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PMC4285945
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of levofloxacin injection in healthy Chinese volunteers and dosing regimen optimization
Pharmacokinetics and pharmacodynamics of levofloxacin injection in healthy Chinese volunteers and dosing regimen optimization Abstract Abstract What is known and objective The pharmacokinetics (PK) and pharmacodynamics (PD) of levofloxacin were investigated following administration of levofloxacin injection in healthy ...
PMC10035072
core_pubmed_pmc
Therapeutic drug monitoring guided dosing versus standard dosing of alectinib in advanced ALK positive non-small cell lung cancer patients: Study protocol for an international, multicenter phase IV randomized controlled trial (ADAPT ALEC)
Therapeutic drug monitoring guided dosing versus standard dosing of alectinib in advanced ALK positive non-small cell lung cancer patients: Study protocol for an international, multicenter phase IV randomized controlled trial (ADAPT ALEC) Abstract Abstract Background Alectinib is first-line therapy in patients with sta...
PMC8940791
core_pubmed_pmc
Exposure-response modeling improves selection of radiation and radiosensitizer combinations
Exposure-response modeling improves selection of radiation and radiosensitizer combinations Abstract A central question in drug discovery is how to select drug candidates from a large number of available compounds. This analysis presents a model-based approach for comparing and ranking combinations of radiation and rad...
PMC8495142
core_pubmed_pmc
Development of an UPLC-MS/MS Method for the Quantitative Analysis of Upadacitinib in Beagle Dog Plasma and Pharmacokinetics Study
Development of an UPLC-MS/MS Method for the Quantitative Analysis of Upadacitinib in Beagle Dog Plasma and Pharmacokinetics Study Abstract Background Upadacitinib, a novel selective Janus kinase 1 (JAK1) inhibitor, has been recently approved by the US FDA for the treatment of adult patients with moderately to severely ...
PMC10761359
core_pubmed_pmc
Chemo-informatics applications in the design of novel 7-keto-sempervirol derivatives as SmCB1 inhibitors with potential for treatment of Schistosomiasis
Chemo-informatics applications in the design of novel 7-keto-sempervirol derivatives as SmCB1 inhibitors with potential for treatment of Schistosomiasis Abstract The quest for a sound treatment on the vulnerable population suffering and dying as a result of the blood flukes, S. mansoni is on the increase because both P...
PMC4605839
core_pubmed_pmc
Single and Multiple Dose Pharmacokinetics, Pharmacodynamics and Safety of the Novel Lipoprotein-Associated Phospholipase A 2 Enzyme Inhibitor Darapladib in Healthy Chinese Subjects: An Open Label Phase-1 Clinical Trial
Single and Multiple Dose Pharmacokinetics, Pharmacodynamics and Safety of the Novel Lipoprotein-Associated Phospholipase A 2 Enzyme Inhibitor Darapladib in Healthy Chinese Subjects: An Open Label Phase-1 Clinical Trial Abstract Abstract Background and Objectives Darapladib is a lipoprotein-associated phospholipase A 2 ...
PMC9802358
core_pubmed_pmc
Maintenance Golimumab Treatment in Pediatric UC Patients With Moderately to Severely Active UC: PURSUIT PEDS PK Long-Term Study Results
Maintenance Golimumab Treatment in Pediatric UC Patients With Moderately to Severely Active UC: PURSUIT PEDS PK Long-Term Study Results Abstract Abstract Background Long-term safety, pharmacokinetics, and efficacy of open-label golimumab therapy in children with moderate–severe ulcerative colitis were evaluated. Method...
PMC5760783
core_pubmed_pmc
LC-MS determination and pharmacokinetic study of salidroside in rat plasma after oral administration of suspensions of traditional Chinese medicine Erzhi Wan and Fructus Ligustri lucidi
LC-MS determination and pharmacokinetic study of salidroside in rat plasma after oral administration of suspensions of traditional Chinese medicine Erzhi Wan and Fructus Ligustri lucidi Abstract Abstract A simple, rapid and sensitive liquid chromatography-mass spectrometry (LC-MS) method was developed for the determina...
PMC5904241
core_pubmed_pmc
Higher Midazolam Clearance in Obese Adolescents Compared with Morbidly Obese Adults
Higher Midazolam Clearance in Obese Adolescents Compared with Morbidly Obese Adults Abstract Abstract Background The clearance of cytochrome P450 (CYP) 3A substrates is reported to be reduced with lower age, inflammation and obesity. As it is unknown what the overall influence is of these factors in the case of obese a...
PMC9290557
core_pubmed_pmc
Temporal dynamics of intranasal oxytocin in human brain electrophysiology
Temporal dynamics of intranasal oxytocin in human brain electrophysiology Abstract Abstract Oxytocin (OT) is a key modulator of human social cognition, popular in behavioral neuroscience. To adequately design and interpret intranasal OT (IN-OT) research, it is crucial to know for how long it affects human brain functio...
PMC10040594
core_pubmed_pmc
Dose adjustment not required for contezolid in patients with moderate hepatic impairment based on pharmacokinetic/pharmacodynamic analysis
Dose adjustment not required for contezolid in patients with moderate hepatic impairment based on pharmacokinetic/pharmacodynamic analysis Abstract Objective: Contezolid is an oxazolidinone antimicrobial agent newly approved for treatment of Gram-positive bacterial infections. It is primarily metabolized by the liver. ...
PMC6929516
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics Estimation of Eculizumab in a 2-Year-Old Girl With Atypical Hemolytic Uremic Syndrome: A Case Report With 4-Year Follow-Up
Pharmacokinetics and Pharmacodynamics Estimation of Eculizumab in a 2-Year-Old Girl With Atypical Hemolytic Uremic Syndrome: A Case Report With 4-Year Follow-Up Abstract Abstract Background: Eculizumab has dramatically changed poor outcomes of complement-mediated atypical hemolytic uremic syndrome (aHUS) as first-line ...
PMC4404619
core_pubmed_pmc
A multicenter study on the effect of continuous hemodiafiltration intensity on antibiotic pharmacokinetics
A multicenter study on the effect of continuous hemodiafiltration intensity on antibiotic pharmacokinetics Abstract Introduction Continuous renal replacement therapy (CRRT) may alter antibiotic pharmacokinetics and increase the risk of incorrect dosing. In a nested cohort within a large randomized controlled trial, we ...
PMC9607806
core_pubmed_pmc
COVID-19 drugs: potential interaction with ATP-binding cassette transporters P-glycoprotein and breast cancer resistance protein
COVID-19 drugs: potential interaction with ATP-binding cassette transporters P-glycoprotein and breast cancer resistance protein Abstract Background The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome coronavirus 2, has resulted in acute respiratory distress, fatal systemic man...
PMC11602949
core_pubmed_pmc
Establishing the capacity to monitor proteins relevant to the study of drug exposure and response using liver‐derived extracellular vesicles
Establishing the capacity to monitor proteins relevant to the study of drug exposure and response using liver‐derived extracellular vesicles Abstract Aims Drug exposure and response is determined by pharmacokinetic (PK) and pharmacodynamic (PD) profiles. Interindividual differences in abundance of drug metabolizing enz...
PMC12598135
core_pubmed_pmc
Predicting OCT2/MATEs‐Mediated Drug Interactions in Healthy Volunteers and Patients with Chronic Kidney Disease: Insights from Extended Clearance Concept, Endogenous Biomarkers, and In Vitro Inhibition Studies (Perspectives from the International Transporter Consortium)
Predicting OCT2/MATEs‐Mediated Drug Interactions in Healthy Volunteers and Patients with Chronic Kidney Disease: Insights from Extended Clearance Concept, Endogenous Biomarkers, and In Vitro Inhibition Studies (Perspectives from the International Transporter Consortium) Abstract Abstract Organic cation transporter (OCT...
PMC4388670
core_pubmed_pmc
Sex Differences in Liver Toxicity—Do Female and Male Human Primary Hepatocytes React Differently to Toxicants In Vitro ?
Sex Differences in Liver Toxicity—Do Female and Male Human Primary Hepatocytes React Differently to Toxicants In Vitro ? Abstract There is increasing amount of evidence for sex variation in drug efficiency and toxicity profiles. Women are more susceptible than men to acute liver injury from xenobiotics. In general, thi...
PMC10400434
core_pubmed_pmc
Oral prednisolone suppresses skin inflammation in a healthy volunteer imiquimod challenge model
Oral prednisolone suppresses skin inflammation in a healthy volunteer imiquimod challenge model Abstract Imiquimod (IMQ) is a topical agent that induces local inflammation via the Toll-like receptor 7 pathway. Recently, an IMQ-driven skin inflammation model was developed in healthy volunteers for proof-of-pharmacology ...
PMC10009879
core_pubmed_pmc
α-Glucosidase inhibitory activities of flavonoid derivatives isolated from Bouea macrophylla : in vitro and in silico studies †
α-Glucosidase inhibitory activities of flavonoid derivatives isolated from Bouea macrophylla : in vitro and in silico studies † Abstract In continuation of our search for bioactive compounds from the Bouea macrophylla ( B. macrophylla ) plant, we describe herein eight flavonoid-type compounds including mearsetin (1), m...
PMC11580248
core_pubmed_pmc
Phase I dose escalation study of IO-108, an anti-LILRB2 antibody, in patients with advanced solid tumors
Phase I dose escalation study of IO-108, an anti-LILRB2 antibody, in patients with advanced solid tumors Abstract Abstract Purpose In this first-in-human dose escalation study, the safety and efficacy of IO-108, a fully human monoclonal antibody targeting leukocyte immunoglobulin-like receptor B2 (LILRB2), was investig...
PMC6001687
core_pubmed_pmc
Phase 1 studies to assess the safety, tolerability and pharmacokinetics of JTE‐052 (a novel Janus kinase inhibitor) ointment in Japanese healthy volunteers and patients with atopic dermatitis
Phase 1 studies to assess the safety, tolerability and pharmacokinetics of JTE‐052 (a novel Janus kinase inhibitor) ointment in Japanese healthy volunteers and patients with atopic dermatitis Abstract Abstract The purpose of the present two phase 1 studies was to assess the safety, tolerability and pharmacokinetics for...
PMC9369335
core_pubmed_pmc
Tailoring the Structure of Cell Penetrating DNA and RNA Binding Nucleopeptides
Tailoring the Structure of Cell Penetrating DNA and RNA Binding Nucleopeptides Abstract Synthetic nucleic acid interactors represent an exciting research field due to their biotechnological and potential therapeutic applications. The translation of these molecules into drugs is a long and difficult process that justifi...
PMC5312436
core_pubmed_pmc
Chemotherapy for primary mediastinal yolk sac tumor in a patient undergoing chronic hemodialysis: a case report
Chemotherapy for primary mediastinal yolk sac tumor in a patient undergoing chronic hemodialysis: a case report Abstract Abstract Background The safety and efficacy of chemotherapy for patients undergoing concomitant hemodialysis have not been fully established and optimal doses of anti-cancer drugs and best timing of ...
PMC9227873
core_pubmed_pmc
Establishment of Level a In Vitro–In Vivo Correlation (IVIVC) via Extended DoE-IVIVC Model: A Donepezil Case Study
Establishment of Level a In Vitro–In Vivo Correlation (IVIVC) via Extended DoE-IVIVC Model: A Donepezil Case Study Abstract Abstract This study aimed to establish an extended design of experiment (DoE)-in vitro in vivo correlation (IVIVC) model that defines the relationship between formulation composition, in vitro dis...
PMC7727629
core_pubmed_pmc
Bariatric Surgery can Lower the Efficacy of DOACs
Bariatric Surgery can Lower the Efficacy of DOACs Abstract A 39-year-old woman who was taking the contraceptive pill was admitted with right leg deep venous thrombosis (DVT). She was started on apixaban tablets, but after 8 days developed proximal progression of the DVT and pulmonary embolism. Her medical history later...
PMC10764261
core_pubmed_pmc
Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsions
Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsions Abstract This study aimed to prepare an o/w mitiglinide microemulsion (MTGME) to improve the drug solubility and bioavailability. The formulation of o/w MTGME was optimized by the solubility study of drug, pseudo-ternary phase diagram an...
PMC10787197
core_pubmed_pmc
Integrating machine learning with pharmacokinetic models: Benefits of scientific machine learning in adding neural networks components to existing PK models
Integrating machine learning with pharmacokinetic models: Benefits of scientific machine learning in adding neural networks components to existing PK models Abstract Abstract Recently, the use of machine‐learning (ML) models for pharmacokinetic (PK) modeling has grown significantly. Although most of the current approac...
PMC10368248
core_pubmed_pmc
A Phase-I pharmacokinetic, safety and food-effect study on flubentylosin, a novel analog of Tylosin-A having potent anti- Wolbachia and antifilarial activity
A Phase-I pharmacokinetic, safety and food-effect study on flubentylosin, a novel analog of Tylosin-A having potent anti- Wolbachia and antifilarial activity Abstract Background The parasitic filariae responsible for onchocerciasis and lymphatic filariasis are host to an endosymbiotic bacterium, Wolbachia , which is es...
PMC8901485
core_pubmed_pmc
Qualitative Analysis of Drug-Containing Plasma and its Application to Quantitative Analysis and Pharmacokinetic Study of Zexie Decoction Using UPLC-MS/MS
Qualitative Analysis of Drug-Containing Plasma and its Application to Quantitative Analysis and Pharmacokinetic Study of Zexie Decoction Using UPLC-MS/MS Abstract ZeXie Decoction (ZXD) is one of the traditional Chinese medicine formulas (TCMFs) comprising Alisma orientalis (Sam.) Juzep. (ZX) and Atractylodes macrocepha...
PMC12539612
core_pubmed_pmc
Pharmacokinetics of Double‐Layer Patches With Microneedles Containing Procyclidine and Rivastigmine in Guinea Pigs
Pharmacokinetics of Double‐Layer Patches With Microneedles Containing Procyclidine and Rivastigmine in Guinea Pigs Abstract ABSTRACT Reversible cholinesterase inhibitors have been investigated to address prophylactic and therapeutic outcomes against organophosphorus nerve poisoning, and procyclidine is concomitantly us...
PMC5209422
core_pubmed_pmc
Pharmacokinetic Drug–Drug Interactions Between Vonoprazan and Low-Dose Aspirin or Nonsteroidal Anti-inflammatory Drugs: A Phase 2, Open-Label, Study in Healthy Japanese Men
Pharmacokinetic Drug–Drug Interactions Between Vonoprazan and Low-Dose Aspirin or Nonsteroidal Anti-inflammatory Drugs: A Phase 2, Open-Label, Study in Healthy Japanese Men Abstract Abstract Background Gastroprotective agents are recommended for patients receiving low-dose aspirin (LDA) or nonsteroidal anti-inflammator...
PMC11157048
core_pubmed_pmc
The influence of drug-induced metabolic enzyme activity inhibition and CYP3A4 gene polymorphism on aumolertinib metabolism
The influence of drug-induced metabolic enzyme activity inhibition and CYP3A4 gene polymorphism on aumolertinib metabolism Abstract The purpose of this study is to clarify the drug interaction profile of aumolertinib, and the influence of CYP3A4 genetic polymorphism on aumolertinib metabolic characteristics. Through mi...
PMC9545189
core_pubmed_pmc
Innovative approaches and recent advances in the study of ontogeny of drug metabolism and transport
Innovative approaches and recent advances in the study of ontogeny of drug metabolism and transport Abstract The disposition of a drug is driven by various processes, such as drug metabolism, drug transport, glomerular filtration and body composition. These processes are subject to developmental changes reflecting grow...
PMC5025135
core_pubmed_pmc
Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial
Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial Abstract Introduction Rupatadine is a marketed second generation antihistamine, with anti-PAF activity, indicated for symptomatic treatment of allergic rhinitis and ...
PMC6482279
core_pubmed_pmc
A Retrospective Evaluation of Allometry, Population Pharmacokinetics, and Physiologically‐Based Pharmacokinetics for Pediatric Dosing Using Clearance as a Surrogate
A Retrospective Evaluation of Allometry, Population Pharmacokinetics, and Physiologically‐Based Pharmacokinetics for Pediatric Dosing Using Clearance as a Surrogate Abstract Abstract Physiologically‐based pharmacokinetic models are increasingly applied for pediatric dose selection along with traditional methods such as...
PMC11534120
core_pubmed_pmc
Preclinical and phase I studies of an antisense oligonucleotide drug targeting IGF-1R in liver cancer
Preclinical and phase I studies of an antisense oligonucleotide drug targeting IGF-1R in liver cancer Abstract Abstract Aim: To evaluate a novel antisense oligonucleotide drug targeting human IGF-1R in preclinical and phase I studies of liver cancer. Materials & methods: The tolerability and safety of an investigationa...
PMC11186846
core_pubmed_pmc
Safety, pharmacokinetics, pharmacodynamics, and antitumor activity of SAR439459, a TGFβ inhibitor, as monotherapy and in combination with cemiplimab in patients with advanced solid tumors: Findings from a phase 1/1b study
Safety, pharmacokinetics, pharmacodynamics, and antitumor activity of SAR439459, a TGFβ inhibitor, as monotherapy and in combination with cemiplimab in patients with advanced solid tumors: Findings from a phase 1/1b study Abstract Abstract SAR439459 (SAR'459), a “second‐generation” human anti‐transforming growth factor...
PMC5915609
core_pubmed_pmc
Prediction of the Pharmacokinetics of Pravastatin as an OATP Substrate Using Plateable Human Hepatocytes With Human Plasma Data and PBPK Modeling
Prediction of the Pharmacokinetics of Pravastatin as an OATP Substrate Using Plateable Human Hepatocytes With Human Plasma Data and PBPK Modeling Abstract Abstract Plateable human hepatocytes with human plasma were utilized to generate the uptake transporter kinetic data for pravastatin, an organic anion‐transporting p...
