Buparlisib

Buparlisib
Clinical data
ATC code
  • None
Identifiers
IUPAC name
  • 5-[2,6-bis(morpholin-4-yl)pyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard100.232.248
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Chemical and physical data
FormulaC18H21F3N6O2
Molar mass410.401 g·mol−1
3D model (JSmol)
SMILES
  • NC1=NC=C(C2=CC(=NC(=N2)N2CCOCC2)N2CCOCC2)C(=C1)C(F)(F)F
InChI
  • InChI=1S/C18H21F3N6O2/c19-18(20,21)13-9-15(22)23-11-12(13)14-10-16(26-1-5-28-6-2-26)25-17(24-14)27-3-7-29-8-4-27/h9-11H,1-8H2,(H2,22,23) ☒N
  • Key:CWHUFRVAEUJCEF-UHFFFAOYSA-N ☒N

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]Lawrence L (11 December 2015). "Buparlisib Benefits Women With PIK3CA Mutations in Circulating Tumor DNA". Cancer Network.</ref>

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.[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. S2CID 40698715.
  3. 1 2 Johnson K (14 December 2015). "PI3K Inhibitor Penetrates Endocrine-Resistant Breast Cancer". MedScape.
  4. ↑ Mayer IA, Abramson VG, Isakoff SJ, Forero A, Balko JM, Kuba MG, et al. (April 2014). "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". Journal of Clinical Oncology. 32 (12): 1202–9. doi:10.1200/JCO.2013.54.0518. PMC 3986383. PMID 24663045.
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