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PMC7492243 | core_pubmed_pmc | Early treatment-related neutropenia predicts response to palbociclib | Early treatment-related neutropenia predicts response to palbociclib Abstract Background Palbociclib is highly active in oestrogen-receptor positive (ER+) metastatic breast cancer, but neutropenia is dose limiting. The goal of this study was to determine whether early neutropenia is associated with disease response to ... |
PMC12943562 | core_pubmed_pmc | Therapeutic Drug Monitoring of Direct Oral Anticoagulants and Its Association with Clinical Outcomes: A Systematic Review and Meta-Analysis | Therapeutic Drug Monitoring of Direct Oral Anticoagulants and Its Association with Clinical Outcomes: A Systematic Review and Meta-Analysis Abstract Abstract Background: Direct oral anticoagulants (DOACs) are now the preferred anticoagulant over vitamin K antagonists for patients with atrial fibrillation (AF) and venou... |
PMC8212710 | core_pubmed_pmc | Characterization of LY2775240, a selective phosphodiesterase‐4 inhibitor, in nonclinical models and in healthy subjects | Characterization of LY2775240, a selective phosphodiesterase‐4 inhibitor, in nonclinical models and in healthy subjects Abstract Abstract LY2775240 is a highly selective, potent and orally‐administered inhibitor of phosphodiesterase 4 (PDE4), and is being investigated as a treatment option for inflammatory disorders, s... |
PMC4673554 | core_pubmed_pmc | ODM-201: a new-generation androgen receptor inhibitor in castration-resistant prostate cancer | ODM-201: a new-generation androgen receptor inhibitor in castration-resistant prostate cancer Abstract Abstract Androgen deprivation therapy is the standard of care for patients with advanced hormone-sensitive prostate cancer. Despite an initial response, most patients progress to castration-resistant prostate cancer (... |
PMC11456789 | core_pubmed_pmc | Nonlinear mixed models and related approaches in infectious disease modeling: A systematic and critical review | Nonlinear mixed models and related approaches in infectious disease modeling: A systematic and critical review Abstract The level of surveillance and preparedness against epidemics varies across countries, resulting in different responses to outbreaks. When conducting an in-depth analysis of microinfection dynamics, on... |
PMC7245748 | core_pubmed_pmc | High fat diet significantly changed the global gene expression profile involved in hepatic drug metabolism and pharmacokinetic system in mice | High fat diet significantly changed the global gene expression profile involved in hepatic drug metabolism and pharmacokinetic system in mice Abstract Background High fat diet impact transcription of hepatic genes responsible for drug metabolism and pharmacokinetics. Until now, researches just focused on a couple speci... |
PMC12841128 | core_pubmed_pmc | LASSBio-1986 as a Multifunctional Antidiabetic Lead: SGLT1/2 Docking, Redox–Inflammatory Modulation and Metabolic Benefits in C57BL/6 Mice | LASSBio-1986 as a Multifunctional Antidiabetic Lead: SGLT1/2 Docking, Redox–Inflammatory Modulation and Metabolic Benefits in C57BL/6 Mice Abstract Abstract Type 2 diabetes mellitus (T2DM) involves chronic hyperglycemia, insulin resistance, low-grade inflammation, and oxidative stress that drive cardiometabolic and ren... |
PMC7706287 | core_pubmed_pmc | Targeting the myeloid checkpoint receptor SIRPα potentiates innate and adaptive immune responses to promote anti-tumor activity | Targeting the myeloid checkpoint receptor SIRPα potentiates innate and adaptive immune responses to promote anti-tumor activity Abstract Abstract Background Signal regulatory protein α (SIRPα) is a myeloid-lineage inhibitory receptor that restricts innate immunity through engagement of its cell surface ligand CD47. Blo... |
PMC12256560 | core_pubmed_pmc | An Integrative Mechanistic Model of Type 1 IFN‐Mediated Inflammation in Systemic Lupus Erythematosus | An Integrative Mechanistic Model of Type 1 IFN‐Mediated Inflammation in Systemic Lupus Erythematosus Abstract ABSTRACT Type I interferon (IFN1) pathway–targeting therapies represent a highly promising class of remedies for the treatment of systemic lupus erythematosus. However, the overall clinical benefit of these com... |
PMC5200844 | core_pubmed_pmc | Development of a Web-Accessible Population Pharmacokinetic Service—Hemophilia (WAPPS-Hemo): Study Protocol | Development of a Web-Accessible Population Pharmacokinetic Service—Hemophilia (WAPPS-Hemo): Study Protocol Abstract Background Individual pharmacokinetic assessment is a critical component of tailored prophylaxis for hemophilia patients. Population pharmacokinetics allows using individual sparse data, thus simplifying ... |
PMC12196396 | core_pubmed_pmc | DFT-Based Elucidation and Evaluation of Selenium-Modified Tacrine Derivatives: Theoretical and Physicochemical Insights for Alzheimer’s Disease Therapy | DFT-Based Elucidation and Evaluation of Selenium-Modified Tacrine Derivatives: Theoretical and Physicochemical Insights for Alzheimer’s Disease Therapy Abstract Abstract The incorporation of selenium into tacrine derivatives has been explored as a novel strategy to enhance therapeutic efficacy while minimizing toxicity... |
PMC9315316 | core_pubmed_pmc | Pharmacokinetics of Cannabis and Its Derivatives in Animals and Humans During Pregnancy and Breastfeeding | Pharmacokinetics of Cannabis and Its Derivatives in Animals and Humans During Pregnancy and Breastfeeding Abstract Cannabis is one of the most widely used illicit drugs during pregnancy and lactation. With the recent legalization of cannabis in many countries, health professionals are increasingly exposed to pregnant a... |
PMC3882252 | core_pubmed_pmc | Anti-Prion Activity of a Panel of Aromatic Chemical Compounds: In Vitro and In Silico Approaches | Anti-Prion Activity of a Panel of Aromatic Chemical Compounds: In Vitro and In Silico Approaches Abstract Abstract The prion protein (PrP) is implicated in the Transmissible Spongiform Encephalopathies (TSEs), which comprise a group of fatal neurodegenerative diseases affecting humans and other mammals. Conversion of c... |
PMC9521607 | core_pubmed_pmc | Bioequivalence and safety evaluation of two preparations of metformin hydrochloride sustained-release tablets (Boke ® and Glucophage ® -XR) in healthy Chinese volunteers: a randomized phase I clinical trial | Bioequivalence and safety evaluation of two preparations of metformin hydrochloride sustained-release tablets (Boke ® and Glucophage ® -XR) in healthy Chinese volunteers: a randomized phase I clinical trial Abstract Abstract Background As per the National Medical Products Administration (NMPA) requirements, the quality... |
PMC8401685 | core_pubmed_pmc | Levetiracetam Therapeutic Drug Monitoring in a Large Cohort of Korean Epileptic Patients | Levetiracetam Therapeutic Drug Monitoring in a Large Cohort of Korean Epileptic Patients Abstract Levetiracetam is a new antiepileptic drug (AED) used for treating and preventing partial or generalized seizures. The usefulness of levetiracetam therapeutic drug monitoring (TDM) is related to inter- or intra-individual p... |
PMC10891722 | core_pubmed_pmc | Population Pharmacodynamic Models of Risperidone on PANSS Total Scores and Prolactin Levels in Schizophrenia | Population Pharmacodynamic Models of Risperidone on PANSS Total Scores and Prolactin Levels in Schizophrenia Abstract Currently, research predominantly focuses on evaluating clinical effects at specific time points while neglecting underlying patterns within the treatment process. This study aims to analyze the dynamic... |
PMC11649743 | core_pubmed_pmc | Population Pharmacokinetics of Intravenous Paracetamol and Its Metabolites in Extreme Preterm Neonates in the Context of Patent Ductus Arteriosus Treatment | Population Pharmacokinetics of Intravenous Paracetamol and Its Metabolites in Extreme Preterm Neonates in the Context of Patent Ductus Arteriosus Treatment Abstract Abstract Aims Our aim was to describe the pharmacokinetics of paracetamol and its metabolites in extreme preterm neonates in the context of patent ductus a... |
PMC9534946 | core_pubmed_pmc | Injectable Nanoparticle‐Based Hydrogels Enable the Safe and Effective Deployment of Immunostimulatory CD40 Agonist Antibodies | Injectable Nanoparticle‐Based Hydrogels Enable the Safe and Effective Deployment of Immunostimulatory CD40 Agonist Antibodies Abstract Abstract When properly deployed, the immune system can eliminate deadly pathogens, eradicate metastatic cancers, and provide long‐lasting protection from diverse diseases. Unfortunately... |
PMC4269819 | core_pubmed_pmc | No Interacting Influence of Lavender Oil Preparation Silexan on Oral Contraception Using an Ethinyl Estradiol/Levonorgestrel Combination | No Interacting Influence of Lavender Oil Preparation Silexan on Oral Contraception Using an Ethinyl Estradiol/Levonorgestrel Combination Abstract Abstract Purpose Silexan is an oral Lavender oil preparation with proven anxiolytic efficacy. Given the high prevalence of anxiety and restlessness in younger women, oral con... |
PMC4475818 | core_pubmed_pmc | Utilization of model-based meta-analysis to delineate the net efficacy of taspoglutide from the response of placebo in clinical trials | Utilization of model-based meta-analysis to delineate the net efficacy of taspoglutide from the response of placebo in clinical trials Abstract The objective of this study was to develop quantitative models to delineate the net efficacy of taspoglutide on fasting plasma glucose (FPG) and glycosylated hemoglobin (HbA1c)... |
PMC8485129 | core_pubmed_pmc | Importance of beta-lactam pharmacokinetics and pharmacodynamics on the recovery of microbial diversity in the airway of persons with cystic fibrosis | Importance of beta-lactam pharmacokinetics and pharmacodynamics on the recovery of microbial diversity in the airway of persons with cystic fibrosis Abstract Abstract Cystic fibrosis (CF) is a chronic lung disease characterized by acute pulmonary exacerbations (PExs) that are frequently treated with antibiotics. The im... |
PMC9412669 | core_pubmed_pmc | Potential Pharmaceutical Applications of Quercetin in Cardiovascular Diseases | Potential Pharmaceutical Applications of Quercetin in Cardiovascular Diseases Abstract Abstract Quercetin, as a member of flavonoids, has emerged as a potential therapeutic agent in cardiovascular diseases (CVDs) in recent decades. In this comprehensive literature review, our goal was a critical appraisal of the pathop... |
PMC8129719 | core_pubmed_pmc | Population pharmacokinetic modeling and simulation to support qualification of pyridoxic acid as endogenous biomarker of OAT1/3 renal transporters | Population pharmacokinetic modeling and simulation to support qualification of pyridoxic acid as endogenous biomarker of OAT1/3 renal transporters Abstract Abstract Renal clearance of many drugs is mediated by renal organic anion transporters OAT1/3 and inhibition of these transporters may lead to drug‐drug interaction... |
PMC6960404 | core_pubmed_pmc | Colistin Combined With Tigecycline: A Promising Alternative Strategy to Combat Escherichia coli Harboring bla NDM– 5 and mcr-1 | Colistin Combined With Tigecycline: A Promising Alternative Strategy to Combat Escherichia coli Harboring bla NDM– 5 and mcr-1 Abstract Infections due to carbapenem-resistant NDM-producing Escherichia coli represent a major therapeutic challenge, especially in situations of pre-existing colistin resistance. The aim of ... |
PMC8229286 | core_pubmed_pmc | Pharmacokinetics-Driven Evaluation of the Antioxidant Activity of Curcuminoids and Their Major Reduced Metabolites—A Medicinal Chemistry Approach | Pharmacokinetics-Driven Evaluation of the Antioxidant Activity of Curcuminoids and Their Major Reduced Metabolites—A Medicinal Chemistry Approach Abstract Curcuminoids are the main bioactive components of the well-known Asian spice and traditional medicine turmeric. Curcuminoids have poor chemical stability and bioavai... |
PMC7494611 | core_pubmed_pmc | A Homodimeric Aptamer Variant Generated from Ligand-Guided Selection Activates the T Cell Receptor Cluster of Differentiation 3 Complex | A Homodimeric Aptamer Variant Generated from Ligand-Guided Selection Activates the T Cell Receptor Cluster of Differentiation 3 Complex Abstract Recently, immunotherapeutic modalities with engineered cells and monoclonal antibodies have been effective in treating several malignancies. Nucleic acid aptamers can serve as... |
PMC9880438 | core_pubmed_pmc | Pharmacokinetics of active compounds of a Terminalia chebula Retz. Ethanolic extract after oral administration rats using UPLC-MS/MS | Pharmacokinetics of active compounds of a Terminalia chebula Retz. Ethanolic extract after oral administration rats using UPLC-MS/MS Abstract Abstract Terminalia chebula Retz. (TC) is a well-known Chinese herbal medicine and rich in chemical components with multiple pharmacological effects. In this study, an ultra-perf... |
PMC3538059 | core_pubmed_pmc | Short term serum pharmacokinetics of diammine silver fluoride after oral application | Short term serum pharmacokinetics of diammine silver fluoride after oral application Abstract Abstract Background There is growing interest in the use of diammine silver fluoride (DSF) as a topical agent to treat dentin hypersensitivity and dental caries as gauged by increasing published research from many parts of the... |
PMC11070715 | core_pubmed_pmc | Pharmacodynamic rationale for the choice of antiseizure medications in the paediatric population | Pharmacodynamic rationale for the choice of antiseizure medications in the paediatric population Abstract Abstract In the landscape of paediatric epilepsy treatment, over 20 anti-seizure medications (ASMs) have gained approval from Drug Regulatory Agencies, each delineating clear indications. However, the complexity of... |
PMC7238388 | core_pubmed_pmc | Biological Evaluation of Newly Synthesized Biaryl Guanidine Derivatives to Arrest β -Secretase Enzymatic Activity Involved in Alzheimer's Disease | Biological Evaluation of Newly Synthesized Biaryl Guanidine Derivatives to Arrest β -Secretase Enzymatic Activity Involved in Alzheimer's Disease Abstract Abstract Proteases BACE1 ( β -secretases) enzymes have been recognized as a promising target associated with Alzheimer's disease (AD). This study was carried out on ... |
PMC7876056 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Yimitasvir in Chinese Healthy Volunteers and Patients With Chronic Hepatitis C Virus Infection | Population Pharmacokinetic Analysis of Yimitasvir in Chinese Healthy Volunteers and Patients With Chronic Hepatitis C Virus Infection Abstract Abstract Yimitasvir is a novel, oral hepatitis C virus (HCV) non-structural protein 5A inhibitor for the treatment of chronic HCV genotype 1 infection. The objective of this ana... |
PMC11047331 | core_pubmed_pmc | Comparative Impact of an Optimized PK/PD Target Attainment of Piperacillin-Tazobactam vs. Meropenem on the Trend over Time of SOFA Score and Inflammatory Biomarkers in Critically Ill Patients Receiving Continuous Infusion Monotherapy for Treating Documented Gram-Negative BSIs and/or VAP | Comparative Impact of an Optimized PK/PD Target Attainment of Piperacillin-Tazobactam vs. Meropenem on the Trend over Time of SOFA Score and Inflammatory Biomarkers in Critically Ill Patients Receiving Continuous Infusion Monotherapy for Treating Documented Gram-Negative BSIs and/or VAP Abstract Abstract (1) Background... |
PMC5518866 | core_pubmed_pmc | Phase I dose-escalation studies of roniciclib, a pan-cyclin-dependent kinase inhibitor, in advanced malignancies | Phase I dose-escalation studies of roniciclib, a pan-cyclin-dependent kinase inhibitor, in advanced malignancies Abstract Background: To evaluate safety, pharmacokinetics, and maximum tolerated dose of roniciclib in patients with advanced malignancies, with dose expansion to evaluate clinical benefit at the recommended... |
PMC7252145 | core_pubmed_pmc | Dose selection of chloroquine phosphate for treatment of COVID-19 based on a physiologically based pharmacokinetic model | Dose selection of chloroquine phosphate for treatment of COVID-19 based on a physiologically based pharmacokinetic model Abstract Chloroquine (CQ) phosphate has been suggested to be clinically effective in the treatment of coronavirus disease 2019 (COVID-19). To develop a physiologically-based pharmacokinetic (PBPK) mo... |
PMC12516987 | core_pubmed_pmc | Mechanistic data-informed multiscale quantitative systems pharmacology modeling framework enables the clinical translation and efficacy assessment of CAR-T therapy in solid tumors | Mechanistic data-informed multiscale quantitative systems pharmacology modeling framework enables the clinical translation and efficacy assessment of CAR-T therapy in solid tumors Abstract Abstract Background Chimeric antigen receptor (CAR)-T cell therapy represents an innovative and potentially revolutionary modality ... |
PMC12203839 | core_pubmed_pmc | Translational minimal physiologically based pharmacokinetic model for transferrin receptor-mediated brain delivery of antibodies | Translational minimal physiologically based pharmacokinetic model for transferrin receptor-mediated brain delivery of antibodies Abstract ABSTRACT Successful development of monoclonal antibodies (mAbs) for the treatment of central nervous system disorders has been challenging due to their minimal ability to cross the b... |
PMC9197537 | core_pubmed_pmc | Introduction of an artificial neural network–based method for concentration‐time predictions | Introduction of an artificial neural network–based method for concentration‐time predictions Abstract Abstract Pharmacometrics and the application of population pharmacokinetic (PK) modeling play a crucial role in clinical pharmacology. These methods, which describe data with well‐defined equations and estimate physiol... |
PMC6706930 | core_pubmed_pmc | A novel oral micellar fenretinide formulation with enhanced bioavailability and antitumour activity against multiple tumours from cancer stem cells | A novel oral micellar fenretinide formulation with enhanced bioavailability and antitumour activity against multiple tumours from cancer stem cells Abstract Abstract Background An increasing number of anticancer agents has been proposed in recent years with the attempt to overcome treatment-resistant cancer cells and p... |
PMC4078515 | core_pubmed_pmc | Part Two: Evaluation of N- methylbupropion as a Potential Bupropion Prodrug | Part Two: Evaluation of N- methylbupropion as a Potential Bupropion Prodrug Abstract Abstract N- methylbupropion was selected as a potential prodrug from our in vitro screening of analogues of bupropion described in the preceding paper. This study describes in vivo pharmacokinetics of N- methylbupropion in the guinea-p... |
PMC12336149 | core_pubmed_pmc | Mathematical modelling of the heterogeneity of disease progression and treatment outcomes in patients with COVID-19 | Mathematical modelling of the heterogeneity of disease progression and treatment outcomes in patients with COVID-19 Abstract Pneumonia caused by SARS-CoV-2 infection is a self-limiting disease. Its progression and prognosis are highly heterogeneous among people of different ages, genders, and living with different life... |
PMC11570809 | core_pubmed_pmc | Novel N -phenyl-2-(aniline) benzamide hydrochloride salt development for colon cancer therapy | Novel N -phenyl-2-(aniline) benzamide hydrochloride salt development for colon cancer therapy Abstract Introduction N -phenyl-2-(aniline) analog N53 is a previously discovered dual inhibitor of Topo I and COX-2, which exhibited significant anti-colon cancer activity in vitro , but the poor solubility and moderate anti-... |
PMC8596686 | core_pubmed_pmc | Validation of a perioperative population factor VIII pharmacokinetic model with a large cohort of pediatric hemophilia a patients | Validation of a perioperative population factor VIII pharmacokinetic model with a large cohort of pediatric hemophilia a patients Abstract Abstract Aims Population pharmacokinetic (PK) models are increasingly applied to perform individualized dosing of factor VIII (FVIII) concentrates in haemophilia A patients. To guar... |
PMC5908896 | core_pubmed_pmc | Association of STAT -3 rs1053004 and VDR rs11574077 With FOLFIRI-Related Gastrointestinal Toxicity in Metastatic Colorectal Cancer Patients | Association of STAT -3 rs1053004 and VDR rs11574077 With FOLFIRI-Related Gastrointestinal Toxicity in Metastatic Colorectal Cancer Patients Abstract Abstract Pharmacogenomics has largely been applied to the personalization of irinotecan-based treatment, focusing mainly on the study of genetic variants in adsorption, di... |
PMC3747110 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Recombinant Human EPO-Fc Fusion Protein In Vivo | Pharmacokinetics and Pharmacodynamics of Recombinant Human EPO-Fc Fusion Protein In Vivo Abstract Abstract In this study, the in vivo pharmacokinetics and pharmacodynamics of a novel recombinant human erythropoietin (rhEPO) Fc fusion protein, rhEPO-Fc, were studied in both rodents and rhesus monkeys. Animal models of a... |
PMC6492438 | core_pubmed_pmc | Review of traditional uses, botany, chemistry, pharmacology, pharmacokinetics, and toxicology of Radix Cyathulae | Review of traditional uses, botany, chemistry, pharmacology, pharmacokinetics, and toxicology of Radix Cyathulae Abstract Cyathulae Radix (CR), also known as “Chuanniux” is a well-known traditional Chinese herbal medicine that has been used in China for thousands of years. The present work reviewed advances in traditio... |
PMC5868634 | core_pubmed_pmc | Pharmacokinetics of glycopyrronium/formoterol fumarate dihydrate delivered via metered dose inhaler using co-suspension delivery technology in patients with moderate-to-very severe COPD | Pharmacokinetics of glycopyrronium/formoterol fumarate dihydrate delivered via metered dose inhaler using co-suspension delivery technology in patients with moderate-to-very severe COPD Abstract Abstract Purpose The efficacy and tolerability of GFF MDI (Bevespi Aerosphere ® ), a fixed-dose combination of glycopyrronium... |
PMC11078956 | core_pubmed_pmc | Structural investigation of interactions between halogenated flavonoids and the lipid membrane along with their role as cytotoxic agents | Structural investigation of interactions between halogenated flavonoids and the lipid membrane along with their role as cytotoxic agents Abstract Abstract This study focuses on understanding the structural and molecular changes in lipid membranes under the influence of six halogenated flavonoid derivatives differing in... |
PMC5743552 | core_pubmed_pmc | Circulating Magnetic Microbubbles for Localized Real-Time Control of Drug Delivery by Ultrasonography-Guided Magnetic Targeting and Ultrasound | Circulating Magnetic Microbubbles for Localized Real-Time Control of Drug Delivery by Ultrasonography-Guided Magnetic Targeting and Ultrasound Abstract Abstract Image-guided and target-selective modulation of drug delivery by external physical triggers at the site of pathology has the potential to enable tailored contr... |
PMC11466214 | core_pubmed_pmc | Advancements in the investigation of chemical components and pharmacological properties of Codonopsis : A review | Advancements in the investigation of chemical components and pharmacological properties of Codonopsis : A review Abstract Species of the genus Codonopsis (Campanulaceae) have a long history of application, acclaimed for its edible and therapeutic attributes. Scholarly inquiries into Codonopsis span botany, phytochemist... |
PMC9054019 | core_pubmed_pmc | Overcoming differential tumor penetration of BRAF inhibitors using computationally guided combination therapy | Overcoming differential tumor penetration of BRAF inhibitors using computationally guided combination therapy Abstract BRAF-targeted kinase inhibitors (KIs) are used to treat malignancies including BRAF-mutant non–small cell lung cancer, colorectal cancer, anaplastic thyroid cancer, and, most prominently, melanoma. How... |
PMC8890665 | core_pubmed_pmc | The Traditional Uses, Phytochemistry, Pharmacokinetics, Pharmacology, Toxicity, and Applications of Corydalis saxicola Bunting: A Review | The Traditional Uses, Phytochemistry, Pharmacokinetics, Pharmacology, Toxicity, and Applications of Corydalis saxicola Bunting: A Review Abstract Abstract Background: Corydalis saxicola Bunting (CSB) is a perennial herb belonging to genus Corydalis (Papaveraceae), called “Yan-huang-lian” in the Chinese folk. Traditiona... |
PMC3585900 | core_pubmed_pmc | Axitinib for the Management of Metastatic Renal Cell Carcinoma | Axitinib for the Management of Metastatic Renal Cell Carcinoma Abstract In recent years, targeted agents have changed the treatment landscape for patients with advanced renal cell carcinoma (RCC), greatly improving treatment outcomes. Several targeted agents are now licensed for the treatment of metastatic RCC (mRCC), ... |
PMC8116740 | core_pubmed_pmc | ABCG2 Single Nucleotide Polymorphism Affects Imatinib Pharmacokinetics in Lower Alpha-1-Acid Glycoprotein Levels in Humans | ABCG2 Single Nucleotide Polymorphism Affects Imatinib Pharmacokinetics in Lower Alpha-1-Acid Glycoprotein Levels in Humans Abstract Abstract Imatinib is transported extracellularly by ABCB1 and ABCG2 efflux transporters and bound to alpha-1-acid glycoprotein (AGP) in the bloodstream. However, the clinical and pharmacok... |
PMC5777971 | core_pubmed_pmc | Pharmacokinetics of monoclonal antibodies and Fc-fusion proteins | Pharmacokinetics of monoclonal antibodies and Fc-fusion proteins Abstract There are many factors that can influence the pharmacokinetics (PK) of a mAb or Fc-fusion molecule with the primary determinant being FcRn-mediated recycling. Through Fab or Fc engineering, IgG-FcRn interaction can be used to generate a variety o... |
PMC11206245 | core_pubmed_pmc | Pharmacokinetics, Dose-Proportionality, and Tolerability of Intravenous Tanespimycin (17-AAG) in Single and Multiple Doses in Dogs: A Potential Novel Treatment for Canine Visceral Leishmaniasis | Pharmacokinetics, Dose-Proportionality, and Tolerability of Intravenous Tanespimycin (17-AAG) in Single and Multiple Doses in Dogs: A Potential Novel Treatment for Canine Visceral Leishmaniasis Abstract Abstract In the New World, dogs are considered the main reservoir of visceral leishmaniasis (VL). Due to inefficacies... |
PMC10749360 | core_pubmed_pmc | A phase I study to evaluate the safety, tolerability, and pharmacokinetics of a novel, potent GABA analog HSK16149 in healthy Chinese subjects | A phase I study to evaluate the safety, tolerability, and pharmacokinetics of a novel, potent GABA analog HSK16149 in healthy Chinese subjects Abstract Abstract Purpose: HSK16149 is a novel, potent gamma-aminobutyric acid (GABA) analog for the treatment of neuropathic pain. This study aimed to evaluate the safety, tole... |
PMC7652802 | core_pubmed_pmc | Composite midazolam and 1′-OH midazolam population pharmacokinetic model for constitutive, inhibited and induced CYP3A activity | Composite midazolam and 1′-OH midazolam population pharmacokinetic model for constitutive, inhibited and induced CYP3A activity Abstract CYP3A plays an important role in drug metabolism and, thus, can be a considerable liability for drug-drug interactions. Population pharmacokinetics may be an efficient tool for detect... |
PMC9888030 | core_pubmed_pmc | Biochemical exploration of β-lactamase inhibitors | Biochemical exploration of β-lactamase inhibitors Abstract The alarming rise of microbial resistance to antibiotics has severely limited the efficacy of current treatment options. The prevalence of β-lactamase enzymes is a significant contributor to the emergence of antibiotic resistance. There are four classes of β-la... |
PMC11186998 | core_pubmed_pmc | Updates on antifungal pharmacotherapy in elasmobranchs: pharmacokinetics of 4 mg/kg voriconazole after IM and IV administration in undulate skates ( Raja undulata ) maintained under human care | Updates on antifungal pharmacotherapy in elasmobranchs: pharmacokinetics of 4 mg/kg voriconazole after IM and IV administration in undulate skates ( Raja undulata ) maintained under human care Abstract Introduction Fungal diseases are frequently associated with elevated mortality rates in elasmobranchs. Currently, ther... |
PMC7315936 | core_pubmed_pmc | Bivalirudin for Maintenance Anticoagulation During Venovenous Extracorporeal Membrane Oxygenation for COVID-19 | Bivalirudin for Maintenance Anticoagulation During Venovenous Extracorporeal Membrane Oxygenation for COVID-19 Abstract In its severe manifestation, coronavirus disease 2019 (COVID-19) compromises oxygenation in a manner that is refractory to maximal conventional support and requires escalation to extracorporeal membra... |
PMC10629260 | core_pubmed_pmc | Non-Clinical Toxicology Evaluation of the Novel Non-ATP Competitive Oral PI3 Kinase Delta Inhibitor Roginolisib | Non-Clinical Toxicology Evaluation of the Novel Non-ATP Competitive Oral PI3 Kinase Delta Inhibitor Roginolisib Abstract Roginolisib (IOA-244) is a novel, non-ATP competitive phosphoinositide-3-kinase (PI3K) delta inhibitor that regulates Akt/mTOR signaling. Roginolisib was administered once daily to rats and dogs in d... |
PMC11903455 | core_pubmed_pmc | Reversal of anxiety-like depression induced by chronic corticosterone by crocin I and surface-enhanced Raman spectroscopy monitoring of plasma metabolites | Reversal of anxiety-like depression induced by chronic corticosterone by crocin I and surface-enhanced Raman spectroscopy monitoring of plasma metabolites Abstract Abstract Anxiety disorders and depression often co-occur and lack broadly available treatments. Gardenia extract significantly associated with treatment of ... |
