Development of encorafenib for BRAF-mutated advanced melanoma

Development of encorafenib for BRAF-mutated advanced melanoma Purpose of reviewTo describe the pharmacological properties, preclinical and clinical data of the novel V-Raf Murine Sarcoma Viral Oncogene Homolog B (BRAF)-inhibitor encorafenib (LGX818) and to compare these with established BRAF-inhibitors in the treatment of locally advanced or metastatic melanoma.Recent findingsEncorafenib has shown improved efficacy in the treatment of metastatic melanoma in comparison with vemurafenib. Combination with the MEK inhibitor (MEKi) binimetinib allows for higher dose intensities of encorafenib further improving response rates (RRs).SummaryCombination therapy with BRAF and MEKi has evolved as a standard of care in the treatment of locally advanced or metastatic BRAFV600-mutated melanoma. Despite compelling initial RRs, development of treatment resistance eventually leads to tumor progression in the majority of BRAF/MEK-inhibitor treated patients. Moreover, treatment-related adverse events are frequent, resulting in a substantial proportion of dose modifications and/or treatment discontinuations. The second-generation BRAF inhibitor encorafenib has been developed aiming at improved efficacy and tolerability through modifications in pharmacological properties. Clinical phase 3 data show improved progression-free survival both for encorafenib monotherapy and combination therapy with binimetinib compared with vemurafenib. Overall survival data and regulatory approval of this novel substance are eagerly awaited. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Current Opinion in Oncology Wolters Kluwer Health

Development of encorafenib for BRAF-mutated advanced melanoma

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Publisher
Wolters Kluwer Health
Copyright
Copyright © 2018 The Author(s). Published by Wolters Kluwer Health, Inc.
ISSN
1040-8746
eISSN
1531-703X
D.O.I.
10.1097/CCO.0000000000000426
Publisher site
See Article on Publisher Site

Abstract

Purpose of reviewTo describe the pharmacological properties, preclinical and clinical data of the novel V-Raf Murine Sarcoma Viral Oncogene Homolog B (BRAF)-inhibitor encorafenib (LGX818) and to compare these with established BRAF-inhibitors in the treatment of locally advanced or metastatic melanoma.Recent findingsEncorafenib has shown improved efficacy in the treatment of metastatic melanoma in comparison with vemurafenib. Combination with the MEK inhibitor (MEKi) binimetinib allows for higher dose intensities of encorafenib further improving response rates (RRs).SummaryCombination therapy with BRAF and MEKi has evolved as a standard of care in the treatment of locally advanced or metastatic BRAFV600-mutated melanoma. Despite compelling initial RRs, development of treatment resistance eventually leads to tumor progression in the majority of BRAF/MEK-inhibitor treated patients. Moreover, treatment-related adverse events are frequent, resulting in a substantial proportion of dose modifications and/or treatment discontinuations. The second-generation BRAF inhibitor encorafenib has been developed aiming at improved efficacy and tolerability through modifications in pharmacological properties. Clinical phase 3 data show improved progression-free survival both for encorafenib monotherapy and combination therapy with binimetinib compared with vemurafenib. Overall survival data and regulatory approval of this novel substance are eagerly awaited.

Journal

Current Opinion in OncologyWolters Kluwer Health

Published: Mar 1, 2018

References

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