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PMC9135478 | core_pubmed_pmc | Immune Tolerance Induction (ITI) with a pdFVIII/VWF Concentrate (octanate) in 100 Patients in the Observational ITI (ObsITI) Study | Immune Tolerance Induction (ITI) with a pdFVIII/VWF Concentrate (octanate) in 100 Patients in the Observational ITI (ObsITI) Study Abstract Background Immune tolerance induction (ITI) with repeated factor VIII (FVIII) administration is the only strategy proven to eradicate inhibitors. The observational ITI study is eva... |
PMC12146923 | core_pubmed_pmc | Plant extracts with antioxidant and hepatoprotective benefits for liver health: A bibliometric analysis of drug delivery systems | Plant extracts with antioxidant and hepatoprotective benefits for liver health: A bibliometric analysis of drug delivery systems Abstract BACKGROUND The rising global burden of liver diseases, such as non-alcoholic fatty liver disease and liver fibrosis, has necessitated innovative therapeutic approaches. Plant-based t... |
PMC7862084 | core_pubmed_pmc | Different Fumaric Acid Esters Elicit Distinct Pharmacologic Responses | Different Fumaric Acid Esters Elicit Distinct Pharmacologic Responses Abstract Abstract Objective To test the hypothesis that dimethyl fumarate (DMF, Tecfidera) elicits different biological changes from DMF combined with monoethyl fumarate (MEF) (Fumaderm, a psoriasis therapy), we investigated DMF and MEF in rodents an... |
PMC12587539 | core_pubmed_pmc | Model-informed drug development in public health emergency of international concern: accelerating marketing authorization of simnotrelvir | Model-informed drug development in public health emergency of international concern: accelerating marketing authorization of simnotrelvir Abstract ABSTRACT During a Public Health Emergency of International Concern (PHEIC), rapid drug development is critical, but traditional clinical trials are time-consuming and high-r... |
PMC6955804 | core_pubmed_pmc | RETRACTED: Attenuation of Benign Prostatic Hyperplasia by Optimized Tadalafil Loaded Pumpkin Seed Oil-Based Self Nanoemulsion: In Vitro and In Vivo Evaluation | RETRACTED: Attenuation of Benign Prostatic Hyperplasia by Optimized Tadalafil Loaded Pumpkin Seed Oil-Based Self Nanoemulsion: In Vitro and In Vivo Evaluation Abstract The FDA has approved tadalafil (TDL) for the treatment of benign prostatic hyperplasia (BPH)-associated symptoms. Pumpkin seed oil (PSO) has shown promi... |
PMC9171282 | core_pubmed_pmc | Therapeutic drug monitoring of biopharmaceuticals in inflammatory rheumatic and musculoskeletal disease: a systematic literature review informing EULAR points to consider | Therapeutic drug monitoring of biopharmaceuticals in inflammatory rheumatic and musculoskeletal disease: a systematic literature review informing EULAR points to consider Abstract Abstract The objectives of this review were to collect and summarise evidence on therapeutic drug monitoring (TDM) of biopharmaceuticals in ... |
PMC7738956 | core_pubmed_pmc | Inhibition of human amylin aggregation by Flavonoid Chrysin: An in-silico and in-vitro approach | Inhibition of human amylin aggregation by Flavonoid Chrysin: An in-silico and in-vitro approach Abstract Abstract Islet amyloid polypeptide (amylin), consecrated by the pancreatic β-cells with insulin, has a significant role to play in maintaining homeostasis of islet cell hormones. Alzheimer's disease is the predomina... |
PMC10505864 | core_pubmed_pmc | Cytotoxicity Activity of Graviola Fruit Extract with Carbamazepine and Valproic Acid Show Antagonistic and Indifferent Effects | Cytotoxicity Activity of Graviola Fruit Extract with Carbamazepine and Valproic Acid Show Antagonistic and Indifferent Effects Abstract Objective: Graviola is a tropical fruit with medicinal properties, used for treating various diseases such as inflammation, diabetes, and cancer. Histone deacetylase inhibitors (HDACIs... |
PMC10870118 | core_pubmed_pmc | Phase Ia/b Study of Giredestrant ± Palbociclib and ± Luteinizing Hormone-Releasing Hormone Agonists in Estrogen Receptor–Positive, HER2-Negative, Locally Advanced/Metastatic Breast Cancer | Phase Ia/b Study of Giredestrant ± Palbociclib and ± Luteinizing Hormone-Releasing Hormone Agonists in Estrogen Receptor–Positive, HER2-Negative, Locally Advanced/Metastatic Breast Cancer Abstract Abstract Purpose: Giredestrant is an investigational next-generation, oral, selective estrogen receptor antagonist and degr... |
PMC10298764 | core_pubmed_pmc | Pharmacokinetics, feasibility and safety of co-administering azithromycin, albendazole, and ivermectin during mass drug administration: A review | Pharmacokinetics, feasibility and safety of co-administering azithromycin, albendazole, and ivermectin during mass drug administration: A review Abstract Introduction Traditionally, health ministries implement mass drug administration programmes for each neglected tropical disease (NTD) as separate and distinct campaig... |
PMC10451719 | core_pubmed_pmc | Melatonin as a Therapy for Preterm Brain Injury: What Is the Evidence? | Melatonin as a Therapy for Preterm Brain Injury: What Is the Evidence? Abstract Despite significant improvements in survival following preterm birth in recent years, the neurodevelopmental burden of prematurity, with its long-term cognitive and behavioral consequences, remains a significant challenge in neonatology. Ne... |
PMC6775268 | core_pubmed_pmc | Effects of semi-solidification of enteral nutrients on the pharmacokinetic behavior of orally administered carbamazepine in rats | Effects of semi-solidification of enteral nutrients on the pharmacokinetic behavior of orally administered carbamazepine in rats Abstract Abstract The use of semi-solid enteral nutrients plays an extremely important role in accurate nutrition management. In the present study, we compared the pharmacokinetic profile of ... |
PMC3414212 | core_pubmed_pmc | Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study | Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study Abstract Abstract Background The clinical application of nimodipine (NIM) is limited by several unfavorable properties, which are induced by its low aqueous solubility. In the present study, nimodipine-loaded... |
