Drug intelligence / Profile preview

pomalidomide + zanubrutinib

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Pomalidomide + zanubrutinib is an investigational combination therapy consisting of two small molecule drugs with distinct mechanisms of action. Pomalidomide is an immunomodulatory agent and thalidomide derivative that exerts anti-angiogenic, anti-proliferative, and immunomodulatory effects primarily through modulation of the cereblon E3 ubiquitin ligase complex, leading to degradation of specific transcription factors involved in tumor cell survival. Zanubrutinib is a Bruton's tyrosine kinase (BTK) inhibitor that binds covalently to the Cys481 residue in BTK's ATP-binding pocket, thereby blocking B-cell receptor signaling and inhibiting proliferation and survival of malignant B cells. This combination has been explored for use in relapsed or refractory hematologic malignancies such as multiple myeloma and lymphoma[1][6][10]. Both agents are orally administered small molecules.

02

Targets

CRBN (Cereblon)BTK (Bruton tyrosine kinase)

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