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PMC4946738 | core_pubmed_pmc | Plasma pharmacokinetics of once-daily abacavir- and lamivudine-containing regimens and week 96 efficacy in HIV-infected Thai children | Plasma pharmacokinetics of once-daily abacavir- and lamivudine-containing regimens and week 96 efficacy in HIV-infected Thai children Abstract Abstract Background Abacavir and lamivudine are approved for once-daily use in HIV-infected adults. Limited pharmacokinetic (PK) data for abacavir and lamivudine in children are... |
PMC8160337 | core_pubmed_pmc | Effects of danofloxacin dosing regimen on gastrointestinal pharmacokinetics and fecal microbiome in steers | Effects of danofloxacin dosing regimen on gastrointestinal pharmacokinetics and fecal microbiome in steers Abstract Fluoroquinolones are a class of antimicrobial commonly used in human medicine, and deemed critical by the World Health Organization. Nonetheless, two formulations are approved for the treatment of respira... |
PMC6452870 | core_pubmed_pmc | Levodopa‐carbidopa intestinal gel high concentration formulation is clinically bioequivalent to commercial formulation | Levodopa‐carbidopa intestinal gel high concentration formulation is clinically bioequivalent to commercial formulation Abstract Abstract A new levodopa‐carbidopa intestinal gel ( LCIG ) system featuring a higher levodopa/carbidopa ( LD / CD ) concentration and viscosity, LCIG ‐ HV , is being developed to reduce the int... |
PMC12518061 | core_pubmed_pmc | Study on cerebrospinal fluid meropenem, vancomycin and tigecycline monitoring in patients with central nervous system infection following neurosurgery under different drug regimens | Study on cerebrospinal fluid meropenem, vancomycin and tigecycline monitoring in patients with central nervous system infection following neurosurgery under different drug regimens Abstract Abstract Introduction Central nervous system infection (CNSI) following neurosurgery is challenging to treat and carries a high ri... |
PMC8441053 | core_pubmed_pmc | Factors associated with fluoxetine and norfluoxetine plasma concentrations and clinical response in Mexican patients with mental disorders | Factors associated with fluoxetine and norfluoxetine plasma concentrations and clinical response in Mexican patients with mental disorders Abstract Abstract Over the last few years, fluoxetine has been one of the most prescribed medications for the treatment of diverse psychiatric conditions in Mexico. Fluoxetine thera... |
PMC12675599 | core_pubmed_pmc | Asiatic acid potentiates the activity of common antidepressant drugs in mice | Asiatic acid potentiates the activity of common antidepressant drugs in mice Abstract Rationale Conventional pharmacotherapy for depression faces numerous challenges, including side effects. Moreover, less than 50–70% of patients fully respond to treatment, and 20–30% experience recurrence. This has led to a growing in... |
PMC12937273 | core_pubmed_pmc | Saliva as an Alternative Matrix for Pharmacokinetic Research and Therapeutic Drug Monitoring of the Antituberculosis Drug Pyrazinamide | Saliva as an Alternative Matrix for Pharmacokinetic Research and Therapeutic Drug Monitoring of the Antituberculosis Drug Pyrazinamide Abstract Abstract Introduction : Plasma is the standard biological fluid used in pharmacokinetic (PK) studies and therapeutic drug monitoring (TDM) of pyrazinamide, a key antituberculos... |
PMC12505258 | core_pubmed_pmc | Development of a Universal In Vivo Predictive Dissolution Method for a Borderline BCS III/IV Drug Guided by Modeling and SimulationsAcyclovir as a Case Study | Development of a Universal In Vivo Predictive Dissolution Method for a Borderline BCS III/IV Drug Guided by Modeling and SimulationsAcyclovir as a Case Study Abstract Establishing in vivo predictive dissolution (IPD) conditions requires the consideration of biopredictive aspects during dissolution. For acyclovir, lowe... |
PMC10432868 | core_pubmed_pmc | Exposure‐response analysis for nivolumab plus ipilimumab combination therapy in patients with advanced hepatocellular carcinoma (CheckMate 040) | Exposure‐response analysis for nivolumab plus ipilimumab combination therapy in patients with advanced hepatocellular carcinoma (CheckMate 040) Abstract Abstract This analysis was conducted to inform dose selection of a combination of nivolumab plus ipilimumab for the treatment of sorafenib‐experienced patients with he... |
PMC6212487 | core_pubmed_pmc | The small molecule alpha-synuclein misfolding inhibitor, NPT200-11, produces multiple benefits in an animal model of Parkinson’s disease | The small molecule alpha-synuclein misfolding inhibitor, NPT200-11, produces multiple benefits in an animal model of Parkinson’s disease Abstract Accumulation of alpha-synuclein (ASYN) in neurons and other CNS cell types may contribute to the underlying pathology of synucleinopathies including Parkinson’s disease (PD),... |
PMC12721284 | core_pubmed_pmc | Comparative evaluation of ternary amorphous solid dispersions: Identifying optimal excipient systems for enhancing drug solubility | Comparative evaluation of ternary amorphous solid dispersions: Identifying optimal excipient systems for enhancing drug solubility Abstract The limited aqueous solubility of numerous active pharmaceutical ingredients (APIs) remains a major barrier to achieving optimal oral bioavailability, therapeutic efficacy, and cli... |
PMC11955020 | core_pubmed_pmc | Antiepileptic activity and potential mechanism of full-spectrum hemp extract | Antiepileptic activity and potential mechanism of full-spectrum hemp extract Abstract Abstract Epilepsy is the fourth most common neuropsychiatric disorder. Although the approval of Epidiolex has ignited hope for patients, there is still a large gap in the field of anti-seizure research. The effect and underlying mecha... |
PMC10784567 | core_pubmed_pmc | The HER2-directed antibody-drug conjugate DHES0815A in advanced and/or metastatic breast cancer: preclinical characterization and phase 1 trial results | The HER2-directed antibody-drug conjugate DHES0815A in advanced and/or metastatic breast cancer: preclinical characterization and phase 1 trial results Abstract Abstract Approved antibody-drug conjugates (ADCs) for HER2-positive breast cancer include trastuzumab emtansine and trastuzumab deruxtecan. To develop a differ... |
PMC7939532 | core_pubmed_pmc | Development of a ghrelin receptor inverse agonist for positron emission tomography | Development of a ghrelin receptor inverse agonist for positron emission tomography Abstract Abstract Imaging of Ghrelin receptors in vivo provides unique potential to gain deeper understanding on Ghrelin and its receptors in health and disease, in particular, in cancer. Ghrelin, an octanoylated 28-mer peptide hormone a... |
PMC3169777 | core_pubmed_pmc | Macitentan: entry-into-humans study with a new endothelin receptor antagonist | Macitentan: entry-into-humans study with a new endothelin receptor antagonist Abstract Abstract Purpose To study the pharmacokinetics, pharmacodynamics, and tolerability of rising single doses of macitentan, an endothelin receptor antagonist, in healthy male subjects. Methods This double-blind, placebo-controlled study... |
PMC7953729 | core_pubmed_pmc | Pre-clinical study of IRDye800CW-nimotuzumab formulation, stability, pharmacokinetics, and safety | Pre-clinical study of IRDye800CW-nimotuzumab formulation, stability, pharmacokinetics, and safety Abstract Abstract Background Epidermal growth factor receptor (EGFR) is a target for cancer therapy as it is overexpressed in a wide variety of cancers. Therapeutic antibodies that bind EGFR are being evaluated in clinical... |
PMC12403636 | core_pubmed_pmc | In vitro and in vivo evaluation of humanized monoclonal antibodies targeting pneumolysin | In vitro and in vivo evaluation of humanized monoclonal antibodies targeting pneumolysin Abstract ABSTRACT Streptococcus pneumoniae is a gram-positive bacterium that causes a variety of diseases, including otitis media, sinusitis, pneumonia, bacteremia, and meningitis. While pneumococcal conjugate vaccines have reduced... |
PMC10301570 | core_pubmed_pmc | Simultaneous Estimation of Quercetin and trans -Resveratrol in Cissus quadrangularis Extract in Rat Serum Using Validated LC-MS/MS Method: Application to Pharmacokinetic and Stability Studies | Simultaneous Estimation of Quercetin and trans -Resveratrol in Cissus quadrangularis Extract in Rat Serum Using Validated LC-MS/MS Method: Application to Pharmacokinetic and Stability Studies Abstract Abstract Cissus quadrangularis is a nutrient-rich plant with a history of use in traditional medicine. It boasts a dive... |
PMC9292215 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of FAAH Inhibitor BIA 10‐2474: A Double‐Blind, Randomized, Placebo‐Controlled Study in Healthy Volunteers | Safety, Tolerability, and Pharmacokinetics of FAAH Inhibitor BIA 10‐2474: A Double‐Blind, Randomized, Placebo‐Controlled Study in Healthy Volunteers Abstract Abstract This study evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of BIA 10‐2474, a fatty acid amide hydrolase (FAAH) inhibitor, afte... |
PMC11020404 | core_pubmed_pmc | Protective effect and pharmacokinetics of dihydromyricetin nanoparticles on oxidative damage of myocardium | Protective effect and pharmacokinetics of dihydromyricetin nanoparticles on oxidative damage of myocardium Abstract Purpose This study aims to investigate the protective mechanism of dihydromyricetin PLGA nanoparticles (DMY-PLGA NPs) against myocardial ischemia-reperfusion injury (MIRI) in vitro and the improvement of ... |
PMC6858297 | core_pubmed_pmc | A pharmacokinetic-pharmacodynamic assessment of oral antibiotics for pyelonephritis | A pharmacokinetic-pharmacodynamic assessment of oral antibiotics for pyelonephritis Abstract Abstract Antibiotic resistance to oral antibiotics recommended for pyelonephritis is increasing. The objective was to determine if there is a pharmacological basis to consider alternative treatments/novel dosing regimens for th... |
PMC5589124 | core_pubmed_pmc | Effects of sedation on subjective perception of pain intensity and autonomic nervous responses to pain: A preliminary study | Effects of sedation on subjective perception of pain intensity and autonomic nervous responses to pain: A preliminary study Abstract Rather than relying solely on subjective pain evaluation using means such as the visual analogue scale (VAS), in clinical situations it is possible to observe evoked responses of the auto... |
PMC9224877 | core_pubmed_pmc | What’s New in Intravenous Anaesthesia? New Hypnotics, New Models and New Applications | What’s New in Intravenous Anaesthesia? New Hypnotics, New Models and New Applications Abstract Abstract New anaesthetic drugs and new methods to administer anaesthetic drugs are continually becoming available, and the development of new PK-PD models furthers the possibilities of using arget controlled infusion (TCI) fo... |
PMC6535513 | core_pubmed_pmc | No Dose Adjustment for Isavuconazole Based on Age or Sex | No Dose Adjustment for Isavuconazole Based on Age or Sex Abstract This phase 1, open-label, single-dose, parallel-group study evaluated the pharmacokinetics (PK) of isavuconazole after a single oral dose of the prodrug isavuconazonium sulfate in healthy nonelderly (age, 18 to 45 years) and elderly (age, ≥65 years) male... |
PMC3398575 | core_pubmed_pmc | TB and HIV Therapeutics: Pharmacology Research Priorities | TB and HIV Therapeutics: Pharmacology Research Priorities Abstract Abstract An unprecedented number of investigational drugs are in the development pipeline for the treatment of tuberculosis. Among patients with tuberculosis, co-infection with HIV is common, and concurrent treatment of tuberculosis and HIV is now the s... |
