Compounds which inhibit or antagonize the biosynthesis or action of estradiol.
DrugDrug NameDrug Indication
DB00357AminoglutethimideFor the suppression of adrenal function in selected patients with Cushing's syndrome, malignant neoplasm of the female breast, and carcinoma in situ of the breast.
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.
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.
DB00947FulvestrantFor the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy.
DB00990ExemestaneFor the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.
DB01006LetrozoleFor the extended adjuvant treatment of early breast cancer in postmenopausal women who have received 5 years of adjuvant tamoxifen therapy. Also for first-line treatment of postmenopausal women with hormone receptor positive or hormone receptor unknown locally advanced or metastatic breast cancer. Also indicated for the treatment of advanced breast cancer in postmenopausal women with disease progression following antiestrogen therapy.
DB01217AnastrozoleFor adjuvant treatment of hormone receptor positive breast cancer , as well as hormonal treatment of advanced breast cancer in post-menopausal women. Has also been used to treat pubertal gynecomastia and McCune-Albright syndrome; however, manufacturer states that efficacy for these indications have not been established.
DB01406DanazolFor the treatment of endometriosis and fibrocystic breast disease (in patients unresponsive to simple measures). Also used for the prophylactic treatment of all types of hereditary angioedema in males and females.
DB03467NaringeninNot Available
DB04468AfimoxifeneFor the potential treatment of menstrual-cycle related mastalgia, fibrocystic breast disease, breast disease, gynecomastia and Keloid scarring.
DB06735EnclomipheneNot Available
DB06789Hydroxyprogesterone caproateHydroxyprogesterone caproate is indicated for the prevention of spontaneous preterm births in singleton pregnancies in women who have previously had a spontaneous preterm birth. (1)
DB08905FormestaneFor the treatment of estrogen-receptor positive breast cancer in post-menopausal women.
DrugDrug NameTargetType
DB00357AminoglutethimideCytochrome P450 19A1target
DB00357AminoglutethimideCytochrome P450 1A2enzyme
DB00357AminoglutethimideCytochrome P450 2C19enzyme
DB00357AminoglutethimideCytochrome P450 3A4enzyme
DB00357AminoglutethimideCholesterol side-chain cleavage enzyme, mitochondrialtarget
DB00481RaloxifeneEstrogen receptortarget
DB00481RaloxifeneEstrogen receptor betatarget
DB00481RaloxifeneAldehyde oxidaseenzyme
DB00481RaloxifeneCytochrome P450 2C8enzyme
DB00481RaloxifeneCytochrome P450 2B6enzyme
DB00481RaloxifeneCytochrome P450 19A1enzyme
DB00481RaloxifeneCytochrome P450 3A4enzyme
DB00675TamoxifenEstrogen receptortarget
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 1-4enzyme
DB00675TamoxifenSulfotransferase 1A1enzyme
DB00675TamoxifenCanalicular multispecific organic anion transporter 1transporter
DB00675Tamoxifen3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerasetarget
DB00675TamoxifenProtein kinase Ctarget
DB00882ClomifeneEstrogen receptortarget
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
DB00947FulvestrantEstrogen receptortarget
DB00947FulvestrantCytochrome P450 3A4enzyme
DB00990ExemestaneCytochrome P450 19A1target
DB00990ExemestaneCytochrome P450 3A4enzyme
DB00990ExemestaneCytochrome P450 19A1enzyme
DB01006LetrozoleCytochrome P450 19A1target
DB01006LetrozoleCytochrome P450 3A4enzyme
DB01006LetrozoleCytochrome P450 2A6enzyme
DB01006LetrozoleCytochrome P450 19A1enzyme
DB01217AnastrozoleCytochrome P450 19A1target
DB01217AnastrozoleCytochrome P450 19A1enzyme
DB01217AnastrozoleCytochrome P450 1A2enzyme
DB01217AnastrozoleCytochrome P450 2C9enzyme
DB01217AnastrozoleCytochrome P450 3A4enzyme
DB01406DanazolEstrogen receptortarget
DB01406DanazolGonadotropin-releasing hormone receptortarget
DB01406DanazolPutative gonadotropin-releasing hormone II receptortarget
DB01406DanazolSex hormone-binding globulincarrier
DB01406DanazolC-C motif chemokine 2target
DB01406DanazolCytochrome P450 19A1enzyme
DB01406DanazolAndrogen receptortarget
DB01406DanazolProgesterone receptortarget
DB01406DanazolCytochrome P450 3A4enzyme
DB03467NaringeninSolute carrier organic anion transporter family member 2B1transporter
DB03467NaringeninMultidrug resistance protein 1transporter
DB03467NaringeninMultidrug resistance-associated protein 1transporter
DB03467NaringeninATP-binding cassette sub-family G member 2transporter
DB03467NaringeninHTH-type transcriptional regulator TtgRtarget
DB04468AfimoxifeneEstrogen receptortarget
DB04468AfimoxifeneEstrogen receptor betatarget
DB04468AfimoxifeneEstrogen-related receptor gammatarget
DB06735EnclomipheneCytochrome P450 2D6enzyme
DB06789Hydroxyprogesterone caproateProgesterone receptortarget
DB06789Hydroxyprogesterone caproateCytochrome P450 3A4enzyme
DB06789Hydroxyprogesterone caproateCytochrome P450 3A5enzyme
DB06789Hydroxyprogesterone caproateCytochrome P450 2C19enzyme