Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C12H9ClN2O4 |
| Molecular Weight | 280.664 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CNC(=O)C1=C(O)C2=CC=CC=C2C(Cl)=N1
InChI
InChIKey=OUQVKRKGTAUJQA-UHFFFAOYSA-N
InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17)
DescriptionCurator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/23234607 | https://www.ncbi.nlm.nih.gov/pubmed/23547775 | https://www.ncbi.nlm.nih.gov/pubmed/21115615
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/23234607 | https://www.ncbi.nlm.nih.gov/pubmed/23547775 | https://www.ncbi.nlm.nih.gov/pubmed/21115615
FG 2216 is an erythropoietic small molecule prolyl hydroxylase inhibitor, originally developed by FibroGen, that is undergoing development for the treatment of anemia. PDH inhibitor FG-2216 was orally bioavailable and induced significant and reversible EPO induction in vivo. Chronic oral dosing in male rhesus macaques was well tolerated, significantly increased erythropoiesis, and prevented anemia induced by weekly phlebotomy. Furthermore, modest increases in HbF-containing red cells and reticulocytes were demonstrated by flow cytometry. FG 2216 had been in phase II clinical trials for the treatment of anemia, however, all researchers on this drug candidate were discontinued.
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
179 μg/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21115615 |
20 mg/kg single, oral dose: 20 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
FG-2216 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3660 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21115615 |
20 mg/kg single, oral dose: 20 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
FG-2216 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
15.7 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21115615 |
20 mg/kg single, oral dose: 20 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
FG-2216 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
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DB08687
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6914666
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223387-75-5
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RU921DS4Z5
Created by
admin on Mon Mar 31 20:16:48 GMT 2025 , Edited by admin on Mon Mar 31 20:16:48 GMT 2025
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ACTIVE MOIETY
