DGIdb - PILARALISIB Drug Record

PILARALISIB chembl:CHEMBL3360203 Antineoplastic

Alternate Names:

PILARALISIB
SAR-245408
XL147
XL-147

Drug Info:

Notes	pan-PI3K inhibitor
Drug Class	Kinase Inhibitors

(5 More Sources)

Publications:

Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.
Foster et al., 2015, The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models., Mol. Cancer Ther.
Shapiro et al., 2014, Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors., Clin. Cancer Res.
Rexer et al., 2013, Human breast cancer cells harboring a gatekeeper T798M mutation in HER2 overexpress EGFR ligands and are sensitive to dual inhibition of EGFR and HER2., Clin. Cancer Res.
Chakrabarty et al., 2013, Trastuzumab-resistant cells rely on a HER2-PI3K-FoxO-survivin axis and are sensitive to PI3K inhibitors., Cancer Res.

PILARALISIB PIK3R1

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers MyCancerGenome ChemblInteractions
PILARALISIB STK11

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25637314

Sources:
JAX-CKB
PILARALISIB PIK3C2B

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
PILARALISIB PIK3C3

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
PILARALISIB PIK3C2G

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
PILARALISIB PIK3C2A

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
PILARALISIB PIK3CD

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:
MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions
PILARALISIB PIK3R4

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
PILARALISIB PIK3R5

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
PILARALISIB PIK3R6

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
PILARALISIB PIK3R3

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
PILARALISIB PIK3R2

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:
MyCancerGenome ChemblInteractions
PILARALISIB PIK3CA

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

Indication/Tumor Type Advanced Solid Tumor

PMIDs:
21216929 25637314 24166903

Sources:
ClearityFoundationBiomarkers MyCancerGenome JAX-CKB ChemblInteractions
PILARALISIB PIK3CB

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
PILARALISIB PIK3CG

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions TTD
PILARALISIB PTEN

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25637314

Sources:
ClearityFoundationBiomarkers JAX-CKB
PILARALISIB ERBB2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trastuzumab + XL147

Evidence Type Actionable

Approval Status Preclinical

PMIDs:
23948973 23204226

Sources:
JAX-CKB CIViC
PILARALISIB KRAS

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy XL147 + Carboplatin

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
21216929 25637314

Sources:
JAX-CKB
PILARALISIB BRAF

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25637314

Sources:
JAX-CKB
PILARALISIB MET

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
25637314

Sources:
JAX-CKB

MyCancerGenome: XL147
- Version: 20-Jun-2017
Alternate Names:

SAR245408 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes pan-PI3K inhibitor

Publications:

JAX-CKB: XL147

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Shapiro et al., 2014, Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors., Clin. Cancer Res.

Foster et al., 2015, The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models., Mol. Cancer Ther.

Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.

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

Drug Info:

Publications:

Chakrabarty et al., 2013, Trastuzumab-resistant cells rely on a HER2-PI3K-FoxO-survivin axis and are sensitive to PI3K inhibitors., Cancer Res.
TTD: XL147
- Version: 2020.06.01
Alternate Names:

D03KAC TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL3360203
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL3360203
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: XL-147
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:
TALC: XL147
- Version: 12-May-2016
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: XL147
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:

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

Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive
Approval Status	Preclinical - Cell line xenograft

Indication/Tumor Type	glioblastoma multiforme
Response Type	sensitive
Approval Status	Preclinical - Cell line xenograft

combination therapy	Trastuzumab + XL147
Evidence Type	Actionable
Approval Status	Preclinical

combination therapy	XL147 + Carboplatin
Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive

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

PILARALISIB Drug Record

PILARALISIB chembl:CHEMBL3360203 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ClearityFoundationBiomarkers MyCancerGenome ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type non-small cell lung carcinoma Response Type sensitive Approval Status Preclinical - Cell line xenograft

PMIDs: 25637314

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

PMIDs: None found

Sources: MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

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:

PMIDs: None found

Sources: MyCancerGenome

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 Indication/Tumor Type Advanced Solid Tumor

PMIDs: 21216929 25637314 24166903

Sources: ClearityFoundationBiomarkers MyCancerGenome JAX-CKB 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: Direct Interaction yes Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality: n/a

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

PMIDs: 25637314

Sources: ClearityFoundationBiomarkers JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Trastuzumab + XL147 Evidence Type Actionable Approval Status Preclinical

PMIDs: 23948973 23204226

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy XL147 + Carboplatin Indication/Tumor Type non-small cell lung carcinoma Response Type sensitive

PMIDs: 21216929 25637314

Sources: JAX-CKB

Interaction Types & Directionality: n/a

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

PMIDs: 25637314

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25637314

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)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

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)

PMIDs:
None found

Sources:
MyCancerGenome

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

Indication/Tumor Type Advanced Solid Tumor

PMIDs:
21216929 25637314 24166903

Sources:
ClearityFoundationBiomarkers MyCancerGenome JAX-CKB 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:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25637314

Sources:
ClearityFoundationBiomarkers JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trastuzumab + XL147

Evidence Type Actionable

Approval Status Preclinical

PMIDs:
23948973 23204226

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy XL147 + Carboplatin

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
21216929 25637314

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25637314

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
25637314

Sources:
JAX-CKB

Alternate Names:

SAR245408 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes pan-PI3K inhibitor

Publications:

Chakrabarty et al., 2013, Trastuzumab-resistant cells rely on a HER2-PI3K-FoxO-survivin axis and are sensitive to PI3K inhibitors., Cancer Res.

Alternate Names:

D03KAC TTD Drug ID