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PMC11744500
core_pubmed_pmc
Bola-Amphiphilic Dendrimer Enhances Imatinib to Target Metastatic Ovarian Cancer via β-Catenin-HRP2 Signaling Axis
Bola-Amphiphilic Dendrimer Enhances Imatinib to Target Metastatic Ovarian Cancer via β-Catenin-HRP2 Signaling Axis Abstract Abstract Ovarian cancer is the leading cause of death among all gynecological malignancies, and drug resistance renders the current chemotherapy agents ineffective for patients with advanced metas...
PMC11646939
core_pubmed_pmc
In‐host modeling of dengue virus and non‐structural protein 1 and the effects of ivermectin in patients with acute dengue fever
In‐host modeling of dengue virus and non‐structural protein 1 and the effects of ivermectin in patients with acute dengue fever Abstract Abstract The increased incidence of dengue poses a substantially global public health challenge. There are no approved antiviral drugs to treat dengue infections. Ivermectin, an old a...
PMC3004585
core_pubmed_pmc
Role of intranasal fentanyl in breakthrough pain management in cancer patients
Role of intranasal fentanyl in breakthrough pain management in cancer patients Abstract Fentanyl is a strong opioid analgesic, which is commonly used in the form of a transdermal patch for the treatment of chronic cancer pain. An intranasal route of fentanyl administration is a novel treatment for breakthrough cancer p...
PMC10600053
core_pubmed_pmc
Effect of CYP2D6 pharmacogenetic phenotype and phenoconversion on serum concentrations of antidepressants and antipsychotics: a retrospective cohort study
Effect of CYP2D6 pharmacogenetic phenotype and phenoconversion on serum concentrations of antidepressants and antipsychotics: a retrospective cohort study Abstract Background Pharmacogenetics (PGx), especially in regard to CYP2D6 , is gaining more importance in routine clinical settings. Including phenoconversion effec...
PMC9699030
core_pubmed_pmc
Machine-Learning Exploration of Exposure-Effect Relationships of Cisplatin in Head and Neck Cancer Patients
Machine-Learning Exploration of Exposure-Effect Relationships of Cisplatin in Head and Neck Cancer Patients Abstract Abstract Background: Cisplatin is a pivotal drug in the treatment of head and neck cancer, and personalized dosage should help the preservation of an optimal toxicity–efficacy ratio. Methods: We analyzed...
PMC5363796
core_pubmed_pmc
Development of an evidence evaluation and synthesis system for drug-drug interactions, and its application to a systematic review of HIV and malaria co-infection
Development of an evidence evaluation and synthesis system for drug-drug interactions, and its application to a systematic review of HIV and malaria co-infection Abstract Background In all settings, there are challenges associated with safely treating patients with multimorbidity and polypharmacy. The need to character...
PMC11925699
core_pubmed_pmc
The Chicken Embryo: An Alternative Animal Model in Development, Disease and Pharmacological Treatment
The Chicken Embryo: An Alternative Animal Model in Development, Disease and Pharmacological Treatment Abstract ABSTRACT To examine various medications and substances, in vivo models such as rats and mice are routinely used. However, it is utterly desirable to reduce extensive amounts of animals for these experimental m...
PMC6223994
core_pubmed_pmc
Pharmacokinetics and Exposure–Response Analyses of Daratumumab in Combination Therapy Regimens for Patients with Multiple Myeloma
Pharmacokinetics and Exposure–Response Analyses of Daratumumab in Combination Therapy Regimens for Patients with Multiple Myeloma Abstract Abstract Introduction Daratumumab, a human IgG monoclonal antibody targeting CD38, has demonstrated activity as monotherapy and in combination with standard-of-care regimens in mult...
PMC11259557
core_pubmed_pmc
Phase I study of TQB3602 , an oral proteasome inhibitor, in relapsed and refractory multiple myeloma
Phase I study of TQB3602 , an oral proteasome inhibitor, in relapsed and refractory multiple myeloma Abstract Abstract Objective TQB3602 is a novel orally bioavailable proteasome inhibitor. This study is the first‐in‐human phase I clinical trial to evaluate the safety, tolerability, pharmacokinetics, and preliminary ef...
PMC4305106
core_pubmed_pmc
Clinical and Preclinical Pharmacokinetics and Pharmacodynamics of Mipomersen (Kynamro ® ): A Second-Generation Antisense Oligonucleotide Inhibitor of Apolipoprotein B
Clinical and Preclinical Pharmacokinetics and Pharmacodynamics of Mipomersen (Kynamro ® ): A Second-Generation Antisense Oligonucleotide Inhibitor of Apolipoprotein B Abstract Abstract Mipomersen (Kynamro ® ), a second-generation 2′- O -methoxyethyl chimeric antisense oligonucleotide (ASO), inhibits the synthesis of ap...
PMC12044641
core_pubmed_pmc
Systematic evidence map (SEM) template: Report format and methods used for the US EPA Integrated Risk Information System (IRIS) program, Provisional Peer Reviewed Toxicity Value (PPRTV) program, and other “fit for purpose” literature-based human health analyses
Systematic evidence map (SEM) template: Report format and methods used for the US EPA Integrated Risk Information System (IRIS) program, Provisional Peer Reviewed Toxicity Value (PPRTV) program, and other “fit for purpose” literature-based human health analyses Abstract Background: Systematic evidence maps (SEMs) are g...
PMC7223855
core_pubmed_pmc
Antimicrobial therapeutic drug monitoring in critically ill adult patients: a Position Paper #
Antimicrobial therapeutic drug monitoring in critically ill adult patients: a Position Paper # Abstract Abstract Purpose This Position Paper aims to review and discuss the available data on therapeutic drug monitoring (TDM) of antibacterials, antifungals and antivirals in critically ill adult patients in the intensive ...
PMC8698960
core_pubmed_pmc
Health Benefits and Pharmacological Properties of Carvone
Health Benefits and Pharmacological Properties of Carvone Abstract Carvone is a monoterpene ketone contained in the essential oils of several aromatic and medicinal plants of the Lamiaceae and Asteraceae families. From aromatic plants, this monoterpene is secreted at different concentrations depending on the species, t...
