CS-3150 (esaxerenone (r-INN))

CS-3150 (esaxerenone) is an oral, non-steroidal, selective antagonist of 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 2 diabetic patients with nephropathy. As a non-steroidal, selective MR antagonist, CS-3150 may have the potential for the treatment of hypertension and congestive heart failure, and may provide protection from end organ damage due to vascular complications.

CS-3150 is one of the compounds identified during Exelixis’ research collaboration with Daiichi Sankyo, which the companies entered into in March 2006. Under the terms of the agreement, Exelixis granted Daiichi Sankyo an exclusive, worldwide license to certain intellectual property primarily relating to compounds that modulate MR. In exchange, Exelixis received a $20 million upfront payment, research funding for a joint research period, and the potential for substantial clinical development, regulatory and commercialization milestone payments, as well as double-digit royalties on sales. Since the conclusion of the joint research period in November 2007, Daiichi Sankyo has been responsible for all subsequent preclinical and clinical development, and will also oversee regulatory, manufacturing and commercialization activities for the compound.

In September 2016, Daiichi Sankyo announced it is undertaking a phase 3 clinical development program to evaluate CS-3150 as a treatment for essential hypertension in Japanese patients. In addition to a phase 3 pivotal trial, ESAX-HTN, Daiichi Sankyo is sponsoring six smaller phase 3 clinical trials of CS-3150 in specific populations of patients with hypertension, either as monotherapy or in combination with other therapies used to treat the condition. For more information on the clinical trial program for CS-3150, please visit www.clinicaltrials.gov.