PMC11865562
core_pubmed_pmc
Molecular mechanism of type ib MET inhibitors and their potential for CNS tumors
Molecular mechanism of type ib MET inhibitors and their potential for CNS tumors Abstract Abstract The emergence of targeted therapies for MET exon 14 (METex14) skipping mutations has significantly changed the treatment landscape for NSCLC and other solid tumors. The skipping of METex14 results in activating the MET-HG...
PMC4426553
core_pubmed_pmc
Modern insulins, old paradigms and pragmatism: choosing wisely when deciding how to treat type 1 diabetes
Modern insulins, old paradigms and pragmatism: choosing wisely when deciding how to treat type 1 diabetes Abstract There is a clinical imperative to improve metabolic control in the treatment of patients with type 1 diabetes, but in doing so, hypoglycemia should be avoided at all costs. Insulin analogues and the assump...
PMC8699120
core_pubmed_pmc
Population Pharmacokinetic Model-Based Evaluation of Intact Oxaliplatin in Rats with Acute Kidney Injury
Population Pharmacokinetic Model-Based Evaluation of Intact Oxaliplatin in Rats with Acute Kidney Injury Abstract Simple Summary Acute kidney injury (AKI) complicates the dose setting of oxaliplatin (L-OHP), making it difficult to continue treatment cycles and retain antitumor efficacies with minimum L-OHP-related toxi...
PMC8614892
core_pubmed_pmc
A Strategy for Hospital Pharmacists to Control Antimicrobial Resistance (AMR) in Japan
A Strategy for Hospital Pharmacists to Control Antimicrobial Resistance (AMR) in Japan Abstract In Japan, there is concern regarding the relation between the inappropriate use of antibiotics and antibiotic resistance (AMR). Increased bacterial resistance is due in part to the inappropriate use of antimicrobial agents. ...
PMC8780429
core_pubmed_pmc
Quantitative Analysis of the Phase Transition Mechanism Underpinning the Systemic Self-Assembly of a Mechanopharmaceutical Device
Quantitative Analysis of the Phase Transition Mechanism Underpinning the Systemic Self-Assembly of a Mechanopharmaceutical Device Abstract Abstract Clofazimine (CFZ) is a poorly soluble, weakly basic, small molecule antibiotic clinically used to treat leprosy and is now in clinical trials as a treatment for multidrug r...
PMC9810488
core_pubmed_pmc
Common ABCB1 SNP, C3435T could affect systemic exposure of dapagliflozin in healthy subject
Common ABCB1 SNP, C3435T could affect systemic exposure of dapagliflozin in healthy subject Abstract P-glycoprotein (P-gp) is a transporter that plays an excretory role in epithelial cells. It is encoded by ABCB1 , and single nucleotide polymorphisms (SNPs) in this gene can affect systemic drug exposure. Dapagliflozin ...
PMC5170674
core_pubmed_pmc
A Phase I study evaluating the effect of age and weight on the pharmacokinetics of an injectable formulation of diclofenac solubilized with hydroxypropyl-β-cyclodextrin
A Phase I study evaluating the effect of age and weight on the pharmacokinetics of an injectable formulation of diclofenac solubilized with hydroxypropyl-β-cyclodextrin Abstract Abstract Purpose The analgesic and opioid-sparing effects of nonsteroidal anti-inflammatory drugs can be beneficial in postoperative populatio...
PMC11860030
core_pubmed_pmc
Impact of Genetic Variants on Pregabalin Pharmacokinetics and Safety
Impact of Genetic Variants on Pregabalin Pharmacokinetics and Safety Abstract Abstract Background/Objectives: Pregabalin is a useful therapeutic option for patients with anxiety or neuropathic pain. Genetic variants in certain genes encoding for transporters related to absorption and distribution could have an impact o...
PMC9218571
core_pubmed_pmc
Exploring the Scientific Rationality of the Phenomenon of “Different Dosage Forms of the Same Prescription” of Chinese Proprietary Medicine Based on Biopharmaceutical Properties of Powder and Pill of Chuanxiong Chatiao Prescription
Exploring the Scientific Rationality of the Phenomenon of “Different Dosage Forms of the Same Prescription” of Chinese Proprietary Medicine Based on Biopharmaceutical Properties of Powder and Pill of Chuanxiong Chatiao Prescription Abstract Abstract Background: The 2020 edition of the Pharmacopoeia of the People’s Repu...
PMC12531128
core_pubmed_pmc
Reduced Metformin Concentrations in Obese Women With Human Immunodeficiency Virus Treated With Dolutegravir
Reduced Metformin Concentrations in Obese Women With Human Immunodeficiency Virus Treated With Dolutegravir Abstract Background. Obesity among women with human immunodeficiency virus (WWH) is nearly 2-fold higher than in men. Obesity is closely associated with dysglycemia, and frequently necessitates the coadministrati...
PMC10658092
core_pubmed_pmc
Administration of lipid emulsion reduced the hypnotic potency of propofol more than that of thiamylal in mice
Administration of lipid emulsion reduced the hypnotic potency of propofol more than that of thiamylal in mice Abstract Abstract Administration in a lipid emulsion can modify the pharmacodynamics of drugs via a process known as lipid resuscitation. However, the detailed mechanism remains unclear. We studied the volume a...
PMC3299201
core_pubmed_pmc
Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery
Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery Abstract Purpose The main objective of this study was to develop a novel aerosolized liposome formulation for pulmonary delivery of anti-asthmatic medication and to explore the relationship between the bioavailability and anti-...
PMC8994032
core_pubmed_pmc
Pharmacokinetic Studies in Elasmobranchs: Meloxicam Administered at 0.5 mg/kg Using Intravenous, Intramuscular, and Oral Routes to Nursehound Sharks ( Scyliorhinus stellaris )
Pharmacokinetic Studies in Elasmobranchs: Meloxicam Administered at 0.5 mg/kg Using Intravenous, Intramuscular, and Oral Routes to Nursehound Sharks ( Scyliorhinus stellaris ) Abstract Abstract Infectious and inflammatory diseases are the most frequently diagnosed pathologies in elasmobranchs maintained under human car...
