Brukinsa

Last reviewed on RxList: 10/13/2020
Brukinsa Side Effects Center

Medical Editor: John P. Cunha, DO, FACOEP

What Is Brukinsa?

Brukinsa (zanubrutinib) is a kinase inhibitor used to treat adult patients with mantle cell lymphoma (MCL) who have received at least one prior therapy.

What Are Side Effects of Brukinsa?

Common side effects of Brukinsa include:

Dosage for Brukinsa

The recommended dose of Brukinsa is 160 mg orally twice daily or 320 mg orally once daily; swallow whole with water and with or without food.

Brukinsa In Children

Safety and effectiveness of Brukinsa in pediatric patients have not been established.

What Drugs, Substances, or Supplements Interact with Brukinsa?

Brukinsa may interact with other medicines such as:

  • itraconazole,
  • fluconazole,
  • clarithromycin,
  • erythromycin,
  • diltiazem,
  • rifampin,
  • efavirenz,
  • midazolam,
  • omeprazole, and
  • digoxin

Tell your doctor all medications and supplements you use.

Brukinsa During Pregnancy and Breastfeeding

Brukinsa is not recommended for use during pregnancy; it may harm a fetus. Pregnancy testing is recommended for females of reproductive potential prior to initiating Brukinsa therapy. Female patients of reproductive potential are advised to use effective contraception during treatment with Brukinsa and for at least 1 week following the last dose. It is unknown if Brukinsa passes into breast milk. Because of the potential for serious adverse reactions from Brukinsa in a breastfed child, breastfeeding is not recommended during treatment with Brukinsa and for at least two weeks following the last dose.

Additional Information

Our Brukinsa (zanubrutinib) Capsules, for Oral Use Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

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Brukinsa Consumer Information

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Zanubrutinib can cause serious or life-threatening side effects. Call your doctor at once if you have:

  • pounding heartbeats or fluttering in your chest;
  • chest discomfort;
  • a light-headed feeling, like you might pass out;
  • liver problems--right-sided upper stomach pain, vomiting, loss of appetite, yellowing of your skin or eyes, and not feeling well;
  • low platelets in your blood--easy bruising, unusual bleeding, purple or red spots under your skin;
  • low red blood cells--pale skin, weakness, unusual tiredness, feeling light-headed or short of breath, cold hands and feet, fast or irregular heartbeat;
  • low white blood cell counts--fever, mouth sores, skin sores, sore throat, cough, trouble breathing;
  • signs of bleeding inside your body--red or pink urine, bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds, severe headache, vision problems, numbness or weakness on one side, trouble speaking or understanding what is said to you; or
  • signs of infection--fever, chills, redness or swelling, cough with mucus, feeling short of breath.

Your cancer treatments may be delayed or permanently discontinued if you have certain side effects.

Common side effects may include:

  • diarrhea;
  • low platelet or other blood cell counts;
  • easy bruising or bleeding;
  • rash; or
  • cold symptoms such as stuffy nose, sneezing, sore throat or cough.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Brukinsa (Zanubrutini Capsules)

Brukinsa Professional Information

SIDE EFFECTS

The following clinically significant adverse reactions are discussed in more detail in other sections of the labeling:

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

The data in the WARNINGS AND PRECAUTIONS reflect exposure to BRUKINSA as a single agent at 160 mg twice daily in 524 patients in clinical trials BGB-3111-AU-003, BGB-3111-206, BGB-3111-205, BGB-3111-210, and BGB-3111-1002 and to BRUKINSA at 320 mg once daily in 105 patients in trials BGB-3111-AU-003 and BGB-3111-1002. Among 629 patients receiving BRUKINSA, 79% were exposed for 6 months or longer and 61% were exposed for greater than one year.

In this pooled safety population, the most common adverse reactions in > 10% of patients who received BRUKINSA were neutrophil count decreased (53%), platelet count decreased (39%), upper respiratory tract infection (38%), white blood cell count decreased (30%), hemoglobin decreased (29%), rash (25%), bruising (23%), diarrhea (20%), cough (20%), musculoskeletal pain (19%), pneumonia (18%), urinary tract infection (13%), hematuria (12%), fatigue (11%), constipation (11%), and hemorrhage (10%).

