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PMC10116519
core_pubmed_pmc
Prediction for Plasma Trough Concentration and Optimal Dosing of Imatinib under Multiple Clinical Situations Using Physiologically Based Pharmacokinetic Modeling
Prediction for Plasma Trough Concentration and Optimal Dosing of Imatinib under Multiple Clinical Situations Using Physiologically Based Pharmacokinetic Modeling Abstract (1) Purpose : This study aimed to develop a physiologically based pharmacokinetic (PBPK) model to predict the trough concentration ( C trough ) of im...
PMC9617823
core_pubmed_pmc
Effect of Food on the Pharmacokinetics of Senaparib (IMP4297) in Healthy Chinese Subjects
Effect of Food on the Pharmacokinetics of Senaparib (IMP4297) in Healthy Chinese Subjects Abstract Background and Objectives Data on the effect of food on the pharmacokinetics of senaparib (previously IMP4297), an oral poly (adenosine diphosphate-ribose) polymerase inhibitor, are limited. This study was conducted to ev...
PMC8953816
core_pubmed_pmc
Enhancement of the Solubility and Bioavailability of Pitavastatin through a Self-Nanoemulsifying Drug Delivery System (SNEDDS)
Enhancement of the Solubility and Bioavailability of Pitavastatin through a Self-Nanoemulsifying Drug Delivery System (SNEDDS) Abstract The purpose of the study was to develop an SNEDDS to improve the solubility and bioavailability of pitavastatin. The solubility of pitavastatin in different oils, surfactants, and co-s...
PMC11043191
core_pubmed_pmc
A Modified Delphi Study to Establish Essential Clinical Pharmacology Competencies
A Modified Delphi Study to Establish Essential Clinical Pharmacology Competencies Abstract Abstract Introduction Competency-based education has been commonly used to enhance the healthcare workforce for some time. A translational discipline that is integral to drug development and impactful on healthcare and public hea...
PMC9340768
core_pubmed_pmc
Discovery and Optimization of a Synthetic Class of Nectin-4-Targeted CD137 Agonists for Immuno-oncology
Discovery and Optimization of a Synthetic Class of Nectin-4-Targeted CD137 Agonists for Immuno-oncology Abstract Abstract CD137 (4-1BB) is a co-stimulatory receptor on immune cells and Nectin-4 is a cell adhesion molecule that is overexpressed in multiple tumor types. Using a series of poly(ethylene glycol) (PEG)-based...
PMC4614130
core_pubmed_pmc
Abnormal dopaminergic modulation of striato-cortical networks underlies levodopa-induced dyskinesias in humans
Abnormal dopaminergic modulation of striato-cortical networks underlies levodopa-induced dyskinesias in humans Abstract Abnormal dopaminergic modulation of connectivity between the putamen and cortex is thought to underlie the emergence of levodopa-induced dyskinesias. Herz et al . confirm this directly by showing that...
PMC12584216
core_pubmed_pmc
A 3D non-human primate digital model for pharmacokinetic prediction of intra-cerebrospinal fluid drug neuraxial dispersion
A 3D non-human primate digital model for pharmacokinetic prediction of intra-cerebrospinal fluid drug neuraxial dispersion Abstract Abstract Background Intra-cerebrospinal fluid (CSF) drug delivery bypasses the blood-brain barrier, making it a promising route of delivery to treat central nervous system (CNS) diseases. ...
PMC9099132
core_pubmed_pmc
A phase I evaluation of the effect of curcumin on dose‐limiting toxicity and pharmacokinetics of irinotecan in participants with solid tumors
A phase I evaluation of the effect of curcumin on dose‐limiting toxicity and pharmacokinetics of irinotecan in participants with solid tumors Abstract Abstract Curcumin inhibits UDP‐glucuronyltransferases, a primary metabolic pathway for cancer chemotherapeutic agents like irinotecan. Concurrent administration of both ...
PMC8982769
core_pubmed_pmc
Kimyrsa, An Oritavancin-Containing Product: Clinical Study and Review of Properties
Kimyrsa, An Oritavancin-Containing Product: Clinical Study and Review of Properties Abstract Abstract Background There is a need for improved antibiotic formulations for the treatment of acute bacterial skin and soft structure infection (ABSSSI), especially with the rise of antimicrobial resistance among Gram-positive ...
PMC10867185
core_pubmed_pmc
Constituents, pharmacological activities, pharmacokinetic studies, clinical applications, and safety profile on the classical prescription Kaixinsan
Constituents, pharmacological activities, pharmacokinetic studies, clinical applications, and safety profile on the classical prescription Kaixinsan Abstract Kaixinsan (KXS) is a noteworthy classical prescription, which consists of four Chinese medicinal herbs, namely Polygalae Radix, Ginseng Radix et Rhizoma, Poria, a...
PMC8992361
core_pubmed_pmc
Overcoming Stenotrophomonas maltophilia Resistance for a More Rational Therapeutic Approach
Overcoming Stenotrophomonas maltophilia Resistance for a More Rational Therapeutic Approach Abstract Abstract Stenotrophomonas maltophilia is an underappreciated source of morbidity and mortality among gram-negative pathogens. Effective treatment options with acceptable toxicity profiles are limited. Phenotypic suscept...
PMC11093219
core_pubmed_pmc
Safety, Efficacy, and Pharmacokinetics of Combination SARS-CoV-2 Neutralizing Monoclonal Antibodies BMS-986414 (C135-LS) and BMS-986413 (C144-LS) Administered Subcutaneously in Non-Hospitalized Persons with COVID-19 in a Phase 2 Trial
Safety, Efficacy, and Pharmacokinetics of Combination SARS-CoV-2 Neutralizing Monoclonal Antibodies BMS-986414 (C135-LS) and BMS-986413 (C144-LS) Administered Subcutaneously in Non-Hospitalized Persons with COVID-19 in a Phase 2 Trial Abstract Background: Outpatient COVID-19 monoclonal antibody (mAb) treatment via subc...
PMC8674127
core_pubmed_pmc
A phase 1 trial of lipid-encapsulated mRNA encoding a monoclonal antibody with neutralizing activity against Chikungunya virus
A phase 1 trial of lipid-encapsulated mRNA encoding a monoclonal antibody with neutralizing activity against Chikungunya virus Abstract Chikungunya virus (CHIKV) infection causes acute disease characterized by fever, rash and arthralgia, which progresses to severe and chronic arthritis in up to 50% of patients. Moreove...
PMC11530871
core_pubmed_pmc
Sex Differences on the Pharmacokinetics of Drugs for Children with Chronic Kidney Disease: A Narrative Review
Sex Differences on the Pharmacokinetics of Drugs for Children with Chronic Kidney Disease: A Narrative Review Abstract Abstract Effective optimal pharmacotherapy requires a comprehensive understanding of the drug’s pharmacokinetic properties. Chronic kidney disease (CKD) influences medication pharmacokinetics. However,...
PMC3457677
core_pubmed_pmc
Modification of polyethylene glycol onto solid lipid nanoparticles encapsulating a novel chemotherapeutic agent (PK-L4) to enhance solubility for injection delivery
Modification of polyethylene glycol onto solid lipid nanoparticles encapsulating a novel chemotherapeutic agent (PK-L4) to enhance solubility for injection delivery Abstract Abstract Background The synthetic potential chemotherapeutic agent 3-Chloro-4-[(4-methoxyphenyl) amino]furo[2,3-b]quinoline (PK-L4) is an analog o...
PMC12209990
core_pubmed_pmc
Effect of Cytochrome P450 3A Inhibition and Induction by Itraconazole and Rifampin on Tazemetostat Pharmacokinetics in Patients With Advanced Malignancies
Effect of Cytochrome P450 3A Inhibition and Induction by Itraconazole and Rifampin on Tazemetostat Pharmacokinetics in Patients With Advanced Malignancies Abstract Abstract This study ( NCT04537715 ) investigated itraconazole (strong cytochrome P450 [CYP] 3A inhibitor) and rifampin (strong CYP3A inducer) on tazemetosta...
PMC12434611
core_pubmed_pmc
Pharmacokinetics and Bioequivalence of Mycophenolate Sodium Enteric-Coated Tablets Under Fasting and Fed Conditions: A Single-Dose, Open-Label, Four-Period Replicated Crossover Study in Healthy Chinese Male Subjects
Pharmacokinetics and Bioequivalence of Mycophenolate Sodium Enteric-Coated Tablets Under Fasting and Fed Conditions: A Single-Dose, Open-Label, Four-Period Replicated Crossover Study in Healthy Chinese Male Subjects Abstract Aim Enteric-coated mycophenolate sodium (EC-MPS) is an immunosuppressant used to prevent organ ...
PMC9271619
core_pubmed_pmc
Better Bioactivity, Cerebral Metabolism and Pharmacokinetics of Natural Medicine and Its Advanced Version
Better Bioactivity, Cerebral Metabolism and Pharmacokinetics of Natural Medicine and Its Advanced Version Abstract Abstract Currently, many people are afflicted by cerebral diseases that cause dysfunction in the brain and perturb normal daily life of people. Cerebral diseases are greatly affected by cerebral metabolism...
PMC11055145
core_pubmed_pmc
Improving Pharmacokinetics of Peptides Using Phage Display
Improving Pharmacokinetics of Peptides Using Phage Display Abstract Abstract Phage display is a versatile method often used in the discovery of peptides that targets disease-related biomarkers. A major advantage of this technology is the ease and cost efficiency of affinity selection, also known as biopanning, to ident...
PMC5539056
core_pubmed_pmc
Nebulized antibiotics in mechanically ventilated patients: a challenge for translational research from technology to clinical care
Nebulized antibiotics in mechanically ventilated patients: a challenge for translational research from technology to clinical care Abstract Nebulized antibiotic therapy directly targets airways and lung parenchyma resulting in high local concentrations and potentially lower systemic toxicities. Experimental and clinica...
PMC9737891
core_pubmed_pmc
Neuroprotective Effects of the Psychoactive Compound Biatractylolide (BD) in Alzheimer’s Disease
Neuroprotective Effects of the Psychoactive Compound Biatractylolide (BD) in Alzheimer’s Disease Abstract Mitochondria play a central role in the survival or death of neuronal cells, and they are regulators of energy metabolism and cell death pathways. Many studies support the role of mitochondrial dysfunction and oxid...
PMC9299459
core_pubmed_pmc
Evaluation of Proton Pump Inhibitor Esomeprazole on Crizotinib Pharmacokinetics in Healthy Participants
Evaluation of Proton Pump Inhibitor Esomeprazole on Crizotinib Pharmacokinetics in Healthy Participants Abstract Abstract Crizotinib is a small‐molecule, multitargeted tyrosine kinase inhibitor that exhibits decreased aqueous solubility at a higher pH. This open‐label, randomized, phase 1 study (NCT01549574) evaluated ...
PMC8505310
core_pubmed_pmc
Activity of preclinical and phase I clinical trial of a novel androgen receptor antagonist GT0918 in metastatic breast cancer
Activity of preclinical and phase I clinical trial of a novel androgen receptor antagonist GT0918 in metastatic breast cancer Abstract Abstract Purpose To evaluate GT0918, a 2nd-generation AR antagonist, for its AR down-regulation activity among breast cancer patients. Methods The effect of GT0918 on AR protein express...
PMC7693334
core_pubmed_pmc
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models Abstract Abstract Hepatic metabolic stability is a key pharmacokinetic parameter in drug discovery. Metabolic stability is usually assessed in microsomal fractions and only the best compounds progress in the drug discovery process...
PMC7587198
core_pubmed_pmc
Protease Inhibitory Effect of Natural Polyphenolic Compounds on SARS-CoV-2: An In Silico Study
Protease Inhibitory Effect of Natural Polyphenolic Compounds on SARS-CoV-2: An In Silico Study Abstract Abstract The current pandemic, caused by SARS-CoV-2 virus, is a severe challenge for human health and the world economy. There is an urgent need for development of drugs that can manage this pandemic, as it has alrea...
