Buparlisib

Buparlisib
Clinical data
ATC code
  • None
Identifiers
PubChem CID
ChemSpider
KEGG
Chemical and physical data
Formula C18H21F3N6O2
Molar mass 410.39 g/mol
3D model (JSmol)

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]

A Phase Ib clinical trial combined buparlisib and letrozole in the treatment of estrogen receptor-positive/human epidermal growth factor receptor 2-negative metastatic cancer. Results indicated that the drug combination was safe on two different treatment schedules and the clinical benefit rate was 31%. Common toxicities included hyperglycemia, nausea, fatigue, transaminitis, and mood disorders, though the toxicities are reversible and well-tolerated.[5]

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. 1 2 PI3K Inhibitor Penetrates Endocrine-Resistant Breast Cancer. Dec 2015
  4. ↑ Buparlisib Benefits Women With PIK3CA Mutations in Circulating Tumor DNA. Dec 2015
  5. ↑ Stand Up to Cancer Phase Ib Study of Pan-Phosphoinositide-3-Kinase Inhibitor Buparlisib With Letrozole in Estrogen Receptor-Positive/Human Epidermal Growth Factor Receptor 2-Negative Metastatic Breast Cancer April 2014
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