Pharmacokinetic interactions in mice between irinotecan and MBL-II-141, an ABCG2 inhibitor.

Abstract:

PURPOSE:The chromone derivative MBL-II-141, specifically designed to inhibit ABCG2, was previously demonstrated to combine strong inhibition potency, low toxicity and good efficiency in reversing resistance to irinotecan in a xenografted mouse model. Here, the pharmacokinetic interactions in mice between irinotecan, its active metabolite SN-38 and MBL-II-141 were characterized quantitatively in the blood and in the brain. METHODS:Compartmental models were used to fit the data. Goodness-of-fit was assessed by simulation-based diagnostic tools. RESULTS:Irinotecan increased the MBL-II-141 apparent clearance and Vss 1.5-fold, probably by increasing the MBL-II-141 unbound fraction. MBL-II-141 decreased the total apparent clearance of irinotecan by 23%, by decreasing its biliary clearance. MBL-II-141 increased 3-fold the brain accumulation of irinotecan, as a result of the rise of systemic exposure combined with the inhibition of ABCG2-mediated efflux at the blood-brain barrier. Finally, SN-38 exposure was increased by 1.16-fold under treatment with MBL-II-141, owing to the higher irinotecan exposure with increased metabolism towards the formation of SN-38. CONCLUSIONS:These results may help to anticipate the pharmacokinetic interactions between MBL-II-141 and other ABCG2 substrates. The irinotecan-MBL-II-141 interaction is also expected to occur in humans. Copyright © 2017 John Wiley & Sons, Ltd.

journal_name

Biopharm Drug Dispos

authors

Hénin E,Honorat M,Guitton J,Di Pietro A,Payen L,Tod M

doi

10.1002/bdd.2069

subject

Has Abstract

pub_date

2017-07-01 00:00:00

pages

351-362

issue

5

eissn

0142-2782

issn

1099-081X

journal_volume

38

pub_type

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