Mantle Cell Lymphoma (MCL)

The safety of BRUKINSA was evaluated in 118 patients with MCL who received at least one prior therapy in two single-arm clinical trials, BGB-3111-206 [NCT03206970] and BGB-3111AU-003 [NCT02343120] [see Clinical Studies]. The median age of patients who received BRUKINSA in studies BGB-3111-206 and BGB-3111-AU-003 was 62 years (range: 34 to 86), 75% were male, 75% were Asian, 21% were White, and 94% had an ECOG performance status of 0 to 1. Patients had a median of 2 prior lines of therapy (range: 1 to 4). The BGB-3111-206 trial required a platelet count ≥ 75 x 109/L and an absolute neutrophil count ≥ 1 x 109/L independent of growth factor support, hepatic enzymes ≤ 2.5 x upper limit of normal, total bilirubin ≤ 1.5 x ULN. The BGB-3111-AU-003 trial required a platelet count ≥ 50 x 109/L and an absolute neutrophil count ≥ 1 x 109/L independent of growth factor support, hepatic enzymes ≤ 3 x upper limit of normal, total bilirubin ≤ 1.5 x ULN. Both trials required a CLcr ≥ 30 mL/min. Both trials excluded patients with prior allogeneic hematopoietic stem cell transplant, exposure to a BTK inhibitor, known infection with HIV, and serologic evidence of active hepatitis B or hepatitis C infection and patients requiring strong CYP3A inhibitors or strong CYP3A inducers. Patients received BRUKINSA 160 mg twice daily or 320 mg once daily. Among patients receiving BRUKINSA, 79% were exposed for 6 months or longer and 68% were exposed for greater than one year.

Fatal events within 30 days of the last dose of BRUKINSA occurred in 8 (7%) of 118 patients with MCL. Fatal cases included pneumonia in 2 patients and cerebral hemorrhage in one patient.

Serious adverse reactions were reported in 36 patients (31%). The most frequent serious adverse reactions that occurred were pneumonia (11%), and hemorrhage (5%).

Of the 118 patients with MCL treated with BRUKINSA, 8 (7%) patients discontinued treatment due to adverse reactions in the trials. The most frequent adverse reaction leading to treatment discontinuation was pneumonia (3.4%). One (0.8%) patient experienced an adverse reaction leading to dose reduction (hepatitis B).

Table 3 summarizes the adverse reactions in BGB-3111-206 and BGB-3111-AU-003.

Table 3: Adverse Reactions (≥ 10%) in Patients Receiving BRUKINSA in BGB-3111206 and BGB-3111-AU-003 Trials

Body System Adverse Reaction Percent of Patients (N=118)
All Grades % Grade 3 or Higher %
Blood and lymphatic system disorders Neutropenia and Neutrophil count decreased 38 15
Thrombocytopenia and Platelet count decreased 27 5
Leukopenia and White blood count decreased 25 5
Anemia and Hemoglobin decreased 14 8
Infections and infestations Upper respiratory tract infection 39 0
Pneumonia § 15 10^
Urinary tract infection 11 0.8
Skin and subcutaneous tissue disorders Rash ‖ 36 0
Bruising * 14 0
Gastrointestinal disorders Diarrhea 23 0.8
Constipation 13 0
Vascular disorders Hypertension 12 3.4
Hemorrhage 11 3.4^
Musculoskeletal and connective tissue disorders Musculoskeletal pain 14 3.4
Metabolism and nutrition disorders Hypokalemia 14 1.7
Respiratory, thoracic and mediastinal disorders Cough 12 0
^ Includes fatal adverse reaction
* Bruising includes all related terms containing bruise, bruising, contusion, ecchymosis
Hemorrhage includes all related terms containing hemorrhage, hematoma
Musculoskeletal pain includes musculoskeletal pain, musculoskeletal discomfort, myalgia, back pain, arthralgia, arthritis
§ Pneumonia includes pneumonia, pneumonia fungal, pneumonia cryptococcal, pneumonia streptococcal, atypical pneumonia, lung infection, lower respiratory tract infection, lower respiratory tract infection bacterial, lower respiratory tract infection viral
‖ Rash includes all related terms containing rash
Upper respiratory tract infection includes upper respiratory tract infection, upper respiratory tract infection viral

Other clinically significant adverse reactions that occurred in < 10% of patients with mantle cell lymphoma include major hemorrhage (defined as ≥ Grade 3 hemorrhage or CNS hemorrhage of any grade) (5%), hyperuricemia (6%) and headache (4.2%).

Table 4: Selected Laboratory Abnormalities* (> 20%) in Patients with MCL in Studies BGB-3111-206 and BGB-3111-AU-003

Laboratory Parameter Percent of Patients (N=118)
All Grades (%) Grade 3 or 4 (%)
  Neutrophils decreased 45 20
  Platelets decreased 40 7
  Hemoglobin decreased 27 6
  Lymphocytosis 41 16
Chemistry abnormalities    
  Blood uric acid increased 29 2.6
  ALT increased 28 0.9
  Bilirubin increased 24 0.9
* Based on laboratory measurements.
Asymptomatic lymphocytosis is a known effect of BTK inhibition.

Read the entire FDA prescribing information for Brukinsa (Zanubrutini Capsules)

© Brukinsa Patient Information is supplied by Cerner Multum, Inc. and Brukinsa Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

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