Arzoxifene

Arzoxifene

Arzoxifene is a Selective estrogen receptor modulator (SERM) that was under development for the treatment and prevention of osteoporosis, breast cancer, and endometrial cancer. It was developed by Eli Lilly and Company, but its development was discontinued in 2009.

History

Arzoxifene was first synthesized in the 1980s by Eli Lilly and Company. It was part of a new class of drugs known as Selective estrogen receptor modulators (SERMs), which were designed to provide the beneficial effects of estrogen without its potential side effects.

Pharmacology

Arzoxifene acts as an antagonist at estrogen receptors in certain tissues such as the breast and uterus, but as an agonist at estrogen receptors in other tissues such as bone and lipid metabolism. This selective action is what gives SERMs their unique therapeutic potential.

Clinical trials

Arzoxifene entered clinical trials in the 1990s. It was tested for the treatment and prevention of osteoporosis, breast cancer, and endometrial cancer. However, in 2009, Eli Lilly announced that it was discontinuing the development of arzoxifene, despite the drug having reached phase III clinical trials.

Potential uses

Despite its development being discontinued, arzoxifene has shown potential in several areas. It has been found to reduce the risk of vertebral fracture in postmenopausal women with osteoporosis. It has also shown promise in the treatment of breast cancer, with studies indicating that it may reduce the risk of invasive breast cancer in postmenopausal women.

See also

• Selective estrogen receptor modulator
• Osteoporosis
• Breast cancer
• Endometrial cancer