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PMC5519037
core_pubmed_pmc
Polymorphisms associated with everolimus pharmacokinetics, toxicity and survival in metastatic breast cancer
Polymorphisms associated with everolimus pharmacokinetics, toxicity and survival in metastatic breast cancer Abstract Abstract Purpose Metastatic breast cancer (MBC) progressing after endocrine therapy frequently activates PI3K/AKT/mTOR pathway. The BOLERO-2 trial showed that everolimus-exemestane achieves increased pr...
PMC6828636
core_pubmed_pmc
Drug–Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies
Drug–Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies Abstract Background and Objectives Darolutamide is a novel androgen receptor (AR) antagonist approved for the treatment of nonmetastatic castration-resistant prostate cancer (nmCRPC). Accordingly, the drug–drug interaction (DDI) potential of...
PMC11595589
core_pubmed_pmc
A Pharmacokinetic and Bioavailability Study of Ecklonia cava Phlorotannins Following Intravenous and Oral Administration in Sprague–Dawley Rats
A Pharmacokinetic and Bioavailability Study of Ecklonia cava Phlorotannins Following Intravenous and Oral Administration in Sprague–Dawley Rats Abstract Abstract This study examines the pharmacokinetics and bioavailability of phlorotannins from Ecklonia cava in rats following intravenous and oral administration. Known ...
PMC4469299
core_pubmed_pmc
Circadian variation in tamoxifen pharmacokinetics in mice and breast cancer patients
Circadian variation in tamoxifen pharmacokinetics in mice and breast cancer patients Abstract Abstract The anti-estrogen tamoxifen is characterized by a large variability in response, partly due to pharmacokinetic differences. We examined circadian variation in tamoxifen pharmacokinetics in mice and breast cancer patie...
PMC9540481
core_pubmed_pmc
Genomewide Association Study of Simvastatin Pharmacokinetics
Genomewide Association Study of Simvastatin Pharmacokinetics Abstract We investigated genetic determinants of single‐dose simvastatin pharmacokinetics in a prospective study of 170 subjects and a retrospective cohort of 59 healthy volunteers. In a microarray‐based genomewide association study with the prospective data,...
PMC9841306
core_pubmed_pmc
Optimization of blood pressure measurement practices for pharmacodynamic analyses of tyrosine‐kinase inhibitors
Optimization of blood pressure measurement practices for pharmacodynamic analyses of tyrosine‐kinase inhibitors Abstract Abstract Blood pressure measurements form a critical component of adverse event monitoring for tyrosine kinase inhibitors, but might also serve as a biomarker for dose titrations. This study explored...
PMC12816544
core_pubmed_pmc
Vedolizumab in inflammatory bowel disease: pharmacokinetics and the role of immunomodulator co-therapy
Vedolizumab in inflammatory bowel disease: pharmacokinetics and the role of immunomodulator co-therapy Abstract Vedolizumab (VED) is a gut-selective monoclonal antibody and an effective biological agent for many patients with inflammatory bowel disease (IBD). Therapeutic drug monitoring has been used to optimise treatm...
PMC6002508
core_pubmed_pmc
Applying a Global Sensitivity Analysis Workflow to Improve the Computational Efficiencies in Physiologically-Based Pharmacokinetic Modeling
Applying a Global Sensitivity Analysis Workflow to Improve the Computational Efficiencies in Physiologically-Based Pharmacokinetic Modeling Abstract Abstract Traditionally, the solution to reduce parameter dimensionality in a physiologically-based pharmacokinetic (PBPK) model is through expert judgment. However, this a...
PMC6221254
core_pubmed_pmc
Elucidating the active interaction mechanism of phytochemicals withanolide and withanoside derivatives with human serum albumin
Elucidating the active interaction mechanism of phytochemicals withanolide and withanoside derivatives with human serum albumin Abstract Abstract Withania somnifera (Ashwagandha) is an efficient medicinal plant known in Ayurveda and Chinese medicine since ancient times, whose extracts are consumed orally as food supple...
PMC11067504
core_pubmed_pmc
Effects of the selective AMPA modulator NBI‐1065845 on the pharmacokinetics of midazolam or ethinyl estradiol–levonorgestrel in healthy adults
Effects of the selective AMPA modulator NBI‐1065845 on the pharmacokinetics of midazolam or ethinyl estradiol–levonorgestrel in healthy adults Abstract Abstract This parallel‐arm, phase I study investigated the potential cytochrome P450 (CYP)3A induction effect of NBI‐1065845 (TAK‐653), an investigational α‐amino‐3‐hyd...
PMC12375587
core_pubmed_pmc
Assessment of heated herbal products’ tobacco harm reduction potential: pre‐clinical and clinical studies
Assessment of heated herbal products’ tobacco harm reduction potential: pre‐clinical and clinical studies Abstract Abstract Data from pre-clinical and clinical studies form part of an integrated assessment of the tobacco harm reduction (THR) potential of novel products that may act as cigarette alternatives for adult s...
PMC10457845
core_pubmed_pmc
Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: II. Antidepressant Effect in an Experimental Animal Model
Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: II. Antidepressant Effect in an Experimental Animal Model Abstract Abstract Depression is a serious mental disorder and the most prevalent cause of disability and suicide worldwide. Quercetin (QER) demonstrated antidepressant effects in rats exhibiting an...
PMC4603953
core_pubmed_pmc
Oseltamivir Population Pharmacokinetics in the Ferret: Model Application for Pharmacokinetic/Pharmacodynamic Study Design
Oseltamivir Population Pharmacokinetics in the Ferret: Model Application for Pharmacokinetic/Pharmacodynamic Study Design Abstract The ferret is a suitable small animal model for preclinical evaluation of efficacy of antiviral drugs against various influenza strains, including highly pathogenic H5N1 viruses. Rigorous p...
