Mechanism Of Action:
Trametinib functions as a reversible allosteric inhibitor, showing exceptional specificity towards both MEK1 and MEK2. By binding with high affinity to unphosphorylated MEK1/2, it blocks their catalytic activity. Additionally, it prevents phosphorylation of MEK1/2, thereby maintaining these enzymes in an inactive state and inhibiting downstream signaling via the MAP kinase pathway.
Indication:
Melanoma, As adjuvant
Trametinib combined with dabrafenib is indicated after complete surgical resection in patients with BRAF V600E or V600K mutation-positive melanoma with nodal involvement.
NSCLC, Metastatic
Trametinib in combination with dabrafenib is approved for BRAF V600E mutation-positive metastatic NSCLC. The combination is FDA-designated as an orphan drug for this application.
Anaplastic Thyroid Cancer, Locally advanced or metastatic
Trametinib with dabrafenib is used in BRAF V600E mutation-positive patients when satisfactory locoregional treatments are unavailable. The combination is FDA-designated as an orphan drug for this application.