PMC7282712 | core_pubmed_pmc | A New Oral Testosterone Undecanoate Formulation Restores Testosterone to Normal Concentrations in Hypogonadal Men | A New Oral Testosterone Undecanoate Formulation Restores Testosterone to Normal Concentrations in Hypogonadal Men Abstract Abstract Context A novel formulation of oral testosterone (T) undecanoate (TU) was evaluated in a phase 3 clinical trial. Objective Determine efficacy, short-term safety, and alignment of new oral ... |
PMC8604240 | core_pubmed_pmc | Evaluation of drug‐drug interaction potential between omecamtiv mecarbil and rosuvastatin, a BCRP substrate, with a clinical study in healthy subjects and using a physiologically‐based pharmacokinetic model | Evaluation of drug‐drug interaction potential between omecamtiv mecarbil and rosuvastatin, a BCRP substrate, with a clinical study in healthy subjects and using a physiologically‐based pharmacokinetic model Abstract Abstract Omecamtiv mecarbil (OM) is a novel cardiac myosin activator in development for the treatment of... |
PMC7507523 | core_pubmed_pmc | Risk to human health related to the presence of perfluoroalkyl substances in food | Risk to human health related to the presence of perfluoroalkyl substances in food Abstract Abstract The European Commission asked EFSA for a scientific evaluation on the risks to human health related to the presence of perfluoroalkyl substances ( PFAS s) in food. Based on several similar effects in animals, toxicokinet... |
PMC7939741 | core_pubmed_pmc | Despite Blocking Doxorubicin-Induced Vascular Damage, Quercetin Ameliorates Its Antibreast Cancer Activity | Despite Blocking Doxorubicin-Induced Vascular Damage, Quercetin Ameliorates Its Antibreast Cancer Activity Abstract Quercetin is a naturally occurring flavonol present in many foods. Doxorubicin is an effective anticancer agent despite its dose-limiting cardiovascular toxicity. Herein, we investigated the potential pro... |
PMC11785799 | core_pubmed_pmc | Fragment optimized chalcone derivatives targeting OmpA protein as a therapeutic approach against multidrug resistant Acinetobacter baumannii | Fragment optimized chalcone derivatives targeting OmpA protein as a therapeutic approach against multidrug resistant Acinetobacter baumannii Abstract Acinetobacter baumannii is a notorious pathogen associated with life-threatening infections, with its outer membrane protein A ( OmpA ) being a key contributor to its pat... |
PMC11633683 | core_pubmed_pmc | The implications of frailty in older adults with epilepsy | The implications of frailty in older adults with epilepsy Abstract Abstract Older adults constitute a large proportion of people with epilepsy (PWE) due to the changing demographics worldwide and epilepsy's natural history. Aging‐related pathophysiological changes lower the tolerance and increase our vulnerability to s... |
PMC6994455 | core_pubmed_pmc | SAGE-217, A Novel GABA A Receptor Positive Allosteric Modulator: Clinical Pharmacology and Tolerability in Randomized Phase I Dose-Finding Studies | SAGE-217, A Novel GABA A Receptor Positive Allosteric Modulator: Clinical Pharmacology and Tolerability in Randomized Phase I Dose-Finding Studies Abstract Abstract Background SAGE-217, a novel γ-aminobutyric acid A (GABA A ) receptor positive allosteric modulator, was evaluated in phase I, double-blind, placebo-contro... |
PMC7093107 | core_pubmed_pmc | Randomized, Double-Masked, Placebo-Controlled Dose Escalation Study of TAK-639 Topical Ophthalmic Solution in Subjects with Ocular Hypertension or Primary Open-Angle Glaucoma | Randomized, Double-Masked, Placebo-Controlled Dose Escalation Study of TAK-639 Topical Ophthalmic Solution in Subjects with Ocular Hypertension or Primary Open-Angle Glaucoma Abstract Abstract Purpose TAK-639 is a topical, nine-amino acid, synthetic, C-type natriuretic peptide analog in Phase 1 development for the trea... |
PMC11768185 | core_pubmed_pmc | Development and Application of Physiologically-Based Pharmacokinetic Model to Predict Systemic and Organ Exposure of Colorectal Cancer Drugs | Development and Application of Physiologically-Based Pharmacokinetic Model to Predict Systemic and Organ Exposure of Colorectal Cancer Drugs Abstract Background/Objectives: Colorectal cancer (CRC) holds the third and second position among cancers affecting men and women, respectively. Frequently, the first-line treatme... |
PMC9939828 | core_pubmed_pmc | Pharmacokinetics of single- and multiple-dose flumatinib in patients with chronic phase chronic myeloid leukemia | Pharmacokinetics of single- and multiple-dose flumatinib in patients with chronic phase chronic myeloid leukemia Abstract Introduction Flumatinib is a novel, oral breakpoint cluster region-abelson (BCR-ABL) tyrosine kinase inhibitor that has demonstrated manageable safety and promising efficacy in patients with newly d... |
PMC6055687 | core_pubmed_pmc | Single and multiple dose evaluation of a novel MetAP2 inhibitor: Results of a randomized, double‐blind, placebo‐controlled clinical trial | Single and multiple dose evaluation of a novel MetAP2 inhibitor: Results of a randomized, double‐blind, placebo‐controlled clinical trial Abstract Aims Methionine aminopeptidase 2 (MetAP2) inhibition has been shown to result in significant weight loss and improved glucose control. This Phase 1 clinical trial assessed t... |
PMC11004774 | core_pubmed_pmc | Application of the Hollow-Fiber Infection Model to Personalized Precision Dosing of Isoniazid in a Clinical Setting | Application of the Hollow-Fiber Infection Model to Personalized Precision Dosing of Isoniazid in a Clinical Setting Abstract Background The hollow-fiber infection model (HFIM) is a valuable tool for evaluating pharmacokinetics/pharmacodynamics relationships and determining the optimal antibiotic dose in monotherapy or ... |
