Drug intelligence / Profile preview

ibrutinib + dexamethasone

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

Overview

**Ibrutinib + dexamethasone** is a combination of an irreversible Bruton’s tyrosine kinase (BTK) inhibitor (ibrutinib) and a synthetic glucocorticoid corticosteroid (dexamethasone) used in clinical studies for relapsed or refractory multiple myeloma and other B-cell–mediated hematological malignancies. - **Ibrutinib** selectively and covalently binds BTK, a kinase that mediates B-cell receptor signaling, leading to decreased cell survival and proliferation and increased apoptosis in malignant B-cells. It also inhibits interleukin-2 inducible kinase (ITK) in T cells and affects PI3K signaling[2][8][6]. - **Dexamethasone** binds and activates the glucocorticoid receptor, modulating gene expression and producing anti-inflammatory, immunosuppressive, and apoptotic effects. Primary indications in combination trials have included treatment of relapsed/refractory multiple myeloma, with data indicating enhanced apoptosis of myeloma cells via PI3K/PARP pathway and complementary anti-myeloma activity[4][3][5].

Other names
ibrutinib and dexamethasone
02

Targets

ITK (Interleukin 2-inducible T-cell kinase)GR (Glucocorticoid receptor)BTK (Bruton tyrosine kinase)

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