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trametinib (Mekinist)
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:
1) common
- rash
- diarrhea
- peripheral edema
- skin lesions resembling acne
2) serious
- heart failure
- lung inflammation
- skin infections
- loss of vision
3) may cause infertility
Mechanism of action:
- inhibits MEK
General
small inhibitory antineoplastic agent (ib drug)
enzyme inhibitor
Database Correlations
PUBCHEM correlations
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
- Novartis: Tafinlar (dabrafenib) + Mekinist (trametinib)
http://www.hcp.novartis.com/products/tafinlar-mekinist/advanced-metastatic-melanoma/
- 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: 28919011
- Prescribing Information
https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/mekinist.pdf