e-Drug3D

930

ERLOTINIB


INN
ERLOTINIB

cas 183321-74-6
CLASS

ANTINEOPLASTIC
SIGNAL TRANSDUCTION INHIBITOR
GROWTH HORMONE RECEPTOR INHIBITOR
ANTICANCER
PROTEIN KINASE INHIBITORS
TREATMENT OF NON-SMALL CELL LUNG CANCER

ROUTE (list)

ORAL

ATC code

L01EB02

PK parameters

F 100 PERCENT
VD 232 LITER
Cl 4.4 LITER / HOUR (EQN)
PPB 93 PERCENT
t1/2 36.2 HOUR

Solubility

VERY SLIGHTLY SOLUBLE IN WATER


Target

TARGET EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR)

PDB
4HJO (CRYSTAL STRUCTURE OF THE INACTIVE EGFR TYROSINE KINASE DOMAIN WITH ERLOTINIB)

Ligand code = AQ4 (link to the list of PDB complexes)

Download experimental 3D coordinates of AQ4 with added hydrogens

DrugCentral

Epidermal growth factor receptor UNIPROT P00533 EGFR

Download SDF file N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine

Formula:
C22H23N3O4

Calculated chemical properties:

MW 393.43
NB_atoms 29
XLogP 3.41
PSA 74.211
NB_HD 1
NB_HA 7
fsp3 0.27
Lipinski(0=no;1=yes) 1

FDA
NDA 021743 (label) INN (ERLOTINIB HYDROCHLORIDE) TARCEVA (OSI PHARMS) APPROVAL= AP YEAR= 2004 DISCONTINUED
NDA 091002 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (RISING) APPROVAL= AP YEAR= 2014
NDA 091059 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (TEVA PHARMS USA INC) APPROVAL= AP YEAR= 2015
NDA 208488 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (NATCO PHARMA LTD) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 208396 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (APOTEX) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 210300 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (SUN PHARM) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 211960 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (SHILPA) APPROVAL= AP YEAR= 2019
NDA 211083 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (ACCORD HLTHCARE) APPROVAL= AP YEAR= 2020 DISCONTINUED
NDA 213065 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (ZYDUS PHARMS) APPROVAL= AP YEAR= 2020
NDA 214366 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (MSN) APPROVAL= AP YEAR= 2021
NDA 214719 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (ALEMBIC) APPROVAL= AP YEAR= 2021
NDA 216342 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (EUGIA PHARMA) APPROVAL= AP YEAR= 2022 DISCONTINUED
NDA 209267 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (HETERO LABS LTD V) APPROVAL= AP YEAR= 2024
NDA 203843 (pdf not found) INN (ERLOTINIB HYDROCHLORIDE) ERLOTINIB HYDROCHLORIDE (CHARTWELL RX) APPROVAL= AP YEAR= 2024

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL