DGIdb - BUPARLISIB Drug Record

BUPARLISIB chembl:CHEMBL2017974 Antineoplastic

Alternate Names:

NVP-BKM120
BKM120-NX
BKM-120NX
BKM-120
NVP-BKM-120
BUPARLISIB
BKM 120
BKM120
drugbank:11666
chembl:CHEMBL2017974
pubchem.compound:16654980
chemidplus:944396-07-0

Drug Info:

Notes	pan-PI3K inhibitor
Drug Class	Kinase Inhibitors
Pharmaceutical Developer	Novartis
Source Reported Drug Name(s)	BKM120
Drug Class	PI3K Inhibitor

(6 More Sources)

Publications:

Roper et al., 2014, Combination PI3K/MEK inhibition promotes tumor apoptosis and regression in PIK3CA wild-type, KRAS mutant colorectal cancer., Cancer Lett.
Vansteenkiste et al., 2015, Safety and Efficacy of Buparlisib (BKM120) in Patients with PI3K Pathway-Activated Non-Small Cell Lung Cancer: Results from the Phase II BASALT-1 Study., J Thorac Oncol
Hong et al., 2016, Targeting the PI3K signaling pathway in KRAS mutant colon cancer., Cancer Med
Park et al., 2012, NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutations., Int. J. Oncol.
Packer et al., 2017, PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2(mutant) Endometrial Cancers., Mol. Cancer Ther.
Hanker et al., 2013, Mutant PIK3CA accelerates HER2-driven transgenic mammary tumors and induces resistance to combinations of anti-HER2 therapies., Proc. Natl. Acad. Sci. U.S.A.
Saura et al., 2014, Phase Ib study of Buparlisib plus Trastuzumab in patients with HER2-positive advanced or metastatic breast cancer that has progressed on Trastuzumab-based therapy., 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
Bonelli et al., 2015, Inhibition of PI3K Pathway Reduces Invasiveness and Epithelial-to-Mesenchymal Transition in Squamous Lung Cancer Cell Lines Harboring PIK3CA Gene Alterations., Mol. Cancer Ther.
Kodack et al., 2017, The brain microenvironment mediates resistance in luminal breast cancer to PI3K inhibition through HER3 activation., Sci Transl Med
Wang et al., 2016, Effective use of PI3K inhibitor BKM120 and PARP inhibitor Olaparib to treat PIK3CA mutant ovarian cancer., Oncotarget
Wang et al., 2017, A Functional Genetic Screen Identifies the Phosphoinositide 3-kinase Pathway as a Determinant of Resistance to Fibroblast Growth Factor Receptor Inhibitors in FGFR Mutant Urothelial Cell Carcinoma., Eur. Urol.
Kiessling et al., 2015, Mutant HRAS as novel target for MEK and mTOR inhibitors., Oncotarget
Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. Cancer Res.
Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov
Hyman et al., 2015, Parallel phase Ib studies of two schedules of buparlisib (BKM120) plus carboplatin and paclitaxel (q21 days or q28 days) for patients with advanced solid tumors., Cancer Chemother. Pharmacol.
Ichihara et al., 2017, SFK/FAK Signaling Attenuates Osimertinib Efficacy in Both Drug-Sensitive and Drug-Resistant Models of EGFR-Mutant Lung Cancer., 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.

BUPARLISIB PIK3CA

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

combination therapy Buparlisib + Fulvestrant

Indication/Tumor Type non-small cell lung carcinoma

PMIDs:
28119489 23940356 24470511 27974663 26013318 28539475 26715098 26909613 22159814 26098748

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CancerCommons TTD OncoKB
BUPARLISIB PIK3CD

Interaction Score: 0.22

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 TTD
BUPARLISIB PIK3C2B

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BUPARLISIB PIK3C2A

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BUPARLISIB PIK3C3

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BUPARLISIB PIK3C2G

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BUPARLISIB PIK3R4

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BUPARLISIB PIK3R5

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
BUPARLISIB PIK3R6

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BUPARLISIB PIK3R3

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
BUPARLISIB PTEN

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BKM120 + Trastuzumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type predicted – sensitive

PMIDs:
26098748 28119489 24470511 25672916

Sources:
JAX-CKB CIViC
BUPARLISIB PIK3R1

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
BUPARLISIB HRAS

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung squamous cell carcinoma

Response Type no benefit

Approval Status Preclinical - Cell culture

PMIDs:
26544513

Sources:
JAX-CKB
BUPARLISIB PIK3CB

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions TTD
BUPARLISIB PIK3R2

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
BUPARLISIB NRAS

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Binimetinib + BKM120

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
27307593

Sources:
JAX-CKB
BUPARLISIB FGFR2

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + BKM120

Indication/Tumor Type endometrial cancer

Response Type sensitive

PMIDs:
28119489

Sources:
JAX-CKB
BUPARLISIB KRAS

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BKM120 + AG490

Indication/Tumor Type stomach cancer

Response Type sensitive

PMIDs:
24576621 26098748 26715098 22159814

Sources:
JAX-CKB
BUPARLISIB PIK3CG

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions TTD
BUPARLISIB ERBB2

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BKM120 + Bevacizumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
24470511 23948973 28539475 23940356

Sources:
JAX-CKB
BUPARLISIB FGFR3

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

PMIDs:
28108151

Sources:
JAX-CKB
BUPARLISIB BRAF

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Binimetinib + BKM120

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
24265152 27307593

Sources:
JAX-CKB
BUPARLISIB FGFR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD4547 + BKM120

Indication/Tumor Type transitional cell carcinoma

Response Type sensitive

PMIDs:
28108151

Sources:
JAX-CKB
BUPARLISIB EGFR

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BKM120 + Osimertinib

Indication/Tumor Type lung cancer

Response Type sensitive

PMIDs:
28416483

Sources:
JAX-CKB

CancerCommons: BKM120
- Version: 25-July-2013
Alternate Names:

BKM120 PubChem Drug Name

16654980 PubChem Drug ID

BKM120 Drug Trade Name

Drug Info:

Drug Class PI3K Inhibitor

Source Reported Drug Name(s) BKM120

Pharmaceutical Developer Novartis

Publications:
MyCancerGenome: BKM120
- Version: 20-Jun-2017
Alternate Names:

BKM120 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes pan-PI3K inhibitor

Publications:

JAX-CKB: BKM120

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Hong et al., 2016, Targeting the PI3K signaling pathway in KRAS mutant colon cancer., Cancer Med

Park et al., 2012, NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutations., Int. J. Oncol.

