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PMC12073189
core_pubmed_pmc
Synthesis and Evaluation of a Novel Zuranolone Analog with High GABA A Receptor PAM Activity and Excellent Pharmacokinetic Profiles
Synthesis and Evaluation of a Novel Zuranolone Analog with High GABA A Receptor PAM Activity and Excellent Pharmacokinetic Profiles Abstract Zuranolone (SAGE-217), the first FDA-approved oral neurosteroid (NAS), a positive allosteric modulator (PAM) of γ-aminobutyric acid type A (GABA A ) receptor for postpartum depres...
PMC10570684
core_pubmed_pmc
Axicabtagene Ciloleucel in Combination with the 4–1BB Agonist Utomilumab in Patients with Relapsed/Refractory Large B-Cell Lymphoma: Phase 1 Results from ZUMA-11
Axicabtagene Ciloleucel in Combination with the 4–1BB Agonist Utomilumab in Patients with Relapsed/Refractory Large B-Cell Lymphoma: Phase 1 Results from ZUMA-11 Abstract Abstract Purpose: Chimeric antigen receptor (CAR) T-cell therapies have shown clinical benefit for patients with relapsed/refractory (R/R) large B-ce...
PMC11304715
core_pubmed_pmc
Phase 1 study of the pharmacokinetics and clinical proof-of-concept activity of a biofilm-disrupting human monoclonal antibody in patients with chronic prosthetic joint infection of the knee or hip
Phase 1 study of the pharmacokinetics and clinical proof-of-concept activity of a biofilm-disrupting human monoclonal antibody in patients with chronic prosthetic joint infection of the knee or hip Abstract ABSTRACT We report the results of a first-in-human phase 1 clinical study to evaluate TRL1068, a native human mon...
PMC4148334
core_pubmed_pmc
Pharmacodynamic Effects of Canagliflozin, a Sodium Glucose Co-Transporter 2 Inhibitor, from a Randomized Study in Patients with Type 2 Diabetes
Pharmacodynamic Effects of Canagliflozin, a Sodium Glucose Co-Transporter 2 Inhibitor, from a Randomized Study in Patients with Type 2 Diabetes Abstract Introduction This randomized, double-blind, placebo-controlled, single and multiple ascending-dose study evaluated the pharmacodynamic effects and safety/tolerability ...
PMC7083422
core_pubmed_pmc
Quantifying breast milk intake by term and preterm infants for input into paediatric physiologically based pharmacokinetic models
Quantifying breast milk intake by term and preterm infants for input into paediatric physiologically based pharmacokinetic models Abstract Abstract Despite the many benefits of breast milk, mothers taking medication are often uncertain about the risks of drug exposure to their infants and decide not to breastfeed. Phys...
PMC3098207
core_pubmed_pmc
Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with malaria
Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with malaria Abstract Background The World Health Organization endorses the use of artemisinin-based combination therapy for treatment of acute uncomplicated falciparum malaria in the second and third trimesters of pregn...
PMC4745848
core_pubmed_pmc
Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation
Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation Abstract Abstract In this study, optimized freeze-dried finasteride nanoparticles (NPs) were prepared from drug nanosuspension formulation that was developed using the bottom–up technique. ...
PMC11524821
core_pubmed_pmc
Evaluation of the role of metabolizing enzymes and transporter variants in ezetimibe pharmacokinetics
Evaluation of the role of metabolizing enzymes and transporter variants in ezetimibe pharmacokinetics Abstract Introduction Ezetimibe inhibits cholesterol uptake by modulation of intestinal sterol absorption. Currently, although some studies have shown alterations in ezetimibe levels caused by alterations in the ABCG5 ...
PMC2950407
core_pubmed_pmc
In vivo biodistribution, anti-inflammatory, and hepatoprotective effects of liver targeting dexamethasone acetate loaded nanostructured lipid carrier system
In vivo biodistribution, anti-inflammatory, and hepatoprotective effects of liver targeting dexamethasone acetate loaded nanostructured lipid carrier system Abstract Abstract We aimed to evaluate whether the enhancement of the liver accumulation and anti-inflammatory activity of dexamethasone acetate (DXMA) could be ac...
PMC7811991
core_pubmed_pmc
Comparison of the Pharmacokinetics of RIPK1 Inhibitor GSK2982772 in Healthy Western and Japanese Subjects
Comparison of the Pharmacokinetics of RIPK1 Inhibitor GSK2982772 in Healthy Western and Japanese Subjects Abstract Abstract Background and Objectives GSK2982772 is an oral small-molecule RIPK1 inhibitor with potential therapeutic efficacy in immune-mediated inflammatory diseases (IMIDs). An inter-ethnic comparison of G...
PMC6956038
core_pubmed_pmc
Using Supercritical Fluid Technology as a Green Alternative During the Preparation of Drug Delivery Systems
Using Supercritical Fluid Technology as a Green Alternative During the Preparation of Drug Delivery Systems Abstract Micro- and nano-carrier formulations have been developed as drug delivery systems for active pharmaceutical ingredients (APIs) that suffer from poor physico-chemical, pharmacokinetic, and pharmacodynamic...
PMC12839390
core_pubmed_pmc
Advancing Drug–Drug Interaction Prediction with Biomimetic Improvements: Leveraging the Latest Artificial Intelligence Techniques to Guide Researchers in the Field
Advancing Drug–Drug Interaction Prediction with Biomimetic Improvements: Leveraging the Latest Artificial Intelligence Techniques to Guide Researchers in the Field Abstract Drug–drug interactions (DDIs) can cause adverse reactions or reduce the efficiency of a drug. Using computers to predict DDIs is now critical in ph...
PMC9877293
core_pubmed_pmc
Insights in the maturational processes influencing hydrocortisone pharmacokinetics in congenital adrenal hyperplasia patients using a middle-out approach
Insights in the maturational processes influencing hydrocortisone pharmacokinetics in congenital adrenal hyperplasia patients using a middle-out approach Abstract Abstract Introduction: Hydrocortisone is the standard of care in cortisol replacement therapy for congenital adrenal hyperplasia patients. Challenges in mimi...
PMC10287555
core_pubmed_pmc
Camonsertib in DNA damage response-deficient advanced solid tumors: phase 1 trial results
Camonsertib in DNA damage response-deficient advanced solid tumors: phase 1 trial results Abstract Predictive biomarkers of response are essential to effectively guide targeted cancer treatment. Ataxia telangiectasia and Rad3-related kinase inhibitors (ATRi) have been shown to be synthetic lethal with loss of function ...
PMC11891766
core_pubmed_pmc
Association of NR1I2 Polymorphism with Midazolam Clearance in Mechanically Ventilated ICU Patients: A Population Pharmacokinetic and Pharmacogenetic Study
Association of NR1I2 Polymorphism with Midazolam Clearance in Mechanically Ventilated ICU Patients: A Population Pharmacokinetic and Pharmacogenetic Study Abstract Background Significant variability in the metabolism of midazolam (MDZ) exists among mechanically ventilated (MV) patients in the intensive care unit (ICU) ...
PMC3121587
core_pubmed_pmc
Pharmacokinetics study of bio-adhesive tablet of Panax notoginseng saponins
Pharmacokinetics study of bio-adhesive tablet of Panax notoginseng saponins Abstract Abstract Panax notoginseng saponin (PNS) is the main active gradient of Chinese traditional medicine Panax notoginseng. Although its prominent therapeutic efficacy has been demonstrated by various researchers, the broader application i...
PMC10648942
core_pubmed_pmc
Safety and pharmacokinetics of SPR206 in subjects with varying degrees of renal impairment
Safety and pharmacokinetics of SPR206 in subjects with varying degrees of renal impairment Abstract ABSTRACT SPR206 is a novel polymyxin derivative with potent in vitro activity against susceptible and multidrug-resistant strains of Acinetobacter baumannii , Pseudomonas aeruginosa , Klebsiella pneumoniae , Escherichia ...
PMC11769232
core_pubmed_pmc
Voriconazole Pharmacokinetics Administered at 4 mg/kg IM and IV in Nursehound Sharks ( Scyliorhinus stellaris ) Under Human Care
Voriconazole Pharmacokinetics Administered at 4 mg/kg IM and IV in Nursehound Sharks ( Scyliorhinus stellaris ) Under Human Care Abstract Simple Summary Sharks and rays are a vital part of the collections of many aquariums around the world. The study of these species kept under human care has revealed a number of healt...
PMC7034029
core_pubmed_pmc
Highly loaded deoxypodophyllotoxin nano-formulation delivered by methoxy polyethylene glycol-block-poly (D,L-lactide) micelles for efficient cancer therapy
Highly loaded deoxypodophyllotoxin nano-formulation delivered by methoxy polyethylene glycol-block-poly (D,L-lactide) micelles for efficient cancer therapy Abstract Abstract Cancer is a kind of malignant diseases that threatens human health and the research application of anti-tumor drug therapeutics is growingly alway...
PMC8524144
core_pubmed_pmc
The combined effect of permeation enhancement and proteolysis inhibition on the systemic exposure of orally administrated peptides: Salcaprozate sodium, soybean trypsin inhibitor, and teriparatide study in pigs
The combined effect of permeation enhancement and proteolysis inhibition on the systemic exposure of orally administrated peptides: Salcaprozate sodium, soybean trypsin inhibitor, and teriparatide study in pigs Abstract Abstract Oral delivery of peptides and proteins is hindered by their rapid proteolysis in the gastro...
PMC8912117
core_pubmed_pmc
Identification of Molecular Fragments in Equilibrium with Polysiloxane Ultrasmall Nanoparticles
Identification of Molecular Fragments in Equilibrium with Polysiloxane Ultrasmall Nanoparticles Abstract During recent decades, ultrasmall inorganic nanoparticles have attracted considerable interest due to their favorable biodistribution, pharmacokinetics and theranostic properties. In particular, AGuIX nanoparticles ...
PMC8899820
core_pubmed_pmc
Pharmacokinetics, Tissue Distribution, and Excretion Characteristics of a Radix Polygoni Multiflori Extract in Rats
Pharmacokinetics, Tissue Distribution, and Excretion Characteristics of a Radix Polygoni Multiflori Extract in Rats Abstract Abstract Although progress has been achieved in the pharmacological activity and toxicity of Radix Polygoni Multiflori (RPM), the chemical basis of its toxicity is still unclear. Here, we perform...
PMC12511228
core_pubmed_pmc
Comparative pharmacokinetics and bioequivalence of 145-mg fenofibrate formulations in healthy Korean participants
Comparative pharmacokinetics and bioequivalence of 145-mg fenofibrate formulations in healthy Korean participants Abstract Fenofibrate is a serum lipid-modifying agent that is commonly used to treat dyslipidemia. This study aimed to compare the pharmacokinetics (PKs) and establish bioequivalence of two 145-mg fenofibra...
PMC11904221
core_pubmed_pmc
Repression of apelin Furin cleavage sites provides antimetastatic strategy in colorectal cancer
Repression of apelin Furin cleavage sites provides antimetastatic strategy in colorectal cancer Abstract Abstract The adipokine apelin has been directly implicated in various physiological processes during embryogenesis and human cancers. Nevertheless, the importance of the conversion of its precursor proapelin to matu...
PMC11535701
core_pubmed_pmc
Safety and efficacy of apixaban versus warfarin in peritoneal dialysis patients with non-valvular atrial fibrillation: protocol for a prospective, randomised, open-label, blinded endpoint trial (APIDP2)
Safety and efficacy of apixaban versus warfarin in peritoneal dialysis patients with non-valvular atrial fibrillation: protocol for a prospective, randomised, open-label, blinded endpoint trial (APIDP2) Abstract Abstract Introduction Several randomised controlled trials have demonstrated that novel oral anticoagulants ...
