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Encorafenib information


Encorafenib
Clinical data
Trade namesBraftovi
Other namesLGX818
AHFS/Drugs.comMonograph
MedlinePlusa618040
License data
  • US DailyMed: Encorafenib
Routes of
administration
By mouth
Drug classAntineoplastic agents
ATC code
  • L01EC03 (WHO)
Legal status
Legal status
  • CA: ℞-only[1]
  • US: ℞-only
  • EU: Rx-only
Identifiers
IUPAC name
  • Methyl [(2S)-1-{[4-(3-{5-chloro-2-fluoro-3-[(methylsulfonyl)amino]phenyl}-1-isopropyl-1H-pyrazol-4-yl)-2-pyrimidinyl]amino}-2-propanyl]carbamate
CAS Number
  • 1269440-17-6
PubChem CID
  • 50922675
DrugBank
  • DB11718
ChemSpider
  • 28536139
UNII
  • 8L7891MRB6
KEGG
  • D11053
ChEMBL
  • ChEMBL3301612
CompTox Dashboard (EPA)
  • DTXSID00155347 Edit this at Wikidata
Chemical and physical data
FormulaC22H27ClFN7O4S
Molar mass540.01 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • C[C@@H](CNc1nccc(n1)c2cn(nc2c3cc(cc(c3F)NS(=O)(=O)C)Cl)C(C)C)NC(=O)OC
InChI
  • InChI=1S/C22H27ClFN7O4S/c1-12(2)31-11-16(17-6-7-25-21(28-17)26-10-13(3)27-22(32)35-4)20(29-31)15-8-14(23)9-18(19(15)24)30-36(5,33)34/h6-9,11-13,30H,10H2,1-5H3,(H,27,32)(H,25,26,28)/t13-/m0/s1
  • Key:CMJCXYNUCSMDBY-ZDUSSCGKSA-N

Encorafenib, sold under the brand name Braftovi, is a medication for the treatment of certain melanoma cancers. It is a small molecule BRAF inhibitor [2] that targets key enzymes in the MAPK signaling pathway. This pathway occurs in many different cancers including melanoma and colorectal cancers.[3] The substance was being developed by Novartis and then by Array BioPharma. In June 2018, it was approved by the FDA in combination with binimetinib for the treatment of patients with unresectable or metastatic BRAF V600E or V600K mutation-positive melanoma.[4][5]

The most common (≥25%) adverse reactions include fatigue, nausea, diarrhea, vomiting, abdominal pain, and arthralgia.[4]

  1. ^ "Summary Basis of Decision (SBD) for Braftovi". Health Canada. 23 October 2014. Retrieved 29 May 2022.
  2. ^ Koelblinger P, Thuerigen O, Dummer R (March 2018). "Development of encorafenib for BRAF-mutated advanced melanoma". Current Opinion in Oncology. 30 (2): 125–133. doi:10.1097/CCO.0000000000000426. PMC 5815646. PMID 29356698.
  3. ^ Burotto M, Chiou VL, Lee JM, Kohn EC (November 2014). "The MAPK pathway across different malignancies: a new perspective". Cancer. 120 (22): 3446–56. doi:10.1002/cncr.28864. PMC 4221543. PMID 24948110.
  4. ^ a b "FDA approves encorafenib and binimetinib in combination for unresectable or metastatic melanoma with BRAF mutations". U.S. Food and Drug Administration (FDA) (Press release). 27 June 2018. Archived from the original on 19 December 2019. Retrieved 28 June 2018. Public Domain This article incorporates text from this source, which is in the public domain.
  5. ^ "Drug Trial Snapshot: Braftovi". U.S. Food and Drug Administration (FDA). 16 July 2018. Archived from the original on 19 December 2019. Retrieved 18 December 2019. Public Domain This article incorporates text from this source, which is in the public domain.

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Encorafenib

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Encorafenib, sold under the brand name Braftovi, is a medication for the treatment of certain melanoma cancers. It is a small molecule BRAF inhibitor...

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Binimetinib

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cancers. In June 2018 it was approved by the FDA in combination with encorafenib for the treatment of patients with unresectable or metastatic BRAF V600E...

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MEK inhibitor

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Binimetinib (MEK162), approved by the FDA in June 2018 in combination with encorafenib for the treatment of patients with unresectable or metastatic BRAF V600E...

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Novartis

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candidates; the MEK inhibitor binimetinib (MEK 162) and the BRAF inhibitor encorafenib (LGX818), for $85 million. In addition, the company sold its RNAi portfolio...

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Array BioPharma

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inhibitor - Approved 2020, owned by Seagen (Seattle Genetics) BRAFTOVI (Encorafenib) - BRAF inhibitor - Approved 2018, acquired by Pfizer KRAZATI (Adagrasib)...

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Melanoma

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In June 2018, the FDA approved the combination of a BRAF inhibitor encorafenib and a MEK inhibitor binimetinib for the treatment of un-resectable or...

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ATC code L01

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L01EB11 Aumolertinib L01EC01 Vemurafenib L01EC02 Dabrafenib L01EC03 Encorafenib L01ED01 Crizotinib L01ED02 Ceritinib L01ED03 Alectinib L01ED04 Brigatinib...

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V600E

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increase in its basal activity and hence is oncogenic. Vemurafenib, encorafenib, and dabrafenib are approved by the FDA for treatment of metastatic melanomas...

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Cancer immunotherapy

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doi:10.2147/cmar.s33979. PMC 3421468. PMID 22904643. "FDA approves Encorafenib and Binimetinib in combination for unresectable or metastatic melanoma...

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