Etravirine is an inhibitor of ABCG2 but not ABCB1 in vitro able to inhibit ABCG2-mediated efflux of TDF and abacavir.
Through inhibition of ABCG2, etravirine increases placental passage of tenofovir disoproxil fumarate from mother to fetus.
ABCG2-mediated pharmacokinetic DDI of etravirine with ABCG2 substrates during pharmacotherapy of HIV infection may occur.