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PMC8880691
core_pubmed_pmc
Impact of Linker Modification and PEGylation of Vancomycin Conjugates on Structure-Activity Relationships and Pharmacokinetics
Impact of Linker Modification and PEGylation of Vancomycin Conjugates on Structure-Activity Relationships and Pharmacokinetics Abstract As multidrug-resistant bacteria represent a concerning burden, experts insist on the need for a dramatic rethinking on antibiotic use and development in order to avoid a post-antibioti...
PMC5516849
core_pubmed_pmc
Model-based dietary optimization for late-stage, levodopa-treated, Parkinson’s disease patients
Model-based dietary optimization for late-stage, levodopa-treated, Parkinson’s disease patients Abstract Abstract Levodopa has been the gold standard for Parkinson’s disease treatment for more than 40 years. Its bioavailability is hindered by dietary amino acids, leading to fluctuations in the motor response particular...
PMC2938306
core_pubmed_pmc
Profile of olanzapine long-acting injection for the maintenance treatment of adult patients with schizophrenia
Profile of olanzapine long-acting injection for the maintenance treatment of adult patients with schizophrenia Abstract Abstract Olanzapine long-acting injection (OLAI) is a crystalline salt composed of olanzapine and pamoic acid, which permits a depot intramuscular formulation of olanzapine. The half-life of olanzapin...
PMC11559592
core_pubmed_pmc
A randomized, placebo‐controlled first‐in‐human study of oral TQS‐168 in healthy volunteers: Assessment of safety, tolerability, pharmacokinetics, pharmacodynamics, and food effect
A randomized, placebo‐controlled first‐in‐human study of oral TQS‐168 in healthy volunteers: Assessment of safety, tolerability, pharmacokinetics, pharmacodynamics, and food effect Abstract Abstract TQS‐168, a first‐in‐class small‐molecule inducer of peroxisome proliferator‐activated receptor gamma coactivator 1‐alpha ...
PMC10643601
core_pubmed_pmc
Utilizing network pharmacology and experimental validation to explore the potential molecular mechanisms of raw Pinellia ternate in treating esophageal cancer
Utilizing network pharmacology and experimental validation to explore the potential molecular mechanisms of raw Pinellia ternate in treating esophageal cancer Abstract Abstract Background Esophageal cancer (EC) is a highly lethal malignancy with a grim prognosis and high mortality rates, primarily treated through surge...
PMC7004075
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Insulin Tregopil in Relation to Premeal Dosing Time, Between Meal Interval, and Meal Composition in Patients With Type 2 Diabetes Mellitus
Pharmacokinetics and Pharmacodynamics of Insulin Tregopil in Relation to Premeal Dosing Time, Between Meal Interval, and Meal Composition in Patients With Type 2 Diabetes Mellitus Abstract Abstract We evaluated the pharmacokinetics and pharmacodynamics of oral insulin tregopil in relation to premeal dosing time, betwee...
PMC11707323
core_pubmed_pmc
Adrenaline Auto‐Injectors for Preventing Fatal Anaphylaxis
Adrenaline Auto‐Injectors for Preventing Fatal Anaphylaxis Abstract ABSTRACT Anaphylaxis affects up to 5% of people during their lifetime. Although anaphylaxis usually resolves without long‐term physical consequences, it can result in anxiety and quality of life impairment. Rarely and unpredictably, community anaphylax...
PMC12547498
core_pubmed_pmc
Exploring the Interaction Between Injection Site and Biological Sex on the Real-world Population Pharmacokinetics of Long-acting Cabotegravir and Rilpivirine in People With HIV
Exploring the Interaction Between Injection Site and Biological Sex on the Real-world Population Pharmacokinetics of Long-acting Cabotegravir and Rilpivirine in People With HIV Abstract Abstract Background Long-acting injectable antiretroviral therapy with cabotegravir and rilpivirine is efficacious though demonstrates...
PMC10175975
core_pubmed_pmc
Seeing what is behind the smokescreen: A systematic review of methodological aspects of smoking interaction studies over the last three decades and implications for future clinical trials
Seeing what is behind the smokescreen: A systematic review of methodological aspects of smoking interaction studies over the last three decades and implications for future clinical trials Abstract Abstract Smoking drug interaction studies represent a common approach for the clinical investigation of CYP1A2 induction. D...
PMC6935279
core_pubmed_pmc
Levonadifloxacin, a Novel Broad-Spectrum Anti-MRSA Benzoquinolizine Quinolone Agent: Review of Current Evidence
Levonadifloxacin, a Novel Broad-Spectrum Anti-MRSA Benzoquinolizine Quinolone Agent: Review of Current Evidence Abstract Abstract Levonadifloxacin and its prodrug alalevonadifloxacin are novel broad-spectrum anti-MRSA agents belonging to the benzoquinolizine subclass of quinolone, formulated for intravenous and oral ad...
PMC6155430
core_pubmed_pmc
Simultaneous Determination of Three Furanocoumarins by UPLC/MS/MS: Application to Pharmacokinetic Study of Angelica dahurica Radix after Oral Administration to Normal and Experimental Colitis-Induced Rats
Simultaneous Determination of Three Furanocoumarins by UPLC/MS/MS: Application to Pharmacokinetic Study of Angelica dahurica Radix after Oral Administration to Normal and Experimental Colitis-Induced Rats Abstract In traditional oriental medicine, Angelica dahurica Radix (ADR) is used in the treatment of gastrointestin...
PMC8953614
core_pubmed_pmc
Mitigating the Risk of Adverse Effects Related to Augmentation Therapy for Resistant Major Depressive Disorder: A Case Report
Mitigating the Risk of Adverse Effects Related to Augmentation Therapy for Resistant Major Depressive Disorder: A Case Report Abstract Polypharmacy of psychotropic medications predisposes older adults to adverse drug events (ADEs). One contributing factor is inhibition of metabolic pathways between substrates (competit...
PMC11289212
core_pubmed_pmc
In-label, off-label prescription, efficacy and tolerability of dalbavancin: report from a National Registry
In-label, off-label prescription, efficacy and tolerability of dalbavancin: report from a National Registry Abstract Abstract Purpose Although dalbavancin is currently approved for the treatment of ABSSIs, several studies suggest its efficacy and tolerance as long-term therapy for other off-label indications requiring ...
PMC5732553
core_pubmed_pmc
Sodium cholate-enhanced polymeric micelle system for tumor-targeting delivery of paclitaxel
Sodium cholate-enhanced polymeric micelle system for tumor-targeting delivery of paclitaxel Abstract Abstract Purpose Polymeric micelles are attractive nanocarriers for tumor-targeted delivery of paclitaxel (PTX). High antitumor efficacy and low toxicity require that PTX mainly accumulated in tumors with little drug ex...
PMC12526383
core_pubmed_pmc
Pharmacokinetics, Safety and Tolerability of Intravenous Lenzilumab, an Anti-GM-CSF Monoclonal Antibody Drug, in Healthy Korean Subjects
Pharmacokinetics, Safety and Tolerability of Intravenous Lenzilumab, an Anti-GM-CSF Monoclonal Antibody Drug, in Healthy Korean Subjects Abstract Abstract Background Lenzilumab is a recombinant monoclonal antibody neutralizing human granulocyte macrophage-colony stimulating factor. By modulating proinflammatory cytokin...
PMC5080318
core_pubmed_pmc
A phase I study of BI 811283, an Aurora B kinase inhibitor, in patients with advanced solid tumors
A phase I study of BI 811283, an Aurora B kinase inhibitor, in patients with advanced solid tumors Abstract Abstract Purpose This phase I study investigated the maximum tolerated dose (MTD), safety, pharmacokinetics, pharmacodynamics, and antitumor activity of the Aurora B kinase inhibitor BI 811283 in patients with ad...
PMC8141810
core_pubmed_pmc
Isobutyrylcarnitine as a Biomarker of OCT1 Activity and Interspecies Differences in its Membrane Transport
Isobutyrylcarnitine as a Biomarker of OCT1 Activity and Interspecies Differences in its Membrane Transport Abstract Genome-wide association studies have identified an association between isobutyrylcarnitine (IBC) and organic cation transporter 1 (OCT1) genotypes. Higher IBC blood concentrations in humans with active OC...
PMC5771548
core_pubmed_pmc
Single-Dose Pharmacokinetics of HLD200, a Delayed-Release and Extended-Release Methylphenidate Formulation, in Healthy Adults and in Adolescents and Children with Attention-Deficit/Hyperactivity Disorder
Single-Dose Pharmacokinetics of HLD200, a Delayed-Release and Extended-Release Methylphenidate Formulation, in Healthy Adults and in Adolescents and Children with Attention-Deficit/Hyperactivity Disorder Abstract Abstract Objective: Current extended-release (ER) formulations of psychostimulants used for treatment of at...
PMC8654833
core_pubmed_pmc
Evaluation of a 5-HT 2B receptor agonist in a murine model of amyotrophic lateral sclerosis
Evaluation of a 5-HT 2B receptor agonist in a murine model of amyotrophic lateral sclerosis Abstract Degeneration of brainstem serotonin neurons has been demonstrated in ALS patients and mouse models and was found responsible for the development of spasticity. Consistent with involvement of central serotonin pathways, ...
PMC9050413
core_pubmed_pmc
Chemical Reactivity and Optical and Pharmacokinetics Studies of 14 Multikinase Inhibitors and Their Docking Interactions Toward ACK1 for Precision Oncology
Chemical Reactivity and Optical and Pharmacokinetics Studies of 14 Multikinase Inhibitors and Their Docking Interactions Toward ACK1 for Precision Oncology Abstract Abstract Activated Cdc42-associated kinase 1 (ACK1/TNK2) has a significant role in cell endocytosis, survival, proliferation, and migration. Mutations in A...
PMC10720588
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic (PK/PD) simulation for dosage optimization of colistin and sitafloxacin, alone and in combination, against carbapenem-, multidrug-, and colistin-resistant Acinetobacter baumannii
Pharmacokinetic/pharmacodynamic (PK/PD) simulation for dosage optimization of colistin and sitafloxacin, alone and in combination, against carbapenem-, multidrug-, and colistin-resistant Acinetobacter baumannii Abstract Abstract To the best of our knowledge, to date, no study has investigated the optimal dosage regimen...
PMC5934791
core_pubmed_pmc
Vemurafenib in Chinese patients with BRAF V600 mutation–positive unresectable or metastatic melanoma: an open-label, multicenter phase I study
Vemurafenib in Chinese patients with BRAF V600 mutation–positive unresectable or metastatic melanoma: an open-label, multicenter phase I study Abstract Background Melanoma is a rare, deadly disease without effective treatment options in China. Vemurafenib is a selective inhibitor of oncogenic BRAF V600 kinase approved ...
PMC12670832
core_pubmed_pmc
A commentary on the article “Controlled Ovarian Stimulation (COS) with follitropin delta results in higher cumulative live birth rates compared with r-hFSH alfa/beta in a large retrospectively analysed real-world data set”
A commentary on the article “Controlled Ovarian Stimulation (COS) with follitropin delta results in higher cumulative live birth rates compared with r-hFSH alfa/beta in a large retrospectively analysed real-world data set” Abstract Abstract Follitropin delta, a recombinant human follicle-stimulating hormone (r-hFSH), i...
PMC11286609
core_pubmed_pmc
In vitro and in vivo analyses of eFAP: a novel FAP-targeting small molecule for radionuclide theranostics and other oncological interventions
In vitro and in vivo analyses of eFAP: a novel FAP-targeting small molecule for radionuclide theranostics and other oncological interventions Abstract Background Fibroblast activation protein (FAP), a transmembrane serine protease overexpressed by cancer-associated fibroblasts in the tumor stroma, is an interesting bio...
