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PMC11479929 | core_pubmed_pmc | Development and application of a physiologically-based pharmacokinetic model for ractopamine in goats | Development and application of a physiologically-based pharmacokinetic model for ractopamine in goats Abstract Abstract Physiologically Based Pharmacokinetic (PBPK) models can provide forecasts of the drug residues within the organism. Ractopamine (RAC) is a typical β-agonist. In this study, we developed a PBPK model f... |
PMC11874020 | core_pubmed_pmc | Oxazole-Based Ferroptosis Inhibitors with Promising Properties to Treat Central Nervous System Diseases | Oxazole-Based Ferroptosis Inhibitors with Promising Properties to Treat Central Nervous System Diseases Abstract Ferroptosis plays an important role in the occurrence and development of many diseases, including neurodegenerative diseases. Thus, ferroptosis inhibitors able to cross the blood-brain barrier may have thera... |
PMC10558965 | core_pubmed_pmc | Dose rationale for gabapentin and tramadol in pediatric patients with chronic pain | Dose rationale for gabapentin and tramadol in pediatric patients with chronic pain Abstract Abstract Despite off‐label use, the efficacy and safety of gabapentin and tramadol in pediatric patients (3 months to <18 years old) diagnosed with chronic pain has not been characterized. However, generating evidence based on r... |
PMC10433949 | core_pubmed_pmc | Phage-Antibiotic Cocktail Rescues Daptomycin and Phage Susceptibility against Daptomycin-Nonsusceptible Enterococcus faecium in a Simulated Endocardial Vegetation Ex Vivo Model | Phage-Antibiotic Cocktail Rescues Daptomycin and Phage Susceptibility against Daptomycin-Nonsusceptible Enterococcus faecium in a Simulated Endocardial Vegetation Ex Vivo Model Abstract ABSTRACT Enterococcus faecium is a difficult-to-treat pathogen with emerging resistance to most clinically available antibiotics. Dapt... |
PMC3832778 | core_pubmed_pmc | The effect of hepatic or renal impairment on the pharmacokinetics of edivoxetine, a selective norepinephrine transporter reuptake inhibitor | The effect of hepatic or renal impairment on the pharmacokinetics of edivoxetine, a selective norepinephrine transporter reuptake inhibitor Abstract Abstract Purpose To assess the impact of hepatic or renal impairment on the pharmacokinetics (PK) of edivoxetine. Methods Two separate multi-center, open-label studies wit... |
PMC6462165 | core_pubmed_pmc | Characterization and bioactivity of self-assembled anti-angiogenic chondroitin sulfate-ES2-AF nanoparticle conjugate | Characterization and bioactivity of self-assembled anti-angiogenic chondroitin sulfate-ES2-AF nanoparticle conjugate Abstract Abstract Background In the past few years, significant progress has been made in inhibiting neovascularization at the tumor site, cutting off the nutrient supply of the tumor, and inhibiting tum... |
PMC4506385 | core_pubmed_pmc | A phase II and pharmacodynamic study of sunitinib in relapsed/refractory oesophageal and gastro-oesophageal cancers | A phase II and pharmacodynamic study of sunitinib in relapsed/refractory oesophageal and gastro-oesophageal cancers Abstract Background: Blockade of the vascular endothelial growth factor (VEGF) pathway shows evidence of activity in gastro-oesophageal (GE) and oesophageal cancer. We investigated the efficacy of sunitin... |
PMC6215984 | core_pubmed_pmc | Antibiotic Elution Characteristics and Pharmacokinetics of Gentamicin and Vancomycin from a Mineral Antibiotic Carrier: An in vivo Evaluation of 32 Clinical Cases | Antibiotic Elution Characteristics and Pharmacokinetics of Gentamicin and Vancomycin from a Mineral Antibiotic Carrier: An in vivo Evaluation of 32 Clinical Cases Abstract Introduction: Locally implanted antibiotic-eluting carriers may be a valuable adjuvant to the management of prosthetic joint infections. Aim: to ass... |
PMC7352358 | core_pubmed_pmc | First-In-Class CD13-Targeted Tissue Factor tTF-NGR in Patients with Recurrent or Refractory Malignant Tumors: Results of a Phase I Dose-Escalation Study | First-In-Class CD13-Targeted Tissue Factor tTF-NGR in Patients with Recurrent or Refractory Malignant Tumors: Results of a Phase I Dose-Escalation Study Abstract Background: Aminopeptidase N (CD13) is present on tumor vasculature cells and some tumor cells. Truncated tissue factor (tTF) with a C-terminal NGR-peptide (t... |
PMC5063143 | core_pubmed_pmc | Biological effect on drug distribution and vascular healing via paclitaxel‐coated balloon technology in drug eluting stent restenosis swine model | Biological effect on drug distribution and vascular healing via paclitaxel‐coated balloon technology in drug eluting stent restenosis swine model Abstract Abstract Objectives To evaluate the biological effect of a paclitaxel‐coated balloon (PCB) technology on vascular drug distribution and healing in drug eluting stent... |
PMC6820614 | core_pubmed_pmc | A prospective phase I multicentre randomized cross-over pharmacokinetic study to determine the effect of food on abiraterone pharmacokinetics | A prospective phase I multicentre randomized cross-over pharmacokinetic study to determine the effect of food on abiraterone pharmacokinetics Abstract Purpose Abiraterone acetate is used at a fixed oral dose of 1000 mg once daily (OD) taken fasted. By administering abiraterone acetate with food, a reduced dose can pote... |
PMC9705466 | core_pubmed_pmc | Pharmacokinetics of Morphine Sulfate Orodispersible Tablets and Bioequivalence with Immediate-Release Oral Morphine Sulfate Formulations in Healthy Adult Subjects Under Fasting Conditions: Single-Dose Comparative Bioavailability Studies | Pharmacokinetics of Morphine Sulfate Orodispersible Tablets and Bioequivalence with Immediate-Release Oral Morphine Sulfate Formulations in Healthy Adult Subjects Under Fasting Conditions: Single-Dose Comparative Bioavailability Studies Abstract Abstract Background and Objective An orodispersible tablet (ODT) formulati... |
