BeiGene’s BTKi is approved in more than 65 markets globally

BASEL, Switzerland & BEIJING & CAMBRIDGE, Mass.--(BUSINESS WIRE)--$BGNE #BTKi--BeiGene, Ltd. (NASDAQ: BGNE; HKEX: 06160; SSE: 688235), a global biotechnology company, announced today that BRUKINSA (zanubrutinib), a Bruton's tyrosine kinase inhibitor (BTKi), has been approved by Health Canada for the treatment of adult patients with chronic lymphocytic leukemia (CLL).

“BRUKINSA now has four approved indications in Canada, demonstrating our commitment to bring this innovative BTKi treatment option to more patients across the world,” said Mehrdad Mobasher, M.D., M.P.H., Chief Medical Officer, Hematology at BeiGene. “Our bold development program for BRUKINSA in CLL provided evidence for superior efficacy in the first-line and relapsed/refractory treatment settings, positioning BRUKINSA to become the BTKi of choice.”

Typically diagnosed among individuals in their early 70s, CLL is a slow-growing, incurable blood cancer and is the most common leukemia in adults.¹

“Because CLL is a chronic disease with many patients often living with multiple health conditions, access to effective treatment options with safe and favorable tolerability profiles is critical,” says Dr. Christine Chen, MMEd, MD, FRCPC, Clinician Investigator, Princess Margaret Cancer Centre. “That is why the approval of zanubrutinib is seen as a clinical home run - not only did it demonstrate a significant clinical benefit in the first line CLL setting but it delivered superior efficacy versus ibrutinib in patients with relapsed or refractory disease and did so with less toxicity. And because most CLL patients are ultimately treated on and off for years, zanubrutinib may represent a safer and more effective option for patients with CLL.”

The Health Canada approval of BRUKINSA for CLL is based on positive efficacy results and a favorable safety profile from two global Phase 3, randomized, open-label, multicenter clinical trials: SEQUOIA (NCT03336333), comparing zanubrutinib against bendamustine plus rituximab (BR) in patients with previously untreated CLL, and ALPINE (NCT03734016), comparing zanubrutinib against ibrutinib in patients with relapsed or refractory (R/R) CLL.²

Considered the largest head-to-head study of BTK inhibitors in R/R CLL, the final ALPINE trial data were presented in a late-breaking session at the 64th American Society of Hematology Annual Meeting in December 2022 and simultaneously reported in The New England Journal of Medicine.^3,4 SEQUOIA trial results were published in The Lancet Oncology in August 2022.⁵

“CLL Canada applauds continued innovation when it comes to addressing the needs of Canadians who live with CLL. The approval of zanubrutinib represents a significant advance for patients who can benefit from an additional treatment option,” says Raymond Vles, Board Chair, CLL Canada. “More importantly, becoming informed and connecting with the CLL patient community will enable people with CLL to discuss with their doctor the treatment and dosing options that will work best for them and their lifestyle.”

About CLL²

CLL is a type of blood cancer. Over 2,200 people in Canada are diagnosed with CLL each year. CLL is more common in men and occurs mainly in people over 60, with the average age of diagnosis in the early 70s.

About BRUKINSA (zanubrutinib)

BRUKINSA is a small-molecule inhibitor of Bruton’s tyrosine kinase discovered by BeiGene scientists that is currently being evaluated globally in a broad clinical program as a monotherapy and in combination with other therapies to treat various B-cell malignancies. BRUKINSA was specifically designed to deliver targeted and sustained inhibition of the BTK protein by optimizing bioavailability, half-life, and selectivity. With differentiated pharmacokinetics compared to other approved BTK inhibitors, BRUKINSA has been demonstrated to inhibit the proliferation of malignant B cells within a number of disease-relevant tissues.

BRUKINSA is supported by a broad clinical program which includes more than 4,900 subjects in 35 trials across 29 markets. To date, BRUKINSA is approved in more than 65 markets around the world, including the United States, China, the European Union, Great Britain, Canada, Australia, South Korea, and Switzerland.

About BeiGene

BeiGene is a global biotechnology company that is discovering and developing innovative oncology treatments that are more affordable and accessible to cancer patients worldwide. With a broad portfolio, we are expediting development of our diverse pipeline of novel therapeutics through our internal capabilities and collaborations. We are committed to radically improving access to medicines for far more patients who need them. Our growing global team of more than 9,400 colleagues spans five continents, with administrative offices in Basel; Beijing; and Cambridge, U.S. To learn more about BeiGene, please visit www.beigene.com and follow us on Twitter at @BeiGeneGlobal.

