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PMC10002220 | core_pubmed_pmc | In Vivo Reversal of P-Glycoprotein-Mediated Drug Resistance in a Breast Cancer Xenograft and in Leukemia Models Using a Novel, Potent, and Nontoxic Epicatechin EC31 | In Vivo Reversal of P-Glycoprotein-Mediated Drug Resistance in a Breast Cancer Xenograft and in Leukemia Models Using a Novel, Potent, and Nontoxic Epicatechin EC31 Abstract Abstract The modulation of P-glycoprotein (P-gp, ABCB1) can reverse multidrug resistance (MDR) and potentiate the efficacy of anticancer drugs. Te... |
PMC11408354 | core_pubmed_pmc | A phase III study to access the safety and efficacy of prolgolimab 250 mg fixed dose administered every 3 weeks versus prolgolimab 1 mg/kg every 2 weeks in patients with metastatic melanoma (FLAT) | A phase III study to access the safety and efficacy of prolgolimab 250 mg fixed dose administered every 3 weeks versus prolgolimab 1 mg/kg every 2 weeks in patients with metastatic melanoma (FLAT) Abstract Abstract Background Prolgolimab is the first Russian PD-1 inhibitor approved for the first-line treatment of unres... |
PMC6867677 | core_pubmed_pmc | Pharmacokinetics of Enteric-Coated Mycophenolate Sodium in Lupus Nephritis (POEMSLUN) | Pharmacokinetics of Enteric-Coated Mycophenolate Sodium in Lupus Nephritis (POEMSLUN) Abstract Background: Mycophenolate mofetil or enteric-coated mycophenolate sodium (EC-MPS) and steroids are used for induction and maintenance therapy in severe lupus nephritis. Blood concentrations of mycophenolic acid (MPA), the act... |
PMC12263781 | core_pubmed_pmc | Population Pharmacokinetics and Exposure–Response Analysis of Benralizumab in Chinese Adults, Adolescents, and Pediatric Participants with Severe Eosinophilic Asthma | Population Pharmacokinetics and Exposure–Response Analysis of Benralizumab in Chinese Adults, Adolescents, and Pediatric Participants with Severe Eosinophilic Asthma Abstract Introduction Benralizumab is approved as add-on subcutaneous therapy in patients aged ≥ 12 years with severe eosinophilic asthma in > 80 countrie... |
PMC8143524 | core_pubmed_pmc | The Use of Translational Modelling and Simulation to Develop Immunomodulatory Therapy as an Adjunct to Antibiotic Treatment in the Context of Pneumonia | The Use of Translational Modelling and Simulation to Develop Immunomodulatory Therapy as an Adjunct to Antibiotic Treatment in the Context of Pneumonia Abstract Abstract The treatment of respiratory tract infections is threatened by the emergence of bacterial resistance. Immunomodulatory drugs, which enhance airway inn... |
PMC5908295 | core_pubmed_pmc | A novel, dual pan-PIM/FLT3 inhibitor SEL24 exhibits broad therapeutic potential in acute myeloid leukemia | A novel, dual pan-PIM/FLT3 inhibitor SEL24 exhibits broad therapeutic potential in acute myeloid leukemia Abstract Fms-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) is one of the most common genetic lesions in acute myeloid leukemia patients (AML). Although FLT3 tyrosine kinase inhibitors initially exhi... |
PMC12246821 | core_pubmed_pmc | De novo drug design and biological evaluation of coumarin–pyrimidine co-drug derivatives as diabetic inhibitors: expanding a multi-algorithm approach with the integration of machine learning in pharmaceutical research † | De novo drug design and biological evaluation of coumarin–pyrimidine co-drug derivatives as diabetic inhibitors: expanding a multi-algorithm approach with the integration of machine learning in pharmaceutical research † Abstract Abstract Optimization of hit compounds was carried out using the density functional theory.... |
PMC4806770 | core_pubmed_pmc | Glucagon Nasal Powder: A Promising Alternative to Intramuscular Glucagon in Youth With Type 1 Diabetes | Glucagon Nasal Powder: A Promising Alternative to Intramuscular Glucagon in Youth With Type 1 Diabetes Abstract Abstract OBJECTIVE Treatment of severe hypoglycemia outside of the hospital setting is limited to intramuscular glucagon requiring reconstitution prior to injection. The current study examined the safety and ... |
PMC7664215 | core_pubmed_pmc | Recent Advances in Synthesis, Bioactivity, and Pharmacokinetics of Pterostilbene, an Important Analog of Resveratrol | Recent Advances in Synthesis, Bioactivity, and Pharmacokinetics of Pterostilbene, an Important Analog of Resveratrol Abstract Pterostilbene is a natural 3,5-dimethoxy analog of resveratrol. This stilbene compound has a strong bioactivity and exists widely in Dalbergia and Vaccinium spp. Besides natural extraction, pter... |
PMC12352173 | core_pubmed_pmc | First-in-human phase 1 study of the ICOS agonist feladilimab on patients with advanced solid tumors | First-in-human phase 1 study of the ICOS agonist feladilimab on patients with advanced solid tumors Abstract Abstract Background Inducible costimulator (ICOS) receptor belongs to the CD28/CTLA immunoglobulin super family, whose expression is restricted to T cells and is weakly expressed on resting TH17, follicular help... |
PMC12905995 | core_pubmed_pmc | Simulating treatment effects for gonorrhoea using a within-host mathematical model | Simulating treatment effects for gonorrhoea using a within-host mathematical model Abstract Abstract Neisseria gonorrhoeae (NG) bacteria have evolved resistance to many of the antibiotics used to treat gonorrhoea infection. To explore potential treatment options for gonorrhoea, we extend a previously developed within-h... |
PMC8360206 | core_pubmed_pmc | A phase 1 study of the pan‐bromodomain and extraterminal inhibitor mivebresib (ABBV‐075) alone or in combination with venetoclax in patients with relapsed/refractory acute myeloid leukemia | A phase 1 study of the pan‐bromodomain and extraterminal inhibitor mivebresib (ABBV‐075) alone or in combination with venetoclax in patients with relapsed/refractory acute myeloid leukemia Abstract Abstract Background Acute myeloid leukemia (AML) is a heterogenous malignancy driven by genetic and epigenetic factors. In... |
