Drug intelligence / Profile preview

dabrafenib + LTT462

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

Overview

This is an **experimental combination therapy** of dabrafenib, a BRAF inhibitor, and LTT462, a selective ERK1/2 inhibitor. Dabrafenib selectively inhibits mutated forms of BRAF kinase, particularly BRAF V600 mutations, thereby blocking the MAPK/ERK signaling pathway that drives tumor cell proliferation. LTT462 is a small molecule inhibitor that targets ERK1/2, acting downstream of BRAF in the same pathway. The combination is being developed primarily for treatment of adults with advanced or metastatic cancers harboring BRAF V600 mutations, such as colorectal cancer, to overcome resistance to BRAF inhibition by suppressing pathway reactivation through ERK. This combination is under clinical investigation in a dose-escalation trial to determine safety and recommended dose in patients with advanced/metastatic BRAF V600 mutant colorectal cancer[1][6].

Brand names
Tafinlar + LTT462
02

Targets

MAPK3 (Mitogen-activated protein kinase 1)BRAF (B-Raf proto-oncogene, serine/threonine kinase)

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