PMC8092554 | core_pubmed_pmc | Piperaquine Pharmacokinetics during Intermittent Preventive Treatment for Malaria in Pregnancy | Piperaquine Pharmacokinetics during Intermittent Preventive Treatment for Malaria in Pregnancy Abstract Dihydroartemisinin-piperaquine (DP) is a long-acting artemisinin combination treatment that provides effective chemoprevention and has been proposed as an alternative antimalarial drug for intermittent preventive the... |
PMC3193779 | core_pubmed_pmc | Choosing a Gliptin | Choosing a Gliptin Abstract The treatment of type 2 diabetes mellitus (T2DM) has included the use of metformin and sulfonylurea (SU) as first-line anti-diabetic therapies world over since years. This remains, despite the knowledge that the combination results in a progressive decline in [beta]-cell function and by 3 ye... |
PMC10229467 | core_pubmed_pmc | Cannabidiol for the Treatment of Brain Disorders: Therapeutic Potential and Routes of Administration | Cannabidiol for the Treatment of Brain Disorders: Therapeutic Potential and Routes of Administration Abstract Abstract The use of cannabidiol (CBD) for treating brain disorders has gained increasing interest. While the mechanism of action of CBD in these conditions is still under investigation, CBD has been shown to af... |
PMC8516621 | core_pubmed_pmc | Penetration of Antibacterial Agents into Pulmonary Epithelial Lining Fluid: An Update | Penetration of Antibacterial Agents into Pulmonary Epithelial Lining Fluid: An Update Abstract A comprehensive review of drug penetration into pulmonary epithelial lining fluid (ELF) was previously published in 2011. Since then, an extensive number of studies comparing plasma and ELF concentrations of antibacterial age... |
PMC4434771 | core_pubmed_pmc | Charge-mediated influence of the antibody variable domain on FcRn-dependent pharmacokinetics | Charge-mediated influence of the antibody variable domain on FcRn-dependent pharmacokinetics Abstract Significance Therapeutic antibodies of the immunoglobulin G (IgG) isotype show a pharmacokinetic (PK) profile that is strongly mediated by the interaction with the neonatal Fc receptor (FcRn). Therefore, modulating the... |
PMC8748343 | core_pubmed_pmc | Pharmacokinetics of cannabichromene in a medical cannabis product also containing cannabidiol and Δ 9 -tetrahydrocannabinol: a pilot study | Pharmacokinetics of cannabichromene in a medical cannabis product also containing cannabidiol and Δ 9 -tetrahydrocannabinol: a pilot study Abstract Abstract Purpose Cannabichromene (CBC) is a phytocannabinoid commonly found in cannabis, yet its acute post-dose pharmacokinetics (PK) have not been examined in humans. Thi... |
PMC8522775 | core_pubmed_pmc | Population Pharmacokinetics of Rezafungin in Patients with Fungal Infections | Population Pharmacokinetics of Rezafungin in Patients with Fungal Infections Abstract ABSTRACT Rezafungin is a novel antifungal agent of the echinocandin class with potent activity against species of Candida and Aspergillus , including subsets of resistant strains, and Pneumocystis jirovecii . The objective of this ana... |
PMC8860396 | core_pubmed_pmc | Association of Drug-Metabolizing Enzyme and Transporter Gene Polymorphisms and Lipid-Lowering Response to Statins in Thai Patients with Dyslipidemia | Association of Drug-Metabolizing Enzyme and Transporter Gene Polymorphisms and Lipid-Lowering Response to Statins in Thai Patients with Dyslipidemia Abstract Abstract Purpose Statins are increasingly widely used in the primary and secondary prevention of cardiovascular disease. However, there is an inter-individual var... |
PMC10377668 | core_pubmed_pmc | Target therapy for high-risk neuroblastoma treatment: integration of regulatory and scientific tools is needed | Target therapy for high-risk neuroblastoma treatment: integration of regulatory and scientific tools is needed Abstract Abstract Introduction Several new active substances (ASs) targeting neuroblastoma (NBL) are under study. We aim to describe the developmental and regulatory status of a sample of ASs targeting NBL to ... |
PMC12261970 | core_pubmed_pmc | Pharmacokinetics and Safety of Polaprezinc Granules Oral Administration in Healthy Chinese Volunteers Under Fasting and Fed Conditions | Pharmacokinetics and Safety of Polaprezinc Granules Oral Administration in Healthy Chinese Volunteers Under Fasting and Fed Conditions Abstract ABSTRACT The study aimed to demonstrate bioequivalence between generic and original polaprezinc granules by comparing pharmacokinetic (PK) profiles in healthy Chinese subjects ... |
PMC3606940 | core_pubmed_pmc | Integrated Pharmacometrics and Systems Pharmacology Model-Based Analyses to Guide GnRH Receptor Modulator Development for Management of Endometriosis | Integrated Pharmacometrics and Systems Pharmacology Model-Based Analyses to Guide GnRH Receptor Modulator Development for Management of Endometriosis Abstract Abstract Endometriosis is a gynecological condition resulting from proliferation of endometrial-like tissue outside the endometrial cavity. Estrogen suppression ... |
PMC7114283 | core_pubmed_pmc | Identification of phenanthroindolizines and phenanthroquinolizidines as novel potent anti-coronaviral agents for porcine enteropathogenic coronavirus transmissible gastroenteritis virus and human severe acute respiratory syndrome coronavirus | Identification of phenanthroindolizines and phenanthroquinolizidines as novel potent anti-coronaviral agents for porcine enteropathogenic coronavirus transmissible gastroenteritis virus and human severe acute respiratory syndrome coronavirus Abstract The discovery and development of new, highly potent anti-coronavirus ... |
PMC8613112 | core_pubmed_pmc | Impact of Inflammation on Cytochromes P450 Activity in Pediatrics: A Systematic Review | Impact of Inflammation on Cytochromes P450 Activity in Pediatrics: A Systematic Review Abstract Abstract Background and Objective Cytochromes P450 (CYP) are the major enzymes involved in hepatic metabolism of drugs. Personalization of treatment in pediatrics is a major challenge, as it must not only take into account g... |
