Neratinib

Neratinib
Clinical data
Routes of; administration	Oral
ATC code	none;
Identifiers
	IUPAC name (2E)-N-[4-[[3-chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide;
CAS Number	698387-09-6 ;
PubChem CID	9915743;
IUPHAR/BPS	5686;
ChemSpider	8091392 ;
UNII	JJH94R3PWB;
KEGG	D08950 ;
ChEMBL	ChEMBL180022 ;
CompTox Dashboard (EPA)	DTXSID70220132 ;
ECHA InfoCard	100.241.512
Chemical and physical data
Formula	C30H29ClN6O3
Molar mass	557.04 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C(/C=C/CN(C)C)Nc4cc1c(ncc(C#N)c1Nc3ccc(OCc2ncccc2)c(Cl)c3)cc4OCC;
	InChI InChI=1S/C30H29ClN6O3/c1-4-39-28-16-25-23(15-26(28)36-29(38)9-7-13-37(2)3)30(20(17-32)18-34-25)35-21-10-11-27(24(31)14-21)40-19-22-8-5-6-12-33-22/h5-12,14-16,18H,4,13,19H2,1-3H3,(H,34,35)(H,36,38)/b9-7+ ; Key:JWNPDZNEKVCWMY-VQHVLOKHSA-N ;
	(what is this?) (verify)

Neratinib (HKI-272) is a tyrosine kinase inhibitor^[1]^[2] under investigation for the treatment of breast cancer^[3] and other solid tumours.

It is in development for the treatment of early- and late-stage HER2-positive breast cancer.^[4]

Clinical trials

Neratanib is being developed by Puma Biotechnology. It will be included in the forthcoming I-SPY2 breast cancer trial.^[6]

Neratinib inhibits the epidermal growth factor receptor by covalently binding with a cysteine side chain in that protein.^[7]

^ "Definition of neratinib - National Cancer Institute Drug Dictionary". Retrieved 2008-12-01.
^ Rabindran SK, Discafani CM, Rosfjord EC, et al. (June 2004). "Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase". Cancer Res. 64 (11): 3958–65. doi:10.1158/0008-5472.CAN-03-2868. PMID 15173008.
^ Clinical trial number NCT00398567 for "A Phase 1/2 Study Of HKI-272 In Combination With Herceptin In Subjects With Advanced Breast Cancer" at ClinicalTrials.gov
^ "Puma Acquires Global Rights to Pfizer's Phase III Breast Cancer Drug Neratinib".
^ Minami Y, Shimamura T, Shah K, et al. (July 2007). "The major lung cancer-derived mutants of ERBB2 are oncogenic and are associated with sensitivity to the irreversible EGFR/ERBB2 inhibitor HKI-272". Oncogene. 26 (34): 5023–7. doi:10.1038/sj.onc.1210292. PMID 17311002.
^ http://www.reuters.com/article/idUSN1612347120100317 "Breast cancer study aims to speed drugs, cooperation" March 2010
^ http://www.biomedicale.univ-paris5.fr/enseignement/toxico/M2THERV_2013_2014/documents/C15/DANSETTE/EH_CB_RM_M2/CovalentDrug_Baillie_nrd3410.pdf

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