PMC10299984
core_pubmed_pmc
Pharmacokinetics and Safety of iGlarLixi in Healthy Chinese Participants: Results of a Phase 1 Randomized Study
Pharmacokinetics and Safety of iGlarLixi in Healthy Chinese Participants: Results of a Phase 1 Randomized Study Abstract Abstract Introduction The Chinese Diabetes Society recommends basal insulin and glucagon-like peptide-1 receptor agonists as an add-on therapy to first-line oral antihyperglycemic drugs for people wi...
PMC9019490
core_pubmed_pmc
Population Pharmacokinetics of Danofloxacin in Yellow River Carp ( Cyprinus carpio haematopterus ) After One Single Oral Dose
Population Pharmacokinetics of Danofloxacin in Yellow River Carp ( Cyprinus carpio haematopterus ) After One Single Oral Dose Abstract Abstract This study aimed to determine the population pharmacokinetics of danofloxacin in healthy Yellow River carp ( Cyprinus carpio Haematopterus ) after single oral administration at...
PMC5914547
core_pubmed_pmc
Theoretical overview of clinical and pharmacological aspects of the use of etelcalcetide in diabetic patients undergoing hemodialysis
Theoretical overview of clinical and pharmacological aspects of the use of etelcalcetide in diabetic patients undergoing hemodialysis Abstract Etelcalcetide is the first intravenous calcimimetic agent authorized for the treatment of secondary hyperparathyroidism (sHPT) in patients undergoing hemodialysis in Europe, the...
PMC9199885
core_pubmed_pmc
Physiologically‐based pharmacokinetic model‐based translation of OATP1B ‐mediated drug–drug interactions from coproporphyrin I to probe drugs
Physiologically‐based pharmacokinetic model‐based translation of OATP1B ‐mediated drug–drug interactions from coproporphyrin I to probe drugs Abstract Abstract The accurate prediction of OATP1B‐mediated drug–drug interactions (DDIs) is challenging for drug development. Here, we report a physiologically‐based pharmacoki...
PMC4808073
core_pubmed_pmc
Dependence of treatment planning accuracy in peptide receptor radionuclide therapy on the sampling schedule
Dependence of treatment planning accuracy in peptide receptor radionuclide therapy on the sampling schedule Abstract Background Peptide receptor radionuclide therapy (PRRT) plays an important role in the treatment of neuroendocrine tumors (NET). Pre-therapeutic dosimetry using the area under the measured time-activity ...
PMC7712907
core_pubmed_pmc
Personalized Medicine for Antibiotics: The Role of Nanobiosensors in Therapeutic Drug Monitoring
Personalized Medicine for Antibiotics: The Role of Nanobiosensors in Therapeutic Drug Monitoring Abstract Abstract Due to the high bacterial resistance to antibiotics (AB), it has become necessary to adjust the dose aimed at personalized medicine by means of therapeutic drug monitoring (TDM). TDM is a fundamental tool ...
PMC11336326
core_pubmed_pmc
The anti-COVID-19 drug nirmatrelvir crosses the blood‒brain barrier and exhibits herb–drug pharmacokinetic interactions with Scutellaria baicalensis formulations
The anti-COVID-19 drug nirmatrelvir crosses the blood‒brain barrier and exhibits herb–drug pharmacokinetic interactions with Scutellaria baicalensis formulations Abstract Aim of the study Our hypothesis is that nirmatrelvir can penetrate the blood‒brain barrier and reach effective concentrations in the brain. Furthermo...
PMC5683617
core_pubmed_pmc
Delivery of epirubicin via slow infusion as a strategy to mitigate chemotherapy-induced cardiotoxicity
Delivery of epirubicin via slow infusion as a strategy to mitigate chemotherapy-induced cardiotoxicity Abstract Abstract Background Continuous infusion of doxorubicin has been a strategy to reduce cardiotoxicity. Epirubicin is another anthracycline in common clinical use. However, evidence is lacking regarding whether ...
PMC12850597
core_pubmed_pmc
Pharmacokinetics of teicoplanin in paediatric patients—A systematic review of current literature
Pharmacokinetics of teicoplanin in paediatric patients—A systematic review of current literature Abstract Background and Objective Teicoplanin is commonly used in children to treat gram‐positive infections and is sometimes used off‐label prophylactically in surgical or paediatric oncology settings. The pharmacokinetics...
PMC12570718
core_pubmed_pmc
Identification of potential natural BCL-2 inhibitors for leukemia through an integrated virtual screening approach
Identification of potential natural BCL-2 inhibitors for leukemia through an integrated virtual screening approach Abstract Abstract Leukemia, a hematologic malignancy, frequently involves the overexpression of BCL-2 proteins, contributing to cell survival and apoptosis resistance. Although current BCL-2 inhibitors, in...
PMC11631598
core_pubmed_pmc
Population pharmacokinetics and dose optimization of ceftazidime in critically ill children
Population pharmacokinetics and dose optimization of ceftazidime in critically ill children Abstract Abstract Objective The aim of this study was to develop a population pharmacokinetic model for ceftazidime in critically ill children in the pediatric intensive care unit (PICU) and optimize an appropriate dosing regime...
PMC10024091
core_pubmed_pmc
The association between UGT1A1 polymorphisms and treatment toxicities of liposomal irinotecan
The association between UGT1A1 polymorphisms and treatment toxicities of liposomal irinotecan Abstract Abstract Background Initial dose adjustment is recommended for patients with known UGT1A1 ∗28 homozygosity for both conventional irinotecan and liposomal irinotecan (nal-IRI). A recent population pharmacokinetic (PK) ...
PMC10279797
core_pubmed_pmc
A critical review of Roxadustat formulations, solid state studies, and analytical methodology
A critical review of Roxadustat formulations, solid state studies, and analytical methodology Abstract Abstract This review aims to collate information about the analytical methodologies, bioanalytical methodologies, pharmaceutical formulations, solid-state studies, and the current and future market scenario for a rela...
PMC9300521
core_pubmed_pmc
A phase I/II study of 10-min dosing of bendamustine hydrochloride (rapid infusion formulation) in patients with previously untreated indolent B-cell non-Hodgkin lymphoma, mantle cell lymphoma, or relapsed/refractory diffuse large B-cell lymphoma in Japan
A phase I/II study of 10-min dosing of bendamustine hydrochloride (rapid infusion formulation) in patients with previously untreated indolent B-cell non-Hodgkin lymphoma, mantle cell lymphoma, or relapsed/refractory diffuse large B-cell lymphoma in Japan Abstract Purpose This phase I/II clinical study was conducted to ...
PMC5558752
core_pubmed_pmc
Surgical versus percutaneous isolated pelvic perfusion (IPP) for advanced melanoma: comparison in terms of melphalan pharmacokinetic pelvic bio-availability
Surgical versus percutaneous isolated pelvic perfusion (IPP) for advanced melanoma: comparison in terms of melphalan pharmacokinetic pelvic bio-availability Abstract Abstract Background Isolated pelvic perfusion (IPP) can be used to treat unresectable melanoma metastases of the pelvis. IPP can be performed either by su...
PMC6718004
core_pubmed_pmc
A Phase 1, Multiple‐Dose Study of Vedolizumab in Japanese Patients With Ulcerative Colitis
A Phase 1, Multiple‐Dose Study of Vedolizumab in Japanese Patients With Ulcerative Colitis Abstract Abstract Although previous studies have shown that patients with ulcerative colitis may benefit from treatment with vedolizumab, a humanized monoclonal antibody targeting the α 4 β 7 integrin heterodimer, no data exist i...
PMC8316117
core_pubmed_pmc
Efficacy and Associated Drug Exposures of Isavuconazole and Fluconazole in an Experimental Model of Coccidioidomycosis
Efficacy and Associated Drug Exposures of Isavuconazole and Fluconazole in an Experimental Model of Coccidioidomycosis Abstract ABSTRACT Coccidioides spp. are important pathogens in regions where they are endemic, and new treatment options are needed. Here, isavuconazonium sulfate (ISAVUSULF) and fluconazole (FLU) were...
PMC7798018
core_pubmed_pmc
Nebulised surface-active hybrid nanoparticles of voriconazole for pulmonary Aspergillosis demonstrate clathrin-mediated cellular uptake, improved antifungal efficacy and lung retention
Nebulised surface-active hybrid nanoparticles of voriconazole for pulmonary Aspergillosis demonstrate clathrin-mediated cellular uptake, improved antifungal efficacy and lung retention Abstract Abstract Background Incidence of pulmonary aspergillosis is rising worldwide, owing to an increased population of immunocompro...
PMC7032248
core_pubmed_pmc
Mixed PEGylated surfactant modifying system decrease the accelerated blood clearance phenomenon of nanoemulsions in rats
Mixed PEGylated surfactant modifying system decrease the accelerated blood clearance phenomenon of nanoemulsions in rats Abstract The accelerated blood clearance (ABC) phenomenon which is induced by repeated injection of poly (ethylene glycol) (PEG)-coated colloidal carriers gives clinical challenge to the promising dr...
PMC12863264
core_pubmed_pmc
Effect of Testosterone Therapy on Cytochrome P450 3A and P‐Glycoprotein Activities Using Midazolam and Digoxin as Probe Substrates Among Transgender Adults
Effect of Testosterone Therapy on Cytochrome P450 3A and P‐Glycoprotein Activities Using Midazolam and Digoxin as Probe Substrates Among Transgender Adults Abstract ABSTRACT Background Gender‐affirming testosterone therapy is one part of the standard of care for more than 1 million transgender adults in the United Stat...
PMC10459686
core_pubmed_pmc
Preclinical Evaluation of a New Series of Albumin-Binding 177 Lu-Labeled PSMA-Based Low-Molecular-Weight Radiotherapeutics
Preclinical Evaluation of a New Series of Albumin-Binding 177 Lu-Labeled PSMA-Based Low-Molecular-Weight Radiotherapeutics Abstract Abstract Prostate-specific membrane antigen (PSMA)-based low-molecular-weight agents using beta(β)-particle-emitting radiopharmaceuticals is a new treatment paradigm for patients with meta...
PMC8958267
core_pubmed_pmc
Ponesimod in the Treatment of Relapsing Forms of Multiple Sclerosis: An Update on the Emerging Clinical Data
Ponesimod in the Treatment of Relapsing Forms of Multiple Sclerosis: An Update on the Emerging Clinical Data Abstract Abstract Sphingosine 1-phosphate (S1P) receptors are bioactive lipid metabolites that bind five different types of receptors expressed ubiquitously in human body and mediate a broad range of biological ...
PMC6642527
core_pubmed_pmc
A prospective cohort study on the pharmacokinetics of nivolumab in metastatic non-small cell lung cancer, melanoma, and renal cell cancer patients
A prospective cohort study on the pharmacokinetics of nivolumab in metastatic non-small cell lung cancer, melanoma, and renal cell cancer patients Abstract Background Nivolumab is administered in a weight-based or fixed-flat dosing regimen. For patients with non-small cell lung cancer (NSCLC), a potential exposure-resp...
PMC9979997
core_pubmed_pmc
Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complex
Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complex Abstract Abstract In present, there was no detailed report on the formulation optimization and quality evaluation of aprepitant (APT) injectable lipid emulsion (APT-IE). The aim of the present investigation was ...
PMC4245888
core_pubmed_pmc
Pharmacokinetic non-interaction analysis in a fixed-dose formulation in combination of atorvastatin and ezetimibe
Pharmacokinetic non-interaction analysis in a fixed-dose formulation in combination of atorvastatin and ezetimibe Abstract Abstract Recent clinical research has shown that atorvastatin (ATO) in combination with cholesterol absorption inhibitor ezetimibe (EZE) significantly reduces LDL-C level in patients with hyperchol...
PMC11938128
core_pubmed_pmc
Exploring shared therapeutic targets for Alzheimer’s disease and glioblastoma using network pharmacology and protein-protein interaction approach
Exploring shared therapeutic targets for Alzheimer’s disease and glioblastoma using network pharmacology and protein-protein interaction approach Abstract Abstract Background Alzheimer’s disease (AD) and glioblastoma (GBM) are complex neurological disorders with distinct pathologies but overlapping molecular mechanisms...
PMC12049887
core_pubmed_pmc
A phase I, open-label, multicentre, first-in-human study to evaluate safety, pharmacokinetics and efficacy of AMG 404, a PD-1 inhibitor, in patients with advanced solid tumours
A phase I, open-label, multicentre, first-in-human study to evaluate safety, pharmacokinetics and efficacy of AMG 404, a PD-1 inhibitor, in patients with advanced solid tumours Abstract Abstract Objective To evaluate the safety, tolerability, pharmacokinetics (PK) and preliminary antitumour activity of AMG 404, a fully...
PMC11468074
core_pubmed_pmc
Edoxaban pharmacokinetics during in vitro continuous renal replacement therapy
Edoxaban pharmacokinetics during in vitro continuous renal replacement therapy Abstract Abstract Background To evaluate the clearance of edoxaban during modeled in vitro continuous renal replacement therapy (CRRT), assess protein binding and circuit adsorption, and provide initial dosing recommendations. Methods Edoxab...
PMC6836748
core_pubmed_pmc
Quinolone antibiotics
Quinolone antibiotics Abstract The quinolone antibiotics arose in the early 1960s, with the first examples possessing a narrow-spectrum activity with unfavorable pharmacokinetic properties. Abstract The quinolone antibiotics arose in the early 1960s, with the first examples possessing a narrow-spectrum of activity with...
PMC5532403
core_pubmed_pmc
Potential for a novel manganese porphyrin compound as adjuvant canine lymphoma therapy
Potential for a novel manganese porphyrin compound as adjuvant canine lymphoma therapy Abstract Abstract Purpose Manganese porphyrins are redox-active drugs and superoxide dismutase mimics, which have been shown to chemosensitize lymphoma, a cancer which frequently occurs in dogs. This study aimed to identify critical ...
PMC9691676
core_pubmed_pmc
Evaluation of vancomycin pharmacokinetics in patients with augmented renal clearances: A randomized clinical trial
Evaluation of vancomycin pharmacokinetics in patients with augmented renal clearances: A randomized clinical trial Abstract Purpose: Vancomycin is a narrow therapeutic window glycopeptide antibiotic that acts against Gram-positive bacteria. As it is renally eliminated, therapeutic drug monitoring is recommended for van...
PMC11832027
core_pubmed_pmc
Hemodynamic and Pharmacokinetic Interactions of TPN171 with Alcohol in Healthy Male Subjects
Hemodynamic and Pharmacokinetic Interactions of TPN171 with Alcohol in Healthy Male Subjects Abstract ABSTRACT This study aimed to evaluate the effects of the concomitant administration of TPN171 and alcohol on hemodynamic and pharmacokinetic characteristics in healthy Chinese male subjects. Fifteen eligible subjects w...
PMC4772335
core_pubmed_pmc
First-In-Human safety and long-term exposure data for AAB-003 (PF-05236812) and biomarkers after intravenous infusions of escalating doses in patients with mild to moderate Alzheimer’s disease
First-In-Human safety and long-term exposure data for AAB-003 (PF-05236812) and biomarkers after intravenous infusions of escalating doses in patients with mild to moderate Alzheimer’s disease Abstract Abstract Background In the First-In-Human (FIH), 39-week, randomized, adaptive design study, safety, tolerability, pha...
PMC8918542
core_pubmed_pmc
Clinical Importance of Potential Genetic Determinants Affecting Propofol Pharmacokinetics and Pharmacodynamics
Clinical Importance of Potential Genetic Determinants Affecting Propofol Pharmacokinetics and Pharmacodynamics Abstract Interindividual variability in response to drugs used in anesthesia has long been considered the rule, not the exception. It is important to mention that in anesthesiology, the variability in response...
PMC4699723
core_pubmed_pmc
A Pilot Study of the Effect of Daikenchuto on Rectal Sensation in Patients with Irritable Bowel Syndrome
A Pilot Study of the Effect of Daikenchuto on Rectal Sensation in Patients with Irritable Bowel Syndrome Abstract Abstract Background/Aims Daikenchuto (TU 100), a botanical agent that modulates gastrointestinal nerves, is used in the treatment of motility and functional disorders. Our aim was to study the effects of TU...
PMC8316766
core_pubmed_pmc
Genetic Polymorphisms Associated With the Pharmacokinetics, Pharmacodynamics and Adverse Effects of Olanzapine, Aripiprazole and Risperidone
Genetic Polymorphisms Associated With the Pharmacokinetics, Pharmacodynamics and Adverse Effects of Olanzapine, Aripiprazole and Risperidone Abstract Olanzapine, aripiprazole and risperidone are atypical antipsychotics or neuroleptics widely used for schizophrenia treatment. They induce various adverse drug reactions d...
PMC7403827
core_pubmed_pmc
Dual blockade of EGFR and VEGFR pathways: Results from a pilot study evaluating apatinib plus gefitinib as a first‐line treatment for advanced EGFR‐mutant non‐small cell lung cancer
Dual blockade of EGFR and VEGFR pathways: Results from a pilot study evaluating apatinib plus gefitinib as a first‐line treatment for advanced EGFR‐mutant non‐small cell lung cancer Abstract Abstract Background Dual blockade of both EGFR and VEGFR pathways in EGFR‐mutant NSCLC have shown enhanced antitumor efficacy ver...
PMC4151799
core_pubmed_pmc
Preclinical antitumor activity of SST0116CL1: A novel heat shock protein 90 inhibitor
Preclinical antitumor activity of SST0116CL1: A novel heat shock protein 90 inhibitor Abstract Abstract 4-Amino substituted resorcino-isoxazole (SST0116CL1) (property of Sigma-Tau Research Switzerland S.A.) is a potent, second generation, small-molecule heat shock protein 90 inhibitor (Hsp90i). SST0116CL1 binds to the ...
