e-Drug3D

1831

NERATINIB


INN
NERATINIB

cas 698387-09-6
CLASS

ANTINEOPLASTIC
TREATMENT OF ADULT PATIENTS WITH EARLY STAGE HER2-OVEREXPRESSED/AMPLIFIED BREAST CANCER
EGFR KINASE INHIBITOR
HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2) AND HER4 INHIBITOR

ROUTE (list)

ORAL

ATC code

L01EH02

PK parameters

Tmax 5 HOUR
VD 6433 LITER
Cl 281 LITER / HOUR
PPB 99 PERCENT
t1/2 14.6 HOUR

Solubility

SPARINGLY SOLUBLE AT PH 1.2 (32.90 MG/ML) AND INSOLUBLE AT APPROXIMATE PH 5.0 AND ABOVE (0.08 MG/ML OR LESS)


Target

TARGET EGFR
HER2
HER4

DrugCentral

Receptor tyrosine-protein kinase erbB-4 UNIPROT Q15303 ERBB4

Epidermal growth factor receptor UNIPROT P00533 EGFR

Download SDF file 2-Butenamide, N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-, (2E)-

Formula:
C30H29ClN6O3

Calculated chemical properties:

MW 557.04
NB_atoms 40
XLogP 5.93
PSA 102.26
NB_HD 2
NB_HA 9
fsp3 0.20
Lipinski(0=no;1=yes) 0

FDA
NDA 208051 (label) INN (NERATINIB MALEATE) NERLYNX (PUMA BIOTECH) APPROVAL= AP YEAR= 2017 NEWMOLECULARENTITY
NDA 216236 (pdf not found) INN (NERATINIB MALEATE) NERATINIB MALEATE (SANDOZ INC) APPROVAL= TA YEAR= 2022

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL