MEK inhibitors: selumetinib

BRAF targets in melanoma. Biological mechanisms, resistance, and drug discovery. Cancer drug discovery and development. Volume 82. Ed. Ryan J. Sullivan. Springer (2015)


Selumetinib (AZD-6244, AstraZeneca) is a selective MEK1/2 inhibitor which demonstrated pre-clinical efficacy against BRAF mutant melanoma cell lines. In an unselected melanoma population, selumetinib was compared with temozolomide and did not demonstrate any improvement in PFS [21]. In a randomized phase II trial, selumetinib combined with dacarbazine was compared to dacarbazine alone in BRAF mutant melanoma. The combination arm demonstrated improved PFS (5.6 vs. 3 months) but no change in OS [22]. Although this agent is undergoing further development in other malignancies (lung adenocarcinoma, thyroid carcinoma, leukemias), it is not likely selumetinib will be used in BRAF mutant melanoma in the future.

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