2018 EORTC: A novel ERK1/2 inhibitor has potent activity in NRAS-mutant melanoma cancer models

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A novel ERK1/2 inhibitor has potent activity in NRAS-mutant melanoma cancer models

Summary

  • NRAS mutations occuring 15- 20% of melanoma cancer patients. Currently there is no approved molecularly targeted therapy for NRAS mutant melanoma, an indication which is associated with aggressive clinical outcome and a poor prognosis.
  • The NRAS mutation leads to constitutive activation of the MAPK pathway. AsERK1/2(ERK) is the primary downstream effect or of the MAPK pathway, its direct inhibition may provide an attractive therapeutic approach for the treatment of NRAS-mutant melanoma.
  • As previously described, using fragment-based drug discovery we have identified a novel and selective inhibitor of ERK which inhibits in vitro ERK catalytic activity as well as ERK phosphorylation 1.
  • Here, we demonstrate the in vitro and in vivo activity of a novel, highly potent, selective ERK inhibitor in models of NRAS-mutant melanoma.