DGIdb - IPATASERTIB Drug Record

IPATASERTIB chembl:CHEMBL2177390 Antineoplastic

Alternate Names:

GDC-0068
RG-7440
IPATASERTIB

Drug Info:

FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent
Notes	catalytic inhibitor
Drug Class	Kinase Inhibitors

(7 More Sources)

Publications:

Lin et al., 2013, Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models., Clin. Cancer Res.
Yan et al., 2013, Evaluation and clinical analyses of downstream targets of the Akt inhibitor GDC-0068., Clin. Cancer Res.
Saura et al., 2017, A First-in-Human Phase I Study of the ATP-Competitive AKT Inhibitor Ipatasertib Demonstrates Robust and Safe Targeting of AKT in Patients with Solid Tumors., Cancer Discov
de Bono JS et al., 2019, Randomized Phase II Study Evaluating Akt Blockade with Ipatasertib, in Combination with Abiraterone, in Patients with Metastatic Prostate Cancer with and without PTEN Loss., Clin Cancer Res
Blake JF et al., 2012, Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors., J Med Chem
Hayes et al., 2016, Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression., Cancer Cell

IPATASERTIB AKT3

Interaction Score: 1.61

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name GDC-0068

Novel drug target Novel Target

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial
IPATASERTIB AKT2

Interaction Score: 1.61

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Direct Interaction yes

Trial Name GDC-0068

PMIDs:
None found

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial
IPATASERTIB AKT1

Interaction Score: 1.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Approval Status Phase II

Response Type predicted – sensitive

Indication/Tumor Type triple-receptor negative breast cancer

PMIDs:
27872130 22934575

Sources:
DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial TTD
IPATASERTIB PTEN

Interaction Score: 0.55

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ipatasertib + Paclitaxel

Indication/Tumor Type triple-receptor negative breast cancer

Response Type predicted – sensitive

PMIDs:
23287563 24141624 27872130 30037818

Sources:
JAX-CKB CIViC
IPATASERTIB KRAS

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
26725216

Sources:
JAX-CKB
IPATASERTIB PIK3CA

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
24141624

Sources:
JAX-CKB
IPATASERTIB ERBB2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
24141624

Sources:
JAX-CKB

MyCancerGenome: GDC-0068
- Version: 20-Jun-2017
Alternate Names:

GDC-0068 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes catalytic inhibitor

Publications:
TdgClinicalTrial: GDC-0068
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:
DTC: IPATASERTIB
- Version: 02-September-2020
Alternate Names:

CHEMBL2177390 ChEMBL Drug ID

Drug Info:

Publications:

Blake JF et al., 2012, Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors., J Med Chem

JAX-CKB: Ipatasertib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Yan et al., 2013, Evaluation and clinical analyses of downstream targets of the Akt inhibitor GDC-0068., Clin. Cancer Res.

Saura et al., 2017, A First-in-Human Phase I Study of the ATP-Competitive AKT Inhibitor Ipatasertib Demonstrates Robust and Safe Targeting of AKT in Patients with Solid Tumors., Cancer Discov

Hayes et al., 2016, Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression., Cancer Cell

CIViC: IPATASERTIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

de Bono JS et al., 2019, Randomized Phase II Study Evaluating Akt Blockade with Ipatasertib, in Combination with Abiraterone, in Patients with Metastatic Prostate Cancer with and without PTEN Loss., Clin Cancer Res

Lin et al., 2013, Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models., Clin. Cancer Res.

TTD: GDC-0068
- Version: 2020.06.01
Alternate Names:

D0I4TH TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2177390
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: GDC-0068
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL2177390
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
JAX-CKB: GDC-0068
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: GDC-0068
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:

Trial Name	GDC-0068
Novel drug target	Novel Target
Mechanism of Interaction	Serine/threonine-protein kinase AKT inhibitor

Mechanism of Interaction	Serine/threonine-protein kinase AKT inhibitor
Direct Interaction	yes
Trial Name	GDC-0068

Approval Status	Phase II
Response Type	predicted – sensitive
Indication/Tumor Type	triple-receptor negative breast cancer

combination therapy	Ipatasertib + Paclitaxel
Indication/Tumor Type	triple-receptor negative breast cancer
Response Type	predicted – sensitive

Evidence Type	Actionable
Approval Status	Preclinical - Cell culture
Response Type	sensitive

Indication/Tumor Type	Her2-receptor positive breast cancer
Response Type	sensitive
Approval Status	Preclinical - Cell line xenograft

IPATASERTIB Drug Record

IPATASERTIB chembl:CHEMBL2177390 Antineoplastic

Alternate Names:

Drug Info:

Publications:

IPATASERTIB AKT3

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name GDC-0068 Novel drug target Novel Target Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

PMIDs: None found

Sources: TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

IPATASERTIB AKT2

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor Direct Interaction yes Trial Name GDC-0068

PMIDs: None found

Sources: TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

IPATASERTIB AKT1

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Approval Status Phase II Response Type predicted – sensitive Indication/Tumor Type triple-receptor negative breast cancer

PMIDs: 27872130 22934575

Sources: DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial TTD

IPATASERTIB PTEN

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Ipatasertib + Paclitaxel Indication/Tumor Type triple-receptor negative breast cancer Response Type predicted – sensitive

PMIDs: 23287563 24141624 27872130 30037818

Sources: JAX-CKB CIViC

IPATASERTIB KRAS

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Cell culture Response Type sensitive

PMIDs: 26725216

Sources: JAX-CKB

IPATASERTIB PIK3CA

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type Her2-receptor positive breast cancer Response Type sensitive Approval Status Preclinical - Cell line xenograft

PMIDs: 24141624

Sources: JAX-CKB

IPATASERTIB ERBB2

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type Her2-receptor positive breast cancer Response Type sensitive Approval Status Preclinical - Cell line xenograft

PMIDs: 24141624

Sources: JAX-CKB

MyCancerGenome: GDC-0068

Alternate Names: GDC-0068 Development Name

Drug Info: Drug Class Kinase Inhibitors Notes catalytic inhibitor

Publications:

TdgClinicalTrial: GDC-0068

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class Small molecule FDA Approval not approved

Publications:

DTC: IPATASERTIB

Alternate Names: CHEMBL2177390 ChEMBL Drug ID

Drug Info:

Publications: Blake JF et al., 2012, Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors., J Med Chem

JAX-CKB: Ipatasertib

Alternate Names:

Drug Info:

CIViC: IPATASERTIB

Alternate Names:

Drug Info:

TTD: GDC-0068

Alternate Names: D0I4TH TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL2177390

Alternate Names:

Drug Info:

Publications:

MyCancerGenomeClinicalTrial: GDC-0068

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL2177390

Alternate Names:

Drug Info:

Publications:

JAX-CKB: GDC-0068

Alternate Names:

Drug Info:

Publications:

ClearityFoundationClinicalTrial: GDC-0068

Alternate Names:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name GDC-0068

Novel drug target Novel Target

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Direct Interaction yes

Trial Name GDC-0068

PMIDs:
None found

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Approval Status Phase II

Response Type predicted – sensitive

Indication/Tumor Type triple-receptor negative breast cancer

PMIDs:
27872130 22934575

Sources:
DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ipatasertib + Paclitaxel

Indication/Tumor Type triple-receptor negative breast cancer

Response Type predicted – sensitive

PMIDs:
23287563 24141624 27872130 30037818

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
26725216

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
24141624

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
24141624

Sources:
JAX-CKB

Alternate Names:

GDC-0068 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes catalytic inhibitor

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

CHEMBL2177390 ChEMBL Drug ID

Publications:

Blake JF et al., 2012, Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors., J Med Chem

Alternate Names:

D0I4TH TTD Drug ID