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PMC6152074
core_pubmed_pmc
Structural Characterization of the Low-Molecular-Weight Heparin Dalteparin by Combining Different Analytical Strategies
Structural Characterization of the Low-Molecular-Weight Heparin Dalteparin by Combining Different Analytical Strategies Abstract A number of low molecular weight heparin (LMWH) products are available for clinical use and although all share a similar mechanism of action, they are classified as distinct drugs because of ...
PMC11680592
core_pubmed_pmc
Quinoline-thiosemicarbazone-1,2,3-triazole-acetamide derivatives as new potent α-glucosidase inhibitors
Quinoline-thiosemicarbazone-1,2,3-triazole-acetamide derivatives as new potent α-glucosidase inhibitors Abstract In this work, a novel series of quinoline-thiosemicarbazone-1,2,3-triazole-aceamide derivatives 10a-n as new potent α-glucosidase inhibitors was designed, synthesized, and evaluated. All the synthesized deri...
PMC4713719
core_pubmed_pmc
Panobinostat PK/PD profile in combination with bortezomib and dexamethasone in patients with relapsed and relapsed/refractory multiple myeloma
Panobinostat PK/PD profile in combination with bortezomib and dexamethasone in patients with relapsed and relapsed/refractory multiple myeloma Abstract Abstract Purpose Panobinostat, a potent pan-deacetylase inhibitor, improved progression-free survival (PFS) in patients with relapsed and refractory multiple myeloma wh...
PMC10146798
core_pubmed_pmc
Curcumin and Its Derivatives as Potential Antimalarial and Anti-Inflammatory Agents: A Review on Structure–Activity Relationship and Mechanism of Action
Curcumin and Its Derivatives as Potential Antimalarial and Anti-Inflammatory Agents: A Review on Structure–Activity Relationship and Mechanism of Action Abstract Abstract Curcumin, one of the major ingredients of turmeric ( Curcuma longa ), has been widely reported for its diverse bioactivities, including against malar...
PMC12435667
core_pubmed_pmc
Adherence thresholds for emtricitabine-tenofovir disoproxil fumarate preexposure prophylaxis against HIV acquisition in cisgender women: A randomized directly observed dosing study
Adherence thresholds for emtricitabine-tenofovir disoproxil fumarate preexposure prophylaxis against HIV acquisition in cisgender women: A randomized directly observed dosing study Abstract Background Oral emtricitabine/tenofovir disoproxil fumarate (F/TDF) preexposure prophylaxis (PrEP) effectiveness against HIV acqui...
PMC10213937
core_pubmed_pmc
Interaction and potential mechanisms between atorvastatin and voriconazole, agents used to treat dyslipidemia and fungal infections
Interaction and potential mechanisms between atorvastatin and voriconazole, agents used to treat dyslipidemia and fungal infections Abstract Purpose: Voriconazole (VOR) is combined with atorvastatin (ATO) to treat fungal infections in patients with dyslipidemia in clinical practice. However, the pharmacokinetic interac...
PMC9620236
core_pubmed_pmc
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors Abstract Abstract The soluble epoxide hydrolase (sEH) has been suggested as a pharmacological target for the treatment of several diseases, including pain...
PMC9907485
core_pubmed_pmc
The Impact of Extended Treatment With Artemether-lumefantrine on Antimalarial Exposure and Reinfection Risks in Ugandan Children With Uncomplicated Malaria: A Randomized Controlled Trial
The Impact of Extended Treatment With Artemether-lumefantrine on Antimalarial Exposure and Reinfection Risks in Ugandan Children With Uncomplicated Malaria: A Randomized Controlled Trial Abstract Abstract Background Artemether-lumefantrine (AL) is the most widely used artemisinin-based combination therapy in Sub-Sahara...
PMC11605395
core_pubmed_pmc
Population pharmacokinetics of rilpivirine following oral administration and long-acting intramuscular injection in real-world people with HIV
Population pharmacokinetics of rilpivirine following oral administration and long-acting intramuscular injection in real-world people with HIV Abstract Background The pharmacokinetics of long-acting rilpivirine has mostly been studied in clinical trials, which do not fully address the uncertainties that arise in routin...
PMC11130269
core_pubmed_pmc
Mechanism-based organization of neural networks to emulate systems biology and pharmacology models
Mechanism-based organization of neural networks to emulate systems biology and pharmacology models Abstract Abstract Deep learning neural networks are often described as black boxes, as it is difficult to trace model outputs back to model inputs due to a lack of clarity over the internal mechanisms. This is even true f...
PMC11946950
core_pubmed_pmc
From Prospective Evaluation to Practice: Model-Informed Dose Optimization in Oncology
From Prospective Evaluation to Practice: Model-Informed Dose Optimization in Oncology Abstract One dose does not fit all, especially in oncolytic drugs, where side effects and therapy failures highlight the need for personalized dosing approaches. In recent years, the quest to apply model-informed precision dosing to o...
PMC12009819
core_pubmed_pmc
Pharmacophore-based virtual screening and in silico investigations of small molecule library for discovery of human hepatic ketohexokinase inhibitors for the treatment of fructose metabolic disorders
Pharmacophore-based virtual screening and in silico investigations of small molecule library for discovery of human hepatic ketohexokinase inhibitors for the treatment of fructose metabolic disorders Abstract Introduction Excessive fructose consumption is a significant driver of metabolic disorders, including obesity, ...
PMC11787891
core_pubmed_pmc
Safety, tolerability and pharmacokinetics of subcutaneous cefazolin as an alternative to intravenous administration
Safety, tolerability and pharmacokinetics of subcutaneous cefazolin as an alternative to intravenous administration Abstract Abstract Background Subcutaneous (SC) administration of antibiotics is a practical alternative to IV administration. Cefazolin is widely used for skin and soft tissue infections and other complex...
PMC8041381
core_pubmed_pmc
Physiologically Based Biopharmaceutics Modeling of Regional and Colon Absorption in Dogs
Physiologically Based Biopharmaceutics Modeling of Regional and Colon Absorption in Dogs Abstract Abstract Colon absorption is a key determinant for the successful development of modified-release (MR) formulations, and the risk that colon absorption may limit the in vivo performance of an MR product can be assessed ear...
PMC8025653
core_pubmed_pmc
Gamithromycin in swine: Pharmacokinetics and clinical evaluation against swine respiratory disease
Gamithromycin in swine: Pharmacokinetics and clinical evaluation against swine respiratory disease Abstract Abstract The pharmacokinetics of gamithromycin were evaluated in 26 male castrated and female crossbred swine administered gamithromycin 15% w/v (Zactran®, Boehringer Ingelheim) intravenously at 6 mg/kg bodyweigh...
PMC12067441
core_pubmed_pmc
Discovery of NLX-266, an Orally Available and Metabolically Stable ERK1/2-Biased 5-HT 1A R Agonist with Superior Antidepressant and Antiparkinsonian Activity
Discovery of NLX-266, an Orally Available and Metabolically Stable ERK1/2-Biased 5-HT 1A R Agonist with Superior Antidepressant and Antiparkinsonian Activity Abstract Abstract We report the discovery of NLX-266 ( 31 ), an orally available and metabolically stable ERK1/2-biased 5-HT 1A receptor agonist, which demonstrat...
PMC11868598
core_pubmed_pmc
CITRINO: phase 1 dose escalation study of anti-LAG-3 antibody encelimab alone or in combination with anti-PD-1 dostarlimab in patients with advanced/metastatic solid tumours
CITRINO: phase 1 dose escalation study of anti-LAG-3 antibody encelimab alone or in combination with anti-PD-1 dostarlimab in patients with advanced/metastatic solid tumours Abstract Abstract Background Dual programmed cell death protein (ligand)-1 (PD-[L]1) and lymphocyte-activation gene-3 (LAG-3) blockade has demonst...
PMC12149652
core_pubmed_pmc
Hemodynamic subtype classification of type II endoleaks using time-enhanced curves and its association with aneurysmal enlargement
Hemodynamic subtype classification of type II endoleaks using time-enhanced curves and its association with aneurysmal enlargement Abstract Abstract Objective This study aimed to: (1) investigate the hemodynamic characteristics of type II endoleaks using mathematical simulations based on pharmacokinetic analysis; and (...
PMC10651660
core_pubmed_pmc
Application of a physiologically based pharmacokinetic model to predict isoniazid disposition during pregnancy
Application of a physiologically based pharmacokinetic model to predict isoniazid disposition during pregnancy Abstract Abstract Pregnancy can increase the risk of latent tuberculosis infection (LTBI) progression to tuberculosis (TB) disease. Isoniazid (INH) is the preferred preventative treatment for LTBI in pregnancy...
PMC5343543
core_pubmed_pmc
Efficacy, safety and population pharmacokinetics of sapropterin in PKU patients <4 years: results from the SPARK open-label, multicentre, randomized phase IIIb trial
Efficacy, safety and population pharmacokinetics of sapropterin in PKU patients <4 years: results from the SPARK open-label, multicentre, randomized phase IIIb trial Abstract Abstract Background Sapropterin dihydrochloride, a synthetic formulation of BH 4 , the cofactor for phenylalanine hydroxylase (PAH, EC 1.14.16.1)...
PMC9608689
core_pubmed_pmc
Development of a Luliconazole Nanoemulsion as a Prospective Ophthalmic Delivery System for the Treatment of Fungal Keratitis: In Vitro and In Vivo Evaluation
Development of a Luliconazole Nanoemulsion as a Prospective Ophthalmic Delivery System for the Treatment of Fungal Keratitis: In Vitro and In Vivo Evaluation Abstract Abstract Luliconazole (LCZ), a novel imidazole drug, has broad-spectrum and potential antifungal effects, which makes it a possible cure for fungal kerat...
PMC6290634
core_pubmed_pmc
Precise Dissolution Control and Bioavailability Evaluation for Insoluble Drug Berberine via a Polymeric Particle Prepared Using Supercritical CO 2
Precise Dissolution Control and Bioavailability Evaluation for Insoluble Drug Berberine via a Polymeric Particle Prepared Using Supercritical CO 2 Abstract It is still controversial whether poor aqueous solubility is the most primary reason for the low oral bioavailability of insoluble drugs. Therefore, in this study, ...
PMC10376946
core_pubmed_pmc
Advantage of First-Line Therapeutic Drug Monitoring-Driven Use of Infliximab for Treating Acute Intestinal and Liver GVHD in Children: A Prospective, Single-Center Study
Advantage of First-Line Therapeutic Drug Monitoring-Driven Use of Infliximab for Treating Acute Intestinal and Liver GVHD in Children: A Prospective, Single-Center Study Abstract Simple Summary Acute GVHD is a common life-threatening complication of allogeneic HSCT and the second most common cause of death in allogenei...
PMC7306616
core_pubmed_pmc
Leveraging Quantitative Systems Pharmacology Approach into Development of Human Recombinant Follistatin Fusion Protein for Duchenne Muscular Dystrophy
Leveraging Quantitative Systems Pharmacology Approach into Development of Human Recombinant Follistatin Fusion Protein for Duchenne Muscular Dystrophy Abstract Abstract Quantitative understanding about the dynamics of drug–target interactions in biological systems is essential, especially in rare disease programs with ...
PMC11124785
core_pubmed_pmc
Integrating Clopidogrel’s First-Pass Effect in a Joint Semi-Physiological Population Pharmacokinetic Model of the Drug and Its Inactive Carboxylic Acid Metabolite
Integrating Clopidogrel’s First-Pass Effect in a Joint Semi-Physiological Population Pharmacokinetic Model of the Drug and Its Inactive Carboxylic Acid Metabolite Abstract Clopidogrel (CLO), a pro-drug for preventing thrombotic events, undergoes rapid absorption and extensive metabolism, with approximately 85–90% conve...
PMC5192061
core_pubmed_pmc
High thioredoxin-1 levels in rheumatoid arthritis patients diminish binding and signalling of the monoclonal antibody Tregalizumab
High thioredoxin-1 levels in rheumatoid arthritis patients diminish binding and signalling of the monoclonal antibody Tregalizumab Abstract Abstract The humanized non-depleting anti-CD4 monoclonal antibody Tregalizumab (BT-061) is able to selectively activate the suppressive function of regulatory T cells and has been ...
PMC4871539
core_pubmed_pmc
Impact on Bacterial Resistance of Therapeutically Nonequivalent Generics: The Case of Piperacillin-Tazobactam
Impact on Bacterial Resistance of Therapeutically Nonequivalent Generics: The Case of Piperacillin-Tazobactam Abstract Previous studies have demonstrated that pharmaceutical equivalence and pharmacokinetic equivalence of generic antibiotics are necessary but not sufficient conditions to guarantee therapeutic equivalenc...
PMC10146250
core_pubmed_pmc
Study on the liver Drug’s dominant metabolic enzymes for six effective components of the Huang qi Liuyi decoction
Study on the liver Drug’s dominant metabolic enzymes for six effective components of the Huang qi Liuyi decoction Abstract Abstract Objective: To investigate the dominant metabolic enzymes of six effective components (astragaloside IV, glycyrrhizic acid, calycosin-glucuronide, formononetin, ononin, calycosin-7-O-β-D- g...
PMC7329787
core_pubmed_pmc
Integration of Placental Transfer in a Fetal–Maternal Physiologically Based Pharmacokinetic Model to Characterize Acetaminophen Exposure and Metabolic Clearance in the Fetus
Integration of Placental Transfer in a Fetal–Maternal Physiologically Based Pharmacokinetic Model to Characterize Acetaminophen Exposure and Metabolic Clearance in the Fetus Abstract Abstract Background and Objective Although acetaminophen is frequently used during pregnancy, little is known about fetal acetaminophen p...
PMC12833862
core_pubmed_pmc
From Discovery to Clinical Trial: YCT-529, an Oral NonHormonal Male Contraceptive Targeting the Retinoic Acid Receptor Alpha
From Discovery to Clinical Trial: YCT-529, an Oral NonHormonal Male Contraceptive Targeting the Retinoic Acid Receptor Alpha Abstract Abstract The retinoic acid receptor alpha (RARα) has emerged as a compelling genetically and pharmacologically validated target for nonhormonal male contraception due to its essential ro...
PMC3616221
core_pubmed_pmc
Proton Pump Inhibitors in Pediatrics
Proton Pump Inhibitors in Pediatrics Abstract Proton pump inhibitors (PPIs) have become some of the most frequently prescribed medications for treatment of adults and children. Their effectiveness for treatment of peptic conditions in the pediatric population, including gastric ulcers, gastroesophageal reflux disease (...
PMC10526130
core_pubmed_pmc
MRI Assessment of Changes in Tumor Vascularization during Neoadjuvant Anti-Angiogenic Treatment in Locally Advanced Breast Cancer Patients
MRI Assessment of Changes in Tumor Vascularization during Neoadjuvant Anti-Angiogenic Treatment in Locally Advanced Breast Cancer Patients Abstract Abstract Simple Summary Experimental and clinical studies have revealed that vascular endothelial growth factor (VEGF) is the predominant angiogenic factor in breast cancer...
PMC12635115
core_pubmed_pmc
Cardiotoxicity of different 5-HT3 receptor antagonists analyzed using the FAERS database and pharmacokinetic study
Cardiotoxicity of different 5-HT3 receptor antagonists analyzed using the FAERS database and pharmacokinetic study Abstract To comprehensively compare the risk of cardiotoxicity with 5-HT3 receptor antagonists (5-HT3RAs) and to explore the underlying pharmacokinetic factors that might contribute to cardiotoxicity. The ...
PMC11136735
core_pubmed_pmc
A phase 1/2 study of NS-87/CPX-351 (cytarabine and daunorubicin liposome) in Japanese patients with high-risk acute myeloid leukemia
A phase 1/2 study of NS-87/CPX-351 (cytarabine and daunorubicin liposome) in Japanese patients with high-risk acute myeloid leukemia Abstract Objectives NS-87/CPX-351 is a dual-drug liposomal encapsulation of cytarabine and daunorubicin. NS-87/CPX-351 exerts antileukemic action by maintaining a synergistic molar ratio ...
PMC9142443
core_pubmed_pmc
Long-Term Efficacy and Safety of Dupilumab in Adolescents with Moderate-to-Severe Atopic Dermatitis: Results Through Week 52 from a Phase III Open-Label Extension Trial (LIBERTY AD PED-OLE)
Long-Term Efficacy and Safety of Dupilumab in Adolescents with Moderate-to-Severe Atopic Dermatitis: Results Through Week 52 from a Phase III Open-Label Extension Trial (LIBERTY AD PED-OLE) Abstract Abstract Background For adolescent patients (aged ≥ 12 to < 18 years) with uncontrolled moderate-to-severe atopic dermati...
PMC12080569
core_pubmed_pmc
Population Pharmacokinetic-pharmacodynamic Model Analysis of Dapagliflozin for HbA1c-lowering Effects in Japanese Patients with Type 2 Diabetes Mellitus using Long-term Real-world Data
Population Pharmacokinetic-pharmacodynamic Model Analysis of Dapagliflozin for HbA1c-lowering Effects in Japanese Patients with Type 2 Diabetes Mellitus using Long-term Real-world Data Abstract Abstract Objectives: Dapagliflozin, a sodium-glucose cotransporter 2 inhibitor, has demonstrated population-level benefits in ...
PMC7015154
core_pubmed_pmc
Joint and independent neurotoxic effects of early life exposures to a chemical mixture
Joint and independent neurotoxic effects of early life exposures to a chemical mixture Abstract Supplemental Digital Content is available in the text. Keywords: Chemical mixtures, Children, G-computation, mercury, Neurodevelopment, Perfluoroalkyl substances, Superlearner Abstract Background: Exposure to mercury (Hg) is...
PMC11620678
core_pubmed_pmc
Utility of quantitative whole-body autoradiography (QWBA) and oxidative combustion (OC) analysis in the assessment of tissue distribution of [ 14 C]Mefuparib (CVL218) in SD and LE rats
Utility of quantitative whole-body autoradiography (QWBA) and oxidative combustion (OC) analysis in the assessment of tissue distribution of [ 14 C]Mefuparib (CVL218) in SD and LE rats Abstract Abstract Background In tissue distribution studies of radiopharmaceuticals, quantitative whole-body autoradiography (QWBA) and...
PMC10383682
core_pubmed_pmc
Bioanalytical LC-QTOF/MS Method for a N -phenylpiperazine Derivate (LQFM05): An Anxiolytic- and Antidepressant-like Prototype Drug Applied to Pharmacokinetic and Biodistribution Studies
Bioanalytical LC-QTOF/MS Method for a N -phenylpiperazine Derivate (LQFM05): An Anxiolytic- and Antidepressant-like Prototype Drug Applied to Pharmacokinetic and Biodistribution Studies Abstract The LQFM05 is a prototype drug designed for treatment of psychiatric disorders, such as schizophrenia, exhibiting anxiolytic-...
PMC7452555
core_pubmed_pmc
Pharmacokinetic characteristics of the triple inactivated plasma-derived Kedrion FIX concentrate: data from the KB037 clinical trial
Pharmacokinetic characteristics of the triple inactivated plasma-derived Kedrion FIX concentrate: data from the KB037 clinical trial Abstract The pharmacokinetics data of phase I/II clinical trials (EudraCT Number: 2005-006186-14) of the new, triple inactivated plasma-derived Kedrion FIX concentrate was designed accord...
PMC5306244
core_pubmed_pmc
Ocular Drug Distribution After Topical Administration: Population Pharmacokinetic Model in Rabbits
Ocular Drug Distribution After Topical Administration: Population Pharmacokinetic Model in Rabbits Abstract Abstract Background and Objective When eye diseases are treated by topical administration, the success of treatment lies in the effective drug concentration in the target tissue. This is why the drug’s pharmacoki...
PMC3385223
core_pubmed_pmc
Simultaneous Quantitative Analysis of Olmesartan Medoxomil and Amlodipine Besylate in Plasma by High-performance Liquid Chromatography Technique
Simultaneous Quantitative Analysis of Olmesartan Medoxomil and Amlodipine Besylate in Plasma by High-performance Liquid Chromatography Technique Abstract A rapid, simple and sensitive high-performance liquid chromatography (HPLC) method has been developed for quantification of olmesartan medoxomil (OLM) and amlodipine ...
PMC8305798
core_pubmed_pmc
From the Magic Bullet to Theragnostics: Certitudes and Hypotheses, Trying to Optimize the Somatostatin Model
From the Magic Bullet to Theragnostics: Certitudes and Hypotheses, Trying to Optimize the Somatostatin Model Abstract Abstract Simple Summary In oncology, the hypothetical “perfect magic bullet” should have a specific target on tumor cells which allows one to target only the tumor, in the absence of uptake in normal an...
PMC8006272
core_pubmed_pmc
Sex Proportionality in Pre-clinical and Clinical Trials: An Evaluation of 22 Marketing Authorization Application Dossiers Submitted to the European Medicines Agency
Sex Proportionality in Pre-clinical and Clinical Trials: An Evaluation of 22 Marketing Authorization Application Dossiers Submitted to the European Medicines Agency Abstract Abstract This study assessed to what extent women were included in all phases of drug development; whether the clinical studies in the marketing a...
PMC7480878
core_pubmed_pmc
Mathematical model and tool to explore shorter multi-drug therapy options for active pulmonary tuberculosis
Mathematical model and tool to explore shorter multi-drug therapy options for active pulmonary tuberculosis Abstract Abstract Standard treatment for active tuberculosis (TB) requires drug treatment with at least four drugs over six months. Shorter-duration therapy would mean less need for strict adherence, and reduced ...
PMC5935606
core_pubmed_pmc
Study on the interaction between active components from traditional Chinese medicine and plasma proteins
Study on the interaction between active components from traditional Chinese medicine and plasma proteins Abstract Abstract Traditional Chinese medicine (TCM), as a unique form of natural medicine, has been used in Chinese traditional therapeutic systems over two thousand years. Active components in Chinese herbal medic...
PMC12289775
core_pubmed_pmc
Management of cytotoxic chemotherapy in patients undergoing dialysis: a still unresolved issue of onconephrology
Management of cytotoxic chemotherapy in patients undergoing dialysis: a still unresolved issue of onconephrology Abstract Abstract The incidence of tumors increases significantly in individuals with chronic kidney disease (CKD), particularly among those undergoing dialysis. This dialysis-associated condition not only i...
PMC7478943
core_pubmed_pmc
Evaluation of patient-reported severity of hand–foot syndrome under capecitabine using a Markov modeling approach
Evaluation of patient-reported severity of hand–foot syndrome under capecitabine using a Markov modeling approach Abstract Purpose The inclusion of the patient’s perspective has become increasingly important when reporting adverse events and may assist in management of toxicity. The relationship between drug exposure a...
PMC4189701
core_pubmed_pmc
Pharmacokinetics and tolerability of the new second-generation nonnucleoside reverse- transcriptase inhibitor KM-023 in healthy subjects
Pharmacokinetics and tolerability of the new second-generation nonnucleoside reverse- transcriptase inhibitor KM-023 in healthy subjects Abstract Abstract Background KM-023 is a new second-generation nonnucleoside reverse-transcriptase inhibitor that is under development for the treatment of human immunodeficiency viru...
PMC8230177
core_pubmed_pmc
A Rational Designed Novel Bispecific Antibody for the Treatment of GBM
A Rational Designed Novel Bispecific Antibody for the Treatment of GBM Abstract Abstract Epidermal growth factor receptor variant III (EGFRvIII) is highly and specifically expressed in a subset of lethal glioblastoma (GBM), making the receptor a unique therapeutic target for GBM. Recently, bispecific antibodies (BsAbs)...
PMC8539483
core_pubmed_pmc
Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition
Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition Abstract The ATP-binding cassette (ABC) transporters play a key role in drug pharmacokinetics. These membrane transporters expressed within physiological barriers can ...
PMC12766911
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of the denosumab biosimilar FKS518 and reference denosumab in healthy subjects: the Lumiade-1 study
Pharmacokinetics and pharmacodynamics of the denosumab biosimilar FKS518 and reference denosumab in healthy subjects: the Lumiade-1 study Abstract Abstract Denosumab is a fully human monoclonal antibody that increases BMD, inhibits bone resorption and reduces fracture risk. This double-blind, randomized, parallel group...
PMC11201946
core_pubmed_pmc
Population Pharmacokinetics of Trametinib and Impact of Nonadherence on Drug Exposure in Oncology Patients as Part of the Optimizing Oral Targeted Anticancer Therapies Study
Population Pharmacokinetics of Trametinib and Impact of Nonadherence on Drug Exposure in Oncology Patients as Part of the Optimizing Oral Targeted Anticancer Therapies Study Abstract Simple Summary Poor adherence to trametinib, an oral anticancer drug, may be the consequence of side effects that severely impact the pat...
PMC12030426
core_pubmed_pmc
Translational Pharmacokinetic-Pharmacodynamic Modeling of a Novel Oral Dihydroorotate Dehydrogenase (DHODH) Inhibitor, HOSU-53 (JBZ-001)
Translational Pharmacokinetic-Pharmacodynamic Modeling of a Novel Oral Dihydroorotate Dehydrogenase (DHODH) Inhibitor, HOSU-53 (JBZ-001) Abstract Background: HOSU-53 (JBZ-001), an orally bioavailable new chemical entity, represents a highly potent dihydroorotate dehydrogenase (DHODH) inhibitor in late preclinical devel...
PMC8972168
core_pubmed_pmc
Genetic Polymorphisms and the Clinical Response to Systemic Lupus Erythematosus Treatment Towards Personalized Medicine
Genetic Polymorphisms and the Clinical Response to Systemic Lupus Erythematosus Treatment Towards Personalized Medicine Abstract Systemic lupus erythematosus (SLE) is a chronic autoimmune disease characterized by a broad spectrum of clinical manifestations, an aberrant autoimmune response to self-antigens, which affect...
PMC12035573
core_pubmed_pmc
Reconstructing population exposures to acrylamide from human monitoring data using a pharmacokinetic framework
Reconstructing population exposures to acrylamide from human monitoring data using a pharmacokinetic framework Abstract Abstract Background: Acrylamide toxicity involves several metabolic pathways. Thus, a panel of blood and urinary biomarkers for the evaluation of acrylamide exposure was deemed appropriate. Objective:...
PMC12654632
core_pubmed_pmc
Small-Molecule GLP-1 Receptor Agonists: A Promising Pharmacological Approach
Small-Molecule GLP-1 Receptor Agonists: A Promising Pharmacological Approach Abstract Glucagon-like peptide-1 receptor (GLP-1R) agonists are injectable peptide-based therapies that have become a focal point in the medical community due to their significant therapeutic efficacy in type 2 diabetes and obesity treatment. ...
PMC11944554
core_pubmed_pmc
Amikacin Dosing Adjustment in Critically Ill Oncologic Patients: A Study with Real-World Patients, PBPK Analysis, and Digital Twins
Amikacin Dosing Adjustment in Critically Ill Oncologic Patients: A Study with Real-World Patients, PBPK Analysis, and Digital Twins Abstract Background/Objectives: Guidelines recommend adjusting amikacin dosing based on patients’ renal function. Nevertheless, for critically ill cancer patients, the renal function equat...
PMC7267071
core_pubmed_pmc
Membrane Trafficking and Subcellular Drug Targeting Pathways
Membrane Trafficking and Subcellular Drug Targeting Pathways Abstract Abstract The movement of micro and macro molecules into and within a cell significantly governs several of their pharmacokinetic and pharmacodynamic parameters, thus regulating the cellular response to exogenous and endogenous stimuli. Trafficking of...
PMC10642303
core_pubmed_pmc
Development and validation of an LC–MS/MS method for the simultaneous quantification of milbemycin oxime and praziquantel in plasma: application to a pharmacokinetic study in cats
Development and validation of an LC–MS/MS method for the simultaneous quantification of milbemycin oxime and praziquantel in plasma: application to a pharmacokinetic study in cats Abstract Introduction Milbemycin oxime (MBO) and praziquantel (PZQ) have a broad spectrum of biological activity and are commonly used to tr...
PMC7031742
core_pubmed_pmc
Tolerability and pharmacokinetics of ginsenosides Rb1, Rb2, Rc, Rd, and compound K after single or multiple administration of red ginseng extract in human beings
Tolerability and pharmacokinetics of ginsenosides Rb1, Rb2, Rc, Rd, and compound K after single or multiple administration of red ginseng extract in human beings Abstract Abstract Background We investigated the tolerability and pharmacokinetic properties of various ginsenosides, including Rb1, Rb2, Rc, Rd, and compound...
PMC5963674
core_pubmed_pmc
Bioavailability of Oral Hydrocortisone Corrected for Binding Proteins and Measured by LC-MS/MS Using Serum Cortisol and Salivary Cortisone
Bioavailability of Oral Hydrocortisone Corrected for Binding Proteins and Measured by LC-MS/MS Using Serum Cortisol and Salivary Cortisone Abstract Context The assessment absolute bioavailability of oral hydrocortisone is complicated by its saturable binding to cortisol binding globulin (CBG). Previous assessment of bi...
PMC8199937
core_pubmed_pmc
Association of IgG1 Antibody Clearance with FcγRIIA Polymorphism and Platelet Count in Infliximab-Treated Patients
Association of IgG1 Antibody Clearance with FcγRIIA Polymorphism and Platelet Count in Infliximab-Treated Patients Abstract The FcγRIIA/CD32A is mainly expressed on platelets, myeloid and several endothelial cells. Its affinity is considered insufficient for allowing significant binding of monomeric IgG, while its H131...
PMC8194258
core_pubmed_pmc
Pharmacokinetics of Intraperitoneal Vancomycin and Amikacin in Automated Peritoneal Dialysis Patients With Peritonitis
Pharmacokinetics of Intraperitoneal Vancomycin and Amikacin in Automated Peritoneal Dialysis Patients With Peritonitis Abstract Abstract Objective: The study aimed to evaluate the vancomycin and amikacin concentrations in serum and dialysate for automatic peritoneal dialysis (APD) patients . Methods: A total of 558 ser...
PMC3500922
core_pubmed_pmc
Skin permeability and pharmacokinetics of diclofenac epolamine administered by dermal patch in Yorkshire-Landrace pigs
Skin permeability and pharmacokinetics of diclofenac epolamine administered by dermal patch in Yorkshire-Landrace pigs Abstract Abstract Purpose This study compared the pharmacokinetic profile, and systemic and local absorption of diclofenac, following dermal patch application and oral administration in Yorkshire-Landr...
PMC6389347
core_pubmed_pmc
A Survey of Software Tool Utilization and Capabilities for Quantitative Systems Pharmacology: What We Have and What We Need
A Survey of Software Tool Utilization and Capabilities for Quantitative Systems Pharmacology: What We Have and What We Need Abstract Quantitative systems pharmacology (QSP) is a rapidly emerging discipline with application across a spectrum of challenges facing the pharmaceutical industry, including mechanistically inf...
PMC10018608
core_pubmed_pmc
A new generation M pro inhibitor with potent activity against SARS-CoV-2 Omicron variants
A new generation M pro inhibitor with potent activity against SARS-CoV-2 Omicron variants Abstract Emerging SARS-CoV-2 variants, particularly the Omicron variant and its sublineages, continually threaten the global public health. Small molecule antivirals are an effective treatment strategy to fight against the virus. ...
PMC3775155
core_pubmed_pmc
Pharmacokinetic Drug Interactions Involving Vortioxetine (Lu AA21004), a Multimodal Antidepressant
Pharmacokinetic Drug Interactions Involving Vortioxetine (Lu AA21004), a Multimodal Antidepressant Abstract Background and Objective The identification and quantification of potential drug–drug interactions is important for avoiding or minimizing the interaction-induced adverse events associated with specific drug comb...
PMC2861941
core_pubmed_pmc
Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration
Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration Abstract Purpose To evaluate the pharmacokinetic properties of besifloxacin, gatifloxacin, and moxifloxacin in the conjunctival tissue of healthy volunteers after topical application. Methods One-hund...
PMC9532942
core_pubmed_pmc
Dose optimization of β-lactams antibiotics in pediatrics and adults: A systematic review
Dose optimization of β-lactams antibiotics in pediatrics and adults: A systematic review Abstract Abstract Background: β-lactams remain the cornerstone of the empirical therapy to treat various bacterial infections. This systematic review aimed to analyze the data describing the dosing regimen of β-lactams. Methods: Sy...
PMC4712351
core_pubmed_pmc
Morphine delays and attenuates ticagrelor exposure and action in patients with myocardial infarction: the randomized, double-blind, placebo-controlled IMPRESSION trial
Morphine delays and attenuates ticagrelor exposure and action in patients with myocardial infarction: the randomized, double-blind, placebo-controlled IMPRESSION trial Abstract Abstract Aims The currently available data indicate a drug–drug interaction between morphine and oral P2Y12 receptor inhibitors, when administe...
PMC8923172
core_pubmed_pmc
Preclinical Pharmacokinetics and Safety of Intravenous RTD-1
Preclinical Pharmacokinetics and Safety of Intravenous RTD-1 Abstract ABSTRACT Severe illness caused by coronavirus disease 2019 (COVID-19) is characterized by an overexuberant inflammatory response resulting in acute respiratory distress syndrome (ARDS) and progressive respiratory failure (A. Gupta, M. V. Madhavan, K....
PMC7028104
core_pubmed_pmc
CYP2B6 *6 Genotype Specific Differences in Artemether‐Lumefantrine Disposition in Healthy Volunteers
CYP2B6 *6 Genotype Specific Differences in Artemether‐Lumefantrine Disposition in Healthy Volunteers Abstract Abstract Cytochrome P450 2B6 (CYP2B6) is involved in the metabolism of the antimalarial drugs artemether and lumefantrine. Here we investigated the effect of CYP2B6 *6 on the plasma pharmacokinetics of artemeth...
PMC10611828
core_pubmed_pmc
Side-by-side comparison of the two widely studied GRPR radiotracers, radiolabeled NeoB and RM2, in a preclinical setting
Side-by-side comparison of the two widely studied GRPR radiotracers, radiolabeled NeoB and RM2, in a preclinical setting Abstract Abstract Introduction NeoB and RM2 are the most investigated gastrin-releasing peptide receptor (GRPR)–targeting radiotracers in preclinical and clinical studies. Therefore, an extensive sid...
PMC12135276
core_pubmed_pmc
Escalating doses of intravenous APAC demonstrate antithrombotic effect in pigs
Escalating doses of intravenous APAC demonstrate antithrombotic effect in pigs Abstract Background Locally acting antiplatelet and anticoagulant (APAC) is developed as an antithrombotic agent for administration during vascular interventions and in thrombo-inflammatory conditions. APAC has entered human studies as a dua...
PMC7916352
core_pubmed_pmc
Carbapenem Therapeutic Drug Monitoring in Critically Ill Adult Patients and Clinical Outcomes: A Systematic Review with Meta-Analysis
Carbapenem Therapeutic Drug Monitoring in Critically Ill Adult Patients and Clinical Outcomes: A Systematic Review with Meta-Analysis Abstract Abstract Drug monitoring is one strategy of antibiotic stewardship to face antimicrobial resistance. This strategy could have a determinant role in critically ill patients treat...
PMC7051945
core_pubmed_pmc
Conducting a Virtual Clinical Trial in HER2-Negative Breast Cancer Using a Quantitative Systems Pharmacology Model With an Epigenetic Modulator and Immune Checkpoint Inhibitors
Conducting a Virtual Clinical Trial in HER2-Negative Breast Cancer Using a Quantitative Systems Pharmacology Model With an Epigenetic Modulator and Immune Checkpoint Inhibitors Abstract Abstract The survival rate of patients with breast cancer has been improved by immune checkpoint blockade therapies, and the efficacy ...
PMC3428530
core_pubmed_pmc
Phase 1 study of ganitumab (AMG 479), a fully human monoclonal antibody against the insulin-like growth factor receptor type I (IGF1R), in Japanese patients with advanced solid tumors
Phase 1 study of ganitumab (AMG 479), a fully human monoclonal antibody against the insulin-like growth factor receptor type I (IGF1R), in Japanese patients with advanced solid tumors Abstract Purpose This study was to investigate the safety and tolerability of ganitumab in Japanese patients with advanced solid tumors....
PMC10755719
core_pubmed_pmc
Cerebrospinal fluid exploratory proteomics and ketamine metabolite pharmacokinetics in human volunteers after ketamine infusion
Cerebrospinal fluid exploratory proteomics and ketamine metabolite pharmacokinetics in human volunteers after ketamine infusion Abstract Summary Ketamine is a treatment for both refractory depression and chronic pain syndromes. In order to explore ketamine’s potential mechanism of action and whether ketamine or its met...
PMC12746509
core_pubmed_pmc
Safety, Pharmacokinetics, and Pharmacodynamics of Osivelotor for Sickle Cell Disease: First‐in‐Human Studies in Healthy Participants and Patients
Safety, Pharmacokinetics, and Pharmacodynamics of Osivelotor for Sickle Cell Disease: First‐in‐Human Studies in Healthy Participants and Patients Abstract The investigational agent osivelotor, a small molecule hemoglobin (Hb) modifier in development for the treatment of sickle cell disease (SCD), acts by increasing Hb‐...
PMC9286713
core_pubmed_pmc
Evaluation of drug–drug interaction potential for pemigatinib using physiologically based pharmacokinetic modeling
Evaluation of drug–drug interaction potential for pemigatinib using physiologically based pharmacokinetic modeling Abstract Abstract Pemigatinib is a potent inhibitor of fibroblast growth factor receptor being developed for oncology indications. It is primarily metabolized by cytochrome P450 (CYP) 3A4, and the ratio of...
PMC9698010
core_pubmed_pmc
Ileocolonic-Targeted JAK Inhibitor: A Safer and More Effective Treatment for Inflammatory Bowel Disease
Ileocolonic-Targeted JAK Inhibitor: A Safer and More Effective Treatment for Inflammatory Bowel Disease Abstract Abstract Janus kinase (JAK) inhibitors, such as tofacitinib (Xeljanz) and filgotinib (Jyseleca), have been approved for treatment of ulcerative colitis with several other JAK inhibitors in late-stage clinica...
PMC8485898
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of a Novel Mitochondrial Modulator, TRC150094, in Overweight and Obese Subjects: A Randomized Phase-I Clinical Trial
Safety, Tolerability, and Pharmacokinetics of a Novel Mitochondrial Modulator, TRC150094, in Overweight and Obese Subjects: A Randomized Phase-I Clinical Trial Abstract Abstract TRC150094, a novel mitochondrial modulator, can restore metabolic flexibility by improving insulin resistance in preclinical studies. This stu...
PMC5519937
core_pubmed_pmc
Acetylsalicylic acid in critically ill patients: a cross‐sectional and a randomized trial
Acetylsalicylic acid in critically ill patients: a cross‐sectional and a randomized trial Abstract Abstract Background Despite decades of clinical use, the pharmacokinetics and the effects of acetylsalicylic acid (ASA) in critically ill patients remain ill‐defined. We aimed to investigate the pharmacokinetics and the e...
PMC12491383
core_pubmed_pmc
Organ and tumour dosimetry of 177 Lu-rhPSMA-10.1, a novel PSMA-targeted therapy: results from a Phase I trial
Organ and tumour dosimetry of 177 Lu-rhPSMA-10.1, a novel PSMA-targeted therapy: results from a Phase I trial Abstract Abstract Purpose To evaluate tumour and normal organ dosimetry of PSMA-targeted RLT 177 Lu-rhPSMA-10.1. Methods PSMA-positive mCRPC patients experiencing disease progression following standard-of-care ...
PMC6790106
core_pubmed_pmc
Optimizing drug selection in psychopharmacology based on 40 significant CYP2C19- and CYP2D6-biased adverse drug reactions of selective serotonin reuptake inhibitors
Optimizing drug selection in psychopharmacology based on 40 significant CYP2C19- and CYP2D6-biased adverse drug reactions of selective serotonin reuptake inhibitors Abstract Background Selective serotonin reuptake inhibitors (SSRIs) are among the most widely prescribed class of drugs in the practice of psychiatry. Cyto...
PMC10218030
core_pubmed_pmc
Combined Effects of Multiple Per- and Polyfluoroalkyl Substances Exposure on Allostatic Load Using Bayesian Kernel Machine Regression
Combined Effects of Multiple Per- and Polyfluoroalkyl Substances Exposure on Allostatic Load Using Bayesian Kernel Machine Regression Abstract This study aims to investigate the combined effects of per- and polyfluoroalkyl substances (PFAS) on allostatic load, an index of chronic stress that is linked to several chroni...
PMC10880095
core_pubmed_pmc
Elucidation of the mechanism of action of ailanthone in the treatment of colorectal cancer: integration of network pharmacology, bioinformatics analysis and experimental validation
Elucidation of the mechanism of action of ailanthone in the treatment of colorectal cancer: integration of network pharmacology, bioinformatics analysis and experimental validation Abstract Background: Ailanthone, a small compound derived from the bark of Ailanthus altissima (Mill.) Swingle, has several anti-tumour pro...
PMC12625149
core_pubmed_pmc
Comparison of Model‐Predicted and Observed Evinacumab Pharmacokinetics and Efficacy in Children Aged < 5 Years With Homozygous Familial Hypercholesterolemia
Comparison of Model‐Predicted and Observed Evinacumab Pharmacokinetics and Efficacy in Children Aged < 5 Years With Homozygous Familial Hypercholesterolemia Abstract ABSTRACT Evinacumab, an angiopoietin‐like 3 inhibitor, significantly reduces low‐density lipoprotein cholesterol (LDL‐C) in patients with homozygous famil...
PMC6396708
core_pubmed_pmc
Translating Pharmacogenetics and Pharmacogenomics to the Clinic: Progress in Human and Veterinary Medicine
Translating Pharmacogenetics and Pharmacogenomics to the Clinic: Progress in Human and Veterinary Medicine Abstract Abstract As targeted personalized therapy becomes more widely used in human medicine, clients will expect the veterinary clinician to be able to implement an evidence-based strategy regarding both the pre...
PMC12333629
core_pubmed_pmc
Qingwen Hufei Granules Attenuate Lipopolysaccharide-Induced Acute Lung Injury by Suppressing NLRP3 Inflammasome-Dependent Pyroptosis
Qingwen Hufei Granules Attenuate Lipopolysaccharide-Induced Acute Lung Injury by Suppressing NLRP3 Inflammasome-Dependent Pyroptosis Abstract Background Currently, clinical treatments for ALI include vasodilators, glucocorticoids, and mechanical ventilation; however, these therapies are associated with various adverse ...
PMC8618518
core_pubmed_pmc
PharmVIP: A Web-Based Tool for Pharmacogenomic Variant Analysis and Interpretation
PharmVIP: A Web-Based Tool for Pharmacogenomic Variant Analysis and Interpretation Abstract Abstract The increasing availability of next generation sequencing (NGS) for personal genomics could promote pharmacogenomics (PGx) discovery and application. However, current tools for analysis and interpretation of pharmacogen...
PMC11746028
core_pubmed_pmc
LC-MS/MS assisted pharmacokinetic and tissue distribution study of ropivacaine and 3-OH-ropivacaine on rats after plane block anesthesia
LC-MS/MS assisted pharmacokinetic and tissue distribution study of ropivacaine and 3-OH-ropivacaine on rats after plane block anesthesia Abstract Knowledge of drug pharmacokinetics and tissue distribution is precious for ensuring patient safety and optimizing treatments. The varied use of local anesthetics, as well as ...
PMC12837888
core_pubmed_pmc
Multidrug-Resistant Acinetobacter baumannii : Resistance Mechanisms, Emerging Therapies, and Prevention—A Narrative Review
Multidrug-Resistant Acinetobacter baumannii : Resistance Mechanisms, Emerging Therapies, and Prevention—A Narrative Review Abstract Acinetobacter baumannii is a leading intensive care unit (ICU) pathogen associated with high rates of carbapenem resistance and poor clinical outcomes. This narrative review synthesizes re...
PMC11359152
core_pubmed_pmc
Functionalized Polymeric Micelles for Targeted Cancer Therapy: Steps from Conceptualization to Clinical Trials
Functionalized Polymeric Micelles for Targeted Cancer Therapy: Steps from Conceptualization to Clinical Trials Abstract Abstract Cancer is still ranked among the top three causes of death in the 30- to 69-year-old age group in most countries and carries considerable societal and macroeconomic costs that differ dependin...
PMC10473786
core_pubmed_pmc
How Many Patients Do You Need? Investigating Trial Designs for Anti-Seizure Treatment in Acute Brain Injury Patients
How Many Patients Do You Need? Investigating Trial Designs for Anti-Seizure Treatment in Acute Brain Injury Patients Abstract Objectives: Epileptiform activity (EA) worsens outcomes in patients with acute brain injuries (e.g., aneurysmal subarachnoid hemorrhage [aSAH]). Randomized trials (RCTs) assessing anti-seizure i...
PMC9607266
core_pubmed_pmc
Drug–Drug Interaction Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Ipatasertib in Combination with Darolutamide in Patients with Advanced Prostate Cancer
Drug–Drug Interaction Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Ipatasertib in Combination with Darolutamide in Patients with Advanced Prostate Cancer Abstract Abstract Ipatasertib is a selective, small molecule Akt inhibitor that is currently being developed for the treatment of metastatic ca...
PMC8241152
core_pubmed_pmc
Enhancing both oral bioavailability and brain penetration of puerarin using borneol in combination with preparation technologies
Enhancing both oral bioavailability and brain penetration of puerarin using borneol in combination with preparation technologies Abstract Abstract Now there are few good oral preparations of puerarin used in cerebrovascular diseases because of its poor oral absorption caused by the low water solubility and the poor pen...
PMC9138693
core_pubmed_pmc
Experimental Models for Testing the Efficacy of Pharmacological Treatments for Neonatal Hypoxic-Ischemic Encephalopathy
Experimental Models for Testing the Efficacy of Pharmacological Treatments for Neonatal Hypoxic-Ischemic Encephalopathy Abstract Abstract Representing an important cause of long–term disability, term neonatal hypoxic-ischemic encephalopathy (HIE) urgently needs further research aimed at repurposing existing drug as wel...
PMC9109889
core_pubmed_pmc
Pharmacokinetics and Safety of Single and Multiple Doses of Peficitinib (ASP015K) in Healthy Chinese Subjects
Pharmacokinetics and Safety of Single and Multiple Doses of Peficitinib (ASP015K) in Healthy Chinese Subjects Abstract Abstract Objective To investigate the pharmacokinetics and safety of peficitinib (Janus kinase inhibitor for the treatment of rheumatoid arthritis) in healthy Chinese subjects following single and mult...