PMC12736231
core_pubmed_pmc
Pharmacokinetic Evaluation of GB-5001, a Long-Acting Injectable Formulation of Donepezil, in Healthy Korean Participants: Population Pharmacokinetics with Phase 1 Study
Pharmacokinetic Evaluation of GB-5001, a Long-Acting Injectable Formulation of Donepezil, in Healthy Korean Participants: Population Pharmacokinetics with Phase 1 Study Abstract Abstract Background/Objectives : Oral donepezil, an acetylcholinesterase (AChE) inhibitor for Alzheimer’s disease, faces adherence challenges....
PMC11762590
core_pubmed_pmc
A Pooled Pharmacokinetic Analysis for Piperacillin/Tazobactam Across Different Patient Populations: From Premature Infants to the Elderly
A Pooled Pharmacokinetic Analysis for Piperacillin/Tazobactam Across Different Patient Populations: From Premature Infants to the Elderly Abstract Abstract Background and Objectives The pharmacokinetics (PK) of piperacillin/tazobactam (PIP/TAZ) is highly variable across different patient populations and there are contr...
PMC6500101
core_pubmed_pmc
Desmopressin treatment combined with clotting factor VIII concentrates in patients with non-severe haemophilia A: protocol for a multicentre single-armed trial, the DAVID study
Desmopressin treatment combined with clotting factor VIII concentrates in patients with non-severe haemophilia A: protocol for a multicentre single-armed trial, the DAVID study Abstract Introduction Haemophilia A is an inherited bleeding disorder characterised by factor VIII (FVIII) deficiency. In patients with non-sev...
PMC11076820
core_pubmed_pmc
Pharmacokinetics study of ginsenoside Rg1 liposome by pulmonary administration
Pharmacokinetics study of ginsenoside Rg1 liposome by pulmonary administration Abstract Ginsenoside Rg1 (Rg1), a monomer saponin component, is one of the components with the highest content in total saponins of Panaxnotoginseng. It had various pharmacological effects. The bioavailability of oral tablets is only 1–20 %,...
PMC11249239
core_pubmed_pmc
Dual-targeting class I HDAC inhibitor and ATM activator, SP-1-303, preferentially inhibits estrogen receptor positive breast cancer cell growth
Dual-targeting class I HDAC inhibitor and ATM activator, SP-1-303, preferentially inhibits estrogen receptor positive breast cancer cell growth Abstract Abstract Dual-targeting chromatin regulation and DNA damage repair signaling presents a promising avenue for cancer therapy. Applying rational drug design, we synthesi...
PMC10980136
core_pubmed_pmc
Translational modeling-based evidence for enhanced efficacy of standard-of-care drugs in combination with anti-microRNA-155 in non-small-cell lung cancer
Translational modeling-based evidence for enhanced efficacy of standard-of-care drugs in combination with anti-microRNA-155 in non-small-cell lung cancer Abstract Abstract Elevated microRNA-155 (miR-155) expression in non-small-cell lung cancer (NSCLC) promotes cisplatin resistance and negatively impacts treatment outc...
PMC12521058
core_pubmed_pmc
PBPK Modeling to Predict Clinical Drug–Drug Interaction and Impact of Hepatic Impairment for an ADC With the Payload Auristatin F‐Hydroxypropylamide
PBPK Modeling to Predict Clinical Drug–Drug Interaction and Impact of Hepatic Impairment for an ADC With the Payload Auristatin F‐Hydroxypropylamide Abstract ABSTRACT Upifitamab rilsodotin—an antibody drug conjugate (ADC)—comprises a NaPi2b‐targeted antibody conjugated to an auristatin‐based payload (auristatin F‐hydro...
PMC7367551
core_pubmed_pmc
Phase I Escalation and Expansion Study of Bemarituzumab (FPA144) in Patients With Advanced Solid Tumors and FGFR2b-Selected Gastroesophageal Adenocarcinoma
Phase I Escalation and Expansion Study of Bemarituzumab (FPA144) in Patients With Advanced Solid Tumors and FGFR2b-Selected Gastroesophageal Adenocarcinoma Abstract Abstract PURPOSE To evaluate the safety, pharmacokinetics, and preliminary activity of bemarituzumab in patients with FGFR2b-overexpressing gastric and gas...
PMC2850393
core_pubmed_pmc
Design, recruitment, and retention of African-American smokers in a pharmacokinetic study
Design, recruitment, and retention of African-American smokers in a pharmacokinetic study Abstract Background African-Americans remain underrepresented in clinical research despite experiencing a higher burden of disease compared to all other ethnic groups in the United States. The purpose of this article is to describ...
PMC6325987
core_pubmed_pmc
Pharmacokinetic–Pharmacodynamic Modeling in Pediatric Drug Development, and the Importance of Standardized Scaling of Clearance
Pharmacokinetic–Pharmacodynamic Modeling in Pediatric Drug Development, and the Importance of Standardized Scaling of Clearance Abstract Abstract Pharmacokinetic/pharmacodynamic (PKPD) modeling is important in the design and conduct of clinical pharmacology research in children. During drug development, PKPD modeling a...
PMC10239737
core_pubmed_pmc
Potential herb–drug interactions between anti-COVID-19 drugs and traditional Chinese medicine
Potential herb–drug interactions between anti-COVID-19 drugs and traditional Chinese medicine Abstract Coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has spread worldwide. Effective treatments against COVID-19 remain urgently in need although vaccination sig...
PMC9577026
core_pubmed_pmc
Pharmacokinetic data in pregnancy: A review of available literature data and important considerations in collecting clinical data
Pharmacokinetic data in pregnancy: A review of available literature data and important considerations in collecting clinical data Abstract Pregnancy-related physiological changes can alter the absorption, distribution, metabolism and excretion of medicines which may affect the safety and efficacy of the medicines admin...
