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PMC9066631 | core_pubmed_pmc | Population pharmacokinetic model and limited sampling strategy for clozapine using plasma and dried blood spot samples | Population pharmacokinetic model and limited sampling strategy for clozapine using plasma and dried blood spot samples Abstract Background: To improve efficacy, therapeutic drug monitoring is often used in clozapine therapy. Trough level monitoring is regular, but trough levels provide limited information about the pha... |
PMC11108815 | core_pubmed_pmc | Comparative pharmacokinetic study on phenolic acids and flavonoids in normal and microcirculation dysfunction rats plasma by UPLC-TQ/MS/MS after oral administration of Salvia miltiorrhiza stem-leaf extracts | Comparative pharmacokinetic study on phenolic acids and flavonoids in normal and microcirculation dysfunction rats plasma by UPLC-TQ/MS/MS after oral administration of Salvia miltiorrhiza stem-leaf extracts Abstract According to the Standard of Chinese Medicinal Materials of Shaanxi Province (2015 edition), Salvia milt... |
PMC9782902 | core_pubmed_pmc | An Updated Review of the Genus Humulus : A Valuable Source of Bioactive Compounds for Health and Disease Prevention | An Updated Review of the Genus Humulus : A Valuable Source of Bioactive Compounds for Health and Disease Prevention Abstract Abstract The medicinal potential of hop ( Humulus lupulus L.) is widely cited in ancient literature and is also allowed in several official pharmacopoeias for the treatment of a variety of ailmen... |
PMC12208389 | core_pubmed_pmc | Small-Molecule Neutrophil Modulator ADS051 is Safe and Well-Tolerated in a Phase 1 Single Ascending Dose Study | Small-Molecule Neutrophil Modulator ADS051 is Safe and Well-Tolerated in a Phase 1 Single Ascending Dose Study Abstract Abstract INTRODUCTION: A need for better treatment options for moderate to severe ulcerative colitis (UC) persists because of the efficacy and safety limitations of current therapies. Neutrophil epith... |
PMC6556864 | core_pubmed_pmc | Development and validation of a high performance liquid chromatography method to determine nevirapine in plasma in a resource-limited setting | Development and validation of a high performance liquid chromatography method to determine nevirapine in plasma in a resource-limited setting Abstract Background There are several instances where nevirapine pharmacokinetic monitoring may be useful, such as in special populations or pharmacokinetic drug interaction stud... |
PMC5198948 | core_pubmed_pmc | Phase I trial of GBS ‐01 for advanced pancreatic cancer refractory to gemcitabine | Phase I trial of GBS ‐01 for advanced pancreatic cancer refractory to gemcitabine Abstract GBS ‐01, an extract from the fruit of Arctium lappa L. is an orally administered drug rich in arctigenin, which has been reported to exert antitumor activity by attenuating the tolerance of cancer cells to glucose deprivation. We... |
PMC8596653 | core_pubmed_pmc | Extracorporeal membrane oxygenation may decrease the plasma concentration of remdesivir in a patient with severe coronavirus disease 2019 | Extracorporeal membrane oxygenation may decrease the plasma concentration of remdesivir in a patient with severe coronavirus disease 2019 Abstract Abstract Remdesivir is an antiviral drug that results in clinical improvement after five days of treatment and accelerates recovery by 31%. No studies have discussed the pha... |
PMC10456556 | core_pubmed_pmc | In Silico Analysis of the Effect of Hydrastis canadensis on Controlling Breast Cancer | In Silico Analysis of the Effect of Hydrastis canadensis on Controlling Breast Cancer Abstract Abstract Background and Objectives: Breast cancer is a significant type of cancer among women worldwide. Studies have reported the anti-carcinogenic activity of Hydrastis Canadensis (Goldenseal) in cancer cell lines. Hydrasti... |
PMC6503553 | core_pubmed_pmc | Establishment of a rat ovarian peritoneal metastasis model to study pressurized intraperitoneal aerosol chemotherapy (PIPAC) | Establishment of a rat ovarian peritoneal metastasis model to study pressurized intraperitoneal aerosol chemotherapy (PIPAC) Abstract Abstract Background pressurized intraperitoneal aerosol chemotherapy (PIPAC), with or without electrostatic precipitation (ePIPAC), was recently introduced in the treatment of peritoneal... |
PMC3983397 | core_pubmed_pmc | Pharmacokinetics of Equol, a Soy Isoflavone Metabolite, Changes with the Form of Equol (Dietary versus Intestinal Production) in Ovariectomized Rats | Pharmacokinetics of Equol, a Soy Isoflavone Metabolite, Changes with the Form of Equol (Dietary versus Intestinal Production) in Ovariectomized Rats Abstract Recent findings indicate that soy isoflavones and their metabolites may play a role in mitigating postmenopausal bone loss. Equol, a metabolite of the soy isoflav... |
PMC6519195 | core_pubmed_pmc | A Phase 1 Randomized Study of Single Intravenous Infusions of the Novel Nitroxyl Donor BMS‐986231 in Healthy Volunteers | A Phase 1 Randomized Study of Single Intravenous Infusions of the Novel Nitroxyl Donor BMS‐986231 in Healthy Volunteers Abstract Abstract Nitroxyl (HNO) is a reactive nitrogen molecule that has potential therapeutic benefits for patients with acute heart failure. The results of the first‐in‐human study for BMS‐986231, ... |
PMC12615189 | core_pubmed_pmc | Flavonoids as Immunoregulators: Molecular Mechanisms in Regulating Immune Cells and Their Therapeutic Applications in Inflammatory Diseases | Flavonoids as Immunoregulators: Molecular Mechanisms in Regulating Immune Cells and Their Therapeutic Applications in Inflammatory Diseases Abstract Flavonoids are a vital class of dietary polyphenolic compounds that have attracted considerable attention owing to their powerful immunoregulatory and anti-inflammatory ef... |
