Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032 - PubMed (original) (raw)

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Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032

Jill C Rubinstein et al. J Transl Med. 2010.

Abstract

Activating mutations in BRAF kinase are common in melanomas. Clinical trials with PLX4032, the mutant-BRAF inhibitor, show promising preliminary results in patients selected for the presence of V600E mutation. However, activating V600K mutation is the other most common mutation, yet patients with this variant are currently excluded from the PLX4032 trials. Here we present evidence that a patient bearing the BRAF V600K mutation responded remarkably to PLX4032, suggesting that clinical trials should include all patients with activating BRAF V600E/K mutations.

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Figures

Figure 1

Figure 1

Chest wall lesions before treatment with PLX4032 (A) and on the first day of the fifth treatment cycle (B).

Figure 2

Figure 2

Electropherogram from Sanger dideoxy sequencing showing the patient's melanoma tumor BRAF codon 600 mutation (AAG/GTG), encoding V600K/WT protein.

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