Trametinib (Mekinist)
Targeted Therapy · Approved since 2013
Description
Trametinib is a selective MEK1/MEK2 inhibitor that blocks the MAPK signaling pathway downstream of RAS and RAF mutations. In colorectal cancer, trametinib is used in combination with other targeted agents like EGFR inhibitors in patients with RAS/RAF wild-type tumors, or as part of precision medicine approaches for tumors harboring specific MAPK pathway alterations. The drug targets the MEK kinases that are critical components of the cell proliferation pathway commonly dysregulated in colorectal malignancies.
Mechanism of Action
Trametinib selectively inhibits MEK1 and MEK2 kinases, which are downstream effectors in the RAS/RAF/MEK/ERK signaling cascade. By blocking MEK activity, trametinib prevents phosphorylation and activation of ERK1/2, ultimately disrupting cellular proliferation, survival signals, and tumor growth in cancers dependent on MAPK pathway activation.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Mekinist |
| Category | Targeted Therapy |
 Status | Off-label |
 Estado EMA | med_ema_approved |
 Acceso España | med_spain_hospital_use med_crc_off_label |
| Administration | Oral |
| Year Approved | 2013 |
| Clinical Trials | 18 |
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Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.