Study evaluating BRUKINSA^® in combination with venetoclax in high-risk, treatment-naïve CLL/SLL patients to be shared as oral presentation

BCL2 inhibitor sonrotoclax subject of multiple presentations highlighting promising safety and efficacy as monotherapy and in combinations, including with backbone therapy BRUKINSA

Phase 1/2 results for BTK degrader BGB-16673 showcasing encouraging efficacy and tolerability, including in BTK inhibitor resistant disease

SAN MATEO, Calif.--(BUSINESS WIRE)-- BeiGene, Ltd. (NASDAQ: BGNE; HKEX: 06160; SSE: 688235), a global oncology company, today announced it will share new data from its hematology portfolio and pipeline at the European Hematology Association 2024 Hybrid Congress (EHA2024) in Madrid, Spain, June 13-16, 2024. BeiGene has 28 abstracts accepted at EHA2024, with four scheduled for oral presentations.

“As part of our dedication to bringing high-quality therapies to patients around the world, our presentations at EHA2024 underscore our continued commitment to expanding our hematology portfolio and our efforts to build on the success of BRUKINSA’s unique clinical profile across multiple B-cell malignancies,” said Mehrdad Mobasher, M.D., M.P.H., Chief Medical Officer, Hematology at BeiGene. “The data highlight the potential of our differentiated investigational BCL2 inhibitor, sonrotoclax, as a monotherapy and in combination regimens, and the promise of BTK degradation to address the unmet needs of patients facing certain blood cancers.”

New Data Expand Evidence Base for BRUKINSA (zanubrutinib)

• Oral presentation of new data from an arm of the SEQUOIA study in patients with high-risk treatment-naïve (TN) chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) with del(17p) and/or TP53 mutation treated with BRUKINSA and venetoclax, demonstrating strong efficacy and favorable safety (Abstract S160)
• Oral presentation sharing the results of an adverse event (AE) based economic analysis comparing BRUKINSA with acalabrutinib; in terms of AE management, BRUKINSA was cost-saving and associated with quality of life benefits compared to acalabrutinib (Abstract S333)
• Presentation of a post hoc analysis evaluating the risk of developing hypertension among ALPINE trial participants with relapsed or refractory (R/R) CLL/SLL, which demonstrated patients in the ibrutinib arm initiated new and/or a new class of anti-hypertensive medications more frequently than patients in the BRUKINSA arm (Abstract P1836)
• Results of an intra-patient comparative analysis from ROSEWOOD study of BRUKINSA plus obinutuzumab in patients with R/R follicular lymphoma (FL), supporting the efficacy benefit of the combination in this patient population (Abstract P1143)
• Multiple additional presentations featuring patient-reported outcomes and real-world differentiation of BRUKINSA among BTK inhibitors

Emerging Data Demonstrate Hematology Pipeline Strengths

• Oral presentation of a Phase 1 study of BeiGene’s novel BCL2 inhibitor sonrotoclax (BGB-11417) in combination with BRUKINSA, demonstrating deep and durable responses with a tolerable safety profile in patients with R/R CLL/SLL; the combination of sonrotoclax with backbone therapy BRUKINSA is being evaluated in the randomized Phase 3 CELESTIAL study (NCT06073821) in patients with TN CLL (Abstract S156)
• Poster presentation of Phase 1a/1b open-label dose escalation and expansion study of sonrotoclax in combination with BRUKINSA in R/R mantle cell lymphoma (MCL), showing the combination was generally well tolerated and demonstrated promising efficacy, including high rate of deep and durable responses (Abstract P1112)
• Additional presentations highlighting Phase 1 results for sonrotoclax, demonstrating encouraging response rates, durable responses and manageable safety profiles spanning multiple indications across B-cell and myeloid malignancies, including:
  • As monotherapy in R/R Waldenström's macroglobulinemia (Abstract P1110)
  • In combination with azacitidine in both TN and R/R acute myeloid leukemia (Abstracts P538 and P562)
  • In combination with dexamethasone in R/R multiple myeloma harboring t(11;14) (Abstract P898)
• Oral presentation of data from the ongoing, first-in-human Phase 1/2 study of BeiGene’s Bruton tyrosine kinase (BTK) degrader BGB-16673, highlighting tolerable safety and promising efficacy in heavily pretreated patients with R/R CLL/SLL (NCT05006716); BGB-16673, which induces BTK degradation, is the first investigational drug from BeiGene’s chimeric degradation activation compound (CDAC) platform (Abstract S157)
• Additional data from the Phase 1/2 study of BTK CDAC BGB-16673, demonstrating a tolerable safety profile and preliminary efficacy in heavily pretreated patients with different types of non-Hodgkin lymphoma, including those with BTKi-resistant disease (Abstract P1119)

BeiGene Presentations During EHA2024

About BRUKINSA^® (zanubrutinib)

BRUKINSA is a small molecule inhibitor of Bruton’s tyrosine kinase (BTK) designed to deliver complete and sustained inhibition of the BTK protein by optimizing bioavailability, half-life, and selectivity. With differentiated pharmacokinetics compared with other approved BTK inhibitors, BRUKINSA has been demonstrated to inhibit the proliferation of malignant B cells within a number of disease-relevant tissues.

About Sonrotoclax (BGB-11417)

Sonrotoclax is an investigational small molecule B-cell lymphoma 2 (BCL2) inhibitor. It belongs to a class of BCL2 homology 3 (BH3) mimetics, and preclinical and IND-enabling studies have demonstrated potent activity and high selectivity of sonrotoclax against the antiapoptotic protein BCL2. Sonrotoclax is more potent and selective for BCL2 relative to BCLxL than venetoclax and shows the potential to overcome common BCL2 resistance mutations.

About BGB-16673

BGB-16673 is an orally available Bruton’s tyrosine kinase (BTK) targeting chimeric degradation activation compound (CDAC) designed to induce degradation of wildtype and multiple mutant forms of BTK, including those that commonly confer resistance to BTK inhibitors in patients who experience progressive disease.

U.S. Indications and Important Safety Information for BRUKINSA (zanubrutinib)

INDICATIONS

BRUKINSA is a kinase inhibitor indicated for the treatment of adult patients with:

• Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).
• 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.
• Relapsed or refractory follicular lymphoma (FL), in combination with obinutuzumab, after two or more lines of systemic therapy.

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

IMPORTANT SAFETY INFORMATION

Warnings and Precautions

Hemorrhage

Fatal and serious hemorrhage has occurred in patients with hematological malignancies treated with BRUKINSA. Grade 3 or higher hemorrhage including intracranial and gastrointestinal hemorrhage, hematuria, and hemothorax was reported in 3.8% of patients treated with BRUKINSA in clinical trials, with fatalities occurring in 0.2% of patients. Bleeding of any grade, excluding purpura and petechiae, occurred in 32% 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 before and after 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. Grade 3 or higher infections occurred in 26% of patients, most commonly pneumonia (7.9%), with fatal infections occurring in 3.2% of patients. Infections due to hepatitis B virus (HBV) reactivation have occurred.

Consider prophylaxis for herpes simplex virus, pneumocystis jirovecii 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 (21%), thrombocytopenia (8%) and anemia (8%) based on laboratory measurements, developed in patients treated with BRUKINSA. Grade 4 neutropenia occurred in 10% of patients, and Grade 4 thrombocytopenia occurred in 2.5% 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 14% of patients treated with BRUKINSA. The most frequent second primary malignancy was non-melanoma skin cancers (8%), followed by other solid tumors in 7% of the patients (including melanoma in 1% of patients) and hematologic malignancies (0.7%). 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 4.4% patients treated with BRUKINSA, including Grade 3 or higher cases in 1.9% 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 0.3% of patients.

Monitor for signs and symptoms of 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, in patients who received BRUKINSA (N=1729) are decreased neutrophil count (51%), decreased platelet count (41%), upper respiratory tract infection (38%), hemorrhage (32%), and musculoskeletal pain (31%).

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

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

Please see full U.S. Prescribing Information including U.S. Patient Information.

This information is intended for a global audience. Product indications vary by region.

About BeiGene

BeiGene is a global oncology company that is discovering and developing innovative 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 10,000 colleagues spans five continents. To learn more about BeiGene, please visit www.beigene.com and follow us on LinkedIn, X (formerly known as Twitter), and Facebook.

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 BeiGene’s continued commitment to expanding its hematology portfolio; the promise of BTK degradation to address unmet needs of blood cancer patients; 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, commercialization, and other services; BeiGene’s limited experience in obtaining regulatory approvals and commercializing pharmaceutical products; BeiGene’s ability to obtain additional funding for operations and to complete the development of its drug candidates and achieve and maintain profitability; and 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.

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Investor Contact:
Liza Heapes
+1 857-302-5663
ir@beigene.com

Media Contact:
Kyle Blankenship
+1 667-351-5176
media@beigene.com

Source: BeiGene, Ltd.