PMC12270941
core_pubmed_pmc
Acute alcohol in prefrontal cortex is characterized by enhanced inhibition that transitions to excitation
Acute alcohol in prefrontal cortex is characterized by enhanced inhibition that transitions to excitation Abstract Summary Acute alcohol can have profound effects on the brain and behavior. Dorsal medial prefrontal cortex (dmPFC) function is especially sensitive to disruption from acute alcohol exposure. The acute, bro...
PMC3643872
core_pubmed_pmc
A model of HIV drug resistance driven by heterogeneities in host immunity and adherence patterns
A model of HIV drug resistance driven by heterogeneities in host immunity and adherence patterns Abstract Background Population transmission models of antiretroviral therapy (ART) and pre-exposure prophylaxis (PrEP) use simplistic assumptions – typically constant, homogeneous rates – to represent the short-term risk an...
PMC7913149
core_pubmed_pmc
Simulation-Based Assessment of the Impact of Non-Adherence on Endoxifen Target Attainment in Different Tamoxifen Dosing Strategies
Simulation-Based Assessment of the Impact of Non-Adherence on Endoxifen Target Attainment in Different Tamoxifen Dosing Strategies Abstract Abstract Tamoxifen is widely used in breast cancer treatment and minimum steady-state concentrations of its active metabolite endoxifen (C SS,min ENDX ) above 5.97 ng/mL have been ...
PMC7051932
core_pubmed_pmc
Clinical Pharmacology of Elagolix: An Oral Gonadotropin-Releasing Hormone Receptor Antagonist for Endometriosis
Clinical Pharmacology of Elagolix: An Oral Gonadotropin-Releasing Hormone Receptor Antagonist for Endometriosis Abstract Abstract The clinical pharmacology of elagolix was extensively evaluated in clinical studies in healthy subjects and in women with endometriosis. Elagolix pharmacokinetics (PK) show significant popul...
PMC8458697
core_pubmed_pmc
Influence of CYP2D6 and CYP3A5 Polymorphisms on the Pharmacokinetics and Pharmacodynamics of Bisoprolol in Hypertensive Chinese Patients
Influence of CYP2D6 and CYP3A5 Polymorphisms on the Pharmacokinetics and Pharmacodynamics of Bisoprolol in Hypertensive Chinese Patients Abstract Abstract Purpose: This study was performed to investigate the effects of common polymorphisms in CYP2D6 and CYP3A5 on the plasma concentrations and antihypertensive effects o...
PMC7873121
core_pubmed_pmc
Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview
Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview Abstract Abstract The availability of long-acting injectable (LAI) antipsychotics for the treatment of schizophrenia provides clinicians with options that deliver continuous drug exposure and may improve adherence co...
PMC4863049
core_pubmed_pmc
Adalimumab induction and maintenance therapy achieve clinical remission and response in Chinese patients with Crohn's disease
Adalimumab induction and maintenance therapy achieve clinical remission and response in Chinese patients with Crohn's disease Abstract Abstract Background/Aims This was a Phase 2 study ( NCT02015793 ) to evaluate the pharmacokinetics, safety, and efficacy of adalimumab in Chinese patients with Crohn's disease (CD). Met...
PMC7969932
core_pubmed_pmc
Population pharmacokinetics and dose optimization of vancomycin in neonates
Population pharmacokinetics and dose optimization of vancomycin in neonates Abstract The pharmacokinetics of vancomycin vary among neonates, and we aimed to conduct population pharmacokinetic analysis to determine the optimal dosage of vancomycin in Korean neonates. From a retrospective chart review, neonates treated w...
PMC7991039
core_pubmed_pmc
Adalimumab Biosimilars in the Treatment of Rheumatoid Arthritis: A Systematic Review of the Evidence for Biosimilarity
Adalimumab Biosimilars in the Treatment of Rheumatoid Arthritis: A Systematic Review of the Evidence for Biosimilarity Abstract Abstract Although treatment with biologic disease-modifying antirheumatic drugs (bDMARDs) has significantly improved clinical outcomes in patients with rheumatoid arthritis (RA), many patients...
PMC7965833
core_pubmed_pmc
Population pharmacokinetics of letermovir following oral and intravenous administration in healthy participants and allogeneic hematopoietic cell transplantation recipients
Population pharmacokinetics of letermovir following oral and intravenous administration in healthy participants and allogeneic hematopoietic cell transplantation recipients Abstract Abstract Letermovir is indicated for prophylaxis of cytomegalovirus infection and disease in allogeneic hematopoietic stem cell transplant...
PMC8380488
core_pubmed_pmc
Safety, Virologic Efficacy, and Pharmacokinetics of CT-P59, a Neutralizing Monoclonal Antibody Against SARS-CoV-2 Spike Receptor-Binding Protein: Two Randomized, Placebo-Controlled, Phase I Studies in Healthy Individuals and Patients With Mild SARS-CoV-2 Infection
Safety, Virologic Efficacy, and Pharmacokinetics of CT-P59, a Neutralizing Monoclonal Antibody Against SARS-CoV-2 Spike Receptor-Binding Protein: Two Randomized, Placebo-Controlled, Phase I Studies in Healthy Individuals and Patients With Mild SARS-CoV-2 Infection Abstract Purpose Neutralizing antibodies can reduce SAR...
PMC8149637
core_pubmed_pmc
Genetic influence of CYP2D6 on pharmacokinetics and acute subjective effects of LSD in a pooled analysis
Genetic influence of CYP2D6 on pharmacokinetics and acute subjective effects of LSD in a pooled analysis Abstract Abstract Lysergic acid diethylamide (LSD) is a classic psychedelic substance that is used recreationally and investigated in psychiatric research. There are no pharmacogenetic studies on LSD. In vitro metab...
PMC10385763
core_pubmed_pmc
Artificial Intelligence in Pharmaceutical Technology and Drug Delivery Design
Artificial Intelligence in Pharmaceutical Technology and Drug Delivery Design Abstract Abstract Artificial intelligence (AI) has emerged as a powerful tool that harnesses anthropomorphic knowledge and provides expedited solutions to complex challenges. Remarkable advancements in AI technology and machine learning prese...
PMC9052773
core_pubmed_pmc
In silico evidence of antiviral activity against SARS-CoV-2 main protease of oligosaccharides from Porphyridium sp.
In silico evidence of antiviral activity against SARS-CoV-2 main protease of oligosaccharides from Porphyridium sp. Abstract The coronavirus pandemic (COVID-19) has created an urgent need to develop effective strategies for prevention and treatment. In this context, therapies against protease M pro , a conserved viral ...
PMC6676569
core_pubmed_pmc
Population pharmacokinetics of sirolimus in pediatric patients with kaposiform hemangioendothelioma: A retrospective study
Population pharmacokinetics of sirolimus in pediatric patients with kaposiform hemangioendothelioma: A retrospective study Abstract Numerous studies have established population pharmacokinetics (PPK) models of sirolimus in various populations. However, a PPK model of sirolimus in Chinese patients with pediatric kaposif...
PMC7526832
core_pubmed_pmc
In Vitro Activity of Omadacycline, a New Tetracycline Analog, and Comparators against Clostridioides difficile
In Vitro Activity of Omadacycline, a New Tetracycline Analog, and Comparators against Clostridioides difficile Abstract Omadacycline is a potent aminomethylcycline with in vitro activity against Gram-positive, Gram-negative, and anaerobic bacteria. Preliminary data demonstrated that omadacycline has in vitro activity a...
PMC5664587
core_pubmed_pmc
Revisiting atenolol as a low passive permeability marker
Revisiting atenolol as a low passive permeability marker Abstract Background Atenolol, a hydrophilic beta blocker, has been used as a model drug for studying passive permeability of biological membranes such as the blood–brain barrier (BBB) and the intestinal epithelium. However, the extent of S-atenolol (the active en...
PMC6175296
core_pubmed_pmc
Clopidogrel but Not Prasugrel Significantly Inhibits the CYP2C8‐Mediated Metabolism of Montelukast in Humans
Clopidogrel but Not Prasugrel Significantly Inhibits the CYP2C8‐Mediated Metabolism of Montelukast in Humans Abstract Abstract The oxidation of montelukast is mainly mediated by cytochrome P450 (CYP) 2C8, but other mechanisms may contribute to its disposition. In healthy volunteers, we investigated the effects of two w...
PMC12896373
core_pubmed_pmc
Repurposing Oxfendazole for Onchocerciasis: Population Pharmacokinetics of a Tablet Formulation in Healthy African Adults
Repurposing Oxfendazole for Onchocerciasis: Population Pharmacokinetics of a Tablet Formulation in Healthy African Adults Abstract ABSTRACT Global efforts to eliminate onchocerciasis are hampered by the lack of a macrofilaricidal drug capable of killing adult parasites. Oxfendazole, a veterinary anthelminthic, exhibits...
PMC6585895
core_pubmed_pmc
Pharmacokinetics‐Pharmacodynamics of High‐Dose Ivermectin with Dihydroartemisinin‐Piperaquine on Mosquitocidal Activity and QT‐Prolongation (IVERMAL)
Pharmacokinetics‐Pharmacodynamics of High‐Dose Ivermectin with Dihydroartemisinin‐Piperaquine on Mosquitocidal Activity and QT‐Prolongation (IVERMAL) Abstract Abstract High‐dose ivermectin, co‐administered for 3 days with dihydroartemisinin‐piperaquine (DP), killed mosquitoes feeding on individuals for at least 28 days...
PMC10339510
core_pubmed_pmc
Earth-friendly micellar UPLC technique for determination of four hypoglycemic drugs in different pharmaceutical dosage forms and spiked human plasma
Earth-friendly micellar UPLC technique for determination of four hypoglycemic drugs in different pharmaceutical dosage forms and spiked human plasma Abstract A novel, sensitive, and green micellar UPLC method was proposed and validated for the simultaneous determination of four hypoglycemic agents used in type II diabe...
PMC6058699
core_pubmed_pmc
Development of novel bioadhesive granisetron hydrochloride spanlastic gel and insert for brain targeting and study their effects on rats
Development of novel bioadhesive granisetron hydrochloride spanlastic gel and insert for brain targeting and study their effects on rats Abstract Abstract The aim of this study was to formulate granisetron hydrochloride (GH) spanlastic in mucoadhesive gels and lyophilized inserts for intranasal administration to improv...
PMC5204012
core_pubmed_pmc
Acinetobacter Prosthetic Joint Infection Treated with Debridement and High-Dose Tigecycline
Acinetobacter Prosthetic Joint Infection Treated with Debridement and High-Dose Tigecycline Abstract Abstract Prosthesis retention is not recommended for multidrug-resistant Acinetobacter prosthetic joint infection due to its high failure rate. Nevertheless, replacing the prosthesis implies high morbidity and prolonged...
PMC11994481
core_pubmed_pmc
Lung-Targeted Itraconazole Delivery Using PVA-Based Nano-in-Microparticles for Improved Treatment of Pulmonary Aspergillosis
Lung-Targeted Itraconazole Delivery Using PVA-Based Nano-in-Microparticles for Improved Treatment of Pulmonary Aspergillosis Abstract Abstract Purpose Pulmonary aspergillosis (PA) presents a substantial therapeutic challenge, especially in immunocompromised patients, where conventional systemic treatments like oral and...
PMC7822074
core_pubmed_pmc
Long-Term Outcomes of Previously Treated Adult and Adolescent Patients with Severe Hemophilia A Receiving Prophylaxis with Extended Half-Life FVIII Treatments: An Economic Analysis from a United Kingdom Perspective
Long-Term Outcomes of Previously Treated Adult and Adolescent Patients with Severe Hemophilia A Receiving Prophylaxis with Extended Half-Life FVIII Treatments: An Economic Analysis from a United Kingdom Perspective Abstract Background The standard of care for patients with hemophilia A is prophylaxis with factor VIII (...
PMC8765294
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Coadministered Ruxolitinib and Artemether-Lumefantrine in Healthy Adults
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Coadministered Ruxolitinib and Artemether-Lumefantrine in Healthy Adults Abstract ABSTRACT Despite repeated malaria infection, individuals living in areas where malaria is endemic remain vulnerable to reinfection. The Janus kinase (JAK1/2) inhibitor ruxoli...
PMC10581202
core_pubmed_pmc
Subgroup analysis of phase 2 study of ceftolozane/tazobactam in neonates and young infants with pyelonephritis
Subgroup analysis of phase 2 study of ceftolozane/tazobactam in neonates and young infants with pyelonephritis Abstract ABSTRACT Ceftolozane/tazobactam is approved for the treatment of patients from birth to <18 y old with complicated urinary tract infections (cUTI). This post hoc analysis evaluated the safety, efficac...
PMC8173314
core_pubmed_pmc
In silico identification of novel chemical compounds with antituberculosis activity for the inhibition of InhA and EthR proteins from Mycobacterium tuberculosis
In silico identification of novel chemical compounds with antituberculosis activity for the inhibition of InhA and EthR proteins from Mycobacterium tuberculosis Abstract Abstract Tuberculosis (TB) continuously poses a major public health concern around the globe, with a mounting death toll of approximately 1.4 million ...
PMC4500855
core_pubmed_pmc
Potential cardiovascular adverse events when phenylephrine is combined with paracetamol: simulation and narrative review
Potential cardiovascular adverse events when phenylephrine is combined with paracetamol: simulation and narrative review Abstract Background Increased bioavailability of phenylephrine is reported when combined with paracetamol in over-the-counter formulations for the symptomatic treatment of the common cold and influen...
PMC9268445
core_pubmed_pmc
Pharmacokinetics Study of Jin-Gu-Lian Prescription and Its Core Drug Pair ( Sargentodoxa cuneata (Oliv.) Rehd. et W and Alangium chinense (Lour.) Harms) by UPLC-MS/MS
Pharmacokinetics Study of Jin-Gu-Lian Prescription and Its Core Drug Pair ( Sargentodoxa cuneata (Oliv.) Rehd. et W and Alangium chinense (Lour.) Harms) by UPLC-MS/MS Abstract Jin-Gu-Lian (JGL) is traditionally used by Miao for the treatment of rheumatism arthralgia. At the same time, the combination of Sargentodoxa cu...
PMC5591364
core_pubmed_pmc
Mitomycin C hypoxic pelvic perfusion for unresectable recurrent rectal cancer: pharmacokinetic comparison of surgical and percutaneous techniques
Mitomycin C hypoxic pelvic perfusion for unresectable recurrent rectal cancer: pharmacokinetic comparison of surgical and percutaneous techniques Abstract Abstract Patients with unresectable recurrent rectal cancer that progresses after standard and multi-modular treatments are candidates for hypoxic pelvic perfusion. ...
PMC6409996
core_pubmed_pmc
Pharmacodynamics and Pharmacokinetics of a New Type of Compound Lansoprazole Capsule in Gastric Ulcer Rats and Beagle Dogs: Importance of Adjusting Oxidative Stress and Inflammation
Pharmacodynamics and Pharmacokinetics of a New Type of Compound Lansoprazole Capsule in Gastric Ulcer Rats and Beagle Dogs: Importance of Adjusting Oxidative Stress and Inflammation Abstract The aim of this study was to investigate the pharmacodynamics and pharmacokinetics of a new type of compound lansoprazole capsule...
PMC11257179
core_pubmed_pmc
Argon pharmacokinetics: measurements in pigs and analysis in humans using a physiologically based pharmacokinetics model
Argon pharmacokinetics: measurements in pigs and analysis in humans using a physiologically based pharmacokinetics model Abstract Abstract The primary objective of this study was to investigate the pharmacokinetics of inhaled argon in young pigs using mechanical ventilation. Also a physiologically based model of argon ...
PMC4224839
core_pubmed_pmc
Evaluation of drug-drug interaction between daclatasvir and methadone or buprenorphine/naloxone
Evaluation of drug-drug interaction between daclatasvir and methadone or buprenorphine/naloxone Abstract Abstract Introduction Daclatasvir (DCV) is a potent hepatitis C virus (HCV) NS5A replication complex inhibitor with pangenotypic (1–6) activity in vitro. Methadone (MET) and buprenorphine (BUP) are opioid medication...
PMC6105166
core_pubmed_pmc
An open-label, multicenter, phase Ib study investigating the effect of apalutamide on ventricular repolarization in men with castration-resistant prostate cancer
An open-label, multicenter, phase Ib study investigating the effect of apalutamide on ventricular repolarization in men with castration-resistant prostate cancer Abstract Purpose Phase Ib study evaluating the effect of apalutamide, at therapeutic exposure, on ventricular repolarization by applying time-matched pharmaco...
PMC6040239
core_pubmed_pmc
Effect of lidocaine on kanamycin injection-site pain in patients with multidrug-resistant tuberculosis
Effect of lidocaine on kanamycin injection-site pain in patients with multidrug-resistant tuberculosis Abstract Abstract SETTING: Reducing pain from intramuscular injection of kanamycin (KM) could improve the tolerability of multidrug-resistant tuberculosis (MDR-TB) treatment. Lidocaine has been shown to be an effectiv...
PMC7995584
core_pubmed_pmc
Biologic disease modifying antirheumatic drugs and Janus kinase inhibitors in paediatric rheumatology – what we know and what we do not know from randomized controlled trials
Biologic disease modifying antirheumatic drugs and Janus kinase inhibitors in paediatric rheumatology – what we know and what we do not know from randomized controlled trials Abstract Background Biologic disease modifying antirheumatic drugs (bDMARDs) and Janus Kinase (JAK) inhibitors are prescribed in adult and paedia...
PMC5720630
core_pubmed_pmc
Extending Metformin Use in Diabetic Kidney Disease: A Pharmacokinetic Study in Stage 4 Diabetic Nephropathy
Extending Metformin Use in Diabetic Kidney Disease: A Pharmacokinetic Study in Stage 4 Diabetic Nephropathy Abstract Abstract Introduction Metformin use in advanced chronic kidney disease is controversial. This study sought to examine the pharmacokinetics, safety, and efficacy of low-dose metformin in patients with typ...
