DGIdb - ENCORAFENIB Drug Record

ENCORAFENIB chembl:CHEMBL3301612 ApprovedAntineoplastic

Alternate Names:

NVP-LGX818
ENCORAFENIB
LGX-818
NVP-LGX818-NXA
NVP-LGX-818-NXA
BRAFTOVI
LGX818
pubchem.compound:50922675
drugbank:11718
chemidplus:1269440-17-6
chembl:CHEMBL3301612

Drug Info:

Pharmaceutical Developer	Novartis
Source Reported Drug Name(s)	LGX818
Drug Class	RAF Inhibitor
Drug Class	Kinase Inhibitors

(8 More Sources)

Publications:

Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.
Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. 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
Tripathy et al., 2017, Ribociclib (LEE011): Mechanism of Action and Clinical Impact of This Selective Cyclin-Dependent Kinase 4/6 Inhibitor in Various Solid Tumors., Clin. Cancer Res.
Dummer R et al., 2018, Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial., Lancet Oncol
Kopetz S et al., 2019, Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer., N Engl J Med
Koelblinger P et al., 2018, Development of encorafenib for BRAF-mutated advanced melanoma., Curr Opin Oncol
Moschos SJ et al., 2015, Targeted therapies in melanoma., Surg Oncol Clin N Am
Li Z et al., 2016, Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells., Cancer Lett
Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov

ENCORAFENIB BRAF

Interaction Score: 1.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
27307593 28363909 28351928 27312529 26577700 29573941 31566309 29356698 25769717 26586345

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons PharmGKB TTD FDA OncoKB
ENCORAFENIB ARAF

Interaction Score: 0.89

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
ENCORAFENIB MAP2K1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type resistant

Evidence Type Actionable

Approval Status Preclinical - Cell culture

PMIDs:
27312529

Sources:
JAX-CKB
ENCORAFENIB RAF1

Interaction Score: 0.31

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
ENCORAFENIB KRAS

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
27312529 25673644

Sources:
JAX-CKB CIViC
ENCORAFENIB PTEN

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GSK2636771 + LGX818

Indication/Tumor Type melanoma

Response Type no benefit

PMIDs:
26577700

Sources:
JAX-CKB
ENCORAFENIB EGFR

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
27312529

Sources:
JAX-CKB
ENCORAFENIB TP53

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy CGM097 + LGX818

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB

MyCancerGenome: LGX818
- Version: 20-Jun-2017
Alternate Names:

LGX818 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:
CancerCommons: LGX818
- Version: 25-July-2013
Alternate Names:

LGX818 Drug Development Name

LGX818 Drug Trade Name

Drug Info:

Drug Class RAF Inhibitor

Source Reported Drug Name(s) LGX818

Pharmaceutical Developer Novartis

Publications:

JAX-CKB: Encorafenib

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.

Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. 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

JAX-CKB: LGX818

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

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

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

CIViC: ENCORAFENIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Kopetz S et al., 2019, Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer., N Engl J Med

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

Dummer R et al., 2018, Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial., Lancet Oncol

TALC: LGX818
- Version: 12-May-2016
Alternate Names:

LGX818 Drug Synonym

LGX818 Primary Drug Name

Drug Info:

Publications:
TTD: LGX818
- Version: 2020.06.01
Alternate Names:

D0TK7R TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL3301612
- Version: ChEMBL_27
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
ChemblInteractions: CHEMBL3301612
- Version: chembl_23
Alternate Names:

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:

combination therapy	Cetuximab + Encorafenib
Indication/Tumor Type	colorectal cancer
Response Type	resistant

Response Type	resistant
Evidence Type	Actionable
Approval Status	Preclinical - Cell culture

combination therapy	GSK2636771 + LGX818
Indication/Tumor Type	melanoma
Response Type	no benefit

combination therapy	CGM097 + LGX818
Indication/Tumor Type	melanoma
Response Type	sensitive

ENCORAFENIB Drug Record

ENCORAFENIB chembl:CHEMBL3301612 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: combination therapy Cetuximab + Encorafenib Indication/Tumor Type colorectal cancer Response Type resistant

PMIDs: 27307593 28363909 28351928 27312529 26577700 29573941 31566309 29356698 25769717 26586345

Sources: TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: n/a

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

PMIDs: 27312529

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Cetuximab + Encorafenib Indication/Tumor Type colorectal cancer Response Type resistant

PMIDs: 27312529 25673644

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy GSK2636771 + LGX818 Indication/Tumor Type melanoma Response Type no benefit

PMIDs: 26577700

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Cetuximab + Encorafenib Indication/Tumor Type colorectal cancer Response Type resistant

PMIDs: 27312529

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy CGM097 + LGX818 Indication/Tumor Type melanoma Response Type sensitive

PMIDs: None found

Sources: JAX-CKB

MyCancerGenome: LGX818

Alternate Names: LGX818 Development Name

Drug Info: Drug Class Kinase Inhibitors

Publications:

CancerCommons: LGX818

Alternate Names: LGX818 Drug Development Name LGX818 Drug Trade Name

Drug Info: Drug Class RAF Inhibitor Source Reported Drug Name(s) LGX818 Pharmaceutical Developer Novartis

Publications:

JAX-CKB: Encorafenib

Alternate Names:

Drug Info:

JAX-CKB: LGX818

Alternate Names:

Drug Info:

CIViC: ENCORAFENIB

Alternate Names:

Drug Info:

TALC: LGX818

Alternate Names: LGX818 Drug Synonym LGX818 Primary Drug Name

Drug Info:

Publications:

TTD: LGX818

Alternate Names: D0TK7R TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL3301612

Alternate Names:

Drug Info:

Publications:

FDA: Encorafenib

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL3301612

Alternate Names:

Drug Info:

Publications:

OncoKB: Encorafenib

Alternate Names:

Drug Info:

Publications:

PharmGKB: encorafenib

Alternate Names:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
27307593 28363909 28351928 27312529 26577700 29573941 31566309 29356698 25769717 26586345

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type resistant

Evidence Type Actionable

Approval Status Preclinical - Cell culture

PMIDs:
27312529

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
27312529 25673644

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GSK2636771 + LGX818

Indication/Tumor Type melanoma

Response Type no benefit

PMIDs:
26577700

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
27312529

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy CGM097 + LGX818

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB

Alternate Names:

LGX818 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Alternate Names:

LGX818 Drug Development Name

LGX818 Drug Trade Name

Drug Info:

Drug Class RAF Inhibitor

Source Reported Drug Name(s) LGX818

Pharmaceutical Developer Novartis

Alternate Names:

LGX818 Drug Synonym

LGX818 Primary Drug Name

Alternate Names:

D0TK7R TTD Drug ID