Antineoplastic Agents, Hormonal

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 NameDrug Indication
DB00007LeuprolideFor treatment of prostate cancer, endometriosis, uterine fibroids and premature puberty
DB00014GoserelinUsed to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty.
DB00104OctreotideFor treatment of acromegaly and reduction of side effects from cancer chemotherapy
DB00255DiethylstilbestrolUsed 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.
DB00269ChlorotrianiseneUsed 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 be used to prevent breast engorgement following childbirth.
DB00351Megestrol acetateFor the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Also used for the palliative management of recurrent, inoperable, or metastatic breast cancer, endometrial cancer, and prostate cancer in Canada and some other countries.
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.
DB00603Medroxyprogesterone acetateUsed as a contraceptive and to treat secondary amenorrhea, abnormal uterine bleeding, pain associated with endometriosis, endometrial and renal cell carcinomas, paraphilia in males, GnRH-dependent forms of precocious puberty, as well as to prevent endometrial changes associated with estrogens.
DB00635PrednisoneFor the treatment of drug-induced allergic reactions, perennial or seasonal allergic rhinitis, serum sickness, giant cell arteritis acute rheumatic or nonrheumatic carditis, systemic dermatomyositis, systemic lupus erythematosus, atopic dermatitis, contact dermatitis, exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe (Stevens-Johnson syndrome) erythema multiforme, mycosis fungoides, pemphigus, severe psoriasis, acute adrenocortical insufficiency, Addison's disease, secondary adrenocortical insufficiency, congenital adrenal hyperplasia, hypercalcemia associated with neoplasms, nonsuppurative thyroiditis, ulceratice colitis, Crohn's disease, acquired hemolytic anemia, congenital hypoplastic anemia, erythroblastopenia, adult secondary thrombocytopenia, adult idiopathic thrombocytopenia purpura, acute or subacute bursitis, epicondylitis, acute nonspecific tenosynovitis, acute or chronic lymphocytic leukemia, Hodgkin's or non-Hodgkin's lynphomas, Waldenstrom's macroglobulinemia, primary brain tumors (adjunct), nephrotic syndrome, tuberculous meningitis, multiple sclerosis, myasthenia gravis. cerebral edema, chorioretinitis, diffuse posterior choroiditis, aleergic conjunctivitis, Herpes zoster ophthalmicus, anterior segment inflammation, iridocyclitis, iritis, keratitis, optoc neuritis, sympathetic ophthalmia, corneal marginal allergic ulcers, symptomatic sarcoidosis, Loeffler's syndrome not manageable by other means, berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy and aspiration pneumonitis.
DB00648MitotaneFor treatment of inoperable adrenocortical tumours; Cushing's syndrome
DB00675TamoxifenTamoxifen is indicated for the treatment of metastatic breast cancer in women and men and ductal carcinoma in Situ.
DB00860PrednisoloneFor the treatment of primary or secondary adrenocortical insufficiency, such as congenital adrenal hyperplasia, thyroiditis. Also used to treat psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis, bursitis, acute gouty arthritis and epicondylitis. Also indicated for treatment of systemic lupus erythematosus, pemphigus and acute rhematic carditis. Can be used in the treatment of leukemias, lymphomas, thrombocytopenia purpura and autoimmune hemolytic anemia. Can be used to treat celiac disease, insulin resistance, ulcerative colitis and liver disorders.
DB00894TestolactoneFor palliative treatment of advanced breast cancer in postmenopausal women.
DB00947FulvestrantFor the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy.
DB00959MethylprednisoloneAdjunctive therapy for short-term administration in rheumatoid arthritis.
DB01196EstramustineFor the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate
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.
DB01234DexamethasoneInjection: for the treatment of endocrine disorders, rheumatic D=disorders, collagen diseases, dermatologic diseases, allergic statesc, ophthalmic diseases, gastrointestinal diseases, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, cerebral edema.
Ophthalmic ointment and solution: for the treatment of steroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe.
Ophthalmic solution only: for the treatment of steroid responsive inflammatory conditions of the external auditory meatus
Topic cream: for relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses
Oral aerosol: for the treatment of bronchial asthma and related corticosteroid responsive bronchospastic states intractable to adequate trial of conventional therapy
Intranasal aerosol: for the treatment of allergic ot inflammatory nasal conditions, and nasal polyps
DB06710MethyltestosteroneMethyltestosterone is an anabolic steroid hormone used to treat men with a testosterone deficiency. It is also used in women to treat breast cancer, breast pain, swelling due to pregnancy, and with the addition of estrogen it can treat symptoms of menopause.
DB06825TriptorelinTriptorelin is indicated for the palliative treatment of advanced prostate cancer.
DB07931HexestrolNot Available
DB09070TiboloneNot Available
DB09123DienogestIndicated for use as the treatment of endometriosis alone and as a contraceptive in combination with ethinylestradiol.
DB09124MedrogestoneNot Available
DB13066LiarozoleNot Available
DrugDrug NameTargetType
DB00007LeuprolideGonadotropin-releasing hormone receptortarget
DB00014GoserelinLutropin-choriogonadotropic hormone receptortarget
DB00014GoserelinGonadotropin-releasing hormone receptortarget
DB00104OctreotideSomatostatin receptor type 1target
DB00104OctreotideSomatostatin receptor type 5target
DB00104OctreotideSomatostatin receptor type 2target
DB00104OctreotideMyeloperoxidaseenzyme
DB00255DiethylstilbestrolEstrogen receptor alphatarget
DB00255DiethylstilbestrolEstrogen-related receptor gammatarget
DB00255DiethylstilbestrolTransthyretincarrier
DB00255DiethylstilbestrolCatechol O-methyltransferaseenzyme
DB00255DiethylstilbestrolCytochrome P450 19A1enzyme
DB00255DiethylstilbestrolCytochrome P450 2A6enzyme
DB00255DiethylstilbestrolATP-binding cassette sub-family G member 2transporter
DB00255DiethylstilbestrolMultidrug resistance protein 1transporter
DB00255DiethylstilbestrolEstrogen receptor betatarget
DB00255DiethylstilbestrolCytochrome P450 3A4enzyme
DB00255DiethylstilbestrolCytochrome P450 2C8enzyme
DB00255DiethylstilbestrolCytochrome P450 2C9enzyme
DB00255DiethylstilbestrolCytochrome P450 2E1enzyme
DB00255DiethylstilbestrolSteroid hormone receptor ERR1target
DB00255DiethylstilbestrolSteroid hormone receptor ERR2target
DB00255DiethylstilbestrolNuclear receptor coactivator 2target
DB00255DiethylstilbestrolNuclear receptor subfamily 1 group I member 2target
DB00255DiethylstilbestrolAndrogen receptortarget
DB00255DiethylstilbestrolSex hormone-binding globulintarget
DB00269ChlorotrianiseneEstrogen receptor alphatarget
DB00269ChlorotrianiseneCytochrome P450 19A1enzyme
DB00351Megestrol acetateProgesterone receptortarget
DB00351Megestrol acetateGlucocorticoid receptortarget
DB00351Megestrol acetateMultidrug resistance protein 1transporter
DB00357AminoglutethimideCytochrome P450 19A1target
DB00357AminoglutethimideCytochrome P450 1A2enzyme
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
DB00539ToremifeneMultidrug resistance protein 1transporter
DB00539ToremifeneCytochrome P450 1A1enzyme
DB00539ToremifeneCytochrome P450 1A2enzyme
DB00539ToremifeneSex hormone-binding globulintarget
DB00603Medroxyprogesterone acetateProgesterone receptortarget
DB00603Medroxyprogesterone acetateEstrogen receptor alphatarget
DB00603Medroxyprogesterone acetateCytochrome P450 3A4enzyme
DB00603Medroxyprogesterone acetateCytochrome P450 2C8enzyme
DB00603Medroxyprogesterone acetate3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2enzyme
DB00603Medroxyprogesterone acetateCytochrome P450 2C9enzyme
DB00635PrednisoneGlucocorticoid receptortarget
DB00635PrednisoneCytochrome P450 3A4enzyme
DB00635PrednisoneMultidrug resistance protein 1transporter
DB00635PrednisoneSolute carrier organic anion transporter family member 1A2transporter
DB00635PrednisoneCytochrome P450 2C19enzyme
DB00635PrednisoneSerum albumincarrier
DB00635PrednisoneCorticosteroid 11-beta-dehydrogenase isozyme 1target
DB00648MitotaneCytochrome P450 11B1, mitochondrialtarget
DB00648MitotaneAdrenodoxin, mitochondrialtarget
DB00648MitotaneSex hormone-binding globulincarrier
DB00648MitotaneCorticosteroid-binding globulincarrier
DB00648MitotaneCytochrome P450 3A4enzyme
DB00648MitotaneEstrogen receptor alphatarget
DB00648MitotaneProgesterone receptortarget
DB00648MitotaneAndrogen receptortarget
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 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 1-10enzyme
