Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H16N2O5 |
Molecular Weight | 352.3407 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NC(C(=O)NCC(O)=O)=C(O)C2=C1C=C(OC3=CC=CC=C3)C=C2
InChI
InChIKey=YOZBGTLTNGAVFU-UHFFFAOYSA-N
InChI=1S/C19H16N2O5/c1-11-15-9-13(26-12-5-3-2-4-6-12)7-8-14(15)18(24)17(21-11)19(25)20-10-16(22)23/h2-9,24H,10H2,1H3,(H,20,25)(H,22,23)
Molecular Formula | C19H16N2O5 |
Molecular Weight | 352.3407 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://newdrugapprovals.org/2016/06/21/roxadustat/Curator's Comment: Description was created based on several sources, including
https://www.sps.nhs.uk/medicines/roxadustat/
http://adisinsight.springer.com/drugs/800023523
Sources: https://newdrugapprovals.org/2016/06/21/roxadustat/
Curator's Comment: Description was created based on several sources, including
https://www.sps.nhs.uk/medicines/roxadustat/
http://adisinsight.springer.com/drugs/800023523
Roxadustat (FG-4592) is an HIF α prolyl hydroxylase inhibitor in a cell-free assay. It stabilizes HIF-2 and induces EPO production and stimulates erythropoiesis. Roxadustat transiently and moderately increased endogenous erythropoietin and reduced hepcidin. It is currently being investigated as an oral treatment for anemia associated with chronic kidney disease (CKD). In April 2006, Roxadustat (FG-4592) was licensed to Astellas Pharma by originator FibroGen in Asia, Europe and South Africa for the treatment of anemia. FibroGen retains rights in the rest of the world. In 2007, the FDA put the trial on clinical hold due to one case of death by fulminant hepatitis during a phase II clinical trial for patients with anemia associated with chronic kidney disease and not requiring dialysis. However, in 2008, the FDA informed the company that clinical trials could be resumed. Phase II/III clinical trials for this indication resumed in 2012. In 2013, the compound was licensed to AstraZeneca by FibroGen for development and marketing in US, CN and all major markets excluding JP, Europe, the Commonwealth of Independent States, the Middle East and South Africa, for the treatment of anemia associated with chronic kidney disease (CKD) and end-stage renal disease (ESRD).
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3028 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27352308 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02174627
The initial study drug dose is 70 mg three times a week (TIW). The dose is subsequently adjusted to achieve and maintain Hb 11±1 g/dL.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27021233
Roxadustat (5 uM) increases the differentiation of ADMSCs in hypoxic conditions.
Substance Class |
Chemical
Created
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Sat Dec 16 06:34:56 GMT 2023
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Record UNII |
X3O30D9YMX
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Validated (UNII)
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C471
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B03XA05
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Roxadustat
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ACTIVE MOIETY |