Levormeloxifene

Levormeloxifene is a selective estrogen receptor modulator (SERM) that was under development for the treatment and prevention of osteoporosis and breast cancer, but was discontinued due to the risk of serious side effects.

Chemistry

Levormeloxifene is a synthetic compound of the benzothiophene class. It is a nonsteroidal SERM, similar to raloxifene and tamoxifen, but differs in its specific chemical structure and binding affinity to estrogen receptors.

Pharmacology

Levormeloxifene acts as an agonist in bone and an antagonist in breast and uterine tissue. This tissue-selective action is what classifies levormeloxifene as a SERM. It has the potential to prevent bone loss and reduce the risk of breast cancer without stimulating the uterus, which can lead to uterine cancer.

Clinical trials

Levormeloxifene underwent Phase III clinical trials for the treatment of osteoporosis and breast cancer. However, the trials were halted due to an increased risk of venous thromboembolism and other serious side effects. Despite its potential benefits, the risks associated with levormeloxifene were deemed too high, leading to its discontinuation.

See also

• Selective estrogen receptor modulator
• Osteoporosis
• Breast cancer