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 (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
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.
‡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: 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 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
or email info@mybeigene.ca
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
THE BEIGENE SAMPLE PROGRAM
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.
It is unlawful to sell, trade, barter, return for credit, utilize to seek reimbursement or bill patients for samples.
