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Dabrafenib

Anti-cancer medication

Summary

Anti-cancer medication

FieldValue
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tradenameTafinlar
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DailyMedIDDabrafenib
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routes_of_administrationBy mouth
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CAS_number1195765-45-7
PubChem44462760
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ChemSpiderID25948204
KEGGD10064
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ChEBI75045
ChEMBL2028663
PDB_ligandP06
synonymsGSK-2118436
IUPAC_nameN-{3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide
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| Drugs.com =

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Dabrafenib, sold under the brand name Tafinlar among others, is an anti-cancer medication used for the treatment of cancers associated with a mutated version of the gene BRAF. Dabrafenib acts as an inhibitor of the associated enzyme B-Raf, which plays a role in the regulation of cell growth.

The most common side effects include papilloma (warts), headache, nausea, vomiting, hyperkeratosis (thickening and toughening of the skin), hair loss, rash, joint pain, fever and tiredness. When taken in combination with trametinib, the most common side effects include fever, tiredness, nausea, chills, headache, diarrhea, vomiting, joint pain and rash.

Dabrafenib was approved for medical use in the United States in May 2013, and in the European Union in August 2013.

Medical uses

Dabrafenib is indicated as a single agent for the treatment of people with unresectable or metastatic melanoma with BRAF V600E mutation. Dabrafenib is indicated, in combination with trametinib, for BRAF V600E-positive unresectable or metastatic melanoma, metastatic non-small cell lung cancer, metastatic anaplastic thyroid cancer, and unresectable or metastatic solid tumors.

History

Clinical trial data demonstrated that resistance to dabrafenib and other BRAF inhibitors occurs within six to seven months. To overcome this resistance, the BRAF inhibitor dabrafenib was combined with the MEK inhibitor trametinib. In January 2014, the FDA approved this combination of dabrafenib and trametinib for BRAF V600E/K-mutant metastatic melanoma. In May 2018, the FDA approved the combination dabrafenib/trametinib as an adjuvant treatment for BRAF V600E-mutated, stage III melanoma after surgical resection based on the results of the COMBI-AD phase 3 study, making it the first oral chemotherapy regimen that prevents cancer relapse for node positive, BRAF-mutated melanoma.

Society and culture

United States

The US Food and Drug Administration (FDA) approved dabrafenib as a single agent treatment for people with BRAF V600E mutation-positive advanced melanoma in May 2013.

European Union

Dabrafenib was approved for use in the European Union in August 2013.

In April 2017, the European Union approved the combination of dabrafenib with trametinib for BRAF V600-positive advanced or metastatic non small-cell lung cancer (NSCLC).

In September 2023, the Committee for Medicinal Products for Human Use of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Finlee, intended for the treatment of low- and high-grade glioma (LGG and HGG). The applicant for this medicinal product is Novartis Europharm Limited. Finlee was approved for medical use in the European Union in November 2023.

Brand names

Dabrafenib is the international nonproprietary name.

Dabrafenib is sold under the brand names Tafinlar and Finlee.

Research

Dabrafenib has clinical activity with a manageable safety profile in clinical trials of phase I and II in patients with BRAF (V600)-mutated metastatic melanoma.

References

References

  1. (February 2024). "Product monograph brand safety updates".
  2. (June 22, 2022). "Tafinlar- dabrafenib capsule". U.S. National Library of Medicine.
  3. (August 29, 2013). "Tafinlar Product information".
  4. (November 16, 2023). "Finlee Product information".
  5. (March 16, 2023). "FDA approves dabrafenib with trametinib for pediatric patients with low-grade glioma with a BRAF V600E mutation".
  6. (November 2012). "Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations". The New England Journal of Medicine.
  7. (January 9, 2013). "Dabrafenib/Trametinib Combination Approved for Advanced Melanoma". OncLive.
  8. (May 2015). "Metastatic melanoma - a review of current and future treatment options". Acta Dermato-Venereologica.
  9. (November 2017). "Adjuvant Dabrafenib plus Trametinib in Stage III BRAF-Mutated Melanoma". The New England Journal of Medicine.
  10. "FDA Approves Adjuvant Combo for BRAF+ Melanoma". WebMD LLC.
  11. (December 24, 1999). "Drug Approval Package: Tafinlar (dabrafenib) Capsules NDA #202806".
  12. (May 30, 2013). "GSK melanoma drugs add to tally of U.S. drug approvals". Reuters.
  13. (September 17, 2018). "Tafinlar EPAR".
  14. (April 4, 2017). "EU Approves Dabrafenib/Trametinib Combination in BRAF+ NSCLC".
  15. (September 17, 2018). "Mekinist EPAR".
  16. (September 15, 2023). "Finlee: Pending EC decision".
  17. (November 15, 2023). "Finlee EPAR".
  18. (2012). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 67". WHO Drug Information.
  19. (July 2013). "Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies". Expert Opinion on Drug Metabolism & Toxicology.
  20. (April 2013). "B-Raf and the inhibitors: from bench to bedside". Journal of Hematology & Oncology.
Wikipedia Source

This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page.

aminopyrimidines chemotherapy cyp3a4-inducers sulfonamides thiazoles organofluorides b-raf-inhibitors tert-butyl-compounds fluoroarenes drugs-developed-by-novartis enzyme-inhibitors orphan-drugs
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