A Blueprint to Win with Next-Gen Conjugates

Over the past decade, antibody drug conjugates (ADCs) have emerged as one of the most exciting innovations in cancer therapy. These “guided missiles” of modern oncology combine the precision of antibodies with the power of potent drugs, targeting cancer cells while sparing healthy tissue[1].

But the story doesn’t end there. Researchers are now designing next-generation ADCs and radionuclide drug conjugates (RDCs) that promise to overcome the limitations of current treatments, making them more specific, more durable, and potentially more effective across cancer types that have long resisted therapy.

The Basics: How Traditional ADCS Work

An ADC is made up of three main parts:

• An antibody, which acts as a homing device that recognizes a specific target protein (antigen) on cancer cells.

• A linker, which connects the antibody to the drug.

• A cytotoxic drug (payload), which kills the cancer cell once delivered inside.

The idea is simple but powerful: the antibody identifies and anchors to the cancer cell, the drug is released within it, and the healthy cells nearby are left mostly unharmed[1].

ADCs have already transformed the treatment landscape for cancers like breast cancer (HER2-positive), lymphomas, and lung cancer, with several FDA-approved options now in use. However, cancer’s ability to evolve has presented new challenges, including resistance, antigen loss, and off-target toxicity[2].

This has led scientists to engineer a next generation of ADCs with smarter designs and broader capabilities.

The Rise of Multi-Specific ADCS

Traditional ADCs recognize just one target on the cancer cell surface. But tumors are clever; they can stop producing that single target, or vary it, to escape detection.

That’s where multi-specific ADCs, such as bispecific and trispecific ADCs, come in. These advanced designs can recognize two or even three different targets simultaneously, improving their ability to bind to diverse cancer cells and reducing the risk of resistance.

More than 100 bispecific ADC formats are currently in development. Some combine recognition of surface antigen HER2 and the prolactin receptor, while others target EpCAM and CLDN3. This dual targeting not only boosts tumor selectivity and internalization, but also reduces the chances of harming healthy cells.

Early studies have shown that bispecific ADCs can deliver drugs more efficiently, even in tumors that express low levels of traditional targets. For instance, bispecific ADCS have demonstrated promising activity in EGFR-mutated non-small cell lung cancer (NSCLC), one of the most treatment-resistant cancer types[2].

Beyond Dual Targeting: Trispecific and Multifunctional Antibodies

Trispecific ADCs take this concept further, engaging three antigens at once or combining multiple functions into a single molecule. These can attack tumors from multiple angles, addressing tumor heterogeneity (when different cells within a tumor express different proteins) and overcoming receptor redundancy, where cancer cells switch to alternative growth pathways when one is blocked.

Such approaches mark a step toward personalized therapy, where treatments are tailored to a patient’s unique tumor profile rather than a “one-size-fits-all” target[2].

Improving Stability and Precision

One of the biggest advancements in ADC engineering has been site-specific conjugation-a precise method of attaching the drug to the antibody so that every molecule behaves consistently. This improves stability and reduces unwanted side effects.

Similarly, scientists are designing smarter linkers that control exactly when and where the drug is released. New dual payloads allow two different drugs to be delivered at once, attacking cancer cells through complementary mechanisms. These refinements not only enhance treatment efficacy but also reduce the likelihood of multidrug resistance, a major obstacle in cancer therapy.

Beyond ADCs: The Promise of Radionuclide Drug Conjugates (RDCs)

While ADCs deliver chemical drugs, radionuclide drug conjugates (RDCs) use a different kind of weapon: radiation.

RDCs link a targeting molecule (often an antibody or peptide) with a radioactive isotope, delivering highly focused radiation directly to tumor cells[3].

This approach has dual benefits:

1. Therapeutic use, to kill cancer cells with minimal damage to healthy tissue.

2. Diagnostic use, through imaging techniques like PET scans that track the drug’s distribution in the body.

So far, RDCs are showing particular promise in prostate cancer, where novel PSMA-targeting ligands have improved tumor uptake and retention, leading to encouraging clinical results[3].

However, balancing effective tumor targeting with minimal radiation exposure to healthy organs remains a challenge. Researchers are now using Al and machine learning to fine-tune dosage, predict therapy responses, and customize treatments for individual patients.

Building the Future of Cancer Treatment

To stay ahead, researchers and companies are focusing on five key strategies:

• Multi-specific targeting to outsmart tumor adaptation.

• Innovative payload and linker designs to enhance selectivity.

• Expansion into new conjugate types such as peptide- or degrader-based therapies.

• Al-driven analytics to personalize and optimize treatments.

• Strong regulatory and manufacturing partnerships to ensure quality and scalability[4].

A Step Toward Smarter, More Personalized Cancer Care

As science moves forward, next-generation conjugates represent more than just an evolution in drug design, they symbolize a shift in cancer care philosophy.

By combining precision targeting, controlled delivery, and advanced data-driven design, next-generation ADCs and RDCs have the potential to transform the treatment of cancers that were once considered incurable.

At Helix BioPharma, we are deeply committed to this vision. Our research focuses on developing innovative conjugate technologies that not only enhance treatment precision but also improve patient quality of life. For us, the goal is clear: to create therapies that are not just more powerful, but also smarter, safer, and more personalized, bringing renewed hope to patients where few options once existed.

References

1. Long R, Zuo H, Tang G, Zhang C, Yue X, Yang J, et al. Antibody-drug conjugates in cancer therapy: applications and future advances. Front Immunol [Internet]. 2025:16:1516419. Available from: http://dx.doi.org/10.3389/fimmu.2025.1516419

2. Gu Y, Wang Z, Wang Y. Bispecific antibody drug conjugates: Making 1+1>2. Acta Pharm Sin B [Internet]. 2024;14(5):1965-86. Available from: http://dx.doi.org/10.1016/j.apsb.2024.01.009

3. Zhang S, Wang X, Gao X, Chen X, Li L, Li G, et al. Radiopharmaceuticals and their applications in medicine. Signal Transduct Target Ther [Internet]. 2025 [cited 2025 Nov 8];10(1):1. Available from: https://www.nature.com/articles/s41392-024-02041-6

4. Zhou M, Huang Z, Ma Z, Chen J, Lin S, Yang X, et al. The next frontier in antibody-drug conjugates: challenges and opportunities in cancer and autoimmune therapy. Canc Drug Resist [Internet]. 2025;8:34. Available from: http://dx.doi.org/10.20517/cdr.2025.49

Jacek Antas

Chief Executive Officer

Jacek Antas is a shareholder of the Company, has spent more than 25 years in the financial services industry holding various positions in sales and consulting.

Mr. Antas obtained a master’s degree from the Warsaw School of Economics and has served as a board member of various
companies throughout his career.

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James B. Murphy

Chief Financial Officer

Mr. Murphy is a certified public accountant with over thirty years of experience in finance and operations management. He is currently a consultant with Danforth Advisors LLC (“Danforth”), a leading provider of outsourced strategic and operational specialists across functions in the life sciences industry. While at Danforth, Mr. Murphy has served over fifteen private and publicly held life sciences companies as CFO and CFO Advisor, helping them secure over USD 0.5 billion in financing and successfully execute pivotal asset transactions. Mr. Murphy functions as a consultant to Helix pursuant to a consulting agreement between the Company and Danforth.

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Thomas Mehrling

Medical Adviser

Thomas Mehrling (PhD in Pharmacology and MD) has over 20 years’ experience in multinational Pharma companies developing novel oncology compounds from preclinical research through to registration. Prior to entering the industry, he spent 13 years as an MD at the University Hospital in Frankfurt, working on preclinical and translational projects. He served as Director of European Oncology at Mundipharma International (2003–2013), building the company’s first European oncology business from the ground up out of Cambridge, UK, and completing the clinical development, registration and launch of two major products in Europe, DepoCyte® and Levact® (Ribomustin® and Treanda®). In 2013, he led the establishment of the Mundipharma Group’s start-up, Mundipharma EDO, developing anti-cancer therapeutics for solid tumours out of Basel, Switzerland.

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Kim Gaspar

Director Quality Assurance

Kim is the Director of Quality Assurance at Helix BioPharma Corp. An experienced quality assurance professional with expertise in Canadian, US, and EU regulations, she has been involved in all aspects of Phase I/II biopharmaceutical product development over the years, including regulatory submissions, QC laboratory compliance, tech transfer and third-party oversight of CMC activities, clinical QA, and bioanalytical data analysis. Kim joined Helix in 2000, transitioning into QA in 2003. She holds a B.Sc in Biochemistry and a Ph.D in Veterinary Physiological Sciences, both from the University of Saskatchewan.

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Brenda Lee

Director Clinical Operations

Brenda is the Clinical Operations Director at Helix Biopharma Corp. A clinical research operations professional with 25 years of experience managing clinical trials, ranging from early Phase I to late Phase IIIb/IV studies, she brings experience in clinical study protocol writing and development, trial start-up and vendor management, and a proven track record in planning and managing clinical trials to quality standards, timelines and budget. Brenda joined Helix Biopharma Corp. in 2018, working to advance the clinical program of L-DOS47. She holds B.Sc and M.Sc. degrees from the University of Toronto, specializing in Nutritional Sciences and Human Biology.

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Jerzy Leszczynski

Director

Jerzy Leszczynski is a shareholder of the Company, has spent more than 35 years developing businesses and has served in the capacity of board member of various real estate development companies. Mr. Leszczynski obtained his Master of Science in Chemistry from the Warsaw Institute of Technology.

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Janusz Grabski

Director, Chair of Audit Committee

Janusz (John) Grabski is a lawyer specialized in corporate and real estate law with over twenty years of experience.

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Malgorzata Laube

Director

Malgorzata Laube has over 19 years of experience in nuclear medicine. In her last role with Alberta Health Services, she was the Department Supervisor, Nuclear Medicine at Royal Alexandra Hospital. Ms. Laube obtained a MSc degree in Environmental Engineering from the Warsaw University of Technology and is based in Edmonton, Alberta, Canada.

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Jacek Antas

Chairman of the Board

Jacek Antas is a shareholder of the Company, has spent more than 25 years in the financial services industry holding various positions in sales and consulting.

Mr. Antas obtained a master’s degree from the Warsaw School of Economics and has served as a board member of various
companies throughout his career.

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Jonathan Davis

Advisor, ADC Discovery

Jonathan Davis received his Ph.D. from University of California, San Francisco, where he studied protein structure and function using NMR. After a post-doc at Harvard Medical School exploring RNA selection and structure in the labs of Jack Szostak and Gerhard Wagner, he went to work at EMD Serono, where his work involved improving antibody-based therapeutics, inventing a platform technology for generating heterodimeric Fcs as a basis for multifunctional molecules, and developing a novel scaffold based on an artificially-designed protein from David Baker’s lab. In 2008 he took a job at Bristol-Myers Squibb in Waltham/Cambridge MA, working on antibody discovery and platform development in a wide range of therapeutic areas, with a particular focus on multispecific therapeutics. He moved to Madison, WI in 2019 to take on the role of VP of Innovation and Strategy at Invenra, a biotech focused on bispecific antibodies, and where he is currently head of the Scientific Advisory Board. In early 2024 he left the corporate world to found Creative Antibodies, a consulting firm that helps guide companies to successful antibody discovery and development projects, from mAbs to multispecifics, ADCs, and other formats. Outside of science, Jonathan is a conservatory trained cellist, plays numerous other instruments, and founded the UCSF Orchestra (now Symphony Parnassus) in San Francisco, where he was Music Director for six years.

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Davide Guggi

Advisor, CMC

Davide graduated as a pharmacist and received his PhD in Pharmaceutical Technology and Biotechnology from the University of Vienna. He has over 20 years of experience in the pharmaceutical industry, principally in the field of oncology. At the beginning of his career, Davide led oncology business units and commercial departments at Mundipharma and Gilead across Austria and Eastern Europe. Since over 10 years he has been working as a CMC expert, covering operational and regulatory CMC functions on behalf of over 20 different small- and medium-sized biotech companies across the world. He has served as CMC Director and CSO/CTO for several years, developing both small molecules and biologics (mABs, Fab, ADCs and Radio-immuno-conjugates) from early discovery to NDA/BLA in the US, EU and Canada, with a focus on First-in-Human and Phase I/II studies in oncology indications.

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