PMC9293126 | core_pubmed_pmc | Pharmacokinetics of butorphanol in male neutered cats anesthetized with isoflurane | Pharmacokinetics of butorphanol in male neutered cats anesthetized with isoflurane Abstract Abstract This study characterized the pharmacokinetics of butorphanol in cats anesthetized with isoflurane. Six young healthy male neutered cats were used. Cats were anesthetized with isoflurane in oxygen. Catheters were placed ... |
PMC11181325 | core_pubmed_pmc | Glycopolymer Inhibitors of Galectin-3 Suppress the Markers of Tissue Remodeling in Pulmonary Hypertension | Glycopolymer Inhibitors of Galectin-3 Suppress the Markers of Tissue Remodeling in Pulmonary Hypertension Abstract Abstract Pulmonary hypertension is a cardiovascular disease with a low survival rate. The protein galectin-3 (Gal-3) binding β-galactosides of cellular glycoproteins plays an important role in the onset an... |
PMC6760534 | core_pubmed_pmc | Therapeutic potential of adenovirus-mediated TFF2-CTP-Flag peptide for treatment of colorectal cancer | Therapeutic potential of adenovirus-mediated TFF2-CTP-Flag peptide for treatment of colorectal cancer Abstract TFF2 is a small, secreted protein with anti-inflammatory properties. We previously have shown that TFF2 gene delivery via adenovirus (Ad- Tff2) suppresses colon tumor growth in colitis associated cancer. There... |
PMC4230438 | core_pubmed_pmc | In silico drug metabolism and pharmacokinetic profiles of natural products from medicinal plants in the Congo basin | In silico drug metabolism and pharmacokinetic profiles of natural products from medicinal plants in the Congo basin Abstract Purpose Drug metabolism and pharmacokinetics (DMPK) assessment has come to occupy a place of interest during the early stages of drug discovery today. The use of computer modelling to predict the... |
PMC12512397 | core_pubmed_pmc | Association between oxidative balance score and congestive heart failure in hypertensive patients: NHANES 2009–2018 | Association between oxidative balance score and congestive heart failure in hypertensive patients: NHANES 2009–2018 Abstract Objective Evidence on the correlation between Oxidative Balance Score (OBS) and the risk of congestive heart failure (CHF) in hypertensive patients remains limited. This study aimed to explore th... |
PMC7339658 | core_pubmed_pmc | Accelerating Therapeutics for Opportunities in Medicine: A Paradigm Shift in Drug Discovery | Accelerating Therapeutics for Opportunities in Medicine: A Paradigm Shift in Drug Discovery Abstract Conventional drug discovery is long and costly, and suffers from high attrition rates, often leaving patients with limited or expensive treatment options. Recognizing the overwhelming need to accelerate this process and... |
PMC10107257 | core_pubmed_pmc | Pharmacokinetic, Safety, and Tolerability Evaluations of Gepotidacin (GSK2140944) in Healthy Japanese Participants | Pharmacokinetic, Safety, and Tolerability Evaluations of Gepotidacin (GSK2140944) in Healthy Japanese Participants Abstract Abstract Gepotidacin is a novel, bactericidal, first‐in‐class triazaacenaphthylene antibiotic in late‐phase development for uncomplicated urinary tract infection and uncomplicated urogenital gonor... |
PMC12616243 | core_pubmed_pmc | Phase I Clinical Trial of the Bifunctional EGFR/TGF-β Fusion Protein Ficerafusp Alfa (BCA101) Alone and in Combination with Pembrolizumab for Advanced Solid Tumors | Phase I Clinical Trial of the Bifunctional EGFR/TGF-β Fusion Protein Ficerafusp Alfa (BCA101) Alone and in Combination with Pembrolizumab for Advanced Solid Tumors Abstract Abstract Purpose: To evaluate the safety, pharmacokinetics, pharmacodynamics, and efficacy of ficerafusp alfa (BCA101), a first-in-class bifunction... |
PMC10143603 | core_pubmed_pmc | Usefulness of Oral Fluid for Measurement of Methylone and Its Metabolites: Correlation with Plasma Drug Concentrations and the Effect of Oral Fluid pH | Usefulness of Oral Fluid for Measurement of Methylone and Its Metabolites: Correlation with Plasma Drug Concentrations and the Effect of Oral Fluid pH Abstract Abstract The aim of this study was to investigate methylone and its metabolites concentration in oral fluid following controlled increasing doses, focusing on t... |
PMC7017397 | core_pubmed_pmc | Preclinical Pharmacokinetics of Complement C5a Receptor Antagonists PMX53 and PMX205 in Mice | Preclinical Pharmacokinetics of Complement C5a Receptor Antagonists PMX53 and PMX205 in Mice Abstract Abstract The cyclic hexapeptides PMX53 and PMX205 are potent noncompetitive inhibitors of complement C5a receptor 1 (C5aR1). They are widely utilized to study the role of C5aR1 in mouse models, including central nervou... |
PMC11045871 | core_pubmed_pmc | Bile acid metabolism and signaling in health and disease: molecular mechanisms and therapeutic targets | Bile acid metabolism and signaling in health and disease: molecular mechanisms and therapeutic targets Abstract Abstract Bile acids, once considered mere dietary surfactants, now emerge as critical modulators of macronutrient (lipid, carbohydrate, protein) metabolism and the systemic pro-inflammatory/anti-inflammatory ... |
PMC9561470 | core_pubmed_pmc | Population Pharmacokinetics and Exposure–Response Analyses for Risankizumab in Patients with Active Psoriatic Arthritis | Population Pharmacokinetics and Exposure–Response Analyses for Risankizumab in Patients with Active Psoriatic Arthritis Abstract Abstract Introduction Risankizumab is an anti-IL23 monoclonal antibody approved for the treatment of moderate to severe plaque psoriasis and active psoriatic arthritis (PsA). This work charac... |
PMC5555209 | core_pubmed_pmc | Population pharmacokinetics of peginterferon α2a in patients with chronic hepatitis B | Population pharmacokinetics of peginterferon α2a in patients with chronic hepatitis B Abstract Abstract There were significant differences in response and pharmacokinetic characteristics to the peginterferon α2a treatment among Chronic Hepatitis B (CHB) patients. The aim of this study is to identify factors which could... |
PMC11361989 | core_pubmed_pmc | A simple HPLC–MS/MS method for the determination of polymyxin B in human plasma and its application in the pharmacokinetic study in elderly patients infected with multidrug-resistant Gram-negative bacteria | A simple HPLC–MS/MS method for the determination of polymyxin B in human plasma and its application in the pharmacokinetic study in elderly patients infected with multidrug-resistant Gram-negative bacteria Abstract Introduction: Polymyxin B is widely used to treat infections caused by multidrug-resistant Gram-negative ... |
PMC8020853 | core_pubmed_pmc | A simple and validated HPLC method for vancomycin assay in plasma samples: the necessity of TDM center development in Southern Iran | A simple and validated HPLC method for vancomycin assay in plasma samples: the necessity of TDM center development in Southern Iran Abstract Abstract Background and purpose: Vancomycin is a glycopeptide antibiotic which is the drug of choice against methicillin-resistant Staphylococcus aureus . It has a narrow therapeu... |
PMC12562276 | core_pubmed_pmc | Effects of Intramuscular Vasopressin on Pharmacokinetics and Pharmacodynamics in Healthy Neonatal Piglets: A Dose–Response Study | Effects of Intramuscular Vasopressin on Pharmacokinetics and Pharmacodynamics in Healthy Neonatal Piglets: A Dose–Response Study Abstract Abstract Background: Neonatal resuscitation guidelines recommend the use of the vasopressor epinephrine during neonatal cardiopulmonary resuscitation (CPR); however, vasopressin may ... |
PMC5633780 | core_pubmed_pmc | System Pharmacology-Based Dissection of the Synergistic Mechanism of Huangqi and Huanglian for Diabetes Mellitus | System Pharmacology-Based Dissection of the Synergistic Mechanism of Huangqi and Huanglian for Diabetes Mellitus Abstract The rapidly increasing diabetes mellitus (DM) is becoming a major global public health issue. Traditional Chinese medicine (TCM) has a long history of the treatment of DM with good efficacy. Huangqi... |
PMC10025095 | core_pubmed_pmc | New flavone-based arylamides as potential V600E-BRAF inhibitors: Molecular docking, DFT, and pharmacokinetic properties | New flavone-based arylamides as potential V600E-BRAF inhibitors: Molecular docking, DFT, and pharmacokinetic properties Abstract Objectives The V600E-BRAF protein kinase is an attractive and essential therapeutic target in melanoma and other tumors. However, because of its resistance to the known inhibitors and side ef... |
PMC8350126 | core_pubmed_pmc | Regulatory Considerations for the Mother, Fetus and Neonate in Fetal Pharmacology Modeling | Regulatory Considerations for the Mother, Fetus and Neonate in Fetal Pharmacology Modeling Abstract Abstract The regulatory framework for considering the fetal effects of new drugs is limited. This is partially due to the fact that pediatric regulations (21 CFR subpart D) do not apply to the fetus, and only US Health a... |
PMC9863752 | core_pubmed_pmc | Nanotechnology-Based Approaches for Voriconazole Delivery Applied to Invasive Fungal Infections | Nanotechnology-Based Approaches for Voriconazole Delivery Applied to Invasive Fungal Infections Abstract Invasive fungal infections increase mortality and morbidity rates worldwide. The treatment of these infections is still limited due to the low bioavailability and toxicity, requiring therapeutic monitoring, especial... |
PMC12905623 | core_pubmed_pmc | Modeling response to high-purity von Willebrand factor: toward tailored dosing during surgery in von Willebrand disease ∗ | Modeling response to high-purity von Willebrand factor: toward tailored dosing during surgery in von Willebrand disease ∗ Abstract Key Points • Even with high-purity VWF, FVIII response varies greatly between individuals, requiring monitoring for safe, effective, repeated infusions. • This challenges whether dose-adjus... |
PMC12402831 | core_pubmed_pmc | Combined Immediate‐Release and Extended‐Release Formulation of Sodium Valproate Provides Stable Plasma Levels for Inhibition of Histone Deacetylation | Combined Immediate‐Release and Extended‐Release Formulation of Sodium Valproate Provides Stable Plasma Levels for Inhibition of Histone Deacetylation Abstract Abstract A modified controlled‐release sodium valproate formulation (VAL001, test) was compared with an approved enteric‐coated tablet formulation (Absenor, refe... |
PMC11812943 | core_pubmed_pmc | Uncovering the interleukin‐12 pharmacokinetic desensitization mechanism and its consequences with mathematical modeling | Uncovering the interleukin‐12 pharmacokinetic desensitization mechanism and its consequences with mathematical modeling Abstract Abstract The cytokine interleukin‐12 (IL‐12) is a potential immunotherapy because of its ability to induce a Th1 immune response. However, success in the clinic has been limited due to a phen... |
PMC11787490 | core_pubmed_pmc | Feasibility assessment of a pharmaco-kinetic behavior based yield model of salivary cotinine among tobacco users | Feasibility assessment of a pharmaco-kinetic behavior based yield model of salivary cotinine among tobacco users Abstract Abstract Methods A secondary analysis was conducted using puff topography and salivary cotinine biomarker data from a prior two arm, two period cross-over study conducted in the natural environment ... |
PMC5904784 | core_pubmed_pmc | Water in the human body: An anesthesiologist's perspective on the connection between physicochemical properties of water and physiologic relevance | Water in the human body: An anesthesiologist's perspective on the connection between physicochemical properties of water and physiologic relevance Abstract The unique structure and multifaceted physicochemical properties of the water molecule, in addition to its universal presence in body compartments, make water a key... |
PMC8950597 | core_pubmed_pmc | HIV-1 Integrase Inhibitory Effects of Major Compounds Present in CareVid™: An Anti-HIV Multi-Herbal Remedy | HIV-1 Integrase Inhibitory Effects of Major Compounds Present in CareVid™: An Anti-HIV Multi-Herbal Remedy Abstract Abstract In our continued study on the anti-HIV activity of compounds present in CareVid TM , we report the HIV-1 integrase ((HIV-1 IN) inhibitory effects of pellitorine ( 1 ), oleuropein ( 2 ), magnoflor... |
PMC4966675 | core_pubmed_pmc | Alcohol Interactions with Psychostimulants: An Overview of Animal and Human Studies | Alcohol Interactions with Psychostimulants: An Overview of Animal and Human Studies Abstract Alcohol consumption with psychostimulants is very common among drug addicts. There is little known about the possible pharmacological interactions between alcohol and psychostimulants. Among most commonly co-abused psychostimul... |
PMC12877788 | core_pubmed_pmc | POLB 001, a p38 MAPK inhibitor, decreases local and systemic inflammatory responses following in vivo LPS administration in healthy volunteers: a randomised, double-blind, placebo-controlled study | POLB 001, a p38 MAPK inhibitor, decreases local and systemic inflammatory responses following in vivo LPS administration in healthy volunteers: a randomised, double-blind, placebo-controlled study Abstract Abstract Background and aim POLB 001 is an oral p38 mitogen-activated protein kinase (MAPK) inhibitor in developme... |
PMC9290613 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic bioequivalence between regular human insulin ( rDNA origin) in 0.9% sodium chloride ready‐to‐use infusion 1 U / mL and 100 U / mL concentrate diluted to 1 U / mL in healthy males | Pharmacokinetic and pharmacodynamic bioequivalence between regular human insulin ( rDNA origin) in 0.9% sodium chloride ready‐to‐use infusion 1 U / mL and 100 U / mL concentrate diluted to 1 U / mL in healthy males Abstract Abstract Aim To show pharmacokinetic (PK) and pharmacodynamic (PD) bioequivalence between Myxred... |
PMC12721278 | core_pubmed_pmc | MK-7602: a potent multi-stage dual-targeting antimalarial | MK-7602: a potent multi-stage dual-targeting antimalarial Abstract Summary Background The global burden of malaria remains substantial, and increasing parasite resistance to current antimalarials necessitates the development of drugs with unique mechanisms of action. This study aimed to develop and characterise a new a... |
PMC7333380 | core_pubmed_pmc | An Integrated Spatial Dynamics—Pharmacokinetic Model Explaining Poor Penetration of Anti-retroviral Drugs in Lymph Nodes | An Integrated Spatial Dynamics—Pharmacokinetic Model Explaining Poor Penetration of Anti-retroviral Drugs in Lymph Nodes Abstract Although combined anti-retroviral therapy (cART) suppresses plasma HIV viremia below the limit of detection in a majority of HIV patients, evidence is emerging that the distribution of the a... |
PMC8705689 | core_pubmed_pmc | Discovery of Octahydroisoindolone as a Scaffold for the Selective Inhibition of Chitinase B1 from Aspergillus fumigatus : In Silico Drug Design Studies | Discovery of Octahydroisoindolone as a Scaffold for the Selective Inhibition of Chitinase B1 from Aspergillus fumigatus : In Silico Drug Design Studies Abstract Abstract Chitinases represent an alternative therapeutic target for opportunistic invasive mycosis since they are necessary for fungal cell wall remodeling. Th... |
PMC5391828 | core_pubmed_pmc | Pharmacokinetics and safety of olopatadine hydrochloride 0.77% in healthy subjects with asymptomatic eyes: data from 2 independent clinical studies | Pharmacokinetics and safety of olopatadine hydrochloride 0.77% in healthy subjects with asymptomatic eyes: data from 2 independent clinical studies Abstract Purpose To assess the pharmacokinetics and safety of hydrochloride ophthalmic solution 0.77% olopatadine from 2 independent (Phase I and Phase III, respectively) c... |
PMC7234962 | core_pubmed_pmc | Applying Different Techniques to Improve the Bioavailability of Candesartan Cilexetil Antihypertensive Drug | Applying Different Techniques to Improve the Bioavailability of Candesartan Cilexetil Antihypertensive Drug Abstract Purpose The objective of this study was to compare different techniques to enhance the solubility and dissolution rate, and hence the bioavailability of candesartan cilexetil. Methods To achieve this tar... |
PMC11587475 | core_pubmed_pmc | Evaluating Pharmacists’ Knowledge of Food–Drug Interactions in Croatia: Identifying Gaps and Opportunities | Evaluating Pharmacists’ Knowledge of Food–Drug Interactions in Croatia: Identifying Gaps and Opportunities Abstract Abstract Food–drug interactions (FDIs) are pharmacokinetic or pharmacodynamic changes in drug effects caused by the presence of specific foods. To identify and prevent FDIs, pharmacists, alongside other h... |
PMC10972926 | core_pubmed_pmc | Pharmacokinetic Analysis of [ 18 F]FES PET in the Human Brain and Pituitary Gland | Pharmacokinetic Analysis of [ 18 F]FES PET in the Human Brain and Pituitary Gland Abstract Abstract Purpose Estrogen receptors (ER) are implicated in psychiatric disorders. We assessed if ER availability in the human brain could be quantified using 16α-[ 18 F]-fluoro-17β-estradiol ([ 18 F]FES) positron emission tomogra... |
PMC10864595 | core_pubmed_pmc | Optimizing the initial tacrolimus dosage in Chinese children with lung transplantation within normal hematocrit levels | Optimizing the initial tacrolimus dosage in Chinese children with lung transplantation within normal hematocrit levels Abstract Background The appropriate initial dosage of tacrolimus is undefined in Chinese pediatric lung transplant patients with normal hematocrit values. The purpose of this study is to optimize the i... |
PMC5973992 | core_pubmed_pmc | Population Pharmacokinetic and Pharmacodynamic Analysis of Belimumab Administered Subcutaneously in Healthy Volunteers and Patients with Systemic Lupus Erythematosus | Population Pharmacokinetic and Pharmacodynamic Analysis of Belimumab Administered Subcutaneously in Healthy Volunteers and Patients with Systemic Lupus Erythematosus Abstract Background Intravenous belimumab 10 mg/kg every 4 weeks is indicated in patients with active, autoantibody-positive systemic lupus erythematosus ... |
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