Imbruvica (ibrutinib)

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


Approval Status:

Approved January 2015

Specific Treatments:

Waldenström’s macroglobulinemia

Therapeutic Areas

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General Information

Imbruvica (ibrutinib) is small molecule inhibitor of Bruton’s tyrosine kinase (BTK). 

Imbruvica is specifically indicated for the treatment of adult patients with Waldenström’s macroglobulinemia. 

Imbuvica is supplied as a tablet for oral administration. The recommended dose of Imbruvica for WM as a single agent or in combination with rituximab for WM is 420 mg orally once daily until disease progression or unacceptable toxicity. When administering Imbruvica in combination with rituximab, consider administering Imbruvica prior to rituximab when given on the same day. 

Clinical Results

FDA Approval

The FDA approval for Waldenström’s macroglobulinemia was based on a clinical study of 63 previously treated subjects. All study subjects received a daily 420 milligram orally administered dose of the medication until disease progression or side effects became intolerable. Results showed 62% of subjects had their cancer shrink after treatment (overall response rate). At the time of the study, the duration of response ranged from 2.8 months to approximately 18.8 months.

The FDA approval of Imbruvica in combination with rituximab was based on results from the randomized, double-blind, placebo-controlled iNNOVATE study (PCYC-1127). The iNNOVATE study evaluated Imbruvica in combination with rituximab versus placebo plus rituximab in 150 patients with either relapsed/refractory (r/r) disease or previously untreated WM. At a median follow up of 26.5 months, a significant improvement in the Independent Review Committee (IRC)-assessed primary endpoint of progression-free survival (PFS) was seen with Imbruvica plus rituximab when compared with placebo plus rituximab (30-month PFS rates were 82% vs. 28%, respectively). Patients in the Imbruvica plus rituximab treatment arm experienced an 80% reduction in relative risk of disease progression or death compared with patients treated with placebo plus rituximab.

Side Effects

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





musculoskeletal pain







Mechanism of Action

Imbruvica (ibrutinib) is small molecule 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 role 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 Waldenström’s macroglobulinemia, please visit