Discovery of TQ-3959 as a Potent and Orally Bioavailable BTK PROTAC Degrader Incorporating a Novel Benzisoxazole-Based CRBN Ligand for the Treatment of B-Cell Malignancies

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This research reveals TQ-3959 as a potent BTK PROTAC degrader, indicating it may provide a new strategy for lymphoma treatment.

TQ-3959 significantly reduced BTK levels, achieving nearly complete tumor regression in a mouse model.
The compound demonstrated a degradation potency of 0.4 nM and 58.0% oral bioavailability in mice.
Utilizing a novel benzisoxazole-based CRBN ligand, TQ-3959 effectively inhibited multiple lymphoma cell lines.
The findings suggest that BTK PROTAC degradation can overcome limitations of traditional BTK inhibitors.

Ren et al. (2025) studied this question.

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