Imbruvica (ibrutinib)

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

Company:

Approval Status:

Approved February 2014

Specific Treatments:

chronic lymphocytic leukemia and Waldenstrom macroglobulinemia

Therapeutic Areas

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General Information

Imbruvica (ibrutinib) is an orally available, selective inhibitor of Bruton's tyrosine kinase (Btk), a gene that is disrupted in the human disease X-linked agammaglobulenemia (XLA). BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways.

Imbruvica is specifically approved for chronic lymphocytic leukemia in patients who have received at least one prior therapy.

Imbruvica is supplied as a capsule for oral administration. The recommended dose is 420 mg taken orally once daily (three 140 mg capsules once daily). Capsules should be taken orally with a glass of water. Do not open, break, or chew the capsules.

Clinical Results

FDA Approval
The FDA approval of Imbruvica for chronic lymphocytic leukemia was based on an open-label, multi-center trial of 48 previously treated patients. Imbruvica was administered orally at 420 mg once daily until disease progression or unacceptable toxicity. The overall response rate (ORR) and duration of response (DOR) were assessed using a modified version of the International Workshop on CLL Criteria by an Independent Review Committee. The ORR was 58.3%, all partial responses. None of the patients achieved a complete response. The DOR ranged from 5.6 to 24.2+ months. The median DOR was not reached.

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.

Side Effects

Adverse events associated with the use of Imbruvica for chronic lymphocytic leukemia may include, but are not limited to, the following:

  • thrombocytopenia
  • diarrhea
  • bruising
  • neutropenia
  • anemia
  • upper respiratory tract infection
  • fatigue
  • musculoskeletal pain
  • rash
  • pyrexia
  • constipation
  • peripheral edema
  • arthralgia
  • nausea
  • stomatitissinusitis
  • dizziness

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 lymphocytic leukemia, please visit the Imbruvica web page.