DGIdb - SAPANISERTIB Drug Record

SAPANISERTIB chembl:CHEMBL3545097 Antineoplastic

Alternate Names:

INK128
INK-128
SAPANISERTIB
TAK-228
MLN-0128
MLN0128

Drug Info:

Notes	catalytic inhibitor
Notes	TORC1/2, catalytic inhibitor
Drug Class	Kinase Inhibitors
FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent

(5 More Sources)

Publications:

Hassan et al., 2014, Catalytic mTOR inhibitors can overcome intrinsic and acquired resistance to allosteric mTOR inhibitors., Oncotarget
Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med
García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.
Gökmen-Polar et al., 2012, Investigational drug MLN0128, a novel TORC1/2 inhibitor, demonstrates potent oral antitumor activity in human breast cancer xenograft models., Breast Cancer Res. Treat.
Momcilovic et al., 2015, Heightening Energetic Stress Selectively Targets LKB1-Deficient Non-Small Cell Lung Cancers., Cancer Res.
Gild et al., 2013, Targeting mTOR in RET mutant medullary and differentiated thyroid cancer cells., Endocr. Relat. Cancer

SAPANISERTIB DEPTOR

Interaction Score: 0.98

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
SAPANISERTIB MAPKAP1

Interaction Score: 0.98

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
SAPANISERTIB CRTC1

Interaction Score: 0.98

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Novel Target

Trial Name INK128

PMIDs:
None found

Sources:
TdgClinicalTrial
SAPANISERTIB MLST8

Interaction Score: 0.98

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
SAPANISERTIB AKT1S1

Interaction Score: 0.74

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
SAPANISERTIB RICTOR

Interaction Score: 0.74

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
SAPANISERTIB RPTOR

Interaction Score: 0.74

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
SAPANISERTIB CRTC2

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name INK128

Novel drug target Novel Target

PMIDs:
None found

Sources:
TdgClinicalTrial
SAPANISERTIB SMAD4

Interaction Score: 0.49

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
25261369

Sources:
JAX-CKB
SAPANISERTIB APC

Interaction Score: 0.31

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
25261369

Sources:
JAX-CKB
SAPANISERTIB CDKN2A

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
25261369

Sources:
JAX-CKB
SAPANISERTIB RB1

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type skin cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
25261369

Sources:
JAX-CKB
SAPANISERTIB STK11

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
26574479

Sources:
JAX-CKB
SAPANISERTIB PTEN

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type no benefit

PMIDs:
27974663 26272063 25261369

Sources:
JAX-CKB
SAPANISERTIB PIK3CA

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
27974663 26272063 23085766 25261369

Sources:
JAX-CKB
SAPANISERTIB RET

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23828865

Sources:
CIViC
SAPANISERTIB BRAF

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
26272063 25261369

Sources:
JAX-CKB
SAPANISERTIB MTOR

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase mTOR inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions TTD
SAPANISERTIB KRAS

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Indication/Tumor Type lung cancer

Response Type sensitive

PMIDs:
26574479 26272063

Sources:
JAX-CKB
SAPANISERTIB TP53

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type no benefit

PMIDs:
26272063 25261369

Sources:
JAX-CKB
SAPANISERTIB NFE2L2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
CIViC

MyCancerGenome: MLN0128
- Version: 20-Jun-2017
Alternate Names:

MLN0128 Development Name

INK128 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes TORC1/2, catalytic inhibitor

Notes catalytic inhibitor

Publications:
TdgClinicalTrial: INK128
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

JAX-CKB: Sapanisertib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Hassan et al., 2014, Catalytic mTOR inhibitors can overcome intrinsic and acquired resistance to allosteric mTOR inhibitors., Oncotarget

Momcilovic et al., 2015, Heightening Energetic Stress Selectively Targets LKB1-Deficient Non-Small Cell Lung Cancers., Cancer Res.

Gökmen-Polar et al., 2012, Investigational drug MLN0128, a novel TORC1/2 inhibitor, demonstrates potent oral antitumor activity in human breast cancer xenograft models., Breast Cancer Res. Treat.

JAX-CKB: MLN0128

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.

Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med

Momcilovic et al., 2015, Heightening Energetic Stress Selectively Targets LKB1-Deficient Non-Small Cell Lung Cancers., Cancer Res.

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

Drug Info:

Publications:

Gild et al., 2013, Targeting mTOR in RET mutant medullary and differentiated thyroid cancer cells., Endocr. Relat. Cancer
TTD: INK128
- Version: 2020.06.01
Alternate Names:

D03DPZ TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL3545097
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL3545097
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL3545056
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	colorectal cancer
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	breast cancer
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	skin cancer
Response Type	sensitive
Approval Status	Preclinical

Evidence Type	Actionable
Approval Status	Preclinical
Response Type	sensitive

combination therapy	MLN0128 + PD-0325901
Indication/Tumor Type	colorectal cancer
Response Type	no benefit

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

Novel drug target	Novel Target
Trial Name	INK128

Trial Name	INK128
Novel drug target	Novel Target

SAPANISERTIB Drug Record

SAPANISERTIB chembl:CHEMBL3545097 Antineoplastic

Alternate Names:

Drug Info:

Publications:

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: n/a

Interaction Info: Novel drug target Novel Target Trial Name INK128

PMIDs: None found

Sources: TdgClinicalTrial

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: n/a

Interaction Info: Trial Name INK128 Novel drug target Novel Target

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colorectal cancer Response Type sensitive Approval Status Preclinical

PMIDs: 25261369

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colorectal cancer Response Type sensitive Approval Status Preclinical

PMIDs: 25261369

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type breast cancer Response Type sensitive Approval Status Preclinical

PMIDs: 25261369

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type skin cancer Response Type sensitive Approval Status Preclinical

PMIDs: 25261369

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical Response Type sensitive

PMIDs: 26574479

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy MLN0128 + PD-0325901 Indication/Tumor Type colorectal cancer Response Type no benefit

PMIDs: 27974663 26272063 25261369

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: combination therapy MLN0128 + PD-0325901 Indication/Tumor Type colorectal cancer Response Type sensitive

PMIDs: 27974663 26272063 23085766 25261369

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23828865

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy MLN0128 + PD-0325901 Indication/Tumor Type colorectal cancer Response Type sensitive

PMIDs: 26272063 25261369

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Indication/Tumor Type lung cancer Response Type sensitive

PMIDs: 26574479 26272063

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Novel Target

Trial Name INK128

PMIDs:
None found

Sources:
TdgClinicalTrial

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:

n/a

Interaction Info:

Trial Name INK128

Novel drug target Novel Target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
25261369

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
25261369

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
25261369

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type skin cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
25261369

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
26574479

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type no benefit

PMIDs:
27974663 26272063 25261369

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
27974663 26272063 23085766 25261369

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
23828865

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
26272063 25261369

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase mTOR inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Indication/Tumor Type lung cancer

Response Type sensitive

PMIDs:
26574479 26272063

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type no benefit

PMIDs:
26272063 25261369

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
CIViC

Alternate Names:

MLN0128 Development Name

INK128 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes TORC1/2, catalytic inhibitor

Notes catalytic inhibitor

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

Gild et al., 2013, Targeting mTOR in RET mutant medullary and differentiated thyroid cancer cells., Endocr. Relat. Cancer