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PMC11307036
core_pubmed_pmc
Neuroimaging to Facilitate Clinical Trials in Huntington’s Disease: Current Opinion from the EHDN Imaging Working Group
Neuroimaging to Facilitate Clinical Trials in Huntington’s Disease: Current Opinion from the EHDN Imaging Working Group Abstract Abstract Neuroimaging is increasingly being included in clinical trials of Huntington’s disease (HD) for a wide range of purposes from participant selection and safety monitoring, through to ...
PMC4728804
core_pubmed_pmc
PK/PD analysis of biapenem in patients undergoing continuous hemodiafiltration
PK/PD analysis of biapenem in patients undergoing continuous hemodiafiltration Abstract Abstract Background Continuous hemodiafiltration (CHDF) is used as renal replacement therapy for critically ill patients with renal failure, and to treat hypercytokinemia. Since CHDF also clears therapeutic agents, drug pharmacokine...
PMC10196440
core_pubmed_pmc
Minimal physiologically‐based hybrid model of pharmacokinetics in pregnant women: Application to antenatal corticosteroids
Minimal physiologically‐based hybrid model of pharmacokinetics in pregnant women: Application to antenatal corticosteroids Abstract Abstract Minimal physiologically‐based pharmacokinetic (mPBPK) models are an alternative to full physiologically‐based pharmacokinetic (PBPK) models as they offer reduced complexity while ...
PMC3554664
core_pubmed_pmc
The Pharmacokinetic-Pharmacodynamic Model of Azithromycin for Lipopolysaccharide-Induced Depressive-Like Behavior in Mice
The Pharmacokinetic-Pharmacodynamic Model of Azithromycin for Lipopolysaccharide-Induced Depressive-Like Behavior in Mice Abstract Abstract A mechanism-based model was developed to describe the time course of lipopolysaccharide-induced depressive-like behavior and azithromycin pharmacodynamics in mice. The lipopolysacc...
PMC7997578
core_pubmed_pmc
Design, Synthesis, Dynamic Docking, Biochemical Characterization, and in Vivo Pharmacokinetics Studies of Novel Topoisomerase II Poisons with Promising Antiproliferative Activity
Design, Synthesis, Dynamic Docking, Biochemical Characterization, and in Vivo Pharmacokinetics Studies of Novel Topoisomerase II Poisons with Promising Antiproliferative Activity Abstract Abstract We previously reported a first set of hybrid topoisomerase II (topoII) poisons whose chemical core merges key pharmacophori...
PMC6701640
core_pubmed_pmc
Augmented renal clearance is associated with inadequate antibiotic pharmacokinetic/pharmacodynamic target in Asian ICU population: a prospective observational study
Augmented renal clearance is associated with inadequate antibiotic pharmacokinetic/pharmacodynamic target in Asian ICU population: a prospective observational study Abstract Abstract Background Augmented renal clearance (ARC) is common in critically ill patients and could result in subtherapeutic antibiotic concentrati...
PMC6734620
core_pubmed_pmc
Levetiracetam and brivaracetam: a review of evidence from clinical trials and clinical experience
Levetiracetam and brivaracetam: a review of evidence from clinical trials and clinical experience Abstract Until the early 1990s, a limited number of antiepileptic drugs (AEDs) were available. Since then, a large variety of new AEDs have been developed and introduced, several of them offering new modes of action. One o...
PMC3868344
core_pubmed_pmc
A Computational Hypothesis for Allostasis: Delineation of Substance Dependence, Conventional Therapies, and Alternative Treatments
A Computational Hypothesis for Allostasis: Delineation of Substance Dependence, Conventional Therapies, and Alternative Treatments Abstract The allostatic theory of drug abuse describes the brain’s reward system alterations as substance misuse progresses. Neural adaptations arising from the reward system itself and fro...
PMC3880615
core_pubmed_pmc
New algorithm for valganciclovir dosing in pediatric solid organ transplant recipients
New algorithm for valganciclovir dosing in pediatric solid organ transplant recipients Abstract CMV infections are common after SOT. v-GCV is increasingly used in children. The aim of this study was to evaluate presently used dosing algorithms. Data from 104 pediatric SOT recipients (kidney, liver, and heart) aged 0.3–...
PMC12549492
core_pubmed_pmc
The Safety, Tolerability, and Pharmacokinetics of ALT-BB4 (A Novel Recombinant Hyaluronidase): A Randomized, Double-Blinded, Placebo-Controlled, Phase 1 Study in Healthy Volunteers
The Safety, Tolerability, and Pharmacokinetics of ALT-BB4 (A Novel Recombinant Hyaluronidase): A Randomized, Double-Blinded, Placebo-Controlled, Phase 1 Study in Healthy Volunteers Abstract Introduction Hyaluronidase has been used as an adjuvant to facilitate subcutaneous drug delivery by degrading hyaluronic acid, a v...
PMC3356223
core_pubmed_pmc
Effect of intratumoral administration on biodistribution of 64 Cu-labeled nanoshells
Effect of intratumoral administration on biodistribution of 64 Cu-labeled nanoshells Abstract Abstract Background Gold nanoshells are excellent agents for photothermal ablation cancer therapy and are currently under clinical trial for solid tumors. Previous studies showed that passive delivery of gold nanoshells throug...
PMC5362674
core_pubmed_pmc
HATT: a phase IV, single-arm, open-label study of sorafenib in Taiwanese patients with advanced hepatocellular carcinoma
HATT: a phase IV, single-arm, open-label study of sorafenib in Taiwanese patients with advanced hepatocellular carcinoma Abstract Abstract Background Sorafenib significantly improves survival in patients with advanced hepatocellular carcinoma (HCC). This phase IV study assessed sorafenib efficacy/safety in Taiwanese pa...
PMC8066993
core_pubmed_pmc
Population Pharmacokinetics and Dose Optimization of Ceftazidime and Imipenem in Patients with Acute Exacerbations of Chronic Obstructive Pulmonary Disease
Population Pharmacokinetics and Dose Optimization of Ceftazidime and Imipenem in Patients with Acute Exacerbations of Chronic Obstructive Pulmonary Disease Abstract Background: Ceftazidime and imipenem have been increasingly used to treat Acute Exacerbations of Chronic Obstructive Pulmonary Disease (AECOPD) due to thei...
PMC7566350
core_pubmed_pmc
Clofazimine pharmacokinetics in patients with TB: dosing implications
Clofazimine pharmacokinetics in patients with TB: dosing implications Abstract Abstract Background Clofazimine is in widespread use as a key component of drug-resistant TB regimens, but the recommended dose is not evidence based. Pharmacokinetic data from relevant patient populations are needed to inform dose optimizat...
PMC8532763
core_pubmed_pmc
Population Pharmacokinetics and Dosing Simulation of Vancomycin Administered by Continuous Injection in Critically Ill Patient
Population Pharmacokinetics and Dosing Simulation of Vancomycin Administered by Continuous Injection in Critically Ill Patient Abstract Background: Vancomycin is widely used for empirical antimicrobial therapy in critically ill patients with sepsis. Continuous infusion (CI) may provide more stable exposure than intermi...
PMC8252052
core_pubmed_pmc
Pharmacokinetics and safety of ubrogepant when coadministered with calcitonin gene‒related peptide‐targeted monoclonal antibody migraine preventives in participants with migraine: A randomized phase 1b drug–drug interaction study
Pharmacokinetics and safety of ubrogepant when coadministered with calcitonin gene‒related peptide‐targeted monoclonal antibody migraine preventives in participants with migraine: A randomized phase 1b drug–drug interaction study Abstract Abstract Objective To evaluate the impact of two calcitonin gene–related peptide ...
PMC12188803
core_pubmed_pmc
The future of target-controlled infusion and new pharmacokinetic models
The future of target-controlled infusion and new pharmacokinetic models Abstract Abstract Purpose of review To summarize recent developments in the understanding of the pharmacology of the hypnotic and opioid drugs, with relevance to target-controlled infusions and newer pharmacokinetic models. Recent findings General-...
PMC10658028
core_pubmed_pmc
Syringe immersion test as in vitro bioassay against Rhipicephalus microplus : Macrocyclic lactones dose-response relationship
Syringe immersion test as in vitro bioassay against Rhipicephalus microplus : Macrocyclic lactones dose-response relationship Abstract Background: For the diagnosis of tick sensitivity against different acaricides, there are in vitro and in vivo methods. The main in vivo method, the stable test, is considered a definin...
PMC11717216
core_pubmed_pmc
DigiLoCS: A leap forward in predictive organ-on-chip simulations
DigiLoCS: A leap forward in predictive organ-on-chip simulations Abstract Digital twins, driven by data and mathematical modelling, have emerged as powerful tools for simulating complex biological systems. In this work, we focus on modelling the clearance on a liver-on-chip as a digital twin that closely mimics the cle...
PMC11070758
core_pubmed_pmc
Development and translation of thiometallate sulfide donors using a porcine model of coronary occlusion and reperfusion
Development and translation of thiometallate sulfide donors using a porcine model of coronary occlusion and reperfusion Abstract Abstract Sulfide-releasing compounds reduce reperfusion injury by decreasing mitochondria-derived reactive oxygen species production. We previously characterised ammonium tetrathiomolybdate (...
PMC4509428
core_pubmed_pmc
A clinical review of GLP-1 receptor agonists: efficacy and safety in diabetes and beyond
A clinical review of GLP-1 receptor agonists: efficacy and safety in diabetes and beyond Abstract Abstract The prevalence of type 2 diabetes is increasing at an astounding rate. Many of the agents used to treat type 2 diabetes have undesirable adverse effects of hypoglycemia and weight gain. Glucagon-like peptide-1 (GL...
PMC10520196
core_pubmed_pmc
Population Pharmacokinetic Modeling of Dolutegravir to Optimize Pediatric Dosing in HIV-1-Infected Infants, Children, and Adolescents
Population Pharmacokinetic Modeling of Dolutegravir to Optimize Pediatric Dosing in HIV-1-Infected Infants, Children, and Adolescents Abstract Background and Objective HIV treatment options remain limited in children. Dolutegravir is a potent and well-tolerated, once-daily HIV-1 integrase inhibitor recommended for HIV-...
PMC8604211
core_pubmed_pmc
Model‐based assessments of CYP3A‐mediated drug‐drug interaction risk of milademetan
Model‐based assessments of CYP3A‐mediated drug‐drug interaction risk of milademetan Abstract Abstract Milademetan is a small‐molecule inhibitor of murine double minute 2 (MDM2) that is in clinical development for advanced solid tumors and hematological cancers, including liposarcoma and acute myeloid leukemia. Milademe...
PMC6765695
core_pubmed_pmc
Maternal–Neonatal Raltegravir Population Pharmacokinetics Modeling: Implications for Initial Neonatal Dosing
Maternal–Neonatal Raltegravir Population Pharmacokinetics Modeling: Implications for Initial Neonatal Dosing Abstract Abstract Raltegravir readily crosses the placenta to the fetus with maternal use during pregnancy. After birth, neonatal raltegravir elimination is highly variable and often extremely prolonged, with so...
PMC12477134
core_pubmed_pmc
Precision dosing of voriconazole in immunocompromised children under 2 years: integrated machine learning and population pharmacokinetic modeling
Precision dosing of voriconazole in immunocompromised children under 2 years: integrated machine learning and population pharmacokinetic modeling Abstract Objective This study aimed to develop an individualized dosing strategy for voriconazole (VRZ) in children under 2 years of age by integrating machine learning (ML) ...
PMC12850555
core_pubmed_pmc
Population pharmacokinetic modelling revealed large variability in oromucosal absorption of Δ 9 ‐tetrahydrocannabinol in older patients with poor appetite
Population pharmacokinetic modelling revealed large variability in oromucosal absorption of Δ 9 ‐tetrahydrocannabinol in older patients with poor appetite Abstract Aim Cannabis‐based medicines are gaining interest and being explored for new therapeutic indications, many of which commonly affect older medical patients. ...
PMC9381907
core_pubmed_pmc
Population pharmacokinetic/pharmacodynamic joint modeling of ixazomib efficacy and safety using data from the pivotal phase III TOURMALINE‐MM1 study in multiple myeloma patients
Population pharmacokinetic/pharmacodynamic joint modeling of ixazomib efficacy and safety using data from the pivotal phase III TOURMALINE‐MM1 study in multiple myeloma patients Abstract Abstract Ixazomib is an oral proteasome inhibitor approved in combination with lenalidomide and dexamethasone for the treatment of re...
PMC9606572
core_pubmed_pmc
Development of an innovative in vivo model of PJI treated with DAIR
Development of an innovative in vivo model of PJI treated with DAIR Abstract Abstract Introduction Prosthetic Joint Infection (PJI) are catastrophic complications of joint replacement. Debridement, implant retention, and antibiotic therapy (DAIR) is the usual strategy in acute infections but fails in 45% of MRSA infect...
PMC6398836
core_pubmed_pmc
Phase 1 Study of Edasalonexent (CAT-1004), an Oral NF- κ B Inhibitor, in Pediatric Patients with Duchenne Muscular Dystrophy
Phase 1 Study of Edasalonexent (CAT-1004), an Oral NF- κ B Inhibitor, in Pediatric Patients with Duchenne Muscular Dystrophy Abstract Background: Edasalonexent is an orally administered small molecule designed to inhibit NF- κ B, which is activated from infancy in Duchenne muscular dystrophy and is central to causing m...
PMC6204859
core_pubmed_pmc
Enhanced oral bioavailability of fluvastatin by using nanosuspensions containing cyclodextrin
Enhanced oral bioavailability of fluvastatin by using nanosuspensions containing cyclodextrin Abstract Background In this study, fluvastatin (FVT) nanosuspensions containing cyclodextrin were developed to improve oral bioavailability. Methods FVT nanosuspensions containing cyclodextrin were prepared by a high pressure ...
PMC7577015
core_pubmed_pmc
Pharmacokinetic Characterization to Enable Medicine Use in Pregnancy, the Potential Role of Physiologically‐Based Pharmacokinetic Modeling: A Regulatory Perspective
Pharmacokinetic Characterization to Enable Medicine Use in Pregnancy, the Potential Role of Physiologically‐Based Pharmacokinetic Modeling: A Regulatory Perspective Modeling A Role for PBPK Modeling? PBPK modeling is increasingly used in drug development and regulatory submissions, and the purpose of the models has exp...
PMC11441729
core_pubmed_pmc
A Comprehensive Overview of the Efficacy and Safety of Gadopiclenol: A New Contrast Agent for MRI of the CNS and Body
A Comprehensive Overview of the Efficacy and Safety of Gadopiclenol: A New Contrast Agent for MRI of the CNS and Body Abstract Abstract This review describes the pharmacokinetics, efficacy, and safety of gadopiclenol, a new macrocyclic gadolinium-based contrast agent (GBCA) recently approved by the Food and Drug Admini...
PMC9284347
core_pubmed_pmc
Natural-product-inspired design and synthesis of thiolated coenzyme Q analogs as promising agents against Gram-positive bacterial strains: insights into structure–activity relationship, activity profile, mode of action, and molecular docking †
Natural-product-inspired design and synthesis of thiolated coenzyme Q analogs as promising agents against Gram-positive bacterial strains: insights into structure–activity relationship, activity profile, mode of action, and molecular docking † Abstract In an attempt to develop effective and potentially active antibacte...
PMC4876175
core_pubmed_pmc
Population pharmacokinetics of oseltamivir and oseltamivir carboxylate in obese and non‐obese volunteers
Population pharmacokinetics of oseltamivir and oseltamivir carboxylate in obese and non‐obese volunteers Abstract Aims The aims of the present study were to compare the pharmacokinetics of oseltamivir and its active antiviral metabolite oseltamivir carboxylate in obese and non‐obese individuals and to determine the eff...
PMC11852064
core_pubmed_pmc
Multidose Dalbavancin Population Pharmacokinetic Analysis for Prolonged Target Attainment in Patients Requiring Long-Term Treatment
Multidose Dalbavancin Population Pharmacokinetic Analysis for Prolonged Target Attainment in Patients Requiring Long-Term Treatment Abstract Abstract Introduction: Dalbavancin (DAL) is a long-acting lipoglycopeptide active against Gram-positive bacteria, including multidrug-resistant isolates. A growing body of evidenc...
PMC10091729
core_pubmed_pmc
Population PK and Semimechanistic PK/PD Modeling and Simulation of Relugolix Effects on Testosterone Suppression in Men with Prostate Cancer
Population PK and Semimechanistic PK/PD Modeling and Simulation of Relugolix Effects on Testosterone Suppression in Men with Prostate Cancer Abstract Relugolix, the first orally active, nonpeptide gonadotropin‐releasing hormone receptor antagonist, is approved in the United States and the European Union for the treatme...
PMC9569447
core_pubmed_pmc
Novel Long-Acting Oxytocin Analog with Increased Efficacy in Reducing Food Intake and Body Weight
Novel Long-Acting Oxytocin Analog with Increased Efficacy in Reducing Food Intake and Body Weight Abstract Oxytocin (OXT) analogues have been designed to overcome the limitation of the short half-life of the native OXT peptide. Here, we tested ASK2131 on obesity related outcomes in diet-induced obese (DIO) Sprague Dawl...
PMC8067335
core_pubmed_pmc
Optimal Dosing Regimen of Osteoporosis Drugs in Relation to Food Intake as the Key for the Enhancement of the Treatment Effectiveness—A Concise Literature Review
Optimal Dosing Regimen of Osteoporosis Drugs in Relation to Food Intake as the Key for the Enhancement of the Treatment Effectiveness—A Concise Literature Review Abstract Bisphosphonates and selective estrogen receptor modulators (SERMs) represent the two most important groups of medications taken orally and employed i...
PMC11555515
core_pubmed_pmc
Exploring the Interplay Between Radioimmunoconjugates and Fcγ Receptors in Genetically Engineered Mouse Models of Cancer
Exploring the Interplay Between Radioimmunoconjugates and Fcγ Receptors in Genetically Engineered Mouse Models of Cancer Abstract Fcγ receptors (FcγR) are responsible for many of the interactions between immunoglobulins (IgG) and immune cells. In biomedicine, this interplay is critical to the activity of several types ...
PMC12030195
core_pubmed_pmc
Recent Advances in Vitamin E TPGS-Based Organic Nanocarriers for Enhancing the Oral Bioavailability of Active Compounds: A Systematic Review
Recent Advances in Vitamin E TPGS-Based Organic Nanocarriers for Enhancing the Oral Bioavailability of Active Compounds: A Systematic Review Abstract Abstract Background: D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), an amphiphilic derivative of natural vitamin E, functions as both a drug efflux inhibitor a...
PMC8233650
core_pubmed_pmc
Fluconazole nanoparticles prepared by antisolvent precipitation technique: Physicochemical, in vitro , ex vivo and in vivo ocular evaluation
Fluconazole nanoparticles prepared by antisolvent precipitation technique: Physicochemical, in vitro , ex vivo and in vivo ocular evaluation Abstract Abstract The goal of this research was to prepare and characterize nanonized particles of the antifungal drug, fluconazole (FLZ) using antisolvent precipitation nanonizat...
PMC5036534
core_pubmed_pmc
Quantifying the pharmacology of antimalarial drug combination therapy
Quantifying the pharmacology of antimalarial drug combination therapy Abstract Most current antimalarial drugs are combinations of an artemisinin plus a ‘partner’ drug from another class, and are known as artemisinin-based combination therapies (ACTs). They are the frontline drugs in treating human malaria infections. ...
PMC6669312
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Oral and Intravenous Omadacycline
Pharmacokinetics and Pharmacodynamics of Oral and Intravenous Omadacycline Abstract Abstract Oral and intravenous (IV) omadacycline formulations are approved in the United States for treating acute bacterial skin and skin structure infections and community-acquired bacterial pneumonia in adults. Oral omadacycline bioav...
PMC12354863
core_pubmed_pmc
Safety and efficacy of HH2853, a novel EZH1/2 dual inhibitor, in patients with refractory solid tumours or non-Hodgkin lymphomas: a phase I study
Safety and efficacy of HH2853, a novel EZH1/2 dual inhibitor, in patients with refractory solid tumours or non-Hodgkin lymphomas: a phase I study Abstract Summary Background HH2853 is a novel dual EZH1/2 inhibitor that exhibits superior antitumour activity compared to tazemetostat across various preclinical models. Her...
PMC9963808
core_pubmed_pmc
Comparing Salivary Caffeine Kinetics of 13 C and 12 C Caffeine for Gastric Emptying of 50 mL Water
Comparing Salivary Caffeine Kinetics of 13 C and 12 C Caffeine for Gastric Emptying of 50 mL Water Abstract Gastric water emptying as a critical parameter for oral drug absorption can be investigated by several imaging techniques or by the interpretation of pharmacokinetics of appropriate substances. Recently introduce...
PMC11083707
core_pubmed_pmc
Pharmacodynamic and Toxicity Studies of 6-Isopropyldithio-2′-guanosine Analogs in Acute T-Lymphoblastic Leukemia
Pharmacodynamic and Toxicity Studies of 6-Isopropyldithio-2′-guanosine Analogs in Acute T-Lymphoblastic Leukemia Abstract Abstract Simple Summary Acute T-lymphoblastic leukemia is a disease with a very low survival rate after relapse, and the search for new therapeutic agents is important for the clinical benefit of pa...
PMC12299335
core_pubmed_pmc
Association of SLCO1B3 and SLCO1B1 Polymorphisms with Methotrexate Efficacy and Toxicity in Saudi Rheumatoid Arthritis Patients
Association of SLCO1B3 and SLCO1B1 Polymorphisms with Methotrexate Efficacy and Toxicity in Saudi Rheumatoid Arthritis Patients Abstract Background: Methotrexate (MTX) remains the most commonly prescribed drug used to treat rheumatoid arthritis (RA). Polymorphisms in solute carrier organic anion transporter family memb...
PMC8877306
core_pubmed_pmc
Chiral Switch: Between Therapeutical Benefit and Marketing Strategy
Chiral Switch: Between Therapeutical Benefit and Marketing Strategy Abstract Chirality of pharmaceutical substances is an important aspect in drug research because it determines how enantiomers will interact with chiral biological targets. Enantiomers of a chiral drug can have different pharmacokinetic and pharmacologi...
PMC11401669
core_pubmed_pmc
Exploring Lead-Like Molecules of Traditional Chinese Medicine for Treatment Quest against Aliarcobacter butzleri : In Silico Toxicity Assessment, Dynamics Simulation, and Pharmacokinetic Profiling
Exploring Lead-Like Molecules of Traditional Chinese Medicine for Treatment Quest against Aliarcobacter butzleri : In Silico Toxicity Assessment, Dynamics Simulation, and Pharmacokinetic Profiling Abstract Background Aliarcobacter butzleri is a Gram-negative, curved or spiral-shaped, microaerophilic bacterium and cause...
PMC6882492
core_pubmed_pmc
Synthesis and biological evaluation of novel thienopyrimidine derivatives as diacylglycerol acyltransferase 1 (DGAT-1) inhibitors
Synthesis and biological evaluation of novel thienopyrimidine derivatives as diacylglycerol acyltransferase 1 (DGAT-1) inhibitors Abstract Abstract A novel series of thieno[3,2- d ]pyrimidine derivatives were synthesised and their inhibitory effects against diacylglycerol acyltransferase 1 (DGAT-1) were assessed. cis-I...
