Drug intelligence / Profile preview

dabrafenib + LTT462 + trametinib

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

Overview

This combination consists of **dabrafenib**, **LTT462**, and **trametinib**—three investigational and/or approved targeted therapies used together, primarily in research settings, for advanced/metastatic cancers harboring BRAF V600 mutations. Dabrafenib is a selective inhibitor of mutant BRAF kinase, trametinib is a selective inhibitor of MEK1/2, and LTT462 is a highly selective ERK1/2 inhibitor. The combination is being tested to overcome resistance mechanisms in the MAPK pathway and achieve more sustained inhibition than dual BRAF-MEK inhibition alone. It is primarily under clinical investigation in advanced/metastatic BRAF V600 colorectal cancer and possibly other solid tumors[5]. Dabrafenib and trametinib are approved drugs, while LTT462 is an investigational agent developed by Novartis.

Other names
dabrafenib + LTT462 + trametinib
02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)BRAF (B-Raf proto-oncogene, serine/threonine kinase)KSR1/KSR2 (Kinase suppressor of Ras 1/Kinase suppressor of Ras 2 scaffold complex interface)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)RAF1 (c-Raf-1 (Y340D/Y341D))Serine/threonine-protein kinase B-raf (BRAF) V600 mutant formsMAPK3 (Mitogen-activated protein kinase 1)

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