PMC12122143 | core_pubmed_pmc | Population pharmacokinetics and dosing of dispersible moxifloxacin formulation in children with rifampicin‐resistant tuberculosis | Population pharmacokinetics and dosing of dispersible moxifloxacin formulation in children with rifampicin‐resistant tuberculosis Abstract Abstract Aims Moxifloxacin is a priority drug for treating rifampicin‐resistant tuberculosis (RR‐TB). We assessed the pharmacokinetics of a child‐friendly, dispersible 100 mg tablet... |
PMC10352257 | core_pubmed_pmc | In vivo effects of the alpha-synuclein misfolding inhibitor minzasolmin supports clinical development in Parkinson’s disease | In vivo effects of the alpha-synuclein misfolding inhibitor minzasolmin supports clinical development in Parkinson’s disease Abstract Abstract Direct targeting of alpha-synuclein (ASYN) has emerged as a disease-modifying strategy for Parkinson’s disease and other synucleinopathies which is being approached using both s... |
PMC12397715 | core_pubmed_pmc | Physiologically Based Pharmacokinetic (PBPK) Model to Predict the Magnitude of Drug–Drug Interaction Between Fezolinetant and CYP1A2 Inhibitors | Physiologically Based Pharmacokinetic (PBPK) Model to Predict the Magnitude of Drug–Drug Interaction Between Fezolinetant and CYP1A2 Inhibitors Abstract Abstract Fezolinetant is a non‐hormonal, selective neurokinin 3 receptor antagonist approved in multiple countries including the United States, in Europe, and in Asia ... |
PMC7341107 | core_pubmed_pmc | Differential Monocyte Actuation in a Three‐Organ Functional Innate Immune System‐on‐a‐Chip | Differential Monocyte Actuation in a Three‐Organ Functional Innate Immune System‐on‐a‐Chip Abstract Abstract A functional, human, multiorgan, pumpless, immune system‐on‐a‐chip featuring recirculating THP‐1 immune cells with cardiomyocytes, skeletal muscle, and liver in separate compartments in a serum‐free medium is de... |
PMC12670072 | core_pubmed_pmc | Preclinical Pharmacokinetic, Pharmacodynamic, and Safety Profile of OBI-992: A Novel TROP2-Targeted Antibody–Drug Conjugate | Preclinical Pharmacokinetic, Pharmacodynamic, and Safety Profile of OBI-992: A Novel TROP2-Targeted Antibody–Drug Conjugate Abstract Abstract OBI-992, a novel TROP2-targeted antibody–drug conjugate (ADC), is composed of an anti-TROP2 antibody conjugated to exatecan, a topoisomerase 1 inhibitor, via an enzyme-cleavable ... |
PMC12214470 | core_pubmed_pmc | Dosage Regimen Optimization of Ertapenem Against ESBL ‐Producing Enterobacterales Infection in Critically Ill Patients Using Monte Carlo Simulation | Dosage Regimen Optimization of Ertapenem Against ESBL ‐Producing Enterobacterales Infection in Critically Ill Patients Using Monte Carlo Simulation Abstract ABSTRACT Extended‐spectrum beta‐lactamase (ESBL)‐producing Enterobacterales infections are associated with high mortality rates. Ertapenem is recommended as one of... |
PMC5351328 | core_pubmed_pmc | Pharmacokinetics, Safety, and CCR2/CCR5 Antagonist Activity of Cenicriviroc in Participants With Mild or Moderate Hepatic Impairment | Pharmacokinetics, Safety, and CCR2/CCR5 Antagonist Activity of Cenicriviroc in Participants With Mild or Moderate Hepatic Impairment Abstract Cenicriviroc, a dual CCR2/CCR5 antagonist, is being evaluated for treatment of nonalcoholic steatohepatitis and liver fibrosis (CENTAUR; NCT02217475 ). As it is metabolized by th... |
PMC12455078 | core_pubmed_pmc | Synthesis, pharmacokinetic studies, and metabolite analysis of meridianin C in rats using a validated ultra high performance liquid chromatography-tandem mass spectrometry method | Synthesis, pharmacokinetic studies, and metabolite analysis of meridianin C in rats using a validated ultra high performance liquid chromatography-tandem mass spectrometry method Abstract Introduction Meridianin C (MC) is a marine-derived indole alkaloid that has demonstrated kinase inhibitory and anti-tumor activities... |
PMC6766976 | core_pubmed_pmc | Characterization of the Effect of Hepatic Impairment on Upadacitinib Pharmacokinetics | Characterization of the Effect of Hepatic Impairment on Upadacitinib Pharmacokinetics Abstract Abstract Upadacitinib is a selective Janus kinase 1 inhibitor being developed for the treatment of several inflammatory autoimmune diseases, including rheumatoid arthritis. Upadacitinib is a nonsensitive substrate for metabol... |
PMC9365377 | core_pubmed_pmc | Phase Ib/II Trial of Ribociclib in Combination with Binimetinib in Patients with NRAS -mutant Melanoma | Phase Ib/II Trial of Ribociclib in Combination with Binimetinib in Patients with NRAS -mutant Melanoma Abstract Abstract Purpose: Enhanced MAPK pathway signaling and cell-cycle checkpoint dysregulation are frequent in NRAS -mutant melanoma and, as such, the regimen of the MEK inhibitor binimetinib and the selective CDK... |
PMC4504433 | core_pubmed_pmc | Structure-Guided DOT1L Probe Optimization by Label-Free Ligand Displacement | Structure-Guided DOT1L Probe Optimization by Label-Free Ligand Displacement Abstract The DOT1L lysine methyltransferase has emerged as a validated therapeutic target in MLL -rearranged (MLLr) acute leukemias. Although S-adenosylmethionine competitive inhibitors have demonstrated pharmacological proof-of-principle in ML... |
PMC7764829 | core_pubmed_pmc | Use of Oral Tetracyclines in the Treatment of Adult Patients with Community-Acquired Bacterial Pneumonia: A Literature Review on the Often-Overlooked Antibiotic Class | Use of Oral Tetracyclines in the Treatment of Adult Patients with Community-Acquired Bacterial Pneumonia: A Literature Review on the Often-Overlooked Antibiotic Class Abstract Abstract Oral tetracyclines have been used in clinical practice for over 60 years. Overall, one of the most common indications for use of oral t... |
PMC4897679 | core_pubmed_pmc | Effect of Catnip Charcoal on the In Vivo Pharmacokinetics of the Main Alkaloids of Rhizoma Coptidis | Effect of Catnip Charcoal on the In Vivo Pharmacokinetics of the Main Alkaloids of Rhizoma Coptidis Abstract Abstract This study aims to explore the effect of catnip Nepeta cataria (CNC) charcoal on the pharmacokinetics of the main alkaloids of Rhizoma Coptidis in vivo . Twenty-four rabbits were randomly divided into f... |
PMC6079592 | core_pubmed_pmc | Pharmacokinetics and Bioavailability Study of Tubeimoside I in ICR Mice by UPLC-MS/MS | Pharmacokinetics and Bioavailability Study of Tubeimoside I in ICR Mice by UPLC-MS/MS Abstract Abstract The aim of this study is to establish and validate a rapid, selective, and sensitive ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method to determine tubeimoside I (TBMS-I) in ICR (In... |
PMC5072573 | core_pubmed_pmc | Pharmacist-managed dose adjustment feedback using therapeutic drug monitoring of vancomycin was useful for patients with methicillin-resistant Staphylococcus aureus infections: a single institution experience | Pharmacist-managed dose adjustment feedback using therapeutic drug monitoring of vancomycin was useful for patients with methicillin-resistant Staphylococcus aureus infections: a single institution experience Abstract Background Vancomycin (VCM) requires dose adjustment based on therapeutic drug monitoring. At Aomori P... |
PMC11923190 | core_pubmed_pmc | Credibility assessment of a mechanistic model of atherosclerosis to predict cardiovascular outcomes under lipid-lowering therapy | Credibility assessment of a mechanistic model of atherosclerosis to predict cardiovascular outcomes under lipid-lowering therapy Abstract Abstract Demonstrating cardiovascular (CV) benefits with lipid-lowering therapy (LLT) requires long-term randomized clinical trials (RCTs) with thousands of patients. Innovative appr... |
PMC8212499 | core_pubmed_pmc | IMI2-PainCare-BioPain-RCT3: a randomized, double-blind, placebo-controlled, crossover, multi-center trial in healthy subjects to investigate the effects of lacosamide, pregabalin, and tapentadol on biomarkers of pain processing observed by electroencephalography (EEG) | IMI2-PainCare-BioPain-RCT3: a randomized, double-blind, placebo-controlled, crossover, multi-center trial in healthy subjects to investigate the effects of lacosamide, pregabalin, and tapentadol on biomarkers of pain processing observed by electroencephalography (EEG) Abstract Background IMI2-PainCare-BioPain-RCT3 is o... |
PMC10983867 | core_pubmed_pmc | A low-footprint, fluorescence-based bacterial time-kill assay for estimating dose-dependent cell death dynamics | A low-footprint, fluorescence-based bacterial time-kill assay for estimating dose-dependent cell death dynamics Abstract Dose-response curves that describe the relationship between antibiotic dose and growth rate in bacteria are commonly measured with optical density (OD) based assays. While being simple and high-throu... |
PMC7566361 | core_pubmed_pmc | Dose recommendations for gentamicin in the real-world obese population with varying body weight and renal (dys)function | Dose recommendations for gentamicin in the real-world obese population with varying body weight and renal (dys)function Abstract Abstract Background The impact of weight on pharmacokinetics of gentamicin was recently elucidated for (morbidly) obese individuals with normal renal function. Objectives To characterize the ... |
PMC12440713 | core_pubmed_pmc | Pharmacometrics modeling and simulation to assist phenobarbital dose optimization in dogs | Pharmacometrics modeling and simulation to assist phenobarbital dose optimization in dogs Abstract Introduction Phenobarbital (PB) remains the first-line treatment for canine epilepsy due to its efficacy, affordability, and favorable pharmacokinetics. However, its narrow therapeutic index and substantial interindividua... |
PMC11944613 | core_pubmed_pmc | Intravenous vs. Oral Dose Comparison of Ibuprofen and Tramadol Combinations—Enantiomers, Metabolite, Linearity, and Sex-Related Effects: A Pharmacokinetics Randomized Clinical Trial | Intravenous vs. Oral Dose Comparison of Ibuprofen and Tramadol Combinations—Enantiomers, Metabolite, Linearity, and Sex-Related Effects: A Pharmacokinetics Randomized Clinical Trial Abstract Abstract Background/Objectives: Using a combination of analgesics allows for the use of lower doses of each, therefore, lowering ... |
PMC7470835 | core_pubmed_pmc | Preclinical PK/PD model for the combinatorial use of dexamethasone and sulpiride in the treatment of breast cancer | Preclinical PK/PD model for the combinatorial use of dexamethasone and sulpiride in the treatment of breast cancer Abstract Abstract Previous studies show that dopamine D 2 -like receptor (D2DR) antagonist sulpiride (SUL) enhances the antitumor efficacy of dexamethasone (DEX) in drug-resistant breast cancer involving c... |
PMC11123961 | core_pubmed_pmc | Design, Synthesis, and Biological Evaluation of the Quorum-Sensing Inhibitors of Pseudomonas aeruginosa PAO1 | Design, Synthesis, and Biological Evaluation of the Quorum-Sensing Inhibitors of Pseudomonas aeruginosa PAO1 Abstract Abstract Due to the resistance of Gram-negative bacteria Pseudomonas aeruginosa PAO1 to most clinically relevant antimicrobials, the use of traditional antibiotic treatments in hospitals is challenging.... |
PMC5516232 | core_pubmed_pmc | Results From the First‐in‐Human Study With Ozanimod, a Novel, Selective Sphingosine‐1‐Phosphate Receptor Modulator | Results From the First‐in‐Human Study With Ozanimod, a Novel, Selective Sphingosine‐1‐Phosphate Receptor Modulator Abstract Abstract The sphingosine‐1‐phosphate 1 receptor (S1P 1R ) is expressed by lymphocytes, dendritic cells, and vascular endothelial cells and plays a role in the regulation of chronic inflammation an... |
PMC6062633 | core_pubmed_pmc | Pharmacokinetics of Single-Dose Oral Pregabalin Administration in Normal Cats | Pharmacokinetics of Single-Dose Oral Pregabalin Administration in Normal Cats Abstract Abstract Objective: To describe the pharmacokinetic parameters of oral pregabalin in normal cats after single oral dosing. Animals: Six healthy adult research cats. Procedures: Following sedation and indwelling catheter placement, on... |