PMC11881557
core_pubmed_pmc
Model-informed dose optimization for prophylactic piperacillin-tazobactam in perioperative pediatric critically ill patients
Model-informed dose optimization for prophylactic piperacillin-tazobactam in perioperative pediatric critically ill patients Abstract ABSTRACT Piperacillin/tazobactam (PTZ) is frequently prescribed during the perioperative period as prophylaxis in critically ill patients. Current international guidelines recommend that...
PMC5096768
core_pubmed_pmc
Sedation with a remifentanil infusion to facilitate rapid awakening and tracheal extubation in an infant with a potentially compromised airway
Sedation with a remifentanil infusion to facilitate rapid awakening and tracheal extubation in an infant with a potentially compromised airway Abstract Abstract Sedation is generally required during endotracheal intubation and mechanical ventilation in infants and children. While there are many options for the provisio...
PMC3468079
core_pubmed_pmc
A new solid oral tablet formulation of posaconazole: a randomized clinical trial to investigate rising single- and multiple-dose pharmacokinetics and safety in healthy volunteers
A new solid oral tablet formulation of posaconazole: a randomized clinical trial to investigate rising single- and multiple-dose pharmacokinetics and safety in healthy volunteers Abstract Objectives Posaconazole is an extended-spectrum triazole with proven efficacy as antifungal treatment and prophylaxis. The marketed ...
PMC10232258
core_pubmed_pmc
Population pharmacokinetic modelling to characterize the effect of chronic kidney disease on tenofovir exposure after tenofovir alafenamide administration
Population pharmacokinetic modelling to characterize the effect of chronic kidney disease on tenofovir exposure after tenofovir alafenamide administration Abstract Abstract Background Tenofovir alafenamide is gradually replacing tenofovir disoproxil fumarate, both prodrugs of tenofovir, in HIV prevention and treatment....
PMC7698783
core_pubmed_pmc
Performance of Population Pharmacokinetic Models in Predicting Polymyxin B Exposures
Performance of Population Pharmacokinetic Models in Predicting Polymyxin B Exposures Abstract Abstract Polymyxin B is the last line of defense in treating multidrug-resistant gram-negative bacterial infections. Dosing of polymyxin B is currently based on total body weight, and a substantial intersubject variability has...
PMC10499415
core_pubmed_pmc
A phase I, open‐label, single‐dose study to evaluate the effect of hepatic impairment on the pharmacokinetics and safety of futibatinib
A phase I, open‐label, single‐dose study to evaluate the effect of hepatic impairment on the pharmacokinetics and safety of futibatinib Abstract Abstract Futibatinib is a covalently binding FGFR1–4 inhibitor that received US Food and Drug Administration approval for the treatment of patients with previously treated, ad...
PMC4574831
core_pubmed_pmc
Octreotide s.c. depot provides sustained octreotide bioavailability and similar IGF‐1 suppression to octreotide LAR in healthy volunteers
Octreotide s.c. depot provides sustained octreotide bioavailability and similar IGF‐1 suppression to octreotide LAR in healthy volunteers Abstract Abstract Aims The aim was to assess the pharmacokinetics, pharmacodynamics, safety and tolerability of octreotide subcutaneous (s.c.) depot, a novel octreotide formulation. ...
PMC2963932
core_pubmed_pmc
Pharmacokinetic parameters and tissue distribution of magnetic Fe 3 O 4 nanoparticles in mice
Pharmacokinetic parameters and tissue distribution of magnetic Fe 3 O 4 nanoparticles in mice Abstract Background This study explored the pharmacokinetic parameters and tissue distribution of magnetic iron oxide nanoparticles (Fe 3 O 4 MNPs) in imprinting control region (ICR) mice. Methods The Fe 3 O 4 MNPs were synthe...
PMC6394541
core_pubmed_pmc
Development of a nonlinear hierarchical model to describe the disposition of deuterium in mother–infant pairs to assess exclusive breastfeeding practice
Development of a nonlinear hierarchical model to describe the disposition of deuterium in mother–infant pairs to assess exclusive breastfeeding practice Abstract Abstract The World Health Organization recommends exclusive breastfeeding (EBF) for the first 6 months after birth. The deuterium oxide dose-to-the-mother (DT...
PMC10910614
core_pubmed_pmc
Effects of meal type on the bioavailability of vutiglabridin, a novel anti‐obesity agent, in healthy subjects
Effects of meal type on the bioavailability of vutiglabridin, a novel anti‐obesity agent, in healthy subjects Abstract Abstract Vutiglabridin, which affects the pharmacokinetics (PKs) of food, is currently under clinical development for the treatment of obesity. This study aimed to evaluate the effects of low‐ and high...
PMC7125476
core_pubmed_pmc
Intraocular Pharmacokinetics and Safety of Subretinal Injection Compared with Intravitreal Application of Conbercept in Vitrectomized Rabbit Eyes
Intraocular Pharmacokinetics and Safety of Subretinal Injection Compared with Intravitreal Application of Conbercept in Vitrectomized Rabbit Eyes Abstract Purpose To evaluate the ocular pharmacokinetic properties of subretinal conbercept injection in vitrectomized rabbit eyes and to compare them with those by intravitr...
PMC12433203
core_pubmed_pmc
Establishment and Validation of a UPLC-MS/MS Method for Quantitative Determination of Zanubrutinib and Posaconazole in Rat Plasma: Application in Drug–Drug Interaction Studies
Establishment and Validation of a UPLC-MS/MS Method for Quantitative Determination of Zanubrutinib and Posaconazole in Rat Plasma: Application in Drug–Drug Interaction Studies Abstract Abstract Purpose Zanubrutinib, a second-generation Bruton’s tyrosine kinase (BTK) inhibitor, has been demonstrated to treat multiple B-...
PMC8829446
core_pubmed_pmc
Changes in CYP3A4 Enzyme Expression and Biochemical Markers Under Acute Hypoxia Affect the Pharmacokinetics of Sildenafil
Changes in CYP3A4 Enzyme Expression and Biochemical Markers Under Acute Hypoxia Affect the Pharmacokinetics of Sildenafil Abstract Abstract To investigate the effects of pathological, physiological, biochemical and metabolic enzymes CYP3A4 on the pharmacokinetics of sildenafil under acute hypoxia, rats were randomly di...
