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PMC5942341
core_pubmed_pmc
How are growth hormone and insulin-like growth factor-1 reported as markers for drug effectiveness in clinical acromegaly research? A comprehensive methodologic review
How are growth hormone and insulin-like growth factor-1 reported as markers for drug effectiveness in clinical acromegaly research? A comprehensive methodologic review Abstract Objective In rare disease research, most randomized prospective clinical trials can only use limited number of patients and are comprised of hi...
PMC9017352
core_pubmed_pmc
Combination of Mycobacterium tuberculosis RS Ratio and CFU Improves the Ability of Murine Efficacy Experiments to Distinguish between Drug Treatments
Combination of Mycobacterium tuberculosis RS Ratio and CFU Improves the Ability of Murine Efficacy Experiments to Distinguish between Drug Treatments Abstract ABSTRACT Murine tuberculosis drug efficacy studies have historically monitored bacterial burden based on CFU of Mycobacterium tuberculosis in lung homogenate. In...
PMC10720604
core_pubmed_pmc
Kappa opioid agonists in the treatment of itch: just scratching the surface?
Kappa opioid agonists in the treatment of itch: just scratching the surface? Abstract Chronic pruritus is a debilitating condition affecting 23–44 million Americans. Recently, kappa opioid agonists (KOAs) have emerged as a novel class of potent antipruritic agents. In 2021, the Food and Drug Administration approved dif...
PMC12796783
core_pubmed_pmc
Differences in Plasma Exposure of Cannabidiol and Cannabidiolic Acid Following Oral Administration to Horses
Differences in Plasma Exposure of Cannabidiol and Cannabidiolic Acid Following Oral Administration to Horses Abstract ABSTRACT There has been a growing interest in the use of cannabinoids in horses in recent years. Several studies have reported on the pharmacokinetics of cannabidiol (CBD) in horses. However, cannabidio...
PMC8797816
core_pubmed_pmc
Pharmacokinetics study of chitosan-coated liposomes containing sumatriptan in the treatment of migraine
Pharmacokinetics study of chitosan-coated liposomes containing sumatriptan in the treatment of migraine Abstract Abstract Background: Sumatriptan is a routine medication in the treatment of migraine and cluster headache that is generally given by oral or parental routes. However, a substantial proportion of patients su...
PMC9166308
core_pubmed_pmc
Intravenous tocilizumab for the treatment of giant cell arteritis: a phase Ib dose-ranging pharmacokinetic bridging study
Intravenous tocilizumab for the treatment of giant cell arteritis: a phase Ib dose-ranging pharmacokinetic bridging study Abstract Background Subcutaneous tocilizumab (TCZ SC) is approved globally for giant cell arteritis (GCA). This phase Ib study investigated the pharmacokinetics, pharmacodynamics, safety, and explor...
PMC12389006
core_pubmed_pmc
In Vitro and In Vivo Evaluation of Alectinib-Loaded Dendrimer Nanoparticles as a Drug Delivery System for Non-Small Cell Lung Carcinoma
In Vitro and In Vivo Evaluation of Alectinib-Loaded Dendrimer Nanoparticles as a Drug Delivery System for Non-Small Cell Lung Carcinoma Abstract Abstract Background/Objectives : Alectinib, a second-generation tyrosine kinase inhibitor indicated for the treatment of non-small-cell lung cancer (NSCLC), exhibits suboptima...
PMC9570053
core_pubmed_pmc
In Vitro/In Vivo Translation of Synergistic Combination of MDM2 and MEK Inhibitors in Melanoma Using PBPK/PD Modelling: Part II
In Vitro/In Vivo Translation of Synergistic Combination of MDM2 and MEK Inhibitors in Melanoma Using PBPK/PD Modelling: Part II Abstract Abstract The development of in vitro/in vivo translational methods for synergistically acting drug combinations is needed to identify the most effective therapeutic strategies. We per...
PMC4435993
core_pubmed_pmc
Effect of Arterial Deprivation on Growing Femoral Epiphysis: Quantitative Magnetic Resonance Imaging Using a Piglet Model
Effect of Arterial Deprivation on Growing Femoral Epiphysis: Quantitative Magnetic Resonance Imaging Using a Piglet Model Abstract Objective To investigate the usefulness of dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) and diffusion MRI for the evaluation of femoral head ischemia. Materials and Method...
PMC11031915
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic evaluation of gamithromycin against rabbit pasteurellosis
Pharmacokinetic/pharmacodynamic evaluation of gamithromycin against rabbit pasteurellosis Abstract Background Gamithromycin is an effective therapy for bovine and swine respiratory diseases but not utilized for rabbits. Given its potent activity against respiratory pathogens, we sought to determine the pharmacokinetic ...
PMC11912776
core_pubmed_pmc
Efficacy and mechanism of action of harmine derivative H-2-104 against Echinococcus granulosus infection in mice
Efficacy and mechanism of action of harmine derivative H-2-104 against Echinococcus granulosus infection in mice Abstract Background Cystic echinococcosis (CE) is a chronic zoonotic parasitic disease caused by the parasite Echinococcus granulosus ( E. granulosus ). Currently, pharmacologic treatments are limited to alb...
PMC8245695
core_pubmed_pmc
A Randomized, Double-Blind, Single-Dose Study Comparing the Biosimilarity of HOT-1010 With Bevacizumab (Avastin®) in Chinese Healthy Male Subjects
A Randomized, Double-Blind, Single-Dose Study Comparing the Biosimilarity of HOT-1010 With Bevacizumab (Avastin®) in Chinese Healthy Male Subjects Abstract Objective: This study was conducted to compare the pharmacokinetics, safety and immunogenicity of HOT-1010 with bevacizumab (Avastin®) in Chinese healthy male subje...
PMC5472793
core_pubmed_pmc
In vitro Pharmacokinetics/Pharmacodynamics Evaluation of Fosfomycin Combined with Amikacin or Colistin against KPC2-Producing Klebsiella pneumoniae
In vitro Pharmacokinetics/Pharmacodynamics Evaluation of Fosfomycin Combined with Amikacin or Colistin against KPC2-Producing Klebsiella pneumoniae Abstract Abstract Objectives: The emergence of carbapenem-resistant Enterobacteriaceae , especially Klebsiella pneumoniae , has become a major concern in clinic settings. C...
PMC5036421
core_pubmed_pmc
Levofloxacin‐Induced QTc Prolongation Depends on the Time of Drug Administration
Levofloxacin‐Induced QTc Prolongation Depends on the Time of Drug Administration Abstract Understanding the factors influencing a drug's potential to prolong the QTc interval on an electrocardiogram is essential for the correct evaluation of its safety profile. To explore the effect of dosing time on drug‐induced QTc p...
PMC7707096
core_pubmed_pmc
Anti‐tuberculosis effect of isoniazid scales accurately from zebrafish to humans
Anti‐tuberculosis effect of isoniazid scales accurately from zebrafish to humans Abstract Background and Purpose There is a clear need for innovation in anti‐tuberculosis drug development. The zebrafish larva is an attractive disease model in tuberculosis research. To translate pharmacological findings to higher verteb...
PMC12466149
core_pubmed_pmc
Therapeutic assessment of a novel mitochondrial complex I inhibitor in in vitro and in vivo models of Alzheimer's disease
Therapeutic assessment of a novel mitochondrial complex I inhibitor in in vitro and in vivo models of Alzheimer's disease Abstract Summary Background Despite recent approval of monoclonal antibodies that reduce amyloid (Aβ) accumulation, the development of disease-modifying strategies targeting the underlying mechanism...
PMC4777252
core_pubmed_pmc
Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective N ‐methyl‐D‐aspartate receptor antagonist
Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective N ‐methyl‐D‐aspartate receptor antagonist Abstract Abstract The preclinical pharmacodynamic and pharmacokinetic properties of 4‐methylbenzyl (3S, 4R)‐3‐fluoro‐4‐[(Pyrimidin‐2‐ylamino) methyl] piperidine‐1‐carboxylate ( CERC ‐301), an orally b...
PMC9008788
core_pubmed_pmc
Polyethylene Glycol‐Like Brush Polymer Conjugate of a Protein Drug Does Not Induce an Antipolymer Immune Response and Has Enhanced Pharmacokinetics than Its Polyethylene Glycol Counterpart
Polyethylene Glycol‐Like Brush Polymer Conjugate of a Protein Drug Does Not Induce an Antipolymer Immune Response and Has Enhanced Pharmacokinetics than Its Polyethylene Glycol Counterpart Abstract Abstract Protein therapeutics, except for antibodies, have a short plasma half‐life and poor stability in circulation. Cov...
PMC6403312
core_pubmed_pmc
The gravity dependence of pharmacodynamics: the integration of lidocaine into membranes in microgravity
The gravity dependence of pharmacodynamics: the integration of lidocaine into membranes in microgravity Abstract To realize long-term manned space missions, e.g. to Mars, some important questions about pharmacology under conditions of different gravity will have to be answered to ensure safe usage of pharmaceuticals. E...
PMC8809372
core_pubmed_pmc
Systems Pharmacology Modeling Identifies a Novel Treatment Strategy for Bortezomib-Induced Neuropathic Pain
Systems Pharmacology Modeling Identifies a Novel Treatment Strategy for Bortezomib-Induced Neuropathic Pain Abstract Abstract Chemotherapy-induced peripheral neurotoxicity is a common dose-limiting side effect of several cancer chemotherapeutic agents, and no effective therapies exist. Here we constructed a systems pha...
PMC7689088
core_pubmed_pmc
Randomised, double-blind, multicentre, phase Ⅰ/Ⅱ dose escalation and expansion trial of GR1501 in patients with plaque psoriasis: study protocol
Randomised, double-blind, multicentre, phase Ⅰ/Ⅱ dose escalation and expansion trial of GR1501 in patients with plaque psoriasis: study protocol Abstract Abstract Introduction Psoriasis is a life-long, immune-mediated disease that greatly reduces the quality of life of patients. Plaque psoriasis is the most common form...
PMC5446362
core_pubmed_pmc
Anticipating the Unpredictable: A Review of Antimicrobial Stewardship and Acinetobacter Infections
Anticipating the Unpredictable: A Review of Antimicrobial Stewardship and Acinetobacter Infections Abstract Acinetobacter remains one of the most challenging pathogens in the field of infectious diseases owing primarily to the uniqueness and multiplicity of its resistance mechanisms. This resistance often leads to deva...
PMC12756217
core_pubmed_pmc
Omadacycline Pharmacokinetics: Characteristics, Contributing Factors, and Clinical Significance
Omadacycline Pharmacokinetics: Characteristics, Contributing Factors, and Clinical Significance Abstract Abstract Omadacycline is a novel tetracycline with a wide range of antibacterial activity. A comprehensive understanding of the factors influencing its metabolic processes is essential to optimize its therapeutic be...
PMC10980608
core_pubmed_pmc
An Open-Label Study to Assess Monthly Risperidone Injections (180 mg) Following Switch from Daily Oral Risperidone (6 mg) in Stable Schizophrenic Patients
An Open-Label Study to Assess Monthly Risperidone Injections (180 mg) Following Switch from Daily Oral Risperidone (6 mg) in Stable Schizophrenic Patients Abstract Background and Objective Long-acting injectable antipsychotics have shown benefits over oral medications with reduced hospitalization rates and improved hea...
PMC10423691
core_pubmed_pmc
Medication adjustment of afatinib and combination therapy with sitagliptin for alleviating afatinib-induced diarrhea in rats
Medication adjustment of afatinib and combination therapy with sitagliptin for alleviating afatinib-induced diarrhea in rats Abstract Afatinib, as the first-line treatment for non-small cell lung cancer (NSCLC), causes severe gastrointestinal adverse reactions that greatly affect patients' quality of life and even pote...
