Taselisib

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	1282512-48-4;
PubChem CID	51001932;
ChemSpider	29315044;
UNII	L08J2O299M;
KEGG	D11774;
ChEMBL	ChEMBL2387080;
CompTox Dashboard (EPA)	DTXSID00155842 ;
Chemical and physical data
Formula	C24H28N8O2
Molar mass	460.542 g·mol−1
3D model (JSmol)	Interactive image;
	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).^[1]^[2]

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

^ "Definition of taselisib - NCI Drug Dictionary - National Cancer Institute". Cancer.gov. Retrieved 2017-01-10.
^ 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.
^ "Roche dumps its PhIII PI3K effort on taselisib after researchers track poor survival edge, harsh side effects for breast cancer".
^ "ClinicalTrials.gov". clinicaltrials.gov.

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[1] "Definition of taselisib - NCI Drug Dictionary - National Cancer Institute". Cancer.gov. Retrieved 2017-01-10.

[pmid26589432-2] 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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[2]

[3]

[4]

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	1282512-48-4
PubChem CID	51001932
ChemSpider	29315044
UNII	L08J2O299M
KEGG	D11774
ChEMBL	ChEMBL2387080
CompTox Dashboard (EPA)	DTXSID00155842
Chemical and physical data
Formula	C₂₄H₂₈N₈O₂
Molar mass	460.542 g·mol⁻¹
3D model (JSmol)	Interactive image
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