Drug intelligence / Profile preview

LY3214996 + abemaciclib

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

**LY3214996 + abemaciclib** is an experimental oral combination therapy consisting of LY3214996, a selective small molecule inhibitor of extracellular signal-regulated kinase 1/2 (ERK1/2), and abemaciclib, a selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). This combination is being studied for its antitumor effects in cancers characterized by aberrant activation of the MAPK pathway (such as RAS or BRAF mutations) and cell cycle dysregulation. Preclinical and early-phase clinical studies have shown that the combination can provide enhanced pathway suppression and greater tumor growth inhibition compared to either agent alone, particularly in tumors harboring resistance to single-agent therapy. Key indications under investigation include advanced solid tumors, particularly those with MAPK pathway alterations, and recurrent glioblastoma[1][2][3][5].

02

Targets

CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)MAPK3 (Mitogen-activated protein kinase 1)

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