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PMC6222889 | core_pubmed_pmc | An Ultra-High Performance Liquid Chromatography with Tandem Mass Spectrometry Method for Determination of 10 Alkaloids in Beagle Dog Plasma after the Oral Administration of the Corydalis yanhusuo W.T. Wang Extract and Yuanhuzhitong Tablets | An Ultra-High Performance Liquid Chromatography with Tandem Mass Spectrometry Method for Determination of 10 Alkaloids in Beagle Dog Plasma after the Oral Administration of the Corydalis yanhusuo W.T. Wang Extract and Yuanhuzhitong Tablets Abstract Abstract This study has developed a sensitive and simple ultra-high per... |
PMC6147689 | core_pubmed_pmc | Comparison between prefilled syringe and autoinjector devices on patient-reported experiences and pharmacokinetics in galcanezumab studies | Comparison between prefilled syringe and autoinjector devices on patient-reported experiences and pharmacokinetics in galcanezumab studies Abstract Abstract Purpose The aim of this study was to compare the usability and patient-rated experiences of an autoinjector with a prefilled syringe in patients with migraine, who... |
PMC12243904 | core_pubmed_pmc | Tramadol overdose in total knee arthroplasty: A case report | Tramadol overdose in total knee arthroplasty: A case report Abstract BACKGROUND Tramadol is a synthetic opioid analgesic commonly employed in postoperative pain control due to its moderate efficacy and comparatively favorable safety profile. Nonetheless, overdose can result in significant adverse effects, notably centr... |
PMC12538123 | core_pubmed_pmc | Polygenic scores and antidepressant treatment outcomes in major depression: a critical integrative review | Polygenic scores and antidepressant treatment outcomes in major depression: a critical integrative review Abstract Abstract Major depressive disorder (MDD) shows a large heterogeneity in antidepressant treatment outcome, a variability explained in part by common-variant liability captured by polygenic scores (PGSs). We... |
PMC8970962 | core_pubmed_pmc | Comparative Pharmacokinetic Study of Three Major Bioactive Components in the Normal and Different Courses of Liver-Stagnation and Spleen-Deficiency Syndrome Depressive Rats after Intragastric Administration of Zhi-Zi-Hou-Po Decoction | Comparative Pharmacokinetic Study of Three Major Bioactive Components in the Normal and Different Courses of Liver-Stagnation and Spleen-Deficiency Syndrome Depressive Rats after Intragastric Administration of Zhi-Zi-Hou-Po Decoction Abstract To reveal the pharmacokinetic process of narirutin, naringin, and honokiol in... |
PMC10097767 | core_pubmed_pmc | Dose Rationale of Nasal Glucagon in Japanese Pediatric Patients with Diabetes Using Pharmacokinetic/Pharmacodynamic Modeling and Simulation | Dose Rationale of Nasal Glucagon in Japanese Pediatric Patients with Diabetes Using Pharmacokinetic/Pharmacodynamic Modeling and Simulation Abstract Abstract Background Nasal glucagon (NG) 3 mg is approved in Japan to treat hypoglycemia in pediatric patients with diabetes, but an NG clinical study has not been performe... |
PMC11154777 | core_pubmed_pmc | Phase 2 study of the efficacy and safety of ponsegromab in patients with cancer cachexia: PROACC‐1 study design | Phase 2 study of the efficacy and safety of ponsegromab in patients with cancer cachexia: PROACC‐1 study design Abstract Abstract Background Cancer cachexia is a multifactorial metabolic wasting syndrome characterized by anorexia, unintentional loss of weight involving both skeletal muscle and adipose tissues, progress... |
PMC5013402 | core_pubmed_pmc | Impact of symptomatic upper respiratory tract infections on insulin absorption and action of Technosphere inhaled insulin | Impact of symptomatic upper respiratory tract infections on insulin absorption and action of Technosphere inhaled insulin Abstract Objective Uncomplicated, acute upper respiratory tract infections (URTIs) occur in patients with diabetes at a similar frequency to the general population. This study ( NCT00642681 ) invest... |
PMC3271538 | core_pubmed_pmc | The peak bispectral index time cannot predict early phase propofol pharmacodynamics with effect site-controlled infusion algorithm | The peak bispectral index time cannot predict early phase propofol pharmacodynamics with effect site-controlled infusion algorithm Abstract Objectives: The plasma-effect site equilibration rate constant (ke0) of propofol was determined with peak bispectral index (BIS) time (T PEAK ) in our previous study. The present s... |
PMC4533485 | core_pubmed_pmc | A Multicenter Phase I/II Study of the BCNU Implant (Gliadel ® Wafer) for Japanese Patients with Malignant Gliomas | A Multicenter Phase I/II Study of the BCNU Implant (Gliadel ® Wafer) for Japanese Patients with Malignant Gliomas Abstract Abstract Carmustine (BCNU) implants (Gliadel ® Wafer, Eisai Inc., New Jersey, USA) for the treatment of malignant gliomas (MGs) were shown to enhance overall survival in comparison to placebo in co... |
PMC7811513 | core_pubmed_pmc | Cross-species analysis of hepatic cytochrome P450 and transport protein expression | Cross-species analysis of hepatic cytochrome P450 and transport protein expression Abstract Most drugs and xenobiotics are metabolized in the liver. Amongst others, different cytochrome P450 (CYP) enzymes catalyze the metabolic conversion of foreign compounds, and various transport proteins are engaged in the excretion... |
PMC8157589 | core_pubmed_pmc | Comparative Gene Signature of (−)-Oleocanthal Formulation Treatments in Heterogeneous Triple Negative Breast Tumor Models: Oncological Therapeutic Target Insights | Comparative Gene Signature of (−)-Oleocanthal Formulation Treatments in Heterogeneous Triple Negative Breast Tumor Models: Oncological Therapeutic Target Insights Abstract Abstract Triple negative breast cancer (TNBC) heterogeneity and limited therapeutic options confer its phenotypic aggressiveness. The discovery of a... |
PMC7785372 | core_pubmed_pmc | An UPLC-MS/MS Method for Determination of Osimertinib in Rat Plasma: Application to Investigating the Effect of Ginsenoside Rg3 on the Pharmacokinetics of Osimertinib | An UPLC-MS/MS Method for Determination of Osimertinib in Rat Plasma: Application to Investigating the Effect of Ginsenoside Rg3 on the Pharmacokinetics of Osimertinib Abstract Osimertinib is a novel oral, potent, and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) for treatment of adv... |
PMC6770293 | core_pubmed_pmc | Overview of the Anticancer Profile of Avenanthramides from Oat | Overview of the Anticancer Profile of Avenanthramides from Oat Abstract Abstract Cancer represents one of the leading causes of death worldwide. Progresses in treatment of cancer have continued at a rapid pace. However, undesirable side effects and drug resistance remain major challenges for therapeutic success. Natura... |
PMC10491600 | core_pubmed_pmc | Structural variation of the coding and non-coding human pharmacogenome | Structural variation of the coding and non-coding human pharmacogenome Abstract Genetic variants in drug targets and genes encoding factors involved in drug absorption, distribution, metabolism and excretion (ADME) can have pronounced impacts on drug pharmacokinetics, response, and toxicity. While the landscape of gene... |
PMC7364767 | core_pubmed_pmc | Evaluation of the Switch From Amiodarone to Dronedarone in Patients With Atrial Fibrillation: Results of the ARTEMIS AF Studies | Evaluation of the Switch From Amiodarone to Dronedarone in Patients With Atrial Fibrillation: Results of the ARTEMIS AF Studies Abstract Abstract Background: Switching between antiarrhythmic drugs is timed to minimize arrhythmia recurrence and adverse reactions. Dronedarone and amiodarone have similar electrophysiologi... |
PMC7813410 | core_pubmed_pmc | Intraperitoneal insulin administration in pigs: effect on circulating insulin and glucose levels | Intraperitoneal insulin administration in pigs: effect on circulating insulin and glucose levels Abstract Introduction The effect of intraperitoneal insulin infusion has limited evidence in the literature. Therefore, the aim of the study was to investigate the pharmacokinetics and pharmacodynamics of different intraper... |
PMC11745150 | core_pubmed_pmc | Red Yeast Rice or Lovastatin? A Comparative Evaluation of Safety and Efficacy Through a Multifaceted Approach | Red Yeast Rice or Lovastatin? A Comparative Evaluation of Safety and Efficacy Through a Multifaceted Approach Abstract ABSTRACT The increasing use of red yeast rice (RYR) as a natural supplement to manage blood cholesterol levels is driven by its active compound, monacolin K (MK), which is chemically identical to the s... |
PMC3766776 | core_pubmed_pmc | The determinants of propofol induction time in anesthesia | The determinants of propofol induction time in anesthesia Abstract Background The required dose of anesthetics is generally smaller in patients with low cardiac output (CO). A high CO decreases the blood concentration of anesthetics during induction and maintenance of anesthesia. However, a high CO may also shorten the... |
PMC8009217 | core_pubmed_pmc | Effects of the combination of second-generation antipsychotics on serum concentrations of aripiprazole and dehydroaripiprazole in Chinese patients with schizophrenia | Effects of the combination of second-generation antipsychotics on serum concentrations of aripiprazole and dehydroaripiprazole in Chinese patients with schizophrenia Abstract Background Aripiprazole (ARI) is often prescribed alone or in combination with other second-generation antipsychotics (SGAs) to treat patients wi... |
PMC7927832 | core_pubmed_pmc | Population Pharmacokinetic Properties of Antituberculosis Drugs in Vietnamese Children with Tuberculous Meningitis | Population Pharmacokinetic Properties of Antituberculosis Drugs in Vietnamese Children with Tuberculous Meningitis Abstract Optimal dosing of children with tuberculous meningitis (TBM) remains uncertain and is currently based on the treatment of pulmonary tuberculosis in adults. This study aimed to investigate the popu... |
PMC12458661 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of inhaled molgramostim in healthy people | Pharmacokinetics and pharmacodynamics of inhaled molgramostim in healthy people Abstract Abstract Background Inhaled molgramostim, a form of recombinant human granulocyte–macrophage colony stimulating factor (GM-CSF), is a promising investigational pharmacotherapy for autoimmune pulmonary alveolar proteinosis (aPAP); h... |
PMC11200783 | core_pubmed_pmc | Meropenem/Vaborbactam—A Mechanistic Review for Insight into Future Development of Combinational Therapies | Meropenem/Vaborbactam—A Mechanistic Review for Insight into Future Development of Combinational Therapies Abstract Abstract Beta-lactam antibiotics have been a major climacteric in medicine for being the first bactericidal compound available for clinical use. They have continually been prescribed since their developmen... |
PMC10916370 | core_pubmed_pmc | Limitations of antifungal prophylaxis in preventing invasive Candida surgical site infections after liver transplant surgery | Limitations of antifungal prophylaxis in preventing invasive Candida surgical site infections after liver transplant surgery Abstract ABSTRACT Invasive primary Candida surgical site infections (IP-SSIs) are a common complication of liver transplantation, and targeted antifungal prophylaxis is an efficient strategy to l... |
PMC7691413 | core_pubmed_pmc | Population Pharmacokinetic Model of Plasma and Cellular Mycophenolic Acid in Kidney Transplant Patients from the CIMTRE Study | Population Pharmacokinetic Model of Plasma and Cellular Mycophenolic Acid in Kidney Transplant Patients from the CIMTRE Study Abstract Background and Objective Mycophenolate mofetil is widely used in kidney transplant recipients. Mycophenolate mofetil is hydrolysed by blood esterases to mycophenolic acid (MPA), the act... |
PMC9643401 | core_pubmed_pmc | Pharmacokinetics and efficacy of topical inserts containing tenofovir alafenamide fumarate and elvitegravir administered rectally in macaques | Pharmacokinetics and efficacy of topical inserts containing tenofovir alafenamide fumarate and elvitegravir administered rectally in macaques Abstract Summary Background Topical on-demand forms for HIV pre-exposure prophylaxis (PrEP) may be a desirable alternative for people that prefer not to use daily PrEP. CONRAD ha... |
PMC6437518 | core_pubmed_pmc | DSM265 at 400 Milligrams Clears Asexual Stage Parasites but Not Mature Gametocytes from the Blood of Healthy Subjects Experimentally Infected with Plasmodium falciparum | DSM265 at 400 Milligrams Clears Asexual Stage Parasites but Not Mature Gametocytes from the Blood of Healthy Subjects Experimentally Infected with Plasmodium falciparum Abstract DSM265 is a novel antimalarial drug in clinical development that acts as a selective inhibitor of Plasmodium dihydroorotate dehydrogenase. In ... |
PMC8415261 | core_pubmed_pmc | Case Report: Low Hematocrit Leading to Tacrolimus Toxicity | Case Report: Low Hematocrit Leading to Tacrolimus Toxicity Abstract Abstract Tacrolimus is a calcineurin inhibitor characterized by a narrow therapeutic index and high intra- and inter-individual pharmacokinetic variability. Therapeutic drug monitoring in whole-blood is the standard monitoring procedure. However, tacro... |
PMC9065877 | core_pubmed_pmc | Safety, tolerability and pharmacokinetics of the oligomer modulator anle138b with exposure levels sufficient for therapeutic efficacy in a murine Parkinson model: A randomised, double-blind, placebo-controlled phase 1a trial | Safety, tolerability and pharmacokinetics of the oligomer modulator anle138b with exposure levels sufficient for therapeutic efficacy in a murine Parkinson model: A randomised, double-blind, placebo-controlled phase 1a trial Abstract Summary Background Synucleinopathies such as Parkinson ´s disease (PD), Dementia with ... |
PMC10386916 | core_pubmed_pmc | A Randomized Open-Label Study of Relugolix Alone or Relugolix Combination Therapy in Premenopausal Women | A Randomized Open-Label Study of Relugolix Alone or Relugolix Combination Therapy in Premenopausal Women Abstract Background and Objective Relugolix is a gonadotropin-releasing hormone receptor antagonist. Relugolix 40-mg monotherapy is associated with vasomotor symptoms and long-term bone mineral density loss due to h... |
PMC6522587 | core_pubmed_pmc | A Retrospective Analysis of Probability of Target Attainment in Community-Acquired Pneumonia: Ceftaroline Fosamil Versus Comparators | A Retrospective Analysis of Probability of Target Attainment in Community-Acquired Pneumonia: Ceftaroline Fosamil Versus Comparators Abstract Introduction This retrospective analysis compares the probability of target attainment (PTA) for ceftriaxone, levofloxacin and ceftaroline fosamil against Staphylococcus aureus ,... |
PMC4825616 | core_pubmed_pmc | Rapid Quantitative Pharmacodynamic Imaging with Bayesian Estimation | Rapid Quantitative Pharmacodynamic Imaging with Bayesian Estimation Abstract We recently described rapid quantitative pharmacodynamic imaging, a novel method for estimating sensitivity of a biological system to a drug. We tested its accuracy in simulated biological signals with varying receptor sensitivity and varying ... |
PMC8304466 | core_pubmed_pmc | Simplified and Rapid Determination of Primaquine and 5,6-Orthoquinone Primaquine by UHPLC-MS/MS: Its Application to a Pharmacokinetic Study | Simplified and Rapid Determination of Primaquine and 5,6-Orthoquinone Primaquine by UHPLC-MS/MS: Its Application to a Pharmacokinetic Study Abstract Abstract The method for the determination of primaquine (PQ) and 5,6-orthoquinone primaquine (5,6-PQ), the representative marker for PQ active metabolites, via CYP2D6 in h... |
PMC6099598 | core_pubmed_pmc | Upregulation of UDP-Glucuronosyltransferases 1a1 and 1a7 Are Involved in Altered Puerarin Pharmacokinetics in Type II Diabetic Rats | Upregulation of UDP-Glucuronosyltransferases 1a1 and 1a7 Are Involved in Altered Puerarin Pharmacokinetics in Type II Diabetic Rats Abstract Puerarin is an isoflavonoid extracted from Pueraria lobata roots, and displays a broad range of pharmacological activities, including antidiabetic activity. However, information a... |
PMC6402189 | core_pubmed_pmc | Single‐Dose and Multiple‐Dose Pharmacokinetics of Vaniprevir in Healthy Men | Single‐Dose and Multiple‐Dose Pharmacokinetics of Vaniprevir in Healthy Men Abstract Abstract Vaniprevir is an inhibitor of the hepatitis C virus (HCV) NS3/4A protease. The aim of these double‐blind, placebo‐controlled phase I studies was to evaluate the safety and pharmacokinetics of vaniprevir in healthy male volunte... |
PMC4556830 | core_pubmed_pmc | The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method | The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method Abstract Abstract MGCD0103, an isotype-selective histone deacetylase inhibitor (HDACi), has been clinically evaluated for the treatment of hematologic malignancies and advanced solid tumors, alone and in combination with standard-of-care agen... |
PMC7010620 | core_pubmed_pmc | Multi-scale modeling of drug binding kinetics to predict drug efficacy | Multi-scale modeling of drug binding kinetics to predict drug efficacy Abstract Abstract Optimizing drug therapies for any disease requires a solid understanding of pharmacokinetics (the drug concentration at a given time point in different body compartments) and pharmacodynamics (the effect a drug has at a given conce... |
PMC5762451 | core_pubmed_pmc | The pharmacokinetic study of rutin in rat plasma based on an electrochemically reduced graphene oxide modified sensor ☆ | The pharmacokinetic study of rutin in rat plasma based on an electrochemically reduced graphene oxide modified sensor ☆ Abstract Abstract An electrochemical method based on a directly electrochemically reduced graphene oxide (ERGO) film coated on a glassy carbon electrode (GCE) was developed for the rapid and convenien... |
PMC7187626 | core_pubmed_pmc | A Single-Dose Combination Study with the Experimental Antimalarials Artefenomel and DSM265 To Determine Safety and Antimalarial Activity against Blood-Stage Plasmodium falciparum in Healthy Volunteers | A Single-Dose Combination Study with the Experimental Antimalarials Artefenomel and DSM265 To Determine Safety and Antimalarial Activity against Blood-Stage Plasmodium falciparum in Healthy Volunteers Abstract Artefenomel and DSM265 are two new compounds that have been shown to be well tolerated and effective when admi... |
PMC5351339 | core_pubmed_pmc | Characterizing Class‐Specific Exposure‐Viral Load Suppression Response of HIV Antiretrovirals Using A Model‐Based Meta‐Analysis | Characterizing Class‐Specific Exposure‐Viral Load Suppression Response of HIV Antiretrovirals Using A Model‐Based Meta‐Analysis Abstract Abstract We applied model‐based meta‐analysis of viral suppression as a function of drug exposure and in vitro potency for short‐term monotherapy in human immunodeficiency virus type ... |
PMC10794428 | core_pubmed_pmc | A minimal PBPK model to accelerate preclinical development of drugs against tuberculosis | A minimal PBPK model to accelerate preclinical development of drugs against tuberculosis Abstract Abstract Introduction: Understanding drug exposure at disease target sites is pivotal to profiling new drug candidates in terms of tolerability and efficacy. Such quantification is particularly tedious for anti-tuberculosi... |
PMC4171595 | core_pubmed_pmc | Midazolam Pharmacokinetics in Morbidly Obese Patients Following Semi-Simultaneous Oral and Intravenous Administration: A Comparison with Healthy Volunteers | Midazolam Pharmacokinetics in Morbidly Obese Patients Following Semi-Simultaneous Oral and Intravenous Administration: A Comparison with Healthy Volunteers Abstract Abstract Background While in vitro and animal studies have shown reduced cytochrome P450 (CYP) 3A activity due to obesity, clinical studies in (morbidly) o... |
PMC9922681 | core_pubmed_pmc | Analytical approaches for determination of COVID-19 candidate drugs in human biological matrices | Analytical approaches for determination of COVID-19 candidate drugs in human biological matrices Abstract Abstract Since the outbreak of the COVID-19 pandemic, the use of antiviral and other available drugs has been considered to combat or reduce the clinical symptoms of patients. In this regard, it would be necessary ... |
PMC8550736 | core_pubmed_pmc | OptiDose: Computing the Individualized Optimal Drug Dosing Regimen Using Optimal Control | OptiDose: Computing the Individualized Optimal Drug Dosing Regimen Using Optimal Control Abstract Providing the optimal dosing strategy of a drug for an individual patient is an important task in pharmaceutical sciences and daily clinical application. We developed and validated an optimal dosing algorithm (OptiDose) th... |
PMC11632551 | core_pubmed_pmc | Impact of potential multiple drug-drug interactions on the adverse event profile of patients with hepatitis C treated with pangenotypic direct-acting antivirals in Spain | Impact of potential multiple drug-drug interactions on the adverse event profile of patients with hepatitis C treated with pangenotypic direct-acting antivirals in Spain Abstract Abstract Objectives: Direct-acting antivirals (DAAs) share pharmacokinetic pathways with many comedications commonly administered to patients... |
PMC7939511 | core_pubmed_pmc | Individualized Vancomycin Dosing with Therapeutic Drug Monitoring and Pharmacokinetic Consultation Service: A Large-Scale Retrospective Observational Study | Individualized Vancomycin Dosing with Therapeutic Drug Monitoring and Pharmacokinetic Consultation Service: A Large-Scale Retrospective Observational Study Abstract Abstract Background To date, outcome data with a large sample size and data regarding the clinical outcomes of pharmacokinetic-guided (PK) dosing of vancom... |
PMC12486805 | core_pubmed_pmc | Preclinical evaluation of tridecaptin M: in vitro and in vivo efficacy against colistin-resistant Gram-negative bacterial pathogens and pharmacokinetics | Preclinical evaluation of tridecaptin M: in vitro and in vivo efficacy against colistin-resistant Gram-negative bacterial pathogens and pharmacokinetics Abstract ABSTRACT The escalating threat of antimicrobial resistance (AMR), particularly among gram-negative pathogens, necessitates the development of novel therapeuti... |
PMC12402880 | core_pubmed_pmc | Bioequivalence of a Donepezil/Memantine 10/20 mg Fixed‐Dose Combination Versus Single‐Component Tablets in Healthy Korean Males | Bioequivalence of a Donepezil/Memantine 10/20 mg Fixed‐Dose Combination Versus Single‐Component Tablets in Healthy Korean Males Abstract Abstract A fixed‐dose combination (FDC) tablet formulation of donepezil/memantine (10/20 mg) was developed to improve medication compliance in patients with Alzheimer's disease (AD). ... |
PMC12872115 | core_pubmed_pmc | Stochastic Gates for Covariate Selection in Population Pharmacokinetics Modeling | Stochastic Gates for Covariate Selection in Population Pharmacokinetics Modeling Abstract ABSTRACT Covariate selection in population pharmacokinetics modeling is essential for understanding interindividual variability in drug response and optimizing dosing. Traditional stepwise covariate modeling is often time‐consumin... |
PMC7605398 | core_pubmed_pmc | Brigatinib Versus Crizotinib in Advanced ALK Inhibitor–Naive ALK-Positive Non–Small Cell Lung Cancer: Second Interim Analysis of the Phase III ALTA-1L Trial | Brigatinib Versus Crizotinib in Advanced ALK Inhibitor–Naive ALK-Positive Non–Small Cell Lung Cancer: Second Interim Analysis of the Phase III ALTA-1L Trial Abstract PURPOSE Brigatinib, a next-generation anaplastic lymphoma kinase (ALK) inhibitor, demonstrated superior progression-free survival (PFS) and improved healt... |
PMC11492913 | core_pubmed_pmc | Preliminary Study on Pharmacokinetics and Antitumor Pharmacodynamics of Folic Acid Modified Crebanine Polyethyleneglycol-Polylactic Acid Hydroxyacetic Acid Copolymer Nanoparticles | Preliminary Study on Pharmacokinetics and Antitumor Pharmacodynamics of Folic Acid Modified Crebanine Polyethyleneglycol-Polylactic Acid Hydroxyacetic Acid Copolymer Nanoparticles Abstract Abstract Purpose Liver cancer is associated significantly with morbidity and mortality. The combination of low-intensity ultrasound... |
PMC8960550 | core_pubmed_pmc | Adverse Reactions in a Phase 1 Trial of the Anti-Malarial DM1157: An Example of Pharmacokinetic Modeling and Simulation Guiding Clinical Trial Decisions | Adverse Reactions in a Phase 1 Trial of the Anti-Malarial DM1157: An Example of Pharmacokinetic Modeling and Simulation Guiding Clinical Trial Decisions Abstract Introduction There is an urgent need to develop new drugs to treat malaria due to increasing resistance to first-line therapeutics targeting the causative org... |
PMC8110997 | core_pubmed_pmc | Structural analogues in herbal medicine ginseng hit a shared target to achieve cumulative bioactivity | Structural analogues in herbal medicine ginseng hit a shared target to achieve cumulative bioactivity Abstract By a pilot trial on investigating immunomodulatory activity and target of ginsenosides, the major bioactive components of ginseng, here we report that structural analogues in herbal medicines hit a shared targ... |
PMC4695179 | core_pubmed_pmc | Suppression of Rituximab-resistant B-cell lymphoma with a novel multi-component anti-CD20 mAb nanocluster | Suppression of Rituximab-resistant B-cell lymphoma with a novel multi-component anti-CD20 mAb nanocluster Abstract Abstract Although the anti-CD20 antibody Rituximab has revolutionized the treatment of Non-Hodgkin Lymphoma (NHL), resistance to treatment still existed. Thus, strategies for suppressing Rituximab-resistan... |
PMC10748103 | core_pubmed_pmc | In Vitro Screening of Antimicrobial and Anti-Coagulant Activities, ADME Profiling, and Molecular Docking Study of Citrus limon L. and Citrus paradisi L. Cold-Pressed Volatile Oils | In Vitro Screening of Antimicrobial and Anti-Coagulant Activities, ADME Profiling, and Molecular Docking Study of Citrus limon L. and Citrus paradisi L. Cold-Pressed Volatile Oils Abstract Abstract Citrus , which belongs to the Rutaceae family, is a very widespread genus in the Mediterranean Basin. In Tunisia, various ... |
PMC8312709 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Models Are Effective Support for Pediatric Drug Development | Physiologically Based Pharmacokinetic Models Are Effective Support for Pediatric Drug Development Abstract Abstract Pediatric drug development faces many difficulties. Traditionally, pediatric drug doses are simply calculated linearly based on the body weight, age, and body surface area of adults. Due to the ontogeny o... |
PMC12790504 | core_pubmed_pmc | Can Alpha-Glucosidase Activity in Plasma or Leukocytes Serve as a Biomarker for Future Gene Therapy in Classic Infantile Pompe Disease? | Can Alpha-Glucosidase Activity in Plasma or Leukocytes Serve as a Biomarker for Future Gene Therapy in Classic Infantile Pompe Disease? Abstract We studied alpha-glucosidase activity in plasma and leukocytes after an infusion of 40 mg/kg of recombinant alglucosidase alpha in patients with classic infantile Pompe diseas... |
PMC5114325 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic study of doxorubicin in children with cancer: results of a “European Pediatric Oncology Off-patents Medicines Consortium” trial | Pharmacokinetic and pharmacodynamic study of doxorubicin in children with cancer: results of a “European Pediatric Oncology Off-patents Medicines Consortium” trial Abstract Abstract Purpose Doxorubicin is a key component in many pediatric oncology treatment regimens; still pharmacology data on which current dosing regi... |
PMC12135528 | core_pubmed_pmc | Determining an appropriate fosfomycin (ZTI-01) dosing regimen in pneumonia patients by utilizing minimal PBPK modeling and target attainment analysis | Determining an appropriate fosfomycin (ZTI-01) dosing regimen in pneumonia patients by utilizing minimal PBPK modeling and target attainment analysis Abstract ABSTRACT Fosfomycin, a broad-spectrum antibiotic used for uncomplicated cystitis, represents a potential promising candidate in combating resistant pneumonia. To... |
PMC8480901 | core_pubmed_pmc | Anti-inflammatory activity of lefamulin versus azithromycin and dexamethasone in vivo and in vitro in a lipopolysaccharide-induced lung neutrophilia mouse model | Anti-inflammatory activity of lefamulin versus azithromycin and dexamethasone in vivo and in vitro in a lipopolysaccharide-induced lung neutrophilia mouse model Abstract Abstract Several antibiotics demonstrate both antibacterial and anti-inflammatory/immunomodulatory activities and are used to treat inflammatory pulmo... |
PMC5525741 | core_pubmed_pmc | [ 177 Lu]pentixather: Comprehensive Preclinical Characterization of a First CXCR4-directed Endoradiotherapeutic Agent | [ 177 Lu]pentixather: Comprehensive Preclinical Characterization of a First CXCR4-directed Endoradiotherapeutic Agent Abstract Purpose: Based on the clinical relevance of the chemokine receptor 4 (CXCR4) as a molecular target in cancer and on the success of [ 68 Ga]pentixafor as an imaging probe for high-contrast visua... |
PMC8674255 | core_pubmed_pmc | Safety and tolerability of asunercept plus standard radiotherapy/temozolomide in Asian patients with newly-diagnosed glioblastoma: a phase I study | Safety and tolerability of asunercept plus standard radiotherapy/temozolomide in Asian patients with newly-diagnosed glioblastoma: a phase I study Abstract Asunercept (company code APG101 [Apogenix AG]; company code CAN008 [CANbridge Pharmaceuticals]) is a novel glycosylated fusion protein that has shown promising effe... |
