Potent and sustained inhibition*
100%, 24-hour inhibition in PBMCs and 94% in lymph nodes when dosed at 320 mg QD1,2
Target tissue exposure at therapeutic concentrations
Reaches and occupies BTK in plasma and lymph nodes1,2
High affinity for BTK
Minimal off-target binding to other tyrosine kinases3
*The clinical significance of 100% inhibition has not been established.
BID=twice a day; BTK=Bruton's tyrosine kinase; PBMCs=peripheral blood mononuclear cells; QD=once a day.
The primary study results did not reach statistical significance in the R/R analysis set (2-sided P=0.12), thus the study did not meet the primary efficacy endpoint.
COHORT 2: VGPR/CR rates in MYD88 WT WM patients†1
†No CRs were observed.
‡Overall median follow-up time was 19.4 months.5
§R/R median follow-up time was 18.8 months.
Adverse Reactions (ARs) in ≥10% of patients with WM in COHORT 11
|System Organ Class||Adverse Reaction||BRUKINSA (N=101)||Ibrutinib (N=98)|
|Grade 3 or Higher
|Grade 3 or Higher
|Blood and lymphatic system disorders||Neutropenia||25||16||12||8|
|Cardiac disorders||Atrial fibrillation||2||0||14||3|
|General disorders and administration site conditions||Fatigue||19||1||15||1|
|Infections and infestations||Upper respiratory tract infection||24||0||29||1|
|Urinary tract infection||10||0||10||2|
|Musculoskeletal and connective tissue disorders||Musculoskeletal pain||30||7||24||0|
|Pain in extremity||11||1||7||0|
|Nervous system disorders||Headache||15||1||11||1|
|Renal and urinary disorders||Hematuria||7||0||10||2|
|Respiratory, thoracic and mediastinal disorders||Dyspnea||14||0||6||0|
|Skin and subcutaneous tissue disorders||Rash||18||0||21||0|
The safety profile for Cohort 2 (patients with MYD88WT) was generally consistent with
COHORT 1: BRUKINSA dose reduction and treatment discontinuation rates (N=101)1
due to ARs¶
due to ARs#
¶The events leading to discontinuation were cardiomegaly, neutropenia, plasma cell myeloma, and subdural hemorrhage (1% each).
#The most common adverse events leading to dose reduction were neutropenia (3%) and diarrhea (2%).
2 Dosing Options1
- Can be taken with or without food. Can be taken with a high-fat meal—BRUKINSA drug concentration (AUC) is not affected
- Advise patients to swallow capsules whole with water—do not open, dissolve, or chew capsules
- BRUKINSA must not be taken with grapefruit juice, grapefruit, and/or Seville oranges
- If a dose of BRUKINSA is missed, it can be taken as soon as possible on the same day with a return to the normal schedule the following day
Treatment with BRUKINSA should continue until disease progression or unacceptable toxicity.
Dose Modification for ≥Grade 3 ARs1
ARs that require dose modification
- Grade 4 neutropenia (lasting more than
10 consecutive days)
- Grade 4 thrombocytopenia (lasting more than
10 consecutive days)
Recommended Dose Modification by Occurrence for ≥Grade 3 ARs
AR=adverse reaction; AUC=area under the plasma drug concentration over time curve; BID=twice a day; BTK=Bruton's tyrosine kinase; CI=confidence interval; CR=complete response; ECOG=Eastern Cooperative Oncology Group; IRC=independent review committee; MR=minor response; PD=progressive disease; PPI=proton pump inhibitor; QD=once a day; R/R=relapsed/refractory; TN=treatment-naïve; VGPR=very good partial response; WM=Waldenström’s macroglobulinemia.
BRUKINSA Ordering Information
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