PMC6585649
core_pubmed_pmc
Pharmacokinetics of Upadacitinib With the Clinical Regimens of the Extended‐Release Formulation Utilized in Rheumatoid Arthritis Phase 3 Trials
Pharmacokinetics of Upadacitinib With the Clinical Regimens of the Extended‐Release Formulation Utilized in Rheumatoid Arthritis Phase 3 Trials Abstract Abstract Upadacitinib is a Janus kinase 1 inhibitor under development for the treatment of several inflammatory disorders including rheumatoid arthritis (RA). Upadacit...
PMC5511016
core_pubmed_pmc
Pharmacodynamic genetic polymorphisms affect adverse drug reactions of haloperidol in patients with alcohol-use disorder
Pharmacodynamic genetic polymorphisms affect adverse drug reactions of haloperidol in patients with alcohol-use disorder Abstract Background Antipsychotic action of haloperidol is due to blockade of D 2 receptors in the mesolimbic dopamine pathway, while the adverse drug reactions are associated with striatal D 2 recep...
PMC8492391
core_pubmed_pmc
Pharmacokinetic properties and bioequivalence of gefitinib 250 mg in healthy Korean male subjects
Pharmacokinetic properties and bioequivalence of gefitinib 250 mg in healthy Korean male subjects Abstract Abstract Gefitinib is an anti-cancer drug used to treat non-small cell lung cancer. The objective of this study was to compare the pharmacokinetics and evaluate the bioequivalence of 2 orally administered gefitini...
PMC3215888
core_pubmed_pmc
Efficacy and pharmacokinetic/pharmacodynamic evaluation of the Aurora kinase A inhibitor MLN8237 against preclinical models of pediatric cancer
Efficacy and pharmacokinetic/pharmacodynamic evaluation of the Aurora kinase A inhibitor MLN8237 against preclinical models of pediatric cancer Abstract Purpose To gain a greater understanding of the potential of the Aurora kinase A inhibitor MLN8237 in the treatment of pediatric malignancies. Methods The activity of M...
PMC6304249
core_pubmed_pmc
Pharmacokinetic interactions and tolerability of berberine chloride with simvastatin and fenofibrate: an open-label, randomized, parallel study in healthy Chinese subjects
Pharmacokinetic interactions and tolerability of berberine chloride with simvastatin and fenofibrate: an open-label, randomized, parallel study in healthy Chinese subjects Abstract Purpose Fenofibrate (Fbt) is a prodrug that has been used to reduce low-density-lipoprotein cholesterol, triglycerides, and increase high-d...
PMC12445561
core_pubmed_pmc
First-line Selpercatinib or Chemotherapy and Pembrolizumab in Patients From East Asia With RET Fusion–Positive NSCLC: A LIBRETTO-431 Subgroup Analysis
First-line Selpercatinib or Chemotherapy and Pembrolizumab in Patients From East Asia With RET Fusion–Positive NSCLC: A LIBRETTO-431 Subgroup Analysis Abstract Introduction Selpercatinib’s consistent efficacy and manageable safety profile were observed in patients with RET fusion–positive NSCLC across geographies in si...
PMC4525301
core_pubmed_pmc
Reformulating Tylocrebrine in Epidermal Growth Factor Receptor Targeted Polymeric Nanoparticles Improves Its Therapeutic Index
Reformulating Tylocrebrine in Epidermal Growth Factor Receptor Targeted Polymeric Nanoparticles Improves Its Therapeutic Index Abstract Abstract Several promising anticancer drug candidates have been sidelined owing to their poor physicochemical properties or unfavorable pharmacokinetics, resulting in high overall cost...
PMC10689320
core_pubmed_pmc
Pharmacokinetics and Safety of the Tyrosine Kinase 2 Inhibitor Deucravacitinib in Healthy Chinese Subjects
Pharmacokinetics and Safety of the Tyrosine Kinase 2 Inhibitor Deucravacitinib in Healthy Chinese Subjects Abstract Introduction Deucravacitinib, an oral, selective, allosteric tyrosine kinase 2 inhibitor, blocks cytokine signaling involved in psoriasis pathogenesis. This ethnic-bridging study evaluated deucravacitinib...
PMC5307903
core_pubmed_pmc
Feeble Antipyretic, Analgesic, and Anti-inflammatory Activities were Found with Regular Dose 4’-O-β-D-Glucosyl-5-O-Methylvisamminol, One of the Conventional Marker Compounds for Quality Evaluation of Radix Saposhnikoviae
Feeble Antipyretic, Analgesic, and Anti-inflammatory Activities were Found with Regular Dose 4’-O-β-D-Glucosyl-5-O-Methylvisamminol, One of the Conventional Marker Compounds for Quality Evaluation of Radix Saposhnikoviae Abstract Introduction: 4’-O-β-D-glucosyl-5-O-methylvisamminol (GML) is a conventional marker compou...
PMC11527895
core_pubmed_pmc
Targeting of immune checkpoint regulator V-domain Ig suppressor of T-cell activation (VISTA) with 89 Zr-labelled CI-8993
Targeting of immune checkpoint regulator V-domain Ig suppressor of T-cell activation (VISTA) with 89 Zr-labelled CI-8993 Abstract Abstract Background CI-8993 is a fully human IgG1κ monoclonal antibody (mAb) that binds specifically to immune checkpoint molecule VISTA (V-domain Ig suppressor of T-cell activation). Phase ...
PMC7413711
core_pubmed_pmc
Effect of the sphingosine-1-phosphate receptor modulator ozanimod on leukocyte subtypes in relapsing MS
Effect of the sphingosine-1-phosphate receptor modulator ozanimod on leukocyte subtypes in relapsing MS Abstract Objective To better understand ozanimod's mechanism of action (MOA), we conducted exploratory analyses from a phase 1 study to characterize ozanimod's effect on circulating leukocyte subsets in patients with...
PMC8014105
core_pubmed_pmc
Model‐Informed Drug Development for Anti‐Infectives: State of the Art and Future
Model‐Informed Drug Development for Anti‐Infectives: State of the Art and Future Abstract Model‐informed drug development (MIDD) has a long and rich history in infectious diseases. This review describes foundational principles of translational anti‐infective pharmacology, including choice of appropriate measures of exp...
PMC12656301
core_pubmed_pmc
Visual Tracking and Organ Targeting of Naja atra and Deinagkistrodon acutus Venoms in Mice
Visual Tracking and Organ Targeting of Naja atra and Deinagkistrodon acutus Venoms in Mice Abstract In China, bites caused by the Naja atra and Deinagkistrodona acutus are the most common types of snakebites. While the functional characteristics of the two venom components have been well documented, their in vivo metab...
PMC5488123
core_pubmed_pmc
A Pharmacometric Framework for Axitinib Exposure, Efficacy, and Safety in Metastatic Renal Cell Carcinoma Patients
A Pharmacometric Framework for Axitinib Exposure, Efficacy, and Safety in Metastatic Renal Cell Carcinoma Patients Abstract Abstract The relationships between exposure, biomarkers (vascular endothelial growth factor (VEGF), soluble VEGF receptors (sVEGFR)‐1, ‐2, ‐3, and soluble stem cell factor receptor (sKIT)), tumor ...
PMC7971317
core_pubmed_pmc
Pharmacokinetic interaction between peimine and paeoniflorin in rats and its potential mechanism
Pharmacokinetic interaction between peimine and paeoniflorin in rats and its potential mechanism Abstract Abstract Context Peimine and paeoniflorin can be combined for the treatment of cough in paediatrics. The interaction during the co-administration could dramatically affect the bioavailability of drugs. Objective Th...
PMC6459286
core_pubmed_pmc
Intestinal TGR5 agonism improves hepatic steatosis and insulin sensitivity in Western diet-fed mice
Intestinal TGR5 agonism improves hepatic steatosis and insulin sensitivity in Western diet-fed mice Abstract Abstract Takeda G protein-coupled receptor 5 (TGR5) agonists induce systemic release of glucagon-like peptides (GLPs) from intestinal L cells, a potentially therapeutic action against metabolic diseases such as ...
PMC12932792
core_pubmed_pmc
Synthesis and preclinical development of a novel 68 Ga/ 89 Zr-Labelled ανβ6-integrin targeting trimer
Synthesis and preclinical development of a novel 68 Ga/ 89 Zr-Labelled ανβ6-integrin targeting trimer Abstract Abstract Background The αvβ6 integrin has emerged as a valuable target for theranostic applications in nuclear medicine with high applicability across a variety of cancers, including head-and-neck, lung, breas...
PMC11676690
core_pubmed_pmc
Inhibiting De Novo Biosynthesis of Ceramide by L-Cycloserine Can Prevent Light-Induced Retinal Degeneration in Albino BALB/c Mice
Inhibiting De Novo Biosynthesis of Ceramide by L-Cycloserine Can Prevent Light-Induced Retinal Degeneration in Albino BALB/c Mice Abstract Abstract Retinal degenerative diseases lead to irreversible vision loss due to photoreceptor cell death, driven by complex genetic and environmental factors. Ceramide, a sphingolipi...
PMC6416077
core_pubmed_pmc
Rational Reprogramming of O -Methylation Regioselectivity for Combinatorial Biosynthetic Tailoring of Benzenediol Lactone Scaffolds
Rational Reprogramming of O -Methylation Regioselectivity for Combinatorial Biosynthetic Tailoring of Benzenediol Lactone Scaffolds Abstract O- Methylation modulates the pharmacokinetic and pharmacodynamic (PK/PD) properties of small-molecule natural products, affecting their bioavailability, stability, and binding to ...
PMC9519840
core_pubmed_pmc
Pharmacokinetic Similarity between Biosimilar Insulin Aspart Premix SAR341402 Mix 70/30 and Originator Insulin Aspart Mix 70/30 (NovoMix 30) in Indian Adults with Type 2 Diabetes: GEMELLI M Substudy
Pharmacokinetic Similarity between Biosimilar Insulin Aspart Premix SAR341402 Mix 70/30 and Originator Insulin Aspart Mix 70/30 (NovoMix 30) in Indian Adults with Type 2 Diabetes: GEMELLI M Substudy Abstract Background: We compared the pharmacokinetic exposure, efficacy, safety and immunogenicity of biosimilar insulin ...
PMC12929683
core_pubmed_pmc
Can evolutionary therapy be applied in non-small cell lung cancer?
Can evolutionary therapy be applied in non-small cell lung cancer? Abstract Evolutionary therapy (ET) applies principles of evolutionary biology to steer tumour dynamics and forestall or delay treatment resistance, typically guided by data-driven mathematical models. Our aim is to assess whether ET protocols, and speci...
PMC7452813
core_pubmed_pmc
Plerixafor combined with standard regimens for hematopoietic stem cell mobilization in pediatric patients with solid tumors eligible for autologous transplants: two-arm phase I/II study (MOZAIC)
Plerixafor combined with standard regimens for hematopoietic stem cell mobilization in pediatric patients with solid tumors eligible for autologous transplants: two-arm phase I/II study (MOZAIC) Abstract Abstract This study ( NCT01288573 ) investigated plerixafor’s safety and efficacy in children with cancer. Stage 1 i...
PMC11387799
core_pubmed_pmc
Physiologically based pharmacokinetic models for systemic disposition of protein therapeutics in rabbits
Physiologically based pharmacokinetic models for systemic disposition of protein therapeutics in rabbits Abstract Physiologically based pharmacokinetic (PBPK) modelling is an important tool to predict drug disposition in the body. Rabbits play a pivotal role as a highly valued small animal model, particularly in the fi...
PMC12114195
core_pubmed_pmc
Synthesis, Experimental and Computational Evaluation of SERAAK1 as a 5-HT 2A Receptor Ligand
Synthesis, Experimental and Computational Evaluation of SERAAK1 as a 5-HT 2A Receptor Ligand Abstract Many drug discovery efforts have identified potentially promising molecules; however, a common limitation of these reports is the lack of further experimental confirmation of pharmacokinetic properties and behavioral e...
PMC4362658
core_pubmed_pmc
Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers
Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers Abstract Abstract Background Donepezil is an acetylcholinesterase inhibitor indicated for Alzheimer’s disease. The aim of this randomized, single-blind, placebo-controlled, single-dose, dose-escalation study was to investigate t...
PMC10747337
core_pubmed_pmc
The Impact of Sex on the Response to Proton Pump Inhibitor Treatment
The Impact of Sex on the Response to Proton Pump Inhibitor Treatment Abstract Abstract Proton pump inhibitor (PPI) treatment is responsible for substantial gastrin elevation secondary to reduced intragastric acidity. Due to the increasing global prevalence of PPI users, concerns have been raised about the clinical sign...
PMC8304213
core_pubmed_pmc
New In Vitro-In Silico Approach for the Prediction of In Vivo Performance of Drug Combinations
New In Vitro-In Silico Approach for the Prediction of In Vivo Performance of Drug Combinations Abstract Pharmacokinetic (PK) studies improve the design of dosing regimens in preclinical and clinical settings. In complex diseases like cancer, single-agent approaches are often insufficient for an effective treatment, and...
PMC4829189
core_pubmed_pmc
Azilsartan medoxomil in the management of hypertension: an evidence-based review of its place in therapy
Azilsartan medoxomil in the management of hypertension: an evidence-based review of its place in therapy Abstract Abstract Background Azilsartan (AZI) is a relatively new angiotensin receptor blocker available for the treatment of any stage of hypertension, which was eventually given in combination with chlorthalidone ...
PMC11379606
core_pubmed_pmc
Nanoparticle-mediated gene delivery of TRAIL to resistant cancer cells: A review
Nanoparticle-mediated gene delivery of TRAIL to resistant cancer cells: A review Abstract Abstract Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), also known as APO2L, has emerged as a highly potential anticancer agent because of its capacity to effectively trigger apoptosis in tumor cells by specifica...
PMC11209072
core_pubmed_pmc
Recent Progress on Physiologically Based Pharmacokinetic (PBPK) Model: A Review Based on Bibliometrics
Recent Progress on Physiologically Based Pharmacokinetic (PBPK) Model: A Review Based on Bibliometrics Abstract Abstract Physiologically based pharmacokinetic/toxicokinetic (PBPK/PBTK) models are designed to elucidate the mechanism of chemical compound action in organisms based on the physiological, biochemical, anatom...
PMC8262675
core_pubmed_pmc
Physiologically Based Pharmacokinetics Model in Pregnancy: A Regulatory Perspective on Model Evaluation
Physiologically Based Pharmacokinetics Model in Pregnancy: A Regulatory Perspective on Model Evaluation Abstract Abstract Physiologically based pharmacokinetics (PBPK) modelling is widely used in medicine development and regulatory submissions. The lack of clinical pharmacokinetic data in pregnancy is widely acknowledg...
PMC4402028
core_pubmed_pmc
Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline
Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline Abstract The effects of OATP1B1, OAT3, and MRP2 on the pharmacokinetics of eluxadoline, an oral, locally active, opioid receptor agonist/antagonist being developed for treatment of IBS-d were assessed in vi...
PMC9306950
core_pubmed_pmc
Effect of Roxadustat on the Pharmacokinetics of Simvastatin, Rosuvastatin, and Atorvastatin in Healthy Subjects: Results From 3 Phase 1, Open‐Label, 1‐Sequence, Crossover Studies
Effect of Roxadustat on the Pharmacokinetics of Simvastatin, Rosuvastatin, and Atorvastatin in Healthy Subjects: Results From 3 Phase 1, Open‐Label, 1‐Sequence, Crossover Studies Abstract Abstract Roxadustat inhibits breast cancer resistance protein and organic anion transporting polypeptide 1B1, which can affect coadm...
PMC7475059
core_pubmed_pmc
Pharmacokinetics of Oral Levonorgestrel in Women After Roux-en-Y Gastric Bypass Surgery and in BMI-Matched Controls
Pharmacokinetics of Oral Levonorgestrel in Women After Roux-en-Y Gastric Bypass Surgery and in BMI-Matched Controls Abstract Abstract Background Women are advised to primarily use non-oral contraceptive alternatives after Roux-en-Y gastric bypass since it is not known if the surgery affects the pharmacokinetics of oral...
PMC11789357
core_pubmed_pmc
Overview of preclinical and phase II clinical studies on Pegmolesatide’s long-term erythropoiesis stimulating effect via EPOR-mediated signal transduction
Overview of preclinical and phase II clinical studies on Pegmolesatide’s long-term erythropoiesis stimulating effect via EPOR-mediated signal transduction Abstract Introduction Anemia is a prevalent complication of chronic kidney disease (CKD), primarily due to insufficient erythropoietin (EPO). Pegmolesatide (by Hanso...
PMC10100908
core_pubmed_pmc
Functional Characterization of a Bacillus -Derived Novel Broad-Spectrum Antifungal Lipopeptide Variant against Candida tropicalis and Candida auris and Unravelling Its Mode of Action
Functional Characterization of a Bacillus -Derived Novel Broad-Spectrum Antifungal Lipopeptide Variant against Candida tropicalis and Candida auris and Unravelling Its Mode of Action Abstract ABSTRACT Limited treatment options, recalcitrance, and resistance to existing therapeutics encourage the discovery of novel anti...
PMC6222357
core_pubmed_pmc
Liquid Chromatography-Tandem Mass Spectrometry Simultaneous Determination and Pharmacokinetic Study of Fourteen Alkaloid Components in Dog Plasma after Oral Administration of Corydalis bungeana Turcz Extract
Liquid Chromatography-Tandem Mass Spectrometry Simultaneous Determination and Pharmacokinetic Study of Fourteen Alkaloid Components in Dog Plasma after Oral Administration of Corydalis bungeana Turcz Extract Abstract Abstract A rapid and sensitive Ultra high-performance liquid chromatography-tandem mass spectrometry (U...
