The BeOne Pipeline

Zanubrutinib 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, zanubrutinib has been demonstrated to inhibit the proliferation of malignant B cells in a number of hematologic malignancies.

*Approved in at least one major market, such as the USA, EU, China and/or Japan.

Tislelizumab is a uniquely designed humanized immunoglobulin G4 (IgG4) anti-programmed cell death protein 1 (PD-1) monoclonal antibody with high affinity and binding specificity against PD-1. It is designed to minimize binding to Fc-gamma (Fcγ) receptors on macrophages, helping the body’s immune cells detect and fight tumors.

*Approved in at least one major market, such as the USA, EU, China and/or Japan.

Sonrotoclax is designed to block the B-cell lymphoma 2 (BCL2) protein, which helps cancer cells survive. It is part of a group of drugs called BH3 mimetics, which mimic natural cell death signals.

Studies during early drug development have shown that sonrotoclax is a potent and specific inhibitor of BCL2 with a short half-life and no accumulation. Sonrotoclax has shown promising clinical activity across a range of B-cell malignancies.

Tarlatamab is a first-in-class immunotherapy engineered by Amgen researchers that binds to both DLL3 on tumor cells and CD3 on T cells, activating T cells to kill DLL3-expressing SCLC cells. This results in the formation of a cytolytic synapse with lysis of the cancer cell.^2,3

DLL3 is a protein that is expressed on the surface of SCLC cells in ~85-94% of patients with SCLC, but is minimally expressed on healthy cells, making it an exciting target.^4,5

Zanidatamab is an investigational HER2-targeted bispecific antibody that can simultaneously bind two non-overlapping epitopes of the HER2 receptor, known as biparatopic binding. This unique design and increased binding results in multiple mechanisms of action, including dual HER2 signal blockade, removal of HER2 protein from the cell surface, and immune-mediated cytotoxicity leading to encouraging antitumor activity in patients.

Zanidatamab is being studied in multiple clinical trials as a targeted treatment option for patients with solid tumors that express HER2. Zanidatamab is being developed by Jazz and BeOne Medicines, Ltd. under license agreements from Zymeworks, which first developed the molecule.

BGB‑16673 is an orally available, brain-penetrating Bruton’s tyrosine kinase (BTK) targeting chimeric degradation activation compound (CDAC) 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.

Blinatumomab is a BiTE® (bi-specific T-cell engager) immuno-oncology therapy that targets CD19 surface antigens on B cells. BiTE molecules fight cancer by helping the body’s immune system detect and target malignant cells by engaging T cells (a type of white blood cell capable of killing other cells perceived as threats) to cancer cells. By bringing T cells near cancer cells, the T cells can inject toxins and trigger cancer cell death (apoptosis).

BiTE immuno-oncology therapies are currently being investigated for their potential to treat a wide variety of cancers.

BG-68501 is a highly potent and selective cyclin-dependent kinase (CDK) 2 inhibitor that targets elevated CDK2 activity, which is a key resistance mechanism to commonly used CDK4/6 inhibition treatments in HR+/HER2- breast cancer.

BGB-43395 is a next-generation molecule designed to inhibit CDK4, which is a cyclin-dependent kinase that drives cancer cell growth. By selectively inhibiting CDK4, BGB-43395 can potentially slow cancer cell growth while reducing other toxicities, including GI toxicity and neutropenia.

Antibody drug conjugates (ADCs) combine antibodies with cancer drugs to deliver treatment directly to cancer cells. They are designed to maximize efficacy while minimizing damage to other tissues.

BG-C9074 targets B7-H4 (B7 – homolog 4) which is found in high amounts on many cancer cells but is rare in normal, healthy cells. It helps tumors grow and hide from the immune system, making the cancer harder to fight.

Kirsten Rat Sarcoma (KRAS) is a signaling protein that regulates cell processes like growth and division. KRAS mutations occur in about 19% of all tumor types and can be a significant contributor to tumor growth.^9,10,11

BGB-53038 is designed to target mutated KRAS proteins to inhibit tumor growth. It has shown broad activity against KRAS mutations in multiple tumor types in preclinical models and may limit toxicity by sparing other RAS proteins.

Antibody drug conjugates (ADCs) combine antibodies with cancer drugs to deliver treatment directly to cancer cells. They are designed to maximize efficacy while minimizing damage to other tissues.

BGB-C354 targets carcinoembryonic antigen (CEA), which is highly expressed on many types of cancer cells but has limited presence on normal, healthy tissues. CEA is a protein that plays a role in cell adhesion, meaning it helps cells stick together. In many cancers, CEA is overproduced contributing to tumor growth and spread.

BG-89894 targets solid tumors that have a mutation called MTAP deletion, which is estimated to be present in approximately 15% of all cancer types with the most common including glioblastoma, pancreatic cancer and non-small cell lung cancer.

BGB-58067 is designed to block the activity of an enzyme called PRMT5 (Protein Arginine Methyltransferase 5), which some cancer cells rely on for survival.

Cancer tumors become dependent on PRMT5 because they are missing a key gene called MTAP (Methylthioadenosine Phosphorylase), which normally helps cells manage important building blocks for metabolism. Since normal cells still have MTAP, they don’t rely on PRMT5 as much. This makes PRMT5 a good target for cancer treatment—the cancer cells that depend on it die, while normal cells can survive.

Antibody drug conjugates (ADCs) combine antibodies with cancer drugs to deliver treatment directly to cancer cells. They are designed to maximize efficacy while minimizing damage to other tissues.

BG-C137 targets Fibroblast Growth Factor Receptor 2b (FGFR2b), which plays a key role in cell growth, repair and development. In some cancers, FGFR2b becomes overactive, leading to uncontrolled tumor growth.

BG-60366 is a Chimeric Degradation Activation Compound (CDAC), a type of degrader, that targets Epidermal Growth Factor Receptor (EGFR), a protein that helps cancer cells grow and spread.

Some cancers have too much EGFR, making them more aggressive. Unlike traditional drugs that block EGFR, a degrader completely eliminates it, which may be more effective in stopping cancer and overcoming drug resistance.

HPK1 is a key negative feedback regulator of T-cell receptor signaling, which is believed to play a key role in antitumor immune response. In preclinical studies, the inhibition of HPK1 enhanced T-cell activation, which is expected to enhance the anti-tumor activity of anti-PD-1 inhibitors such as BeOne’s tislelizumab.

Antibody drug conjugates (ADCs) combine antibodies with cancer drugs to deliver treatment directly to cancer cells. They are designed to maximize efficacy while minimizing damage to other tissues.

BGB-C354 targets B7-H3 (B7 – homolog 3) which is a protein belonging to the B7 family of immune checkpoint molecules. These molecules help regulate the immune system, particularly how immune cells respond to threats like infections or cancer.

In cancer, B7-H3 can suppress the immune system’s ability to attack tumors, making it a promising target for new cancer treatments. B7-H3 is found in high amounts on many types of cancer cells but is present in much lower levels on normal, healthy cells.

Xaluritamig is an experimental cancer drug that helps the immune system target and destroy prostate cancer cells by linking T-cells (immune fighters) to cancer cells displaying the STEAP1 protein.¹³ This connection activates T-cells to attack and kill the cancer cells.¹⁴ It is currently being studied in clinical trials for its effectiveness in treating advanced prostate cancer.