Estrogen Antagonists

Compounds which inhibit or antagonize the biosynthesis or action of estradiol.
DrugDrug NameDrug Description
DB00357AminoglutethimideAn adrenocortical steroid synthesis inhibitor used in the treatment of Cushing's syndrome.
DB00481RaloxifeneA selective estrogen receptor modulator that is used to prevent and treat osteoporosis and reduce the risk of invasive breast cancer in high-risk postmenopausal women.
DB00675TamoxifenA selective estrogen receptor modulator used to treat estrogen receptor positive breast cancer, reduce the risk of invasive breast cancer following surgery, or reduce the risk of breast cancer in high risk women.
DB00882ClomifeneA medication used to induce ovulation.
DB00947FulvestrantAn estrogen receptor antagonist used to treat HR+ breast cancer that may also be HER2-.
DB00990ExemestaneAn aromatase inhibitor used to treat breast cancer in postmenopausal women after treatment with tamoxifen.
DB01006LetrozoleAn aromatase inhibitor used to treat breast cancer in postmenopausal women.
DB01217AnastrozoleA competitive, selective, non-steroidal aromatase inhibitor used as adjuvant therapy for the treatment of hormone receptor-positive breast cancer in postmenopausal women.
DB01406DanazolA synthetic steroid and pituitary gonadotropin inhibitor used in the treatment of endometriosis and symptomatic treatment of severe pain and tenderness associated with benign fibrocystic breasts.
DB03467NaringeninNot Available
DB04468AfimoxifeneFor the potential treatment of menstrual-cycle related mastalgia, fibrocystic breast disease, breast disease, gynecomastia and Keloid scarring.
DB06735EnclomipheneNot Annotated
DB06789Hydroxyprogesterone caproateA synthetic progestin used for the prevention of spontaneous preterm births in singleton pregnancies in women who have previously had a spontaneous preterm birth.
DB08905FormestaneFor the treatment of estrogen-receptor positive breast cancer in post-menopausal women.
DB13418MoxestrolNot Annotated
DB13767VorozoleNot Annotated
DB03860ICI-164384Not Available
DrugDrug NameTargetType
DB00357AminoglutethimideCytochrome P450 19A1target
DB00357AminoglutethimideCytochrome P450 2C19enzyme
DB00357AminoglutethimideCytochrome P450 3A4enzyme
DB00357AminoglutethimideCholesterol side-chain cleavage enzyme, mitochondrialtarget
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
DB00481RaloxifeneUDP-glucuronosyltransferase 1-1enzyme
DB00481RaloxifeneSerum albumincarrier
DB00481RaloxifeneAlpha-1-acid glycoprotein 1carrier
DB00481RaloxifeneSolute carrier organic anion transporter family member 1B1transporter
DB00481RaloxifeneSolute carrier organic anion transporter family member 1B3transporter
DB00481RaloxifeneP-glycoprotein 1transporter
DB00481RaloxifeneATP-binding cassette sub-family G member 2transporter
DB00481RaloxifeneCanalicular multispecific organic anion transporter 1transporter
DB00481RaloxifeneCanalicular multispecific organic anion transporter 2transporter
DB00481RaloxifeneMultidrug resistance-associated protein 4transporter
DB00481RaloxifeneUDP-glucuronosyltransferase 1-10enzyme
DB00481RaloxifeneUDP-glucuronosyltransferase 1-8enzyme
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 1B1enzyme
DB00675TamoxifenCytochrome P450 2C19enzyme
DB00675TamoxifenDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
DB00675TamoxifenDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB00675TamoxifenCytochrome P450 3A7enzyme
DB00675TamoxifenP-glycoprotein 1transporter
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
DB00675TamoxifenBile salt export pumptransporter
DB00675TamoxifenThyroxine-binding globulincarrier
DB00675TamoxifenBile salt sulfotransferaseenzyme
DB00675TamoxifenCytochrome P450 1A2enzyme
DB00675TamoxifenUDP-glucuronosyltransferase 2B7enzyme
DB00675TamoxifenUDP-glucuronosyltransferase 2B17enzyme
DB00675TamoxifenEstrogen sulfotransferaseenzyme
DB00675TamoxifenATP-binding cassette sub-family A member 1transporter
DB00675TamoxifenMitogen-activated protein kinase 8target
DB00675TamoxifenSerum albumincarrier
DB00882ClomifeneEstrogen receptor alphatarget
DB00882ClomifeneP-glycoprotein 1transporter
DB00882ClomifeneSex hormone-binding globulintarget
DB00882ClomifeneSteroid 17-alpha-hydroxylase/17,20 lyaseenzyme
DB00947FulvestrantEstrogen receptor alphatarget
DB00947FulvestrantCytochrome P450 3A4enzyme
DB00947FulvestrantUDP-glucuronosyltransferase 1-1enzyme
DB00990ExemestaneCytochrome P450 19A1target
DB00990ExemestaneCytochrome P450 3A4enzyme
DB00990ExemestaneCytochrome P450 19A1enzyme
DB01006LetrozoleCytochrome P450 19A1target
DB01006LetrozoleCytochrome P450 3A4enzyme
DB01006LetrozoleCytochrome P450 2A6enzyme
DB01006LetrozoleCytochrome P450 19A1enzyme
DB01006LetrozoleCytochrome P450 2C19enzyme
DB01006LetrozoleUDP-glucuronosyltransferase 2B7enzyme
DB01006LetrozoleSerum albumincarrier
DB01006LetrozoleP-glycoprotein 1transporter
DB01217AnastrozoleCytochrome P450 19A1target
DB01217AnastrozoleP-glycoprotein 1transporter
DB01217AnastrozoleCytochrome P450 3A4enzyme
DB01217AnastrozoleCytochrome P450 3A5enzyme
DB01217AnastrozoleCytochrome P450 2C8enzyme
DB01217AnastrozoleUDP-glucuronosyltransferase 1-4enzyme
DB01217AnastrozoleUDP-glucuronosyltransferase 1-3enzyme
DB01217AnastrozoleUDP-glucuronosyltransferase 2B7enzyme
DB01217AnastrozoleCytochrome P450 1A2enzyme
DB01217AnastrozoleCytochrome P450 2C9enzyme
DB01406DanazolEstrogen receptor alphatarget
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
DB03467NaringeninP-glycoprotein 1transporter
DB03467NaringeninMultidrug resistance-associated protein 1transporter
DB03467NaringeninATP-binding cassette sub-family G member 2transporter
DB03467NaringeninHTH-type transcriptional regulator TtgRtarget
DB03467NaringeninEstrogen receptor alphatarget
DB03467NaringeninAldo-keto reductase family 1 member C1target
DB03467NaringeninCytochrome P450 1B1target
DB03467NaringeninKAT8 regulatory NSL complex subunit 3target
DB03467NaringeninSex hormone-binding globulintarget
DB03467NaringeninCytochrome P450 19A1target
DB03467NaringeninEstrogen receptor betatarget
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
DB06735EnclomipheneCytochrome P450 2D6enzyme
DB06789Hydroxyprogesterone caproateProgesterone receptortarget
DB06789Hydroxyprogesterone caproateCytochrome P450 3A4enzyme
DB06789Hydroxyprogesterone caproateCytochrome P450 3A5enzyme
DB06789Hydroxyprogesterone caproateCytochrome P450 2C19enzyme
DB08905FormestaneCytochrome P450 3A4enzyme
DB03860ICI-164384Estrogen receptor betatarget