PMC7445428
core_pubmed_pmc
Simplified dolutegravir dosing for children with HIV weighing 20 kg or more: pharmacokinetic and safety substudies of the multicentre, randomised ODYSSEY trial
Simplified dolutegravir dosing for children with HIV weighing 20 kg or more: pharmacokinetic and safety substudies of the multicentre, randomised ODYSSEY trial Abstract Summary Background Paediatric dolutegravir doses approved by stringent regulatory authorities (SRAs) for children weighing 20 kg to less than 40 kg unt...
PMC8376136
core_pubmed_pmc
A population pharmacokinetic‐pharmacodynamic model of YH12852, a highly selective 5‐hydroxytryptamine 4 receptor agonist, in healthy subjects and patients with functional constipation
A population pharmacokinetic‐pharmacodynamic model of YH12852, a highly selective 5‐hydroxytryptamine 4 receptor agonist, in healthy subjects and patients with functional constipation Abstract Abstract YH12852, a novel, highly selective 5‐hydroxytryptamine 4 (5‐HT 4 ) receptor agonist, is currently under development to...
PMC10526061
core_pubmed_pmc
A Systematic Review on the Clinical Pharmacokinetics of Cephalexin in Healthy and Diseased Populations
A Systematic Review on the Clinical Pharmacokinetics of Cephalexin in Healthy and Diseased Populations Abstract Abstract Cephalexin is a first-generation β-lactam antibiotic used in adults and pediatrics to treat various streptococcal and staphylococcal infections. This review aims to summarize and evaluate all the pha...
PMC11257885
core_pubmed_pmc
Getting the dose right using physiologically-based pharmacokinetic modeling: dexamethasone to prevent post-extubation stridor in children as proof of concept
Getting the dose right using physiologically-based pharmacokinetic modeling: dexamethasone to prevent post-extubation stridor in children as proof of concept Abstract Abstract Introduction Critically ill patients show large variability in drug disposition due to e.g., age, size, disease and treatment modalities. Physio...
PMC10853450
core_pubmed_pmc
Surgical procedure of intratympanic injection and inner ear pharmacokinetics simulation in domestic pigs
Surgical procedure of intratympanic injection and inner ear pharmacokinetics simulation in domestic pigs Abstract Introduction: One major obstacle in validating drugs for the treatment or prevention of hearing loss is the limited data available on the distribution and concentration of drugs in the human inner ear. Alth...
PMC7204663
core_pubmed_pmc
Excessive lysosomal ion-trapping of hydroxychloroquine and azithromycin
Excessive lysosomal ion-trapping of hydroxychloroquine and azithromycin Abstract A recent report identified significant reductions or disappearance of viral load in COVID-19 patients given a combination of hydroxychloroquine and azithromycin. The present communication discusses some common pharmacokinetic properties of...
PMC5824342
core_pubmed_pmc
Positron Emission Tomography Imaging of Prostate Cancer with Ga-68-Labeled Gastrin-Releasing Peptide Receptor Agonist BBN 7–14 and Antagonist RM26
Positron Emission Tomography Imaging of Prostate Cancer with Ga-68-Labeled Gastrin-Releasing Peptide Receptor Agonist BBN 7–14 and Antagonist RM26 Abstract Abstract Radiolabeled bombesin (BBN) analogs have long been used for developing gastrin-releasing peptide receptor (GRPR) targeted imaging probes, and tracers with ...
PMC5571318
core_pubmed_pmc
Pharmacodynamics and Biodistribution of Single-Dose Liposomal Amphotericin B at Different Stages of Experimental Visceral Leishmaniasis
Pharmacodynamics and Biodistribution of Single-Dose Liposomal Amphotericin B at Different Stages of Experimental Visceral Leishmaniasis Abstract ABSTRACT Visceral leishmaniasis is a neglected tropical disease that causes significant morbidity and mortality worldwide. Characterization of the pharmacokinetics and pharmac...
PMC7499079
core_pubmed_pmc
Potential pharmacodynamic and pharmacokinetic interactions of Nigella Sativa and Trigonella Foenum-graecum with losartan in L-NAME induced hypertensive rats
Potential pharmacodynamic and pharmacokinetic interactions of Nigella Sativa and Trigonella Foenum-graecum with losartan in L-NAME induced hypertensive rats Abstract The objective of this investigation was to study whether Nigella Sativa and Trigonella Foenum-graecum , could modulate the losartan pharmacodynamic (PD) a...
PMC10357575
core_pubmed_pmc
Biopolymer-Capped Pyrazinamide-Loaded Colloidosomes: In Vitro Characterization and Bioavailability Studies
Biopolymer-Capped Pyrazinamide-Loaded Colloidosomes: In Vitro Characterization and Bioavailability Studies Abstract Abstract This study aimed to prepare colloidosome particles loaded with pyrazinamide (PZA). These drug-loaded colloidosomes were prepared using an in situ gelation technique using a central composite desi...
PMC8509428
core_pubmed_pmc
The Phenoxyalkyltriazine Antagonists for 5-HT 6 Receptor with Promising Procognitive and Pharmacokinetic Properties In Vivo in Search for a Novel Therapeutic Approach to Dementia Diseases
The Phenoxyalkyltriazine Antagonists for 5-HT 6 Receptor with Promising Procognitive and Pharmacokinetic Properties In Vivo in Search for a Novel Therapeutic Approach to Dementia Diseases Abstract Abstract Among the serotonin receptors, one of the most recently discovered 5-HT 6 subtype is an important protein target a...
PMC8609688
core_pubmed_pmc
Foslevodopa/Foscarbidopa Is Well Tolerated and Maintains Stable Levodopa and Carbidopa Exposure Following Subcutaneous Infusion
Foslevodopa/Foscarbidopa Is Well Tolerated and Maintains Stable Levodopa and Carbidopa Exposure Following Subcutaneous Infusion Abstract Background: Foslevodopa/foscarbidopa, formerly known as ABBV-951, is a formulation of levodopa/carbidopa prodrugs with solubility that allows for subcutaneous (SC) infusion and is in ...
PMC12919684
core_pubmed_pmc
Pharmacokinetics of Aztreonam–Avibactam After Single‐ and Multiple‐Dose Administration: A Phase 1, Open‐Label Study in Healthy Chinese Participants and Ethnic Comparison with Non‐Chinese Participants
Pharmacokinetics of Aztreonam–Avibactam After Single‐ and Multiple‐Dose Administration: A Phase 1, Open‐Label Study in Healthy Chinese Participants and Ethnic Comparison with Non‐Chinese Participants Abstract ABSTRACT Combined treatment with aztreonam (an established intravenous antibiotic) and avibactam (a β‐lactamase...
PMC7188728
core_pubmed_pmc
A phase I study investigation of metabolism, and disposition of [ 14 C]-anlotinib after an oral administration in patients with advanced refractory solid tumors
A phase I study investigation of metabolism, and disposition of [ 14 C]-anlotinib after an oral administration in patients with advanced refractory solid tumors Abstract Abstract Purpose Anlotinib is a novel oral multi-targeted receptor tyrosine kinase inhibitor, which selectively inhibits VEGFR2/3, FGFR1-4, PDGFR α/β,...
PMC7269464
core_pubmed_pmc
Pharmacokinetic-Pharmacodynamic Characterization of Omadacycline against Haemophilus influenzae Using a One-Compartment In Vitro Infection Model
Pharmacokinetic-Pharmacodynamic Characterization of Omadacycline against Haemophilus influenzae Using a One-Compartment In Vitro Infection Model Abstract Omadacycline is a novel aminomethylcycline with activity against Gram-positive and -negative organisms, including Haemophilus influenzae , which is one of the leading...
PMC9245728
core_pubmed_pmc
Dose Proportionality and Steady-State Pharmacokinetics of Serdexmethylphenidate/Dexmethylphenidate, a Novel Prodrug Combination to Treat Attention-Deficit/Hyperactivity Disorder
Dose Proportionality and Steady-State Pharmacokinetics of Serdexmethylphenidate/Dexmethylphenidate, a Novel Prodrug Combination to Treat Attention-Deficit/Hyperactivity Disorder Abstract Objective: The study was designed to determine (1) the pharmacokinetic (PK) profile of dexmethylphenidate (d-MPH) after oral administ...
PMC7599917
core_pubmed_pmc
Gellan Gum Promotes the Differentiation of Enterocytes from Human Induced Pluripotent Stem Cells
Gellan Gum Promotes the Differentiation of Enterocytes from Human Induced Pluripotent Stem Cells Abstract The evaluation of drug pharmacokinetics in the small intestine is critical for developing orally administered drugs. Caucasian colon adenocarcinoma (Caco-2) cells are employed to evaluate drug absorption in preclin...
PMC8227856
core_pubmed_pmc
Antibacterial Activity of a Promising Antibacterial Agent: 22-(4-(2-(4-Nitrophenyl-piperazin-1-yl)-acetyl)-piperazin-1-yl)-22-deoxypleuromutilin
Antibacterial Activity of a Promising Antibacterial Agent: 22-(4-(2-(4-Nitrophenyl-piperazin-1-yl)-acetyl)-piperazin-1-yl)-22-deoxypleuromutilin Abstract Abstract A novel pleuromutilin derivative, 22-(4-(2-(4-nitrophenyl-piperazin-1-yl)-acetyl)-piperazin-1-yl)-22-deoxypleuromutilin (NPDM), was synthesized in our labora...
PMC6151824
core_pubmed_pmc
Glycyrrhetinic Acid Liposomes Containing Mannose-Diester Lauric Diacid-Cholesterol Conjugate Synthesized by Lipase-Catalytic Acylation for Liver-Specific Delivery
Glycyrrhetinic Acid Liposomes Containing Mannose-Diester Lauric Diacid-Cholesterol Conjugate Synthesized by Lipase-Catalytic Acylation for Liver-Specific Delivery Abstract Abstract Mannose-diester lauric diacid-cholesterol (Man-DLD-Chol), as a liposomal target ligand, was synthesized by lipase catalyzed in a non-aqueou...
PMC7032223
core_pubmed_pmc
Development of a method to quantify total and free irinotecan and 7-ethyl-10-hydroxycamptothecin (SN-38) for pharmacokinetic and bio-distribution studies after administration of irinotecan liposomal formulation
Development of a method to quantify total and free irinotecan and 7-ethyl-10-hydroxycamptothecin (SN-38) for pharmacokinetic and bio-distribution studies after administration of irinotecan liposomal formulation Abstract Abstract In 2015, liposomal formulation of irinotecan (ONIVYDE) has been approved by FDA and widely ...
PMC11384982
core_pubmed_pmc
Optimising infliximab induction dosing to achieve clinical remission in Chinese patients with Crohn’s disease
Optimising infliximab induction dosing to achieve clinical remission in Chinese patients with Crohn’s disease Abstract Aims A strategy based on therapeutic drug monitoring and population pharmacokinetic (popPK) models would likely increase the rate of clinical remission (CR) after infliximab (IFX) induction in patients...
PMC12570999
core_pubmed_pmc
Cyp3a4-Mediated in vitro Metabolism and in vivo Disposition of Lorlatinib in Rats
Cyp3a4-Mediated in vitro Metabolism and in vivo Disposition of Lorlatinib in Rats Abstract Abstract Purpose Lorlatinib, a third-generation inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1), undergoes extensive metabolism, with its disposition influenced by drug–drug interactions (DDIs). This stu...
PMC3228569
core_pubmed_pmc
Trichloroethylene and Cancer: Systematic and Quantitative Review of Epidemiologic Evidence for Identifying Hazards
Trichloroethylene and Cancer: Systematic and Quantitative Review of Epidemiologic Evidence for Identifying Hazards Abstract We conducted a meta-analysis focusing on studies with high potential for trichloroethylene (TCE) exposure to provide quantitative evaluations of the evidence for associations between TCE exposure ...
PMC4341874
core_pubmed_pmc
Are standard doses of piperacillin sufficient for critically ill patients with augmented creatinine clearance?
Are standard doses of piperacillin sufficient for critically ill patients with augmented creatinine clearance? Abstract Abstract Introduction The aim of this study was to explore the impact of augmented creatinine clearance and differing minimum inhibitory concentrations (MIC) on piperacillin pharmacokinetic/pharmacody...
