CS-3150 (XL550) is a small-molecule antagonist the mineralocorticoid receptor (MR), a nuclear hormone receptor implicated in a variety of cardiovascular and metabolic diseases. MR antagonists can be used to treat hypertension and congestive heart failure due to their vascular protective effects. Recent studies have also shown beneficial effects of adding MR antagonists to the treatment regimen for Type II diabetic patients with nephropathy. CS-3150 is a non-steroidal, selective MR antagonist that has the potential for the treatment of hypertension, congestive heart failure, or end organ protection due to vascular damage.
Exelixis discovered CS-3150 and out-licensed the compound to Daiichi-Sankyo. A phase 2 clinical trial in patients with hypertension was initiated by Daiichi-Sankyo in August 2012.