Drug intelligence / Profile preview

davelizomib

Development stage
Phase 1
Lead developer
Sino Biopharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

TQB3602 (davelizomib) is a novel orally bioavailable small molecule proteasome inhibitor developed as an optimized derivative of ixazomib. It incorporates an acridine ring into the structure of ixazomib to improve metabolic stability while maintaining high activity and selectivity for the 20S proteasome enzyme. Upon oral administration, TQB3602 is rapidly hydrolyzed to its active boronic acid form (WXFL10410333), which selectively inhibits the 20S proteasome and disrupts protein degradation in cancer cells. Preclinical studies demonstrated potent antitumor efficacy in multiple myeloma models with favorable toxicity profiles compared to existing agents. In phase I clinical trials for relapsed/refractory multiple myeloma (RRMM), TQB3602 showed good tolerability, a favorable neurotoxicity profile, and preliminary evidence of efficacy[1][3][4][5][6].

Other names
davelizomibTQB3602TQB-3602TQB 3602WXFL10410333WXFL-10410333WXFL 10410333
02

Targets

PSMB5 (Proteasome subunit beta Type-5)

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