PMC12494133
core_pubmed_pmc
Population pharmacokinetics of bictegravir in real-world people with HIV
Population pharmacokinetics of bictegravir in real-world people with HIV Abstract Abstract Objectives Bictegravir is an integrase strand transfer inhibitor widely prescribed due to its good efficacy and safety profile. Its pharmacokinetic (PK) profile has not been described in real-world settings yet. This study aimed ...
PMC8481739
core_pubmed_pmc
Comparative Bioavailability and Pharmacokinetics Between the Solid Form of Metformin vs a Novel Liquid Extemporaneous Formulation in Children
Comparative Bioavailability and Pharmacokinetics Between the Solid Form of Metformin vs a Novel Liquid Extemporaneous Formulation in Children Abstract Abstract Metformin pharmacokinetics in a liquid extemporaneous formulation from commercial tablets was determined in paediatric patients. A randomized, transversal clini...
PMC6766590
core_pubmed_pmc
Protocatechuic acid from chicory is bioavailable and undergoes partial glucuronidation and sulfation in healthy humans
Protocatechuic acid from chicory is bioavailable and undergoes partial glucuronidation and sulfation in healthy humans Abstract Abstract Protocatechuic acid exerts multiple health‐promoting effects such as anticancer, anti‐atherosclerosis, and neuroprotection in animal models. While protocatechuic acid produced in the ...
PMC7316526
core_pubmed_pmc
Operative Gynecological Laparoscopy Under Conscious Sedation
Operative Gynecological Laparoscopy Under Conscious Sedation Abstract Background and Objectives: Operative laparoscopy is generally performed under general anesthesia. Local anesthesia and conscious sedation may be useful in select short procedures. In the present study, we evaluated safety and efficacy of operative la...
PMC3229549
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of VEGF-neutralizing antibodies
Pharmacokinetics and pharmacodynamics of VEGF-neutralizing antibodies Abstract Abstract Background Vascular endothelial growth factor (VEGF) is a potent regulator of angiogenesis, and its role in cancer biology has been widely studied. Many cancer therapies target angiogenesis, with a focus being on VEGF-mediated signa...
PMC12872619
core_pubmed_pmc
Burixafor, a CXCR4 inhibitor with a differentiated kinetics profile: results of a phase 2 study for rapid cell mobilization in multiple myeloma and lymphoma patients undergoing transplant
Burixafor, a CXCR4 inhibitor with a differentiated kinetics profile: results of a phase 2 study for rapid cell mobilization in multiple myeloma and lymphoma patients undergoing transplant Abstract Abstract Inhibitors of C-X-C chemokine receptor type 4 (CXCR4) are standard of care for mobilization of hematopoietic stem ...
PMC12355006
core_pubmed_pmc
The Application of Mesoporous Silica Nanoparticles in Enhancing the Efficacy of Anti-Atherosclerosis Therapies: A Review
The Application of Mesoporous Silica Nanoparticles in Enhancing the Efficacy of Anti-Atherosclerosis Therapies: A Review Abstract Abstract Atherosclerosis (AS) is a chronic inflammatory condition of large arteries and a major contributor to cardiovascular disease (CVD) and stroke. The prevention of AS diseases involves...
PMC8540141
core_pubmed_pmc
Variants in COMT , CYP3A5 , CYP2B6, and ABCG2 Alter Quetiapine Pharmacokinetics
Variants in COMT , CYP3A5 , CYP2B6, and ABCG2 Alter Quetiapine Pharmacokinetics Abstract Abstract Quetiapine is an atypical antipsychotic widely used for the treatment of schizophrenia and the depressive episodes of bipolar disorder. The aim of this work was to investigate the effect of variants in relevant pharmacogen...
PMC5114206
core_pubmed_pmc
An Updated Overview on Therapeutic Drug Monitoring of Recent Antiepileptic Drugs
An Updated Overview on Therapeutic Drug Monitoring of Recent Antiepileptic Drugs Abstract Abstract Given the distinctive characteristics of both epilepsy and antiepileptic drugs (AEDs), therapeutic drug monitoring (TDM) can make a significant contribution to the field of epilepsy. The measurement and interpretation of ...
PMC5089583
core_pubmed_pmc
Brentuximab vedotin, an antibody–drug conjugate, in patients with CD30‐positive haematologic malignancies and hepatic or renal impairment
Brentuximab vedotin, an antibody–drug conjugate, in patients with CD30‐positive haematologic malignancies and hepatic or renal impairment Abstract Abstract Aims Brentuximab vedotin, an antibody–drug conjugate (ADC), selectively delivers the microtubule‐disrupting agent monomethyl auristatin E (MMAE) into CD30‐expressin...
PMC8512154
core_pubmed_pmc
Fabrication and Characterization of Paclitaxel and Resveratrol Loaded Soluplus Polymeric Nanoparticles for Improved BBB Penetration for Glioma Management
Fabrication and Characterization of Paclitaxel and Resveratrol Loaded Soluplus Polymeric Nanoparticles for Improved BBB Penetration for Glioma Management Abstract Abstract Gliomas are one of the prominent cancers of the central nervous system with limited therapeutic modalities. The present investigation evaluated the ...
PMC10361232
core_pubmed_pmc
Natural fulvic acids inhibit non-small-cell lung cancer through the COX-2/PGE2/EP4 axis: In silico and in vivo assessments
Natural fulvic acids inhibit non-small-cell lung cancer through the COX-2/PGE2/EP4 axis: In silico and in vivo assessments Abstract Abstract Purpose Non-small-cell lung cancer (NSCLC) is a major public health concern with a high incidence worldwide. Coal-derived fulvic acids (FAs) contain functional groups in their che...
PMC12032439
core_pubmed_pmc
Comparative Analysis of Adverse Event Profiles Among Seven Statins for Hypercholesterolemia Management Using the United States FDA Adverse Event Reporting System
Comparative Analysis of Adverse Event Profiles Among Seven Statins for Hypercholesterolemia Management Using the United States FDA Adverse Event Reporting System Abstract Abstract Background Statins are fundamental in hypercholesterolemia management, with seven primary drugs available: atorvastatin, simvastatin, rosuva...