Belvarafenib (developed by Hanmi Pharmaceuticals and Genentech) is a small molecule RAF dimer (type II) inhibitor[1] which shows anti-tumor clinical activity in cancer patients with BRAFV600E- and NRAS- mutations.[2]

Belvarafenib
Clinical data
Other namesHM95573

GDC5573

RG6185
Routes of
administration
By mouth
Identifiers
  • 4-amino-N-[1-(3-chloro-2-fluoroanilino)-6-methylisoquinolin-5-yl]thieno[3,2-d]pyrimidine-7-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC23H16ClFN6OS
Molar mass478.93 g·mol−1
3D model (JSmol)
  • CC1=C(C2=C(C=C1)C(=NC=C2)NC3=C(C(=CC=C3)Cl)F)NC(=O)C4=CSC5=C4N=CN=C5N
  • InChI=InChI=1S/C23H16ClFN6OS/c1-11-5-6-13-12(7-8-27-22(13)30-16-4-2-3-15(24)17(16)25)18(11)31-23(32)14-9-33-20-19(14)28-10-29-21(20)26/h2-10H,1H3,(H,27,30)(H,31,32)(H2,26,28,29)
  • Key:KVCQTKNUUQOELD-UHFFFAOYSA-N

References

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  1. ^ Awada G, Neyns B (March 2022). "Melanoma with genetic alterations beyond the BRAFV600 mutation: management and new insights". Current Opinion in Oncology. 34 (2): 115–122. doi:10.1097/CCO.0000000000000817. PMID 35050937.
  2. ^ Kim TW, Lee J, Shin SJ, Kim JS, Kim YJ, Han HS, Lee SJ, Lim HS, Hong YH, Noh YS, Kyoung Y (31 May 2019). "Belvarafenib, a novel pan-RAF inhibitor, in solid tumor patients harboring BRAF, KRAS, or NRAS mutations: Phase I study". Journal of Clinical Oncology. 37 (15 suppl): 3000. doi:10.1200/JCO.2019.37.15_suppl.3000.