PMC12059368 | core_pubmed_pmc | Hepatoprotective Effects of Resveratrol on Acetaminophen-Induced Acute Liver Injury and Its Implications for Tofacitinib Disposition in Rats | Hepatoprotective Effects of Resveratrol on Acetaminophen-Induced Acute Liver Injury and Its Implications for Tofacitinib Disposition in Rats Abstract Tofacitinib, which is used to treat rheumatoid arthritis (RA), is primarily metabolized by the hepatic cytochrome P450 (CYP) enzymes, CYP3A1/2 and CYP2C11. Acetaminophen ... |
PMC5286432 | core_pubmed_pmc | The antibacterial activities of aditoprim and its efficacy in the treatment of swine streptococcosis | The antibacterial activities of aditoprim and its efficacy in the treatment of swine streptococcosis Abstract Abstract Aditoprim (ADP) has potential use as an antimicrobial agent in animals. However, its pharmacodynamic properties have not been systematically studied yet. In this study, the in vitro antibacterial activ... |
PMC5865560 | core_pubmed_pmc | Bioequivalence of a biosimilar enoxaparin sodium to Clexane ® after single 100 mg subcutaneous dose: results of a randomized, double-blind, crossover study in healthy volunteers | Bioequivalence of a biosimilar enoxaparin sodium to Clexane ® after single 100 mg subcutaneous dose: results of a randomized, double-blind, crossover study in healthy volunteers Abstract Purpose To demonstrate the pharmacokinetic/pharmacodynamic (PK/PD) equivalence of a biosimilar enoxaparin to the reference drug, and ... |
PMC9868777 | core_pubmed_pmc | Food Interactions Observed in a Pharmacokinetic Investigation Comparing Two Marketed Cold Preparations (BNO1016 and ELOM-080) after Administration to Beagle Dogs – A Pilot Study | Food Interactions Observed in a Pharmacokinetic Investigation Comparing Two Marketed Cold Preparations (BNO1016 and ELOM-080) after Administration to Beagle Dogs – A Pilot Study Abstract Sinupret extract (BNO 1016) and Gelomyrtol forte (ELOM-080) represent the two top-selling cold remedies in Germany nowadays. Whereas ... |
PMC5759177 | core_pubmed_pmc | A Low Concentration of Tacrolimus/Semifluorinated Alkane (SFA) Eyedrop Suppresses Intraocular Inflammation in Experimental Models of Uveitis | A Low Concentration of Tacrolimus/Semifluorinated Alkane (SFA) Eyedrop Suppresses Intraocular Inflammation in Experimental Models of Uveitis Abstract Abstract Purpose: Corticosteroids remain the mainstay therapy for uveitis, a major cause of blindness in the working age population. However, a substantial number of pati... |
PMC7020275 | core_pubmed_pmc | Analysis of Longitudinal‐Ordered Categorical Data for Muscle Spasm Adverse Event of Vismodegib: Comparison Between Different Pharmacometric Models | Analysis of Longitudinal‐Ordered Categorical Data for Muscle Spasm Adverse Event of Vismodegib: Comparison Between Different Pharmacometric Models Abstract Abstract Longitudinal‐ordered categorical data, common in clinical trials, can be effectively analyzed with nonlinear mixed effect models. In this article, we syste... |
PMC9476784 | core_pubmed_pmc | Preparation and pharmacokinetics in vivo of linarin solid dispersion and liposome | Preparation and pharmacokinetics in vivo of linarin solid dispersion and liposome Abstract Objective The current investigation aimed to determine the appropriate dosage form by comparing solid dispersion and liposome to achieve the purpose of improving the solubility and bioavailability of linarin. Methods Linarin soli... |
PMC8235690 | core_pubmed_pmc | Development of Bisphosphonate-Conjugated Antibiotics to Overcome Pharmacodynamic Limitations of Local Therapy: Initial Results with Carbamate Linked Sitafloxacin and Tedizolid | Development of Bisphosphonate-Conjugated Antibiotics to Overcome Pharmacodynamic Limitations of Local Therapy: Initial Results with Carbamate Linked Sitafloxacin and Tedizolid Abstract Abstract The use of local antibiotics to treat bone infections has been questioned due to a lack of clinical efficacy and emerging info... |
PMC4588194 | core_pubmed_pmc | Influence of Differing Analgesic Formulations of Aspirin on Pharmacokinetic Parameters | Influence of Differing Analgesic Formulations of Aspirin on Pharmacokinetic Parameters Abstract Abstract Aspirin has been used therapeutically for over 100 years. As the originator and an important marketer of aspirin-containing products, Bayer’s clinical trial database contains numerous reports of the pharmacokinetics... |
PMC3277823 | core_pubmed_pmc | Feasibility study of two schedules of sunitinib in combination with pemetrexed in patients with advanced solid tumors | Feasibility study of two schedules of sunitinib in combination with pemetrexed in patients with advanced solid tumors Abstract Summary Background Sunitinib is an oral multitargeted tyrosine kinase inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptors, as well as of other receptor ... |
PMC12647317 | core_pubmed_pmc | Pharmacokinetics and safety of gadopiclenol in Japanese healthy volunteers | Pharmacokinetics and safety of gadopiclenol in Japanese healthy volunteers Abstract Abstract Purpose The aim of this study was to evaluate the pharmacokinetics and safety of gadopiclenol in Japanese healthy volunteers. A population-based pharmacokinetic approach was used to compare pharmacokinetic parameters with a non... |
PMC9246806 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamic Effect of a Blood-Brain Barrier-Crossing Fusion Protein Therapeutic for Alzheimer’s Disease in Rat and Dog | Pharmacokinetics and Pharmacodynamic Effect of a Blood-Brain Barrier-Crossing Fusion Protein Therapeutic for Alzheimer’s Disease in Rat and Dog Abstract Purpose We have recently demonstrated the brain-delivery of an Amyloid-ß oligomer (Aßo)-binding peptide-therapeutic fused to the BBB-crossing single domain antibody FC... |
PMC8917008 | core_pubmed_pmc | A Phase I Study to Evaluate the Pharmacokinetics and Safety of Lorlatinib in Adults with Mild, Moderate, and Severe Renal Impairment | A Phase I Study to Evaluate the Pharmacokinetics and Safety of Lorlatinib in Adults with Mild, Moderate, and Severe Renal Impairment Abstract Background and Objectives Lorlatinib is approved (100 mg once daily [QD]) for the treatment of patients with anaplastic lymphoma kinase - (ALK) positive metastatic non-small cell... |