PMC11964177 | core_pubmed_pmc | Intratumoral or Subcutaneous MK-2118, a Noncyclic Dinucleotide STING Agonist, with or without Pembrolizumab, for Advanced or Metastatic Solid Tumors or Lymphomas | Intratumoral or Subcutaneous MK-2118, a Noncyclic Dinucleotide STING Agonist, with or without Pembrolizumab, for Advanced or Metastatic Solid Tumors or Lymphomas Abstract Abstract Purpose: We evaluated the noncyclic dinucleotide stimulator of IFN genes agonist MK-2118 ± pembrolizumab in participants with advanced solid... |
PMC4435096 | core_pubmed_pmc | Influence of cancer cachexia on drug liver metabolism and renal elimination in rats | Influence of cancer cachexia on drug liver metabolism and renal elimination in rats Abstract Abstract Background Body wasting and cachexia change body composition and organ function, with effects on drug pharmacokinetics. The aim of this study was to investigate how cancer and cancer cachexia modify liver metabolism an... |
PMC6617838 | core_pubmed_pmc | Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate | Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate Abstract Purpose: The objective of this study was to exploit a novel methotrexate (MTX)-loaded solid self-microemulsifying drug delivery system (SMEDDS) with enhanced bioavailability and photostability. Mat... |
PMC6068695 | core_pubmed_pmc | Effect of Carbohydration on the Theranostic Tracer PSMA I&T | Effect of Carbohydration on the Theranostic Tracer PSMA I&T Abstract To investigate the effect of carbohydrate moieties on the pharmacokinetic profile of prostate-specific membrane antigen (PSMA) inhibitors, carbohydrated derivatives of the established PSMA-targeted radiopharmaceutical PSMA I&T were developed and evalu... |
PMC9939800 | core_pubmed_pmc | Development of a Fast Onset Proton Pump Inhibitor: Comparison of Fixed-Dose Combination of Rabeprazole and Sodium Bicarbonate (YPI-011) to the Conventional Enteric-Coated Rabeprazole | Development of a Fast Onset Proton Pump Inhibitor: Comparison of Fixed-Dose Combination of Rabeprazole and Sodium Bicarbonate (YPI-011) to the Conventional Enteric-Coated Rabeprazole Abstract Abstract Purpose Proton pump inhibitors (PPIs) are the first-line therapy for gastroesophageal reflux disorder (GERD). Unlike co... |
PMC10264945 | core_pubmed_pmc | Pharmacokinetics of intranasal amiloride in healthy volunteers | Pharmacokinetics of intranasal amiloride in healthy volunteers Abstract Abstract Anxiety and panic disorders are the most common mental illnesses in the United States and lack effective treatment options. Acid‐sending ion channels (ASICs) in the brain were shown to be associated with fear conditioning and anxiety respo... |
PMC9964381 | core_pubmed_pmc | Therapeutic Efficacy and Radiobiological Effects of Boric-Acid-Mediated BNCT in an Osteosarcoma-Bearing SD Rat Model | Therapeutic Efficacy and Radiobiological Effects of Boric-Acid-Mediated BNCT in an Osteosarcoma-Bearing SD Rat Model Abstract Abstract Background: Osteosarcoma (OS) is the most common primary malignancy of the bone and is notoriously resistant to radiation therapy. High-dose cytotoxic chemotherapy and surgical resectio... |
PMC7028138 | core_pubmed_pmc | Ledipasvir‐Sofosbuvir for 12 Weeks in Children 3 to <6 Years Old With Chronic Hepatitis C | Ledipasvir‐Sofosbuvir for 12 Weeks in Children 3 to <6 Years Old With Chronic Hepatitis C Abstract For children under 12 years of age who have chronic hepatitis C virus (HCV) infection, there are currently no approved treatments with direct‐acting antiviral agents. We therefore evaluated the safety and efficacy of ledi... |
PMC9360106 | core_pubmed_pmc | RELAY, ramucirumab plus erlotinib versus placebo plus erlotinib in untreated EGFR -mutated metastatic non-small cell lung cancer: exposure–response relationship | RELAY, ramucirumab plus erlotinib versus placebo plus erlotinib in untreated EGFR -mutated metastatic non-small cell lung cancer: exposure–response relationship Abstract Abstract Purpose In RELAY, ramucirumab plus erlotinib (RAM + ERL) improved progression-free survival (PFS) in patients with untreated, metastatic, EGF... |
PMC11279738 | core_pubmed_pmc | Intestinal Metabolism of Crocin and a Pharmacokinetics and Pharmacodynamics Study in the Chronic Social Defeat Stress Mouse Model | Intestinal Metabolism of Crocin and a Pharmacokinetics and Pharmacodynamics Study in the Chronic Social Defeat Stress Mouse Model Abstract Abstract Orally administered crocin rapidly and efficiently rescues depressive-like behaviors in depression models; however, crocin levels in the circulatory and central nervous sys... |
PMC8927291 | core_pubmed_pmc | Predictive Simulations in Preclinical Oncology to Guide the Translation of Biologics | Predictive Simulations in Preclinical Oncology to Guide the Translation of Biologics Abstract Abstract Preclinical in vivo studies form the cornerstone of drug development and translation, bridging in vitro experiments with first-in-human trials. However, despite the utility of animal models, translation from the bench... |
PMC6890991 | core_pubmed_pmc | Fluconazole Monotherapy Is a Suboptimal Option for Initial Treatment of Cryptococcal Meningitis Because of Emergence of Resistance | Fluconazole Monotherapy Is a Suboptimal Option for Initial Treatment of Cryptococcal Meningitis Because of Emergence of Resistance Abstract Cryptococcal meningitis is a lethal disease with few treatment options. The incidence remains high and intricately linked with the HIV/AIDS epidemic. In many parts of the world, fl... |
PMC5613127 | core_pubmed_pmc | Humans Vary, So Cardiac Models Should Account for That Too! | Humans Vary, So Cardiac Models Should Account for That Too! Abstract Abstract The utilization of mathematical modeling and simulation in drug development encompasses multiple mathematical techniques and the location of a drug candidate in the development pipeline. Historically speaking they have been used to analyze ex... |
PMC5176000 | core_pubmed_pmc | Randomized, Open-Label, Phase 1/2a Study to Determine the Maximum Tolerated Dose of Intraventricular Sustained Release Nimodipine for Subarachnoid Hemorrhage (NEWTON [Nimodipine Microparticles to Enhance Recovery While Reducing Toxicity After Subarachnoid Hemorrhage]) | Randomized, Open-Label, Phase 1/2a Study to Determine the Maximum Tolerated Dose of Intraventricular Sustained Release Nimodipine for Subarachnoid Hemorrhage (NEWTON [Nimodipine Microparticles to Enhance Recovery While Reducing Toxicity After Subarachnoid Hemorrhage]) Abstract Supplemental Digital Content is available ... |
PMC8353398 | core_pubmed_pmc | Elabela Protects Spontaneously Hypertensive Rats From Hypertension and Cardiorenal Dysfunctions Exacerbated by Dietary High-Salt Intake | Elabela Protects Spontaneously Hypertensive Rats From Hypertension and Cardiorenal Dysfunctions Exacerbated by Dietary High-Salt Intake Abstract Abstract Objectives: Arterial hypertension, when exacerbated by excessive dietary salt intake, worsens the morbidity and mortality rates associated with cardiovascular and ren... |
PMC9188947 | core_pubmed_pmc | Effect of cytochrome P450 3A5 polymorphism on the pharmacokinetics of tacrolimus in renal transplant recipients | Effect of cytochrome P450 3A5 polymorphism on the pharmacokinetics of tacrolimus in renal transplant recipients Abstract Background Renal transplant is an effective treatment option for end-stage kidney disease and tacrolimus is one of the most commonly used immunosuppressant drugs in renal transplant patients. Tacroli... |
PMC9617580 | core_pubmed_pmc | High Intrapulmonary Rifampicin and Isoniazid Concentrations Are Associated With Rapid Sputum Bacillary Clearance in Patients With Pulmonary Tuberculosis | High Intrapulmonary Rifampicin and Isoniazid Concentrations Are Associated With Rapid Sputum Bacillary Clearance in Patients With Pulmonary Tuberculosis Abstract Abstract Background Intrapulmonary pharmacokinetics may better explain response to tuberculosis (TB) treatment than plasma pharmacokinetics. We explored these... |
PMC8564421 | core_pubmed_pmc | Ultra‐Fast Insulin–Pramlintide Co‐Formulation for Improved Glucose Management in Diabetic Rats | Ultra‐Fast Insulin–Pramlintide Co‐Formulation for Improved Glucose Management in Diabetic Rats Abstract Abstract Dual‐hormone replacement therapy with insulin and amylin in patients with type 1 diabetes has the potential to improve glucose management. Unfortunately, currently available formulations require burdensome s... |
PMC5299197 | core_pubmed_pmc | Influence of IL-18 and IL-10 Polymorphisms on Tacrolimus Elimination in Chinese Lung Transplant Patients | Influence of IL-18 and IL-10 Polymorphisms on Tacrolimus Elimination in Chinese Lung Transplant Patients Abstract Abstract Aims. The influence of interleukin-10 (IL-10) and interleukin-18 (IL-18) polymorphisms on tacrolimus pharmacokinetics had been described in liver and kidney transplantation. The expression of cytok... |
PMC12457255 | core_pubmed_pmc | Proteinuria and influence on monoclonal antibody excretion: a pembrolizumab case report and literature review | Proteinuria and influence on monoclonal antibody excretion: a pembrolizumab case report and literature review Abstract Abstract Therapeutic monoclonal antibodies (mAbs) have revolutionized the treatment landscape of various diseases, offering targeted therapy options with high specificity. Under normal physiological co... |
PMC12298654 | core_pubmed_pmc | MWB_Analyzer: An Automated Embedded System for Real-Time Quantitative Analysis of Morphine Withdrawal Behaviors in Rodents | MWB_Analyzer: An Automated Embedded System for Real-Time Quantitative Analysis of Morphine Withdrawal Behaviors in Rodents Abstract Background/Objectives: Substance use disorders, particularly opioid addiction, continue to pose a major global health and toxicological challenge. Morphine dependence represents a signific... |
PMC7485346 | core_pubmed_pmc | Sorafenib for Patients with Hepatocellular Carcinoma and Child‐Pugh B Liver Cirrhosis: Lessons Learned from a Terminated Study | Sorafenib for Patients with Hepatocellular Carcinoma and Child‐Pugh B Liver Cirrhosis: Lessons Learned from a Terminated Study Abstract Abstract Lessons Learned Recruitment of patients with advanced hepatocellular carcinoma and Child‐Pugh B for sorafenib treatment and additional pharmacokinetic studies is challenging. ... |
PMC9428491 | core_pubmed_pmc | Impact of extracorporeal membrane oxygenation on voriconazole plasma concentrations: A retrospective study | Impact of extracorporeal membrane oxygenation on voriconazole plasma concentrations: A retrospective study Abstract Aims: We aimed to assess the impact of extracorporeal membrane oxygenation (ECMO) on voriconazole exposure. Methods: Adult critically ill patients with or without ECMO support receiving intravenous vorico... |
PMC6310870 | core_pubmed_pmc | A Quantitative Systems Pharmacology Kidney Model of Diabetes Associated Renal Hyperfiltration and the Effects of SGLT Inhibitors | A Quantitative Systems Pharmacology Kidney Model of Diabetes Associated Renal Hyperfiltration and the Effects of SGLT Inhibitors Abstract The early stage of diabetes mellitus is characterized by increased glomerular filtration rate ( GFR ), known as hyperfiltration, which is believed to be one of the main causes leadin... |
PMC11215664 | core_pubmed_pmc | Clinical Pharmacokinetics of Semaglutide: A Systematic Review | Clinical Pharmacokinetics of Semaglutide: A Systematic Review Abstract Purpose The aim of this review was to provide all the pharmacokinetic data for semaglutide in humans concerning its pharmacokinetics after subcutaneously and oral applications in healthy and diseased populations, to provide recommendations for clini... |
PMC9855885 | core_pubmed_pmc | Factors Influencing Pharmacokinetics of Tamoxifen in Breast Cancer Patients: A Systematic Review of Population Pharmacokinetic Models | Factors Influencing Pharmacokinetics of Tamoxifen in Breast Cancer Patients: A Systematic Review of Population Pharmacokinetic Models Abstract Simple Summary Breast cancer is the most common type of cancer in women. Tamoxifen is the most preferred drug used to treat breast cancer. It has been reported that tamoxifen an... |
PMC4856711 | core_pubmed_pmc | Recent Advances in Development and Application of Physiologically-Based Pharmacokinetic (PBPK) Models: a Transition from Academic Curiosity to Regulatory Acceptance | Recent Advances in Development and Application of Physiologically-Based Pharmacokinetic (PBPK) Models: a Transition from Academic Curiosity to Regulatory Acceptance Abstract Abstract There is a renewed surge of interest in applications of physiologically-based pharmacokinetic (PBPK) models by the pharmaceutical industr... |
PMC5238805 | core_pubmed_pmc | Effect of food on the pharmacokinetics of dronabinol oral solution versus dronabinol capsules in healthy volunteers | Effect of food on the pharmacokinetics of dronabinol oral solution versus dronabinol capsules in healthy volunteers Abstract Dronabinol is a pharmaceutical tetrahydrocannabinol originally developed as an oral capsule. A dronabinol oral solution was recently approved, and the effects of food on absorption and bioavailab... |
PMC7679074 | core_pubmed_pmc | Semimechanistic Clearance Models of Oncology Biotherapeutics and Impact of Study Design: Cetuximab as a Case Study | Semimechanistic Clearance Models of Oncology Biotherapeutics and Impact of Study Design: Cetuximab as a Case Study Abstract This study aimed to explore the currently competing and new semimechanistic clearance models for monoclonal antibodies and the impact of clearance model misspecification on exposure metrics under ... |
PMC9210856 | core_pubmed_pmc | In silico prediction of flavan-3-ol as a bioactive compound of Calophyllum macrophyllum as a potential drug against angiostrongylus eosinophilic meningitis | In silico prediction of flavan-3-ol as a bioactive compound of Calophyllum macrophyllum as a potential drug against angiostrongylus eosinophilic meningitis Abstract Abstract Background and Aim: Angiostrongylus eosinophilic meningitis is caused by larvae of the rat lungworm Angiostrongylus cantonensis . It manifests as ... |
PMC6797402 | core_pubmed_pmc | Scoping review to map evidence on mechanism of action, pharmacokinetics, effectiveness and side effects of centchroman as a contraceptive pill | Scoping review to map evidence on mechanism of action, pharmacokinetics, effectiveness and side effects of centchroman as a contraceptive pill Abstract Objective To systematically identify and map the available evidence on effectiveness, side effects, pharmacokinetics and mechanism of action of centchroman as a contrac... |
PMC6988309 | core_pubmed_pmc | Preclinical efficacy for a novel tyrosine kinase inhibitor, ArQule 531 against acute myeloid leukemia | Preclinical efficacy for a novel tyrosine kinase inhibitor, ArQule 531 against acute myeloid leukemia Abstract Background Acute myeloid leukemia (AML) is the most common type of adult leukemia. Several studies have demonstrated that oncogenesis in AML is enhanced by kinase signaling pathways such as Src family kinases ... |
PMC10010313 | core_pubmed_pmc | A Phase I Study of Pelabresib (CPI-0610), a Small-Molecule Inhibitor of BET Proteins, in Patients with Relapsed or Refractory Lymphoma | A Phase I Study of Pelabresib (CPI-0610), a Small-Molecule Inhibitor of BET Proteins, in Patients with Relapsed or Refractory Lymphoma Abstract Abstract Purpose: NF-κB, a transcription factor essential for inflammatory responses, is constitutively activated in many lymphomas. In preclinical studies, pelabresib (CPI-061... |
PMC11207217 | core_pubmed_pmc | Improving the Solubility and Bioavailability of Progesterone Cocrystals with Selected Carboxylic Acids | Improving the Solubility and Bioavailability of Progesterone Cocrystals with Selected Carboxylic Acids Abstract Abstract Progesterone (PROG) is a natural steroid hormone with low solubility and high permeability that belongs to biopharmaceutics classification system class II. In this study, novel pharmaceutical cocryst... |
PMC7485568 | core_pubmed_pmc | ARGX-117, a therapeutic complement inhibiting antibody targeting C2 | ARGX-117, a therapeutic complement inhibiting antibody targeting C2 Abstract Background Activation of the classical and lectin pathway of complement may contribute to tissue damage and organ dysfunction of antibody-mediated diseases and ischemia-reperfusion conditions. Complement factors are being considered as targets... |
PMC7928481 | core_pubmed_pmc | Pharmacokinetic profile of injectable tramadol in the koala ( Phascolarctos cinereus ) and prediction of its analgesic efficacy | Pharmacokinetic profile of injectable tramadol in the koala ( Phascolarctos cinereus ) and prediction of its analgesic efficacy Abstract Abstract Tramadol is used as an analgesic in humans and some animal species. When tramadol is administered to most species it undergoes metabolism to its main metabolites M1 or O-desm... |
PMC5971383 | core_pubmed_pmc | Antisense oligonucleotides in neurological disorders | Antisense oligonucleotides in neurological disorders Abstract Abstract The introduction of genetics revolutionized the field of neurodegenerative and neuromuscular diseases and has provided considerable insight into the underlying pathomechanisms. Nevertheless, effective treatment options have been limited. This change... |
PMC4203722 | core_pubmed_pmc | Evaluation of the Highly Variable Agomelatine Pharmacokinetics in Chinese Healthy Subjects to Support Bioequivalence Study | Evaluation of the Highly Variable Agomelatine Pharmacokinetics in Chinese Healthy Subjects to Support Bioequivalence Study Abstract Objectives We aim to obtain the intra-subject coefficient of variability of a highly variable antidepressant agomelatine in humans, and propose an adjusted bioequivalence assessment strate... |