PMC11222188
core_pubmed_pmc
The Effect of Various Degrees of Renal or Hepatic Impairment on the Pharmacokinetic Properties of Once-Weekly Insulin Icodec
The Effect of Various Degrees of Renal or Hepatic Impairment on the Pharmacokinetic Properties of Once-Weekly Insulin Icodec Abstract Abstract Background and Objective Icodec is a once-weekly insulin being developed to provide basal insulin coverage in diabetes mellitus. This study evaluated the effects of renal or hep...
PMC12281596
core_pubmed_pmc
Preclinical Development and Phase I Study of ZSYY001 , a Polymeric Micellar Paclitaxel for Advanced Solid Tumor
Preclinical Development and Phase I Study of ZSYY001 , a Polymeric Micellar Paclitaxel for Advanced Solid Tumor Abstract ABSTRACT Purpose A novel paclitaxel delivery system has the potential to avoid the side effects associated with Cremophor EL and thus enhance therapeutic efficacy. Here, we report the results of a pr...
PMC7979338
core_pubmed_pmc
Pharmacokinetics, Bioequivalence and Safety Evaluation of Two Ticagrelor Tablets Under Fasting and Fed Conditions in Healthy Chinese Subjects
Pharmacokinetics, Bioequivalence and Safety Evaluation of Two Ticagrelor Tablets Under Fasting and Fed Conditions in Healthy Chinese Subjects Abstract Purpose To evaluate the pharmacokinetics (PK), bioequivalence and safety profiles of test drug and reference drug of 90 mg ticagrelor tablets and their main active metab...
PMC8399023
core_pubmed_pmc
Species Differences in Metabolism of Soluble Epoxide Hydrolase Inhibitor, EC1728, Highlight the Importance of Clinically Relevant Screening Mechanisms in Drug Development
Species Differences in Metabolism of Soluble Epoxide Hydrolase Inhibitor, EC1728, Highlight the Importance of Clinically Relevant Screening Mechanisms in Drug Development Abstract There are few novel therapeutic options available for companion animals, and medications rely heavily on repurposed drugs developed for othe...
PMC8622919
core_pubmed_pmc
Effect of the Interrelation between CYP3A5 Genotype, Concentration/Dose Ratio and Intrapatient Variability of Tacrolimus on Kidney Graft Function: Monte Carlo Simulation Approach
Effect of the Interrelation between CYP3A5 Genotype, Concentration/Dose Ratio and Intrapatient Variability of Tacrolimus on Kidney Graft Function: Monte Carlo Simulation Approach Abstract Abstract Background : Tacrolimus (Tac) is characterized by large between- and within-patient (IPV) variability in pharmacokinetics a...
PMC8200345
core_pubmed_pmc
Pharmacokinetics of Ruxolitinib in Patients with Atopic Dermatitis Treated With Ruxolitinib Cream: Data from Phase II and III Studies
Pharmacokinetics of Ruxolitinib in Patients with Atopic Dermatitis Treated With Ruxolitinib Cream: Data from Phase II and III Studies Abstract Background Pathogenesis of atopic dermatitis (AD) involves the Janus kinase (JAK)/signal transducer and activator of transcription (STAT) pathway. A cream formulation of ruxolit...
PMC9320929
core_pubmed_pmc
First randomized evaluation of safety, pharmacodynamics, and pharmacokinetics of BAY 1831865, an antibody targeting coagulation factor XI and factor XIa, in healthy men
First randomized evaluation of safety, pharmacodynamics, and pharmacokinetics of BAY 1831865, an antibody targeting coagulation factor XI and factor XIa, in healthy men Abstract Abstract Background Bleeding is a clinically significant issue with all current anticoagulants. Safer antithrombotic strategies are required. ...
PMC12031506
core_pubmed_pmc
The Impact of Vaccination Frequency on COVID-19 Public Health Outcomes: A Model-Based Analysis
The Impact of Vaccination Frequency on COVID-19 Public Health Outcomes: A Model-Based Analysis Abstract Abstract Background: While the rapid deployment of SARS-CoV-2 vaccines had a significant impact on the ongoing COVID-19 pandemic, rapid viral immune evasion and waning neutralizing antibody titers have degraded vacci...
PMC3925623
core_pubmed_pmc
Human Pharmacokinetics of High Dose Oral Curcumin and Its Effect on Heme Oxygenase-1 Expression in Healthy Male Subjects
Human Pharmacokinetics of High Dose Oral Curcumin and Its Effect on Heme Oxygenase-1 Expression in Healthy Male Subjects Abstract Purpose . Heme oxygenase-1 (HO-1) has been proposed to exert pharmacological benefits by its antioxidative and anti-inflammatory effects. HO-1 expression may be affected by the GT length pol...
PMC12460216
core_pubmed_pmc
Bioequivalence Study of Two Formulations of Flunarizine Hydrochloride Capsules in Healthy Chinese Subjects Under Fasting and Fed Conditions
Bioequivalence Study of Two Formulations of Flunarizine Hydrochloride Capsules in Healthy Chinese Subjects Under Fasting and Fed Conditions Abstract Background and Objectives Flunarizine, a selective calcium channel blocker with vasodilatory and neuroprotective effects, is a mainstay for migraine prophylaxis and vertig...
PMC4859859
core_pubmed_pmc
Exposure–safety–efficacy analysis of single-agent ixazomib, an oral proteasome inhibitor, in relapsed/refractory multiple myeloma: dose selection for a phase 3 maintenance study
Exposure–safety–efficacy analysis of single-agent ixazomib, an oral proteasome inhibitor, in relapsed/refractory multiple myeloma: dose selection for a phase 3 maintenance study Abstract Summary Background Ixazomib is the first oral, small molecule proteasome inhibitor to reach phase 3 trials. The current analysis char...
