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PMC12205163 | core_pubmed_pmc | A randomized, double-blind, placebo-controlled, Phase 1 study to investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of an immediate-release oral ketamine capsule in healthy volunteers | A randomized, double-blind, placebo-controlled, Phase 1 study to investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of an immediate-release oral ketamine capsule in healthy volunteers Abstract Background: Ketamine, a rapid-acting N-methyl-D-aspartate receptor antagonist used as a therapeutic fo... |
PMC4026380 | core_pubmed_pmc | Safety, Pharmacokinetic, and Functional Effects of the Nogo-A Monoclonal Antibody in Amyotrophic Lateral Sclerosis: A Randomized, First-In-Human Clinical Trial | Safety, Pharmacokinetic, and Functional Effects of the Nogo-A Monoclonal Antibody in Amyotrophic Lateral Sclerosis: A Randomized, First-In-Human Clinical Trial Abstract The neurite outgrowth inhibitor, Nogo-A, has been shown to be overexpressed in skeletal muscle in amyotrophic lateral sclerosis (ALS); it is both a pot... |
PMC4371799 | core_pubmed_pmc | Phase I study of azacitidine and oxaliplatin in patients with advanced cancers that have relapsed or are refractory to any platinum therapy | Phase I study of azacitidine and oxaliplatin in patients with advanced cancers that have relapsed or are refractory to any platinum therapy Abstract Background Demethylation process is necessary for the expression of various factors involved in chemotherapy cytotoxicity or resistance. Platinum-resistant cells may have ... |
PMC12361969 | core_pubmed_pmc | Effect of physiological characteristics, smoking, and alcohol use on isoniazid hair drug levels among pulmonary TB patients: a cross-sectional study at one month of intensive TB treatment | Effect of physiological characteristics, smoking, and alcohol use on isoniazid hair drug levels among pulmonary TB patients: a cross-sectional study at one month of intensive TB treatment Abstract Background Tuberculosis(TB) is still among the leading causes of death from a single infectious pathogen worldwide. TB trea... |
PMC4755468 | core_pubmed_pmc | Toward a general physiologically-based pharmacokinetic model for intravenously injected nanoparticles | Toward a general physiologically-based pharmacokinetic model for intravenously injected nanoparticles Abstract To assess the potential toxicity of nanoparticles (NPs), information concerning their uptake and disposition (biokinetics) is essential. Experience with industrial chemicals and pharmaceutical drugs reveals th... |
PMC6003088 | core_pubmed_pmc | An empirical model for educational simulation of cervical dilation in first-stage labor | An empirical model for educational simulation of cervical dilation in first-stage labor Abstract Abstract Background Several models for educational simulation of labor and delivery were published in the literature and incorporated into a commercially available training simulator (CAE Healthcare Lucina). However, the en... |
PMC12641130 | core_pubmed_pmc | Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Türkiye: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints | Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Türkiye: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints Abstract Abstract Objectives To determine the antibiotic susceptibility of Streptococcus pneumoniae and Haemophilus influenzae from community-acq... |
PMC8698281 | core_pubmed_pmc | Is Dosing of Ethambutol as Part of a Fixed-Dose Combination Product Optimal for Mechanically Ventilated ICU Patients with Tuberculosis? A Population Pharmacokinetic Study | Is Dosing of Ethambutol as Part of a Fixed-Dose Combination Product Optimal for Mechanically Ventilated ICU Patients with Tuberculosis? A Population Pharmacokinetic Study Abstract Abstract Background: Tuberculosis (TB) patients admitted to intensive care units (ICU) have high mortality rates. It is uncertain whether th... |
PMC3576865 | core_pubmed_pmc | C609T Polymorphism of NADPH Quinone Oxidoreductase 1 Correlates Clinical Hematological Toxicities in Lung Cancer Patients Treated with Amrubicin | C609T Polymorphism of NADPH Quinone Oxidoreductase 1 Correlates Clinical Hematological Toxicities in Lung Cancer Patients Treated with Amrubicin Abstract Background: Amrubicin hydrochloride (AMR) is a key agent for lung cancer. NADPH quinone oxidoreductase 1 (NQO1) metabolizes the quinone structures contained in both a... |
PMC8453552 | core_pubmed_pmc | Migalastat Tissue Distribution: Extrapolation From Mice to Humans Using Pharmacokinetic Modeling and Comparison With Agalsidase Beta Tissue Distribution in Mice | Migalastat Tissue Distribution: Extrapolation From Mice to Humans Using Pharmacokinetic Modeling and Comparison With Agalsidase Beta Tissue Distribution in Mice Abstract Abstract Approved therapies for Fabry disease (FD) include migalastat, an oral pharmacological chaperone, and agalsidase beta and agalsidase alfa, 2 f... |
PMC12185600 | core_pubmed_pmc | A Clinical Pharmacological Perspective on Intraperitoneal Chemotherapy | A Clinical Pharmacological Perspective on Intraperitoneal Chemotherapy Abstract Peritoneal metastases (PM), frequently observed in malignancies such as ovarian, colorectal, pancreatic, and gastric cancers, present a significant therapeutic challenge due to poor prognosis and limited effectiveness to systemic chemothera... |
PMC11911779 | core_pubmed_pmc | A Phase 1b/2a Trial of a Half-life Extended Respiratory Syncytial Virus Neutralizing Antibody, Clesrovimab, in Healthy Preterm and Full-term Infants | A Phase 1b/2a Trial of a Half-life Extended Respiratory Syncytial Virus Neutralizing Antibody, Clesrovimab, in Healthy Preterm and Full-term Infants Abstract Abstract Background Clesrovimab is an investigational monoclonal antibody with an extended half-life targeting site IV of the respiratory syncytial virus (RSV) fu... |
