Mekinist, as a MEK1/2 inhibitor, is mainly used for the treatment of BRAFV600 mutation positive tumors. Its indications include melanoma and non-small cell lung cancer, and special attention should be paid to cardiovascular, ocular, and skin toxicity risks during medication. The following provides a detailed explanation from two aspects: indications and medication precautions.

1. Indications

(1) Melanoma

Monotherapy or combination therapy with dalafenib can significantly prolong progression free survival in BRAFV600E/K mutation positive unresectable or metastatic melanoma.

(2) Non small cell lung cancer

The combination of dalafenib for first-line treatment of BRAFV600E mutation positive metastatic non-small cell lung cancer achieved an objective response rate of 64%.

2. Medication precautions

(1) Cardiovascular toxicity

May cause left ventricular dysfunction, regular monitoring of cardiac function is necessary before and during treatment, and symptomatic heart failure should be reduced or discontinued.

(2) Eye effects

It can cause retinal vein occlusion, serous retinopathy, etc. Patients with visual impairment should immediately undergo ophthalmic evaluation and adjust the dosage.

(3) Skin reaction

Common rashes, photosensitivity reactions, and in severe cases, Stevens Johnson syndrome may occur, requiring sun protection and monitoring of skin symptoms.

(4) Risk of bleeding

Combination therapy may increase the risk of gastrointestinal or intracranial bleeding, and permanent discontinuation of medication may be necessary in the event of severe bleeding.

(5) Embryotoxicity

Women of childbearing age should confirm their pregnancy status before taking medication, and take effective contraceptive measures during treatment and 4 weeks after discontinuing medication.

(6) Liver function monitoring

During the treatment period, ALT/AST should be tested monthly. If liver toxicity occurs, medication should be interrupted until recovery, and subsequent reduction or discontinuation of medication should be carried out.