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PMC7206479 | core_pubmed_pmc | Anti-Epcam Aptamer (Syl3c)-Functionalized Liposome for Targeted Delivery Of Doxorubicin: In Vitro And In Vivo Antitumor Studies in Mice Bearing C26 Colon Carcinoma | Anti-Epcam Aptamer (Syl3c)-Functionalized Liposome for Targeted Delivery Of Doxorubicin: In Vitro And In Vivo Antitumor Studies in Mice Bearing C26 Colon Carcinoma Abstract In this study, we have surface-functionalized PEGylated-nanoliposomal doxorubicin (DOX) with anti-EpCAM (epithelial cell adhesion molecule) aptamer... |
PMC4624834 | core_pubmed_pmc | Inter occasion variability in individual optimal design | Inter occasion variability in individual optimal design Abstract Inter occasion variability (IOV) is of importance to consider in the development of a design where individual pharmacokinetic or pharmacodynamic parameters are of interest. IOV may adversely affect the precision of maximum a posteriori (MAP) estimated ind... |
PMC6202468 | core_pubmed_pmc | A Regression Approach to Visual Predictive Checks for Population Pharmacometric Models | A Regression Approach to Visual Predictive Checks for Population Pharmacometric Models Abstract A visual predictive check ( VPC ) is a common diagnostic procedure for population pharmacometric models. Typically, VPC s are generated by specifying intervals, or “bins”, of an independent variable (e.g., time). However, bi... |
PMC11879237 | core_pubmed_pmc | Short, extended and continuous infusion of β-lactams: predicted impact on target attainment and risk for toxicity in an ICU patient cohort | Short, extended and continuous infusion of β-lactams: predicted impact on target attainment and risk for toxicity in an ICU patient cohort Abstract Abstract Objectives This study aimed to predict the impact of different infusion strategies on pharmacokinetic/pharmacodynamic (PK/PD) target attainment and the potential r... |
PMC12531246 | core_pubmed_pmc | Exploring the pharmacokinetics, drug-likeness, and toxicological features of anticancer flavonoids: a Boulevard to explore their clinical translational potential | Exploring the pharmacokinetics, drug-likeness, and toxicological features of anticancer flavonoids: a Boulevard to explore their clinical translational potential Abstract Abstract Background Flavonoids that are widely distributed across various plant species exhibit significant anticancer activity in various preclinica... |
PMC8512114 | core_pubmed_pmc | Multi-Targeted Molecular Docking, Pharmacokinetics, and Drug-Likeness Evaluation of Okra-Derived Ligand Abscisic Acid Targeting Signaling Proteins Involved in the Development of Diabetes | Multi-Targeted Molecular Docking, Pharmacokinetics, and Drug-Likeness Evaluation of Okra-Derived Ligand Abscisic Acid Targeting Signaling Proteins Involved in the Development of Diabetes Abstract Abstract Diabetes mellitus is a global threat affecting millions of people of different age groups. In recent years, the dev... |
PMC8548879 | core_pubmed_pmc | Pharmacokinetics, Safety, and Efficacy of Glecaprevir/Pibrentasvir in Children With Chronic HCV: Part 2 of the DORA Study | Pharmacokinetics, Safety, and Efficacy of Glecaprevir/Pibrentasvir in Children With Chronic HCV: Part 2 of the DORA Study Abstract Background and Aims Glecaprevir/pibrentasvir (GLE/PIB) has shown high efficacy and safety in chronic HCV‐infected adults and adolescents; data in children were limited. DORA part 2 is a pha... |
PMC11567870 | core_pubmed_pmc | MEDI1814 selectively reduces free Aβ42 in cerebrospinal fluid of non‐clinical species and Alzheimer's disease patients | MEDI1814 selectively reduces free Aβ42 in cerebrospinal fluid of non‐clinical species and Alzheimer's disease patients Abstract Abstract INTRODUCTION Small molecules and antibodies are being developed to lower amyloid beta (Aβ) peptides. METHODS We describe MEDI1814, a fully human high‐affinity monoclonal antibody sele... |
PMC9240599 | core_pubmed_pmc | Influence of Gender, Body Mass Index, and Age on the Pharmacokinetics of Itraconazole in Healthy Subjects: Non-Compartmental Versus Compartmental Analysis | Influence of Gender, Body Mass Index, and Age on the Pharmacokinetics of Itraconazole in Healthy Subjects: Non-Compartmental Versus Compartmental Analysis Abstract Abstract Itraconazole is a triazole antifungal agent with highly variable pharmacokinetics, with not yet fully identified factors as the source of this vari... |
PMC10426106 | core_pubmed_pmc | Topical, contact, and oral susceptibility of adult Culicoides biting midges (Diptera: Ceratopogonidae) to fluralaner | Topical, contact, and oral susceptibility of adult Culicoides biting midges (Diptera: Ceratopogonidae) to fluralaner Abstract Abstract Background Culicoides biting midges (Diptera: Ceratopogonidae) are economically important blood-feeding pests closely associated with livestock production. They are the principal vector... |
PMC6155777 | core_pubmed_pmc | Role of UDP-Glucuronosyltransferase 1A1 in the Metabolism and Pharmacokinetics of Silymarin Flavonolignans in Patients with HCV and NAFLD | Role of UDP-Glucuronosyltransferase 1A1 in the Metabolism and Pharmacokinetics of Silymarin Flavonolignans in Patients with HCV and NAFLD Abstract Silymarin is the most commonly used herbal medicine by patients with chronic liver disease. Silymarin flavonolignans undergo rapid first-pass metabolism primarily by glucuro... |
PMC7562806 | core_pubmed_pmc | Review of Clinically Relevant Drug Interactions with Next Generation Hepatitis C Direct-acting Antiviral Agents | Review of Clinically Relevant Drug Interactions with Next Generation Hepatitis C Direct-acting Antiviral Agents Abstract Abstract In this review, we examine the pharmacokinetics and clinically relevant drug interactions of the newer generation direct-acting antivirals (DAAs) for the treatment of chronic hepatitis C, sp... |
