SAFETY INFORMATION
| Signal word | Warning |
|---|---|
| Pictogram(s) |
 Exclamation Mark Irritant GHS07 |
| GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation |
| Precautionary Statement Codes |
P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P270:Do not eat, drink or smoke when using this product. P280:Wear protective gloves/protective clothing/eye protection/face protection. P362:Take off contaminated clothing and wash before reuse. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P332+P313:IF SKIN irritation occurs: Get medical advice/attention. P337+P313:IF eye irritation persists: Get medical advice/attention. P405:Store locked up. P501:Dispose of contents/container to..… |
COMPUTED DESCRIPTORS
| Molecular Weight | 393.4 g/mol |
|---|---|
| XLogP3 | 2.5 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 5 |
| Exact Mass | 393.18998559 g/mol |
| Monoisotopic Mass | 393.18998559 g/mol |
| Topological Polar Surface Area | 124 Ų |
| Heavy Atom Count | 28 |
| Formal Charge | 0 |
| Complexity | 627 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently-Bonded Unit Count | 1 |
| Compound Is Canonicalized | Yes |
PRODUCT INTRODUCTION
description
Daprodustat is a small-molecule hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor. It was developed by GSK for the treatment of anemia in patients with chronic kidney disease (CKD). In patients with CKD, the diseased kidney cannot induce erythropoietin (EPO) production in response to hypoxia or anemia. As a potent inhibitor of PHD1, PHD2 and PHD3 (≥ 1000-fold selectivity), daprodustat leads to the stabilization of cellular HIF1α and HIF2α and the induction of erythropoiesis. A phase 3 clinical trial (NCT02879305) found that in patients with CKD undergoing dialysis, daprodustat was non-inferior to erythropoiesis-stimulating agents regarding the change in the hemoglobin level from baseline and cardiovascular outcomes. In June 2020, daprodustat was first approved in Japan for the treatment of renal anemia. Daprodustat is currently under EMA and FDA review. On October 2022, the FDA Cardiovascular and Renal Drugs Advisory Committee (CRDAC) supported that the benefit of treatment with daprodustat outweighs the risks for adult dialysis patients with anemia of CKD but not for non-dialysis patients with anemia of CKD.