PMC9925909
core_pubmed_pmc
Relationship between raltegravir trough plasma concentration and virologic response and the impact of therapeutic drug monitoring during pregnancy
Relationship between raltegravir trough plasma concentration and virologic response and the impact of therapeutic drug monitoring during pregnancy Abstract Abstract Background Limited data is available on raltegravir (RAL) pharmacokinetics during pregnancy and the value of therapeutic drug monitoring (TDM) in pregnancy...
PMC12386444
core_pubmed_pmc
Evaluation of Different Initial Doses of Envarsus in De Novo Kidney Transplant Recipients
Evaluation of Different Initial Doses of Envarsus in De Novo Kidney Transplant Recipients Abstract Abstract Background/Objectives : Envarsus is a novel prolonged-release formulation of tacrolimus with enhanced bioavailability. The summary of product characteristics recommends an initial dose of 0.17 mg/kg/day for the p...
PMC8445944
core_pubmed_pmc
Azithromycin concentrations during long-term regimen, a pilot study in patients with MALT lymphoma
Azithromycin concentrations during long-term regimen, a pilot study in patients with MALT lymphoma Abstract In view of the antineoplastic effects of the macrolide clarithromycin in mucosa associated lymphatic tissue (MALT)-lymphoma, we performed a pilot study assessing levels of azithromycin in plasma, peripheral blood...
PMC6931142
core_pubmed_pmc
Interaction of Selected Terpenoids From Dalbergia sissoo With Catalytic Domain of Matrix Metalloproteinase-1: An In Silico Assessment of Their Anti-wrinkling Potential
Interaction of Selected Terpenoids From Dalbergia sissoo With Catalytic Domain of Matrix Metalloproteinase-1: An In Silico Assessment of Their Anti-wrinkling Potential Abstract Abstract Matrix metalloproteinase-1 (MMP-1) is a predominant collagenase enzyme that cleaves collagen fibers, contributing to skin wrinkling. M...
PMC3912353
core_pubmed_pmc
Pharmacokinetics of bevacizumab after topical and intravitreal administration in human eyes
Pharmacokinetics of bevacizumab after topical and intravitreal administration in human eyes Abstract Abstract Background Topical bevacizumab is a potential treatment modality for corneal neovascularization, and several recent studies have demonstrated its efficacy. No previous study of the pharmacokinetics of topical b...
PMC7922275
core_pubmed_pmc
A Phase II Study Demonstrates No Feasibility of Adjuvant Treatment with Six Cycles of S-1 and Oxaliplatin in Resectable Esophageal Adenocarcinoma, with ERCC1 as Biomarker for Response to SOX
A Phase II Study Demonstrates No Feasibility of Adjuvant Treatment with Six Cycles of S-1 and Oxaliplatin in Resectable Esophageal Adenocarcinoma, with ERCC1 as Biomarker for Response to SOX Abstract Abstract Simple Summary Neoadjuvant chemoradiotherapy followed by surgery is currently standard of care in esophageal ad...
PMC10267184
core_pubmed_pmc
Immunological evaluation of herbal extracts commonly used for treatment of mental diseases during pregnancy
Immunological evaluation of herbal extracts commonly used for treatment of mental diseases during pregnancy Abstract Abstract Nonpsychotic mental diseases (NMDs) affect approximately 15% of pregnant women in the US. Herbal preparations are perceived a safe alternative to placenta-crossing antidepressants or benzodiazep...
PMC6825643
core_pubmed_pmc
Benefit:Risk Profile of Budesonide in Obstructive Airways Disease
Benefit:Risk Profile of Budesonide in Obstructive Airways Disease Abstract Abstract Airway inflammation is a major contributing factor in both asthma and chronic obstructive pulmonary disease (COPD) and represents an important target for treatment. Inhaled corticosteroids (ICS) as monotherapy or in combination therapy ...
PMC6824364
core_pubmed_pmc
Differentiating Basal Insulin Preparations: Understanding How They Work Explains Why They Are Different
Differentiating Basal Insulin Preparations: Understanding How They Work Explains Why They Are Different Abstract Since the introduction of insulin as a life-saving agent for patients with type 1 diabetes, insulin preparations have evolved to approximate physiologic insulin delivery profiles to meet prandial and basal i...
PMC8920379
core_pubmed_pmc
The discovery of berberine erythrocyte-hemoglobin self-assembly delivery system: a neglected carrier underlying its pharmacokinetics
The discovery of berberine erythrocyte-hemoglobin self-assembly delivery system: a neglected carrier underlying its pharmacokinetics Abstract Abstract Berberine (BBR) has extremely low concentration and high tissue distribution. However, current pharmacokinetic studies predominantly focus on its concentration in plasma...
PMC7200768
core_pubmed_pmc
Evidence mapping of interactions on concomitant use of Chinese medicine and platinum-based chemotherapy: a scoping review protocol
Evidence mapping of interactions on concomitant use of Chinese medicine and platinum-based chemotherapy: a scoping review protocol Abstract Abstract Background The utilization of Chinese herbal medicine (CHM) has gained popularity and acceptance worldwide. Increasing use of CHM either as a stand-alone or an adjunctive ...
PMC12783389
core_pubmed_pmc
Microbiological, Clinical, and Pharmacokinetic/Pharmacodynamic Data to Support EUCAST Aztreonam–Avibactam Minimum Inhibitory Concentration Susceptibility Breakpoints Against Enterobacterales
Microbiological, Clinical, and Pharmacokinetic/Pharmacodynamic Data to Support EUCAST Aztreonam–Avibactam Minimum Inhibitory Concentration Susceptibility Breakpoints Against Enterobacterales Abstract Abstract Introduction Aztreonam–avibactam was approved for adults with limited treatment options for multiple infections...
PMC7557955
core_pubmed_pmc
Evaluation of the Pharmacokinetic Drug–Drug Interaction between Micronized Fenofibrate and Pitavastatin in Healthy Volunteers
Evaluation of the Pharmacokinetic Drug–Drug Interaction between Micronized Fenofibrate and Pitavastatin in Healthy Volunteers Abstract Dyslipidemia is a major risk factor for development of atherosclerosis and cardiovascular disease (CVD). Effective lipid-lowering therapies has led to CVD risk reduction. This study eva...
