e-Drug3D

1591

M ENZALUTAMIDE

INN
ENZALUTAMIDE

cas 1242137-16-1

CLASS

ANTINEOPLASTIC
ANDROGEN RECEPTOR INHIBITOR
TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-RESISTANT PROSTATE CANCER
DECREASED PROLIFERATION AND INDUCED CELL DEATH

ROUTE (list)

ATC code

L02BB04

PK parameters

Cmax 28.2 MICROMOLAR
Cl 1.02 LITER / HOUR
PPB 95 PERCENT
t1/2 196 HOUR

Target

TARGET ANDROGEN RECEPTOR (AR)

DrugCentral

Androgen receptor UNIPROT P10275 AR

Download SDF file

Benzamide, 4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro

Formula:
C20H14F4N4O2S

Calculated chemical properties:

MW 450.42
NB_atoms 31
XLogP 3.73
PSA 80.218
NB_HD 2
NB_HA 6
fsp3 0.20
Lipinski(0=no;1=yes) 1

FDA
-

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

1590

ENZALUTAMIDE

INN
ENZALUTAMIDE

(has an active metabolite)

cas 915087-33-1

CLASS

ANTINEOPLASTIC
ANDROGEN RECEPTOR INHIBITOR
TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-RESISTANT PROSTATE CANCER
DECREASED PROLIFERATION AND INDUCED CELL DEATH

ROUTE (list)

ORAL

ATC code

L02BB04

PK parameters

Tmax 1 HOUR
Cmax 35.7 MICROMOLAR
VD 110 LITER
Cl 0.56 LITER / HOUR
PPB 97 PERCENT
t1/2 139 HOUR

Solubility

PRACTICALLY INSOLUBLE IN WATER

Target

TARGET ANDROGEN RECEPTOR (AR)

DrugCentral

Androgen receptor UNIPROT P10275 AR

Download SDF file

Benzamide, 4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methyl-

Formula:
C21H16F4N4O2S

Calculated chemical properties:

MW 464.45
NB_atoms 32
XLogP 3.99
PSA 68.24
NB_HD 1
NB_HA 6
fsp3 0.24
Lipinski(0=no;1=yes) 1

FDA
NDA 203415 (label) INN (ENZALUTAMIDE) XTANDI (ASTELLAS) APPROVAL= AP YEAR= 2012
NDA 213674 (label) INN (ENZALUTAMIDE) XTANDI (ASTELLAS) APPROVAL= AP YEAR= 2020
NDA 209614 (pdf not found) INN (ENZALUTAMIDE) ENZALUTAMIDE (ACTAVIS LABS FL INC) APPROVAL= AP YEAR= 2021 DISCONTINUED
NDA 209645 (pdf not found) INN (ENZALUTAMIDE) ENZALUTAMIDE (APOTEX) APPROVAL= AP YEAR= 2022 DISCONTINUED
NDA 209667 (pdf not found) INN (ENZALUTAMIDE) ENZALUTAMIDE (ZYDUS PHARMS) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 217322 (pdf not found) INN (ENZALUTAMIDE) ENZALUTAMIDE (ZYDUS PHARMS USA INC) APPROVAL= TA YEAR= 2024
NDA 219675 (pdf not found) INN (ENZALUTAMIDE) ENZALUTAMIDE (HAIMEN PHARMA INC) APPROVAL= TA YEAR= 2025
NDA 216068 (pdf not found) INN (ENZALUTAMIDE) ENZALUTAMIDE (SANDOZ) APPROVAL= AP YEAR= 2026
NDA 218731 (pdf not found) INN (ENZALUTAMIDE) ENZALUTAMIDE (HIKMA PHARMACEUTICALS USA INC) APPROVAL= TA YEAR= 2026