PMC7076527
core_pubmed_pmc
Quantitative Proteomics of Clinically Relevant Drug-Metabolizing Enzymes and Drug Transporters and Their Intercorrelations in the Human Small Intestine
Quantitative Proteomics of Clinically Relevant Drug-Metabolizing Enzymes and Drug Transporters and Their Intercorrelations in the Human Small Intestine Abstract The levels of drug-metabolizing enzymes (DMEs) and transporter proteins in the human intestine are pertinent to determine oral drug bioavailability. Despite th...
PMC8653186
core_pubmed_pmc
First‐in‐Human Study of Bamlanivimab in a Randomized Trial of Hospitalized Patients With COVID‐19
First‐in‐Human Study of Bamlanivimab in a Randomized Trial of Hospitalized Patients With COVID‐19 Abstract Abstract Therapeutics for patients hospitalized with coronavirus disease 2019 (COVID‐19) are urgently needed during the pandemic. Bamlanivimab is a potent neutralizing monoclonal antibody that blocks severe acute ...
PMC3371469
core_pubmed_pmc
Propofol pharmacokinetics in young healthy Indian subjects
Propofol pharmacokinetics in young healthy Indian subjects Abstract Abstract Objectives: To analyze population pharmacokinetics of Propofol in Indian patients after single bolus dose of Propofol using WINNONLIN program. Materials and Methods: Population pharmacokinetics of Propofol was investigated in Indian subjects i...
PMC6294406
core_pubmed_pmc
Pharmacokinetics and Abuse Potential of Benzhydrocodone, a Novel Prodrug of Hydrocodone, After Intranasal Administration in Recreational Drug Users
Pharmacokinetics and Abuse Potential of Benzhydrocodone, a Novel Prodrug of Hydrocodone, After Intranasal Administration in Recreational Drug Users Abstract Abstract Objective Developing an acetaminophen-free, immediate-release hydrocodone product remains an unmet medical need; however, new opioid analgesics should not...
PMC5703746
core_pubmed_pmc
Pharmacogenetic Variation in Over 100 Genes in Patients Receiving Acenocumarol
Pharmacogenetic Variation in Over 100 Genes in Patients Receiving Acenocumarol Abstract Coumarins are widely prescribed worldwide, and in Mexico acenocumarol is the preferred form. It is well known that despite its efficacy, coumarins show a high variability for dose requirements. We investigated the pharmacogenetic va...
PMC12875509
core_pubmed_pmc
Optimizing vedolizumab therapy in ulcerative colitis: A critical synthesis of trial evidence and the emerging role of artificial intelligence
Optimizing vedolizumab therapy in ulcerative colitis: A critical synthesis of trial evidence and the emerging role of artificial intelligence Abstract Abstract Background Vedolizumab, a monoclonal antibody targeting the α4β7 integrin, offers gut-selective immunosuppression and represents a cornerstone biologic therapy ...
PMC9649511
core_pubmed_pmc
Oral bioavailability of microdoses and therapeutic doses of midazolam as a 2-dimensionally printed orodispersible film in healthy volunteers
Oral bioavailability of microdoses and therapeutic doses of midazolam as a 2-dimensionally printed orodispersible film in healthy volunteers Abstract Abstract Purpose The use of two-dimensional (2D) printing technologies of drugs on orodispersible films (ODF) can promote dose individualization and facilitate drug deliv...
PMC11533106
core_pubmed_pmc
Population pharmacokinetics of valproic acid in children with epilepsy: Implications for dose tailoring when switching from oral syrup to sustained‐release tablets
Population pharmacokinetics of valproic acid in children with epilepsy: Implications for dose tailoring when switching from oral syrup to sustained‐release tablets Abstract Abstract Significant pharmacokinetic (PK) differences exist between different forms of valproic acid (VPA), such as syrup and sustained‐release (SR...
PMC10935712
core_pubmed_pmc
Phase 1 randomized pharmacokinetic and safety study of a 90‐day tenofovir vaginal ring in the United States
Phase 1 randomized pharmacokinetic and safety study of a 90‐day tenofovir vaginal ring in the United States Abstract Abstract Introduction Tenofovir‐based oral pre‐exposure prophylaxis is currently approved for HIV prevention; however, adherence in women has been low. A vaginal gel containing tenofovir (TFV) demonstrat...
PMC7046201
core_pubmed_pmc
Unexpected differences in the pharmacokinetics of N-acetyl-DL-leucine enantiomers after oral dosing and their clinical relevance
Unexpected differences in the pharmacokinetics of N-acetyl-DL-leucine enantiomers after oral dosing and their clinical relevance Abstract Abstract The enantiomers of many chiral drugs not only exhibit different pharmacological effects in regard to targets that dictate therapeutic and toxic effects, but are also handled...
PMC11494825
core_pubmed_pmc
Development and comparison of model‐integrated evidence approaches for bioequivalence studies with pharmacokinetic end points
Development and comparison of model‐integrated evidence approaches for bioequivalence studies with pharmacokinetic end points Abstract Abstract By applying nonlinear mixed‐effect (NLME) models, model‐integrated evidence (MIE) approaches are able to analyze bioequivalence (BE) data with pharmacokinetic end points that h...
PMC4768222
core_pubmed_pmc
Albumin-bound nanoparticle ( nab ) paclitaxel exhibits enhanced paclitaxel tissue distribution and tumor penetration
Albumin-bound nanoparticle ( nab ) paclitaxel exhibits enhanced paclitaxel tissue distribution and tumor penetration Abstract Purpose nab -paclitaxel demonstrates improved clinical efficacy compared with conventional Cremophor EL (CrEL)-paclitaxel in multiple tumor types. This study explored the distinctions in drug di...
PMC4913628
core_pubmed_pmc
Effect of Sucralfate on the Relative Bioavailability of Enrofloxacin and Ciprofloxacin in Healthy Fed Dogs
Effect of Sucralfate on the Relative Bioavailability of Enrofloxacin and Ciprofloxacin in Healthy Fed Dogs Abstract Abstract Background Sucralfate impairs absorption of ciprofloxacin and other fluoroquinolones in humans, but no sucralfate–fluoroquinolone interaction has been reported in dogs. Veterinary formularies rec...
