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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... |
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