National Stroke Foundation

Imbruvica (ibrutinib)

The following drug information is obtained from various newswires, published medical journal articles, and medical conference presentations.

Company:

Approval Status:

Approved August 2017

Specific Treatments:

chronic graft-versus-host disease

General Information

Imbruvica (ibrutinib) is an orally available, selective inhibitor of Bruton's tyrosine kinase (Btk).

Imbruvica is specifically indicated for the treatment of adult patients with chronic graft-versus-host disease (cGVHD) after failure of one or more lines of systemic therapy. 

Imbruvica is supplied as a tablet or capsule for oral administration. The recommended dose of Imbruvica for cGVHD is 420 mg orally once daily until cGVHD progression, recurrence of an underlying malignancy, or unacceptable toxicity. When a patient no longer requires therapy for the treatment of cGVHD, Imbruvica should be discontinued considering the medical assessment of the individual patient. 

Clinical Results

FDA Approval

The FDA approval of Imbruvica for chronic Graft vs Host disease (cGVHD) was based on a single-arm trial of 42 patients with cGVHD whose symptoms persisted despite standard treatment with corticosteroids. Most patients’ symptoms included mouth ulcers and skin rashes, and more than 50 percent of patients had two or more organs affected by cGVHD. In the trial, 67 percent of patients experienced improvements in their cGVHD symptoms. The improvement of symptoms lasted for up to five months or longer in 48% of the subjects.

Side Effects

Adverse effects associated with the use of Imbruvica for cGVHD may include, but are not limited to, the following:

fatigue

bruising

diarrhea

thrombocytopenia

muscle spasms

stomatitis

nausea

hemorrhage

anemia

pneumonia

Mechanism of Action

Imbruvica (ibrutinib) is an orally available, selective inhibitor of Bruton's tyrosine kinase (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 crole in signaling through the B-cell surface receptors results in activation of pathways necessary for B-cell trafficking, chemotaxis, and adhesion.

Additional Information

For additional information regarding Imbruvica or chronic graft-versus-host disease, please visit https://www.imbruvica.com/