A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63)
DrugDrug NameDrug Indication
DB00481RaloxifeneFor the prevention and treatment of osteoporosis in post-menopausal women, as well as prevention and treatment of corticosteroid-induced bone loss. Also for the reduction in the incidence of invasive breast cancer in postmenopausal women with osteoporosis or have a high risk for developing breast cancer.
DB06401BazedoxifeneInvestigated for use/treatment in osteoporosis and menopause.
DB00539ToremifeneFor the treatment of metastatic breast cancer in postmenopausal women with estrogen receptor-positive or receptor-unknown tumors. Toremifene is currently under investigation as a preventative agent for prostate cancer in men with high-grade prostatic intraepithelial neoplasia and no evidence of prostate cancer.
DB00675TamoxifenTamoxifen is indicated for the treatment of metastatic breast cancer in women and men and ductal carcinoma in Situ.
DB00882ClomifeneUsed mainly in female infertility due to anovulation (e.g. due to polycystic ovary syndrome) to induce ovulation.
DB04468AfimoxifeneFor the potential treatment of menstrual-cycle related mastalgia, fibrocystic breast disease, breast disease, gynecomastia and Keloid scarring.
DB06735EnclomipheneNot Available
DB04938OspemifeneOspemifene is used for the treatment of moderate to dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause.
DB06202LasofoxifeneInvestigated for use/treatment in postmenopausal osteoporosis to reduce the risk of both vertebral and novertebral fractures, as well as address other postmenopausal conditions, including reduction in risk of breast cancer and treatment of vulvar and vaginal atrophy (VVA)
DrugDrug NameTargetType
DB00481RaloxifeneEstrogen receptor alphatarget
DB00481RaloxifeneEstrogen receptor betatarget
DB00481RaloxifeneAldehyde oxidaseenzyme
DB00481RaloxifeneCytochrome P450 2C8enzyme
DB00481RaloxifeneCytochrome P450 2B6enzyme
DB00481RaloxifeneCytochrome P450 19A1enzyme
DB00481RaloxifeneCytochrome P450 3A4enzyme
DB00481RaloxifeneSerpin B9target
DB00481RaloxifeneTrefoil factor 1target
DB00539ToremifeneEstrogen receptor alphatarget
DB00539ToremifeneCytochrome P450 3A4enzyme
DB00539ToremifeneMultidrug resistance protein 1transporter
DB00539ToremifeneCytochrome P450 1A1enzyme
DB00539ToremifeneCytochrome P450 1A2enzyme
DB00539ToremifeneSex hormone-binding globulintarget
DB00675TamoxifenEstrogen receptor alphatarget
DB00675TamoxifenEstrogen receptor betatarget
DB00675TamoxifenCytochrome P450 2C9enzyme
DB00675TamoxifenCytochrome P450 3A4enzyme
DB00675TamoxifenCytochrome P450 2D6enzyme
DB00675TamoxifenCytochrome P450 2C8enzyme
DB00675TamoxifenCytochrome P450 2B6enzyme
DB00675TamoxifenLiver carboxylesterase 1enzyme
DB00675TamoxifenCytochrome P450 3A5enzyme
DB00675TamoxifenCytochrome P450 1A1enzyme
DB00675TamoxifenCytochrome P450 1A2enzyme
DB00675TamoxifenCytochrome P450 1B1enzyme
DB00675TamoxifenCytochrome P450 2C19enzyme
DB00675TamoxifenDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
DB00675TamoxifenDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB00675TamoxifenCytochrome P450 3A7enzyme
DB00675TamoxifenMultidrug resistance protein 1transporter
DB00675TamoxifenBile salt export pumptransporter
DB00675TamoxifenATP-binding cassette sub-family G member 2transporter
DB00675TamoxifenCytochrome P450 19A1enzyme
DB00675TamoxifenCytochrome P450 2A6enzyme
DB00675TamoxifenCytochrome P450 2E1enzyme
DB00675TamoxifenUDP-glucuronosyltransferase 1-10enzyme
DB00675TamoxifenSulfotransferase 1A1enzyme
DB00675TamoxifenCanalicular multispecific organic anion transporter 1transporter
DB00675Tamoxifen3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerasetarget
DB00675TamoxifenProtein kinase Ctarget
DB00675TamoxifenAndrogen receptortarget
DB00675TamoxifenPotassium voltage-gated channel subfamily H member 2target
DB00675TamoxifenNuclear receptor subfamily 1 group I member 2target
DB00675TamoxifenEstrogen-related receptor gammatarget
DB00675TamoxifenSex hormone-binding globulintarget
DB00882ClomifeneEstrogen receptor alphatarget
DB00882ClomifeneMultidrug resistance protein 1transporter
DB00882ClomifeneCholesterol side-chain cleavage enzyme, mitochondrialenzyme
DB00882ClomifeneCytochrome P450 19A1enzyme
DB00882ClomifeneCytochrome P450 1A1enzyme
DB00882ClomifeneCytochrome P450 1A2enzyme
DB00882ClomifeneCytochrome P450 2A6enzyme
DB00882ClomifeneCytochrome P450 2E1enzyme
DB00882ClomifeneCytochrome P450 3A4enzyme
DB00882ClomifeneSex hormone-binding globulintarget
DB04468AfimoxifeneEstrogen receptor alphatarget
DB04468AfimoxifeneEstrogen receptor betatarget
DB04468AfimoxifeneEstrogen-related receptor gammatarget
DB04468AfimoxifeneTrefoil factor 1target
DB04468AfimoxifeneSteroid hormone receptor ERR1target
DB04468AfimoxifeneNuclear receptor subfamily 1 group I member 2target
DB04468AfimoxifeneSex hormone-binding globulintarget
DB04938OspemifeneEstrogen receptor alphatarget
DB04938OspemifeneCytochrome P450 3A4enzyme
DB04938OspemifeneCytochrome P450 2C9enzyme
DB04938OspemifeneCytochrome P450 2C19enzyme
DB04938OspemifeneCytochrome P450 2B6enzyme
DB04938OspemifeneCytochrome P450 2D6enzyme
DB06202LasofoxifeneEstrogen receptor alphatarget
DB06202LasofoxifeneEstrogen receptor betatarget
DB06202LasofoxifeneCannabinoid receptor 2target
DB06401BazedoxifeneEstrogen receptor alphatarget
DB06401BazedoxifeneUDP-glucuronosyltransferase 1A1enzyme
DB06401BazedoxifeneEstrogen receptor betatarget
DB06735EnclomipheneCytochrome P450 2D6enzyme