PMC5613202
core_pubmed_pmc
Population Pharmacokinetic and Pharmacodynamic Modeling of LY2510924 in Patients With Advanced Cancer
Population Pharmacokinetic and Pharmacodynamic Modeling of LY2510924 in Patients With Advanced Cancer Abstract Abstract The objectives of this study were to characterize the pharmacokinetics (PK) of LY2510924, a potent peptide antagonist of the CXCR4 receptor, after subcutaneous administration in patients with advanced...
PMC11316428
core_pubmed_pmc
Drug-induced liver injury associated with savolitinib: a novel case report and causality assessment
Drug-induced liver injury associated with savolitinib: a novel case report and causality assessment Abstract Background Savolitinib, a small molecule inhibitor, has gained approval as the inaugural medication in China that specifically targets MET kinase. Patients with advanced non-small cell lung cancer (NSCLC) who sh...
PMC7853441
core_pubmed_pmc
Tapentadol for the Treatment of Moderate-to-Severe Acute Pain in Children Under the Age of Two Years
Tapentadol for the Treatment of Moderate-to-Severe Acute Pain in Children Under the Age of Two Years Abstract Abstract Background Pharmacokinetics (PK), efficacy, and safety of the opioid analgesic tapentadol in the treatment of moderate-to-severe acute pain have so far not been investigated in pediatric patients <2 ye...
PMC7000358
core_pubmed_pmc
Effect of Different Media on the Bactericidal Activity of Colistin and on the Synergistic Combination With Azidothymidine Against mcr-1- Positive Colistin-Resistant Escherichia coli
Effect of Different Media on the Bactericidal Activity of Colistin and on the Synergistic Combination With Azidothymidine Against mcr-1- Positive Colistin-Resistant Escherichia coli Abstract Antimicrobial susceptibility testing (AST) performed according to defined guidelines is important to identify resistance and to p...
PMC8147656
core_pubmed_pmc
Interaction between Omeprazole and Gliclazide in Relation to CYP2C19 Phenotype
Interaction between Omeprazole and Gliclazide in Relation to CYP2C19 Phenotype Abstract The antidiabetic drug gliclazide is partly metabolized by CYP2C19, the main enzyme involved in omeprazole metabolism. The aim of the study was to explore the interaction between omeprazole and gliclazide in relation to CYP2C19 pheno...
PMC5488155
core_pubmed_pmc
A Prospective Population Pharmacokinetic Study on Morphine Metabolism in Cancer Patients
A Prospective Population Pharmacokinetic Study on Morphine Metabolism in Cancer Patients Abstract Background Oral and subcutaneous morphine is widely used for the treatment of cancer-related pain; however, solid pharmacokinetic data on this practice are lacking. Furthermore, it is largely unknown which factors contribu...
PMC12401982
core_pubmed_pmc
Unexpected renal influence on isavuconazole trough concentrations: two case reports and literature review
Unexpected renal influence on isavuconazole trough concentrations: two case reports and literature review Abstract Isavuconazole (ISA) is a first-line treatment for invasive aspergillosis, with routine therapeutic drug monitoring (TDM) typically deemed unnecessary. Although the drug label and prior studies suggest rena...
PMC11493394
core_pubmed_pmc
Nanomedicine Therapies for Pediatric Diseases
Nanomedicine Therapies for Pediatric Diseases Abstract ABSTRACT In 2020, the top 10 causes of death among children and adolescents between the ages of 1 and 19 years old included cancer, congenital anomalies, heart disease, and chronic respiratory disease; all these conditions are potentially treatable with medical int...
PMC12702287
core_pubmed_pmc
Use of Neuromuscular Blocking Agents in Elderly Patients: A Narrative Review in Geriatric Medicine
Use of Neuromuscular Blocking Agents in Elderly Patients: A Narrative Review in Geriatric Medicine Abstract Abstract With the growing number of elderly patients undergoing surgical procedures, the use of neuromuscular blocking agents (NMBAs) in geriatric anesthesia has become increasingly relevant. Aging is associated ...
PMC12081364
core_pubmed_pmc
Population pharmacokinetic model of high-dose methotrexate in Chinese patients with intracranial germ cell tumors
Population pharmacokinetic model of high-dose methotrexate in Chinese patients with intracranial germ cell tumors Abstract This study aims to investigate the pharmacokinetics of methotrexate (MTX) in Chinese patients with intracranial germ cell tumors (iGCTs) and to develop a robust population pharmacokinetic (PPK) mod...
PMC11213815
core_pubmed_pmc
Pharmacokinetic Comparison of a Fixed-Dose Combination of Candesartan Cilexetil/Amlodipine/Atorvastatin Versus Co-administration of Individual Formulations in Healthy Participants
Pharmacokinetic Comparison of a Fixed-Dose Combination of Candesartan Cilexetil/Amlodipine/Atorvastatin Versus Co-administration of Individual Formulations in Healthy Participants Abstract Abstract Introduction Fixed-dose combinations (FDCs) of angiotensin II receptor blockers, calcium channel blockers, and statins are...
PMC10511884
core_pubmed_pmc
Synthesis, in-vitro inhibition of cyclooxygenases and in silico studies of new isoxazole derivatives
Synthesis, in-vitro inhibition of cyclooxygenases and in silico studies of new isoxazole derivatives Abstract Isoxazole belongs to the class of five-membered heterocyclic compounds. The process of developing new drugs has significantly gained attention due to inadequate pharmacokinetic and safety attributes of the avai...
PMC12184080
core_pubmed_pmc
Albumin Corona Overturns Long‐Acting Behaviors of Myristic Acid‐Conjugated Quetiapine Nanosuspension
Albumin Corona Overturns Long‐Acting Behaviors of Myristic Acid‐Conjugated Quetiapine Nanosuspension Abstract Abstract This work aimed to investigate the interaction of a self‐assembled myristic acid‐conjugated quetiapine nanosuspension (QMN) with human serum albumin and its overturning effect on QMN's long‐acting perf...
PMC6520324
core_pubmed_pmc
Pharmacokinetics and Safety of Recombinant Human Interleukin-1 Receptor Antagonist GR007 in Healthy Chinese Subjects
Pharmacokinetics and Safety of Recombinant Human Interleukin-1 Receptor Antagonist GR007 in Healthy Chinese Subjects Abstract Background and Objectives The recombinant human interleukin-1 receptor antagonist (rhIL-1Ra) GR007 is a candidate drug with the potential to prevent the toxicity induced by chemotherapy agents b...
PMC11957584
core_pubmed_pmc
Significant PK variability of plasma-derived FIX concentrates in chinese children with Haemophilia B: A fixed single-dose study of factor IX-CTBB
Significant PK variability of plasma-derived FIX concentrates in chinese children with Haemophilia B: A fixed single-dose study of factor IX-CTBB Abstract Background The pharmacokinetics (PK) characters of plasma-derived Factor IX (pdFIX) concentrate in Chinese children with Haemophilia B(HB) have not yet been reported...
PMC12354486
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of NRL-1049, a Rho-Associated Kinase Inhibitor, in Healthy Volunteers: A Phase 1, First-in-Human, Single-Ascending Dose, Randomized, Placebo-Controlled Trial
Safety, Tolerability, and Pharmacokinetics of NRL-1049, a Rho-Associated Kinase Inhibitor, in Healthy Volunteers: A Phase 1, First-in-Human, Single-Ascending Dose, Randomized, Placebo-Controlled Trial Abstract Abstract Background and Objectives Cerebral cavernous malformations (CCMs) are vascular lesions of the brain t...
PMC9298338
core_pubmed_pmc
No significant influence of OCT1 genotypes on the pharmacokinetics of morphine in adult surgical patients
No significant influence of OCT1 genotypes on the pharmacokinetics of morphine in adult surgical patients Abstract Abstract We investigated the impact of genetic variants in OCT1 ( SLC22A1 ) on morphine, morphine‐3‐glucuronide (M3G) and morphine‐6‐glucuronide (M6G) pharmacokinetics in adult patients scheduled for major...
PMC9495994
core_pubmed_pmc
Evaluating Antibody Pharmacokinetics as Prerequisite for Determining True Efficacy as Shown by Dual Targeting of PD-1 and CD96
Evaluating Antibody Pharmacokinetics as Prerequisite for Determining True Efficacy as Shown by Dual Targeting of PD-1 and CD96 Abstract One important prerequisite for developing a therapeutic monoclonal antibody is to evaluate its in vivo efficacy. We tested the therapeutic potential of an anti-CD96 antibody alone or i...
PMC11416364
core_pubmed_pmc
Learning pharmacometric covariate model structures with symbolic regression networks
Learning pharmacometric covariate model structures with symbolic regression networks Abstract Efficiently finding covariate model structures that minimize the need for random effects to describe pharmacological data is challenging. The standard approach focuses on identification of relevant covariates, and present meth...
PMC8123270
core_pubmed_pmc
Xanthohumol for Human Malignancies: Chemistry, Pharmacokinetics and Molecular Targets
Xanthohumol for Human Malignancies: Chemistry, Pharmacokinetics and Molecular Targets Abstract Abstract Xanthohumol (XH) is an important prenylated flavonoid that is found within the inflorescence of Humulus lupulus L. (Hop plant). XH is an important ingredient in beer and is considered a significant bioactive agent du...
PMC6114503
core_pubmed_pmc
Relationship between danofloxacin PK/PD parameters and emergence and mechanism of resistance of Mycoplasma gallisepticum in In Vitro model
Relationship between danofloxacin PK/PD parameters and emergence and mechanism of resistance of Mycoplasma gallisepticum in In Vitro model Abstract Abstract Mycoplasma gallisepticum is a serious pathogen for poultry that causes chronic respiratory disease in chickens. Increased embryonic mortality, as well as reduced w...
PMC12301662
core_pubmed_pmc
Exposure-response analyses of venetoclax combined with hypomethylating agents in myelodysplastic syndromes: a retrospective study
Exposure-response analyses of venetoclax combined with hypomethylating agents in myelodysplastic syndromes: a retrospective study Abstract Background Venetoclax (VEN), an orally bioavailable B-cell lymphoma-2 inhibitor, shows promising activity in patients with myelodysplastic syndromes (MDS) when combined with hypomet...
PMC9155633
core_pubmed_pmc
Vancomycin-arginine (STM-001) abrogates ESBL carrier and carbapenem-resistant Escherichia coli burden in a murine complicated urinary tract infection model
Vancomycin-arginine (STM-001) abrogates ESBL carrier and carbapenem-resistant Escherichia coli burden in a murine complicated urinary tract infection model Abstract Abstract Objectives STM-001, a retargeted glycopeptide, is active against MDR E. coli expressing ESBLs including carbapenemases. Herein, we assessed its ca...
PMC11598598
core_pubmed_pmc
Nose to Brain: Exploring the Progress of Intranasal Delivery of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers
Nose to Brain: Exploring the Progress of Intranasal Delivery of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers Abstract Abstract The intranasal (IN) route of drug delivery can effectively penetrate the blood-brain barrier and deliver drugs directly to the brain for the treatment of central nervous system (...
PMC10107774
core_pubmed_pmc
A Randomized, Placebo‐Controlled Study of Methotrexate to Increase Response Rates in Patients with Uncontrolled Gout Receiving Pegloticase: Primary Efficacy and Safety Findings
A Randomized, Placebo‐Controlled Study of Methotrexate to Increase Response Rates in Patients with Uncontrolled Gout Receiving Pegloticase: Primary Efficacy and Safety Findings Abstract Objective To assess efficacy, safety, pharmacokinetics, and immunogenicity of pegloticase plus methotrexate (MTX) versus pegloticase p...
PMC4067807
core_pubmed_pmc
Two different approaches for pharmacokinetic modeling of exhaled drug concentrations
Two different approaches for pharmacokinetic modeling of exhaled drug concentrations Abstract Abstract Online measurement of drug concentrations in patient's breath is a promising approach for individualized dosage. A direct transfer from breath- to blood-concentrations is not possible. Measured exhaled concentrations ...
PMC12515910
core_pubmed_pmc
Antibiotic-sparing strategies for multidrug-resistant organism (MDRO) infections
Antibiotic-sparing strategies for multidrug-resistant organism (MDRO) infections Abstract The global rise of multidrug-resistant organisms (MDROs), such as carbapenem-resistant Enterobacteriaceae (CRE) and methicillin-resistant Staphylococcus aureus (MRSA), has rendered conventional antibiotics increasingly ineffective...
PMC6271918
core_pubmed_pmc
Determination and Pharmacokinetic Study of Gentiopicroside, Geniposide, Baicalin, and Swertiamarin in Chinese Herbal Formulae after Oral Administration in Rats by LC-MS/MS
Determination and Pharmacokinetic Study of Gentiopicroside, Geniposide, Baicalin, and Swertiamarin in Chinese Herbal Formulae after Oral Administration in Rats by LC-MS/MS Abstract Abstract A sensitive and efficient liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for the simultaneous dete...
PMC11701966
core_pubmed_pmc
Scp776, A Novel IGF‐1 Fusion Protein for Acute Therapy to Promote Escape From Apoptosis in Tissues Affected by Ischemic Injury: 2 Randomized Placebo‐Controlled Phase 1 Studies in Healthy Adults
Scp776, A Novel IGF‐1 Fusion Protein for Acute Therapy to Promote Escape From Apoptosis in Tissues Affected by Ischemic Injury: 2 Randomized Placebo‐Controlled Phase 1 Studies in Healthy Adults Abstract Abstract Apoptosis is a major driver of cell loss and infarct expansion in ischemic injuries such as acute ischemic s...
PMC4424554
core_pubmed_pmc
The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment
The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment Abstract Background HIV-malaria co-infected patients in most parts of sub-Saharan Africa are treated with both artemether-lumefantrine (AL) an...
PMC11651915
core_pubmed_pmc
Small molecule protein assembly modulators with pan-cancer therapeutic efficacy
Small molecule protein assembly modulators with pan-cancer therapeutic efficacy Abstract Two structurally unrelated small molecule chemotypes, represented by compounds PAV-617 and PAV-951, with antiviral activity in cell culture against Mpox virus (formerly known as monkeypox virus) and human immunodeficiency virus (HI...
PMC7323384
core_pubmed_pmc
Timing of Antiviral Treatment Initiation is Critical to Reduce SARS‐CoV‐2 Viral Load
Timing of Antiviral Treatment Initiation is Critical to Reduce SARS‐CoV‐2 Viral Load Abstract Abstract We modeled the viral dynamics of 13 untreated patients infected with severe acute respiratory syndrome‐coronavirus 2 to infer viral growth parameters and predict the effects of antiviral treatments. In order to reduce...
PMC9518288
core_pubmed_pmc
The mechanism and pharmacodynamics of 2-((1H-indol-3-yl)thio/sulfinyl)-N-pheny acetamide derivative as a novel inhibitor against human respiratory syncytial virus
The mechanism and pharmacodynamics of 2-((1H-indol-3-yl)thio/sulfinyl)-N-pheny acetamide derivative as a novel inhibitor against human respiratory syncytial virus Abstract Abstract Human respiratory syncytial virus (RSV) is a leading cause of lower respiratory tract infection worldwide. Until now, there are no licenced...
PMC12027185
core_pubmed_pmc
Pharmacological Behavior of Propylene Glycol/Polyvinyl Alcohol Hydrogel Incorporating Indomethacin Nanocrystals in the Skin
Pharmacological Behavior of Propylene Glycol/Polyvinyl Alcohol Hydrogel Incorporating Indomethacin Nanocrystals in the Skin Abstract Abstract Background: We previously reported that carbopol hydrogels incorporating indomethacin nanoparticles (IMC NPs) improved the low permeability and bioavailability of skin formulatio...
PMC4471648
core_pubmed_pmc
Review of clinical studies of Polygonum multiflorum Thunb. and its isolated bioactive compounds
Review of clinical studies of Polygonum multiflorum Thunb. and its isolated bioactive compounds Abstract Abstract Polygonum multiflorum Thunb. (PMT), officially listed in the Chinese Pharmacopoeia, is one of the most popular perennial Chinese traditional medicines known as He shou wu in China and East Asia, and as Fo-t...
PMC12814311
core_pubmed_pmc
Relative Bioavailability, Food Effect, and Bioequivalence Studies to Assess a New Zanubrutinib 160‐mg Tablet: Results From 2 Phase 1 Studies in Healthy Volunteers
Relative Bioavailability, Food Effect, and Bioequivalence Studies to Assess a New Zanubrutinib 160‐mg Tablet: Results From 2 Phase 1 Studies in Healthy Volunteers Abstract Abstract Zanubrutinib is a next‐generation Bruton tyrosine kinase inhibitor approved for treating B‐cell malignancies. Two phase 1 studies evaluated...
PMC6906481
core_pubmed_pmc
Development of an in silico prediction system of human renal excretion and clearance from chemical structure information incorporating fraction unbound in plasma as a descriptor
Development of an in silico prediction system of human renal excretion and clearance from chemical structure information incorporating fraction unbound in plasma as a descriptor Abstract Abstract Prediction of pharmacokinetic profiles of new chemical entities is essential in drug development to minimize the risks of po...
PMC10523002
core_pubmed_pmc
Nimbolide-based nanomedicine inhibits breast cancer stem-like cells by epigenetic reprogramming of DNMTs-SFRP1-Wnt/β-catenin signaling axis
Nimbolide-based nanomedicine inhibits breast cancer stem-like cells by epigenetic reprogramming of DNMTs-SFRP1-Wnt/β-catenin signaling axis Abstract Abstract Triple-negative breast cancer (TNBC) harbors a high percentage of breast cancer stem-like cells (BCSCs) that significantly contribute to poor prognosis, metastasi...
PMC10817111
core_pubmed_pmc
The impact of biological sex in peripheral nerve blockade: A prospective pharmacodynamic, pharmacokinetic and morphometric study in volunteers
The impact of biological sex in peripheral nerve blockade: A prospective pharmacodynamic, pharmacokinetic and morphometric study in volunteers Abstract Abstract Study objective The impact of biological sex in peripheral regional anaesthesia is largely unknown. We therefore designed a prospective study in volunteers to ...
