Hormone Antagonists and Related Agents

DrugDrug NameDrug Indication
DB00106AbarelixFor palliative treatment of advanced prostate cancer.
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.
DB00499FlutamideFor the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate
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.
DB00665NilutamideFor use in combination with surgical castration for the treatment of metastatic prostate cancer involving distant lymph nodes, bone, or visceral organs (Stage D2).
DB00675TamoxifenTamoxifen is indicated to treat estrogen receptor positive metastatic breast cancer in adults, as an adjuvant in the treatment of early stage estrogen receptor positive breast cancer in adults, to reduce the risk of invasive breast cancer after surgery and radiation in adult women with ductal carcinoma in situ.[L7802]
DB00947FulvestrantFor the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy, as monotherapy or in combination with other antineoplastic agents.
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.
DB01128BicalutamideFor treatment (together with surgery or LHRH analogue) of advanced prostatic cancer.
DB01217AnastrozoleAnastrozole is indicated as adjunct therapy in the treatment of hormone receptor-positive early breast cancer in postmenopausal women, and as a first-line treatment for hormone receptor-positive (or hormone receptor-unknown) locally advanced or metastatic breast cancer in postmenopausal women.[L8863] It may also be used in the treatment of advanced breast cancer in postmenopausal women who experience disease progression despite treatment with [tamoxifen].[L8866,L8863]
DB05812AbirateroneUsed in combination with prednisone for the treatment of metastatic, castration-resistant prostate cancer.
DB06699DegarelixDegaralix is used for the management of advanced prostate cancer.
DB08899EnzalutamideEnzalutamide is indicated for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel.
DB08905FormestaneFor the treatment of estrogen-receptor positive breast cancer in post-menopausal women.
DB13767VorozoleNot Available
DB11901ApalutamideIndicated for the treatment of patients with non-metastatic, castration-resistant prostate cancer (NM-CRPC) [FDA Label].
DrugDrug NameTargetType
DB00106AbarelixGonadotropin-releasing hormone receptortarget
DB00357AminoglutethimideCytochrome P450 19A1target
DB00357AminoglutethimideCytochrome P450 2C19enzyme
DB00357AminoglutethimideCytochrome P450 3A4enzyme
DB00357AminoglutethimideCholesterol side-chain cleavage enzyme, mitochondrialtarget
DB00499FlutamideAndrogen receptortarget
DB00499FlutamideCytochrome P450 1A2enzyme
DB00499FlutamideCytochrome P450 3A4enzyme
DB00499FlutamideCytochrome P450 1A1enzyme
DB00499FlutamideCytochrome P450 1B1enzyme
DB00499FlutamideCytochrome P450 2C19enzyme
DB00499FlutamideCytochrome P450 3A5enzyme
DB00499FlutamideAryl hydrocarbon receptortarget
DB00499FlutamideNuclear receptor subfamily 1 group I member 2target
DB00539ToremifeneEstrogen receptor alphatarget
DB00539ToremifeneCytochrome P450 3A4enzyme
DB00539ToremifeneP-glycoprotein 1transporter
DB00539ToremifeneCytochrome P450 1A1enzyme
DB00539ToremifeneSex hormone-binding globulintarget
DB00665NilutamideAndrogen receptortarget
DB00665NilutamideCytochrome P450 2C19enzyme
DB00665NilutamideNADPH--cytochrome P450 reductaseenzyme
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
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
DB01128BicalutamideAndrogen receptortarget
DB01128BicalutamideCytochrome P450 3A4enzyme
DB01128BicalutamideCytochrome P450 2C19enzyme
DB01128BicalutamideCytochrome P450 2C9enzyme
DB01128BicalutamideCytochrome P450 2D6enzyme
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
DB05812AbirateroneSteroid 17-alpha-hydroxylase/17,20 lyasetarget
DB05812AbirateroneSerum albumincarrier
DB05812AbirateroneAlpha-1-acid glycoprotein 1carrier
DB05812AbirateroneCytochrome P450 3A4enzyme
DB05812AbirateroneBile salt sulfotransferaseenzyme
DB05812AbirateroneMultidrug resistance-associated protein 1transporter
DB05812AbirateroneCytochrome P450 2D6enzyme
DB05812AbirateroneCytochrome P450 2C8enzyme
DB05812AbirateroneCytochrome P450 1A2enzyme
DB05812AbirateroneCytochrome P450 2C19enzyme
DB05812AbirateroneCytochrome P450 2C9enzyme
DB06699DegarelixGonadotropin-releasing hormone receptortarget
DB08899EnzalutamideSerum albumincarrier
DB08899EnzalutamideCytochrome P450 2C8enzyme
DB08899EnzalutamideCytochrome P450 3A4enzyme
DB08899EnzalutamideAndrogen receptortarget
DB08899EnzalutamideCytochrome P450 2C9enzyme
DB08899EnzalutamideCytochrome P450 2C19enzyme
DB08899EnzalutamideCytochrome P450 2B6enzyme
DB08899EnzalutamideCytochrome P450 3A5enzyme
DB08899EnzalutamideP-glycoprotein 1transporter
DB08899EnzalutamideThyroxine-binding globulincarrier
DB08905FormestaneCytochrome P450 3A4enzyme
DB11901ApalutamideAndrogen receptortarget
DB11901ApalutamideCytochrome P450 3A4enzyme
DB11901ApalutamideCytochrome P450 2C8enzyme
DB11901ApalutamideCytochrome P450 2C19enzyme
DB11901ApalutamideCytochrome P450 2C9enzyme
DB11901ApalutamideP-glycoprotein 1transporter
DB11901ApalutamideATP-binding cassette sub-family G member 2transporter
DB11901ApalutamideSolute carrier organic anion transporter family member 1B1transporter
DB11901ApalutamideSolute carrier family 22 member 2transporter
DB11901ApalutamideSolute carrier family 22 member 8transporter
DB11901ApalutamideMultidrug and toxin extrusion protein 2transporter
DB11901ApalutamideGABA-A receptor (anion channel)target