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sontigidomide

Development stage: Discontinued
Modality: PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules

Overview

**Sontigidomide** is a small molecule antineoplastic agent in early development, characterized as a PROTAC degrader targeting GSPT1 and IKZF1/3. It demonstrates potent antiproliferative activity, inhibiting over 80% proliferation of MOLM-13 acute myeloid leukemia cells at 1 μM after 3 days, and shows efficacy against AML and solid tumor cells. Its structure features a racemic N-substituted glutarimide moiety akin to thalidomide derivatives, with proposed INN status by WHO, indicating preclinical to early clinical evaluation for oncology.

Targets

CRBN (Cereblon)GSPT1 (G1 to S phase transition 1)IKZF1 (Ikaros family zinc finger protein 1)IKZF3 (Zinc finger protein Aiolos)

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