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PMC10317875
core_pubmed_pmc
PET imaging of PARP expression using 68 Ga-labelled inhibitors
PET imaging of PARP expression using 68 Ga-labelled inhibitors Abstract Purpose Imaging the PARP expression using 18 F probes has been approved in clinical trials. Nevertheless, hepatobiliary clearance of both 18 F probes hindered their application in monitoring abdominal lesions. Our novel 68 Ga-labelled probes aim fo...
PMC8245910
core_pubmed_pmc
Preclinical efficacy against acute myeloid leukaemia of SH1573, a novel mutant IDH2 inhibitor approved for clinical trials in China
Preclinical efficacy against acute myeloid leukaemia of SH1573, a novel mutant IDH2 inhibitor approved for clinical trials in China Abstract Acute myeloid leukaemia (AML) is the most common form of acute leukaemia in adults, with increasing incidence with age and a generally poor prognosis. Almost 20% of AML patients e...
PMC5408714
core_pubmed_pmc
A Robust Pneumonia Model in Immunocompetent Rodents to Evaluate Antibacterial Efficacy against S. pneumoniae , H. influenzae , K. pneumoniae , P. aeruginosa or A. baumannii
A Robust Pneumonia Model in Immunocompetent Rodents to Evaluate Antibacterial Efficacy against S. pneumoniae , H. influenzae , K. pneumoniae , P. aeruginosa or A. baumannii Abstract Abstract Efficacy of candidate antibacterial treatments must be demonstrated in animal models of infection as part of the discovery and de...
PMC3110312
core_pubmed_pmc
Orange Juice and Its Component, Hesperidin, Decrease the Expression of Multidrug Resistance-Associated Protein 2 in Rat Small Intestine and Liver
Orange Juice and Its Component, Hesperidin, Decrease the Expression of Multidrug Resistance-Associated Protein 2 in Rat Small Intestine and Liver Abstract Abstract We investigated the effects of orange juice (OJ) or hesperidin, a component of OJ, on the pharmacokinetics of pravastatin (PRV) and the expression of both p...
PMC3249185
core_pubmed_pmc
Optimal dose finding of garenoxacin based on population pharmacokinetics/pharmacodynamics and Monte Carlo simulation
Optimal dose finding of garenoxacin based on population pharmacokinetics/pharmacodynamics and Monte Carlo simulation Abstract Abstract Purpose Garenoxacin, a novel des-F(6)-quinolone, possesses potent antibacterial activity against infectious pathogens in the respiratory tract. Population pharmacokinetic/pharmacodynami...
PMC11911801
core_pubmed_pmc
Randomized Phase II Study of Bevacizumab with Weekly Anetumab Ravtansine or Weekly Paclitaxel in Platinum-Resistant/Refractory High-Grade Ovarian Cancer (NCI Trial)
Randomized Phase II Study of Bevacizumab with Weekly Anetumab Ravtansine or Weekly Paclitaxel in Platinum-Resistant/Refractory High-Grade Ovarian Cancer (NCI Trial) Abstract Abstract Purpose: Mesothelin (MSLN) is highly expressed in high-grade serous/endometrioid ovarian cancers (HGOC). Anetumab ravtansine (AR) is an a...
PMC4418331
core_pubmed_pmc
Semaglutide, a Once-Weekly Human GLP-1 Analog, Does Not Reduce the Bioavailability of the Combined Oral Contraceptive, Ethinylestradiol/Levonorgestrel
Semaglutide, a Once-Weekly Human GLP-1 Analog, Does Not Reduce the Bioavailability of the Combined Oral Contraceptive, Ethinylestradiol/Levonorgestrel Abstract Abstract The effect of semaglutide, a once-weekly human glucagon-like peptide-1 (GLP-1) analog in development for type 2 diabetes (T2D), on the bioavailability ...
PMC3913857
core_pubmed_pmc
Regorafenib in Japanese patients with solid tumors: phase I study of safety, efficacy, and pharmacokinetics
Regorafenib in Japanese patients with solid tumors: phase I study of safety, efficacy, and pharmacokinetics Abstract Abstract The safety, pharmacokinetics, and antitumor activity of the multikinase inhibitor regorafenib in Japanese patients was assessed in this multicenter, single-arm, phase I trial. Fifteen patients w...
PMC12528213
core_pubmed_pmc
Tumor organoids may be more suitable for clinical personalized chemotherapeutic drug screening in lung adenocarcinoma
Tumor organoids may be more suitable for clinical personalized chemotherapeutic drug screening in lung adenocarcinoma Abstract Abstract Objective The formulation of precision treatment strategies and the analysis of drug-resistance mechanisms for lung adenocarcinoma are highly dependent on in vitro models that can fait...
PMC9904966
core_pubmed_pmc
Selective Serotonin Reuptake Inhibitor Use and Risk of Major Bleeding during Treatment with Vitamin K Antagonists: Results of A Cohort Study
Selective Serotonin Reuptake Inhibitor Use and Risk of Major Bleeding during Treatment with Vitamin K Antagonists: Results of A Cohort Study Abstract Background Selective serotonin reuptake inhibitors (SSRIs) may increase the risk of major bleeding by decreasing platelet function or decreasing vitamin K antagonist (VKA...
PMC11533111
core_pubmed_pmc
Making PBPK models more reproducible in practice
Making PBPK models more reproducible in practice Abstract Abstract Systems biology aims to understand living organisms through mathematically modeling their behaviors at different organizational levels, ranging from molecules to populations. Modeling involves several steps, from determining the model purpose to develop...
PMC12260505
core_pubmed_pmc
First-in-Human Phase I/IIa Study of the First-in-Class CDK2/4/6 Inhibitor PF-06873600 Alone or with Endocrine Therapy in Patients with Breast Cancer
First-in-Human Phase I/IIa Study of the First-in-Class CDK2/4/6 Inhibitor PF-06873600 Alone or with Endocrine Therapy in Patients with Breast Cancer Abstract Abstract Purpose: The discovery that cyclin E overexpression is a key cyclin-dependent kinase (CDK) 4/6 inhibitor resistance mechanism has reinvigorated interest ...
PMC12315921
core_pubmed_pmc
A Novel, Long-Acting, Small Molecule PKM2 Activator and Its Potential Broad Application Against Photoreceptor Degeneration
A Novel, Long-Acting, Small Molecule PKM2 Activator and Its Potential Broad Application Against Photoreceptor Degeneration Abstract Abstract Purpose Activating pyruvate kinase M2 (PKM2) has been shown to be neuroprotective in preclinical models of photoreceptor degeneration. We recently developed novel, small molecule ...
PMC8384972
core_pubmed_pmc
Absence of QTc Prolongation with Sodium N -(8-[2-Hydroxybenzoyl] Amino) Caprylate (SNAC), an Absorption Enhancer Co-Formulated with the GLP-1 Analogue Semaglutide for Oral Administration
Absence of QTc Prolongation with Sodium N -(8-[2-Hydroxybenzoyl] Amino) Caprylate (SNAC), an Absorption Enhancer Co-Formulated with the GLP-1 Analogue Semaglutide for Oral Administration Abstract Abstract Introduction Oral delivery of proteins, including glucagon-like peptide 1 (GLP-1) receptor agonists, is impeded by ...
PMC9061949
core_pubmed_pmc
Dose Optimisation of Posaconazole and Therapeutic Drug Monitoring in Pediatric Patients
Dose Optimisation of Posaconazole and Therapeutic Drug Monitoring in Pediatric Patients Abstract Abstract Experience in the clinical use of posaconazole (PCZ) in pediatric patients is limited, and no specific dose recommendations exist. This study aimed to investigate an appropriate dosing regimen, and assess the expos...
PMC12933200
core_pubmed_pmc
Advances in pharmacokinetic-pharmacodynamic modeling for anesthesia, 1987–2024: a review
Advances in pharmacokinetic-pharmacodynamic modeling for anesthesia, 1987–2024: a review Abstract Abstract In the field of individualized anesthesia, pharmacokinetic-pharmacodynamic (PKPD) models are crucial as they assist in determining the appropriate dosage for various patient groups. This research reviews the devel...
PMC5438479
core_pubmed_pmc
Bryostatin Effects on Cognitive Function and PKCɛ in Alzheimer’s Disease Phase IIa and Expanded Access Trials
Bryostatin Effects on Cognitive Function and PKCɛ in Alzheimer’s Disease Phase IIa and Expanded Access Trials Abstract Abstract Bryostatin 1, a potent activator of protein kinase C epsilon (PKC ɛ ), has been shown to reverse synaptic loss and facilitate synaptic maturation in animal models of Alzheimer’s disease (AD), ...
PMC11052869
core_pubmed_pmc
Demonstrating Bioequivalence for Two Dose Strengths of Niraparib and Abiraterone Acetate Dual-Action Tablets Versus Single Agents: Utility of Clinical Study Data Supplemented with Modeling and Simulation
Demonstrating Bioequivalence for Two Dose Strengths of Niraparib and Abiraterone Acetate Dual-Action Tablets Versus Single Agents: Utility of Clinical Study Data Supplemented with Modeling and Simulation Abstract Background and Objective The combination of niraparib and abiraterone acetate (AA) plus prednisone is under...
PMC5618502
core_pubmed_pmc
Self-Nanoemulsifying Drug Delivery System for Resveratrol: Enhanced Oral Bioavailability and Reduced Physical Fatigue in Rats
Self-Nanoemulsifying Drug Delivery System for Resveratrol: Enhanced Oral Bioavailability and Reduced Physical Fatigue in Rats Abstract Resveratrol (RES), a natural polyphenolic compound, exerts anti-fatigue activity, but its administration is complicated by its low water solubility. To improve RES bioavailability, this...
PMC10999516
core_pubmed_pmc
Ionic liquids as the effective technology for enhancing transdermal drug delivery: Design principles, roles, mechanisms, and future challenges
Ionic liquids as the effective technology for enhancing transdermal drug delivery: Design principles, roles, mechanisms, and future challenges Abstract Abstract Ionic liquids (ILs) have been proven to be an effective technology for enhancing drug transdermal absorption. However, due to the unique structural components ...
PMC9464749
core_pubmed_pmc
Switching Between Adalimumab Reference Product and BI 695501 in Patients with Chronic Plaque Psoriasis (VOLTAIRE-X): A Randomized Controlled Trial
Switching Between Adalimumab Reference Product and BI 695501 in Patients with Chronic Plaque Psoriasis (VOLTAIRE-X): A Randomized Controlled Trial Abstract Abstract Background BI 695501 is an FDA-approved biosimilar to adalimumab reference product (RP). VOLTAIRE-X was a randomized clinical trial to assess outcomes with...
PMC9081762
core_pubmed_pmc
Extra Loading Dose of Dexmedetomidine Enhances Intestinal Function Recovery After Colorectal Resection: A Retrospective Cohort Study
Extra Loading Dose of Dexmedetomidine Enhances Intestinal Function Recovery After Colorectal Resection: A Retrospective Cohort Study Abstract Importance: Postoperative gastrointestinal dysfunction (POGD) may be caused by postoperative vagus nerve tension inhibition and systemic inflammation. Dexmedetomidine (Dex) incre...
PMC5591795
core_pubmed_pmc
Population Pharmacokinetic Model and Pharmacokinetic Target Attainment of Micafungin in Intensive Care Unit Patients
Population Pharmacokinetic Model and Pharmacokinetic Target Attainment of Micafungin in Intensive Care Unit Patients Abstract Abstract Objective To study the pharmacokinetics of micafungin in intensive care patients and assess pharmacokinetic (PK) target attainment for various dosing strategies. Methods Micafungin PK d...
PMC10840023
core_pubmed_pmc
Phase 1/2 study of monalizumab plus durvalumab in patients with advanced solid tumors
Phase 1/2 study of monalizumab plus durvalumab in patients with advanced solid tumors Abstract Background The combination of monalizumab (anti-NKG2A/CD94) and durvalumab (anti-programmed death ligand-1) may promote antitumor immunity by targeting innate and adaptive immunity. This phase 1/2 study of monalizumab and dur...
PMC9226521
core_pubmed_pmc
Considerations and recommendations for assessment of plasma protein binding and drug–drug interactions for siRNA therapeutics
Considerations and recommendations for assessment of plasma protein binding and drug–drug interactions for siRNA therapeutics Abstract Abstract At the time of writing, although siRNA therapeutics are approved for human use, no official regulatory guidance specific to this modality is available. In the absence of guidan...
PMC8590079
core_pubmed_pmc
Time and metabolic state-dependent effects of GLP-1R agonists on NPY/AgRP and POMC neuronal activity in vivo
Time and metabolic state-dependent effects of GLP-1R agonists on NPY/AgRP and POMC neuronal activity in vivo Abstract Abstract Objective Long-acting glucagon-like peptide-1 receptor agonists (GLP-1RAs), like liraglutide and semaglutide, are viable treatments for diabetes and obesity. Liraglutide directly activates hypo...
PMC3291881
core_pubmed_pmc
Assessment of Extracts from Red Yeast Rice for Herb-Drug Interaction by in-vitro and in-vivo assays
Assessment of Extracts from Red Yeast Rice for Herb-Drug Interaction by in-vitro and in-vivo assays Abstract Abstract Red yeast rice (RYR) is made by fermenting the yeast Monascus purpureus over rice. It is a source of natural red food colorants, a food garnish and a traditional medication. Results of the current study...
PMC9412174
core_pubmed_pmc
Are Non-animal Systemic Safety Assessments Protective? A Toolbox and Workflow
Are Non-animal Systemic Safety Assessments Protective? A Toolbox and Workflow Abstract Abstract An important question in toxicological risk assessment is whether non-animal new approach methodologies (NAMs) can be used to make safety decisions that are protective of human health, without being overly conservative. In t...
PMC3786533
core_pubmed_pmc
Breath Powered Nasal Delivery: A New Route to Rapid Headache Relief
Breath Powered Nasal Delivery: A New Route to Rapid Headache Relief Abstract Abstract The nose offers an attractive noninvasive alternative for drug delivery. Nasal anatomy, with a large mucosal surface area and high vascularity, allows for rapid systemic absorption and other potential benefits. However, the complex na...
PMC7408216
core_pubmed_pmc
Food Effects on Oral Drug Absorption: Application of Physiologically-Based Pharmacokinetic Modeling as a Predictive Tool
Food Effects on Oral Drug Absorption: Application of Physiologically-Based Pharmacokinetic Modeling as a Predictive Tool Abstract The bioavailability of an orally administered small molecule is often dictated by drug-specific physicochemical characteristics and is influenced by many biological processes. For example, i...
PMC5310560
core_pubmed_pmc
Influence of the selective antagonist of the NR2B subunit of the NMDA receptor, traxoprodil, on the antidepressant-like activity of desipramine, paroxetine, milnacipran, and bupropion in mice
Influence of the selective antagonist of the NR2B subunit of the NMDA receptor, traxoprodil, on the antidepressant-like activity of desipramine, paroxetine, milnacipran, and bupropion in mice Abstract Abstract Pre-clinical and clinical studies indicated that a blockade of the NMDA receptor complex creates new opportuni...
PMC7113218
core_pubmed_pmc
A Randomized, Double-Blind, Efficacy and Safety Study of PF-05280586 (a Rituximab Biosimilar) Compared with Rituximab Reference Product (MabThera ® ) in Subjects with Previously Untreated CD20-Positive, Low-Tumor-Burden Follicular Lymphoma (LTB-FL)
A Randomized, Double-Blind, Efficacy and Safety Study of PF-05280586 (a Rituximab Biosimilar) Compared with Rituximab Reference Product (MabThera ® ) in Subjects with Previously Untreated CD20-Positive, Low-Tumor-Burden Follicular Lymphoma (LTB-FL) Abstract Abstract Background Biosimilars are highly similar to the lice...
PMC9653173
core_pubmed_pmc
Trotabresib (CC-90010) in combination with adjuvant temozolomide or concomitant temozolomide plus radiotherapy in patients with newly diagnosed glioblastoma
Trotabresib (CC-90010) in combination with adjuvant temozolomide or concomitant temozolomide plus radiotherapy in patients with newly diagnosed glioblastoma Abstract Abstract Background Standard-of-care treatment for newly diagnosed glioblastoma (ndGBM), consisting of surgery followed by radiotherapy (RT) and temozolom...
PMC8623740
core_pubmed_pmc
Infliximab Efficacy May Be Linked to Full TNF-α Blockade in Peripheral Compartment—A Double Central-Peripheral Target-Mediated Drug Disposition (TMDD) Model
Infliximab Efficacy May Be Linked to Full TNF-α Blockade in Peripheral Compartment—A Double Central-Peripheral Target-Mediated Drug Disposition (TMDD) Model Abstract Infliximab is an anti-TNF-α monoclonal antibody approved in chronic inflammatory bowel diseases (IBD). This study aimed at providing an in-depth descripti...
PMC4415995
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Safety of Luseogliflozin in Japanese Patients with Type 2 Diabetes Mellitus: A Randomized, Single-blind, Placebo-controlled Trial
Pharmacokinetics, Pharmacodynamics, and Safety of Luseogliflozin in Japanese Patients with Type 2 Diabetes Mellitus: A Randomized, Single-blind, Placebo-controlled Trial Abstract Abstract Introduction Luseogliflozin, a potent, selective sodium glucose cotransporter 2 inhibitor, promotes urinary glucose excretion (UGE) ...
PMC7679073
core_pubmed_pmc
Exposure‐Safety Analyses Identify Predictors of Change in Bone Mineral Density and Support Elagolix Labeling for Endometriosis‐Associated Pain
Exposure‐Safety Analyses Identify Predictors of Change in Bone Mineral Density and Support Elagolix Labeling for Endometriosis‐Associated Pain Abstract Abstract Elagolix is a novel oral gonadotropin releasing hormone receptor antagonist, that can suppress estradiol in a dose‐dependent manner. It is indicated for manage...
PMC10936461
core_pubmed_pmc
High response rate with extended dosing of cemiplimab in advanced cutaneous squamous cell carcinoma
High response rate with extended dosing of cemiplimab in advanced cutaneous squamous cell carcinoma Abstract Abstract Background Cemiplimab (Libtayo ® ), a human monoclonal immunoglobulin G4 antibody to the programmed cell death-1 receptor, is approved for the treatment of patients with advanced cutaneous squamous cell...
PMC8225544
core_pubmed_pmc
Population pharmacokinetic characteristics of cemiplimab in patients with advanced malignancies
Population pharmacokinetic characteristics of cemiplimab in patients with advanced malignancies Abstract Cemiplimab, a human monoclonal antibody targeting programmed cell death-1 (PD-1) receptor, demonstrated antitumor activity in patients with advanced malignancies and a safety profile comparable to other anti–PD-1 th...
PMC9579148
core_pubmed_pmc
Rational design of the zonulin inhibitor AT1001 derivatives as potential anti SARS-CoV-2
Rational design of the zonulin inhibitor AT1001 derivatives as potential anti SARS-CoV-2 Abstract Abstract Although vaccines are greatly mitigating the worldwide pandemic diffusion of SARS-Cov-2, therapeutics should provide many distinct advantages as complementary approach to control the viral spreading. Here, we repo...
PMC8851335
core_pubmed_pmc
Repurposing the Veterinary Antibiotic Apramycin for Antibacterial and Antibiofilm Activity Against Pseudomonas aeruginosa From Cystic Fibrosis Patients
Repurposing the Veterinary Antibiotic Apramycin for Antibacterial and Antibiofilm Activity Against Pseudomonas aeruginosa From Cystic Fibrosis Patients Abstract Objectives: To evaluate the in vitro antibacterial, antibiofilm, and antivirulence activities of apramycin, comparatively to tobramycin, against a set of P. ae...
PMC10547744
core_pubmed_pmc
The ascending limb of the cocaine unit dose–response function in rats as an experimental artifact
The ascending limb of the cocaine unit dose–response function in rats as an experimental artifact Abstract Abstract The cocaine unit dose–response function is an inverted U with the ascending and descending limbs representing the positive and rate limiting cocaine effects, respectively. Higher fixed ratio (FR) schedule...
PMC5655053
core_pubmed_pmc
Pharmacological Basis of CD101 Efficacy: Exposure Shape Matters
Pharmacological Basis of CD101 Efficacy: Exposure Shape Matters Abstract ABSTRACT CD101 is a novel echinocandin with concentration-dependent fungicidal activity in vitro and a long half-life (∼133 h in humans, ∼70 to 80 h in mice). Given these characteristics, it is likely that the shape of the CD101 exposure (i.e., th...
PMC10302851
core_pubmed_pmc
Evaluation of Real-World Vancomycin Dosing and Attainment of Therapeutic Drug Monitoring Targets
Evaluation of Real-World Vancomycin Dosing and Attainment of Therapeutic Drug Monitoring Targets Abstract Abstract In 2020, the Infectious Diseases Society of America (IDSA) recommended a change in vancomycin therapeutic drug monitoring from trough-based to AUC/MIC-based to optimize vancomycin’s efficacy and reduce nep...
PMC8216138
core_pubmed_pmc
Ten‐Year Simulation of the Effects of Denosumab on Bone Remodeling in Human Biopsies
Ten‐Year Simulation of the Effects of Denosumab on Bone Remodeling in Human Biopsies Abstract ABSTRACT Postmenopausal osteoporosis is a disease manifesting in degradation of bone mass and microarchitecture, leading to weakening and increased risk of fracture. Clinical trials are an essential tool for evaluating new tre...
PMC10551964
core_pubmed_pmc
Non-invasive PD-L1 quantification using [ 18 F]DK222-PET imaging in cancer immunotherapy
Non-invasive PD-L1 quantification using [ 18 F]DK222-PET imaging in cancer immunotherapy Abstract Background Combination therapies that aim to improve the clinical efficacy to immune checkpoint inhibitors have led to the need for non-invasive and early pharmacodynamic biomarkers. Positron emission tomography (PET) is a...
PMC5270290
core_pubmed_pmc
Quantitative Characterization of the Exposure–Response Relationship for Cancer Immunotherapy: A Case Study of Nivolumab in Patients With Advanced Melanoma
Quantitative Characterization of the Exposure–Response Relationship for Cancer Immunotherapy: A Case Study of Nivolumab in Patients With Advanced Melanoma Abstract To inform the benefit–risk assessment of nivolumab in patients with advanced melanoma, analyses of efficacy and safety exposure–response (E–R) relationships...
PMC7902566
core_pubmed_pmc
Exploration for the real causative agents of licorice-induced pseudoaldosteronism
Exploration for the real causative agents of licorice-induced pseudoaldosteronism Abstract Abstract I investigated the causative agents of licorice-induced pseudoaldosteronism, which is a frequent side effect of Japanese traditional Kampo medicines. Glycyrrhizin (GL), the main ingredient of licorice, is absorbed after ...
PMC9505734
core_pubmed_pmc
Design, Synthesis, and Evaluation of a Set of Carboxylic Acid and Phosphate Prodrugs Derived from HBV Capsid Protein Allosteric Modulator NVR 3-778
Design, Synthesis, and Evaluation of a Set of Carboxylic Acid and Phosphate Prodrugs Derived from HBV Capsid Protein Allosteric Modulator NVR 3-778 Abstract Hepatitis B virus (HBV) capsid protein (Cp) is necessary for viral replication and the maintenance of viral persistence, having become an attractive target of anti...
PMC7375048
core_pubmed_pmc
The impact of acute rosiglitazone on insulin pharmacokinetics at the blood‐brain barrier
The impact of acute rosiglitazone on insulin pharmacokinetics at the blood‐brain barrier Abstract Abstract Introduction CNS insulin levels are decreased and insulin receptor signalling is dampened in Alzheimer's disease (AD). Increasing CNS insulin levels through a variety of methods has been shown to improve memory. I...
PMC12943270
core_pubmed_pmc
Multi-Targeted Therapeutic Mechanisms of Huangqi Guizhi Wuwu Decoction Against Rheumatoid Arthritis: An Integrated Approach Combining Serum Pharmacochemistry, Network Pharmacology, Metabolomics, and Experimental Validation
Multi-Targeted Therapeutic Mechanisms of Huangqi Guizhi Wuwu Decoction Against Rheumatoid Arthritis: An Integrated Approach Combining Serum Pharmacochemistry, Network Pharmacology, Metabolomics, and Experimental Validation Abstract Abstract Background : The pathogenesis of rheumatoid arthritis (RA) is closely related t...
