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PMC8400050
core_pubmed_pmc
Preparation of Curcumin-Eudragit ® E PO Solid Dispersions with Gradient Temperature through Hot-Melt Extrusion
Preparation of Curcumin-Eudragit ® E PO Solid Dispersions with Gradient Temperature through Hot-Melt Extrusion Abstract Abstract Hot-melt extrusion (HME) has great advantages for the preparation of solid dispersion (SD), for instance, it does not require any organic solvents. Nevertheless, its application to high-melti...
PMC7154775
core_pubmed_pmc
Recovery of cefazolin and clindamycin in in vitro pediatric CPB systems
Recovery of cefazolin and clindamycin in in vitro pediatric CPB systems Abstract Abstract Cardiopulmonary bypass (CPB) is often necessary for congenital cardiac surgery, but CPB can alter drug pharmacokinetic parameters resulting in underdosing. Inadequate plasma levels of antibiotics could lead to postoperative infect...
PMC8932701
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic modeling for dose selection for the first‐in‐human trial of the activated Factor XII inhibitor garadacimab (CSL312)
Pharmacokinetic/pharmacodynamic modeling for dose selection for the first‐in‐human trial of the activated Factor XII inhibitor garadacimab (CSL312) Abstract Abstract Factor XII (FXII) is a serine protease involved in multiple cascades, including the kallikrein–kinin system. It may play a role in diseases in which the d...
PMC9906007
core_pubmed_pmc
Reinstating apoptosis using putative Bcl-xL natural product inhibitors: Molecular docking and ADMETox profiling investigations
Reinstating apoptosis using putative Bcl-xL natural product inhibitors: Molecular docking and ADMETox profiling investigations Abstract Objectives While a fine balance in the pro-apoptotic and anti-apoptotic family members of the B-cell lymphoma-2 (Bcl-2) protein family represents a normal signaling profile, a tilt in ...
PMC5869871
core_pubmed_pmc
Effects of rifampin, itraconazole and esomeprazole on the pharmacokinetics of alisertib, an investigational aurora a kinase inhibitor in patients with advanced malignancies
Effects of rifampin, itraconazole and esomeprazole on the pharmacokinetics of alisertib, an investigational aurora a kinase inhibitor in patients with advanced malignancies Abstract Summary Aim Two studies investigated the effect of gastric acid reducing agents and strong inducers/inhibitors of CYP3A4 on the pharmacoki...
PMC11809180
core_pubmed_pmc
RA-PR058, a novel ramalin derivative, reduces BACE1 expression and phosphorylation of tau in Alzheimer’s disease mouse models
RA-PR058, a novel ramalin derivative, reduces BACE1 expression and phosphorylation of tau in Alzheimer’s disease mouse models Abstract ABSTRACT Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder characterized by cognitive decline, anxiety-like behavior, β-amyloid (Aβ) accumulation, and tau hyperpho...
PMC5800388
core_pubmed_pmc
Practical considerations in clinical strategy to support the development of injectable drug-device combination products for biologics
Practical considerations in clinical strategy to support the development of injectable drug-device combination products for biologics Abstract ABSTRACT The development of an injectable drug-device combination (DDC) product for biologics is an intricate and evolving process that requires substantial investments of time ...
PMC3108739
core_pubmed_pmc
Drug resistance in community-acquired respiratory tract infections: role for an emerging antibacterial
Drug resistance in community-acquired respiratory tract infections: role for an emerging antibacterial Abstract Abstract The nasopharynx is the ecological niche where evolution towards resistance occurs in respiratory tract isolates. Dynamics of different bacterial populations in antibiotic-free multibacterial niches a...
PMC10824831
core_pubmed_pmc
Moxidectin is a candidate for use as an in vivo internal standard in pharmacokinetic studies, as demonstrated with use in simultaneous tissue cage and ultrafiltration fluid collection
Moxidectin is a candidate for use as an in vivo internal standard in pharmacokinetic studies, as demonstrated with use in simultaneous tissue cage and ultrafiltration fluid collection Abstract In vivo ultrafiltration has been used in veterinary pharmacokinetics since the early 2000’s as an improvement on the tissue cag...
PMC12199099
core_pubmed_pmc
Assessment of ethnic differences in pharmacokinetics and clinical responses of acalabrutinib between Chinese and White patients with B‐cell malignancies
Assessment of ethnic differences in pharmacokinetics and clinical responses of acalabrutinib between Chinese and White patients with B‐cell malignancies Abstract Abstract Aims The aim of this study was to assess differences between Chinese and White patients in pharmacokinetics (PK) of, and clinical response to, acalab...
PMC6853149
core_pubmed_pmc
Clinical Pharmacology‐Driven Translational Research to Optimize Bedside Therapeutics of Sotalol Therapy
Clinical Pharmacology‐Driven Translational Research to Optimize Bedside Therapeutics of Sotalol Therapy Abstract Oral sotalol, used in adults for sinus rhythm control, is initiated at 80 mg b.i.d. and titrated to a maximum safe dose. The US Food and Drug Administration recommends monitoring the corrected QT interval (Q...
PMC4538962
core_pubmed_pmc
Serotonin Syndrome in the Setting of Lamotrigine, Aripiprazole, and Cocaine Use
Serotonin Syndrome in the Setting of Lamotrigine, Aripiprazole, and Cocaine Use Abstract Abstract Serotonin syndrome is a potentially life-threatening condition associated with increased serotonergic activity in the central nervous system. It is classically associated with the simultaneous administration of two seroton...
PMC6868113
core_pubmed_pmc
Tumor necrosis factor-mediated disposition of infliximab in ulcerative colitis patients
Tumor necrosis factor-mediated disposition of infliximab in ulcerative colitis patients Abstract Ulcerative Colitis (UC) is an inflammatory bowel disease typically affecting the colon. Patients with active UC have elevated tumor necrosis factor (TNF) concentrations in serum and colonic tissue. Infliximab is a monoclona...
PMC10985948
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, and safety of fesomersen, a novel antisense inhibitor of factor XI, in healthy Chinese, Japanese, and Caucasian volunteers
Pharmacokinetics, pharmacodynamics, and safety of fesomersen, a novel antisense inhibitor of factor XI, in healthy Chinese, Japanese, and Caucasian volunteers Abstract Abstract The inhibition of coagulation factor XI (FXI) presents an attractive approach for anticoagulation as it is not expected to increase the risk of...
PMC9796919
core_pubmed_pmc
Robenacoxib pharmacokinetics in sheep following oral, subcutaneous, and intravenous administration
Robenacoxib pharmacokinetics in sheep following oral, subcutaneous, and intravenous administration Abstract Abstract The aim of this study was to evaluate the pharmacokinetics (PK) of robenacoxib (RX), a COX‐2 selective non‐steroidal anti‐inflammatory drug, in sheep after single subcutaneous (SC), oral (PO), and intrav...
PMC9726570
core_pubmed_pmc
The impact of coronavirus disease 2019 (COVID-19) on the antimicrobial stewardship pharmacist workforce: A multicenter survey
The impact of coronavirus disease 2019 (COVID-19) on the antimicrobial stewardship pharmacist workforce: A multicenter survey Abstract Abstract Objective: The coronavirus disease 2019 (COVID-19) pandemic has required healthcare systems and hospitals to rapidly modify standard practice, including antimicrobial stewardsh...
PMC8609999
core_pubmed_pmc
A Phase I trial of talazoparib in patients with advanced hematologic malignancies
A Phase I trial of talazoparib in patients with advanced hematologic malignancies Abstract Aim: The objective of this study was to establish the maximum tolerated dose (MTD), safety, pharmacokinetics, and anti-leukemic activity of talazoparib. Patients & methods: This Phase I, two-cohort, dose-escalation trial evaluate...
PMC9879693
core_pubmed_pmc
Ciprofol: A Novel Alternative to Propofol in Clinical Intravenous Anesthesia?
Ciprofol: A Novel Alternative to Propofol in Clinical Intravenous Anesthesia? Abstract Abstract Ciprofol is a novel compound that was independently developed in China. According to the Chinese product instructions approved by the China National Medical Products Administration and the information of official website, in...
PMC7008171
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling to Understand the Absorption of Risperidone Orodispersible Film
Physiologically Based Pharmacokinetic Modeling to Understand the Absorption of Risperidone Orodispersible Film Abstract Objective The aim of the present study was to investigate the absorption routes as well as the potential application of the oral transmucosal delivery of risperidone orodispersible film (ODF) using ph...
PMC3985299
core_pubmed_pmc
Single Ascending Dose Safety and Pharmacokinetics of CDRI-97/78: First-in-Human Study of a Novel Antimalarial Drug
Single Ascending Dose Safety and Pharmacokinetics of CDRI-97/78: First-in-Human Study of a Novel Antimalarial Drug Abstract Background . CDRI 97/78 has shown efficacy in animal models of falciparum malaria. The present study is the first in-human phase I trial in healthy volunteers. Methods . The study was conducted in...
PMC8483230
core_pubmed_pmc
A Phase 3 Open-Label Study of Elexacaftor/Tezacaftor/Ivacaftor in Children 6 through 11 Years of Age with Cystic Fibrosis and at Least One F508del Allele
A Phase 3 Open-Label Study of Elexacaftor/Tezacaftor/Ivacaftor in Children 6 through 11 Years of Age with Cystic Fibrosis and at Least One F508del Allele Abstract Rationale: Elexacaftor/tezacaftor/ivacaftor (ELX/TEZ/IVA) was shown to be efficacious and safe in patients ≥12 years of age with cystic fibrosis and at least...
PMC9304184
core_pubmed_pmc
Combining factor VIII levels and thrombin/plasmin generation: A population pharmacokinetic‐pharmacodynamic model for patients with haemophilia A
Combining factor VIII levels and thrombin/plasmin generation: A population pharmacokinetic‐pharmacodynamic model for patients with haemophilia A Abstract Abstract Aims Prophylactic treatment of haemophilia A patients with factor VIII (FVIII) concentrate focuses on maintaining a minimal trough FVIII activity level to pr...
PMC11652163
core_pubmed_pmc
Impact of fresh grape juice on the pharmacokinetics of omeprazole: results of a food–drug interaction study
Impact of fresh grape juice on the pharmacokinetics of omeprazole: results of a food–drug interaction study Abstract Grapes have been widely used for dietary ailments due to their attributed pharmacological activities. Resveratrol, the chief constituent of grapes, is responsible for their pharmacological benefits. Howe...
PMC3786641
core_pubmed_pmc
A randomised, double-blind, parallel-group study to demonstrate equivalence in efficacy and safety of CT-P13 compared with innovator infliximab when coadministered with methotrexate in patients with active rheumatoid arthritis: the PLANETRA study
A randomised, double-blind, parallel-group study to demonstrate equivalence in efficacy and safety of CT-P13 compared with innovator infliximab when coadministered with methotrexate in patients with active rheumatoid arthritis: the PLANETRA study Abstract Abstract Objectives To compare the efficacy and safety of innova...
PMC5513124
core_pubmed_pmc
A randomized clinical pharmacokinetic trial of Tenofovir in blood, plasma and urine in adults with perfect, moderate and low PrEP adherence: the TARGET study
A randomized clinical pharmacokinetic trial of Tenofovir in blood, plasma and urine in adults with perfect, moderate and low PrEP adherence: the TARGET study Abstract Background Tenofovir disoproxil fumarate (TDF) is key component of pre-exposure prophylaxis (PrEP) and antiretroviral therapy (ART) for HIV, but existing...
PMC8367903
core_pubmed_pmc
Pharmacokinetics of preoperative intraperitoneal 5-FU in patients with pancreatic ductal adenocarcinoma
Pharmacokinetics of preoperative intraperitoneal 5-FU in patients with pancreatic ductal adenocarcinoma Abstract Abstract Purpose The aim was to investigate the pharmacokinetics of preoperatively administered intraperitoneal (IP) 5-FU in patients with resectable pancreatic ductal adenocarcinoma (PDAC) by analyzing leve...
PMC11015083
core_pubmed_pmc
Tofacitinib pharmacokinetics in children and adolescents with juvenile idiopathic arthritis
Tofacitinib pharmacokinetics in children and adolescents with juvenile idiopathic arthritis Abstract Abstract These analyses characterized tofacitinib pharmacokinetics (PKs) in children and adolescents with juvenile idiopathic arthritis (JIA). Data were pooled from phase I ( NCT01513902 ), phase III ( NCT02592434 ), an...
PMC11641104
core_pubmed_pmc
Two-in-one nanoparticle platform induces a strong therapeutic effect of targeted therapies in P-selectin–expressing cancers
Two-in-one nanoparticle platform induces a strong therapeutic effect of targeted therapies in P-selectin–expressing cancers Abstract Abstract Combined therapies in cancer treatment aim to enhance antitumor activity. However, delivering multiple small molecules imposes challenges, as different drugs have distinct pharma...
PMC6884979
core_pubmed_pmc
Co-Delivery of Docetaxel and Salinomycin to Target Both Breast Cancer Cells and Stem Cells by PLGA/TPGS Nanoparticles
Co-Delivery of Docetaxel and Salinomycin to Target Both Breast Cancer Cells and Stem Cells by PLGA/TPGS Nanoparticles Abstract Purpose Conventional chemotherapy is hampered by the presence of breast cancer stem cells (BCSCs). It is crucial to eradicating both the bulky breast cancer cells and BCSCs, using a combination...
PMC9293353
core_pubmed_pmc
The effect of chemotherapy on the exposure–response relation of abiraterone in metastatic castration‐resistant prostate cancer
The effect of chemotherapy on the exposure–response relation of abiraterone in metastatic castration‐resistant prostate cancer Abstract Abstract Aims To assess whether the exposure–response relation for abiraterone is different in pre‐chemotherapy patients compared to post‐chemotherapy patients with metastatic castrati...
PMC6683301
core_pubmed_pmc
A simple method for evaluation pharmacokinetics of glycyrrhetinic acid and potential drug-drug interaction between herbal ingredients
A simple method for evaluation pharmacokinetics of glycyrrhetinic acid and potential drug-drug interaction between herbal ingredients Abstract A simple validated high performance liquid chromatography method was developed for the evaluation of the effect of three kinds of active ingredients in traditional Chinese medic...
PMC6151750
core_pubmed_pmc
Construction of a Bivalent Thrombin Binding Aptamer and Its Antidote with Improved Properties
Construction of a Bivalent Thrombin Binding Aptamer and Its Antidote with Improved Properties Abstract Aptamers are short synthetic DNA or RNA oligonucleotides that adopt secondary and tertiary conformations based on Watson–Crick base-pairing interactions and can be used to target a range of different molecules. Two ap...
PMC6636803
core_pubmed_pmc
Estradiol and progesterone bioavailability for moderate to severe vasomotor symptom treatment and endometrial protection with the continuous-combined regimen of TX-001HR (oral estradiol and progesterone capsules)
Estradiol and progesterone bioavailability for moderate to severe vasomotor symptom treatment and endometrial protection with the continuous-combined regimen of TX-001HR (oral estradiol and progesterone capsules) Abstract Abstract Objective: In the REPLENISH trial, women receiving TX-001HR—an oral, softgel capsule, com...
PMC8886374
core_pubmed_pmc
Click Chemistry and Multicomponent Reaction for Linker Diversification of Zinc Dipicolylamine-Based Drug Conjugates
Click Chemistry and Multicomponent Reaction for Linker Diversification of Zinc Dipicolylamine-Based Drug Conjugates Abstract An efficient Ugi multicomponent reaction with strain promoted azide-alkyne cycloaddition protocol has been utilized in concert or independently to prepare a small family of bioactive zinc(II) dip...
PMC10220917
core_pubmed_pmc
Transdermal Delivery of α-Aminophosphonates as Semisolid Formulations—An In Vitro-Ex Vivo Study
Transdermal Delivery of α-Aminophosphonates as Semisolid Formulations—An In Vitro-Ex Vivo Study Abstract α-Aminophosphonates are organophosphorus compounds with an obvious similarity with α-amino acids. Owing to their biological and pharmacological characteristics, they have attracted the attention of many medicinal ch...
PMC12962483
core_pubmed_pmc
Purification and pharmacokinetic study of gadoxetate isomers for enhanced rabbit liver MR imaging
Purification and pharmacokinetic study of gadoxetate isomers for enhanced rabbit liver MR imaging Abstract This study aimed to purify and prepare two isomers of Gadoxetate (Gd-A and Gd-B) from Pumexian and evaluate their stability, magnetic resonance (MR) imaging characteristics, and pharmacokinetics in rabbits. Revers...
PMC12184692
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamic, Safety and Tolerability of Fazamorexant, a Novel Dual Orexin Receptor Antagonist: Report of the First-in-Human Study
Pharmacokinetics, Pharmacodynamic, Safety and Tolerability of Fazamorexant, a Novel Dual Orexin Receptor Antagonist: Report of the First-in-Human Study Abstract Abstract Purpose This is the first-in-human study to investigate the pharmacokinetic and pharmacodynamic profiles, safety, and tolerability of Fazamorexant (a ...
PMC12242392
core_pubmed_pmc
Association between the difference in creatinine-based and creatinine-cystatin C-based estimated glomerular filtration rates and vancomycin systemic exposure after ventricular assist device surgery
Association between the difference in creatinine-based and creatinine-cystatin C-based estimated glomerular filtration rates and vancomycin systemic exposure after ventricular assist device surgery Abstract Vancomycin is widely used as a prophylactic antibiotic for ventricular assist device (VAD) implantation to preven...
PMC12852064
core_pubmed_pmc
Development and Validation of a Novel Scoring Model Integrating Clinical Risk Factors and Pharmacokinetic Parameters to Predict Vancomycin‐Induced Nephrotoxicity
Development and Validation of a Novel Scoring Model Integrating Clinical Risk Factors and Pharmacokinetic Parameters to Predict Vancomycin‐Induced Nephrotoxicity Abstract ABSTRACT Background Vancomycin (VCM), a first‐line treatment option for infections caused by methicillin‐resistant Staphylococcus aureus , has been r...
PMC10058579
core_pubmed_pmc
Use of In Vitro Dynamic Colon Model (DCM) to Inform a Physiologically Based Biopharmaceutic Model (PBBM) to Predict the In Vivo Performance of a Modified-Release Formulation of Theophylline
Use of In Vitro Dynamic Colon Model (DCM) to Inform a Physiologically Based Biopharmaceutic Model (PBBM) to Predict the In Vivo Performance of a Modified-Release Formulation of Theophylline Abstract A physiologically based biopharmaceutic model (PBBM) of a modified-release formulation of theophylline (Uniphyllin Contin...
PMC12862634
core_pubmed_pmc
Development and pilot testing of U1 Adaptor therapy targeting SOD1 expression for dogs with degenerative myelopathy
Development and pilot testing of U1 Adaptor therapy targeting SOD1 expression for dogs with degenerative myelopathy Abstract Abstract Background Degenerative myelopathy (DM) is a progressive neurodegenerative disease in dogs associated with a superoxide dismutase 1 ( SOD1 ) gene mutation, resulting in SOD1 protein aggr...
PMC11449743
core_pubmed_pmc
A quantitative systems pharmacology (QSP) platform for preclinical to clinical translation of in-vivo CRISPR-Cas therapy
A quantitative systems pharmacology (QSP) platform for preclinical to clinical translation of in-vivo CRISPR-Cas therapy Abstract Background: In-vivo CRISPR Cas genome editing is a complex therapy involving lipid nanoparticle (LNP), messenger RNA (mRNA), and single guide RNA (sgRNA). This novel modality requires prior ...
PMC6211373
core_pubmed_pmc
Darunavir–cobicistat–emtricitabine–tenofovir alafenamide: safety and efficacy of a protease inhibitor in the modern era
Darunavir–cobicistat–emtricitabine–tenofovir alafenamide: safety and efficacy of a protease inhibitor in the modern era Abstract Abstract A fixed-dose combination consisting of darunavir (Drv), cobicistat (Cobi), emtricitabine (2′,3′-dideoxy-5-fluoro-3′-thiacytidine [FTC]), and tenofovir alafenamide (Taf) has been rece...
PMC10154607
core_pubmed_pmc
A phase I study to assess safety, pharmacokinetics, and pharmacodynamics of a vaginal insert containing tenofovir alafenamide and elvitegravir
A phase I study to assess safety, pharmacokinetics, and pharmacodynamics of a vaginal insert containing tenofovir alafenamide and elvitegravir Abstract Abstract Background New multi-purpose prevention technology (MPT) products are needed to prevent human immunodeficiency virus (HIV) and herpes simplex virus type 2 (HSV...
PMC7163368
core_pubmed_pmc
Safety, tolerability, pharmacokinetics and pharmacodynamics of parenterally administered dutogliptin: A prospective dose‐escalating trial
Safety, tolerability, pharmacokinetics and pharmacodynamics of parenterally administered dutogliptin: A prospective dose‐escalating trial Abstract Abstract Aims Animal studies suggest that inhibition of dipeptidyl peptidase 4 (DPP‐IV) may improve heart function and survival after myocardial infarction by increasing car...
PMC12731757
core_pubmed_pmc
Mechanistic Insights into Antioxidant Interventions Targeting Obesity-Induced Oxidative Stress in the Pathogenesis and Complications of Type 2 Diabetes Mellitus
Mechanistic Insights into Antioxidant Interventions Targeting Obesity-Induced Oxidative Stress in the Pathogenesis and Complications of Type 2 Diabetes Mellitus Abstract Abstract Diabetes mellitus (DM) is a complex, heterogeneous, hyperglycemic chronic metabolic disorder. Type 2 diabetes mellitus (T2DM) is characterize...
PMC8578158
core_pubmed_pmc
Preclinical Evaluation of 89 Zr-Df-IAB22M2C PET as an Imaging Biomarker for the Development of the GUCY2C-CD3 Bispecific PF-07062119 as a T Cell Engaging Therapy
Preclinical Evaluation of 89 Zr-Df-IAB22M2C PET as an Imaging Biomarker for the Development of the GUCY2C-CD3 Bispecific PF-07062119 as a T Cell Engaging Therapy Abstract Abstract Purpose A sensitive and specific imaging biomarker to monitor immune activation and quantify pharmacodynamic responses would be useful for d...
PMC10003737
core_pubmed_pmc
Impact of Hypoalbuminemia on Ceftriaxone Treatment Failure in Patients With Enterobacterales Bacteremia: A Propensity-Matched, Retrospective Cohort Study
Impact of Hypoalbuminemia on Ceftriaxone Treatment Failure in Patients With Enterobacterales Bacteremia: A Propensity-Matched, Retrospective Cohort Study Abstract Abstract Background Ceftriaxone is frequently prescribed due to its convenience of dosing and robust antimicrobial activity. However, patients with hypoalbum...
PMC9370395
core_pubmed_pmc
Pharmacokinetic Comparison of Chitosan-Derived and Biofermentation-Derived Glucosamine in Nutritional Supplement for Bone Health
Pharmacokinetic Comparison of Chitosan-Derived and Biofermentation-Derived Glucosamine in Nutritional Supplement for Bone Health Abstract Glucosamine and chondroitin sulfate have been used as nutritional supplementation for joint tissues and osteoarthritis (OA). Biofermented glucosamine is of great interest in the supp...
PMC5335600
core_pubmed_pmc
SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules
SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules Abstract To be effective as a drug, a potent molecule must reach its target in the body in sufficient concentration, and stay there in a bioactive form long enough for the expected biologic eve...
PMC5398684
core_pubmed_pmc
Pharmacokinetics and relative bioavailability of an oral amoxicillin-apramycin combination in pigs
Pharmacokinetics and relative bioavailability of an oral amoxicillin-apramycin combination in pigs Abstract A new compound granular premix of amoxicillin (20% w/w dry mass)/apramycin (5% w/w dry mass) was developed, and its pharmacokinetics and relative bioavailability were determined in pigs following oral administrat...
PMC3862057
core_pubmed_pmc
High-Performance Liquid Chromatographic Determination of Rivastigmine in Human Plasma for Application in Pharmacokinetic Studies
High-Performance Liquid Chromatographic Determination of Rivastigmine in Human Plasma for Application in Pharmacokinetic Studies Abstract A simple and reproducible HPLC method with spectrophotometric detection was developed for determination of rivastigmine in human plasma. Liquid-liquid extraction of rivastigmine and ...
PMC12497816
core_pubmed_pmc
Dual-edged mechanisms of α-tomatine in hepatocellular carcinoma by suppression of Wnt/β-catenin signaling versus RelB-Driven resistance in tumor therapy
Dual-edged mechanisms of α-tomatine in hepatocellular carcinoma by suppression of Wnt/β-catenin signaling versus RelB-Driven resistance in tumor therapy Abstract Abstract Background The plant-derived steroidal alkaloid α-tomatine has emerged as a promising pan-cancer therapeutic agent, its multifaceted biological effec...
PMC6594085
core_pubmed_pmc
Absence of Drug‐Drug Interaction of Anastrozole on Levonorgestrel Delivered Simultaneously by an Intravaginal Ring: Results of a Phase 2 Trial
Absence of Drug‐Drug Interaction of Anastrozole on Levonorgestrel Delivered Simultaneously by an Intravaginal Ring: Results of a Phase 2 Trial Abstract Abstract Intravaginal rings (IVRs) are an established option for continuous administration of drugs in women. The combination of anastrozole (ATZ) and levonorgestrel (L...
PMC4142138
core_pubmed_pmc
The pharmacokinetics of conventional and bioenhanced tablet formulations of danirixin (GSK1325756) following oral administration in healthy, elderly, human volunteers
The pharmacokinetics of conventional and bioenhanced tablet formulations of danirixin (GSK1325756) following oral administration in healthy, elderly, human volunteers Abstract Abstract Danirixin (GSK1325756) is a small, high-affinity, selective and reversible CXCR2 antagonist in development for treatment of chronic obs...
PMC12174962
core_pubmed_pmc
A Pharmacokinetic Study of Zavegepant Nasal Spray in Healthy Adults Comparing Conventional Venous Blood Sampling With Patient‐Centric Microsampling
A Pharmacokinetic Study of Zavegepant Nasal Spray in Healthy Adults Comparing Conventional Venous Blood Sampling With Patient‐Centric Microsampling Abstract ABSTRACT This Phase 1, non‐randomized, open‐label, 2‐period study compared the pharmacokinetics (PK) of zavegepant nasal spray, using samples collected via patient...
PMC8875492
core_pubmed_pmc
IDELVION: A Comprehensive Review of Clinical Trial and Real-World Data
IDELVION: A Comprehensive Review of Clinical Trial and Real-World Data Abstract Hemophilia B is a bleeding disorder caused by a deficiency of coagulation factor IX (FIX). Treatment with FIX replacement products can increase FIX activity levels to minimize or prevent bleeding events. However, frequent dosing with standa...
PMC7996295
core_pubmed_pmc
Pharmacometric Evaluation of Umbilical Cord Blood Concentration-Based Early Initiation of Treatment in Methadone-Exposed Preterm Neonates
Pharmacometric Evaluation of Umbilical Cord Blood Concentration-Based Early Initiation of Treatment in Methadone-Exposed Preterm Neonates Abstract In methadone-exposed preterm neonates, early identification of those at risk of severe neonatal abstinence syndrome (NAS) and use of a methadone dosing regimen that can prov...
PMC12394267
core_pubmed_pmc
Bioequivalence and Pharmacokinetic Evaluation of Two Metformin Hydrochloride Tablets Under Fasting and Fed Conditions in Healthy Chinese Volunteers
Bioequivalence and Pharmacokinetic Evaluation of Two Metformin Hydrochloride Tablets Under Fasting and Fed Conditions in Healthy Chinese Volunteers Abstract Background and Objectives With diabetes prevalence rising and original formulations unable to meet demand, establishing generic equivalence is crucial for treatmen...
PMC7318514
core_pubmed_pmc
Pharmacokinetic study of two different rifabutin doses co-administered with lopinavir/ritonavir in African HIV and tuberculosis co-infected adult patients
Pharmacokinetic study of two different rifabutin doses co-administered with lopinavir/ritonavir in African HIV and tuberculosis co-infected adult patients Abstract Abstract Background This study aimed to assess the pharmacokinetic profile of 150 mg rifabutin (RBT) taken every other day (every 48 h) versus 300 mg RBT ta...
PMC3066559
core_pubmed_pmc
Antibody-Hapten Recognition at the Surface of Functionalized Liposomes Studied by SPR: Steric Hindrance of Pegylated Phospholipids in Stealth Liposomes Prepared for Targeted Radionuclide Delivery
Antibody-Hapten Recognition at the Surface of Functionalized Liposomes Studied by SPR: Steric Hindrance of Pegylated Phospholipids in Stealth Liposomes Prepared for Targeted Radionuclide Delivery Abstract Abstract Targeted PEGylated liposomes could increase the amount of drugs or radionuclides delivered to tumor cells....
PMC8946248
core_pubmed_pmc
Radiolabeled Antibodies for Cancer Imaging and Therapy
Radiolabeled Antibodies for Cancer Imaging and Therapy Abstract Simple Summary Monoclonal antibodies (mAbs) have the ability to specifically target tumor-cell antigens. This unique property has led to their use in the delivery of radioisotopes to tumor sites (scintigraphic imaging and radioimmunotherapy (RIT)). The cho...
PMC8249270
core_pubmed_pmc
Exposure–Bleeding Count Modeling of Emicizumab for the Prophylaxis of Bleeding in Persons with Hemophilia A with/Without Inhibitors Against Factor VIII
Exposure–Bleeding Count Modeling of Emicizumab for the Prophylaxis of Bleeding in Persons with Hemophilia A with/Without Inhibitors Against Factor VIII Abstract Abstract Background and Objective Emicizumab is a monoclonal antibody that bridges activated coagulation factor IX and factor X to restore effective hemostasis...
PMC8274693
core_pubmed_pmc
Health Effects of Naphthalene Exposure: A Systematic Evidence Map and Analysis of Potential Considerations for Dose–Response Evaluation
Health Effects of Naphthalene Exposure: A Systematic Evidence Map and Analysis of Potential Considerations for Dose–Response Evaluation Abstract Background: Naphthalene is a polycyclic aromatic hydrocarbon that has been associated with health effects, including cancer. As the state of the science on naphthalene toxicit...
PMC4067622
core_pubmed_pmc
Small molecule inhibitors of HCV replication from Pomegranate
Small molecule inhibitors of HCV replication from Pomegranate Abstract Hepatitis C virus (HCV) is the causative agent of end-stage liver disease. Recent advances in the last decade in anti HCV treatment strategies have dramatically increased the viral clearance rate. However, several limitations are still associated, w...
PMC3108736
core_pubmed_pmc
Prevention strategies for antimicrobial resistance: a systematic review of the literature
Prevention strategies for antimicrobial resistance: a systematic review of the literature Abstract Abstract Antibiotics offer great benefits by reducing the duration and severity of illnesses and aiding in infection transmission control. With this being said, the inexorable process of antimicrobial drug resistance is t...
PMC9486188
core_pubmed_pmc
Randomized, placebo-controlled, single-blind phase 1 studies of the safety, tolerability, and pharmacokinetics of BRII-196 and BRII-198, SARS-CoV-2 spike-targeting monoclonal antibodies with an extended half-life in healthy adults
Randomized, placebo-controlled, single-blind phase 1 studies of the safety, tolerability, and pharmacokinetics of BRII-196 and BRII-198, SARS-CoV-2 spike-targeting monoclonal antibodies with an extended half-life in healthy adults Abstract Abstract Background: BRII-196 and BRII-198 are two anti-SARS-CoV-2 monoclonal ne...
PMC12964010
core_pubmed_pmc
Specific in vivo detection of V2R-positive metastatic ccRCC using a toxin-based PET radioligand
Specific in vivo detection of V2R-positive metastatic ccRCC using a toxin-based PET radioligand Abstract Abstract Background The diagnosis of metastatic clear cell renal cell carcinoma (mccRCC) remains challenging due to the tumor's molecular heterogeneity, often resulting in low sensitivity and a high false-positive r...
PMC9291822
core_pubmed_pmc
Pharmacokinetics of capmatinib in participants with hepatic impairment: A phase 1, open‐label, single‐dose, parallel‐group study
Pharmacokinetics of capmatinib in participants with hepatic impairment: A phase 1, open‐label, single‐dose, parallel‐group study Abstract Aims Capmatinib, a mesenchymal–epithelial transition factor tyrosine kinase inhibitor, is metabolized by cytochrome P450 (CYP) 3A4 and aldehyde oxidase. In individuals with hepatic i...
PMC5238771
core_pubmed_pmc
Radiosynthesis and pharmacokinetics of [ 18 F]fluoroethyl bufalin in hepatocellular carcinoma-bearing mice
Radiosynthesis and pharmacokinetics of [ 18 F]fluoroethyl bufalin in hepatocellular carcinoma-bearing mice Abstract Purpose Bufalin, the main component of a Chinese traditional medicine chansu, shows convincing anticancer effects in a lot of tumor cell lines. However, its in vivo behavior is still unclear. This researc...
PMC7214659
core_pubmed_pmc
Impact of SLCO1B1 Genetic Variation on Rosuvastatin Systemic Exposure in Pediatric Hypercholesterolemia
Impact of SLCO1B1 Genetic Variation on Rosuvastatin Systemic Exposure in Pediatric Hypercholesterolemia Abstract Abstract This study investigated the impact of SLCO1B1 genotype on rosuvastatin systemic exposure in hypercholesterolemic children and adolescents. Participants (8–21 years) with at least one allelic variant...
PMC8780701
core_pubmed_pmc
Pharmacokinetics and Metabolism Study of Deep-Sea-Derived Butyrolactone I in Rats by UHPLC–MS/MS and UHPLC–Q-TOF-MS
Pharmacokinetics and Metabolism Study of Deep-Sea-Derived Butyrolactone I in Rats by UHPLC–MS/MS and UHPLC–Q-TOF-MS Abstract Butyrolactone I (BTL-I) is a butanolide isolated from the deep-sea-derived fungus, Aspergillus sp. It provides a potential new target for the prevention and treatment of food allergies. This stud...
PMC11672110
core_pubmed_pmc
Phase 1b/2 study of orally administered pexidartinib in combination with radiation therapy and temozolomide in patients with newly diagnosed glioblastoma
Phase 1b/2 study of orally administered pexidartinib in combination with radiation therapy and temozolomide in patients with newly diagnosed glioblastoma Abstract Abstract Background Glioblastoma (GBM) has a median survival of <2 years. Pexidartinib (PLX3397) is a small-molecule inhibitor of CSF1R, KIT, and oncogenic F...
PMC9738601
core_pubmed_pmc
HPLC with Fluorescence and Photodiode Array Detection for Quantifying Capmatinib in Biological Samples: Application to In Vivo and In Vitro Studies
HPLC with Fluorescence and Photodiode Array Detection for Quantifying Capmatinib in Biological Samples: Application to In Vivo and In Vitro Studies Abstract Capmatinib, a recently approved tyrosine kinase inhibitor, is used for the treatment of non-small cell lung cancer. We describe two new HPLC methods for capmatinib...
PMC6071274
core_pubmed_pmc
Nucleobase and Nucleoside Analogues: Resistance and Re-Sensitisation at the Level of Pharmacokinetics, Pharmacodynamics and Metabolism
Nucleobase and Nucleoside Analogues: Resistance and Re-Sensitisation at the Level of Pharmacokinetics, Pharmacodynamics and Metabolism Abstract Antimetabolites, in particular nucleobase and nucleoside analogues, are cytotoxic drugs that, starting from the small field of paediatric oncology, in combination with other ch...
PMC4569392
core_pubmed_pmc
Randomized placebo-controlled dose-ranging and pharmacodynamics study of roxadustat (FG-4592) to treat anemia in nondialysis-dependent chronic kidney disease (NDD-CKD) patients
Randomized placebo-controlled dose-ranging and pharmacodynamics study of roxadustat (FG-4592) to treat anemia in nondialysis-dependent chronic kidney disease (NDD-CKD) patients Abstract Background Roxadustat (FG-4592) is an oral hypoxia-inducible factor prolyl hydroxylase inhibitor that stimulates erythropoiesis. This ...
PMC6591616
core_pubmed_pmc
A First-in-Human Study To Assess the Safety and Pharmacokinetics of LYS228, a Novel Intravenous Monobactam Antibiotic in Healthy Volunteers
A First-in-Human Study To Assess the Safety and Pharmacokinetics of LYS228, a Novel Intravenous Monobactam Antibiotic in Healthy Volunteers Abstract Infections caused by antibiotic-resistant Gram-negative bacteria expressing extended-spectrum β-lactamases and carbapenemases are a growing global problem resulting in inc...
PMC9401498
core_pubmed_pmc
A Phase I Dose-Escalation and Expansion Study of Telaglenastat in Patients with Advanced or Metastatic Solid Tumors
A Phase I Dose-Escalation and Expansion Study of Telaglenastat in Patients with Advanced or Metastatic Solid Tumors Abstract Abstract Purpose: Glutamine is a critical fuel for solid tumors. Interference with glutamine metabolism is deleterious to neoplasia in preclinical models. A phase I study of the oral, first-in-cl...
PMC11750724
core_pubmed_pmc
Autogene cevumeran with or without atezolizumab in advanced solid tumors: a phase 1 trial
Autogene cevumeran with or without atezolizumab in advanced solid tumors: a phase 1 trial Abstract Effective targeting of somatic cancer mutations to enhance the efficacy of cancer immunotherapy requires an individualized approach. Autogene cevumeran is a uridine messenger RNA lipoplex-based individualized neoantigen-s...
PMC9431699
core_pubmed_pmc
Activity of Delafloxacin and Levofloxacin against Stenotrophomonas maltophilia at Simulated Plasma and Intrapulmonary pH Values
Activity of Delafloxacin and Levofloxacin against Stenotrophomonas maltophilia at Simulated Plasma and Intrapulmonary pH Values Abstract ABSTRACT Fluoroquinolones have become a popular treatment option for Stenotrophomonas maltophilia infections. Although levofloxacin is most commonly used, delafloxacin demonstrates co...
PMC4962284
core_pubmed_pmc
Environmental Risk Factors in Psoriasis: The Point of View of the Nutritionist
Environmental Risk Factors in Psoriasis: The Point of View of the Nutritionist Abstract Abstract Psoriasis is a common, chronic, immune-mediated skin disease with systemic pro-inflammatory activation, where both environmental and genetic factors contribute to its pathogenesis. Among the risk factors for psoriasis, evid...
PMC5487209
core_pubmed_pmc
A mathematical analysis of rebound in a target-mediated drug disposition model: II. With feedback
A mathematical analysis of rebound in a target-mediated drug disposition model: II. With feedback Abstract Abstract We consider the possibility of free receptor (antigen/cytokine) levels rebounding to higher than the baseline level after the application of an antibody drug using a target-mediated drug disposition model...
PMC3827994
core_pubmed_pmc
Novel preclinical models of topical PrEP pharmacodynamics provide rationale for combination of drugs with complementary properties
Novel preclinical models of topical PrEP pharmacodynamics provide rationale for combination of drugs with complementary properties Abstract Background The limited success of recent HIV topical pre-exposure prophylaxis clinical trials highlights the need for more predictive models of drug efficacy that better simulate w...
PMC6955125
core_pubmed_pmc
Comparative Pharmacokinetic Study of Taxifolin after Oral Administration of Fructus Polygoni Orientalis Extract in Normal and Fibrotic Rats by UPLC-MS/MS
Comparative Pharmacokinetic Study of Taxifolin after Oral Administration of Fructus Polygoni Orientalis Extract in Normal and Fibrotic Rats by UPLC-MS/MS Abstract Abstract Fructus polygoni orientalis (FPO) is widely used in clinical practice in China, especially in treatment of liver diseases including viral hepatitis,...
PMC7696733
core_pubmed_pmc
A Physiologically-Based Pharmacokinetic Model of Trimethoprim for MATE1, OCT1, OCT2, and CYP2C8 Drug–Drug–Gene Interaction Predictions
A Physiologically-Based Pharmacokinetic Model of Trimethoprim for MATE1, OCT1, OCT2, and CYP2C8 Drug–Drug–Gene Interaction Predictions Abstract Abstract Trimethoprim is a frequently-prescribed antibiotic and therefore likely to be co-administered with other medications, but it is also a potent inhibitor of multidrug an...
PMC11149917
core_pubmed_pmc
Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers
Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers Abstract Abstract RAS-driven cancers comprise up to 30% of human cancers. RMC-6236 is a RAS(ON) multi-selective noncovalent inhibitor of the active, GTP-bound state of both mutant and wild-type variants of canonical RAS iso...
PMC4777954
core_pubmed_pmc
The Influence of Patient Characteristics on Anticholinergic Events in Older People
The Influence of Patient Characteristics on Anticholinergic Events in Older People Abstract Aims To examine patient characteristics that predict adverse anticholinergic-type events in older people. Methods This retrospective population-level study included 2,248 hospitalised patients. Individual data on medicines that ...
PMC6709421
core_pubmed_pmc
Physiologically‐Based Pharmacokinetic Modeling for the Prediction of CYP2D6‐Mediated Gene–Drug–Drug Interactions
Physiologically‐Based Pharmacokinetic Modeling for the Prediction of CYP2D6‐Mediated Gene–Drug–Drug Interactions Abstract Abstract The aim of this work was to predict the extent of Cytochrome P450 2D6 (CYP2D6)‐mediated drug–drug interactions (DDIs) in different CYP2D6 genotypes using physiologically‐based pharmacokinet...
PMC6709501
core_pubmed_pmc
Safety, Pharmacokinetics, and Food Effect of Tebipenem Pivoxil Hydrobromide after Single and Multiple Ascending Oral Doses in Healthy Adult Subjects
Safety, Pharmacokinetics, and Food Effect of Tebipenem Pivoxil Hydrobromide after Single and Multiple Ascending Oral Doses in Healthy Adult Subjects Abstract Tebipenem pivoxil hydrobromide (TBPM-PI-HBr, formerly SPR994) is an orally available prodrug of tebipenem, a carbapenem with activity versus multidrug-resistant (...
PMC11869757
core_pubmed_pmc
SHR-1916: A Novel PEGylated Interleukin-2 Analogue with Altered Cellular Selectivity and Improved Pharmacokinetic Profiles for Cancer Immunotherapy
SHR-1916: A Novel PEGylated Interleukin-2 Analogue with Altered Cellular Selectivity and Improved Pharmacokinetic Profiles for Cancer Immunotherapy Abstract Purpose Human interleukin-2 (IL-2) stimulates the differentiation and expansion of diverse immune cells dose-dependently. As an immunotherapy agent to treat metast...
PMC7886095
core_pubmed_pmc
Self-Nanoemulsifying Drug Delivery System of Genkwanin: A Novel Approach for Anti-Colitis-Associated Colorectal Cancer
Self-Nanoemulsifying Drug Delivery System of Genkwanin: A Novel Approach for Anti-Colitis-Associated Colorectal Cancer Abstract Purpose The aim of the present study was to develop an optimized Genkwanin (GKA)-loaded self-nanoemulsifying drug delivery system (SNEDDS) formulation to enhance the solubility, intestinal per...
PMC6861974
core_pubmed_pmc
Self-Reported Sleep Disturbance from Road, Rail and Aircraft Noise: Exposure-Response Relationships and Effect Modifiers in the SiRENE Study
Self-Reported Sleep Disturbance from Road, Rail and Aircraft Noise: Exposure-Response Relationships and Effect Modifiers in the SiRENE Study Abstract This survey investigates the cross-sectional association between nighttime road, rail and aircraft noise exposure and the probability to be highly sleep disturbed (%HSD),...
PMC12462467
core_pubmed_pmc
Ophthalmic drug discovery and development using artificial intelligence and digital health technologies
Ophthalmic drug discovery and development using artificial intelligence and digital health technologies Abstract Abstract Globally, drug discovery and development programs are complex, multi-decade long and prohibitively expensive. Artificial intelligence (AI) and other digital health technologies have the potential to...
PMC6307086
core_pubmed_pmc
Modular Nanoparticulate Prodrug Design Enables Efficient Treatment of Solid Tumors Using Bioorthogonal Activation
Modular Nanoparticulate Prodrug Design Enables Efficient Treatment of Solid Tumors Using Bioorthogonal Activation Abstract Abstract Prodrug strategies that facilitate localized and controlled activity of small-molecule therapeutics can reduce systemic exposure and improve pharmacokinetics, yet limitations in activation...
PMC9811530
core_pubmed_pmc
Selective Inhibition of 11beta-Hydroxysteroiddehydrogenase-1 with BI 187004 in Patients with Type 2 Diabetes and Overweight or Obesity: Safety, Pharmacokinetics, and Pharmacodynamics After Multiple Dosing Over 14 Days
Selective Inhibition of 11beta-Hydroxysteroiddehydrogenase-1 with BI 187004 in Patients with Type 2 Diabetes and Overweight or Obesity: Safety, Pharmacokinetics, and Pharmacodynamics After Multiple Dosing Over 14 Days Abstract Objective To assess safety, tolerability, pharmacokinetics, and pharmacodynamics of treatment...
PMC11968426
core_pubmed_pmc
The effect of high-fat diet on the pharmacokinetics of ondansetron hydrochloride tablets in healthy Chinese subjects
The effect of high-fat diet on the pharmacokinetics of ondansetron hydrochloride tablets in healthy Chinese subjects Abstract Abstract Background This study aimed to assess how a high-fat diet impacts the pharmacokinetics and safety characteristics of 8 mg Ondansetron hydrochloride tablets among healthy Chinese individ...
PMC4302156
core_pubmed_pmc
Fixed dose artesunate amodiaquine – a phase IIb, randomized comparative trial with non-fixed artesunate amodiaquine
Fixed dose artesunate amodiaquine – a phase IIb, randomized comparative trial with non-fixed artesunate amodiaquine Abstract Abstract Background Pharmacokinetic (PK) and pharmacodynamic (PD) data are limited for artesunate (AS) and amodiaquine (AQ) in uncomplicated Plasmodium falciparum . Methods From 2007-8, 54 P. fal...
PMC6373376
core_pubmed_pmc
Effect of Fluconazole Coadministration and CYP2C9 Genetic Polymorphism on Siponimod Pharmacokinetics in Healthy Subjects
Effect of Fluconazole Coadministration and CYP2C9 Genetic Polymorphism on Siponimod Pharmacokinetics in Healthy Subjects Abstract Objectives The aim of this study was to assess the pharmacokinetics (PK) and safety/tolerability of siponimod in healthy subjects when coadministered with (1) the moderate cytochrome P450 (C...
PMC12312931
core_pubmed_pmc
Dalpiciclib combined with pyrotinib and endocrine therapy in women with ER-positive, HER2-positive advanced breast cancer: A prospective, multicenter, single-arm, phase 2 trial
Dalpiciclib combined with pyrotinib and endocrine therapy in women with ER-positive, HER2-positive advanced breast cancer: A prospective, multicenter, single-arm, phase 2 trial Abstract Abstract Background Combination of HER2-targeted therapy and endocrine therapy offers a more tolerable alternative to HER2-targeted ch...
PMC11098157
core_pubmed_pmc
A physiologically‐based pharmacokinetic/pharmacodynamic modeling approach for drug–drug‐gene interaction evaluation of S‐warfarin with fluconazole
A physiologically‐based pharmacokinetic/pharmacodynamic modeling approach for drug–drug‐gene interaction evaluation of S‐warfarin with fluconazole Abstract Abstract Warfarin is a widely used anticoagulant, and its S‐enantiomer has higher potency compared to the R‐enantiomer. S‐warfarin is mainly metabolized by cytochro...