Literature DB >> 30190849

Dabrafenib and its use in the treatment of metastatic melanoma.

Samantha Bowyer1,1, Rebecca Lee1,1, Alberto Fusi1,1, Paul Lorigan1,2,1,2.   

Abstract

Approximately 50% of melanomas have mutations in the gene encoding BRAF. In recent years, new targeted therapies have transformed the landscape of metastatic melanoma treatment. Dabrafenib, a potent kinase inhibitor of mutated BRAF, has been showed to have high response rates with a rapid onset of response, as well as improved overall and progression-free survival when compared with chemotherapy. Dabrafenib in combination with trametinib, a MEK inhibitor, has demonstrated higher responses and improved clinical efficacy compared with monotherapy. Toxicity is distinct compared with chemotherapy but manageable. This article summarizes the pharmacology, key clinical trial data as well as practical experience with dabrafenib in clinical practice, and future directions.

Entities:  

Keywords:  BRAF; V600; dabrafenib; metastatic melanoma

Year:  2015        PMID: 30190849      PMCID: PMC6094610          DOI: 10.2217/mmt.15.21

Source DB:  PubMed          Journal:  Melanoma Manag        ISSN: 2045-0885


  42 in total

1.  Improved overall survival in melanoma with combined dabrafenib and trametinib.

Authors:  Caroline Robert; Boguslawa Karaszewska; Jacob Schachter; Piotr Rutkowski; Andrzej Mackiewicz; Daniil Stroiakovski; Michael Lichinitser; Reinhard Dummer; Florent Grange; Laurent Mortier; Vanna Chiarion-Sileni; Kamil Drucis; Ivana Krajsova; Axel Hauschild; Paul Lorigan; Pascal Wolter; Georgina V Long; Keith Flaherty; Paul Nathan; Antoni Ribas; Anne-Marie Martin; Peng Sun; Wendy Crist; Jeff Legos; Stephen D Rubin; Shonda M Little; Dirk Schadendorf
Journal:  N Engl J Med       Date:  2014-11-16       Impact factor: 91.245

2.  The nature and management of metastatic melanoma after progression on BRAF inhibitors: effects of extended BRAF inhibition.

Authors:  Matthew M K Chan; Lauren E Haydu; Alexander M Menzies; Mary W F Azer; Oliver Klein; Megan Lyle; Arthur Clements; Alexander Guminski; Richard F Kefford; Georgina V Long
Journal:  Cancer       Date:  2014-07-01       Impact factor: 6.860

Review 3.  Combining immunotherapy and targeted therapies in cancer treatment.

Authors:  Matthew Vanneman; Glenn Dranoff
Journal:  Nat Rev Cancer       Date:  2012-03-22       Impact factor: 60.716

4.  Dabrafenib in patients with Val600Glu or Val600Lys BRAF-mutant melanoma metastatic to the brain (BREAK-MB): a multicentre, open-label, phase 2 trial.

Authors:  Georgina V Long; Uwe Trefzer; Michael A Davies; Richard F Kefford; Paolo A Ascierto; Paul B Chapman; Igor Puzanov; Axel Hauschild; Caroline Robert; Alain Algazi; Laurent Mortier; Hussein Tawbi; Tabea Wilhelm; Lisa Zimmer; Julie Switzky; Suzanne Swann; Anne-Marie Martin; Mary Guckert; Vicki Goodman; Michael Streit; John M Kirkwood; Dirk Schadendorf
Journal:  Lancet Oncol       Date:  2012-10-08       Impact factor: 41.316

5.  Vemurafenib in patients with BRAF(V600) mutated metastatic melanoma: an open-label, multicentre, safety study.

Authors:  James Larkin; Michele Del Vecchio; Paolo A Ascierto; Ivana Krajsova; Jacob Schachter; Bart Neyns; Enrique Espinosa; Claus Garbe; Vanna Chiarion Sileni; Helen Gogas; Wilson H Miller; Mario Mandalà; Geke A P Hospers; Ana Arance; Paola Queirolo; Axel Hauschild; Michael P Brown; Lada Mitchell; Luisa Veronese; Christian U Blank
Journal:  Lancet Oncol       Date:  2014-02-27       Impact factor: 41.316

6.  A case of vemurafenib-induced polyarhritis in a patient with melanoma: how to manage it?

Authors:  Taner Babacan; Ibrahim Halil Türkbeyler; Ozan Balakan; Yavuz Pehlivan; Ali Suner; Bunyamin Kısacık
Journal:  Int J Rheum Dis       Date:  2014-05-12       Impact factor: 2.454

Review 7.  Specificity of receptor tyrosine kinase signaling: transient versus sustained extracellular signal-regulated kinase activation.

Authors:  C J Marshall
Journal:  Cell       Date:  1995-01-27       Impact factor: 41.582

8.  Sequencing of BRAF inhibitors and ipilimumab in patients with metastatic melanoma: a possible algorithm for clinical use.

Authors:  Paolo A Ascierto; Ester Simeone; Diana Giannarelli; Antonio M Grimaldi; Anna Romano; Nicola Mozzillo
Journal:  J Transl Med       Date:  2012-05-28       Impact factor: 5.531

9.  RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E).

Authors:  Poulikos I Poulikakos; Yogindra Persaud; Manickam Janakiraman; Xiangju Kong; Charles Ng; Gatien Moriceau; Hubing Shi; Mohammad Atefi; Bjoern Titz; May Tal Gabay; Maayan Salton; Kimberly B Dahlman; Madhavi Tadi; Jennifer A Wargo; Keith T Flaherty; Mark C Kelley; Tom Misteli; Paul B Chapman; Jeffrey A Sosman; Thomas G Graeber; Antoni Ribas; Roger S Lo; Neal Rosen; David B Solit
Journal:  Nature       Date:  2011-11-23       Impact factor: 49.962

10.  Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions.

Authors:  Alastair J King; Marc R Arnone; Maureen R Bleam; Katherine G Moss; Jingsong Yang; Kelly E Fedorowicz; Kimberly N Smitheman; Joseph A Erhardt; Angela Hughes-Earle; Laurie S Kane-Carson; Robert H Sinnamon; Hongwei Qi; Tara R Rheault; David E Uehling; Sylvie G Laquerre
Journal:  PLoS One       Date:  2013-07-03       Impact factor: 3.240

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  4 in total

Review 1.  Synthetic Vulnerabilities in the KRAS Pathway.

Authors:  Marta Roman; Elizabeth Hwang; E Alejandro Sweet-Cordero
Journal:  Cancers (Basel)       Date:  2022-06-08       Impact factor: 6.575

Review 2.  Mitochondrial Metabolism in Melanoma.

Authors:  Christina Huang; Rakan H Radi; Jack L Arbiser
Journal:  Cells       Date:  2021-11-16       Impact factor: 6.600

3.  Impressive and durable clinical responses obtained with dabrafenib and trametinib in low-grade serous ovarian cancer harbouring a BRAF V600E mutation.

Authors:  Bárbara Lima; Miguel Henriques Abreu; Susana Sousa; Carla Bartosch; Deolinda Pereira
Journal:  Gynecol Oncol Rep       Date:  2022-02-23

4.  Population Pharmacokinetics/Pharmacodynamics of Dabrafenib Plus Trametinib in Patients with BRAF-Mutated Metastatic Melanoma.

Authors:  David Balakirouchenane; Sarah Guégan; Chantal Csajka; Anne Jouinot; Valentine Heidelberger; Alicja Puszkiel; Ouidad Zehou; Nihel Khoudour; Perrine Courlet; Nora Kramkimel; Coralie Lheure; Nathalie Franck; Olivier Huillard; Jennifer Arrondeau; Michel Vidal; Francois Goldwasser; Eve Maubec; Nicolas Dupin; Selim Aractingi; Monia Guidi; Benoit Blanchet
Journal:  Cancers (Basel)       Date:  2020-04-09       Impact factor: 6.639

  4 in total

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