PMC10772524
core_pubmed_pmc
Safety and efficacy of tenalisib in combination with romidepsin in patients with relapsed/refractory T-cell lymphoma: results from a phase I/II open-label multicenter study
Safety and efficacy of tenalisib in combination with romidepsin in patients with relapsed/refractory T-cell lymphoma: results from a phase I/II open-label multicenter study Abstract Tenalisib, a selective phosphoinositide-3-kinase δ/γ, and salt-inducible-kinase-3 inhibitor has shown efficacy and was well-tolerated in p...
PMC11786611
core_pubmed_pmc
Bictegravir/emtricitabine/tenofovir alafenamide in adults with HIV ‐1 and end‐stage kidney disease on chronic haemodialysis
Bictegravir/emtricitabine/tenofovir alafenamide in adults with HIV ‐1 and end‐stage kidney disease on chronic haemodialysis Abstract Abstract Introduction Treatment for people with HIV‐1 and end‐stage kidney disease (ESKD) on haemodialysis (HD) has previously required complex dose‐adjusted regimens, with limited data o...
PMC12426855
core_pubmed_pmc
Randomized phase 2a trial assessing a novel septin molecular glue in Alzheimer's disease
Randomized phase 2a trial assessing a novel septin molecular glue in Alzheimer's disease Abstract Abstract INTRODUCTION Pharmacological restoration of septin filament integrity has the potential to provide symptomatic benefit and disease modification in Alzheimer's disease (AD). METHODS REM127, a septin modulator, was ...
PMC6921293
core_pubmed_pmc
Phase I dose-escalation study to determine the safety, tolerability, preliminary efficacy and pharmacokinetics of an intratumoral injection of tigilanol tiglate (EBC-46)
Phase I dose-escalation study to determine the safety, tolerability, preliminary efficacy and pharmacokinetics of an intratumoral injection of tigilanol tiglate (EBC-46) Abstract Abstract Background Tigilanol tiglate, a short-chain diterpene ester, is being developed as intratumoral treatment of a broad range of cancer...
PMC8049115
core_pubmed_pmc
Stratified Management for Bacterial Infections in Late Preterm and Term Neonates: Current Strategies and Future Opportunities Toward Precision Medicine
Stratified Management for Bacterial Infections in Late Preterm and Term Neonates: Current Strategies and Future Opportunities Toward Precision Medicine Abstract Abstract Bacterial infections remain a major cause of morbidity and mortality in the neonatal period. Therefore, many neonates, including late preterm and term...
PMC11511194
core_pubmed_pmc
Key Factors for Improving Predictive Accuracy and Avoiding Overparameterization of the PBPK Absorption Model in Food Effect Studies of Weakly Basic Water-Insoluble Compounds in Immediate Release Formulations
Key Factors for Improving Predictive Accuracy and Avoiding Overparameterization of the PBPK Absorption Model in Food Effect Studies of Weakly Basic Water-Insoluble Compounds in Immediate Release Formulations Abstract Background/Objectives : Physiologically based pharmacokinetic (PBPK) absorption models are instrumental...
PMC12636028
core_pubmed_pmc
Rate-Tunable, Metal-Mediated Amide Bond Cleavage for the Controlled Release of Pharmaceuticals
Rate-Tunable, Metal-Mediated Amide Bond Cleavage for the Controlled Release of Pharmaceuticals Abstract Abstract That the incorporation of N -methyl amino acids adjacent to a hydrolytic, azamacrocyclic metal complex results in rate-tunable, metal-mediated amide bond cleavage (TMAC) under physiological conditions. Spect...
PMC2887166
core_pubmed_pmc
Prospective monitoring of cefepime in intensive care unit adult patients
Prospective monitoring of cefepime in intensive care unit adult patients Abstract Abstract Introduction Cefepime has been associated with a greater risk of mortality than other beta-lactams in patients treated for severe sepsis. Hypotheses for this failure include possible hidden side-effects (for example, neurological...
PMC6590112
core_pubmed_pmc
Phase I study of single‐dose pharmacokinetics and pharmacodynamics of belatacept in adolescent kidney transplant recipients
Phase I study of single‐dose pharmacokinetics and pharmacodynamics of belatacept in adolescent kidney transplant recipients Abstract Abstract Belatacept is an intravenously infused selective T cell costimulation blocker approved for preventing organ rejection in renal transplant recipients aged ≥18 years. This phase I ...
PMC3664752
core_pubmed_pmc
Pharmacokinetics, Tolerability, and Safety of Intranasal Administration of Reformulated OxyContin ® Tablets Compared with Original OxyContin ® Tablets in Healthy Adults
Pharmacokinetics, Tolerability, and Safety of Intranasal Administration of Reformulated OxyContin ® Tablets Compared with Original OxyContin ® Tablets in Healthy Adults Abstract Abstract Background and Objective Reformulated OxyContin ® (oxycodone-HCl controlled release) tablets (ORF) became available in the United Sta...
PMC6510383
core_pubmed_pmc
Impact of Insulin Tregopil and Its Permeation Enhancer on Pharmacokinetics of Metformin in Healthy Volunteers: Randomized, Open‐Label, Placebo‐Controlled, Crossover Study
Impact of Insulin Tregopil and Its Permeation Enhancer on Pharmacokinetics of Metformin in Healthy Volunteers: Randomized, Open‐Label, Placebo‐Controlled, Crossover Study Abstract Oral insulin tregopil ( IN ‐105; a new drug under development) may be coadministered with oral antidiabetic drugs, such as metformin in pati...
PMC12114607
core_pubmed_pmc
A Successful Experience of Individualized Vancomycin Dosing in Critically Ill Patients by Using a Loading Dose and Maintenance Dose
A Successful Experience of Individualized Vancomycin Dosing in Critically Ill Patients by Using a Loading Dose and Maintenance Dose Abstract Background/Objective: Vancomycin, a hydrophilic glycopeptide antibiotic with bactericidal activity against Gram-positive microorganisms, is one of the most commonly used antibioti...
