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FG-4592 (ASP1517) | HIF prolyl-hydroxylase inhibitor

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Product Description

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. [1] 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. [1]

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. [2, 3]

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. [4]

Technical information:

Chemical Formula:   C19H16N2O5
CAS #:   808118-40-3
Molecular Weight:   352.34
Purity:   > 98%
Appearance:   Yellow
Chemical Name:   2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic acid
Solubility:   Up to 100 mM in DMSO
Synonyms:   FG-4592, FG4592, ASP1517

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


1. "Correction of anemia without IV iron supplementation in incident dialysis patients" Fibrogen press release, Nov. 5, 2012
2. "FG-4592 and epoetin alpha in Phase II anemia study", Datamonitor Research Store, Nov. 11, 1012.
3. "Hemoglobin correction and maintenance in end-stage renal patients" Fibrogen press release, Nov. 5, 2012
4. Fibrogen press release, Dec. 11, 2012 (Phase 3 announcement)

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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