Carine Bardinet

Ruxolitinib Pharmacokinetics and Exposure–Toxicity Relationship in Hematologic Malignancies and Immune‐Mediated Diseases: A Prospective Observational Study

Jérémie Tachet, Sara C. Meyer, Francesco Grandoni, Emmanuel Haefliger et autres

Ruxolitinib pharmacokinetics (PK) has been characterized in clinical trials but remains poorly documented in real‐world practice. This project aimed to investigate ruxolitinib PK in routine clinical practice, identify factors driving its variability, and explore exposure–response relationships to assess the potential role of …

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Human prostaglandin reductases dearomatize and inactivate benzothiazinone antitubercular drugs

Myriam Briki, Caroline Wagner, Vincent Desfontaine, Anthony Vocat et autres

Abstract Macozinone (MCZ, PBTZ169) is a potent clinical stage benzothiazinone antitubercular agent that covalently inhibits the essential mycobacterial flavoenzyme DprE1. In some mammals, MCZ undergoes reductive dearomatization to H 2 MCZ, a Hydride Meisenheimer Complex, identified as the major circulating metabolite in …

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Population Pharmacokinetics of Levosimendan and its Metabolites OR-1855 and OR-1896 in Critically Ill Adults, Neonates and Infants on Veno-Arterial ECMO

Stéphane Bertin, Monia Guidi, David Haefliger, Paul Thoueille et autres

BACKGROUND AND OBJECTIVE: Levosimendan is an inotrope and vasodilator agent commonly used in critical care, particularly to facilitate weaning from veno-arterial extracorporeal membrane oxygenation (VA-ECMO). However, critical illness and ECMO may affect levosimendan and its clinically relevant metabolites' pharmacokinetics, potentially compromising circulating …

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POS0148 THERAPEUTIC DRUG MONITORING FOR PRECISION MEDICINE AND DOSE OPTIMIZATION OF UPADACITINIB: A REAL-WORLD PROSPECTIVE OBSERVATIONAL STUDY

Jérémie Tachet, Alexandre Dumusc, Pascal Juillerat, C. Conrad et autres

Background: The Janus kinase inhibitor (JAKI) upadacitinib is an orally administered small molecule that selectively inhibits the Janus Kinase 1 (JAK1) and is indicated for the treatment of rheumatological and dermatological disorders as well as inflammatory bowel diseases (IBDs). Dose-response relationship and …

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Novel Patient‐Friendly Orodispersible Formulation of Ivermectin is Associated With Enhanced Palatability, Controlled Absorption, and Less Variability: High Potential for Pediatric Use

Kim Dao, Michael Buettcher, Klervi Golhen, Jonas Kost et autres

Abstract Ivermectin has been used since the 1980s as an anthelmintic and antiectoparasite agent worldwide. Currently, the only available oral formulation is tablets designed for adult patients. A patient‐friendly orodispersible tablet formulation designed for pediatric use (CHILD‐IVITAB) has been developed and is …

ch, us (code pays fourni par la source)

An innovative ethosuximide granule formulation designed for pediatric use: Comparative pharmacokinetics, safety, tolerability, and palatability profile versus reference syrup

Léonore Diezi, Kim Dao, Vincent Jullien, Caroline Roussel‐Maupetit et autres

Abstract Ethosuximide, the first‐line therapy for childhood absence epilepsy, is currently formulated as a syrup (Zarontin®, Pfizer) with a bitter taste and high sugar content, poorly adapted to children, and a ketogenic diet. The collaborative European FP7 project KIEKIDS aimed at developing …

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Optimized LC-MS/MS quantification of tuberculosis drug candidate macozinone (PBTZ169), its dearomatized Meisenheimer Complex and other metabolites, in human plasma and urine

Vincent Desfontaine, Sylvie Guinchard, Sara Rute Marques, Anthony Vocat et autres

Tuberculosis, and especially multidrug-resistant tuberculosis (MDR-TB), is a major global health threat which emphasizes the need to develop new agents to improve and shorten treatment of this difficult-to-manage infectious disease. Among the new agents, macozinone (PBTZ169) is one of the most promising …

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Quantification of serotonin and eight of its metabolites in plasma of healthy volunteers by mass spectrometry

Philippe J. Eugster, Marielle Dunand, Baptiste Grund, Anton Ivanyuk et autres

Serotonin is transformed into melatonin under the control of the light/dark cycle, representing a cornerstone of circadian rhythmicity. Serotonin also undergoes extensive metabolism to produce 5-hydroxyindoleacetic acid (5-HIAA), a biomarker for the diagnosis and monitoring of serotonin secreting neuroendocrine tumors (NETs). While …

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Corrigendum to “LC–MS/MS method for the simultaneous analysis of seven antimalarials and two active metabolites in dried blood spots for applications in field trials: Analytical and clinical validation” [J. Pharm. Biomed. Anal. 154 (2018) 263–277]

Joanna Gallay, S Prod'hom, Thomas Mercier, Carine Bardinet et autres

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Sultiame pharmacokinetic profile in plasma and erythrocytes after single oral doses: A pilot study in healthy volunteers

Kim Dao, Paul Thoueille, Laurent Arthur Decosterd, Thomas Mercier et autres

Abstract A pilot study was conducted aiming at specifying sultiame's pharmacokinetic profile, completed by in vitro assays evaluating the intraerythrocytic transfer of sultiame and by a pharmacokinetic model assessing its distribution. Single oral doses of sultiame (Ospolot® 50, 100, and 200 mg) …

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Development and validation of a multiplex UHPLC-MS/MS method for the determination of the investigational antibiotic against multi-resistant tuberculosis macozinone (PBTZ169) and five active metabolites in human plasma

Dany Spaggiari, Vincent Desfontaine, Sandra Cruchon, Sylvie Guinchard et autres

The emergence of Mycobacterium tuberculosis strains resistant to current first-line antibiotic regimens constitutes a major global health threat. New treatments against multidrug-resistant tuberculosis (MDR-TB) are thus eagerly needed in particular in countries with a high MDR-TB prevalence. In this context, macozinone (PBTZ169), …

ch, ru (code pays fourni par la source)

LC–MS/MS method for the simultaneous analysis of seven antimalarials and two active metabolites in dried blood spots for applications in field trials: Analytical and clinical validation

Joanna Gallay, S Prod'hom, Thomas Mercier, Carine Bardinet et autres

ch (code pays fourni par la source)