Chemical Formula: C19H16N2O5
Exact Mass: 352.10592
CODE FG-4592; ASP1517
WHO NUMBER 9717
FG-4592 (also known as ASP1517), 2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic acid,
is a potent small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH),
an enzyme up-regulating the expression of endogenous human erythropoietin (Epo).
It is currently being investigated as an oral treatment for anemia associated with chronic kidney disease (CKD).
Unlike other anemia treating agents, erythropoiesis-stimulating agents (ESAs),
FG-4592 inhibits HIF, through a distinctive mechanism, by stabilization of HIF. According to previous studies,
FG-4592 is capable of correcting and maintaining hemoglobin levels in CKD patients not
receiving dialysis and in patients of end-stage renal disease
who receives dialysis but do not need intravenous iron supplement.
1. Luis Borges. Different modalities of erythropoiesis stimulating agents.
Port J Nephrol Hypert 2010; 24(2): 137-145
2. “FibroGen and Astellas announce initiation of phase 3 trial of FG-4592/ASP1517 for treatment
of anemia of chronic kidney disease” Fibrogen Press Release. Dec 11 2012
3. “FibroGen announces initiation of phase 2b studies of FG-4592,
an oral HIF prolyl hydroxylase inhibitor, for treatment of anemia”
- Originator FibroGen
- Developer Astellas Pharma; AstraZeneca; FibroGen
- Class Amides; Antianaemics; Carboxylic acids; Isoquinolines; Small molecules
- Mechanism of Action Basic helix loop helix transcription factor modulators; Hypoxia-inducible factor-proline dioxygenase inhibitors
- Phase III Anaemia
- Discontinued Sickle cell anaemia
Most Recent Events
- 09 Jun 2016 Phase-III clinical trials in Anaemia in Japan (PO)
- 20 May 2016 In collaboration with FibroGen, Astellas Pharma plans a phase III trial for Anaemia (In chronic kidney disease patients undergoing peritoneal dialysis) in Japan (PO) (NCT02780726)
- 19 May 2016 In collaboration with FibroGen, Astellas Pharma plans a phase III trial for Anaemia (In erythropoiesis stimulating agent-naive, chronic kidney disease patients undergoing haemodialysis) in Japan (PO) (NCT02780141)
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