Drug intelligence / Profile preview

PF-07284890 + binimetinib

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

Overview

PF-07284890 + binimetinib is an **oral combination therapy** consisting of PF-07284890, a next-generation, investigational, brain-penetrant BRAF monomer inhibitor, and binimetinib, a clinically approved MEK inhibitor. PF-07284890 is designed to inhibit BRAF V600 mutant kinases, including those in brain and non-brain solid tumors, and is being evaluated for its efficacy in overcoming acquired resistance to prior BRAF inhibitor therapies. Binimetinib (also known as ARRY-461) is a selective inhibitor of MEK1 and MEK2 kinases, often used in combination with BRAF inhibitors. This combination is primarily being developed for BRAF V600-mutated advanced solid tumors, with a particular focus on malignancies involving the brain, such as primary brain tumors and metastatic melanoma with brain involvement. Developed by Pfizer, this combination is undergoing early clinical trials to assess safety, pharmacokinetics, and preliminary anti-tumor activity, especially in patients who have progressed on, or are refractory to, approved BRAF inhibitor-based regimens[1][2][5][7].

02

Targets

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

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