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


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.

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 
Cohort 2 
Median age 70 years
(range: 38-90)
72 years
(range: 39-87)
>75 years 28% 43%
Male 67% 50%
Caucasian 91% 96%


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

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)
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


Dose reduction 
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 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 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

BRUKINSA is supplied through Sentrex Health Solutions
For product ordering information, please call 1-833-234-4366 
or email

 Patient Support Dedicated to Helping Patients

A personalized and comprehensive support program designed to help guide and assist patients, caregivers, and practices.

Complete commitment to your patients

The program is staffed with nurses who have prior experience working with oncology patients

Practices and their patients get a dedicated Oncology Nurse Advocate assigned to them

We seek to offer comprehensive patient support, including connecting patients to helpful resources that can address their personal needs

The myBeiGene program is designed to provide appropriate information and assistance to patients, including**:

Reimbursement/payment support

  • Insurance verification support
  • Bridge, co-pay, and free product for certain eligible patients

Education and support

  • Helps provide information about their disease and treatment with BRUKINSA
  • Patient and caregiver follow-up support
  • Dedicated Oncology Nurse Advocates for practices, patients, and caregivers

Connections to third-party advocacy organizations

  • Assists patients and caregivers with practical help through connections to advocacy groups and local/national free resources such as:
    • Counseling services
    • Support group information

Enroll in myBeiGene

Call myBeiGene


Fax Enrollment Form to 1-833-567-0696



BeiGene provides you with samples of BRUKINSA (zanubrutinib) for your patients

Receive a sample in 2 easy steps


Click “Request Sample” below or request a sample form from your Regional Manager.

Complete the form and submit.
Receive the sample(s) in approximately two business days, shipped directly to your office.
Each sample request for BRUKINSA is fulfilled with up to two 120-count bottle(s), each bottle allocated for one patient.
Your BeiGene Regional Manager will provide you with patient materials to accompany the sample(s).
Upon enrollment into the myBeiGene Patient Support Program, a BRUKINSA Patient Starter Kit will be provided.
These are prescription drug samples provided in accordance with Food and Drug Regulations.
It is unlawful to sell, trade, barter, return for credit, utilize to seek reimbursement or bill patients for samples.