Tacabrutideg (BGB-16673, BTK degrader) showed durable responses in heavily pretreated R/R CLL and BTK inhibitor–naïve patients, signaling potential for earlier lines of treatment

BRUKINSA plus sonrotoclax (ZS) delivered deep, durable responses and high uMRD rates across TN CLL and R/R MCL and CLL, reinforcing its potential as an all-oral, fixed-duration treatment

BeOne Medicines Ltd. (NASDAQ:ONC, HKEX: 06160, SSE: 688235)), a global oncology company, today announced new data from its foundational hematology franchise at the 2026 European Hematology Association (EHA) Congress in Stockholm. Updated results from tacabrutideg (BGB-16673), a potential best-in-class Bruton's tyrosine kinase (BTK) degrader, demonstrated durable responses in pretreated relapsed/refractory (R/R) chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), with early activity also seen in BTK inhibitor–naïve patients. These data are complemented by results from the all-oral combination of BRUKINSA^® (zanubrutinib) plus next-generation BCL2 inhibitor BEQALZI^™ (sonrotoclax; ZS), which continue to demonstrate rapid, deep, durable responses across multiple B-cell malignancies.

Amit Agarwal, M.D., Ph.D., Chief Medical Officer, Hematology, BeOne Medicines, said:

"BTK inhibition has reshaped the treatment of B-cell cancers, and we believe degradation is the next leap forward. At EHA, tacabrutideg is showing durable responses in heavily pretreated CLL, where patients have limited options, with early data suggesting potential in earlier lines of treatment. At the same time, the depth and consistency of responses we're seeing with our ZS combination supports its potential to become the foundation of time-limited therapy, bringing us closer to a future where durable, treatment-free remission is possible. Together, these data reflect our ambition to define the next era of care in B-cell malignancies."

Updated CaDAnCe-101 data show durable responses with tacabrutideg in heavily pretreated R/R CLL/SLL and R/R WM (Oral Presentation: S152; June 14, 11:00 AM-12:15 PM CEST; Poster Presentation: PS2033; June 13, 2026, 6:45-7:45 PM CEST)

The oral presentation, which was selected for inclusion in the EHA Press Program, will highlight data from 67 patients with R/R CLL/SLL treated with tacabrutideg across the different dose levels (50-500 mg), including patients with high-risk disease features (del(17p)/TP53 mutation, unmutated IGHV, complex karyotype, and BTK inhibitor resistance mutations). With a median study follow-up of 25.4 (range, 0.3-40.1) months, the analysis showed:

Overall response rate (ORR): 85.1%
Median time to first response (TTFR): 2.8 months (range, 2.0-19.4)
Median duration of response (DOR): 20.7 months (range, 0-27.6)
24-month progression-free survival (PFS) rate: 53.8% (95% CI, 38.8%-66.6%)
Safety: tacabrutideg was generally well tolerated in this heavily pretreated population with no treatment-related deaths and no new toxicities identified; patients with treatment response had rapid and sustained cytopenia improvement

In patients with R/R Waldenstrom macroglobulinemia (WM), tacabrutideg showed substantial responses in heavily pretreated patients, including those bearing BTK, CXCR4, and TP53 mutations, with major response rate (MRR) of 76.3% and very good partial response (VGPR) of 30.2% and a 15-month PFS rate of 70.4% (95% CI, 52.6-82.5) at a median PFS follow-up of 16.6 months.

Stephan Stilgenbauer, Professor of Medicine and Medical Director of the Comprehensive Cancer Center Ulm (CCCU), Head of the Early Clinical Trials Unit (ECTU), and Head of the Division of CLL Dept. of Internal Medicine III at Ulm University, said:

"Once patients with relapsed or refractory CLL progress after both BTK and BCL2 inhibitors, treatment options become extremely limited. In this study, tacabrutideg, which is designed to degrade BTK rather than inhibit it, achieved durable responses even in patients with high-risk clinical and biological characteristics, such as resistance mutations. These findings suggest a promising new approach for patients who currently have few effective therapies available."

First report of tacabrutideg in BTK inhibitor–naïve patients shows potential for improved efficacy in earlier treatment lines (Poster Presentation: PS1693; June 13, 2026, 6:45-7:45 PM CEST)

In the first clinical evaluation of tacabrutideg in patients who had not previously received a BTK inhibitor (N=54; CLL/SLL, n=29; mantle cell lymphoma [MCL], n=8; marginal zone lymphoma, n=10; Richter transformation, n=2; WM, n=5), tacabrutideg was well tolerated and showed promising and rapid antitumor activity. In 22 evaluable patients with CLL/SLL with median follow-up of 8.2 (range: 0.4-12.8) months, the study shows:

ORR: 86.4% Median TTFR: 2.8 (range, 2.7-5.6) months
At 6 months, none of the patients had progressed
Safety: tacabrutideg was generally well tolerated with no reported opportunistic infections, major hemorrhage or febrile neutropenia

Rapid, deep, and durable responses with ZS reinforce the potential to redefine time-limited treatment across CLL and MCL (Multiple Presentations)

Across multiple presentations at EHA 2026, the all-oral ZS combination demonstrated rapid, deep, and durable responses across both treatment-naïve and relapsed/refractory settings. These data highlight the ability of ZS to drive high rates of undetectable minimal residual disease (uMRD) and sustained disease control regardless of risk factors reinforcing its potential to redefine expectations for fixed-duration, time-limited therapy in B-cell malignancies.

In treatment-naïve CLL (Oral Presentation: S145; June 12, 2026; 5:15-6:30 PM CEST):

ORR: 100%, with complete responses in 59.5% of patients
Best uMRD4 rate: 98.8%
- No patient that achieved uMRD4 reverted to uMRD positivity
Best uMRD in patients with TP53 mutation/del(17p): 92.9% across 2 dose levels
Median time from combination start to uMRD4: 4.5 months
At a median follow-up of 34.1 months, no disease progression events were observed at the recommended Phase 2 dose of 320mg, including patients who electively discontinued therapy

In R/R CLL (Poster Presentation: PS1697; June 13, 2026, 6:45-7:45 PM CEST), at the 320mg (RP2D) of sonrotoclax:

ORR: 100%, with complete responses in 52% of patients
Best uMRD4 rate: 85%
- No patient that achieved uMRD4 reverted to uMRD positivity
36-month PFS: 95.5% (95% CI, 83.2%-98.9%) across all dose cohorts at a median follow-up of 40.6 months (range, 10.2-60.6 months)

In R/R MCL (Poster Presentation: PF933; June 12, 2026, 6:45-7:45 PM CEST), at the 320mg (RP2D) of sonrotoclax:

ORR: 82%, with complete responses in 59% of patients
Median duration of response (DOR): not reached
30-mo DOR: 78.3% (95% CI, 51.3.%-91.4%)

About Tacabrutideg (BGB-16673)

With first-in-class and best-in-class potential, tacabrutideg is a foundational, orally administered Bruton's tyrosine kinase (BTK) degrader. Tacabrutideg is the most advanced BTK degrader in the clinic with 1,200+ patients dosed to date in an extensive global clinical development program. This program includes three randomized Phase 3 trials in R/R CLL, including the head-to-head Phase 3 trial versus pirtobrutinib, which began enrolling in Q4 2025. Originating from BeOne's chimeric degradation activation compound (CDAC) platform, tacabrutideg is designed to promote the degradation, or breakdown, of both wildtype and mutant forms of BTK, including those that commonly result in resistance to BTK inhibitors in patients who experience progressive disease.

The U.S. Food and Drug Administration (FDA) granted Fast Track Designation to tacabrutideg for the treatment of adult patients with relapsed or refractory (R/R) chronic lymphocytic leukemia or small lymphocytic lymphoma (CLL/SLL), and adult patients with R/R mantle cell lymphoma (MCL). Additionally, the European Medicines Agency (EMA) granted tacabrutideg PRIority MEdicines (PRIME) designation for the treatment of patients with Waldenstrom's macroglobulinemia (WM) previously treated with a BTK inhibitor.

About BEQALZI^™ (sonrotoclax)

BEQALZI^™ (bee-KAHL-zee; sonrotoclax) is a foundational, next-generation and potentially best-in-class B-cell lymphoma 2 (BCL2) inhibitor with a unique pharmacokinetic and pharmacodynamic profile. Preclinical and clinical studies in early drug development have shown that sonrotoclax is a highly potent and specific BCL2 inhibitor with a short half-life and no drug accumulation. Sonrotoclax has shown promising clinical activity across a range of B-cell malignancies, including chronic lymphocytic leukemia (CLL), and is in development as a monotherapy and in combination with other therapeutics, including zanubrutinib. To date, more than 2,500 patients have been enrolled across the broad sonrotoclax global development program.

