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mezigdomide + BMS-986158 + dexamethasone

Development stage: Unknown
Lead developer: Bristol Myers Squibb
Modality: Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration: Oral

Overview

**mezigdomide + BMS-986158 + dexamethasone** is an investigational, all-oral, triple-agent combination regimen evaluated for the treatment of relapsed/refractory multiple myeloma. - **Mezigdomide** (CC-92480, MEZI) is a next-generation CELMoD™ (cereblon E3 ligase modulator) that induces targeted degradation of transcription factors such as Ikaros and Aiolos, resulting in immunomodulatory and antiproliferative activity in multiple myeloma. - **BMS-986158** is a selective small molecule inhibitor of bromodomain and extraterminal domain (BET) proteins (BRD2, BRD3, BRD4), acting as an epigenetic modulator that impacts oncogenic transcriptional programs by inhibiting BET-mediated gene expression. - **Dexamethasone** is a synthetic glucocorticoid corticosteroid with anti-inflammatory and antineoplastic activity, widely used as part of combination regimens in myeloma. This triplet is being studied in the CA057-003 clinical trial with promising efficacy and manageable safety for relapsed/refractory multiple myeloma, especially for patients with prior exposure to BCMA-targeted therapies[3][5][7].

Other names: MEZId + BMS-986158 + dexamethasone

Targets

BRD4 (Bromodomain-containing protein 4)BRD3 (Bromodomain-containing protein 3)BRD2 (Bromodomain-containing protein 2)CRBN (Cereblon)IKZF3 (Zinc finger protein Aiolos)IKZF1 (Ikaros family zinc finger protein 1)GR (Glucocorticoid receptor)

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