The Sound of Evolution
Fulvestrant
Mechanism of action:
Fulvestrant is an estrogen receptor antagonist and also a selective estrogen receptor degrader. Fulvestrant has a higher binding affinity for the estrogen receptor than estradiol. It inhibits the binding of the estrogen receptor to estrogen response elements on DNA, thereby preventing the initiation of estrogen-related gene transcription. This reduces estrogen-dependent proliferation and survival signaling in breast cancer cells and can also induce apoptosis-related pathways.
Reference(s):
1. Kansra S et al. (2005). Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release. Mol Cell Endocrinol.
2. Kabos P et al. (2010). Fulvestrant: a unique antiendocrine agent for estrogen-sensitive breast cancer. Expert Opin Pharmacother.
3. Bross PF et al. (2002). FDA drug approval summaries: fulvestrant. Oncologist.