trametinib (Mekinist)
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Indications
- metastatic melanoma
- BRAF V600E or BRAF V600K gene mutation-positive
- metastatic BRAF V600E mutation positive non-small-cell lung cancer[3]
* may be used in combination with dabrafenib[2][3]
Contraindications
- not approved for use in combination with other antineoplastic agents
- not indicated for treatment of patients who have received prior BRAF-inhibitor therapy[2]
- pregnancy: may cause harm to fetus
Adverse effects
- common
- rash
- diarrhea
- peripheral edema
- skin lesions resembling acne
- serious
- may cause infertility
Mechanism of action
- inhibits MEK
More general terms
References
- ↑ FDA News Release: May 29, 2013 FDA approves two drugs, companion diagnostic test for advanced skin cancer. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm354199
- ↑ 2.0 2.1 2.2 Novartis: Tafinlar (dabrafenib) + Mekinist (trametinib) http://www.hcp.novartis.com/products/tafinlar-mekinist/advanced-metastatic-melanoma/
- ↑ 3.0 3.1 3.2 Planchard D, Smit EF, Groen HJM et al Dabrafenib plus trametinib in patients with previously untreated BRAF-V600E-mutant metastatic non-small-cell lung cancer: an open-label, phase 2 trial. Lancet Oncol. 2017 Oct;18(10):1307-1316. PMID: https://www.ncbi.nlm.nih.gov/pubmed/28919011
- ↑ Prescribing Information https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/mekinist.pdf