PMC4670909 | core_pubmed_pmc | Fishing for Nature's Hits: Establishment of the Zebrafish as a Model for Screening Antidiabetic Natural Products | Fishing for Nature's Hits: Establishment of the Zebrafish as a Model for Screening Antidiabetic Natural Products Abstract Diabetes mellitus affects millions of people worldwide and significantly impacts their quality of life. Moreover, life threatening diseases, such as myocardial infarction, blindness, and renal disor... |
PMC6996546 | core_pubmed_pmc | Development of a Novel Controlled-Release Tablet of Pregabalin: Formulation Variation and Pharmacokinetics in Dogs and Humans | Development of a Novel Controlled-Release Tablet of Pregabalin: Formulation Variation and Pharmacokinetics in Dogs and Humans Abstract Abstract Background Novel three-layered (TL) tablet systems were compared with both monolithic matrix (MM) formulations and a commercial immediate-release (IR) capsule to develop once-a... |
PMC10624742 | core_pubmed_pmc | Unraveling the Effects of Acute Inflammation on Pharmacokinetics: A Model-Based Analysis Focusing on Renal Glomerular Filtration Rate and Cytochrome P450 3A4-Mediated Metabolism | Unraveling the Effects of Acute Inflammation on Pharmacokinetics: A Model-Based Analysis Focusing on Renal Glomerular Filtration Rate and Cytochrome P450 3A4-Mediated Metabolism Abstract Abstract Background and Objectives Acute inflammation caused by infections or sepsis can impact pharmacokinetics. We used a model-bas... |
PMC7928873 | core_pubmed_pmc | Human Monoclonal Antibody Cocktail for the Treatment or Prophylaxis of Middle East Respiratory Syndrome Coronavirus | Human Monoclonal Antibody Cocktail for the Treatment or Prophylaxis of Middle East Respiratory Syndrome Coronavirus Abstract Abstract Background REGN3048 and REGN3051 are human monoclonal antibodies (mAb) targeting the spike glycoprotein on the Middle East respiratory syndrome coronavirus (MERS-CoV), which binds to the... |
PMC3901214 | core_pubmed_pmc | Metabolic and Pharmacokinetic Differentiation of STX209 and Racemic Baclofen in Humans | Metabolic and Pharmacokinetic Differentiation of STX209 and Racemic Baclofen in Humans Abstract STX209 is an exploratory drug comprising the single, active R-enantiomer of baclofen which is in later stage clinical trials for the treatment of fragile x syndrome (FXS) and autism spectrum disorders (ASD). New clinical dat... |
PMC8451804 | core_pubmed_pmc | A Phase 1 Study of KHK4083: A Single‐Blind, Randomized, Placebo‐Controlled Single‐Ascending‐Dose Study in Healthy Adults and an Open‐Label Multiple‐Dose Study in Patients With Ulcerative Colitis | A Phase 1 Study of KHK4083: A Single‐Blind, Randomized, Placebo‐Controlled Single‐Ascending‐Dose Study in Healthy Adults and an Open‐Label Multiple‐Dose Study in Patients With Ulcerative Colitis Abstract Abstract OX40 plays an essential role in maintaining late T‐cell proliferation and survival by suppressing apoptosis... |
PMC7032968 | core_pubmed_pmc | Elucidation of the pathophysiology of intradialytic muscle cramps: pharmacokinetics applied to translational research | Elucidation of the pathophysiology of intradialytic muscle cramps: pharmacokinetics applied to translational research Abstract Abstract In the conventional concept of translational research, investigations flow from the laboratory bench to the bedside. However, clinical research can also serve as the starting point for... |
PMC12595923 | core_pubmed_pmc | Drug–Drug Interactions and Individualized Clozapine Therapy in Patients with Depression: Insights from Real-World Data | Drug–Drug Interactions and Individualized Clozapine Therapy in Patients with Depression: Insights from Real-World Data Abstract Abstract Objective Clozapine is widely used in patients with depression but its metabolism via multiple hepatic enzymes raises concerns about drug–drug interactions (DDIs). The extent of these... |
PMC5762609 | core_pubmed_pmc | Determination of 6258-70, a new semi-synthetic taxane, in rat plasma and tissues: Application to the pharmacokinetics and tissue distribution study ☆ | Determination of 6258-70, a new semi-synthetic taxane, in rat plasma and tissues: Application to the pharmacokinetics and tissue distribution study ☆ Abstract Cancer is the leading cause of death all over the world. Among the chemotherapy drugs, taxanes play an important role in cancer treatment. 6258-70 is a new semi-... |
PMC9737653 | core_pubmed_pmc | Traditional Knowledge, Phytochemistry, and Biological Properties of Vachellia tortilis | Traditional Knowledge, Phytochemistry, and Biological Properties of Vachellia tortilis Abstract Abstract Vachellia tortilis is a medicinal plant of the Fabaceae family, widely distributed in arid and semi-arid regions of North, East and Southern Africa, the Middle East and the Arabian Peninsula. In traditional medicine... |
PMC4771108 | core_pubmed_pmc | Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells | Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells Abstract In the present study, a new type of DSPE-PEG2000 polymeric liposome for the brain-targeted deliv... |
PMC12439288 | core_pubmed_pmc | Pharmacokinetics of Intrapartum Benzylpenicillin: Insights Into Candidate Regimens to Prevent Early Onset Neonatal Group B Streptococcus Disease | Pharmacokinetics of Intrapartum Benzylpenicillin: Insights Into Candidate Regimens to Prevent Early Onset Neonatal Group B Streptococcus Disease Abstract ABSTRACT Early onset neonatal Group B Streptococcus (GBS) infection accounts for significant global morbidity and mortality. Intrapartum prophylaxis with benzylpenici... |
PMC9305478 | core_pubmed_pmc | Understanding the Blood‐Brain Barrier and Beyond: Challenges and Opportunities for Novel CNS Therapeutics | Understanding the Blood‐Brain Barrier and Beyond: Challenges and Opportunities for Novel CNS Therapeutics Abstract This review addresses questions on how to accomplish successful central nervous system (CNS) drug delivery (i.e., having the right concentration at the right CNS site, at the right time), by understanding ... |