PMC11107231
core_pubmed_pmc
Evaluation of gender differences in the pharmacokinetics of oral zileuton nanocrystalline formulation using a rat model
Evaluation of gender differences in the pharmacokinetics of oral zileuton nanocrystalline formulation using a rat model Abstract Zileuton is a leukotriene inhibitor used to treat asthma. As a BCS class II drug it exhibits challenges with solubility which likely impact its absorption. As patient gender significantly imp...
PMC6167333
core_pubmed_pmc
Pharmacokinetics of enrofloxacin HCl-2H 2 O (Enro-C) in dogs and pharmacokinetic/pharmacodynamic Monte Carlo simulations against Leptospira spp.
Pharmacokinetics of enrofloxacin HCl-2H 2 O (Enro-C) in dogs and pharmacokinetic/pharmacodynamic Monte Carlo simulations against Leptospira spp. Abstract Pharmacokinetic/pharmacodynamic (PK/PD) ratios of reference enrofloxacin (Enro-R) and enrofloxacin as HCl-2H 2 O (Enro-C), as well as Monte Carlo simulations based on...
PMC6721124
core_pubmed_pmc
Photoactive Liposomal Formulation of PVP-Conjugated Chlorin e6 for Photodynamic Reduction of Atherosclerotic Plaque
Photoactive Liposomal Formulation of PVP-Conjugated Chlorin e6 for Photodynamic Reduction of Atherosclerotic Plaque Abstract Abstract Background: Liposomes serve as delivery systems for biologically active compounds. Existing technologies inefficiently encapsulate large hydrophilic macromolecules, such as PVP-conjugate...
PMC7495289
core_pubmed_pmc
Enantiomer specific pharmacokinetics of ibuprofen in preterm neonates with patent ductus arteriosus
Enantiomer specific pharmacokinetics of ibuprofen in preterm neonates with patent ductus arteriosus Abstract Aims Racemic ibuprofen is widely used for the treatment of preterm neonates with patent ductus arteriosus. Currently used bodyweight‐based dosing guidelines are based on total ibuprofen, while only the S‐enantio...
PMC10145266
core_pubmed_pmc
Pharmacokinetic Evaluation of Tacrolimus in Chinese Adult Patients during the Early Stages Post-Lung Transplantation
Pharmacokinetic Evaluation of Tacrolimus in Chinese Adult Patients during the Early Stages Post-Lung Transplantation Abstract Background: Although tacrolimus has been widely used in patients undergoing lung transplantation, few studies have reported the pharmacokinetics of tacrolimus in Chinese patients after lung tran...
PMC11247124
core_pubmed_pmc
Navigating the landscape of parameter identifiability methods: A workflow recommendation for model development
Navigating the landscape of parameter identifiability methods: A workflow recommendation for model development Abstract Abstract In pharmacometric modeling, it is often important to know whether the data is sufficiently rich to identify the parameters of a proposed model. While it may be possible to assess this based o...
PMC12650508
core_pubmed_pmc
Triptolide Affects the Function of Hepatocellular Drug Uptake Transporter Organic Anion Transporting Polypeptide 1B1 Through the Suppression of SGK1
Triptolide Affects the Function of Hepatocellular Drug Uptake Transporter Organic Anion Transporting Polypeptide 1B1 Through the Suppression of SGK1 Abstract Simple Summary Organic anion transporting polypeptide 1B1 (OATP1B1) is a liver-specific drug transporter that plays a crucial role in the uptake of many clinicall...
PMC11663749
core_pubmed_pmc
Evaluation of the safety, tolerability, pharmacokinetics and pharmacodynamics of SM17 in healthy volunteers: results from pre-clinical models and a first-in-human, randomized, double blinded clinical trial
Evaluation of the safety, tolerability, pharmacokinetics and pharmacodynamics of SM17 in healthy volunteers: results from pre-clinical models and a first-in-human, randomized, double blinded clinical trial Abstract Background Alarmins mediate type 2 T helper cell (Th2) inflammation and serve as upstream signaling eleme...
PMC7525091
core_pubmed_pmc
Inhibitory Effect of Imperatorin on the Pharmacokinetics of Diazepam In Vitro and In Vivo
Inhibitory Effect of Imperatorin on the Pharmacokinetics of Diazepam In Vitro and In Vivo Abstract Abstract Background Diazepam is a benzodiazepine drug used to treat anxiety, insomnia, and muscle spasms. Imperatorin is a phytochemical isolated from medicinal plants and is widely used in herbal medicine. The aim of thi...
PMC12648076
core_pubmed_pmc
Research on the dose calculation of BNCT based on the time-varying boron concentration in pharmacokinetics
Research on the dose calculation of BNCT based on the time-varying boron concentration in pharmacokinetics Abstract ABSTRACT Boron Neutron Capture Therapy (BNCT) is a targeted radiotherapy that utilizes the nuclear reaction of 10 B with thermal neutrons to destroy tumor cells while sparing healthy tissue. Its effective...
PMC11273951
core_pubmed_pmc
Novel Antibiotics for Gram-Negative Nosocomial Pneumonia
Novel Antibiotics for Gram-Negative Nosocomial Pneumonia Abstract Nosocomial pneumonia, including hospital-acquired pneumonia and ventilator-associated pneumonia, is the leading cause of death related to hospital-acquired infections among critically ill patients. A growing proportion of these cases are attributed to mu...
PMC5192133
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of MEDI4893, an Investigational, Extended-Half-Life, Anti- Staphylococcus aureus Alpha-Toxin Human Monoclonal Antibody, in Healthy Adults
Safety, Tolerability, and Pharmacokinetics of MEDI4893, an Investigational, Extended-Half-Life, Anti- Staphylococcus aureus Alpha-Toxin Human Monoclonal Antibody, in Healthy Adults Abstract ABSTRACT MEDI4893 is an investigational immunoglobulin G1(κ) monoclonal antibody that specifically binds to and neutralizes alpha-...
