Trametinib

Mekinist®

Inhibition of MEK kinases 1 and 2. The MEK kinases are phosphorylated and activated by the mutated V600-BRAF kinases (MAP kinase signaling pathway).

02/2016 (unresectable, metastatic melanoma), 08/2018 (adjuvant)

In combination with dabrafenib: for unresectable or metastatic melanoma with a BRAF V600E/K mutation; adjuvant therapy for stage III melanoma with a BRAF V600 mutation following complete resection

Off-label use for NRAS mutations as monotherapy, for uveal melanomas or melanomas arising from congenital nevi with mosaic NRAS mutations

Differential blood count, blood chemistry panel, glucose, high-sensitivity troponin T, troponin I, NT-proBNP, S100, blood pressure, ECG (QT interval < 500 ms), echocardiography (LVEF > 50%)

Dermatological examination and ophthalmological examination (if ophthalmological symptoms are present)

2 mg once daily by mouth on an empty stomach.

For adjuvant therapy, a maximum of 12 months;

In the metastatic stage, until disease progression or the onset of unacceptable toxicity.

Once a month: Differential blood count, blood chemistry panel, glucose, S-100, blood pressure.

Once monthly through month 3, then quarterly: ECG (QT interval).

Dermatological examination: quarterly.

After 4 weeks, then quarterly: echocardiography, high-sensitivity troponin T, troponin I, NT-proBNP.

Ophthalmological examination in case of changes in visual acuity.

Use caution when taking this medication concurrently with strong CYP2C8 and CYP3A4 inhibitors (e.g., grapefruit, itraconazole) or inducers (e.g., St. John's wort, rifampicin, phenytoin, carbamazepine).

See the relevant specialist literature, guidelines, and study results.