PMC6394493 | core_pubmed_pmc | A phase I study of single-agent BEZ235 special delivery system sachet in Japanese patients with advanced solid tumors | A phase I study of single-agent BEZ235 special delivery system sachet in Japanese patients with advanced solid tumors Abstract Abstract Purpose BEZ235 is a dual kinase inhibitor of phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin, which are key components of the PI3K pathway. This was an open-labe... |
PMC7385074 | core_pubmed_pmc | Pharmacokinetics/Pharmacodynamics of Antiviral Agents Used to Treat SARS-CoV-2 and Their Potential Interaction with Drugs and Other Supportive Measures: A Comprehensive Review by the PK/PD of Anti-Infectives Study Group of the European Society of Antimicrobial Agents | Pharmacokinetics/Pharmacodynamics of Antiviral Agents Used to Treat SARS-CoV-2 and Their Potential Interaction with Drugs and Other Supportive Measures: A Comprehensive Review by the PK/PD of Anti-Infectives Study Group of the European Society of Antimicrobial Agents Abstract Abstract There is an urgent need to identif... |
PMC9337295 | core_pubmed_pmc | High-throughput liquid chromatography tandem mass spectrometry method for simultaneous determination of fampridine, paroxetine, and quinidine in rat plasma: Application to in vivo perfusion study | High-throughput liquid chromatography tandem mass spectrometry method for simultaneous determination of fampridine, paroxetine, and quinidine in rat plasma: Application to in vivo perfusion study Abstract Abstract A selective and high-throughput liquid chromatography–mass spectrometry method has been developed and vali... |
PMC7513348 | core_pubmed_pmc | Chiral Chromatographic Isolation on Milligram Scale of the Human African Trypanosomiasis Treatment d - and l -Eflornithine | Chiral Chromatographic Isolation on Milligram Scale of the Human African Trypanosomiasis Treatment d - and l -Eflornithine Abstract Abstract Eflornithine is a recommended treatment against the otherwise fatal parasitic disease late stage human African trypanosomiasis (HAT), also known as Gambian sleeping sickness. It i... |
PMC11345944 | core_pubmed_pmc | More Than a Gut Feeling—A Combination of Physiologically Driven Dissolution and Pharmacokinetic Modeling as a Tool for Understanding Human Gastric Motility | More Than a Gut Feeling—A Combination of Physiologically Driven Dissolution and Pharmacokinetic Modeling as a Tool for Understanding Human Gastric Motility Abstract Abstract In vivo studies of formulation performance with in vitro and/or in silico simulations are often limited by significant gaps in our knowledge of th... |
PMC12655103 | core_pubmed_pmc | Harnessing Nature for Breast Cancer Management: Effects of Fisetin-Loaded Nigellasomes Embedded in Microneedles Improve Tumor Suppression and Reduce Oxidative Stress | Harnessing Nature for Breast Cancer Management: Effects of Fisetin-Loaded Nigellasomes Embedded in Microneedles Improve Tumor Suppression and Reduce Oxidative Stress Abstract Abstract Background : Natural compounds such as fisetin have promising in breast cancer treatment, but their poor pharmacokinetics limit their th... |
PMC9587026 | core_pubmed_pmc | SPINA Carb: a simple mathematical model supporting fast in-vivo estimation of insulin sensitivity and beta cell function | SPINA Carb: a simple mathematical model supporting fast in-vivo estimation of insulin sensitivity and beta cell function Abstract Modelling insulin-glucose homeostasis may provide novel functional insights. In particular, simple models are clinically useful if they yield diagnostic methods. Examples include the homeost... |
PMC7658092 | core_pubmed_pmc | Population Modelling of Dexmedetomidine Pharmacokinetics and Haemodynamic Effects After Intravenous and Subcutaneous Administration | Population Modelling of Dexmedetomidine Pharmacokinetics and Haemodynamic Effects After Intravenous and Subcutaneous Administration Abstract Background and Objective Dexmedetomidine is a potent agonist of α 2 -adrenoceptors causing dose-dependent sedation in humans. Intravenous dexmedetomidine is commonly used perioper... |
PMC12030391 | core_pubmed_pmc | Drug Discovery for Histone Deacetylase Inhibition: Past, Present and Future of Zinc-Binding Groups | Drug Discovery for Histone Deacetylase Inhibition: Past, Present and Future of Zinc-Binding Groups Abstract Abstract Histone deacetylases (HDACs) are key regulators of gene expression, influencing chromatin remodeling and playing a crucial role in various physiological and pathological processes. Aberrant HDAC activity... |
PMC12473801 | core_pubmed_pmc | A Comprehensive Physiologically Based Pharmacokinetic Framework of Ofloxacin: Predicting Disposition in Renal Impairment | A Comprehensive Physiologically Based Pharmacokinetic Framework of Ofloxacin: Predicting Disposition in Renal Impairment Abstract Background : In the last several years, “physiologically based pharmacokinetic (PBPK) modeling” has gathered significant emphasis in the modeling of drug absorption, disposition, and metabol... |
PMC10844532 | core_pubmed_pmc | The in vivo study on antioxidant activity of wendan decoction in treating hyperlipidemia: a pharmacokinetic-pharmacodynamic (PK-PD) model | The in vivo study on antioxidant activity of wendan decoction in treating hyperlipidemia: a pharmacokinetic-pharmacodynamic (PK-PD) model Abstract Background: Wendan Decoction (WDD) is a six-herb Chinese medicine recipe that was first mentioned in about 652 AD. It is frequently used to treat hyperlipidemic patients’ cl... |
PMC12727974 | core_pubmed_pmc | Lentinan inhibits colorectal cancer stemness by binding CD133 and suppressing the CD133/p85/p-AKT signaling axis | Lentinan inhibits colorectal cancer stemness by binding CD133 and suppressing the CD133/p85/p-AKT signaling axis Abstract Background Colorectal cancer (CRC) ranks third in the global cancer incidence rate worldwide. Cancer stem cells (CSCs) are key drivers of CRC recurrence, metastasis, and therapy resistance, while th... |
