Brukinsa 80mg Capsules

Zanubrutinib is a small molecule inhibitor of Bruton's tyrosine kinase (BTK). Zanubrutinib forms a covalent bond with a cysteine residue (Cys-481) in the BTK active site, leading to irreversible inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. BTK plays a crucial role in B-cell development, activation, signaling, and survival. Inhibition of BTK results in the inhibition of B-cell proliferation and survival.

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:

Allergic Reaction: Rash, hives, itching, redness, swelling, blistering, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or speaking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Infection: Fever, chills, severe sore throat, ear or sinus pain, cough, increased or discolored sputum, painful urination, mouth sores, or a wound that won't heal.
Bleeding: Vomiting or coughing up blood, coffee ground-like vomit, blood in the urine, black, red, or tarry stools, gum bleeding, abnormal vaginal bleeding, unexplained bruises or bruises that enlarge, or uncontrollable bleeding.
High Blood Pressure: Severe headache or dizziness, fainting, or changes in vision.
Electrolyte Imbalance: Mood changes, confusion, muscle pain, cramps, or spasms, weakness, shakiness, balance problems, abnormal heartbeat, seizures, loss of appetite, or severe nausea and vomiting.
High Blood Sugar: Confusion, drowsiness, excessive thirst or hunger, frequent urination, flushing, rapid breathing, or fruity-smelling breath.
Neurological Symptoms: Weakness on one side of the body, speech or thinking difficulties, balance problems, drooping on one side of the face, or blurred vision.
Urinary Changes: Increased frequency of urination.
Skin Changes: Changes in mole color or size, skin lumps or growths.
Cardiovascular Symptoms: Chest pain or pressure, rapid or irregular heartbeat.
Dizziness or Fainting: Feeling lightheaded or passing out.
Respiratory Symptoms: Shortness of breath.
Swelling: Swelling in the arms or legs.
Severe Liver Problems: Although rare, severe liver problems can occur, which may be life-threatening. If you experience dark urine, fatigue, decreased appetite, nausea, stomach pain, light-colored stools, vomiting, or yellow skin and eyes, seek medical attention immediately.

Other Possible Side Effects

While many people may not experience side effects or may only have mild ones, it's essential to be aware of the following:

Common Cold Symptoms
Pain: Back, bone, joint, muscle, or neck pain
Fatigue or Weakness
Muscle Spasm
Headache
Gastrointestinal Symptoms: Constipation, diarrhea, vomiting, and nausea are common with this medication. If these symptoms occur, consult your doctor about ways to manage them. If they persist, worsen, or bother you, seek medical attention.

Reporting Side Effects

If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins, that may interact with this medication. Certain medications used to treat HIV, infections, seizures, and other conditions should not be taken with this drug.
* If you are breastfeeding or plan to breastfeed. You should not breastfeed while taking this medication and for 2 weeks after your last dose.

Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to discuss all of your medications, health problems, and concerns with your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your other medications and health conditions.

Remember, do not start, stop, or change the dose of any medication without first consulting your doctor.

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Your doctor may advise you to stop taking this drug before certain surgical procedures, and will provide guidance on when to resume taking it after the surgery or procedure.

Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. High blood pressure is a potential side effect of this medication, so it is crucial to have your blood pressure checked as advised by your doctor.

If you have diabetes (high blood sugar), discuss this with your doctor, as this medication may increase your blood sugar levels. Additionally, this drug may affect the bone marrow's ability to produce essential blood cells, which can lead to bleeding problems, infections, or anemia. If you have concerns, consult your doctor.

You may be more susceptible to infections, some of which can be severe or life-threatening. To minimize this risk, practice good hygiene by washing your hands frequently, and avoid close contact with people who have infections, colds, or flu.

This medication may also increase your risk of bleeding easily. Be cautious and take steps to prevent injury, such as using a soft toothbrush and an electric razor. Although rare, some bleeding problems can be fatal.

