FG-2216, also known as YM311, is orally bioavailable HIF-prolyl hydroxylase inhibitor. FG-2216 induced significant and reversible Epo induction in vivo. FG-2216 showed the ability to stabilize HIF-α, to stimulate EPO secretion in in vitro studies, and to increase hematocrit, red blood cell count, and hemoglobin levels in an animal efficacy study.