Selective Estrogen Receptor Modulators

Name
Selective Estrogen Receptor Modulators
Accession Number
DBCAT000918
Description

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)

ATC Classification
Drugs
DrugDrug Description
RaloxifeneA 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.
BazedoxifeneA selective estrogen receptor modulator (SERM) used to treat moderate to severe vasomotor symptoms in menopause and osteoporosis alone or in combination with conjugated estrogens.
ToremifeneA first generation nonsteroidal selective estrogen receptor modulator used to treat certain breast cancers.
TamoxifenA 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.
ClomifeneA medication used to induce ovulation.
AfimoxifeneFor the potential treatment of menstrual-cycle related mastalgia, fibrocystic breast disease, breast disease, gynecomastia and Keloid scarring.
EnclomipheneNot Annotated
OspemifeneA non-hormonal estrogen receptor modulator (SERM) used to treat moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause.
LasofoxifeneInvestigated 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...
OrmeloxifeneA selective estrogen receptor modulator used as a non-hormonal, non-steroidal oral contraceptive.
CyclofenilNot Annotated
FulvestrantAn estrogen receptor antagonist used to treat HR+ breast cancer that may also be HER2-.
Drugs & Drug Targets
DrugTargetType
RaloxifeneEstrogen receptor alphatarget
RaloxifeneEstrogen receptor betatarget
RaloxifeneAldehyde oxidaseenzyme
RaloxifeneCytochrome P450 2C8enzyme
RaloxifeneCytochrome P450 2B6enzyme
RaloxifeneCytochrome P450 19A1enzyme
RaloxifeneCytochrome P450 3A4enzyme
RaloxifeneSerpin B9target
RaloxifeneTrefoil factor 1target
RaloxifeneUDP-glucuronosyltransferase 1-1enzyme
RaloxifeneSerum albumincarrier
RaloxifeneAlpha-1-acid glycoprotein 1carrier
RaloxifeneSolute carrier organic anion transporter family member 1B1transporter
RaloxifeneSolute carrier organic anion transporter family member 1B3transporter
RaloxifeneP-glycoprotein 1transporter
RaloxifeneATP-binding cassette sub-family G member 2transporter
RaloxifeneCanalicular multispecific organic anion transporter 1transporter
RaloxifeneCanalicular multispecific organic anion transporter 2transporter
RaloxifeneMultidrug resistance-associated protein 4transporter
RaloxifeneUDP-glucuronosyltransferase 1-10enzyme
RaloxifeneUDP-glucuronosyltransferase 1-8enzyme
BazedoxifeneEstrogen receptor alphatarget
BazedoxifeneUDP-glucuronosyltransferase 1-4enzyme
BazedoxifeneEstrogen receptor betatarget
BazedoxifeneUDP-glucuronosyltransferase 1-8enzyme
BazedoxifeneUDP-glucuronosyltransferase 1-10enzyme
ToremifeneEstrogen receptor alphatarget
ToremifeneCytochrome P450 3A4enzyme
ToremifeneP-glycoprotein 1transporter
ToremifeneCytochrome P450 1A1enzyme
ToremifeneSex hormone-binding globulintarget
TamoxifenEstrogen receptor alphatarget
TamoxifenEstrogen receptor betatarget
TamoxifenCytochrome P450 2C9enzyme
TamoxifenCytochrome P450 3A4enzyme
TamoxifenCytochrome P450 2D6enzyme
TamoxifenCytochrome P450 2C8enzyme
TamoxifenCytochrome P450 2B6enzyme
TamoxifenLiver carboxylesterase 1enzyme
TamoxifenCytochrome P450 3A5enzyme
TamoxifenCytochrome P450 1A1enzyme
TamoxifenCytochrome P450 1B1enzyme
TamoxifenCytochrome P450 2C19enzyme
TamoxifenDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
TamoxifenDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
TamoxifenCytochrome P450 3A7enzyme
TamoxifenP-glycoprotein 1transporter
TamoxifenATP-binding cassette sub-family G member 2transporter
TamoxifenCytochrome P450 19A1enzyme
TamoxifenCytochrome P450 2A6enzyme
TamoxifenCytochrome P450 2E1enzyme
TamoxifenUDP-glucuronosyltransferase 1-10enzyme
TamoxifenSulfotransferase 1A1enzyme
TamoxifenCanalicular multispecific organic anion transporter 1transporter
Tamoxifen3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerasetarget
TamoxifenProtein kinase Ctarget
TamoxifenAndrogen receptortarget
TamoxifenPotassium voltage-gated channel subfamily H member 2target
TamoxifenNuclear receptor subfamily 1 group I member 2target
TamoxifenEstrogen-related receptor gammatarget
TamoxifenSex hormone-binding globulintarget
TamoxifenBile salt export pumptransporter
TamoxifenThyroxine-binding globulincarrier
TamoxifenBile salt sulfotransferaseenzyme
TamoxifenCytochrome P450 1A2enzyme
TamoxifenUDP-glucuronosyltransferase 2B7enzyme
TamoxifenUDP-glucuronosyltransferase 2B17enzyme
TamoxifenEstrogen sulfotransferaseenzyme
TamoxifenATP-binding cassette sub-family A member 1transporter
TamoxifenMitogen-activated protein kinase 8target
TamoxifenSerum albumincarrier
ClomifeneEstrogen receptor alphatarget
ClomifeneP-glycoprotein 1transporter
ClomifeneSex hormone-binding globulintarget
ClomifeneSteroid 17-alpha-hydroxylase/17,20 lyaseenzyme
AfimoxifeneEstrogen receptor alphatarget
AfimoxifeneEstrogen receptor betatarget
AfimoxifeneEstrogen-related receptor gammatarget
AfimoxifeneTrefoil factor 1target
AfimoxifeneSteroid hormone receptor ERR1target
AfimoxifeneNuclear receptor subfamily 1 group I member 2target
AfimoxifeneSex hormone-binding globulintarget
EnclomipheneCytochrome P450 2D6enzyme
OspemifeneEstrogen receptor alphatarget
OspemifeneCytochrome P450 3A4enzyme
OspemifeneCytochrome P450 2C9enzyme
OspemifeneCytochrome P450 2C19enzyme
OspemifeneCytochrome P450 2B6enzyme
OspemifeneCytochrome P450 2D6enzyme
LasofoxifeneEstrogen receptor alphatarget
LasofoxifeneEstrogen receptor betatarget
LasofoxifeneCannabinoid receptor 2target
OrmeloxifeneEstrogen receptor alphatarget
OrmeloxifeneEstrogen receptor betatarget
OrmeloxifeneSerum albumincarrier
FulvestrantEstrogen receptor alphatarget
FulvestrantCytochrome P450 3A4enzyme
FulvestrantUDP-glucuronosyltransferase 1-1enzyme