Goutal S, Gerstenmayer M, Auvity S, Caillé F, Mériaux S, Buvat I, et al
. Physical blood-brain barrier disruption induced by focused ultrasound does not overcome the transporter-mediated efflux of erlotinib. J Control Release. 2018;292:210-220 pubmed publisher
..05), in any of the tested conditions. BBB integrity is not the rate limiting step for erlotinib delivery to the brain which is mainly governed by ABC-mediated efflux. Efflux transport of erlotinib persisted despite BBB disruption. ..
Auvity S, Caillé F, Marie S, Wimberley C, Bauer M, Langer O, et al
. P-glycoprotein (ABCB1) inhibits the influx and increases the efflux of 11C-metoclopramide across the blood-brain barrier: a PET study on non-human primates. J Nucl Med. 2018;: pubmed publisher
..The overall impact of ABCB1 on drug delivery to the brain can be non-invasively estimated from image-derived outcome parameters without the need for an arterial input function. ..
Amor D, Goutal S, Marie S, Caillé F, Bauer M, Langer O, et al
. Impact of rifampicin-inhibitable transport on the liver distribution and tissue kinetics of erlotinib assessed with PET imaging in rats. EJNMMI Res. 2018;8:81 pubmed publisher
..Decreased 11C-erlotinib uptake by elimination organs did not translate into changes in systemic exposure and exposure to the lungs, which are a target tissue for erlotinib therapy. ..
Damont A, Goutal S, Auvity S, Valette H, Kuhnast B, Saba W, et al
. Imaging the impact of cyclosporin A and dipyridamole on P-glycoprotein (ABCB1) function at the blood-brain barrier: A [(11)C]-N-desmethyl-loperamide PET study in nonhuman primates. Eur J Pharm Sci. 2016;91:98-104 pubmed publisher
..Despite in vitro P-gp inhibition potency, usual doses DPy are not likely to inhibit P-gp function at the BBB. ..
Tournier N, Goutal S, Auvity S, Traxl A, Mairinger S, Wanek T, et al
. Strategies to Inhibit ABCB1- and ABCG2-Mediated Efflux Transport of Erlotinib at the Blood-Brain Barrier: A PET Study on Nonhuman Primates. J Nucl Med. 2017;58:117-122 pubmed publisher
..For patients with brain tumors, such inhibition protocols may ultimately be applied to create more effective treatments using drugs that undergo efflux transport at the BBB. ..
Auvity S, Goutal S, Thézé B, Chaves C, Hosten B, Kuhnast B, et al
. Evaluation of TSPO PET imaging, a marker of glial activation, to study the neuroimmune footprints of morphine exposure and withdrawal. Drug Alcohol Depend. 2017;170:43-50 pubmed publisher
..Accordingly, expression of glial markers did not increase after morphine discontinuation. Morphine tolerance and withdrawal did not detectably activate microglia and had no impact on [18F]DPA-714 brain kinetics in vivo. ..
Goutal S, Langer O, Auvity S, Andrieux K, Coulon C, Caillé F, et al
. Intravenous infusion for the controlled exposure to the dual ABCB1 and ABCG2 inhibitor elacridar in nonhuman primates. Drug Deliv Transl Res. 2018;8:536-542 pubmed publisher
Tournier N, Valette H, Peyronneau M, Saba W, Goutal S, Kuhnast B, et al
. Transport of selected PET radiotracers by human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2): an in vitro screening. J Nucl Med. 2011;52:415-23 pubmed publisher
..Efflux transporters at the BBB-P-glycoprotein (P-gp) and the breast cancer resistance protein (BCRP)-could limit their uptake by the brain...
Tournier N, Saba W, Cisternino S, Peyronneau M, Damont A, Goutal S, et al
. Effects of selected OATP and/or ABC transporter inhibitors on the brain and whole-body distribution of glyburide. AAPS J. 2013;15:1082-90 pubmed publisher
..Conversely, P-gp, BCRP, and probably multidrug resistance protein 4 work in synergy to limit GLB brain uptake. ..