DGIdb - OMIPALISIB Drug Record

OMIPALISIB chembl:CHEMBL1236962 Antineoplastic

Alternate Names:

OMIPALISIB
GSK2126458

Drug Info:

(4 More Sources)

Publications:

Greger et al., 2012, Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations., Mol. Cancer Ther.
Posch et al., 2013, Combined targeting of MEK and PI3K/mTOR effector pathways is necessary to effectively inhibit NRAS mutant melanoma in vitro and in vivo., Proc. Natl. Acad. Sci. U.S.A.
Munster et al., 2016, First-in-Human Phase I Study of GSK2126458, an Oral Pan-Class I Phosphatidylinositol-3-Kinase Inhibitor, in Patients with Advanced Solid Tumor Malignancies., Clin. Cancer Res.
Khalili et al., 2012, Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner., Clin. Cancer Res.

OMIPALISIB GNAQ

Interaction Score: 0.5

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GSK2126458 + Trametinib

Indication/Tumor Type uveal melanoma

Response Type sensitive

PMIDs:
22733540

Sources:
JAX-CKB
OMIPALISIB PIK3R1

Interaction Score: 0.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers ChemblInteractions MyCancerGenomeClinicalTrial
OMIPALISIB NRAS

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type decreased response

Approval Status Preclinical

PMIDs:
23431193 22389471

Sources:
JAX-CKB CIViC
OMIPALISIB PIK3CD

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial
OMIPALISIB PIK3R6

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
OMIPALISIB PIK3R4

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
OMIPALISIB PIK3R3

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions MyCancerGenomeClinicalTrial
OMIPALISIB PIK3R5

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
ChemblInteractions MyCancerGenomeClinicalTrial
OMIPALISIB PIK3R2

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 MyCancerGenomeClinicalTrial
OMIPALISIB AKT2

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
OMIPALISIB AKT3

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
OMIPALISIB MAP2K1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type conflicting

Response Type no benefit

combination therapy GSK2126458 + Trametinib

PMIDs:
22389471

Sources:
JAX-CKB
OMIPALISIB PIK3CB

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:
ChemblInteractions MyCancerGenomeClinicalTrial
OMIPALISIB PIK3CA

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Phase I

Response Type no benefit

PMIDs:
26603258

Sources:
ClearityFoundationBiomarkers JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial
OMIPALISIB PIK3CG

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 MyCancerGenomeClinicalTrial TTD
OMIPALISIB BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dabrafenib + GSK2126458

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
22389471

Sources:
JAX-CKB
OMIPALISIB AKT1

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
OMIPALISIB PTEN

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers
OMIPALISIB MTOR

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase mTOR inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

JAX-CKB: GSK2126458

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Greger et al., 2012, Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations., Mol. Cancer Ther.

Khalili et al., 2012, Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner., Clin. Cancer Res.

Munster et al., 2016, First-in-Human Phase I Study of GSK2126458, an Oral Pan-Class I Phosphatidylinositol-3-Kinase Inhibitor, in Patients with Advanced Solid Tumor Malignancies., Clin. Cancer Res.

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

Drug Info:

Publications:

Posch et al., 2013, Combined targeting of MEK and PI3K/mTOR effector pathways is necessary to effectively inhibit NRAS mutant melanoma in vitro and in vivo., Proc. Natl. Acad. Sci. U.S.A.
TTD: GSK2126458
- Version: 2020.06.01
Alternate Names:

D03EZE TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1236962
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: GSK2126458
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: GSK2126458
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1236962
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: GSK2126458
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:

combination therapy	GSK2126458 + Trametinib
Indication/Tumor Type	uveal melanoma
Response Type	sensitive

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

Indication/Tumor Type	melanoma
Response Type	decreased response
Approval Status	Preclinical

Response Type	conflicting
Response Type	no benefit
combination therapy	GSK2126458 + Trametinib

Evidence Type	Actionable
Approval Status	Phase I
Response Type	no benefit

combination therapy	Dabrafenib + GSK2126458
Indication/Tumor Type	melanoma
Response Type	sensitive

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

OMIPALISIB Drug Record

OMIPALISIB chembl:CHEMBL1236962 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: combination therapy GSK2126458 + Trametinib Indication/Tumor Type uveal melanoma Response Type sensitive

PMIDs: 22733540

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: ClearityFoundationBiomarkers ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type melanoma Response Type decreased response Approval Status Preclinical

PMIDs: 23431193 22389471

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: ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: Response Type conflicting Response Type no benefit combination therapy GSK2126458 + Trametinib

PMIDs: 22389471

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 MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Evidence Type Actionable Approval Status Phase I Response Type no benefit

PMIDs: 26603258

Sources: ClearityFoundationBiomarkers JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Dabrafenib + GSK2126458 Indication/Tumor Type melanoma Response Type sensitive

PMIDs: 22389471

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationBiomarkers

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GSK2126458 + Trametinib

Indication/Tumor Type uveal melanoma

Response Type sensitive

PMIDs:
22733540

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:
ClearityFoundationBiomarkers ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type decreased response

Approval Status Preclinical

PMIDs:
23431193 22389471

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:
ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type conflicting

Response Type no benefit

combination therapy GSK2126458 + Trametinib

PMIDs:
22389471

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 MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Phase I

Response Type no benefit

PMIDs:
26603258

Sources:
ClearityFoundationBiomarkers JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dabrafenib + GSK2126458

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
22389471

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase mTOR inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Publications:

Posch et al., 2013, Combined targeting of MEK and PI3K/mTOR effector pathways is necessary to effectively inhibit NRAS mutant melanoma in vitro and in vivo., Proc. Natl. Acad. Sci. U.S.A.

Alternate Names:

D03EZE TTD Drug ID