Drug intelligence / Profile preview

vemurafenib + aldesleukin

Development stage
Unknown
Lead developer
Plexxikon
Modality
Cytokines & Interferons → Recombinant Proteins and Enzymes, Small Molecules
Administration
Oral (vemurafenib), Intravenous (aldesleukin)
01

Overview

Vemurafenib + aldesleukin is a combination of a targeted small molecule kinase inhibitor (vemurafenib) and a recombinant cytokine (aldesleukin, also known as interleukin-2). Vemurafenib selectively inhibits the mutant BRAF kinase (especially BRAF V600E), blocking the MAPK pathway signaling required for the growth of certain melanomas. Aldesleukin activates CD8 T cells and other immune effector cells, aiming to stimulate anti-tumor immunity. This combination has been investigated for its ability to leverage tumor microenvironment changes induced by BRAF inhibition and increase immune infiltration through cytokine therapy. The main indication under investigation is unresectable or metastatic melanoma harboring the BRAF V600E mutation[1][5][7].

Brand names
Zelboraf + Proleukin
Other names
vemurafenib + interleukin-2vemurafenib + IL-2vemurafenib + HD-IL-2
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)IL-2R (Interleukin-2/interleukin-15 receptor complex)

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