Vemurafenib and BRAF inhibition: a new class of treatment for metastatic melanoma.
作者： Jason J. Luke , F. Stephen Hodi
DOI: 10.1158/1078-0432.CCR-11-2197
关键词: Melanoma 、 Drug development 、 Drug 、 Dacarbazine 、 Internal medicine 、 Pharmacology 、 Stage (cooking) 、 Vemurafenib 、 Oncology 、 V600E 、 Medicine 、 Chemotherapy
摘要: The U.S. Food and Drug Administration recently approved vemurafenib for the treatment of BRAF valine in exon 15, at codon 600 (V600E) mutant metastatic melanoma. Vemurafenib is a competitive small-molecule serine-threonine kinase inhibitor that functions by binding to ATP-binding domain BRAF. Compared with dacarbazine chemotherapy, significantly improved 6-month overall survival patients from 64% 84% exhibited response rate approximately 50%. Median progression-free was also as compared (5.3 versus 1.6 months, respectively), this consistent among groups analyzed, including age, sex, geography, Eastern Cooperative Oncology Group status, disease stage, serum lactate dehydrogenase. success targeting melanoma genomics has created paradigm shift future drug development. Currently, elucidation resistant mechanisms therapy remains an important area active investigation will shape rational treatments development vemurafenib, role targeting, changing landscape provide new foundation clinical investigation.
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