Lasofoxifene

Selective estrogen receptor modulator

Lasofoxifene
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Lasofoxifene is a non-steroidal selective estrogen receptor modulator (SERM) that is used in the treatment of osteoporosis and other conditions related to estrogen deficiency. It is known for its ability to mimic the effects of estrogen in certain tissues while blocking its effects in others, making it a valuable therapeutic agent in postmenopausal women.

Pharmacology

Lasofoxifene acts as an agonist on estrogen receptors in bone and the cardiovascular system, promoting bone density and cardiovascular health. Conversely, it acts as an antagonist in breast and uterine tissues, reducing the risk of breast cancer and endometrial cancer. This dual action is characteristic of SERMs, which are designed to provide the beneficial effects of estrogen while minimizing the risks associated with hormone replacement therapy.

Clinical Uses

Lasofoxifene is primarily used for the prevention and treatment of osteoporosis in postmenopausal women. Osteoporosis is a condition characterized by decreased bone mass and increased fracture risk. By acting on estrogen receptors in bone tissue, lasofoxifene helps to maintain bone density and reduce the incidence of fractures.

Mechanism of Action

Chemical structure of Lasofoxifene

Lasofoxifene binds to estrogen receptors, altering their conformation and modulating the transcription of estrogen-responsive genes. This modulation results in tissue-specific effects, with agonistic activity in bone and cardiovascular tissues and antagonistic activity in breast and uterine tissues. The precise mechanism involves the recruitment of coactivators and corepressors that influence gene expression.

Side Effects

Common side effects of lasofoxifene include hot flashes, leg cramps, and an increased risk of venous thromboembolism. These side effects are similar to those observed with other SERMs and are related to its estrogenic and anti-estrogenic activities in different tissues.

Development and Approval

Lasofoxifene was developed as part of a class of drugs aimed at providing the benefits of estrogen without the associated risks. It has undergone extensive clinical trials to evaluate its efficacy and safety in the treatment of osteoporosis and other estrogen-related conditions.

Related pages

• Selective estrogen receptor modulator
• Osteoporosis
• Breast cancer
• Hormone replacement therapy