Ibrutinib
Generic Name: ibrutinib
Brand Names:
Imbruvica
11 DESCRIPTION Ibrutinib is a kinase inhibitor. It is a white to off-white solid with the empirical formula C 25 H 24 N 6 O 2 and a molecular weight 440.50. Ibrutinib is freely soluble in dimethyl sulfoxide, soluble in methanol and practically insoluble in water.
Overview
11 DESCRIPTION Ibrutinib is a kinase inhibitor. It is a white to off-white solid with the empirical formula C 25 H 24 N 6 O 2 and a molecular weight 440.50. Ibrutinib is freely soluble in dimethyl sulfoxide, soluble in methanol and practically insoluble in water.
Uses
1 INDICATIONS AND USAGE IMBRUVICA is a kinase inhibitor indicated for the treatment of: Adult patients with chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) ( 1.1 ). Adult patients with chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) with 17p deletion ( 1.2 ). Adult patients with Waldenström’s macroglobulinemia (WM) ( 1.3 ). Adult and pediatric patients age 1 year and older with chronic graft versus host disease (cGVHD) after failure of one or more lines of systemic therapy ( 1.4 ). 1.1 Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma IMBRUVICA is indicated for the treatment of adult patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL). 1.
Dosage
2 DOSAGE AND ADMINISTRATION CLL/SLL and WM : 420 mg taken orally once daily ( 2.1 ). cGVHD : ◦ Patients 12 years and older: 420 mg taken orally once daily ( 2.1 ). ◦ Patients 1 to less than 12 years of age: 240 mg/m 2 taken orally once daily (up to a dose of 420 mg) ( 2.1 ). Tablets or capsules should be taken orally with a glass of water. Do not open, break, or chew the capsules. Do not cut, crush, or chew the tablets. See full prescribing information for oral suspension administration instructions ( 2.1 ). 2.1 Recommended Dosage Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma and Waldenström’s Macroglobulinemia The recommended dosage of IMBRUVICA for CLL/SLL and WM is 420 mg orally once daily until disease progression or unacceptable toxicity.
Side Effects
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Hemorrhage [see Warnings and Precautions ( 5.1 )] Infections [see Warnings and Precautions ( 5.2 )] Cardiac Arrhythmias, Cardiac Failure, and Sudden Death [see Warnings and Precautions ( 5.3 )] Hypertension [see Warnings and Precautions ( 5.4 )] Cytopenias [see Warnings and Precautions ( 5.5 )] Second Primary Malignancies [see Warnings and Precautions ( 5.6 )] Hepatotoxicity, including DILI [see Warning s and Precautions ( 5.7 )] Tumor Lysis Syndrome [see Warnings and Precautions ( 5.8 )] The most common (≥30%) adverse reactions in patients with B-cell malignancies are thrombocytopenia, diarrhea, fatigue, musculoskeletal pain, neutropenia, rash, anemia, bruising, and nausea (...
Interactions
7 DRUG INTERACTIONS CYP3A Inhibitors: Modify IMBRUVICA dose as described ( 2.3 , 7.1 ). CYP3A Inducers: Avoid coadministration with strong CYP3A inducers ( 7.2 ). 7.1 Effect of CYP3A Inhibitors on Ibrutinib The coadministration of IMBRUVICA with a strong or moderate CYP3A inhibitor may increase ibrutinib plasma concentrations [see Clinical Pharmacology ( 12.3 )] . Increased ibrutinib concentrations may increase the risk of drug-related toxicity. Dose modifications of IMBRUVICA are recommended when used concomitantly with posaconazole, voriconazole and moderate CYP3A inhibitors [see Dosage and Administration ( 2.3 )]. Avoid concomitant use of other strong CYP3A inhibitors.
