Drug intelligence / Profile preview

M3258 + dexamethasone

Development stage
Discontinued
Lead developer
EMD Serono
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

M3258 + dexamethasone is a combination therapy studied for relapsed or refractory multiple myeloma. M3258 is an orally bioavailable, potent, reversible, and highly selective inhibitor of the immunoproteasome subunit LMP7 (also known as β5i or PSMB8), which is highly expressed in malignant hematolymphoid cells such as multiple myeloma. Inhibition of LMP7 disrupts protein degradation and induces apoptosis in target cells. Dexamethasone is a synthetic glucocorticoid with anti-inflammatory and anti-proliferative effects, commonly used in combination therapies for hematological malignancies. The combination was evaluated in a Phase 1 clinical trial, but development was terminated at this stage[1][5][7].

02

Targets

PSMB5 (Proteasome subunit beta Type-5)PSMB8 (Immunoproteasome)

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