PMC12868571
core_pubmed_pmc
Case series: Clinical management strategies of pediatric clonazepam poisoning informed by pharmacokinetics
Case series: Clinical management strategies of pediatric clonazepam poisoning informed by pharmacokinetics Abstract Abstract This study aimed to investigate the clinical manifestations of pediatric clonazepam poisoning and to analyze treatment strategies based on its pharmacokinetic characteristics, thereby providing e...
PMC12634716
core_pubmed_pmc
Identification and Evaluation of Natural Compounds as Potential Inhibitors of NS2B-NS3 Zika Virus Protease: A Computational Approach
Identification and Evaluation of Natural Compounds as Potential Inhibitors of NS2B-NS3 Zika Virus Protease: A Computational Approach Abstract Abstract Abstract The Zika virus (ZIKV), an arbovirus within the Flavivirus genus, is associated with severe neurological complications, including Guillain-Barré syndrome in affe...
PMC4060462
core_pubmed_pmc
Induced and pre-existing anti-polyethylene glycol antibody in a trial of every 3-week dosing of pegloticase for refractory gout, including in organ transplant recipients
Induced and pre-existing anti-polyethylene glycol antibody in a trial of every 3-week dosing of pegloticase for refractory gout, including in organ transplant recipients Abstract Introduction Pegloticase, a PEGylated recombinant porcine uricase, is approved for treating refractory gout at a dose of 8 mg intravenous (IV...
PMC10066948
core_pubmed_pmc
Subcutaneous Infliximab Monotherapy Versus Combination Therapy with Immunosuppressants in Inflammatory Bowel Disease: A Post Hoc Analysis of a Randomised Clinical Trial
Subcutaneous Infliximab Monotherapy Versus Combination Therapy with Immunosuppressants in Inflammatory Bowel Disease: A Post Hoc Analysis of a Randomised Clinical Trial Abstract Abstract Background and Objective Whether benefits and risks of intravenous (IV) infliximab combotherapy with immunosuppressants versus inflix...
PMC10092591
core_pubmed_pmc
Challenges in the Development of Intravenous Neurokinin‐1 Receptor Antagonists: Results of a Safety and Pharmacokinetics Dose‐Finding, Phase 1 Study of Intravenous Fosnetupitant
Challenges in the Development of Intravenous Neurokinin‐1 Receptor Antagonists: Results of a Safety and Pharmacokinetics Dose‐Finding, Phase 1 Study of Intravenous Fosnetupitant Abstract Abstract Oral NEPA is the fixed‐combination antiemetic comprising netupitant (neurokinin‐1 receptor antagonist [NK 1 RA]) and palonos...
PMC8795706
core_pubmed_pmc
The Contribution of Liver Sinusoidal Endothelial Cells to Clearance of Therapeutic Antibody
The Contribution of Liver Sinusoidal Endothelial Cells to Clearance of Therapeutic Antibody Abstract Many chronic inflammatory diseases are treated by administration of “biological” therapies in terms of fully human and humanized monoclonal antibodies or Fc fusion proteins. These tools have widespread efficacy and are ...
PMC7760477
core_pubmed_pmc
Pharmacokinetics of Sodium and Calcium Salts of (6S)-5-Methyltetrahydrofolic Acid Compared to Folic Acid and Indirect Comparison of the Two Salts
Pharmacokinetics of Sodium and Calcium Salts of (6S)-5-Methyltetrahydrofolic Acid Compared to Folic Acid and Indirect Comparison of the Two Salts Abstract (6S)-5-Methyltetrahydrofolic acid ((6S)-5-Methyl-THF) salts and folic acid may differ in their abilities to raise plasma (6S)-5-Methyl-THF levels. We compared the ar...
PMC4237897
core_pubmed_pmc
Bioavailability, distribution and clearance of tracheally-instilled and gavaged uncoated or silica-coated zinc oxide nanoparticles
Bioavailability, distribution and clearance of tracheally-instilled and gavaged uncoated or silica-coated zinc oxide nanoparticles Abstract Background Nanoparticle pharmacokinetics and biological effects are influenced by several factors. We assessed the effects of amorphous SiO 2 coating on the pharmacokinetics of zin...
PMC3689918
core_pubmed_pmc
Pharmacokinetics of Coadministered Guanfacine Extended Release and Lisdexamfetamine Dimesylate
Pharmacokinetics of Coadministered Guanfacine Extended Release and Lisdexamfetamine Dimesylate Abstract Abstract Background In clinical practice, α 2 -adrenoceptor agonists have been adjunctively administered with psychostimulants for the treatment of attention-deficit/hyperactivity disorder (ADHD). Two studies have ex...
PMC7136599
core_pubmed_pmc
A pharmacodynamic model of clinical synergy in multiple myeloma
A pharmacodynamic model of clinical synergy in multiple myeloma Abstract Abstract Background Multiagent therapies, due to their ability to delay or overcome resistance, are a hallmark of treatment in multiple myeloma (MM). The growing number of therapeutic options in MM requires high-throughput combination screening to...
PMC6565642
core_pubmed_pmc
Tolvaptan use in children and adolescents with autosomal dominant polycystic kidney disease: rationale and design of a two-part, randomized, double-blind, placebo-controlled trial
Tolvaptan use in children and adolescents with autosomal dominant polycystic kidney disease: rationale and design of a two-part, randomized, double-blind, placebo-controlled trial Abstract This report describes the rationale and design of a study assessing tolvaptan in children with autosomal dominant polycystic kidney...
PMC10388294
core_pubmed_pmc
DruMAP: A Novel Drug Metabolism and Pharmacokinetics Analysis Platform
DruMAP: A Novel Drug Metabolism and Pharmacokinetics Analysis Platform Abstract We developed a novel drug metabolism and pharmacokinetics (DMPK) analysis platform named DruMAP. This platform consists of a database for DMPK parameters and programs that can predict many DMPK parameters based on the chemical structure of ...