PMC4016869
core_pubmed_pmc
In Search of the Active Metabolites of an Anticancer Piperazinedione, TW01003, in Rats
In Search of the Active Metabolites of an Anticancer Piperazinedione, TW01003, in Rats Abstract TW01003, a piperazinedione derivative designed as an antimitotic agent, exhibited potent anticancer and antiangiogenesis activities in mice. However, oral administration of this compound in rats led to poor systemic bioavail...
PMC8017437
core_pubmed_pmc
Impact of the Epithelial Lining Fluid Milieu on Amikacin Pharmacodynamics Against Pseudomonas aeruginosa
Impact of the Epithelial Lining Fluid Milieu on Amikacin Pharmacodynamics Against Pseudomonas aeruginosa Abstract Background Even though nebulised administration of amikacin can achieve high epithelial lining fluid concentrations, this has not translated into improved patient outcomes in clinical trials. One possible r...
PMC5426253
core_pubmed_pmc
Daily Mean Temperature and Urolithiasis Presentation in Six Cities in Korea: Time-Series Analysis
Daily Mean Temperature and Urolithiasis Presentation in Six Cities in Korea: Time-Series Analysis Abstract Abstract Seasonal variation in urinary stone presentation is well described in the literature. However, previous studies have some limitations. To explore overall cumulative exposure-response and the heterogeneity...
PMC10759627
core_pubmed_pmc
A network pharmacology approach to decipher the mechanism of total flavonoids from Dracocephalum Moldavica L. in the treatment of cardiovascular diseases
A network pharmacology approach to decipher the mechanism of total flavonoids from Dracocephalum Moldavica L. in the treatment of cardiovascular diseases Abstract Aim of the study Cardiovascular disease (CVD) seriously endangers human health and is characterized by high mortality and disability. The effectiveness of Dr...
PMC8945214
core_pubmed_pmc
The Role of Epigenetic Modifications in Human Cancers and the Use of Natural Compounds as Epidrugs: Mechanistic Pathways and Pharmacodynamic Actions
The Role of Epigenetic Modifications in Human Cancers and the Use of Natural Compounds as Epidrugs: Mechanistic Pathways and Pharmacodynamic Actions Abstract Abstract Cancer is a complex disease resulting from the genetic and epigenetic disruption of normal cells. The mechanistic understanding of the pathways involved ...
PMC12787101
core_pubmed_pmc
Phytochemistry, Bioactivity, and Toxicological Duality of Oxytropis glabra DC: A Review
Phytochemistry, Bioactivity, and Toxicological Duality of Oxytropis glabra DC: A Review Abstract Oxytropis glabra DC, a Fabaceae species distributed across Central Asia, is characterized by a dual biological profile encompassing pronounced toxicity alongside promising pharmacological potential. This review synthesizes ...
PMC12330440
core_pubmed_pmc
Clinical and translational study of ivosidenib plus nivolumab in advanced solid tumors harboring IDH1 mutations
Clinical and translational study of ivosidenib plus nivolumab in advanced solid tumors harboring IDH1 mutations Abstract Background: Cancers that do not respond to immunotherapy typically harbor a non-T cell-inflamed tumor microenvironment (TME), characterized by the absence of type I/II interferon (IFN) signaling and ...
PMC12108424
core_pubmed_pmc
Genetically Modified Mesenchymal Stromal/Stem Cells as a Delivery Platform for SE-33, a Cathelicidin LL-37 Analogue: Preclinical Pharmacokinetics and Tissue Distribution in C57BL/6 Mice
Genetically Modified Mesenchymal Stromal/Stem Cells as a Delivery Platform for SE-33, a Cathelicidin LL-37 Analogue: Preclinical Pharmacokinetics and Tissue Distribution in C57BL/6 Mice Abstract Background: The genetic modification of mesenchymal stromal/stem cells (MSCs) to express antimicrobial peptides may provide a...
PMC12722920
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of cannabigerol (CBG) in the C57BL/6Crl mouse
Pharmacokinetics and pharmacodynamics of cannabigerol (CBG) in the C57BL/6Crl mouse Abstract Introduction Cannabis holds therapeutic potential; however, activation of the type 1 cannabinoid receptor (CB1R) via Δ 9- tetrahydrocannabinol (THC) is also responsible for the characteristic “high” induced by cannabis. The pha...
PMC8199881
core_pubmed_pmc
Early Survival Prediction Framework in CD19-Specific CAR-T Cell Immunotherapy Using a Quantitative Systems Pharmacology Model
Early Survival Prediction Framework in CD19-Specific CAR-T Cell Immunotherapy Using a Quantitative Systems Pharmacology Model Abstract Abstract Simple Summary Treatment with chimeric antigen receptor (CAR)-T cells has improved the prognosis of patients with non-Hodgkin lymphoma (NHL) substantially. Yet, as up to 60% of...
PMC10751915
core_pubmed_pmc
A highly potent anti-VISTA antibody KVA12123 - a new immune checkpoint inhibitor and a promising therapy against poorly immunogenic tumors
A highly potent anti-VISTA antibody KVA12123 - a new immune checkpoint inhibitor and a promising therapy against poorly immunogenic tumors Abstract Background Immune checkpoint therapies have led to significant breakthroughs in cancer patient treatment in recent years. However, their efficiency is variable, and resista...
PMC12046717
core_pubmed_pmc
Combination therapy of adagrasib and abemaciclib in non-small cell lung cancer brain metastasis models genomically characterized by KRAS-G12C and homozygous loss of CDKN2A
Combination therapy of adagrasib and abemaciclib in non-small cell lung cancer brain metastasis models genomically characterized by KRAS-G12C and homozygous loss of CDKN2A Abstract KRAS mutations are prevalent in brain metastases (BM) from non-small cell lung cancer (NSCLC). The activity of KRAS-G12C selective, brain-p...
