Neratinib

Neratinib
Neratinib
Systematic (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
Clinical data
Pregnancy cat.  ?
Legal status  ?
Routes Oral
Identifiers
CAS number 698387-09-6 YesY
ATC code None
PubChem CID 9915743
ChemSpider 8091392 YesY
UNII JJH94R3PWB N
KEGG D08950 YesY
ChEMBL CHEMBL180022 YesY
Chemical data
Formula C30H29ClN6O3 
Mol. mass 557.04 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

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

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

Like lapatinib and afatinib, it is a dual inhibitor of the human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases.[5]

Clinical trials

It will be included in the forthcoming I-SPY2 breast cancer trial.[6]

References

  1. ^ "Definition of neratinib - National Cancer Institute Drug Dictionary". http://www.cancer.gov/Templates/drugdictionary.aspx?CdrID=453548. Retrieved 2008-12-01. 
  2. ^ 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. http://cancerres.aacrjournals.org/cgi/pmidlookup?view=long&pmid=15173008. 
  3. ^ ClinicalTrials.gov NCT00398567 A Phase 1/2 Study Of HKI-272 In Combination With Herceptin In Subjects With Advanced Breast Cancer
  4. ^ "Puma Acquires Global Rights to Pfizer’s Phase III Breast Cancer Drug Neratinib". http://www.genengnews.com/gen-news-highlights/puma-acquires-global-rights-to-pfizer-s-phase-iii-breast-cancer-drug-neratinib/81245787/. 
  5. ^ 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. 
  6. ^ http://www.reuters.com/article/idUSN1612347120100317 "Breast cancer study aims to speed drugs, cooperation" March 2010
v · d · eTargeted therapy / extracellular chemotherapeutic agents/antineoplastic agents (L01)
CI monoclonal antibodies ("-mab")
Others for solid tumors
Tyrosine-kinase inhibitors ("-nib")

ErbB: HER1/EGFR (Erlotinib, Gefitinib, Vandetanib) • HER1/EGFR and HER2/neu (Afatinib, Lapatinib, Neratinib)

RTK class III: C-kit and PDGFR (Axitinib, Pazopanib, Sunitinib, Sorafenib, Toceranib) • FLT3 (Lestaurtinib)

VEGFR (Axitinib, Cediranib, Pazopanib, Regorafenib, Semaxanib, Sorafenib, Sunitinib, Toceranib, Vandetanib)
Other
fusion protein against VEGF (Aflibercept) • proapoptotic peptide against ANXA2 and prohibitin (Adipotide) • exotoxin against IL-2 (Denileukin diftitox)

M: NEO

tsoc, mrkr

tumr, epon, para

drug (L1i/1e/V03)


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