PMC11599425 | core_pubmed_pmc | Trends of in vitro pharmacological potency and in vivo pharmacokinetics parameters of modern drugs: Can the therapeutic/subtherapeutic dose be estimated from in vitro K i and pharmacokinetic parameters? | Trends of in vitro pharmacological potency and in vivo pharmacokinetics parameters of modern drugs: Can the therapeutic/subtherapeutic dose be estimated from in vitro K i and pharmacokinetic parameters? Abstract Abstract In drug discovery and development, estimating therapeutic and subtherapeutic doses is crucial for d... |
PMC8942630 | core_pubmed_pmc | Combination Therapy with TCM Preparation Kumu Injection and Azithromycin against Bacterial Infection and Inflammation: In Vitro and In Vivo | Combination Therapy with TCM Preparation Kumu Injection and Azithromycin against Bacterial Infection and Inflammation: In Vitro and In Vivo Abstract Background Azithromycin (AZM) is one of the most common broad-spectrum antibiotics. However, drug resistance is increasing and combination therapy has attracted great atte... |
PMC7839558 | core_pubmed_pmc | Inter‐individual variability in atrasentan exposure partly explains variability in kidney protection and fluid retention responses: A post hoc analysis of the SONAR trial | Inter‐individual variability in atrasentan exposure partly explains variability in kidney protection and fluid retention responses: A post hoc analysis of the SONAR trial Abstract Abstract Aim To evaluate whether atrasentan plasma exposure explains between‐patient variability in urinary albumin‐to‐creatinine ratio (UAC... |
PMC12031654 | core_pubmed_pmc | Elucidation of Mechanism of Action in Drug Invention: Using Stable Isotope Tracers to Unravel Biochemical Kinetics | Elucidation of Mechanism of Action in Drug Invention: Using Stable Isotope Tracers to Unravel Biochemical Kinetics Abstract ABSTRACT The invention of a therapeutic begins by characterizing features that differentiate healthy versus diseased states; this often presents as changes in the concentration of an analyte. Exam... |
PMC8343923 | core_pubmed_pmc | Optimizing gentamicin dosing in different pediatric age groups using population pharmacokinetics and Monte Carlo simulation | Optimizing gentamicin dosing in different pediatric age groups using population pharmacokinetics and Monte Carlo simulation Abstract Abstract Introduction The use of once daily dosing of aminoglycosides in pediatrics is increasing but studies on dose optimization targeting the pediatric population are limited. This stu... |
PMC10999383 | core_pubmed_pmc | Pharmacokinetics of L-theanine and the effect on amino acid composition in mice administered with L-theanine | Pharmacokinetics of L-theanine and the effect on amino acid composition in mice administered with L-theanine Abstract L-theanine, an amino acid component of the tea leaves of Camellia sinensis , is sold in Japan as a supplement for good sleep. Although several studies in humans and mice have reported the effects of L-t... |
PMC5874785 | core_pubmed_pmc | Cytotoxicity Enhancement in Breast Cancer Cells with Carbonate Apatite-Facilitated Intracellular Delivery of Anti-Cancer Drugs | Cytotoxicity Enhancement in Breast Cancer Cells with Carbonate Apatite-Facilitated Intracellular Delivery of Anti-Cancer Drugs Abstract Pharmacotherapy as the mainstay in the management of breast cancer has demonstrated various drawbacks, including non-targeted bio distribution and narrow therapeutic and safety windows... |
PMC4718956 | core_pubmed_pmc | A phase I trial of ANG1/2-Tie2 inhibitor trebaninib (AMG386) and temsirolimus in advanced solid tumors (PJC008/NCI♯9041) | A phase I trial of ANG1/2-Tie2 inhibitor trebaninib (AMG386) and temsirolimus in advanced solid tumors (PJC008/NCI♯9041) Abstract Summary Background There is crosstalk between the ANG-Tie2 and the PI3K/Akt/mTOR pathways. Combined ANG1/2 and mTOR blockade may have additive anti-cancer activity. The combination of treban... |
PMC9030606 | core_pubmed_pmc | Theophylline: Old Drug in a New Light, Application in COVID-19 through Computational Studies | Theophylline: Old Drug in a New Light, Application in COVID-19 through Computational Studies Abstract Abstract Theophylline (3-methyxanthine) is a historically prominent drug used to treat respiratory diseases, alone or in combination with other drugs. The rapid onset of the COVID-19 pandemic urged the development of e... |
PMC8251589 | core_pubmed_pmc | Targeting of antithrombin in hemophilia A or B with investigational siRNA therapeutic fitusiran—Results of the phase 1 inhibitor cohort | Targeting of antithrombin in hemophilia A or B with investigational siRNA therapeutic fitusiran—Results of the phase 1 inhibitor cohort Abstract Abstract Background Fitusiran, an investigational small interfering RNA therapy, reduces antithrombin production to rebalance hemostasis in people with hemophilia A or B, with... |
PMC11204675 | core_pubmed_pmc | A Genome-Wide Association Study of Oxypurinol Concentrations in Patients Treated with Allopurinol | A Genome-Wide Association Study of Oxypurinol Concentrations in Patients Treated with Allopurinol Abstract Cohort studies have identified several genetic determinants that could predict the clinical response to allopurinol. However, they have not been commonly used for genome-wide investigations to identify genetic det... |
PMC12824526 | core_pubmed_pmc | Quantitative Prediction of Human Pharmacokinetics for Fc‐Engineered Therapeutic Monoclonal Antibodies With Increased FcRn Binding Mutations After Subcutaneous Injection | Quantitative Prediction of Human Pharmacokinetics for Fc‐Engineered Therapeutic Monoclonal Antibodies With Increased FcRn Binding Mutations After Subcutaneous Injection Abstract ABSTRACT Fc‐engineered antibodies (mAbs) enhancing FcRn binding have rapidly expanded in drug discovery and development. Although an approach ... |
PMC12446697 | core_pubmed_pmc | A Multi‐Scale Mechanistic Model of Ulcerative Colitis to Investigate the Effects of Selective Suppression of IL‐6 Trans‐Signaling | A Multi‐Scale Mechanistic Model of Ulcerative Colitis to Investigate the Effects of Selective Suppression of IL‐6 Trans‐Signaling Abstract ABSTRACT Interleukin 6 (IL‐6) has previously been identified as playing a role in ulcerative colitis (UC) by activating the signal‐transducing element gp130 through ligation of eith... |
