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PLX-4545

Development stage: Unknown
Lead developer: Plexium
Modality: Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration: Oral

Overview

PLX-4545 is an orally available, cereblon (CRBN)-based molecular glue degrader that selectively targets the transcription factor IKZF2, also known as Helios. Developed by Plexium, Inc., PLX-4545 is designed to destabilize highly suppressive regulatory T cells (Tregs) within the tumor microenvironment by inducing rapid and selective degradation of IKZF2. This mechanism aims to overcome anti-tumor immunity suppression and potentially address resistance to checkpoint inhibitor therapies in cancer. The drug is currently in Phase 1 clinical trials for neoplasms (cancers), with initial studies evaluating safety and pharmacokinetics in healthy volunteers[1][3][4][6].

Other names: Helios molecular glue degrader

Targets

CRBN (Cereblon)IKZF2

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