Science

Unleashing Our innovative Targeted Therapeutics Redefines Cancer Treatment

Our science delves deep, uncovering potential solutions for challenging cancers that others may overlook.

What unites and inspires our team is the desire to profoundly impact the quality of life for patients. We focus on a wide range of serious cancers that currently have limited or no treatment options. By utilizing advanced technologies and innovative approaches to drug discovery, delivery, and development, our aim is to introduce potentially life-transforming therapies that address the most urgent unmet needs of patients.

Our Development Team

Our team leads the development of innovative cancer treatments. We have created a first-in-class small molecule BAK activator that selectively induces cancer cell death, leading to significant tumor suppression in vivo while sparing normal tissues. Our work also involves pioneering ComBYSelect-Based bispecific antibodies, which target different tumor-associated antigens with high specificity, functionality, and sustainability.

By utilizing bispecific antibodies and the potent BAK activator 7PB-100 as a payload, our goal is to improve treatment effectiveness and reduce off-tumor and off-target toxicities, creating innovative and precise cancer treatments for the benefits of patients.

Targeted Cancer Therapeutic using BAK Activation

CombYSelect Platform Creating IgG Heterodimers

CombYSelect-based bispecific antibody and bispecific antibody-drug conjugate

Have questions or want to know more about our ground breaking targeted cancer therapeutics? Feel free to reach out to our dedicated team.

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Targeted Cancer Therapeutic using BAK Activation

BAK, a pro-apoptotic effector, plays a crucial role in causing cancer cell death. When activated by apoptotic signals, it forms oligomers, leading to MOMP (Mitochondrial Outer Membrane Permeabilization) and the release of cytochrome c, resulting in cell death. Increased expression of BAK is linked to a poor prognosis in NSCLC, making it a potentially attractive target for NSCLC.

7PB-100 is the a first-in-class BAK activator that selectively binds to the BH3 region of the BAK molecule, promoting oligomerization, mitochondrial priming, and inducing apoptosis. In multiple lung cancer model, including SCLC and NSCLC xenografts, patient-derved xenografts, and a genetically engineered mouse model of mutant KRAS-driven cancer, it effectively suppressed tumor growth without harming normal tissues, further more, it has revered acquired radio-resistance to ionizing radiation in lung cancer xenografts. 7PB-100 also showed strong synergy with the Bcl-2 inhibitor venetoclax in suppressing tumor growth in lung cancer xenografts.

CombYSelect Platform Creating IgG Heterodimers

The CombYSelect (Combinatorial Tyrosine (Y)/Serine (S) Selection) is a computational AI approach that uses AlphaFold and RoseTTAFold to determine the change in binding free energy (ΔΔG) of protein interfaces with a highly restricted library of tyrosine and serine. This AI approach identified CombYSelect 1 and 2 mutation sets in the CH3 region of the IgG1 molecule, capable of creating a near optimal IgG heterodimer, while reducing homodimer formation, significantly.

We focus on tyrosine and serine residues in the interface based on experimental evidence that high-affinity Fabs from phage display libraries with antibody CDR loops contain only serine and tyrosine residues. Tyrosine’s chemical diversity allows for polar contacts and hydrophobic π interactions, while serine’s flexibility allows for the formation of contacts with a variety of residues and additional hydrogen bonding potential. The x-ray crystal structures of the CombYSelect heterodimers demonstrate the flexibility of a Tyr/Ser-populated interface.

Overall, the CombYSelect-based mutation sets can be used to redesign the interface between the CH3 domains of the IgG1 Fc molecules to form functional heterodimeric IgG Fc regions for bispecific antibodies.

CombYSelect-based bispecific antibody and bispecific antibody-drug conjugate

1.Bispecific antibodies

Bispecific antibodies offer improved clinical efficacy and safety compared to combinations of two monoclonal antibodies. To functionally evaluate the CombYSelect platform, one of the Fabs of the bispecific antibody is replaced with a heavy chain-only nanobody (anti-CD20 Fab + HER2 nanobody) to avoid unnecessary heavy chain and light chain mismatches, confirming binding specificities to dual tumor-associated antigens. The engineered cytokine trap (IL-1RI + IL-1RAcP) also successfully traps IL-1β.


Our CombYSelect platform is highly effective in designing IgG-like bispecific antibodies, which retain long serum half-lives due to their physiological binding to FcRn. The resulting IgG-like bispecific antibodies closely resemble the functionality, stability, and long half-life of a monoclonal antibody while retaining the advantages of dual-antigen specificity. This platform can also be applied to other isotypes of IgG, such as IgA or IgE, considering their conformations and homodimer interfaces of the Fcs of other isotypes are similar to those of IgG Fcs.

2. Bispecific Antibody-Drug Conjugate

Bispecific antibody-drug conjugates (BADCs) represent the next generation of targeted therapies, combining bispecific antibodies with potent anti-cancer small molecule payloads. However, many ADCs face limitations due to the unintended release of cytotoxic payloads before reaching their intended targets, leading to severe side effects. Our bispecific ADC overcomes these limitations by using the BAK activator, 7PB-100, as a payload capable of inducing apoptosis in cancer cells with high BAK expression, along with bispecific antibodies that recognize dual tumor-associated antigens, thereby enhancing specificity and therapeutic impact on cancer cells while sparing normal cells with little or no BAK expression.


Key advantages include:

  1. Lower Toxicity:
    7PB-100 is expected to have lower toxicity than other conventional cytotoxic agents, inducing apoptosis in cancer cells with high BAK expression while sparing normal cells with little or no BAK expression.
  2. Selective Tumor-Associated Antigen Recognition:
    The bispecific antibody can recognize two tumor-associated antigens on the cell surface, delivering the payload specifically to cancer cells and enhancing the treatment’s impact.
  3. Versatile Targeting:
    By combining various tumor-associated antigens, it can be applied to many types of cancer.
  4. Overcoming Antigen Escape from Tumor:
    The dual antigen targeting enables it to overcome epitope escape from tumors, ensuring the sustained efficacy of the treatment.
  5. Bystander Effect:
    The bystander effect is expected to impact nearby cancer cells and enhance the overall effectiveness of the treatment.