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Waldenström’s Macroglobulinemia (WM)

BRUKINSA: MAKE A POWERFUL IMPACT IN WALDENSTRÖM'S MACROGLOBULINEMIA

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

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, multicentre 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 
MYD88MUT
(n=201) 		Cohort 2 
MYD88WT
(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% in the ibrutinib arm, 33% in the BRUKINSA arm).
READ
ASPEN STUDY PUBLICATION – COHORT 1
READ ASPEN STUDY PUBLICATION – COHORT 2 SUBSTUDY
READ PHASE 1/2
3-YEAR FOLLOW-UP OF WM PATIENTS

Efficacy results based on IRC assessment1

  • * No CRs were observed.
  • † Overall median follow-up time was 19.4 months.5
  • * No CRs were observed.
  • * No CRs were observed.
  • † 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 patients1*

Treatment-naïve
(TN)

20

(95% CI: 1, 72; n=5)

Relapsed/refractory
(R/R)

29

(95% CI: 11, 52; n=21)

  • * No CRs were observed.
  • BID=twice a day; ECOG=Eastern Cooperative Oncology Group; IRC=independent review committee; MR=minor response; PD=progressive disease; PR=partial response; QD=once a day.

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 Haemorrhage 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 haemorrhage (1% each).
  • †The most common adverse events leading to dose reduction were neutropenia (3%) and diarrhea (2%).

DOSING

ONCE- OR TWICE-DAILY DOSING1

The only BTKi that can be dosed either ONCE or TWICE daily1

Administration1

  • 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 with a return to the normal schedule the following day

BRUKINSA should be taken until disease progression or unacceptable toxicity.

  • AUC=area under the concentration-time curve.

RECOMMENDED DOSE ADJUSTMENTS1

CYP Coadministered drug Recommended dose
Inhibition Strong CYP3A inhibitor (e.g., posaconazole, voriconazole, ketoconazole, itraconazole, clarithromycin, lopinavir, ritonavir, telaprevir) 80 mg once daily
Interrupt dose as recommended for adverse reactions
Moderate CYP3A inhibitor (e.g., erythromycin, ciprofloxacin, diltiazem, dronedarone, fluconazole, verapamil, aprepitant) 80 mg twice daily
Modify dose as recommended for adverse reactions
Induction Strong CYP3A inducer (e.g., carbamazepine, phenytoin, rifampin) Avoid concomitant use; consider alternative agents with less CYP3A induction
Moderate CYP3A inducer (e.g., bosentan, efavirenz, etravirine, modafinil, nafcillin) Avoid concomitant use. If concomitant use cannot be avoided, increase BRUKINSA dose to 320 mg twice daily. Monitor closely for toxicity.

No dose adjustment is recommended in patients with mild to moderate renal or hepatic impairment.

Straightforward Dose Modification for ≥Grade 3 Adverse Reactions (ARs)1

Recommended dose modification for ≥Grade 3 ARs

  • Grade ≥3: non-hematological toxicities
  • Grade 3: febrile neutropenia/thrombocytopenia with significant bleeding
  • Grade 4: neutropenia*/thrombocytopenia*
Starting Dose 1st Occurrence 2nd Occurrence 3rd Occurrence 4th Occurrence
Start at
320 mg†
total dose 		Interrupt BRUKINSA Interrupt BRUKINSA Interrupt BRUKINSA Discontinue
Resume BRUKINSA once toxicity has resolved to
≤Grade 1
or baseline 		Resume BRUKINSA once toxicity has resolved to
≤Grade 1
or baseline 		Resume BRUKINSA once toxicity has resolved to
≤Grade 1
or baseline
No dose reduction.
320 mg†
total dose 		Reduce to
160 mg
total dose 		Reduce to
80 mg
total dose
  • * Lasting >10 consecutive days.
  • † 160 mg BID or 320 mg OD.
  • ARs=adverse reactions; BID=twice a day; OD=once daily.

Pooled treatment-emergent adverse reactions in ≥10% of patients with hematologic malignancies* (N=1,550)6

Treatment-Emergent Adverse Reactions BRUKINSA (N=1,550)
All Grades (%) Grade ≥3 (%)
Upper respiratory tract infection† 37.1 2.2
Bruising† 30.4 0.5
Neutropenia† 27.5 18.5
Haemorrhage/hematoma† 27.4 3.0
Musculoskeletal pain† 27.0 1.8
Rash† 25.0 0.7
Diarrhea 18.8 1.5
Cough† 18.6 0.1
Pneumonia† 17.9 9.4
Fatigue† 16.2 1.2
Thrombocytopenia† 15.9 5.7
Anemia† 14.1 5.2
Hypertension† 13.0 6.5
Constipation 12.3 0.3
Urinary tract infection† 11.6 1.7
Dizziness† 10.7 0.3
  • * Chronic lymphocytic leukemia, small lymphocytic lymphoma, Waldenström’s macroglobulinemia, mantle cell lymphoma, follicular lymphoma, marginal zone lymphoma, hairy cell leukemia, diffuse large B-cell lymphoma, and Richter’s transformation.
  • † Indicates grouped term that includes multiple preferred terms.