PMC10281928 | core_pubmed_pmc | Invasive Mold Infections in Children: Navigating Troubled Waters with a Broken Compass | Invasive Mold Infections in Children: Navigating Troubled Waters with a Broken Compass Abstract Abstract Incidence of invasive mold infections in children, while rare, is increasing as the population of high-risk patients expands, including premature infants, pediatric patients undergoing treatment for hematological ma... |
PMC9605490 | core_pubmed_pmc | Opposite Response to Vitamin K Antagonists: A Report of Two Cases and Systematic Review of Literature | Opposite Response to Vitamin K Antagonists: A Report of Two Cases and Systematic Review of Literature Abstract Vitamin K antagonists (VKAs) are used in the prophylaxis and treatment of thromboembolic disorders. Despite a high efficacy, their narrow therapeutic window and high response variability hamper their managemen... |
PMC9942414 | core_pubmed_pmc | The Alzheimer’s disease-linked protease BACE1 modulates neuronal IL-6 signaling through shedding of the receptor gp130 | The Alzheimer’s disease-linked protease BACE1 modulates neuronal IL-6 signaling through shedding of the receptor gp130 Abstract Abstract Background The protease BACE1 is a major drug target for Alzheimer’s disease, but chronic BACE1 inhibition is associated with non-progressive cognitive worsening that may be caused by... |
PMC11878927 | core_pubmed_pmc | Identifying novel inhibitors against drug-resistant mutant CYP-51 Candida albicans : A computational study to combat fungal infections | Identifying novel inhibitors against drug-resistant mutant CYP-51 Candida albicans : A computational study to combat fungal infections Abstract Candida albicans (C. albicans) is an opportunistic pathogen in immunocompromised individuals and a normal inhabitant of the oral cavity, throat, gastrointestinal tract, and gen... |
PMC6544603 | core_pubmed_pmc | Towards a Generic Tool for Prediction of Meropenem Systemic and Infection-Site Exposure: A Physiologically Based Pharmacokinetic Model for Adult Patients with Pneumonia | Towards a Generic Tool for Prediction of Meropenem Systemic and Infection-Site Exposure: A Physiologically Based Pharmacokinetic Model for Adult Patients with Pneumonia Abstract Objective The objective of this study was to develop a physiologically based pharmacokinetic model for meropenem using a retrograde approach, ... |
PMC7099768 | core_pubmed_pmc | A positron emission tomography imaging study to confirm target engagement in the lungs of patients with idiopathic pulmonary fibrosis following a single dose of a novel inhaled αvβ6 integrin inhibitor | A positron emission tomography imaging study to confirm target engagement in the lungs of patients with idiopathic pulmonary fibrosis following a single dose of a novel inhaled αvβ6 integrin inhibitor Abstract Abstract Background Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive lung disease with poor progn... |
PMC12055767 | core_pubmed_pmc | Comprehensive characterisation of the active ingredients of Smilax glabra Roxb based on chemical fingerprinting, metabolic fingerprinting and pharmacodynamic fingerprinting | Comprehensive characterisation of the active ingredients of Smilax glabra Roxb based on chemical fingerprinting, metabolic fingerprinting and pharmacodynamic fingerprinting Abstract Background Smilax glabra Roxb (SGR) is a traditional Chinese medicine known for its medicinal and edible properties, with a long history o... |
PMC6780994 | core_pubmed_pmc | Evaluation and use of an anti‐cynomolgus monkey CD79b surrogate antibody–drug conjugate to enable clinical development of polatuzumab vedotin | Evaluation and use of an anti‐cynomolgus monkey CD79b surrogate antibody–drug conjugate to enable clinical development of polatuzumab vedotin Abstract Abstract Background and Purpose Polatuzumab vedotin is an antibody–drug conjugate (ADC) being developed for non‐Hodgkin's lymphoma. It contains a humanized anti‐CD79b Ig... |
PMC11243415 | core_pubmed_pmc | The Impact of Chemical Modifications on the Interferon-Inducing and Antiproliferative Activity of Short Double-Stranded Immunostimulating RNA | The Impact of Chemical Modifications on the Interferon-Inducing and Antiproliferative Activity of Short Double-Stranded Immunostimulating RNA Abstract Abstract A short 19 bp dsRNA with 3′-trinucleotide overhangs acting as immunostimulating RNA (isRNA) demonstrated strong antiproliferative action against cancer cells, i... |
PMC3946503 | core_pubmed_pmc | Impact of the Smoothened Inhibitor, IPI-926, on Smoothened Ciliary Localization and Hedgehog Pathway Activity | Impact of the Smoothened Inhibitor, IPI-926, on Smoothened Ciliary Localization and Hedgehog Pathway Activity Abstract Abstract A requisite step for canonical Hedgehog (Hh) pathway activation by Sonic Hedgehog (Shh) ligand is accumulation of Smoothened (Smo) to the primary cilium (PC). Activation of the Hh pathway has ... |
PMC4430595 | core_pubmed_pmc | Pharmacokinetics of intravenous telavancin in healthy subjects with varying degrees of renal impairment | Pharmacokinetics of intravenous telavancin in healthy subjects with varying degrees of renal impairment Abstract Purpose We evaluated the effect of renal impairment (RI) on the pharmacokinetics of telavancin and hydroxypropylbetadex (excipient in the telavancin drug product). Methods Adults with normal, mild, moderate ... |
PMC12699107 | core_pubmed_pmc | Volume kinetics of lactated Ringer's solution in adult horses | Volume kinetics of lactated Ringer's solution in adult horses Abstract Abstract Background Fluid therapy in horses is primarily empirical. Evidence‐based quantification of the disposition of intravenous (IV) crystalloids used in clinical practice could enhance the effectiveness of fluid therapy. Objectives To determine... |
PMC4156447 | core_pubmed_pmc | Slow clearance of Plasmodium vivax with chloroquine amongst children younger than six months of age in the Brazilian Amazon | Slow clearance of Plasmodium vivax with chloroquine amongst children younger than six months of age in the Brazilian Amazon Abstract Abstract Plasmodium vivax is the most widespread parasite causing malaria, being especially prevalent in the Americas and Southeast Asia. Children are one of the most affected populations... |
