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PMC8698708
core_pubmed_pmc
Predicting Antimicrobial Activity at the Target Site: Pharmacokinetic/Pharmacodynamic Indices versus Time–Kill Approaches
Predicting Antimicrobial Activity at the Target Site: Pharmacokinetic/Pharmacodynamic Indices versus Time–Kill Approaches Abstract Antibiotic dosing strategies are generally based on systemic drug concentrations. However, drug concentrations at the infection site drive antimicrobial effect, and efficacy predictions and...
PMC5955430
core_pubmed_pmc
Using antibody directed phototherapy to target oesophageal adenocarcinoma with heterogeneous HER2 expression
Using antibody directed phototherapy to target oesophageal adenocarcinoma with heterogeneous HER2 expression Abstract Early oesophageal adenocarcinoma (OA) and pre-neoplastic dysplasia may be treated with endoscopic resection and ablative techniques such as photodynamic therapy (PDT). Though effective, discrete areas o...
PMC12590907
core_pubmed_pmc
Pharmacokinetics, safety and efficacy of an optimized dose of artemether–lumefantrine in the treatment of acute uncomplicated Plasmodium falciparum malaria in neonates and infants of less than 5 kg body weight: a multicentre, open-label, single-arm phase 2/3 study (CALINA)
Pharmacokinetics, safety and efficacy of an optimized dose of artemether–lumefantrine in the treatment of acute uncomplicated Plasmodium falciparum malaria in neonates and infants of less than 5 kg body weight: a multicentre, open-label, single-arm phase 2/3 study (CALINA) Abstract Background Treatment recommendations ...
PMC6046171
core_pubmed_pmc
A Validated LC-MS/MS Method for Simultaneous Determination of Six Aconitum Alkaloids and Seven Ginsenosides in Rat Plasma and Application to Pharmacokinetics of Shen-Fu Prescription
A Validated LC-MS/MS Method for Simultaneous Determination of Six Aconitum Alkaloids and Seven Ginsenosides in Rat Plasma and Application to Pharmacokinetics of Shen-Fu Prescription Abstract Abstract A sensitive and reliable LC-MS/MS method has been developed and validated for simultaneous determination of six Aconitum...
PMC4875954
core_pubmed_pmc
Pharmacokinetics of Morphine, Morphine-3-Glucuronide and Morphine-6-Glucuronide in Terminally Ill Adult Patients
Pharmacokinetics of Morphine, Morphine-3-Glucuronide and Morphine-6-Glucuronide in Terminally Ill Adult Patients Abstract Abstract Background and Objective Morphine dosing can be challenging in terminally ill adult patients due to the heterogeneous nature of the population and the difficulty of accurately assessing pai...
PMC7614325
core_pubmed_pmc
Cardiovascular concentration–effect relationships of amodiaquine and its metabolite desethylamodiaquine: Clinical and preclinical studies
Cardiovascular concentration–effect relationships of amodiaquine and its metabolite desethylamodiaquine: Clinical and preclinical studies Abstract Aims Amodiaquine is a 4‐aminoquinoline used extensively for the treatment and prevention of malaria. Orally administered amodiaquine is largely converted to the active metab...
PMC8066800
core_pubmed_pmc
EV20/NMS-P945, a Novel Thienoindole Based Antibody-Drug Conjugate Targeting HER-3 for Solid Tumors
EV20/NMS-P945, a Novel Thienoindole Based Antibody-Drug Conjugate Targeting HER-3 for Solid Tumors Abstract Abstract HER-3 is becoming an attractive target for antibody–drug conjugate (ADC)-based therapy. Indeed, this receptor and its ligands are found to be overexpressed in several malignancies, and re-activation of i...
PMC3872531
core_pubmed_pmc
Pharmacometrics and Systems Pharmacology Software Tutorials and Use: Comments and Guidelines for PSP Contributions
Pharmacometrics and Systems Pharmacology Software Tutorials and Use: Comments and Guidelines for PSP Contributions Abstract In addition to methodological Tutorials, 1 CPT:PSP has recently started to publish software Tutorials. 2 , 3 Our readership and authors may be wondering what kind of format or product is expected,...
PMC9968262
core_pubmed_pmc
Pharmacokinetics of Roflumilast Cream in Chronic Plaque Psoriasis: Data from Phase I to Phase III Studies
Pharmacokinetics of Roflumilast Cream in Chronic Plaque Psoriasis: Data from Phase I to Phase III Studies Abstract Abstract Background Most patients with chronic plaque psoriasis receive topical treatment; however, available options lack a balance of efficacy with long-term safety and tolerability. Roflumilast cream 0....
PMC6149762
core_pubmed_pmc
Melatonin Pharmacokinetics Following Oral Administration in Preterm Neonates
Melatonin Pharmacokinetics Following Oral Administration in Preterm Neonates Abstract Abstract Melatonin possesses potential efficacy in perinatal brain injuries, and has been proposed as adjunctive pharmacological therapy in combination with hypothermia in the clinical setting. However, the pharmacokinetics of melaton...
PMC9952796
core_pubmed_pmc
Evaluation of Drug Interactions in Hospitalized Patients with Respiratory Disorders in Greece
Evaluation of Drug Interactions in Hospitalized Patients with Respiratory Disorders in Greece Abstract Highlights What are the main findings? Patients admitted for hospitalization in Greece due to respiratory disorders are patients with multimorbidity, polypharmacy, and a high prevalence of drug–drug interactions (DDIs...
PMC7151081
core_pubmed_pmc
Drug Delivery to the Posterior Segment of the Eye: Biopharmaceutic and Pharmacokinetic Considerations
Drug Delivery to the Posterior Segment of the Eye: Biopharmaceutic and Pharmacokinetic Considerations Abstract Abstract The treatment of the posterior-segment ocular diseases, such as age-related eye diseases (AMD) or diabetic retinopathy (DR), present a challenge for ophthalmologists due to the complex anatomy and phy...
PMC8547083
core_pubmed_pmc
Association of vancomycin trough concentration on the treatment outcome of patients with bacteremia caused by Enterococcus species
Association of vancomycin trough concentration on the treatment outcome of patients with bacteremia caused by Enterococcus species Abstract Abstract Background Pharmacokinetic-pharmacodynamic (PK/PD) targets of vancomycin therapy have been recognized for methicillin-resistant Staphylococcus aureus infections but not fo...
PMC12669309
core_pubmed_pmc
Weight-Based Pembrolizumab Dosing at 4 mg/kg Every 6 Weeks Leads to Exposures Below Approved Doses with Unestablished Efficacy: A Pharmacokinetic Model-Based Simulation Analysis
Weight-Based Pembrolizumab Dosing at 4 mg/kg Every 6 Weeks Leads to Exposures Below Approved Doses with Unestablished Efficacy: A Pharmacokinetic Model-Based Simulation Analysis Abstract Abstract Background Pembrolizumab is approved globally at a dose of 200 mg every 3 weeks (Q3W) or 400 mg every 6 weeks (Q6W) intraven...
PMC7341284
core_pubmed_pmc
Pharmacokinetic Profile of Oral Administration of Mefloquine to Clinically Normal Cats: A Preliminary In-Vivo Study of a Potential Treatment for Feline Infectious Peritonitis (FIP)
Pharmacokinetic Profile of Oral Administration of Mefloquine to Clinically Normal Cats: A Preliminary In-Vivo Study of a Potential Treatment for Feline Infectious Peritonitis (FIP) Abstract Simple Summary In searching for antiviral agents against feline coronaviruses and feline caliciviruses, mefloquine, a human anti-m...
PMC5697692
core_pubmed_pmc
Exposure–Response Analysis of Nivolumab in Patients With Previously Treated or Untreated Advanced Melanoma
Exposure–Response Analysis of Nivolumab in Patients With Previously Treated or Untreated Advanced Melanoma Methods Methods The analysis population consisted of previously treated and untreated patients with advanced melanoma in the following studies who had been treated with nivolumab, and for whom nivolumab serum conc...
PMC6854236
core_pubmed_pmc
Opioid Safety and Concomitant Benzodiazepine Use in End-Stage Renal Disease Patients
Opioid Safety and Concomitant Benzodiazepine Use in End-Stage Renal Disease Patients Abstract Abstract Background Opioid use is common in end-stage renal disease (ESRD) patients. However, safety of individual opioids and concomitant benzodiazepine use has not been studied. Objective To study the epidemiology of opioid ...
PMC5951785
core_pubmed_pmc
Pharmacokinetics of Hydroxyprogesterone Caproate and its Primary Metabolites during Pregnancy
Pharmacokinetics of Hydroxyprogesterone Caproate and its Primary Metabolites during Pregnancy Abstract Objective To measure pharmacokinetics of hydroxyprogesterone caproate (OHPC) and its major metabolites throughout pregnancy. Study Design Thirty women were prescribed OHPC for recurrent preterm birth prevention. Three...
PMC11315861
core_pubmed_pmc
Understanding Drug Exposure and Trichuris trichiura Cure Rates: A Pharmacometric Approach for Albendazole-Ivermectin Co-medication in Tanzania and Côte d’Ivoire
Understanding Drug Exposure and Trichuris trichiura Cure Rates: A Pharmacometric Approach for Albendazole-Ivermectin Co-medication in Tanzania and Côte d’Ivoire Abstract Abstract Background and Objective Trichuriasis caused by the human whipworm Trichuris trichiura poses a significant public health concern. Albendazole...
PMC10327396
core_pubmed_pmc
The impact of ABCB1 , CYP3A4/5 and ABCG2 gene polymorphisms on rivaroxaban trough concentrations and bleeding events in patients with non-valvular atrial fibrillation
The impact of ABCB1 , CYP3A4/5 and ABCG2 gene polymorphisms on rivaroxaban trough concentrations and bleeding events in patients with non-valvular atrial fibrillation Abstract Abstract Background The influence of genetic factors on the pharmacokinetics and clinical outcomes of rivaroxaban in patients with non-valvular ...
PMC8021898
core_pubmed_pmc
COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms
COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms Abstract Abstract SARS-CoV-2 infection is required for COVID-19, but many signs and symptoms of COVID-19 differ from common acute viral diseases. SARS-CoV-2 infection is necessary but not sufficient for development of clinical COVID-19 disease. Currently, ther...
PMC6431017
core_pubmed_pmc
Bayesian network-based framework for exposure-response study design and interpretation
Bayesian network-based framework for exposure-response study design and interpretation Abstract Abstract Conventional environmental-health risk-assessment methods are often limited in their ability to account for uncertainty in contaminant exposure, chemical toxicity and resulting human health risk. Exposure levels and...
PMC9399922
core_pubmed_pmc
Pharmacokinetics and bioequivalence of two cyclosporine oral solution formulations in cats
Pharmacokinetics and bioequivalence of two cyclosporine oral solution formulations in cats Abstract Abstract The pharmacokinetic profiles and bioequivalence of two cyclosporine oral solutions were investigated in cats. Twenty-four cats were randomly allocated to two equally sized treatment groups in a randomized four-c...
PMC10252891
core_pubmed_pmc
Pharmacometabolic Effects of Pteryxin and Valproate on Pentylenetetrazole-Induced Seizures in Zebrafish Reveal Vagus Nerve Stimulation
Pharmacometabolic Effects of Pteryxin and Valproate on Pentylenetetrazole-Induced Seizures in Zebrafish Reveal Vagus Nerve Stimulation Abstract Abstract Zebrafish (Danio rerio) assays provide a versatile pharmacological platform to test compounds on a wide range of behaviors in a whole organism. A major challenge lies ...
