DGIdb - ALPELISIB Drug Record

ALPELISIB chembl:CHEMBL2396661 ApprovedAntineoplastic

Alternate Names:

PIQRAY
NVP-BYL719
BYL-719
ALPELISIB
BYL719
BYL 719
chembl:CHEMBL2396661
chemidplus:1217486-61-7
pubchem.compound:56649450

Drug Info:

Pharmaceutical Developer	Novartis
Source Reported Drug Name(s)	BYL719
Drug Class	PI3K/mTOR dual Inhibitor
Drug Class	Kinase Inhibitors
Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational
Drug Categories	antineoplastic agents
Drug Categories	bcrp/abcg2 substrates
Drug Categories	breast cancer resistance protein inhibitors
Drug Categories	breast neoplasms
Drug Categories	cytochrome p-450 cyp2b6 inducers
Drug Categories	cytochrome p-450 cyp2b6 inducers (moderate)
Drug Categories	cytochrome p-450 cyp2c19 inhibitors
Drug Categories	cytochrome p-450 cyp2c19 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c8 inhibitors
Drug Categories	cytochrome p-450 cyp2c8 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c9 inducers
Drug Categories	cytochrome p-450 cyp2c9 inducers (moderate)
Drug Categories	cytochrome p-450 cyp2c9 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp3a inducers
Drug Categories	cytochrome p-450 cyp3a inhibitors
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inducers
Drug Categories	cytochrome p-450 cyp3a4 inducers (weak)
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (weak)
Drug Categories	cytochrome p-450 cyp3a4 substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates (strength unknown)
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 enzyme inducers
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	p-glycoprotein inhibitors
Drug Categories	phosphatidylinositol 3-kinases, antagonists & inhibitors
Drug Categories	sulfur compounds

(13 More Sources)

Publications:

Fritsch et al., 2014, Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials., Mol. Cancer Ther.
André F et al., 2019, Alpelisib for <i>PIK3CA</i>-Mutated, Hormone Receptor-Positive Advanced Breast Cancer., N Engl J Med
Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med
Castel et al., 2016, PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition., Cancer Cell
Mayer et al., 2017, A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer., Clin. Cancer Res.
Packer et al., 2017, PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2(mutant) Endometrial Cancers., Mol. Cancer Ther.
Le et al., 2016, Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer., Cancer Discov
Fernandes MS et al., 2016 Oct 18, Specific inhibition of p110α subunit of PI3K: putative therapeutic strategy for KRAS mutant colorectal cancers., Oncotarget
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.
Dogruluk et al., 2015, Identification of Variant-Specific Functions of PIK3CA by Rapid Phenotyping of Rare Mutations., Cancer Res.
Chen IC et al., 2017, Phosphatidylinositol-3 Kinase Inhibitors, Buparlisib and Alpelisib, Sensitize Estrogen Receptor-positive Breast Cancer Cells to Tamoxifen., Sci Rep
Yang X et al., 2017, New Insights into PI3K Inhibitor Design using X-ray Structures of PI3Kα Complexed with a Potent Lead Compound., Sci Rep
Gritsman et al., 2014, Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α., J. Clin. Invest.
Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
Schwartz et al., 2015, Feedback suppression of PI3Kα signaling in PTEN-mutated tumors is relieved by selective inhibition of PI3Kβ., Cancer Cell
Juric et al., 2015, Convergent loss of PTEN leads to clinical resistance to a PI(3)Kα inhibitor., Nature
Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.
Costa et al., 2015, Discovery and functional characterization of a neomorphic PTEN mutation., Proc. Natl. Acad. Sci. U.S.A.
Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.
Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol
van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov

ALPELISIB PIK3CA

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type no benefit

combination therapy Alpelisib + WEHI-539

Approval Status Preclinical - Cell line xenograft

Publications:

Fritsch et al., 2014, Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials., Mol. Cancer Ther.

André F et al., 2019, Alpelisib for <i>PIK3CA</i>-Mutated, Hormone Receptor-Positive Advanced Breast Cancer., N Engl J Med

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

ALPELISIB PIK3CB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
ALPELISIB PIK3CD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
ALPELISIB PIK3CG

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
ALPELISIB PIK3C2B

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
ALPELISIB PIK3R4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
ALPELISIB PIK3C2A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
ALPELISIB PIK3R1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
ALPELISIB PIK3R6

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
ALPELISIB PIK3R3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
ALPELISIB PIK3R5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
ALPELISIB PIK3R2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
ALPELISIB MTOR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Lung

Publications:
ALPELISIB PIK3C2G

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
ALPELISIB PIK3C3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
ALPELISIB NRAS

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

Publications:

Gritsman et al., 2014, Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α., J. Clin. Invest.
ALPELISIB FGFR2

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

Publications:

Packer et al., 2017, PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2(mutant) Endometrial Cancers., Mol. Cancer Ther.
ALPELISIB FGFR1

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Indication/Tumor Type estrogen-receptor positive breast cancer

Publications:

Mayer et al., 2017, A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer., Clin. Cancer Res.

ALPELISIB PTEN

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family PIK3CA inhibitor

Alteration PTEN:.

Indication/Tumor Type prostate cancer

Publications:

Schwartz et al., 2015, Feedback suppression of PI3Kα signaling in PTEN-mutated tumors is relieved by selective inhibition of PI3Kβ., Cancer Cell

Juric et al., 2015, Convergent loss of PTEN leads to clinical resistance to a PI(3)Kα inhibitor., Nature

Le et al., 2016, Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer., Cancer Discov

ALPELISIB KRAS

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ABT-263 + Alpelisib + CGM097 + Trametinib

Indication/Tumor Type colorectal cancer

Response Type sensitive

Publications:

Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.

Fernandes MS et al., 2016 Oct 18, Specific inhibition of p110α subunit of PI3K: putative therapeutic strategy for KRAS mutant colorectal cancers., Oncotarget

Fritsch et al., 2014, Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials., Mol. Cancer Ther.

ALPELISIB MAP2K1

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

Publications:

Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
ALPELISIB TP53

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ABT-263 + Alpelisib + CGM097 + Trametinib

Indication/Tumor Type colorectal cancer

Response Type sensitive

Publications:

Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.

ALPELISIB BRAF

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Alpelisib + PLX4720

Indication/Tumor Type melanoma

Response Type sensitive

Publications:

Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.

Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol

van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov

ALPELISIB AKT1

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type resistant

Approval Status Preclinical - Cell culture

Publications:

Le et al., 2016, Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer., Cancer Discov
ALPELISIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + BYL719

Indication/Tumor Type transitional cell carcinoma

Response Type predicted – sensitive

Publications:
ALPELISIB HRAS

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BYL719 + MEK162

Indication/Tumor Type ovarian cancer

Response Type predicted – sensitive

Publications:
ALPELISIB SGK1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Castel et al., 2016, PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition., Cancer Cell
ALPELISIB CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
ALPELISIB RB1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
ALPELISIB PI4KA

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ALPELISIB ESR1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ALPELISIB ESR2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ALPELISIB ERBB2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

DrugBank: DB12015

Version: 5.1.7

Alternate Names:

ALPELISIB DrugBank Drug Name

1217486-61-7 CAS Number

Piqray Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Yang X et al., 2017, New Insights into PI3K Inhibitor Design using X-ray Structures of PI3Kα Complexed with a Potent Lead Compound., Sci Rep

Chen IC et al., 2017, Phosphatidylinositol-3 Kinase Inhibitors, Buparlisib and Alpelisib, Sensitize Estrogen Receptor-positive Breast Cancer Cells to Tamoxifen., Sci Rep

MyCancerGenome: BYL719
- Version: 20-Jun-2017
Alternate Names:

BYL719 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:
CancerCommons: BYL719
- Version: 25-July-2013
Alternate Names:

BYL719 PubChem Drug Name

56649450 PubChem Drug ID

BYL719 Drug Trade Name

Drug Info:

Drug Class PI3K/mTOR dual Inhibitor

Source Reported Drug Name(s) BYL719

Pharmaceutical Developer Novartis

Publications:

JAX-CKB: BYL719

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.

van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov

Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.

JAX-CKB: Alpelisib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Mayer et al., 2017, A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer., Clin. Cancer Res.

Castel et al., 2016, PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition., Cancer Cell

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

CIViC: ALPELISIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell

André F et al., 2019, Alpelisib for <i>PIK3CA</i>-Mutated, Hormone Receptor-Positive Advanced Breast Cancer., N Engl J Med

Fritsch et al., 2014, Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials., Mol. Cancer Ther.

GuideToPharmacology: 249565638
- Version: 29-September-2020
Alternate Names:

ALPELISIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: BYL719
- Version: 2020.06.01
Alternate Names:

D0W7HE TTD Drug ID

Drug Info:

Publications:
FDA: Alpelisib
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2396661
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: BYL719
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: BYL719
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: BYL719
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:
CGI: BYL719
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL2396661
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
PharmGKB: alpelisib
- Version: 18-August-2020
Alternate Names:

Drug Info:

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

Drug Info:

Publications:

Response Type	no benefit
combination therapy	Alpelisib + WEHI-539
Approval Status	Preclinical - Cell line xenograft