PMC12929527 | core_pubmed_pmc | Mechanistic modeling of amyloid dynamics relating to Alzheimer's disease progression | Mechanistic modeling of amyloid dynamics relating to Alzheimer's disease progression Abstract The use of mechanistic models to support personalized medicine and precision diagnostics offers transformative potential for neurology. In this study, we developed a mechanistic model of Alzheimer's Disease progression (mAD) t... |
PMC11035541 | core_pubmed_pmc | Hexahydrocannabinol (HHC) and Δ 9 -tetrahydrocannabinol (Δ 9 -THC) driven activation of cannabinoid receptor 1 results in biased intracellular signaling | Hexahydrocannabinol (HHC) and Δ 9 -tetrahydrocannabinol (Δ 9 -THC) driven activation of cannabinoid receptor 1 results in biased intracellular signaling Abstract Abstract The Cannabis sativa plant has been used for centuries as a recreational drug and more recently in the treatment of patients with neurological or psyc... |
PMC6613258 | core_pubmed_pmc | Continuous high-dose infusion of doripenem in a pneumonia patient infected by carbapenem-resistant Pseudomonas aeruginosa : a case report | Continuous high-dose infusion of doripenem in a pneumonia patient infected by carbapenem-resistant Pseudomonas aeruginosa : a case report Abstract Abstract Background Despite the high mortality of patients with sepsis and carbapenem-resistant bacteria infection, appropriate antimicrobial therapies are yet to be establi... |
PMC12897697 | core_pubmed_pmc | Natural Products Targeting Key Molecular Hallmarks in Gastric Cancer: Focus on Apoptosis, Inflammation, and Chemoresistance | Natural Products Targeting Key Molecular Hallmarks in Gastric Cancer: Focus on Apoptosis, Inflammation, and Chemoresistance Abstract Abstract Natural products have emerged as promising multi-target agents for addressing the complex biology of gastric cancer, a malignancy characterized by marked molecular heterogeneity,... |
PMC11388056 | core_pubmed_pmc | A phase I drug–drug interaction study to assess the effect of futibatinib on P‐gp and BCRP substrates and of P‐gp inhibition on the pharmacokinetics of futibatinib | A phase I drug–drug interaction study to assess the effect of futibatinib on P‐gp and BCRP substrates and of P‐gp inhibition on the pharmacokinetics of futibatinib Abstract Abstract Futibatinib, an inhibitor of fibroblast growth factor receptor 1–4, is approved for the treatment of patients with advanced cholangiocarci... |
PMC8349538 | core_pubmed_pmc | What to Do About Missed Doses? A Retrospective Study of Olanzapine in the Elderly | What to Do About Missed Doses? A Retrospective Study of Olanzapine in the Elderly Abstract Abstract Background Schizophrenia is characterized by a high disease burden. Olanzapine is a common drug used in antipsychotic medication. Little is known about the population pharmacokinetics of olanzapine in elderly patients. M... |
PMC12619605 | core_pubmed_pmc | Population Pharmacokinetics of Tigecycline and Implications for Individualized Therapy Optimization: A Systematic Review | Population Pharmacokinetics of Tigecycline and Implications for Individualized Therapy Optimization: A Systematic Review Abstract Background Tigecycline, owing to its broad-spectrum antimicrobial activity, has emerged as an important option in the treatment of infections. However, its optimal dosing strategy remains co... |
PMC3939965 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacokinetic-Pharmacodynamic Relationships of Methadone in a Sample of Iranian (Mazandarani) Opiate Users Undergoing Methadone Maintenance Treatment | Population Pharmacokinetics and Pharmacokinetic-Pharmacodynamic Relationships of Methadone in a Sample of Iranian (Mazandarani) Opiate Users Undergoing Methadone Maintenance Treatment Abstract Abstract Objective: To investigate the pharmacokinetics (PK) and PK- pharmacodynamic (PD) relationship of methadone in a cohort... |
PMC10257984 | core_pubmed_pmc | Serotonin Syndrome: The Role of Pharmacology in Understanding Its Occurrence | Serotonin Syndrome: The Role of Pharmacology in Understanding Its Occurrence Abstract Serotonin syndrome (SS) is a potentially fatal adverse drug reaction characterized by an exaggerated increase in serotonergic activity in the central and peripheral nervous systems. It presents a constellation of signs and symptoms re... |
PMC7066225 | core_pubmed_pmc | Comparative pharmacokinetics of maxacalcitol in healthy Taiwanese and Japanese subjects | Comparative pharmacokinetics of maxacalcitol in healthy Taiwanese and Japanese subjects Abstract Abstract Pharmacokinetic studies of maxacalcitol in healthy Taiwanese subjects have been conducted. This study to compare the pharmacokinetic properties of maxacalcitol in healthy Taiwanese and Japanese subjects. Healthy ma... |
PMC10506774 | core_pubmed_pmc | First Pharmacokinetic Data of Tenofovir Alafenamide Fumarate and Tenofovir With Dolutegravir or Boosted Protease Inhibitors in African Children: A Substudy of the CHAPAS-4 Trial | First Pharmacokinetic Data of Tenofovir Alafenamide Fumarate and Tenofovir With Dolutegravir or Boosted Protease Inhibitors in African Children: A Substudy of the CHAPAS-4 Trial Abstract Abstract Background We evaluated the pharmacokinetics of tenofovir alafenamide fumarate (TAF) and tenofovir in a subset of African ch... |
PMC7803711 | core_pubmed_pmc | Serotonin syndrome by drug interactions with linezolid: clues from pharmacovigilance-pharmacokinetic/pharmacodynamic analysis | Serotonin syndrome by drug interactions with linezolid: clues from pharmacovigilance-pharmacokinetic/pharmacodynamic analysis Abstract Abstract Purpose To characterize the post-marketing reporting of serotonin syndrome (SS) due to drug-drug interactions (DDIs) with linezolid and investigate the relationship with pharma... |
PMC11489428 | core_pubmed_pmc | N-acetylcysteine in Kidney Disease: Molecular Mechanisms, Pharmacokinetics, and Clinical Effectiveness | N-acetylcysteine in Kidney Disease: Molecular Mechanisms, Pharmacokinetics, and Clinical Effectiveness Abstract Abstract N-acetylcysteine (NAC) has shown beneficial effects in both acute kidney disease and chronic kidney disease (CKD) in preclinical and clinical studies. Different dosage and administration forms of NAC... |
PMC9934922 | core_pubmed_pmc | Impact of polymorphisms in CYP and UGT enzymes and ABC and SLCO1B1 transporters on the pharmacokinetics and safety of desvenlafaxine | Impact of polymorphisms in CYP and UGT enzymes and ABC and SLCO1B1 transporters on the pharmacokinetics and safety of desvenlafaxine Abstract Venlafaxine pharmacokinetic variability and pharmacotherapy outcomes are well known to be related to CYP2D6 pharmacogenetic phenotype. In contrast, scarce pharmacogenetic informa... |
PMC12959138 | core_pubmed_pmc | Optimization strategies for voriconazole dosing in pediatric populations: integrating therapeutic indications and age-stratified pharmacokinetics | Optimization strategies for voriconazole dosing in pediatric populations: integrating therapeutic indications and age-stratified pharmacokinetics Abstract ABSTRACT There is limited evidence on the recommended voriconazole (VCZ) concentration ranges for prophylactic versus therapeutic use, and the factors influencing in... |
PMC11672802 | core_pubmed_pmc | Analysis of the Antibiotic-Potentiating Activity, Absorption, Distribution, Metabolism, and Excretion (ADME) and the Molecular Docking Properties of Phytol Against Multi-Drug-Resistant (MDR) Strains | Analysis of the Antibiotic-Potentiating Activity, Absorption, Distribution, Metabolism, and Excretion (ADME) and the Molecular Docking Properties of Phytol Against Multi-Drug-Resistant (MDR) Strains Abstract Background: Phytol is a diterpene from the long-chain unsaturated acyclic alcohols, known for its diverse biolog... |
PMC10559273 | core_pubmed_pmc | Tobramycin-loaded nanoparticles of thiolated chitosan for ocular drug delivery: Preparation, mucoadhesion and pharmacokinetic evaluation | Tobramycin-loaded nanoparticles of thiolated chitosan for ocular drug delivery: Preparation, mucoadhesion and pharmacokinetic evaluation Abstract The present work aimed to develop nanoparticles of tobramycin (TRM) using thiolated chitosan (TCS) in order to improve the mucoadhesion, antibacterial effect and pharmacokine... |
PMC5256391 | core_pubmed_pmc | Colonic microbiota can promote rapid local improvement of murine colitis by thioguanine independently of T lymphocytes and host metabolism | Colonic microbiota can promote rapid local improvement of murine colitis by thioguanine independently of T lymphocytes and host metabolism Abstract Abstract Objective Mercaptopurine (MP) and pro-drug azathioprine are ‘first-line’ oral therapies for maintaining remission in IBD. It is believed that their pharmacodynamic... |
PMC7734090 | core_pubmed_pmc | Vancomycin Prescribing Practices and Therapeutic Drug Monitoring for Critically Ill Neonatal and Pediatric Patients: A Survey of Physicians and Pharmacists in Hong Kong | Vancomycin Prescribing Practices and Therapeutic Drug Monitoring for Critically Ill Neonatal and Pediatric Patients: A Survey of Physicians and Pharmacists in Hong Kong Abstract Abstract Background: Deviations from the optimal vancomycin dosing may occur in the neonatal and pediatric population due to inconsistencies i... |
PMC11293501 | core_pubmed_pmc | Real-World Pharmacokinetics, Effectiveness, and Safety of Atezolizumab in Patients With Unresectable Advanced or Recurrent NSCLC: An Exploratory Study of J-TAIL | Real-World Pharmacokinetics, Effectiveness, and Safety of Atezolizumab in Patients With Unresectable Advanced or Recurrent NSCLC: An Exploratory Study of J-TAIL Abstract Abstract Introduction This study validated real-world pharmacokinetic (PK) data using an established population PK (PopPK) model for atezolizumab in J... |
PMC6572355 | core_pubmed_pmc | Danggui Buxue Decoction Sensitizes the Response of Non-Small-Cell Lung Cancer to Gemcitabine via Regulating Deoxycytidine Kinase and P-glycoprotein | Danggui Buxue Decoction Sensitizes the Response of Non-Small-Cell Lung Cancer to Gemcitabine via Regulating Deoxycytidine Kinase and P-glycoprotein Abstract Abstract This study aimed to investigate whether the anti-tumor effect of gemcitabine (GEM) in non-small-cell lung cancer (NSCLC) treatment was affected by Danggui... |
PMC9095771 | core_pubmed_pmc | Bioavailability and Safety of a New Highly Concentrated Midazolam Nasal Spray Compared to Buccal and Intravenous Midazolam Treatment in Chinese Healthy Volunteers | Bioavailability and Safety of a New Highly Concentrated Midazolam Nasal Spray Compared to Buccal and Intravenous Midazolam Treatment in Chinese Healthy Volunteers Abstract Abstract Introduction Buccal midazolam treatment is licensed in the European Union for prolonged acute convulsive seizures in children and adolescen... |
PMC6036088 | core_pubmed_pmc | Effects of Tranexamic Acid Based on its Population Pharmacokinetics in Pediatric Patients Undergoing Distraction Osteogenesis for Craniosynostosis: Rotational Thromboelastometry (ROTEM TM ) Analysis | Effects of Tranexamic Acid Based on its Population Pharmacokinetics in Pediatric Patients Undergoing Distraction Osteogenesis for Craniosynostosis: Rotational Thromboelastometry (ROTEM TM ) Analysis Abstract Abstract Background : Distraction osteogenesis for craniosynostosis is associated with significant hemorrhage. A... |
PMC7849189 | core_pubmed_pmc | Evaluation of Serum/Urine Genomic and Metabolomic Profiles to Improve the Adherence to Sildenafil Therapy in Patients with Erectile Dysfunction | Evaluation of Serum/Urine Genomic and Metabolomic Profiles to Improve the Adherence to Sildenafil Therapy in Patients with Erectile Dysfunction Abstract Type V-phosphodiesterase-inhibitors (PDE5i) are the first choice drugs in the treatment of erectile dysfunction (ED), being effective in 60–70% of patients. However, a... |
PMC10175065 | core_pubmed_pmc | Safety, Tolerability and Pharmacokinetics of Half-Life Extended Severe Acute Respiratory Syndrome Coronavirus 2 Neutralizing Monoclonal Antibodies AZD7442 (Tixagevimab-Cilgavimab) in Healthy Adults | Safety, Tolerability and Pharmacokinetics of Half-Life Extended Severe Acute Respiratory Syndrome Coronavirus 2 Neutralizing Monoclonal Antibodies AZD7442 (Tixagevimab-Cilgavimab) in Healthy Adults Abstract Abstract Background AZD7442 is a combination of extended half-life, severe acute respiratory syndrome coronavirus... |
