DGIdb - APITOLISIB Drug Record

APITOLISIB chembl:CHEMBL1922094 Antineoplastic

Alternate Names:

G-038390.1
GDC-0980
GDC-0980.1
APITOLISIB
G-038390
RG-7422

Drug Info:

Notes	catalytic, dual PI3K/mTOR inhibitor
Drug Class	Kinase Inhibitors

(1 More Sources)

Publications:

Powles et al., 2016, Randomized Open-Label Phase II Trial of Apitolisib (GDC-0980), a Novel Inhibitor of the PI3K/Mammalian Target of Rapamycin Pathway, Versus Everolimus in Patients With Metastatic Renal Cell Carcinoma., J. Clin. Oncol.
Dolly et al., 2016, Phase I Study of Apitolisib (GDC-0980), Dual Phosphatidylinositol-3-Kinase and Mammalian Target of Rapamycin Kinase Inhibitor, in Patients with Advanced Solid Tumors., Clin. Cancer Res.
Wallin et al., 2011, GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway., Mol. Cancer Ther.
Soares et al., 2015, Dual PI3K/mTOR Inhibitors Induce Rapid Overactivation of the MEK/ERK Pathway in Human Pancreatic Cancer Cells through Suppression of mTORC2., Mol. Cancer Ther.
Parrotta R et al., 2017, A Novel BRCA1-Associated Protein-1 Isoform Affects Response of Mesothelioma Cells to Drugs Impairing BRCA1-Mediated DNA Repair., J Thorac Oncol

APITOLISIB BARD1

Interaction Score: 1.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28389374

Sources:
CIViC
APITOLISIB BAP1

Interaction Score: 0.98

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28389374

Sources:
CIViC
APITOLISIB VHL

Interaction Score: 0.39

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type renal cell carcinoma

Response Type no benefit

Approval Status Phase II

PMIDs:
26951309

Sources:
JAX-CKB
APITOLISIB PIK3C2A

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
APITOLISIB PIK3C2B

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
APITOLISIB PIK3C3

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
APITOLISIB PIK3C2G

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
APITOLISIB PIK3R6

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
APITOLISIB PIK3R4

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
APITOLISIB 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:
MyCancerGenome ChemblInteractions
APITOLISIB 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:
MyCancerGenome ChemblInteractions
APITOLISIB PIK3R1

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
APITOLISIB PIK3R2

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
APITOLISIB PIK3CD

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
APITOLISIB PIK3CA

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type no benefit

Indication/Tumor Type renal cell carcinoma

Indication/Tumor Type malignant pleural mesothelioma

PMIDs:
26951309 26787751 21998291

Sources:
MyCancerGenome JAX-CKB ChemblInteractions
APITOLISIB 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:
MyCancerGenome ChemblInteractions
APITOLISIB PIK3CG

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
APITOLISIB KRAS

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colon cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25673820 21998291

Sources:
JAX-CKB
APITOLISIB PTEN

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type endometrial cancer

Response Type sensitive

Approval Status Phase II

PMIDs:
26951309

Sources:
JAX-CKB
APITOLISIB MTOR

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase mTOR inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
APITOLISIB AKT1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type endometrial cancer

Response Type sensitive

Approval Status Phase II

PMIDs:
None found

Sources:
JAX-CKB

MyCancerGenome: GDC-0980
- Version: 20-Jun-2017
Alternate Names:

GDC-0980 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes catalytic, dual PI3K/mTOR inhibitor

Publications:

JAX-CKB: GDC-0980

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Powles et al., 2016, Randomized Open-Label Phase II Trial of Apitolisib (GDC-0980), a Novel Inhibitor of the PI3K/Mammalian Target of Rapamycin Pathway, Versus Everolimus in Patients With Metastatic Renal Cell Carcinoma., J. Clin. Oncol.

Soares et al., 2015, Dual PI3K/mTOR Inhibitors Induce Rapid Overactivation of the MEK/ERK Pathway in Human Pancreatic Cancer Cells through Suppression of mTORC2., Mol. Cancer Ther.

Wallin et al., 2011, GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway., Mol. Cancer Ther.

CIViC: APITOLISIB
- Version: 14-September-2020
Alternate Names:

Drug Info:

Publications:

Parrotta R et al., 2017, A Novel BRCA1-Associated Protein-1 Isoform Affects Response of Mesothelioma Cells to Drugs Impairing BRCA1-Mediated DNA Repair., J Thorac Oncol
ChemblDrugs: chembl:CHEMBL1922094
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1922094
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	renal cell carcinoma
Response Type	no benefit
Approval Status	Phase II

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

Indication/Tumor Type	colon cancer
Response Type	sensitive
Approval Status	Preclinical - Cell line xenograft

Indication/Tumor Type	endometrial cancer
Response Type	sensitive
Approval Status	Phase II

Mechanism of Interaction	Serine/threonine-protein kinase mTOR inhibitor
Direct Interaction	yes

APITOLISIB Drug Record

APITOLISIB chembl:CHEMBL1922094 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28389374

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28389374

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type renal cell carcinoma Response Type no benefit Approval Status Phase II

PMIDs: 26951309

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Response Type no benefit Indication/Tumor Type renal cell carcinoma Indication/Tumor Type malignant pleural mesothelioma

PMIDs: 26951309 26787751 21998291

Sources: MyCancerGenome JAX-CKB ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colon cancer Response Type sensitive Approval Status Preclinical - Cell line xenograft

PMIDs: 25673820 21998291

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type endometrial cancer Response Type sensitive Approval Status Phase II

PMIDs: 26951309

Interaction Types & Directionality:

n/a

PMIDs:
28389374

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
28389374

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type renal cell carcinoma

Response Type no benefit

Approval Status Phase II

PMIDs:
26951309

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type no benefit

Indication/Tumor Type renal cell carcinoma

Indication/Tumor Type malignant pleural mesothelioma

PMIDs:
26951309 26787751 21998291

Sources:
MyCancerGenome JAX-CKB ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colon cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25673820 21998291

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type endometrial cancer

Response Type sensitive

Approval Status Phase II

PMIDs:
26951309

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase mTOR inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type endometrial cancer

Response Type sensitive

Approval Status Phase II

PMIDs:
None found

Sources:
JAX-CKB

Alternate Names:

GDC-0980 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes catalytic, dual PI3K/mTOR inhibitor

Publications:

Parrotta R et al., 2017, A Novel BRCA1-Associated Protein-1 Isoform Affects Response of Mesothelioma Cells to Drugs Impairing BRCA1-Mediated DNA Repair., J Thorac Oncol