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PMC6954163
core_pubmed_pmc
Clinical pharmacokinetics of 3-h extended infusion of meropenem in adult patients with severe sepsis and septic shock: implications for empirical therapy against Gram-negative bacteria
Clinical pharmacokinetics of 3-h extended infusion of meropenem in adult patients with severe sepsis and septic shock: implications for empirical therapy against Gram-negative bacteria Abstract Background Optimal anti-bacterial activity of meropenem requires maintenance of its plasma concentration (Cp) above the minimu...
PMC12649812
core_pubmed_pmc
Optimizing Venlafaxine Therapy in Pregnancy: A Maternal–Fetal PBPK Modeling Approach
Optimizing Venlafaxine Therapy in Pregnancy: A Maternal–Fetal PBPK Modeling Approach Abstract Background Pregnancy-induced physiological changes can substantially alter venlafaxine pharmacokinetics. Despite the clinical relevance of both venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), no physiologi...
PMC11106153
core_pubmed_pmc
Biotransformation and toxicokinetics of 2-phenoxyethanol after oral exposure in humans: a volunteer study
Biotransformation and toxicokinetics of 2-phenoxyethanol after oral exposure in humans: a volunteer study Abstract 2-Phenoxyethanol (PhE) is an aromatic glycol ether and is used in a variety of functions and applications, e.g., as preservative in pharmaceuticals, cosmetic and personal care products, as biocide in disin...
PMC5080912
core_pubmed_pmc
Miscellaneous Topics in Computer-Aided Drug Design: Synthetic Accessibility and GPU Computing, and Other Topics
Miscellaneous Topics in Computer-Aided Drug Design: Synthetic Accessibility and GPU Computing, and Other Topics Abstract Abstract: Background Computer-aided drug design is still a state-of-the-art process in medicinal chemistry, and the main topics in this field have been extensively studied and well reviewed. These to...
PMC7027936
core_pubmed_pmc
SHP656, a polysialylated recombinant factor VIII (PSA‐rFVIII): First‐in‐human study evaluating safety, tolerability and pharmacokinetics in patients with severe haemophilia A
SHP656, a polysialylated recombinant factor VIII (PSA‐rFVIII): First‐in‐human study evaluating safety, tolerability and pharmacokinetics in patients with severe haemophilia A Abstract Abstract Introduction SHP656 is the first factor VIII (FVIII) product developed using polysialylation (PSA) technology, in which full‐le...
PMC6334903
core_pubmed_pmc
Short-course, oral flubendazole does not mediate significant efficacy against Onchocerca adult male worms or Brugia microfilariae in murine infection models
Short-course, oral flubendazole does not mediate significant efficacy against Onchocerca adult male worms or Brugia microfilariae in murine infection models Abstract Abstract The Onchocerca ochengi adult implant and Brugia malayi microfilariemic Severe-Combined Immunodeficient (SCID) mouse models are validated screens ...
PMC7379180
core_pubmed_pmc
Concizumab restores thrombin generation potential in patients with haemophilia: Pharmacokinetic/pharmacodynamic modelling results of concizumab phase 1/1b data
Concizumab restores thrombin generation potential in patients with haemophilia: Pharmacokinetic/pharmacodynamic modelling results of concizumab phase 1/1b data Abstract Abstract Introduction Concizumab enhances thrombin generation (TG) potential in haemophilia patients by inhibiting tissue factor pathway inhibitor (TFP...
PMC8028730
core_pubmed_pmc
Topical ophthalmic atropine in horses, pharmacokinetics and effect on intestinal motility
Topical ophthalmic atropine in horses, pharmacokinetics and effect on intestinal motility Abstract Background Topical ophthalmic atropine sulfate is an important part of the treatment protocol in equine uveitis. Frequent administration of topical atropine may cause decreased intestinal motility and colic in horses due ...
PMC11393195
core_pubmed_pmc
An Evidence-Based Rationale for Dose De-escalation of Subcutaneous Atezolizumab
An Evidence-Based Rationale for Dose De-escalation of Subcutaneous Atezolizumab Abstract Background Atezolizumab is a programmed death-ligand 1 (PD-L1) checkpoint inhibitor for the treatment of different forms of cancer. The subcutaneous formulation of atezolizumab has recently received approval. However, treatment wit...
PMC8084107
core_pubmed_pmc
Screening of cryptogamic secondary metabolites as putative inhibitors of SARS-CoV-2 main protease and ribosomal binding domain of spike glycoprotein by molecular docking and molecular dynamics approaches
Screening of cryptogamic secondary metabolites as putative inhibitors of SARS-CoV-2 main protease and ribosomal binding domain of spike glycoprotein by molecular docking and molecular dynamics approaches Abstract Abstract The unprecedented quick spreading of newly emerged SARS-CoV-2, the virus responsible for causing C...
PMC11768577
core_pubmed_pmc
Improving Individualized Salbutamol Treatment: A Population Pharmacokinetic Model for Oral Salbutamol in Virtual Patients
Improving Individualized Salbutamol Treatment: A Population Pharmacokinetic Model for Oral Salbutamol in Virtual Patients Abstract Abstract Background: Salbutamol, a short-acting β 2 -agonist used in asthma treatment, is available in multiple formulations, including inhalers, nebulizers, oral tablets, and intravenous, ...
PMC10150273
core_pubmed_pmc
The Pharmacokinetics/Pharmacodynamic Relationship of Durlobactam in Combination With Sulbactam in In Vitro and In Vivo Infection Model Systems Versus Acinetobacter baumannii-calcoaceticus Complex
The Pharmacokinetics/Pharmacodynamic Relationship of Durlobactam in Combination With Sulbactam in In Vitro and In Vivo Infection Model Systems Versus Acinetobacter baumannii-calcoaceticus Complex Abstract Abstract Sulbactam-durlobactam is a β-lactam/β-lactamase inhibitor combination currently in development for the tre...
PMC8082448
core_pubmed_pmc
High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy Subjects
High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy Subjects Abstract Purpose: Albendazole is a benzimidazole carbamate drug with anthelmintic and antiprotozoal activity against intestinal and tissue parasites. It has been described that the administra...