PMC9218519
core_pubmed_pmc
Pharmacokinetics of extrafine beclometasone dipropionate/formoterol fumarate/glycopyrronium bromide in adolescent and adult patients with asthma
Pharmacokinetics of extrafine beclometasone dipropionate/formoterol fumarate/glycopyrronium bromide in adolescent and adult patients with asthma Abstract Abstract The single‐inhaler extrafine formulation triple combination beclometasone dipropionate (BDP), formoterol fumarate (FF) plus glycopyrronium bromide (GB) is av...
PMC11242565
core_pubmed_pmc
A New Application for Cenicriviroc, a Dual CCR2/CCR5 Antagonist, in the Treatment of Painful Diabetic Neuropathy in a Mouse Model
A New Application for Cenicriviroc, a Dual CCR2/CCR5 Antagonist, in the Treatment of Painful Diabetic Neuropathy in a Mouse Model Abstract Abstract The ligands of chemokine receptors 2 and 5 (CCR2 and CCR5, respectively) are associated with the pathomechanism of neuropathic pain development, but their role in painful d...
PMC11126565
core_pubmed_pmc
Systemic exposure to aflibercept after intravitreal injection in premature neonates with retinopathy of prematurity: results from the FIREFLEYE randomized phase 3 study
Systemic exposure to aflibercept after intravitreal injection in premature neonates with retinopathy of prematurity: results from the FIREFLEYE randomized phase 3 study Abstract Abstract Background There are no data on pharmacokinetics, pharmacodynamics, and immunogenicity of intravitreal aflibercept in preterm infants...
PMC5149013
core_pubmed_pmc
Preparation, Properties and Preclinical Pharmacokinetics of Low Molecular Weight Heparin-modified Isoliquiritigenin-loaded Solid Lipid Nanoparticle
Preparation, Properties and Preclinical Pharmacokinetics of Low Molecular Weight Heparin-modified Isoliquiritigenin-loaded Solid Lipid Nanoparticle Abstract Abstract Low molecular weight heparin-modified isoliquiritigenin-loaded solid lipid nanoparticle (LMWH-ISL-SLN) was developed for injective application. The morpho...
PMC5089614
core_pubmed_pmc
Pharmacokinetics of ixazomib, an oral proteasome inhibitor, in solid tumour patients with moderate or severe hepatic impairment
Pharmacokinetics of ixazomib, an oral proteasome inhibitor, in solid tumour patients with moderate or severe hepatic impairment Abstract Aim The aim of the present study was to characterize the pharmacokinetics of the oral proteasome inhibitor, ixazomib, in patients with solid tumours and moderate or severe hepatic imp...
PMC12565818
core_pubmed_pmc
Therapeutic Repurposing of Sertraline: Evidence for Its Antifungal Activity from In Vitro, In Vivo, and Clinical Studies
Therapeutic Repurposing of Sertraline: Evidence for Its Antifungal Activity from In Vitro, In Vivo, and Clinical Studies Abstract Sertraline, a selective serotonin reuptake inhibitor (SSRI), has emerged as a candidate for therapeutic repurposing due to its reported antifungal activity. We systematically reviewed in vit...
PMC10719466
core_pubmed_pmc
Vericiguat, a novel sGC stimulator: Mechanism of action, clinical, and translational science
Vericiguat, a novel sGC stimulator: Mechanism of action, clinical, and translational science Abstract Abstract Vericiguat, a novel soluble guanylate cyclase (sGC) stimulator, is approved for the treatment of heart failure (HF) with reduced ejection fraction (HFrEF). Decreased nitric oxide (NO) availability, sGC desensi...
PMC10338388
core_pubmed_pmc
A Population Pharmacokinetic Model of Pentobarbital for Children with Status Epilepticus and Severe Traumatic Brain Injury
A Population Pharmacokinetic Model of Pentobarbital for Children with Status Epilepticus and Severe Traumatic Brain Injury Abstract Background Pentobarbital pharmacokinetics (PK) remain elusive and the therapeutic windows narrow. Administration is frequent in critically ill children with refractory status epilepticus (...
PMC11022729
core_pubmed_pmc
Discovery of a Small Molecule Activator of Slack (Kcnt1) Potassium Channels That Significantly Reduces Scratching in Mouse Models of Histamine‐Independent and Chronic Itch
Discovery of a Small Molecule Activator of Slack (Kcnt1) Potassium Channels That Significantly Reduces Scratching in Mouse Models of Histamine‐Independent and Chronic Itch Abstract Abstract Various disorders are accompanied by histamine‐independent itching, which is often resistant to the currently available therapies....
PMC4422947
core_pubmed_pmc
Methylation and its role in the disposition of tanshinol, a cardiovascular carboxylic catechol from Salvia miltiorrhiza roots (Danshen)
Methylation and its role in the disposition of tanshinol, a cardiovascular carboxylic catechol from Salvia miltiorrhiza roots (Danshen) Abstract Aim: Tanshinol is an important catechol in the antianginal herb Salvia miltiorrhiza roots (Danshen). This study aimed to characterize tanshinol methylation. Methods: Metabolit...
PMC4350608
core_pubmed_pmc
Dendrimer Nanocarriers for Transport Modulation Across Models of the Pulmonary Epithelium
Dendrimer Nanocarriers for Transport Modulation Across Models of the Pulmonary Epithelium Abstract The purpose of this study was to determine the effect of PEGylation on the interaction of poly(amidoamine) (PAMAM) dendrimer nanocarriers (DNCs) with in vitro and in vivo models of the pulmonary epithelium. Generation-3 P...
PMC12660627
core_pubmed_pmc
LC-MS/MS Method Validation for Quantification of Nirmatrelvir in Human Plasma
LC-MS/MS Method Validation for Quantification of Nirmatrelvir in Human Plasma Abstract Abstract Nirmatrelvir, a key antiviral agent in the treatment of COVID-19, requires accurate and reliable monitoring of drug levels to optimize therapeutic efficacy. In this study, we developed and validated a sensitive and specific ...
