Drug intelligence / Profile preview

surzetoclax

Development stage
Phase 2
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral
01

Overview

Surzetoclax is an orally bioavailable, selective small-molecule inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (BCL-2), being developed by AbbVie for the treatment of BCL-2–dependent hematologic malignancies, particularly relapsed or refractory multiple myeloma with t(11;14) translocation.[2][6][10][12] By binding BCL-2 with sub-nanomolar affinity and displacing pro-apoptotic proteins, surzetoclax restores mitochondrial apoptosis signaling and has shown potent antitumor activity in BCL-2–driven cell lines and xenograft models, with a pharmacokinetic and safety profile engineered to mitigate tumor lysis syndrome and other toxicities seen with first-generation BCL-2 inhibitors.[2][6] It is currently in phase 1 clinical trials as monotherapy and in combination regimens such as daratumumab plus dexamethasone in adults with relapsed or refractory multiple myeloma.[6][10][12]

02

Targets

BCL-2 (BCL-2 family)

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