PMC8308912 | core_pubmed_pmc | Review of Pharmacokinetics and Pharmacogenetics in Atypical Long-Acting Injectable Antipsychotics | Review of Pharmacokinetics and Pharmacogenetics in Atypical Long-Acting Injectable Antipsychotics Abstract Abstract Over the last two decades, pharmacogenetics and pharmacokinetics have been increasingly used in clinical practice in Psychiatry due to the high variability regarding response and side effects of antipsych... |
PMC7273837 | core_pubmed_pmc | Recommendation of Antimicrobial Dosing Optimization During Continuous Renal Replacement Therapy | Recommendation of Antimicrobial Dosing Optimization During Continuous Renal Replacement Therapy Abstract Abstract Continuous Renal Replacement Therapy (CRRT) is more and more widely used in patients for various indications recent years. It is still intricate for clinicians to decide a suitable empiric antimicrobial dos... |
PMC5111841 | core_pubmed_pmc | Physiological and pharmacokinetic effects of multilevel caging on Sprague Dawley rats under ketamine-xylazine anesthesia | Physiological and pharmacokinetic effects of multilevel caging on Sprague Dawley rats under ketamine-xylazine anesthesia Abstract Abstract While the cage refinement is a necessary step towards improving the welfare of research rats, increasing the complexity and surface area of the living space of an animal may have ph... |
PMC12525942 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modelling of Serum 25-Hydroxyvitamin D Concentrations in Schoolchildren Receiving Weekly Oral Vitamin D 3 Supplementation | Physiologically Based Pharmacokinetic Modelling of Serum 25-Hydroxyvitamin D Concentrations in Schoolchildren Receiving Weekly Oral Vitamin D 3 Supplementation Abstract Abstract Background: Following vitamin D 3 oral administration, attained serum concentrations of its metabolite 25-hydroxyvitamin D 3 (25(OH)D 3 ) are ... |
PMC10044067 | core_pubmed_pmc | Predictive Factors of Piperacillin Exposure and the Impact on Target Attainment after Continuous Infusion Administration to Critically Ill Patients | Predictive Factors of Piperacillin Exposure and the Impact on Target Attainment after Continuous Infusion Administration to Critically Ill Patients Abstract Abstract Critically ill patients undergo significant pathophysiological changes that affect antibiotic pharmacokinetics. Piperacillin/tazobactam administered by co... |
PMC5760932 | core_pubmed_pmc | Determination of cefcapene acid by LC–MS and their application to a pharmacokinetic study in healthy Chinese volunteers | Determination of cefcapene acid by LC–MS and their application to a pharmacokinetic study in healthy Chinese volunteers Abstract Simple, rapid and specific liquid chromatography–mass spectrometry (LC–MS) methods have been developed and validated for the quantification of cefcapene acid in human plasma and urine. Plasma... |
PMC10094415 | core_pubmed_pmc | 131 I-Labeled Anti-HER2 Nanobody for Targeted Radionuclide Therapy of HER2-Positive Breast Cancer | 131 I-Labeled Anti-HER2 Nanobody for Targeted Radionuclide Therapy of HER2-Positive Breast Cancer Abstract Purpose The unique structure of nanobodies is advantageous for the development of radiopharmaceuticals for nuclear medicine. Nanobodies targeted to human epidermal growth factor receptor 2 (HER2) can be used as to... |
PMC11832700 | core_pubmed_pmc | Defining preclinical efficacy with the DNAPK inhibitor AZD7648 in combination with olaparib: a minimal systems pharmacokinetic–pharmacodynamic model | Defining preclinical efficacy with the DNAPK inhibitor AZD7648 in combination with olaparib: a minimal systems pharmacokinetic–pharmacodynamic model Abstract Abstract AZD7648 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK), which is part of the non-homologous end-joining DNA repair pathway. When combined... |
PMC8511316 | core_pubmed_pmc | Eicosanoid Metabolomic Profile of Remdesivir Treatment in Rat Plasma by High-Performance Liquid Chromatography Mass Spectrometry | Eicosanoid Metabolomic Profile of Remdesivir Treatment in Rat Plasma by High-Performance Liquid Chromatography Mass Spectrometry Abstract Remdesivir, a nucleotide analog prodrug, has displayed pharmacological activity against SARS-CoV-2. Recently, eicosanoids are widely involved in regulating immunity and inflammation ... |
PMC10675155 | core_pubmed_pmc | The Trends and Future Prospective of In Silico Models from the Viewpoint of ADME Evaluation in Drug Discovery | The Trends and Future Prospective of In Silico Models from the Viewpoint of ADME Evaluation in Drug Discovery Abstract Drug discovery and development are aimed at identifying new chemical molecular entities (NCEs) with desirable pharmacokinetic profiles for high therapeutic efficacy. The plasma concentrations of NCEs a... |
PMC9157771 | core_pubmed_pmc | External Evaluation of Population Pharmacokinetic Models to Inform Precision Dosing of Meropenem in Critically Ill Patients | External Evaluation of Population Pharmacokinetic Models to Inform Precision Dosing of Meropenem in Critically Ill Patients Abstract Routine clinical meropenem therapeutic drug monitoring data can be applied to model-informed precision dosing. The current study aimed to evaluate the adequacy and predictive capabilities... |
PMC10175306 | core_pubmed_pmc | Predictive Potential of BCS and Pharmacokinetic Parameters on Study Outcome: Analysis of 198 In Vivo Bioequivalence Studies | Predictive Potential of BCS and Pharmacokinetic Parameters on Study Outcome: Analysis of 198 In Vivo Bioequivalence Studies Abstract Background and Objectives Understanding predictive potential of parameters to perform early bioequivalence (BE) risk assessment is crucial for good planning and risk mitigation during pro... |
PMC9050051 | core_pubmed_pmc | LC-MS/MS determination of avanafil and its metabolites in rat plasma and brain: pharmacokinetic study after oral administration and transdermal film application | LC-MS/MS determination of avanafil and its metabolites in rat plasma and brain: pharmacokinetic study after oral administration and transdermal film application Abstract Abstract Avanafil (AVA) has been FDA approved in 2012 as a phosphodiesterase-type five inhibitor drug (PDE-5), for the treatment of erectile dysfuncti... |
