Generic Name |
Dabrafenib mesylate | |
---|---|---|
IND |
GSK2118436 | |
Brand Name (US) |
TAFINLAR | |
Manufacturer |
GlaxoSmithKline | |
Drug Type |
Tyrosine Kinase Inhibitor | |
Delivery |
Oral | |
Approval Status |
Approved for a non-GIST cancer | |
Indications |
Melanoma, BRAF driven cancers | |
Overall Strategy |
Oncogenic Signal Path Based | |
Strategy |
Block BRAF | |
Drug Category |
BRAF inhibitor |
Dabrafenib, a BRAF inhibitor that is approved for melanoma with BRAF V600E or V600K mutations. It is a potent BRAF inhibitor that has recently shown activity in a phase 3 trial of melanoma patients. In addition, it has been shown to be effective against brain metastases in melanoma patients with BRAF mutations. Most drugs are not effective against brain metastases because they don't cross the brain-blood barrier.
A very small percentage of GIST patients have BRAF mutations; either as the primary mutation, or in very rare cases, a secondary mutation. Dabrafenib is the first BRAF inhibitor to demonstrate activity in a GIST patient (see link to full text article below).