PMC11247107 | core_pubmed_pmc | Population pharmacokinetics and pharmacodynamics of nasal glucagon in patients with type 1 or 2 diabetes | Population pharmacokinetics and pharmacodynamics of nasal glucagon in patients with type 1 or 2 diabetes Abstract Abstract The objective was to characterize the pharmacokinetics (PK) and pharmacodynamics (PD) of glucagon after injectable or nasal administration and confirm the appropriate therapeutic dose of nasal gluc... |
PMC9047896 | core_pubmed_pmc | Computational Site Saturation Mutagenesis of Canonical and Non-Canonical Amino Acids to Probe Protein-Peptide Interactions | Computational Site Saturation Mutagenesis of Canonical and Non-Canonical Amino Acids to Probe Protein-Peptide Interactions Abstract Abstract Technologies for discovering peptides as potential therapeutics have rapidly advanced in recent years with significant interest from both academic and pharmaceutical labs. These a... |
PMC11234153 | core_pubmed_pmc | Isolation of 6-gingerol and semi-synthesis of 1,4-benzodiazepines derivatives: An in-situ pharmacokinetics properties, molecular docking and molecular dynamics simulation assessments | Isolation of 6-gingerol and semi-synthesis of 1,4-benzodiazepines derivatives: An in-situ pharmacokinetics properties, molecular docking and molecular dynamics simulation assessments Abstract Abstract This paper outlines a methodical approach for isolating 6-gingerol (1a) from Zingiber officinale Roscoe rhizomes on a g... |
PMC9996394 | core_pubmed_pmc | Association between simulated ketamine exposures and oxygen saturations in children | Association between simulated ketamine exposures and oxygen saturations in children Abstract Aim We performed a real-world data analysis to evaluate the relationship between simulated ketamine exposures and oxygen desaturation in children. Materials & methods A previously developed population pharmacokinetic model was ... |
PMC6590404 | core_pubmed_pmc | Urinary glucose excretion after dapagliflozin treatment: An exposure‐response modelling comparison between Japanese and non‐Japanese patients diagnosed with type 1 diabetes mellitus | Urinary glucose excretion after dapagliflozin treatment: An exposure‐response modelling comparison between Japanese and non‐Japanese patients diagnosed with type 1 diabetes mellitus Abstract Abstract Aims To assess the dapagliflozin exposure‐response relationship in Japanese and non‐Japanese patients with type 1 diabet... |
PMC9561909 | core_pubmed_pmc | Incorporating stand density effects and regression techniques for stem taper modeling of a Larix principis-rupprechtii plantation | Incorporating stand density effects and regression techniques for stem taper modeling of a Larix principis-rupprechtii plantation Abstract Abstract Stem form is the shape of the trunk, differs among tree species and mainly affected by stand density factor. Accurate taper equations are crucial for estimating the stem di... |
PMC6804407 | core_pubmed_pmc | Determination of Cytochrome P450 Isoenzyme 2D6 (CYP2D6) Genotypes and Pharmacogenomic Impact on Primaquine Metabolism in an Active-Duty US Military Population | Determination of Cytochrome P450 Isoenzyme 2D6 (CYP2D6) Genotypes and Pharmacogenomic Impact on Primaquine Metabolism in an Active-Duty US Military Population Abstract Abstract Background Plasmodium vivax malaria requires a 2-week course of primaquine (PQ) for radical cure. Evidence suggests that the hepatic isoenzyme ... |
PMC5465246 | core_pubmed_pmc | Camelid Single-Domain Antibodies As an Alternative to Overcome Challenges Related to the Prevention, Detection, and Control of Neglected Tropical Diseases | Camelid Single-Domain Antibodies As an Alternative to Overcome Challenges Related to the Prevention, Detection, and Control of Neglected Tropical Diseases Abstract Due mainly to properties such as high affinity and antigen specificity, antibodies have become important tools for biomedical research, diagnosis, and treat... |
PMC11762721 | core_pubmed_pmc | Pharmacokinetics of Hydrogen During Hydrogen-Saturated Saline Infusion in Pigs | Pharmacokinetics of Hydrogen During Hydrogen-Saturated Saline Infusion in Pigs Abstract Background : Hydrogen gas (H 2 ) has been shown to be effective in the treatment of various clinical conditions, from acute illnesses to chronic illnesses. However, its clinical indications and the corresponding appropriate hydrogen... |
PMC12767642 | core_pubmed_pmc | Fitness Landscape for Antibodies 2: Benchmarking Reveals That Protein AI Models Cannot Yet Consistently Predict Developability Properties | Fitness Landscape for Antibodies 2: Benchmarking Reveals That Protein AI Models Cannot Yet Consistently Predict Developability Properties Abstract A prominent application of machine learning in therapeutic antibody design is the development of models that can generate or screen antibody candidates with a high probabili... |
PMC6442999 | core_pubmed_pmc | Biomarker results from a phase II study of MEK1/2 inhibitor binimetinib (MEK162) in patients with advanced NRAS - or BRAF -mutated melanoma | Biomarker results from a phase II study of MEK1/2 inhibitor binimetinib (MEK162) in patients with advanced NRAS - or BRAF -mutated melanoma Abstract Abstract BRAF and RAS are the most frequently mutated mitogen-activated protein kinase (MAPK) genes in melanoma. Binimetinib is a highly selective MAPK kinase (MEK) 1/2 in... |
PMC12272296 | core_pubmed_pmc | A Review of Pharmacokinetic and Pharmacodynamic Properties of Quetiapine IR and XR: Insights and Clinical Practice Implications | A Review of Pharmacokinetic and Pharmacodynamic Properties of Quetiapine IR and XR: Insights and Clinical Practice Implications Abstract Treatment adherence is a key consideration for patients with psychiatric illnesses. One of the strategies to improve compliance is the development of extended-release (XR) formulation... |
PMC12655451 | core_pubmed_pmc | Topical β-Caryophyllene for Dermatologic Disorders: Mechanisms, Human Evidence, and Clinical Translation | Topical β-Caryophyllene for Dermatologic Disorders: Mechanisms, Human Evidence, and Clinical Translation Abstract Background: Chronic inflammatory skin disorders, including atopic dermatitis, psoriasis, acne, and chronic wounds, affect nearly two billion people worldwide, impose substantial morbidity and economic burde... |
PMC10344656 | core_pubmed_pmc | Plasma pharmacokinetics of tigolaner, emodepside, and praziquantel following topical administration of a combination product (Felpreva®) and of intravenous administration of the individual active ingredients in cats | Plasma pharmacokinetics of tigolaner, emodepside, and praziquantel following topical administration of a combination product (Felpreva®) and of intravenous administration of the individual active ingredients in cats Abstract Abstract Felpreva® for cats contains the new acaricidal/insecticidal active ingredient tigolane... |
PMC12799507 | core_pubmed_pmc | Aspirin inhibition and recovery of cyclooxygenase activity and thromboxane biosynthesis in human megakaryocytes: a translational surrogate model | Aspirin inhibition and recovery of cyclooxygenase activity and thromboxane biosynthesis in human megakaryocytes: a translational surrogate model Abstract Abstract Low-dose aspirin irreversibly acetylates cyclooxygenase (COX)-1 in anucleate platelets and progenitor megakaryocytes, permanently suppressing thromboxane (TX... |
PMC9749037 | core_pubmed_pmc | Pharmacokinetic boosting to enable a once-daily reduced dose of tofacitinib in patients with rheumatoid arthritis and psoriatic arthritis (the PRACTICAL study) | Pharmacokinetic boosting to enable a once-daily reduced dose of tofacitinib in patients with rheumatoid arthritis and psoriatic arthritis (the PRACTICAL study) Abstract Abstract Background: Tofacitinib is a Janus Kinase (JAK) inhibitor used for the treatment of rheumatoid arthritis (RA) and psoriatic arthritis (PsA), d... |
PMC10325562 | core_pubmed_pmc | Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor | Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor Abstract Background: Inhibition of PCSK9 (proprotein convertase subtilisin/kexin type 9)-low density lipoprotein receptor interaction with injectable monoclonal antibodies or small interfering RNA lowers plasm... |
PMC6800464 | core_pubmed_pmc | Population pharmacokinetic modeling to facilitate dose selection of tapentadol in the pediatric population | Population pharmacokinetic modeling to facilitate dose selection of tapentadol in the pediatric population Abstract Abstract Objective The main aim of this analysis was to characterize the pharmacokinetics (PK) of the strong analgesic tapentadol in 2-year-old to <18-year-old patients with acute pain and to inform the o... |
PMC10889795 | core_pubmed_pmc | Management of Polypharmacy and Potential Drug–Drug Interactions in Patients with Pulmonary Aspergillosis: A 2-Year Study of a Multidisciplinary Outpatient Clinic | Management of Polypharmacy and Potential Drug–Drug Interactions in Patients with Pulmonary Aspergillosis: A 2-Year Study of a Multidisciplinary Outpatient Clinic Abstract Pulmonary aspergillosis mainly affects elderly patients, patients with pulmonary complications, patients with hematological malignancies, organ trans... |
PMC11755583 | core_pubmed_pmc | ABCB1 Polymorphism Is Associated with Higher Carbamazepine Clearance in Children | ABCB1 Polymorphism Is Associated with Higher Carbamazepine Clearance in Children Abstract Abstract The aim of our study was to investigate the role of ABCB1 polymorphism in the pharmacokinetics of carbamazepine (CBZ) in children. The study enrolled 47 Serbian pediatric epileptic patients on CBZ treatment. Genotyping fo... |
PMC5874814 | core_pubmed_pmc | Prediction of Drug-Drug Interactions with Bupropion and Its Metabolites as CYP2D6 Inhibitors Using a Physiologically-Based Pharmacokinetic Model | Prediction of Drug-Drug Interactions with Bupropion and Its Metabolites as CYP2D6 Inhibitors Using a Physiologically-Based Pharmacokinetic Model Abstract The potential of inhibitory metabolites of perpetrator drugs to contribute to drug-drug interactions (DDIs) is uncommon and underestimated. However, the occurrence of... |
PMC5278714 | core_pubmed_pmc | Safety and Pharmacokinetics of CD101 IV, a Novel Echinocandin, in Healthy Adults | Safety and Pharmacokinetics of CD101 IV, a Novel Echinocandin, in Healthy Adults Abstract ABSTRACT CD101 IV is a novel echinocandin with distinctive pharmacokinetic properties that is being developed as a once-weekly treatment for candidemia and invasive candidiasis. CD101 has potent in vitro activity and in vivo effic... |
PMC8504808 | core_pubmed_pmc | Dose selection for intracerebroventricular cerliponase alfa in children with CLN2 disease, translation from animal to human in a rare genetic disease | Dose selection for intracerebroventricular cerliponase alfa in children with CLN2 disease, translation from animal to human in a rare genetic disease Abstract Abstract Neuronal ceroid lipofuscinosis type 2 (CLN2 disease) is an ultra‐rare pediatric neurodegenerative disorder characterized by deficiency of the lysosomal ... |
PMC9205771 | core_pubmed_pmc | Safety and antiviral activity of triple combination broadly neutralizing monoclonal antibody therapy against HIV-1: a phase 1 clinical trial | Safety and antiviral activity of triple combination broadly neutralizing monoclonal antibody therapy against HIV-1: a phase 1 clinical trial Abstract Abstract HIV-1 therapy with single or dual broadly neutralizing antibodies (bNAbs) has shown viral escape, indicating that at least a triple bNAb therapy may be needed fo... |
PMC9609254 | core_pubmed_pmc | Comparison of Certain Intrarectal versus Intramuscular Pharmacodynamic Effects of Ketamine, Dexmedetomidine and Midazolam in Cats | Comparison of Certain Intrarectal versus Intramuscular Pharmacodynamic Effects of Ketamine, Dexmedetomidine and Midazolam in Cats Abstract Abstract Simple Summary The chemical immobilization of cats is widely required in veterinary clinical practice; sedative drugs are administered intramuscularly and routinely, but th... |
