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PMC4744262 | core_pubmed_pmc | Pharmacokinetics, Tissue Distribution and Therapeutic Effect of Cationic Thermosensitive Liposomal Doxorubicin Upon Mild Hyperthermia | Pharmacokinetics, Tissue Distribution and Therapeutic Effect of Cationic Thermosensitive Liposomal Doxorubicin Upon Mild Hyperthermia Abstract Abstract Purpose To evaluate pharmacokinetic profile, biodistribution and therapeutic effect of cationic thermosensitive liposomes (CTSL) encapsulating doxorubicin (Dox) upon mi... |
PMC10245557 | core_pubmed_pmc | Mechanistic inhibition of Monkeypox and Marburg virus infection by O-rhamnosides and Kaempferol-o-rhamnosides derivatives: a new-fangled computational approach | Mechanistic inhibition of Monkeypox and Marburg virus infection by O-rhamnosides and Kaempferol-o-rhamnosides derivatives: a new-fangled computational approach Abstract Abstract The increasing incidence of Monkeypox virus (Mpox) and Marburg virus (MARV) infections worldwide presents a significant challenge to global he... |
PMC12228802 | core_pubmed_pmc | Using cocaine and apomorphine self-administration in rats to measure the pharmacokinetics of competitive dopamine receptor antagonists administered by different routes | Using cocaine and apomorphine self-administration in rats to measure the pharmacokinetics of competitive dopamine receptor antagonists administered by different routes Abstract Abstract Cocaine self-administration behavior in rats is explained by a pharmacokinetic/pharmacodynamic interaction model. This self-administra... |
PMC9229966 | core_pubmed_pmc | Application of a Physiologically Based Pharmacokinetic Model to Predict Cefazolin and Cefuroxime Disposition in Obese Pregnant Women Undergoing Caesarean Section | Application of a Physiologically Based Pharmacokinetic Model to Predict Cefazolin and Cefuroxime Disposition in Obese Pregnant Women Undergoing Caesarean Section Abstract Abstract Intravenous (IV) cefuroxime and cefazolin are used prophylactically in caesarean sections (CS). Currently, there are concerns regarding sub-... |
PMC11283663 | core_pubmed_pmc | Antiviral Activity, Pharmacoinformatics, Molecular Docking, and Dynamics Studies of Azadirachta indica Against Nipah Virus by Targeting Envelope Glycoprotein: Emerging Strategies for Developing Antiviral Treatment | Antiviral Activity, Pharmacoinformatics, Molecular Docking, and Dynamics Studies of Azadirachta indica Against Nipah Virus by Targeting Envelope Glycoprotein: Emerging Strategies for Developing Antiviral Treatment Abstract Abstract The Nipah virus (NiV) belongs to the Henipavirus genus is a serious public health concer... |
PMC12575351 | core_pubmed_pmc | Prevalence of on time administration of carbapenem and its impact on PK/PD target attainment in hospitalized patients: a multicenter retrospective study | Prevalence of on time administration of carbapenem and its impact on PK/PD target attainment in hospitalized patients: a multicenter retrospective study Abstract Abstract Objective On time administration of carbapenem is important, but there are few data concerning the prevalence of timeliness and its impact on pharmac... |
PMC9876374 | core_pubmed_pmc | Novel modelling approaches to predict the role of antivirals in reducing influenza transmission | Novel modelling approaches to predict the role of antivirals in reducing influenza transmission Abstract To aid understanding of the effect of antiviral treatment on population-level influenza transmission, we used a novel pharmacokinetic–viral kinetic transmission model to test the correlation between nasal viral load... |
PMC11642194 | core_pubmed_pmc | Safety, outcomes, and pharmacokinetics of isavuconazole as a treatment for invasive fungal diseases in pediatric patients: a non-comparative phase 2 trial | Safety, outcomes, and pharmacokinetics of isavuconazole as a treatment for invasive fungal diseases in pediatric patients: a non-comparative phase 2 trial Abstract ABSTRACT Invasive aspergillosis (IA) and mucormycosis (IM) cause significant morbidity and mortality in immunocompromised and/or hospitalized patients. Isav... |
PMC4015983 | core_pubmed_pmc | Generation of Anti-Idiotype scFv for Pharmacokinetic Measurement in Lymphoma Patients Treated with Chimera Anti-CD22 Antibody SM03 | Generation of Anti-Idiotype scFv for Pharmacokinetic Measurement in Lymphoma Patients Treated with Chimera Anti-CD22 Antibody SM03 Abstract Pre-clinical and clinical studies of therapeutic antibodies require highly specific reagents to examine their immune responses, bio-distributions, immunogenicity, and pharmacodynam... |
PMC10477119 | core_pubmed_pmc | Imipenem/funobactam (formerly XNW4107) in vivo pharmacodynamics against serine carbapenemase-producing Gram-negative bacteria: a novel modelling approach for time-dependent killing | Imipenem/funobactam (formerly XNW4107) in vivo pharmacodynamics against serine carbapenemase-producing Gram-negative bacteria: a novel modelling approach for time-dependent killing Abstract Abstract Background Imipenem/funobactam (formerly XNW4107) is a novel β-lactam/β-lactamase inhibitor with activity against MDR Aci... |
PMC11900062 | core_pubmed_pmc | A Real-Life Study of Prolonged Meropenem Infusion in Neonates and Children Admitted to Intensive Care Units: Are Three Hours Long Enough? | A Real-Life Study of Prolonged Meropenem Infusion in Neonates and Children Admitted to Intensive Care Units: Are Three Hours Long Enough? Abstract Background/Objectives : Meropenem is a broad-spectrum antibiotic essential for treating resistant Gram-negative infections in pediatric patients. Current dosing recommendati... |
PMC6989572 | core_pubmed_pmc | Pharmacokinetics and Safety of a Single Oral Dose of Peficitinib (ASP015K) in Japanese Subjects with Normal and Impaired Renal Function | Pharmacokinetics and Safety of a Single Oral Dose of Peficitinib (ASP015K) in Japanese Subjects with Normal and Impaired Renal Function Abstract Background and Objective This study measured and compared the exposure and safety of peficitinib (ASP015K), a novel oral Janus kinase inhibitor, in subjects with normal and im... |
