Trametinib

MEKINIST

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Pronunciation: tra-ME-ti-nib (MEK-in-ist)

Trametinib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Trametinib ballicule

What it isMEK inhibitor; BRAF V600 melanoma and other BRAF-mutant tumors, with dabrafenib.

Why this oneCombining MEK with BRAF blockade delays resistance and reduces the paradoxical skin toxicity of BRAF inhibition alone.

What limits itRash, diarrhea, reduced ejection fraction and retinal vein occlusion. Pyrexia is common with the combination.

Trametinib molecular structure (skeletal formula) — Molecular structure: Trametinib

FDA-approved for

BRAF V600 melanoma with dabrafenib (2013)
NSCLC, anaplastic thyroid cancer

FDA label

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FDA dosing	Population	Start	Target	Max
BRAF V600E/K melanoma, NSCLC, ATC, solid tumors, low-grade glioma (per indication, +/- dabrafenib)	Adult	2 mg QD	2 mg QD	2 mg QD
Same (tablets, weight-based)	Peds >=26 kg	1 mg QD (26-37 kg); 1.5 mg QD (38-50 kg); 2 mg QD (>=51 kg)

Renal Undefined

Hepatic No adjustment in mild impairment; not established in moderate/severe

Instructions

Confirm BRAF V600 mutation before starting.
Take on an empty stomach (>=1 h before or >=2 h after a meal), same time each day ~24 h apart.
Do not crush or break tablets.
Do not take a missed dose within 12 h of the next dose.

Available strengths

tab 0.5, 2 mg
sol 0.05 mg/mL

Cautions

Cardiomyopathy / decreased LVEF
Retinal vein occlusion, retinal pigment epithelial detachment
Interstitial lung disease/pneumonitis
Serious skin toxicity
Hemorrhage; venous thromboembolism
Embryo-fetal toxicity

Adverse reactions

Rash
Diarrhea
Lymphedema (single agent)
With dabrafenib: pyrexia, nausea, chills, vomiting, hypertension, peripheral edema, fatigue

Pregnancy Can cause fetal harm; advise effective contraception

Lactation Do not breastfeed during and after treatment (potential serious adverse reactions)

Cost

Trametinib (MEKINIST)

Strength		#/mo	CostPlus
0.5 mg	tab	30 qd	not offered
2 mg	tab	30 qd	not offered
0.05 mg/mL	sol	per unit	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Trametinib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2034 est.

NO BOXED WARNINGS

Principal riskReduced ejection fraction; retinal vein occlusion

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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