PMC9673343
core_pubmed_pmc
Relevance of the pyroptosis-related inflammasome drug targets in the Chuanxiong to improve diabetic nephropathy
Relevance of the pyroptosis-related inflammasome drug targets in the Chuanxiong to improve diabetic nephropathy Abstract Background A chronic inflammatory disease caused by disturbances in metabolism, diabetic nephropathy (DN) is a chronic inflammatory disease. Pyroptosis is a novel form of programmed cell death in man...
PMC8760204
core_pubmed_pmc
GC–MS Analysis, Molecular Docking and Pharmacokinetic Properties of Phytocompounds from Solanum torvum Unripe Fruits and Its Effect on Breast Cancer Target Protein
GC–MS Analysis, Molecular Docking and Pharmacokinetic Properties of Phytocompounds from Solanum torvum Unripe Fruits and Its Effect on Breast Cancer Target Protein Abstract Abstract This study was designed to identify phytocompounds from the aqueous extract of Solanum torvum unripe fruits using GC–MS analysis against b...
PMC12666311
core_pubmed_pmc
The Bi-steric, mTORC1-Selective Inhibitor, RMC-5552, in Advanced Solid Tumors: A Phase 1 Trial
The Bi-steric, mTORC1-Selective Inhibitor, RMC-5552, in Advanced Solid Tumors: A Phase 1 Trial Abstract Abstract Purpose: PI3K/mTOR pathway activation drives oncogenesis and progression of many cancers. RMC-5552 is a bi-steric, mTOR complex 1 (mTORC1)-selective inhibitor that potently inhibits phosphorylation of key mT...
PMC12745379
core_pubmed_pmc
Ceftazidime-avibactam for the treatment of multidrug-resistant or extensively drug-resistant bacteria infection in preterm infants: case series study and literature review
Ceftazidime-avibactam for the treatment of multidrug-resistant or extensively drug-resistant bacteria infection in preterm infants: case series study and literature review Abstract Abstract Objective To evaluate efficacy and safety of ceftazidime-avibactam (CZA) in preterm infants with multidrug-resistant (MDR) or exte...
PMC12000890
core_pubmed_pmc
Traditional Chinese medicine compounds modulate signaling pathways to improve cardiac-related pathology
Traditional Chinese medicine compounds modulate signaling pathways to improve cardiac-related pathology Abstract Abstract Cardiovascular disease poses a significant risk to human health and remains the leading cause of illness and death globally, with its incidence continuing to rise. The intricate pathophysiological m...
PMC12061375
core_pubmed_pmc
Development and Validation of a High-Performance Liquid Chromatography–Ultraviolet Spectrometry Method for Ampicillin and Its Application in Routine Therapeutic Drug Monitoring of Intensive Care Patients
Development and Validation of a High-Performance Liquid Chromatography–Ultraviolet Spectrometry Method for Ampicillin and Its Application in Routine Therapeutic Drug Monitoring of Intensive Care Patients Abstract Supplemental Digital Content is Available in the Text. Background: Ampicillin/sulbactam, a combination of a...
PMC8444857
core_pubmed_pmc
Immune‐viral dynamics modeling for SARS‐CoV‐2 drug development
Immune‐viral dynamics modeling for SARS‐CoV‐2 drug development Abstract Abstract Coronavirus disease 2019 (COVID‐19) global pandemic is caused by severe acute respiratory syndrome‐coronavirus 2 (SARS‐CoV‐2) viral infection, which can lead to pneumonia, lung injury, and death in susceptible populations. Understanding vi...
PMC7555839
core_pubmed_pmc
A Novel Promazine Derivative Shows High in vitro and in vivo Antimicrobial Activity Against Staphylococcus aureus
A Novel Promazine Derivative Shows High in vitro and in vivo Antimicrobial Activity Against Staphylococcus aureus Abstract The emergence of multidrug-resistant bacteria constitutes a significant public health issue worldwide. Consequently, there is an urgent clinical need for novel treatment solutions. It has been show...
PMC12944691
core_pubmed_pmc
Reviving Old Antibiotics: New Indications and Therapeutic Perspectives—A Review
Reviving Old Antibiotics: New Indications and Therapeutic Perspectives—A Review Abstract The rapid global spread of antimicrobial resistance (AMR) has significantly reduced the effectiveness of many modern antibiotics, creating an urgent need for alternative therapeutic strategies. One promising approach is the revival...
PMC6964681
core_pubmed_pmc
Window of opportunity clinical trial designs to study cancer metabolism
Window of opportunity clinical trial designs to study cancer metabolism Abstract Window of opportunity trials exploit the ‘window’ of time after cancer diagnosis, typically prior to initiation of cancer therapy. In recent years this study design has become a more regular feature of drug development, as this ‘window’ pr...
PMC10223211
core_pubmed_pmc
Development of a Swellable and Floating Gastroretentive Drug Delivery System ( sf GRDDS) of Ciprofloxacin Hydrochloride
Development of a Swellable and Floating Gastroretentive Drug Delivery System ( sf GRDDS) of Ciprofloxacin Hydrochloride Abstract Abstract Sangelose ® (SGL) is a novel hydroxypropyl methylcellulose (HPMC) derivative that has been hydrophobically modified. Due to its high viscosity, SGL has the potential as a gel-forming...
PMC12947250
core_pubmed_pmc
QX008N, an Anti‐TSLP Monoclonal Antibody: Pharmacokinetics, Tolerability, and Immunogenicity in Healthy Chinese Subjects
QX008N, an Anti‐TSLP Monoclonal Antibody: Pharmacokinetics, Tolerability, and Immunogenicity in Healthy Chinese Subjects Abstract ABSTRACT QX008N, a humanized IgG1 monoclonal antibody against thymic stromal lymphopoietin (TSLP) with Fc engineering to extend half‐life, was developed with the aim of exploring whether its...
PMC6250255
core_pubmed_pmc
Effects of Low- and High-Mineral Content Water on the Relative Bioavailability of a Coformulated Abacavir/Dolutegravir/Lamivudine Dispersible Tablet in Healthy Adults
Effects of Low- and High-Mineral Content Water on the Relative Bioavailability of a Coformulated Abacavir/Dolutegravir/Lamivudine Dispersible Tablet in Healthy Adults Abstract Supplemental Digital Content is Available in the Text. Key Words: dispersible, bioequivalence, pharmacokinetics, palatability, Contrex water Abs...