PMC9700577 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics, and antitumour activity of oleclumab in Japanese patients with advanced solid malignancies: a phase I, open-label study | Safety, tolerability, pharmacokinetics, and antitumour activity of oleclumab in Japanese patients with advanced solid malignancies: a phase I, open-label study Abstract Background Cluster of differentiation (CD) 73-targeted immunotherapy and CD73 inhibition may reduce adenosine production, which can augment the host an... |
PMC8583409 | core_pubmed_pmc | Single-Shot Local Injection of Microfragmented Fat Tissue Loaded with Paclitaxel Induces Potent Growth Inhibition of Hepatocellular Carcinoma in Nude Mice | Single-Shot Local Injection of Microfragmented Fat Tissue Loaded with Paclitaxel Induces Potent Growth Inhibition of Hepatocellular Carcinoma in Nude Mice Abstract Simple Summary Therapeutic approaches to increase localization of chemotherapy at the tumor site, reducing systemic toxicity, are under deep investigation. ... |
PMC12420762 | core_pubmed_pmc | Impact of Extracorporeal Membrane Oxygenation Life Support on Vancomycin Population Pharmacokinetics in Critical Illness: A Systematic Review | Impact of Extracorporeal Membrane Oxygenation Life Support on Vancomycin Population Pharmacokinetics in Critical Illness: A Systematic Review Abstract Abstract Background An extracorporeal membrane oxygenation (ECMO) device represents an additional functional body compartment, potentially impacting vancomycin pharmacok... |
PMC10208276 | core_pubmed_pmc | A Very Long-acting Exatecan and Its Synergism with DNA Damage Response Inhibitors | A Very Long-acting Exatecan and Its Synergism with DNA Damage Response Inhibitors Abstract Exatecan (Exa) is a very potent inhibitor of topoisomerase I and anticancer agent. It has been intensively studied as a single agent, a large macromolecular conjugate and as the payload component of antigen-dependent antibody–dru... |
PMC8252455 | core_pubmed_pmc | Prediction of a clinically effective dose of THY1773, a novel V 1B receptor antagonist, based on preclinical data | Prediction of a clinically effective dose of THY1773, a novel V 1B receptor antagonist, based on preclinical data Abstract Abstract THY1773 is a novel arginine vasopressin 1B (V 1B ) receptor antagonist that is under development as an oral drug for the treatment of major depressive disorder (MDD). Here we report our st... |
PMC3086193 | core_pubmed_pmc | The pharmacokinetics of Iranian scorpion Odonthubuthus doriae venom and the available antivenom | The pharmacokinetics of Iranian scorpion Odonthubuthus doriae venom and the available antivenom Abstract In Iran intramuscular (IM) administration of antivenoms is used for the treatment of human scorpion envenoming of six medically dangerous scorpion species, including Odonthubuthus doriae (O. doriae ). The purpose of... |
PMC11678225 | core_pubmed_pmc | Advances in Canine Anesthesia: Physiologically Based Pharmacokinetic Modeling for Predicting Propofol Plasma Profiles in Canines with Hepatic Impairment | Advances in Canine Anesthesia: Physiologically Based Pharmacokinetic Modeling for Predicting Propofol Plasma Profiles in Canines with Hepatic Impairment Abstract Background : A PBPK model allows the prediction of the concentration of drug amounts in different tissues and organs over time and can be used to simulate and... |
PMC8177795 | core_pubmed_pmc | Safety and antitumor activity of acalabrutinib for relapsed/refractory B‐cell malignancies: A Japanese phase I study | Safety and antitumor activity of acalabrutinib for relapsed/refractory B‐cell malignancies: A Japanese phase I study Abstract This multicenter, open‐label, phase I study assessed the safety and antitumor activity of acalabrutinib in Japanese patients with relapsed/refractory (r/r) B‐cell malignancies. Parts 1 (dose con... |
PMC11935331 | core_pubmed_pmc | Development and validation of a population pharmacokinetic model to guide perioperative tacrolimus dosing after lung transplantation | Development and validation of a population pharmacokinetic model to guide perioperative tacrolimus dosing after lung transplantation Abstract Abstract Background Tacrolimus therapy is standard of care for immunosuppression after lung transplantation. However, tacrolimus exposure variability during the early postoperati... |
PMC12485565 | core_pubmed_pmc | Operationalizing a complex acute clinical trial: Lessons from the BEACH study | Operationalizing a complex acute clinical trial: Lessons from the BEACH study Abstract This report outlines the workflow, challenges, and key roles involved in operationalizing a complex, disruptive, acute clinical trial protocol requiring multidisciplinary collaboration. Yale University School of Medicine and the Neur... |
PMC10451962 | core_pubmed_pmc | Clinical Experience with Off-Label Intrathecal Administration of Selected Antibiotics in Adults: An Overview with Pharmacometric Considerations | Clinical Experience with Off-Label Intrathecal Administration of Selected Antibiotics in Adults: An Overview with Pharmacometric Considerations Abstract Drain-associated intracerebral infections are life-threatening emergencies. Their treatment is challenging due to the limited penetration of antibiotics to the site of... |
PMC3200335 | core_pubmed_pmc | Identification of Direct Target Engagement Biomarkers for Kinase-Targeted Therapeutics | Identification of Direct Target Engagement Biomarkers for Kinase-Targeted Therapeutics Abstract Pharmacodynamic (PD) biomarkers are an increasingly valuable tool for decision-making and prioritization of lead compounds during preclinical and clinical studies as they link drug-target inhibition in cells with biological ... |
PMC10213535 | core_pubmed_pmc | Nirmatrelvir/Ritonavir for hemodialysis patients with COVID-19 | Nirmatrelvir/Ritonavir for hemodialysis patients with COVID-19 Abstract Abstract Background: Hemodialysis patients have a high risk of severe/critical COVID-19 and related high mortality, but nirmatrelvir/ritonavir is not recommended for hemodialysis patients with COVID-19 infection because of lack of evidence of safet... |
PMC4875924 | core_pubmed_pmc | Population Pharmacokinetic Modelling of FE 999049, a Recombinant Human Follicle-Stimulating Hormone, in Healthy Women After Single Ascending Doses | Population Pharmacokinetic Modelling of FE 999049, a Recombinant Human Follicle-Stimulating Hormone, in Healthy Women After Single Ascending Doses Abstract Objective The purpose of this analysis was to develop a population pharmacokinetic model for a novel recombinant human follicle-stimulating hormone (FSH) (FE 999049... |
PMC11883060 | core_pubmed_pmc | In silico screening and molecular dynamics analysis of natural DHPS enzyme inhibitors targeting Acinetobacter baumannii | In silico screening and molecular dynamics analysis of natural DHPS enzyme inhibitors targeting Acinetobacter baumannii Abstract Abstract Over time, antimicrobial agents are losing their credibility in curbing infections due to the development of resistant pathogen strains. The resistant strains have proven to invade l... |
PMC12072273 | core_pubmed_pmc | Modifying Pharmacokinetic Properties of the Gram-Negative Bacteria Targeting Endolysin ML06 Without Affecting Antibacterial Activity | Modifying Pharmacokinetic Properties of the Gram-Negative Bacteria Targeting Endolysin ML06 Without Affecting Antibacterial Activity Abstract Abstract With the rise of antibiotic resistance, there is a need for innovative drugs with alternative mechanisms of action. Endolysins meet most of the requirements, but are lim... |
PMC8604247 | core_pubmed_pmc | Toward pharmacogenetic SLCO1B1 ‐guided dosing of methotrexate in arthritis using a murine Slco1b2 knockout model | Toward pharmacogenetic SLCO1B1 ‐guided dosing of methotrexate in arthritis using a murine Slco1b2 knockout model Abstract Abstract Low‐dose methotrexate (MTX) is a first‐line therapy for the treatment of arthritis. However, there is considerable interindividual variability in MTX exposure following standard dosing. Pol... |
PMC3130126 | core_pubmed_pmc | Pain Management in Patients with Cancer: Focus on Opioid Analgesics | Pain Management in Patients with Cancer: Focus on Opioid Analgesics Abstract Cancer pain is generally treated with pharmacological measures, relying on using opioids alone or in combination with adjuvant analgesics. Weak opioids are used for mild-to-moderate pain as monotherapy or in a combination with nonopioids. For ... |
PMC11807079 | core_pubmed_pmc | Reliability of in vitro data for the mechanistic prediction of brain extracellular fluid pharmacokinetics of P-glycoprotein substrates in vivo; are we scaling correctly? | Reliability of in vitro data for the mechanistic prediction of brain extracellular fluid pharmacokinetics of P-glycoprotein substrates in vivo; are we scaling correctly? Abstract Abstract Plasma pharmacokinetic (PK) profiles often do not resemble the PK within the central nervous system (CNS) because of blood–brain-bor... |
PMC4513223 | core_pubmed_pmc | Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection | Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection Abstract Abstract Background and Objectives Filgotinib (GLPG0634) is a selective inhibitor of Janus kinase 1 (JAK1) currently in development for the treatment of rhe... |
PMC12009784 | core_pubmed_pmc | Quantification of Methylene Blue and Evaluation of Its Pharmacokinetics in ICR Mice by Liquid Chromatography‐Quadrupole Time‐of‐Flight Mass Spectrometry Using Difluoroacetic Acid | Quantification of Methylene Blue and Evaluation of Its Pharmacokinetics in ICR Mice by Liquid Chromatography‐Quadrupole Time‐of‐Flight Mass Spectrometry Using Difluoroacetic Acid Abstract ABSTRACT Methylene blue (MB), a phenothiazine derivative, is currently under clinical trials for Alzheimer's disease ( ad ) due to i... |
PMC6720748 | core_pubmed_pmc | A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb ® Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects | A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb ® Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects Abstract Cannabidiol (CBD), a phytocannabinoid compound of Cannabis sativa , shows limited oral bioavailability due to its lipophilicity and extensive fi... |
PMC3753169 | core_pubmed_pmc | Options for treating postherpetic neuralgia in the medically complicated patient | Options for treating postherpetic neuralgia in the medically complicated patient Abstract Abstract Patients with postherpetic neuralgia (PHN) are often of advanced age or immunocompromised and likely to have ≥1 comorbid medical condition for which they receive ≥1 medication (polypharmacy). Comorbidities affecting renal... |
PMC10030409 | core_pubmed_pmc | Population Pharmacokinetics, Pharmacogenomics, and Adverse Events of Osimertinib and its Two Active Metabolites, AZ5104 and AZ7550, in Japanese Patients with Advanced Non-small Cell Lung Cancer: a Prospective Observational Study | Population Pharmacokinetics, Pharmacogenomics, and Adverse Events of Osimertinib and its Two Active Metabolites, AZ5104 and AZ7550, in Japanese Patients with Advanced Non-small Cell Lung Cancer: a Prospective Observational Study Abstract Abstract Background: Potential novel strategies for adverse event (AE) management ... |
PMC6153549 | core_pubmed_pmc | The concomitant use of lapatinib and paracetamol - the risk of interaction | The concomitant use of lapatinib and paracetamol - the risk of interaction Abstract Summary Lapatinib is a tyrosine kinase inhibitor used for the treatment of breast cancer. Paracetamol is an analgesic commonly applied to patients with mild or moderate pain and fever. Cancer patients are polymedicated, which involves h... |
