While other drugs of this type (sitaxentan, ambrisentan) exploit the vasoconstrictive properties of endothelin and are mainly used for the treatment of pulmonary arterial hypertension, atrasentan blocks endothelin induced cell proliferation.

[citation needed] Atrasentan failed a phase 3 trial for prostate cancer in patients unresponsive to hormone therapy.

Patients in the 1.25 mg dose group had increased weight gain which was presumably due to increased edema and had to withdraw from the study more than the placebo or 0.75 mg dose group.

[6] Reductions in proteinuria have been associated with beneficial patient outcomes in diabetic kidney disease with other interventions but is not an accepted end-point by the FDA.

[8] In 2024, the phase 3 ALIGN trial found atrasentan to be effective in reducing proteinuria in patients with IgA nephropathy.