PMC8234416 | core_pubmed_pmc | Pharmacodynamics and Outcomes of a De-Escalation Strategy with Half-Dose Prasugrel or Ticagrelor in East Asians Patients with Acute Coronary Syndrome: Results from HOPE-TAILOR Trial | Pharmacodynamics and Outcomes of a De-Escalation Strategy with Half-Dose Prasugrel or Ticagrelor in East Asians Patients with Acute Coronary Syndrome: Results from HOPE-TAILOR Trial Abstract Abstract East Asians treated with potent P2Y12 inhibitors (prasugrel or ticagrelor) generally experience more intense platelet in... |
PMC9800240 | core_pubmed_pmc | Low and Highly Variable Exposure to Prophylactic LMWH Nadroparin in Critically Ill Patients: Back to the Drawing Board for Prophylactic Dosing? | Low and Highly Variable Exposure to Prophylactic LMWH Nadroparin in Critically Ill Patients: Back to the Drawing Board for Prophylactic Dosing? Abstract Background and Objective Low-molecular-weight heparins are routinely administered to patients in the intensive care unit to prevent venous thromboembolisms. There is c... |
PMC5961452 | core_pubmed_pmc | Quantitative translational modeling to facilitate preclinical to clinical efficacy & toxicity translation in oncology | Quantitative translational modeling to facilitate preclinical to clinical efficacy & toxicity translation in oncology Abstract Abstract Significant scientific advances in biomedical research have expanded our knowledge of the molecular basis of carcinogenesis, mechanisms of cancer growth, and the importance of the canc... |
PMC7884963 | core_pubmed_pmc | Post-Dialysis Parenteral Antimicrobial Therapy in Patients Receiving Intermittent High-Flux Hemodialysis | Post-Dialysis Parenteral Antimicrobial Therapy in Patients Receiving Intermittent High-Flux Hemodialysis Abstract Abstract Patients with end-stage renal disease (ESRD) requiring intermittent hemodialysis (IHD) are at increased risk of infection, which represents a leading cause of mortality in this population. The use ... |
PMC9182099 | core_pubmed_pmc | Individualized Dosage of Tacrolimus for Renal Transplantation Patients Based on Pharmacometabonomics | Individualized Dosage of Tacrolimus for Renal Transplantation Patients Based on Pharmacometabonomics Abstract Abstract The clinical pharmacodynamics of tacrolimus in renal transplant patients has significant interindividual variability. T lymphocytes were selected to study the pharmacodynamic response of tacrolimus, wh... |
PMC6757358 | core_pubmed_pmc | Preparation, optimization and in vitro–in vivo evaluation of Shunxin sustained release granules | Preparation, optimization and in vitro–in vivo evaluation of Shunxin sustained release granules Abstract Background Shunxinzufang decoction is tutors, empirical formula and has been used in Chinese patients of HFpEF for several years. The aim of this study was to make into sustained release granules and select the best... |
PMC4281361 | core_pubmed_pmc | A pharmacokinetic and pharmacodynamic investigation of Modufolin ® compared to Isovorin ® after single dose intravenous administration to patients with colon cancer: a randomized study | A pharmacokinetic and pharmacodynamic investigation of Modufolin ® compared to Isovorin ® after single dose intravenous administration to patients with colon cancer: a randomized study Abstract Purpose Leucovorin is commonly used as folate supplement in 5-fluorouracil-based chemotherapy, but needs to be converted to ac... |
PMC12024143 | core_pubmed_pmc | A Laboratory Protocol for Routine Therapeutic Drug Monitoring of Beta-Lactams Antimicrobials in Horses and Dogs | A Laboratory Protocol for Routine Therapeutic Drug Monitoring of Beta-Lactams Antimicrobials in Horses and Dogs Abstract Background: Although antibiotic resistance is a well-known issue in veterinary medicine, studies proposing real-time therapeutic monitoring (TDM) are lacking. The objective of the present study was t... |
PMC9578392 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of the Novel Antiviral Agent Ensitrelvir Fumaric Acid, a SARS-CoV-2 3CL Protease Inhibitor, in Healthy Adults | Safety, Tolerability, and Pharmacokinetics of the Novel Antiviral Agent Ensitrelvir Fumaric Acid, a SARS-CoV-2 3CL Protease Inhibitor, in Healthy Adults Abstract ABSTRACT Ensitrelvir is a novel selective inhibitor of the 3C-like protease of SARS-CoV-2, which is essential for viral replication. This phase 1 study of ens... |
PMC9774199 | core_pubmed_pmc | Catechin Bioavailability Following Consumption of a Green Tea Extract Confection Is Reduced in Obese Persons without Affecting Gut Microbial-Derived Valerolactones | Catechin Bioavailability Following Consumption of a Green Tea Extract Confection Is Reduced in Obese Persons without Affecting Gut Microbial-Derived Valerolactones Abstract Abstract Obesity-related cardiometabolic disorders are driven by inflammation, oxidative stress, and gut dysbiosis. Green tea catechins protect aga... |
PMC10090391 | core_pubmed_pmc | Commentary: Sweet taste is complex: Signaling cascades and circuits involved in sweet sensation | Commentary: Sweet taste is complex: Signaling cascades and circuits involved in sweet sensation Modeling Pharmacokinetic models for sweet taste mixtures in humans Developing and testing a model for smell and taste in humans poses some challenges because human experimentation necessarily involves chemosensory psychophys... |
PMC3847280 | core_pubmed_pmc | Effective concentration-based serum pharmacodynamics for antifungal azoles in a murine model of disseminated Candida albicans infection | Effective concentration-based serum pharmacodynamics for antifungal azoles in a murine model of disseminated Candida albicans infection Abstract Abstract An assessment of the effective in vivo concentrations of antifungal drugs is important in determining their pharmacodynamics, and therefore, their optimal dosage regi... |
PMC9656984 | core_pubmed_pmc | Development and Validation of a UHPLC–MS/MS-Based Method to Quantify Cenobamate in Human Plasma Samples | Development and Validation of a UHPLC–MS/MS-Based Method to Quantify Cenobamate in Human Plasma Samples Abstract Abstract Cenobamate (CNB) is the newest antiseizure medication (ASM) approved by the FDA in 2019 to reduce uncontrolled partial-onset seizures in adult patients. Marketed as Xcopri in the USA or Ontozry in t... |
