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. Author manuscript; available in PMC: 2017 Jul 25.
Published in final edited form as: Hemodial Int. 2017 Jun;21(Suppl 1):S110–S124. doi: 10.1111/hdi.12567

Table 1.

HIF-PHIs in clinical development for the treatment of anemia

Compound Ref. Development status HIF-a stabilization HIF-PHD targets
AKB-6548
(Vadadustat)
Akebia Therapeutics
86,88,89 Phase 3 HIF-2α > HIF-1α PHD3 > PHD2
GSK-1278863
(Daprodustat)
GlaxoSmithKline
81,9092 Phase 3 HIF-1α and HIF-2α PHD2 and PHD3
FG-4592
(Roxadustat)
Fibrogen/Astellas Pharma/AstraZeneca
82,85 Phase 3 HIF-1α and HIF-2α PHD1, 2 and 3
BAY 85-3934
(Molidustat)
Bayer Pharma
9395 Phase 2 HIF-1α and HIF-2α PHD2 > PHD1/PHD3
JTZ-951
Japan Tabacco, Inc./Akros Pharma, Inc.
96 Phase 2 Not published Not published
Zyan1
Cadila Healthcare
97,98 Phase 1 Not published Not published
JNJ-42905343
Janssen Pharmaceutica
99 Pre-clinical HIF-1α and HIF-2α PHD1, 2 and 3
DS-1093
Daiichi Sankyo, Inc.
Discontinued for anemia, under evaluation for other indications Not published Not published

The above table is based on a review of the literature and other publicly available resources such as patent applications. A direct comparison of half maximal inhibitory concentrations (IC50) of various compounds for HIF-PHDs, FIH, and other dioxygenases has not yet been published.