PMC6224042 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of long-acting injectable cabotegravir in low-risk HIV-uninfected individuals: HPTN 077, a phase 2a randomized controlled trial | Safety, tolerability, and pharmacokinetics of long-acting injectable cabotegravir in low-risk HIV-uninfected individuals: HPTN 077, a phase 2a randomized controlled trial Abstract Abstract Background Cabotegravir (CAB) is a novel strand-transfer integrase inhibitor being developed for HIV treatment and prevention. CAB ... |
PMC3586167 | core_pubmed_pmc | Cardiovascular Safety of Anagrelide in Healthy Subjects: Effects of Caffeine and Food Intake on Pharmacokinetics and Adverse Reactions | Cardiovascular Safety of Anagrelide in Healthy Subjects: Effects of Caffeine and Food Intake on Pharmacokinetics and Adverse Reactions Abstract Background Essential thrombocythaemia (ET) is a rare clonal myeloproliferative disorder characterized by a sustained elevation in platelet count and megakaryocyte hyperplasia. ... |
PMC12275966 | core_pubmed_pmc | Remimazolam as a Novel Anesthetic in Pediatric Procedural Sedation and Anesthesia: A Narrative Review | Remimazolam as a Novel Anesthetic in Pediatric Procedural Sedation and Anesthesia: A Narrative Review Abstract As an ultra-short-acting benzodiazepine, remimazolam demonstrates rapid onset, quick offset, and a short half-life. Current evidence suggests that its metabolism is not dependent on hepatic or renal function, ... |
PMC8492211 | core_pubmed_pmc | Tenofovir Diphosphate Concentrations in Dried Blood Spots From Pregnant and Postpartum Adolescent and Young Women Receiving Daily Observed Pre-exposure Prophylaxis in Sub-Saharan Africa | Tenofovir Diphosphate Concentrations in Dried Blood Spots From Pregnant and Postpartum Adolescent and Young Women Receiving Daily Observed Pre-exposure Prophylaxis in Sub-Saharan Africa Abstract Abstract Background Intracellular tenofovir diphosphate (TFV-DP) concentration in dried blood spots (DBSs) is used to monitor... |
PMC3049499 | core_pubmed_pmc | Intravenous anakinra can achieve experimentally effective concentrations in the central nervous system within a therapeutic time window: results of a dose-ranging study | Intravenous anakinra can achieve experimentally effective concentrations in the central nervous system within a therapeutic time window: results of a dose-ranging study Abstract Abstract The naturally occurring antagonist of interleukin-1, IL-1RA, is highly neuroprotective experimentally, shows few adverse effects, and... |
PMC11703263 | core_pubmed_pmc | NECTIN-4 PET FOR OPTIMIZING ENFORTUMAB VEDOTIN DOSE-RESPONSE IN UROTHELIAL CARCINOMA | NECTIN-4 PET FOR OPTIMIZING ENFORTUMAB VEDOTIN DOSE-RESPONSE IN UROTHELIAL CARCINOMA Abstract Abstract The optimization of dosing strategies is critical for maximizing efficacy and minimizing toxicity in drug development, particularly for drugs with narrow therapeutic windows such as antibody-drug conjugates (ADCs). Th... |
PMC11729552 | core_pubmed_pmc | A novel ROR1-targeting antibody-PROTAC conjugate promotes BRD4 degradation for solid tumor treatment | A novel ROR1-targeting antibody-PROTAC conjugate promotes BRD4 degradation for solid tumor treatment Abstract Rationale: Proteolysis Targeting Chimeras (PROTACs) are bifunctional compounds that have been extensively studied for their role in targeted protein degradation (TPD). The capacity to degrade validated or undru... |
PMC12885395 | core_pubmed_pmc | Dual agonism and selective T-cell depletion activity of a PD-1-directed antibody for treating autoimmune diseases | Dual agonism and selective T-cell depletion activity of a PD-1-directed antibody for treating autoimmune diseases Abstract ABSTRACT Precise inhibition of autoreactivity without concomitant induction of general immunosuppression is an overarching goal that remains elusive for the treatment of autoimmune diseases. PD-1 i... |
PMC11619402 | core_pubmed_pmc | In vivo efficacy of enmetazobactam combined with cefepime in a murine pneumonia model induced by OXA-48-producing Klebsiella pneumoniae | In vivo efficacy of enmetazobactam combined with cefepime in a murine pneumonia model induced by OXA-48-producing Klebsiella pneumoniae Abstract ABSTRACT Cefepime/enmetazobactam is a new β-lactam/β-lactamase inhibitor combination with broad-spectrum activity against multidrug-resistant Enterobacterales, including OXA-4... |
PMC6219560 | core_pubmed_pmc | An Electroencephalography Bioassay for Preclinical Testing of Analgesic Efficacy | An Electroencephalography Bioassay for Preclinical Testing of Analgesic Efficacy Abstract We present a multimodal method combining quantitative electroencephalography (EEG), behavior and pharmacology for pre-clinical screening of analgesic efficacy in vivo . The method consists of an objective and non-invasive approach... |
PMC11335985 | core_pubmed_pmc | Radiosynthesis and preclinical evaluation of a 68 Ga-labeled tetrahydroisoquinoline-based ligand for PET imaging of C-X-C chemokine receptor type 4 in an animal model of glioblastoma | Radiosynthesis and preclinical evaluation of a 68 Ga-labeled tetrahydroisoquinoline-based ligand for PET imaging of C-X-C chemokine receptor type 4 in an animal model of glioblastoma Abstract Background This study aimed to develop a novel positron emission tomography (PET) tracer, [ 68 Ga]Ga-TD-01, for CXCR4 imaging. T... |
PMC10609870 | core_pubmed_pmc | Hydrogel-Based Microneedle as a Drug Delivery System | Hydrogel-Based Microneedle as a Drug Delivery System Abstract Abstract The skin is considered the largest and most accessible organ in the human body, and allows the use of noninvasive and efficient strategies for drug administration, such as the transdermal drug delivery system (TDDS). TDDSs are systems or patches, wi... |
PMC9871362 | core_pubmed_pmc | Metabolomic mechanism and pharmacodynamic material basis of Buxue Yimu pills in the treatment of anaemia in women of reproductive age | Metabolomic mechanism and pharmacodynamic material basis of Buxue Yimu pills in the treatment of anaemia in women of reproductive age Abstract Abstract Objective: To explore the pharmacological basis and mechanism of Buxue Yimu pills (BYP) in the treatment of anaemia in women from the perspective of metabolomics and ne... |
