Trametinib Dimethyl Sulfoxide

Class: Antineoplastic Agents
Chemical Name: N-[3-[3-Cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]-acetamide compd. with 1,1′-sulfinylbis[methane] (1:1)
Molecular Formula: C₂₆H₂₃FIN₅O₄•C₂H₆OS
CAS Number: 1187431-43-1
Brands: Mekinist

Medically reviewed by Drugs.com on May 17, 2022. Written by ASHP.

Introduction

Antineoplastic agent; an inhibitor of mitogen-activated extracellular signal-regulated kinase (MEK) 1 and MEK2 in cells with b-Raf serine-threonine kinase (BRAF) V600E or V600K mutations.

Uses for Trametinib Dimethyl Sulfoxide

Melanoma

In combination with dabrafenib as adjuvant therapy following complete resection of melanoma with BRAF V600E or V600K mutation and nodal involvement.

Alone or in combination with dabrafenib for treatment of unresectable or metastatic melanoma in selected patients with BRAF V600E or V600K mutation (designated an orphan drug by FDA as monotherapy or when used in combination for this use).

FDA-approved in vitro diagnostic test (e.g., THxID BRAF kit) required to confirm presence of BRAF V600E or V600K mutation prior to initiation of monotherapy or combination therapy.

Not recommended for use in patients with melanoma who have experienced disease progression following treatment with a BRAF inhibitor.

NSCLC

Used in combination with dabrafenib for treatment of metastatic non-small cell lung cancer (NSCLC) in patients with BRAF V600E mutation (designated an orphan drug by FDA when used in combination for this use).

FDA-approved diagnostic test (e.g., THxID BRAF kit) required to confirm presence of BRAF V600E mutation prior to initiation of therapy.

Anaplastic Thyroid Cancer

Used in combination with dabrafenib for treatment of locally advanced or metastatic anaplastic thyroid cancer in patients with BRAF V600E mutation when no satisfactory locoregional treatment options are available (designated an orphan drug by FDA when used in combination for this use).

FDA-approved diagnostic test (e.g., THxID BRAF kit) required to confirm presence of BRAF V600E mutation prior to initiation of therapy.

Trametinib Dimethyl Sulfoxide Dosage and Administration

General

• Confirm presence of BRAF V600E or V600K mutation prior to initiation of monotherapy for the treatment of unresectable or metastatic melanoma or trametinib/dabrafenib combination therapy for the treatment of unresectable or metastatic melanoma or for the adjuvant treatment of melanoma.

• Confirm presence of BRAF V600E mutation prior to initiation of trametinib/dabrafenib combination therapy for the treatment of metastatic NSCLC or locally advanced or metastatic anaplastic thyroid cancer.

Administration

Oral Administration

Administer orally once daily, approximately every 24 hours, at least 1 hour before or 2 hours after a meal.

Dosage

Available as trametinib dimethyl sulfoxide; dosage expressed in terms of tram...