Strategies to Inhibit ABCB1- and ABCG2-Mediated Efflux Transport of Erlotinib at the Blood–Brain Barrier: A PET Study on Nonhuman Primates - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Journal of Nuclear Medicine Année : 2017

Strategies to Inhibit ABCB1- and ABCG2-Mediated Efflux Transport of Erlotinib at the Blood–Brain Barrier: A PET Study on Nonhuman Primates

Résumé

The tyrosine kinase inhibitor erlotinib poorly penetrates the blood-brain barrier (BBB) because of efflux transport by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2), thereby limiting its utility in the treatment of non-small cell lung cancer metastases in the brain. Pharmacologic strategies to inhibit ABCB1/ABCG2-mediated efflux transport at the BBB have been successfully developed in rodents, but it remains unclear whether these can be translated to humans given the pronounced species differences in ABCG2/ABCB1 expression ratios at the BBB. We assessed the efficacy of two different ABCB1/ABCG2 inhibitors to enhance brain distribution of 11C-erlotinib in nonhuman primates as a model of the human BBB.

Dates et versions

hal-02401400 , version 1 (09-12-2019)

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Citer

Nicolas Tournier, Sébastien Goutal, Sylvain Auvity, Alexander Traxl, Severin Mairinger, et al.. Strategies to Inhibit ABCB1- and ABCG2-Mediated Efflux Transport of Erlotinib at the Blood–Brain Barrier: A PET Study on Nonhuman Primates. Journal of Nuclear Medicine, 2017, 58 (1), pp.117-122. ⟨10.2967/jnumed.116.178665⟩. ⟨hal-02401400⟩
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