PMC11443569 | core_pubmed_pmc | Epigallocatechin-3-gallate at the nanoscale: a new strategy for cancer treatment | Epigallocatechin-3-gallate at the nanoscale: a new strategy for cancer treatment Abstract Abstract Context Epigallocatechin-3-gallate (EGCG), the predominant catechin in green tea, has shown the potential to combat various types of cancer cells through its ability to modulate multiple signaling pathways. However, its l... |
PMC11695272 | core_pubmed_pmc | Population Pharmacokinetic–Pharmacodynamic Modeling of Granulocyte Colony‐Stimulating Factor to Optimize Dosing and Timing for CD34 + Cell Harvesting | Population Pharmacokinetic–Pharmacodynamic Modeling of Granulocyte Colony‐Stimulating Factor to Optimize Dosing and Timing for CD34 + Cell Harvesting Abstract ABSTRACT Granulocyte colony‐stimulating factor (G‐CSF) mobilizes peripheral blood (PB) progenitor cells from bone marrow (BM) into circulation for PB stem cell t... |
PMC7102409 | core_pubmed_pmc | A Comprehensive Review on Schisandrin B and Its Biological Properties | A Comprehensive Review on Schisandrin B and Its Biological Properties Abstract Abstract Nature is a vast source of bioactive molecules and has provided an active and efficient reservoir for drug discovery. Among natural compounds, one of the most promising is Schisandrin B (Sch B), isolated from Schisandra chinensis, w... |
PMC6916132 | core_pubmed_pmc | Population pharmacokinetics of piperacillin in febrile children receiving cancer chemotherapy: the impact of body weight and target on an optimal dosing regimen | Population pharmacokinetics of piperacillin in febrile children receiving cancer chemotherapy: the impact of body weight and target on an optimal dosing regimen Abstract Abstract Background The β-lactam antibiotic piperacillin (in combination with tazobactam) is commonly chosen for empirical treatment of suspected bact... |
PMC11367195 | core_pubmed_pmc | Anti-T-lymphocyte globulin exposure is associated with ac ute g ra ft- versus -host disease and relapse in pediatric acute lymphoblastic leukemia patients undergoing hematopoietic stem cell transplantation: a multinational prospective study | Anti-T-lymphocyte globulin exposure is associated with ac ute g ra ft- versus -host disease and relapse in pediatric acute lymphoblastic leukemia patients undergoing hematopoietic stem cell transplantation: a multinational prospective study Abstract Anti-T-lymphocyte globulin (ATLG) is used in hematopoietic stem cell t... |
PMC10472096 | core_pubmed_pmc | Phase I Study of Acalabrutinib Plus Danvatirsen (AZD9150) in Relapsed/Refractory Diffuse Large B-Cell Lymphoma Including Circulating Tumor DNA Biomarker Assessment | Phase I Study of Acalabrutinib Plus Danvatirsen (AZD9150) in Relapsed/Refractory Diffuse Large B-Cell Lymphoma Including Circulating Tumor DNA Biomarker Assessment Abstract Abstract Purpose: Novel targeted and immunotherapies have improved outcomes in relapsed/refractory (R/R) diffuse large B-cell lymphoma (DLBCL), but... |
PMC12415837 | core_pubmed_pmc | Is Rifampin (Rifampicin) Essential for the Treatment of Rhodococcus equi Infections in Foals? A Critical Review of the Role of Rifampin | Is Rifampin (Rifampicin) Essential for the Treatment of Rhodococcus equi Infections in Foals? A Critical Review of the Role of Rifampin Abstract ABSTRACT Rifampin is an enigma among antimicrobials. Blood and tissue compartment concentrations are a “moving target” along the treatment course due to the complex pharmacody... |
PMC10223163 | core_pubmed_pmc | Application of the Population Pharmacokinetics Model-Based Approach to the Prediction of Drug–Drug Interaction between Rivaroxaban and Carbamazepine in Humans | Application of the Population Pharmacokinetics Model-Based Approach to the Prediction of Drug–Drug Interaction between Rivaroxaban and Carbamazepine in Humans Abstract Abstract Rivaroxaban (RIV) is one of the direct oral anticoagulants used to prevent and treat venous and arterial thromboembolic events. Considering the... |
PMC8452296 | core_pubmed_pmc | V 2 ACHER: Visualization of complex trial data in pharmacometric analyses with covariates | V 2 ACHER: Visualization of complex trial data in pharmacometric analyses with covariates Abstract Abstract Pharmacometric models can enhance clinical decision making, with covariates exposing potential contributions to variability of subpopulation characteristics, for example, demographics or disease status. Intuitive... |
PMC7818062 | core_pubmed_pmc | Hydroxychloroquine and COVID-19: a Rheumatologist’s Take on the Lessons Learned | Hydroxychloroquine and COVID-19: a Rheumatologist’s Take on the Lessons Learned Abstract Abstract Purpose of Review Told from the viewpoint of rheumatologists, this review tells the story of hydroxychloroquine and its swift ascent to become a household name as a therapeutic strategy against the novel SARS-CoV-2 virus. ... |
PMC11695910 | core_pubmed_pmc | Therapeutic drug monitoring (TDM) of β-lactam/β-lactamase inhibitor (BL/BLI) drug combinations: insights from a pharmacometric simulation study | Therapeutic drug monitoring (TDM) of β-lactam/β-lactamase inhibitor (BL/BLI) drug combinations: insights from a pharmacometric simulation study Abstract Abstract Background The emergence of β-lactamase-producing bacteria has led to the use of β-lactam (BL) antibiotic and β-lactamase inhibitor (BLI) drug combinations. D... |
PMC7078102 | core_pubmed_pmc | The Reliability of Histamine Pharmacodynamic Response Phenotype Classification in Children With Allergic Disease | The Reliability of Histamine Pharmacodynamic Response Phenotype Classification in Children With Allergic Disease Abstract We have identified distinct histamine pharmacodynamic response phenotypes in children with allergic disease utilizing histamine iontophoresis with laser Doppler (HILD). These response phenotypes may... |
PMC12146577 | core_pubmed_pmc | Proton pump inhibitors reduce survival outcomes in patients treated with capecitabine: meta-analysis | Proton pump inhibitors reduce survival outcomes in patients treated with capecitabine: meta-analysis Abstract Abstract Proton pump inhibitors (PPIs) are widely used over-the-counter drugs. The interaction between capecitabine and PPIs is still ambiguous within the literature, with some discrepancies still being present... |
PMC8573339 | core_pubmed_pmc | Pharmacokinetic Engineering of OX40-Blocking Anticalin Proteins Using Monomeric Plasma Half-Life Extension Domains | Pharmacokinetic Engineering of OX40-Blocking Anticalin Proteins Using Monomeric Plasma Half-Life Extension Domains Abstract Anticalin ® proteins have been proven as versatile clinical stage biotherapeutics. Due to their small size (∼20 kDa), they harbor a short intrinsic plasma half-life which can be extended, e.g., by... |
PMC5761050 | core_pubmed_pmc | Simultaneous quantitation of atorvastatin and its two active metabolites in human plasma by liquid chromatography/(–) electrospray tandem mass spectrometry | Simultaneous quantitation of atorvastatin and its two active metabolites in human plasma by liquid chromatography/(–) electrospray tandem mass spectrometry Abstract A sensitive, accurate and selective liquid chromatography–tandem mass spectrometry method (LC–MS/MS) was developed and validated for the simultaneous quant... |
PMC5786804 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Cefiderocol, a Parenteral Siderophore Cephalosporin, in Healthy Subjects, Subjects with Various Degrees of Renal Function, and Patients with Complicated Urinary Tract Infection or Acute Uncomplicated Pyelonephritis | Population Pharmacokinetic Analysis of Cefiderocol, a Parenteral Siderophore Cephalosporin, in Healthy Subjects, Subjects with Various Degrees of Renal Function, and Patients with Complicated Urinary Tract Infection or Acute Uncomplicated Pyelonephritis Abstract ABSTRACT Cefiderocol, a novel parenteral siderophore ceph... |
PMC11235362 | core_pubmed_pmc | Tacrolimus—why pharmacokinetics matter in the clinic | Tacrolimus—why pharmacokinetics matter in the clinic Abstract The calcineurin inhibitor (CNI) Tacrolimus (Tac) is the most prescribed immunosuppressant drug after solid organ transplantation. After renal transplantation (RTx) approximately 95% of recipients are discharged with a Tac-based immunosuppressive regime. Desp... |
PMC3242598 | core_pubmed_pmc | Phase I study of BIBF 1120 with docetaxel and prednisone in metastatic chemo-naive hormone-refractory prostate cancer patients | Phase I study of BIBF 1120 with docetaxel and prednisone in metastatic chemo-naive hormone-refractory prostate cancer patients Abstract Background: BIBF 1120 is an oral, potent, tyrosine kinase inhibitor that simultaneously targets vascular endothelial growth factor receptors 1–3, platelet-derived growth factor recepto... |
PMC4773233 | core_pubmed_pmc | A Study to Investigate the Efficacy and Safety of an Anti-Interleukin-18 Monoclonal Antibody in the Treatment of Type 2 Diabetes Mellitus | A Study to Investigate the Efficacy and Safety of an Anti-Interleukin-18 Monoclonal Antibody in the Treatment of Type 2 Diabetes Mellitus Abstract Abstract Objective Evidence suggests that chronic subclinical inflammation plays an important role in the pathogenesis of type 2 diabetes (T2DM). Circulating levels of inter... |
PMC12308912 | core_pubmed_pmc | Influence of pharmacokinetics‐related gene polymorphisms on plasma levels of clozapine and its metabolites in Japanese patients with schizophrenia | Influence of pharmacokinetics‐related gene polymorphisms on plasma levels of clozapine and its metabolites in Japanese patients with schizophrenia Abstract Abstract Aim Clozapine is an atypical antipsychotic drug that is most effective against treatment‐resistant schizophrenia and causes serious adverse effects, includ... |
PMC7982429 | core_pubmed_pmc | Design, synthesis and biological evaluation of pyrazolo[3,4- d ]pyridazinone derivatives as covalent FGFR inhibitors | Design, synthesis and biological evaluation of pyrazolo[3,4- d ]pyridazinone derivatives as covalent FGFR inhibitors Abstract Abstract Fibroblast growth factor receptors (FGFRs) have emerged as promising targets for anticancer therapy. In this study, we synthesized and evaluated the biological activity of 66 pyrazolo[3... |
PMC11279853 | core_pubmed_pmc | Advancing Virtual Bioequivalence for Orally Administered Drug Products: Methodology, Real-World Applications and Future Outlook | Advancing Virtual Bioequivalence for Orally Administered Drug Products: Methodology, Real-World Applications and Future Outlook Abstract Bioequivalence studies are pivotal in generic drug development wherein therapeutic equivalence is provided with an innovator product. However, bioequivalence studies represent signifi... |
PMC7241551 | core_pubmed_pmc | Incorporation of ion exchange functionalized-montmorillonite into solid lipid nanoparticles with low irritation enhances drug bioavailability for glaucoma treatment | Incorporation of ion exchange functionalized-montmorillonite into solid lipid nanoparticles with low irritation enhances drug bioavailability for glaucoma treatment Abstract Abstract Montmorillonite-loaded solid lipid nanoparticles with good biocompatibility, using Betaxolol hydrochloride as model drug, were prepared b... |
PMC3899495 | core_pubmed_pmc | Insulin Degludec: Pharmacokinetics in Patients with Renal Impairment | Insulin Degludec: Pharmacokinetics in Patients with Renal Impairment Abstract Background Insulin degludec is a new-generation basal insulin with an ultra-long duration of action. We evaluated the pharmacokinetic properties of insulin degludec in subjects with normal renal function; mild, moderate or severe renal impair... |
PMC11662058 | core_pubmed_pmc | Translational pharmacokinetic and pharmacodynamic modelling of the anti-ADAMTS-5 NANOBODY ® (M6495) using the neo-epitope ARGS as a biomarker | Translational pharmacokinetic and pharmacodynamic modelling of the anti-ADAMTS-5 NANOBODY ® (M6495) using the neo-epitope ARGS as a biomarker Abstract Abstract M6495 is a first-in-class NANOBODY ® molecule and an inhibitor of ADAMTS-5, with the potential to be a disease modifying osteoarthritis drug. In order to invest... |
PMC11944934 | core_pubmed_pmc | The Importance of Murine Models in Determining In Vivo Pharmacokinetics, Safety, and Efficacy in Antimalarial Drug Discovery | The Importance of Murine Models in Determining In Vivo Pharmacokinetics, Safety, and Efficacy in Antimalarial Drug Discovery Abstract Abstract New chemical entities are constantly being investigated towards antimalarial drug discovery, and they require animal models for toxicity and efficacy testing. Murine models show... |
PMC11597218 | core_pubmed_pmc | A Phase 1 Study to Assess the Pharmacokinetics, Food Effect, Safety, and Tolerability of Sepiapterin in Healthy Japanese and Non-Japanese Participants | A Phase 1 Study to Assess the Pharmacokinetics, Food Effect, Safety, and Tolerability of Sepiapterin in Healthy Japanese and Non-Japanese Participants Abstract Background: Sepiapterin is a natural precursor of tetrahydrobiopterin (BH 4 ), a key cofactor for phenylalanine hydroxylase. It is being developed for the treat... |
PMC12153978 | core_pubmed_pmc | Fitness seascapes are necessary for realistic modeling of the evolutionary response to drug therapy | Fitness seascapes are necessary for realistic modeling of the evolutionary response to drug therapy Abstract Abstract Pharmacokinetic (PK) and pharmacodynamic (PD) modeling of host-pathogen interactions has enhanced our understanding of drug resistance. However, how combinations of drug resistance mutations affect dose... |
PMC12704357 | core_pubmed_pmc | Advancing Epigenetic Combination Therapy in Oncology: Multifunctional Nano-Drug Delivery Systems for Synergistic Efficacy and Precision Modulation | Advancing Epigenetic Combination Therapy in Oncology: Multifunctional Nano-Drug Delivery Systems for Synergistic Efficacy and Precision Modulation Abstract Abstract Epigenetic modifications regulate gene expression at the transcriptional level, contributing to tumorigenesis and progression. While epigenetic-targeted co... |
PMC9316000 | core_pubmed_pmc | Preclinical Drug Pharmacokinetic, Tissue Distribution and Excretion Profiles of the Novel Limonin Derivate HY-071085 as an Anti-Inflammatory and Analgesic Candidate in Rats and Beagle Dogs | Preclinical Drug Pharmacokinetic, Tissue Distribution and Excretion Profiles of the Novel Limonin Derivate HY-071085 as an Anti-Inflammatory and Analgesic Candidate in Rats and Beagle Dogs Abstract Limonin is one of the research hotspots in natural drug development. However, its low solubility in water leads to poor or... |
PMC6175146 | core_pubmed_pmc | Maintenance dose conversion between oral risperidone and paliperidone palmitate 1 month: Practical guidance based on pharmacokinetic simulations | Maintenance dose conversion between oral risperidone and paliperidone palmitate 1 month: Practical guidance based on pharmacokinetic simulations Abstract Summary Aim We assessed the dosage strengths of paliperidone palmitate 1‐month ( PP 1M) long‐acting injectable resulting in similar steady‐state ( SS ) exposures to t... |
PMC10824469 | core_pubmed_pmc | Pharmacokinetics and pharmacogenomics of clozapine in an ancestrally diverse sample: a longitudinal analysis and genome-wide association study using UK clinical monitoring data | Pharmacokinetics and pharmacogenomics of clozapine in an ancestrally diverse sample: a longitudinal analysis and genome-wide association study using UK clinical monitoring data Abstract Summary Background The antipsychotic, clozapine, is the only licensed drug against the treatment-resistant symptoms that affect 20–30%... |
PMC12305497 | core_pubmed_pmc | Discovery of AZD4144, a Selective and Potent NLRP3 Inhibitor for the Treatment of Inflammatory Diseases | Discovery of AZD4144, a Selective and Potent NLRP3 Inhibitor for the Treatment of Inflammatory Diseases Abstract Abstract Inflammatory disease is a major burden on health care, and new treatments are needed to manage exaggerated inflammatory responses. The NLRP3 inflammasome is a key player in inflammation, the activat... |
PMC11739744 | core_pubmed_pmc | Exposure–Response Analyses of Sacituzumab Govitecan Efficacy and Safety in Patients With Metastatic Triple‐Negative Breast Cancer | Exposure–Response Analyses of Sacituzumab Govitecan Efficacy and Safety in Patients With Metastatic Triple‐Negative Breast Cancer Abstract Abstract Sacituzumab govitecan (SG), a Trop‐2‐directed antibody‐drug conjugate, is approved for patients with metastatic triple‐negative breast cancer (mTNBC) who received ≥2 prior ... |
PMC5145146 | core_pubmed_pmc | Maternal and Fetal Pharmacokinetics of Oral Radiolabeled and Authentic Bisphenol A in the Rhesus Monkey | Maternal and Fetal Pharmacokinetics of Oral Radiolabeled and Authentic Bisphenol A in the Rhesus Monkey Abstract The present study was conducted in pregnant rhesus monkeys to determine the rapidity and extent to which BPA reaches the fetal compartment following oral ingestion, and the 24-hr fate of BPA. To assess metab... |
PMC11489601 | core_pubmed_pmc | Continuous Subcutaneous Foslevodopa‐Foscarbidopa in Parkinson's Disease: A Mini‐Review of Current Scope and Future Outlook | Continuous Subcutaneous Foslevodopa‐Foscarbidopa in Parkinson's Disease: A Mini‐Review of Current Scope and Future Outlook Abstract Abstract Background Parkinson's disease (PD) is a progressive neurodegenerative disorder characterized by motor and non‐motor symptoms, primarily because of the impairment of dopaminergic ... |
PMC6044685 | core_pubmed_pmc | Cryptotanshinone-Loaded Cerasomes Formulation: In Vitro Drug Release, in Vivo Pharmacokinetics, and in Vivo Efficacy for Topical Therapy of Acne | Cryptotanshinone-Loaded Cerasomes Formulation: In Vitro Drug Release, in Vivo Pharmacokinetics, and in Vivo Efficacy for Topical Therapy of Acne Abstract Abstract Cerasomes (CS), evolved from liposomes, are novel drug-delivery systems that have potential medical application as carriers for drugs or active ingredients. ... |
PMC8950491 | core_pubmed_pmc | Pharmacokinetics of Haloperidol in Critically Ill Patients: Is There an Association with Inflammation? | Pharmacokinetics of Haloperidol in Critically Ill Patients: Is There an Association with Inflammation? Abstract Abstract Haloperidol is considered the first-line treatment for delirium in critically ill patients. However, clinical evidence of efficacy is lacking and no pharmacokinetic studies have been performed in int... |