PMC6783648 | core_pubmed_pmc | GSTZ1 genotypes correlate with dichloroacetate pharmacokinetics and chronic side effects in multiple myeloma patients in a pilot phase 2 clinical trial | GSTZ1 genotypes correlate with dichloroacetate pharmacokinetics and chronic side effects in multiple myeloma patients in a pilot phase 2 clinical trial Abstract Abstract Dichloroacetate (DCA) is an investigational drug targeting the glycolytic hallmark of cancer by inhibiting pyruvate dehydrogenase kinases (PDK). It is... |
PMC9474281 | core_pubmed_pmc | A Computational Study of Carbazole Alkaloids from Murraya koenigii as Potential SARS-CoV-2 Main Protease Inhibitors | A Computational Study of Carbazole Alkaloids from Murraya koenigii as Potential SARS-CoV-2 Main Protease Inhibitors Abstract Despite COVID-19 vaccination, immune escape of new SARS-CoV-2 variants has created an urgent priority to identify additional antiviral drugs. Targeting main protease (M pro ) expressed by SARS-Co... |
PMC12034072 | core_pubmed_pmc | A methodology for determining dosing recommendations for anticancer drugs in patients with reduced kidney function | A methodology for determining dosing recommendations for anticancer drugs in patients with reduced kidney function Abstract Summary Reduced kidney function (or kidney dysfunction) is commonly an exclusion criterion for randomised controlled trials (RCTs) in cancer. Consequently, high quality evidence for anticancer dru... |
PMC7069368 | core_pubmed_pmc | Methyl sulfonamide substituents improve the pharmacokinetic properties of bicyclic 2-pyridone based Chlamydia trachomatis inhibitors | Methyl sulfonamide substituents improve the pharmacokinetic properties of bicyclic 2-pyridone based Chlamydia trachomatis inhibitors Abstract Methyl sulfonamide substituents effectively improve the pharmacokinetic properties of bicyclic 2-pyridones, a new class of Chlamydia trachomatis infectivity inhibitors. Chlamydia... |
PMC5746435 | core_pubmed_pmc | Pharmacokinetics of tilmicosin in healthy pigs and in pigs experimentally infected with Haemophilus parasuis | Pharmacokinetics of tilmicosin in healthy pigs and in pigs experimentally infected with Haemophilus parasuis Abstract Abstract A comparative in vivo pharmacokinetic (PK) study of tilmicosin (TIL) was conducted in 6 crossbred healthy pigs and 6 crossbred pigs infected with Haemophilus ( H .) parasuis following oral admi... |
PMC11236470 | core_pubmed_pmc | Benzoylaconine: Potential Therapeutic Agent for Cardiovascular Diseases From Fuzi | Benzoylaconine: Potential Therapeutic Agent for Cardiovascular Diseases From Fuzi Abstract Abstract Modern pharmacological studies have elucidated the presence of aconitine (AC) alkaloids, polysaccharides, and saponins as the primary bioactive constituents of Fuzi. Among these, benzoylaconine, a pivotal active compound... |
PMC10788173 | core_pubmed_pmc | Safety and pharmacokinetics of thalidomide in tumor-bearing dogs | Safety and pharmacokinetics of thalidomide in tumor-bearing dogs Abstract Abstract Thalidomide, an angiogenesis inhibitor, has recently been used to treat malignant canine tumors. This study retrospectively investigated the adverse events (AEs) of thalidomide administered to tumor-bearing dogs. We investigated the phar... |
PMC5299597 | core_pubmed_pmc | Evaluation of the safety, pharmacokinetics, pharmacodynamics, and drug-drug interaction potential of a selective Lp-PLA2 inhibitor (GSK2647544) in healthy volunteers | Evaluation of the safety, pharmacokinetics, pharmacodynamics, and drug-drug interaction potential of a selective Lp-PLA2 inhibitor (GSK2647544) in healthy volunteers Abstract Abstract. Objective: To evaluate in healthy volunteers the safety, pharmacokinetics (PK), pharmacodynamics (PD), and drug-drug interaction (DDI) ... |
PMC12802961 | core_pubmed_pmc | Pharmacodynamic studies of taniborbactam (VNRX-5133) combined with cefepime against β-lactamase–producing Gram-negative bacteria in a neutropenic murine thigh infection model | Pharmacodynamic studies of taniborbactam (VNRX-5133) combined with cefepime against β-lactamase–producing Gram-negative bacteria in a neutropenic murine thigh infection model Abstract Abstract Background Taniborbactam (VNRX-5133) is a novel boronate-based β-lactamase inhibitor that directly inhibits all four classes of... |
PMC9099127 | core_pubmed_pmc | Utility of the 13 C‐pantoprazole breath test as a CYP2C19 phenotyping probe for children | Utility of the 13 C‐pantoprazole breath test as a CYP2C19 phenotyping probe for children Abstract Abstract The 13 C‐pantoprazole breath test (PAN‐BT) is a safe, noninvasive, in vivo CYP2C19 phenotyping probe for adults. Our objective was to evaluate PAN‐BT performance in children, with a focus on discriminating individ... |
PMC8851058 | core_pubmed_pmc | Pharmacodynamics and Pharmacokinetics of HSK3486, a Novel 2,6-Disubstituted Phenol Derivative as a General Anesthetic | Pharmacodynamics and Pharmacokinetics of HSK3486, a Novel 2,6-Disubstituted Phenol Derivative as a General Anesthetic Abstract Abstract Background: The purpose of this study was to characterize the novel sedative/hypnotic agent HSK3486, a 2,6-disubstituted alkylphenol analogue. Methods: The mechanism of action of HSK34... |
PMC4480577 | core_pubmed_pmc | Pharmacokinetic analysis of the chronic administration of the inert gases Xe and Ar using a physiological based model | Pharmacokinetic analysis of the chronic administration of the inert gases Xe and Ar using a physiological based model Abstract Abstract Background New gas therapies using inert gases such as xenon and argon are being studied, which would require chronically administered repeating doses. The pharmacokinetics of this typ... |
PMC10980152 | core_pubmed_pmc | Extreme Phenotype Sampling and Next Generation Sequencing to Identify Genetic Variants Associated with Tacrolimus in African American Kidney Transplant Recipients | Extreme Phenotype Sampling and Next Generation Sequencing to Identify Genetic Variants Associated with Tacrolimus in African American Kidney Transplant Recipients Abstract African American (AA) kidney transplant recipients (KTRs) have poor outcomes, which may in-part be due to tacrolimus (TAC) sub-optimal immunosuppres... |
