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Buparlisib

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Buparlisib
Clinical data
ATC code
  • None
Identifiers
  • 5-[2,6-bis(morpholin-4-yl)pyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine
PubChem CID
ChemSpider
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard100.232.248 Edit this at Wikidata
Chemical and physical data
FormulaC18H21F3N6O2
Molar mass410.39 g/mol
3D model (JSmol)
  • NC1=NC=C(C2=CC(=NC(=N2)N2CCOCC2)N2CCOCC2)C(=C1)C(F)(F)F

Buparlisib (INN,[1] codenamed BKM120) is an investigational small molecule orally-available pan-class I phosphoinositide 3-kinase inhibitor.[2]

Clinical trials

In December 2015 it is reporting results for the phase III BELLE-2 clinical trial for advanced HR+/HER2 endocrine-resistant breast cancer.[3] Encouraging results are reported in some sub-populations — e.g., some PI3K mutations.[3][4]

See also

References

  1. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 68" (PDF). World Health Organization. p. 304. Retrieved 16 April 2016.
  2. ^ Geuna, E; Milani, A; Martinello, R; Aversa, C; Valabrega, G; Scaltriti, M; Montemurro, F (March 2015). "Buparlisib, an oral pan-PI3K inhibitor for the treatment of breast cancer". Expert Opinion on Investigational Drugs. 24 (3): 421–31. doi:10.1517/13543784.2015.1008132. PMID 25645727.
  3. ^ a b PI3K Inhibitor Penetrates Endocrine-Resistant Breast Cancer. Dec 2015
  4. ^ Buparlisib Benefits Women With PIK3CA Mutations in Circulating Tumor DNA. Dec 2015
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