Drug Name | Mechanism of action | Chemical formula | History | Applications |
Tamoxifen | It is metabolized in the liver by the cytochrome p450 isoform CYP2D6 and CYP3A4 into active metabolites such as 4-hydroxytamoxifen and N-desmethyl-4-hydroxytamoxifen.which have 30 - 100 times more affinity with the estrogen receptor than tamoxifen itself. | C26H29NO | Discover in 1967 most important drug need for basic health system. | Tamoxifen is currently used for the treatment of both early and advanced ER+ (estrogen receptor positive) breast cancer in pre- and post-menopausal women. |
Fulvestrant | When fulvestrant binds to estrogen receptor monomers it inhibits receptor dimerization, activating function 1 (AF1) and AF2 are rendered inactive, translocation of receptor to the nucleus is reduced, and degradation of the estrogen receptor is accelerated. | C32H47F5O3S | Fulvestrant is another antiestrogen, and is the only pure antiestrogen, or silent 4 KB (380 words)-16:12, 21 January 2016 | It is indicated for the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women. |
Aromatase inhibitors | Aromatase inhibitors work by inhibiting the action of the enzyme aromatase, which converts androgens into estrogens by a process called aromatization. | C17-H11-N5 | The commercial names and year of approval in the United States are: letrozole (Femara, 1995). | Used in the treatment of breast cancer and ovarian cancer in postmenopa-usal women and gynecomastia in men. |
Raloxifene | Enter the nucleus of the target organ cells in order to bind there to a series of unoccupied, inactive proteins, called ER. | C28H27NO4S | Tumor registry and membership files identify women diagnosed with breast cancer after 1994 who were health plan members in 1998 or later, when raloxifene became available | Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women. |