PMC11424990
core_pubmed_pmc
Population Pharmacokinetics of Dolutegravir in African Children: Results From the CHAPAS-4 Trial
Population Pharmacokinetics of Dolutegravir in African Children: Results From the CHAPAS-4 Trial Abstract Abstract We characterized population pharmacokinetics in 42 African children receiving once-daily 25 mg (14 to <20 kg) or 50 mg (>20 kg) dolutegravir. Coadministration with emtricitabine and tenofovir alafenamide r...
PMC12888851
core_pubmed_pmc
A mechanism-based pharmacokinetic/pharmacodynamic analysis of polymyxin B-based combination therapy against carbapenem-resistant Klebsiella pneumoniae isolates with diverse phenotypic and genotypic resistance mechanisms
A mechanism-based pharmacokinetic/pharmacodynamic analysis of polymyxin B-based combination therapy against carbapenem-resistant Klebsiella pneumoniae isolates with diverse phenotypic and genotypic resistance mechanisms Abstract ABSTRACT Increased resistance to β-lactams/β-lactamase inhibitors by mutations in β-lactama...
PMC10201013
core_pubmed_pmc
Remifentanil does not affect human microglial immune activation in response to pro-inflammatory cytokines
Remifentanil does not affect human microglial immune activation in response to pro-inflammatory cytokines Abstract Abstract Remifentanil is a potent ultra-short acting μ-opioid analgesic drug, frequently used in anaesthesia due to its favorable pharmacodynamic and pharmacokinetic profile. It may be associated with the ...
PMC9686516
core_pubmed_pmc
Pharmacokinetic Characteristics of Nebulized Colistimethate Sodium Using Two Different Types of Nebulizers in Critically Ill Patients with Ventilator-Associated Respiratory Infections
Pharmacokinetic Characteristics of Nebulized Colistimethate Sodium Using Two Different Types of Nebulizers in Critically Ill Patients with Ventilator-Associated Respiratory Infections Abstract Background: Rising antimicrobial resistance has led to a revived interest in inhaled colistin treatment in the critically ill p...
PMC12297955
core_pubmed_pmc
Comparative Study: Biguanide-, Sulfonamide-, and Natural Agent-Based Interventions in an In Vivo Experimental Diabetes Model
Comparative Study: Biguanide-, Sulfonamide-, and Natural Agent-Based Interventions in an In Vivo Experimental Diabetes Model Abstract Background/Objectives: In the context of diabetes, a multifactorial metabolic disorder with significant clinical implications, the present study investigates the hypoglycemic effects of ...
PMC5625161
core_pubmed_pmc
Mechanistic in vitro studies confirm that inhibition of the renal apical efflux transporter multidrug and toxin extrusion ( MATE ) 1, and not altered absorption, underlies the increased metformin exposure observed in clinical interactions with cimetidine, trimethoprim or pyrimethamine
Mechanistic in vitro studies confirm that inhibition of the renal apical efflux transporter multidrug and toxin extrusion ( MATE ) 1, and not altered absorption, underlies the increased metformin exposure observed in clinical interactions with cimetidine, trimethoprim or pyrimethamine Abstract Abstract Metformin is a c...
PMC3570248
core_pubmed_pmc
Development and validation of a HPLC-MS/MS method with electrospray ionization for quantitation of potassium oxonate in human plasma: Application to a pharmacokinetic study
Development and validation of a HPLC-MS/MS method with electrospray ionization for quantitation of potassium oxonate in human plasma: Application to a pharmacokinetic study Abstract Abstract A rapid, sensitive and specific HPLC-MS/MS method was developed and validated for the quantification of potassium oxonate (Oxo) i...
PMC9527281
core_pubmed_pmc
Comparative pharmacokinetic study of the five anti-inflammatory active ingredients of Inula cappa in a normal and an LPS-induced inflammatory cell model
Comparative pharmacokinetic study of the five anti-inflammatory active ingredients of Inula cappa in a normal and an LPS-induced inflammatory cell model Abstract Inula cappa is a commonly used medicine in the Miao area of Guizhou Province in China. We established an in vitro inflammatory model of mouse macrophage RAW26...
PMC11319711
core_pubmed_pmc
A Bayesian framework for virtual comparative trials and bioequivalence assessments
A Bayesian framework for virtual comparative trials and bioequivalence assessments Abstract Abstract Introduction In virtual bioequivalence (VBE) assessments, pharmacokinetic models informed with in vitro data and verified with small clinical trials’ data are used to simulate otherwise unfeasibly large trials. Simulate...
PMC3124128
core_pubmed_pmc
Pharmacokinetics of p -Aminohippuric Acid and Inulin in Rabbits with Aristolochic Acid Nephropathy
Pharmacokinetics of p -Aminohippuric Acid and Inulin in Rabbits with Aristolochic Acid Nephropathy Abstract The characteristics of aristolochic acid nephropathy (AAN) are interstitial fibrosis and atrophy of the proximal tubules, but with no change in glomeruli. To investigate the effects of AA on renal functions and t...
PMC3570332
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic analysis of 5-aza-2’-deoxycytidine (decitabine) in the design of its dose-schedule for cancer therapy
Pharmacokinetic and pharmacodynamic analysis of 5-aza-2’-deoxycytidine (decitabine) in the design of its dose-schedule for cancer therapy Abstract Abstract 5-Aza-2′-deoxycytidine (5-AZA-CdR, decitabine), an epigenetic drug that inhibits DNA methylation, is currently used to treat myelodysplastic syndrome (MDS), and is ...
PMC10982100
core_pubmed_pmc
Low-dimensional neural ODEs and their application in pharmacokinetics
Low-dimensional neural ODEs and their application in pharmacokinetics Abstract Machine Learning (ML) is a fast-evolving field, integrated in many of today’s scientific disciplines. With the recent development of neural ordinary differential equations (NODEs), ML provides a new tool to model dynamical systems in the fie...
