A phase I trial assessing the safety, pharmacokinetics, cerebrospinal fluid penetrance, and food effect of BTK inhibitor tolebrutinib in healthy volunteers

Autor: Marie‐José Cabanis, Olivier Nicolas, Olivier Vitse, Christelle Jan, Priscilla Brun, Patrick Soubayrol, William B. Smith, Timothy J. Turner, Emmanuel Krupka

Publikováno v: Clinical and Translational Science, Vol 17, Iss 2, Pp n/a-n/a (2024)

Abstract Tolebrutinib is an oral, brain‐penetrant, covalent Bruton's tyrosine kinase inhibitor in development to treat multiple sclerosis at 60 mg/day with food. A phase I trial was conducted in healthy volunteers to assess the safety and pharmacok

Externí odkaz: https://doaj.org/article/f3570e172454421c89380f625b1876c5

Preclinical in vitro and in vivo pharmacokinetic properties of danicamtiv, a new targeted myosin activator for the treatment of dilated cardiomyopathy

Autor: Mark P. Grillo, Svetlana Markova, Marc Evanchik, Marc Trellu, Patricia Moliner, Priscilla Brun, Anne Perreard-Dumaine, Pascale Vicat, Chun Yang, James P. Driscoll, Tim J. Carlson

Publikováno v: Xenobiotica. 51:222-238

Dilated cardiomyopathy (DCM) is a disease of the myocardium defined by left ventricular enlargement and systolic dysfunction leading to heart failure. Danicamtiv, a new targeted myosin activator de...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6e1361f51b200ee3d2f156a0c2ce1187
https://doi.org/10.1080/00498254.2020.1839982

IMI – oral biopharmaceutics tools project – evaluation of bottom-up PBPK prediction success part 1: Characterisation of the OrBiTo database of compounds

Autor: Franziska Graf, Wolfgang Mück, Dominique Swerts, Kerstin J. Frank, Dorina van der Mey, Joanne Bennett, Marta Venczel, Thomas Müller, Uwe Muenster, Hans Lennernäs, Florent Mazuir, Jan Bevernage, Mei Wong, Mark McAllister, Stéphane Beilles, Loic Laplanche, Alison Margolskee, Stefania Beato, Lieve Adriaenssen, Loeckie de Zwart, Jonas Angstenberger, Xavier Pepin, Anh-Thu Nguyen-Trung, Alexander Marker, Amin Rostami-Hodjegan, P. Zane, Céline Ollier, An Van Den Bergh, Adam S. Darwich, Shriram M. Pathak, Dónal Murphy, Markus Kolhmann, Pankaj Daga, Susanne Greschat-Schade, Michael B. Bolger, Achiel Van Peer, Christer Tannergren, Priscilla Brun, Mohammed Yasin, Bertil Abrahamsson, Sara Carlert, Richard Lloyd, Christophe Tistaert, Leon Aarons, Petra Loos, Xavier Boulenc, Pascale Vicat

Publikováno v: Margolskee, A, Darwich, A, Pepin, X, Pathak, S M, Bolger et al, M B, Aarons, L, Rostami-Hochaghan, A, Angstenberger, J, Graf, F, Laplanche, L, Muller, T, Carlert, S, Daga, P, Murphy, D, Tannergren, C, Yasin, M, Greschat-Schade, S, Muck, W, Muenster, U, van der Mey, D, Frank, K, Lloyd, R, Adriaenssen, L, Bevernage, J, De Zwart, L, Swerts, D, Tistaert, C, Van Den Bergh, A, Van Peer, A, Beato, S, Nguyen-Trung, A-T, Bennett, J, McAllister, M, Wong, M, Zane, P, Ollier, C, Vicat, P, Kolhmann, M, Marker, A, Brun, P, Mazuir, F, Beilles, S, Venczel, M, Boulenc, X, Loos, P, Lennernas, H & Abrahamsson, B 2016, ' IMI – oral biopharmaceutics tools project – evaluation of bottom-up PBPK prediction success part 1: Characterisation of the OrBiTo database of compounds ', European Journal of Pharmaceutical Sciences . https://doi.org/10.1016/j.ejps.2016.09.027

Predicting oral bioavailability (Foral) is of importance for estimating systemic exposure of orally administered drugs. Physiologically-based pharmacokinetic (PBPK) modelling and simulation have been applied extensively in biopharmaceutics recently.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eeb52ebb9ed35fea70aa7eb44eca0076
https://doi.org/10.1016/j.ejps.2016.09.027

In vitro and in vivo pharmacokinetic characterization of mavacamten, a first-in-class small molecule allosteric modulator of beta cardiac myosin

Autor: Marc J. Evanchik, Priscilla Brun, John C L Erve, Nicole V Haste, Mark P. Grillo, Svetlana Markova, Ryan Dick, Timothy J. Carlson, James P Driscoll

Publikováno v: Xenobiotica; the fate of foreign compounds in biological systems. 49(6)

Mavacamten is a small molecule modulator of cardiac myosin designed as an orally administered drug for the treatment of patients with hypertrophic cardiomyopathy. The current study objectives were to assess the preclinical pharmacokinetics of mavacam

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b176f29dbd3a994fef4811bf6c9c748d
https://pubmed.ncbi.nlm.nih.gov/30044681

PBPK modeling of irbesartan: incorporation of hepatic uptake

Autor: Helene, Chapy, Sylvie, Klieber, Priscilla, Brun, Sabine, Gerbal-Chaloin, Xavier, Boulenc, Olivier, Nicolas

Publikováno v: Biopharmaceuticsdrug disposition. 36(8)

Physiological based pharmacokinetic (PBPK) modeling is now commonly used in drug development to integrate human or animal physiological data in order to predict pharmacokinetic profiles. The aim of this work was to construct and refine a PBPK model o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::5eef2afd42e88acfea923726f08a1193
https://pubmed.ncbi.nlm.nih.gov/26037524