REVIEW FG-4592 is an orally-available isoquinoline-based inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase for the treatment of anemia and patients with chronic kidney disease. Phase 2 studies indicate that oral administration of FG-4592 three times a week increased mean hemoglobin levels in the first eight weeks, regardless of supplementation with IV or oral iron, or no iron supplementation. FG-4592 is novel in that it allows integration of red blood cell production and efficient iron incorporation simultaneously. Data from Phase 2 trials comparing with epoetin alpha indicate that treatment with FG-4592 alone results in a sustained reduction of total plasma cholesterol levels by an average of 20%, while no reduction was seen with epoetin alpha. In December, 2012, Fibrogen and Astellas Pharma announced the initiation of a Phase 3 clinical development program for the treatment of anemia associated with chronic kidney disease in patients not on dialysis and on dialysis.
REFERENCES
[1]
Arend, Michael P.; Flippin, Lee A.; Guenzler-Pukall, Volkmar; Ho, Wen-Bin; Turtle, Eric D.; Du, Xiaohui; Preparation of isoquinolinecarboxamides and their use in mediating hypoxia inducible factor and increasing endogenous erythropoietin. PCT Int. Appl. (2004), WO 2004108681 A1 20041216.
[2]
Kang, Xinshan; Long, Wei; Zhang, Jianxi; Hu, Yunyan; Wang, Yinxiang; Preparation and polymorphic forms of an isoquinolylcarbonyl glycine derivative as a prolyl hydroxylase inhibitor. PCT Int. Appl. (2013), WO 2013013609 A1 20130131.
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Beuck S, Schänzer W, Thevis M. Hypoxia-inducible factor stabilizers and other small-molecule erythropoiesis-stimulating agents in current and preventive doping analysis. Drug Test Anal. 2012 Nov;4(11):830-45.
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