FLT3 and MERTK. Here, we present preclinical data about CT053PTSA, and we conducted t... |
PMC4620023 | core_pubmed_pmc | Improved intraocular bioavailability of ganciclovir by mucoadhesive polymer based ocular microspheres: development and simulation process in Wistar rats | Improved intraocular bioavailability of ganciclovir by mucoadhesive polymer based ocular microspheres: development and simulation process in Wistar rats Abstract Abstract Background The poor ocular bioavailability of the conventional eye drops is due to lack of corneal permeability, nasolacrimal drainage and metabolic ... |
PMC12751358 | core_pubmed_pmc | Therapeutic Drug Monitoring-Guided Antifungal Therapy Under Tyrosine Kinase Inhibitor Treatment in an Advanced Osteosarcoma Patient with Invasive Pulmonary Aspergillosis | Therapeutic Drug Monitoring-Guided Antifungal Therapy Under Tyrosine Kinase Inhibitor Treatment in an Advanced Osteosarcoma Patient with Invasive Pulmonary Aspergillosis Abstract Abstract Antifungal therapy for invasive pulmonary aspergillosis (IPA) can be challenging in cancer patients due to interpatient variability ... |
PMC5129817 | core_pubmed_pmc | Genotypes of CYP2C8 and FGD4 and their association with peripheral neuropathy or early dose reduction in paclitaxel-treated breast cancer patients | Genotypes of CYP2C8 and FGD4 and their association with peripheral neuropathy or early dose reduction in paclitaxel-treated breast cancer patients Abstract Abstract Background: The purpose of this study was to evaluate single-nucleotide polymorphisms (SNPs) in genes encoding key metabolising enzymes or involved in phar... |
PMC4612322 | core_pubmed_pmc | Pharmacokinetics of eribulin mesylate in cancer patients with normal and impaired renal function | Pharmacokinetics of eribulin mesylate in cancer patients with normal and impaired renal function Abstract Purpose To evaluate the effect of renal impairment on eribulin mesylate pharmacokinetics following a single dose in adults with advanced solid tumors. Methods Patients were grouped by renal function: moderate impai... |
PMC7065716 | core_pubmed_pmc | Mitigation of Rheumatic Arthritis in a Rat Model via Transdermal Delivery of Dapoxetine HCl Amalgamated as a Nanoplatform: In vitro and in vivo Assessment | Mitigation of Rheumatic Arthritis in a Rat Model via Transdermal Delivery of Dapoxetine HCl Amalgamated as a Nanoplatform: In vitro and in vivo Assessment Abstract Abstract Purpose Dapoxetine HCl (DH), a selective serotonin reuptake inhibitor, may be useful for the treatment of rheumatic arthritis (RA). The purpose of ... |
PMC2850153 | core_pubmed_pmc | Absorption, Distribution, Excretion, and Pharmacokinetics of 14 C-Pyronaridine Tetraphosphate in Male and Female Sprague-Dawley Rats | Absorption, Distribution, Excretion, and Pharmacokinetics of 14 C-Pyronaridine Tetraphosphate in Male and Female Sprague-Dawley Rats Abstract Abstract The main objective of this investigation was to determine the absorption, distribution, excretion, and pharmacokinetics of the antimalarial drug pyronaridine tetraphosph... |
PMC5980117 | core_pubmed_pmc | Phase I study of taselisib in Japanese patients with advanced solid tumors or hormone receptor‐positive advanced breast cancer | Phase I study of taselisib in Japanese patients with advanced solid tumors or hormone receptor‐positive advanced breast cancer Abstract Taselisib is a potent and selective phosphatidylinositide 3‐kinase ( PI 3K) inhibitor. The present article reports the first study of taselisib administration in Japanese patients. The... |
PMC6166198 | core_pubmed_pmc | A “novel” association to treat pain: tramadol/dexketoprofen. The first drug of a “new pharmacological class” | A “novel” association to treat pain: tramadol/dexketoprofen. The first drug of a “new pharmacological class” Abstract Abstract Acute and chronic pain have an important socio-economical impact. In order to help physicians to choose the appropriate drug, especially for cancer pain, in 1986 WHO has developed a three-step ... |
PMC11903783 | core_pubmed_pmc | Exploiting metabolic vulnerability in glioblastoma using a brain-penetrant drug with a safe profile | Exploiting metabolic vulnerability in glioblastoma using a brain-penetrant drug with a safe profile Abstract Abstract Glioblastoma is one of the most treatment-resistant and lethal cancers, with a subset of self-renewing brain tumour stem cells (BTSCs), driving therapy resistance and relapse. Here, we report that mubri... |
PMC3835938 | core_pubmed_pmc | Effects of the mu-opioid receptor antagonist GSK1521498 on hedonic and consummatory eating behaviour: a proof of mechanism study in binge-eating obese subjects | Effects of the mu-opioid receptor antagonist GSK1521498 on hedonic and consummatory eating behaviour: a proof of mechanism study in binge-eating obese subjects Abstract Abstract The opioid system is implicated in the hedonic and motivational processing of food, and in binge eating, a behaviour strongly linked to obesit... |
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