Drug intelligence / Profile preview

encorafenib + binimetinib + capmatinib

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

This drug is a **combination therapy** consisting of three small-molecule inhibitors: encorafenib, binimetinib, and capmatinib. - **Encorafenib** is a selective BRAF inhibitor, blocking the BRAF V600E/K/D mutant kinases and interrupting the MAPK signaling pathway, leading to decreased cancer cell proliferation[2][3][4]. - **Binimetinib** is a reversible MEK1 and MEK2 inhibitor, also acting on the MAPK pathway and further suppressing cell growth signals downstream from BRAF[2][3][4]. - **Capmatinib** is a selective inhibitor of the MET (hepatocyte growth factor receptor) proto-oncogene tyrosine kinase, targeting tumors with dysregulated MET signaling and is approved for non-small cell lung cancer with MET exon 14 skipping mutations (this is NOT part of the encorafenib + binimetinib currently approved regimens, but is listed here per your query context). Currently, there is no evidence of a marketed, FDA-, or EMA-approved product or published clinical trial using this specific triple combination. However, each component has clinical utility in targeted cancer therapy, and dual combinations of encorafenib + binimetinib are FDA-approved for unresectable or metastatic melanoma with BRAF V600E or V600K mutations and metastatic NSCLC with BRAF V600E mutations[1][2][3][4][6][7]. No published clinical data or regulatory approvals exist for the combined use of capmatinib with encorafenib and binimetinib. Clinical logic for such a combination could stem from seeking to block MAPK and MET signaling pathways simultaneously in selected cancers, but as of now, this is hypothetical.

02

Targets

MET (Mesenchymal-epithelial transition factor receptor)BRAF V600ERAF1 (c-Raf-1 (Y340D/Y341D))MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)

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