Forward-Looking Statements

This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995 and other federal securities laws, including statements regarding the potential for BRUKINSA to provide clinical benefit to patients with CLL and to become the BTKi of choice; the potential for BRUKINSA to be a safer and more effective treatment option for patients; the future development, regulatory filing and approval, commercialization, and market access of BRUKINSA; and BeiGene’s plans, commitments, aspirations, and goals under the heading “About BeiGene.” Actual results may differ materially from those indicated in the forward-looking statements as a result of various important factors, including BeiGene's ability to demonstrate the efficacy and safety of its drug candidates; the clinical results for its drug candidates, which may not support further development or marketing approval; actions of regulatory agencies, which may affect the initiation, timing, and progress of clinical trials and marketing approval; BeiGene's ability to achieve commercial success for its marketed medicines and drug candidates, if approved; BeiGene's ability to obtain and maintain protection of intellectual property for its medicines and technology; BeiGene's reliance on third parties to conduct drug development, manufacturing, and other services; BeiGene’s limited experience in obtaining regulatory approvals and commercializing pharmaceutical products and its ability to obtain additional funding for operations and to complete the development and commercialization of its drug candidates and achieve and maintain profitability; and the impact of the COVID-19 pandemic on BeiGene’s clinical development, regulatory, commercial, manufacturing, and other operations, as well as those risks more fully discussed in the section entitled “Risk Factors” in BeiGene’s most recent quarterly report on Form 10-Q, as well as discussions of potential risks, uncertainties, and other important factors in BeiGene's subsequent filings with the U.S. Securities and Exchange Commission. All information in this press release is as of the date of this press release, and BeiGene undertakes no duty to update such information unless required by law.

IMPORTANT U.S. SAFETY INFORMATION

Warnings and Precautions

Hemorrhage

Fatal and serious hemorrhage has occurred in patients with hematological malignancies treated with BRUKINSA monotherapy. Grade 3 or higher hemorrhage, including intracranial and gastrointestinal hemorrhage, hematuria and hemothorax have been reported in 3.6% of patients treated with BRUKINSA monotherapy in clinical trials, with fatalities occurring in 0.3% of patients. Bleeding of any grade, excluding purpura and petechiae, occurred in 30% of patients.

Bleeding has occurred in patients with and without concomitant antiplatelet or anticoagulation therapy. Coadministration of BRUKINSA with antiplatelet or anticoagulant medications may further increase the risk of hemorrhage.

Monitor for signs and symptoms of bleeding. Discontinue BRUKINSA if intracranial hemorrhage of any grade occurs. Consider the benefit-risk of withholding BRUKINSA for 3-7 days pre- and post-surgery depending upon the type of surgery and the risk of bleeding.

Infections

Fatal and serious infections (including bacterial, viral, or fungal infections) and opportunistic infections have occurred in patients with hematological malignancies treated with BRUKINSA monotherapy. Grade 3 or higher infections occurred in 24% of patients, most commonly pneumonia (11%), with fatal infections occurring in 2.9% of patients. Infections due to hepatitis B virus (HBV) reactivation have occurred.

Consider prophylaxis for herpes simplex virus, pneumocystis jiroveci pneumonia, and other infections according to standard of care in patients who are at increased risk for infections. Monitor and evaluate patients for fever or other signs and symptoms of infection and treat appropriately.

Cytopenias

Grade 3 or 4 cytopenias, including neutropenia (22%), thrombocytopenia (8%) and anemia (7%) based on laboratory measurements, developed in patients treated with BRUKINSA monotherapy. Grade 4 neutropenia occurred in 11% of patients, and Grade 4 thrombocytopenia occurred in 2.8% of patients.

Monitor complete blood counts regularly during treatment and interrupt treatment, reduce the dose, or discontinue treatment as warranted. Treat using growth factor or transfusions, as needed.

Second Primary Malignancies

Second primary malignancies, including non-skin carcinoma, have occurred in 13% of patients treated with BRUKINSA monotherapy. The most frequent second primary malignancy was non-melanoma skin cancer reported in 7% of patients. Other second primary malignancies included malignant solid tumors (5%), melanoma (1.2%), and hematologic malignancies (0.5%). Advise patients to use sun protection and monitor patients for the development of second primary malignancies.