PMC6490236 | core_pubmed_pmc | Evaluation of treatment options for methicillin-resistant Staphylococcus aureus infections in the obese patient | Evaluation of treatment options for methicillin-resistant Staphylococcus aureus infections in the obese patient Abstract Abstract Methicillin-resistant Staphylococcus aureus (MRSA) has emerged as a major cause of infection in both the hospital and community setting. Obesity is a risk factor for infection, and the preva... |
PMC8865634 | core_pubmed_pmc | Polypharmacy occurrence and the related risk of premature death among older adults in Denmark: A nationwide register-based cohort study | Polypharmacy occurrence and the related risk of premature death among older adults in Denmark: A nationwide register-based cohort study Abstract Abstract Background Polypharmacy, defined as the concurrent use of ≥5 medications, increases the risk of drug-drug and drug-disease interactions as well as non-adherence to dr... |
PMC9967085 | core_pubmed_pmc | Properly Substituted Benzimidazoles as a New Promising Class of Nicotinate Phosphoribosyltransferase (NAPRT) Modulators | Properly Substituted Benzimidazoles as a New Promising Class of Nicotinate Phosphoribosyltransferase (NAPRT) Modulators Abstract Abstract The prevention of nicotinamide adenine dinucleotide (NAD) biosynthesis is considered an attractive therapeutic approach against cancer, considering that tumor cells are characterized... |
PMC6274250 | core_pubmed_pmc | Simultaneous Determination of Eight Alkaloids in Rat Plasma by UHPLC-MS/MS after Oral Administration of Coptis deltoidea C. Y. Cheng et Hsiao and Coptis chinensis Franch | Simultaneous Determination of Eight Alkaloids in Rat Plasma by UHPLC-MS/MS after Oral Administration of Coptis deltoidea C. Y. Cheng et Hsiao and Coptis chinensis Franch Abstract A ultra-high performance liquid chromatography-electrospray ionization tandem mass spectrometry (UHPLC-ESI-MS/MS) method was successfully dev... |
PMC11549176 | core_pubmed_pmc | Does Age Influence Immunosuppressant Drug Pharmacokinetics in Kidney Transplant Recipients? | Does Age Influence Immunosuppressant Drug Pharmacokinetics in Kidney Transplant Recipients? Abstract Abstract Background The pharmacokinetics of immunosuppressant drugs may change with advancing age, potentially affecting patient outcomes. Objective To characterise the effects of age on the pharmacokinetic and exposure... |
PMC3476964 | core_pubmed_pmc | Organic anion transporting polypeptides OATP1B1 and OATP1B3 and their genetic variants influence the pharmacokinetics and pharmacodynamics of raloxifene | Organic anion transporting polypeptides OATP1B1 and OATP1B3 and their genetic variants influence the pharmacokinetics and pharmacodynamics of raloxifene Abstract Background Raloxifene, a selective estrogen receptor modulator, exhibits quite large and unexplained interindividual variability in pharmacokinetics and pharm... |
PMC7466894 | core_pubmed_pmc | Drug–Drug Interactions of 257 Antineoplastic and Supportive Care Agents With 7 Anticoagulants: A Comprehensive Review of Interactions and Mechanisms | Drug–Drug Interactions of 257 Antineoplastic and Supportive Care Agents With 7 Anticoagulants: A Comprehensive Review of Interactions and Mechanisms Abstract Abstract Data on drug–drug interactions (DDI) of antineoplastic drugs with anticoagulants is scarce. We aim to evaluate factors associated with DDI of antineoplas... |
PMC12842333 | core_pubmed_pmc | Macrocytosis as an Early Pharmacodynamic Marker of Imatinib Efficacy in Chronic Myeloid Leukemia | Macrocytosis as an Early Pharmacodynamic Marker of Imatinib Efficacy in Chronic Myeloid Leukemia Abstract Background: Macrocytosis commonly develops during imatinib therapy, but its relationship with cytogenetic and molecular outcomes in chronic myeloid leukemia (CML) remains unclear. We investigated whether increases ... |
PMC7059611 | core_pubmed_pmc | The K Ca 2 Channel Inhibitor AP30663 Selectively Increases Atrial Refractoriness, Converts Vernakalant-Resistant Atrial Fibrillation and Prevents Its Reinduction in Conscious Pigs | The K Ca 2 Channel Inhibitor AP30663 Selectively Increases Atrial Refractoriness, Converts Vernakalant-Resistant Atrial Fibrillation and Prevents Its Reinduction in Conscious Pigs Abstract Abstract Aims To describe the effects of the K Ca 2 channel inhibitor AP30663 in pigs regarding tolerability, cardiac electrophysio... |
PMC7191910 | core_pubmed_pmc | In vitro and in vivo evaluation of liposomes modified with polypeptides and red cell membrane as a novel drug delivery system for myocardium targeting | In vitro and in vivo evaluation of liposomes modified with polypeptides and red cell membrane as a novel drug delivery system for myocardium targeting Abstract Abstract Ischemic cardiac disease (ICD) is a cardiovascular disease with high morbidity and mortality. In this study, a novel myocardial targeted drug delivery ... |
PMC10451857 | core_pubmed_pmc | β -Lactam Pharmacokinetic/Pharmacodynamic Target Attainment in Intensive Care Unit Patients: A Prospective, Observational, Cohort Study | β -Lactam Pharmacokinetic/Pharmacodynamic Target Attainment in Intensive Care Unit Patients: A Prospective, Observational, Cohort Study Abstract Abstract Background: The aims of this study were to describe pharmacokinetic/pharmacodynamic target attainment in intensive care unit (ICU) patients treated with continuously ... |
PMC9709760 | core_pubmed_pmc | Translational Approach for Predicting Human Pharmacokinetics of Engineered Therapeutic Monoclonal Antibodies with Increased FcRn-Binding Mutations | Translational Approach for Predicting Human Pharmacokinetics of Engineered Therapeutic Monoclonal Antibodies with Increased FcRn-Binding Mutations Abstract Abstract Introduction Recently, increasing FcRn binding by Fc engineering has become a promising approach for prolonging the half-life of therapeutic monoclonal ant... |
