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IMBRUVICA™ (ibrutinib) capsules, for oral use
Initial U.S. Approval: 2013
Ibrutinib is an inhibitor of Bruton's tyrosine kinase (BTK). It is a
white to off-white solid with the empirical formula C25H24N6O2 and a
molecular weight 440.50. Ibrutinib is freely soluble in dimethyl
sulfoxide, soluble in methanol and practically insoluble in water.
IMBRUVICA (ibrutinib) capsules for oral administration are supplied as
white opaque capsules that contain 140 mg ibrutinib as the active
ingredient. Each capsule also contains the following inactive
ingredients: croscarmellose sodium, magnesium stearate, microcrystalline
cellulose, sodium lauryl sulfate. The capsule shell contains gelatin,
titanium dioxide and black ink. Each white opaque capsule is marked with
"ibr 140 mg" in black ink.
Mechanism of Action:
Ibrutinib is a small-molecule inhibitor of BTK. Ibrutinib forms a
covalent bond with a cysteine residue in the BTK active site, leading to
inhibition of BTK enzymatic activity. BTK is a signaling molecule of the
B-cell antigen receptor (BCR) and cytokine receptor pathways. BTK's role
in signaling through the B-cell surface receptors results in activation
of pathways necessary for B-cell trafficking, chemotaxis, and adhesion.
Nonclinical studies show that ibrutinib inhibits malignant B-cell
proliferation and survival in vivo as well as cell migration and
substrate adhesion in vitro.