Drug intelligence / Profile preview

mirdametinib + BGB-3245

Development stage
Unknown
Lead developer
SpringWorks Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

mirdametinib + BGB-3245 is an investigational combination therapy for advanced solid cancers harboring MAPK pathway mutations. Mirdametinib is a selective MEK1/2 inhibitor, blocking downstream ERK signaling, while BGB-3245 (brimarafenib) is a next-generation RAF dimer inhibitor that targets all RAF isoforms, including those with class I (BRAF V600), class II/III mutations, fusions, and splice variants. The combination aims to inhibit aberrant MAPK pathway signaling through dual blockade, overcoming resistance to prior BRAF/MEK inhibitor therapies and addressing a broad spectrum of molecular alterations. The regimen is being evaluated for safety, tolerability, and antitumor activity in unresectable or metastatic solid tumors refractory to or progressed after standard therapies, particularly when MAPK pathway genetic alterations are present[1][3][5].

02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)RAF1 (c-Raf-1 (Y340D/Y341D))MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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