Drug intelligence / Profile preview

dabrafenib + oxaliplatin + trametinib

Development stage
Preclinical
Lead developer
Novartis
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of three small molecule drugs: - **Dabrafenib** is a BRAF inhibitor that targets and inhibits the activity of mutant BRAF kinase (most notably BRAF V600E), thereby blocking downstream signaling in the MAPK/ERK pathway and inhibiting tumor cell proliferation. - **Trametinib** is a MEK inhibitor that blocks MEK1 and MEK2 activity in the same pathway as BRAF, providing synergistic inhibition when combined with dabrafenib. This dual blockade helps prevent or delay resistance mechanisms seen with single-agent therapy. - **Oxaliplatin** is a platinum-based chemotherapeutic agent that forms DNA crosslinks leading to apoptosis in rapidly dividing cells. While combinations of dabrafenib plus trametinib are FDA-approved for several solid tumors harboring BRAF V600E mutations—including melanoma, non-small cell lung cancer (NSCLC), anaplastic thyroid cancer, low-grade glioma, and other solid tumors—there are no known regulatory approvals or published clinical trials specifically evaluating the triple combination of "dabrafenib + oxaliplatin + trametinib." The rationale for such a combination would be to pair targeted therapy against MAPK pathway alterations (BRAF/MEK) with cytotoxic chemotherapy (oxaliplatin), potentially for investigational use in cancers where both approaches may have benefit.

02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)DNAMEK1 (Dual specificity mitogen-activated protein kinase kinase 1)

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