Drug intelligence / Profile preview

trametinib

Development stage
Approved
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Trametinib is an orally bioavailable small molecule kinase inhibitor that selectively targets mitogen‑activated extracellular signal-regulated kinase 1 (MEK1) and MEK2. It is primarily used, alone or in combination with dabrafenib, to treat unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as well as to prevent recurrence after surgery. Trametinib is also approved for use in combination therapy for non-small cell lung cancer (NSCLC), thyroid cancer, certain solid tumors in adults and children aged six years and older, and low-grade glioma in children one year of age or older. By inhibiting MEK1/2 within the MAPK pathway—a key signaling cascade involved in cell proliferation—trametinib blocks abnormal signals that drive cancer growth[1][2][3][4][5]. The drug was originally developed by Japan Tobacco and later advanced by Novartis.

Brand names
MekinistMecinistMekinisutoMeqselSpexotrasTasu Mekinisuto
Other names
trametinib dimethyl sulfoxidetrametinib DMSO
02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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