PMC10209533 | core_pubmed_pmc | Fluoroquinolone-resistant latent tuberculosis infection: A literature review and case series of 5 patients treated with linezolid monotherapy | Fluoroquinolone-resistant latent tuberculosis infection: A literature review and case series of 5 patients treated with linezolid monotherapy Abstract Latent tuberculosis infection (LTBI) constitutes an important public health problem because of risk of progression to TB disease. Effective treatment of multi-drug resis... |
PMC10391911 | core_pubmed_pmc | Differential effects of two phosphodiesterase 4 inhibitors against lipopolysaccharide-induced neuroinflammation in mice | Differential effects of two phosphodiesterase 4 inhibitors against lipopolysaccharide-induced neuroinflammation in mice Abstract Background Several phosphodiesterase 4 (PDE4) inhibitors have emerged as potential therapeutics for central nervous system (CNS) diseases. This study investigated the pharmacological effects ... |
PMC7992287 | core_pubmed_pmc | Effects of dosing frequency on the clinical efficacy of ampicillin/sulbactam in Japanese elderly patients with pneumonia: A single‐center retrospective observational study | Effects of dosing frequency on the clinical efficacy of ampicillin/sulbactam in Japanese elderly patients with pneumonia: A single‐center retrospective observational study Abstract Abstract This study sought to investigate whether dosing frequency (the number of doses per day) affects the antimicrobial efficacy and saf... |
PMC12389022 | core_pubmed_pmc | Drug Metabolism and Pharmacokinetic Evaluation of a Novel RNase H2 Inhibitor for the Treatment of Triple-Negative Breast Cancer | Drug Metabolism and Pharmacokinetic Evaluation of a Novel RNase H2 Inhibitor for the Treatment of Triple-Negative Breast Cancer Abstract Abstract Objectives: A thorough understanding of pharmacokinetics and metabolism is critical during early drug development. This study investigates the absorption, distribution, metab... |
PMC10787203 | core_pubmed_pmc | Application of the model‐informed drug development paradigm to datopotamab deruxtecan dose selection for late‐stage development | Application of the model‐informed drug development paradigm to datopotamab deruxtecan dose selection for late‐stage development Abstract Abstract To replace the conventional maximum tolerated dose (MTD) approach, a paradigm for dose optimization and dose selection that relies on model‐informed drug development (MIDD) a... |
PMC11343776 | core_pubmed_pmc | Population Pharmacokinetics of Capivasertib in Patients with Advanced or Metastatic Solid Tumours | Population Pharmacokinetics of Capivasertib in Patients with Advanced or Metastatic Solid Tumours Abstract Abstract Background and Objective Overactivation of the PI3K/AKT pathway can occur in many cancers. Capivasertib is a potent, selective pan-AKT inhibitor. The objectives of this analysis were to develop a populati... |
PMC8591492 | core_pubmed_pmc | The influence of the site of drug administration on florfenicol pharmacokinetics in turkeys | The influence of the site of drug administration on florfenicol pharmacokinetics in turkeys Abstract Florfenicol is a broad-spectrum antibacterial drug used in the treatment of farm animals, including poultry. This drug is poorly soluble in water, therefore, administration in drinking water may lead to high variability... |
PMC12377956 | core_pubmed_pmc | Essential Oil From Dittrichia viscosa L.: A Potential Source of Bioactive Substances With Antioxidant, Antimicrobial, and Antidiabetic Properties: In Vitro and In Silico Studies | Essential Oil From Dittrichia viscosa L.: A Potential Source of Bioactive Substances With Antioxidant, Antimicrobial, and Antidiabetic Properties: In Vitro and In Silico Studies Abstract Abstract In Morocco, Dittrichia viscosa L. has long been used to treat a variety of illnesses. The objective of this work was to comp... |
PMC11671569 | core_pubmed_pmc | Pharmacokinetics of cisplatin in the systemic versus hyperthermic intrathoracic or intraperitoneal chemotherapy | Pharmacokinetics of cisplatin in the systemic versus hyperthermic intrathoracic or intraperitoneal chemotherapy Abstract Objective To compare the pharmacokinetics and adverse effects of cisplatin administered via intravenous infusion for systemic chemotherapy (SC) versus injection into the perfusate during hyperthermic... |
PMC9482478 | core_pubmed_pmc | Population Pharmacokinetics of Enteric-Coated Mycophenolate Sodium in Children after Renal Transplantation and Initial Dosage Recommendation Based on Body Surface Area | Population Pharmacokinetics of Enteric-Coated Mycophenolate Sodium in Children after Renal Transplantation and Initial Dosage Recommendation Based on Body Surface Area Abstract Objective Enteric-coated mycophenolate sodium (EC-MPS) is widely used in renal transplant recipients. There is a lack of study on the pharmacok... |
PMC7482398 | core_pubmed_pmc | Pharmacokinetic Modeling of [ 18 F]MC225 for Quantification of the P-Glycoprotein Function at the Blood–Brain Barrier in Non-Human Primates with PET | Pharmacokinetic Modeling of [ 18 F]MC225 for Quantification of the P-Glycoprotein Function at the Blood–Brain Barrier in Non-Human Primates with PET Abstract [ 18 F]MC225 has been developed as a weak substrate of P-glycoprotein (P-gp) aimed to measure changes in the P-gp function at the blood–brain barrier with positro... |
PMC3858196 | core_pubmed_pmc | Life-Stage-, Sex-, and Dose-Dependent Dietary Toxicokinetics and Relationship to Toxicity of 2,4-Dichlorophenoxyacetic Acid (2,4-D) in Rats: Implications for Toxicity Test Dose Selection, Design, and Interpretation | Life-Stage-, Sex-, and Dose-Dependent Dietary Toxicokinetics and Relationship to Toxicity of 2,4-Dichlorophenoxyacetic Acid (2,4-D) in Rats: Implications for Toxicity Test Dose Selection, Design, and Interpretation Abstract Abstract Life-stage-dependent toxicity and dose-dependent toxicokinetics (TK) were evaluated in ... |
PMC8066500 | core_pubmed_pmc | A Model-Informed Drug Development (MIDD) Approach for a Low Dose of Empagliflozin in Patients with Type 1 Diabetes | A Model-Informed Drug Development (MIDD) Approach for a Low Dose of Empagliflozin in Patients with Type 1 Diabetes Abstract Abstract In clinical trials, sodium-glucose co-transporter (SGLT) inhibitor use as adjunct to insulin therapy in type 1 diabetes (T1D) provides glucometabolic benefits while diabetic ketoacidosis ... |
PMC3428523 | core_pubmed_pmc | Phase I study of the Aurora B kinase inhibitor barasertib (AZD1152) to assess the pharmacokinetics, metabolism and excretion in patients with acute myeloid leukemia | Phase I study of the Aurora B kinase inhibitor barasertib (AZD1152) to assess the pharmacokinetics, metabolism and excretion in patients with acute myeloid leukemia Abstract Abstract Purpose Barasertib (AZD1152) is a pro-drug that rapidly undergoes phosphatase-mediated cleavage in serum to release barasertib-hQPA, a se... |
PMC12044090 | core_pubmed_pmc | A heterodimeric radioligand labeled with gallium-68 targeting fibroblast activation protein | A heterodimeric radioligand labeled with gallium-68 targeting fibroblast activation protein Abstract Background Fibroblast activation protein (FAP) targeting radiotracers have emerged as promising agents for cancer imaging and therapy. Recent advancements have focused on optimizing these agents for better tumor targeti... |
PMC10518482 | core_pubmed_pmc | Evaluating the bioequivalence of levetiracetam brand and generic oral tablets available in the Saudi market in vivo | Evaluating the bioequivalence of levetiracetam brand and generic oral tablets available in the Saudi market in vivo Abstract Background Epilepsy is a common global neurological disorder. About 30% of epileptic patients are managed with anti-epileptic Drugs (AEDs). Since 2000, Levetiracetam (LEV) has been marketed aroun... |
PMC6611373 | core_pubmed_pmc | Using pharmacokinetics for tailoring prophylaxis in people with hemophilia switching between clotting factor products: A scoping review | Using pharmacokinetics for tailoring prophylaxis in people with hemophilia switching between clotting factor products: A scoping review Abstract Abstract The objective of this scoping review is to summarize the current use of pharmacokinetics for tailoring prophylaxis in hemophilia patients switching between clotting f... |
PMC9174081 | core_pubmed_pmc | Repurposing of anti-lung cancer drugs as multi-target inhibitors of SARS-CoV-2 proteins: An insight from molecular docking and MD-simulation study | Repurposing of anti-lung cancer drugs as multi-target inhibitors of SARS-CoV-2 proteins: An insight from molecular docking and MD-simulation study Abstract Herein we have selected seventeen anti-lung cancer drugs to screen against Mpro, PLpro and spike glycoproteins of SARS-CoV-2to ascertain the potential therapeutic a... |
PMC12143825 | core_pubmed_pmc | Safety and pharmacokinetics of ralinepag, a novel oral prostacyclin receptor agonist | Safety and pharmacokinetics of ralinepag, a novel oral prostacyclin receptor agonist Abstract Background Ralinepag is an oral, potent, highly selective prostacyclin receptor agonist and is in development for pulmonary arterial hypertension. Ralinepag was formulated as an immediate-release (IR) capsule, later modified t... |
PMC11746908 | core_pubmed_pmc | Kinetic-pharmacodynamic model to predict post-rituximab B-cell repletion as a predictor of relapse in pediatric idiopathic nephrotic syndrome | Kinetic-pharmacodynamic model to predict post-rituximab B-cell repletion as a predictor of relapse in pediatric idiopathic nephrotic syndrome Abstract Purpose Rituximab has proven efficacy in children with idiopathic nephrotic syndrome (INS). However, vast majority of children inevitably experience relapse with B-cell ... |
PMC7044355 | core_pubmed_pmc | Clinical efficacy of osimertinib for a patient with ileus due to peritoneal carcinomatosis | Clinical efficacy of osimertinib for a patient with ileus due to peritoneal carcinomatosis Abstract Abstract We report a patient of stage IV lung adenocarcinoma who developed ileus due to peritoneal carcinomatosis. We placed an ileus tube and started an oral intake of osimertinib. Within one month, the tumor had shrunk... |
PMC2895603 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic profiling of four antimicrobials against Gram-negative bacteria collected from Shenyang, China | Pharmacokinetic-pharmacodynamic profiling of four antimicrobials against Gram-negative bacteria collected from Shenyang, China Abstract Background To examine common antimicrobial regimens used in eradicating certain nosocomial Gram-negative pathogens and determine which ones are likely to be the most suitable as empiri... |
PMC12664035 | core_pubmed_pmc | Identifying Barriers and Facilitators to Pain Management With Buprenorphine for Patients With Kidney Failure: A Thematic Analysis of Interviews With Key Partners | Identifying Barriers and Facilitators to Pain Management With Buprenorphine for Patients With Kidney Failure: A Thematic Analysis of Interviews With Key Partners Abstract Abstract Rationale & Objective Treating pain with analgesic medications in patients with kidney failure receiving dialysis is often complicated owing... |
PMC9693581 | core_pubmed_pmc | Population Pharmacokinetics of Doxycycline, Administered Alone or with N-Acetylcysteine, in Chickens with Experimental Mycoplasma gallisepticum Infection | Population Pharmacokinetics of Doxycycline, Administered Alone or with N-Acetylcysteine, in Chickens with Experimental Mycoplasma gallisepticum Infection Abstract Mycoplasmosis is a bacterial infection that significantly affects poultry production, and it is often controlled with antibiotics, including doxycycline. The... |
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