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PLX-66140

Development stage: Unknown
Lead developer: Plexium
Modality: Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
Administration: Oral

Overview

PLX-66140 is a small molecule molecular glue degrader developed by Plexium that targets Cyclin-dependent kinase 2 (CDK2). It functions by facilitating the recruitment of CDK2 to the Cereblon (CRBN) E3 ligase complex, leading to its ubiquitination and subsequent degradation via the proteasome. This targeted protein degradation approach is specifically aimed at treating ER+/HER2- breast cancer and other solid tumors characterized by CCNE1 amplification, which are often resistant to standard CDK4/6 inhibitors.

Targets

CRBN (Cereblon)CDK2 (Cyclin-dependent kinase 2)

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