PMC8724687 | core_pubmed_pmc | Recent Advances in the Clinical Value and Potential of Dexmedetomidine | Recent Advances in the Clinical Value and Potential of Dexmedetomidine Abstract Abstract Dexmedetomidine, a highly selective α2-adrenoceptor agonist, has sedative, anxiolytic, analgesic, sympatholytic, and opioid-sparing properties and induces a unique sedative response which shows an easy transition from sleep to wake... |
PMC5793121 | core_pubmed_pmc | Azemiopsin, a Selective Peptide Antagonist of Muscle Nicotinic Acetylcholine Receptor: Preclinical Evaluation as a Local Muscle Relaxant | Azemiopsin, a Selective Peptide Antagonist of Muscle Nicotinic Acetylcholine Receptor: Preclinical Evaluation as a Local Muscle Relaxant Abstract Azemiopsin (Az), a linear peptide from the Azemiops feae viper venom, contains no disulfide bonds, is a high-affinity and selective inhibitor of nicotinic acetylcholine recep... |
PMC5854750 | core_pubmed_pmc | Safety, Tolerability and Pharmacokinetics of Oral BI 425809, a Glycine Transporter 1 Inhibitor, in Healthy Male Volunteers: A Partially Randomised, Single-Blind, Placebo-Controlled, First-in-Human Study | Safety, Tolerability and Pharmacokinetics of Oral BI 425809, a Glycine Transporter 1 Inhibitor, in Healthy Male Volunteers: A Partially Randomised, Single-Blind, Placebo-Controlled, First-in-Human Study Abstract Abstract Background and objectives Schizophrenia and Alzheimer’s disease are characterised by glutamatergic ... |
PMC3573372 | core_pubmed_pmc | Flurbiprofen-Loaded Stealth Liposomes: Studies on the Development, Characterization, Pharmacokinetics, and Biodistribution | Flurbiprofen-Loaded Stealth Liposomes: Studies on the Development, Characterization, Pharmacokinetics, and Biodistribution Abstract Abstract Flurbiprofen (FP) is a phenyl alkanoic acid derivative and a family of non–steroidal anti-inflammatory drug used in the treatment of arthritis. The aim of this study was to prepar... |
PMC9292001 | core_pubmed_pmc | Bayesian dose regimen assessment in early phase oncology incorporating pharmacokinetics and pharmacodynamics | Bayesian dose regimen assessment in early phase oncology incorporating pharmacokinetics and pharmacodynamics Abstract Abstract Phase I dose‐finding trials in oncology seek to find the maximum tolerated dose of a drug under a specific schedule. Evaluating drug schedules aims at improving treatment safety while maintaini... |
PMC4629263 | core_pubmed_pmc | Study on pharmacokinetics and tissue distribution of the isocorydine derivative (AICD) in rats by HPLC-DAD method | Study on pharmacokinetics and tissue distribution of the isocorydine derivative (AICD) in rats by HPLC-DAD method Abstract A simple and effective high-performance liquid chromatography with diode-array detection method coupled with a liquid-liquid extraction pretreatment has been developed for determining the pharmacok... |
PMC6201559 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic modeling of tylosin against Streptococcus suis in pigs | Pharmacokinetic-pharmacodynamic modeling of tylosin against Streptococcus suis in pigs Abstract Abstract Background The aim of this study was to optimize the dosage regimen of tylosin against S.suis in Pigs using pharmacokinetic-pharmacodynamic (PK-PD) modeling. The antibacterial activity of tylosin against S.suis CVCC... |
PMC12255549 | core_pubmed_pmc | Same-Day Sedative and Night-Time Sleep Effects Following Combined Cannabinoid Formulations: A Randomised-Controlled Trial | Same-Day Sedative and Night-Time Sleep Effects Following Combined Cannabinoid Formulations: A Randomised-Controlled Trial Abstract Background and objectives Cannabinoid treatments are commonly used for sleep conditions, but the direct sedating effects of daytime treatment consumption and indirect effects on night-time ... |
PMC4159922 | core_pubmed_pmc | Pharmacokinetics and tissue distribution study of tanshinone IIA after oral administration of Bushen Huoxue Qubi granules to rats with blood stasis syndrome | Pharmacokinetics and tissue distribution study of tanshinone IIA after oral administration of Bushen Huoxue Qubi granules to rats with blood stasis syndrome Abstract Background: Bushen Huoxue Qubi (BHQ) granules, a traditional Chinese medicine preparation, has been clinically used for the treatment of the blood stasis ... |
PMC12480940 | core_pubmed_pmc | Tailored collagen binding of albumin-fused hyperactive coagulation factor IX dictates in vivo distribution and functional properties | Tailored collagen binding of albumin-fused hyperactive coagulation factor IX dictates in vivo distribution and functional properties Abstract The efficacy of hemophilia B (HB) replacement therapy is evaluated by coagulation factor IX (FIX) activity in plasma, although FIX bound to extravascular type IV collagen (Col4) ... |
PMC6202470 | core_pubmed_pmc | A Partial Differential Equation Approach to Inhalation Physiologically Based Pharmacokinetic Modeling | A Partial Differential Equation Approach to Inhalation Physiologically Based Pharmacokinetic Modeling Abstract Abstract The heterogeneous nature of the lungs and the range of processes affecting pulmonary drug disposition make prediction of inhaled drugs challenging. These predictions are critical, as the local exposur... |
PMC10831447 | core_pubmed_pmc | Novel Methionine Aminopeptidase 2 Inhibitor M8891 Synergizes with VEGF Receptor Inhibitors to Inhibit Tumor Growth of Renal Cell Carcinoma Models | Novel Methionine Aminopeptidase 2 Inhibitor M8891 Synergizes with VEGF Receptor Inhibitors to Inhibit Tumor Growth of Renal Cell Carcinoma Models Abstract Abstract N-terminal processing by methionine aminopeptidases (MetAP) is a crucial step in the maturation of proteins during protein biosynthesis. Small-molecule inhi... |
PMC7889563 | core_pubmed_pmc | Evaluation of Cardiac Repolarization in the Randomized Phase 2 Study of Intermediate- or High-Risk Smoldering Multiple Myeloma Patients Treated with Daratumumab Monotherapy | Evaluation of Cardiac Repolarization in the Randomized Phase 2 Study of Intermediate- or High-Risk Smoldering Multiple Myeloma Patients Treated with Daratumumab Monotherapy Abstract Introduction Daratumumab is a CD38-targeting monoclonal antibody that has demonstrated clinical benefit for multiple myeloma. Daratumumab ... |
PMC7054475 | core_pubmed_pmc | Cefiderocol: A Novel Agent for the Management of Multidrug-Resistant Gram-Negative Organisms | Cefiderocol: A Novel Agent for the Management of Multidrug-Resistant Gram-Negative Organisms Abstract Abstract Cefiderocol, formerly S-649266, is a first in its class, an injectable siderophore cephalosporin that combines a catechol-type siderophore and cephalosporin core with side chains similar to cefepime and ceftaz... |
PMC3953667 | core_pubmed_pmc | Determination of (4 E ,6 E ,12 E )-Tetradecatriene-8,10-diyne-1,3-diyl Diacetate in Rat Plasma and Tissues by HPLC-UV Method and Their Application to a Pharmacokinetic and Tissue Distribution Study | Determination of (4 E ,6 E ,12 E )-Tetradecatriene-8,10-diyne-1,3-diyl Diacetate in Rat Plasma and Tissues by HPLC-UV Method and Their Application to a Pharmacokinetic and Tissue Distribution Study Abstract Abstract In China Atractylodis Rhizoma is widely used for the treatment of rheumatic diseases and digestive disor... |
PMC9975698 | core_pubmed_pmc | Hyperoside alleviates toxicity of β-amyloid via endoplasmic reticulum-mitochondrial calcium signal transduction cascade in APP/PS1 double transgenic Alzheimer's disease mice | Hyperoside alleviates toxicity of β-amyloid via endoplasmic reticulum-mitochondrial calcium signal transduction cascade in APP/PS1 double transgenic Alzheimer's disease mice Abstract Alzheimer's disease is a neurodegenerative disorder characterized by a decline in cognitive function. The β-amyloid (Aβ) hypothesis sugge... |
PMC8771860 | core_pubmed_pmc | Serotherapy as Graft-Versus-Host Disease Prophylaxis in Haematopoietic Stem Cell Transplantation for Acute Lymphoblastic Leukaemia | Serotherapy as Graft-Versus-Host Disease Prophylaxis in Haematopoietic Stem Cell Transplantation for Acute Lymphoblastic Leukaemia Abstract Abstract Serotherapy comprising agents such as anti-thymocyte globulin, anti-T-lymphocyte globulin, and the anti-CD52 monoclonal antibody alemtuzumab is used widely to reduce the i... |
PMC4166983 | core_pubmed_pmc | ING116070: A Study of the Pharmacokinetics and Antiviral Activity of Dolutegravir in Cerebrospinal Fluid in HIV-1–Infected, Antiretroviral Therapy–Naive Subjects | ING116070: A Study of the Pharmacokinetics and Antiviral Activity of Dolutegravir in Cerebrospinal Fluid in HIV-1–Infected, Antiretroviral Therapy–Naive Subjects Abstract Median dolutegravir concentrations in cerebrospinal fluid were similar to unbound concentrations in plasma and all subjects exceeded the in vitro 50%... |
PMC11818621 | core_pubmed_pmc | Network Pharmacology Analysis and Biological Validation Systemically Identified the Active Ingredients and Molecular Targets of Kudzu Root on Osteoporosis | Network Pharmacology Analysis and Biological Validation Systemically Identified the Active Ingredients and Molecular Targets of Kudzu Root on Osteoporosis Abstract Abstract As a traditional medicinal food, Kudzu root (KR) has been proven to be an effective medicine for treating osteoporosis (OP). However, its precise t... |
PMC6862831 | core_pubmed_pmc | A case of dyskinesia after levetiracetam administration | A case of dyskinesia after levetiracetam administration Abstract Abstract Background Antiepileptic drug (AED) induced dyskinesia is an unusual manifestation in the medical field. In the previous case reports describing first generation-AED related involuntary movements, the authors suggested that a plausible cause is p... |
PMC6531516 | core_pubmed_pmc | A phase 0 study of the pharmacokinetics, biodistribution, and dosimetry of 188 Re-liposome in patients with metastatic tumors | A phase 0 study of the pharmacokinetics, biodistribution, and dosimetry of 188 Re-liposome in patients with metastatic tumors Abstract Background Liposomes are drug nano-carriers that are capable of targeting therapeutics to tumor sites because of enhanced permeability retention (EPR). In several preclinical studies wi... |
PMC6974496 | core_pubmed_pmc | Advances in CNS PET: the state-of-the-art for new imaging targets for pathophysiology and drug development | Advances in CNS PET: the state-of-the-art for new imaging targets for pathophysiology and drug development Abstract Abstract Purpose A limit on developing new treatments for a number of central nervous system (CNS) disorders has been the inadequate understanding of the in vivo pathophysiology underlying neurological an... |
PMC12577147 | core_pubmed_pmc | Switching From Aflibercept 2 mg to 8 mg in Vitrectomized Eyes With Neovascular Age-Related Macular Degeneration | Switching From Aflibercept 2 mg to 8 mg in Vitrectomized Eyes With Neovascular Age-Related Macular Degeneration Abstract Vitrectomy may alter intravitreal pharmacokinetics through the removal of the vitreous gel, potentially accelerating the clearance of anti-vascular endothelial growth factor (VEGF) agents. Clinical t... |
PMC12649507 | core_pubmed_pmc | From Tears to Toxins: Mapping Antibiotic Passage Through the Eye–Liver Axis | From Tears to Toxins: Mapping Antibiotic Passage Through the Eye–Liver Axis Abstract Abstract Traditionally used to combat infections, systemic effects of antibiotics are increasingly recognized in the context of absorption through unconventional routes. One such as the ocular surface. This review tackles the bidirecti... |
PMC7610229 | core_pubmed_pmc | Perspectives on Nanodelivery to the Brain: Prerequisites for Successful Brain Treatment | Perspectives on Nanodelivery to the Brain: Prerequisites for Successful Brain Treatment Abstract Abstract Nanocarriers (NCs) are promising tools to improve drug delivery across the blood–brain barrier (BBB) for more effective treatment of brain disorders, although there is a scarcity of clinical translation of brain-di... |
PMC6263664 | core_pubmed_pmc | Population Pharmacokinetics of Apixaban in Subjects With Nonvalvular Atrial Fibrillation | Population Pharmacokinetics of Apixaban in Subjects With Nonvalvular Atrial Fibrillation Abstract Abstract This analysis describes the population pharmacokinetics (PPK) of apixaban in nonvalvular atrial fibrillation (NVAF) subjects, and quantifies the impact of intrinsic and extrinsic factors on exposure. The PPK model... |
PMC11121921 | core_pubmed_pmc | The Role of Olorofim in the Treatment of Filamentous Fungal Infections: A Review of In Vitro and In Vivo Studies | The Role of Olorofim in the Treatment of Filamentous Fungal Infections: A Review of In Vitro and In Vivo Studies Abstract Invasive fungal infections have recently been recognized by the WHO as a major health, epidemiological, and economic issue. Their high mortality rates and the emergence of drug resistance have drive... |
PMC3093392 | core_pubmed_pmc | Contribution of Cytochrome P450 and ABCB1 Genetic Variability on Methadone Pharmacokinetics, Dose Requirements, and Response | Contribution of Cytochrome P450 and ABCB1 Genetic Variability on Methadone Pharmacokinetics, Dose Requirements, and Response Abstract Abstract Although the efficacy of methadone maintenance treatment (MMT) in opioid dependence disorder has been well established, the influence of methadone pharmacokinetics in dose requi... |
PMC7827928 | core_pubmed_pmc | Validation of an HPLC–MS/MS Method for the Determination of Plasma Ticagrelor and Its Active Metabolite Useful for Research and Clinical Practice | Validation of an HPLC–MS/MS Method for the Determination of Plasma Ticagrelor and Its Active Metabolite Useful for Research and Clinical Practice Abstract Abstract Ticagrelor is an antiplatelet agent which is extensively metabolized in an active metabolite: AR-C124910XX. Ticagrelor antagonizes P2Y12 receptors, but rece... |
PMC9833411 | core_pubmed_pmc | Advances for pharmacological activities of Polygonum cuspidatum - A review | Advances for pharmacological activities of Polygonum cuspidatum - A review Abstract Abstract Context Polygonum cuspidatum Sieb. et Zucc (Polygonaceae), the root of which is included in the Chinese Pharmcopoeia under the name ‘Huzhang', has a long history as a medicinal plant and vegetable. Polygonum cuspidatum has been... |
PMC10510183 | core_pubmed_pmc | Perampanel’s forgiveness factor in a variable medication adherence paradigm in a rat model of chronic epilepsy | Perampanel’s forgiveness factor in a variable medication adherence paradigm in a rat model of chronic epilepsy Abstract Abstract Background Poor medication adherence contributes to increased morbidity and mortality in patients with epilepsy and may be under-addressed in clinical practice. Ethical concerns make it impos... |
PMC5425494 | core_pubmed_pmc | Lack of Clinical Pharmacokinetic Studies to Optimize the Treatment of Neglected Tropical Diseases: A Systematic Review | Lack of Clinical Pharmacokinetic Studies to Optimize the Treatment of Neglected Tropical Diseases: A Systematic Review Abstract Abstract Introduction Neglected tropical diseases (NTDs) affect more than one billion people, mainly living in developing countries. For most of these NTDs, treatment is suboptimal. To optimiz... |
PMC5642506 | core_pubmed_pmc | A phase I study of foretinib plus erlotinib in patients with previously treated advanced non-small cell lung cancer: Canadian cancer trials group IND.196 | A phase I study of foretinib plus erlotinib in patients with previously treated advanced non-small cell lung cancer: Canadian cancer trials group IND.196 Abstract Purpose MET and AXL mediate resistance to EGFR TKI in NSCLC. Foretinib, a MET/RON/AXL/TIE-2/VEGFR kinase inhibitor may overcome EGFR kinase resistance. This ... |
PMC8457124 | core_pubmed_pmc | Longitudinal Impact of Acute Spinal Cord Injury on Clinical Pharmacokinetics of Riluzole, a Potential Neuroprotective Agent | Longitudinal Impact of Acute Spinal Cord Injury on Clinical Pharmacokinetics of Riluzole, a Potential Neuroprotective Agent Abstract Abstract Riluzole, a benzothiazole sodium channel blocker that received US Food and Drug Administration approval to attenuate neurodegeneration in amyotrophic lateral sclerosis in 1995, w... |
PMC3885667 | core_pubmed_pmc | Evaluation of 131 I-Anti-Angiotensin II Type 1 Receptor Monoclonal Antibody as a Reporter for Hepatocellular Carcinoma | Evaluation of 131 I-Anti-Angiotensin II Type 1 Receptor Monoclonal Antibody as a Reporter for Hepatocellular Carcinoma Abstract Background Finding a specific agent is useful for early detection of tumor. Angiotensin II type 1 receptor (AT 1 R) was reported to be elevated in a variety of tumors and participate in tumor ... |
PMC6217055 | core_pubmed_pmc | Novel hybrid molecule overcomes the limited response of solid tumours to HDAC inhibitors via suppressing JAK1-STAT3-BCL2 signalling | Novel hybrid molecule overcomes the limited response of solid tumours to HDAC inhibitors via suppressing JAK1-STAT3-BCL2 signalling Abstract Despite initial progress in preclinical models, most known histone deacetylase inhibitors (HDACis) used as a single agent have failed to show clinical benefits in nearly all types... |
PMC12114846 | core_pubmed_pmc | Interleukin-15Rα-Sushi-Fc Fusion Protein Co-Hitchhikes Interleukin-15 and Pheophorbide A for Cancer Photoimmunotherapy | Interleukin-15Rα-Sushi-Fc Fusion Protein Co-Hitchhikes Interleukin-15 and Pheophorbide A for Cancer Photoimmunotherapy Abstract Abstract Background : Interleukin-15 (IL-15) stimulates the proliferation of natural killer cells or T cells, which, in combination with photodynamic therapy (PDT), has emerged as an effective... |
PMC8063959 | core_pubmed_pmc | Description and Analysis of Glycosidic Residues in the Largest Open Natural Products Database | Description and Analysis of Glycosidic Residues in the Largest Open Natural Products Database Abstract Abstract Natural products (NPs), biomolecules produced by living organisms, inspire the pharmaceutical industry and research due to their structural characteristics and the substituents from which they derive their ac... |
PMC10466041 | core_pubmed_pmc | Treating depression in clinical practice: new insights on the multidisciplinary use of trazodone | Treating depression in clinical practice: new insights on the multidisciplinary use of trazodone Abstract Depression is estimated to be a leading contributor to the global mental health-related burden. The determinants of this huge prevalence lie in the fact that depressive symptoms may be comorbid in a wide variety of... |
PMC12339864 | core_pubmed_pmc | The 96-week outcomes and pharmacokinetics of long-acting cabotegravir plus rilpivirine in South Africans | The 96-week outcomes and pharmacokinetics of long-acting cabotegravir plus rilpivirine in South Africans Abstract Abstract Background Evaluating long-term efficacy, safety and pharmacokinetics of long-acting cabotegravir + rilpivirine (CAB+RPV LA) in sub-Saharan African populations is important because of the region’s ... |
PMC4029757 | core_pubmed_pmc | Effect of MMX ® mesalamine coadministration on the pharmacokinetics of amoxicillin, ciprofloxacin XR, metronidazole, and sulfamethoxazole: results from four randomized clinical trials | Effect of MMX ® mesalamine coadministration on the pharmacokinetics of amoxicillin, ciprofloxacin XR, metronidazole, and sulfamethoxazole: results from four randomized clinical trials Abstract Abstract Background MMX ® mesalamine is a once daily oral 5-aminosalicylic acid formulation, effective in induction and mainten... |
PMC9128166 | core_pubmed_pmc | Parsaclisib in Japanese patients with relapsed or refractory B‐cell lymphoma (CITADEL‐111): A phase Ib study | Parsaclisib in Japanese patients with relapsed or refractory B‐cell lymphoma (CITADEL‐111): A phase Ib study Abstract Abstract Parsaclisib, a potent, selective, next‐generation PI3Kδ inhibitor, has shown clinical benefit in patients with relapsed or refractory B‐cell lymphoma. We undertook a phase Ib study (CITADEL‐111... |
PMC10681425 | core_pubmed_pmc | A model‐based approach leveraging in vitro data to support dose selection from the outset: A framework for bispecific antibodies in immuno‐oncology | A model‐based approach leveraging in vitro data to support dose selection from the outset: A framework for bispecific antibodies in immuno‐oncology Abstract Abstract FAP‐4‐1BBL is a bispecific antibody exerting 4‐1BB‐associated T‐cell activation only while simultaneously bound to the fibroblast activation protein (FAP)... |
PMC12316140 | core_pubmed_pmc | First-in-Human Safety, Tolerability, Efficacy, and Pharmacokinetics of Pegfosimer Manganese (SN132D) for Contrast-Enhanced MRI of Breast Cancer | First-in-Human Safety, Tolerability, Efficacy, and Pharmacokinetics of Pegfosimer Manganese (SN132D) for Contrast-Enhanced MRI of Breast Cancer Abstract Objectives: The primary objective of the first-in-human (FIH) study was to evaluate the safety and tolerability of the manganese (Mn)-based contrast agent pegfosimer m... |
PMC5863859 | core_pubmed_pmc | Hypoglycemic Coma in a Hemodialysis Patient Receiving Blood Glucose-Lowering Therapy With the Single Agent Teneligliptin | Hypoglycemic Coma in a Hemodialysis Patient Receiving Blood Glucose-Lowering Therapy With the Single Agent Teneligliptin Abstract Abstract Blood glucose management in patients undergoing dialysis is clinically challenging. In this population, most conventional oral hypoglycemic agents are contraindicated, especially fr... |
PMC9782816 | core_pubmed_pmc | Ingestible sensor system for measuring, monitoring and enhancing adherence to antiretroviral therapy: An open-label, usual care-controlled, randomised trial | Ingestible sensor system for measuring, monitoring and enhancing adherence to antiretroviral therapy: An open-label, usual care-controlled, randomised trial Abstract Summary Background Co-encapsulated antiretrovirals (ARVs) with ingestible sensor (IS) has the capacity to monitor adherence in real-time using a sensor pa... |
PMC10440472 | core_pubmed_pmc | Exposure-response analysis of alemtuzumab in pediatric allogeneic HSCT for nonmalignant diseases: the ARTIC study | Exposure-response analysis of alemtuzumab in pediatric allogeneic HSCT for nonmalignant diseases: the ARTIC study Abstract Key Points • An alemtuzumab population pharmacokinetic model has been developed for more accurate intravenous dosing in pediatric HSCT. • Optimal exposure is associated with early T-cell recovery a... |
PMC3838992 | core_pubmed_pmc | The discovery of rivaroxaban: translating preclinical assessments into clinical practice | The discovery of rivaroxaban: translating preclinical assessments into clinical practice Abstract Direct oral anticoagulants that target a single coagulation factor (such as factor Xa or thrombin) have been developed in recent years in an attempt to address some of the limitations of traditional anticoagulants. Rivarox... |
PMC9697306 | core_pubmed_pmc | The C30-Modulation of Betulinic Acid Using 1,2,4-Triazole: A Promising Strategy for Increasing Its Antimelanoma Cytotoxic Potential | The C30-Modulation of Betulinic Acid Using 1,2,4-Triazole: A Promising Strategy for Increasing Its Antimelanoma Cytotoxic Potential Abstract Abstract Cancer, in all its types and manifestations, remains one of the most frequent causes of death worldwide; an important number of anticancer drugs have been developed from ... |
PMC11561498 | core_pubmed_pmc | Impact of Brief Exposure to Lysozyme and Lactoferrin on Pathogenic Attributes of Oral Candida | Impact of Brief Exposure to Lysozyme and Lactoferrin on Pathogenic Attributes of Oral Candida Abstract Abstract Introduction and aims Adhesion to buccal epithelial cells (BEC) and denture acrylic surfaces (DAS), germ tube (GT) formation, cell surface hydrophobicity (CSH), and haemolysin production are attributes associ... |
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