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1 INNClassRoute (list)PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that value was calculated using VD=(Cl*t1/2)/0.693)Primary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
AFATINIB

AFATINIB


ATC L01XE13

ANTINEOPLASTIC
TREATMENT OF METASTATIC NON-SMALL CELL LUNG CANCER
TYROSINE KINASE INHIBITOR
COVALENTLY BINDS TO THE KINASE DOMAINS OF EGFR (ERBB1), HER2 (ERBB2), AND HER4 (ERBB4) AND IRREVERSIBLY INHIBITS TYROSINE KINASE AUTOPHOSPHORYLATION, RESULTING IN DOWNREGULATION OF ERBB SIGNALING

ORAL

Tmax 3.5 HOUR

F 92 PERCENT

PPB 95 PERCENT

HT 37 HOUR

SOLUBILITY SOLUBLE IN WATER

EGFR (ERBB1)
HER2 (ERBB2)
HER4 (ERBB4)

PDB 4G5J (CRYSTAL STRUCTURE OF EGFR KINASE IN COMPLEX WITH BIBW2992)

LIGAND CODE = 0WM (link to the list of PDB complexes)

Download experimental 3D coordinates of 0WM with added hydrogens

EPIDERMAL GROWTH FACTOR RECEPTOR ERBB1 INHIBITOR CHEMBL203 EPIDERMAL GROWTH FACTOR RECEPTOR ERBB1 P00533 EPIDERMAL GROWTH FACTOR RECEPTOR HOMO SAPIENS ENZYME KINASE PROTEIN KINASE TK EGFREMA

ANSM (in French)

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