PMC3150493
core_pubmed_pmc
Determination of the Pharmacokinetics and Oral Bioavailability of Salicylamine, a Potent γ-Ketoaldehyde Scavenger, by LC/MS/MS
Determination of the Pharmacokinetics and Oral Bioavailability of Salicylamine, a Potent γ-Ketoaldehyde Scavenger, by LC/MS/MS Abstract Abstract Levels of reactive γ-ketoaldehydes derived from arachidonate increase in diseases associated with inflammation and oxidative injury. To assess the biological importance of the...
PMC11406518
core_pubmed_pmc
Intranasal Administration of Bedaquiline-Loaded Fucosylated Liposomes Provides Anti-Tubercular Activity while Reducing the Potential for Systemic Side Effects
Intranasal Administration of Bedaquiline-Loaded Fucosylated Liposomes Provides Anti-Tubercular Activity while Reducing the Potential for Systemic Side Effects Abstract Liposomal formulations of antibiotics for inhalation offer the potential for the delivery of high drug doses, controlled drug release kinetics in the lu...
PMC8071675
core_pubmed_pmc
Pharmacokinetics of Vancomycin in Pediatric Patients Receiving Intermittent Hemodialysis or Hemodiafiltration
Pharmacokinetics of Vancomycin in Pediatric Patients Receiving Intermittent Hemodialysis or Hemodiafiltration Abstract Abstract Introduction Vancomycin is a common antibiotic used to treat hemodialysis (HD) or hemodiafiltration (HDF)-related infections in pediatric patients, but optimal dosing remains unknown. This is ...
PMC12793993
core_pubmed_pmc
Remimazolam: a comprehensive review
Remimazolam: a comprehensive review Abstract Abstract Remimazolam is a novel, ultra-short-acting benzodiazepine that has emerged as a promising agent in modern anesthetic and intensive care practice. This review presents a detailed analysis of its pharmacokinetic and pharmacodynamic properties, clinical efficacy, and s...
PMC8635129
core_pubmed_pmc
Dose Optimization of Combined Linezolid and Fosfomycin against Enterococcus by Using an In Vitro Pharmacokinetic/Pharmacodynamic Model
Dose Optimization of Combined Linezolid and Fosfomycin against Enterococcus by Using an In Vitro Pharmacokinetic/Pharmacodynamic Model Abstract ABSTRACT The rapid spread of antibiotic resistance among Enterococcus has prompted considerable interest in determining the dosage regimen of linezolid combined with fosfomycin...
PMC3630197
core_pubmed_pmc
Pharmacokinetics and Interspecies Allometric Scaling of ST-246, an Oral Antiviral Therapeutic for Treatment of Orthopoxvirus Infection
Pharmacokinetics and Interspecies Allometric Scaling of ST-246, an Oral Antiviral Therapeutic for Treatment of Orthopoxvirus Infection Abstract Abstract Plasma pharmacokinetics of ST-246, smallpox therapeutic, was evaluated in mice, rabbits, monkeys and dogs following repeat oral administrations by gavage. The dog show...
PMC7032131
core_pubmed_pmc
Preparation of poly(lactide-co-glycolide) microspheres and evaluation of pharmacokinetics and tissue distribution of BDMC-PLGA-MS in rats
Preparation of poly(lactide-co-glycolide) microspheres and evaluation of pharmacokinetics and tissue distribution of BDMC-PLGA-MS in rats Abstract The aim of the present study was to develop a novel long-acting Poly (lactic-co-glycolic acid) (PLGA)-based microspheres formulation of Bisdemethoxycurcum (BDMC) by emulsion...
PMC10298604
core_pubmed_pmc
Peptides of a Feather: How Computation Is Taking Peptide Therapeutics under Its Wing
Peptides of a Feather: How Computation Is Taking Peptide Therapeutics under Its Wing Abstract Abstract Leveraging computation in the development of peptide therapeutics has garnered increasing recognition as a valuable tool to generate novel therapeutics for disease-related targets. To this end, computation has transfo...
PMC12925894
core_pubmed_pmc
Vasoactive drugs and the distribution of crystalloid fluid during acute sepsis
Vasoactive drugs and the distribution of crystalloid fluid during acute sepsis Abstract Abstract Background Crystalloid fluid is combined with vasoactive drugs when treating acute sepsis. We used kinetic analysis to compare the effects of vasoactive drugs on the hemodynamics and the volume kinetics of crystalloid fluid...
PMC12053634
core_pubmed_pmc
Mechanistic insights into synergistic effects using coupled PK-PD modeling
Mechanistic insights into synergistic effects using coupled PK-PD modeling Abstract Develop a novel coupled PK-PD model and apply it to quantitatively evaluate the synergistic effects of Hydroxysafflor Yellow A (HSYA) combined with Calycosin (CA) in the treatment of ischemic stroke. A total of 6 rats were modelled for ...
PMC7763445
core_pubmed_pmc
Finding the Dose for Ceftolozane-Tazobactam in Critically Ill Children with and without Acute Kidney Injury
Finding the Dose for Ceftolozane-Tazobactam in Critically Ill Children with and without Acute Kidney Injury Abstract Background: Ceftolozane-tazobactam is a new antibiotic against multidrug-resistant pathogens such as Pseudomonas aeruginosas . Ceftolozane-tazobactam dosage is still uncertain in children, especially in ...
PMC6440678
core_pubmed_pmc
PF ‐04447943, a Phosphodiesterase 9A Inhibitor, in Stable Sickle Cell Disease Patients: A Phase Ib Randomized, Placebo‐Controlled Study
PF ‐04447943, a Phosphodiesterase 9A Inhibitor, in Stable Sickle Cell Disease Patients: A Phase Ib Randomized, Placebo‐Controlled Study Abstract This phase Ib study randomized patients with stable sickle cell disease ( SCD ) aged 18–65 years to twice‐daily PF ‐04447943 (a phosphodiesterase 9A inhibitor; 5 or 25 mg) or ...
PMC12892940
core_pubmed_pmc
Development and evaluation of novel zein-based artemisinin sustained-release formulation for treating drug-resistant malaria
Development and evaluation of novel zein-based artemisinin sustained-release formulation for treating drug-resistant malaria Abstract ABSTRACT Artemisinin antimalarial drugs initially exhibited remarkable efficacy against Plasmodium falciparum . However, their poor solubility and low bioavailability necessitate high do...
PMC12539353
core_pubmed_pmc
Pharmacokinetics and Safety of Fospropofol Disodium for Injection in Subjects with Hepatic Impairment Compared with Healthy Matched Controls: A Prospective Cohort Study
Pharmacokinetics and Safety of Fospropofol Disodium for Injection in Subjects with Hepatic Impairment Compared with Healthy Matched Controls: A Prospective Cohort Study Abstract Abstract Purpose Fospropofol disodium for injection (Fospropofol FP ) is a new water-soluble propofol prodrug for procedural sedation and gene...
PMC4951511
core_pubmed_pmc
An Open-Label Investigation of the Pharmacokinetics and Tolerability of Oral Cysteamine in Adults with Cystic Fibrosis
An Open-Label Investigation of the Pharmacokinetics and Tolerability of Oral Cysteamine in Adults with Cystic Fibrosis Abstract Background and Objective Cysteamine is licensed for use in nephropathic cystinosis but preclinical data suggest a role in managing cystic fibrosis (CF). This study aimed to determine whether o...
PMC11302439
core_pubmed_pmc
Comparison of the Areas Under the Curve of Vancomycin Continuous vs. Intermittent Infusion in Critically Ill Pediatrics: A Randomized Clinical Trial
Comparison of the Areas Under the Curve of Vancomycin Continuous vs. Intermittent Infusion in Critically Ill Pediatrics: A Randomized Clinical Trial Abstract Abstract Background Providing data on the superior efficacy of vancomycin administered based on the area under the curve over 24 hours to the minimum inhibitory c...
PMC8613126
core_pubmed_pmc
Exposures of Phenylacetic Acid and Phenylacetylglutamine Across Different Subpopulations and Correlation with Adverse Events
Exposures of Phenylacetic Acid and Phenylacetylglutamine Across Different Subpopulations and Correlation with Adverse Events Abstract Background Elevated plasma ammonia is central to the pathogenesis of hepatic encephalopathy. Sodium phenylacetate or glycerol phenylbutyrate is approved for urea cycle disorders, but lim...
PMC12608633
core_pubmed_pmc
Coumarin Derivatives as Anticancer Agents: Mechanistic Landscape with an Emphasis on Breast Cancer
Coumarin Derivatives as Anticancer Agents: Mechanistic Landscape with an Emphasis on Breast Cancer Abstract Coumarin derivatives constitute a versatile small-molecule chemotype with broad anticancer potential. This narrative review synthesizes recent in vitro and in vivo evidence on coumarin-based scaffolds, emphasizin...
PMC5511594
core_pubmed_pmc
Pharmacokinetics of Daratumumab Following Intravenous Infusion in Relapsed or Refractory Multiple Myeloma After Prior Proteasome Inhibitor and Immunomodulatory Drug Treatment
Pharmacokinetics of Daratumumab Following Intravenous Infusion in Relapsed or Refractory Multiple Myeloma After Prior Proteasome Inhibitor and Immunomodulatory Drug Treatment Abstract Abstract Daratumumab is a CD38 monoclonal antibody recently approved for the treatment of multiple myeloma (MM). We report daratumumab p...
PMC6615282
core_pubmed_pmc
Population pharmacokinetics of intravenous sufentanil in critically ill patients supported with extracorporeal membrane oxygenation therapy
Population pharmacokinetics of intravenous sufentanil in critically ill patients supported with extracorporeal membrane oxygenation therapy Abstract Background Sufentanil is commonly used for analgesia and sedation during extracorporeal membrane oxygenation (ECMO). Both ECMO and the pathophysiological changes derived f...
PMC9284020
core_pubmed_pmc
The role of direct oral anticoagulants in the era of COVID-19: are antiviral therapy and pharmacogenetics limiting factors?
The role of direct oral anticoagulants in the era of COVID-19: are antiviral therapy and pharmacogenetics limiting factors? Abstract Abstract In patients with COVID-19, thromboinflammation is one of the main causes of morbidity and mortality, which makes anticoagulation an integral part of treatment. However, pharmacod...
PMC8743929
core_pubmed_pmc
Physicochemical Variation in Nanogold-Based Ayurved Medicine Suvarna Bhasma Produced by Various Manufacturers Lead to Different In Vivo Bioaccumulation Profiles
Physicochemical Variation in Nanogold-Based Ayurved Medicine Suvarna Bhasma Produced by Various Manufacturers Lead to Different In Vivo Bioaccumulation Profiles Abstract Abstract Suvarna Bhasma (SB) is a gold particle-based medicine that is used in Ayurved to treat tuberculosis, arthritis and nervous diseases. Traditio...
PMC11870343
core_pubmed_pmc
Molecular screening and dynamics simulation reveal potential phytocompounds in Swertia chirayita targeting the UspA1 protein of Moraxella catarrhalis for COPD therapy
Molecular screening and dynamics simulation reveal potential phytocompounds in Swertia chirayita targeting the UspA1 protein of Moraxella catarrhalis for COPD therapy Abstract Abstract Chronic obstructive pulmonary disease (COPD) is a global health burden, with Moraxella catarrhalis significantly contributing to acute ...
PMC7070898
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, Target Occupancy, and Concentration‐QT Analysis of the Novel BTK Inhibitor Evobrutinib in Healthy Volunteers
Safety, Tolerability, Pharmacokinetics, Target Occupancy, and Concentration‐QT Analysis of the Novel BTK Inhibitor Evobrutinib in Healthy Volunteers Abstract Bruton's tyrosine kinase (BTK) is a key regulator of B cell receptor and Fc receptor signaling, and a rational therapeutic target for autoimmune diseases. This fi...