PMC5042051 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of mepolizumab, an anti–interleukin 5 monoclonal antibody, in healthy Japanese male subjects | Pharmacokinetics and pharmacodynamics of mepolizumab, an anti–interleukin 5 monoclonal antibody, in healthy Japanese male subjects Abstract Abstract Interleukin 5 (IL‐5) and eosinophils are thought to play an important role in the pathology of asthma. This study evaluated the pharmacokinetics, pharmacodynamics, safety,... |
PMC11379133 | core_pubmed_pmc | Tobacco, nicotine, and cannabis use and exposure in an Australian Indigenous population during pregnancy: A protocol to measure parental and foetal exposure and outcomes | Tobacco, nicotine, and cannabis use and exposure in an Australian Indigenous population during pregnancy: A protocol to measure parental and foetal exposure and outcomes Abstract Background The Australian National Perinatal Data Collection collates all live and stillbirths from States and Territories in Australia. In t... |
PMC9143053 | core_pubmed_pmc | Swine as the Animal Model for Testing New Formulations of Anti-Inflammatory Drugs: Carprofen Pharmacokinetics and Bioavailability of the Intramuscular Route | Swine as the Animal Model for Testing New Formulations of Anti-Inflammatory Drugs: Carprofen Pharmacokinetics and Bioavailability of the Intramuscular Route Abstract Abstract Carprofen (CP) is a non-steroidal anti-inflammatory drug (NSAID) frequently used to treat respiratory diseases in numerous small animals, but als... |
PMC11897275 | core_pubmed_pmc | High-performance PBPK model for predicting CYP3A4 induction-mediated drug interactions: a refined and validated approach | High-performance PBPK model for predicting CYP3A4 induction-mediated drug interactions: a refined and validated approach Abstract Abstract Introduction The cytochrome P450 enzyme 3A4 (CYP3A4) mediates numerous drug-drug interactions (DDIs) by inducing the metabolism of co-administered drugs, which can result in reduced... |
PMC7055461 | core_pubmed_pmc | Immunogenicity of TNF-Inhibitors | Immunogenicity of TNF-Inhibitors Abstract Tumor necrosis factor inhibitors (TNFi) have significantly improved treatment outcome of rheumatic diseases since their incorporation into treatment protocols two decades ago. Nevertheless, a substantial fraction of patients experiences either primary or secondary failure to TN... |
PMC7716921 | core_pubmed_pmc | Pharmacokinetics and Glucodynamics of Ultra Rapid Lispro (URLi) versus Humalog ® (Lispro) in Younger Adults and Elderly Patients with Type 1 Diabetes Mellitus: A Randomised Controlled Trial | Pharmacokinetics and Glucodynamics of Ultra Rapid Lispro (URLi) versus Humalog ® (Lispro) in Younger Adults and Elderly Patients with Type 1 Diabetes Mellitus: A Randomised Controlled Trial Abstract Abstract Background Ultra rapid lispro (URLi) is a novel insulin lispro formulation developed to more closely match physi... |
PMC6610244 | core_pubmed_pmc | In Vivo Metabolism of Ibuprofen in Growing Conventional Pigs: A Pharmacokinetic Approach | In Vivo Metabolism of Ibuprofen in Growing Conventional Pigs: A Pharmacokinetic Approach Abstract The juvenile conventional pig has been suggested as a preclinical animal model to evaluate pharmacokinetic (PK), pharmacodynamic (PD), and safety parameters in children. However, a lot of developmental changes in pig physi... |
PMC11371656 | core_pubmed_pmc | Pharmacokinetics of olverembatinib (HQP1351) in the presence of a strong CYP3A4 inhibitor (itraconazole) or inducer (rifampin) in healthy volunteers | Pharmacokinetics of olverembatinib (HQP1351) in the presence of a strong CYP3A4 inhibitor (itraconazole) or inducer (rifampin) in healthy volunteers Abstract Abstract Olverembatinib (HQP1351) is a BCR‐ABL1 tyrosine kinase inhibitor with promising clinical activity. It is approved in China for the treatment of patients ... |
PMC3560109 | core_pubmed_pmc | Optimization of a high-throughput whole blood expression profiling methodology and its application to assess the pharmacodynamics of interferon (IFN) beta-1a or polyethylene glycol-conjugated IFN beta-1a in healthy clinical trial subjects | Optimization of a high-throughput whole blood expression profiling methodology and its application to assess the pharmacodynamics of interferon (IFN) beta-1a or polyethylene glycol-conjugated IFN beta-1a in healthy clinical trial subjects Abstract Abstract Background Clinical trials offer a unique opportunity to study ... |
PMC6208608 | core_pubmed_pmc | Application of a Novel ‘Make and Test in Parallel’ Strategy to Investigate the Effect of Formulation on the Pharmacokinetics of GDC-0810 in Healthy Subjects | Application of a Novel ‘Make and Test in Parallel’ Strategy to Investigate the Effect of Formulation on the Pharmacokinetics of GDC-0810 in Healthy Subjects Abstract Abstract Purpose GDC-0810, administered orally, was used in Phase I and II clinical studies to treat estrogen receptor positive breast cancers. It contain... |
PMC8195371 | core_pubmed_pmc | Ayurveda botanicals in COVID-19 management: An in silico multi-target approach | Ayurveda botanicals in COVID-19 management: An in silico multi-target approach Abstract The Coronavirus disease (COVID-19) caused by the virus SARS-CoV-2 has become a global pandemic in a very short time span. Currently, there is no specific treatment or vaccine to counter this highly contagious disease. There is an ur... |
PMC5591816 | core_pubmed_pmc | Effect of Short-Term Fasting on Systemic Cytochrome P450-Mediated Drug Metabolism in Healthy Subjects: A Randomized, Controlled, Crossover Study Using a Cocktail Approach | Effect of Short-Term Fasting on Systemic Cytochrome P450-Mediated Drug Metabolism in Healthy Subjects: A Randomized, Controlled, Crossover Study Using a Cocktail Approach Abstract Abstract Background and Objective Short-term fasting can alter drug exposure but it is unknown whether this is an effect of altered oral bio... |