PMC9933477 | core_pubmed_pmc | Discovery of a Novel Class of Dual GPBAR1 Agonists–RORγt Inverse Agonists for the Treatment of IL-17-Mediated Disorders | Discovery of a Novel Class of Dual GPBAR1 Agonists–RORγt Inverse Agonists for the Treatment of IL-17-Mediated Disorders Abstract Retinoic acid receptor-related orphan receptor γ-t (RORγt) and GPBAR1, a transmembrane G-protein-coupled receptor for bile acids, are attractive drug targets to develop clinically relevant sm... |
PMC2921063 | core_pubmed_pmc | A general process for the development of peptide-based immunoassays for monoclonal antibodies | A general process for the development of peptide-based immunoassays for monoclonal antibodies Abstract Abstract Purpose Monoclonal antibodies (mAb) are an important and growing class of cancer therapeutics, but pharmacokinetic analyses have in many cases been constrained by the lack of standard and robust pharmacologic... |
PMC3770982 | core_pubmed_pmc | Active Metabolites as Antidepressant Drugs: The Role of Norquetiapine in the Mechanism of Action of Quetiapine in the Treatment of Mood Disorders | Active Metabolites as Antidepressant Drugs: The Role of Norquetiapine in the Mechanism of Action of Quetiapine in the Treatment of Mood Disorders Abstract Abstract Active metabolites of some antipsychotic drugs exhibit pharmacodynamic and pharmacokinetic properties that may be similar to or differ from the original com... |
PMC12706413 | core_pubmed_pmc | Population Pharmacokinetic and Pharmacodynamic Modeling for the Prediction of the Extended Amlitelimab Phase 3 Dosing Regimen in Atopic Dermatitis | Population Pharmacokinetic and Pharmacodynamic Modeling for the Prediction of the Extended Amlitelimab Phase 3 Dosing Regimen in Atopic Dermatitis Abstract ABSTRACT Amlitelimab is a fully human, nondepleting, anti‐OX40 ligand monoclonal antibody being investigated for the treatment of moderate‐to‐severe atopic dermatit... |
PMC10716708 | core_pubmed_pmc | A systematic review of pregnancy-related clinical intervention of drug regimens due to pharmacokinetic reasons | A systematic review of pregnancy-related clinical intervention of drug regimens due to pharmacokinetic reasons Abstract Abstract Background and objective Published works have discussed the pharmacokinetic interactions of drugs with pregnancy, but none comprehensively identify all the approved United States Food and Dru... |
PMC5233986 | core_pubmed_pmc | Increased Renal Clearance of Rocuronium Compensates for Chronic Loss of Bile Excretion, via upregulation of Oatp2 | Increased Renal Clearance of Rocuronium Compensates for Chronic Loss of Bile Excretion, via upregulation of Oatp2 Abstract Abstract Requirement for rocuronium upon surgery changes only minimally in patients with end-stage liver diseases. Our study consisted of both human and rat studies to explore the reason. The reduc... |
PMC6924312 | core_pubmed_pmc | Pharmacokinetics and metabolism of icaritin in rats by UPLC‐MS/MS | Pharmacokinetics and metabolism of icaritin in rats by UPLC‐MS/MS Abstract Abstract Icaritin (ICT) has distinct bioactivities, especially known for its beneficial effects on bone‐related degenerative disorders; however, its pharmacokinetic properties remain unknown. A novel developed UPLC‐MS/MS method for the determina... |
PMC9103742 | core_pubmed_pmc | The Fight Just Born—Neonatal Cancer: Rare Occurrence with a Favorable Outcome but Challenging Management | The Fight Just Born—Neonatal Cancer: Rare Occurrence with a Favorable Outcome but Challenging Management Abstract Abstract Simple Summary Neonatal cancer represents a heterogeneous group of neoplasms with a wide range of clinical, biological, and prognostic features. Characterizing genetic cancer risk is critical for i... |
PMC10636136 | core_pubmed_pmc | Sphingomyelin-derived nanovesicles for the delivery of the IDO1 inhibitor epacadostat enhance metastatic and post-surgical melanoma immunotherapy | Sphingomyelin-derived nanovesicles for the delivery of the IDO1 inhibitor epacadostat enhance metastatic and post-surgical melanoma immunotherapy Abstract Abstract Epacadostat (EPA), the most advanced IDO1 inhibitor, in combination with PD-1 checkpoint inhibitor, has failed in a recent Phase III clinical trial for trea... |
PMC8624029 | core_pubmed_pmc | Compartmental and COMSOL Multiphysics 3D Modeling of Drug Diffusion to the Vitreous Following the Administration of a Sustained-Release Drug Delivery System | Compartmental and COMSOL Multiphysics 3D Modeling of Drug Diffusion to the Vitreous Following the Administration of a Sustained-Release Drug Delivery System Abstract The purpose of this study was to examine antibiotic drug transport from a hydrogel drug delivery system (DDS) using a computational model and a 3D model o... |
PMC3791559 | core_pubmed_pmc | Modafinil as a Catecholaminergic Agent: Empirical Evidence and Unanswered Questions | Modafinil as a Catecholaminergic Agent: Empirical Evidence and Unanswered Questions Abstract Modafinil, in its two clinical formulations (Provigil ® and Nuvigil ® ), is a widely prescribed wake-promoting therapeutic agent. It binds competitively to the cell-membrane dopamine (DA) transporter and is dependent on catecho... |
PMC12444745 | core_pubmed_pmc | A Novel Hybrid LC-MS/MS Methodology for the Quantitative Bioanalysis of Antibody-siRNA Conjugates | A Novel Hybrid LC-MS/MS Methodology for the Quantitative Bioanalysis of Antibody-siRNA Conjugates Abstract Abstract Small interfering RNA (siRNA) is a new class of oligonucleotide therapeutics that is rapidly growing in drug research and development for the treatment of various diseases. One major challenge for siRNA t... |
PMC11773776 | core_pubmed_pmc | Impact of vancomycin area under the curve in early or later phase on efficacy and nephrotoxicity in patients with enterococcal bloodstream infections: a multicenter study | Impact of vancomycin area under the curve in early or later phase on efficacy and nephrotoxicity in patients with enterococcal bloodstream infections: a multicenter study Abstract Background The optimal pharmacokinetic and pharmacodynamic (PK/PD) parameters of vancomycin that can improve outcomes in enterococcal infect... |
