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Mechanism of Action

Mechanism of Action

MAPK Pathway

TAFINLAR + MEKINIST TARGETS THE UNDERLYING CAUSE OF BRAF+ CANCERS1-3

  • TAFINLAR + MEKINIST inhibits 2 points on the MAPK pathway, which is constitutively active in BRAF V600+ solid tumors1,2

  • TAFINLAR + MEKINIST has been studied extensively as monotherapies and in combination1,2

  • MEKINIST is an inhibitor of MEK1 and MEK2 with established efficacy as monotherapy2

Inhibiting MEK1 and MEK2 can suppress downstream signaling of the MAPK pathway. Suppressing downstream signaling can reduce ERK–driven gene expression and cellular proliferation, invasion, and survival.4

Combination TAFINLAR + MEKINIST resulted in greater and more prolonged inhibition of tumor growth compared with either drug alone in BRAF V600–mutant melanoma in vitro and in vivo.1,2,*

TAFINLAR + MEKINIST mechanism of action

ERK, extracellular signal-related kinase; MAPK, mitogen-activated protein kinase; MEK, mitogen-activated extracellular signal-regulated kinase; RAS, monomeric G protein. 
*Shown in in vitro and in vivo studies.

References: 1. Tafinlar. Prescribing information. Novartis Pharmaceuticals Corp. 2. Mekinist. Prescribing information. Novartis Pharmaceuticals Corp. 3. Gouda MA, Subbiah V. Precision oncology for BRAF-mutant cancers with BRAF and MEK inhibitors: from melanoma to tissue-agnostic therapy. ESMO Open. 2023;8(2):100788. doi:10.1016/j.esmoop.2023.100788 4. Vultur A, Villanueva J, Herlyn M. Targeting BRAF in advanced melanoma: a first step toward manageable disease. Clin Cancer Res. 2011;17(7):1658-1663.