PMC7696487
core_pubmed_pmc
Antioxidant Activities of a New Chemotype of Piper cubeba L. Fruit Essential Oil (Methyleugenol/Eugenol): In Silico Molecular Docking and ADMET Studies
Antioxidant Activities of a New Chemotype of Piper cubeba L. Fruit Essential Oil (Methyleugenol/Eugenol): In Silico Molecular Docking and ADMET Studies Abstract Abstract Piper cubeba L. fruit is an important species used in folk medicine for different types of pains such as rheumatism, chills, flu, colds, muscular ache...
PMC10675291
core_pubmed_pmc
Etoricoxib Coated Tablets: Bioequivalence Assessment between Two Formulations Administered under Fasting Conditions
Etoricoxib Coated Tablets: Bioequivalence Assessment between Two Formulations Administered under Fasting Conditions Abstract Etoricoxib is a non-steroidal anti-inflammatory drug with high selectivity for cyclooxygenase 2 (COX-2), exerting a pronounced anti-inflammatory effect with fewer adverse events when compared to ...
PMC9774561
core_pubmed_pmc
Pharmacokinetic of Cefiderocol in Critically Ill Patients Receiving Renal Replacement Therapy: A Case Series
Pharmacokinetic of Cefiderocol in Critically Ill Patients Receiving Renal Replacement Therapy: A Case Series Abstract Background: Cefiderocol is a novel parenteral siderophore cephalosporin, demonstrating enhanced activity against multidrug-resistant (MDR) Gram-negative bacteria and difficult-to-treat Acinetobacter bau...
PMC10794461
core_pubmed_pmc
The natural breakthrough: phytochemicals as potent therapeutic agents against spinocerebellar ataxia type 3
The natural breakthrough: phytochemicals as potent therapeutic agents against spinocerebellar ataxia type 3 Abstract There is no FDA-approved drug for neurological disorders like spinocerebellar ataxia type 3. CAG repeats mutation in the ATXN3 gene, causing spinocerebellar ataxia type 3 disease. Symptoms include sleep ...
PMC9228797
core_pubmed_pmc
Enalapril and Enalaprilat Pharmacokinetics in Children with Heart Failure Due to Dilated Cardiomyopathy and Congestive Heart Failure after Administration of an Orodispersible Enalapril Minitablet (LENA-Studies)
Enalapril and Enalaprilat Pharmacokinetics in Children with Heart Failure Due to Dilated Cardiomyopathy and Congestive Heart Failure after Administration of an Orodispersible Enalapril Minitablet (LENA-Studies) Abstract Abstract Angiotensin-converting enzyme inhibitors (ACEI), such as enalapril, are a cornerstone of tr...
PMC8959600
core_pubmed_pmc
The repurposing of Tebipenem pivoxil as alternative therapy for severe gastrointestinal infections caused by extensively drug-resistant Shigella spp
The repurposing of Tebipenem pivoxil as alternative therapy for severe gastrointestinal infections caused by extensively drug-resistant Shigella spp Abstract Background: Diarrhoea remains one of the leading causes of childhood mortality globally. Recent epidemiological studies conducted in low-middle income countries (...
PMC8834031
core_pubmed_pmc
Modeled Early Longitudinal PSA Kinetics Prognostic Value in Rising PSA Prostate Cancer Patients after Local Therapy Treated with ADT +/− Docetaxel
Modeled Early Longitudinal PSA Kinetics Prognostic Value in Rising PSA Prostate Cancer Patients after Local Therapy Treated with ADT +/− Docetaxel Abstract Abstract Simple Summary In prostate cancer patients with rising prostate-specific antigens (PSAs) after primary local therapy, and at high risk of metastatic diseas...
PMC4961080
core_pubmed_pmc
Towards a Best Practice Approach in PBPK Modeling: Case Example of Developing a Unified Efavirenz Model Accounting for Induction of CYPs 3A4 and 2B6
Towards a Best Practice Approach in PBPK Modeling: Case Example of Developing a Unified Efavirenz Model Accounting for Induction of CYPs 3A4 and 2B6 Abstract Abstract In this study, we present efavirenz physiologically based pharmacokinetic (PBPK) model development as an example of our best practice approach that uses ...
PMC12664141
core_pubmed_pmc
Opioid overdose associated with concomitant use of hydrocodone and selective serotonin reuptake inhibitors
Opioid overdose associated with concomitant use of hydrocodone and selective serotonin reuptake inhibitors Abstract Background Selective serotonin reuptake inhibitors (SSRIs) are frequently co-prescribed with opioids, increasing the risk of pharmacokinetic and pharmacodynamic interactions. Hydrocodone, a commonly presc...
PMC9043614
core_pubmed_pmc
Strategies for Glycoengineering Therapeutic Proteins
Strategies for Glycoengineering Therapeutic Proteins Abstract Almost all therapeutic proteins are glycosylated, with the carbohydrate component playing a long-established, substantial role in the safety and pharmacokinetic properties of this dominant category of drugs. In the past few years and moving forward, glycosyl...
PMC10812782
core_pubmed_pmc
Surgical Antibiotic Prophylaxis: A Proposal for a Global Evidence-Based Bundle
Surgical Antibiotic Prophylaxis: A Proposal for a Global Evidence-Based Bundle Abstract In the multimodal strategy context, to implement healthcare-associated infection prevention, bundles are one of the most commonly used methods to adapt guidelines in the local context and transfer best practices into routine clinica...
PMC5601478
core_pubmed_pmc
The effects of different enrofloxacin dosages on clinical efficacy and resistance development in chickens experimentally infected with Salmonella Typhimurium
The effects of different enrofloxacin dosages on clinical efficacy and resistance development in chickens experimentally infected with Salmonella Typhimurium Abstract To investigate the optimal dosage which can improve clinical efficacy and minimize resistance, pharmacokinetics/pharmacodynamics model of enrofloxacin wa...