PMC9913758 | core_pubmed_pmc | Important Requirements for Desorption/Ionization Mass Spectrometric Measurements of Temozolomide-Induced 2′-Deoxyguanosine Methylations in DNA | Important Requirements for Desorption/Ionization Mass Spectrometric Measurements of Temozolomide-Induced 2′-Deoxyguanosine Methylations in DNA Abstract Simple Summary Monitoring chemical action of drugs directly at their molecular target would be particularly valuable for personalized medicine. In temozolomide-exposed ... |
PMC8145459 | core_pubmed_pmc | Development of a Virtual Chinese Pediatric Population Physiological Model Targeting Specific Metabolism and Kidney Elimination Pathways | Development of a Virtual Chinese Pediatric Population Physiological Model Targeting Specific Metabolism and Kidney Elimination Pathways Abstract Background: Physiologically based pharmacokinetic (PBPK) modeling and simulating may be a powerful tool in predicting drug behaviors in specific populations. It is a mathemati... |
PMC7384040 | core_pubmed_pmc | Potent and rapid reversal of the von Willebrand factor inhibitor aptamer BT200 | Potent and rapid reversal of the von Willebrand factor inhibitor aptamer BT200 Abstract Abstract Background BT200, a pegylated form of the aptamer BT100, inhibits binding of von Willebrand factor (VWF) to platelet glycoprotein GPIb, preventing arterial thrombosis in cynomolgus monkeys. It is being developed for seconda... |
PMC8359225 | core_pubmed_pmc | Pregabalin Population Pharmacokinetic and Exposure‐Response Analyses for Focal Onset Seizures in Children (4–16 years) and Adults, to Support Dose Recommendations in Children | Pregabalin Population Pharmacokinetic and Exposure‐Response Analyses for Focal Onset Seizures in Children (4–16 years) and Adults, to Support Dose Recommendations in Children Abstract Abstract Pregabalin is approved in multiple countries as adjunctive therapy for adult patients with focal onset seizures (FOS; previousl... |
PMC9032325 | core_pubmed_pmc | Antiosteoporosis Effects, Pharmacokinetics, and Drug Delivery Systems of Icaritin: Advances and Prospects | Antiosteoporosis Effects, Pharmacokinetics, and Drug Delivery Systems of Icaritin: Advances and Prospects Abstract Abstract Osteoporosis is a systemic skeletal disorder affecting over 200 million people worldwide and contributes dramatically to global healthcare costs. Available anti-osteoporotic drug treatments includ... |
PMC10957598 | core_pubmed_pmc | Waiting times between examinations with intravascularly administered contrast media: a review of contrast media pharmacokinetics and updated ESUR Contrast Media Safety Committee guidelines | Waiting times between examinations with intravascularly administered contrast media: a review of contrast media pharmacokinetics and updated ESUR Contrast Media Safety Committee guidelines Abstract Abstract Abstract The pharmacokinetics of contrast media (CM) will determine how long safe waiting intervals between succe... |
PMC12008503 | core_pubmed_pmc | Advances in nanomaterials for precision drug delivery: Insights into pharmacokinetics and toxicity | Advances in nanomaterials for precision drug delivery: Insights into pharmacokinetics and toxicity Abstract Abstract By integrating the cutting-edge principles of nanotechnology with medical science, nanomedicine offers unprecedented opportunities to develop advanced drug delivery systems that surpass the limitations o... |
PMC10030201 | core_pubmed_pmc | Low Escitalopram Concentrations in Patients with Depression predict Treatment Failure: A Naturalistic Retrospective Study | Low Escitalopram Concentrations in Patients with Depression predict Treatment Failure: A Naturalistic Retrospective Study Abstract Introduction Cross sectional therapeutic drug monitoring (TDM) data mining introduces new opportunities for the investigation of medication treatment effects to find optimal therapeutic win... |
PMC11339140 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Nipocalimab, a Neonatal Fc Receptor Blocker, in Healthy Japanese Volunteers | Pharmacokinetics and Pharmacodynamics of Nipocalimab, a Neonatal Fc Receptor Blocker, in Healthy Japanese Volunteers Abstract Abstract Background and Objectives Nipocalimab is a high-affinity, fully human, effectorless immunoglobulin G1 monoclonal antibody targeting the neonatal Fc receptor and is currently under evalu... |
PMC4920237 | core_pubmed_pmc | Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation | Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation Abstract Abstract Most of the dental surgeries require preoperative anesthetic and postoperative analgesic for painless procedures. A multidrug transmucosal drug delivery system loaded with lignocaine (Li... |
PMC4966428 | core_pubmed_pmc | Anticancer activity of TTAC-0001, a fully human anti-vascular endothelial growth factor receptor 2 (VEGFR-2/KDR) monoclonal antibody, is associated with inhibition of tumor angiogenesis | Anticancer activity of TTAC-0001, a fully human anti-vascular endothelial growth factor receptor 2 (VEGFR-2/KDR) monoclonal antibody, is associated with inhibition of tumor angiogenesis Abstract Vascular endothelial growth factor (VEGF) and its receptors are considered the primary cause of tumor-induced angiogenesis. S... |
PMC9696548 | core_pubmed_pmc | Pharmacological Validation of Long-Term Treatment with Antiretroviral Drugs in a Model of SIV-Infected Non-Human Primates | Pharmacological Validation of Long-Term Treatment with Antiretroviral Drugs in a Model of SIV-Infected Non-Human Primates Abstract The development of animal models undergoing long-term antiretroviral treatment (ART) makes it possible to understand a number of immunological, virological, and pharmacological issues, key ... |
PMC4937633 | core_pubmed_pmc | Interaction potential of Carmegliptin with P-glycoprotein (Pgp) transporter in healthy volunteers | Interaction potential of Carmegliptin with P-glycoprotein (Pgp) transporter in healthy volunteers Abstract Objective The primary objective of this study was to investigate the interaction potential of carmegliptin with P-glycoprotein transporter in vitro and in vivo . A secondary objective was to investigate the safety... |
PMC10826739 | core_pubmed_pmc | Pharmacokinetic analysis of placental transfer of ritonavir as a component of paxlovid using microdialysis in pregnant rats | Pharmacokinetic analysis of placental transfer of ritonavir as a component of paxlovid using microdialysis in pregnant rats Abstract Abstract Background Ritonavir is one of the most potent CYP3A4 inhibitor currently on the market, and is often used together with other antiviral drugs to increase their bioavailability a... |
PMC7211193 | core_pubmed_pmc | Evaluation of absorption, distribution, metabolism, and excretion of [ 14 C]-rucaparib, a poly(ADP-ribose) polymerase inhibitor, in patients with advanced solid tumors | Evaluation of absorption, distribution, metabolism, and excretion of [ 14 C]-rucaparib, a poly(ADP-ribose) polymerase inhibitor, in patients with advanced solid tumors Abstract Summary Rucaparib, a poly(ADP-ribose) polymerase inhibitor, is licensed for use in recurrent ovarian, fallopian tube, or primary peritoneal can... |
PMC8210165 | core_pubmed_pmc | Treating infections caused by carbapenemase-producing Enterobacterales (CPE): a pragmatic approach to antimicrobial stewardship on behalf of the UKCPA Pharmacy Infection Network (PIN) | Treating infections caused by carbapenemase-producing Enterobacterales (CPE): a pragmatic approach to antimicrobial stewardship on behalf of the UKCPA Pharmacy Infection Network (PIN) Abstract Abstract The emergence of carbapenemase-producing Enterobacterales (CPE) as a major cause of invasive infection both within the... |
PMC11739755 | core_pubmed_pmc | The Potential of Disease Progression Modeling to Advance Clinical Development and Decision Making | The Potential of Disease Progression Modeling to Advance Clinical Development and Decision Making Abstract Abstract While some model‐informed drug development frameworks are well recognized as enabling clinical trials, the value of disease progression modeling (DPM) in impacting medical product development has yet to b... |
PMC6783563 | core_pubmed_pmc | Continuous Subcutaneous Delivery of Proline-Rich Antimicrobial Peptide Api137 Provides Superior Efficacy to Intravenous Administration in a Mouse Infection Model | Continuous Subcutaneous Delivery of Proline-Rich Antimicrobial Peptide Api137 Provides Superior Efficacy to Intravenous Administration in a Mouse Infection Model Abstract Apidaecins are cationic, proline-rich antimicrobial peptides originally isolated from honeybees and exhibit high Gram-negative activity by inhibiting... |
PMC7352351 | core_pubmed_pmc | CYP3A5 Genotype as a Potential Pharmacodynamic Biomarker for Tacrolimus Therapy in Ulcerative Colitis in Japanese Patients | CYP3A5 Genotype as a Potential Pharmacodynamic Biomarker for Tacrolimus Therapy in Ulcerative Colitis in Japanese Patients Abstract Tacrolimus has been used to induce remission in patients with steroid-refractory ulcerative colitis. It poses a problem of large individual differences in dosage necessary to attain target... |
PMC9101870 | core_pubmed_pmc | Development, In-Vitro Characterization and Preclinical Evaluation of Esomeprazole-Encapsulated Proniosomal Formulation for the Enhancement of Anti-Ulcer Activity | Development, In-Vitro Characterization and Preclinical Evaluation of Esomeprazole-Encapsulated Proniosomal Formulation for the Enhancement of Anti-Ulcer Activity Abstract Abstract Objective: The present study aimed to develop and optimize esomeprazole loaded proniosomes (EZL-PNs) to improve bioavailability and therapeu... |
PMC4744661 | core_pubmed_pmc | Lixisenatide reduces postprandial hyperglycaemia via gastrostatic and insulinotropic effects | Lixisenatide reduces postprandial hyperglycaemia via gastrostatic and insulinotropic effects Abstract Abstract Background Lixisenatide is a once‐daily, prandial, short‐acting glucagon‐like peptide‐1 receptor agonist. Its main antidiabetic effect is to delay gastric emptying to control postprandial plasma glucose excurs... |
PMC5817835 | core_pubmed_pmc | Pharmacokinetic equivalence, comparable safety, and immunogenicity of an adalimumab biosimilar product (M923) to Humira in healthy subjects | Pharmacokinetic equivalence, comparable safety, and immunogenicity of an adalimumab biosimilar product (M923) to Humira in healthy subjects Abstract Abstract The aims of this randomized, double‐blind, three‐arm, single‐dose study were to demonstrate pharmacokinetic (PK) equivalence of the adalimumab biosimilar M923 (he... |
PMC10946252 | core_pubmed_pmc | Exploring inter-ethnic and inter-patient variability and optimal dosing of osimertinib: a physiologically based pharmacokinetic modeling approach | Exploring inter-ethnic and inter-patient variability and optimal dosing of osimertinib: a physiologically based pharmacokinetic modeling approach Abstract Abstract Purpose: This study aimed to develop and validate a physiologically based pharmacokinetic (PBPK) model for osimertinib (OSI) to predict plasma trough concen... |
PMC5040747 | core_pubmed_pmc | Preparation and Evaluation of a Novel Class of Amphiphilic Amines as Antitumor Agents and Nanocarriers for Bioactive Molecules | Preparation and Evaluation of a Novel Class of Amphiphilic Amines as Antitumor Agents and Nanocarriers for Bioactive Molecules Abstract Abstract Purpose We describe a novel class of antitumor amphiphilic amines (RCn) based on a tricyclic amine hydrophilic head and a hydrophobic linear alkyl tail of variable length. Met... |
PMC12533794 | core_pubmed_pmc | Anxiolytic Effects of Indole Alkaloids From Rauvolfia ligustrina in Adult Zebrafish: Involvement of the GABAergic and 5‐HT Systems | Anxiolytic Effects of Indole Alkaloids From Rauvolfia ligustrina in Adult Zebrafish: Involvement of the GABAergic and 5‐HT Systems Abstract ABSTRACT Benzodiazepines are widely used in the treatment of anxiety, but their use may be interrupted due to side effects. This study evaluated the indole alkaloids isocarapanaubi... |