Vansteenkiste et al., 2015, Safety and Efficacy of Buparlisib (BKM120) in Patients with PI3K Pathway-Activated Non-Small Cell Lung Cancer: Results from the Phase II BASALT-1 Study., J Thorac Oncol

CIViC: BUPARLISIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Hyman et al., 2015, Parallel phase Ib studies of two schedules of buparlisib (BKM120) plus carboplatin and paclitaxel (q21 days or q28 days) for patients with advanced solid tumors., Cancer Chemother. Pharmacol.

TTD: Buparlisib
- Version: 2020.06.01
Alternate Names:

D01QSO TTD Drug ID

Drug Info:

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

BUPARLISIB Primary Drug Name

BUPARLISIB Drug Generic Name

BKM120 Drug Synonym

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2017974
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL2017974
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: BKM120
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
OncoKB: Buparlisib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:

Reported Cancer Type	Melanoma
combination therapy	Buparlisib + Fulvestrant
Indication/Tumor Type	non-small cell lung carcinoma

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

combination therapy	BKM120 + Trastuzumab
Indication/Tumor Type	Her2-receptor positive breast cancer
Response Type	predicted – sensitive

Indication/Tumor Type	lung squamous cell carcinoma
Response Type	no benefit
Approval Status	Preclinical - Cell culture

combination therapy	Binimetinib + BKM120
Indication/Tumor Type	melanoma
Response Type	sensitive

combination therapy	BGJ398 + BKM120
Indication/Tumor Type	endometrial cancer
Response Type	sensitive

combination therapy	BKM120 + AG490
Indication/Tumor Type	stomach cancer
Response Type	sensitive

combination therapy	BKM120 + Bevacizumab
Indication/Tumor Type	Her2-receptor positive breast cancer
Response Type	sensitive

Evidence Type	Actionable
Approval Status	Preclinical - Cell line xenograft
Response Type	sensitive

combination therapy	AZD4547 + BKM120
Indication/Tumor Type	transitional cell carcinoma
Response Type	sensitive

combination therapy	BKM120 + Osimertinib
Indication/Tumor Type	lung cancer
Response Type	sensitive

BKM120	PubChem Drug Name
16654980	PubChem Drug ID
BKM120	Drug Trade Name

BUPARLISIB	Primary Drug Name
BUPARLISIB	Drug Generic Name
BKM120	Drug Synonym

BUPARLISIB Drug Record

BUPARLISIB chembl:CHEMBL2017974 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Reported Cancer Type Melanoma combination therapy Buparlisib + Fulvestrant Indication/Tumor Type non-small cell lung carcinoma

PMIDs: 28119489 23940356 24470511 27974663 26013318 28539475 26715098 26909613 22159814 26098748

Sources: MyCancerGenome JAX-CKB ChemblInteractions CancerCommons TTD OncoKB

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 TTD

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:

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: n/a

Interaction Info: combination therapy BKM120 + Trastuzumab Indication/Tumor Type Her2-receptor positive breast cancer Response Type predicted – sensitive

PMIDs: 26098748 28119489 24470511 25672916

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: MyCancerGenome ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type lung squamous cell carcinoma Response Type no benefit Approval Status Preclinical - Cell culture

PMIDs: 26544513

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: MyCancerGenome ChemblInteractions TTD

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: combination therapy Binimetinib + BKM120 Indication/Tumor Type melanoma Response Type sensitive

PMIDs: 27307593

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BGJ398 + BKM120 Indication/Tumor Type endometrial cancer Response Type sensitive

PMIDs: 28119489

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BKM120 + AG490 Indication/Tumor Type stomach cancer Response Type sensitive

PMIDs: 24576621 26098748 26715098 22159814

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

combination therapy Buparlisib + Fulvestrant

Indication/Tumor Type non-small cell lung carcinoma

PMIDs:
28119489 23940356 24470511 27974663 26013318 28539475 26715098 26909613 22159814 26098748

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CancerCommons TTD OncoKB

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 TTD

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)

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:

n/a

Interaction Info:

combination therapy BKM120 + Trastuzumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type predicted – sensitive

PMIDs:
26098748 28119489 24470511 25672916

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:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung squamous cell carcinoma

Response Type no benefit

Approval Status Preclinical - Cell culture

PMIDs:
26544513

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:
MyCancerGenome ChemblInteractions TTD

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:

combination therapy Binimetinib + BKM120

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
27307593

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + BKM120

Indication/Tumor Type endometrial cancer

Response Type sensitive

PMIDs:
28119489

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BKM120 + AG490

Indication/Tumor Type stomach cancer

Response Type sensitive

PMIDs:
24576621 26098748 26715098 22159814

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:
MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BKM120 + Bevacizumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
24470511 23948973 28539475 23940356

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

PMIDs:
28108151

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Binimetinib + BKM120

Indication/Tumor Type melanoma

Response Type sensitive