Antineoplastic Agents, Hormonal

Antineoplastic Agents, Hormonal
Accession Number

Antineoplastic agents that are used to treat hormone-sensitive tumors. Hormone-sensitive tumors may be hormone-dependent, hormone-responsive, or both. A hormone-dependent tumor regresses on removal of the hormonal stimulus, by surgery or pharmacological block. Hormone-responsive tumors may regress when pharmacologic amounts of hormones are administered regardless of whether previous signs of hormone sensitivity were observed. The major hormone-responsive cancers include carcinomas of the breast, prostate, and endometrium; lymphomas; and certain leukemias. (From AMA Drug Evaluations Annual 1994, p2079)

DrugDrug Description
LeuprolideA protein-based luteinizing hormone agonist used to treat prostate cancer, endometriosis, and precocious puberty.
GoserelinA synthetic analog of luteinizing hormone-releasing hormone used to treat breast cancer and prostate cancer by reducing secretion of gonadotropins from the pituitary.
OctreotideA peptide drug used to treat acromegaly as well as diarrhea associated with metastatic carcinoid tumors and vasoactive intestinal peptide secreting tumors.
DiethylstilbestrolUsed in the treatment of prostate cancer. Previously used in the prevention of miscarriage or premature delivery in pregnant women prone to miscarriage or premature delivery.
ChlorotrianiseneUsed to treat symptoms of menopause, deficiencies in ovary function (including underdevelopment of female sexual characteristics and some types of infertility), and in rare cases, prostate cancer. Chlorotrianisene may also...
Megestrol acetateA progestin that is administered orally to treat anorexia and cachexia or serious unexplained weight loss and is also used as an antineoplastic agent to treat certain types of malignancy.
AminoglutethimideAn adrenocortical steroid synthesis inhibitor used in the treatment of Cushing's syndrome.
FlutamideAn antiandrogen used for locally confined stage B2-C and D-2 metastatic prostate carcinoma.
ToremifeneA first generation nonsteroidal selective estrogen receptor modulator used to treat certain breast cancers.
Medroxyprogesterone acetateA progestin used as a contraceptive and in the treatment of secondary amenorrhea, abnormal uterine bleeding, pain from endometriosis, endometrial and renal carcinomas, paraphilia in males, and GnRH-dependent precocious puberty.
PrednisoneA corticosteroid used to treat inflammation or immune-mediated reactions and to treat endocrine or neoplastic diseases.
MitotaneAn adrenal cortex inhibitor used to treat adrenocortical tumors and Cushing's syndrome.
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.
PrednisoloneA glucocorticoid used to treat adrenocortical insufficiency, inflammatory conditions, and some cancers.
TestolactoneA medication used to treat advanced breast cancer.
FulvestrantAn estrogen receptor antagonist used to treat HR+ breast cancer that may also be HER2-.
EstramustineAn antineoplastic agent used for the management of metastatic and/or progressive prostate cancer in palliative setting.
AnastrozoleA competitive, selective, non-steroidal aromatase inhibitor used as adjuvant therapy for the treatment of hormone receptor-positive breast cancer in postmenopausal women.
DexamethasoneA glucocorticoid available in various modes of administration that is used for the treatment of various inflammatory conditions, including bronchial asthma, as well as endocrine and rheumatic disorders.
MethyltestosteroneA synthetic anabolic steroid used for the replacement therapy in conditions associated with testosterone deficiencies in males, such as hypogonadism, and treatment of advancing inoperable metastatic breast cancer in females.
TriptorelinA GnRH agonist indicated for the palliative treatment of advanced prostate cancer.
HexestrolA synthetic estrogen that has been used as a hormonal antineoplastic agent.
TiboloneFor the relief of post-menopausal symptoms and for the prevention of osteoporosis .
DienogestAn oral progestin used for the treatment of endometriosis as monotherapy or contraception in combination with ethinylestradiol.
MedrogestoneA progestin used as an adjunct to control secondary amenorrhea and dysfunctional bleeding in adolescent and adult females, and treat endometrial shedding in menopausal women.
NomegestrolNomegestrol is an ingredient in the EMA-authorised product Zoely.
LiarozoleLiarozole has been used in trials studying the treatment of Ichthyosis, Lamellar.
Nomegestrol acetateNomegestrol acetate, also known as NOMAC, is a progestin used in oral contraceptives, menopausal hormone therapy, and for the treatment of gynecological disorders.
Methylprednisolone hemisuccinateA water soluble corticosteroid used to treat severe allergic reactions, dermatologic diseases, endocrine disorders, gastrointestinal diseases, hematological disorders, neoplastic diseases, nervous system conditions, ophthalmic diseases, renal diseases, respiratory diseases, and rheumatic disorders.
