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DXTX-1464

Development stage: Preclinical
Lead developer: Differentiated Therapeutics
Modality: PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules

Overview

**DXTX-1464** is a first-in-class, highly potent and selective small molecule targeted protein degrader developed by Differentiated Therapeutics for cancer therapy. It selectively degrades CCNE1/CCNE2-CDK2 complexes, leading to potent inhibition of downstream signaling pathways critical for cell cycle progression in oncology. As a development candidate highlighted at AACR 2025, it targets genetically defined drivers of neoplasms through induced proximity and proteolysis-targeting mechanisms leveraging AI-driven discovery.

Other names: DXTX 1464DXTX1464DXTX-1464

Targets

CCNE2 (G1/S-specific cyclin-E2)CCNE1 (Cyclin E1)CDK2 (Cyclin-dependent kinase 2)

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