Ibrutinib
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From MedlinePlus, U.S. National Library of Medicine
Kinase Inhibitor
Dosing in kidney impairment
This label has no separate kidney-impairment dosing section. Check warnings and clinical pharmacology in the full label.
Dosing in liver impairment
Dosage Modifications for Use in Hepatic Impairment Adult Patients with B-cell Malignancies The recommended dosage is 140 mg daily for patients with mild hepatic impairment (Child-Pugh class A). The recommended dosage is 70 mg daily for patients with moderate hepatic impairment (Child-Pugh class B). Avoid the use of IMBRUVICA in patients with severe hepatic impairment (Child-Pugh class C) [see Use in Specific Populations, Clinical Pharmacology].
Patients with cGVHD The recommended dosage is 140 mg daily for patients 12 years of age and older with total bilirubin level >1.5 to 3 x upper limit of normal (ULN) (unless of non-hepatic origin or due to Gilbert’s syndrome). The recommended dosage is 80 mg/m 2 daily for patients 1 to less than 12 years of age with total bilirubin level >1.5 to 3 x ULN (unless of non-hepatic origin or due to Gilbert’s syndrome).
Avoid the use of IMBRUVICA in these patients with total bilirubin level > 3 x ULN (unless of non-hepatic origin or due to Gilbert’s syndrome) [see Use in Specific Populations, Clinical Pharmacology] .
Preparation and administration
| Recommended dose to achieve 240 mg/m2 | ||
| BSA* (m2) Range | Dose (mg) of IMBRUVICA Capsules/Tablets to Administer | Volume (mL) of IMBRUVICA Oral Suspension (70 mg/mL) to Administer |
| > 0.3 to 0.4 | - | 1.2 mL |
| > 0.4 to 0.5 | - | 1.5 mL |
| > 0.5 to 0.6 | - | 1.9 mL |
| > 0.6 to 0.7 | - | 2.2 mL |
| > 0.7 to 0.8 | 210 mg | 2.6 mL |
| > 0.8 to 0.9 | 210 mg | 2.9 mL |
| > 0.9 to 1 | 210 mg | 3.3 mL |
| > 1 to 1.1 | 280 mg | 3.6 mL |
| > 1.1 to 1.2 | 280 mg | 4 mL |
| > 1.2 to 1.3 | 280 mg | 4.3 mL |
| > 1.3 to 1.4 | 350 mg | 4.6 mL |
| > 1.4 to 1.5 | 350 mg | 5 mL |
| > 1.5 to 1.6 | 350 mg | 5.3 mL |
| > 1.6 | 420 mg | 6 mL |
| Recommended dose to achieve 160 mg/m2 | Recommended dose to achieve 80 mg/m2 | |||
| BSA* (m2) Range | Dose (mg) of IMBRUVICA Capsules/Tablets to Administer | Volume (mL) of IMBRUVICA Oral Suspension (70 mg/mL) to Administer | Dose (mg) of IMBRUVICA Capsules/Tablets to Administer | Volume (mL) of IMBRUVICA Oral Suspension (70 mg/mL) to Administer |
| > 0.3 to 0.4 | - | 0.8 mL | - | 0.4 mL |
| > 0.4 to 0.5 | - | 1 mL | - | 0.5 mL |
| > 0.5 to 0.6 | - | 1.3 mL | - | 0.6 mL |
| > 0.6 to 0.7 | - | 1.5 mL | - | 0.7 mL |
| > 0.7 to 0.8 | 140 mg | 1.7 mL | 70 mg | 0.9 mL |
| > 0.8 to 0.9 | 140 mg | 1.9 mL | 70 mg | 1 mL |
| > 0.9 to 1 | 140 mg | 2.2 mL | 70 mg | 1.1 mL |
| > 1 to 1.1 | 140 mg | 2.4 mL | 70 mg | 1.2 mL |
| > 1.1 to 1.2 | 210 mg | 2.6 mL | - | 1.3 mL |
| > 1.2 to 1.3 | 210 mg | 2.9 mL | - | 1.4 mL |
| > 1.3 to 1.4 | 210 mg | 3.1 mL | - | 1.5 mL |
| > 1.4 to 1.5 | 210 mg | 3.3 mL | 140 mg | 1.7 mL |
| > 1.5 to 1.6 | 280 mg | 3.5 mL | 140 mg | 1.8 mL |
| > 1.6 | 280 mg | 4 mL | 140 mg | 2 mL |
Drug interactions
Check ibrutinib against a medication listLabel text (4 paragraphs)
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. Interrupt IMBRUVICA if these inhibitors will be used short-term (such as anti-infectives for seven days or less) [see Dosage and Administration ( 2.3 ) ] .
Avoid grapefruit and Seville oranges during IMBRUVICA treatment, as these contain strong or moderate inhibitors of CYP3A.
7.2 Effect of CYP3A Inducers on Ibrutinib The coadministration of IMBRUVICA with strong CYP3A inducers may decrease ibrutinib concentrations. Avoid coadministration with strong CYP3A inducers [see Clinical Pharmacology ( 12.3 ) ] .
Contraindications
None None ( 4 )
Pregnancy and lactation
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. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data Ibrutinib was administered orally to pregnant rats during the period of organogenesis at doses of 10, 40 and 80 mg/kg/day. Ibrutinib at a dose of 80 mg/kg/day was associated with visceral malformations (heart and major vessels) and increased resorptions and post-implantation loss.
The dose of 80 mg/kg/day in rats is approximately 20 times the exposure in patients with CLL/SLL or WM administered a dose of 420 mg daily. Ibrutinib at doses of 40 mg/kg/day or greater was associated with decreased fetal weights. The dose of 40 mg/kg/day in rats is approximately 8 times the exposure (AUC) in patients administered a dose of 420 mg daily. Ibrutinib was also administered orally to pregnant rabbits during the period of organogenesis at doses of 5, 15, and 45 mg/kg/day.
Ibrutinib at a dose of 15 mg/kg/day or greater was associated with skeletal variations (fused sternebrae) and ibrutinib at a dose of 45 mg/kg/day was associated with increased resorptions and post-implantation loss. The dose of 15 mg/kg/day in rabbits is approximately 2.8 times the exposure in patients with CLL/SLL or WM administered a dose of 420 mg daily.
For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
Price ladder
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