PMC5638327
core_pubmed_pmc
Comparison of bioavailability and antiplatelet action of ticagrelor in patients with ST-elevation myocardial infarction and non-ST-elevation myocardial infarction: A prospective, observational, single-centre study
Comparison of bioavailability and antiplatelet action of ticagrelor in patients with ST-elevation myocardial infarction and non-ST-elevation myocardial infarction: A prospective, observational, single-centre study Abstract Background Data from available studies suggest that the presence of ST-elevation myocardial infar...
PMC11351853
core_pubmed_pmc
Comparison of gepant effects at therapeutic plasma concentrations: connecting pharmacodynamics and pharmacokinetics
Comparison of gepant effects at therapeutic plasma concentrations: connecting pharmacodynamics and pharmacokinetics Abstract Background Orally administered second-generation gepants are effective for the treatment of migraine. The intranasal administration of the third-generation gepant zavegepant might have additional...
PMC5696726
core_pubmed_pmc
Does anthracycline-based chemotherapy in pregnant women with cancer offer safe cardiac and neurodevelopmental outcomes for the developing fetus?
Does anthracycline-based chemotherapy in pregnant women with cancer offer safe cardiac and neurodevelopmental outcomes for the developing fetus? Abstract Background Cancer treatment during pregnancy is a growing problem especially now that women delay childbearing. Systemic treatment of these malignancies during pregna...
PMC5672142
core_pubmed_pmc
Real-Time qPCR as a Method for Detection of Antibody-Neutralized Phage Particles
Real-Time qPCR as a Method for Detection of Antibody-Neutralized Phage Particles Abstract Abstract The most common method for phage quantitation is the plaque assay, which relies on phage ability to infect bacteria. However, non-infective phage particles may preserve other biological properties; specifically, they may ...
PMC4714737
core_pubmed_pmc
Spotlight on ixazomib: potential in the treatment of multiple myeloma
Spotlight on ixazomib: potential in the treatment of multiple myeloma Abstract Abstract Despite the significant therapeutic advances achieved with proteasome inhibitors (PIs) such as bortezomib and carfilzomib in prolonging the survival of patients with multiple myeloma, the development of drug resistance, peripheral n...
PMC5469903
core_pubmed_pmc
Elucidation of Arctigenin Pharmacokinetics and Tissue Distribution after Intravenous, Oral, Hypodermic and Sublingual Administration in Rats and Beagle Dogs: Integration of In Vitro and In Vivo Findings
Elucidation of Arctigenin Pharmacokinetics and Tissue Distribution after Intravenous, Oral, Hypodermic and Sublingual Administration in Rats and Beagle Dogs: Integration of In Vitro and In Vivo Findings Abstract Although arctigenin ( AG ) has diverse bioactivities, such as anti-oxidant, anti-inflammatory, anti-cancer, ...
PMC10106214
core_pubmed_pmc
Effect and safety of anaprazole in the treatment of duodenal ulcers: a randomized, rabeprazole-controlled, phase III non-inferiority study
Effect and safety of anaprazole in the treatment of duodenal ulcers: a randomized, rabeprazole-controlled, phase III non-inferiority study Abstract Abstract Background: The pharmacokinetic and clinical behaviors of many proton pump inhibitors (PPIs) in peptic ulcer treatment are altered by CYP2C19 genetic polymorphisms...
PMC11739733
core_pubmed_pmc
Utility of Biomarker‐Informed Drug Interaction Evaluation in Drug Development and Regulatory Decision Making
Utility of Biomarker‐Informed Drug Interaction Evaluation in Drug Development and Regulatory Decision Making Abstract The measurement of endogenous biomarkers in plasma and urine before and after administration of an investigational drug in a clinical study may provide an early indication of its drug–drug interaction (...
PMC12629355
core_pubmed_pmc
Drug Design and Delivery for Intracellular Bacteria: Emerging Paradigms
Drug Design and Delivery for Intracellular Bacteria: Emerging Paradigms Abstract ABSTRACT Intracellular bacteria exploit host cell niches, such as lysosomes, phagosomes, cytosol, entire cells, and even erythrocytes, to evade immune clearance and escape conventional antibiotics. These environments pose numerous therapeu...
PMC9000957
core_pubmed_pmc
Effect of topical berberine in murine cutaneous leishmaniasis lesions
Effect of topical berberine in murine cutaneous leishmaniasis lesions Abstract Abstract Objectives More effective topical treatments remain an unmet need for the localized forms of cutaneous leishmaniasis (CL). The aim of this study was to evaluate the efficacy and safety of a topical berberine cream in BALB/c mice inf...
PMC8487273
core_pubmed_pmc
Subcutaneous dosing regimens of tocilizumab in children with systemic or polyarticular juvenile idiopathic arthritis
Subcutaneous dosing regimens of tocilizumab in children with systemic or polyarticular juvenile idiopathic arthritis Abstract Abstract Objectives To determine s.c. tocilizumab (s.c.-TCZ) dosing regimens for systemic JIA (sJIA) and polyarticular JIA (pJIA). Methods In two 52-week phase 1 b trials, s.c.-TCZ (162 mg/dose)...
PMC11253958
core_pubmed_pmc
GFR measurement in patients with CKD: Performance and feasibility of simplified iohexol plasma clearance techniques
GFR measurement in patients with CKD: Performance and feasibility of simplified iohexol plasma clearance techniques Abstract Implementing shortened one-compartment iohexol plasma clearance models for GFR measurement is crucial since the gold standard inulin renal clearance technique and the reference two-compartment, 1...
PMC12466873
core_pubmed_pmc
Temocillin: A Narrative Review of Its Clinical Reappraisal
Temocillin: A Narrative Review of Its Clinical Reappraisal Abstract Abstract Background: The emergence of multidrug-resistant Gram-negative bacteria, particularly extended-spectrum β-lactamase (ESBL) and AmpC-producing Enterobacterales , has brought renewed interest in temocillin, a narrow-spectrum β-lactam antibiotic ...
PMC8048692
core_pubmed_pmc
Model‐Based Selection and Recommendation for Subcutaneous Abatacept Dose in Patients With Polyarticular Juvenile Idiopathic Arthritis
Model‐Based Selection and Recommendation for Subcutaneous Abatacept Dose in Patients With Polyarticular Juvenile Idiopathic Arthritis Abstract Abstract The selective T‐cell costimulation modulator abatacept is approved for treatment of adult rheumatoid arthritis (RA) and polyarticular juvenile idiopathic arthritis (pJI...
