IMBRUVICA™ (ibrutinib) Capsules

Warnings

Description

Clinical pharmacology

Indications and usage

Contraindications

Precautions

Adverse reactions

Dosage and administration

How supplied

Reference

Warnings

See precautions below.

Description

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.

Clinical pharmacology

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.

Indications and usage

INDICATIONS AND USAGE:
IMBRUVICA is a kinase inhibitor indicated for the treatment of patients with mantle cell lymphoma (MCL) who have received at least one prior therapy.

This indication is based on overall response rate. An improvement in survival or disease-related symptoms has not been established

Contraindications

None.

Precautions

WARNINGS AND PRECAUTIONS

Hemorrhage: Monitor for bleeding.
Infections: Monitor patients for fever and infections and evaluate promptly.
Myelosuppression: Check complete blood counts monthly.
Renal Toxicity: Monitor renal function and maintain hydration.
Second Primary Malignancies: Other malignancies have occurred in patients, including skin cancers, and other carcinomas.
Embryo-Fetal Toxicity: Can cause fetal harm. Advise women of the potential risk to a fetus and to avoid pregnancy while taking the drug

Adverse reactions

ADVERSE REACTIONS
The most common adverse reactions (≥20%) in patients with MCL were thrombocytopenia, diarrhea, neutropenia, anemia, fatigue, musculoskeletal pain, peripheral edema, upper respiratory tract infection, nausea, bruising, dyspnea, constipation, rash, abdominal pain, vomiting and decreased appetite.

To report SUSPECTED ADVERSE REACTIONS, contact Pharmacyclics at 1-877-877-3536 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch

DRUG INTERACTIONS
CYP3A Inhibitors: Avoid co-administration with strong and moderate CYP3A inhibitors. If a moderate CYP3A inhibitor must be used, reduce IMBRUVICA dose .

CYP3A Inducers: Avoid co-administration with strong CYP3A inducers.

USE IN SPECIFIC POPULATIONS
Hepatic Impairment: Avoid use of IMBRUVICA in patients with baseline hepatic impairment.

See PACKAGE INSERT for PATIENT COUNSELING INFORMATION and Medication Guide.

Dosage and administration

DOSAGE AND ADMINISTRATION:
560 mg taken orally once daily (four 140 mg capsules once daily.

Capsules should be taken orally with a glass of water. Do not open, break, or chew the capsules.

How supplied

DOSAGE FORMS AND STRENGTHS

Capsule: 140 mg

Reference

Package insert data: [Accessed: Jan 2014].

Distributed and Marketed by:
Pharmacyclics, Inc.
Sunnyvale, CA USA 94085
and
Marketed by:
Janssen Biotech, Inc.
Horsham, PA USA 19044

Patent https://www.imbruvica.com
IMBRUVICA™ is a trademark owned by Pharmacyclics, Inc.

DRUG UPDATES
Drug: IMBRUVICA ® (ibrutinib) capsules, for oral use
[Drug information / PDF]
Dosing: Click (+) next to Dosage and Administration section (drug info link)

Initial U.S. Approval: 2013

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates. A local search option of this data can be found here.