Roxadustat

Overview

Roxadustat (Evrenzo) is a small-molecule HIF-prolyl-hydroxylase inhibitor — not a peptide — that raises endogenous erythropoietin. It is an approved anemia-of-CKD drug in China, Japan, and the EU, but the US FDA rejected it over safety signals. Because it boosts EPO and hemoglobin, it is diverted to the gray market for endurance doping and is WADA-prohibited at all times.

Mechanism of Action

Roxadustat inhibits HIF prolyl-hydroxylase (as a 2-oxoglutarate analog), preventing HIF-α degradation. Stabilized HIF (predominantly HIF-2α) induces endogenous erythropoietin and improves iron mobilization (hepcidin suppression), stimulating erythropoiesis without exogenous EPO (EMA product information).

Research Summary

Roxadustat is supported by extensive human data as an approved anemia drug (China 2018, Japan 2019–2020, EU 2021 as Evrenzo) with numerous Phase 2/3 CKD trials. The US FDA advisory committee voted against approval in July 2021, citing thrombosis, seizures, infections, and mortality signals. No validated recreational or performance dose exists. Not FDA-approved; not a peptide.

Reported Side Effects

• FDA advisory committee flagged increased thromboembolic events, seizures, major infections, and higher all-cause mortality — the basis for US non-approval
• A published case report describes roxadustat overdose toxicity in a CKD patient
• WADA-prohibited at all times (S2, HIF-activating agent) — raises hemoglobin like EPO
• No validated safe dose outside supervised CKD-anemia treatment

Compare Roxadustat with Others

Research References

• Pharmacokinetics of roxadustat: population analysis of 2855 CKD patients. 2021. PMID 33486718.
• Evrenzo (roxadustat) EPAR Product Information. European Medicines Agency. 2021.
• Roxadustat for CKD-related anemia rejected by FDA advisory panel. Kidney News 13(8). 2021.

Frequently asked questions

Has Roxadustat been independently lab-tested?

Disclosed Labs has collected 3 Certificates of Analysis (COA) for Roxadustat from 2 independent testing labs. 1 vendor has submitted material for testing. Products average 99.8% tested purity across the corpus. Full testing data is available at https://www.disclosedlabs.com/peptides/roxadustat/testing.

What is the average purity of Roxadustat on the market?

Based on 3 COAs analyzed by Disclosed Labs, Roxadustat products average 99.8% (±0.1%) tested purity. Individual vendor results vary; see per-vendor COA data at https://www.disclosedlabs.com/peptides/roxadustat/coas.

How does Roxadustat work?

Roxadustat inhibits HIF prolyl-hydroxylase (as a 2-oxoglutarate analog), preventing HIF-α degradation. Stabilized HIF (predominantly HIF-2α) induces endogenous erythropoietin and improves iron mobilization (hepcidin suppression), stimulating erythropoiesis without exogenous EPO (EMA product information).

What does the research say about Roxadustat?

Roxadustat is supported by extensive human data as an approved anemia drug (China 2018, Japan 2019–2020, EU 2021 as Evrenzo) with numerous Phase 2/3 CKD trials. The US FDA advisory committee voted against approval in July 2021, citing thrombosis, seizures, infections, and mortality signals. No validated recreational or performance dose exists. Not FDA-approved; not a peptide.