BRAF represents a novel therapeutic target for the treatment of advanced non-small cell lung cancer (NSCLC).1
Molecular characterisation of NSCLC marked a turning point in the treatment of lung tumours harbouring kinase alterations suitable for targeted drug inhibition.1
Among patients with driver mutations, outcomes for those treated with targeted therapies are prolonged compared with those who do not receive genotype-directed treatment.3
Approximately 1–3% of patients with NSCLC have a BRAF mutation.1
BRAF mutations lead to constitutive activation of the MAPK pathway3
V600E is the most common variant, occurring in roughly 50% of BRAF+ cases
NSCLC with BRAF V600E mutations has histological features suggestive of an aggressive tumour2
Patients with BRAF V600E–mutant NSCLC demonstrated less-favorable outcomes with platinum-based chemotherapy1
Source: Kantar Health Cancer Impact; Multiple secondary sources for Biomarker splits
WT, wild type
Mechanism of action of Tafinlar + Mekinist
Tafinlar (dabrafenib) + Mekinist (trametinib) target two different kinases in the MAPK pathway (BRAF and MEK1/2 respectively) to block the signalling that leads to abnormal cell division and growth.6,7
Combination therapy with Tafinlar + Mekinist results in prolonged inhibition of tumour growth compared with either drug alone in BRAF V600E-mutant tumours, both in vitro and in vivo.6,7
Adapted from Leonetti A, et al. Cancer Treat Rev 2018.1
For more information on Tafinlar + Mekinist please refer to the Summary of Product Characteristics and Patient Information Leaflets.
ALK, anaplastic lymphoma kinase; BRAF, a human gene that encodes a protein called B-Raf. The gene is also referred to as proto-oncogene B-Raf and v-Raf murine sarcoma viral oncogene homolog B, while the protein is more formally known as serine/threonine-protein kinase B-Raf; EGFR, epidermal growth factor receptor; ERK, extracellular signal-regulated kinases; KRAS, a proto-oncogene that is part of the RAS/MAPK signalling pathway; MAPK, mitogen-activated protein (MAP) kinase; MEK, mekinist; MET, a tyrosine kinase receptor; NSCLC, non-small cell lung cancer; RAS, rat sarcoma; ROS, reactive oxygen species; V600E, mutation of the BRAF gene in which valine (V) is substituted by glutamic acid (E) at amino acid 60; WT, wild type.
- Leonetti A, et al. Cancer Treat Rev 2018;66:82–94.
- NHS England. National Genomic Test Directory for cancer. Available at: https://www.england.nhs.uk/publication/national-genomic-test-directories/ (Accessed June 2021).
- Planchard D, et al. Lancet Oncol 2016;17:984–993.
- Kantar Health Cancer Impact; Multiple secondary sources for Biomarker splits.
- Marchetti A, et al. J Clin Oncol 2011;29(26):3574–3579.
- Mekinist (trametinib) Summary of Product Characteristics.
- Tafinlar (dabrafenib) Summary of Product Characteristics.