What is the difference between GW-0742 and Roxadustat?

GW-0742: GW-0742 is a synthetic small-molecule PPARδ (PPAR-beta/delta) agonist developed by GlaxoSmithKline as a phenoxyacetic-acid/thiazole derivative—not a peptide or hormone. It exhibits ~1000-fold selectiv... Roxadustat: Roxadustat (Evrenzo) is a small-molecule HIF-prolyl-hydroxylase inhibitor — not a peptide — that raises endogenous erythropoietin. It is an approved prescription drug for anemia of chronic kidney dise...

What does the research say about GW-0742 vs Roxadustat?

GW-0742: No human efficacy or safety data exist; the only identified human exposure is a single 15 mg oral dose administered to volunteers solely to characterize urinary metabolites for an anti-doping detection assay—a bioanalytical study yielding no therapeutic or safety information. Preclinical rodent findings include: oral GW-0742 (30 mg/kg/day × 3 weeks… 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…

GW-0742 vs Roxadustat

Q: Can you stack GW-0742 and Roxadustat?

GW-0742 (metabolic) and Roxadustat (metabolic) are in the same category and may have overlapping mechanisms — researchers should review both profiles carefully before combining. Consult a licensed provider before combining any compounds.

Head-to-head comparison of GW-0742 and Roxadustat — mechanism, side effects, legal status, and pricing.

GW-0742

GW-0742 is a synthetic small-molecule PPARδ (PPAR-beta/delta) agonist developed by GlaxoSmithKline as a phenoxyacetic-acid/thiazole derivative—not a peptide or hormone. It exhibits ~1000-fold selectivity for human PPARδ (EC50 = 1.1 nM) over PPARα and PPARγ. Never advanced past preclinical development, GW-0742 has no approved human therapeutic use and no registered clinical trials. It is prohibited at all times under WADA as a member of the banned PPARδ-agonist class (Hormone and Metabolic Modulators), though not individually named on the list.

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Roxadustat

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

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GW-0742

Roxadustat

Category

Metabolic

Legal Status

Research Only

Mechanism

GW-0742 is a high-affinity, highly selective agonist of human PPARδ (EC50 = 1.1 nM for hPPARδ transactivation vs ~1.1 µM for hPPARα and ~2 µM for hPPARγ), conferring ~1000-fold selectivity for PPARδ over the other PPAR subtypes. Upon activation, PPARδ heterodimerizes with RXR and binds PPAR-response elements (PPREs) to alter transcription of genes governing fatty-acid oxidation, glucose utilization, and inflammatory signaling. In mice, however, GW-0742-induced hepatomegaly, hepatic/skeletal-muscle peroxisome proliferation, and skeletal myopathy were shown to be predominantly mediated by off-target PPARα cross-activation rather than PPARδ—a mechanism-based toxicity concern at animal-study exposures.

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

Side Effects

Hepatomegaly (liver enlargement) observed in mice
Hepatic and skeletal-muscle peroxisome proliferation (mouse studies)
Skeletal myopathy driven by off-target PPARα cross-activation (mouse studies)
No human safety data beyond single-dose bioanalytical exposure

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GW-0742

Best $/mg

$0.058/mg

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Roxadustat

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Lab Verification

COA corpus from Disclosed Labs — independently tested batches only.

GW-0742

COAs

99.6%

Avg purity

Labs

Full testing data

Roxadustat

COAs

99.8%

Avg purity

Labs

Full testing data

GW-0742 Research Summary

No human efficacy or safety data exist; the only identified human exposure is a single 15 mg oral dose administered to volunteers solely to characterize urinary metabolites for an anti-doping detection assay—a bioanalytical study yielding no therapeutic or safety information. Preclinical rodent findings include: oral GW-0742 (30 mg/kg/day × 3 weeks) reduced right ventricular hypertrophy and systolic pressure in rats with chronic hypoxia-induced pulmonary hypertension but did not prevent pulmonary vascular remodeling; intraperitoneal GW-0742 (0.1 mg/kg) improved survival and reduced intestinal injury, leukocyte activation, cytokines, and apoptosis markers in a mouse gut ischemia/reperfusion model; and GW-0742 ameliorated hepatic steatosis, ER stress, and lung inflammation in various mouse models. Critically, mouse studies also demonstrated hepatomegaly, hepatic/skeletal-muscle peroxisome proliferation, and skeletal myopathy driven predominantly by off-target PPARα cross-activation, indicating mechanism-based toxicity risk.

Key references

Roxadustat 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.

Key references

Can you stack GW-0742 and Roxadustat?

GW-0742 and Roxadustat are both in the Metabolic category and may have overlapping mechanisms. Researchers should review both profiles carefully, understand the mechanisms of action, and monitor the relevant biomarkers when combining compounds in the same class. As always, consult a licensed healthcare provider before making any decisions about combining research compounds.

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This platform provides informational tools only, not medical advice. This comparison is for educational purposes only. Consult a licensed provider.