PMC11944562
core_pubmed_pmc
Model-Informed Dose Optimization of Spironolactone in Neonates and Infants
Model-Informed Dose Optimization of Spironolactone in Neonates and Infants Abstract Abstract Background/Objectives : Spironolactone (SP) has been used off-label in pediatrics since its approval, but its use is challenged by limited pharmacokinetic (PK) data in adults and especially in children. Methods : Physiologicall...
PMC8604214
core_pubmed_pmc
Pharmacokinetics, bioavailability, and bioequivalence of lower‐sodium oxybate in healthy participants in two open‐label, randomized, crossover studies
Pharmacokinetics, bioavailability, and bioequivalence of lower‐sodium oxybate in healthy participants in two open‐label, randomized, crossover studies Abstract Abstract American Academy of Sleep Medicine practice parameters designate sodium oxybate (SXB) as a standard of care for cataplexy, excessive daytime sleepiness...
PMC9929805
core_pubmed_pmc
Pharmacokinetics and bioequivalence study of montelukast sodium oral soluble film and chewable tablet in healthy Chinese volunteers: randomized trials under fasting and fed conditions
Pharmacokinetics and bioequivalence study of montelukast sodium oral soluble film and chewable tablet in healthy Chinese volunteers: randomized trials under fasting and fed conditions Abstract Abstract Background The oral soluble film (OSF) is a new drug delivery system. Whether montelukast sodium OSF has similar pharm...
PMC10338616
core_pubmed_pmc
Intraindividual Variability in Absolute Bioavailability and Clearance of Midazolam in Healthy Individuals
Intraindividual Variability in Absolute Bioavailability and Clearance of Midazolam in Healthy Individuals Abstract Background and Objective Midazolam is the preferred clinical probe drug for assessing CYP3A activity. We have previously shown substantial intraindividual variability in midazolam absolute bioavailability ...
PMC8878168
core_pubmed_pmc
In Vitro and In Vivo Studies of a Verapamil-Containing Gastroretentive Solid Foam Capsule
In Vitro and In Vivo Studies of a Verapamil-Containing Gastroretentive Solid Foam Capsule Abstract Gastroretentive systems may overcome problems associated with incomplete drug absorption by localized release of the API in the stomach. Low-density drug delivery systems can float in the gastric content and improve the b...
PMC11131050
core_pubmed_pmc
Research Note: Pharmacokinetics of bromhexine hydrochloride in broilers after single oral and intravenous administration
Research Note: Pharmacokinetics of bromhexine hydrochloride in broilers after single oral and intravenous administration Abstract The current study aimed to investigate the pharmacokinetics of bromhexine hydrochloride in broilers after single intravenous ( IV ) and oral ( PO ) administration at 2.5 mg/kg body weight (B...
PMC11787509
core_pubmed_pmc
Evaluation of fluorinated phospholipid analogs: A study on ADMET profiles, molecular docking and dynamics simulation in anticancer therapy
Evaluation of fluorinated phospholipid analogs: A study on ADMET profiles, molecular docking and dynamics simulation in anticancer therapy Abstract Abstract Fluorinated phospholipid analogs Edelfosine and Ilmofosine drug reveal expressive potential as antineoplastic factors though targeted interaction with heat shock p...
PMC11002550
core_pubmed_pmc
Antithrombotic pharmacodynamics and metabolomics study in raw and processed products of Whitmania pigra Whitman
Antithrombotic pharmacodynamics and metabolomics study in raw and processed products of Whitmania pigra Whitman Abstract Objective As a traditional Chinese medicine, leech has obvious pharmacological activities in anticoagulantion and antithrombosis. Whitmania pigra Whitman (WP) is the most commonly used leech in the C...
PMC12888855
core_pubmed_pmc
First-in-human safety and pharmacokinetics of MK-7602, the antimalarial inhibitor of plasmepsins IX/X, in single- and multiple-ascending-dose studies
First-in-human safety and pharmacokinetics of MK-7602, the antimalarial inhibitor of plasmepsins IX/X, in single- and multiple-ascending-dose studies Abstract ABSTRACT MK-7602 is a first-in-class dual-plasmepsin inhibitor being developed to treat malaria. Safety, tolerability, and pharmacokinetics (PK) of MK-7602 follo...
PMC5386618
core_pubmed_pmc
Assessment and use of drug information references in Utah pharmacies
Assessment and use of drug information references in Utah pharmacies Abstract Abstract Objective: To determine which drug references Utah pharmacists use most frequently. To determine which types of drug information questions are most commonly asked, and whether Utah pharmacists have access to adequate references to re...
PMC3215866
core_pubmed_pmc
A novel method for quantification of gemcitabine and its metabolites 2′,2′-difluorodeoxyuridine and gemcitabine triphosphate in tumour tissue by LC–MS/MS: comparison with 19 F NMR spectroscopy
A novel method for quantification of gemcitabine and its metabolites 2′,2′-difluorodeoxyuridine and gemcitabine triphosphate in tumour tissue by LC–MS/MS: comparison with 19 F NMR spectroscopy Abstract Abstract Purpose To develop a sensitive analytical method to quantify gemcitabine (2′,2′-difluorodeoxycytidine, dFdC) ...
PMC11190714
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic relationships of enrofloxacin against Klebsiella pneumoniae in an in vivo infection model in young chicks
Pharmacokinetic/pharmacodynamic relationships of enrofloxacin against Klebsiella pneumoniae in an in vivo infection model in young chicks Abstract Abstract Klebsiella pneumoniae is a serious pathogenic bacterium that poses a significant threat to young poultry and the cause of significant chick mortality and economic l...
PMC5706628
core_pubmed_pmc
Pharmacokinetic Properties of DNA Aptamers with Base Modifications
Pharmacokinetic Properties of DNA Aptamers with Base Modifications Abstract The addition of novel side chains at the 5-position of uracil is an effective means to increase chemical diversity of aptamers and hence the success rate for discovery of high-affinity ligands to protein targets. Such modifications also increas...