PMC7493136
core_pubmed_pmc
Plasma, urine and tissue concentrations of Flunixin and Meloxicam in Pigs
Plasma, urine and tissue concentrations of Flunixin and Meloxicam in Pigs Abstract Abstract Background The objective of this study was to determine the renal clearance of flunixin and meloxicam in pigs and compare plasma and urine concentrations and tissue residues. Urine clearance is important for livestock show anima...
PMC11582470
core_pubmed_pmc
Inflammation and depression: A study protocol to dissect pathogenetic mechanisms in the onset, comorbidity and treatment response
Inflammation and depression: A study protocol to dissect pathogenetic mechanisms in the onset, comorbidity and treatment response Abstract Abstract About one third of patients suffering from Major Depressive Disorder (MDD) do not respond to any antidepressant medications and 75% experience relapses and general health d...
PMC12535457
core_pubmed_pmc
Pharmacological and molecular insights into linalool-rich Coriandrum sativum essential oil: Anticonvulsant, analgesic, anti-inflammatory, and antioxidant potential in rodent models
Pharmacological and molecular insights into linalool-rich Coriandrum sativum essential oil: Anticonvulsant, analgesic, anti-inflammatory, and antioxidant potential in rodent models Abstract ABSTRACT Background and Aim: Coriandrum sativum L. (coriander) has long been valued for its culinary and medicinal uses. C. sativu...
PMC5222901
core_pubmed_pmc
Effect of Age and Renal Function on Idarucizumab Pharmacokinetics and Idarucizumab-Mediated Reversal of Dabigatran Anticoagulant Activity in a Randomized, Double-Blind, Crossover Phase Ib Study
Effect of Age and Renal Function on Idarucizumab Pharmacokinetics and Idarucizumab-Mediated Reversal of Dabigatran Anticoagulant Activity in a Randomized, Double-Blind, Crossover Phase Ib Study Abstract Abstract Background and Objectives Idarucizumab is an antibody fragment that specifically reverses dabigatran-mediate...
PMC8747548
core_pubmed_pmc
Population Pharmacokinetics and Dosing Optimization of Gentamicin in Critically Ill Patients Undergoing Continuous Renal Replacement Therapy
Population Pharmacokinetics and Dosing Optimization of Gentamicin in Critically Ill Patients Undergoing Continuous Renal Replacement Therapy Abstract Abstract Purpose Appropriate gentamicin dosing in continuous renal replacement therapy (CRRT) patients remains undefined. This study aimed to develop a population pharmac...
PMC6039208
core_pubmed_pmc
Sorafenib Dose Recommendation in Acute Myeloid Leukemia Based on Exposure‐FLT3 Relationship
Sorafenib Dose Recommendation in Acute Myeloid Leukemia Based on Exposure‐FLT3 Relationship Abstract Abstract Sorafenib administered at the approved dose continuously is not tolerated long‐term in patients with acute myeloid leukemia (AML). The purpose of this study was to optimize the dosing regimen by characterizing ...
PMC9091774
core_pubmed_pmc
Impact of the amount of PEG on prodrug nanoassemblies for efficient cancer therapy
Impact of the amount of PEG on prodrug nanoassemblies for efficient cancer therapy Abstract PEGylation has been widely used to improve the pharmacokinetic properties of prodrug self-assembled nanoparticles (prodrug-SANPs). However, the impacts of the amount of PEG on the self-assemble stability, cellular uptake, pharma...
PMC10376323
core_pubmed_pmc
Oral Tetracycline-Class Drugs in Dermatology: Impact of Food Intake on Absorption and Efficacy
Oral Tetracycline-Class Drugs in Dermatology: Impact of Food Intake on Absorption and Efficacy Abstract Abstract Tetracycline-class drugs are frequently used in dermatology for their anti-inflammatory properties to treat skin diseases such as acne, rosacea, and hidradenitis suppurativa (HS). The American Academy of Der...
PMC6158900
core_pubmed_pmc
Characterization of drug responses of mini patient-derived xenografts in mice for predicting cancer patient clinical therapeutic response
Characterization of drug responses of mini patient-derived xenografts in mice for predicting cancer patient clinical therapeutic response Abstract Abstract Background Patient-derived organoids and xenografts (PDXs) have emerged as powerful models in functional diagnostics with high predictive power for anticancer drug ...
PMC6137118
core_pubmed_pmc
Primaquine Pharmacokinetics in Lactating Women and Breastfed Infant Exposures
Primaquine Pharmacokinetics in Lactating Women and Breastfed Infant Exposures Abstract Abstract Background Primaquine is the only drug providing radical cure of Plasmodium vivax malaria. It is not recommended for breastfeeding women as it causes hemolysis in glucose-6-phosphate dehydrogenase (G6PD)–deficient individual...
PMC9885872
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of Benralizumab: A Phase 1, Randomized, Single-Blind Study of Healthy Chinese Participants
Safety, Tolerability, and Pharmacokinetics of Benralizumab: A Phase 1, Randomized, Single-Blind Study of Healthy Chinese Participants Abstract Abstract Purpose Biological therapies targeting eosinophils have been shown to be effective in treating patients with severe eosinophilic asthma. Benralizumab (Fasenra ® , Astra...
PMC9842218
core_pubmed_pmc
Therapeutic target mapping from the genome of Kingella negevensis and biophysical inhibition assessment through PNP synthase binding with traditional medicinal compounds
Therapeutic target mapping from the genome of Kingella negevensis and biophysical inhibition assessment through PNP synthase binding with traditional medicinal compounds Abstract Abstract Kingella negevensis belongs to the Neisseriaceae family. It is implied that it has significant virulence potential due to RTX toxin ...
PMC5123727
core_pubmed_pmc
Pharmacokinetics and safety of DTS-108, a human oligopeptide bound to SN-38 with an esterase-sensitive cross-linker in patients with advanced malignancies: a Phase I study
Pharmacokinetics and safety of DTS-108, a human oligopeptide bound to SN-38 with an esterase-sensitive cross-linker in patients with advanced malignancies: a Phase I study Abstract Abstract Background DTS-108 is a hydrosoluble prodrug, where the SN-38 moiety is covalently linked to a 20-amino acid vector peptide by a s...
PMC7471499
core_pubmed_pmc
PK/PD modeling based on NO-ET homeostasis for improving management of sunitinib-induced hypertension in rats
PK/PD modeling based on NO-ET homeostasis for improving management of sunitinib-induced hypertension in rats Abstract Sunitinib is an oral small molecule multitargeted tyrosine kinase inhibitor, which is currently used to treat severe cancers. Clinical research has shown that patients treated with sunitinib develop hyp...
PMC8617734
core_pubmed_pmc
Thinking Quantitatively of RNA-Based Information Transfer via Extracellular Vesicles: Lessons to Learn for the Design of RNA-Loaded EVs
Thinking Quantitatively of RNA-Based Information Transfer via Extracellular Vesicles: Lessons to Learn for the Design of RNA-Loaded EVs Abstract Extracellular vesicles (EVs) are 50–1000 nm vesicles secreted by virtually any cell type in the body. They are expected to transfer information from one cell or tissue to anot...
PMC4954844
core_pubmed_pmc
Physiologically based modeling of lisofylline pharmacokinetics following intravenous administration in mice
Physiologically based modeling of lisofylline pharmacokinetics following intravenous administration in mice Abstract Lisofylline (LSF), is the R-(−) enantiomer of the metabolite M1 of pentoxifylline, and is currently under development for the treatment of type 1 diabetes. The aim of the study was to develop a physiolog...
PMC12689928
core_pubmed_pmc
Epigenetic control of antigen presentation failure in osteosarcoma: from single-cell chromatin maps to therapeutic strategies
Epigenetic control of antigen presentation failure in osteosarcoma: from single-cell chromatin maps to therapeutic strategies Abstract Abstract Osteosarcoma arises within heterogeneous tumor–immune ecosystems in which impaired antigen visibility—shaped by chromatin programs—limits immune surveillance and blunts respons...
PMC12925825
core_pubmed_pmc
Pharmacodynamics, Efficacy, and Safety of Intraputaminal Eladocagene Exuparvovec Administered to Pediatric Patients With Aromatic L‐Amino Acid Decarboxylase Deficiency Using an MR‐Compatible Cannula: 48 Weeks of Follow‐Up
Pharmacodynamics, Efficacy, and Safety of Intraputaminal Eladocagene Exuparvovec Administered to Pediatric Patients With Aromatic L‐Amino Acid Decarboxylase Deficiency Using an MR‐Compatible Cannula: 48 Weeks of Follow‐Up Abstract ABSTRACT Aromatic ʟ‐amino acid decarboxylase (AADC) deficiency is a rare pediatric neurot...
PMC7563483
core_pubmed_pmc
The Unique Pharmacometrics of Small Molecule Therapeutic Drug Tracer Imaging for Clinical Oncology
The Unique Pharmacometrics of Small Molecule Therapeutic Drug Tracer Imaging for Clinical Oncology Abstract Simple Summary New clinical radiology scans using trace amounts of therapeutic cancer drugs labeled with radioisotope injected into patients can provide oncologists with fundamentally unique insights about drug d...
PMC11845110
core_pubmed_pmc
Immunocapture LC–MS Methods for Pharmacokinetics of Large Molecule Drugs
Immunocapture LC–MS Methods for Pharmacokinetics of Large Molecule Drugs Abstract Implementation of immunocapture LC–MS methods to characterize the pharmacokinetic profile of large molecule drugs has become a widely used technique over the past decade. As the pharmaceutical industry strives for speediness into clinical...
PMC9283742
core_pubmed_pmc
Pharmacokinetics of asciminib in the presence of CYP3A or P‐gp inhibitors, CYP3A inducers, and acid‐reducing agents
Pharmacokinetics of asciminib in the presence of CYP3A or P‐gp inhibitors, CYP3A inducers, and acid‐reducing agents Abstract Abstract Asciminib is a first‐in‐class inhibitor of BCR::ABL1, specifically targeting the ABL myristoyl pocket. Asciminib is a substrate of CYP3A4 and P‐glycoprotein (P‐gp) and possesses pH‐depen...
PMC5773000
core_pubmed_pmc
Assessment of serum pharmacokinetics and urinary excretion of albendazole and its metabolites in human volunteers
Assessment of serum pharmacokinetics and urinary excretion of albendazole and its metabolites in human volunteers Abstract Background Soil Transmitted Helminth (STH) infections negatively impact physical and mental development in human populations. Current WHO guidelines recommend morbidity control of these infections ...
PMC9569954
core_pubmed_pmc
The Antidepressant-like Activity, Effects on Recognition Memory Deficits, Bioavailability, and Safety after Chronic Administration of New Dual-Acting Small Compounds Targeting Neuropsychiatric Symptoms in Dementia
The Antidepressant-like Activity, Effects on Recognition Memory Deficits, Bioavailability, and Safety after Chronic Administration of New Dual-Acting Small Compounds Targeting Neuropsychiatric Symptoms in Dementia Abstract This study aimed to extend the body of preclinical research on prototype dual-acting compounds co...
PMC5739117
core_pubmed_pmc
HX575: established biosimilarity in the treatment of renal anemia and 10 years of clinical experience
HX575: established biosimilarity in the treatment of renal anemia and 10 years of clinical experience Abstract Abstract Erythropoiesis-stimulating agents, such as recombinant human erythropoietin, are commonly used for the treatment of anemia in patients with chronic kidney disease (CKD). In 2007, HX575 (Binocrit ® ) b...
PMC11125587
core_pubmed_pmc
Therapeutic Drug Monitoring and Biomarkers; towards Better Dosing of Antimicrobial Therapy
Therapeutic Drug Monitoring and Biomarkers; towards Better Dosing of Antimicrobial Therapy Abstract Due to variability in pharmacokinetics and pharmacodynamics, clinical outcomes of antimicrobial drug therapy vary between patients. As such, personalised medication management, considering both pharmacokinetics and pharm...
PMC7284631
core_pubmed_pmc
Towards a Quantitative Mechanistic Understanding of Localized Pulmonary Tissue Retention—A Combined In Vivo/In Silico Approach Based on Four Model Drugs
Towards a Quantitative Mechanistic Understanding of Localized Pulmonary Tissue Retention—A Combined In Vivo/In Silico Approach Based on Four Model Drugs Abstract Abstract Increasing affinity to lung tissue is an important strategy to achieve pulmonary retention and to prolong the duration of effect in the lung. As the ...
PMC9420438
core_pubmed_pmc
The Pharmacokinetics/Pharmacodynamics and Neurotoxicity of Tigecycline Intraventricular Injection for the Treatment of Extensively Drug-Resistant Acinetobacter baumannii Intracranial Infection
The Pharmacokinetics/Pharmacodynamics and Neurotoxicity of Tigecycline Intraventricular Injection for the Treatment of Extensively Drug-Resistant Acinetobacter baumannii Intracranial Infection Abstract Objective This study aimed to provide feasible suggestions for intraventricular injection of tigecycline to treat intr...
PMC12457637
core_pubmed_pmc
An aptamer-drug conjugate for promising cancer therapy with comprehensive evaluation from rodents to non-human primates
An aptamer-drug conjugate for promising cancer therapy with comprehensive evaluation from rodents to non-human primates Abstract Abstract Aptamers serve as unique targeting ligands, making aptamer-drug conjugates (ApDCs) an attractive strategy for targeted cancer therapy. This study performs a comprehensive evaluation ...
PMC12583982
core_pubmed_pmc
Safety and Pharmacokinetics of Long‐Acting Monoclonal Antibodies Tixagevimab and Cilgavimab (AZD7442) in a China Phase 2 Study and Evaluation of Asian Race Effect
Safety and Pharmacokinetics of Long‐Acting Monoclonal Antibodies Tixagevimab and Cilgavimab (AZD7442) in a China Phase 2 Study and Evaluation of Asian Race Effect Abstract Abstract Safety, pharmacokinetics, and impact of race of pharmacokinetics on monoclonal antibodies tixagevimab and cilgavimab (AZD7442) were assesse...
PMC2999583
core_pubmed_pmc
Curcumin activates the p38MPAK-HSP25 pathway in vitro but fails to attenuate diabetic nephropathy in DBA2J mice despite urinary clearance documented by HPLC
Curcumin activates the p38MPAK-HSP25 pathway in vitro but fails to attenuate diabetic nephropathy in DBA2J mice despite urinary clearance documented by HPLC Abstract Background Curcumin has anti-inflammatory, anti-oxidant, and anti-proliferative properties, and depending upon the experimental circumstances, may be pro-...
PMC3931931
core_pubmed_pmc
An open-label, dose-escalation, safety, and pharmacokinetics phase I study of ombrabulin, a vascular disrupting agent, administered as a 30-min intravenous infusion every 3 weeks in Japanese patients with advanced solid tumors
An open-label, dose-escalation, safety, and pharmacokinetics phase I study of ombrabulin, a vascular disrupting agent, administered as a 30-min intravenous infusion every 3 weeks in Japanese patients with advanced solid tumors Abstract Purpose To determine ombrabulin’s maximum tolerated dose and dose recommended for Ja...
PMC3946363
core_pubmed_pmc
Effect of Protease Inhibitors on Steady-State Pharmacokinetics of Oral Norethindrone Contraception in HIV-Infected Women
Effect of Protease Inhibitors on Steady-State Pharmacokinetics of Oral Norethindrone Contraception in HIV-Infected Women Abstract Abstract Objective: Pharmacokinetic interactions exist between combined oral contraceptives and protease inhibitors (PI). However, such information is lacking for progestin-only oral contrac...
PMC3495895
core_pubmed_pmc
PR-104 a bioreductive pre-prodrug combined with gemcitabine or docetaxel in a phase Ib study of patients with advanced solid tumours
PR-104 a bioreductive pre-prodrug combined with gemcitabine or docetaxel in a phase Ib study of patients with advanced solid tumours Abstract Background The purpose of this phase Ib clinical trial was to determine the maximum tolerated dose (MTD) of PR-104 a bioreductive pre-prodrug given in combination with gemcitabin...
PMC10994819
core_pubmed_pmc
A population pharmacokinetic model for posaconazole intravenous solution and oral powder for suspension formulations in pediatric patients with neutropenia
A population pharmacokinetic model for posaconazole intravenous solution and oral powder for suspension formulations in pediatric patients with neutropenia Abstract ABSTRACT The objective of this study was to support posaconazole dose regimens in pediatric patients aged ≥2 years, using a population pharmacokinetic (PK)...
PMC11780677
core_pubmed_pmc
Prediction of potential drug targets and key inhibitors (ZINC67974679, ZINC67982856, and ZINC05668040) against Rickettsia felis using integrated computational approaches
Prediction of potential drug targets and key inhibitors (ZINC67974679, ZINC67982856, and ZINC05668040) against Rickettsia felis using integrated computational approaches Abstract Abstract Rickettsia felis , responsible for flea-borne spotted fever, is a rising zoonotic pathogen posing an increasing global threat due to...
PMC7019645
core_pubmed_pmc
A Systematic Review on the Effect of HIV Infection on the Pharmacokinetics of First-Line Tuberculosis Drugs
A Systematic Review on the Effect of HIV Infection on the Pharmacokinetics of First-Line Tuberculosis Drugs Abstract Abstract Introduction Contrasting findings have been published regarding the effect of human immunodeficiency virus (HIV) on tuberculosis (TB) drug pharmacokinetics (PK). Objectives The aim of this syste...
PMC6590436
core_pubmed_pmc
A Phase 1 Randomized, Placebo‐Controlled Trial With a Topical Inhibitor of Stearoyl‐Coenzyme A Desaturase 1 Under Occluded and Nonoccluded Conditions
A Phase 1 Randomized, Placebo‐Controlled Trial With a Topical Inhibitor of Stearoyl‐Coenzyme A Desaturase 1 Under Occluded and Nonoccluded Conditions Abstract Abstract Stearoyl‐coenzyme A desaturase 1 (SCD‐1) in sebaceous glands is a key enzyme in the synthesis of monounsaturated fatty acids essential for acne developm...
PMC9320978
core_pubmed_pmc
Physiologically based pharmacokinetic modeling and simulations to inform dissolution specifications and clinical relevance of release rates on elagolix exposure
Physiologically based pharmacokinetic modeling and simulations to inform dissolution specifications and clinical relevance of release rates on elagolix exposure Abstract Abstract The aim of this analysis was to use a physiologically based pharmacokinetic (PBPK) model to predict the impact of changes in dissolution rate...
PMC9204533
core_pubmed_pmc
Exposure–Response Analysis of Cardiovascular Outcome Trials With Incretin-Based Therapies
Exposure–Response Analysis of Cardiovascular Outcome Trials With Incretin-Based Therapies Abstract Our study aimed to evaluate the exposure–response relationship between incretin-based medications and the risk of major adverse cardiovascular events (MACE) using cardiovascular outcome trials (CVOTs). Eleven CVOTs with i...
PMC5702950
core_pubmed_pmc
Pharmacokinetics, Tissue Distribution, and Metabolism Study of Icariin in Rat
Pharmacokinetics, Tissue Distribution, and Metabolism Study of Icariin in Rat Abstract Icariin is one of the predominant flavonoids contained in Herba Epimedii (Yin-yang-huo in Chinese), a well-known Chinese medicine for the treatment of cancers and immune system diseases. Although Herba Epimedii has been widely used i...
PMC7417932
core_pubmed_pmc
CYP2D6 Genotype-Based Dose Recommendations for Risperidone in Asian People
CYP2D6 Genotype-Based Dose Recommendations for Risperidone in Asian People Abstract Abstract The aim of this study was to provide dose recommendations for risperidone in Asian people based on cytochrome P450 enzyme CYP2D6 genotype. First, we investigated the influence of CYP2D6 polymorphism on the pharmacokinetics of r...
PMC10026081
core_pubmed_pmc
A pharmacokinetic drug–drug interaction study between rosuvastatin and emvododstat, a potent anti‐SARS‐CoV‐2 (COVID‐19) DHODH (dihydroorotate dehydrogenase) inhibitor
A pharmacokinetic drug–drug interaction study between rosuvastatin and emvododstat, a potent anti‐SARS‐CoV‐2 (COVID‐19) DHODH (dihydroorotate dehydrogenase) inhibitor Abstract Abstract A therapeutic agent that targets both viral replication and the hyper‐reactive immune response would offer a highly desirable treatment...
PMC10761933
core_pubmed_pmc
Acquired and intrinsic resistance to vemurafenib in BRAF V600E ‐driven melanoma brain metastases
Acquired and intrinsic resistance to vemurafenib in BRAF V600E ‐driven melanoma brain metastases Abstract Abstract BRAF V600 ‐mutated melanoma brain metastases (MBMs) are responsive to BRAF inhibitors, but responses are generally less durable than those of extracranial metastases. We tested the hypothesis that the drug...
PMC4622054
core_pubmed_pmc
A novel in vitro assay to predict neonatal Fc receptor-mediated human IgG half-life
A novel in vitro assay to predict neonatal Fc receptor-mediated human IgG half-life Abstract Abstract Immunoglobulin G (IgG) has an unusually long serum half-life in comparison to proteins of a similar size. It is well-known that this phenomenon is due to IgG's ability to bind the neonatal Fc receptor (FcRn) in a pH-de...
PMC7499188
core_pubmed_pmc
A Physiologically‐Based Pharmacokinetic Model for the Prediction of “Half‐Life Extension” and “Catch and Release” Monoclonal Antibody Pharmacokinetics
A Physiologically‐Based Pharmacokinetic Model for the Prediction of “Half‐Life Extension” and “Catch and Release” Monoclonal Antibody Pharmacokinetics Abstract Monoclonal antibodies (mAbs) can be engineered to have “extended half‐life” and “catch and release” properties to improve target coverage. We have developed a m...
PMC8826609
core_pubmed_pmc
Pharmacokinetics and Safety of the Abacavir/Lamivudine/Lopinavir/Ritonavir Fixed-Dose Granule Formulation (4-in-1) in Neonates: PETITE Study
Pharmacokinetics and Safety of the Abacavir/Lamivudine/Lopinavir/Ritonavir Fixed-Dose Granule Formulation (4-in-1) in Neonates: PETITE Study Abstract Background: Antiretroviral options for neonates (younger than 28 days) should be expanded. We evaluated the pharmacokinetics, safety, and acceptability of the "4-in-1" fi...
PMC10525702
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling of Extracellular Vesicles
Physiologically Based Pharmacokinetic Modeling of Extracellular Vesicles Abstract Abstract Simple Summary Extracellular vesicles (EVs) are cell-derived structures that play a vital role in intercellular communication and have potential as drug delivery platforms. Physiologically based pharmacokinetic (PBPK) modeling ca...
PMC3348450
core_pubmed_pmc
Management of axitinib (AG-013736)-induced fatigue and thyroid dysfunction, and predictive biomarkers of axitinib exposure: results from phase I studies in Japanese patients
Management of axitinib (AG-013736)-induced fatigue and thyroid dysfunction, and predictive biomarkers of axitinib exposure: results from phase I studies in Japanese patients Abstract Summary Background Axitinib is an oral, potent and selective inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and ...
PMC7020291
core_pubmed_pmc
Parametric Time‐to‐Event Model for Acute Exacerbations in Idiopathic Pulmonary Fibrosis
Parametric Time‐to‐Event Model for Acute Exacerbations in Idiopathic Pulmonary Fibrosis Abstract Abstract We describe a parametric time‐to‐event model for idiopathic pulmonary fibrosis (IPF) exacerbations and identify predictors of exacerbation risk using data obtained for the tyrosine‐kinase inhibitor nintedanib in tw...