PMC9114963
core_pubmed_pmc
Anti-CSF-1R emactuzumab in combination with anti-PD-L1 atezolizumab in advanced solid tumor patients naïve or experienced for immune checkpoint blockade
Anti-CSF-1R emactuzumab in combination with anti-PD-L1 atezolizumab in advanced solid tumor patients naïve or experienced for immune checkpoint blockade Abstract Background This phase 1b study ( NCT02323191 ) evaluated the safety, antitumor activity, pharmacokinetics, and pharmacodynamics of colony-stimulating factor-1...
PMC11868035
core_pubmed_pmc
Evaluation of the Landscape of Pharmacodynamic Biomarkers in GM1 and GM2 Gangliosidosis
Evaluation of the Landscape of Pharmacodynamic Biomarkers in GM1 and GM2 Gangliosidosis Abstract ABSTRACT GM1 and GM2 gangliosidosis are inherited, progressive, neurodegenerative lysosomal disorders of variable onset and disease progression. GM1 gangliosidosis is a result of biallelic pathogenic variants in the GLB1 ge...
PMC10516122
core_pubmed_pmc
Site-Specific Antibody Conjugation Using Modified Bisected N -Glycans: Method Development and Potential toward Tunable Effector Function
Site-Specific Antibody Conjugation Using Modified Bisected N -Glycans: Method Development and Potential toward Tunable Effector Function Abstract Abstract Antibody–drug conjugates (ADCs) have garnered worldwide attention for disease treatment, as they possess high target specificity, a long half-life, and outstanding p...
PMC9169852
core_pubmed_pmc
Cefquinome Sulfate Oily Nanosuspension Designed for Improving its Bioavailability in the Treatment of Veterinary Infections
Cefquinome Sulfate Oily Nanosuspension Designed for Improving its Bioavailability in the Treatment of Veterinary Infections Abstract Introduction Cefquinome sulfate (CS) is the first fourth-generation antibiotic for animals, which has a wide antibacterial spectrum, strong antibacterial activity and low drug resistance....
PMC11621409
core_pubmed_pmc
Analysis of queries to a Swedish drug information centre identifies scientific knowledge gaps
Analysis of queries to a Swedish drug information centre identifies scientific knowledge gaps Abstract Drug Information Centres (DICs) are providing clinicians with evidence-based support for rational drug treatment. However, knowledge gaps in the literature may hinder DICs from offering optimal guidance. This study ex...
PMC12425547
core_pubmed_pmc
Network pharmacology, molecular docking, and molecular dynamics analyses to explore the molecular mechanism of paclitaxel in atherosclerosis therapy
Network pharmacology, molecular docking, and molecular dynamics analyses to explore the molecular mechanism of paclitaxel in atherosclerosis therapy Abstract Abstract Atherosclerosis is a chronic arterial disease and the leading cause of vascular death. Paclitaxel has long been recognized as an anticancer agent, but re...
PMC12108460
core_pubmed_pmc
High-Dose Ceftriaxone in Elderly Patients with Enterococcal Infective Endocarditis: Population Pharmacokinetics of Free Ceftriaxone and Dose Optimization
High-Dose Ceftriaxone in Elderly Patients with Enterococcal Infective Endocarditis: Population Pharmacokinetics of Free Ceftriaxone and Dose Optimization Abstract Abstract Background: Ampicillin plus ceftriaxone (AC) is a first-line treatment for Enterococcus faecalis infective endocarditis (IE). Its administration in ...
PMC7318010
core_pubmed_pmc
Pooled Multicenter Analysis of Cardiovascular Safety and Population Pharmacokinetic Properties of Piperaquine in African Patients with Uncomplicated Falciparum Malaria
Pooled Multicenter Analysis of Cardiovascular Safety and Population Pharmacokinetic Properties of Piperaquine in African Patients with Uncomplicated Falciparum Malaria Abstract Dihydroartemisinin-piperaquine has shown excellent efficacy and tolerability in malaria treatment. However, concerns have been raised of potent...
PMC9026026
core_pubmed_pmc
Effect of Myricetin on CYP2C8 Inhibition to Assess the Likelihood of Drug Interaction Using In Silico , In Vitro , and In Vivo Approaches
Effect of Myricetin on CYP2C8 Inhibition to Assess the Likelihood of Drug Interaction Using In Silico , In Vitro , and In Vivo Approaches Abstract Abstract Myricetin, a bioflavonoid, is widely used as functional food/complementary medicine and has promising multifaceted pharmacological actions against therapeutically v...
PMC9299784
core_pubmed_pmc
Proteomics of colorectal cancer liver metastasis: A quantitative focus on drug elimination and pharmacodynamics effects
Proteomics of colorectal cancer liver metastasis: A quantitative focus on drug elimination and pharmacodynamics effects Abstract Abstract Aims This study aims to quantify drug‐metabolising enzymes, transporters, receptor tyrosine kinases (RTKs) and protein markers (involved in pathways affected in cancer) in pooled hea...
PMC4674584
core_pubmed_pmc
Evaluation of Waste Anesthetic Gas in the Postanesthesia Care Unit within the Patient Breathing Zone
Evaluation of Waste Anesthetic Gas in the Postanesthesia Care Unit within the Patient Breathing Zone Abstract Potential health hazards from waste anesthetic gases (WAGs) have been a concern since the introduction of inhalational anesthetics into clinical practice. The potential to exceed recommended exposure levels (RE...
PMC11814085
core_pubmed_pmc
Application of drug-induced growth rate inhibition and intracellular drug exposures for comprehensive evaluation of cellular drug sensitivity
Application of drug-induced growth rate inhibition and intracellular drug exposures for comprehensive evaluation of cellular drug sensitivity Abstract In vitro cellular assays are indispensable tools for preclinical understanding of therapeutic candidates. Herein, we have outlined methods for robust determination of ce...
PMC3934716
core_pubmed_pmc
Simultaneous Determination and Pharmacokinetic Comparisons of Multi-Ingredients after Oral Administration of Radix Salviae Miltiorrhizae Extract, Hawthorn Extract, and a Combination of Both Extracts to Rats
Simultaneous Determination and Pharmacokinetic Comparisons of Multi-Ingredients after Oral Administration of Radix Salviae Miltiorrhizae Extract, Hawthorn Extract, and a Combination of Both Extracts to Rats Abstract Abstract A simple and sensitive HPLC method was developed for simultaneous determination of danshensu (D...