PMC7460644 | core_pubmed_pmc | Therapeutic Drug Monitoring Is a Feasible Tool to Personalize Drug Administration in Neonates Using New Techniques: An Overview on the Pharmacokinetics and Pharmacodynamics in Neonatal Age | Therapeutic Drug Monitoring Is a Feasible Tool to Personalize Drug Administration in Neonates Using New Techniques: An Overview on the Pharmacokinetics and Pharmacodynamics in Neonatal Age Abstract Abstract Therapeutic drug monitoring (TDM) should be adopted in all neonatal intensive care units (NICUs), where the most ... |
PMC5377466 | core_pubmed_pmc | Oral intake of curcumin markedly activated CYP 3A4: in vivo and ex-vivo studies | Oral intake of curcumin markedly activated CYP 3A4: in vivo and ex-vivo studies Abstract Curcumin, a specific secondary metabolite of Curcuma species, has potentials for a variety of beneficial health effects. It is nowadays used as a dietary supplement. Everolimus (EVL) is an immunosuppressant indicated for allograft ... |
PMC12961628 | core_pubmed_pmc | Clinical Evaluation of Drug–Drug Interactions With Aficamten | Clinical Evaluation of Drug–Drug Interactions With Aficamten Abstract ABSTRACT Aficamten is a next‐in‐class small molecule cardiac myosin inhibitor that was recently approved by the United States Food and Drug Administration (FDA) for the treatment of symptomatic obstructive hypertrophic cardiomyopathy (oHCM). A compre... |
PMC11945394 | core_pubmed_pmc | Cyclodextrin-Based Drug Delivery Systems for Depression: Improving Antidepressant Bioavailability and Targeted Central Nervous System Delivery | Cyclodextrin-Based Drug Delivery Systems for Depression: Improving Antidepressant Bioavailability and Targeted Central Nervous System Delivery Abstract Abstract Cyclodextrin (CD)-based drug delivery systems have emerged as a promising strategy to overcome limitations commonly encountered in antidepressant therapy, incl... |
PMC11500077 | core_pubmed_pmc | Exploration of phytoconstituents of Medhya Rasayana herbs to identify potential inhibitors for cerebroside sulfotransferase through high-throughput screening | Exploration of phytoconstituents of Medhya Rasayana herbs to identify potential inhibitors for cerebroside sulfotransferase through high-throughput screening Abstract Cerebroside sulfotransferase (CST) is a key enzyme in sulfatide biosynthesis and regulation of the myelin sheath in the nervous system. To counter sulfat... |
PMC12770539 | core_pubmed_pmc | Formulation, development and characterization of fosfomycin tromethamine pessaries for the treatment of vaginal infections | Formulation, development and characterization of fosfomycin tromethamine pessaries for the treatment of vaginal infections Abstract Background The present study investigated the formulation, development, and characterization of Fosfomycin pessaries for the treatment of genitourinary tract infections. To achieve higher ... |
PMC9574734 | core_pubmed_pmc | Physiologically‐based pharmacokinetic modeling of immunoglobulin and antibody coadministration in patients with primary human immunodeficiency | Physiologically‐based pharmacokinetic modeling of immunoglobulin and antibody coadministration in patients with primary human immunodeficiency Abstract Abstract Intravenous immunoglobulin (IVIG) (2000 mg/kg) increased the clearance of the mouse monoclonal antibody 7E3, directed against platelet integrin IIb/IIIa (alpha... |
PMC11750932 | core_pubmed_pmc | Relevance of Neutralizing Antibodies for the Pharmacokinetics of Pegunigalsidase Alfa in Patients with Fabry Disease | Relevance of Neutralizing Antibodies for the Pharmacokinetics of Pegunigalsidase Alfa in Patients with Fabry Disease Abstract Abstract Background Pegunigalsidase alfa is a newly approved drug for the treatment of Fabry disease, designed to increase the plasma half-life and reduce immunogenicity of infused α-galactosida... |
PMC6661244 | core_pubmed_pmc | Physicochemical and Pharmacokinetic Profiles of Gadopiclenol | Physicochemical and Pharmacokinetic Profiles of Gadopiclenol Abstract Abstract Objectives We aimed to evaluate gadopiclenol, a newly developed extracellular nonspecific macrocyclic gadolinium-based contrast agent (GBCA) having high relaxivity properties, which was designed to increase lesion detection and characterizat... |
PMC11812932 | core_pubmed_pmc | Population pharmacokinetic and pharmacodynamic model of evogliptin: Severe uremia increases the bioavailability of evogliptin | Population pharmacokinetic and pharmacodynamic model of evogliptin: Severe uremia increases the bioavailability of evogliptin Abstract Abstract Uremia, a condition characterized by the retention of uremic toxins due to impaired renal function, may affect drug metabolism mediated by CYP3A4 enzymes. Evogliptin is a dipep... |
PMC7788571 | core_pubmed_pmc | Pharmacokinetic Modeling of ( R )-[ 11 C]verapamil to Measure the P-Glycoprotein Function in Nonhuman Primates | Pharmacokinetic Modeling of ( R )-[ 11 C]verapamil to Measure the P-Glycoprotein Function in Nonhuman Primates Abstract Abstract ( R )-[ 11 C]verapamil is a radiotracer widely used for the evaluation of the P-glycoprotein (P-gp) function at the blood–brain barrier (BBB). Several studies have evaluated the pharmacokinet... |
PMC8802796 | core_pubmed_pmc | Pharmacokinetic Evaluation of Cefazolin in the Cerebrospinal Fluid of Critically Ill Patients | Pharmacokinetic Evaluation of Cefazolin in the Cerebrospinal Fluid of Critically Ill Patients Abstract Abstract Background The relative distribution of cefazolin into the cerebrospinal fluid (CSF) remains debated. Determining the distribution of cefazolin into the CSF in noninfected adults may allow for further treatme... |
