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zaloblideg

Development stage: Phase 1
Lead developer: Arvinas
Modality: PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration: Oral

Overview

Zaloblideg (ARV-393) is an orally bioavailable targeted protein degrader (PROTAC) designed to selectively degrade the transcriptional regulator B-cell lymphoma 6 (BCL6) via cereblon (CRBN)-mediated ubiquitination and proteasomal degradation, and is being developed for the treatment of BCL6-dependent non-Hodgkin lymphomas, such as diffuse large B-cell lymphoma and related B-cell malignancies.[4][8][10] By recruiting BCL6 to an E3 ubiquitin ligase complex, zaloblideg promotes sustained removal of the oncogenic protein rather than transient inhibition, aiming to overcome resistance mechanisms associated with conventional BCL6 inhibitors and to deliver a first-in-class therapeutic option in relapsed or refractory lymphoma settings.[4][8]

Other names: compound 81compound81compound-81

Targets

CRBN (Cereblon)BCL6 (B cell lymphoma 6 protein)

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