PMC5363371 | core_pubmed_pmc | Evaluation of Evolocumab (AMG 145), a Fully Human Anti‐PCSK9 IgG2 Monoclonal Antibody, in Subjects With Hepatic Impairment | Evaluation of Evolocumab (AMG 145), a Fully Human Anti‐PCSK9 IgG2 Monoclonal Antibody, in Subjects With Hepatic Impairment Abstract Abstract Evolocumab binds PCSK9, increasing low‐density lipoprotein cholesterol (LDL‐C) receptors and lowering LDL‐C. Target‐mediated evolocumab elimination is attributable to PCSK9 bindin... |
PMC10796410 | core_pubmed_pmc | Bidirectional pharmacokinetic drug interactions between olaparib and metformin | Bidirectional pharmacokinetic drug interactions between olaparib and metformin Abstract Objective Olaparib is a PARP (poly-ADP-ribose polymerase) inhibitor used for maintenance therapy in BRCA-mutated cancers. Metformin is a first-choice drug used in the treatment of type 2 diabetes. Both drugs are commonly co-administ... |
PMC7754485 | core_pubmed_pmc | Population Pharmacokinetics and Exposure‐Response Relationship of Luspatercept, an Erythroid Maturation Agent, in Anemic Patients With β‐Thalassemia | Population Pharmacokinetics and Exposure‐Response Relationship of Luspatercept, an Erythroid Maturation Agent, in Anemic Patients With β‐Thalassemia Abstract Abstract β‐Thalassemia is an inherited blood disorder resulting from defects in hemoglobin production, leading to premature death of red blood cells (RBCs) or the... |
PMC2838227 | core_pubmed_pmc | Scorpion Venom and the Inflammatory Response | Scorpion Venom and the Inflammatory Response Abstract Abstract Scorpion venoms consist of a complex of several toxins that exhibit a wide range of biological properties and actions, as well as chemical compositions, toxicity, and pharmacokinetic and pharmacodynamic characteristics. These venoms are associated with high... |
PMC11348173 | core_pubmed_pmc | A Physiologically Based Pharmacokinetic Model Relates the Subcutaneous Bioavailability of Monoclonal Antibodies to the Saturation of FcRn-Mediated Recycling in Injection-Site-Draining Lymph Nodes | A Physiologically Based Pharmacokinetic Model Relates the Subcutaneous Bioavailability of Monoclonal Antibodies to the Saturation of FcRn-Mediated Recycling in Injection-Site-Draining Lymph Nodes Abstract The bioavailability of a monoclonal antibody (mAb) or another therapeutic protein after subcutaneous (SC) dosing is... |
PMC10791011 | core_pubmed_pmc | Subcutaneous batoclimab in generalized myasthenia gravis: Results from a Phase 2a trial with an open‐label extension | Subcutaneous batoclimab in generalized myasthenia gravis: Results from a Phase 2a trial with an open‐label extension Abstract Abstract Objectives To assess the safety, tolerability, and key pharmacodynamic effects of subcutaneous batoclimab, a fully human anti‐neonatal Fc receptor monoclonal antibody, in patients with ... |
PMC6930858 | core_pubmed_pmc | Population Pharmacokinetics of Nivolumab in Combination With Ipilimumab in Patients With Advanced Malignancies | Population Pharmacokinetics of Nivolumab in Combination With Ipilimumab in Patients With Advanced Malignancies Abstract Nivolumab is a fully human monoclonal antibody that inhibits programmed cell death‐1 activation. To assess covariate effects on nivolumab clearance (CL), a population pharmacokinetics model was develo... |
PMC4699378 | core_pubmed_pmc | Medical and pharmacological approach to adjust the salbutamol anti-doping policy in athletes | Medical and pharmacological approach to adjust the salbutamol anti-doping policy in athletes Abstract Abstract Background Salbutamol abuse detection by athletes is based on a urinary upper threshold defined by the World Anti-Doping Agency (WADA). However, this threshold was determined in healthy, untrained individuals ... |
PMC9147299 | core_pubmed_pmc | Impaired Pharmacokinetics of Amiodarone under Veno-Venous Extracorporeal Membrane Oxygenation: From Bench to Bedside | Impaired Pharmacokinetics of Amiodarone under Veno-Venous Extracorporeal Membrane Oxygenation: From Bench to Bedside Abstract Background: Adjusting drug therapy under veno-venous extracorporeal membrane oxygenation (VV ECMO) is challenging. Although impaired pharmacokinetics (PK) under VV ECMO have been reported for se... |
PMC9570057 | core_pubmed_pmc | Effects of NR1I2 and ABCB1 Genetic Polymorphisms on Everolimus Pharmacokinetics in Japanese Renal Transplant Patients | Effects of NR1I2 and ABCB1 Genetic Polymorphisms on Everolimus Pharmacokinetics in Japanese Renal Transplant Patients Abstract The purpose of this study was to evaluate the effects of NR1I2 (7635G>A and 8055C>T) and ABCB1 (1236C>T, 2677G>T/A, and 3435C>T) genetic polymorphisms on everolimus pharmacokinetics in 98 Japan... |
PMC6300878 | core_pubmed_pmc | In vitro antiplasmodial activity, pharmacokinetic profiles and interference in isoprenoid pathway of 2-aniline-3-hydroxy-1.4-naphthoquinone derivatives | In vitro antiplasmodial activity, pharmacokinetic profiles and interference in isoprenoid pathway of 2-aniline-3-hydroxy-1.4-naphthoquinone derivatives Abstract Abstract Background Plasmodium falciparum has shown multidrug resistance, leading to the necessity for the development of new drugs with novel targets, such as... |
PMC5761000 | core_pubmed_pmc | Simultaneous determination of asenapine and valproic acid in human plasma using LC–MS/MS: Application of the method to support pharmacokinetic study | Simultaneous determination of asenapine and valproic acid in human plasma using LC–MS/MS: Application of the method to support pharmacokinetic study Abstract Abstract Combination of asenapine with valproic acid received regulatory approval for acute treatment of schizophrenia and maniac episodes of bipolar disorders. A... |
PMC8596427 | core_pubmed_pmc | An Integrated Approach for Assessing the Impact of Renal Impairment on Pharmacokinetics of Drugs in Development: Pivotal Role of PBPK Modelling | An Integrated Approach for Assessing the Impact of Renal Impairment on Pharmacokinetics of Drugs in Development: Pivotal Role of PBPK Modelling Modeling QUANTITATIVE ASSESSMENT OF THE EFFECTS OF RENAL IMPAIRMENT USING PBPK MODELING Typically, PBPK model development following best practice approaches involves the use of... |
