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PMC10005129 | core_pubmed_pmc | Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches | Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches Abstract Abstract Supersaturation is a promising strategy to improve gastrointestinal absorption of poorly water-soluble drugs. Supersaturation is a metastable state and therefore dissolved drugs ofte... |
PMC4807435 | core_pubmed_pmc | Model‐Based Analysis of Unbound Lopinavir Pharmacokinetics in HIV‐Infected Pregnant Women Supports Standard Dosing in the Third Trimester | Model‐Based Analysis of Unbound Lopinavir Pharmacokinetics in HIV‐Infected Pregnant Women Supports Standard Dosing in the Third Trimester Abstract Physiological changes during pregnancy can affect drug pharmacokinetics. Here we present a population pharmacokinetic model to describe the longitudinal change of unbound lo... |
PMC3236821 | core_pubmed_pmc | Primary lack of efficacy of infliximab therapy for rheumatoid arthritis: pharmacokinetic characterization and assessment of switching to tocilizumab | Primary lack of efficacy of infliximab therapy for rheumatoid arthritis: pharmacokinetic characterization and assessment of switching to tocilizumab Abstract To characterize primary failure to infliximab and determine the efficacy of switching to tocilizumab in patients with rheumatoid arthritis (RA), we examined 24 RA... |
PMC5529662 | core_pubmed_pmc | Metabolite Profiling, Pharmacokinetics, and In Vitro Glucuronidation of Icaritin in Rats by Ultra-Performance Liquid Chromatography Coupled with Mass Spectrometry | Metabolite Profiling, Pharmacokinetics, and In Vitro Glucuronidation of Icaritin in Rats by Ultra-Performance Liquid Chromatography Coupled with Mass Spectrometry Abstract Icaritin is a naturally bioactive flavonoid with several significant effects. This study aimed to clarify the metabolite profiling, pharmacokinetics... |
PMC12185791 | core_pubmed_pmc | Bioequivalence and Safety of Two Amisulpride Formulations in Healthy Chinese Subjects Under Fasting and Fed Conditions: A Randomized, Open‑Label, Single‑Dose, Crossover Study | Bioequivalence and Safety of Two Amisulpride Formulations in Healthy Chinese Subjects Under Fasting and Fed Conditions: A Randomized, Open‑Label, Single‑Dose, Crossover Study Abstract Background and Objectives Amisulpride is a second-generation antipsychotic drug that selectively binds to D2 and D3 dopaminergic recepto... |
PMC10025217 | core_pubmed_pmc | Artificial intelligence and machine learning disciplines with the potential to improve the nanotoxicology and nanomedicine fields: a comprehensive review | Artificial intelligence and machine learning disciplines with the potential to improve the nanotoxicology and nanomedicine fields: a comprehensive review Abstract The use of nanomaterials in medicine depends largely on nanotoxicological evaluation in order to ensure safe application on living organisms. Artificial inte... |
PMC11618975 | core_pubmed_pmc | Design and Development of Novel Hybrids Based on Pyrrolo[2,1‐ f ][1,2,4]Triazine and 1‐(Methylpiperidin‐4‐yl) Aniline–Based Analogs: Exploring the Utility as Anticancer Agents via MERTK Inhibition | Design and Development of Novel Hybrids Based on Pyrrolo[2,1‐ f ][1,2,4]Triazine and 1‐(Methylpiperidin‐4‐yl) Aniline–Based Analogs: Exploring the Utility as Anticancer Agents via MERTK Inhibition Abstract ABSTRACT Mer‐tyrosine kinase (MERTK), a member of the AXL, TYRO3, and MERTK (TAM) family, is one of the promising ... |
PMC9543720 | core_pubmed_pmc | Prediction of pyrotinib exposure based on physiologically-based pharmacokinetic model and endogenous biomarker | Prediction of pyrotinib exposure based on physiologically-based pharmacokinetic model and endogenous biomarker Abstract Abstract Pyrotinib, a novel irreversible epidermal growth factor receptor dual tyrosine kinase inhibitor, is mainly (about 90%) eliminated through cytochrome P450 (CYP) 3A mediated metabolism in vivo ... |
PMC10275696 | core_pubmed_pmc | Dose finding study for on-demand HIV pre-exposure prophylaxis for insertive sex in sub-Saharan Africa: results from the CHAPS open label randomised controlled trial | Dose finding study for on-demand HIV pre-exposure prophylaxis for insertive sex in sub-Saharan Africa: results from the CHAPS open label randomised controlled trial Abstract Summary Background The efficacy of on-demand HIV pre-exposure prophylaxis (PrEP) for men in sub-Saharan Africa has not been evaluated, and the on-... |
PMC10674156 | core_pubmed_pmc | Oral Drug Absorption and Drug Disposition in Critically Ill Cardiac Patients | Oral Drug Absorption and Drug Disposition in Critically Ill Cardiac Patients Abstract Abstract (1) Background: In critically ill cardiac patients, parenteral and enteral food and drug administration routes may be used. However, it is not well known how drug absorption and metabolism are altered in this group of adult p... |
PMC12823785 | core_pubmed_pmc | A Tutorial on the Development of a Physiologically Inspired PKRO Model for Monoclonal Antibodies | A Tutorial on the Development of a Physiologically Inspired PKRO Model for Monoclonal Antibodies Abstract ABSTRACT Modeling and simulations are indispensable tools to describe pharmacokinetics (PK) and pharmacodynamics to support monoclonal antibody (mAb) development. The linear PK of mAbs is commonly described by a 2‐... |
PMC5469400 | core_pubmed_pmc | Integrated Assessment of Diclofenac Biotransformation, Pharmacokinetics, and Omics-Based Toxicity in a Three-Dimensional Human Liver-Immunocompetent Coculture System | Integrated Assessment of Diclofenac Biotransformation, Pharmacokinetics, and Omics-Based Toxicity in a Three-Dimensional Human Liver-Immunocompetent Coculture System Abstract Abstract In vitro hepatocyte culture systems have inherent limitations in capturing known human drug toxicities that arise from complex immune re... |
PMC11510600 | core_pubmed_pmc | Precious Cargo: The Role of Polymeric Nanoparticles in the Delivery of Covalent Drugs | Precious Cargo: The Role of Polymeric Nanoparticles in the Delivery of Covalent Drugs Abstract Abstract Covalent drugs can offer significant advantages over non-covalent drugs in terms of pharmacodynamics (i.e., target-binding properties). However, the development of covalent drugs is sometimes hampered by pharmacokine... |
PMC11191101 | core_pubmed_pmc | Investigation of Newly Synthesized Fluorinated Isatin-Hydrazones by In Vitro Antiproliferative Activity, Molecular Docking, ADME Analysis, and e-Pharmacophore Modeling | Investigation of Newly Synthesized Fluorinated Isatin-Hydrazones by In Vitro Antiproliferative Activity, Molecular Docking, ADME Analysis, and e-Pharmacophore Modeling Abstract In this study, we investigated the in vitro antiproliferative activities and performed computational studies of newly synthesized fluorinated i... |
PMC10205997 | core_pubmed_pmc | Validation of a pharmacological imaging challenge using 11 C-buprenorphine and 18 F-2-fluoro-2-deoxy-D-glucose positron emission tomography to study the effects of buprenorphine to the rat brain | Validation of a pharmacological imaging challenge using 11 C-buprenorphine and 18 F-2-fluoro-2-deoxy-D-glucose positron emission tomography to study the effects of buprenorphine to the rat brain Abstract Aim Buprenorphine mainly acts as an agonist of mu-opioid receptors (mu-OR). High dose buprenorphine does not cause r... |
PMC12291295 | core_pubmed_pmc | Microbiome-derived reactivation of mycophenolate explains variations in enterohepatic recirculation in kidney transplant recipients | Microbiome-derived reactivation of mycophenolate explains variations in enterohepatic recirculation in kidney transplant recipients Abstract Background The pivotal role of microbes in drug metabolism is increasingly recognized, as variation in the gut microbiome composition between individuals has been shown to impact ... |
PMC10070282 | core_pubmed_pmc | Levothyroxine Bioequivalence Study and Its Narrow Therapeutic Index: Comparative Bioavailability Results Between Two Formulations Available in Latin America | Levothyroxine Bioequivalence Study and Its Narrow Therapeutic Index: Comparative Bioavailability Results Between Two Formulations Available in Latin America Abstract Introduction The history of levothyroxine has been linked to advances in the treatment of thyroid disease and to date it is the standard therapy for the t... |
PMC9448396 | core_pubmed_pmc | Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrin | Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrin Abstract Abstract Isopropoxy benzene guanidine (IBG) is a novel substituted benzene guanidine analogue with antibacterial activity against multidrug-resistant bacteria. However, the bioavailabil... |
PMC6099444 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, and Tolerability of Concomitant Multiple Dose Administration of Verinurad (RDEA3170) and Allopurinol in Adult Male Subjects With Gout | Pharmacokinetics, Pharmacodynamics, and Tolerability of Concomitant Multiple Dose Administration of Verinurad (RDEA3170) and Allopurinol in Adult Male Subjects With Gout Abstract Abstract Verinurad (RDEA3170) is a selective uric acid reabsorption inhibitor in clinical development for treatment of hyperuricemia and gout... |
PMC8229463 | core_pubmed_pmc | Development of Physiologically Based Pharmacokinetic Model for Orally Administered Fexuprazan in Humans | Development of Physiologically Based Pharmacokinetic Model for Orally Administered Fexuprazan in Humans Abstract Fexuprazan is a new drug candidate in the potassium-competitive acid blocker (P-CAB) family. As proton pump inhibitors (PPIs), P-CABs inhibit gastric acid secretion and can be used to treat gastric acid-rela... |
PMC11536336 | core_pubmed_pmc | Clinical pharmacokinetics and pharmacodynamics of ongericimab: A potential long‐acting PCSK9 monoclonal antibody in healthy subjects and patients with hypercholesterolemia: Randomized, double‐blind, placebo‐controlled phase Ia and Ib/II studies | Clinical pharmacokinetics and pharmacodynamics of ongericimab: A potential long‐acting PCSK9 monoclonal antibody in healthy subjects and patients with hypercholesterolemia: Randomized, double‐blind, placebo‐controlled phase Ia and Ib/II studies Abstract Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) inc... |
PMC12414073 | core_pubmed_pmc | A Population Pharmacokinetic Model and Dosing Algorithm to Guide the Tacrolimus Starting and Follow-Up Dose in Living and Deceased Donor Kidney Transplant Recipients | A Population Pharmacokinetic Model and Dosing Algorithm to Guide the Tacrolimus Starting and Follow-Up Dose in Living and Deceased Donor Kidney Transplant Recipients Abstract Abstract Introduction Tacrolimus treatment is complicated by its narrow therapeutic range and large inter- and intra-patient variability. This st... |
PMC11605156 | core_pubmed_pmc | Triterpenoids from Ganoderma lucidum inhibit cytochrome P450 enzymes interfering with the metabolic process of specific clinical drugs | Triterpenoids from Ganoderma lucidum inhibit cytochrome P450 enzymes interfering with the metabolic process of specific clinical drugs Abstract Abstract Background Ganoderma lucidum ( G. lucidum ), which possesses various biological effects, has been widely used as traditional medicine and functional food in Asian coun... |
PMC7913210 | core_pubmed_pmc | Evaluation of Lidocaine and Metabolite Pharmacokinetics in Hyaluronic Acid Injection | Evaluation of Lidocaine and Metabolite Pharmacokinetics in Hyaluronic Acid Injection Abstract Abstract Lidocaine-incorporated hyaluronic acid injection (LHA) is considered a promising way to increase patient compliance. Various reviews and analyses have been conducted to verify that the addition of lidocaine had no eff... |
PMC3287010 | core_pubmed_pmc | Pharmacokinetic Study of Di-Phenyl-Di-(2,4-Difluobenzohydroxamato)Tin(IV): Novel Metal-Based Complex with Promising Antitumor Potential | Pharmacokinetic Study of Di-Phenyl-Di-(2,4-Difluobenzohydroxamato)Tin(IV): Novel Metal-Based Complex with Promising Antitumor Potential Abstract Abstract Di-phenyl-di-(2,4-difluobenzohydroxamato)tin(IV)(DPDFT), a new metal-based arylhydroxamate antitumor complex, showed high in vivo and in vitro antitumor activity with... |
PMC12686497 | core_pubmed_pmc | Exploring neurokinin-1 receptor antagonism for depression with structurally differentiated inhibitors | Exploring neurokinin-1 receptor antagonism for depression with structurally differentiated inhibitors Abstract The neurokinin-1 receptor (NK1R) has been investigated as a potential target for major depressive disorder owing to its role in stress regulation and neuroinflammation. However, clinical trials of NK1R antagon... |
PMC5678849 | core_pubmed_pmc | A Single- and Multiple-Dose, Multicenter Study of Etelcalcetide in Japanese Hemodialysis Patients With Secondary Hyperparathyroidism | A Single- and Multiple-Dose, Multicenter Study of Etelcalcetide in Japanese Hemodialysis Patients With Secondary Hyperparathyroidism Abstract Introduction The pharmacokinetics, pharmacodynamics, and safety and tolerability profile of etelcalcetide (ONO-5163/AMG 416), a novel, i.v., long-acting calcium-sensing receptor ... |
PMC11542398 | core_pubmed_pmc | Azithromycin in severe malaria bacterial co-infection in African children (TABS-PKPD): a phase II randomised controlled trial | Azithromycin in severe malaria bacterial co-infection in African children (TABS-PKPD): a phase II randomised controlled trial Abstract Abstract Background African children with severe malaria are at increased risk of non-typhoidal salmonellae co-infection. Broad-spectrum antibiotics are recommended by guidelines but th... |
PMC8484413 | core_pubmed_pmc | Selectivity Profile of the Tyrosine Kinase 2 Inhibitor Deucravacitinib Compared with Janus Kinase 1/2/3 Inhibitors | Selectivity Profile of the Tyrosine Kinase 2 Inhibitor Deucravacitinib Compared with Janus Kinase 1/2/3 Inhibitors Abstract Introduction Deucravacitinib, a novel, oral, selective inhibitor of tyrosine kinase 2 (TYK2) signaling, acts via an allosteric mechanism by binding to the enzyme’s regulatory domain instead of the... |
PMC6209780 | core_pubmed_pmc | Determination and pharmacokinetic study of AZD‐3759 in rat plasma by ultra performance liquid chromatography with triple quadrupole mass spectrometer | Determination and pharmacokinetic study of AZD‐3759 in rat plasma by ultra performance liquid chromatography with triple quadrupole mass spectrometer Abstract Abstract Background AZD‐3759 is a new, potent, oral, active central nervous system‐penetrant EGFR inhibitor. Despite promising clinical activity among patients p... |
PMC3480239 | core_pubmed_pmc | Mechanism-based model characterizing bidirectional interaction between PEGylated liposomal CKD-602 (S-CKD602) and monocytes in cancer patients | Mechanism-based model characterizing bidirectional interaction between PEGylated liposomal CKD-602 (S-CKD602) and monocytes in cancer patients Abstract Abstract S-CKD602 is a PEGylated liposomal formulation of CKD-602, a potent topoisomerase I inhibitor. The objective of this study was to characterize the bidirectional... |
PMC12332710 | core_pubmed_pmc | Dual-phase multiobjective Bayesian optimization method for estimating hepatocellular carcinoma dynamics parameters from PET/CT scans | Dual-phase multiobjective Bayesian optimization method for estimating hepatocellular carcinoma dynamics parameters from PET/CT scans Abstract Abstract Background Optimization algorithms provide robust analytical frameworks for assessing hepatocellular carcinoma (HCC) pharmacokinetics based on dynamic positron emission ... |
PMC10788923 | core_pubmed_pmc | Development of Highly Potent, G-Protein Pathway Biased, Selective, and Orally Bioavailable GPR84 Agonists | Development of Highly Potent, G-Protein Pathway Biased, Selective, and Orally Bioavailable GPR84 Agonists Abstract Abstract Orphan G-protein-coupled receptor 84 (GPR84) is a receptor that has been linked to cancer, inflammatory, and fibrotic diseases. We have reported DL-175 as a biased agonist at GPR84 which showed di... |
PMC3526234 | core_pubmed_pmc | Randomized Controlled Phase Ib Study of Ghrelin Agonist, RM-131, in Type 2 Diabetic Women With Delayed Gastric Emptying | Randomized Controlled Phase Ib Study of Ghrelin Agonist, RM-131, in Type 2 Diabetic Women With Delayed Gastric Emptying Abstract OBJECTIVE To investigate the pharmacokinetics (PK), pharmacodynamics, and safety of single-dose RM-131 in type 2 diabetic patients with gastrointestinal cardinal symptoms (GCSI) and previousl... |
PMC7470355 | core_pubmed_pmc | Assessment of urinary pharmacokinetic and pharmacodynamic profiles of faropenem against extended-spectrum β -lactamase-producing Escherichia coli with canine ex vivo modelling: a pilot study | Assessment of urinary pharmacokinetic and pharmacodynamic profiles of faropenem against extended-spectrum β -lactamase-producing Escherichia coli with canine ex vivo modelling: a pilot study Abstract Abstract This study was carried out to investigate the urinary pharmacokinetics and pharmacodynamics of faropenem admini... |
PMC6294062 | core_pubmed_pmc | A high bioavailability and sustained-release nano-delivery system for nintedanib based on electrospray technology | A high bioavailability and sustained-release nano-delivery system for nintedanib based on electrospray technology Abstract Background Nintedanib is a new tyrosine kinase inhibitor and growth factor antagonist. It can be used to treat idiopathic pulmonary fibrosis diseases. Nintedanib has poor solubility in the intestin... |
PMC5404535 | core_pubmed_pmc | Pharmacodynamics of Finafloxacin, Ciprofloxacin, and Levofloxacin in Serum and Urine against TEM- and SHV-Type Extended-Spectrum-β-Lactamase-Producing Enterobacteriaceae Isolates from Patients with Urinary Tract Infections | Pharmacodynamics of Finafloxacin, Ciprofloxacin, and Levofloxacin in Serum and Urine against TEM- and SHV-Type Extended-Spectrum-β-Lactamase-Producing Enterobacteriaceae Isolates from Patients with Urinary Tract Infections Abstract ABSTRACT The pharmacodynamics of finafloxacin, ciprofloxacin, and levofloxacin against e... |
PMC11536717 | core_pubmed_pmc | Pharmacokinetic profile of novel multi-layer stable effervescent tablet: a cross-over study with an established European brand in healthy young male adults | Pharmacokinetic profile of novel multi-layer stable effervescent tablet: a cross-over study with an established European brand in healthy young male adults Abstract Effervescent formulation helps in faster and better absorption of drugs, especially those that are rapidly soluble in water. However, these tablets require... |
PMC9349081 | core_pubmed_pmc | Prediction of Maternal and Fetal Doravirine Exposure by Integrating Physiologically Based Pharmacokinetic Modeling and Human Placenta Perfusion Experiments | Prediction of Maternal and Fetal Doravirine Exposure by Integrating Physiologically Based Pharmacokinetic Modeling and Human Placenta Perfusion Experiments Abstract Abstract Background and Objective Doravirine is currently not recommended for pregnant women living with human immunodeficiency virus because efficacy and ... |
PMC4470083 | core_pubmed_pmc | Integration of PK/PD for dose optimization of Cefquinome against Staphylococcus aureus causing septicemia in cattle | Integration of PK/PD for dose optimization of Cefquinome against Staphylococcus aureus causing septicemia in cattle Abstract Cefquinome is a fourth generation cephalosporin with antimicrobial activity against gram negative and gram positive bacterial species, including Staphylococcus aureus . The aim of our study was t... |
PMC8595830 | core_pubmed_pmc | A Review of the Ethnopharmacology, Phytochemistry, Pharmacology, Application, Quality Control, Processing, Toxicology, and Pharmacokinetics of the Dried Rhizome of Atractylodes macrocephala | A Review of the Ethnopharmacology, Phytochemistry, Pharmacology, Application, Quality Control, Processing, Toxicology, and Pharmacokinetics of the Dried Rhizome of Atractylodes macrocephala Abstract Abstract The product investigated herein is the dried rhizome of Atractylodes macrocephala Koidz. [Asteraceae] (Baizhu), ... |
PMC12717852 | core_pubmed_pmc | Evaluating miRNA Sequencing and Integrative Proteomics for Identifying Plasma miRNAs as Potential Pharmacodynamic Biomarkers of IFNβ‐1a Biologics | Evaluating miRNA Sequencing and Integrative Proteomics for Identifying Plasma miRNAs as Potential Pharmacodynamic Biomarkers of IFNβ‐1a Biologics Abstract ABSTRACT We used miRNA sequencing to identify candidate plasma pharmacodynamic (PD) biomarkers of interferon beta‐1a (IFNβ‐1a) biologics and explored miRNA‐mRNA targ... |
PMC6017563 | core_pubmed_pmc | Pharmacokinetic–Pharmacodynamic Model for the Testosterone-Suppressive Effect of Leuprolide in Normal and Prostate Cancer Rats | Pharmacokinetic–Pharmacodynamic Model for the Testosterone-Suppressive Effect of Leuprolide in Normal and Prostate Cancer Rats Abstract This study developed the pharmacokinetic (PK)–pharmacodynamic (PD) model of the testosterone-suppressive effect of leuprolide for evaluation of the sustained release (SR) depot and leu... |
PMC6274697 | core_pubmed_pmc | Biotherapeutics: Challenges and Opportunities for Predictive Toxicology of Monoclonal Antibodies | Biotherapeutics: Challenges and Opportunities for Predictive Toxicology of Monoclonal Antibodies Abstract Biotherapeutics are a rapidly growing portion of the total pharmaceutical market accounting for almost one-half of recent new drug approvals. A major portion of these approvals each year are monoclonal antibodies (... |
PMC5548902 | core_pubmed_pmc | Pharmacodynamic and pharmacokinetic assessment of electronic cigarettes, combustible cigarettes, and nicotine gum: implications for abuse liability | Pharmacodynamic and pharmacokinetic assessment of electronic cigarettes, combustible cigarettes, and nicotine gum: implications for abuse liability Abstract Rationale Electronic cigarettes (ECs) are becoming popular alternatives for smokers, but there has been limited study of their abuse liability. Objectives The obje... |
PMC7999051 | core_pubmed_pmc | Study of the l -Phenylalanine Ammonia-Lyase Penetration Kinetics and the Efficacy of Phenylalanine Catabolism Correction Using In Vitro Model Systems | Study of the l -Phenylalanine Ammonia-Lyase Penetration Kinetics and the Efficacy of Phenylalanine Catabolism Correction Using In Vitro Model Systems Abstract Abstract The kinetics of l -phenylalanine ammonia-lyase (PAL) penetration into the monolayer of liver cells after its release from capsules was studied. The stud... |
PMC9682921 | core_pubmed_pmc | Pharmacokinetics of Teicoplanin in a Patient with Coronavirus Disease 2019 Receiving Veno-venous Extracorporeal Membrane Oxygenation | Pharmacokinetics of Teicoplanin in a Patient with Coronavirus Disease 2019 Receiving Veno-venous Extracorporeal Membrane Oxygenation Abstract Abstract Introduction Patients with severe coronavirus disease 2019 (COVID-19) receiving ventilation or pulmonary support via veno-venous extracorporeal membrane oxygenation (VV-... |
PMC4807465 | core_pubmed_pmc | Combined Analysis of Phase I and Phase II Data to Enhance the Power of Pharmacogenetic Tests | Combined Analysis of Phase I and Phase II Data to Enhance the Power of Pharmacogenetic Tests Abstract Abstract We show through a simulation study how the joint analysis of data from phase I and phase II studies enhances the power of pharmacogenetic tests in pharmacokinetic (PK) studies. PK profiles were simulated under... |
PMC11788159 | core_pubmed_pmc | Computational biology and artificial intelligence in mRNA vaccine design for cancer immunotherapy | Computational biology and artificial intelligence in mRNA vaccine design for cancer immunotherapy Abstract Messenger RNA (mRNA) vaccines offer an adaptable and scalable platform for cancer immunotherapy, requiring optimal design to elicit a robust and targeted immune response. Recent advancements in bioinformatics and ... |
PMC3674329 | core_pubmed_pmc | A Nonlinear Mixed Effects Pharmacokinetic Model for Dapagliflozin and Dapagliflozin 3- O -glucuronide in Renal or Hepatic Impairment | A Nonlinear Mixed Effects Pharmacokinetic Model for Dapagliflozin and Dapagliflozin 3- O -glucuronide in Renal or Hepatic Impairment Abstract Dapagliflozin is a sodium–glucose co-transporter 2 inhibitor in development for the treatment of type 2 diabetes mellitus. A semi-mechanistic population pharmacokinetic (PK) mode... |
PMC12553886 | core_pubmed_pmc | Artificial intelligence in clinical pharmacy—A systematic review of current scenario and future perspectives | Artificial intelligence in clinical pharmacy—A systematic review of current scenario and future perspectives Abstract Objective Medication prescription errors represent a significant and persistent challenge within healthcare systems globally, constituting a primary focus for clinical pharmacy practice. Additional comp... |
PMC12777559 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of a 2 g subcutaneous dose of ceftriaxone as an alternative to intravenous delivery | Safety, tolerability, and pharmacokinetics of a 2 g subcutaneous dose of ceftriaxone as an alternative to intravenous delivery Abstract ABSTRACT Subcutaneous delivery of antibiotics is a practical alternative to intravenous administration. Ceftriaxone is commonly used for a variety of infections with limited data on th... |
PMC10206279 | core_pubmed_pmc | Potentially inappropriate medications use in a psychiatric elderly care hospital: A cross‐sectional study using Beers criteria | Potentially inappropriate medications use in a psychiatric elderly care hospital: A cross‐sectional study using Beers criteria Abstract Abstract Background and Aims Potentially inappropriate medications (PIMs) carry risks that outweigh any potential benefits when compared to safer or more effective alternative treatmen... |
PMC6885571 | core_pubmed_pmc | The Optimization Design Of Lactoferrin Loaded HupA Nanoemulsion For Targeted Drug Transport Via Intranasal Route | The Optimization Design Of Lactoferrin Loaded HupA Nanoemulsion For Targeted Drug Transport Via Intranasal Route Abstract Abstract Background Huperzine A (HupA) is a selective acetylcholinesterase inhibitor used to treat Alzheimer’s disease. The existing dosage of HupA lacks brain selectivity and can cause serious side... |
PMC11639084 | core_pubmed_pmc | Phytochemical, pharmacological, pharmacokinetic and toxicological characteristics of Ziziphi Spinosae Semen : a review | Phytochemical, pharmacological, pharmacokinetic and toxicological characteristics of Ziziphi Spinosae Semen : a review Abstract Ziziphi Spinosae Semen (ZSS) is the seeds of Ziziphus jujuba Mill. var. Spinosa (Bunge) Hu ex H. F. Chou, which has the effects of nourishing heart and liver, tranquilizing heart and tranquili... |
PMC11479002 | core_pubmed_pmc | Antenatal corticosteroids in Singapore: a clinical and scientific assessment | Antenatal corticosteroids in Singapore: a clinical and scientific assessment Abstract Preterm birth (PTB; delivery prior to 37 weeks’ gestation) is the leading cause of early childhood death in Singapore today. Approximately 9% of Singaporean babies are born preterm; the PTB rate is likely to increase given the increas... |
PMC12128672 | core_pubmed_pmc | Efficacy and safety of CT‐P39, an omalizumab biosimilar, in chronic spontaneous urticaria: 16‐week follow‐up study | Efficacy and safety of CT‐P39, an omalizumab biosimilar, in chronic spontaneous urticaria: 16‐week follow‐up study Abstract Abstract Background A double‐blind, randomized Phase 3 study ( NCT04426890 ) confirmed that CT‐P39 and European Union‐approved reference omalizumab (ref‐OMA) were comparable in terms of efficacy, ... |
PMC9162344 | core_pubmed_pmc | An immuno-enrichment free, validated quantification of tau protein in human CSF by LC-MS/MS | An immuno-enrichment free, validated quantification of tau protein in human CSF by LC-MS/MS Abstract Abstract Tau protein is a key target of interest in developing therapeutics for neurodegenerative diseases. Here, we sought to develop a method that quantifies extracellular tau protein concentrations in human cerebrosp... |
PMC12026510 | core_pubmed_pmc | In Silico and In Vitro Analyses of Strawberry-Derived Extracts in Relation to Key Compounds’ Metabolic and Anti-Tumor Effects | In Silico and In Vitro Analyses of Strawberry-Derived Extracts in Relation to Key Compounds’ Metabolic and Anti-Tumor Effects Abstract Plant extracts contain many small molecules that are less investigated. The present paper aims to study in silico physical-chemical, pharmacokinetic, medicinal chemistry and lead/drug-l... |
PMC6630378 | core_pubmed_pmc | Application of Size and Maturation Functions to Population Pharmacokinetic Modeling of Pediatric Patients | Application of Size and Maturation Functions to Population Pharmacokinetic Modeling of Pediatric Patients Abstract Traditionally, dosage for pediatric patients has been optimized using simple weight-scaled methods, but these methods do not always meet the requirements of children. To overcome this discrepancy, populati... |
PMC9508223 | core_pubmed_pmc | Analysis of cellular kinetic models suggest that physiologically based model parameters may be inherently, practically unidentifiable | Analysis of cellular kinetic models suggest that physiologically based model parameters may be inherently, practically unidentifiable Abstract Physiologically-based pharmacokinetic and cellular kinetic models are used extensively to predict concentration profiles of drugs or adoptively transferred cells in patients and... |
PMC11825197 | core_pubmed_pmc | Determination and Pharmacokinetics of Acetylcorynoline in Mouse Plasma by UPLC–MS/MS | Determination and Pharmacokinetics of Acetylcorynoline in Mouse Plasma by UPLC–MS/MS Abstract Abstract Acetylcorynoline is an alkaloid isolated from the tubers of Corydalis ambigua Cham. et Schltdl. It has anti-inflammatory properties with the potential to treat Parkinson's disease. However, the use of UPLC–MS/MS for i... |
PMC9356410 | core_pubmed_pmc | Pharmacokinetic parameter driven outcomes model predicts a reduction in bleeding events associated with BAY 81–8973 versus antihemophilic factor (recombinant) plasma/albumin-free method in a Chinese healthcare setting | Pharmacokinetic parameter driven outcomes model predicts a reduction in bleeding events associated with BAY 81–8973 versus antihemophilic factor (recombinant) plasma/albumin-free method in a Chinese healthcare setting Abstract Background Long-term prophylactic therapy is considered the standard of care for hemophilia A... |
PMC11423396 | core_pubmed_pmc | In Vivo Bioluminescence Imaging Reveals Differences in Leishmania infantum Parasite Killing Kinetics by Antileishmanial Reference Drugs | In Vivo Bioluminescence Imaging Reveals Differences in Leishmania infantum Parasite Killing Kinetics by Antileishmanial Reference Drugs Abstract Abstract The bioluminescent Leishmania infantum BALB/c mouse model was used to evaluate the parasiticidal drug action kinetics of the reference drugs miltefosine, paromomycin,... |
PMC10951409 | core_pubmed_pmc | Effect of chronic vapor nicotine exposure on affective and cognitive behavior in male mice | Effect of chronic vapor nicotine exposure on affective and cognitive behavior in male mice Abstract Abstract Nicotine use is a leading cause of preventable deaths worldwide, and most of those who attempt to quit will relapse. While electronic cigarettes and other electronic nicotine delivery systems (ENDS) were present... |
PMC12578382 | core_pubmed_pmc | Molnupiravir clinical trial simulation suggests that polymerase chain reaction underestimates antiviral potency against SARS-CoV-2 | Molnupiravir clinical trial simulation suggests that polymerase chain reaction underestimates antiviral potency against SARS-CoV-2 Abstract Abstract Molnupiravir is an antiviral medicine that induces lethal copying errors during SARS-CoV-2 RNA replication. Molnupiravir reduced hospitalization in one pivotal trial by 50... |
PMC5109842 | core_pubmed_pmc | Nivolumab dose selection: challenges, opportunities, and lessons learned for cancer immunotherapy | Nivolumab dose selection: challenges, opportunities, and lessons learned for cancer immunotherapy Abstract Background Immuno-oncology (I-O) therapies target the host immune system, providing the potential to choose a uniform dose and schedule across tumor types. However, dose selection for I-O agents usually occurs ear... |
PMC12267686 | core_pubmed_pmc | Antimicrobial activity of new glycoside derivatives of chloroflavones obtained by fungal biotransformation | Antimicrobial activity of new glycoside derivatives of chloroflavones obtained by fungal biotransformation Abstract Abstract Chlorinated flavonoids represent a unique subclass of flavonoids with chlorine substituents. The incorporation of chlorine atoms and glucosyl moieties may influence their bioavailability, bioacti... |
PMC12647067 | core_pubmed_pmc | Tigecycline pharmacodynamics in the hollow fiber system of Mycobacterium avium -complex lung disease and the utility of MICs and time-kill studies in drug development | Tigecycline pharmacodynamics in the hollow fiber system of Mycobacterium avium -complex lung disease and the utility of MICs and time-kill studies in drug development Abstract Abstract Background Guideline-based therapy (GBT) drugs for Mycobacterium avium -complex (MAC) lung disease (LD) were chosen in part because the... |
PMC3456941 | core_pubmed_pmc | A phase I study of BMS-690514 in Japanese patients with advanced or metastatic solid tumors | A phase I study of BMS-690514 in Japanese patients with advanced or metastatic solid tumors Abstract Purpose BMS-690514 is a novel oral tyrosine kinase inhibitor of ErbB and vascular endothelial growth factor receptor. This open-label phase I dose-escalation study (ClinicalTrials.gov Identifier: NCT00516451 ) aimed to ... |
PMC12955364 | core_pubmed_pmc | Advances in Therapeutic Drug Monitoring and Pharmacokinetic Researches of Oxazolidinone Antibacterial Agents in the Elderly Patients | Advances in Therapeutic Drug Monitoring and Pharmacokinetic Researches of Oxazolidinone Antibacterial Agents in the Elderly Patients Abstract Abstract Background Elderly patients are at increased risk of infection with methicillin-resistant Staphylococcus aureus (MRSA). Therefore, this article comprehensively reviews t... |
PMC9293015 | core_pubmed_pmc | Quantifying the Pharmacodynamics of Morphine in the Treatment of Postoperative Pain in Preverbal Children | Quantifying the Pharmacodynamics of Morphine in the Treatment of Postoperative Pain in Preverbal Children Abstract Abstract While the pharmacokinetics of morphine in children have been studied extensively, little is known about the pharmacodynamics of morphine in this population. Here, we quantified the concentration‐e... |
PMC5753827 | core_pubmed_pmc | TRO40303 Ameliorates Alcohol-Induced Pancreatitis Through Reduction of Fatty Acid Ethyl Ester–Induced Mitochondrial Injury and Necrotic Cell Death | TRO40303 Ameliorates Alcohol-Induced Pancreatitis Through Reduction of Fatty Acid Ethyl Ester–Induced Mitochondrial Injury and Necrotic Cell Death Abstract Supplemental digital content is available in the text. Key Words: alcohol, experimental acute pancreatitis, mitochondrial permeability transition pore (MPTP), necro... |
PMC10586512 | core_pubmed_pmc | Hydrocodone, Oxycodone, and Morphine Metabolism and Drug–Drug Interactions | Hydrocodone, Oxycodone, and Morphine Metabolism and Drug–Drug Interactions Abstract Awareness of drug interactions involving opioids is critical for patient treatment as they are common therapeutics used in numerous care settings, including both chronic and disease-related pain. Not only do opioids have narrow therapeu... |
PMC2920021 | core_pubmed_pmc | The insulin-like growth factor-I receptor inhibitor figitumumab (CP-751,871) in combination with docetaxel in patients with advanced solid tumours: results of a phase Ib dose-escalation, open-label study | The insulin-like growth factor-I receptor inhibitor figitumumab (CP-751,871) in combination with docetaxel in patients with advanced solid tumours: results of a phase Ib dose-escalation, open-label study Abstract Background: This phase Ib trial assessed safety, tolerability, and maximum tolerated dose (MTD) of figitumu... |
PMC11963543 | core_pubmed_pmc | A simplified amoxicillin regimen with dose frequency based on post-natal age in neonates with confirmed or suspected infection | A simplified amoxicillin regimen with dose frequency based on post-natal age in neonates with confirmed or suspected infection Abstract ABSTRACT Amoxicillin plus gentamicin is the recommended first-line empiric therapy for neonates with infection. Guidelines vary widely in dose (mg/kg), dose frequency, and adjustments ... |
PMC5606620 | core_pubmed_pmc | Review on Usage of Vancomycin in Livestock and Humans: Maintaining Its Efficacy, Prevention of Resistance and Alternative Therapy | Review on Usage of Vancomycin in Livestock and Humans: Maintaining Its Efficacy, Prevention of Resistance and Alternative Therapy Abstract Abstract Vancomycin is one of the “last-line” classes of antibiotics used in the treatment of life-threatening infections caused by Gram-positive bacteria. Even though vancomycin wa... |
PMC6379219 | core_pubmed_pmc | A population pharmacokinetic model to predict the individual starting dose of tacrolimus in adult renal transplant recipients | A population pharmacokinetic model to predict the individual starting dose of tacrolimus in adult renal transplant recipients Abstract Aims The aims of this study were to describe the pharmacokinetics of tacrolimus immediately after kidney transplantation, and to develop a clinical tool for selecting the best starting ... |
PMC4074695 | core_pubmed_pmc | A study of potential adverse drug-drug interactions among prescribed drugs in medicine outpatient department of a tertiary care teaching hospital | A study of potential adverse drug-drug interactions among prescribed drugs in medicine outpatient department of a tertiary care teaching hospital Abstract Objective: To evaluate prevalence, types, and severity of potential adverse drug-drug interaction in medicine out-patient department. Materials and Methods: A single... |
PMC11118485 | core_pubmed_pmc | Passive accumulation of alkaloids in inconspicuously colored frogs refines the evolutionary paradigm of acquired chemical defenses | Passive accumulation of alkaloids in inconspicuously colored frogs refines the evolutionary paradigm of acquired chemical defenses Abstract Understanding the origins of novel, complex phenotypes is a major goal in evolutionary biology. Poison frogs of the family Dendrobatidae have evolved the novel ability to acquire a... |
PMC11876958 | core_pubmed_pmc | NI-3201 Is a Bispecific Antibody Mediating PD-L1–Dependent CD28 Co-stimulation on T Cells for Enhanced Tumor Control | NI-3201 Is a Bispecific Antibody Mediating PD-L1–Dependent CD28 Co-stimulation on T Cells for Enhanced Tumor Control Abstract Abstract Despite advances in cancer immunotherapy, such as targeting the PD-1/PD-L1 axis, a substantial number of patients harbor tumors that are resistant or relapse. Selective engagement of T-... |
PMC12188194 | core_pubmed_pmc | Pharmacokinetics of Subcutaneous and Intravenous Ceftriaxone in an Older Population: The PhASAge Study | Pharmacokinetics of Subcutaneous and Intravenous Ceftriaxone in an Older Population: The PhASAge Study Abstract Abstract Background Ceftriaxone is frequently administered subcutaneously in France, especially in older patients, although this practice is currently off-label. This work aims to describe the pharmacokinetic... |
PMC7756373 | core_pubmed_pmc | Impact of Physiologically Based Pharmacokinetics, Population Pharmacokinetics and Pharmacokinetics/Pharmacodynamics in the Development of Antibody‐Drug Conjugates | Impact of Physiologically Based Pharmacokinetics, Population Pharmacokinetics and Pharmacokinetics/Pharmacodynamics in the Development of Antibody‐Drug Conjugates Abstract Abstract Antibody‐drug conjugates are important molecular entities in the treatment of cancer, with 8 antibody‐drug conjugates approved by the US Fo... |
PMC4046785 | core_pubmed_pmc | Virus-Inspired Membrane Encapsulation of DNA Nanostructures To Achieve In Vivo Stability | Virus-Inspired Membrane Encapsulation of DNA Nanostructures To Achieve In Vivo Stability Abstract DNA nanotechnology enables engineering of molecular-scale devices with exquisite control over geometry and site-specific functionalization. This capability promises compelling advantages in advancing nanomedicine; neverthe... |
PMC7367914 | core_pubmed_pmc | Considerations and Caveats when Applying Global Sensitivity Analysis Methods to Physiologically Based Pharmacokinetic Models | Considerations and Caveats when Applying Global Sensitivity Analysis Methods to Physiologically Based Pharmacokinetic Models Abstract Abstract Three global sensitivity analysis (GSA) methods (Morris, Sobol and extended Sobol) are applied to a minimal physiologically based PK (mPBPK) model using three model drugs given ... |
PMC7028114 | core_pubmed_pmc | Extended Analysis and Evidence Integration of Chloroprene as a Human Carcinogen | Extended Analysis and Evidence Integration of Chloroprene as a Human Carcinogen Abstract Abstract β‐Chloroprene is used in the production of polychloroprene, a synthetic rubber. In 2010, Environmental Protection Agency (EPA) published the Integrated Risk Information System “Toxicological Review of Chloroprene,” conclud... |
PMC10145625 | core_pubmed_pmc | An Overview of Nanoemulgels for Bioavailability Enhancement in Inflammatory Conditions via Topical Delivery | An Overview of Nanoemulgels for Bioavailability Enhancement in Inflammatory Conditions via Topical Delivery Abstract Abstract The anti-inflammatory drugs that are generally available possess the disadvantage of hydrophobicity, which leads to poor permeability and erratic bioavailability. Nanoemulgels (NEGs) are novel d... |
PMC12464617 | core_pubmed_pmc | External validation of a therapeutic window for risperidone in children with autism spectrum disorder | External validation of a therapeutic window for risperidone in children with autism spectrum disorder Abstract Abstract Although risperidone is an effective pharmacological intervention for managing disruptive behaviour in children with autism spectrum disorder, it may induce metabolic side effects. This study aimed to... |
PMC11867918 | core_pubmed_pmc | Inflammation Decreases Ciclosporin Metabolism in Allogeneic Hematopoietic Stem Cell Transplantation Recipients | Inflammation Decreases Ciclosporin Metabolism in Allogeneic Hematopoietic Stem Cell Transplantation Recipients Abstract Abstract Graft‐versus‐host disease (GVHd) remains a significant challenge following allogeneic hematopoietic stem cell transplantation (HSCT). Prevention of GVHd relies mainly on the use of calcineuri... |
PMC9030333 | core_pubmed_pmc | Studies on Preformulation and Formulation of JIN-001 Liquisolid Tablet with Enhanced Solubility | Studies on Preformulation and Formulation of JIN-001 Liquisolid Tablet with Enhanced Solubility Abstract This study aimed to develop a heat shock protein 90 (Hsp90) inhibitor liquisolid tablet with improved solubility to overcome low bioavailability issues. As an active pharmaceutical ingredient (API), JIN-001, a novel... |
PMC9321699 | core_pubmed_pmc | A Single‐blind, Randomized, Single‐dose, Two‐sequence, Two‐period, Crossover Study to Assess the Bioequivalence between Two Oral Tablet Formulations of Rivaroxaban 20 mg in Healthy Mexican Volunteers | A Single‐blind, Randomized, Single‐dose, Two‐sequence, Two‐period, Crossover Study to Assess the Bioequivalence between Two Oral Tablet Formulations of Rivaroxaban 20 mg in Healthy Mexican Volunteers Abstract Abstract The objective of this study was to demonstrate the bioequivalence of 2 oral tablet formulations of riv... |
PMC7255661 | core_pubmed_pmc | Effects of oral administration of 5 immunosuppressive agents on activated T‐cell cytokine expression in healthy dogs | Effects of oral administration of 5 immunosuppressive agents on activated T‐cell cytokine expression in healthy dogs Abstract Abstract Background Dogs are often adminstered >1 immunosuppressive medication when treating immune‐mediated diseases, and determining whether these different medications affect IL‐2 expression ... |
PMC7032141 | core_pubmed_pmc | Biorelevant test for supersaturable formulation | Biorelevant test for supersaturable formulation Abstract Abstract Supersaturable formulation can generate supersaturation after dissolution, providing kinetic advantage in vivo . However, the supersaturation may precipitate before being absorbed, which makes it difficult to ensure and predict its in vivo performance. T... |
PMC7161550 | core_pubmed_pmc | Preclinical pharmacological evaluation of the fatty acid amide hydrolase inhibitor BIA 10‐2474 | Preclinical pharmacological evaluation of the fatty acid amide hydrolase inhibitor BIA 10‐2474 Abstract Background and Purpose In 2016, one person died and four others had mild‐to‐severe neurological symptoms during a phase I trial of the fatty acid amide hydrolase (FAAH) inhibitor BIA 10‐2474. Experimental Approach Ph... |
PMC9998327 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modelling to Identify Physiological and Drug Parameters Driving Pharmacokinetics in Obese Individuals | Physiologically Based Pharmacokinetic Modelling to Identify Physiological and Drug Parameters Driving Pharmacokinetics in Obese Individuals Abstract Background Obese individuals are often underrepresented in clinical trials, leading to a lack of dosing guidance. Objective This study aimed to investigate which physiolog... |
PMC6010333 | core_pubmed_pmc | The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models | The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models Abstract Poor survival rates of patients with tumors arising from or disseminating into the brain are attributed to an inability to excise all tumor tissue (if operable), a lack of blood-brain barr... |
PMC2941628 | core_pubmed_pmc | The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis | The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis Abstract EphB4 and its cognitive ligand ephrinB2 play an important role in embryonic vessel development and vascular remodeling. In addition, several reports suggest that this receptor ligand pair is also involved in patholo... |
PMC3931832 | core_pubmed_pmc | Pharmacokinetics of Natural and Engineered Secreted Factors Delivered by Mesenchymal Stromal Cells | Pharmacokinetics of Natural and Engineered Secreted Factors Delivered by Mesenchymal Stromal Cells Abstract Abstract Transient cell therapy is an emerging drug class that requires new approaches for pharmacological monitoring during use. Human mesenchymal stem cells (MSCs) are a clinically-tested transient cell therape... |
PMC7551138 | core_pubmed_pmc | Safety, pharmacokinetics, and pharmacodynamics of Gln‐1062, a prodrug of galantamine | Safety, pharmacokinetics, and pharmacodynamics of Gln‐1062, a prodrug of galantamine Abstract Abstract Introduction Gln‐1062 (MEMOGAIN) is an intranasally administered lipophilic prodrug of galantamine. Based on high brain‐to‐blood concentrations observed in pre‐clinical studies, Gln‐1062 is expected to have superior c... |
PMC9847340 | core_pubmed_pmc | Preclinical evaluation of IAP0971, a novel immunocytokine that binds specifically to PD1 and fuses IL15/IL15R α complex | Preclinical evaluation of IAP0971, a novel immunocytokine that binds specifically to PD1 and fuses IL15/IL15R α complex Abstract Abstract Background Currently, cytokine therapy for cancer has demonstrated efficacy in certain diseases but is generally accompanied by severe toxicity. The field of antibody-cytokine fusion... |
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