e-Drug3D

1956

M DAROLUTAMIDE

INN
DAROLUTAMIDE

(is an active metabolite)

cas 1297537-33-7

CLASS

ANTINEOPLASTIC
ANDROGEN RECEPTOR INHIBITOR
TREATMENT OF NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER

ROUTE (list)

-

ATC code

L02BB06

PK parameters

PPB 99.8 PERCENT
t1/2 20 HOUR

Target

TARGET ANDROGEN RECEPTOR (AR)

Androgen receptor UNIPROT P10275 AR

Download SDF file

1H-Pyrazole-3-carboxamide, 5-acetyl-N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-

Formula:
C19H17ClN6O2

Calculated chemical properties:

MW 396.84
NB_atoms 28
XLogP 2.82
PSA 105.608
NB_HD 2
NB_HA 8
fsp3 0.21
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

1954

DAROLUTAMIDE

INN
DAROLUTAMIDE

(has an active metabolite)

cas 1297538-32-9

CLASS

ANTINEOPLASTIC
ANDROGEN RECEPTOR INHIBITOR
TREATMENT OF NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER

ROUTE (list)

ORAL

ATC code

L02BB06

PK parameters

F 30 PERCENT
Tmax 4 HOUR
Cmax 12 MICROMOLAR
VD 119 LITER
Cl 6.96 LITER / HOUR
PPB 92 PERCENT
t1/2 20 HOUR

Solubility

PRACTICALLY INSOLUBLE IN AQUEOUS MEDIUM

Target

TARGET ANDROGEN RECEPTOR (AR)

Androgen receptor UNIPROT P10275 AR

Download SDF file

1H-Pyrazole-3-carboxamide, N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-

Formula:
C19H19ClN6O2

Calculated chemical properties:

MW 398.85
NB_atoms 28
XLogP 2.67
PSA 109.2
NB_HD 3
NB_HA 8
fsp3 0.26
Lipinski(0=no;1=yes) 1

FDA
NDA 212099 (label) INN (DAROLUTAMIDE) NUBEQA (BAYER HEALTHCARE) APPROVAL= AP YEAR= 2019 NEWMOLECULARENTITY

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

1955

DAROLUTAMIDE

INN
DAROLUTAMIDE

(has an active metabolite)

cas 1297538-32-9

CLASS

ANTINEOPLASTIC
ANDROGEN RECEPTOR INHIBITOR
TREATMENT OF NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER

ROUTE (list)

ORAL

ATC code

L02BB06

PK parameters

F 30 PERCENT
Tmax 4 HOUR
Cmax 12 MICROMOLAR
VD 119 LITER
Cl 6.96 LITER / HOUR
PPB 92 PERCENT
t1/2 20 HOUR

Solubility

PRACTICALLY INSOLUBLE IN AQUEOUS MEDIUM

Target

TARGET ANDROGEN RECEPTOR (AR)

Androgen receptor UNIPROT P10275 AR

Download SDF file

1H-Pyrazole-3-carboxamide, N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-

Formula:
C19H19ClN6O2

Calculated chemical properties:

MW 398.85
NB_atoms 28
XLogP 2.67
PSA 109.043
NB_HD 3
NB_HA 8
fsp3 0.26
Lipinski(0=no;1=yes) 1

FDA
NDA 212099 (label) INN (DAROLUTAMIDE) NUBEQA (BAYER HEALTHCARE) APPROVAL= AP YEAR= 2019 NEWMOLECULARENTITY

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL