Taselisib

Taselisib (development code: GDC-0032) is a former cancer drug candidate that was in development by Roche. It is a small molecule phosphoinositide 3-kinase inhibitor targeting the PI3K isoform p110α (PIK3CA).[1][2]

Taselisib
Clinical data
ATC code
  • None
Identifiers
IUPAC name
  • 2-{4-[2-(1-Isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H28N8O2
Molar mass460.542 g·mol−1
3D model (JSmol)
SMILES
  • CC1=NN(C(=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)C5=CN(N=C5)C(C)(C)C(=O)N)C(C)C
InChI
  • InChI=1S/C24H28N8O2/c1-14(2)32-22(27-15(3)29-32)19-13-30-8-9-34-20-10-16(6-7-18(20)21(30)28-19)17-11-26-31(12-17)24(4,5)23(25)33/h6-7,10-14H,8-9H2,1-5H3,(H2,25,33)
  • Key:BEUQXVWXFDOSAQ-UHFFFAOYSA-N

Roche announced in June 2018 that there would be no further development of taselislib following the top line results of the Phase III "Sandpiper" study.[3] Currently running clinical trials[4] were continued for patients exhibiting benefit.

References
  1. "Definition of taselisib - NCI Drug Dictionary - National Cancer Institute". Cancer.gov. Retrieved 2017-01-10.
  2. Zumsteg ZS, Morse N, Krigsfeld G, Gupta G, Higginson DS, Lee NY, et al. (April 2016). "Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations". Clinical Cancer Research. 22 (8): 2009–19. doi:10.1158/1078-0432.CCR-15-2245. PMC 4870591. PMID 26589432.
  3. "Roche dumps its PhIII PI3K effort on taselisib after researchers track poor survival edge, harsh side effects for breast cancer".
  4. https://clinicaltrials.gov/ct2/results?term=taselisib&Search=Apply&recrs=d&age_v=&gndr=&type=&rslt=


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