PMC8897023
core_pubmed_pmc
Fighting type 2 diabetes: Formulation strategies for peptide-based therapeutics
Fighting type 2 diabetes: Formulation strategies for peptide-based therapeutics Abstract Diabetes mellitus is a major health problem with increasing prevalence at a global level. The discovery of insulin in the early 1900s represented a major breakthrough in diabetes management, with further milestones being subsequent...
PMC4322610
core_pubmed_pmc
Design and in vivo evaluation of oxycodone once-a-day controlled-release tablets
Design and in vivo evaluation of oxycodone once-a-day controlled-release tablets Abstract Abstract The aim of present study was to design oxycodone once-a-day controlled-release (CR) tablets and to perform in vitro/in vivo characterizations. Release profiles to achieve desired plasma concentration versus time curves we...
PMC6402555
core_pubmed_pmc
Differences in ex-vivo Chemosensitivity to Anthracyclines in First Line Acute Myeloid Leukemia
Differences in ex-vivo Chemosensitivity to Anthracyclines in First Line Acute Myeloid Leukemia Abstract Background Induction schedules in acute myeloid leukemia (AML) are based on combinations of cytarabine and anthracyclines. The choice of the anthracycline employed has been widely studied in multiple clinical trials ...
PMC10687117
core_pubmed_pmc
The Role of Novel Antifungals in the Management of Candidiasis: A Clinical Perspective
The Role of Novel Antifungals in the Management of Candidiasis: A Clinical Perspective Abstract Abstract Mucosal and invasive candidiasis can be challenging to treat in the setting of drug intolerance, antifungal resistance, drug–drug interactions, or host immune status. Antifungals with novel mechanisms of action and ...
PMC4389578
core_pubmed_pmc
Comparison of praziquantel pharmacokinetics and tissue distribution in fresh and brackish water cultured grass carp ( ctenopharyngodon idellus ) after oral administration of single bolus
Comparison of praziquantel pharmacokinetics and tissue distribution in fresh and brackish water cultured grass carp ( ctenopharyngodon idellus ) after oral administration of single bolus Abstract Abstract Background Praziquantel (PZQ) is an effective pesticide against monogeneans. Its pharmacokinetics in fish may be af...
PMC12090559
core_pubmed_pmc
Safety, pharmacokinetics, preliminary efficacy, pharmacodynamics, and immunogenicity of QX002N, an anti-IL-17A monoclonal antibody, after short-term treatment of active ankylosing spondylitis
Safety, pharmacokinetics, preliminary efficacy, pharmacodynamics, and immunogenicity of QX002N, an anti-IL-17A monoclonal antibody, after short-term treatment of active ankylosing spondylitis Abstract Abstract Background To investigate the safety, pharmacokinetics, preliminary efficacy, pharmacodynamics, and immunogeni...
PMC4240654
core_pubmed_pmc
A Single Chain Variant of Factor VIII Fc Fusion Protein Retains Normal In Vivo Efficacy but Exhibits Altered In Vitro Activity
A Single Chain Variant of Factor VIII Fc Fusion Protein Retains Normal In Vivo Efficacy but Exhibits Altered In Vitro Activity Abstract Abstract Recombinant factor VIII Fc (rFVIIIFc) is a fusion protein consisting of a single B-domain-deleted (BDD) FVIII linked recombinantly to the Fc domain of human IgG1 to extend hal...
PMC4394613
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling of Fluorescently Labeled Block Copolymer Nanoparticles for Controlled Drug Delivery in Leukemia Therapy
Physiologically Based Pharmacokinetic Modeling of Fluorescently Labeled Block Copolymer Nanoparticles for Controlled Drug Delivery in Leukemia Therapy Abstract A physiologically based pharmacokinetic (PBPK) model was developed that describes the concentration and biodistribution of fluorescently labeled nanoparticles i...
PMC8045640
core_pubmed_pmc
Chemoprotective Antimalarial Activity of P218 against Plasmodium falciparum : A Randomized, Placebo-Controlled Volunteer Infection Study
Chemoprotective Antimalarial Activity of P218 against Plasmodium falciparum : A Randomized, Placebo-Controlled Volunteer Infection Study Abstract ABSTRACT P218 is a highly selective dihydrofolate reductase inhibitor with potent in vitro activity against pyrimethamine-resistant Plasmodium falciparum . This single-center...
PMC8214104
core_pubmed_pmc
Population pharmacokinetic modelling of indium-based quantum dot nanoparticles: preclinical in vivo studies
Population pharmacokinetic modelling of indium-based quantum dot nanoparticles: preclinical in vivo studies Abstract Abstract There is considerable interest in biomedical applications of quantum dot (QD) nanoparticles, in particular their use as imaging agents for diagnostic applications. In order to investigate the in...
PMC11492798
core_pubmed_pmc
Validation of Cefiderocol Package Insert Dosing Recommendation for Patients Receiving Continuous Renal Replacement Therapy: A Prospective Multicenter Pharmacokinetic Study
Validation of Cefiderocol Package Insert Dosing Recommendation for Patients Receiving Continuous Renal Replacement Therapy: A Prospective Multicenter Pharmacokinetic Study Abstract Abstract Background Cefiderocol is the first antibiotic with effluent flow rate–based dosing recommendations outlined in the product label ...
PMC9023527
core_pubmed_pmc
Integrated computer-aided drug design and biophysical simulation approaches to determine natural anti-bacterial compounds for Acinetobacter baumannii
Integrated computer-aided drug design and biophysical simulation approaches to determine natural anti-bacterial compounds for Acinetobacter baumannii Abstract Acinetobacter baumannii is a nosocomial bacterial pathogen and is responsible for a wide range of diseases including pneumonia, necrotizing fasciitis, meningitis...
PMC10230630
core_pubmed_pmc
Pharmacokinetic study about compatibility of Eucommia ulmoides and Psoralea corylifolia
Pharmacokinetic study about compatibility of Eucommia ulmoides and Psoralea corylifolia Abstract Abstract Objective The compatibility of Eucommia ulmoides (Eu) and Psoralea corylifolia (Pc) on the pharmacokinetic (PK) properties in the rat was explored in this study. Methods Eu extract, Pc extract and the combined extr...