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Drug intelligence / Profile preview
MLN2480 + alisertib
- Development stage
- Phase 1
- 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
AURKA (Aurora kinase A)AURKB (Aurora kinase B)ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)RAF1 (c-Raf-1 (Y340D/Y341D))
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