Drug intelligence / Profile preview

PF-07799933 + binimetinib

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

Overview

PF-07799933 + binimetinib is a combination therapy under clinical investigation for advanced solid tumors with BRAF mutations. PF-07799933 is an oral, selective, ATP-competitive small molecule RAF kinase inhibitor targeting BRAF signaling in both BRAF V600-mutant and non-V600-mutant tumors. It is distinct in sparing non-mutated RAF dimers, reducing paradoxical MAPK pathway activation compared to first-generation BRAF inhibitors. Binimetinib is a selective, oral MEK inhibitor. The combination is aimed at overcoming acquired resistance mechanisms in BRAF-mutant cancers and enhancing anti-tumor responses, including in tumors refractory to prior BRAF or MEK inhibitor therapy. The therapy is being tested particularly in patients with various classes of BRAF-mutated malignancies, including those with brain involvement[1][2][3].

Other names
ARRY-439162ARRY439162ARRY 439162
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)RAF1 (c-Raf-1 (Y340D/Y341D))MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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