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Taselisib

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Chemical compound Pharmaceutical compound
Taselisib
Clinical data
ATC code
  • None
Identifiers
IUPAC name
  • 2-{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
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

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).

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. Currently running clinical trials 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. "ClinicalTrials.gov". clinicaltrials.gov.


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