Neratinib
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| 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  |
| ATC code | None |
| PubChem | CID 9915743 |
| ChemSpider | 8091392  |
| UNII | JJH94R3PWB |
| KEGG | D08950 |
| ChEMBL | CHEMBL180022 |
| Chemical data | |
| Formula | C30H29ClN6O3 |
| Mol. mass | 557.04 g/mol |
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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 [edit]
It will be included in the forthcoming I-SPY2 breast cancer trial.[6]
References [edit]
- ^ "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.
- ^ ClinicalTrials.gov NCT00398567 A Phase 1/2 Study Of HKI-272 In Combination With Herceptin In Subjects With Advanced Breast Cancer
- ^ "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
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