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trametinib

MEK inhibitor, kinase inhibitor · antineoplastic, targeted therapy

MEK inhibitor, kinase inhibitorantineoplastic, targeted therapy
CDSCO approved
EXCRETION
not curated
INTERACTIONS
1 major
SEVERE in our sources
PREGNANCY
D
FDA category + note
Top interactions
  • PregnancySevereTextbookG&G 14e · p1392

Mechanism

MEK inhibitor.

Indications

anaplastic carcinomas containing BRAF V600E (FDA-approved in combination with dabrafenib)redifferentiation therapy (with or without BRAF inhibition) to induce radioiodine uptake in non–iodine-avid thyroid cancersmutant BRAF V600E/K melanoma (monotherapy, though combination with dabrafenib is preferred)mutant V600E/K metastatic melanoma (in combination with dabrafenib)mutant V600E metastatic NSCLC (in combination with dabrafenib)metastatic anaplastic thyroid cancer (in combination with dabrafenib)combination with BRAF inhibitors for melanomas that harbor a mutation at position 600 in BRAF

Pharmacokinetics

Peak effect
1.5 h
Half-life
4 to 5 days
Bioavailability
72% (oral)
Metabolism
not a substrate of CYP enzymes

Side effects

Common
cutaneous rashacneiform dermatitisdiarrheafatiguenausealymphedemaheadachepyrexiaarthralgias
Serious
  • grade 3 to 4 skin toxicity (6% of patients)
  • cardiomyopathy
  • hypertension
  • hemorrhage
  • interstitial lung disease
  • ocular toxic effects
  • cardiac toxicities
  • ocular toxicities

Pregnancy & lactation

Pregnancy

D

Drug interactions

Pregnancy
Severe
Textbook

Fetal harm.

The risk must be weighed against the potential benefit.

Source: G&G 14e · p1392

11 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.

Related guidelines

Other MEK inhibitor, kinase inhibitor drugs

Ask House about trametinib

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e, Harrison 22e·Verified: 2026-05-10 · House clinical team