PMC9351769 | core_pubmed_pmc | Beverage-induced enhanced bioavailability of carbamazepine and its consequent effect on antiepileptic activity and toxicity | Beverage-induced enhanced bioavailability of carbamazepine and its consequent effect on antiepileptic activity and toxicity Abstract Abstract The present study was undertaken to investigate the food–drug interaction of carbamazepine (CBZ). Common fruit juices [grapefruit juice (GFJ), lime juice (LJ)], known to inhibit ... |
PMC11296254 | core_pubmed_pmc | Direct oral anticoagulants in cirrhosis: Rationale and current evidence | Direct oral anticoagulants in cirrhosis: Rationale and current evidence Abstract Summary Cirrhosis is a major health concern worldwide with a complex pathophysiology affecting various biological systems, including all aspects of haemostasis. Bleeding risk is mainly driven by portal hypertension, but in end-stage liver ... |
PMC12396240 | core_pubmed_pmc | In vivo Pharmacokinetic Interactions Between Palbociclib and Rivaroxaban or Apixaban: Implications for Increased Drug Exposure and Dose Adjustments | In vivo Pharmacokinetic Interactions Between Palbociclib and Rivaroxaban or Apixaban: Implications for Increased Drug Exposure and Dose Adjustments Abstract Background Apixaban and rivaroxaban are oral direct factor Xa inhibitors, primarily eliminated through CYP3A4-mediated metabolism and direct intestinal excretion. ... |
PMC3367410 | core_pubmed_pmc | Update on the clinical utility and optimal use of cefditoren | Update on the clinical utility and optimal use of cefditoren Abstract Abstract This article reviews and updates published data on cefditoren. The in vitro activity of cefditoren and its potential pharmacokinetic/pharmacodynamic adequacy to cover emerging resistance phenotypes in the present decade is reviewed. Cefditor... |
PMC4702411 | core_pubmed_pmc | Early diagnosis of gestational trophoblastic neoplasia based on trajectory classification with compartment modeling | Early diagnosis of gestational trophoblastic neoplasia based on trajectory classification with compartment modeling Abstract Background In randomized clinical trials or observational studies, it is common to collect biomarker values longitudinally on a cohort of individuals. The investigators may be interested in group... |
PMC11369282 | core_pubmed_pmc | Reasons for non-feasibility of therapeutic drug monitoring of oral targeted therapies in oncology – an analysis of the closed cohorts of a multicentre prospective study | Reasons for non-feasibility of therapeutic drug monitoring of oral targeted therapies in oncology – an analysis of the closed cohorts of a multicentre prospective study Abstract Background Therapeutic drug monitoring (TDM) – performing dose adjustments based on measured drug levels and established pharmacokinetic (PK) ... |
PMC11768417 | core_pubmed_pmc | GnRH Peptide Antagonist: Comparative Analysis of Chemistry and Formulation with Implications for Clinical Safety and Efficacy | GnRH Peptide Antagonist: Comparative Analysis of Chemistry and Formulation with Implications for Clinical Safety and Efficacy Abstract Abstract Overexpression of the gonadotropin-releasing hormone receptor (GnRH-R) plays a vital role in the advancement of reproductive malignancies such as ovarian, endometrial, and pros... |
PMC7011244 | core_pubmed_pmc | A randomised, double-blind, active placebo-controlled, parallel groups, dose-response study of scopolamine hydrobromide (4–6 μg/kg) in patients with major depressive disorder | A randomised, double-blind, active placebo-controlled, parallel groups, dose-response study of scopolamine hydrobromide (4–6 μg/kg) in patients with major depressive disorder Abstract Background Depressive disorders are a leading cause of disability, but current behavioural and pharmacological therapies have a slow ons... |
PMC12655160 | core_pubmed_pmc | Nanoparticles Used for the Delivery of RNAi-Based Therapeutics | Nanoparticles Used for the Delivery of RNAi-Based Therapeutics Abstract Abstract RNA interference (RNAi) offers programmable, sequence-specific silencing via small interfering RNA (siRNA) and microRNA (miRNA), but clinical translation hinges on overcoming instability, immunogenicity, and inefficient endosomal escape. T... |
PMC7580710 | core_pubmed_pmc | Pharmacokinetics and biodistribution of a collagen‐targeted peptide amphiphile for cardiovascular applications | Pharmacokinetics and biodistribution of a collagen‐targeted peptide amphiphile for cardiovascular applications Abstract Abstract Atherosclerosis remains a leading cause of death and disability around the world and a major driver of health care spending. Nanomaterials have gained widespread attention due to their promis... |
PMC9939304 | core_pubmed_pmc | Bile duct ligation differently regulates protein expressions of organic cation transporters in intestine, liver and kidney of rats through activation of farnesoid X receptor by cholate and bilirubin | Bile duct ligation differently regulates protein expressions of organic cation transporters in intestine, liver and kidney of rats through activation of farnesoid X receptor by cholate and bilirubin Abstract Abstract Body is equipped with organic cation transporters (OCTs). These OCTs mediate drug transport and are als... |
PMC7016295 | core_pubmed_pmc | PCC0208017, a novel small-molecule inhibitor of MARK3/MARK4, suppresses glioma progression in vitro and in vivo | PCC0208017, a novel small-molecule inhibitor of MARK3/MARK4, suppresses glioma progression in vitro and in vivo Abstract Gliomas are the most common primary intracranial neoplasms among all brain malignancies, and the microtubule affinity regulating kinases (MARKs) have become potential drug targets for glioma. Here, w... |
PMC9695340 | core_pubmed_pmc | Varespladib in the Treatment of Snakebite Envenoming: Development History and Preclinical Evidence Supporting Advancement to Clinical Trials in Patients Bitten by Venomous Snakes | Varespladib in the Treatment of Snakebite Envenoming: Development History and Preclinical Evidence Supporting Advancement to Clinical Trials in Patients Bitten by Venomous Snakes Abstract The availability of effective, reliably accessible, and affordable treatments for snakebite envenoming is a critical and long unmet ... |
