Targeted therapy for melanoma skin cancer

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Targeted therapy uses drugs to target specific molecules (such as proteins) on cancer cells or inside them. These molecules help send signals that tell cells to grow or divide. By targeting these molecules, the drugs stop the growth and spread of cancer cells and limit harm to normal cells. Targeted therapy may also be called molecular targeted therapy.

Some people with melanoma skin cancer have targeted therapy. If you have targeted therapy, your healthcare team will use what they know about the cancer and about your health to plan the drugs, doses and schedules.

You may have targeted therapy to:

  • stop or control the growth and spread of cancer cells
  • lower the risk that the cancer will come back (recur) after surgery
  • shrink metastatic melanoma

Types of targeted therapy for melanoma skin cancer

About half of all melanomas have changes (mutations) in the BRAF gene, specifically a BRAF V600E or BRAF V600K mutation. The mutation changes the BRAF protein, causing melanoma cells to grow and divide out of control.

Mutations in the MEK gene and the C-KIT gene may also happen with melanoma. But these happen much less often than BRAF gene mutations.

Most people with melanoma that has spread to nearby lymph nodes or other parts of the body (called locoregional or metastatic melanoma) will have a sample of the cancer tested for the BRAF, MEK and C-KIT gene mutations. Melanomas that test positive for any of these gene mutations may respond to certain targeted therapy drugs.

The following are the targeted therapy drugs used for locoregional, locally recurrent and metastatic melanoma.

BRAF inhibitors target the BRAF protein directly to help shrink and control the growth of the melanoma. The BRAF inhibitors used for melanoma are:

  • vemurafenib (Zelboraf)
  • dabrafenib (Tafinlar)
  • encorafenib (Braftovi)

MEK inhibitors control the growth of melanoma cells by blocking the MEK protein. Since the MEK protein is normally turned on (activated) by the BRAF protein, MEK inhibitors are another way to treat melanomas with BRAF gene mutations. A MEK inhibitor is usually combined with a BRAF inhibitor. The MEK inhibitors used for melanoma are:

  • cobimetinib (Cotellic)
  • trametinib (Mekinist)
  • binimetinib (Mektovi)

C-KIT inhibitors target the C-KIT protein to help stop the growth of the melanoma. The C-KIT inhibitor used for melanoma is imatinib (Gleevec).

Targeted therapy drugs for melanoma are taken as a pill by mouth (orally) daily. A BRAF inhibitor is usually combined with a MEK inhibitor. How long treatment is given depends on the type of drug used and how well the cancer responds to the treatment.

Side effects of targeted therapy

Side effects of targeted therapy will depend mainly on the type of drug or combination of drugs, the dose and your overall health. Tell your healthcare team if you have side effects that you think are from targeted therapy. The sooner you tell them of any problems, the sooner they can suggest ways to help you deal with them.

BRAF and MEK inhibitors may cause these side effects:

Find out more about targeted therapy

Find out more about targeted therapy. To make the decisions that are right for you, ask your healthcare team questions about targeted therapy.

Details on specific drugs change regularly. Find out more about sources of drug information and where to get details on specific drugs.

Expert review and references

  • Elaine McWhirter, MD, MSc, FRCPC
  • American Cancer Society. Targeted Therapy Drugs for Melanoma Skin Cancer. 2019: https://www.cancer.org/.
  • Michielin O, vanAkkooi A, Lorigan P, et al. ESMO consensus conference recommendations on the management of locoregional melanoma: under the auspices of the ESMO Guidelines Committee. Annals of Oncology. 2020: 31(11):1449–1461.
  • Michielin O, vanAkkooi ACJ, Ascierto PA, Dummer R, Keilholz U. Cutaneous melanoma: ESMO clinical practice guidelines for diagnosis, treatment and follow-up. Annals of Oncology. 2019: 30:1884–1901.
  • National Comprehensive Cancer Network . NCCN Clinical Practice Guidelines in Oncology: Cutaneous Melanoma (Version 2.2023). 2023.
  • Princess Margaret Cancer Centre . Princess Margaret Cancer Centre Clinical Practice Guidelines: Melanoma . University Health Network ; 2015 : https://www.uhn.ca/PrincessMargaret/Health_Professionals/Programs_Departments/Pages/clinical_practice_guidelines.aspx.
  • Provincial Health Services Authority. BC Cancer Protocol Summary: Treatment of Advanced C-Kit Positive Melanoma Using iMAtinib. Vancouver, BC: 2020: https://www.bccancer.bc.ca/.
  • Ribas A, Ariyan CE, Barker CA. Cutaneous melanoma. DeVita VT Jr, Lawrence TS, Rosenberg S. eds. DeVita Hellman and Rosenberg's Cancer: Principles and Practice of Oncology. 12th ed. Philadelphia, PA: Wolters Kluwer; 2023: Kindle version, chapter 63, https://read.amazon.ca/?asin=B0BG3DPT4Q&language=en-CA.
  • Seth R, Messersmith H, Kaur V, et al. Systemic therapy for melanoma: ASCO guideline. Journal of Clinical Oncology. 2020: 38(33):3947–3970 .
  • Tan WW. Medscape Reference: Malignant Melanoma. 2023: https://www.medscape.com/oncology.

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