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
DB00860PrednisoloneCorticosteroid-binding globulincarrier
DB00860PrednisoloneCytochrome P450 3A4enzyme
DB00860PrednisoloneGlucocorticoid receptortarget
DB00860PrednisoloneSolute carrier organic anion transporter family member 1A2transporter
DB00860PrednisoloneMultidrug resistance protein 1transporter
DB00860PrednisoloneCytochrome P450 2A6enzyme
DB00894TestolactoneCytochrome P450 19A1target
DB00947FulvestrantEstrogen receptor alphatarget
DB00947FulvestrantCytochrome P450 3A4enzyme
DB00959MethylprednisoloneGlucocorticoid receptortarget
DB00959MethylprednisoloneCytochrome P450 3A4enzyme
DB00959MethylprednisoloneMultidrug resistance protein 1transporter
DB01196EstramustineEstrogen receptor betatarget
DB01196EstramustineEstrogen receptor alphatarget
DB01196EstramustineMicrotubule-associated protein 2target
DB01196EstramustineMicrotubule-associated protein 1Atarget
DB01196EstramustineMultidrug resistance protein 1transporter
DB01196EstramustineCytochrome P450 3A4enzyme
DB01217AnastrozoleCytochrome P450 19A1target
DB01217AnastrozoleCytochrome P450 19A1enzyme
DB01217AnastrozoleCytochrome P450 1A2enzyme
DB01217AnastrozoleCytochrome P450 2C9enzyme
DB01217AnastrozoleCytochrome P450 3A4enzyme
DB01234DexamethasoneGlucocorticoid receptortarget
DB01234DexamethasoneAnnexin A1target
DB01234DexamethasoneNitric oxide synthase, inducibletarget
DB01234DexamethasoneNuclear receptor subfamily 0 group B member 1target
DB01234DexamethasoneCytochrome P450 3A4enzyme
DB01234DexamethasoneCytochrome P450 2C9enzyme
DB01234DexamethasoneCytochrome P450 3A5enzyme
DB01234DexamethasoneCytochrome P450 3A7enzyme
DB01234DexamethasoneBile salt export pumptransporter
DB01234DexamethasoneMultidrug resistance protein 1transporter
DB01234DexamethasoneCanalicular multispecific organic anion transporter 1transporter
DB01234DexamethasoneSolute carrier organic anion transporter family member 1A2transporter
DB01234DexamethasoneATP-binding cassette sub-family G member 2transporter
DB01234DexamethasoneCholesterol side-chain cleavage enzyme, mitochondrialenzyme
DB01234DexamethasoneSteroid 17-alpha-hydroxylase/17,20 lyaseenzyme
DB01234DexamethasoneCytochrome P450 19A1enzyme
DB01234DexamethasoneCytochrome P450 1A1enzyme
DB01234DexamethasoneCytochrome P450 1B1enzyme
DB01234DexamethasoneCytochrome P450 2A6enzyme
DB01234DexamethasoneCytochrome P450 2B6enzyme
DB01234DexamethasoneCytochrome P450 2C19enzyme
DB01234DexamethasoneCytochrome P450 2C8enzyme
DB01234DexamethasoneCytochrome P450 2D6enzyme
DB01234DexamethasoneCytochrome P450 2E1enzyme
DB01234DexamethasoneCytochrome P450 3A43enzyme
DB01234DexamethasoneCytochrome P450 4A11enzyme
DB01234DexamethasoneNuclear receptor subfamily 1 group I member 2target
DB06710MethyltestosteroneCytochrome P450 19A1enzyme
DB06710MethyltestosteroneCytochrome P450 2B6enzyme
DB06710MethyltestosteroneCytochrome P450 3A4enzyme
DB06710MethyltestosteroneAndrogen receptortarget
DB06710MethyltestosteroneSolute carrier organic anion transporter family member 1A2transporter
DB06710MethyltestosteroneSolute carrier family 22 member 8transporter
DB06710MethyltestosteroneSerum albumincarrier
DB06710MethyltestosteroneSex hormone-binding globulincarrier
DB06710MethyltestosteroneEstrogen receptor alphatarget
DB06825TriptorelinGonadotropin-releasing hormone receptortarget
DB07931HexestrolAldo-keto reductase family 1 member C1target
DB07931HexestrolEstrogen receptor alphatarget
DB07931HexestrolNuclear receptor subfamily 1 group I member 2target
DB07931HexestrolNuclear receptor subfamily 1 group I member 3target
DB09070TiboloneEstrogen receptor alphatarget
DB09123DienogestCytochrome P450 3A4enzyme
DB09123DienogestProgesterone receptortarget
DB09123DienogestAndrogen receptortarget