Prednisone acetateNot Annotated
Drugs & Drug Targets
LeuprolideGonadotropin-releasing hormone receptortarget
LeuprolideCytochrome P450 3A4enzyme
GoserelinLutropin-choriogonadotropic hormone receptortarget
GoserelinGonadotropin-releasing hormone receptortarget
OctreotideSomatostatin receptor type 1target
OctreotideSomatostatin receptor type 5target
OctreotideSomatostatin receptor type 2target
OctreotideCytochrome P450 3A4enzyme
DiethylstilbestrolEstrogen receptor alphatarget
DiethylstilbestrolEstrogen-related receptor gammatarget
DiethylstilbestrolCatechol O-methyltransferaseenzyme
DiethylstilbestrolCytochrome P450 19A1enzyme
DiethylstilbestrolATP-binding cassette sub-family G member 2transporter
DiethylstilbestrolP-glycoprotein 1transporter
DiethylstilbestrolEstrogen receptor betatarget
DiethylstilbestrolCytochrome P450 3A4enzyme
DiethylstilbestrolCytochrome P450 2C8enzyme
DiethylstilbestrolCytochrome P450 2C9enzyme
DiethylstilbestrolCytochrome P450 2E1enzyme
DiethylstilbestrolSteroid hormone receptor ERR1target
DiethylstilbestrolSteroid hormone receptor ERR2target
DiethylstilbestrolNuclear receptor coactivator 2target
DiethylstilbestrolNuclear receptor subfamily 1 group I member 2target
DiethylstilbestrolAndrogen receptortarget
DiethylstilbestrolSex hormone-binding globulintarget
DiethylstilbestrolSolute carrier organic anion transporter family member 1B1transporter
DiethylstilbestrolSolute carrier organic anion transporter family member 2B1transporter
DiethylstilbestrolBile salt export pumptransporter
ChlorotrianiseneEstrogen receptor alphatarget
ChlorotrianiseneCytochrome P450 19A1enzyme
Megestrol acetateProgesterone receptortarget
Megestrol acetateGlucocorticoid receptortarget
Megestrol acetateP-glycoprotein 1transporter
Megestrol acetateCytochrome P450 3A4enzyme
AminoglutethimideCytochrome P450 19A1target
AminoglutethimideCytochrome P450 2C19enzyme
AminoglutethimideCytochrome P450 3A4enzyme
AminoglutethimideCholesterol side-chain cleavage enzyme, mitochondrialtarget
FlutamideAndrogen receptortarget
FlutamideCytochrome P450 1A2enzyme
FlutamideCytochrome P450 3A4enzyme
FlutamideCytochrome P450 1A1enzyme
FlutamideCytochrome P450 1B1enzyme
FlutamideCytochrome P450 2C19enzyme
FlutamideCytochrome P450 3A5enzyme
FlutamideAryl hydrocarbon receptortarget
FlutamideNuclear receptor subfamily 1 group I member 2target
ToremifeneEstrogen receptor alphatarget
ToremifeneCytochrome P450 3A4enzyme
ToremifeneP-glycoprotein 1transporter
ToremifeneCytochrome P450 1A1enzyme
ToremifeneSex hormone-binding globulintarget
Medroxyprogesterone acetateProgesterone receptortarget
Medroxyprogesterone acetateEstrogen receptor alphatarget
Medroxyprogesterone acetateCytochrome P450 3A4enzyme
Medroxyprogesterone acetateCytochrome P450 2C8enzyme
Medroxyprogesterone acetate3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2enzyme
Medroxyprogesterone acetateCytochrome P450 2C9enzyme
Medroxyprogesterone acetateCytochrome P450 3A1enzyme
Medroxyprogesterone acetateSerum albumincarrier
Medroxyprogesterone acetateP-glycoprotein 1target
Medroxyprogesterone acetateGABA-A receptor (anion channel)target
Medroxyprogesterone acetateP-glycoprotein 1transporter
PrednisoneGlucocorticoid receptortarget
PrednisoneCytochrome P450 3A4enzyme
PrednisoneP-glycoprotein 1transporter
PrednisoneSolute carrier organic anion transporter family member 1A2transporter
PrednisoneCytochrome P450 2C19enzyme
PrednisoneSerum albumincarrier
PrednisoneCytochrome P450 3A5enzyme
PrednisoneCorticosteroid-binding globulincarrier
PrednisoneCytochrome P450 3A Subfamilyenzyme
PrednisoneCytochrome P450 2A6enzyme
PrednisoneCytochrome P450 1B1enzyme
PrednisoneCytochrome P450 2B6enzyme
PrednisoneCytochrome P450 2C8enzyme
PrednisoneCytochrome P450 2C9enzyme
PrednisoneCorticosteroid 11-beta-dehydrogenase isozyme 1enzyme
MitotaneCytochrome P450 11B1, mitochondrialtarget
MitotaneAdrenodoxin, mitochondrialtarget
MitotaneSex hormone-binding globulincarrier
MitotaneCorticosteroid-binding globulincarrier
MitotaneCytochrome P450 3A4enzyme
MitotaneEstrogen receptor alphatarget
MitotaneProgesterone receptortarget
MitotaneAndrogen receptortarget
MitotaneThyroxine-binding globulincarrier
MitotaneP-glycoprotein 1transporter
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
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
PrednisoloneCorticosteroid-binding globulincarrier
PrednisoloneCytochrome P450 3A4enzyme
PrednisoloneGlucocorticoid receptortarget
PrednisoloneSolute carrier organic anion transporter family member 1A2transporter
PrednisoloneP-glycoprotein 1transporter
PrednisoloneSerum albumincarrier
TestolactoneCytochrome P450 19A1target
FulvestrantEstrogen receptor alphatarget
FulvestrantCytochrome P450 3A4enzyme
FulvestrantUDP-glucuronosyltransferase 1-1enzyme
EstramustineEstrogen receptor betatarget
EstramustineEstrogen receptor alphatarget
EstramustineMicrotubule-associated protein 2target
EstramustineMicrotubule-associated protein 1Atarget
EstramustineP-glycoprotein 1transporter
EstramustineCytochrome P450 3A4enzyme
AnastrozoleCytochrome P450 19A1target
AnastrozoleP-glycoprotein 1transporter
AnastrozoleCytochrome P450 3A4enzyme
AnastrozoleCytochrome P450 3A5enzyme
AnastrozoleCytochrome P450 2C8enzyme
AnastrozoleUDP-glucuronosyltransferase 1-4enzyme
AnastrozoleUDP-glucuronosyltransferase 1-3enzyme
AnastrozoleUDP-glucuronosyltransferase 2B7enzyme
AnastrozoleCytochrome P450 1A2enzyme
AnastrozoleCytochrome P450 2C9enzyme
DexamethasoneGlucocorticoid receptortarget
DexamethasoneAnnexin A1target
DexamethasoneNitric oxide synthase, inducibletarget
DexamethasoneNuclear receptor subfamily 0 group B member 1target
DexamethasoneCytochrome P450 3A4enzyme
DexamethasoneCytochrome P450 3A5enzyme
DexamethasoneCytochrome P450 3A7enzyme
DexamethasoneBile salt export pumptransporter
DexamethasoneP-glycoprotein 1transporter
DexamethasoneCanalicular multispecific organic anion transporter 1transporter
DexamethasoneSolute carrier organic anion transporter family member 1A2transporter
DexamethasoneATP-binding cassette sub-family G member 2transporter
DexamethasoneSteroid 17-alpha-hydroxylase/17,20 lyaseenzyme
DexamethasoneCytochrome P450 1A1enzyme
DexamethasoneCytochrome P450 2A6enzyme
DexamethasoneCytochrome P450 2B6enzyme
DexamethasoneCytochrome P450 2C19enzyme
DexamethasoneCytochrome P450 2C8enzyme
DexamethasoneCytochrome P450 2E1enzyme
DexamethasoneCytochrome P450 3A43enzyme
DexamethasoneCytochrome P450 4A11enzyme
DexamethasoneNuclear receptor subfamily 1 group I member 2target
DexamethasoneCytochrome P450 11B1, mitochondrialenzyme
DexamethasoneSerum albumincarrier
DexamethasoneCorticosteroid 11-beta-dehydrogenase isozyme 2enzyme
DexamethasoneCorticosteroid 11-beta-dehydrogenase isozyme 1enzyme
DexamethasoneSolute carrier family 22 member 8transporter
MethyltestosteroneCytochrome P450 2B6enzyme
MethyltestosteroneCytochrome P450 3A4enzyme
MethyltestosteroneAndrogen receptortarget
MethyltestosteroneSolute carrier organic anion transporter family member 1A2transporter
MethyltestosteroneSolute carrier family 22 member 8transporter
MethyltestosteroneSerum albumincarrier
MethyltestosteroneSex hormone-binding globulincarrier
MethyltestosteroneEstrogen receptor alphatarget
MethyltestosteroneCytochrome P450 19A1enzyme
TriptorelinGonadotropin-releasing hormone receptortarget
HexestrolAldo-keto reductase family 1 member C1target
HexestrolEstrogen receptor alphatarget
HexestrolNuclear receptor subfamily 1 group I member 2target
HexestrolNuclear receptor subfamily 1 group I member 3target
TiboloneEstrogen receptor alphatarget
Tibolone3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1enzyme
Tibolone3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2enzyme
TiboloneSulfotransferase 1A1enzyme
DienogestCytochrome P450 3A4enzyme
DienogestProgesterone receptortarget
DienogestAndrogen receptortarget
MedrogestoneSerum albumincarrier
MedrogestoneProgesterone receptortarget
MedrogestoneSex hormone-binding globulincarrier
MedrogestoneCorticosteroid-binding globulincarrier
MedrogestoneCytochrome P450 3A4enzyme
NomegestrolCytochrome P450 3A4enzyme
Nomegestrol acetateCytochrome P450 3A4enzyme
Methylprednisolone hemisuccinateCytochrome P450 3A4enzyme
Methylprednisolone hemisuccinateCytochrome P450 3A5enzyme
Prednisone acetateCytochrome P450 3A4enzyme
Prednisone acetateCytochrome P450 3A5enzyme