PMC11368979
core_pubmed_pmc
Pre-therapy PET-based voxel-wise dosimetry prediction by characterizing intra-organ heterogeneity in PSMA-directed radiopharmaceutical theranostics
Pre-therapy PET-based voxel-wise dosimetry prediction by characterizing intra-organ heterogeneity in PSMA-directed radiopharmaceutical theranostics Abstract Background and objective Treatment planning through the diagnostic dimension of theranostics provides insights into predicting the absorbed dose of RPT, with the p...
PMC5328510
core_pubmed_pmc
The Oral β-Lactamase SYN-004 (Ribaxamase) Degrades Ceftriaxone Excreted into the Intestine in Phase 2a Clinical Studies
The Oral β-Lactamase SYN-004 (Ribaxamase) Degrades Ceftriaxone Excreted into the Intestine in Phase 2a Clinical Studies Abstract ABSTRACT SYN-004 (ribaxamase) is a β-lactamase designed to be orally administered concurrently with intravenous β-lactam antibiotics, including most penicillins and cephalosporins. Ribaxamase...
PMC11334417
core_pubmed_pmc
Clopidogrel-Mediated P2Y 12 Inhibition According to Renal Function in Patients With Diabetes Mellitus and CAD
Clopidogrel-Mediated P2Y 12 Inhibition According to Renal Function in Patients With Diabetes Mellitus and CAD Abstract Highlights • Patients with DM have impaired clopidogrel-mediated platelet P2Y12 inhibition, exacerbated if CKD is present. • Potential mechanism(s) include altered drug absorption and/or metabolism and...
PMC12566766
core_pubmed_pmc
Development of Practical Low-Volume Screening Method and Pharmacokinetic Simulation of Levofloxacin-Loaded Nanofiber Inserts for Sustained Ocular Therapy
Development of Practical Low-Volume Screening Method and Pharmacokinetic Simulation of Levofloxacin-Loaded Nanofiber Inserts for Sustained Ocular Therapy Abstract Background / Objectives : Ocular drug delivery faces significant challenges due to anatomical and physiological barriers that limit drug bioavailability, par...
PMC5225185
core_pubmed_pmc
A pharmacokinetic study of lipegfilgrastim in children with Ewing family of tumors or rhabdomyosarcoma
A pharmacokinetic study of lipegfilgrastim in children with Ewing family of tumors or rhabdomyosarcoma Abstract Purpose Neutropenia is a common complication from chemotherapy, limiting optimal dosing and treatment. Lipegfilgrastim is a long-acting granulocyte colony-stimulating factor developed for the management of ch...
PMC8121438
core_pubmed_pmc
Efficacy, pharmacokinetics and safety of subcutaneous versus intravenous CT-P13 in rheumatoid arthritis: a randomized phase I/III trial
Efficacy, pharmacokinetics and safety of subcutaneous versus intravenous CT-P13 in rheumatoid arthritis: a randomized phase I/III trial Abstract Abstract Objective To assess non-inferiority of s.c. to i.v. CT-P13 in RA. Methods Patients with active RA and inadequate response to MTX participated in this phase I/III doub...
PMC5865368
core_pubmed_pmc
Population pharmacokinetic and pharmacodynamic properties of artesunate in patients with artemisinin sensitive and resistant infections in Southern Myanmar
Population pharmacokinetic and pharmacodynamic properties of artesunate in patients with artemisinin sensitive and resistant infections in Southern Myanmar Abstract Abstract Background Artemisinins are the most effective anti-malarial drugs for uncomplicated and severe Plasmodium falciparum malaria. However, widespread...
PMC10432633
core_pubmed_pmc
CLN-978, a novel half-life extended CD19/CD3/HSA-specific T cell-engaging antibody construct with potent activity against B-cell malignancies with low CD19 expression
CLN-978, a novel half-life extended CD19/CD3/HSA-specific T cell-engaging antibody construct with potent activity against B-cell malignancies with low CD19 expression Abstract Abstract Background Despite significant progress in the development of T cell-engaging therapies for various B-cell malignancies, a high medical...
PMC4449939
core_pubmed_pmc
Pharmacokinetic Study and Optimal Formulation of New Anti-Parkinson Natural Compound Schisantherin A
Pharmacokinetic Study and Optimal Formulation of New Anti-Parkinson Natural Compound Schisantherin A Abstract Abstract Our recent studies showed that schisantherin A (StA) is a promising candidate for PD treatment, but the pharmacokinetic profile of StA is largely unknown. The effects of different formulations on the p...
PMC4878309
core_pubmed_pmc
Development of Immunoassays for the Quantitative Assessment of Amyloid-β in the Presence of Therapeutic Antibody: Application to Pre-Clinical Studies
Development of Immunoassays for the Quantitative Assessment of Amyloid-β in the Presence of Therapeutic Antibody: Application to Pre-Clinical Studies Abstract Abstract Utilizing decision making biomarkers in drug development requires thorough assay validation. Special considerations need to be taken into account when m...
PMC4879391
core_pubmed_pmc
Linking Murine and Human Plasmodium falciparum Challenge Models in a Translational Path for Antimalarial Drug Development
Linking Murine and Human Plasmodium falciparum Challenge Models in a Translational Path for Antimalarial Drug Development Abstract Abstract Effective progression of candidate antimalarials is dependent on optimal dosing in clinical studies, which is determined by a sound understanding of pharmacokinetics and pharmacody...
PMC9249726
core_pubmed_pmc
Single-Dose Pharmacokinetics of Milvexian in Participants with Mild or Moderate Hepatic Impairment Compared with Healthy Participants
Single-Dose Pharmacokinetics of Milvexian in Participants with Mild or Moderate Hepatic Impairment Compared with Healthy Participants Abstract Background Patients with hepatic impairment receiving antithrombotic agents metabolized primarily through the liver can be at risk for bleeding. Milvexian (BMS-986177/JNJ-700330...
