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ABSTRACT
Introduction: The mitogen-activated protein kinase (MAPK) pathway plays a critical role in the development of malignant melanoma and is an important therapeutic target. Selumetinib is a selective oral MEK1/2 inhibitor that has been evaluated in metastatic cutaneous and uveal melanoma. It is also currently undergoing further evaluation in clinical trials for other solid tumors including thyroid cancer, non-small cell lung cancer, and neurofibromatosis type 1.
Areas covered: This article summarizes the pharmacology of selumetinib, as well as data from pre-clinical and clinical studies evaluating the efficacy of selumetinib for the treatment of cutaneous and uveal melanoma. The potential future role of selumetinib in combination with other targeted agents and in combination with chemotherapy and immunotherapy is also discussed.
Expert Opinion: In order to improve the efficacy of selumetinib and to advance its use in the clinic for melanoma, further studies should focus on optimizing the dosing schedule of selumetinib, as well as evaluating the combination of selumetinib with other cytotoxic, targeted and immunological therapies.