Zanubrutinib
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Omid Afkhami-Ardakani
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Overview
Zanubrutinib is a Bruton's Tyrosine Kinase (BTK) Inhibitor that is FDA approved for the treatment of Chronic Lymphocytic Leukemia (CLL) or Small Lymphocytic Lymphoma (SLL), Waldenström's Macroglobulinemia (WM), Mantle Cell Lymphoma (MCL), Marginal Zone Lymphoma (MZL), and Follicular Lymphoma (FL) in adults.. Common adverse reactions include Decreased neutrophil count, Upper respiratory tract infection, Decreased platelet count, Hemorrhage, Musculoskeletal pain, Rash, Bruising, Diarrhea, Pneumonia, and Cough..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Recommended Dosage:
160 mg taken orally twice daily; or
320 mg taken orally once daily.
Administration:
Swallow capsules whole with water.
Do not open, break, or chew the capsules.
Can be taken with or without food.
Dose Modifications for Adverse Reactions:
For Grade 3 or greater adverse reactions:
First occurrence: Interrupt treatment. Once toxicity has resolved to Grade 1 or baseline, resume at the same dose.
Second occurrence: Interrupt treatment. Once toxicity has resolved to Grade 1 or baseline, resume at a reduced dose (e.g., 80 mg twice daily).
Third occurrence: Consider discontinuation.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Zanubrutinib in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Zanubrutinib in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding Zanubrutinib FDA-Labeled Indications and Dosage (Pediatric) in the drug label.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Zanubrutinib in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Zanubrutinib in pediatric patients.
Contraindications
Known Hypersensitivity: Zanubrutinib is contraindicated in patients with a known hypersensitivity to zanubrutinib or any of its components.
Warnings
There is limited information regarding Zanubrutinib Warnings' in the drug label.
Adverse Reactions
Clinical Trials Experience
Decreased neutrophil count, Upper respiratory tract infection, Decreased platelet count, Hemorrhage, Musculoskeletal pain, Rash, Bruising, Diarrhea, Pneumonia, and Cough.
Postmarketing Experience
There is limited information regarding Zanubrutinib Postmarketing Experience in the drug label.
Drug Interactions
CYP3A Inhibitors and Inducers: Zanubrutinib is metabolized primarily by CYP3A. Concomitant use with strong or moderate CYP3A inhibitors can increase zanubrutinib exposure, while strong or moderate CYP3A inducers can decrease its exposure. Dose modifications are recommended when co-administering zanubrutinib with these agents.
Anticoagulants and Antiplatelet Agents: Due to the potential increased risk of bleeding, consider the benefit-risk of concomitant use of zanubrutinib with antiplatelet or anticoagulant therapies.
Vaccines: Avoid the use of live attenuated vaccines during treatment with zanubrutinib. The efficacy of vaccines may be reduced when co-administered with zanubrutinib.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Zanubrutinib in women who are pregnant.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Zanubrutinib in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Zanubrutinib during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Zanubrutinib in women who are nursing.
Pediatric Use
There is no FDA guidance on the use of Zanubrutinib in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Zanubrutinib in geriatric settings.
Gender
There is no FDA guidance on the use of Zanubrutinib with respect to specific gender populations.
Race
There is no FDA guidance on the use of Zanubrutinib with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Zanubrutinib in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Zanubrutinib in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Zanubrutinib in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Zanubrutinib in patients who are immunocompromised.
Administration and Monitoring
Administration
Zanubrutinib is administered orally. Swallow the capsules whole with water; do not open, break, or chew them. Zanubrutinib can be taken with or without food.
Monitoring
Regular monitoring is essential to ensure patient safety and treatment efficacy:
Complete Blood Counts (CBC): Monitor regularly to detect cytopenias.
Signs of Infection: Monitor for signs and symptoms of infection and treat promptly.
Cardiac Monitoring: Monitor for symptoms of arrhythmias (e.g., palpitations, dizziness, syncope) and manage appropriately.
Skin Examinations: Advise patients to use sun protection and undergo regular skin examinations due to the risk of second primary malignancies, including skin cancers.
IV Compatibility
There is limited information regarding the compatibility of Zanubrutinib and IV administrations.
Overdosage
There is limited information regarding Zanubrutinib overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Zanubrutinib Pharmacology in the drug label.
Mechanism of Action
Zanubrutinib is a small-molecule inhibitor of Bruton's tyrosine kinase (BTK). By forming a covalent bond with a cysteine residue in the BTK active site, it inhibits BTK activity. This inhibition blocks B-cell receptor signaling, leading to decreased proliferation of malignant B cells.
Structure
There is limited information regarding Zanubrutinib Structure in the drug label.
Pharmacodynamics
There is limited information regarding Zanubrutinib Pharmacodynamics in the drug label.
Pharmacokinetics
Absorption: After oral administration, zanubrutinib is rapidly absorbed, with peak plasma concentrations occurring 2 hours post-dose.
Distribution: The mean volume of distribution at steady state is approximately 601 L.
Metabolism: Zanubrutinib is primarily metabolized by cytochrome P450 enzyme CYP3A.
Elimination: The mean elimination half-life is approximately 2 to 4 hours.
Nonclinical Toxicology
There is limited information regarding Zanubrutinib Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Zanubrutinib Clinical Studies in the drug label.
How Supplied
Zanubrutinib is administered orally. Swallow the capsules whole with water; do not open, break, or chew them. Zanubrutinib can be taken with or without food.
Storage
Store zanubrutinib capsules at room temperature between 20°C to 25°C (68°F to 77°F), with permissible excursions between 15°C to 30°C (59°F to 86°F).
Keep the capsules in their original container to protect from moisture.
Keep out of reach of children.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
Hemorrhage: Inform patients about the potential risk of bleeding and to report any signs of bleeding promptly.
Infections: Advise patients to report any signs or symptoms of infection, such as fever, chills, or sore throat. Second Primary Malignancies: Advise patients to use sun protection and undergo regular skin examinations due to the risk of second primary malignancies, including skin cancers. Cardiac Arrhythmias: Advise patients to report any signs of palpitations, lightheadedness, or fainting.
Administration Instructions: Instruct patients to take zanubrutinib exactly as prescribed, not to open, break, or chew the capsules, and to take missed doses as soon as possible on the same day, returning to the normal schedule the following day. Drug Interactions: Advise patients to inform their healthcare provider of all medications they are taking, including over-the-counter drugs and supplements, due to potential interactions. FDA Access Data
Pregnancy and Lactation: Advise females of reproductive potential to use effective contraception during treatment and for at least one week following the last dose. Advise women not to breastfeed during treatment and for at least two weeks following the last dose.
Precautions with Alcohol
Alcohol-Zanubrutinib interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Zanubrutinib Brand Names in the drug label.
Look-Alike Drug Names
Zanubrutinib is marketed under the brand name Brukinsa.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.