PMC11722891
core_pubmed_pmc
Development of a Population Pharmacokinetic Model Characterizing the Tissue Distribution of Resveratrol After Administration by Different Routes and Doses in Rats
Development of a Population Pharmacokinetic Model Characterizing the Tissue Distribution of Resveratrol After Administration by Different Routes and Doses in Rats Abstract Background: Studies have demonstrated that resveratrol exerts several pharmacological effects. However, the pharmacokinetic parameters are not compl...
PMC9626527
core_pubmed_pmc
SHR2285, the first selectively oral FXIa inhibitor in China: Safety, tolerability, pharmacokinetics and pharmacodynamics combined with aspirin, clopidogrel or ticagrelor
SHR2285, the first selectively oral FXIa inhibitor in China: Safety, tolerability, pharmacokinetics and pharmacodynamics combined with aspirin, clopidogrel or ticagrelor Abstract Purpose: To evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of SHR2285, the first oral coagulation factor XIa (FXIa)...
PMC5225190
core_pubmed_pmc
Etirinotecan pegol administration is associated with lower incidences of neutropenia compared to irinotecan administration
Etirinotecan pegol administration is associated with lower incidences of neutropenia compared to irinotecan administration Abstract Purpose The relationship between incidences of neutropenia and 10-hydroxy-7-ethyl camptothecin (SN38) exposure was explored using SN38 pharmacokinetic and neutrophil count data from toxico...
PMC4785611
core_pubmed_pmc
A phase 1/2 study of carfilzomib in Japanese patients with relapsed and/or refractory multiple myeloma
A phase 1/2 study of carfilzomib in Japanese patients with relapsed and/or refractory multiple myeloma Abstract Summary We conducted a phase 1/2 study of single‐agent carfilzomib in Japanese patients with relapsed/refractory multiple myeloma. Safety, pharmacokinetics and pharmacodynamics of carfilzomib were examined in...
PMC5287433
core_pubmed_pmc
Characterization of ADME gene variation in 21 populations by exome sequencing
Characterization of ADME gene variation in 21 populations by exome sequencing Abstract Supplemental Digital Content is available in the text. Keywords: absorption, distribution, genetic variants, excretion; exome sequencing; metabolism; multiethnic populations; pharmacogenetics Abstract Objective Proteins involving abs...
PMC12189896
core_pubmed_pmc
Therapeutic Drug Monitoring-Based Population Pharmacokinetics of Amikacin in Patients at a Teaching Hospital
Therapeutic Drug Monitoring-Based Population Pharmacokinetics of Amikacin in Patients at a Teaching Hospital Abstract Background : Amikacin is still an essential antimicrobial to treat life-threatening infections, including multidrug-resistant microorganisms. The effectiveness of treatment has been correlated with the ...
PMC10953091
core_pubmed_pmc
Inverse association between plasma chlordecone concentrations and progression of alcoholic liver fibrosis: the role of liver metabolism
Inverse association between plasma chlordecone concentrations and progression of alcoholic liver fibrosis: the role of liver metabolism Abstract Abstract Background and Aims Chlordecone is a persistent organochlorinated insecticide, extensively used in the French West Indies and has been contaminating the population fo...
PMC6748671
core_pubmed_pmc
Distribution of Small Molecular Weight Drugs into the Porcine Lens: Studies on Imaging Mass Spectrometry, Partition Coefficients, and Implications in Ocular Pharmacokinetics
Distribution of Small Molecular Weight Drugs into the Porcine Lens: Studies on Imaging Mass Spectrometry, Partition Coefficients, and Implications in Ocular Pharmacokinetics Abstract Lens is the avascular tissue in the eye between the aqueous humor and vitreous. Drug binding to the lens might affect ocular pharmacokine...
PMC8196087
core_pubmed_pmc
First-in-Human Phase I Study of MP0250, a First-in-Class DARPin Drug Candidate Targeting VEGF and HGF, in Patients With Advanced Solid Tumors
First-in-Human Phase I Study of MP0250, a First-in-Class DARPin Drug Candidate Targeting VEGF and HGF, in Patients With Advanced Solid Tumors Abstract PURPOSE A first-in-human study was performed with MP0250, a DARPin drug candidate. MP0250 specifically inhibits both vascular endothelial growth factor (VEGF) and hepato...
PMC9867068
core_pubmed_pmc
Combined Gamma Conglutin and Lupanine Treatment Exhibits In Vivo an Enhanced Antidiabetic Effect by Modulating the Liver Gene Expression Profile
Combined Gamma Conglutin and Lupanine Treatment Exhibits In Vivo an Enhanced Antidiabetic Effect by Modulating the Liver Gene Expression Profile Abstract Abstract Previous studies have individually shown the antidiabetic potential of gamma conglutin (Cγ) and lupanine from lupins. Until now, the influence of combining b...
PMC3682882
core_pubmed_pmc
Safety, pharmacokinetics and pharmacodynamics of remogliflozin etabonate, a novel SGLT2 inhibitor, and metformin when co-administered in subjects with type 2 diabetes mellitus
Safety, pharmacokinetics and pharmacodynamics of remogliflozin etabonate, a novel SGLT2 inhibitor, and metformin when co-administered in subjects with type 2 diabetes mellitus Abstract Abstract Background The sodium-dependent glucose co-transporter-2 (SGLT2) is expressed in absorptive epithelia of the renal tubules. Re...
PMC3571896
core_pubmed_pmc
Safety and efficacy of high-dose daptomycin as salvage therapy for severe gram-positive bacterial sepsis in hospitalized adult patients
Safety and efficacy of high-dose daptomycin as salvage therapy for severe gram-positive bacterial sepsis in hospitalized adult patients Abstract Abstract Background Increasing the dosage of daptomycin may be advantageous in severe infection by enhancing bactericidal activity and pharmacodynamics. However, clinical data...
PMC12733648
core_pubmed_pmc
GLP-1 Signalling as a Therapeutic Avenue in Parkinson’s Disease: A Comprehensive Review
GLP-1 Signalling as a Therapeutic Avenue in Parkinson’s Disease: A Comprehensive Review Abstract Parkinson’s disease (PD) is a complex neurodegenerative disorder characterised by progressive motor and non-motor impairment, in which current therapies remain symptomatic and fail to halt dopaminergic neuron loss. Growing ...