PMC12816432
core_pubmed_pmc
Large Language Models for Clinical Trial Protocol Assessments
Large Language Models for Clinical Trial Protocol Assessments Abstract The purpose was to evaluate the utility of large language models (LLMs) for reviewing the statistical analysis plan (SAP) and pharmacokinetics–pharmacodynamics (PK–PD) components of clinical trial protocols. Clinical trial protocols and SAPs were ob...
PMC12492336
core_pubmed_pmc
Strategic Modulation of Isoniazid Solubility through Cocrystal Formation for Long-Acting Microneedle Therapy of Tuberculosis
Strategic Modulation of Isoniazid Solubility through Cocrystal Formation for Long-Acting Microneedle Therapy of Tuberculosis Abstract Abstract Tuberculosis (TB), caused by Mycobacterium tuberculosis , remains a global health emergency, particularly in low- and middle-income countries. Despite effective pharmacotherapy,...
PMC11919264
core_pubmed_pmc
A minimal physiologically‐based pharmacokinetic modeling platform to predict intratumor exposure and receptor occupancy of an anti‐LAG‐3 monoclonal antibody
A minimal physiologically‐based pharmacokinetic modeling platform to predict intratumor exposure and receptor occupancy of an anti‐LAG‐3 monoclonal antibody Abstract Abstract In oncology drug development, measuring drug concentrations at the tumor site and at the targeted receptor remains an ongoing challenge. Positron...
PMC9297897
core_pubmed_pmc
Ultra rapid lispro (URLi) shows faster pharmacokinetics and reduces postprandial glucose excursions versus Humalog® in patients with type 2 diabetes mellitus in a randomized, controlled crossover meal test early‐phase study
Ultra rapid lispro (URLi) shows faster pharmacokinetics and reduces postprandial glucose excursions versus Humalog® in patients with type 2 diabetes mellitus in a randomized, controlled crossover meal test early‐phase study Abstract Abstract Aims To compare the pharmacokinetics (PK), glucodynamics (GD) and tolerability...
PMC9075326
core_pubmed_pmc
A Head‐to‐Head Comparison of a Free Fatty Acid Formulation of Omega‐3 Pentaenoic Acids Versus Icosapent Ethyl in Adults With Hypertriglyceridemia: The ENHANCE‐IT Study
A Head‐to‐Head Comparison of a Free Fatty Acid Formulation of Omega‐3 Pentaenoic Acids Versus Icosapent Ethyl in Adults With Hypertriglyceridemia: The ENHANCE‐IT Study Abstract Abstract Background MAT9001 is an omega‐3 free fatty acid (FFA) formulation containing mainly eicosapentaenoic acid (EPA) and docosapentaenoic ...
PMC6813170
core_pubmed_pmc
Physiologically Based Pharmacokinetic Models for Adults and Children Reveal a Role of Intracellular Tubulin Binding in Vincristine Disposition
Physiologically Based Pharmacokinetic Models for Adults and Children Reveal a Role of Intracellular Tubulin Binding in Vincristine Disposition Abstract Abstract Vincristine is a cytotoxic chemotherapeutic agent used as first‐line therapy for pediatric acute lymphocytic leukemia. It is cleared by hepatic oxidative metab...
PMC4153970
core_pubmed_pmc
Improved Utilization of ADAS-Cog Assessment Data Through Item Response Theory Based Pharmacometric Modeling
Improved Utilization of ADAS-Cog Assessment Data Through Item Response Theory Based Pharmacometric Modeling Abstract Abstract Purpose This work investigates improved utilization of ADAS-cog data (the primary outcome in Alzheimer’s disease (AD) trials of mild and moderate AD) by combining pharmacometric modeling and ite...
PMC11387729
core_pubmed_pmc
Impact of ginsenoside Rb1 on gut microbiome and associated changes in pharmacokinetics in rats
Impact of ginsenoside Rb1 on gut microbiome and associated changes in pharmacokinetics in rats Abstract Ginsenoside Rb 1 exhibits a wide range of biological activities, and gut microbiota is considered the main metabolic site for Rb 1 . However, the impact of gut microbiota on the pharmacokinetics of Rb 1 are still unc...
PMC7277053
core_pubmed_pmc
Pharmacokinetics of Lusutrombopag, a Novel Thrombopoietin Receptor Agonist, in Rats by UPLC-MS/MS
Pharmacokinetics of Lusutrombopag, a Novel Thrombopoietin Receptor Agonist, in Rats by UPLC-MS/MS Abstract Lusutrombopag is a second oral thrombopoietin (TPO) receptor agonist that selectively acts on human TPO receptors. In the study, UPLC-MS/MS was used to establish a selective and sensitive method to determine lusut...
PMC8948956
core_pubmed_pmc
Safety and Pharmacokinetic Assessment of Oral Proglumide in Those with Hepatic Impairment
Safety and Pharmacokinetic Assessment of Oral Proglumide in Those with Hepatic Impairment Abstract Proglumide is an orally administered cholecystokinin receptor antagonist that was found to improve nonalcoholic steatohepatitis, reverse liver fibrosis, and decrease incidence of hepatocellular carcinoma (HCC) in animal m...
PMC9375310
core_pubmed_pmc
Tapering of biological treatment in autoinflammatory diseases: a scoping review
Tapering of biological treatment in autoinflammatory diseases: a scoping review Abstract Abstract Background Biological treatment and treat-to-target approaches guide the achievement of inactive disease and clinical remission in Autoinflammatory Diseases (AID). However, there is limited evidence addressing optimal tape...
PMC11314021
core_pubmed_pmc
Advanced Application of Polymer Nanocarriers in Delivery of Active Ingredients from Traditional Chinese Medicines
Advanced Application of Polymer Nanocarriers in Delivery of Active Ingredients from Traditional Chinese Medicines Abstract Abstract Active ingredients from Traditional Chinese Medicines (TCMs) have been a cornerstone of healthcare for millennia, offering a rich source of bioactive compounds with therapeutic potential. ...
PMC9578455
core_pubmed_pmc
Pharmacokinetic study on the co-administration of abemaciclib and astragaloside IV in rats
Pharmacokinetic study on the co-administration of abemaciclib and astragaloside IV in rats Abstract Abstract Context The co-administration of abemaciclib and astragaloside IV might occur in the treatment of breast cancer. Objective This study evaluates the interaction between abemaciclib and astragaloside IV in rats an...
PMC12196422
core_pubmed_pmc
The Impact of Substance Use Disorder and Drug Transfer into Breast Milk: Implications for Maternal and Infant Health
The Impact of Substance Use Disorder and Drug Transfer into Breast Milk: Implications for Maternal and Infant Health Abstract Abstract Breast milk provides significant health benefits to both infants and mothers, offering protection against infections and enhancing cognitive development. This paper examines the complex...
PMC7144168
core_pubmed_pmc
The Accumulation of Psoralen Contributes to Its Hepatotoxicity Revealed by Pharmacokinetic and Toxicokinetic Study after Repeated Administration
The Accumulation of Psoralen Contributes to Its Hepatotoxicity Revealed by Pharmacokinetic and Toxicokinetic Study after Repeated Administration Abstract Abstract Psoralen is a furanocoumarin compound found in many herb medicines and is claimed to contribute to the hepatotoxicity caused by lots of traditional Chinese m...
PMC9869698
core_pubmed_pmc
Pharmacological Activities of Fingerroot Extract and Its Phytoconstituents Against SARS-CoV-2 Infection in Golden Syrian Hamsters
Pharmacological Activities of Fingerroot Extract and Its Phytoconstituents Against SARS-CoV-2 Infection in Golden Syrian Hamsters Abstract Background The outbreak of COVID-19 has led to the suffering of people around the world, with an inaccessibility of specific and effective medication. Fingerroot extract, which show...
PMC8210606
core_pubmed_pmc
Closed-loop trans-skull ultrasound hyperthermia leads to improved drug delivery from thermosensitive drugs and promotes changes in vascular transport dynamics in brain tumors
Closed-loop trans-skull ultrasound hyperthermia leads to improved drug delivery from thermosensitive drugs and promotes changes in vascular transport dynamics in brain tumors Abstract Effective drug delivery in brain tumors remains a major challenge in oncology. Although local hyperthermia and stimuli-responsive delive...
PMC10235879
core_pubmed_pmc
A Phase 1 study for safety and pharmacokinetics of BIO101 (20‐hydroxyecdysone) in healthy young and older adults
A Phase 1 study for safety and pharmacokinetics of BIO101 (20‐hydroxyecdysone) in healthy young and older adults Abstract Abstract Background Sarcopenia is an age‐related skeletal muscle disorder characterized by loss of muscle mass and strength leading to mobility disability. 20‐Hydroxyecdysone (20E) is a polyhydroxyl...
PMC10359690
core_pubmed_pmc
Single-Dose Pharmacokinetics and Total Removal of Cyclophosphamide in a Patient with Acute Kidney Injury Undergoing Intermittent Haemodialysis and Prolonged Intermittent Kidney Replacement Therapy: A Case Report
Single-Dose Pharmacokinetics and Total Removal of Cyclophosphamide in a Patient with Acute Kidney Injury Undergoing Intermittent Haemodialysis and Prolonged Intermittent Kidney Replacement Therapy: A Case Report Abstract Abstract The largest study on cyclophosphamide pharmacokinetics in dialysis patients comprises of 6...
PMC12001278
core_pubmed_pmc
Quantitative Systems Pharmacology Model to Predict Target Occupancy by Bruton Tyrosine Kinase Inhibitors in Patients With B‐Cell Malignancies
Quantitative Systems Pharmacology Model to Predict Target Occupancy by Bruton Tyrosine Kinase Inhibitors in Patients With B‐Cell Malignancies Abstract ABSTRACT The effectiveness of Bruton tyrosine kinase (BTK) inhibitors is influenced by the level of BTK occupancy in target tissues. In randomized phase 3 studies, progr...
PMC9747122
core_pubmed_pmc
Mitigating ipatasertib‐induced glucose increase through dose and meal timing modifications
Mitigating ipatasertib‐induced glucose increase through dose and meal timing modifications Abstract Abstract Ipatasertib, an AKT inhibitor, in combination with prednisone and abiraterone, is under evaluation for the treatment of metastatic castration‐resistant prostate cancer (mCRPC). Hyperglycemia is an on‐target effe...
PMC12717316
core_pubmed_pmc
Pharmacological inhibition of Ubiquitin-Specific Peptidase 10 (USP10) with spautin-1 attenuates adipogenesis through CCAAT/Enhancer-Binding Protein Beta (C/EBPβ) destabilization
Pharmacological inhibition of Ubiquitin-Specific Peptidase 10 (USP10) with spautin-1 attenuates adipogenesis through CCAAT/Enhancer-Binding Protein Beta (C/EBPβ) destabilization Abstract Abstract The pharmacological control of lipid accumulation in white adipose tissue (WAT) is a key area of focus in obesity research, ...
PMC8548711
core_pubmed_pmc
Predicting the Outcome of Voriconazole Individualized Medication Using Integrated Pharmacokinetic/Pharmacodynamic Model
Predicting the Outcome of Voriconazole Individualized Medication Using Integrated Pharmacokinetic/Pharmacodynamic Model Abstract Abstract Therapeutic drug monitoring is considered to be an effective tool for the individualized use of voriconazole. However, drug concentration measurement alone doesn’t take into account ...
PMC3686783
core_pubmed_pmc
Genetic Variants of Pregnane X Receptor (PXR) and CYP2B6 Affect the Induction of Bupropion Hydroxylation by Sodium Ferulate
Genetic Variants of Pregnane X Receptor (PXR) and CYP2B6 Affect the Induction of Bupropion Hydroxylation by Sodium Ferulate Abstract This study investigated the effects of pregnane X receptor (PXR/ NR1I2 ) and CYP2B6 genetic variants on sodium ferulate (SF)-mediated induction of bupropion hydroxylation. The pharmacokin...