PMC8579949 | core_pubmed_pmc | REGEN-COV ® antibody cocktail bioanalytical strategy: comparison of LC-MRM-MS and immunoassay methods for drug quantification | REGEN-COV ® antibody cocktail bioanalytical strategy: comparison of LC-MRM-MS and immunoassay methods for drug quantification Abstract Aim: In response to the COVID-19 pandemic, Regeneron developed the anti-SARS-CoV-2 monoclonal antibody cocktail, REGEN-COV ® (RONAPREVE ® outside the USA). Drug concentration data was i... |
PMC9477486 | core_pubmed_pmc | Hyaluronic acid-enriched bilosomes: an approach to enhance ocular delivery of agomelatine via D-optimal design: formulation, in vitro characterization, and in vivo pharmacodynamic evaluation in rabbits | Hyaluronic acid-enriched bilosomes: an approach to enhance ocular delivery of agomelatine via D-optimal design: formulation, in vitro characterization, and in vivo pharmacodynamic evaluation in rabbits Abstract Abstract Agomelatine (AGO) is a dual-functional drug. It uses as an antidepressant when orally administrated ... |
PMC9796861 | core_pubmed_pmc | Lithium Pharmacokinetics in the Perinatal Patient With Bipolar Disorder | Lithium Pharmacokinetics in the Perinatal Patient With Bipolar Disorder Abstract Abstract The pharmacokinetics of lithium, the gold standard for the treatment of bipolar disorder, are well described in nonpregnant patients. Because lithium is commonly prescribed to women of childbearing age, more data are essential to ... |
PMC10715034 | core_pubmed_pmc | Efficacy of ceftaroline and rifampin, alone or combined, in a rat model of methicillin-resistant Staphylococcus epidermidis osteomyelitis without implant | Efficacy of ceftaroline and rifampin, alone or combined, in a rat model of methicillin-resistant Staphylococcus epidermidis osteomyelitis without implant Abstract ABSTRACT The in vivo efficacy of ceftaroline and rifampin alone or in combination was investigated in an experimental rat model of methicillin-resistant Stap... |
PMC10937388 | core_pubmed_pmc | A phase I trial of SON-1010, a tumor-targeted, interleukin-12-linked, albumin-binding cytokine, shows favorable pharmacokinetics, pharmacodynamics, and safety in healthy volunteers | A phase I trial of SON-1010, a tumor-targeted, interleukin-12-linked, albumin-binding cytokine, shows favorable pharmacokinetics, pharmacodynamics, and safety in healthy volunteers Abstract Background The benefits of recombinant interleukin-12 (rIL-12) as a multifunctional cytokine and potential immunotherapy for cance... |
PMC7356970 | core_pubmed_pmc | A Population Pharmacokinetic and Pharmacodynamic Model of CKD-519 | A Population Pharmacokinetic and Pharmacodynamic Model of CKD-519 Abstract CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor that is being developed for dyslipidemia. Even though CKD-519 has shown potent CETP inhibition, the exposure of CKD-519 was highly varied, depending on food an... |
PMC11387178 | core_pubmed_pmc | Sequential recruitment of body fluid spaces for increasing volumes of crystalloid fluid | Sequential recruitment of body fluid spaces for increasing volumes of crystalloid fluid Abstract Introduction The interstitial space harbours two fluid compartments linked serially to the plasma. This study explores conditions that lead to fluid accumulation in the most secluded compartment, termed the “third space”. M... |
PMC6612080 | core_pubmed_pmc | Phase II trial of AKT inhibitor MK-2206 in patients with advanced breast cancer who have tumors with PIK3CA or AKT mutations, and/or PTEN loss/ PTEN mutation | Phase II trial of AKT inhibitor MK-2206 in patients with advanced breast cancer who have tumors with PIK3CA or AKT mutations, and/or PTEN loss/ PTEN mutation Abstract Background The PI3K/AKT pathway is activated through PIK3CA or AKT1 mutations and PTEN loss in breast cancer. We conducted a phase II trial with an allos... |
PMC9746120 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of intra-articular isoflupredone following administration to horses with lipopolysaccharide-induced synovitis | Pharmacokinetics and pharmacodynamics of intra-articular isoflupredone following administration to horses with lipopolysaccharide-induced synovitis Abstract Background Intra-articular corticosteroids, such as isoflupredone acetate, are commonly used in the treatment of joint inflammation, especially in performance hors... |
PMC4021201 | core_pubmed_pmc | Repositioning: the fast track to new anti-malarial medicines? | Repositioning: the fast track to new anti-malarial medicines? Abstract Background Repositioning of existing drugs has been suggested as a fast track for developing new anti-malarial agents. The compound libraries of GlaxoSmithKline (GSK), Pfizer and AstraZeneca (AZ) comprising drugs that have undergone clinical studies... |
PMC6896233 | core_pubmed_pmc | Population Pharmacokinetic Modeling and Exposure–Response Assessment for the Antibody‐Drug Conjugate Brentuximab Vedotin in Hodgkin's Lymphoma in the Phase III ECHELON‐1 Study | Population Pharmacokinetic Modeling and Exposure–Response Assessment for the Antibody‐Drug Conjugate Brentuximab Vedotin in Hodgkin's Lymphoma in the Phase III ECHELON‐1 Study Abstract The efficacy of the CD 30‐directed antibody‐drug conjugate ( ADC ) brentuximab vedotin was established in combination with chemotherapy... |
PMC6645658 | core_pubmed_pmc | Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid Receptor Agonist | Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid Receptor Agonist Abstract Abstract Recently, targeting the G protein-biased signaling has emerged as an attractive therapeutic strategy for treating severe acute pain with the potential to reduce the side effect of the traditional opioid drug. Herein, we d... |