PMC10117678
core_pubmed_pmc
The pharmacology and mechanisms of platycodin D, an active triterpenoid saponin from Platycodon grandiflorus
The pharmacology and mechanisms of platycodin D, an active triterpenoid saponin from Platycodon grandiflorus Abstract Abstract Chinese doctors widely prescribed Platycodon grandiflorus A. DC. (PG) to treat lung carbuncles in ancient China. Modern clinical experiences have demonstrated that PG plays a crucial role in tr...
PMC7193032
core_pubmed_pmc
Lactobacillus murinus Improved the Bioavailability of Orally Administered Glycyrrhizic Acid in Rats
Lactobacillus murinus Improved the Bioavailability of Orally Administered Glycyrrhizic Acid in Rats Abstract Intestinal microbiota has been extensively studied in the context of host health benefit, and it has recently become clear that the gut microbiota influences drug pharmacokinetics and correspondingly efficacy. I...
PMC4317229
core_pubmed_pmc
Prediction of clinical pharmacokinetics of AMG 181, a human anti- α 4 β 7 monoclonal antibody for treating inflammatory bowel diseases
Prediction of clinical pharmacokinetics of AMG 181, a human anti- α 4 β 7 monoclonal antibody for treating inflammatory bowel diseases Abstract The purpose of this study was to predict a safe starting dose of AMG 181, a human anti- α 4 β 7 antibody for treating inflammatory bowel diseases, based on cynomolgus monkey ph...
PMC4032242
core_pubmed_pmc
Glycoengineering of Interferon-β 1a Improves Its Biophysical and Pharmacokinetic Properties
Glycoengineering of Interferon-β 1a Improves Its Biophysical and Pharmacokinetic Properties Abstract Abstract The purpose of this study was to develop a biobetter version of recombinant human interferon-β 1a (rhIFN-β 1a) to improve its biophysical properties, such as aggregation, production and stability, and pharmacok...
PMC4968874
core_pubmed_pmc
Evaluation of Pharmacokinetics, and Bioavailability of Higher Doses of Tocotrienols in Healthy Fed Humans
Evaluation of Pharmacokinetics, and Bioavailability of Higher Doses of Tocotrienols in Healthy Fed Humans Abstract Background Tocotrienols has been known to lower serum lipid parameters below 500 mg/d, while increase lipid parameters at higher dose of 750 mg/d. δ-Tocotrienol has a novel inflammatory property of concent...
PMC7983974
core_pubmed_pmc
Drug‐drug interaction of atazanavir on UGT1A1‐mediated glucuronidation of molidustat in human
Drug‐drug interaction of atazanavir on UGT1A1‐mediated glucuronidation of molidustat in human Abstract Abstract Molidustat is an oral inhibitor of hypoxia‐inducible factor (HIF) prolyl‐hydroxylase enhancing the erythropoietin (EPO) response to HIF; it is in clinical development for the treatment of anaemia related to c...
PMC4492754
core_pubmed_pmc
Identification of activating enzymes of a novel FBPase inhibitor prodrug, CS-917
Identification of activating enzymes of a novel FBPase inhibitor prodrug, CS-917 Abstract CS-917 (MB06322) is a selective small compound inhibitor of fructose 1,6-bisphosphatase (FBPase), which is expected to be a novel drug for the treatment of type 2 diabetes by inhibiting gluconeogenesis. CS-917 is a bisamidate prod...
PMC3882303
core_pubmed_pmc
Pharmacokinetics, Safety and Antiviral Activity of Fosamprenavir/Ritonavir-containing Regimens in HIV-infected Children Aged 4 Weeks to 2 Years—48-week Study Data
Pharmacokinetics, Safety and Antiviral Activity of Fosamprenavir/Ritonavir-containing Regimens in HIV-infected Children Aged 4 Weeks to 2 Years—48-week Study Data Abstract Supplemental Digital Content is available in the text. Keywords: fosamprenavir, HIV-1, infants, children Abstract Background: Pharmacokinetics, safe...
PMC7311098
core_pubmed_pmc
Piperine Alters the Pharmacokinetics and Anticoagulation of Warfarin in Rats
Piperine Alters the Pharmacokinetics and Anticoagulation of Warfarin in Rats Abstract Abstract Introduction Piperine, the bioactive compound of black pepper, and warfarin are metabolized by cytochrome P450 enzymes and are both highly plasma protein-bound compounds. In this study, we evaluated the effect of co-administe...
PMC6152211
core_pubmed_pmc
Herb-Drug Interaction between the Traditional Hepatoprotective Formulation and Sorafenib on Hepatotoxicity, Histopathology and Pharmacokinetics in Rats
Herb-Drug Interaction between the Traditional Hepatoprotective Formulation and Sorafenib on Hepatotoxicity, Histopathology and Pharmacokinetics in Rats Abstract Abstract Sorafenib has been used as a standard therapy for advanced hepatocellular carcinoma (HCC). In Asia, patients with HCC are potentially treated with the...
PMC2865761
core_pubmed_pmc
Pazopanib-induced hyperbilirubinemia is associated with Gilbert's syndrome UGT1A1 polymorphism
Pazopanib-induced hyperbilirubinemia is associated with Gilbert's syndrome UGT1A1 polymorphism Abstract Abstract Background: Pazopanib has shown clinical activity against multiple tumour types and is generally well tolerated. However, isolated elevations in transaminases and bilirubin have been observed. This study exa...
PMC5902559
core_pubmed_pmc
Dynamics of Erythropoietic Biomarkers in Response to Treatment With Erythropoietin in Belgrade Rats
Dynamics of Erythropoietic Biomarkers in Response to Treatment With Erythropoietin in Belgrade Rats Abstract Abstract Recombinant human erythropoietin (rHuEPO) is used effectively in the treatment of various anemic disorders. Belgrade rat is a useful animal model of anemia caused by defect in iron utilization. The obje...