PMC11878024
core_pubmed_pmc
Characterization of sulopenem antimicrobial activity using in vitro time-kill kinetics, synergy, post-antibiotic effect, and sub-inhibitory MIC effect methods against Escherichia coli and Klebsiella pneumoniae isolates
Characterization of sulopenem antimicrobial activity using in vitro time-kill kinetics, synergy, post-antibiotic effect, and sub-inhibitory MIC effect methods against Escherichia coli and Klebsiella pneumoniae isolates Abstract ABSTRACT Sulopenem is an oral and intravenous penem antibiotic in clinical development for t...
PMC5372358
core_pubmed_pmc
Fluorescent nanodiamonds enable quantitative tracking of human mesenchymal stem cells in miniature pigs
Fluorescent nanodiamonds enable quantitative tracking of human mesenchymal stem cells in miniature pigs Abstract Abstract Cell therapy is a promising strategy for the treatment of human diseases. While the first use of cells for therapeutic purposes can be traced to the 19th century, there has been a lack of general an...
PMC12691663
core_pubmed_pmc
Cerebrospinal fluid penetration of cycloserine/terizidone and clofazimine in patients with pulmonary TB
Cerebrospinal fluid penetration of cycloserine/terizidone and clofazimine in patients with pulmonary TB Abstract ABSTRACT Tuberculous meningitis (TBM) treatment outcomes are poor, partly due to suboptimal drug penetration into the cerebrospinal fluid (CSF). Little is known about the CSF pharmacokinetics of many TB drug...
PMC8589993
core_pubmed_pmc
Systems pharmacology to reveal multi-scale mechanisms of traditional Chinese medicine for gastric cancer
Systems pharmacology to reveal multi-scale mechanisms of traditional Chinese medicine for gastric cancer Abstract Because of the complex etiology, the treatment of gastric cancer is a formidable challenge for contemporary medical. The current treatment method focuses on traditional surgical procedures, supplemented by ...
PMC3948203
core_pubmed_pmc
Clinical Pharmacology of Midazolam in Neonates and Children: Effect of Disease—A Review
Clinical Pharmacology of Midazolam in Neonates and Children: Effect of Disease—A Review Abstract Abstract Midazolam is a benzodiazepine with rapid onset of action and short duration of effect. In healthy neonates the half-life ( t 1/2 ) and the clearance (Cl) are 3.3-fold longer and 3.7-fold smaller, respectively, than...
PMC4075416
core_pubmed_pmc
Does contemporary vancomycin dosing achieve therapeutic targets in a heterogeneous clinical cohort of critically ill patients? Data from the multinational DALI study
Does contemporary vancomycin dosing achieve therapeutic targets in a heterogeneous clinical cohort of critically ill patients? Data from the multinational DALI study Abstract Abstract Introduction The objective of this study was to describe the pharmacokinetics of vancomycin in ICU patients and to examine whether conte...
PMC4837805
core_pubmed_pmc
Population Pharmacokinetics of High-dose Methotrexate After Intravenous Administration in Chinese Osteosarcoma Patients from a Single Institution
Population Pharmacokinetics of High-dose Methotrexate After Intravenous Administration in Chinese Osteosarcoma Patients from a Single Institution Abstract Abstract Background: High-dose methotrexate (HD-MTX) with folinic acid (leucovorin) rescue is the gold standard therapy in the treatment of osteosarcoma. The plasma ...
PMC12145459
core_pubmed_pmc
Evaluation of dimethandrolone undecanoate in non‐human primates as a candidate for long‐acting injectable male contraceptive
Evaluation of dimethandrolone undecanoate in non‐human primates as a candidate for long‐acting injectable male contraceptive Abstract Abstract Background Dimethandrolone undecanoate (DMAU) is under development as a single agent hormonal male contraceptive. DMAU is a prodrug hydrolyzed by esterase(s) to the active metab...
PMC4915614
core_pubmed_pmc
Effect of Bleomycin Hydrolase Gene Polymorphism on Late Pulmonary Complications of Treatment for Hodgkin Lymphoma
Effect of Bleomycin Hydrolase Gene Polymorphism on Late Pulmonary Complications of Treatment for Hodgkin Lymphoma Abstract Abstract Background Bleomycin hydrolase (BLMH), an enzyme that inactivates bleomycin, may be a potential candidate that could influence pulmonary function in ABVD (doxorubicin, bleomycin, vinblasti...
PMC9185960
core_pubmed_pmc
Efficacy and safety of HLX01 in patients with moderate-to-severe rheumatoid arthritis despite methotrexate therapy: a phase 3 study
Efficacy and safety of HLX01 in patients with moderate-to-severe rheumatoid arthritis despite methotrexate therapy: a phase 3 study Abstract Abstract Background To evaluate the efficacy and safety of HLX01, a rituximab biosimilar, as combination therapy with methotrexate in Chinese patients with active rheumatoid arthr...
PMC11916374
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CAMBRIA-1 & CAMBRIA-2 phase III trials: camizestrant versus standard endocrine therapy in ER+/HER2– early breast cancer
CAMBRIA-1 & CAMBRIA-2 phase III trials: camizestrant versus standard endocrine therapy in ER+/HER2– early breast cancer Abstract ABSTRACT Novel selective estrogen receptor degraders (SERDs) are a promising therapeutic option under investigation for patients with estrogen receptor (ER)-positive/human epidermal growth fa...
PMC3969666
core_pubmed_pmc
Effect of various absorption enhancers based on tight junctions on the intestinal absorption of forsythoside A in Shuang-Huang-Lian, application to its antivirus activity
Effect of various absorption enhancers based on tight junctions on the intestinal absorption of forsythoside A in Shuang-Huang-Lian, application to its antivirus activity Abstract Abstract Background: Forsythoside A (FTA), one of the main active ingredients in Shuang–Huang–Lian (SHL), possesses strong antibacterial, an...
PMC3529648
core_pubmed_pmc
Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings
Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings Abstract Abstract Background Considering the observations that linoleic acid conjugated with paclitaxel (CLA-PTX) possesses antitumor activity against brain tumors, is able to cross the blood–brain barrier, but has p...
PMC9148872
core_pubmed_pmc
HLX11, a Proposed Pertuzumab Biosimilar: Pharmacokinetics, Immunogenicity, and Safety Profiles Compared to Three Reference Biologic Products (US-, EU-, and CN-Approved Pertuzumab) Administered to Healthy Male Subjects
HLX11, a Proposed Pertuzumab Biosimilar: Pharmacokinetics, Immunogenicity, and Safety Profiles Compared to Three Reference Biologic Products (US-, EU-, and CN-Approved Pertuzumab) Administered to Healthy Male Subjects Abstract Abstract Background Pertuzumab is a humanized monoclonal antibody for the treatment of breast...
PMC5660969
core_pubmed_pmc
Comparative Long-Term Effect of Three Anti-P2Y12 Drugs after Percutaneous Angioplasty: An Observational Study Based on Electronic Drug Adherence Monitoring
Comparative Long-Term Effect of Three Anti-P2Y12 Drugs after Percutaneous Angioplasty: An Observational Study Based on Electronic Drug Adherence Monitoring Abstract Abstract Aims: Dual platelet inhibition using anti-P2Y12 drugs and aspirin is the standard of care in patients after percutaneous coronary interventions (P...
PMC12624727
core_pubmed_pmc
Benzodeazaoxaflavin Sirtuin Inhibitors Inhibit Schistosoma mansoni Sirt2 and Cause Phenotypic Changes and Lethality in Schistosomula and Adult Worm Stages
Benzodeazaoxaflavin Sirtuin Inhibitors Inhibit Schistosoma mansoni Sirt2 and Cause Phenotypic Changes and Lethality in Schistosomula and Adult Worm Stages Abstract Schistosomiasis, a neglected tropical disease caused by trematodes of Schistosoma genus, urgently requires new treatments due to praziquantel’s limited effi...
PMC12367858
core_pubmed_pmc
Annual Therapeutic Drug Monitoring in Patients with Inflammatory Bowel Disease During Infliximab Maintenance Therapy: Balancing Efficacy with Risk of Pharmacokinetic Failure
Annual Therapeutic Drug Monitoring in Patients with Inflammatory Bowel Disease During Infliximab Maintenance Therapy: Balancing Efficacy with Risk of Pharmacokinetic Failure Abstract Background and Aims Recent studies indicate that proactive therapeutic drug monitoring (TDM) can improve clinical outcomes in patients wi...
PMC12571879
core_pubmed_pmc
Gypenosides, a promising phytochemical triterpenoid: research progress on its pharmacological activity and mechanism
Gypenosides, a promising phytochemical triterpenoid: research progress on its pharmacological activity and mechanism Abstract Abstract Gypenosides (Gyps), a group of dammarane triterpene saponins that are primarily from Gynostemma pentaphyllum , have been identified as promising natural compounds with a diverse array o...
PMC6586067
core_pubmed_pmc
Effects of a State‐ and Use‐Dependent Nav1.7 Channel Blocker on Ambulatory Blood Pressure: A Randomized, Controlled Crossover Study
Effects of a State‐ and Use‐Dependent Nav1.7 Channel Blocker on Ambulatory Blood Pressure: A Randomized, Controlled Crossover Study Abstract Abstract Vixotrigine is a state‐ and use‐dependent Nav1.7 channel blocker being investigated for the treatment of neuropathic pain conditions. This randomized, double‐blind, place...
PMC8581770
core_pubmed_pmc
Dietary polyphenols mitigate SARS-CoV-2 main protease (Mpro)–Molecular dynamics, molecular mechanics, and density functional theory investigations
Dietary polyphenols mitigate SARS-CoV-2 main protease (Mpro)–Molecular dynamics, molecular mechanics, and density functional theory investigations Abstract The recent evolution of the SARS-like Coronavirus has ravaged the world. The deadly virus has claimed over millions of lives across the world and hence highlights t...
PMC12548079
core_pubmed_pmc
Bi-functional integrin degraders cause stronger anti-proliferative effects than a blocking antibody by modulating distinct downstream signaling
Bi-functional integrin degraders cause stronger anti-proliferative effects than a blocking antibody by modulating distinct downstream signaling Abstract ABSTRACT Integrins play a critical role in signaling events that regulate cell adhesion, migration, and proliferation, processes that, when dysregulated, contribute to...
PMC7366348
core_pubmed_pmc
The Evolution of Insulin and How it Informs Therapy and Treatment Choices
The Evolution of Insulin and How it Informs Therapy and Treatment Choices Abstract Abstract Insulin has been available for the treatment of diabetes for almost a century, and the variety of insulin choices today represents many years of discovery and innovation. Insulin has gone from poorly defined extracts of animal p...
PMC3889821
core_pubmed_pmc
A Mechanistic Framework for In Vitro–In Vivo Extrapolation of Liver Membrane Transporters: Prediction of Drug–Drug Interaction Between Rosuvastatin and Cyclosporine
A Mechanistic Framework for In Vitro–In Vivo Extrapolation of Liver Membrane Transporters: Prediction of Drug–Drug Interaction Between Rosuvastatin and Cyclosporine Abstract Abstract Background and Objectives The interplay between liver metabolising enzymes and transporters is a complex process involving system-related...
PMC3124400
core_pubmed_pmc
Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt
Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt Abstract The main purpose of this study was to evaluate liposomes containing a bile salt, sodium deoxycholate (SDC), as oral drug delivery systems to enhance the oral bioavailability of the poorly water-soluble and poorly permeable drug...
PMC11094496
core_pubmed_pmc
Contribution of genetic polymorphism in ABCB1 to individual variations of imatinib plasma levels in patients with gastrointestinal stromal tumor
Contribution of genetic polymorphism in ABCB1 to individual variations of imatinib plasma levels in patients with gastrointestinal stromal tumor Abstract Abstract Background Imatinib mesylate (IM) is a first-line treatment option for the majority of patients diagnosed with gastrointestinal stromal tumors (GISTs). Altho...
PMC6997339
core_pubmed_pmc
Regulation of X-Ray Irradiation on the Activity and Expression Levels of CYP1A2 and CYP2E1 in Rats
Regulation of X-Ray Irradiation on the Activity and Expression Levels of CYP1A2 and CYP2E1 in Rats Abstract The objective of this study was to investigate the regulation of X-ray irradiation and its effect on the activity and protein and mRNA expression levels of CYP1A2 and CYP2E1 in rats. Rats were randomly divided in...
PMC9963881
core_pubmed_pmc
Boosting the In Vivo Transdermal Bioavailability of Asenapine Maleate Using Novel Lavender Oil-Based Lipid Nanocapsules for Management of Schizophrenia
Boosting the In Vivo Transdermal Bioavailability of Asenapine Maleate Using Novel Lavender Oil-Based Lipid Nanocapsules for Management of Schizophrenia Abstract Abstract Lipid nanocapsules (LNCs) are promising for transdermal drug delivery due to their higher permeability-enhancing effects compared to polymeric nanopar...
PMC12146614
core_pubmed_pmc
Second generation CD2-targeting LFA-3 fusion protein SBT115301 to restore immune homeostasis in autoimmune disease
Second generation CD2-targeting LFA-3 fusion protein SBT115301 to restore immune homeostasis in autoimmune disease Abstract Summary In autoimmunity, an imbalance of effector (T eff ) and regulatory (T reg )T cells contributes to inflammation and tissue destruction. CD2, highly expressed on T eff and at lower levels on ...
PMC10108357
core_pubmed_pmc
Anticancer Activity of Region B Capsaicin Analogs
Anticancer Activity of Region B Capsaicin Analogs Abstract The heterocyclic vanilloid compound capsaicin is responsible for the spicy and pungent flavor of chili peppers. Several convergent studies have shown that capsaicin suppresses the growth of multiple human cancers. Apart from capsaicin, natural and synthetic cap...
PMC10083028
core_pubmed_pmc
Customizable Dual-Fluorescent Nanoparticles for Tracing and Quantifying of Cell Transport
Customizable Dual-Fluorescent Nanoparticles for Tracing and Quantifying of Cell Transport Abstract Abstract Purpose Nanotechnology-based drug delivery systems (nano-DDS) have been developed to be a promising strategy to improve the efficacy, safety, physicochemical and pharmacokinetic/pharmacodynamics properties of dru...
PMC12967660
core_pubmed_pmc
Unraveling the Systems Biology of Curcumin: A Mini-review of its Anti-diabetic Potential through Network Pharmacology
Unraveling the Systems Biology of Curcumin: A Mini-review of its Anti-diabetic Potential through Network Pharmacology Abstract Diabetes mellitus (DM) is a complex metabolic disease marked by persistent hyperglycemia and a range of related complications, stemming from intricate molecular mechanisms such as oxidative str...
PMC5510069
core_pubmed_pmc
Evaluation of the immunogenicity of the dabigatran reversal agent idarucizumab during Phase I studies
Evaluation of the immunogenicity of the dabigatran reversal agent idarucizumab during Phase I studies Abstract Abstract Aims Idarucizumab, a humanized monoclonal anti‐dabigatran antibody fragment, is effective in emergency reversal of dabigatran anticoagulation. Pre‐existing and treatment‐emergent anti‐idarucizumab ant...
PMC6220780
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Luseogliflozin, a Selective SGLT2 Inhibitor, in Japanese Patients With Type 2 Diabetes With Mild to Severe Renal Impairment
Pharmacokinetics and Pharmacodynamics of Luseogliflozin, a Selective SGLT2 Inhibitor, in Japanese Patients With Type 2 Diabetes With Mild to Severe Renal Impairment Abstract Abstract This open‐label, parallel‐group, multicenter study aimed to assess the effects of renal impairment on the pharmacokinetics, pharmacodynam...
PMC11296533
core_pubmed_pmc
Assessment and incorporation of in vitro correlates to pharmacokinetic outcomes in antibody developability workflows
Assessment and incorporation of in vitro correlates to pharmacokinetic outcomes in antibody developability workflows Abstract ABSTRACT In vitro assessments for the prediction of pharmacokinetic (PK) behavior of biotherapeutics can help identify corresponding liabilities significantly earlier in the discovery timeline. ...
PMC5463324
core_pubmed_pmc
Influence of Plantago ovata husk (dietary fiber) on the bioavailability and other pharmacokinetic parameters of metformin in diabetic rabbits
Influence of Plantago ovata husk (dietary fiber) on the bioavailability and other pharmacokinetic parameters of metformin in diabetic rabbits Abstract Abstract Background Metformin is an oral hypoglycemic agent frequently used in patients with type 2 diabetes. In this study, we have investigated the influence of the di...
PMC11831578
core_pubmed_pmc
Evaluating the Safety and Efficacy of Ticagrelor vs. Clopidogrel Following Percutaneous Coronary Intervention in Chronic Coronary Disease
Evaluating the Safety and Efficacy of Ticagrelor vs. Clopidogrel Following Percutaneous Coronary Intervention in Chronic Coronary Disease Abstract Objective This study aimed to compare the safety and efficacy of ticagrelor and clopidogrel in reducing major adverse cardiovascular events (MACE) among patients undergoing ...
PMC4441746
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic profile of bendamustine and its metabolites
Pharmacokinetic and pharmacodynamic profile of bendamustine and its metabolites Abstract Abstract Purpose Bendamustine is a unique alkylating agent indicated for the treatment of chronic lymphocytic leukemia and rituximab-refractory, indolent B cell non-Hodgkin’s lymphoma. Despite the extensive experience with bendamus...
PMC3603471
core_pubmed_pmc
CPT: Pharmacometrics and Systems Pharmacology
CPT: Pharmacometrics and Systems Pharmacology Abstract Abstract Welcome to the first issue of CPT: Pharmacometrics and Systems Pharmacology ( CPT:PSP ), a new journal from the American Society for Clinical Pharmacology and Therapeutics. CPT:PSP is a cross-disciplinary journal devoted to publishing advances in quantitat...
PMC6055495
core_pubmed_pmc
Safety and effectiveness of apixaban compared to warfarin in dialysis patients
Safety and effectiveness of apixaban compared to warfarin in dialysis patients Abstract Abstract Essentials The safety of apixaban in patients on dialysis is currently debated. Bleeding events were retrospectively compared for dialysis patients on warfarin vs apixaban. Overall bleeding events were significantly less fr...
PMC10342533
core_pubmed_pmc
Novel Tetrazole Derivatives Targeting Tubulin Endowed with Antiproliferative Activity against Glioblastoma Cells
Novel Tetrazole Derivatives Targeting Tubulin Endowed with Antiproliferative Activity against Glioblastoma Cells Abstract Increasing awareness of the structure of microtubules has made tubulin a relevant target for the research of novel chemotherapies. Furthermore, the particularly high sensitivity of glioblastoma mult...
PMC6484179
core_pubmed_pmc
Pharmacodynamic Analysis of the Influence of Propofol on Left Ventricular Long-Axis Systolic Performance in Cardiac Surgical Patients
Pharmacodynamic Analysis of the Influence of Propofol on Left Ventricular Long-Axis Systolic Performance in Cardiac Surgical Patients Abstract Background Propofol induced a decline in the left ventricular (LV) systolic performance in non-cardiac surgery. We tested the hypothesis that propofol decreased the LV contracti...
PMC5760888
core_pubmed_pmc
Simple and sensitive determination of sparfloxacin in pharmaceuticals and biological samples by immunoassay
Simple and sensitive determination of sparfloxacin in pharmaceuticals and biological samples by immunoassay Abstract Abstract Plasma quinolone concentrations are not routinely measured in clinical practice. However, in order to optimize quinolone treatment, monitoring of plasma concentrations could sometimes be useful ...
PMC4901060
core_pubmed_pmc
Pharmacokinetics of Oral and Inhaled Terbutaline after Exercise in Trained Men
Pharmacokinetics of Oral and Inhaled Terbutaline after Exercise in Trained Men Abstract Abstract Aim: The aim of the study was to investigate pharmacokinetics of terbutaline after oral and inhaled administration in healthy trained male subjects in relation to doping control. Methods: Twelve healthy well-trained young m...
PMC6302106
core_pubmed_pmc
Using Baclofen to Explore GABA-B Receptor Function in Alcohol Dependence: Insights From Pharmacokinetic and Pharmacodynamic Measures
Using Baclofen to Explore GABA-B Receptor Function in Alcohol Dependence: Insights From Pharmacokinetic and Pharmacodynamic Measures Abstract Background: The role of GABA-B neurotransmission in addiction has recently received increased attention, with clinical trials indicating that baclofen, a GABA-B receptor agonist,...
PMC10589089
core_pubmed_pmc
Safety, pharmacokinetics, and pharmacodynamics of intravenous ferric carboxymaltose in children with iron deficiency anemia
Safety, pharmacokinetics, and pharmacodynamics of intravenous ferric carboxymaltose in children with iron deficiency anemia Abstract Abstract Background Iron deficiency is the primary cause of anemia in children. Intravenous (IV) iron formulations circumvent malabsorption and rapidly restore hemoglobin. Methods This Ph...
PMC11370791
core_pubmed_pmc
First Case of HIV Seroconversion With Integrase Resistance Mutations on Long-Acting Cabotegravir for Prevention in Routine Care
First Case of HIV Seroconversion With Integrase Resistance Mutations on Long-Acting Cabotegravir for Prevention in Routine Care Abstract Abstract Background Long-acting cabotegravir (CAB-LA) is highly effective for HIV prevention, but delayed HIV diagnoses and integrase strand transfer inhibitor (INSTI) resistance were...
PMC6955415
core_pubmed_pmc
Population pharmacokinetic modelling and simulation of fremanezumab in healthy subjects and patients with migraine
Population pharmacokinetic modelling and simulation of fremanezumab in healthy subjects and patients with migraine Abstract Abstract Aims Fremanezumab is a fully humanized IgG 2 Δa/κ monoclonal antibody specific for calcitonin gene‐related peptide developed and approved for the preventive treatment of migraine in adult...
PMC12245191
core_pubmed_pmc
Machine learning enabled multiscale model for nanoparticle margination and physiology based pharmacokinetics
Machine learning enabled multiscale model for nanoparticle margination and physiology based pharmacokinetics Abstract Abstract This study presents a multiscale modeling framework for simulating and predicting the behavior and biodistribution of nanoparticles ( NPs ), focusing on applications such as targeted drug deliv...
PMC8243284
core_pubmed_pmc
Evaluation of potential drug interactions with sodium zirconium cyclosilicate: a single-center, open-label, one sequence crossover study in healthy adults
Evaluation of potential drug interactions with sodium zirconium cyclosilicate: a single-center, open-label, one sequence crossover study in healthy adults Abstract Abstract Background Sodium zirconium cyclosilicate (SZC; formerly ZS-9) is an oral potassium binder for the treatment of hyperkalemia in adults. SZC acts in...
PMC12698583
core_pubmed_pmc
Efficacy of sulfonamides targeting malic enzyme in an animal model of Chagas disease
Efficacy of sulfonamides targeting malic enzyme in an animal model of Chagas disease Abstract Abstract Introduction Even after a century since its discovery, Chagas disease remains a major public health concern. Benznidazole and nifurtimox are the only approved treatments, but their limited efficacy and adverse effects...