Droloxifene

Overview of the drug Droloxifene

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

Droloxifene is a selective estrogen receptor modulator (SERM) that has been studied for its potential use in the treatment of breast cancer and osteoporosis. It is a nonsteroidal compound that exhibits both estrogenic and antiestrogenic properties depending on the target tissue.

Pharmacology

Droloxifene acts by binding to estrogen receptors in various tissues. In breast tissue, it functions as an antiestrogen, blocking the proliferative actions of estrogen and thereby inhibiting the growth of estrogen-dependent tumors. Conversely, in bone tissue, droloxifene acts as an estrogen agonist, helping to maintain bone density and reduce the risk of fractures.

Mechanism of Action

Droloxifene's mechanism of action involves its interaction with estrogen receptors, which are nuclear hormone receptors. Upon binding to these receptors, droloxifene can modulate the transcription of estrogen-responsive genes. This dual action is what classifies it as a selective estrogen receptor modulator.

Clinical Applications

Droloxifene has been primarily investigated for its role in the management of breast cancer. Its ability to act as an antiestrogen in breast tissue makes it a candidate for reducing the risk of cancer recurrence in patients with estrogen receptor-positive tumors. Additionally, its bone-preserving effects have been explored for the prevention and treatment of osteoporosis in postmenopausal women.

Side Effects

As with other SERMs, droloxifene may cause side effects such as hot flashes, leg cramps, and an increased risk of thromboembolic events. The risk-benefit profile of droloxifene must be carefully considered in clinical settings.

Research and Development

Droloxifene has undergone various phases of clinical trials to evaluate its efficacy and safety. While promising results have been observed, further studies are needed to fully establish its therapeutic potential and to compare its effectiveness with other SERMs like tamoxifen and raloxifene.

Related pages

• Selective estrogen receptor modulator
• Breast cancer treatment
• Osteoporosis

• 

  Droloxifene