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
Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational
Drug Categories	acids, acyclic
Drug Categories	amides
Drug Categories	antineoplastic agents
Drug Categories	antineoplastic and immunomodulating agents
Drug Categories	cytochrome p-450 cyp2c19 substrates
Drug Categories	cytochrome p-450 cyp2c19 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp2d6 substrates
Drug Categories	cytochrome p-450 cyp2d6 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 substrates
Drug Categories	moderate risk qtc-prolonging agents
Drug Categories	protein kinase inhibitors
Drug Categories	qtc prolonging agents
Drug Categories	sulfones
Drug Categories	sulfur compounds

(9 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.
Li Z et al., 2016, Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells., Cancer Lett
Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. Cancer Res.
Moschos SJ et al., 2015, Targeted therapies in melanoma., Surg Oncol Clin N Am
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
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.
Koelblinger P et al., 2018, Development of encorafenib for BRAF-mutated advanced melanoma., Curr Opin Oncol
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: 1.31

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

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

Sources:
CancerCommons OncoKB FDA PharmGKB JAX-CKB CIViC TTD DrugBank TALC MyCancerGenome ChemblInteractions
ENCORAFENIB CCND1

Interaction Score: 0.9

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26586345 29573941

Sources:
DrugBank
ENCORAFENIB ARAF

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
ENCORAFENIB MAP2K1

Interaction Score: 0.23

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: 0.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
ENCORAFENIB KRAS

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
25673644 27312529

Sources:
JAX-CKB CIViC
ENCORAFENIB PTEN

Interaction Score: 0.13

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: 0.07

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

DrugBank: DB11718

Version: 5.1.7

Alternate Names:

ENCORAFENIB DrugBank Drug Name

1269440-17-6 CAS Number

Braftovi Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Li Z et al., 2016, Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells., Cancer Lett

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

Moschos SJ et al., 2015, Targeted therapies in melanoma., Surg Oncol Clin N Am

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 Trade Name

LGX818 Drug Development 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 Primary Drug Name

LGX818 Drug Synonym

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	DrugBank Drug Name
1269440-17-6	CAS Number
Braftovi	Drug Brand

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: 26586345 27307593 25769717 31566309 28363909 29573941 28351928 29356698 27312529 26577700

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 26586345 29573941

Sources: DrugBank

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: 25673644 27312529

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

DrugBank: DB11718

Alternate Names: ENCORAFENIB DrugBank Drug Name 1269440-17-6 CAS Number Braftovi Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups investigational

MyCancerGenome: LGX818

Alternate Names: LGX818 Development Name

Drug Info: Drug Class Kinase Inhibitors

Publications:

CancerCommons: LGX818

Alternate Names: LGX818 Drug Trade Name LGX818 Drug Development 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 Primary Drug Name LGX818 Drug Synonym

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:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

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

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

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
26586345 29573941

Sources:
DrugBank

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:
25673644 27312529

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:

ENCORAFENIB DrugBank Drug Name

1269440-17-6 CAS Number

Braftovi Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Alternate Names:

LGX818 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Alternate Names:

LGX818 Drug Trade Name

LGX818 Drug Development Name

Drug Info:

Drug Class RAF Inhibitor

Source Reported Drug Name(s) LGX818

Pharmaceutical Developer Novartis

Alternate Names:

LGX818 Primary Drug Name

LGX818 Drug Synonym

Alternate Names:

D0TK7R TTD Drug ID