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

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

Drug family	PIK3CA inhibitor
Alteration	PTEN:.
Indication/Tumor Type	prostate cancer

combination therapy	ABT-263 + Alpelisib + CGM097 + Trametinib
Indication/Tumor Type	colorectal cancer
Response Type	sensitive

combination therapy	Alpelisib + PLX4720
Indication/Tumor Type	melanoma
Response Type	sensitive

Indication/Tumor Type	breast cancer
Response Type	resistant
Approval Status	Preclinical - Cell culture

combination therapy	BGJ398 + BYL719
Indication/Tumor Type	transitional cell carcinoma
Response Type	predicted – sensitive

combination therapy	BYL719 + MEK162
Indication/Tumor Type	ovarian cancer
Response Type	predicted – sensitive

ALPELISIB	DrugBank Drug Name
1217486-61-7	CAS Number
Piqray	Drug Brand

BYL719	PubChem Drug Name
56649450	PubChem Drug ID
BYL719	Drug Trade Name

ALPELISIB Drug Record

ALPELISIB chembl:CHEMBL2396661 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Response Type no benefit combination therapy Alpelisib + WEHI-539 Approval Status Preclinical - Cell line xenograft

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Reported Cancer Type Lung

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: n/a

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

Publications: Gritsman et al., 2014, Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α., J. Clin. Invest.

Interaction Types & Directionality: n/a

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

Publications: Packer et al., 2017, PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2(mutant) Endometrial Cancers., Mol. Cancer Ther.

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Cell culture Indication/Tumor Type estrogen-receptor positive breast cancer

Publications: Mayer et al., 2017, A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer., Clin. Cancer Res.

Interaction Types & Directionality: n/a

Interaction Info: Drug family PIK3CA inhibitor Alteration PTEN:. Indication/Tumor Type prostate cancer

Interaction Types & Directionality: n/a

Interaction Info: combination therapy ABT-263 + Alpelisib + CGM097 + Trametinib Indication/Tumor Type colorectal cancer Response Type sensitive

Interaction Types & Directionality: n/a

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

Publications: Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.

Interaction Types & Directionality: n/a

Interaction Info: combination therapy ABT-263 + Alpelisib + CGM097 + Trametinib Indication/Tumor Type colorectal cancer Response Type sensitive

Publications: Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Alpelisib + PLX4720 Indication/Tumor Type melanoma Response Type sensitive

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type breast cancer Response Type resistant Approval Status Preclinical - Cell culture

Publications: Le et al., 2016, Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer., Cancer Discov

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BGJ398 + BYL719 Indication/Tumor Type transitional cell carcinoma Response Type predicted – sensitive

Publications:

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BYL719 + MEK162 Indication/Tumor Type ovarian cancer Response Type predicted – sensitive

Publications:

Interaction Types & Directionality: n/a

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type no benefit

combination therapy Alpelisib + WEHI-539

Approval Status Preclinical - Cell line xenograft

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Lung

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

Publications:

Gritsman et al., 2014, Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α., J. Clin. Invest.

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

Publications:

Packer et al., 2017, PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2(mutant) Endometrial Cancers., Mol. Cancer Ther.

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Indication/Tumor Type estrogen-receptor positive breast cancer

Publications:

Mayer et al., 2017, A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer., Clin. Cancer Res.

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family PIK3CA inhibitor

Alteration PTEN:.

Indication/Tumor Type prostate cancer

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ABT-263 + Alpelisib + CGM097 + Trametinib

Indication/Tumor Type colorectal cancer

Response Type sensitive

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

Publications:

Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ABT-263 + Alpelisib + CGM097 + Trametinib

Indication/Tumor Type colorectal cancer

Response Type sensitive

Publications:

Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Alpelisib + PLX4720

Indication/Tumor Type melanoma

Response Type sensitive

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type resistant

Approval Status Preclinical - Cell culture

Publications:

Le et al., 2016, Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer., Cancer Discov

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + BYL719

Indication/Tumor Type transitional cell carcinoma

Response Type predicted – sensitive

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BYL719 + MEK162

Indication/Tumor Type ovarian cancer

Response Type predicted – sensitive

Interaction Types & Directionality:

n/a

Publications:

Castel et al., 2016, PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition., Cancer Cell

Interaction Types & Directionality:

n/a

Publications:

Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell

Interaction Types & Directionality:

n/a

Publications:

Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Alternate Names:

ALPELISIB DrugBank Drug Name

1217486-61-7 CAS Number

Piqray Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Alternate Names:

BYL719 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Alternate Names:

BYL719 PubChem Drug Name

56649450 PubChem Drug ID

BYL719 Drug Trade Name

Drug Info:

Drug Class PI3K/mTOR dual Inhibitor

Source Reported Drug Name(s) BYL719

Pharmaceutical Developer Novartis