PMC3133529 | core_pubmed_pmc | Pharmacokinetics of ligustrazine ethosome patch in rats and anti-myocardial ischemia and anti-ischemic reperfusion injury effect | Pharmacokinetics of ligustrazine ethosome patch in rats and anti-myocardial ischemia and anti-ischemic reperfusion injury effect Abstract The objective of this study was to investigate the pharmacokinetics of the ligustrazine ethosome patch and antimyocardial ischemia and anti-ischemic reperfusion injury effect. Male S... |
PMC12406652 | core_pubmed_pmc | Safety and pharmacokinetics of single and multiple doses of ledaborbactam etzadroxil with or without ceftibuten in healthy volunteers | Safety and pharmacokinetics of single and multiple doses of ledaborbactam etzadroxil with or without ceftibuten in healthy volunteers Abstract ABSTRACT Ledaborbactam etzadroxil (LED-E), a novel oral prodrug that converts to the active β-lactamase inhibitor (BLI) ledaborbactam (LED), is being developed in combination wi... |
PMC6945443 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of repeated oral doses of 2-hydroxybenzylamine acetate in healthy volunteers: a double-blind, randomized, placebo-controlled clinical trial | Safety, tolerability, and pharmacokinetics of repeated oral doses of 2-hydroxybenzylamine acetate in healthy volunteers: a double-blind, randomized, placebo-controlled clinical trial Abstract Abstract Background 2-Hydroxybenzylamine (2-HOBA) is a selective dicarbonyl electrophile scavenger being developed as a nutritio... |
PMC5908290 | core_pubmed_pmc | Cisplatin liposome and 6-amino nicotinamide combination to overcome drug resistance in ovarian cancer cells | Cisplatin liposome and 6-amino nicotinamide combination to overcome drug resistance in ovarian cancer cells Abstract Ovarian cancer is an aggressive and lethal cancer usually treated by cytoreductive surgery followed by chemotherapy. Unfortunately, after an initial response, many patients relapse owing mainly to the de... |
PMC7600512 | core_pubmed_pmc | Kava as a Clinical Nutrient: Promises and Challenges | Kava as a Clinical Nutrient: Promises and Challenges Abstract Kava beverages are typically prepared from the root of Piper methysticum. They have been consumed among Pacific Islanders for centuries. Kava extract preparations were once used as herbal drugs to treat anxiety in Europe. Kava is also marketed as a dietary s... |
PMC8349217 | core_pubmed_pmc | LPS-Induced Inflammation Affects Midazolam Clearance in Juvenile Mice in an Age-Dependent Manner | LPS-Induced Inflammation Affects Midazolam Clearance in Juvenile Mice in an Age-Dependent Manner Abstract Purpose Inflammation has a significant impact on CYP3A activity. We hypothesized that this effect might be age dependent. Our objective was to conduct a population pharmacokinetic study of midazolam in mice at diff... |
PMC8778670 | core_pubmed_pmc | Identification of an Orally Bioavailable, Brain-Penetrant Compound with Selectivity for the Cannabinoid Type 2 Receptor | Identification of an Orally Bioavailable, Brain-Penetrant Compound with Selectivity for the Cannabinoid Type 2 Receptor Abstract Abstract Modulation of the endocannabinoid system (ECS) is of great interest for its therapeutic relevance in several pathophysiological processes. The CB2 subtype is largely localized to imm... |
PMC12794297 | core_pubmed_pmc | Impact of structure and formulation changes on the function of insulin products | Impact of structure and formulation changes on the function of insulin products Abstract Abstract Insulin has played an important role in the treatment of diabetes since its discovery in the early 1920s. Initially derived from animal sources, insulin production underwent significant changes with the advent of recombina... |
PMC2906415 | core_pubmed_pmc | The pharmacokinetic profile of a novel fixed-dose combination tablet of ibuprofen and paracetamol | The pharmacokinetic profile of a novel fixed-dose combination tablet of ibuprofen and paracetamol Abstract Abstract Background Ibuprofen and paracetamol differ in their mode of action and related therapeutic effects, suggesting that combined administration may offer improved analgesia. Reported here are the results of ... |
PMC9290518 | core_pubmed_pmc | Association Between Use of Pharmacokinetic‐Interacting Drugs and Effectiveness and Safety of Direct Acting Oral Anticoagulants: Nested Case‐Control Study | Association Between Use of Pharmacokinetic‐Interacting Drugs and Effectiveness and Safety of Direct Acting Oral Anticoagulants: Nested Case‐Control Study Abstract Concomitant use of direct oral anticoagulants (DOACs) and medications with inhibition/induction effect on P‐gp/CYP3A might increase risk of bleeding/treatmen... |
PMC11859385 | core_pubmed_pmc | Ustekinumab Drug Clearance Is Better Associated with Disease Control than Serum Trough Concentrations in a Prospective Cohort of Inflammatory Bowel Disease † | Ustekinumab Drug Clearance Is Better Associated with Disease Control than Serum Trough Concentrations in a Prospective Cohort of Inflammatory Bowel Disease † Abstract Background/Objectives : This study aimed to compare the association of ustekinumab (UST) drug clearance (CL) and trough drug concentrations with disease ... |
PMC9865105 | core_pubmed_pmc | A Mechanistic Pharmacodynamic Modeling Framework for the Assessment and Optimization of Proteolysis Targeting Chimeras (PROTACs) | A Mechanistic Pharmacodynamic Modeling Framework for the Assessment and Optimization of Proteolysis Targeting Chimeras (PROTACs) Abstract Abstract The field of targeted protein degradation is growing exponentially. Yet, there is an unmet need for pharmacokinetic/pharmacodynamic models that provide mechanistic insights,... |