Cardiac Arrhythmias

Serious cardiac arrhythmias have occurred in patients treated with BRUKINSA. Atrial fibrillation and atrial flutter were reported in 3.7% of 1550 patients treated with BRUKINSA monotherapy, including Grade 3 or higher cases in 1.7% of patients. Patients with cardiac risk factors, hypertension and acute infections may be at increased risk. Grade 3 or higher ventricular arrhythmias were reported in 0.2% of patients.

Monitor for signs and symptoms for cardiac arrhythmias (e.g. palpitations, dizziness, syncope, dyspnea, chest discomfort), manage appropriately, and consider the risks and benefits of continued BRUKINSA treatment.

Embryo-Fetal Toxicity

Based on findings in animals, BRUKINSA can cause fetal harm when administered to a pregnant woman. Administration of zanubrutinib to pregnant rats during the period of organogenesis caused embryo-fetal toxicity, including malformations at exposures that were 5 times higher than those reported in patients at the recommended dose of 160 mg twice daily. Advise women to avoid becoming pregnant while taking BRUKINSA and for 1 week after the last dose. Advise men to avoid fathering a child during treatment and for 1 week after the last dose. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to a fetus.

Adverse Reactions

The most common adverse reactions (≥30%), including laboratory abnormalities, included decreased neutrophil count (42%), upper respiratory tract infection (39%), decreased platelet count (34%), hemorrhage (30%), and musculoskeletal pain (30%).

Drug Interactions

CYP3A Inhibitors: When BRUKINSA is co-administered with a strong CYP3A inhibitor, reduce BRUKINSA dose to 80 mg once daily. For coadministration with a moderate CYP3A inhibitor, reduce BRUKINSA dose to 80 mg twice daily.

CYP3A Inducers: Avoid coadministration with strong or moderate CYP3A inducers. Dose adjustment may be recommended with moderate CYP3A inducers.

Specific Populations

Lactation: Advise not to breastfeed.

Hepatic Impairment: The recommended dose of BRUKINSA for patients with severe hepatic impairment is 80 mg orally twice daily.

U.S. INDICATIONS

BRUKINSA is indicated for the treatment of adult patients with:

• Waldenström’s macroglobulinemia (WM).
• Mantle cell lymphoma (MCL) who have received at least one prior therapy.
• Relapsed or refractory marginal zone lymphoma (MZL) who have received at least one anti-CD20-based regimen.
• Chronic lymphocytic leukemia (CLL) or small lymphocytic leukemia (SLL).

The MCL and MZL indications are approved under accelerated approval based on overall response rate. Continued approval for these indications may be contingent upon verification and description of clinical benefit in confirmatory trials.

For more information on BRUKINSA in Canada

Please consult the BRUKINSA Product Monograph. The Product Monograph is also available by calling 1-877-828-5598.

References

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¹Lymphoma Canada www.lymphoma.ca/lymphoma/cll-sll/about-cll-sll/ 

²BRUKINSA (zanubrutinib) Canada Product Monograph. May 23, 2023. Available at: https://pdf.hres.ca/dpd_pm/00070886.PDF
³ Brown JR, Eichhorst, B, Hillmen, P., et al. (2022) Zanubrutinib or Ibrutinib in Relapsed/Refractory Chronic Lymphocytic Leukemia. New England Journal of Medicine. Doi:10.1056/NEJMoa2211582

⁴ Brown JR, Eichhorst, B. Hillmen P, et al.; Zanubrutinib Demonstrates Superior Progression-Free Survival (PFS) Compared with Ibrutinib for Treatment of Relapsed/Refractory Chronic Lymphocytic Leukemia and Small Lymphocytic Lymphoma (r/R CLL/SLL): Results from Final Analysis of ALPINE Randomized Phase 3 Study. Blood.2022: 140(Supplement 2): LBA-6.doi.1182/blood-2022-171538.

⁵ Tam CS, Brown JR, Kahl BS, et al. (2022). Zanubrutinib versus bendamustine and rituximab in untreated chronic lymphocytic leukaemia and small lymphocytic lymphoma (SEQUOIA): a randomised, controlled, phase 3 trial. The Lancet Oncology, 23(8), 1031-1043. DOI: https://doi.org/10.1016/S1470-2045(22)00293-5.

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