PMC3328159
core_pubmed_pmc
Pharmacokinetics of Hyperthermic Intrathoracic Chemotherapy following Pleurectomy and Decortication
Pharmacokinetics of Hyperthermic Intrathoracic Chemotherapy following Pleurectomy and Decortication Abstract Abstract In patients with pseudomyxoma peritonei or peritoneal mesothelioma, direct extension of disease through the hemidiaphragm may result in an isolated progression of tumor within the pleural space. We moni...
PMC9465641
core_pubmed_pmc
Population pharmacokinetics of intravenous colistin sulfate and dosage optimization in critically ill patients
Population pharmacokinetics of intravenous colistin sulfate and dosage optimization in critically ill patients Abstract Aims: To explore the population pharmacokinetics of colistin sulfate and to optimize the dosing strategy for critically ill patients. Methods: The study enrolled critically ill adult patients who rece...
PMC7958305
core_pubmed_pmc
Ligelizumab treatment for severe asthma: learnings from the clinical development programme
Ligelizumab treatment for severe asthma: learnings from the clinical development programme Abstract Abstract Objective Ligelizumab is a humanised IgG1 anti‐IgE antibody that binds IgE with higher affinity than omalizumab. Ligelizumab had greater efficacy than omalizumab on inhaled and skin allergen provocation response...
PMC7303059
core_pubmed_pmc
Comparison of the toxicokinetics of the convulsants picrotoxinin and tetramethylenedisulfotetramine (TETS) in mice
Comparison of the toxicokinetics of the convulsants picrotoxinin and tetramethylenedisulfotetramine (TETS) in mice Abstract Acute intoxication with picrotoxin or the rodenticide tetramethylenedisulfotetramine (TETS) can cause seizures that rapidly progress to status epilepticus and death. Both compounds inhibit γ-amino...
PMC10196151
core_pubmed_pmc
Pharmacokinetic studies of hyperoside -2-hydroxypropyl-β-cyclodextrin inclusion complex and ameliorated DSS-induced colitis in mice
Pharmacokinetic studies of hyperoside -2-hydroxypropyl-β-cyclodextrin inclusion complex and ameliorated DSS-induced colitis in mice Abstract Abstract An inclusion complex formation with cyclodextrin is a promising method to improve the bioavailability of water-insoluble drugs. The pharmacokinetic characteristics of Hyp...
PMC12193971
core_pubmed_pmc
Optimization of Isavuconazole Dosing in Patients with Invasive Fungal Infections Through Therapeutic Drug Monitoring: Real-World Clinical Practice Experience
Optimization of Isavuconazole Dosing in Patients with Invasive Fungal Infections Through Therapeutic Drug Monitoring: Real-World Clinical Practice Experience Abstract Abstract Therapeutic drug monitoring (TDM) is routinely recommended for most antifungal triazoles to ensure efficacy and safety. Isavuconazole, however, ...
PMC4128846
core_pubmed_pmc
Potential patient benefit of a subcutaneous formulation of tocilizumab for the treatment of rheumatoid arthritis: a critical review
Potential patient benefit of a subcutaneous formulation of tocilizumab for the treatment of rheumatoid arthritis: a critical review Abstract Abstract Treatment of rheumatoid arthritis (RA) was revolutionized during the last decade with the development of new biologic disease-modifying anti-rheumatic drugs (DMARDs) enab...
PMC9796261
core_pubmed_pmc
Pharmacokinetic Characteristics, Safety, and Tolerability of Telitacicept, an Injectable Recombinant Human B‐Lymphocyte Stimulating Factor Receptor‐Antibody Fusion Protein, in Healthy Chinese Subjects
Pharmacokinetic Characteristics, Safety, and Tolerability of Telitacicept, an Injectable Recombinant Human B‐Lymphocyte Stimulating Factor Receptor‐Antibody Fusion Protein, in Healthy Chinese Subjects Abstract Abstract Telitacicept, an injectable recombinant human B‐lymphocyte stimulating factor receptor‐antibody fusio...
PMC9727334
core_pubmed_pmc
Molecular Docking and in silico Pharmacological Screening of Oleosin from Cocos Nucifera Complexed with Tamoxifen in Developing Potential Breast Chemotherapeutic Leads
Molecular Docking and in silico Pharmacological Screening of Oleosin from Cocos Nucifera Complexed with Tamoxifen in Developing Potential Breast Chemotherapeutic Leads Abstract Objective: Tamoxifen is a widely used drug for breast cancer therapy; however, concerns and controversies regarding its efficiency arise as it ...
PMC3677634
core_pubmed_pmc
Improved HPLC Method for the Determination of Moxifloxacin in Application to a Pharmacokinetics Study in Patients with Infectious Diseases
Improved HPLC Method for the Determination of Moxifloxacin in Application to a Pharmacokinetics Study in Patients with Infectious Diseases Abstract Objective . To develop a simple and rapid high-performance liquid chromatography (HPLC) method for measuring moxifloxacin concentration in human plasma. Methods . Following...
PMC10019422
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of CSL112
Clinical Pharmacokinetics and Pharmacodynamics of CSL112 Abstract Cardiovascular diseases are the leading cause of death worldwide. Although there have been substantial advances over the last decades, recurrent adverse cardiovascular events after myocardial infarction are still frequent, particularly during the first y...
PMC10497461
core_pubmed_pmc
Acute-on-chronic liver failure alters linezolid pharmacokinetics in critically ill patients with continuous hemodialysis: an observational study
Acute-on-chronic liver failure alters linezolid pharmacokinetics in critically ill patients with continuous hemodialysis: an observational study Abstract Abstract Background In acute-on-chronic liver failure (ACLF), adequate antibiotic dosing is challenging due to changes of drug distribution and elimination. We studie...