PMC11117587
core_pubmed_pmc
Ethnic Aspects of Valproic Acid P-Oxidation
Ethnic Aspects of Valproic Acid P-Oxidation Abstract The safety of the use of psychotropic drugs, widely used in neurological and psychiatric practice, is an urgent problem in personalized medicine. This narrative review demonstrated the variability in allelic frequencies of low-functioning and non-functional single nu...
PMC10508581
core_pubmed_pmc
Development of a multiscale mechanistic modeling framework integrating differential cellular kinetics of CAR T‐cell subsets and immunophenotypes in cancer patients
Development of a multiscale mechanistic modeling framework integrating differential cellular kinetics of CAR T‐cell subsets and immunophenotypes in cancer patients Abstract Abstract Chimeric antigen receptor (CAR) T‐cell subsets and immunophenotypic composition of the pre‐infusion product, as well as their longitudinal...
PMC5600113
core_pubmed_pmc
What is the true in vitro potency of oxytetracycline for the pig pneumonia pathogens Actinobacillus pleuropneumoniae and Pasteurella multocida ?
What is the true in vitro potency of oxytetracycline for the pig pneumonia pathogens Actinobacillus pleuropneumoniae and Pasteurella multocida ? Abstract Abstract The pharmacodynamics of oxytetracycline was determined for pig respiratory tract pathogens, Actinobacillus pleuropneumoniae and Pasteurella multocida . Indic...
PMC8190911
core_pubmed_pmc
Effect of Concomitant Hydroxyurea Therapy with Rutin and Gallic Acid: Integration of Pharmacokinetic and Pharmacodynamic Approaches
Effect of Concomitant Hydroxyurea Therapy with Rutin and Gallic Acid: Integration of Pharmacokinetic and Pharmacodynamic Approaches Abstract Hydroxyurea (HU) is the first-ever approved drug by USFDA for sickle cell anemia (SCA). However, its treatment is associated with severe side effects like myelosuppression. Curren...
PMC10946967
core_pubmed_pmc
Advanced models for respiratory disease and drug studies
Advanced models for respiratory disease and drug studies Abstract Abstract The global burden of respiratory diseases is enormous, with many millions of people suffering and dying prematurely every year. The global COVID‐19 pandemic witnessed recently, along with increased air pollution and wildfire events, increases th...
PMC7145786
core_pubmed_pmc
Bioavailability of aspirin in fasted and fed states of a novel pharmaceutical lipid aspirin complex formulation
Bioavailability of aspirin in fasted and fed states of a novel pharmaceutical lipid aspirin complex formulation Abstract Dyspeptic symptoms are common with aspirin and clinicians frequently recommend that it be taken with food to reduce these side effects. However, food can interfere with absorption, especially with en...
PMC10487306
core_pubmed_pmc
Anticoagulation strategies in COVID-19 infected patients receiving ECMO support
Anticoagulation strategies in COVID-19 infected patients receiving ECMO support Abstract Background : Hospitalized COVID-19 patients with hypoxemic respiratory failure may deteriorate despite invasive mechanical ventilation and thus require extracorporeal membrane oxygenation (ECMO) support. Unfractionated heparin (UFH...
PMC9056844
core_pubmed_pmc
In vivo and in vitro studies of antisense oligonucleotides – a review
In vivo and in vitro studies of antisense oligonucleotides – a review Abstract Abstract The potential of antisense oligonucleotides in gene silencing was discovered over 40 years ago, which resulted in the growing interest in their chemistry, mechanism of action, and metabolic pathways. This review summarizes the selec...
PMC10042977
core_pubmed_pmc
Can Mechanistic Static Models for Drug-Drug Interactions Support Regulatory Filing for Study Waivers and Label Recommendations?
Can Mechanistic Static Models for Drug-Drug Interactions Support Regulatory Filing for Study Waivers and Label Recommendations? Abstract Background and Objective Mechanistic static and dynamic physiologically based pharmacokinetic models are used in clinical drug development to assess the risk of drug–drug interactions...
PMC11257687
core_pubmed_pmc
The Cytochrome P450 2C8*3 Variant (rs11572080) Is Associated with Improved Asthma Symptom Control in Children and Altered Lipid Mediator Production and Inflammatory Response in Human Bronchial Epithelial Cells
The Cytochrome P450 2C8*3 Variant (rs11572080) Is Associated with Improved Asthma Symptom Control in Children and Altered Lipid Mediator Production and Inflammatory Response in Human Bronchial Epithelial Cells Abstract This study investigated an association between the cytochrome P450 (CYP) 2C8*3 polymorphism with asth...
PMC6271088
core_pubmed_pmc
Quantification of the Resveratrol Analogs trans -2,3-Dimethoxy-stilbene and trans -3,4-Dimethoxystilbene in Rat Plasma: Application to Pre-Clinical Pharmacokinetic Studies
Quantification of the Resveratrol Analogs trans -2,3-Dimethoxy-stilbene and trans -3,4-Dimethoxystilbene in Rat Plasma: Application to Pre-Clinical Pharmacokinetic Studies Abstract Abstract trans -2,3-Dimethoxystilbene (2,3-DMS) and trans -3,4-dimethoxystilbene (3,4-DMS) are two synthetic resveratrol ( trans -3,5,4'-tr...
PMC4338649
core_pubmed_pmc
Desmopressin Lyophilisate for the Treatment of Central Diabetes Insipidus: First Experience in Very Young Infants
Desmopressin Lyophilisate for the Treatment of Central Diabetes Insipidus: First Experience in Very Young Infants Abstract Abstract Introduction: In neonates and small infants, early diagnosis of central diabetes insipidus (CDI) and treatment with desmopressin in low doses (avoiding severe hypo- or hypernatremia) are i...
PMC5496345
core_pubmed_pmc
Pharmacogenetic evaluation to assess breakthrough psychosis with aripiprazole long-acting injection: a case report
Pharmacogenetic evaluation to assess breakthrough psychosis with aripiprazole long-acting injection: a case report Abstract Abstract Background Given the complex nature of symptom presentation and medication regimens, psychiatric clinics may benefit from additional tools to personalize treatments. Utilizing pharmacogen...