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Discovery of a Novel Potent and Orally Efficacious PROTAC Degrader of HPK1 for Tumor Immunotherapy

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New PROTAC degrader significantly enhances IL-2 and IFN-γ release in TCR activation, indicating its potential in tumor immunotherapy.

The HPK1 PROTAC degrader 10m demonstrated sustained degradation and inhibited tumor growth in a syngeneic mouse model.
10m achieved a DC50 of 5.0 ± 0.9 nM and a Dmax ≥ 99%, showcasing its potency in degrading HPK1.
Combination of 10m with PD-1 blockade suggested enhanced antitumor effectiveness compared to either treatment alone.
The compound 10m also mitigated immunosuppressive effects from PGE2, NECA, or TGF-β, highlighting its therapeutic versatility.

Tong et al. (2025) studied this question.

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