PMC11137731
core_pubmed_pmc
AlbuCatcher for Long-Acting Therapeutics
AlbuCatcher for Long-Acting Therapeutics Abstract Therapeutic proteins, pivotal for treating diverse human diseases due to their biocompatibility and high selectivity, often face challenges such as rapid serum clearance, enzymatic degradation, and immune responses. To address these issues and enable prolonged therapeut...
PMC5093207
core_pubmed_pmc
Pre-clinical Evaluation of a Cyanine-Based SPECT Probe for Multimodal Tumor Necrosis Imaging
Pre-clinical Evaluation of a Cyanine-Based SPECT Probe for Multimodal Tumor Necrosis Imaging Abstract Abstract Purpose Recently we showed that a number of carboxylated near-infrared fluorescent (NIRF) cyanine dyes possess strong necrosis avid properties in vitro as well as in different mouse models of spontaneous and t...
PMC9039133
core_pubmed_pmc
Cefiderocol for the Treatment of Multidrug-Resistant Gram-Negative Bacteria: A Systematic Review of Currently Available Evidence
Cefiderocol for the Treatment of Multidrug-Resistant Gram-Negative Bacteria: A Systematic Review of Currently Available Evidence Abstract Cefiderocol is a novel synthetic siderophore-conjugated antibiotic that hijacks the bacterial iron transport systems facilitating drug entry into cells, achieving high periplasmic co...
PMC11382518
core_pubmed_pmc
Uncover the anticancer potential of lycorine
Uncover the anticancer potential of lycorine Abstract Background Natural products have a long history in drug discovery. Lycorine is an alkaloid derived from Amaryllidaceae plants, demonstrating significant pharmacological potential. Lycorine and its hydrochloride salt, lycorine hydrochloride, have shown outstanding an...
PMC5347705
core_pubmed_pmc
Combinatorial effects of doxorubicin and retargeted tissue factor by intratumoral entrapment of doxorubicin and proapoptotic increase of tumor vascular infarction
Combinatorial effects of doxorubicin and retargeted tissue factor by intratumoral entrapment of doxorubicin and proapoptotic increase of tumor vascular infarction Abstract Abstract Truncated tissue factor (tTF), retargeted to tumor vasculature by GNGRAHA peptide (tTF-NGR), and doxorubicin have therapeutic activity agai...
PMC6078047
core_pubmed_pmc
In vitro and in vivo Assessment of Keratose as a Novel Excipient of Paclitaxel Coated Balloons
In vitro and in vivo Assessment of Keratose as a Novel Excipient of Paclitaxel Coated Balloons Abstract Purpose: Drug coated balloons (DCB) are continually improving due to advances in coating techniques and more effective excipients. Paclitaxel, the current drug choice of DCB, is a microtubule-stabilizing chemotherape...
PMC3419960
core_pubmed_pmc
Phase I study investigating the safety and feasibility of combining imatinib mesylate (Gleevec) with sorafenib in patients with refractory castration-resistant prostate cancer
Phase I study investigating the safety and feasibility of combining imatinib mesylate (Gleevec) with sorafenib in patients with refractory castration-resistant prostate cancer Abstract Abstract Background: Determining the maximum tolerated dose (MTD) and the dose-limiting toxicity (DLT) of sorafenib (S) plus imatinib (...
PMC7238799
core_pubmed_pmc
Safety, tolerability, and pharmacokinetics of the selective prostacyclin receptor agonist ralinepag in single and multiple dosing studies of an immediate-release oral formulation in healthy volunteers
Safety, tolerability, and pharmacokinetics of the selective prostacyclin receptor agonist ralinepag in single and multiple dosing studies of an immediate-release oral formulation in healthy volunteers Abstract Ralinepag (APD811), an oral, potent, and selective prostacyclin receptor (IP) agonist is being developed for t...
PMC12089282
core_pubmed_pmc
Safety and cognitive pharmacodynamics following dose escalations with 3-methylmethcathinone (3-MMC): a first in human, designer drug study
Safety and cognitive pharmacodynamics following dose escalations with 3-methylmethcathinone (3-MMC): a first in human, designer drug study Abstract Abstract 3-Methylmethcathinone (3-MMC) is a designer drug that belongs to the group of synthetic cathinones. The compound has been scheduled in many jurisdictions because o...
PMC8018653
core_pubmed_pmc
Gender-based differences in brain and plasma pharmacokinetics of letrozole in sprague-dawley rats: Application of physiologically-based pharmacokinetic modeling to gain quantitative insights
Gender-based differences in brain and plasma pharmacokinetics of letrozole in sprague-dawley rats: Application of physiologically-based pharmacokinetic modeling to gain quantitative insights Abstract Based on the discovery that the estrogen synthase aromatase (CYP19A1) is abundantly expressed in high- grade gliomas, th...
PMC8283337
core_pubmed_pmc
Neural-ODE for pharmacokinetics modeling and its advantage to alternative machine learning models in predicting new dosing regimens
Neural-ODE for pharmacokinetics modeling and its advantage to alternative machine learning models in predicting new dosing regimens Abstract Summary Forecasting pharmacokinetics (PK) for individual patients is a fundamental problem in clinical pharmacology. One key challenge is that PK models constructed using data fro...
PMC8376138
core_pubmed_pmc
PK/PD modeling of FXI antisense oligonucleotides to bridge the dose‐FXI activity relation from healthy volunteers to end‐stage renal disease patients
PK/PD modeling of FXI antisense oligonucleotides to bridge the dose‐FXI activity relation from healthy volunteers to end‐stage renal disease patients Abstract Abstract IONIS‐FXI RX (BAY2306001) is an antisense oligonucleotide that inhibits the synthesis of coagulation factor XI (FXI) and has been investigated in health...
PMC3553515
core_pubmed_pmc
Phase I and pharmacodynamic study of high-dose NGR–hTNF in patients with refractory solid tumours
Phase I and pharmacodynamic study of high-dose NGR–hTNF in patients with refractory solid tumours Abstract Abstract Background: NGR–hTNF exploits the peptide asparagine–glycine–arginine (NGR) for selectively targeting tumour necrosis factor (TNF) to CD13-overexpressing tumour vessels. Maximum-tolerated dose (MTD) of NG...
