Drug intelligence / Profile preview

ibrutinib + pomalidomide + dexamethasone

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

Overview

A triplet combination regimen of **ibrutinib**, **pomalidomide**, and **dexamethasone** investigated for relapsed or refractory multiple myeloma, particularly in patients who have progressed following standard therapies including lenalidomide and a proteasome inhibitor. - **Ibrutinib** is a small molecule that irreversibly inhibits Bruton’s tyrosine kinase (BTK), disrupting B-cell receptor signaling and downstream survival pathways in malignant B cells. - **Pomalidomide** is a potent immunomodulatory drug (IMiD) with anti-myeloma activity, acting by promoting ubiquitin-mediated degradation of transcription factors IKZF1/3, modulating the immune microenvironment, inhibiting angiogenesis, and inducing apoptosis in myeloma cells. - **Dexamethasone** is a synthetic glucocorticoid that induces apoptosis and suppresses proliferation in multiple myeloma cells via glucocorticoid receptor activation. This combination is usually administered orally, with ibrutinib and pomalidomide oral capsules/tablets and dexamethasone oral tablets, in clinical trials for patients with relapsed/refractory multiple myeloma[1][7][8][10].

02

Targets

CRBN (Cereblon)GR (Glucocorticoid receptor)BTK (Bruton tyrosine kinase)

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