PMC5762213 | core_pubmed_pmc | Simultaneous determination of four Sudan dyes in rat blood by UFLC–MS/MS and its application to a pharmacokinetic study in rats ☆ | Simultaneous determination of four Sudan dyes in rat blood by UFLC–MS/MS and its application to a pharmacokinetic study in rats ☆ Abstract Abstract A rapid and sensitive method based on ultrafast liquid chromatography–tandem mass spectrometry was developed and validated for simultaneous determination of Sudan I, Sudan ... |
PMC12064575 | core_pubmed_pmc | Variability in Meropenem Distribution and Clearance in Children with Sepsis: Population-Based Pharmacokinetics with Assessment of Renal Biomarkers | Variability in Meropenem Distribution and Clearance in Children with Sepsis: Population-Based Pharmacokinetics with Assessment of Renal Biomarkers Abstract Abstract Background and Objective Meropenem dosing to achieve therapeutic exposure in critically ill children with sepsis is challenging due to a spectrum of renal ... |
PMC8354861 | core_pubmed_pmc | Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2 | Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2 Abstract Abstract The nucleoside metabolite of remdesivir, GS-441524 displays potent anti-SARS-CoV-2 efficacy, and is being evaluated in clinical as an oral antiviral therapeutic for COVID-19. However, this nucleoside has a poor oral bioavailabili... |
PMC7256114 | core_pubmed_pmc | First‐in‐human clinical trial to assess the safety, tolerability and pharmacokinetics of P218, a novel candidate for malaria chemoprotection | First‐in‐human clinical trial to assess the safety, tolerability and pharmacokinetics of P218, a novel candidate for malaria chemoprotection Abstract Abstract Aims This first‐in‐human clinical trial of P218, a novel dihydrofolate reductase inhibitor antimalarial candidate, assessed safety, tolerability, pharmacokinetic... |
PMC9010279 | core_pubmed_pmc | The anti‐C5a antibody vilobelimab efficiently inhibits C5a in patients with severe COVID‐19 | The anti‐C5a antibody vilobelimab efficiently inhibits C5a in patients with severe COVID‐19 Abstract Abstract Recently, we reported the phase II portion of the adaptive phase II/III PANAMO trial exploring potential benefit and safety of selectively blocking C5a with the monoclonal antibody vilobelimab (IFX‐1) in patien... |
PMC12853142 | core_pubmed_pmc | Population Physiologically‐Based Pharmacokinetic Modeling to Determine Ontogeny: A Quantitative Clinical Pharmacology Example in Pediatric Rare Disease | Population Physiologically‐Based Pharmacokinetic Modeling to Determine Ontogeny: A Quantitative Clinical Pharmacology Example in Pediatric Rare Disease Abstract ABSTRACT Pediatric physiologically‐based pharmacokinetic (PBPK) modelling plays an increasing role in selecting doses in children and addressing clinical pharm... |
PMC11458656 | core_pubmed_pmc | Model-informed dose optimization of mycophenolic acid in pediatric kidney transplant patients | Model-informed dose optimization of mycophenolic acid in pediatric kidney transplant patients Abstract Purpose We aimed to develop and evaluate a population PK model of mycophenolic acid (MPA) in pediatric kidney transplant patients to aid MPA dose optimization. Methods Data were collected from pediatric kidney transpl... |
PMC7148462 | core_pubmed_pmc | Population Pharmacokinetic Modeling and Pharmacodynamic Target Attainment Simulation of Piperacillin/Tazobactam for Dosing Optimization in Late Elderly Patients with Pneumonia | Population Pharmacokinetic Modeling and Pharmacodynamic Target Attainment Simulation of Piperacillin/Tazobactam for Dosing Optimization in Late Elderly Patients with Pneumonia Abstract Abstract The aim of this study was to develop a population pharmacokinetic model for piperacillin (PIPC)/tazobactam (TAZ) in late elder... |
PMC7860071 | core_pubmed_pmc | Preclinical Pharmacokinetic Interaction and Histopathological Analyses of Hedyotis diffusa on Sorafenib in Rats | Preclinical Pharmacokinetic Interaction and Histopathological Analyses of Hedyotis diffusa on Sorafenib in Rats Abstract Abstract Sorafenib is one of the most effective target therapeutic agents for patients with late-stage hepatocellular carcinoma. To seek possible alternative adjuvant agents to enhance the efficacy a... |
PMC9283751 | core_pubmed_pmc | Pharmacokinetics of apixaban and tacrolimus or cyclosporine in kidney and lung transplant recipients | Pharmacokinetics of apixaban and tacrolimus or cyclosporine in kidney and lung transplant recipients Abstract Abstract Apixaban is frequently used off‐label in transplant recipients. However, a potential drug interaction exists with the calcineurin inhibitors. We conducted an open‐label drug–drug interaction study to d... |
PMC3356703 | core_pubmed_pmc | Update on a Pharmacokinetic-Centric Alternative Tier II Program for MMT—Part II: Physiologically Based Pharmacokinetic Modeling and Manganese Risk Assessment | Update on a Pharmacokinetic-Centric Alternative Tier II Program for MMT—Part II: Physiologically Based Pharmacokinetic Modeling and Manganese Risk Assessment Abstract Recently, a variety of physiologically based pharmacokinetic (PBPK) models have been developed for the essential element manganese. This paper reviews th... |
PMC5156571 | core_pubmed_pmc | Voriconazole Composited Polyvinyl Alcohol/Hydroxypropyl-β-Cyclodextrin Nanofibers for Ophthalmic Delivery | Voriconazole Composited Polyvinyl Alcohol/Hydroxypropyl-β-Cyclodextrin Nanofibers for Ophthalmic Delivery Abstract Abstract Voriconazole (VRC) incorporated in composited polyvinyl alcohol (PVA)/hydroxypropyl-β-cyclodextrin (HPβCD) blended nanofibers were produced via electrospinning for efficient ophthalmic delivery. T... |
PMC3230563 | core_pubmed_pmc | Oral fondaparinux: use of lipid nanocapsules as nanocarriers and in vivo pharmacokinetic study | Oral fondaparinux: use of lipid nanocapsules as nanocarriers and in vivo pharmacokinetic study Abstract Abstract Oral anticoagulant therapy could be advanced using lipid-based nanoparticulate systems. This study examined lipid nanocapsules for their oral absorption potential as the first step in developing oral fondapa... |
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