PMC9666035 | core_pubmed_pmc | Pharmacological Aspects and Biological Effects of Cannabigerol and Its Synthetic Derivatives | Pharmacological Aspects and Biological Effects of Cannabigerol and Its Synthetic Derivatives Abstract Abstract Cannabigerol (CBG) is a cannabinoid from the plant Cannabis sativa that lacks psychotomimetic effects. Its precursor is the acidic form, cannabigerolic acid (CBGA), which is, in turn, a biosynthetic precursor ... |
PMC10272306 | core_pubmed_pmc | A mechanistic modeling platform of SGLT2 inhibition: Implications for type 1 diabetes | A mechanistic modeling platform of SGLT2 inhibition: Implications for type 1 diabetes Abstract Abstract Type 1 diabetes mellitus (T1DM) is an autoimmune disease characterized by abnormally high blood glucose concentrations due to dysfunction of the insulin‐producing beta‐cells in the pancreas. Dapagliflozin, an inhibit... |
PMC5947602 | core_pubmed_pmc | Assessment of Safety, Tolerability, Pharmacokinetics, and Pharmacological Effect of Orally Administered CORT125134: An Adaptive, Double‐Blind, Randomized, Placebo‐Controlled Phase 1 Clinical Study | Assessment of Safety, Tolerability, Pharmacokinetics, and Pharmacological Effect of Orally Administered CORT125134: An Adaptive, Double‐Blind, Randomized, Placebo‐Controlled Phase 1 Clinical Study Abstract Abstract CORT125134 is an orally active, high‐affinity, selective antagonist of the glucocorticoid receptor that i... |
PMC9824472 | core_pubmed_pmc | Targeted Delivery of Sunitinib by MUC-1 Aptamer-Capped Magnetic Mesoporous Silica Nanoparticles | Targeted Delivery of Sunitinib by MUC-1 Aptamer-Capped Magnetic Mesoporous Silica Nanoparticles Abstract Abstract Magnetic mesoporous silica nanoparticles (MMSNPs) are being widely investigated as multifunctional novel drug delivery systems (DDSs) and play an important role in targeted therapy. Here, magnetic cores wer... |
PMC11489422 | core_pubmed_pmc | Prospective Trial on the Pharmacokinetics of Clopidogrel in Hemodialysis Patients | Prospective Trial on the Pharmacokinetics of Clopidogrel in Hemodialysis Patients Abstract Introduction Hemodialysis patients (HDPs) exhibit extensive cardiovascular risk. The widely prescribed anti-platelet agent clopidogrel is metabolically activated by cytochrome enzymes, which may be impaired by uremia and chronic ... |
PMC12064624 | core_pubmed_pmc | A Systematic Review of Pharmacokinetic Studies of Colistin and Polymyxin B in Adult Populations | A Systematic Review of Pharmacokinetic Studies of Colistin and Polymyxin B in Adult Populations Abstract Abstract Background and Objective The pharmacokinetics of polymyxins are highly variable and conventional dosing regimens may likely lead to sub-optimal exposures and outcomes, particularly in critically ill patient... |
PMC9781251 | core_pubmed_pmc | Assessing Clinical Potential of Old Antibiotics against Severe Infections by Multi-Drug-Resistant Gram-Negative Bacteria Using In Silico Modelling | Assessing Clinical Potential of Old Antibiotics against Severe Infections by Multi-Drug-Resistant Gram-Negative Bacteria Using In Silico Modelling Abstract Abstract In the light of increasing antimicrobial resistance among gram-negative bacteria and the lack of new more potent antimicrobial agents, new strategies have ... |
PMC9733833 | core_pubmed_pmc | Pharmacogenetics-based population pharmacokinetic analysis and dose optimization of valproic acid in Chinese southern children with epilepsy: Effect of ABCB1 gene polymorphism | Pharmacogenetics-based population pharmacokinetic analysis and dose optimization of valproic acid in Chinese southern children with epilepsy: Effect of ABCB1 gene polymorphism Abstract Abstract Objective: The aim of this study was to establish a population pharmacokinetic (PPK) model of valproic acid (VPA) in pediatric... |
PMC6125661 | core_pubmed_pmc | Comparison of twice a day and three times a day meropenem administration in elderly patients in a Japanese community hospital | Comparison of twice a day and three times a day meropenem administration in elderly patients in a Japanese community hospital Abstract ABSTRACT Meropenem (MEPM) is a broad-spectrum antibiotic prescribed to patients with moderate or severe pneumonia. It is well recognized that appropriate medicine reduces the burden on ... |
PMC3889630 | core_pubmed_pmc | Pharmacokinetics of dolutegravir in HIV-seronegative subjects with severe renal impairment | Pharmacokinetics of dolutegravir in HIV-seronegative subjects with severe renal impairment Abstract Abstract Purpose Dolutegravir (DTG), an unboosted HIV integrase inhibitor (INI), is metabolized by UGT1A1 and to a minor extent by CYP3A. Renal elimination of unchanged DTG is very low (< 1 %). As renal impairment may af... |
PMC11822991 | core_pubmed_pmc | Pharmacokinetics of SARS ‐ CoV ‐2 RNA Polymerase Inhibitor Remdesivir in Participants With Moderate and Severe Hepatic Impairment | Pharmacokinetics of SARS ‐ CoV ‐2 RNA Polymerase Inhibitor Remdesivir in Participants With Moderate and Severe Hepatic Impairment Abstract ABSTRACT Remdesivir is an RNA polymerase inhibitor of severe acute respiratory syndrome coronavirus 2 administered intravenously (IV) that is approved for the treatment of coronavir... |
PMC7689749 | core_pubmed_pmc | Characterizing Exposure–Response Relationship for Therapeutic Monoclonal Antibodies in Immuno‐Oncology and Beyond: Challenges, Perspectives, and Prospects | Characterizing Exposure–Response Relationship for Therapeutic Monoclonal Antibodies in Immuno‐Oncology and Beyond: Challenges, Perspectives, and Prospects Abstract Abstract Recent data from immuno‐oncology clinical studies have shown the exposure–response (E–R) relationship for therapeutic monoclonal antibodies (mAbs) ... |
PMC8400465 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Cholic Acid (MT921) after a Subcutaneous Injection in the Submental Area to Humans | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Cholic Acid (MT921) after a Subcutaneous Injection in the Submental Area to Humans Abstract Abstract This study aimed to explore pharmacokinetics, pharmacodynamics, and safety/tolerability of MT921, an injectable cholic acid, after a single subcutaneous ad... |
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