PMC5312557
core_pubmed_pmc
A Novel PEGylation Method for Improving the Pharmacokinetic Properties of Anti-Interleukin-17A RNA Aptamers
A Novel PEGylation Method for Improving the Pharmacokinetic Properties of Anti-Interleukin-17A RNA Aptamers Abstract Abstract The obstacles to the development of therapeutic aptamers for systemic inflammatory diseases, such as nuclease degradation and renal clearance, have not been fully overcome. Here, we report a nov...
PMC11126830
core_pubmed_pmc
Development and validation of an HILIC/MS/MS method for determination of nusinersen in rabbit plasma
Development and validation of an HILIC/MS/MS method for determination of nusinersen in rabbit plasma Abstract A hydrophilic interaction liquid chromatography tandem mass spectrometry (HILIC/MS/MS) method was developed and validated for the quantitative analysis of the fully phosphorothioate modified oligonucleotide nus...
PMC6292884
core_pubmed_pmc
Targeted chemotherapy for subcutaneous and orthotopic non-small cell lung tumors with cyclic RGD-functionalized and disulfide-crosslinked polymersomal doxorubicin
Targeted chemotherapy for subcutaneous and orthotopic non-small cell lung tumors with cyclic RGD-functionalized and disulfide-crosslinked polymersomal doxorubicin Abstract Abstract Lung cancer, with its high mortality and increasing morbidity, has become one of the most lethal malignancies worldwide. Here, we developed...
PMC8055351
core_pubmed_pmc
Plasma Levels of Long-Acting Injectable Antipsychotics in Outpatient Care: A Retrospective Analysis
Plasma Levels of Long-Acting Injectable Antipsychotics in Outpatient Care: A Retrospective Analysis Abstract Abstract Purpose Antipsychotic efficacy in schizophrenia depends on its availability in the body. Although therapeutic outcomes remain still far from satisfactory, therapeutic drug monitoring is not a common par...
PMC7666662
core_pubmed_pmc
Infliximab in young paediatric IBD patients: it is all about the dosing
Infliximab in young paediatric IBD patients: it is all about the dosing Abstract Abstract Infliximab (IFX) is administered intravenously using weight-based dosing (5 mg/kg) in inflammatory bowel disease (IBD) patients. Our hypothesis is that especially young children need a more intensive treatment regimen than the cur...
PMC8590984
core_pubmed_pmc
Transdermal Delivery of Telmisartan: Formulation, in vitro, ex vivo, Iontophoretic Permeation Enhancement and Comparative Pharmacokinetic Study in Rats
Transdermal Delivery of Telmisartan: Formulation, in vitro, ex vivo, Iontophoretic Permeation Enhancement and Comparative Pharmacokinetic Study in Rats Abstract Purpose The purpose of this study was to prepare telmisartan transethosomes, incorporate them into a gel, evaluate them for in vitro drug release and in vivo p...
PMC9867719
core_pubmed_pmc
Therapeutic beta-lactam dosages and broad-spectrum antibiotics are associated with reductions in microbial richness and diversity in persons with cystic fibrosis
Therapeutic beta-lactam dosages and broad-spectrum antibiotics are associated with reductions in microbial richness and diversity in persons with cystic fibrosis Abstract Abstract Persons with cystic fibrosis (PwCF) suffer from pulmonary exacerbations (PEx) related in part to lung infection. While higher microbial dive...
PMC8415744
core_pubmed_pmc
Editorial: Model-Based Evaluation of Antimicrobial Agents in Children
Editorial: Model-Based Evaluation of Antimicrobial Agents in Children Modeling Individualized Antimicrobial Therapy Based on Developed PopPK or PBPK Models In this topic, model-based individualized antimicrobial therapy was recommended. Zhang et al. developed a population pharmacokinetic (PopPK) model of teicoplanin us...
PMC10097993
core_pubmed_pmc
Sex and gender considerations in Alzheimer’s disease: The Women’s Brain Project contribution
Sex and gender considerations in Alzheimer’s disease: The Women’s Brain Project contribution Abstract Abstract The global population is expected to have about 131.5 million people living with Alzheimer’s disease (AD) and other dementias by 2050, posing a severe health crisis. Dementia is a progressive neurodegenerative...
PMC6581063
core_pubmed_pmc
Optimizing Vancomycin Dosing in Chronic Kidney Disease by Deriving and Implementing a Web-Based Tool Using a Population Pharmacokinetics Analysis
Optimizing Vancomycin Dosing in Chronic Kidney Disease by Deriving and Implementing a Web-Based Tool Using a Population Pharmacokinetics Analysis Abstract Background: Chronic kidney disease (CKD) patients requiring intravenous vancomycin bear considerable risks of adverse outcomes both from the infection and vancomycin...
PMC12953650
core_pubmed_pmc
Genetic variability in thrombopoietin receptor and GATA1 influences response to eltrombopag in dengue-induced thrombocytopenia
Genetic variability in thrombopoietin receptor and GATA1 influences response to eltrombopag in dengue-induced thrombocytopenia Abstract Abstract Integrating pharmacogenetic studies into clinical trials enhances personalized medicine by identifying genetic variations that influence drug efficacy and safety. Eltrombopag,...
PMC7549113
core_pubmed_pmc
A radiolabeled drug tracing method to study neurotrophin-3 retention and distribution in the cochlea after nano-based local delivery
A radiolabeled drug tracing method to study neurotrophin-3 retention and distribution in the cochlea after nano-based local delivery Abstract Hearing loss is the most common sensory deficit worldwide with no approved therapeutics for treatment. Local neurotrophin delivery into the cochlea has shown great potential in p...
PMC3413023
core_pubmed_pmc
Management of antipsychotic treatment discontinuation and interruptions using model-based simulations
Management of antipsychotic treatment discontinuation and interruptions using model-based simulations Abstract Background Medication nonadherence is a well described and prevalent clinical occurrence in schizophrenia. These pharmacokinetic model-based simulations analyze predicted antipsychotic plasma concentrations in...