CAS 112859-71-9: Fluasterone

Fluasterone is a synthetic, nonsteroidal compound that belongs to the class of selective androgen receptor modulators (SARMs). It has been shown to have anti-inflammatory properties as well as anabolic effects. Fluasterone is also able to bind to and activate the CB2 receptor. This drug has been shown to be effective in animal models for inflammatory bowel disease and skin tumor formation. Fluasterone has also been found to be metabolized by cytochrome P450 2C8 (CYP2C8) and CYP3A4 enzymes, which may lead to metabolic disorders such as diabetes mellitus and hypercholesterolemia. The drug has low potency due to its inability to bind effectively with the androgen receptor in target tissues.

Fluasterone, an NF-κB activation inhibitor, is used potentially for the treatment of metabolic syndrome.

Applications A synthetic derivative of Dehydroepiandrosterone. The reduced androgenicity of Fluasterone may obviate toxicities associated with the androgenicity of the parent compound. Antitumor agent. Used in clinical trials for prostate cancer prevention. References Bentley, P., et al.: Food Chem. Toxicol., 31, 857 (1993), Rao, K., et al.: Cancer Res., 59, 3084 (1999), Masuzaki, H., et al.: Science, 294, 2166 (2001), Osawa, E., et al.: Life Sci., 70, 2623 (2002),