If you have a history of hepatitis B or are a carrier of the virus, discuss this with your doctor, as this medication can cause the virus to become active again.

There is a potential increased risk of developing new types of cancer, including skin cancer, while taking this medication. To reduce your risk of skin cancer, limit your exposure to sunlight, sunlamps, and tanning beds, and use protective measures such as sunscreen, clothing, and eyewear.

This medication can harm an unborn baby. A pregnancy test will be conducted before you start taking this drug to confirm that you are not pregnant. If you or your partner may become pregnant, it is essential to use birth control while taking this medication and for one week after the final dose. If you or your partner becomes pregnant, notify your doctor immediately.

• Strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, indinavir, nelfinavir, saquinavir, telithromycin, voriconazole, posaconazole, cobicistat, grapefruit, Seville oranges, starfruit): Avoid co-administration. If co-administration cannot be avoided, reduce zanubrutinib dose to 80 mg once daily.
• Strong CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital, St. John's wort): Avoid co-administration.

• Moderate CYP3A inhibitors (e.g., erythromycin, fluconazole, diltiazem, verapamil, amiodarone, aprepitant, ciprofloxacin, crizotinib, imatinib, propafenone, ranolazine): Reduce zanubrutinib dose to 80 mg twice daily or 160 mg once daily.
• Moderate CYP3A inducers (e.g., bosentan, efavirenz, etravirine, modafinil, nafcillin): Avoid co-administration if possible. If co-administration is necessary, monitor for reduced efficacy.

• Bleeding (e.g., bruising, petechiae, epistaxis, hematuria, melena, hematochezia)
• Infection (e.g., fever, chills, fatigue, cough, dyspnea, pain with urination)
• Cardiac symptoms (e.g., palpitations, dizziness, shortness of breath, chest discomfort)
• Diarrhea
• Rash
• Muscle pain/spasms
• Fatigue
• Nausea/vomiting

Zanubrutinib can cause fetal harm when administered to a pregnant woman. Based on animal studies, it is not recommended for use during pregnancy. Females of reproductive potential should be advised to use effective contraception during treatment and for at least 1 month after the last dose. Males with female partners of reproductive potential should use effective contraception during treatment and for at least 3 months after the last dose.

It is not known if zanubrutinib or its metabolites are excreted in human milk. Due to the potential for serious adverse reactions in a breastfed infant, breastfeeding is not recommended during treatment with Brukinsa and for 2 weeks after the last dose.

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

No specific dose adjustment is required for elderly patients. However, patients aged 65 years and older may have a higher incidence of certain adverse reactions (e.g., atrial fibrillation, pneumonia, secondary primary malignancies) compared to younger patients. Monitor closely for adverse events.

• Zanubrutinib is a highly selective BTK inhibitor, which may contribute to a lower incidence of certain off-target effects (e.g., atrial fibrillation) compared to less selective BTK inhibitors, though cardiac arrhythmias can still occur.
• Patients should be advised to report any signs of bleeding, infection, or cardiac symptoms promptly.
• Prophylaxis for opportunistic infections (e.g., Pneumocystis jirovecii pneumonia) may be considered in patients at high risk, especially those with lymphopenia.
• Discontinuation or dose reduction may be required for management of certain adverse reactions, including cytopenias, infections, and cardiac events.
• Consider holding Brukinsa for at least 3 to 7 days prior to and following minor surgical procedures to minimize bleeding risk, as clinically appropriate.

• Ibrutinib (another BTK inhibitor)
• Acalabrutinib (another BTK inhibitor)
• Pirtobrutinib (non-covalent BTK inhibitor)
• Chemotherapy regimens (e.g., bendamustine + rituximab, R-CHOP for MCL)
• Other targeted therapies (e.g., venetoclax, acalabrutinib for CLL/SLL)
• Immunotherapy (e.g., rituximab-based regimens)

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.