Dabrafenib, also known as GSK2118436 or Tafinlar, is an anticancer drug used to treat patients with metastatic melanoma that carries a BRAF V600 mutation. It was developed by GlaxoSmithKline and approved by the United States Food and Drug Administration (FDA) in May 2013. Dabrafenib is a selective inhibitor of the mutated BRAF protein, which is found in approximately 50% of all melanomas. By blocking the activity of this protein, dabrafenib can slow down or stop the growth of cancer cells, enabling better outcomes for patients.
Chemical Name
The chemical name of dabrafenib is N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide.
Molecular Formula
The molecular formula of dabrafenib is C23H20F3N5O2S2.
Formula Weight
The formula weight of dabrafenib is 519.57 g/mol.
CAS No
The CAS number of dabrafenib is 1195765-45-7.
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Health Benefits of Dabrafenib
Dabrafenib has been shown to improve survival rates in patients with metastatic melanoma who carry a BRAF V600 mutation. In a Phase III clinical trial, patients treated with dabrafenib had a median progression-free survival of 5.1 months compared to 2.7 months in the control group. Overall response rate was also significantly higher in the dabrafenib group at 50% compared to 6% in the control group. These results demonstrate the potential of dabrafenib to extend the lives of patients with advanced melanoma.
Potential Effects
Dabrafenib selectively inhibits the mutated BRAF protein that is present in approximately 50% of all melanomas. This inhibition effectively slows down or stops the growth of cancer cells harboring the mutation. Dabrafenib has been shown to shrink tumors in patients with metastatic melanoma, leading to improved overall survival rates.
Product Mechanism
BRAF is a protein kinase that plays a key role in cell signaling pathways involved in regulating cell growth and division. The BRAF V600 mutation, which is found in approximately 50% of all melanomas, leads to the constitutive activation of BRAF and uncontrolled cell growth. Dabrafenib is a selective inhibitor of the mutant BRAF protein, blocking its activity and thereby slowing down or stopping the growth of cancer cells.
Safety
Like all medications, dabrafenib has some safety concerns. The most common side effects of dabrafenib include fever, fatigue, nausea, vomiting, diarrhea, rash, and headache. More serious adverse reactions may occur, such as severe allergic reactions, liver damage, and eye problems. Dabrafenib can also cause new primary melanomas to develop in some patients. Patients taking dabrafenib should be monitored closely for these potential side effects.
Side Effects
Dabrafenib can cause a range of side effects, including:
Dosing Information
The recommended dose of dabrafenib is 150 mg orally twice daily. Dabrafenib should be taken on an empty stomach at least one hour before or two hours after a meal. The duration of treatment with dabrafenib will depend on the individual patient's response to therapy.
Conclusion
Dabrafenib is a promising anticancer drug that has demonstrated significant benefits in the treatment of metastatic melanoma that carries a BRAF V600 mutation. As a selective inhibitor of the mutant BRAF protein, dabrafenib has been shown to slow down or stop the growth of cancer cells, leading to improved survival rates in patients. However, like all medications, dabrafenib has some safety concerns and potential side
