DGIdb - TASELISIB Drug Record

TASELISIB chembl:CHEMBL2387080 Antineoplastic

Alternate Names:

RG-7604
TASELISIB
GDC-0032
GDC0032
drugbank:12108
pubchem.compound:51001932
chembl:CHEMBL2387080
chemidplus:1282512-48-4

Drug Info:

Drug Class	Kinase Inhibitors

(3 More Sources)

Publications:

Zumsteg et al., 2016, Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations., Clin. Cancer Res.
Lopez et al., 2014, Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo., Gynecol. Oncol.
Ndubaku et al., 2013, Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity., J. Med. Chem.
Lopez et al., 2015, Dual HER2/PIK3CA Targeting Overcomes Single-Agent Acquired Resistance in HER2-Amplified Uterine Serous Carcinoma Cell Lines In Vitro and In Vivo., Mol. Cancer Ther.
Juric et al., 2017, Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors., Cancer Discov

TASELISIB PIK3CA

Interaction Score: 0.44

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

Indication/Tumor Type colorectal cancer

PMIDs:
25172762 23662903 26589432 26333383 28331003

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CIViC TTD OncoKB
TASELISIB PIK3R5

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TASELISIB PIK3R3

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TASELISIB PTEN

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

PMIDs:
26589432

Sources:
JAX-CKB CIViC
TASELISIB PIK3R1

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TASELISIB PIK3R2

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
TASELISIB PIK3CG

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
ChemblInteractions TTD
TASELISIB PIK3CD

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TASELISIB ERBB2

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC-0032 + Neratinib

Indication/Tumor Type uterine corpus serous adenocarcinoma

Response Type sensitive

PMIDs:
25172762 26333383

Sources:
JAX-CKB
TASELISIB PIK3CB

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TASELISIB KRAS

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type no benefit

Indication/Tumor Type colorectal cancer

Evidence Type Actionable

PMIDs:
28331003

Sources:
JAX-CKB

MyCancerGenome: GDC-0032
- Version: 20-Jun-2017
Alternate Names:

Drug Info:

Drug Class Kinase Inhibitors

Publications:

JAX-CKB: GDC-0032

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Lopez et al., 2014, Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo., Gynecol. Oncol.

Lopez et al., 2015, Dual HER2/PIK3CA Targeting Overcomes Single-Agent Acquired Resistance in HER2-Amplified Uterine Serous Carcinoma Cell Lines In Vitro and In Vivo., Mol. Cancer Ther.

Juric et al., 2017, Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors., Cancer Discov

CIViC: TASELISIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Zumsteg et al., 2016, Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations., Clin. Cancer Res.

TTD: GDC-0032
- Version: 2020.06.01
Alternate Names:

D0UP1Z TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2387080
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL2387080
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
OncoKB: Taselisib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:

Direct Interaction	yes
Mechanism of Interaction	PI3-kinase class I inhibitor
Indication/Tumor Type	colorectal cancer

Approval Status	Preclinical
Evidence Type	Actionable
Approval Status	Preclinical - Cell line xenograft

combination therapy	GDC-0032 + Neratinib
Indication/Tumor Type	uterine corpus serous adenocarcinoma
Response Type	sensitive

Response Type	no benefit
Indication/Tumor Type	colorectal cancer
Evidence Type	Actionable

TASELISIB Drug Record

TASELISIB chembl:CHEMBL2387080 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction PI3-kinase class I inhibitor Indication/Tumor Type colorectal cancer

PMIDs: 25172762 23662903 26589432 26333383 28331003

Sources: MyCancerGenome JAX-CKB ChemblInteractions CIViC TTD OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction PI3-kinase class I inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction PI3-kinase class I inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Approval Status Preclinical Evidence Type Actionable Approval Status Preclinical - Cell line xenograft

PMIDs: 26589432

Sources: JAX-CKB CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction PI3-kinase class I inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction PI3-kinase class I inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: combination therapy GDC-0032 + Neratinib Indication/Tumor Type uterine corpus serous adenocarcinoma Response Type sensitive

PMIDs: 25172762 26333383

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction PI3-kinase class I inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Response Type no benefit Indication/Tumor Type colorectal cancer Evidence Type Actionable

PMIDs: 28331003

Sources: JAX-CKB

MyCancerGenome: GDC-0032

Alternate Names:

Drug Info: Drug Class Kinase Inhibitors

Publications:

JAX-CKB: GDC-0032

Alternate Names:

Drug Info:

CIViC: TASELISIB

Alternate Names:

Drug Info:

Publications: Zumsteg et al., 2016, Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations., Clin. Cancer Res.

TTD: GDC-0032

Alternate Names: D0UP1Z TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL2387080

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL2387080

Alternate Names:

Drug Info:

Publications:

OncoKB: Taselisib

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

Indication/Tumor Type colorectal cancer

PMIDs:
25172762 23662903 26589432 26333383 28331003

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CIViC TTD OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

PMIDs:
26589432

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC-0032 + Neratinib

Indication/Tumor Type uterine corpus serous adenocarcinoma

Response Type sensitive

PMIDs:
25172762 26333383

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type no benefit

Indication/Tumor Type colorectal cancer

Evidence Type Actionable

PMIDs:
28331003

Sources:
JAX-CKB

Drug Info:

Drug Class Kinase Inhibitors

Publications:

Zumsteg et al., 2016, Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations., Clin. Cancer Res.

Alternate Names:

D0UP1Z TTD Drug ID