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KPG-818 + dexamethasone
- Development stage
- Phase 1
- Lead developer
- Kangpu Biopharmaceuticals
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
KPG-818 + dexamethasone is a combination of two drugs: KPG-818, a novel oral small molecule and molecular glue modulator of the E3 ubiquitin ligase complex CRL4-CRBN, and dexamethasone, a synthetic glucocorticoid corticosteroid. KPG-818 acts by binding cereblon, inducing degradation of transcription factors IKZF1 (Ikaros) and IKZF3 (Aiolos), leading to immunomodulatory, anti-tumor, and anti-angiogenic effects. Dexamethasone acts as a potent anti-inflammatory and immunosuppressant through activation of the glucocorticoid receptor. This combination is being developed primarily for the treatment of hematological malignancies such as multiple myeloma and may be considered in clinical investigations for relapsed/refractory cases[4][7].
02
Targets
IKZF3 (Zinc finger protein Aiolos)CRBN (Cereblon)GR (Glucocorticoid receptor)IKZF1 (Ikaros family zinc finger protein 1)
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