Drug intelligence / Profile preview

epaldeudomide

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

Overview

**Epaldeudomide (KPG-818)** is a novel small molecule immunomodulatory agent developed by Kangpu Biopharmaceuticals as a next-generation cereblon (CRBN) modulator and lenalidomide analog. It functions as a molecular glue that enhances the E3 ubiquitin ligase complex CRL4-CRBN activity, promoting targeted protein degradation, while exhibiting potent TNF-α inhibition (>50% at 100 nM), broad-spectrum immunomodulatory effects, anti-angiogenic properties, and direct anti-tumor activity. Primarily investigated for hematological malignancies like multiple myeloma (with preclinical data and 50% response rates in heavily pre-treated patients), it also advances in Phase II for inflammatory bowel diseases and Phase I/II for systemic lupus erythematosus, showing favorable pharmacokinetics, safety, and tolerability in U.S. Phase I trials (NCT04283097).

Other names
CRL4-CRBN modulator KPG-818CRL-4-CRBN modulator KPG-818CRL 4-CRBN modulator KPG-818
02

Targets

CRBN (Cereblon)TNFA (Tumor necrosis factor alpha (soluble))

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