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BIBW 2992
Systematic (IUPAC) name
N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3''S'')-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4(dimethylamino)-2-butenamide
Identifiers
CAS number 439081-18-2
ATC code none
PubChem 10184653
ChemSpider 8360155
Chemical data
Formula C24H25ClFN5O3 
Mol. mass 485.937 g/mol
SMILES eMolecules & PubChem
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral

BIBW 2992 (planned trade name Tovok) is a candidate drug against non-small cell lung carcinoma, developed by Boehringer Ingelheim. As of December 2008, it is undergoing a Phase III clinical trial for this indication, and Phase II trials for breast, prostate, and head and neck cancers, as well as glioma.[1][2]

Mechanism of action

Like lapatinib and neratinib, BIBW 2992 is a next generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. BIBW-2992 is not only active against EGFR mutations targeted by first generation TKIs like erlotinib or gefitinib, but also against those not sensitive to these standard therapies. Because of its additional activity against Her2, it is investigated for breast cancer as well as other EGFR and Her2 driven cancers.[2]

References

  1. ^ H. Spreitzer (May 13, 2008). "Neue Wirkstoffe - Tovok" (in German). Österreichische Apothekerzeitung (10/2008): 498. 
  2. ^ a b Minkovsky N, Berezov A (December 2008). "BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors". Curr Opin Investig Drugs 9 (12): 1336–46. PMID 19037840. 
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