XL652

Development Status

A Phase 1 clinical trial evaluating the safety of XL652 is ongoing.

Description

XL652 is a novel small-molecule modulator of the Liver X Receptor (LXR), a nuclear hormone receptor implicated in a variety of cardiovascular and metabolic disorders. LXR plays a central role in lipid metabolism, and LXR modulators improve lipid profiles and shrink atherosclerotic plaques in preclinical models. LXR activation by synthetic agonists initiates a cascade of cellular events that both increase "reverse cholesterol transport," thereby removing excess cholesterol from the body, and suppress inflammation. LXR activation therefore directly targets two well-known risk factors for heart disease, and provides a novel approach for decreasing the deposition of fat and lipids in the artery wall and suppressing the inflammatory damage associated with atherosclerosis. LXR is a novel target for therapies to directly impact the pathology of atherosclerosis and coronary artery disease via a dual mechanism of reverse cholesterol transport and repression of inflammation.

Bristol-Myers Squibb Company has primary responsibility for the development and commercialization of XL652.