Drug intelligence / Profile preview

MLN2480 + alisertib

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

Overview

MLN2480 + alisertib is an investigational combination therapy being evaluated primarily in adult patients with advanced nonhematologic malignancies (advanced solid tumors). MLN2480 is a small molecule pan-RAF kinase inhibitor targeting A-RAF, B-RAF, and CRAF within the MAPK pathway, blocking key steps in oncogenic signaling. Alisertib is a small molecule inhibitor of Aurora A kinase, a serine/threonine kinase implicated in the regulation of mitosis and cell division. This combination aims to simultaneously inhibit RAF-driven MAPK signaling and cell division, potentially providing synergistic antitumor effects in cancers with hyperactive MAPK signaling or resistance to standard therapies. The combination has been evaluated in phase 1b trials to characterize safety, pharmacokinetics, and determine the maximum tolerated dose and recommended phase 2 dose[1][3][7][5].

Other names
MLN2480MLN-2480MLN 2480TAK-580TAK580TAK 580alisertibMLN8237MLN-8237MLN 8237
02

Targets

ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)AURKB (Aurora kinase B)AURKA (Aurora kinase A)

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