PMC6440935 | core_pubmed_pmc | Characterization and phase I study of CLR457, an orally bioavailable pan-class I PI3-kinase inhibitor | Characterization and phase I study of CLR457, an orally bioavailable pan-class I PI3-kinase inhibitor Abstract Summary Background CLR457 is an orally bioavailable pan-phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) inhibitor. Methods CLR457 anti-tumor activity and pharmacokinetics (PK) were characterized by in vi... |
PMC7663638 | core_pubmed_pmc | New Methods Used in Pharmacokinetics and Therapeutic Monitoring of the First and Newer Generations of Antiepileptic Drugs (AEDs) | New Methods Used in Pharmacokinetics and Therapeutic Monitoring of the First and Newer Generations of Antiepileptic Drugs (AEDs) Abstract Abstract The review presents data from the last few years on bioanalytical methods used in therapeutic drug monitoring (TDM) of the 1st–3rd generation and the newest antiepileptic dr... |
PMC9879086 | core_pubmed_pmc | Comparison of pharmacokinetics and bioavailability of bedaquiline fumarate, benzoate and maleate in dogs | Comparison of pharmacokinetics and bioavailability of bedaquiline fumarate, benzoate and maleate in dogs Abstract BACKGROUND: Bedaquiline (BDQ) as a fumarate salt is indicated as part of a regimen to treat multidrug-resistant TB (MDR-TB). BDQ benzoate and maleate have been identified as promising alternatives that will... |
PMC8916222 | core_pubmed_pmc | Selective Serotonin Reuptake Inhibitor Pharmacokinetics During Pregnancy: Clinical and Research Implications | Selective Serotonin Reuptake Inhibitor Pharmacokinetics During Pregnancy: Clinical and Research Implications Abstract Abstract Pregnancy and associated physiologic changes affect the pharmacokinetics of many medications, including selective serotonin reuptake inhibitors—the first-line pharmacologic interventions for de... |
PMC4900566 | core_pubmed_pmc | Pharmacokinetic-Pharmacodynamic Analysis on Inflammation Rat Model after Oral Administration of Huang Lian Jie Du Decoction | Pharmacokinetic-Pharmacodynamic Analysis on Inflammation Rat Model after Oral Administration of Huang Lian Jie Du Decoction Abstract Huang-Lian-Jie-Du Decoction (HLJDD) is a classical Traditional Chinese Medicine (TCM) formula with heat-dissipating and detoxifying effects. It is used to treat inflammation-associated di... |
PMC4279609 | core_pubmed_pmc | Effect of severe renal impairment on umeclidinium and umeclidinium/vilanterol pharmacokinetics and safety: a single-blind, nonrandomized study | Effect of severe renal impairment on umeclidinium and umeclidinium/vilanterol pharmacokinetics and safety: a single-blind, nonrandomized study Abstract Abstract Background Umeclidinium and vilanterol, long-acting bronchodilators for the treatment of chronic obstructive pulmonary disease, are primarily eliminated via th... |
PMC9535610 | core_pubmed_pmc | Kinetics and minimal inhibitory concentrations of ceftiofur in tear film following extended-release parenteral administration (Excede ® ) in dogs | Kinetics and minimal inhibitory concentrations of ceftiofur in tear film following extended-release parenteral administration (Excede ® ) in dogs Abstract Purpose Describe the pharmacokinetics of extended-release parenteral ceftiofur (Excede ® ) in canine tear film and compare these concentrations to minimal inhibitory... |
PMC11476076 | core_pubmed_pmc | Comprehensive biomarker and modeling approach to support dose finding for BI 836880, a VEGF/Ang-2 inhibitor | Comprehensive biomarker and modeling approach to support dose finding for BI 836880, a VEGF/Ang-2 inhibitor Abstract Abstract Background BI 836880 is a humanized bispecific nanobody® that binds to and blocks vascular endothelial growth factor (VEGF) and angiopoietin-2 (Ang-2). A comprehensive biomarker and modeling app... |
PMC9945928 | core_pubmed_pmc | Changing Epidemiology of Carbapenemases Among Carbapenem-Resistant Enterobacterales From United States Hospitals and the Activity of Aztreonam-Avibactam Against Contemporary Enterobacterales (2019–2021) | Changing Epidemiology of Carbapenemases Among Carbapenem-Resistant Enterobacterales From United States Hospitals and the Activity of Aztreonam-Avibactam Against Contemporary Enterobacterales (2019–2021) Abstract Abstract Background As the frequency of metallo-β-lactamase (MBL)-producing Enterobacterales is increasing w... |
PMC4823324 | core_pubmed_pmc | Lisdexamfetamine Dimesylate: Prodrug Delivery, Amphetamine Exposure and Duration of Efficacy | Lisdexamfetamine Dimesylate: Prodrug Delivery, Amphetamine Exposure and Duration of Efficacy Abstract Abstract Lisdexamfetamine dimesylate (LDX) is a long-acting d -amphetamine prodrug used to treat attention-deficit/hyperactivity disorder (ADHD) in children, adolescents and adults. LDX is hydrolysed in the blood to yi... |
PMC4354395 | core_pubmed_pmc | A phase 1 randomized study evaluating the effect of omeprazole on the pharmacokinetics of a novel 5-hydroxytryptamine receptor 4 agonist, revexepride (SSP-002358), in healthy adults | A phase 1 randomized study evaluating the effect of omeprazole on the pharmacokinetics of a novel 5-hydroxytryptamine receptor 4 agonist, revexepride (SSP-002358), in healthy adults Abstract Background About 30% of patients with gastroesophageal reflux disease continue to experience symptoms despite treatment with prot... |
PMC6150220 | core_pubmed_pmc | An Optimized and Sensitive Pharmacokinetic Quantitative Method of Investigating Gastrodin, Parishin, and Parishin B, C and E in Beagle Dog Plasma using LC-MS/MS after Intragastric Administration of Tall Gastrodia Capsules | An Optimized and Sensitive Pharmacokinetic Quantitative Method of Investigating Gastrodin, Parishin, and Parishin B, C and E in Beagle Dog Plasma using LC-MS/MS after Intragastric Administration of Tall Gastrodia Capsules Abstract Abstract Gastrodia elata Blume, called Tianma in China, has been widely used to treat hea... |
PMC11510411 | core_pubmed_pmc | Model-Informed Precision Dosing for Personalized Ustekinumab Treatment in Plaque Psoriasis | Model-Informed Precision Dosing for Personalized Ustekinumab Treatment in Plaque Psoriasis Abstract Abstract Background/Objectives: Implementing model-informed precision dosing (MIPD) strategies guided by population pharmacokinetic/pharmacodynamic (PK/PD) models could enhance the management of inflammatory diseases suc... |