PMC12905974
core_pubmed_pmc
Discontinuation of the development of remimazolam for ICU sedation in Japan: background and rationale
Discontinuation of the development of remimazolam for ICU sedation in Japan: background and rationale Abstract Abstract Remimazolam, an ultra-short-acting benzodiazepine rapidly metabolized by carboxylesterase-1, was developed as a promising alternative for ICU sedation. It was anticipated to overcome the unpredictable...
PMC11578139
core_pubmed_pmc
Population PK modeling of certolizumab pegol in pregnant women with chronic inflammatory diseases
Population PK modeling of certolizumab pegol in pregnant women with chronic inflammatory diseases Abstract Abstract Certolizumab pegol (CZP; CIMZIA™) is the only Fc‐free tumor necrosis factor inhibitor with data from a clinical study demonstrating no to minimal placental transfer. The pharmacokinetics (PK) of certolizu...
PMC12891982
core_pubmed_pmc
Gentamicin fails to eradicate Staphylococcus aureus biofilm in vitro, even in combination with rifampin
Gentamicin fails to eradicate Staphylococcus aureus biofilm in vitro, even in combination with rifampin Abstract Abstract Introduction : Biofilm formation is one of the key elements making orthopaedic device-related infections (ODRIs) difficult to eradicate. Aminoglycosides such as gentamicin are frequently applied via...
PMC12146541
core_pubmed_pmc
Evaluation of pharmacokinetics of intravenous protein C concentrate in protein C deficiency: implications for treatment initiation and maintenance
Evaluation of pharmacokinetics of intravenous protein C concentrate in protein C deficiency: implications for treatment initiation and maintenance Abstract Abstract Background Dosing of intravenous protein C concentrate (Ceprotin) in patients with protein C deficiency is guided by pharmacokinetics (PK) of plasma protei...
PMC9317565
core_pubmed_pmc
Tumor-Localized Administration of α-GalCer to Recruit Invariant Natural Killer T Cells and Enhance Their Antitumor Activity against Solid Tumors
Tumor-Localized Administration of α-GalCer to Recruit Invariant Natural Killer T Cells and Enhance Their Antitumor Activity against Solid Tumors Abstract Abstract Invariant natural killer T (iNKT) cells have the capacity to mount potent anti-tumor reactivity and have therefore become a focus in the development of cell-...
PMC5322938
core_pubmed_pmc
Biosimilars and the extrapolation of indications for inflammatory conditions
Biosimilars and the extrapolation of indications for inflammatory conditions Abstract Extrapolation is the approval of a biosimilar for use in an indication held by the originator biologic not directly studied in a comparative clinical trial with the biosimilar. Extrapolation is a scientific rationale that bridges all ...
PMC10604776
core_pubmed_pmc
Real-Time TDM-Based Expert Clinical Pharmacological Advice Program for Attaining Aggressive Pharmacokinetic/Pharmacodynamic Target of Continuous Infusion Meropenem in the Treatment of Critically Ill Patients with Documented Gram-Negative Infections Undergoing Continuous Veno-Venous Hemodiafiltration
Real-Time TDM-Based Expert Clinical Pharmacological Advice Program for Attaining Aggressive Pharmacokinetic/Pharmacodynamic Target of Continuous Infusion Meropenem in the Treatment of Critically Ill Patients with Documented Gram-Negative Infections Undergoing Continuous Veno-Venous Hemodiafiltration Abstract Abstract (...
PMC12038368
core_pubmed_pmc
Impacts of Pharmacokinetic Gene Polymorphisms on Steady‐State Plasma Concentrations of Simvastatin in Thai Population
Impacts of Pharmacokinetic Gene Polymorphisms on Steady‐State Plasma Concentrations of Simvastatin in Thai Population Abstract ABSTRACT Simvastatin, an HMG‐CoA reductase inhibitor, is widely used for hypercholesterolemia but may cause myotoxicity linked to its plasma concentration. Pharmacokinetic gene polymorphisms in...
PMC8301550
core_pubmed_pmc
Evolving drug regulatory landscape in China: A clinical pharmacology perspective
Evolving drug regulatory landscape in China: A clinical pharmacology perspective Abstract Abstract In order to encourage innovative medicine to address Chinese unmet medical needs, China has changed its drug regulatory landscape to speed up access to new medicines. In order to understand the fast‐changing landscape and...
PMC11041816
core_pubmed_pmc
Comparison of Fat-Free Mass and Ideal Body Weight Scalar for Anesthetic Induction Dose of Propofol in Patients with Morbid Obesity: A Double-Blind, Randomized Clinical Trial
Comparison of Fat-Free Mass and Ideal Body Weight Scalar for Anesthetic Induction Dose of Propofol in Patients with Morbid Obesity: A Double-Blind, Randomized Clinical Trial Abstract Background Obesity is a growing problem worldwide and can affect both the pharmacodynamics and pharmacokinetics of various drugs, includi...
PMC6468928
core_pubmed_pmc
Population pharmacokinetics of tacrolimus in pediatric refractory nephrotic syndrome and a summary of other pediatric disease models
Population pharmacokinetics of tacrolimus in pediatric refractory nephrotic syndrome and a summary of other pediatric disease models Abstract Abstract Different tacrolimus (TAC) population pharmacokinetic (PPK) models have been established in various pediatric disease populations. However, a TAC PPK model for pediatric...
PMC10303079
core_pubmed_pmc
Bioinformatics Tools for the Analysis of Active Compounds Identified in Ranunculaceae Species
Bioinformatics Tools for the Analysis of Active Compounds Identified in Ranunculaceae Species Abstract Abstract The chemical compounds from extracts of three Ranunculaceae species, Aconitum toxicum Rchb., Anemone nemorosa L. and Helleborus odorus Waldst. & Kit. ex Willd., respectively, were isolated using the HPLC puri...
