e-Drug3D

1883

APALUTAMIDE


INN
APALUTAMIDE

(has an active metabolite)

cas 956104-40-8
CLASS

ANTINEOPLASTIC
ANDROGEN RECEPTOR INHIBITOR INDICATED FOR THE TREATMENT OF PATIENTS WITH NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER

ROUTE (list)

ORAL

ATC code

L02BB05

PK parameters

F 100 PERCENT
Tmax 3 HOUR
VD 276 LITER
Cl 1.3 LITER / HOUR
PPB 96 PERCENT
t1/2 72 HOUR

Solubility

PRACTICALLY INSOLUBLE IN AQUEOUS MEDIA OVER A WIDE RANGE OF PH VALUES


Target

TARGET ANDROGEN RECEPTOR

DrugCentral

Androgen receptor UNIPROT P10275 AR

Download SDF file Benzamide, 4-[7-[6-cyano-5-(trifluoromethyl)-3-pyridinyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methyl-

Formula:
C21H15F4N5O2S

Calculated chemical properties:

MW 477.45
NB_atoms 33
XLogP 3.53
PSA 78.868
NB_HD 1
NB_HA 7
fsp3 0.29
Lipinski(0=no;1=yes) 1

FDA
NDA 210951 (pdf not found) INN (APALUTAMIDE) ERLEADA (JANSSEN BIOTECH) APPROVAL= AP YEAR= 2018 NEWMOLECULARENTITY
NDA 217113 (pdf not found) INN (APALUTAMIDE) APALUTAMIDE (ZYDUS) APPROVAL= AP YEAR= 2025

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL