Binimetinib (Mektovi)

Binimetinib (Mektovi)

This patient-friendly article is about the anti-cancer drug, Binimetinib, which is approved to be used with encorafenib to treat Melanoma that cannot be removed by surgery or has spread to other parts of the body. It is used in patients whose cancer is BRAF modified.

What is BRAF?

BRAF is a human gene, which when copied into mRNA, is then copied into a protein B-Raf, a protein kinase. This protein normally sends signals into cells that direct cell growth. Because of failures in the copying process, the protein message is imperfect and the cell’s division runs out of control (1).

Binimetinib use in cancer treatment

Binimetinib is approved to be used with encorafenib to treat BRAF-inhibited Melanoma, which cannot be removed by surgery or has spread to other parts of the body. At least half of melanoma cases have a problem in the BRAF protein (2).

It is currently being studied for use with other cancers.

Binimetinib Dose

Tablets are given daily, usually at 15 mg.

Binimetinib Side-effects 

Cardiomyopathy, Venous Thromboembolism, Ocular issues, Gastrointestinal issues, Interstitial Lung Disease, liver toxicity, Rhabdomyolysis and  Haemorrhage.

Binimetinib and supplements

  • Berberine decreases the number of cells that are BRAF-inhibited this potentially making it synergistic to Binimetinib (3).

  • Melatonin synergises BRAF-targeting Dabrafenib, a drug which has similar aims and properties to Binimetinib as a selective inhibitor of BRAF kinase (4).

  • Honokiol inhibits drug resistance to BRAF-inhibitors, such as vemurafenib. While patients with BRAF mutations often demonstrate an initial dramatic response to BRAF inhibitors, relapse is extremely common. Honokiol has been shown to extend effectiveness (5).


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References

  1.  No new mutations in cancer DNA - https://www.canceractive.com/article/cancer-drivers%20not%20found%20in%20dna 

  2. The Cancer Genome Atlas Network. Genomic classification of cutaneous melanoma. Cell. 2015;161(7):1681-96.

  3. Berberine Inhibits Human Melanoma A375.S2 Cell Migration and Invasion; Molecules; Jia Fang Liu et al; 2018 Aug 13;23(8):2019.  

  4. Melatonin synergizes BRAF-targeting agent dabrafenib; Yena Liao et al; J Cell Mol Med, 2020 Oct;24(20):12119-12130. 

  5. Honokiol bis-dichloroacetate (Honokiol DCA) demonstrates activity in vemurafenib-resistant melanoma in vivo; Michael Y Bonner et al; Oncotarget, 2016 Mar 15;7(11):12857-68.

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