PMC6342245 | core_pubmed_pmc | Relative Bioavailability of Orally Dispersible Tablet Formulations of Levo‐ and Racemic Praziquantel: Two Phase I Studies | Relative Bioavailability of Orally Dispersible Tablet Formulations of Levo‐ and Racemic Praziquantel: Two Phase I Studies Abstract Abstract Orally dispersible tablet (ODT) formulations of levo praziquantel (L‐PZQ) and racemic PZQ (rac‐PZQ) are being developed to treat schistosomiasis in preschool‐aged children. Two cro... |
PMC9319868 | core_pubmed_pmc | Synthesis, In Vitro Antiproliferative Activity, and In Silico Evaluation of Novel Oxiranyl-Quinoxaline Derivatives | Synthesis, In Vitro Antiproliferative Activity, and In Silico Evaluation of Novel Oxiranyl-Quinoxaline Derivatives Abstract Abstract The quinoxaline core is a promising scaffold in medicinal chemistry. Multiple quinoxaline derivatives, such as the topoisomerase IIβ inhibitor XK-469 and the tissue transglutaminase 2 inh... |
PMC5713701 | core_pubmed_pmc | The effect of medication nonadherence on progression-free survival among patients with renal cell carcinoma | The effect of medication nonadherence on progression-free survival among patients with renal cell carcinoma Abstract Objective To examine how observed medication nonadherence to 2 second-line, oral anticancer medications (axitinib and everolimus) affects progression-free survival (PFS) among patients with renal cell ca... |
PMC11687215 | core_pubmed_pmc | External evaluation of neonatal vancomycin population pharmacokinetic models: Moving from first‐order equations to Bayesian‐guided therapeutic monitoring | External evaluation of neonatal vancomycin population pharmacokinetic models: Moving from first‐order equations to Bayesian‐guided therapeutic monitoring Abstract Abstract Introduction Guidelines for vancomycin therapeutic monitoring recommend using a Bayesian approach with a population pharmacokinetic model to estimat... |
PMC5980133 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of the cytolytic anti‐CD38 human monoclonal antibody TAK‐079 in monkey – model assisted preparation for the first in human trial | Pharmacokinetics and pharmacodynamics of the cytolytic anti‐CD38 human monoclonal antibody TAK‐079 in monkey – model assisted preparation for the first in human trial Abstract Abstract We are studying the fully human, IgG1λ cytolytic monoclonal antibody TAK‐079, which binds CD38. CD38 is expressed on plasma and natural... |
PMC10649860 | core_pubmed_pmc | Tuning the Envelope Structure of Enzyme Nanoreactors for In Vivo Detoxification of Organophosphates | Tuning the Envelope Structure of Enzyme Nanoreactors for In Vivo Detoxification of Organophosphates Abstract Abstract Encapsulated phosphotriesterase nanoreactors show their efficacy in the prophylaxis and post-exposure treatment of poisoning by paraoxon. A new enzyme nanoreactor (E-nRs) containing an evolved multiple ... |
PMC9509244 | core_pubmed_pmc | Determination of Tropifexor in Beagle Dog Plasma by UPLC-MS/MS and Its Application in Pharmacokinetics | Determination of Tropifexor in Beagle Dog Plasma by UPLC-MS/MS and Its Application in Pharmacokinetics Abstract The primary objective of this study was to develop and validate an efficient and accurate ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) approach as a means to detect tropifexor... |
PMC9311711 | core_pubmed_pmc | Pharmacokinetics of Subcutaneous Dupilumab Injection With an Autoinjector Device or Prefilled Syringe | Pharmacokinetics of Subcutaneous Dupilumab Injection With an Autoinjector Device or Prefilled Syringe Abstract Abstract Dupilumab, a human monoclonal antibody against interleukin‐4 receptor alpha, has demonstrated efficacy and an acceptable safety profile in adult and pediatric patients with moderate‐to‐severe atopic d... |
PMC4543587 | core_pubmed_pmc | Plotting of Ethylene Glycol Blood Concentrations Using Linear Regression before and during Hemodialysis in a Case of Intoxication and Pharmacokinetic Review | Plotting of Ethylene Glycol Blood Concentrations Using Linear Regression before and during Hemodialysis in a Case of Intoxication and Pharmacokinetic Review Abstract Introduction . As blood concentration measurement of commonly abused alcohol is readily available, the equation was proposed in previous publication to pr... |
PMC7982400 | core_pubmed_pmc | Meta-Analysis of ABCG2 and ABCB1 Polymorphisms With Sunitinib-Induced Toxicity and Efficacy in Renal Cell Carcinoma | Meta-Analysis of ABCG2 and ABCB1 Polymorphisms With Sunitinib-Induced Toxicity and Efficacy in Renal Cell Carcinoma Abstract Abstract Background: ABCG2 and ABCB1 are genes related to the pharmacokinetics of sunitinib and have been associated with its toxicity and efficacy. However, the results have been controversial. ... |
PMC5571342 | core_pubmed_pmc | Bioavailability of Lumefantrine Is Significantly Enhanced with a Novel Formulation Approach, an Outcome from a Randomized, Open-Label Pharmacokinetic Study in Healthy Volunteers | Bioavailability of Lumefantrine Is Significantly Enhanced with a Novel Formulation Approach, an Outcome from a Randomized, Open-Label Pharmacokinetic Study in Healthy Volunteers Abstract ABSTRACT The artemether-lumefantrine combination requires food intake for the optimal absorption of lumefantrine. In an attempt to en... |
PMC12769267 | core_pubmed_pmc | An LC–MS/MS Method for the Quantitation of Metabolites M9, M12, and M20 of Bexicaserin in Human Cerebrospinal Fluid | An LC–MS/MS Method for the Quantitation of Metabolites M9, M12, and M20 of Bexicaserin in Human Cerebrospinal Fluid Abstract ABSTRACT The investigational molecule bexicaserin is a highly selective 5‐HT 2C superagonist currently in Phase 3 clinical studies for the treatment of seizures associated with developmental and ... |
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