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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
LAPATINIB

LAPATINIB


ATC L01EH01

ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
METASTATIC BREAST CANCER WHOSE TUMORS OVEREXPRESS HER2

ORAL

Cmax 4.18 MICROMOLAR (1.250 MILLIGRAM DAILY))

Tmax 4 HOUR

PPB 99 PERCENT

HT 14.2 HOUR

SOLUBILITY 0.007 MILLIGRAM / MILLILITER

HUMAN EPIDERMAL RECEPTOR TYPE 2 (RECEPTOR TYROSINE-PROTEIN KINASE HER2 ERBB-2 KI = 3 NANOMOLAR)
EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR KI = 13 NANOMOLAR)

PDB 1XKK (EGFR KINASE DOMAIN COMPLEXED WITH A QUINAZOLINE INHIBITOR- GW572016)

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

Download experimental 3D coordinates of FMM with added hydrogens

Epidermal growth factor receptor UNIPROT P00533 EGFR -- Receptor tyrosine-protein kinase erbB-2 UNIPROT P04626 ERBB2

more at DrugCentral

EMA

ANSM (in French)

Inxight Drugs
Dailymed
Drugs.com

SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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