PMC7679071 | core_pubmed_pmc | Application of the Nested Enzyme‐Within‐Enterocyte (NEWE) Turnover Model for Predicting the Time Course of Pharmacodynamic Effects | Application of the Nested Enzyme‐Within‐Enterocyte (NEWE) Turnover Model for Predicting the Time Course of Pharmacodynamic Effects Abstract The gut wall consists of many biological elements, including enterocytes. Rapid turnover, a prominent feature of the enterocytes, has generally been ignored in the development of e... |
PMC12794103 | core_pubmed_pmc | Ocular gene therapy as a sustained drug delivery system: pharmacokinetic and genokinetic perspectives | Ocular gene therapy as a sustained drug delivery system: pharmacokinetic and genokinetic perspectives Abstract Ocular pharmacotherapy is constrained by compartmental anatomy and clearance barriers that limit sustained posterior-segment exposure. Intravitreal bolus dosing, therefore, remains dominant for retinal disease... |
PMC8466838 | core_pubmed_pmc | NAC and Vitamin D Improve CNS and Plasma Oxidative Stress in Neonatal HIE and Are Associated with Favorable Long-Term Outcomes | NAC and Vitamin D Improve CNS and Plasma Oxidative Stress in Neonatal HIE and Are Associated with Favorable Long-Term Outcomes Abstract N-acetylcysteine (NAC) and vitamin D provide effective neuroprotection in animal models of severe or inflammation-sensitized hypoxic ischemic encephalopathy (HIE). To translate these F... |
PMC5853719 | core_pubmed_pmc | Idebenone: Novel Strategies to Improve Its Systemic and Local Efficacy | Idebenone: Novel Strategies to Improve Its Systemic and Local Efficacy Abstract Abstract The key role of antioxidants in treating and preventing many systemic and topical diseases is well recognized. One of the most potent antioxidants available for pharmaceutical and cosmetic use is Idebenone (IDE), a synthetic analog... |
PMC7652256 | core_pubmed_pmc | Intranasal GSK2245035, a Toll-like receptor 7 agonist, does not attenuate the allergen-induced asthmatic response in a randomized, double-blind, placebo-controlled experimental medicine study | Intranasal GSK2245035, a Toll-like receptor 7 agonist, does not attenuate the allergen-induced asthmatic response in a randomized, double-blind, placebo-controlled experimental medicine study Abstract Background Allergic asthma is a heterogenous disorder predominantly driven by a type 2 inflammatory response to aeroall... |
PMC11315484 | core_pubmed_pmc | Serum and urinary biomarkers of vancomycin-induced acute kidney injury: A prospective, observational analysis | Serum and urinary biomarkers of vancomycin-induced acute kidney injury: A prospective, observational analysis Abstract Vancomycin, a first-line drug for treating methicillin-resistant Staphylococcus aureus infections, is associated with acute kidney injury (AKI). This study involved an evaluation of biomarkers for AKI ... |
PMC8048900 | core_pubmed_pmc | Applications of Physiologically Based Pharmacokinetic Modeling of Rivaroxaban—Renal and Hepatic Impairment and Drug‐Drug Interaction Potential | Applications of Physiologically Based Pharmacokinetic Modeling of Rivaroxaban—Renal and Hepatic Impairment and Drug‐Drug Interaction Potential Abstract Abstract The non–vitamin K antagonist oral anticoagulant rivaroxaban is used in several thromboembolic disorders. Rivaroxaban is eliminated via both metabolic degradati... |
PMC3444451 | core_pubmed_pmc | Pharmacokinetics and Biodistribution of a Human Monoclonal Antibody to Oxidized LDL in Cynomolgus Monkey Using PET Imaging | Pharmacokinetics and Biodistribution of a Human Monoclonal Antibody to Oxidized LDL in Cynomolgus Monkey Using PET Imaging Abstract Abstract Purpose Oxidized low-density lipoprotein (LDL) plays an essential role in the pathogenesis of atherosclerosis. The purpose of this study was to characterize the pharmacokinetics (... |
PMC4917800 | core_pubmed_pmc | A phase I pharmacokinetics trial comparing PF‐05280586 (a potential biosimilar) and rituximab in patients with active rheumatoid arthritis | A phase I pharmacokinetics trial comparing PF‐05280586 (a potential biosimilar) and rituximab in patients with active rheumatoid arthritis Abstract Abstract Aims Pharmacokinetic (PK) similarity was assessed among PF‐05280586 (a proposed biosimilar) vs . rituximab sourced from the European Union (rituximab‐EU) and the U... |
PMC10042768 | core_pubmed_pmc | Predictions of Bedaquiline and Pretomanid Target Attainment in Lung Lesions of Tuberculosis Patients using Translational Minimal Physiologically Based Pharmacokinetic Modeling | Predictions of Bedaquiline and Pretomanid Target Attainment in Lung Lesions of Tuberculosis Patients using Translational Minimal Physiologically Based Pharmacokinetic Modeling Abstract Background Site-of-action concentrations for bedaquiline and pretomanid from tuberculosis patients are unavailable. The objective of th... |
PMC10867212 | core_pubmed_pmc | Comparative pharmacokinetics of polymyxin B in critically ill elderly patients with extensively drug-resistant gram-negative bacteria infections | Comparative pharmacokinetics of polymyxin B in critically ill elderly patients with extensively drug-resistant gram-negative bacteria infections Abstract Abstract Introduction: Elderly patients are more prone to develop acute kidney injury during infections and polymyxin B (PMB)-associated nephrotoxicity than young pat... |
PMC3827219 | core_pubmed_pmc | Subcutaneous versus Intravenous Administration of Rituximab: Pharmacokinetics, CD20 Target Coverage and B-Cell Depletion in Cynomolgus Monkeys | Subcutaneous versus Intravenous Administration of Rituximab: Pharmacokinetics, CD20 Target Coverage and B-Cell Depletion in Cynomolgus Monkeys Abstract The CD20-specific monoclonal antibody rituximab (MabThera ® , Rituxan ® ) is widely used as the backbone of treatment for patients with hematologic disorders. Intraveno... |
PMC5063175 | core_pubmed_pmc | Relative Bioavailability of a Single Dose of Belimumab Administered Subcutaneously by Prefilled Syringe or Autoinjector in Healthy Subjects | Relative Bioavailability of a Single Dose of Belimumab Administered Subcutaneously by Prefilled Syringe or Autoinjector in Healthy Subjects Abstract Abstract Intravenous belimumab is approved for the treatment of systemic lupus erythematosus; subcutaneous self‐administration would enable greater patient access. This st... |
PMC10715014 | core_pubmed_pmc | Biological Role and Related Natural Products of SIRT1 in Nonalcoholic Fatty Liver | Biological Role and Related Natural Products of SIRT1 in Nonalcoholic Fatty Liver Abstract Abstract Non-alcoholic fatty liver disease(NAFLD) is an umbrella term for a range of diseases ranging from hepatic fat accumulation and steatosis to non-alcoholic steatohepatitis (NASH) in the absence of excessive alcohol consump... |
PMC11387175 | core_pubmed_pmc | Model informed dose regimen optimizing in development of leritrelvir for the treatment of mild or moderate COVID-19 | Model informed dose regimen optimizing in development of leritrelvir for the treatment of mild or moderate COVID-19 Abstract Introduction Leritrelvir (RAY1216) acts as a main protease inhibitor that hinders the cleavage of viral precursor proteins, thereby inhibiting virus replication of SARS-CoV-2). This antiviral mec... |
PMC3971850 | core_pubmed_pmc | Comparative Pharmacokinetics of Levofloxacin in Healthy and Renal Damaged Muscovy Ducks following Intravenous and Oral Administration | Comparative Pharmacokinetics of Levofloxacin in Healthy and Renal Damaged Muscovy Ducks following Intravenous and Oral Administration Abstract Abstract The pharmacokinetics aspects of levofloxacin were studied in healthy and experimentally renal damaged Muscovy ducks after single intravenous (IV) and oral (PO) dose of ... |
PMC7210126 | core_pubmed_pmc | Does the conventional dosage of linezolid necessitate therapeutic drug monitoring?—Experience from a prospective observational study | Does the conventional dosage of linezolid necessitate therapeutic drug monitoring?—Experience from a prospective observational study Abstract Abstract Background The objectives of the present prospective observational study conducted in patients receiving conventional dosage of linezolid was to define the pharmacodynam... |
PMC7704495 | core_pubmed_pmc | The atypical neuroleptics iloperidone and lurasidone inhibit human cytochrome P450 enzymes in vitro. Evaluation of potential metabolic interactions | The atypical neuroleptics iloperidone and lurasidone inhibit human cytochrome P450 enzymes in vitro. Evaluation of potential metabolic interactions Abstract Background The present study aimed at examining the inhibitory effect of two atypical neuroleptics iloperidone and lurasidone on the main human cytochrome P450 (CY... |
PMC10983000 | core_pubmed_pmc | Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein | Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein Abstract Abstract The H1047R mutation of PIK3CA is highly prevalent in breast cancers and other solid tumors. Selectively targeting PI3Kα H1047R over PI3Kα WT is crucial due to the role that PI3Kα WT plays in normal cellular proce... |
PMC9679284 | core_pubmed_pmc | An LC-MS/MS method for the simultaneous determination of 18 antibacterial drugs in human plasma and its application in therapeutic drug monitoring | An LC-MS/MS method for the simultaneous determination of 18 antibacterial drugs in human plasma and its application in therapeutic drug monitoring Abstract Abstract Antimicrobial resistance (AMR) is a major threat to global health due to the wide use of antibacterial drugs. Multiple studies show that the pharmacokineti... |
PMC5663928 | core_pubmed_pmc | Transition state-based ST6Gal I inhibitors: Mimicking the phosphodiester linkage with a triazole or carbamate through an enthalpy-entropy compensation | Transition state-based ST6Gal I inhibitors: Mimicking the phosphodiester linkage with a triazole or carbamate through an enthalpy-entropy compensation Abstract Human β-galactoside α-2,6-sialyltransferase I (ST6Gal I) catalyses the synthesis of sialylated glycoconjugates. Overexpression of ST6Gal I is observed in many c... |
PMC3636497 | core_pubmed_pmc | Basic Concepts in Population Modeling, Simulation, and Model-Based Drug Development—Part 2: Introduction to Pharmacokinetic Modeling Methods | Basic Concepts in Population Modeling, Simulation, and Model-Based Drug Development—Part 2: Introduction to Pharmacokinetic Modeling Methods Methods Software and Estimation Methods Numerous population modeling software packages are available. Choosing a package requires careful consideration including number of users i... |
PMC8073514 | core_pubmed_pmc | Time Is Brain: Acute Control of Repetitive Seizures and Status Epilepticus Using Alternative Routes of Administration of Benzodiazepines | Time Is Brain: Acute Control of Repetitive Seizures and Status Epilepticus Using Alternative Routes of Administration of Benzodiazepines Abstract Abstract Time plays a major role in seizure evaluation and treatment. Acute repetitive seizures and status epilepticus are medical emergencies that require immediate assessme... |
PMC12647384 | core_pubmed_pmc | Virtual screening of drugs against multiple targets of Alzheimer's disease | Virtual screening of drugs against multiple targets of Alzheimer's disease Abstract Background Drug repurposing offers a rapid, cost-effective approach for discovering therapies against multiple targets. Objective Here, we screen virtual ligand libraries consisting of 3468 approved drugs against 11 protein targets asso... |
PMC6098032 | core_pubmed_pmc | Physiologically based pharmacokinetic modelling of atomoxetine with regard to CYP2D6 genotypes | Physiologically based pharmacokinetic modelling of atomoxetine with regard to CYP2D6 genotypes Abstract Atomoxetine is a norepinephrine reuptake inhibitor indicated in the treatment of attention-deficit/hyperactivity disorder. It is primarily metabolized by CYP2D6 to its equipotent metabolite, 4-hydroxyatomoxetine, whi... |
PMC6021666 | core_pubmed_pmc | Population Pharmacokinetic Model and Meta-analysis of Outcomes of Amphotericin B Deoxycholate Use in Adults with Cryptococcal Meningitis | Population Pharmacokinetic Model and Meta-analysis of Outcomes of Amphotericin B Deoxycholate Use in Adults with Cryptococcal Meningitis Abstract ABSTRACT There is a limited understanding of the population pharmacokinetics (PK) and pharmacodynamics (PD) of amphotericin B deoxycholate (DAmB) for cryptococcal meningitis.... |
PMC12298270 | core_pubmed_pmc | Development and Validation of a New LC-MS/MS Method for Simultaneous Quantification of Ivacaftor, Tezacaftor and Elexacaftor Plasma Levels in Pediatric Cystic Fibrosis Patients | Development and Validation of a New LC-MS/MS Method for Simultaneous Quantification of Ivacaftor, Tezacaftor and Elexacaftor Plasma Levels in Pediatric Cystic Fibrosis Patients Abstract Abstract Background : “CFTR modulators” (also named “caftor”) have been developed and introduced into clinical practice to improve the... |
PMC6025039 | core_pubmed_pmc | Clinical Relevant Polymorphisms Affecting Clopidogrel Pharmacokinetics and Pharmacodynamics: Insights from the Puerto Rico Newborn Screening Program | Clinical Relevant Polymorphisms Affecting Clopidogrel Pharmacokinetics and Pharmacodynamics: Insights from the Puerto Rico Newborn Screening Program Abstract Abstract Background: Variations in several clopidogrel-pharmacogenes have been linked to clopidogrel response variability and clinical outcomes. We aimed to deter... |
PMC6161721 | core_pubmed_pmc | Effects of PEG surface density and chain length on the pharmacokinetics and biodistribution of methotrexate-loaded chitosan nanoparticles | Effects of PEG surface density and chain length on the pharmacokinetics and biodistribution of methotrexate-loaded chitosan nanoparticles Abstract Abstract Background One of the most important aspects of drug delivery is extended nanoparticle (NP) residence time in vivo. Herein, we report a series of methotrexate (MTX)... |
PMC12587678 | core_pubmed_pmc | Greenness and hospital admissions for cause specific mental disorders: multicountry time series study | Greenness and hospital admissions for cause specific mental disorders: multicountry time series study Abstract Abstract Objectives To examine the association between exposure to greenness and hospital admissions for mental disorders, and to estimate greenness related hospital admissions under various greenness interven... |
PMC11608994 | core_pubmed_pmc | Amentoflavone for treating cardiocerebrovascular diseases and neurological disorders | Amentoflavone for treating cardiocerebrovascular diseases and neurological disorders Abstract Amentoflavone (AME) is a flavonoid compound found in over 120 plants. Its extensive pharmacological activity for treating cardiocerebrovascular diseases and neurological disorders have attracted the attention of researchers in... |
PMC11419969 | core_pubmed_pmc | Individualized dosing parameters for tacrolimus in the presence of voriconazole: a real-world PopPK study | Individualized dosing parameters for tacrolimus in the presence of voriconazole: a real-world PopPK study Abstract Abstract Objectives Significant increase in tacrolimus exposure was observed during co-administration with voriconazole, and no population pharmacokinetic model exists for tacrolimus in renal transplant re... |
PMC3375006 | core_pubmed_pmc | Recommendations for the treatment of epilepsy in adult patients in general practice in Belgium: an update | Recommendations for the treatment of epilepsy in adult patients in general practice in Belgium: an update Abstract In 2008, a group of Belgian epilepsy experts published recommendations for antiepileptic drug (AED) treatment of epilepsies in adults and children. Selection of compounds was based on the registration and ... |
PMC12388280 | core_pubmed_pmc | Recent Progress in Health Benefits of Hederagenin and Its Glycosides | Recent Progress in Health Benefits of Hederagenin and Its Glycosides Abstract Hederagenin, a pentacyclic triterpenoid saponin from various medicinal plants, shows immense therapeutic potential; however, its inherent low bioavailability severely hinders its clinical translation. This comprehensive review synthesizes rec... |
PMC9744942 | core_pubmed_pmc | Third-generation antipsychotics in patients with schizophrenia and non-responsivity or intolerance to clozapine regimen: What is the evidence? | Third-generation antipsychotics in patients with schizophrenia and non-responsivity or intolerance to clozapine regimen: What is the evidence? Abstract Abstract Clozapine is considered « the golden standard » for the management of treatment-resistant schizophrenia, but many patients do not present adequate responsivity... |
PMC8312626 | core_pubmed_pmc | A Network Pharmacology-Based Investigation to the Pharmacodynamic Material Basis and Mechanisms of the Anti-Inflammatory and Anti-Viral Effect of Isatis indigotica | A Network Pharmacology-Based Investigation to the Pharmacodynamic Material Basis and Mechanisms of the Anti-Inflammatory and Anti-Viral Effect of Isatis indigotica Abstract Abstract Purpose Isatis indigotica ( Ii ) is a cruciferous herb that is widely distributed in China, and its roots and leaves have been used in two... |
PMC11571322 | core_pubmed_pmc | Investigating the effect a single dose of cannabidiol has on measures of stress in cats when being transported in a carrier and meeting a novel person in an unfamiliar environment | Investigating the effect a single dose of cannabidiol has on measures of stress in cats when being transported in a carrier and meeting a novel person in an unfamiliar environment Abstract Domestic cats ( Felis Catus ) are often exposed to stimuli that have the potential to negatively impact their welfare. These can in... |
PMC8783811 | core_pubmed_pmc | Targeting CD38 and PD-1 with isatuximab plus cemiplimab in patients with advanced solid malignancies: results from a phase I/II open-label, multicenter study | Targeting CD38 and PD-1 with isatuximab plus cemiplimab in patients with advanced solid malignancies: results from a phase I/II open-label, multicenter study Abstract Background Preclinical data suggest that concurrent treatment of anti-CD38 and antiprogrammed death 1 (PD-1)/programmed death ligand 1 (PD-L1) antibodies... |