PMC12655500
core_pubmed_pmc
Controlled Release Technologies for Diltiazem Hydrochloride: A Comprehensive Review of Solid Dosage Innovations
Controlled Release Technologies for Diltiazem Hydrochloride: A Comprehensive Review of Solid Dosage Innovations Abstract Introduction : Diltiazem hydrochloride (DH) is a calcium channel blocker used in the treatment of hypertension, angina pectoris, and arrhythmias. Its short half-life and frequent dosing requirements ...
PMC10191434
core_pubmed_pmc
High-precision monitoring of and feedback control over drug concentrations in the brains of freely moving rats
High-precision monitoring of and feedback control over drug concentrations in the brains of freely moving rats Abstract Abstract Knowledge of drug concentrations in the brains of behaving subjects remains constrained on a number of dimensions, including poor temporal resolution and lack of real-time data. Here, however...
PMC11877031
core_pubmed_pmc
Clonazepam repurposing in ARID1B patients through conventional RCT and N-of-1 trials: an experimental strategy for orphan disease development
Clonazepam repurposing in ARID1B patients through conventional RCT and N-of-1 trials: an experimental strategy for orphan disease development Abstract ABSTRACT Background Clinical trials for rare disorders have unique challenges due to low prevalence, patient phenotype variability and high expectations. These challenge...
PMC6373397
core_pubmed_pmc
Lanadelumab for the Prophylactic Treatment of Hereditary Angioedema with C1 Inhibitor Deficiency: A Review of Preclinical and Phase I Studies
Lanadelumab for the Prophylactic Treatment of Hereditary Angioedema with C1 Inhibitor Deficiency: A Review of Preclinical and Phase I Studies Abstract Abstract Hereditary angioedema (HAE) with C1 esterase inhibitor (C1-INH) deficiency (C1-INH-HAE) is a rare disease characterized by diminished levels or dysfunctional ac...
PMC8465302
core_pubmed_pmc
Phytosomes as an Emerging Nanotechnology Platform for the Topical Delivery of Bioactive Phytochemicals
Phytosomes as an Emerging Nanotechnology Platform for the Topical Delivery of Bioactive Phytochemicals Abstract Abstract The emergence of phytosome nanotechnology has a potential impact in the field of drug delivery and could revolutionize the current state of topical bioactive phytochemicals delivery. The main challen...
PMC10188071
core_pubmed_pmc
Pharmacokinetics of tenvermectin in swine, a novel antiparasitic drug candidate—comparison with ivermectin
Pharmacokinetics of tenvermectin in swine, a novel antiparasitic drug candidate—comparison with ivermectin Abstract Abstract Tenvermectin (TVM) is a novel 16‐membered macrolide compound isolated and purified from the fermentation broth of genetically engineered Streptomyces avermitilis strain MHJ1011 . TVM and ivermect...
PMC6055900
core_pubmed_pmc
A Phase I, open-label, randomized, crossover study in healthy subjects to evaluate the bioavailability of, and the food effect on, a pomalidomide oral liquid suspension
A Phase I, open-label, randomized, crossover study in healthy subjects to evaluate the bioavailability of, and the food effect on, a pomalidomide oral liquid suspension Abstract Abstract Objective The aim of this study was to evaluate the bioavailability of a pomalidomide oral liquid suspension relative to the commerci...
PMC9091740
core_pubmed_pmc
Absolute bioavailability, dose proportionality, and tissue distribution of rotundic acid in rats based on validated LC-QqQ-MS/MS method
Absolute bioavailability, dose proportionality, and tissue distribution of rotundic acid in rats based on validated LC-QqQ-MS/MS method Abstract Abstract Rotundic acid (RA), an ursane-type pentacyclic triterpene acid isolated from the dried barks of Ilex rotunda Thunb. (Aquifoliaceae), possesses diverse bioactivities. ...
PMC11967443
core_pubmed_pmc
Evaluating the Lidocaine's Initial Dosing in Patients With Ventricular Arrhythmias and Heart Failure Admitted in Intensive Care Units
Evaluating the Lidocaine's Initial Dosing in Patients With Ventricular Arrhythmias and Heart Failure Admitted in Intensive Care Units Abstract ABSTRACT Introduction Lidocaine is an antiarrhythmic with narrow therapeutic window indicated for refractory ventricular arrhythmia. Limited guidance is available regarding the ...
PMC9698744
core_pubmed_pmc
Rhizophora mucronata Lam. (Mangrove) Bark Extract Reduces Ethanol-Induced Liver Cell Death and Oxidative Stress in Swiss Albino Mice: In Vivo and In Silico Studies
Rhizophora mucronata Lam. (Mangrove) Bark Extract Reduces Ethanol-Induced Liver Cell Death and Oxidative Stress in Swiss Albino Mice: In Vivo and In Silico Studies Abstract The bark extract of Rhizophora mucronata (BERM) was recently reported for its prominent in vitro protective effects against liver cell line toxicit...
PMC10582071
core_pubmed_pmc
Green UPLC method for estimation of ciprofloxacin, diclofenac sodium, and ibuprofen with application to pharmacokinetic study of human samples
Green UPLC method for estimation of ciprofloxacin, diclofenac sodium, and ibuprofen with application to pharmacokinetic study of human samples Abstract Investigation of a unique and fast method for the determination and separation of a mixture of three drugs viz ., ciprofloxacin (CIP), Ibuprofen (IBU), and diclofenac s...
PMC6500982
core_pubmed_pmc
Phase I study of tirabrutinib ( ONO ‐4059/ GS ‐4059) in patients with relapsed or refractory B‐cell malignancies in Japan
Phase I study of tirabrutinib ( ONO ‐4059/ GS ‐4059) in patients with relapsed or refractory B‐cell malignancies in Japan Abstract We evaluated the safety, efficacy, pharmacokinetics, pharmacodynamics and predictive biomarkers of tirabrutinib, a second‐generation, enhanced‐selectivity Bruton's tyrosine kinase inhibitor...
PMC11998891
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GLP‐1RA‐induced delays in gastrointestinal motility: Predicted effects on coadministered drug absorption by PBPK analysis
GLP‐1RA‐induced delays in gastrointestinal motility: Predicted effects on coadministered drug absorption by PBPK analysis Abstract Abstract Background Glucagon‐like peptide‐1 receptor agonists (GLP‐1RAs) are breakthrough medicines for obesity treatment and have rapidly gained widespread clinical application. Although G...
PMC10920180
core_pubmed_pmc
Long-term outcomes of patients with large B-cell lymphoma treated with axicabtagene ciloleucel and prophylactic corticosteroids
Long-term outcomes of patients with large B-cell lymphoma treated with axicabtagene ciloleucel and prophylactic corticosteroids Abstract ZUMA-1 safety management cohort 6 investigated the impact of prophylactic corticosteroids and earlier corticosteroids and/or tocilizumab on the incidence and severity of cytokine rele...
PMC7056460
core_pubmed_pmc
Clinical relevance of St. John's wort drug interactions revisited
Clinical relevance of St. John's wort drug interactions revisited Abstract Abstract The first clinically relevant reports of preparations of St. John's wort (SJW), a herbal medicine with anti‐depressant effects, interacting with other drugs, altering their bioavailability and efficacy, were published about 20 years ago...
PMC9314180
core_pubmed_pmc
Clinical Pharmacist Intervention on Drug-Related Problems among Elderly Patients Admitted to Medical Wards of Northwest Ethiopia Comprehensive Specialized Hospitals: A Multicenter Prospective, Observational Study
Clinical Pharmacist Intervention on Drug-Related Problems among Elderly Patients Admitted to Medical Wards of Northwest Ethiopia Comprehensive Specialized Hospitals: A Multicenter Prospective, Observational Study Abstract Background: Drug therapy in the elderly needs an emphasis on age-related changes in drug pharmacok...
PMC7150795
core_pubmed_pmc
Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics
Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics Abstract In this paper, as an active ingredient, puerarin chitosan nanoparticles (Pur-CS/TPP-NPs) are prepared by an ionic gelation method. The chitosan (CS) concentration, pH of the CS solution, sodium tripolyphosphat...
PMC8093142
core_pubmed_pmc
Population Pharmacokinetics of CC-122
Population Pharmacokinetics of CC-122 Abstract Abstract Background CC-122 is a cereblon-modulating agent that exerts direct cell-autonomous activity against malignant B cells and immunomodulatory effects. Herein, a population pharmacokinetic (popPK) model of CC-122 was developed and the influence of demographic and dis...
PMC10960205
core_pubmed_pmc
A Deep Learning–Based Approach for Prediction of Vancomycin Treatment Monitoring: Retrospective Study Among Patients With Critical Illness
A Deep Learning–Based Approach for Prediction of Vancomycin Treatment Monitoring: Retrospective Study Among Patients With Critical Illness Abstract Abstract Background Vancomycin pharmacokinetics are highly variable in patients with critical illnesses, and clinicians commonly use population pharmacokinetic (PPK) models...
PMC7055509
core_pubmed_pmc
Use of imaging to assess the activity of hepatic transporters
Use of imaging to assess the activity of hepatic transporters Abstract ABSTRACT Introduction : Membrane transporters of the SLC and ABC families are abundantly expressed in the liver, where they control the transfer of drugs/drug metabolites across the sinusoidal and canalicular hepatocyte membranes and play a pivotal ...
PMC8444931
core_pubmed_pmc
Phase I study in healthy participants to evaluate safety, tolerability, and pharmacokinetics of inhaled nezulcitinib, a potential treatment for COVID‐19
Phase I study in healthy participants to evaluate safety, tolerability, and pharmacokinetics of inhaled nezulcitinib, a potential treatment for COVID‐19 Abstract Abstract Nezulcitinib (TD‐0903), a lung‐selective pan–Janus‐associated kinase (JAK) inhibitor designed for inhaled delivery, is under development for treatmen...
PMC9969732
core_pubmed_pmc
Impact of the Recent Clinical and Laboratory Standards Institute Breakpoint Changes on the Antimicrobial Spectrum of Aminoglycosides and the Activity of Plazomicin Against Multidrug-Resistant and Carbapenem-Resistant Enterobacterales From United States Medical Centers
Impact of the Recent Clinical and Laboratory Standards Institute Breakpoint Changes on the Antimicrobial Spectrum of Aminoglycosides and the Activity of Plazomicin Against Multidrug-Resistant and Carbapenem-Resistant Enterobacterales From United States Medical Centers Abstract Abstract Background The Clinical and Labor...
PMC6488550
core_pubmed_pmc
Towards Improved Pharmacokinetic Models for the Analysis of Transporter-Mediated Hepatic Disposition of Drug Molecules with Positron Emission Tomography
Towards Improved Pharmacokinetic Models for the Analysis of Transporter-Mediated Hepatic Disposition of Drug Molecules with Positron Emission Tomography Abstract Positron emission tomography (PET) imaging with radiolabeled drugs holds great promise to assess the influence of membrane transporters on hepatobiliary clear...
PMC3441149
core_pubmed_pmc
Lung cancer and diesel exhaust: an updated critical review of the occupational epidemiology literature
Lung cancer and diesel exhaust: an updated critical review of the occupational epidemiology literature Abstract A recent review concluded that the evidence from epidemiology studies was indeterminate and that additional studies were required to support the diesel exhaust-lung cancer hypothesis. This updated review incl...
PMC4462344
core_pubmed_pmc
Phase-1 study of abiraterone acetate in chemotherapy-naïve Japanese patients with castration-resistant prostate cancer
Phase-1 study of abiraterone acetate in chemotherapy-naïve Japanese patients with castration-resistant prostate cancer Abstract Persistent androgen synthesis under castration status in adrenal gland, testes and tumor cells is thought to be one of the major causes of development and progression of castration-resistant p...