BEQALZI is approved by the U.S. Food and Drug Administration (FDA) and China's National Medical Products Administration for the treatment of adult patients with relapsed or refractory (R/R) mantle cell lymphoma (MCL), after at least two lines of systemic therapy, including a BTK inhibitor. It is also approved in China for adult patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) who have previously received at least one systemic therapy, including a BTK inhibitor.

About BRUKINSA^® (zanubrutinib)

BRUKINSA is an orally available, 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.

With the broadest label globally, BRUKINSA is the foundational BTK inhibitor and is the only BTK inhibitor to demonstrate superiority to another BTK inhibitor in a Phase 3 study. It is also the only BTK inhibitor to provide the flexibility of once or twice daily dosing.

The global BRUKINSA clinical development program includes more than 8,000 patients enrolled in over 30 countries and regions across more than 45 trials. BRUKINSA is approved in 80 markets in at least one indication, and more than 290,000 patients have been treated globally.

Select Important Safety Information for BEQALZI^TM (sonrotoclax)

Serious and sometimes fatal adverse reactions have occurred with BEQALZI, including tumor lysis syndrome (TLS), serious infections, neutropenia, and embryo-fetal toxicity. BEQALZI is contraindicated with strong CYP3A inhibitors at initiation and during the ramp-up phase due to the potential for an increased risk of tumor lysis syndrome.

In the safety population (N=115), tumor lysis syndrome occurred in 7% of patients who followed the recommended dose ramp-up. Serious infections occurred in 14% of patients, and Grade 3 or 4 infections occurred in 17% (fatal: 2.6%), with pneumonia (10%) being the most common Grade 3 or greater infection. Grade 3 or 4 decreases in neutrophils occurred in 18% of patients (Grade 4: 6%), and febrile neutropenia occurred in 1.7% of all patients. The most common adverse reactions (≥15%) were pneumonia (16%) and fatigue (16%). The most common Grade 3–4 laboratory abnormalities (≥15%) were decreases in lymphocytes (29%) and neutrophils (18%).

Please see full Prescribing Information.

Select Important Safety Information for BRUKINSA

Serious adverse reactions, including fatal events, have occurred with BRUKINSA, including hemorrhage, infections, cytopenias, second primary malignancies, cardiac arrhythmias, and hepatotoxicity (including drug-induced liver injury).

In the pooled safety population (N=1729), the most common adverse reactions (≥30%), including laboratory abnormalities, in patients who received BRUKINSA were neutrophil count decreased (51%), platelet count decreased (41%), upper respiratory tract infection (38%), hemorrhage (32%), and musculoskeletal pain (31%).

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

The information provided in this press release is intended for a global audience. Product indications vary by region.

About BeOne

BeOne Medicines is a global oncology company that is discovering and developing innovative treatments for cancer patients worldwide. With a portfolio spanning hematology and solid tumors, BeOne is expediting development of its diverse pipeline of novel therapeutics through its internal capabilities and collaborations. The Company has a growing global team spanning six continents who are driven by scientific excellence and exceptional speed to reach more patients than ever before. To learn more about BeOne, please visit www.beonemedicines.com and follow us on LinkedIn, X, Facebook and Instagram.

Forward-Looking Statement

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 benefits of tacabrutideg and Z+S combination; Z+S combination's potential to become the foundation of time-limited therapy; BeOne's ambition to define the next era of care in B-cell malignancies; clinical development plans of BeOne's product candidates;; and BeOne's plans, commitments, aspirations, and goals under the heading "About BeOne." Actual results may differ materially from those indicated in the forward-looking statements as a result of various important factors, including BeOne'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; BeOne's ability to achieve commercial success for its marketed medicines and drug candidates, if approved; BeOne's ability to obtain and maintain protection of intellectual property for its medicines and technology; BeOne's reliance on third parties to conduct drug development, manufacturing, commercialization, and other services; BeOne'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 of its drug candidates and achieve and maintain profitability; and those risks more fully discussed in the section entitled "Risk Factors" in BeOne's most recent quarterly report on Form 10-Q, as well as discussions of potential risks, uncertainties, and other important factors in BeOne'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 BeOne undertakes no duty to update such information unless required by law.

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