Warnings
5 WARNINGS AND PRECAUTIONS Hemorrhage : Monitor for bleeding and manage ( 5.1 ). Infections : Monitor patients for fever and infections, evaluate promptly, and treat ( 5.2 ). Cardiac Arrhythmias , Cardiac Failure , and Sudden Death : Monitor for symptoms of arrhythmias and cardiac failure and manage ( 5.3 ). Hypertension : Monitor blood pressure and treat ( 5.4 ). Cytopenias : Check complete blood counts monthly ( 5.5 ). Second Primary Malignancies : Other malignancies have occurred in patients, including skin cancers, and other carcinomas ( 5.6 ). Hepatotoxicity, Including Drug- Induced Liver Injury : Monitor hepatic function throughout treatment ( 5.7 ). Tumor Lysis Syndrome (TLS) : Assess baseline risk and take precautions. Monitor and treat for TLS ( 5.8 ). 4 CONTRAINDICATIONS None None ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary IMBRUVICA can cause fetal harm based on findings from animal studies. There are no available data on IMBRUVICA use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage. In animal reproduction studies, administration of ibrutinib to pregnant rats and rabbits during the period of organogenesis at exposures up to 3-20 times the clinical dose of 420 mg daily produced embryofetal toxicity including structural abnormalities (see Data) . Advise pregnant women of the potential risk to a fetus.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING Capsules The 70 mg capsules are supplied as yellow opaque capsules, marked with “ibr 70 mg” in black ink, in white HDPE bottles with a child-resistant closure: 28 capsules per bottle: NDC 57962-070-28 The 140 mg capsules are supplied as white opaque capsules, marked with “ibr 140 mg” in black ink, in white HDPE bottles with a child-resistant closure: 90 capsule...
Frequently Asked Questions
What is Ibrutinib used for?▼
1 INDICATIONS AND USAGE IMBRUVICA is a kinase inhibitor indicated for the treatment of: Adult patients with chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) ( 1.1 ). Adult patients with chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) with 17p deletion ( 1.2 ). Adult patients with Waldenström’s macroglobulinemia (WM) ( 1.3 ). Adult and pediatric patients age 1 year and older with chronic graft versus host disease (cGVHD) after failure of one or more lines of systemic therapy ( 1.4 ). 1.1 Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma IMBRUVICA is indicated for the treatment of adult patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL). 1.
What are the side effects of Ibrutinib?▼
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Hemorrhage [see Warnings and Precautions ( 5.1 )] Infections [see Warnings and Precautions ( 5.2 )] Cardiac Arrhythmias, Cardiac Failure, and Sudden Death [see Warnings and Precautions ( 5.3 )] Hypertension [see Warnings and Precautions ( 5.4 )] Cytopenias [see Warnings and Precautions ( 5.5 )] Second Primary Malignancies [see Warnings and Precautions ( 5.6 )] Hepatotoxicity, including DILI [see Warning s and Precautions ( 5.7 )] Tumor Lysis Syndrome [see Warnings and Precautions ( 5.8 )] The most common (≥30%) adverse reactions in patients with B-cell malignancies are thrombocytopenia, diarrhea, fatigue, musculoskeletal pain, neutropenia, rash, anemia, bruising, and nausea (...
Can I take Ibrutinib during pregnancy?▼
8.1 Pregnancy Risk Summary IMBRUVICA can cause fetal harm based on findings from animal studies. There are no available data on IMBRUVICA use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage. In animal reproduction studies, administration of ibrutinib to pregnant rats and rabbits during the period of organogenesis at exposures up to 3-20 times the clinical dose of 420 mg daily produced embryofetal toxicity including structural abnormalities (see Data) . Advise pregnant women of the potential risk to a fetus.
What are the important warnings for Ibrutinib?▼
5 WARNINGS AND PRECAUTIONS Hemorrhage : Monitor for bleeding and manage ( 5.1 ). Infections : Monitor patients for fever and infections, evaluate promptly, and treat ( 5.2 ). Cardiac Arrhythmias , Cardiac Failure , and Sudden Death : Monitor for symptoms of arrhythmias and cardiac failure and manage ( 5.3 ). Hypertension : Monitor blood pressure and treat ( 5.4 ). Cytopenias : Check complete blood counts monthly ( 5.5 ). Second Primary Malignancies : Other malignancies have occurred in patients, including skin cancers, and other carcinomas ( 5.6 ). Hepatotoxicity, Including Drug- Induced Liver Injury : Monitor hepatic function throughout treatment ( 5.7 ). Tumor Lysis Syndrome (TLS) : Assess baseline risk and take precautions. Monitor and treat for TLS ( 5.8 ). 4 CONTRAINDICATIONS None None ( 4 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.