PMC9806926
core_pubmed_pmc
Nirmatrelvir and COVID-19: development, pharmacokinetics, clinical efficacy, resistance, relapse, and pharmacoeconomics
Nirmatrelvir and COVID-19: development, pharmacokinetics, clinical efficacy, resistance, relapse, and pharmacoeconomics Abstract Abstract Nirmatrelvir/ritonavir (N/R) is one of the most effective antiviral drugs against SARS-CoV-2. The preclinical development, pharmacodynamics and pharmacokinetics of N/R are reviewed h...
PMC10460751
core_pubmed_pmc
Generation and application of avatars in pharmacometric modelling
Generation and application of avatars in pharmacometric modelling Abstract Simulations from population models have critical applications in drug discovery and development. Avatars or digital twins, defined as individual simulations matching clinical criteria of interest compared to observations from a real subject with...
PMC11448427
core_pubmed_pmc
Efficacy and safety of olezarsen in lowering apolipoprotein C-III and triglycerides in healthy Japanese Americans
Efficacy and safety of olezarsen in lowering apolipoprotein C-III and triglycerides in healthy Japanese Americans Abstract Abstract Background Olezarsen is a GalNAc 3 -conjugated, hepatic-targeted antisense oligonucleotide that lowers apolipoprotein C-III (apoC-III) and triglyceride levels. The efficacy and safety of o...
PMC4041957
core_pubmed_pmc
Correction of target-controlled infusion following wrong selection of emulsion concentrations of propofol
Correction of target-controlled infusion following wrong selection of emulsion concentrations of propofol Abstract Background We investigated the correction methods following wrong-settings of emulsion concentrations of propofol as a countermeasure against erroneous target-controlled infusions (TCI). Methods TCIs were ...
PMC8112138
core_pubmed_pmc
Designing and Development of a Tandem Bivalent Nanobody against VEGF 165
Designing and Development of a Tandem Bivalent Nanobody against VEGF 165 Abstract Abstract Background: Inhibition of angiogenesis using monoclonal antibodies is an effective strategy in cancer therapy. However, they could not penetrate sufficiently into solid tumors. Antibody fragments have solved this issue. However, ...
PMC7828117
core_pubmed_pmc
Pharmacokinetic—Pharmacodynamic Modeling of Tumor Targeted Drug Delivery Using Nano-Engineered Mesenchymal Stem Cells
Pharmacokinetic—Pharmacodynamic Modeling of Tumor Targeted Drug Delivery Using Nano-Engineered Mesenchymal Stem Cells Abstract Abstract Nano-engineered mesenchymal stem cells (nano-MSCs) are promising targeted drug delivery platforms for treating solid tumors. MSCs engineered with paclitaxel (PTX) loaded poly(lactide-c...
PMC7397437
core_pubmed_pmc
The Effect of Coffee on Pharmacokinetic Properties of Drugs : A Review
The Effect of Coffee on Pharmacokinetic Properties of Drugs : A Review Abstract Abstract Background Coffee has been the most commercialized food product and most widely consumed stimulant beverage in the world. It is a major source of caffeine which is the most bioactive component of coffee. Although both the United St...
PMC8760752
core_pubmed_pmc
Off-label use of combined antiretroviral therapy, analysis of data collected by the Italian Register for HIV-1 infection in paediatrics in a large cohort of children
Off-label use of combined antiretroviral therapy, analysis of data collected by the Italian Register for HIV-1 infection in paediatrics in a large cohort of children Abstract Abstract Background Early start of highly active antiretroviral therapy (HAART) in perinatally HIV-1 infected children is the optimal strategy to...
PMC4417951
core_pubmed_pmc
Contribution of Organ Vasculature in Rat Renal Analysis for Ochratoxin A: Relevance to Toxicology of Nephrotoxins
Contribution of Organ Vasculature in Rat Renal Analysis for Ochratoxin A: Relevance to Toxicology of Nephrotoxins Abstract Abstract Assumptions surrounding the kidney as a target for accumulation of ochratoxin A (OTA) are addressed because the contribution of the toxin in blood seems invariably to have been ignored. Ad...
PMC10674169
core_pubmed_pmc
PBPK Modeling of Azithromycin Systemic Exposure in a Roux-en-Y Gastric Bypass Surgery Patient Population
PBPK Modeling of Azithromycin Systemic Exposure in a Roux-en-Y Gastric Bypass Surgery Patient Population Abstract Abstract In this investigation, PBPK modeling using the Simcyp ® Simulator was performed to evaluate whether Roux-en-Y gastric bypass (RYGB) surgery impacts the oral absorption and bioavailability of azithr...
PMC5051080
core_pubmed_pmc
Safety, pharmacokinetics, and antitumor properties of anlotinib, an oral multi-target tyrosine kinase inhibitor, in patients with advanced refractory solid tumors
Safety, pharmacokinetics, and antitumor properties of anlotinib, an oral multi-target tyrosine kinase inhibitor, in patients with advanced refractory solid tumors Abstract Background Anlotinib is a novel multi-target tyrosine kinase inhibitor that is designed to primarily inhibit VEGFR2/3, FGFR1-4, PDGFR α/β, c-Kit, an...
PMC11459894
core_pubmed_pmc
Monte Carlo simulations of cefepime in children receiving continuous kidney replacement therapy support continuous infusions for target attainment
Monte Carlo simulations of cefepime in children receiving continuous kidney replacement therapy support continuous infusions for target attainment Abstract Background Sepsis is a leading cause of acute kidney injury requiring continuous kidney replacement therapy (CKRT) and CKRT can alter drug pharmacokinetics (PK). Ce...
PMC8352697
core_pubmed_pmc
Chemical Fingerprint Profiles and Pharmacodynamic Investigation for Quality Evaluation of Moxa Smoke by UHPLC in a Rat Model of Superficial Infection
Chemical Fingerprint Profiles and Pharmacodynamic Investigation for Quality Evaluation of Moxa Smoke by UHPLC in a Rat Model of Superficial Infection Abstract Abstract Introduction Moxibustion, a traditional Chinese medicine technique, involves the use of moxa smoke from Folium Artemisia argyi to treat various disorder...
PMC8377441
core_pubmed_pmc
Reactive oxygen species-based nanomaterials for the treatment of myocardial ischemia reperfusion injuries
Reactive oxygen species-based nanomaterials for the treatment of myocardial ischemia reperfusion injuries Abstract Interventional coronary reperfusion strategies are widely adopted to treat acute myocardial infarction, but morbidity and mortality of acute myocardial infarction are still high. Reperfusion injuries are i...
PMC8563558
core_pubmed_pmc
Ceftaroline Fosamil for Treatment of Pediatric Complicated Skin and Soft Tissue Infections and Community-Acquired Pneumonia
Ceftaroline Fosamil for Treatment of Pediatric Complicated Skin and Soft Tissue Infections and Community-Acquired Pneumonia Abstract Abstract Community-acquired pneumonia (CAP)/community-acquired bacterial pneumonia (CABP) and complicated skin and soft tissue infection (cSSTI)/acute bacterial skin and skin structure in...
PMC4317910
core_pubmed_pmc
Phase I study of olaratumab in Japanese patients with advanced solid tumors
Phase I study of olaratumab in Japanese patients with advanced solid tumors Abstract Olaratumab (IMC-3G3) is a fully human IgG1 monoclonal antibody that selectively binds the external domain of human platelet-derived growth factor receptor-α with high affinity and blocks ligand binding. This was a single-center, dose-e...
PMC12968473
core_pubmed_pmc
Time Kill Curve PD Modelling Experiments Are Affected by Trailing MIC Endpoints: Refinement of MIC Determination for S. pseudintermedius
Time Kill Curve PD Modelling Experiments Are Affected by Trailing MIC Endpoints: Refinement of MIC Determination for S. pseudintermedius Abstract ABSTRACT Trailing endpoints are a recognised challenge in broth microdilution MIC testing, particularly for bacteriostatic agents such as trimethoprim (TMP) and sulphonamides...
PMC7385956
core_pubmed_pmc
The pharmacological and clinical aspects behind dose loading of biological disease modifying anti-rheumatic drugs (bDMARDs) in auto-immune rheumatic diseases (AIRDs): rationale and systematic narrative review of clinical evidence
The pharmacological and clinical aspects behind dose loading of biological disease modifying anti-rheumatic drugs (bDMARDs) in auto-immune rheumatic diseases (AIRDs): rationale and systematic narrative review of clinical evidence Abstract Abstract Background Dose loading of biological disease modifying anti-rheumatic d...
PMC5036422
core_pubmed_pmc
Predictive Performance of Physiologically Based Pharmacokinetic and Population Pharmacokinetic Modeling of Renally Cleared Drugs in Children
Predictive Performance of Physiologically Based Pharmacokinetic and Population Pharmacokinetic Modeling of Renally Cleared Drugs in Children Abstract Predictive performance of physiologically based pharmacokinetic (PBPK) and population pharmacokinetic (PopPK) models of drugs predominantly eliminated through kidney in t...
PMC8844785
core_pubmed_pmc
A phase I/IIa trial of atorvastatin in Japanese patients with acute Kawasaki disease with coronary artery aneurysm: Study protocol of a multicenter, single-arm, open-label trial
A phase I/IIa trial of atorvastatin in Japanese patients with acute Kawasaki disease with coronary artery aneurysm: Study protocol of a multicenter, single-arm, open-label trial Abstract Background Kawasaki disease (KD) is a systemic vasculitis complicated with coronary artery abnormalities (CAAs). Intravenous immunogl...
PMC9250994
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of Fostamatinib and Its Active Moiety R406
Clinical Pharmacokinetics and Pharmacodynamics of Fostamatinib and Its Active Moiety R406 Abstract Abstract Fostamatinib is the first approved spleen tyrosine kinase inhibitor for chronic immune thrombocytopenia. This review summarizes the clinical development, pharmacokinetics, pharmacodynamics, drug–drug interactions...
PMC7757196
core_pubmed_pmc
Ex vivo gadoxetate relaxivities in rat liver tissue and blood at five magnetic field strengths from 1.41 to 7 T
Ex vivo gadoxetate relaxivities in rat liver tissue and blood at five magnetic field strengths from 1.41 to 7 T Abstract Abstract Quantitative mapping of gadoxetate uptake and excretion rates in liver cells has shown potential to significantly improve the management of chronic liver disease and liver cancer. Unfortunat...
PMC10215385
core_pubmed_pmc
Beta-Lactam Dose Optimisation in the Intensive Care Unit: Targets, Therapeutic Drug Monitoring and Toxicity
Beta-Lactam Dose Optimisation in the Intensive Care Unit: Targets, Therapeutic Drug Monitoring and Toxicity Abstract Abstract Beta-lactams are an important family of antibiotics used to treat infections and are commonly used in critically ill patients. Optimal use of these drugs in the intensive care unit (ICU) is impo...
PMC9103789
core_pubmed_pmc
Examination of the Impact of CYP3A4/5 on Drug–Drug Interaction between Schizandrol A/Schizandrol B and Tacrolimus (FK-506): A Physiologically Based Pharmacokinetic Modeling Approach
Examination of the Impact of CYP3A4/5 on Drug–Drug Interaction between Schizandrol A/Schizandrol B and Tacrolimus (FK-506): A Physiologically Based Pharmacokinetic Modeling Approach Abstract Schizandrol A (SZA) and schizandrol B (SZB) are two active ingredients of Wuzhi capsule (WZC), a Chinese proprietary medicine com...
PMC4467139
core_pubmed_pmc
Garcinol sensitizes human head and neck carcinoma to cisplatin in a xenograft mouse model despite downregulation of proliferative biomarkers
Garcinol sensitizes human head and neck carcinoma to cisplatin in a xenograft mouse model despite downregulation of proliferative biomarkers Abstract Abstract Platinum compounds such as cisplatin and carboplatin are frequently used as the first-line chemotherapy for the treatment of the head and neck squamous cell carc...