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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-...