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Expert Opin Drug Discov ; 15(12): 1373-1380, 2020 12.
Article in English | MEDLINE | ID: mdl-32720533

ABSTRACT

INTRODUCTION: Nearly 50% of patients with metastatic melanoma harbor a BRAFV600-mutation, which can be targeted with the use of BRAF and MEK inhibitors, either in the front-line or treatment-refractory setting. Encorafenib is the newest BRAF-inhibitor to have received FDA-approval in combination with the MEK inhibitor binimetinib. AREAS COVERED: The authors provide an overview of the preclinical development and the clinical trials that led to the use of encorafenib in BRAFV600-mutant melanoma. They also give discussion on its current use in clinical practice, providing their expert perspectives on the subject. EXPERT OPINION: Preclinical research has provided strong rationale for upgrading encorafenib investigation into clinical development/testing. However, there is not yet enough data to determine where encorafenib may fit in comparison to other drugs in the same class, and ongoing trials will further define its role in the treatment of melanoma. Of note, there are ongoing studies that further explore the role of encorafenib + binimetinib such as in combination regimens with immunotherapy drugs, and in brain metastases.


Subject(s)
Carbamates/pharmacology , Melanoma/drug therapy , Skin Neoplasms/drug therapy , Sulfonamides/pharmacology , Animals , Drug Development , Drug Discovery , Drug Evaluation, Preclinical , Humans , Melanoma/genetics , Melanoma/pathology , Mutation , Protein Kinase Inhibitors/pharmacology , Proto-Oncogene Proteins B-raf/genetics , Skin Neoplasms/genetics , Skin Neoplasms/pathology
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