PMC8904565
core_pubmed_pmc
Phytochemical Delivery Through Transferosome (Phytosome): An Advanced Transdermal Drug Delivery for Complementary Medicines
Phytochemical Delivery Through Transferosome (Phytosome): An Advanced Transdermal Drug Delivery for Complementary Medicines Abstract Abstract Transdermal drug delivery aims to create a safe and effective method of administering drugs through the skin that attracts a lot of attention and investment due to the constant p...
PMC12495633
core_pubmed_pmc
First therapeutic drug monitoring of experimental favipiravir in Borna disease virus 1 (BoDV-1) encephalitis patients reveals significant gaps in antiviral treatment: a pilot investigation
First therapeutic drug monitoring of experimental favipiravir in Borna disease virus 1 (BoDV-1) encephalitis patients reveals significant gaps in antiviral treatment: a pilot investigation Abstract Abstract Background The Borna disease virus 1 (BoDV-1) causes a rare, but severe form of encephalitis in Germany, characte...
PMC11730311
core_pubmed_pmc
Pipeline for development of acylated peptide based CGRP receptor antagonist with extended half-life for migraine treatment
Pipeline for development of acylated peptide based CGRP receptor antagonist with extended half-life for migraine treatment Abstract Abstract Migraine is a debilitating headache disorder. The disease has neurovascular origin and migraine attacks can be elicited by vasodilative neuropeptides such as alpha calcitonin gene...
PMC10536696
core_pubmed_pmc
Population pharmacokinetic analysis of lopinavir in HIV negative individuals exposed to SARS-CoV-2: a COPEP (COronavirus Post-Exposure Prophylaxis) sub-study
Population pharmacokinetic analysis of lopinavir in HIV negative individuals exposed to SARS-CoV-2: a COPEP (COronavirus Post-Exposure Prophylaxis) sub-study Abstract Background Lopinavir/ritonavir (LPV/r) is a drug traditionally used for the treatment of HIV that has been repurposed as a potential post-exposure prophy...
PMC8807508
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling in Pregnant Women Suggests Minor Decrease in Maternal Exposure to Olanzapine
Physiologically Based Pharmacokinetic Modeling in Pregnant Women Suggests Minor Decrease in Maternal Exposure to Olanzapine Abstract Abstract Pregnancy is accompanied by significant physiological changes that might affect the in vivo drug disposition. Olanzapine is prescribed to pregnant women with schizophrenia, while...
PMC12049548
core_pubmed_pmc
Designing and characterizing first Iranian study evaluating serum levels of lithium in patients for population pharmacokinetics (FIRELOLIPOP): baseline and first report
Designing and characterizing first Iranian study evaluating serum levels of lithium in patients for population pharmacokinetics (FIRELOLIPOP): baseline and first report Abstract Bipolar disorder (BD) is a chronic psychiatric illness characterized by recurrent manic and depressive episodes, leading to significant impair...
PMC9306536
core_pubmed_pmc
Population Pharmacokinetics Analysis of Pemigatinib in Patients With Advanced Malignancies
Population Pharmacokinetics Analysis of Pemigatinib in Patients With Advanced Malignancies Abstract Abstract Pemigatinib is a fibroblast growth factor receptor 1–3 inhibitor used to treat cholangiocarcinoma. A compartmental population pharmacokinetics model was developed using data from 318 patients with cancer enrolle...
PMC9681907
core_pubmed_pmc
Prospective population pharmacokinetic study of tacrolimus in adult recipients early after liver transplantation: A comparison of Michaelis-Menten and theory-based pharmacokinetic models
Prospective population pharmacokinetic study of tacrolimus in adult recipients early after liver transplantation: A comparison of Michaelis-Menten and theory-based pharmacokinetic models Abstract Abstract Background and Objective: Tacrolimus, a calcineurin inhibitor widely used as a potent immunosuppressant to prevent ...
PMC11893724
core_pubmed_pmc
Japanese Phase 1 Study for Global Development of Anti‐ TL1A Antibody PF ‐06480605: A Randomized, Placebo‐Controlled, Single‐Ascending Dose Study
Japanese Phase 1 Study for Global Development of Anti‐ TL1A Antibody PF ‐06480605: A Randomized, Placebo‐Controlled, Single‐Ascending Dose Study Abstract ABSTRACT PF‐06480605, a fully human IgG1 monoclonal antibody targeting tumor necrosis factor α‐like ligand 1A (TL1A), has demonstrated acceptable safety and the poten...
PMC6528385
core_pubmed_pmc
A PK/PD study comparing twice-daily to once-daily dosing regimens of ertugliflozin in healthy subjects
A PK/PD study comparing twice-daily to once-daily dosing regimens of ertugliflozin in healthy subjects Abstract Abstract Objective: Ertugliflozin is approved in the US and European Union as a stand-alone product for adults with type 2 diabetes mellitus as once daily (QD) dosing. The approved fixed-dose combination (FDC...
PMC7300789
core_pubmed_pmc
Predictions of Systemic, Intracellular, and Lung Concentrations of Azithromycin With Different Dosing Regimens Used in COVID‐19 Clinical Trials
Predictions of Systemic, Intracellular, and Lung Concentrations of Azithromycin With Different Dosing Regimens Used in COVID‐19 Clinical Trials Abstract Abstract Azithromycin (AZ), a broad‐spectrum macrolide antibiotic, is being investigated in patients with coronavirus disease 2019 (COVID‐19). A population pharmacokin...
PMC12567466
core_pubmed_pmc
Pregabalin and Duloxetine in Patients with Non-Nociceptive Pain: A Narrative Review Exploring the Pharmacological Effects of This Combination
Pregabalin and Duloxetine in Patients with Non-Nociceptive Pain: A Narrative Review Exploring the Pharmacological Effects of This Combination Abstract Both neuropathic and nociplastic pain (non-nociceptive pain) are characterized by a similar pattern of clinical symptoms, including numbness, dysesthesia, tingling, and ...
PMC10056008
core_pubmed_pmc
Effects of Simvastatin on Pharmacokinetics and Anticoagulant Effects of Dabigatran in Healthy Subjects
Effects of Simvastatin on Pharmacokinetics and Anticoagulant Effects of Dabigatran in Healthy Subjects Abstract Higher risk of major hemorrhage associated with concomitant use of dabigatran and simvastatin compared to other statins was previously reported with a suggestion of P-glycoprotein-mediated interaction. The ai...
PMC7749516
core_pubmed_pmc
Safety and nonclinical and clinical pharmacokinetics of PC945, a novel inhaled triazole antifungal agent
Safety and nonclinical and clinical pharmacokinetics of PC945, a novel inhaled triazole antifungal agent Abstract Abstract PC945 is a novel antifungal triazole formulated for nebulized delivery to treat lung Aspergillus infections. Pharmacokinetic and safety profiles from nonclinical studies and clinical trials in heal...
PMC12734456
core_pubmed_pmc
Study on Stability of Remifentanil, Sufentanil, and Their Metabolites in Human Whole Blood and Urine
Study on Stability of Remifentanil, Sufentanil, and Their Metabolites in Human Whole Blood and Urine Abstract Abstract Background: The accurate detection of remifentanil and sufentanil in biological samples is challenged by their rapid metabolism and instability, complicating clinical and forensic toxicology analysis. ...
PMC9025232
core_pubmed_pmc
Defining the Role of Isoeugenol from Ocimum tenuiflorum against Diabetes Mellitus-Linked Alzheimer’s Disease through Network Pharmacology and Computational Methods
Defining the Role of Isoeugenol from Ocimum tenuiflorum against Diabetes Mellitus-Linked Alzheimer’s Disease through Network Pharmacology and Computational Methods Abstract The present study involves the integrated network pharmacology and phytoinformatics-based investigation of phytocompounds from Ocimum tenuiflorum a...
PMC12467374
core_pubmed_pmc
Pharmacokinetics of Novel Crystalline Buntanetap in Mice, Dogs, and Humans
Pharmacokinetics of Novel Crystalline Buntanetap in Mice, Dogs, and Humans Abstract Buntanetap is an orally bioavailable small molecule that has been shown to improve cognitive function in patients with Alzheimer’s and Parkinson’s diseases and holds promise for use in other neurodegenerative conditions. Until now, a cr...
PMC7279352
core_pubmed_pmc
In Silico Prediction of Intestinal Permeability by Hierarchical Support Vector Regression
In Silico Prediction of Intestinal Permeability by Hierarchical Support Vector Regression Abstract Abstract The vast majority of marketed drugs are orally administrated. As such, drug absorption is one of the important drug metabolism and pharmacokinetics parameters that should be assessed in the process of drug discov...
PMC11064505
core_pubmed_pmc
A nanochitosan-D-galactose formulation increases the accumulation of primaquine in the liver
A nanochitosan-D-galactose formulation increases the accumulation of primaquine in the liver Abstract ABSTRACT Primaquine is the mainstream antimalarial drug to prevent Plasmodium vivax relapses. However, this drug can induce hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency. Nanostructure formula...
PMC3117577
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic drug interactions of carbamazepine and glibenclamide in healthy albino Wistar rats
Pharmacokinetic and pharmacodynamic drug interactions of carbamazepine and glibenclamide in healthy albino Wistar rats Abstract Abstract Aims: To find out the pharmacokinetic and pharmacodynamic drug interaction of carbamazepine, a protype drug used to treat painful diabetic neuropathy with glibenclamide in healthy alb...
PMC10653753
core_pubmed_pmc
The 8-bromobaicalein alleviated chikungunya-induced musculoskeletal inflammation and reduced the viral load in healthy adult mice
The 8-bromobaicalein alleviated chikungunya-induced musculoskeletal inflammation and reduced the viral load in healthy adult mice Abstract ABSTRACT Chikungunya virus is a re-emerging arbovirus that has caused epidemic outbreaks in recent decades. Patients in older age groups with high viral load and severe immunologic ...
PMC12887120
core_pubmed_pmc
Acute postoperative pain control in pediatric patients: a scoping review
Acute postoperative pain control in pediatric patients: a scoping review Abstract Abstract Acute postoperative pain results from tissue injury during surgery and subsequent inflammatory responses. The incidence of chronic postsurgical pain ranges from 10% to 30%, and its development is influenced by various clinical fa...
PMC6421934
core_pubmed_pmc
Association Study Among Candidate Genetic Polymorphisms and Chemotherapy-Related Severe Toxicity in Testicular Cancer Patients
Association Study Among Candidate Genetic Polymorphisms and Chemotherapy-Related Severe Toxicity in Testicular Cancer Patients Abstract Abstract Testicular cancer is one of the most commonly occurring malignant tumors in young men with fourfold higher rate of incidence and threefold higher mortality rates in Chile than...
PMC8314177
core_pubmed_pmc
Pharmacokinetics, Urinary Excretion, and Pharmaco-Metabolomic Study of Tebipenem Pivoxil Granules After Single Escalating Oral Dose in Healthy Chinese Volunteers
Pharmacokinetics, Urinary Excretion, and Pharmaco-Metabolomic Study of Tebipenem Pivoxil Granules After Single Escalating Oral Dose in Healthy Chinese Volunteers Abstract Abstract Tebipenem pivoxil (TBPM-PI), an oral carbapenem antibiotic, has shown special advantages in pediatric infections and was in urgent need in C...
PMC5985852
core_pubmed_pmc
Echinocandins for management of invasive candidiasis in patients with liver disease and liver transplantation
Echinocandins for management of invasive candidiasis in patients with liver disease and liver transplantation Abstract Abstract Candida species remains one of the most important causes of opportunistic infections worldwide. Invasive candidiasis (IC) is associated with considerable morbidity and mortality in liver disea...
PMC8103752
core_pubmed_pmc
A Phase 1 dose-escalation study of disulfiram and copper gluconate in patients with advanced solid tumors involving the liver using S-glutathionylation as a biomarker
A Phase 1 dose-escalation study of disulfiram and copper gluconate in patients with advanced solid tumors involving the liver using S-glutathionylation as a biomarker Abstract Background Disulfiram and metals inactivate key oncoproteins resulting in anti-neoplastic activity. The goal of this study was to determine the ...
PMC4237505
core_pubmed_pmc
Effects of a protein-rich drink or a standard meal on the pharmacokinetics of elvitegravir, cobicistat, emtricitabine and tenofovir in healthy Japanese male subjects: A randomized, three-way crossover study
Effects of a protein-rich drink or a standard meal on the pharmacokinetics of elvitegravir, cobicistat, emtricitabine and tenofovir in healthy Japanese male subjects: A randomized, three-way crossover study Abstract Abstract This study investigated the effects of ingested food types on the pharmacokinetics of elvitegra...
PMC4070517
core_pubmed_pmc
Muscle-Based Pharmacokinetic Modeling of Marrow Perfusion for Osteoporotic Bone in Females
Muscle-Based Pharmacokinetic Modeling of Marrow Perfusion for Osteoporotic Bone in Females Abstract The pharmacokinetic model has been widely used in tissue perfusion analysis, such as bone marrow perfusion. In the modeling process, the arterial input function is important to guarantee the reliability of the fitting re...
PMC9988422
core_pubmed_pmc
Usefulness of a humanized tricellular static transwell blood–brain barrier model as a microphysiological system for drug development applications. - A case study based on the benchmark evaluations of blood-brain barrier microphysiological system
Usefulness of a humanized tricellular static transwell blood–brain barrier model as a microphysiological system for drug development applications. - A case study based on the benchmark evaluations of blood-brain barrier microphysiological system Abstract Microphysiological system (MPS), a new technology for in vitro te...
PMC10339701
core_pubmed_pmc
Model‐informed approach to support pediatric dosing for the pan‐PI3K inhibitor copanlisib in children and adolescents with relapsed/refractory solid tumors
Model‐informed approach to support pediatric dosing for the pan‐PI3K inhibitor copanlisib in children and adolescents with relapsed/refractory solid tumors Abstract Abstract Copanlisib is an intravenously administered phosphatidylinositol 3‐kinase (PI3K) inhibitor which was investigated in pediatric patients with relap...
PMC9495161
core_pubmed_pmc
Phytochemical Profiling, In Vitro Biological Activities, and In-Silico Studies of Ficus vasta Forssk. : An Unexplored Plant
Phytochemical Profiling, In Vitro Biological Activities, and In-Silico Studies of Ficus vasta Forssk. : An Unexplored Plant Abstract Ficus vasta Forssk. (Moraceae family) is an important medicinal plant that has not been previously investigated for its phytochemical and biological potential. Phytochemical screening, to...
PMC6572397
core_pubmed_pmc
Systemic Design and Evaluation of Ticagrelor-Loaded Nanostructured Lipid Carriers for Enhancing Bioavailability and Antiplatelet Activity
Systemic Design and Evaluation of Ticagrelor-Loaded Nanostructured Lipid Carriers for Enhancing Bioavailability and Antiplatelet Activity Abstract Abstract Ticagrelor (TGL), a P2Y 12 receptor antagonist, is classified as biopharmaceutics classification system (BCS) class IV drug due to its poor solubility and permeabil...
PMC9622937
core_pubmed_pmc
Minocycline intra-bacterial pharmacokinetic hysteresis as a basis for pharmacologic memory and a backbone for once-a-week pan-tuberculosis therapy
Minocycline intra-bacterial pharmacokinetic hysteresis as a basis for pharmacologic memory and a backbone for once-a-week pan-tuberculosis therapy Abstract Background: There is need for shorter duration regimens for the treatment of tuberculosis , that can treat patients regardless of multidrug resistance status (pan-t...
PMC12402879
core_pubmed_pmc
Microtracer‐Based Assessment of the Mass Balance, Pharmacokinetics, and Excretion of [ 14 C]Berzosertib, an Intravenous ATR Inhibitor, in Patients With Advanced Solid Tumors: A Phase 1 Study
Microtracer‐Based Assessment of the Mass Balance, Pharmacokinetics, and Excretion of [ 14 C]Berzosertib, an Intravenous ATR Inhibitor, in Patients With Advanced Solid Tumors: A Phase 1 Study Abstract Abstract Berzosertib is a small‐molecule ataxia telangiectasia and Rad3‐related protein inhibitor. To assess the clearan...
PMC6222828
core_pubmed_pmc
Synthesis of Gemcitabine-Threonine Amide Prodrug Effective on Pancreatic Cancer Cells with Improved Pharmacokinetic Properties
Synthesis of Gemcitabine-Threonine Amide Prodrug Effective on Pancreatic Cancer Cells with Improved Pharmacokinetic Properties Abstract Abstract To investigate the amino acid transporter-based prodrug anticancer strategy further, several amino acid-conjugated amide gemcitabine prodrugs were synthesized to target amino ...
PMC12396236
core_pubmed_pmc
Effect of Gene Polymorphism on the Pharmacokinetics and Clinical Outcomes of Rivaroxaban: State-of-the-Art Review
Effect of Gene Polymorphism on the Pharmacokinetics and Clinical Outcomes of Rivaroxaban: State-of-the-Art Review Abstract Abstract Rivaroxaban is a direct oral anticoagulant (DOAC) that directly inhibits coagulation factor Xa and exerts its anticoagulant effects. Although rivaroxaban generally exhibits predictable pha...
PMC7371439
core_pubmed_pmc
Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation
Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation Abstract Abstract Background Low bioavailability and poor permeability of the blood–brain barrier are problematic when delivering therapeutic agents and...
PMC10908274
core_pubmed_pmc
Model-Informed Precision Dosing of Imipenem in an Obese Adolescent Patient with Augmented Renal Clearance and History of Schizophrenia
Model-Informed Precision Dosing of Imipenem in an Obese Adolescent Patient with Augmented Renal Clearance and History of Schizophrenia Abstract Abstract Imipenem is a broad-spectrum antibiotic that has been used in treating severe infections and exhibits a time-dependent PK/PD profile. Its dose should be adjusted based...