PMC9960997
core_pubmed_pmc
Targeted Therapy of Severe Infections Caused by Staphylococcus aureus in Critically Ill Adult Patients: A Multidisciplinary Proposal of Therapeutic Algorithms Based on Real-World Evidence
Targeted Therapy of Severe Infections Caused by Staphylococcus aureus in Critically Ill Adult Patients: A Multidisciplinary Proposal of Therapeutic Algorithms Based on Real-World Evidence Abstract (1) Introduction: To develop evidence-based algorithms for targeted antibiotic therapy of infections caused by Staphylococc...
PMC4949308
core_pubmed_pmc
Transgender women, hormonal therapy and HIV treatment: a comprehensive review of the literature and recommendations for best practices
Transgender women, hormonal therapy and HIV treatment: a comprehensive review of the literature and recommendations for best practices Abstract Abstract Introduction Studies have shown that transgender women (TGW) are disproportionately affected by HIV, with an estimated HIV prevalence of 19.1% among TGW worldwide. Aft...
PMC8390684
core_pubmed_pmc
Optimal loading dose of meropenem before continuous infusion in critically ill patients: a simulation study
Optimal loading dose of meropenem before continuous infusion in critically ill patients: a simulation study Abstract The aim of this study was to investigate optimal loading doses prior to continuous infusion of meropenem in critically ill patients. A previously published and successfully evaluated pharmacokinetic mode...
PMC7828633
core_pubmed_pmc
Impact of CNS Diseases on Drug Delivery to Brain Extracellular and Intracellular Target Sites in Human: A “WHAT-IF” Simulation Study
Impact of CNS Diseases on Drug Delivery to Brain Extracellular and Intracellular Target Sites in Human: A “WHAT-IF” Simulation Study Abstract Abstract The blood–brain barrier (BBB) is equipped with unique physical and functional processes that control central nervous system (CNS) drug transport and the resulting concen...
PMC5715639
core_pubmed_pmc
Effects of mistletoe products on pharmacokinetic drug turnover by inhibition and induction of cytochrome P450 activities
Effects of mistletoe products on pharmacokinetic drug turnover by inhibition and induction of cytochrome P450 activities Abstract Abstract Background European mistletoe ( Viscum album ) products used in cancer therapy are frequently combined with other anti-cancer-drugs. Hence, potential herb-drug interactions have bec...
PMC3978888
core_pubmed_pmc
Safety, tolerability, pharmacokinetics and pharmacodynamics of an anti- oncostatin M monoclonal antibody in rheumatoid arthritis: results from phase II randomized, placebo-controlled trials
Safety, tolerability, pharmacokinetics and pharmacodynamics of an anti- oncostatin M monoclonal antibody in rheumatoid arthritis: results from phase II randomized, placebo-controlled trials Abstract Introduction Oncostatin M (OSM) has been implicated in the pathophysiology of rheumatoid arthritis (RA) through its effec...
PMC5423235
core_pubmed_pmc
Antibacterial Loaded Spray Dried Chitosan Polyelectrolyte Complexes as Dry Powder Aerosol for the Treatment of Lung Infections
Antibacterial Loaded Spray Dried Chitosan Polyelectrolyte Complexes as Dry Powder Aerosol for the Treatment of Lung Infections Abstract Inhalation delivery of aerosolized antibacterials is preferred over conventional methods of delivery for targeting lung infection. The present study is concerned with the development a...
PMC10669052
core_pubmed_pmc
Exploring Differences in Pharmacometrics of Rabeprazole between Genders via Population Pharmacokinetic–Pharmacodynamic Modeling
Exploring Differences in Pharmacometrics of Rabeprazole between Genders via Population Pharmacokinetic–Pharmacodynamic Modeling Abstract Rabeprazole is a proton pump inhibitor that inhibits gastric acid production and increases gastric pH; it is widely used clinically as a treatment option for gastritis and gastric ulc...
PMC5966501
core_pubmed_pmc
Evidence-Based Recommendations to Improve the Safe Use of Drugs in Patients with Liver Cirrhosis
Evidence-Based Recommendations to Improve the Safe Use of Drugs in Patients with Liver Cirrhosis Abstract Introduction The presence of liver cirrhosis can have a major impact on pharmacodynamics and pharmacokinetics, but guidance for prescribing is lacking. Objective The aim of this study is to provide an overview of e...
PMC6182730
core_pubmed_pmc
Extrapolation of praziquantel pharmacokinetics to a pediatric population: a cautionary tale
Extrapolation of praziquantel pharmacokinetics to a pediatric population: a cautionary tale Abstract L-praziquantel (PZQ) pharmacokinetic data were analyzed from two relative bioavailability Phase 1 studies in adult, healthy subjects with two new oral dispersion tablet (ODT) formulations of L-PZQ administered under var...
PMC11148501
core_pubmed_pmc
CYP2D6 isoenzyme and ABCB1 gene polymorphisms associated with postoperative nausea and vomiting in women undergoing laparoscopic cholecystectomy: a randomized trial
CYP2D6 isoenzyme and ABCB1 gene polymorphisms associated with postoperative nausea and vomiting in women undergoing laparoscopic cholecystectomy: a randomized trial Abstract Introduction Postoperative nausea and vomiting is still a common complication. Serotonin receptor antagonists are commonly used in clinical practi...
PMC12945708
core_pubmed_pmc
Population Pharmacokinetics and Exposure‐Response Analyses for Telisotuzumab Vedotin in Patients With c‐Met Protein Overexpressing Tumors
Population Pharmacokinetics and Exposure‐Response Analyses for Telisotuzumab Vedotin in Patients With c‐Met Protein Overexpressing Tumors Abstract ABSTRACT Telisotuzumab vedotin (Teliso‐V) is a c‐Met‐directed antibody‐drug conjugate that delivers a cytotoxic microtubule inhibitor monomethyl auristatin E (MMAE) payload ...
PMC8147951
core_pubmed_pmc
Emergent Drug and Nutrition Interactions in COVID-19: A Comprehensive Narrative Review
Emergent Drug and Nutrition Interactions in COVID-19: A Comprehensive Narrative Review Abstract Coronaviruses are a large family of viruses that are known to cause respiratory tract infections ranging from colds to more severe diseases, such as Middle East Respiratory Syndrome (MERS) and the Severe Acute Respiratory Sy...
PMC5656880
core_pubmed_pmc
Practical Recommendations for Therapeutic Drug Monitoring of Kinase Inhibitors in Oncology
Practical Recommendations for Therapeutic Drug Monitoring of Kinase Inhibitors in Oncology Abstract Abstract Despite the fact that pharmacokinetic exposure of kinase inhibitors (KIs) is highly variable and clear relationships exist between exposure and treatment outcomes, fixed dosing is still standard practice. This r...
PMC10175687
core_pubmed_pmc
Population pharmacokinetic analysis and dosing regimen optimization of teicoplanin in critically ill patients with sepsis
Population pharmacokinetic analysis and dosing regimen optimization of teicoplanin in critically ill patients with sepsis Abstract Abstract Objectives: Teicoplanin has been extensively used in the treatment for infections caused by gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA). How...
PMC4671243
core_pubmed_pmc
Associations of Perfluoroalkyl Substances (PFAS) with Lower Birth Weight: An Evaluation of Potential Confounding by Glomerular Filtration Rate Using a Physiologically Based Pharmacokinetic Model (PBPK)
Associations of Perfluoroalkyl Substances (PFAS) with Lower Birth Weight: An Evaluation of Potential Confounding by Glomerular Filtration Rate Using a Physiologically Based Pharmacokinetic Model (PBPK) Abstract Abstract Background Prenatal exposure to perfluoroalkyl substances (PFAS) has been associated with lower birt...
PMC5498502
core_pubmed_pmc
Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers
Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers Abstract Salvia miltiorrhiza (SM) is widely used to treat microcirculatory disturbance-related diseases; its lipophilic components play important roles in this application. Cryptotanshinon...
PMC5431879
core_pubmed_pmc
Pharmacometabolomics for predicting variable busulfan exposure in paediatric haematopoietic stem cell transplantation patients
Pharmacometabolomics for predicting variable busulfan exposure in paediatric haematopoietic stem cell transplantation patients Abstract Abstract Owing to its narrow therapeutic range and high pharmacokinetic variability, optimal dosing for busulfan is important to minimise overexposure-related systemic toxicity and und...
PMC3304372
core_pubmed_pmc
Development and validation of a rapid HPLC- fluorescence method for simultaneous determination of venlafaxine and its major metabolites in human plasma
Development and validation of a rapid HPLC- fluorescence method for simultaneous determination of venlafaxine and its major metabolites in human plasma Abstract Background and the purpose of the study To develop a simple, rapid and accurate HPLC method for the measurement of the venlafaxine and its main metabolites, O ...
PMC6566363
core_pubmed_pmc
pH-Sensitive Ratiometric Fluorescent Probe for Evaluation of Tumor Treatments
pH-Sensitive Ratiometric Fluorescent Probe for Evaluation of Tumor Treatments Abstract Determining therapeutic efficacy is critical for tumor precision theranostics. In order to monitor the efficacy of anti-cancer drugs (e.g., Paclitaxel), a pH-sensitive ratiometric fluorescent imaging probe was constructed. The pH-sen...
PMC7002734
core_pubmed_pmc
Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method
Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method Abstract To evaluate and compare the pharmacokinetic (PK) characteristics of a newly developed oral osmotically controlled drug delivery system of ...
PMC7335990
core_pubmed_pmc
Integrated Quality by Design Approach for Developing Nanolipidic Drug Delivery Systems of Olmesartan Medoxomil with Enhanced Antihypertensive Action
Integrated Quality by Design Approach for Developing Nanolipidic Drug Delivery Systems of Olmesartan Medoxomil with Enhanced Antihypertensive Action Abstract Abstract Purpose: The present work endeavors to report a systematic approach of developing the lipidic self-nanoemulsifying formulation of olmesartan medoxomil (O...
PMC12096638
core_pubmed_pmc
Targeting heterogeneous depression with trazodone prolonged release: from neuropharmacology to clinical application
Targeting heterogeneous depression with trazodone prolonged release: from neuropharmacology to clinical application Abstract Aim This paper evaluates the clinical efficacy, safety, and practical implications of Trazodone Prolonged Release (PR) in managing depression, anxiety, and sleep disorders, with a focus on its mu...
PMC4624361
core_pubmed_pmc
Pharmacokinetic profile of phytoconstituent(s) isolated from medicinal plants—A comprehensive review
Pharmacokinetic profile of phytoconstituent(s) isolated from medicinal plants—A comprehensive review Abstract Abstract Herbal medicine, the backbone of traditional medicine, has played an important role in human health and welfare for a long period. Traditional therapeutic approaches of regional significance are found ...
PMC9695373
core_pubmed_pmc
Shedding a Light on Acyclovir Pharmacodynamics: A Retrospective Analysis on Pharmacokinetic/Pharmacodynamic Modelling of Acyclovir for the Treatment of Varicella Zoster Virus Infection in Immunocompromised Patients: A Pilot Study
Shedding a Light on Acyclovir Pharmacodynamics: A Retrospective Analysis on Pharmacokinetic/Pharmacodynamic Modelling of Acyclovir for the Treatment of Varicella Zoster Virus Infection in Immunocompromised Patients: A Pilot Study Abstract Abstract Background: Acyclovir and valacyclovir are used for the treatment and pr...
PMC8213417
core_pubmed_pmc
Application of physiologically based biopharmaceutics modeling to understand the impact of dissolution differences on in vivo performance of immediate release products: The case of bisoprolol
Application of physiologically based biopharmaceutics modeling to understand the impact of dissolution differences on in vivo performance of immediate release products: The case of bisoprolol Abstract Abstract Merck KGaA observed slight differences in the dissolution of Concor ® (bisoprolol) batches over the years. The...