e-Drug3D

1906

BINIMETINIB

INN
BINIMETINIB

cas 606143-89-9

CLASS

ANTINEOPLASTIC
MEK1 AND MEK2 KINASE INHIBITOR
TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH A BRAF V600E OR V600K MUTATION

ROUTE (list)

ORAL

ATC code

L01EE03

PK parameters

F 50 PERCENT
Tmax 1.6 HOUR
VD 92 LITER
Cl 20.2 LITER / HOUR
PPB 97 PERCENT
t1/2 3.5 HOUR

Solubility

INSOLUBLE IN WATER AT PH 4.5 AND HIGHER

Target

TARGET MEK1 AND MEK2

PDB
7M0U (CRYSTAL STRUCTURE OF THE BRAF:MEK1 KINASES IN COMPLEX WITH AMPPNP AND BINIMETINIB)

Ligand code = QO7 (link to the list of PDB complexes)

Download experimental 3D coordinates of QO7 with added hydrogens

DrugCentral

Dual specificity mitogen-activated protein kinase kinase 1 UNIPROT Q02750 MAP2K1

Dual specificity mitogen-activated protein kinase kinase 2 UNIPROT P36507 MAP2K2

Download SDF file

1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-

Formula:
C17H15BrF2N4O3

Calculated chemical properties:

MW 441.23
NB_atoms 27
XLogP 3.01
PSA 83.937
NB_HD 3
NB_HA 7
fsp3 0.18
Lipinski(0=no;1=yes) 1

FDA
NDA 210498 (label) INN (BINIMETINIB) MEKTOVI (ARRAY BIOPHARMA INC) APPROVAL= AP YEAR= 2018 NEWMOLECULARENTITY
NDA 217678 (pdf not found) INN (BINIMETINIB) BINIMETINIB (ALEMBIC PHARMS LTD) APPROVAL= TA YEAR= 2024
NDA 217509 (pdf not found) INN (BINIMETINIB) BINIMETINIB (TEVA PHARMACEUTICALS USA, INC.) APPROVAL= TA YEAR= 2024