PMC6208968 | core_pubmed_pmc | DPCPX, a selective adenosine A1 receptor antagonist, enhances the antidepressant-like effects of imipramine, escitalopram, and reboxetine in mice behavioral tests | DPCPX, a selective adenosine A1 receptor antagonist, enhances the antidepressant-like effects of imipramine, escitalopram, and reboxetine in mice behavioral tests Abstract Abstract The main goal of the present study was to evaluate the influence of the adenosine A1 receptor (A1R) antagonist — DPCPX — on depressive-like... |
PMC12795515 | core_pubmed_pmc | Targeting Oxalate Production by Combining Enzyme Inhibition and Proteolysis Activation: A Novel Therapeutic Approach for Primary Hyperoxaluria Type 1 | Targeting Oxalate Production by Combining Enzyme Inhibition and Proteolysis Activation: A Novel Therapeutic Approach for Primary Hyperoxaluria Type 1 Abstract Abstract Primary hyperoxaluria type 1 (PH1) is a rare genetic disorder caused by hepatic oxalate overproduction due to alanine-glyoxylate aminotransferase (AGXT)... |
PMC10247780 | core_pubmed_pmc | Final results of DESTINY-CRC01 investigating trastuzumab deruxtecan in patients with HER2-expressing metastatic colorectal cancer | Final results of DESTINY-CRC01 investigating trastuzumab deruxtecan in patients with HER2-expressing metastatic colorectal cancer Abstract Abstract DESTINY-CRC01 ( NCT03384940 ) was a multicenter, open-label, phase 2 trial assessing the efficacy and safety of trastuzumab deruxtecan (T-DXd) in patients with HER2-express... |
PMC4579403 | core_pubmed_pmc | Differentiated effects of the multimodal antidepressant vortioxetine on sleep architecture: Part 1, a pharmacokinetic/pharmacodynamic comparison with paroxetine in healthy men | Differentiated effects of the multimodal antidepressant vortioxetine on sleep architecture: Part 1, a pharmacokinetic/pharmacodynamic comparison with paroxetine in healthy men Abstract Abstract We compared the effect of vortioxetine, paroxetine and placebo after three days of dosing on sleep architecture. This was a ra... |
PMC12011704 | core_pubmed_pmc | Evaluation of BCRP-Related DDIs Between Methotrexate and Cyclosporin A Using Physiologically Based Pharmacokinetic Modelling | Evaluation of BCRP-Related DDIs Between Methotrexate and Cyclosporin A Using Physiologically Based Pharmacokinetic Modelling Abstract Background and Objective This study provides a physiologically based pharmacokinetic (PBPK) model-based analysis of the potential drug–drug interaction (DDI) between cyclosporin A (CsA),... |
PMC4389137 | core_pubmed_pmc | Clinical manifestation of macrolide antibiotic toxicity in CKD and dialysis patients | Clinical manifestation of macrolide antibiotic toxicity in CKD and dialysis patients Abstract Abstract Macrolide antibiotics, erythromycin, clarithromycin and azithromycin are commonly prescribed for upper respiratory infection, and their use has recently been further linked to immunomodulatory effects. With the widesp... |
PMC5956062 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modelling of Cytochrome P450 2C9-Related Tolbutamide Drug Interactions with Sulfaphenazole and Tasisulam | Physiologically Based Pharmacokinetic Modelling of Cytochrome P450 2C9-Related Tolbutamide Drug Interactions with Sulfaphenazole and Tasisulam Abstract Background and Objectives Cytochrome P450 2C9 (CYP2C9) is involved in the biotransformation of many commonly used drugs, and significant drug interactions have been rep... |
PMC12314527 | core_pubmed_pmc | Development and Application of Radioactive Ligands Targeting Fibroblasts with Albumin-Binding Sites | Development and Application of Radioactive Ligands Targeting Fibroblasts with Albumin-Binding Sites Abstract Abstract Fibroblast activation protein (FAP) is overexpressed on cancer-associated fibroblasts, making it an important target for cancer diagnosis and treatment, but limited tumor retention hinders late-stage di... |
PMC3193806 | core_pubmed_pmc | Meropenem vs standard of care for treatment of late onset sepsis in children of less than 90 days of age: study protocol for a randomised controlled trial | Meropenem vs standard of care for treatment of late onset sepsis in children of less than 90 days of age: study protocol for a randomised controlled trial Abstract Abstract Background Late onset neonatal sepsis (LOS) with the mortality of 17 to 27% is still a serious disease. Meropenem is an antibiotic with wide antiba... |
PMC5482848 | core_pubmed_pmc | A comparison between sphere and rod nanoparticles regarding their in vivo biological behavior and pharmacokinetics | A comparison between sphere and rod nanoparticles regarding their in vivo biological behavior and pharmacokinetics Abstract Abstract In recent years, spherical nanoparticles has been studied extensively on biomedical applications including bioimaging and biosensing, diagnostics and theranostics, but the effect of the s... |
PMC10363869 | core_pubmed_pmc | Oral paclitaxel and encequidar in patients with breast cancer: a pharmacokinetic, safety, and antitumor activity study | Oral paclitaxel and encequidar in patients with breast cancer: a pharmacokinetic, safety, and antitumor activity study Abstract Background: Paclitaxel is widely used for the treatment of metastatic breast cancer (MBC). However, it has a low oral bioavailability due to gut extrusion caused by P-glycoprotein (P-gp). Oral... |
PMC4685865 | core_pubmed_pmc | Paliperidone Palmitate for Schizoaffective Disorder: A Review of the Clinical Evidence | Paliperidone Palmitate for Schizoaffective Disorder: A Review of the Clinical Evidence Abstract Abstract Introduction Despite being frequently diagnosed, there has been very limited study of efficacious treatments for schizoaffective disorder. Paliperidone had been approved for the treatment of schizoaffective disorder... |