PMC8324607 | core_pubmed_pmc | A Large-Scale Observational Study on the Temporal Trends and Risk Factors of Opioid Overdose: Real-World Evidence for Better Opioids | A Large-Scale Observational Study on the Temporal Trends and Risk Factors of Opioid Overdose: Real-World Evidence for Better Opioids Abstract Abstract Background The USA is in the midst of an opioid overdose epidemic. To address the epidemic, we conducted a large-scale population study on opioid overdose. Objectives Th... |
PMC9292718 | core_pubmed_pmc | Concentration‐QT modelling of the novel DHFR inhibitor P218 in healthy male volunteers | Concentration‐QT modelling of the novel DHFR inhibitor P218 in healthy male volunteers Abstract Aims Given the increasing emergence of drug resistance in Plasmodium , new antimalarials are urgently required. P218 is an aminopyridine that inhibits dihydrofolate reductase being developed as a malaria chemoprotective drug... |
PMC11906485 | core_pubmed_pmc | First‐In‐Human Safety, Tolerability, and Pharmacokinetics of PPI ‐1011, a Synthetic Plasmalogen Precursor | First‐In‐Human Safety, Tolerability, and Pharmacokinetics of PPI ‐1011, a Synthetic Plasmalogen Precursor Abstract ABSTRACT PPI‐1011 is a synthetic plasmalogen precursor designed to augment plasmalogen levels in patients with Rhizomelic chondrodysplasia punctata (RCDP), an ultra‐rare genetic disorder caused by a plasma... |
PMC11267949 | core_pubmed_pmc | Susceptibility evaluation and PK/PD integration of tulathromycin against Actinobacillus pleuropneumoniae during the mutant selection window | Susceptibility evaluation and PK/PD integration of tulathromycin against Actinobacillus pleuropneumoniae during the mutant selection window Abstract Introduction Actinobacillus pleuropneumoniae (APP) is a serious pathogen that affects the development of livestock breeding. Due to excessive use of antimicrobial drugs, m... |
PMC9652176 | core_pubmed_pmc | Semi-mechanistic Modeling of Hypoxanthine, Xanthine, and Uric Acid Metabolism in Asphyxiated Neonates | Semi-mechanistic Modeling of Hypoxanthine, Xanthine, and Uric Acid Metabolism in Asphyxiated Neonates Abstract Background and Objective Previously, we developed a pharmacokinetic-pharmacodynamic model of allopurinol, oxypurinol, and biomarkers, hypoxanthine, xanthine, and uric acid, in neonates with hypoxic-ischemic en... |
PMC12379775 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Subcutaneous RE104 | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Subcutaneous RE104 Abstract Abstract Background: This study is the first to formally evaluate in humans the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics of RE104, a prodrug of the synthetic psychedelic known as 4-hydroxy-N,N-diisopropy... |
PMC11276679 | core_pubmed_pmc | Mass Spectrometry Imaging Combined with Sparse Autoencoder Method Reveals Altered Phosphorylcholine Distribution in Imipramine Treated Wild-Type Mice Brains | Mass Spectrometry Imaging Combined with Sparse Autoencoder Method Reveals Altered Phosphorylcholine Distribution in Imipramine Treated Wild-Type Mice Brains Abstract Abstract Mass spectrometry imaging (MSI) is essential for visualizing drug distribution, metabolites, and significant biomolecules in pharmacokinetic stud... |
PMC12953422 | core_pubmed_pmc | Uncertainty undermines the validity of antimicrobial pharmacodynamics | Uncertainty undermines the validity of antimicrobial pharmacodynamics Abstract Abstract Antimicrobial therapy is informed by quantitative models of drug disposition and action. These models utilize experimental and observational evidence, subject to uncertainties, to support drug selection and dosage regimen optimizati... |
PMC11434936 | core_pubmed_pmc | Enhanced Antitumor Efficacy of Cytarabine and Idarubicin in Acute Myeloid Leukemia Using Liposomal Formulation: In Vitro and In Vivo Studies | Enhanced Antitumor Efficacy of Cytarabine and Idarubicin in Acute Myeloid Leukemia Using Liposomal Formulation: In Vitro and In Vivo Studies Abstract Abstract Background: Acute myeloid leukemia (AML) is the most common type of acute leukemia among adults with the recommend therapy of combination of cytarabine and idaru... |
PMC8099395 | core_pubmed_pmc | Population pharmacodynamic modeling of intramuscular and oral dexamethasone and betamethasone effects on six biomarkers with circadian complexities in Indian women | Population pharmacodynamic modeling of intramuscular and oral dexamethasone and betamethasone effects on six biomarkers with circadian complexities in Indian women Abstract Abstract Population pharmacokinetic/pharmacodynamic (PK/PD) analysis was performed for extensive data for differing dosage forms and routes for dex... |
PMC10912587 | core_pubmed_pmc | Ivacaftor pharmacokinetics and lymphatic transport after enteral administration in rats | Ivacaftor pharmacokinetics and lymphatic transport after enteral administration in rats Abstract Abstract Background: Ivacaftor is a modern drug used in the treatment of cystic fibrosis. It is highly lipophilic and exhibits a strong positive food effect. These characteristics can be potentially connected to a pronounce... |
PMC7073489 | core_pubmed_pmc | Pharmacokinetics after Periocular Methylprednisolone Sodium Succinate Injection in Rabbit Eyes | Pharmacokinetics after Periocular Methylprednisolone Sodium Succinate Injection in Rabbit Eyes Abstract The present study aimed to determine the pharmacokinetics and distribution of methylprednisolone sodium succinate (MPSS) and its metabolic product methylprednisolone (MP) in plasma and ocular tissues after periocular... |
PMC7385331 | core_pubmed_pmc | Volume of Distribution is Unaffected by Metabolic Drug–Drug Interactions | Volume of Distribution is Unaffected by Metabolic Drug–Drug Interactions Abstract Abstract Introduction It has been recognized that significant transporter interactions result in volume of distribution changes in addition to potential changes in clearance. For drugs that are not clinically significant transporter subst... |
PMC9208990 | core_pubmed_pmc | Synthesis and Characterization of Novel [2 + 1] Tricarbonyl Rhenium Complexes with the Hydrophilic Phosphine Ligands PTA and CAP | Synthesis and Characterization of Novel [2 + 1] Tricarbonyl Rhenium Complexes with the Hydrophilic Phosphine Ligands PTA and CAP Abstract Abstract In the pursuit of hydrophilic model fac -[Re(CO) 3 ] + complexes for (radio) pharmaceutical applications, six novel [2 + 1] mixed-ligand complexes of the general type fac -[... |
PMC8453865 | core_pubmed_pmc | Evaluation of the Effects of Repeat‐Dose Dabrafenib on the Single‐Dose Pharmacokinetics of Rosuvastatin (OATP1B1/1B3 Substrate) and Midazolam (CYP3A4 Substrate) | Evaluation of the Effects of Repeat‐Dose Dabrafenib on the Single‐Dose Pharmacokinetics of Rosuvastatin (OATP1B1/1B3 Substrate) and Midazolam (CYP3A4 Substrate) Abstract Abstract Dabrafenib is an oral BRAF kinase inhibitor approved for the treatment of various BRAF V600 mutation–positive solid tumors. In vitro observat... |
PMC8116701 | core_pubmed_pmc | Population Pharmacokinetic Model of Iohexol in Dogs to Estimate Glomerular Filtration Rate and Optimize Sampling Time | Population Pharmacokinetic Model of Iohexol in Dogs to Estimate Glomerular Filtration Rate and Optimize Sampling Time Abstract Abstract Monitoring iohexol plasma clearance is considered a useful, reliable, and sensitive tool to establish glomerular filtration rate (GFR) and early stages of kidney disease in both humans... |
PMC11802670 | core_pubmed_pmc | Comparison of Pharmacokinetics of Long-Acting Local Analgesics: CPL-01, a Novel Extended-Release Ropivacaine, Demonstrates Consistent and Predictable Exposure Compared with Liposomal Bupivacaine | Comparison of Pharmacokinetics of Long-Acting Local Analgesics: CPL-01, a Novel Extended-Release Ropivacaine, Demonstrates Consistent and Predictable Exposure Compared with Liposomal Bupivacaine Abstract Abstract Background and Objective There is a significant medical need for improved long-acting local anesthetics to ... |
PMC7423859 | core_pubmed_pmc | Acceptability of Long-Acting Injectable Cabotegravir (CAB LA) in HIV-Uninfected Individuals: HPTN 077 | Acceptability of Long-Acting Injectable Cabotegravir (CAB LA) in HIV-Uninfected Individuals: HPTN 077 Abstract Long-acting injectable PrEP could offer an alternative to daily oral PrEP, improve adherence and protection, if found acceptable, safe and effective. HPTN 077 evaluated injectable cabotegravir safety, tolerabi... |
PMC8880800 | core_pubmed_pmc | Overview of the Biological Activity of Anthraquinons and Flavanoids of the Plant Rumex Species | Overview of the Biological Activity of Anthraquinons and Flavanoids of the Plant Rumex Species Abstract Abstract Rumex confertus belongs to the genus Rumex and is classified as an invasive parasitic plant in agriculture. Despite other Rumex species being widely used in herbal medicine due to their antimicrobial, antiox... |
PMC3698101 | core_pubmed_pmc | Dynamic enhancement of drug product labels to support drug safety, efficacy, and effectiveness | Dynamic enhancement of drug product labels to support drug safety, efficacy, and effectiveness Abstract Abstract Out-of-date or incomplete drug product labeling information may increase the risk of otherwise preventable adverse drug events. In recognition of these concerns, the United States Federal Drug Administration... |
PMC3615533 | core_pubmed_pmc | The Future of Physiologically Based Pharmacokinetic Modeling to Predict Drug Exposure in Pregnant Women | The Future of Physiologically Based Pharmacokinetic Modeling to Predict Drug Exposure in Pregnant Women Modeling Increasing Interest in PBPK—Advantages of Bottom–Up Over Top–Down Compartmental Analysis Most of the early pharmacokinetic data in pregnant women have been obtained from small parallel studies. In recent yea... |
PMC11247108 | core_pubmed_pmc | Evaluating drug interaction potential from cytokine release syndrome using a physiologically based pharmacokinetic model: A case study of teclistamab | Evaluating drug interaction potential from cytokine release syndrome using a physiologically based pharmacokinetic model: A case study of teclistamab Abstract Abstract Cytokine release syndrome (CRS) was associated with teclistamab treatment in the phase I/II MajesTEC‐1 study. Cytokines, especially interleukin (IL)‐6, ... |
PMC7043261 | core_pubmed_pmc | Pharmacological characterization of a novel, potent, selective, and orally active fatty acid amide hydrolase inhibitor, PKM‐833 [( R )‐ N ‐(pyridazin‐3‐yl)‐4‐(7‐(trifluoromethyl)chroman‐4‐yl)piperazine‐1‐carboxamide] in rats: Potential for the treatment of inflammatory pain | Pharmacological characterization of a novel, potent, selective, and orally active fatty acid amide hydrolase inhibitor, PKM‐833 [( R )‐ N ‐(pyridazin‐3‐yl)‐4‐(7‐(trifluoromethyl)chroman‐4‐yl)piperazine‐1‐carboxamide] in rats: Potential for the treatment of inflammatory pain Abstract Abstract Recently, we identified a n... |
PMC4426132 | core_pubmed_pmc | Single- and multiple-dose pharmacokinetics of inhaled indacaterol in healthy Chinese volunteers | Single- and multiple-dose pharmacokinetics of inhaled indacaterol in healthy Chinese volunteers Abstract Indacaterol is an inhaled, ultra–long-acting β 2 -agonist that provides 24-h bronchodilation with once-daily dosing in patients with chronic obstructive pulmonary disorder. This study evaluated the pharmacokinetics,... |
PMC7353006 | core_pubmed_pmc | Mono-PEGylation of a Thermostable Arginine-Depleting Enzyme for the Treatment of Lung Cancer | Mono-PEGylation of a Thermostable Arginine-Depleting Enzyme for the Treatment of Lung Cancer Abstract L-arginine (L-Arg) depletion induced by randomly PEGylated arginine deiminase (ADI-PEG20) can treat arginosuccinate synthase (ASS)-negative cancers, and ADI-PEG20 is undergoing phase III clinical trials. Unfortunately,... |
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