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Drug intelligence / Profile preview
atrasentan
- Development stage
- Approved
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Atrasentan is a selective endothelin A (ETA) receptor antagonist used to reduce proteinuria in adults with primary immunoglobulin A nephropathy (IgAN) at risk of rapid disease progression. It is an orally administered small molecule that works by blocking the ETA receptor, which plays a role in the pathogenesis of IgAN and other kidney diseases by mediating the effects of endothelin-1, a potent vasoconstrictor involved in inflammation and fibrosis. Atrasentan has demonstrated high selectivity for ETA over ETB receptors (>1800-fold). The drug was previously investigated for hormone-refractory prostate cancer under the brand name Xinlay but did not receive FDA approval for this indication. In April 2025, atrasentan (Vanrafia) was approved in the United States for reducing proteinuria in IgAN. It continues to be studied for other rare kidney diseases and certain cancers.
- Brand names
- VanrafiaXinlay
- Other names
- atrasentan
02
Targets
ABCG2 (Breast cancer resistance protein)EDNRA (Endothelin receptor type A)EDNRB (Endothelin receptor type B)ABCB1 (P-glycoprotein)
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