Pooled selected treatment-emergent adverse events of special interest in patients with hematologic malignancies* (N=1,550)6

Treatment-emergent adverse events All Grades (%) Grade ≥3 (%)
Arthralgia 12.8 0.3
Myalgia 3.9 0.3
Atrial fibrillation 2.9 0.8
Atrial flutter 0.3 0.0

Of the 1,550 patients treated with BRUKINSA, 3.0% discontinued therapy and 5.2% experienced a dose reduction due to adverse reactions.1

BRUKINSA Ordering Information

BRUKINSA is available to all pharmacies in Canada. If you are a pharmacy looking to purchase BRUKINSA, it is available through the following wholesalers:

Sentrex order desk:
Email: orders@sentrex.com
Fax: 1-833-736-8739
Phone: 1-888-207-4618, Monday through Friday (8AM - 8PM ET).

Innomar order desk:
Email: specialtylogistics@innomar-strategies.com
Phone: 1-866-949-9927, Monday through Friday (8AM - 8PM ET).

 Patient Support

Designed to provide appropriate information and assistance to BRUKINSA patients, including:

Reimbursement/payment support

  • Dedicated case managers to support insurance verification, bridge, and/or co-pay for patients to gain access to BRUKINSA

Education and support

  • Dedicated nurse case managers for practices, patients, and caregivers
  • Helps provide information about their disease and treatment with BRUKINSA
  • Specialty pharmacists who speak to patients with every refill

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:
    • Education and events
    • Support group information

Enroll in myBeiGene

Call myBeiGene (8:00 am to 8:00 pm)

Fax Enrollment Form to 1-833-567-0696

THE BEIGENE SAMPLE PROGRAM

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

Receive a sample in 2 easy steps

  1. Click “Request Sample” below or request a sample form from your Regional Manager.
  2. 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.

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IMPORTANT SAFETY INFORMATION

INDICATIONS AND CLINICAL USE:

BRUKINSA (zanubrutinib) is indicated:

  • for the treatment of adult patients with Waldenström’s macroglobulinemia (WM).
  • for the treatment of adult patients with mantle cell lymphoma (MCL) who have received at least one prior therapy.
  • for the treatment of adult patients with marginal zone lymphoma (MZL) who have received at least one prior anti-CD20-based therapy.
  • for the treatment of adult patients with chronic lymphocytic leukemia (CLL).
  • in combination with obinutuzumab for the treatment of adult patients with relapsed or refractory grade 1, 2, or 3a follicular lymphoma (FL) who have received at least 2 prior systemic therapies.

CONTRAINDICATIONS:

BRUKINSA is contraindicated in patients who are hypersensitive to zanubrutinib or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container.

Most Serious Warnings and Precautions:

OTHER RELEVANT WARNINGS AND PRECAUTIONS:

For more information:

Please consult the BRUKINSA Product Monograph for important information relating to adverse reactions, drug interactions, and dosing information, which have not been discussed in this piece. The Product Monograph is also available by calling 1-877-828-5598.

References: 1. BRUKINSA (zanubrutinib) Product Monograph. January 31, 2024. 2. Tam CS, Trotman J, Opat S, et al. Phase 1 study of the selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL. Blood. 2019;134(11):851-859. 3. Guo Y, Liu Y, Hu N, et al. Discovery of zanubrutinib (BGB-3111), a novel, potent, and selective covalent inhibitor of Bruton’s tyrosine kinase. J Med Chem. 2019;62(17):7923-7940. 4. Treon SP, Tripsas CK, Meid K, et al. Ibrutinib in previously treated Waldenström’s macroglobulinemia. N Engl J Med. 2015;372(15):1430-1440. 5. Tam CS, Opat S, D’Sa S, et al. A randomized phase 3 trial of zanubrutinib vs ibrutinib in symptomatic Waldenstrom macroglobulinemia: the ASPEN study. Blood. 2020;136(18):2038-2050. 6. Data on file. Pooled Safety. BeiGene Canada. April 12, 2023.