PMC9614201
core_pubmed_pmc
In vivo biodistribution and pharmacokinetics of sotrovimab, a SARS-CoV-2 monoclonal antibody, in healthy cynomolgus monkeys
In vivo biodistribution and pharmacokinetics of sotrovimab, a SARS-CoV-2 monoclonal antibody, in healthy cynomolgus monkeys Abstract Purpose Sotrovimab (VIR-7831), a human IgG1κ monoclonal antibody (mAb), binds to a conserved epitope on the SARS-CoV-2 spike protein receptor binding domain (RBD). The Fc region of VIR-78...
PMC4335258
core_pubmed_pmc
Systems pharmacology approaches for optimization of antiangiogenic therapies: challenges and opportunities
Systems pharmacology approaches for optimization of antiangiogenic therapies: challenges and opportunities Abstract Abstract Targeted therapies have become an important therapeutic paradigm for multiple malignancies. The rapid development of resistance to these therapies impedes the successful management of advanced ca...
PMC4700759
core_pubmed_pmc
Pharmacokinetics of mefloquine and its effect on sulfamethoxazole and trimethoprim steady-state blood levels in intermittent preventive treatment (IPTp) of pregnant HIV-infected women in Kenya
Pharmacokinetics of mefloquine and its effect on sulfamethoxazole and trimethoprim steady-state blood levels in intermittent preventive treatment (IPTp) of pregnant HIV-infected women in Kenya Abstract Abstract Background Intermittent preventive treatment in pregnancy with sulfadoxine/pyrimethamine is contra-indicated ...
PMC8389327
core_pubmed_pmc
Targeting Pro-Oxidant Iron with Deferoxamine as a Treatment for Ischemic Stroke: Safety and Optimal Dose Selection in a Randomized Clinical Trial
Targeting Pro-Oxidant Iron with Deferoxamine as a Treatment for Ischemic Stroke: Safety and Optimal Dose Selection in a Randomized Clinical Trial Abstract Abstract A role of iron as a target to prevent stroke-induced neurodegeneration has been recently revisited due to new evidence showing that ferroptosis inhibitors a...
PMC7904806
core_pubmed_pmc
A phase I dose-finding, pharmacokinetics and genotyping study of olaparib and lurbinectedin in patients with advanced solid tumors
A phase I dose-finding, pharmacokinetics and genotyping study of olaparib and lurbinectedin in patients with advanced solid tumors Abstract The poly (ADP-Ribose) polymerase (PARP) inhibitor olaparib has shown antitumor activity in patients with ovarian or breast cancer with or without BRCA1/2 mutations. Lurbinectedin i...
PMC7235665
core_pubmed_pmc
Safety and efficacy of extended release ketamine tablets in patients with treatment-resistant depression and anxiety: open label pilot study
Safety and efficacy of extended release ketamine tablets in patients with treatment-resistant depression and anxiety: open label pilot study Abstract Abstract Background: Ketamine’s defining side effects are dissociation and increased blood pressure/heart rate. An oral formulation with delayed absorption could minimize...
PMC8864116
core_pubmed_pmc
Effectiveness of Antiviral Therapy in Highly-Transmissible Variants of SARS-CoV-2: A Modeling and Simulation Study
Effectiveness of Antiviral Therapy in Highly-Transmissible Variants of SARS-CoV-2: A Modeling and Simulation Study Abstract As of October 2021, neither established agents (e.g., hydroxychloroquine) nor experimental drugs have lived up to their initial promise as antiviral treatment against SARS-CoV-2 infection. While v...
PMC6796726
core_pubmed_pmc
Studying Interactions between 2’-O-Me-Modified Inhibitors and MicroRNAs Utilizing Microscale Thermophoresis
Studying Interactions between 2’-O-Me-Modified Inhibitors and MicroRNAs Utilizing Microscale Thermophoresis Abstract Abstract Besides the acquisition of pharmacokinetic parameters of antisense oligonucleotide microRNA (miRNA) inhibitors, such as measuring in vivo concentration, their pharmacodynamic characteristics are...
PMC7002685
core_pubmed_pmc
Inhibition of vascular calcification by inositol phosphates derivatized with ethylene glycol oligomers
Inhibition of vascular calcification by inositol phosphates derivatized with ethylene glycol oligomers Abstract Myo -inositol hexakisphosphate (IP6) is a natural product known to inhibit vascular calcification (VC), but with limited potency and low plasma exposure following bolus administration. Here we report the desi...
PMC9779081
core_pubmed_pmc
A Predictive Pharmacokinetic Model for Immune Cell-Mediated Uptake and Retention of Nanoparticles in Tumors
A Predictive Pharmacokinetic Model for Immune Cell-Mediated Uptake and Retention of Nanoparticles in Tumors Abstract A promise of cancer nanomedicine is the “targeted” delivery of therapeutic agents to tumors by the rational design of nanostructured materials. During the past several decades, a realization that in vitr...
PMC11485916
core_pubmed_pmc
GB18-06, a nanobody targeting GDF15, effectively alleviates weight loss and restores physical function in cachexia models
GB18-06, a nanobody targeting GDF15, effectively alleviates weight loss and restores physical function in cachexia models Abstract ABSTRACT Cachexia is a complicated metabolic syndrome mainly associated with cancers, characterized by extreme weight loss and muscle wasting. It is a debilitating condition that negatively...
PMC11424460
core_pubmed_pmc
Inhibitory effects of calcium channel blockers nisoldipine and nimodipine on ivacaftor metabolism and their underlying mechanism
Inhibitory effects of calcium channel blockers nisoldipine and nimodipine on ivacaftor metabolism and their underlying mechanism Abstract Abstract Ivacaftor is the first potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) protein approved for use alone in the treatment of cystic fibrosis (CF)....