PMC7456635 | core_pubmed_pmc | Inter-compound and Intra-compound Global Sensitivity Analysis of a Physiological Model for Pulmonary Absorption of Inhaled Compounds | Inter-compound and Intra-compound Global Sensitivity Analysis of a Physiological Model for Pulmonary Absorption of Inhaled Compounds Abstract Abstract In recent years, global sensitivity analysis (GSA) has gained interest in physiologically based pharmacokinetics (PBPK) modelling and simulation from pharmaceutical indu... |
PMC10068416 | core_pubmed_pmc | Population pharmacokinetics and CSF penetration of flucytosine in adults with HIV-associated cryptococcal meningoencephalitis | Population pharmacokinetics and CSF penetration of flucytosine in adults with HIV-associated cryptococcal meningoencephalitis Abstract Abstract Background There are limited data describing clinical flucytosine pharmacokinetics (PK). The variability of flucytosine partitioning into the CNS is not known. We described the... |
PMC4697853 | core_pubmed_pmc | A Pharmacokinetics-Neural Mass Model (PK-NMM) for the Simulation of EEG Activity during Propofol Anesthesia | A Pharmacokinetics-Neural Mass Model (PK-NMM) for the Simulation of EEG Activity during Propofol Anesthesia Abstract Modeling the effects of anesthetic drugs on brain activity is very helpful in understanding anesthesia mechanisms. The aim of this study was to set up a combined model to relate actual drug levels to EEG... |
PMC6187918 | core_pubmed_pmc | Dose-proportional pharmacokinetic properties of GLA5PR GLARS-NF1 controlled-release pregabalin in healthy Korean volunteers: a randomized, open, single-dose, parallel study | Dose-proportional pharmacokinetic properties of GLA5PR GLARS-NF1 controlled-release pregabalin in healthy Korean volunteers: a randomized, open, single-dose, parallel study Abstract Abstract Purpose The aim of this study was to evaluate the dose-proportional pharmacokinetic characteristics of pregabalin following the a... |
PMC6918846 | core_pubmed_pmc | Pharmacokinetics, Safety, and Intraocular Pressure-Lowering Profile of Omidenepag Isopropyl, a Selective, Nonprostaglandin, Prostanoid EP2 Receptor Agonist, in Healthy Japanese and Caucasian Volunteers (Phase I Study) | Pharmacokinetics, Safety, and Intraocular Pressure-Lowering Profile of Omidenepag Isopropyl, a Selective, Nonprostaglandin, Prostanoid EP2 Receptor Agonist, in Healthy Japanese and Caucasian Volunteers (Phase I Study) Abstract Abstract Purpose: Omidenepag isopropyl (OMDI) is a prodrug of OMD, a selective, nonprostaglan... |
PMC9056619 | core_pubmed_pmc | Characterization and targeting ability evaluation of cell-penetrating peptide LyP-1 modified alginate-based nanoparticles | Characterization and targeting ability evaluation of cell-penetrating peptide LyP-1 modified alginate-based nanoparticles Abstract Abstract Doxorubicin hydrochloride (DOX) shows a powerful treatment effect on breast cancer. However, for its indiscriminate distribution after systemic administration, the therapeutic resp... |
PMC12593346 | core_pubmed_pmc | Meta-Analysis and Machine Learning Prediction of Protein Corona Composition across Nanoparticle Systems in Biological Media | Meta-Analysis and Machine Learning Prediction of Protein Corona Composition across Nanoparticle Systems in Biological Media Abstract Abstract A comprehensive understanding of protein corona (PC) composition is critical for engineering nanoparticles (NPs) with optimal safety and therapeutic performance, because the PC g... |
PMC6859084 | core_pubmed_pmc | A Fixed-Dose Combination Of Gemigliptin And Rosuvastatin Exhibits Similar Pharmacokinetics, Pharmacodynamics, And Safety Compared To That Of A Loose Combination In Healthy Subjects | A Fixed-Dose Combination Of Gemigliptin And Rosuvastatin Exhibits Similar Pharmacokinetics, Pharmacodynamics, And Safety Compared To That Of A Loose Combination In Healthy Subjects Abstract Abstract Purpose Fixed-dose combination (FDC) of gemigliptin and rosuvastatin may improve medication compliance of patients with c... |
PMC7322544 | core_pubmed_pmc | Combining an in silico proarrhythmic risk assay with a tPKPD model to predict QTc interval prolongation in the anesthetized guinea pig assay | Combining an in silico proarrhythmic risk assay with a tPKPD model to predict QTc interval prolongation in the anesthetized guinea pig assay Abstract Abstract Human-based in silico models are emerging as important tools to study the effects of integrating inward and outward ion channel currents to predict clinical proa... |
PMC11975922 | core_pubmed_pmc | Multigenetic pharmacogenomics–guided treatment shows greater improvements on motor symptoms compared to usual therapy in Parkinson’s disease: a small real-word prospective cohort study | Multigenetic pharmacogenomics–guided treatment shows greater improvements on motor symptoms compared to usual therapy in Parkinson’s disease: a small real-word prospective cohort study Abstract Background Dopamine replacement therapy is a cornerstone of Parkinson’s disease treatment. In clinical practice, there is cons... |
PMC12521909 | core_pubmed_pmc | Camizestrant in Combination with Three Globally Approved CDK4/6 Inhibitors in Women with ER+, HER2− Advanced Breast Cancer: Results from SERENA-1 | Camizestrant in Combination with Three Globally Approved CDK4/6 Inhibitors in Women with ER+, HER2− Advanced Breast Cancer: Results from SERENA-1 Abstract Abstract Purpose: This trial investigated the safety and tolerability of camizestrant with cyclin-dependent kinase 4/6 inhibitors (CDK4/6i) in women with estrogen re... |
PMC10199234 | core_pubmed_pmc | Effect of a high‐fat and high‐calorie food on the pharmacokinetics of a novel, potent GABA analog HSK16149 in healthy subjects | Effect of a high‐fat and high‐calorie food on the pharmacokinetics of a novel, potent GABA analog HSK16149 in healthy subjects Abstract Abstract HSK16149 is a novel, potent gamma‐aminobutyric acid (GABA) analog for the treatment of neuropathic pain. The purpose of this study was to assess the effect of a high‐fat and h... |
PMC3523469 | core_pubmed_pmc | Phase I and pharmacokinetic study of dacomitinib (PF-00299804), an oral irreversible, small molecule inhibitor of human epidermal growth factor receptor-1, -2, and -4 tyrosine kinases, in Japanese patients with advanced solid tumors | Phase I and pharmacokinetic study of dacomitinib (PF-00299804), an oral irreversible, small molecule inhibitor of human epidermal growth factor receptor-1, -2, and -4 tyrosine kinases, in Japanese patients with advanced solid tumors Abstract Summary Background Dacomitinib (PF-00299804) is an oral, irreversible, small m... |
PMC9510668 | core_pubmed_pmc | Prediction for optimal dosage of pazopanib under various clinical situations using physiologically based pharmacokinetic modeling | Prediction for optimal dosage of pazopanib under various clinical situations using physiologically based pharmacokinetic modeling Abstract Abstract This study aimed to apply a physiologically based pharmacokinetic (PBPK) model to predict optimal dosing regimens of pazopanib (PAZ) for safe and effective administration w... |
PMC12821552 | core_pubmed_pmc | A Human Mass Balance and Metabolism Study of [ 14 C]‐Ubrogepant in Healthy Male Adults | A Human Mass Balance and Metabolism Study of [ 14 C]‐Ubrogepant in Healthy Male Adults Abstract Abstract Ubrogepant is a calcitonin gene–related peptide receptor antagonist approved for the acute treatment of migraine with or without aura in adults. The mass balance and metabolism of ubrogepant was evaluated in six hea... |
PMC9433621 | core_pubmed_pmc | Bioavailability of Oniria ® , a Melatonin Prolonged-Release Formulation, Versus Immediate-Release Melatonin in Healthy Volunteers | Bioavailability of Oniria ® , a Melatonin Prolonged-Release Formulation, Versus Immediate-Release Melatonin in Healthy Volunteers Abstract Background Melatonin is an endogenous substance which plays a key role in sleep induction by reducing sleep onset latency; it has been approved by the European Food Safety Authority... |
PMC6729057 | core_pubmed_pmc | Optimizing gentamicin conventional and extended interval dosing in neonates using Monte Carlo simulation – a retrospective study | Optimizing gentamicin conventional and extended interval dosing in neonates using Monte Carlo simulation – a retrospective study Abstract Abstract Background Although aminoglycosides are routinely used in neonates, controversy exists regarding empiric dosing regimens. The objectives were to determine gentamicin pharmac... |
PMC11207568 | core_pubmed_pmc | Development of neffy , an Epinephrine Nasal Spray, for Severe Allergic Reactions | Development of neffy , an Epinephrine Nasal Spray, for Severe Allergic Reactions Abstract Epinephrine autoinjectors (EAIs) are used for the treatment of severe allergic reactions in a community setting; however, their utility is limited by low prescription fulfillment rates, failure to carry, and failure to use due to ... |
PMC11652440 | core_pubmed_pmc | Pharmacokinetics and Bioequivalence of Two Powders of Azithromycin for Suspension: A Nonblinded, Single-Dose, Randomized, Three-Way Crossover Study in Fed and Fasting States Among Healthy Chinese Volunteers | Pharmacokinetics and Bioequivalence of Two Powders of Azithromycin for Suspension: A Nonblinded, Single-Dose, Randomized, Three-Way Crossover Study in Fed and Fasting States Among Healthy Chinese Volunteers Abstract Abstract Background and Objectives Azithromycin, a macrolide antibiotic, is commonly used to treat mild-... |
PMC5023393 | core_pubmed_pmc | Phase 1 Study of Intravenous Oncolytic Poxvirus (vvDD) in Patients With Advanced Solid Cancers | Phase 1 Study of Intravenous Oncolytic Poxvirus (vvDD) in Patients With Advanced Solid Cancers Abstract We have conducted a phase 1 study of intravenous vvDD, a Western Reserve strain oncolytic vaccinia virus, on 11 patients with standard treatment-refractory advanced colorectal or other solid cancers. The primary endp... |
PMC9022032 | core_pubmed_pmc | Heteroresistance Is Associated With in vitro Regrowth During Colistin Treatment in Carbapenem-Resistant Klebsiella pneumoniae | Heteroresistance Is Associated With in vitro Regrowth During Colistin Treatment in Carbapenem-Resistant Klebsiella pneumoniae Abstract Polymyxins including polymyxin B and colistin (polymyxin E) are considered the last resort for treating infections caused by carbapenem-resistant gram-negative bacteria. However, in vit... |
PMC5067610 | core_pubmed_pmc | High antiviral activity of NS 5A inhibitor ABT ‐530 with paritaprevir/ritonavir and ribavirin against hepatitis C virus genotype 3 infection | High antiviral activity of NS 5A inhibitor ABT ‐530 with paritaprevir/ritonavir and ribavirin against hepatitis C virus genotype 3 infection Abstract Abstract Background & Aims ABT ‐530 is a next‐generation hepatitis C virus ( HCV ) NS 5A inhibitor with potent pangenotypic antiviral activity in vitro . Paritaprevir is ... |
PMC4675771 | core_pubmed_pmc | Optimizing Polymyxin Combinations Against Resistant Gram-Negative Bacteria | Optimizing Polymyxin Combinations Against Resistant Gram-Negative Bacteria Abstract Abstract Polymyxin combination therapy is increasingly used clinically. However, systematic investigations of such combinations are a relatively recent phenomenon. The emerging pharmacodynamic (PD) and pharmacokinetic (PK) data on CMS/c... |
PMC12828710 | core_pubmed_pmc | Pharmacokinetic Interaction Between Isavuconazole and Rifabutin in a Real‐World Setting | Pharmacokinetic Interaction Between Isavuconazole and Rifabutin in a Real‐World Setting Abstract ABSTRACT Background Since rifabutin has less severe drug interactions, it is preferred over rifampin when administered concomitantly with azole antifungals. However, limited data exist to evaluate this interaction. Methods ... |
PMC10608783 | core_pubmed_pmc | Schnider and Eleveld Models for Propofol Target-Controlled Infusion Anesthesia: A Clinical Comparison | Schnider and Eleveld Models for Propofol Target-Controlled Infusion Anesthesia: A Clinical Comparison Abstract Abstract Background: Various pharmacokinetic/pharmacodynamic (PK/PD) models have been developed to accurately dose propofol administration during total intravenous anesthesia with target-controlled infusion (T... |
PMC5761003 | core_pubmed_pmc | A validated LC–MS/MS method for the determination of tolterodine and its metabolite in rat plasma and application to pharmacokinetic study | A validated LC–MS/MS method for the determination of tolterodine and its metabolite in rat plasma and application to pharmacokinetic study Abstract Liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was used for simultaneous quantification of tolterodine and its metabolite 5-hydroxy methyl tolterodine in ... |
PMC3430621 | core_pubmed_pmc | HPLC–MS/MS Analysis of a Traditional Chinese Medical Formulation of Bu-Yang-Huan-Wu-Tang and Its Pharmacokinetics after Oral Administration to Rats | HPLC–MS/MS Analysis of a Traditional Chinese Medical Formulation of Bu-Yang-Huan-Wu-Tang and Its Pharmacokinetics after Oral Administration to Rats Abstract Abstract Bu-yang-huan-wu-tang (BYHWT) is one of the most popular formulated traditional Chinese medicine prescriptions, and is widely for prevention of ischemic ca... |
PMC9449327 | core_pubmed_pmc | POD1UM-303/InterAACT 2: A phase III, global, randomized, double-blind study of retifanlimab or placebo plus carboplatin–paclitaxel in patients with locally advanced or metastatic squamous cell anal carcinoma | POD1UM-303/InterAACT 2: A phase III, global, randomized, double-blind study of retifanlimab or placebo plus carboplatin–paclitaxel in patients with locally advanced or metastatic squamous cell anal carcinoma Abstract Abstract Background Squamous carcinoma of the anal canal (SCAC) is a human papillomavirus (HPV)-driven ... |
PMC3419963 | core_pubmed_pmc | A phase I dose-escalation study of aflibercept administered in combination with pemetrexed and cisplatin in patients with advanced solid tumours | A phase I dose-escalation study of aflibercept administered in combination with pemetrexed and cisplatin in patients with advanced solid tumours Abstract Abstract Background: To evaluate the safety, pharmacokinetics (PKs), and pharmacodynamics of aflibercept, and to identify the recommended phase II dose (RP2D) of afli... |
PMC12785453 | core_pubmed_pmc | Oral Fluid Concentrations and Pharmacological Effects of Clephedrone and Methylone in Humans | Oral Fluid Concentrations and Pharmacological Effects of Clephedrone and Methylone in Humans Abstract Abstract Synthetic cathinones represent the second most frequently reported group of new psychoactive substances identified annually, according to the United Nations. It remains unknown whether specific derivatives dif... |
PMC4542448 | core_pubmed_pmc | Mechanism of Altered Metformin Distribution in Nonalcoholic Steatohepatitis | Mechanism of Altered Metformin Distribution in Nonalcoholic Steatohepatitis Abstract Abstract Metformin is an antihyperglycemic drug that is widely prescribed for type 2 diabetes mellitus and is currently being investigated for the treatment of nonalcoholic steatohepatitis (NASH). NASH is known to alter hepatic membran... |
PMC4580720 | core_pubmed_pmc | Direct Oral Anticoagulants for the Prevention of Stroke in Patients with Nonvalvular Atrial Fibrillation: Understanding Differences and Similarities | Direct Oral Anticoagulants for the Prevention of Stroke in Patients with Nonvalvular Atrial Fibrillation: Understanding Differences and Similarities Abstract The presence of atrial fibrillation (AF), the most common sustained cardiac arrhythmia, significantly increases the risk for stroke. Current guidelines recommend ... |
PMC11169648 | core_pubmed_pmc | Pharmacological studies and pharmacokinetic modelling to support the development of interventions targeting ecological reservoirs of Lyme disease | Pharmacological studies and pharmacokinetic modelling to support the development of interventions targeting ecological reservoirs of Lyme disease Abstract The development of interventions targeting reservoirs of Borrelia burgdorferi sensu stricto with acaricide to reduce the density of infected ticks faces numerous cha... |
PMC10100751 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Determination of Systemic MIC Breakpoints for Intermittent, Extended, and Continuous Infusion Dosage Regimens of Mecillinam | Pharmacokinetic/Pharmacodynamic Determination of Systemic MIC Breakpoints for Intermittent, Extended, and Continuous Infusion Dosage Regimens of Mecillinam Abstract ABSTRACT Intravenous mecillinam has been used for the treatment of urosepsis at several dosing regimens, including a dose of 1,000 mg three times a day (TI... |
PMC10495394 | core_pubmed_pmc | Adapting physiologically-based pharmacokinetic models for machine learning applications | Adapting physiologically-based pharmacokinetic models for machine learning applications Abstract Abstract Both machine learning and physiologically-based pharmacokinetic models are becoming essential components of the drug development process. Integrating the predictive capabilities of physiologically-based pharmacokin... |
PMC9907348 | core_pubmed_pmc | Defining the Intravital Renal Disposition of Fluorescence-Quenched Exenatide | Defining the Intravital Renal Disposition of Fluorescence-Quenched Exenatide Abstract Abstract Despite the understanding that renal clearance is pivotal for driving the pharmacokinetics of numerous therapeutic proteins and peptides, the specific processes that occur following glomerular filtration remain poorly defined... |
PMC7355632 | core_pubmed_pmc | A Mechanistic, Enantioselective, Physiologically Based Pharmacokinetic Model of Verapamil and Norverapamil, Built and Evaluated for Drug–Drug Interaction Studies | A Mechanistic, Enantioselective, Physiologically Based Pharmacokinetic Model of Verapamil and Norverapamil, Built and Evaluated for Drug–Drug Interaction Studies Abstract Abstract The calcium channel blocker and antiarrhythmic agent verapamil is recommended by the FDA for drug–drug interaction (DDI) studies as a modera... |
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