Lapatinib

Lapatinib
Clinical data
Trade names	Tykerb, Tyverb, others
AHFS/Drugs.com	Monograph
MedlinePlus	a607055
License data	EU EMA: by INN; US DailyMed: Lapatinib; US FDA: Lapatinib;
Pregnancy; category	AU: C;
Routes of; administration	By mouth (tablets)
ATC code	L01EH01 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: WARNINGRx-only; In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	Variable, increased with food
Protein binding	>99%
Metabolism	Liver, mostly CYP3A-mediated (minor 2C19 and 2C8 involvement)
Elimination half-life	24 hours (repeated dosing), 14.2 hours (single dose)
Excretion	Mostly Feces
Identifiers
	IUPAC name N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-; [5-[(2-methylsulfonylethylamino)methyl]-2-furyl]; quinazolin-4-amine;
CAS Number	231277-92-2 ; as salt: 388082-78-8 ;
PubChem CID	208908;
IUPHAR/BPS	5692;
DrugBank	DB01259 ; as salt: DBSALT001785 ;
ChemSpider	181006 ; as salt: 9731817 ;
UNII	0VUA21238F; as salt: G873GX646R ;
KEGG	D08108 ; as salt: D04024 ;
ChEBI	CHEBI:49603 ;
ChEMBL	ChEMBL554 ; as salt: ChEMBL1201179 ;
PDB ligand	FMM (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID7046675 ;
Chemical and physical data
Formula	C29H26ClFN4O4S
Molar mass	581.06 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CS(=O)(=O)CCNCc1ccc(o1)c2ccc3c(c2)c(ncn3)Nc4ccc(c(c4)Cl)OCc5cccc(c5)F;
	InChI InChI=1S/C29H26ClFN4O4S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35) ; Key:BCFGMOOMADDAQU-UHFFFAOYSA-N ;
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Lapatinib (INN), used in the form of lapatinib ditosylate (USAN) (trade names Tykerb and Tyverb marketed by Novartis) is an orally active drug for breast cancer and other solid tumours. It is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways. It is used in combination therapy for HER2-positive breast cancer. It is used for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 (ErbB2).

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