TY - JOUR
T1 - Dabrafenib
AU - Kainthla, Radhika
AU - Kim, Kevin B.
AU - Falchook, Gerald S.
PY - 2014/1/1
Y1 - 2014/1/1
N2 - Dabrafenib was developed as a highly specific reversible inhibitor of V600-mutant BRAF kinase, an oncogenic mutation driving proliferation in many different types of aggressive tumors. Metastatic melanoma has a high prevalence of V600-mutant BRAF, and clinical trials showed that dabrafenib improved response rates and median progression-free survival in patients with V600E BRAF mutations, including those with brain metastasis. Preliminary results suggest that dabrafenib may also have some role in non-melanoma V600-mutant solid tumors; however, more studies are needed. With a welltolerated toxicity profile and few drug interactions, dabrafenib is effective as a monotherapy; however, resistance eventually develops in most patients after persistent exposure to the drug. Current research focuses on combination strategies with dabrafenib to not only improve response rates but also overcome resistance.
AB - Dabrafenib was developed as a highly specific reversible inhibitor of V600-mutant BRAF kinase, an oncogenic mutation driving proliferation in many different types of aggressive tumors. Metastatic melanoma has a high prevalence of V600-mutant BRAF, and clinical trials showed that dabrafenib improved response rates and median progression-free survival in patients with V600E BRAF mutations, including those with brain metastasis. Preliminary results suggest that dabrafenib may also have some role in non-melanoma V600-mutant solid tumors; however, more studies are needed. With a welltolerated toxicity profile and few drug interactions, dabrafenib is effective as a monotherapy; however, resistance eventually develops in most patients after persistent exposure to the drug. Current research focuses on combination strategies with dabrafenib to not only improve response rates but also overcome resistance.
UR - http://www.scopus.com/inward/record.url?scp=84906932962&partnerID=8YFLogxK
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U2 - 10.1007/978-3-642-54490-3_14
DO - 10.1007/978-3-642-54490-3_14
M3 - Article
C2 - 24756796
AN - SCOPUS:84906932962
SN - 0080-0015
VL - 201
SP - 227
EP - 240
JO - Recent Results in Cancer Research
JF - Recent Results in Cancer Research
ER -