Drug intelligence / Profile preview

dabrafenib

Development stage
Approved
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Dabrafenib is a small molecule kinase inhibitor used primarily to treat cancers with specific BRAF mutations, most notably BRAF V600E and V600K. It acts as a reversible ATP-competitive inhibitor of the serine/threonine protein kinase BRAF, which is part of the MAPK/ERK signaling pathway involved in cell proliferation and survival. By selectively inhibiting mutant forms of BRAF (with higher affinity for mutated than wild-type), dabrafenib disrupts downstream MEK and ERK phosphorylation, leading to cell cycle arrest and apoptosis in cancer cells. Dabrafenib is indicated alone or in combination with trametinib for the treatment of unresectable or metastatic melanoma, adjuvant treatment after surgical resection to prevent recurrence, advanced non-small cell lung cancer (NSCLC), anaplastic thyroid cancer, certain solid tumors in adults and children aged 6 years or older, and low-grade glioma in pediatric patients aged 1 year or older—all when associated with relevant BRAF mutations[1][2][3][4][5][6].

Brand names
Tafinlar
Other names
dabrafenib mesylate
02

Targets

ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)CAPN3 (B-Raf proto-oncogene, serine/threonine kinase)CYP3A4 (Cytochrome P450 3A4)BRAF V600ERAF1 (c-Raf-1 (Y340D/Y341D))CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP2C8 (Cytochrome P450 2C8)

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