PMC10469490 | core_pubmed_pmc | Anti-parasitic drug discovery against Babesia microti by natural compounds: an extensive computational drug design approach | Anti-parasitic drug discovery against Babesia microti by natural compounds: an extensive computational drug design approach Abstract Abstract Tick-borne Babesiosis is a parasitic infection caused by Babesia microti that can infect both animals and humans and may spread by tick, blood transfusions, and organ transplanta... |
PMC7341258 | core_pubmed_pmc | The Pharmacokinetics of Medetomidine Administered Subcutaneously during Isoflurane Anaesthesia in Sprague-Dawley Rats | The Pharmacokinetics of Medetomidine Administered Subcutaneously during Isoflurane Anaesthesia in Sprague-Dawley Rats Abstract Simple Summary Rodents, including rats, are used as animal models for research investigating neurological diseases in humans. To enable this research the animals are anaesthetized to facilitate... |
PMC9553805 | core_pubmed_pmc | Evaluation of Safety and Clinically Relevant Drug–Drug Interactions with Tucatinib in Healthy Volunteers | Evaluation of Safety and Clinically Relevant Drug–Drug Interactions with Tucatinib in Healthy Volunteers Abstract Abstract Background and Objective Tucatinib is approved for treatment of human epidermal growth factor receptor 2-positive metastatic breast cancer. Understanding potential drug–drug interactions (DDIs) in... |
PMC7485418 | core_pubmed_pmc | Pharmacokinetics of Intravenous, Intramuscular, Oral, and Transdermal Administration of Flunixin Meglumine in Pre-wean Piglets | Pharmacokinetics of Intravenous, Intramuscular, Oral, and Transdermal Administration of Flunixin Meglumine in Pre-wean Piglets Abstract Castration and tail-docking of pre-wean piglets are common procedures that are known to induce pain and would benefit from pain mitigation. Flunixin meglumine (FM) is a non-steroidal a... |
PMC10932351 | core_pubmed_pmc | Evaluating the Therapeutic Potential of Curcumin and Synthetic Derivatives: A Computational Approach to Anti-Obesity Treatments | Evaluating the Therapeutic Potential of Curcumin and Synthetic Derivatives: A Computational Approach to Anti-Obesity Treatments Abstract Natural compounds such as curcumin, a polyphenolic compound derived from the rhizome of turmeric, have gathered remarkable scientific interest due to their diverse metabolic benefits ... |
PMC10493391 | core_pubmed_pmc | Pharmacokinetics of delta-9-tetrahydrocannabinol following acute cannabis smoke exposure in mice; effects of sex, age, and strain | Pharmacokinetics of delta-9-tetrahydrocannabinol following acute cannabis smoke exposure in mice; effects of sex, age, and strain Abstract Increased use of cannabis and cannabinoids for recreational and medical purposes has led to a growth in research on their effects in animal models. The majority of this work has emp... |
PMC11303580 | core_pubmed_pmc | Population pharmacokinetic, pharmacodynamic and efficacy modeling of SB12 (proposed eculizumab biosimilar) and reference eculizumab | Population pharmacokinetic, pharmacodynamic and efficacy modeling of SB12 (proposed eculizumab biosimilar) and reference eculizumab Abstract Purpose To describe, compare similarity of pharmacokinetic (PK), pharmacodynamic (PD) and efficacy of SB12 and reference eculizumab (ECU) and find clinically significant covariate... |
PMC3725801 | core_pubmed_pmc | UGT2B17 Genotype and the Pharmacokinetic Serum Profile of Testosterone during Substitution Therapy with Testosterone Undecanoate. A Retrospective Experience from 207 Men with Hypogonadism | UGT2B17 Genotype and the Pharmacokinetic Serum Profile of Testosterone during Substitution Therapy with Testosterone Undecanoate. A Retrospective Experience from 207 Men with Hypogonadism Abstract Abstract Background: Testosterone (T) is mainly excreted in the urine as testosterone glucuronide (TG). This glucuronidatio... |
PMC10907394 | core_pubmed_pmc | Optimization of an in vitro Pseudomonas aeruginosa Biofilm Model to Examine Antibiotic Pharmacodynamics at the Air-Liquid Interface | Optimization of an in vitro Pseudomonas aeruginosa Biofilm Model to Examine Antibiotic Pharmacodynamics at the Air-Liquid Interface Abstract Pseudomonas aeruginosa is an important cause of lower respiratory tract infections, such as ventilator-associated bacterial pneumonia (VABP). Using inhaled antibiotics to treat VA... |
PMC11979273 | core_pubmed_pmc | A phase I study to evaluate the safety, tolerability, and pharmacokinetics of HEC113995PA·H 2 O, a novel dual-acting serotonergic antidepressant, in healthy subjects | A phase I study to evaluate the safety, tolerability, and pharmacokinetics of HEC113995PA·H 2 O, a novel dual-acting serotonergic antidepressant, in healthy subjects Abstract Abstract Purpose HEC113995PA·H 2 O is a novel, potent and selective serotonin (5-HT) reuptake inhibitor and a 5-HT1A receptor partial agonist, an... |
PMC7037631 | core_pubmed_pmc | Influence of Germline Genetics on Tacrolimus Pharmacokinetics and Pharmacodynamics in Allogeneic Hematopoietic Stem Cell Transplant Patients | Influence of Germline Genetics on Tacrolimus Pharmacokinetics and Pharmacodynamics in Allogeneic Hematopoietic Stem Cell Transplant Patients Abstract Abstract Tacrolimus exhibits high inter-patient pharmacokinetics (PK) variability, as well as a narrow therapeutic index, and therefore requires therapeutic drug monitori... |
PMC12311024 | core_pubmed_pmc | Comparative analysis of phytocompounds and repurposed drugs against dengue virus serotypes employing an in silico study | Comparative analysis of phytocompounds and repurposed drugs against dengue virus serotypes employing an in silico study Abstract Dengue virus (DENV) has emerged as a formidable global health challenge, with a surging incidence rate across the world. Despite numerous research initiatives aimed at developing effective an... |
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