RO0488071

RO0488071 is a potent, selective small molecule inhibitor of 2,3-oxidosqualene cyclase (OSC), also known as lanosterol synthase (LSS). This enzyme catalyzes the cyclization of 2,3-oxidosqualene to lanosterol, a key step in the cholesterol biosynthesis pathway downstream of HMG-CoA reductase. By targeting this specific step, RO0488071 aims to inhibit cholesterol production without the side effects typically associated with statins, such as the depletion of non-sterol isoprenoids. Developed by Roche, the compound has demonstrated significant anti-tumor activity in preclinical models of drug-resistant ovarian cancer, where it reduces cell viability and suppresses xenograft growth. It has also been observed to upregulate estrogen receptor β (ERβ) expression, suggesting potential for combination therapies with ERβ agonists.

Other names

4′-[6-(Allylmethylamino)hexyloxy]-4-bromo-2′-fluorobenzophenone fumarate