e-Drug3D

2046

MOBOCERTINIB

DISCONTINUED


INN
MOBOCERTINIB

(has an active metabolite)

cas 1847461-43-1
CLASS

ANTINEOPLASTIC
KINASE INHIBITOR
TREATMENT OF NSCLC WITH EGFR EXON 20 INSERTION MUTATIONS
INHIBITS KINASES HER2, HER4 AND BLK WITH IC50 BELOW 2 NANOMOLAR

ROUTE (list)

ORAL

ATC code

L01EB10

PK parameters

F 37 PERCENT
Tmax 4 HOUR
VD 3509 LITER
Cl 138 LITER / HOUR
PPB 99.3 PERCENT
t1/2 18 HOUR

Solubility

17 MILLIGRAM PER MILLILITER AT PH 6.8


Target

TARGET EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) (MUTATED)
HER2
HER4
BLK

DrugCentral

Epidermal growth factor receptor UNIPROT P00533 EGFR

Receptor tyrosine-protein kinase erbB-2 UNIPROT P04626 ERBB2

Download SDF file 5-Pyrimidinecarboxylic acid, 2-[[4-[[2-(dimethylamino)ethyl]methylamino]-2-methoxy-5-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-4-(1-methyl-1H-indol-3-yl)-, 1-methylethyl ester (ACI)

Formula:
C32H39N7O4

Calculated chemical properties:

MW 585.70
NB_atoms 43
XLogP 5.08
PSA 103.901
NB_HD 2
NB_HA 11
fsp3 0.31
Lipinski(0=no;1=yes) 0

FDA
NDA 215310 (pdf not found) INN (MOBOCERTINIB SUCCINATE) EXKIVITY (TAKEDA PHARMS USA) APPROVAL= AP YEAR= 2021 DISCONTINUED

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL