Taselisib Explained

Iupac Name:	2--2-methylpropanamide
Cas Number:	1282512-48-4
Atc Prefix:	None
Pubchem:	51001932
Kegg:	D11774
Chemspiderid:	29315044
Unii:	L08J2O299M
Chembl:	2387080
C:	24
H:	28
N:	8
O:	2
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
Stdinchi:	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)
Stdinchikey:	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.

Notes and References

1. Web site: Definition of taselisib - NCI Drug Dictionary - National Cancer Institute . Cancer.gov . 2017-01-10.
2. Zumsteg ZS, Morse N, Krigsfeld G, Gupta G, Higginson DS, Lee NY, Morris L, Ganly I, Shiao SL, Powell SN, Chung CH, Scaltriti M, Baselga J . 6 . 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 . April 2016 . 26589432 . 4870591 . 10.1158/1078-0432.CCR-15-2245 .
3. Web site: 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=