PMC6950211
core_pubmed_pmc
The Pharmacokinetics of Fucoidan after Topical Application to Rats
The Pharmacokinetics of Fucoidan after Topical Application to Rats Abstract Fucoidan, a fucose-rich polysaccharide from brown algae, has been used for transdermal formulations targeting inflammatory skin conditions, for the treatment of thrombosis, vascular permeability diseases, subcutaneous wounds, and burns. However...
PMC4180634
core_pubmed_pmc
Pharmacokinetic Study and Bioavailability of a Novel Synthetic Trioxane Antimalarial Compound 97/63 in Rats
Pharmacokinetic Study and Bioavailability of a Novel Synthetic Trioxane Antimalarial Compound 97/63 in Rats Abstract Abstract Single dose pharmacokinetics study of 97/63 (IND191710, 2004), a trioxane antimalarial developed by Central Drug Research Institute, Lucknow, India, was studied in rats following intravenous and...
PMC3416900
core_pubmed_pmc
Vitreous pharmacokinetics and electroretinographic findings after intravitreal injection of acyclovir in rabbits
Vitreous pharmacokinetics and electroretinographic findings after intravitreal injection of acyclovir in rabbits Abstract Abstract OBJECTIVES: Acute retinal necrosis is a rapidly progressive and devastating viral retinitis caused by the herpesvirus family. Systemic acyclovir is the treatment of choice; however, the pro...
PMC5397649
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Evaluation of Marbofloxacin in Pig against Korean Local Isolates of Actinobacillus pleuropneumoniae
Pharmacokinetic and Pharmacodynamic Evaluation of Marbofloxacin in Pig against Korean Local Isolates of Actinobacillus pleuropneumoniae Abstract The pharmacokinetics of marbofloxacin in pigs after intravenous (i.v.), intramuscular (i.m.), and peroral (p.o.) administration and pharmacokinetic/pharmacodynamic indices of ...
PMC12929201
core_pubmed_pmc
Maternal and Pediatric Precision in Therapeutic Knowledge Portal ( MPRINT ‐ KP ): Landscape Analysis of Pharmacology Research in Maternal and Pediatric Patient Populations
Maternal and Pediatric Precision in Therapeutic Knowledge Portal ( MPRINT ‐ KP ): Landscape Analysis of Pharmacology Research in Maternal and Pediatric Patient Populations Abstract ABSTRACT Pregnant women and children have been underrepresented in clinical studies due to ethical concerns and perceived vulnerabilities. ...
PMC5784568
core_pubmed_pmc
Immunogenicity of biologics in inflammatory bowel disease
Immunogenicity of biologics in inflammatory bowel disease Abstract Abstract Crohn’s disease and ulcerative colitis are chronic inflammatory disorders of the gastrointestinal tract. Treatment options include biologic therapies; however, a proportion of patients lose response to biologics, partly due to the formation of ...
PMC8962057
core_pubmed_pmc
Views, knowledge, and practices of hospital pharmacists about using clinical pharmacokinetics to optimize pharmaceutical care services: a cross-sectional study
Views, knowledge, and practices of hospital pharmacists about using clinical pharmacokinetics to optimize pharmaceutical care services: a cross-sectional study Abstract Abstract Background Pharmacokinetics (PK) is often used to optimize individualized dosing regimens of some drugs. This study was conducted to determine...
PMC8840528
core_pubmed_pmc
Monthly Increase in Vitamin D Levels upon Supplementation with 2000 IU/Day in Healthy Volunteers: Result from “Integriamoci”, a Pilot Pharmacokinetic Study
Monthly Increase in Vitamin D Levels upon Supplementation with 2000 IU/Day in Healthy Volunteers: Result from “Integriamoci”, a Pilot Pharmacokinetic Study Abstract Abstract Vitamin D (VD) is a calcium- and phosphate-controlling hormone used to treat bone disorders; yet, several other effects are progressively emerging...
PMC7993319
core_pubmed_pmc
Pharmacoenhancement of Low Crizotinib Plasma Concentrations in Patients with Anaplastic Lymphoma Kinase‐Positive Non‐Small Cell Lung Cancer using the CYP3A Inhibitor Cobicistat
Pharmacoenhancement of Low Crizotinib Plasma Concentrations in Patients with Anaplastic Lymphoma Kinase‐Positive Non‐Small Cell Lung Cancer using the CYP3A Inhibitor Cobicistat Abstract Abstract The inhibitor of anaplastic lymphoma kinase (ALK) crizotinib significantly increases survival in patients with ALK‐positive n...
PMC3627029
core_pubmed_pmc
Pharmacokinetics and Excretion of 14 C-Bendamustine in Patients with Relapsed or Refractory Malignancy
Pharmacokinetics and Excretion of 14 C-Bendamustine in Patients with Relapsed or Refractory Malignancy Abstract Abstract Background Bendamustine is an alkylating agent with clinical activity against a variety of hematologic malignancies and solid tumors. To assess the roles of renal and hepatic drug elimination pathway...
PMC8156202
core_pubmed_pmc
Descriptors of Cytochrome Inhibitors and Useful Machine Learning Based Methods for the Design of Safer Drugs
Descriptors of Cytochrome Inhibitors and Useful Machine Learning Based Methods for the Design of Safer Drugs Abstract Roughly 2.8% of annual hospitalizations are a result of adverse drug interactions in the United States, representing more than 245,000 hospitalizations. Drug–drug interactions commonly arise from major ...
PMC11317924
core_pubmed_pmc
Interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young woman
Interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young woman Abstract Abstract Aim The overdose of caffeine, a cytochrome P450 1A2 probe, in young women has become a problem. The aim of this study was to evaluate possible drug interactions between intentionally overdosed ca...
PMC10018922
core_pubmed_pmc
Gut microbiota mediated the individualized efficacy of Temozolomide via immunomodulation in glioma
Gut microbiota mediated the individualized efficacy of Temozolomide via immunomodulation in glioma Abstract Background Temozolomide (TMZ) is the preferred chemotherapy strategy for glioma therapy. As a second-generation alkylating agent, TMZ provides superior oral bio-availability. However, limited response rate (less ...