BRUKINSA (zanubrutinib) is indicated for the treatment of adult patients with Waldenström’s macroglobulinemia (WM).1

1

Potent and sustained inhibition*

100%, 24-hour inhibition in both PBMCs and lymph nodes when dosed at 160 mg BID1,2

100%, 24-hour inhibition in PBMCs and 94% in lymph nodes when dosed at 320 mg QD1,2

2

Target tissue exposure at therapeutic concentrations

Reaches and occupies BTK in plasma and lymph nodes1,2

3

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.

Head-To-Head Study Of Brukinsa vs IBRUTINIB1

The safety and efficacy of BRUKINSA were evaluated in the ASPEN study, a Phase 3, randomized, open-label, multicenter study comparing BRUKINSA and ibrutinib in patients with treatment-naïve (TN) or relapsed/refractory (R/R) MYD88MUT WM.

ASPEN Study Design

The primary endpoint was rate of complete response (CR) or very good partial response (VGPR) in R/R MYD88MUT WM patients, as assessed by IRC.


Evaluated Globally in a Range of Patients

Baseline Patient Characteristics1 Cohort 1 
(n=201)
Cohort 2 
(n=28)
Median age 70 years
(range: 38-90)
72 years
(range: 39-87)
>75 years 28% 43%
Male 67% 50%
Caucasian 91% 96%
ECOG
   0-1
   2

94%
6%

86%
14%
Treatment-naïve (TN) 18% 18%
Relapsed/refractory (R/R) 82% 82%
Median time from initial diagnosis 4.6 years 3.7 years
Median prior therapies 1 (range: 1-8) 1 (range: 1-5)

Patient disposition and demographics of patients in Cohort 1 were generally similar between BRUKINSA and ibrutinib arms except pertaining to percentage of patients >75 years of age (22% on the ibrutinib arm, 33% on the BRUKINSA arm).

Efficacy results based on IRC assessment1

Overall median follow-up time was 19.4 months.5

§R/R median follow-up time was 18.8 months.

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

Treatment-naïve (TN)

20

Relapsed/refractory (R/R)

29

No CRs were observed.

Adverse Reactions (ARs) in ≥10% of patients with WM in COHORT 11

System Organ Class Adverse Reaction BRUKINSA (N=101) Ibrutinib (N=98)
All Grades
(%)
Grade 3 or Higher
(%)
All Grades
(%)
Grade 3 or Higher
(%)
Blood and lymphatic system disorders Neutropenia 25 16 12 8
Anemia 12 5 10 5
Thrombocytopenia 10 6 10 3
Cardiac disorders Atrial fibrillation 2 0 14 3
Gastrointestinal disorders Diarrhea 21 3 32 1
Constipation 16 0 7 0
Nausea 15 0 13 1
Vomiting 9 0 13 1
General disorders and administration site conditions Fatigue 19 1 15 1
Pyrexia 13 2 12 2
Peripheral edema 9 0 19 0
Infections and infestations Upper respiratory tract infection 24 0 29 1
Nasopharyngitis 11 0 7 0
Urinary tract infection 10 0 10 2
Pneumonia 9 3 20 7
Musculoskeletal and connective tissue disorders Musculoskeletal pain 30 7 24 0
Pain in extremity 11 1 7 0
Muscle spasms 10 0 24 1
Nervous system disorders Headache 15 1 11 1
Dizziness 13 0 9 0
Renal and urinary disorders Hematuria 7 0 10 2
Respiratory, thoracic and mediastinal disorders Dyspnea 14 0 6 0
Cough 13 0 17 0
Epistaxis 13 0 19 0
Skin and subcutaneous tissue disorders Rash 18 0 21 0
Bruising 18 0 34 0
Vascular disorders Hemorrhage 21 5 24 4
Hypertension 11 6 16 11

The safety profile for Cohort 2 (patients with MYD88WT) was generally consistent with Cohort 1.

COHORT 1: BRUKINSA dose reduction and treatment discontinuation rates (N=101)1

Discontinuation rate 
due to ARs

4

Dose reduction 
due to ARs#

14

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 Modifications for Grade ≥3 ARs1

ARs that require dose modifications

  • Grade 3 or higher non-hematological toxicities
  • Grade 3 febrile neutropenia
  • Grade 3 thrombocytopenia with significant bleeding
  • Grade 4 neutropenia (lasting more than 10 consecutive days)
  • Grade 4 thrombocytopenia (lasting more than 10 consecutive days)

Recommended Dose Modifications by Occurrence for ≥Grade 3 ARs

NO DOSE EXCHANGE REQUIRED FOR DOSE MODIFICATION

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

Brukinsa is supplied through Innomar Strategies Specialty Wholesale
For product ordering information, please call 1-833-234-4366 
or email [email protected]

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