Drug intelligence / Profile preview

tovorafenib + pimasertib

Development stage
Unknown
Lead developer
Day One Biopharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

**Tovorafenib + pimasertib** is an investigational oral combination therapy of two selective small-molecule inhibitors targeting the MAPK signaling pathway, designed for the treatment of recurrent, progressive, or refractory solid tumors with MAPK pathway aberrations. - **Tovorafenib** is a highly selective, brain-penetrant, type II pan-RAF kinase inhibitor that inhibits RAF monomers and dimers. - **Pimasertib** is a highly selective inhibitor of mitogen-activated protein kinase 1 and 2 (MEK-1/-2). Preclinical and early clinical studies indicate that the combination produces vertical pathway inhibition and may be synergistically active, particularly in tumors driven by BRAF fusions or NF1-loss-of-function mutations, where monotherapy may be insufficient. Ongoing development focuses on adolescent and adult patients with solid tumors, especially those resistant to standard treatments and with MAPK pathway genetic alterations[1][2][6].

Other names
tovorafenib + pimasertib
02

Targets

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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