Drug intelligence / Profile preview

pomalidomide + dexamethasone

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Pomalidomide + dexamethasone is an oral combination therapy used primarily for the treatment of relapsed or refractory multiple myeloma in adults who have received at least two prior therapies, including lenalidomide and a proteasome inhibitor such as bortezomib. Pomalidomide is a second-generation immunomodulatory drug (IMiD) that exerts anti-myeloma effects through several mechanisms: it directly inhibits proliferation and induces apoptosis of malignant plasma cells, modulates immune responses, disrupts interactions between myeloma cells and the bone marrow microenvironment, and inhibits angiogenesis. Mechanistically, pomalidomide binds to cereblon (CRBN), a component of the E3 ubiquitin ligase complex, leading to targeted degradation of transcription factors Ikaros (IKZF1) and Aiolos (IKZF3). Dexamethasone is a synthetic glucocorticoid corticosteroid that enhances the anti-myeloma activity of pomalidomide by inducing apoptosis in lymphoid cells. The combination has become a standard backbone regimen for relapsed/refractory multiple myeloma after failure with other agents[1][4][5][6][8].

Other names
PomDex
02

Targets

GR (Glucocorticoid receptor)CRBN (Cereblon)IKZF1 (Ikaros family zinc finger protein 1)

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