PMC12491331 | core_pubmed_pmc | Using threshold Cox models to estimate change points in exposure-response relationships in an occupational epidemiological study of respirable crystalline silica and silicosis risk | Using threshold Cox models to estimate change points in exposure-response relationships in an occupational epidemiological study of respirable crystalline silica and silicosis risk Abstract Abstract Introduction In occupational epidemiology, accurately quantifying exposure-response relationships is crucial. Methods We ... |
PMC6904839 | core_pubmed_pmc | Route map for the discovery and pre-clinical development of new drugs and treatments for cutaneous leishmaniasis | Route map for the discovery and pre-clinical development of new drugs and treatments for cutaneous leishmaniasis Abstract Although there have been significant advances in the treatment of visceral leishmaniasis (VL) and several novel compounds are currently in pre-clinical and clinical development for this manifestatio... |
PMC10690661 | core_pubmed_pmc | Final analysis of potential drug–drug interactions between highly purified cannabidiol and anti‐seizure medications in an open‐label expanded access program | Final analysis of potential drug–drug interactions between highly purified cannabidiol and anti‐seizure medications in an open‐label expanded access program Abstract Abstract Objective The aim of this study was to assess potential drug–drug interactions between highly purified cannabidiol (CBD) and anti‐seizure medicat... |
PMC6118268 | core_pubmed_pmc | Susceptibility to ceftobiprole of respiratory-tract pathogens collected in the United Kingdom and Ireland during 2014–2015 | Susceptibility to ceftobiprole of respiratory-tract pathogens collected in the United Kingdom and Ireland during 2014–2015 Abstract Abstract Purpose Lower respiratory tract infections (LRTIs) can cause significant morbidity and mortality and are becoming increasingly difficult to treat because of the growing prevalence... |
PMC7806254 | core_pubmed_pmc | Is Lockdown Effective in Limiting SARS-CoV-2 Epidemic Progression?—a Cross-Country Comparative Evaluation Using Epidemiokinetic Tools | Is Lockdown Effective in Limiting SARS-CoV-2 Epidemic Progression?—a Cross-Country Comparative Evaluation Using Epidemiokinetic Tools Abstract Abstract Background To date, the risk/benefit balance of lockdown in controlling severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) epidemic is controversial. Objectiv... |
PMC6502743 | core_pubmed_pmc | Role of nanostructures in improvising oral medicine | Role of nanostructures in improvising oral medicine Abstract Highlights • Nanotechnology facilitates oral administration of drugs. • Various nanostructures have been designed for this purpose. • These nanoformulations are useful for many diseases. Abbreviations: AD, Alzheimer’s disease; AmB, amphotericin B; AMCNS, cati... |
PMC11183306 | core_pubmed_pmc | Influence of β-lactam pharmacodynamics on the systems microbiology of gram-positive and gram-negative polymicrobial communities | Influence of β-lactam pharmacodynamics on the systems microbiology of gram-positive and gram-negative polymicrobial communities Abstract Abstract Objectives We sought to evaluate the pharmacodynamics of β-lactam antibacterials against polymicrobial communities of clinically relevant gram-positive and gram-negative path... |
PMC9504415 | core_pubmed_pmc | Discovery of Pinostrobin as a Melanogenic Agent in cAMP/PKA and p38 MAPK Signaling Pathway | Discovery of Pinostrobin as a Melanogenic Agent in cAMP/PKA and p38 MAPK Signaling Pathway Abstract Abstract Melanogenesis is the process of melanin synthesis to protect the skin against ultraviolet radiation and other external stresses. The loss of skin pigmentation is closely related to depigmented skin disorders. Th... |
PMC12663059 | core_pubmed_pmc | Pharmacokinetics of imipenem in critically ill patients: Continuous infusion versus extended infusion in a real-world study | Pharmacokinetics of imipenem in critically ill patients: Continuous infusion versus extended infusion in a real-world study Abstract Abstract Objective This study compared the pharmacokinetic/pharmacodynamic properties of extended infusion and continuous infusion of imipenem at equivalent daily doses in a real-world se... |
PMC11643521 | core_pubmed_pmc | Evaluation of Quinazolin-2,4-Dione Derivatives as Promising Antibacterial Agents: Synthesis, In Vitro, In Silico ADMET and Molecular Docking Approaches | Evaluation of Quinazolin-2,4-Dione Derivatives as Promising Antibacterial Agents: Synthesis, In Vitro, In Silico ADMET and Molecular Docking Approaches Abstract Abstract A series of new quinazolin-2,4-dione derivatives incorporating amide/eight-membered nitrogen-heterocycles 2a – c , in addition, acylthiourea/amide/dit... |
PMC5466677 | core_pubmed_pmc | Real-time imaging of intestinal bacterial β-glucuronidase activity by hydrolysis of a fluorescent probe | Real-time imaging of intestinal bacterial β-glucuronidase activity by hydrolysis of a fluorescent probe Abstract Intestinal bacterial β-glucuronidase (βG) hydrolyzes glucuronidated metabolites to their toxic form in intestines, resulting in intestinal damage. The development of a method to inhibit βG is thus important ... |
PMC10172697 | core_pubmed_pmc | Improving levodopa delivery: IPX203, a novel extended-release carbidopa-levodopa formulation | Improving levodopa delivery: IPX203, a novel extended-release carbidopa-levodopa formulation Abstract Highlights • IPX203 is a novel oral extended-release formulation of CD and LD. • Aims to address the short half-life and limited absorption area of LD in the GIT. • Contains IR granules and ER coated beads. • Mucoadhes... |
PMC7004090 | core_pubmed_pmc | Safety Profiles, Pharmacokinetics, and Changes in Bone Turnover Markers After Twice‐Weekly Subcutaneous Administration of Teriparatide in Healthy Japanese Postmenopausal Women: A Single‐Blind Randomized Study | Safety Profiles, Pharmacokinetics, and Changes in Bone Turnover Markers After Twice‐Weekly Subcutaneous Administration of Teriparatide in Healthy Japanese Postmenopausal Women: A Single‐Blind Randomized Study Abstract Abstract Once‐weekly injection of 56.5‐μg teriparatide formulation is a potent therapeutic agent for o... |
PMC6748410 | core_pubmed_pmc | A phase 2 study of an oral mTORC1/mTORC2 kinase inhibitor (CC-223) for non-pancreatic neuroendocrine tumors with or without carcinoid symptoms | A phase 2 study of an oral mTORC1/mTORC2 kinase inhibitor (CC-223) for non-pancreatic neuroendocrine tumors with or without carcinoid symptoms Abstract Abstract Second-generation mammalian target of rapamycin (mTOR) inhibitors such as CC-223 may have theoretical advantages over first-generation drugs by inhibiting TOR ... |
PMC4976473 | core_pubmed_pmc | Pharmacokinetics and dose adjustment of etoposide administered in a medium-dose etoposide, cyclophosphamide and total body irradiation regimen before allogeneic hematopoietic stem cell transplantation | Pharmacokinetics and dose adjustment of etoposide administered in a medium-dose etoposide, cyclophosphamide and total body irradiation regimen before allogeneic hematopoietic stem cell transplantation Abstract Abstract Background We investigated the pharmacokinetics of etoposide (ETP) to reduce the inter-individual var... |
PMC3894582 | core_pubmed_pmc | Influence of Polyethylene Glycol Lipid Desorption Rates on Pharmacokinetics and Pharmacodynamics of siRNA Lipid Nanoparticles | Influence of Polyethylene Glycol Lipid Desorption Rates on Pharmacokinetics and Pharmacodynamics of siRNA Lipid Nanoparticles Abstract Lipid nanoparticles (LNPs) encapsulating short interfering RNAs that target hepatic genes are advancing through clinical trials, and early results indicate the excellent gene silencing ... |
PMC3553417 | core_pubmed_pmc | Phase 1, open-label study of MEDI-547 in patients with relapsed or refractory solid tumors | Phase 1, open-label study of MEDI-547 in patients with relapsed or refractory solid tumors Abstract Summary Background Targeting the cell-surface receptor EphA2, which is highly expressed in some solid tumors, is a novel approach for cancer therapy. We aimed to evaluate the safety profile, maximum tolerated dose (MTD),... |
PMC3987191 | core_pubmed_pmc | Population pharmacokinetics of bupivacaine in combined lumbar and sciatic nerve block | Population pharmacokinetics of bupivacaine in combined lumbar and sciatic nerve block Abstract Abstract Objectives: The primary aim of this study was to establish the population pharmacokinetic (PPK) model of bupivacaine after combined lumbar plexus and sciatic nerve blocks and secondary aim is to assess the effect of ... |
PMC8049034 | core_pubmed_pmc | Pharmacokinetics and Optimal Dose Selection of Cefazolin for Surgical Prophylaxis of Pediatric Patients | Pharmacokinetics and Optimal Dose Selection of Cefazolin for Surgical Prophylaxis of Pediatric Patients Abstract Abstract Cefazolin is an antibiotic frequently used for perioperative prophylaxis. Data from healthy adults and pediatric surgery patients were pooled to refine a previously developed population pharmacokine... |
PMC3495881 | core_pubmed_pmc | Role of aldo-keto reductases and other doxorubicin pharmacokinetic genes in doxorubicin resistance, DNA binding, and subcellular localization | Role of aldo-keto reductases and other doxorubicin pharmacokinetic genes in doxorubicin resistance, DNA binding, and subcellular localization Abstract Abstract Background Since proteins involved in chemotherapy drug pharmacokinetics and pharmacodynamics have a strong impact on the uptake, metabolism, and efflux of such... |
PMC10508573 | core_pubmed_pmc | Semimechanistic pharmacokinetic–pharmacodynamic model of tripegfilgrastim for pediatric patients after chemotherapy | Semimechanistic pharmacokinetic–pharmacodynamic model of tripegfilgrastim for pediatric patients after chemotherapy Abstract Abstract Tripegfilgrastim is a long‐acting granulocyte colony‐stimulating factor (G‐CSF) that has been used to prevent chemotherapy‐induced neutropenia in adults. This study aimed to establish a ... |
PMC9315033 | core_pubmed_pmc | Population Pharmacokinetic Modeling and Simulation of TV‐46000: A Long‐Acting Injectable Formulation of Risperidone | Population Pharmacokinetic Modeling and Simulation of TV‐46000: A Long‐Acting Injectable Formulation of Risperidone Abstract Abstract TV‐46000 is a long‐acting subcutaneous antipsychotic that uses a novel copolymer drug delivery technology in combination with a well‐characterized molecule, risperidone, that is in clini... |
PMC11357166 | core_pubmed_pmc | Recent Research Progress on the Chemical Constituents, Pharmacology, and Pharmacokinetics of Alpinae oxyphyllae Fructus | Recent Research Progress on the Chemical Constituents, Pharmacology, and Pharmacokinetics of Alpinae oxyphyllae Fructus Abstract Abstract Alpinae oxyphyllae fructus (AOF), the dried mature fruit of Alpinia oxyphylla Miquel of the Zingiberaceae family, shows many special pharmacological effects. In recent years, there h... |
PMC12369151 | core_pubmed_pmc | High-affinity transferrin receptor binding improves brain delivery of bispecific antibodies at tracer dose | High-affinity transferrin receptor binding improves brain delivery of bispecific antibodies at tracer dose Abstract Abstract Background Transferrin receptor (TfR)-mediated transcytosis is a well-established method for delivering biologic therapeutics and diagnostics to the brain. Although moderate affinity towards TfR ... |
PMC10477127 | core_pubmed_pmc | An artesunate pharmacometric model to explain therapeutic responses in falciparum malaria | An artesunate pharmacometric model to explain therapeutic responses in falciparum malaria Abstract Abstract Background The artemisinins are potent and widely used antimalarial drugs that are eliminated rapidly. A simple concentration–effect pharmacometric model does not explain why dosing more frequently than once dail... |
PMC9579393 | core_pubmed_pmc | Integrating real‐world data to accelerate and guide drug development: A clinical pharmacology perspective | Integrating real‐world data to accelerate and guide drug development: A clinical pharmacology perspective Abstract Abstract Pharmaceutical products in the current accelerated drug development landscape can benefit from tools beyond data generated from randomized control trials. We have seen an abundance of real‐world d... |
PMC10195956 | core_pubmed_pmc | Safety, Tolerability and Pharmacokinetics of Single-Dose Oral SYHA1402 in Healthy Chinese Subjects | Safety, Tolerability and Pharmacokinetics of Single-Dose Oral SYHA1402 in Healthy Chinese Subjects Abstract Abstract Introduction To assess the safety, tolerability and pharmacokinetics of a single dose of SYHA1402 in healthy Chinese subjects. Methods This was a randomized, double-blind, placebo-controlled, single-asce... |
PMC8498896 | core_pubmed_pmc | Survival‐Assured Liver Injury Preconditioning (SALIC) Enables Robust Expansion of Human Hepatocytes in Fah –/– Rag2 –/– IL2rg –/– Rats | Survival‐Assured Liver Injury Preconditioning (SALIC) Enables Robust Expansion of Human Hepatocytes in Fah –/– Rag2 –/– IL2rg –/– Rats Abstract Abstract Although liver‐humanized animals are desirable tools for drug development and expansion of human hepatocytes in large quantities, their development is restricted to mi... |
PMC3634750 | core_pubmed_pmc | The Potential Regimen of Target-Controlled Infusion of Propofol in Flexible Bronchoscopy Sedation: A Randomized Controlled Trial | The Potential Regimen of Target-Controlled Infusion of Propofol in Flexible Bronchoscopy Sedation: A Randomized Controlled Trial Abstract Abstract Objectives Target-controlled infusion (TCI) provides precise pharmacokinetic control of propofol concentration in the effect-site (Ce), eg. brain. This pilot study aims to e... |
PMC4363216 | core_pubmed_pmc | Evaluation of High-Dose Daptomycin Versus Vancomycin Alone or Combined with Clarithromycin or Rifampin Against Staphylococcus aureus and S. epidermidis in a Novel In Vitro PK/PD Model of Bacterial Biofilm | Evaluation of High-Dose Daptomycin Versus Vancomycin Alone or Combined with Clarithromycin or Rifampin Against Staphylococcus aureus and S. epidermidis in a Novel In Vitro PK/PD Model of Bacterial Biofilm Abstract Abstract Introduction Medical device infections are associated with significant morbidity and mortality. T... |
PMC6571706 | core_pubmed_pmc | Nanoemulsion Based Vehicle for Effective Ocular Delivery of Moxifloxacin Using Experimental Design and Pharmacokinetic Study in Rabbits | Nanoemulsion Based Vehicle for Effective Ocular Delivery of Moxifloxacin Using Experimental Design and Pharmacokinetic Study in Rabbits Abstract Abstract Nanoemulsion is one of the potential drug delivery strategies used in topical ocular therapy. The purpose of this study was to design and optimize a nanoemulsion-base... |
PMC12153050 | core_pubmed_pmc | Galactose receptor-mediated hepatic targeting system: engineering of quinary cationic liposomes for resveratrol delivery against hepatic steatosis † | Galactose receptor-mediated hepatic targeting system: engineering of quinary cationic liposomes for resveratrol delivery against hepatic steatosis † Abstract Abstract Resveratrol (RSV), a natural polyphenol with potent antioxidant and anti-inflammatory properties, exhibits significant therapeutic potential for non-alco... |
PMC10535222 | core_pubmed_pmc | Understanding Discordance between In Vitro Dissolution, Local Gut and Systemic Bioequivalence of Budesonide in Healthy and Crohn’s Disease Patients through PBPK Modeling | Understanding Discordance between In Vitro Dissolution, Local Gut and Systemic Bioequivalence of Budesonide in Healthy and Crohn’s Disease Patients through PBPK Modeling Abstract Abstract The most common method for establishing bioequivalence (BE) is to demonstrate similarity of concentration–time profiles in the syste... |
PMC9612322 | core_pubmed_pmc | Effects of Myristicin in Association with Chemotherapies on the Reversal of the Multidrug Resistance (MDR) Mechanism in Cancer | Effects of Myristicin in Association with Chemotherapies on the Reversal of the Multidrug Resistance (MDR) Mechanism in Cancer Abstract Abstract A range of drugs used in cancer treatment comes from natural sources. However, chemotherapy has been facing a major challenge related to multidrug resistance (MDR), a mechanis... |
PMC6271293 | core_pubmed_pmc | Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats | Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats Abstract Abstract Although linarin possesses diverse pharmacological activities, its poor oral bioavailability has been a concern for further development. The present study aimed to demonstrate the feasibility of improving the or... |
PMC4260000 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling and Simulation in Pediatric Drug Development | Physiologically Based Pharmacokinetic Modeling and Simulation in Pediatric Drug Development Abstract Abstract Increased regulatory demands for pediatric drug development research have fostered interest in the use of modeling and simulation among industry and academia. Physiologically based pharmacokinetic (PBPK) modeli... |
PMC8235594 | core_pubmed_pmc | Population Pharmacokinetics and Significant Under-Dosing of Anti-Tuberculosis Medications in People with HIV and Critical Illness | Population Pharmacokinetics and Significant Under-Dosing of Anti-Tuberculosis Medications in People with HIV and Critical Illness Abstract Abstract Critical illness from tuberculosis (TB) bloodstream infection results in a high case fatality rate for people living with human immunodeficiency virus (HIV). Critical illne... |
PMC10146102 | core_pubmed_pmc | Evaluation of [ 18 F]Favipiravir in Rodents and Nonhuman Primates (NHP) with Positron Emission Tomography | Evaluation of [ 18 F]Favipiravir in Rodents and Nonhuman Primates (NHP) with Positron Emission Tomography Abstract Abstract The COVID-19 pandemic has posed a significant challenge to global public health. In response, the search for specific antiviral drugs that can effectively treat the disease caused by the SARS-CoV-... |
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