Galeterone

Galeterone
	File:Galeterone.svg
Systematic (IUPAC) name
	17-(1H-benzimidazol-1-yl)androsta-5,16-dien-3β-ol
Clinical data
Routes of; administration	Oral
Identifiers
CAS Number	851983-85-2
PubChem	CID: 11188409
ChemSpider	9363493
UNII	WA33E149SW
KEGG	D10125
Chemical data
Formula	C26H32N2O
Molecular mass	388.25
	SMILES C[C@]12CC[C@@H](CC1=CC[C@@H]3[C@@H]2CC[C@]4([C@H]3CC=C4N5C=NC6=CC=CC=C65)C)O ;
	InChI InChI=1S/C26H32N2O/c1-25-13-11-18(29)15-17(25)7-8-19-20-9-10-24(26(20,2)14-12-21(19)25)28-16-27-22-5-3-4-6-23(22)28/h3-7,10,16,18-21,29H,8-9,11-15H2,1-2H3/t18-,19-,20-,21-,25-,26-/m0/s1 ; Key:PAFKTGFSEFKSQG-PAASFTFBSA-N ;

Galeterone (TOK-001 or VN/124-1) is a novel steroidal antiandrogen under development by Tokai Pharmaceuticals for the treatment of prostate cancer. It possesses a unique dual mechanism of action, acting as both an androgen receptor antagonist and an inhibitor of CYP17A1, an enzyme required for the biosynthesis of the androgens.^[1] It shows selectivity for 17,20-lyase over 17-hydroxylase.^[2]

As of 2016, galeterone is being compared to enzalutamide in a phase III clinical trial (ARMOR3-SV) for AR-V7-expressing metastatic castration-resistant prostate cancer.^[3]^[4]

References

↑ Lua error in package.lua at line 80: module 'strict' not found.
↑ Lua error in package.lua at line 80: module 'strict' not found.
↑ Lua error in package.lua at line 80: module 'strict' not found.
↑ Lua error in package.lua at line 80: module 'strict' not found.

[pmid19145273-1] Lua error in package.lua at line 80: module 'strict' not found.

[pmid24276076-2] Lua error in package.lua at line 80: module 'strict' not found.

[3] Lua error in package.lua at line 80: module 'strict' not found.

[Silberstein2016-4] Lua error in package.lua at line 80: module 'strict' not found.

[1]

[2]

[3]

[4]

v t e Steroid hormone metabolism modulators
20,22-Desmolase	Inhibitors: 22-ABC 3,3′-Dimethoxybenzidine 3-Methoxybenzidine Aminoglutethimide Canrenone Cyanoketone Danazol Etomidate Ketoconazole Mitotane Spironolactone Trilostane
17α-Hydroxylase, 17,20-Lyase	Inhibitors: 22-ABC 22-Oxime Abiraterone Abiraterone acetate Bifonazole Canrenone CFG-920 Clotrimazole Cyanoketone Cyproterone acetate Danazol Econazole Galeterone Gestrinone Isoconazole Ketoconazole L-39 Levoketoconazole Liarozole LY-207,320 MDL-27,302 Miconazole Mifepristone Orteronel Pioglitazone Prochloraz Rosiglitazone Seviteronel Spironolactone Stanozolol SU-10,603 TGF-β Tioconazole Troglitazone VN/87-1 YM116
3α-HSD	Inhibitors: Coumestrol Daidzein Genistein Indomethacin Medroxyprogesterone acetate Inducers: Fluoxetine Fluvoxamine Mirtazapine Paroxetine Sertraline Venlafaxine
3β-HSD	Inhibitors: 4-MA Abiraterone Abiraterone acetate Azastene Cyanoketone Cyproterone acetate Danazol Epostane Genistein Gestrinone Metyrapone Norethisterone Oxymetholone Pioglitazone Rosiglitazone Trilostane Troglitazone
11β-HSD	Inhibitors: 18α-Glycyrrhizic acid ABT-384 Acetoxolone Carbenoxolone Enoxolone (glycyrrhetinic acid) Epigallocatechin gallate Glycyrrhizin (glycyrrhizic acid)
21-Hydroxylase	Inhibitors: Aminoglutethimide Amphenone B Bifonazole Canrenone Clotrimazole Diazepam Econazole Genistein Isoconazole Ketoconazole Levoketoconazole Metyrapone Miconazole Midazolam Spironolactone Tioconazole
11β-Hydroxylase	Inhibitors: Abiraterone Abiraterone acetate Aminoglutethimide Canrenone Etomidate Fadrozole FETO Ketoconazole Levoketoconazole Metomidate Metyrapone Mitotane Potassium canrenoate Spironolactone Trilostane
18-Hydroxylase	Inhibitors: Aminoglutethimide Canrenone FAD286 Fadrozole Ketoconazole LCI699 Metyrapone Mespirenone Potassium canrenoate Spironolactone
17β-HSD	Inhibitors: Danazol Simvastatin
5α-Reductase	Inhibitors: 22-Oxime Alfatradiol Azelaic acid β-Sitosterol Bexlosteride Chlormadinone acetate Cl-4AS-1 Dutasteride Epitestosterone Epristeride Fatty acids (α-linolenic acid, linoleic acid, γ-linolenic acid, monolinolein, oleic acid) Finasteride Ganoderic acid Izonsteride L-39 Lapisteride Saw palmetto TFM-4AS-1 Turosteride Vitamin B6 Zinc
Aromatase	Inhibitors: 4-AT 4-Cyclohexylaniline 4-Hydroxytestosterone 5α-DHNET Abyssinone II Aminoglutethimide Anastrozole Ascorbic acid (vitamin C) Atamestane ATD Bifonazole CGP-45,688 CGS-47,645 Chalconoids (e.g., isoliquiritigenin) Corynesidone A Clotrimazole DHT Difeconazole Econazole Ellagitannins Endosulfan Exemestane Fadrozole Fatty acids (e.g., conjugated linoleic acid, linoleic acid, linolenic acid, palmitic acid) Fenarimol Finrozole Flavonoids (e.g., 7-hydroxyflavone, 7-hydroxyflavanone, 7,8-DHF, acacetin, apigenin, baicalein, biochanin A, chrysin, EGCG, gossypetin, hesperetin, liquiritigenin, myricetin, naringenin, pinocembrin, rotenone, quercetin, sakuranetin, tectochrysin) Formestane Imazalil Isoconazole Ketoconazole Letrozole Liarozole Melatonin MEN-11066 Miconazole Minamestane Nimorazole NKS01 Norendoxifen ORG-33,201 Penconazole Phenytoin Prochloraz PGE2 (dinoprostone) Plomestane Prochloraz Propioconazole Pyridoglutethimide Quinolinoids (e.g., berberine, casimiroin, triptoquinone A, XHN22, XHN26, XHN27) Resorcylic acid lactones (e.g., zearalenone) Rogletimide Stilbenoids (e.g., resveratrol) Talarozole Terpenoids (e.g., dehydroabietic acid, (–)-dehydrololiolide, retinol (vitamin A), Δ⁹-THC, tretinoin) Testolactone Tioconazole Triadimefon Triadimenol Troglitazone Valproic acid Vorozole Xanthones (e.g., garcinone D, garcinone E, α-mangostin, γ-mangostin, monodictyochrome A, monodictyochrome B) YM-511 Zinc Inducers: Atrazine Flavonoids (e.g., genistein, quercetin)
27-Hydroxylase	Inhibitors: Anastrozole Bicalutamide Dexmedetomidine Fadrozole Posaconazole Ravuconazole
See also: Androgenics • Estrogenics • Glucocorticoidics • Mineralocorticoidics • Progestogenics

Galeterone

See also

References

Navigation menu

Personal tools

Namespaces

Variants

Views

More

Search

Navigation

Tools