BRAF inhibitor
BRAF Inhibitor[edit | edit source]
A BRAF inhibitor is a type of targeted therapy used in the treatment of certain cancers, most notably melanoma. These inhibitors specifically target the BRAF protein, which is part of the MAPK/ERK signaling pathway that regulates cell growth. Mutations in the BRAF gene, particularly the V600E mutation, can lead to uncontrolled cell proliferation and cancer.
Mechanism of Action[edit | edit source]
BRAF inhibitors work by blocking the activity of the mutated BRAF protein. The BRAF protein is a serine/threonine-protein kinase that is involved in sending signals inside cells, which are crucial for cell growth and division. In cancers with BRAF mutations, this signaling pathway is overactive, leading to increased cell growth and survival. By inhibiting BRAF, these drugs help to slow down or stop the growth of cancer cells.
Clinical Use[edit | edit source]
BRAF inhibitors are primarily used in the treatment of metastatic melanoma with the BRAF V600E mutation. They have also been investigated for use in other cancers, such as colorectal cancer and thyroid cancer, that harbor BRAF mutations.
Examples of BRAF Inhibitors[edit | edit source]
Some of the most well-known BRAF inhibitors include:
- Vemurafenib (Zelboraf)
- Dabrafenib (Tafinlar)
- Encorafenib (Braftovi)
These drugs are often used in combination with MEK inhibitors, such as trametinib or binimetinib, to enhance their effectiveness and reduce resistance.
Side Effects[edit | edit source]
Common side effects of BRAF inhibitors include:
- Skin rash
- Photosensitivity
- Joint pain
- Fatigue
- Nausea
More serious side effects can include the development of secondary skin cancers, such as squamous cell carcinoma.
Resistance[edit | edit source]
Resistance to BRAF inhibitors is a significant clinical challenge. Cancer cells can develop resistance through various mechanisms, such as activating alternative signaling pathways or acquiring additional mutations. Combination therapies, such as BRAF inhibitors with MEK inhibitors, are used to overcome or delay resistance.
Also see[edit | edit source]
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