Drug intelligence / Profile preview

binimetinib + belinostat

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

Overview

This drug is a **combination therapy** of two small molecules, **binimetinib** and **belinostat**, currently under investigation for the treatment of uveal melanoma, an aggressive form of eye cancer. **Binimetinib** is a selective, uncompetitive inhibitor of MEK1 and MEK2, key kinases in the MAPK signaling pathway; it suppresses cell proliferation by blocking MEK-mediated phosphorylation of ERK, thereby interrupting growth signals in cancer cells. **Belinostat** is a pan-histone deacetylase (HDAC) inhibitor that causes accumulation of acetylated histones and proteins, leading to cell cycle arrest, apoptosis, and inhibition of tumor angiogenesis. The rationale for this combination is to simultaneously block two different oncogenic signaling axes; MEK inhibition impedes downstream proliferation signals, while HDAC inhibition affects gene expression and cell survival, which together may overcome therapeutic resistance in uveal melanoma. This combination is not currently approved for any indication but is under active clinical investigation for metastatic uveal melanoma[1][6].

02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)HDAC (HDAC family)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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