Atrasentan Hydrochloride is the hydrochloride salt of atrasentan, a selective endothelin type A (ETA) receptor antagonist. Atrasentan selectively blocks the ETA receptor and is used as an active pharmaceutical ingredient in pharmaceutical formulations. FDA identifies atrasentan as an ETA receptor antagonist with high selectivity for ETA over the endothelin type B receptor.
Atrasentan Hydrochloride is identified by CAS No. 195733-43-8, molecular formula C₂₉H₃₈N₂O₆·HCl, and molecular weight 547.09 g/mol. FDA describes the material as a slightly hygroscopic white to off-white powder and slightly soluble in water.
FDA's substance database confirms that Atrasentan is the active moiety and Atrasentan Hydrochloride is its salt/solvate form.
Atrasentan is an orally active selective ETA receptor antagonist. The current U.S. approved product VANRAFIA contains atrasentan and is indicated to reduce proteinuria in adults with primary IgA nephropathy who are at risk of rapid disease progression.
Potential pharmaceutical applications include:
Atrasentan selectively antagonizes the endothelin type A (ETA) receptor. FDA reports a very high affinity for ETA and greater than 1800-fold selectivity compared with the endothelin type B receptor.
Atrasentan Hydrochloride is a slightly hygroscopic white to off-white powder and is slightly soluble in water.
Atrasentan Hydrochloride API should be manufactured and tested according to the applicable approved pharmaceutical specification, with appropriate controls for identity, assay, related substances, residual solvents, water content and elemental impurities.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white, slightly hygroscopic powder |
| Identification | Conforms to identification tests for Atrasentan Hydrochloride |
| Assay (HPLC) | As per approved product specification |
| Solubility | Slightly soluble in water |