Radiotherapeutics: Delivering Targeted Radiation to Tumor

Cancer treatment has progressed dramatically over the years, yet many patients still face a difficult turning point when the disease spreads or stops responding to standard therapies. A new wave of innovation in radiopharmaceuticals is starting to unlock new possibilities within this landscape. These medicines take the power of radiation and guide it directly to cancer cells with a level of accuracy that traditional radiation therapy cannot match. For many patients, this means a treatment that is more focused on the tumor and gentler on the body.

What Are Radiopharmaceuticals?

Radiopharmaceuticals work by pairing a radioactive particle with a molecule that recognizes specific markers on cancer cells. Once the drug is administered, it travels through the bloodstream, finds those markers, and delivers radiation right where it is needed most. This internal approach spares the surrounding healthy tissue and is especially useful for cancers that have spread to distant parts of the body[1].

A radiopharmaceutical contains two main components:

• A radioactive isotope that provides the energy needed to destroy cancer cells.
• A targeting molecule that attaches to cancer-specific proteins or receptors.

Together, they act like a guided treatment. The targeting molecule homes in on the tumor, and the radioactive component emits radiation that disrupts the cancer cells’ DNA, leading to tumor shrinkage over time[1].

Understanding Alpha and Beta Emitters

Radiopharmaceuticals are grouped based on the type of radiation they release. Each works differently and is chosen based on the cancer’s size, location, and behavior.

Alpha Emitters

Alpha particles are tiny yet heavy particles made of the same building blocks as the center of a helium atom, which carry a high level of energy but travel only a very short distance, often through only a small stack of cells. This makes their effect extremely powerful and highly localized, but it also means alpha emitters can only kill the cells they are delivered to. Alpha emitters like Actinium 225 and Radium 223 are especially useful for:

• Tiny clusters of cancer cells;
• Micrometastatic disease;
• Tumors that have become resistant to other treatments;

Their short travel distance helps protect nearby healthy tissues.

Beta Emitters

Beta particles are essentially weightless, fast-moving electrons that travel farther in tissues and disperse their energy over a wider area, resulting in a gentler, less concentrated effect on each individual cell. This makes beta emitters like Lutetium 177 and Yttrium 90 suitable for:

• Larger tumor deposits;
• Widespread disease in bones or lymph nodes;
• Cancers that require broader area coverage;

Although they may affect some nearby tissue, they are still significantly more precise than external radiation.

Where Radiopharmaceuticals Are Used Today

These therapies are already improving outcomes in several cancers:

Prostate cancer
Lutetium 177 PSMA and Radium 223 help men with advanced or metastatic prostate cancer by reducing pain, improving mobility, and slowing disease progression.

Thyroid cancer
Iodine 131 remains a trusted and effective treatment for differentiated thyroid cancers.

Neuroendocrine tumors
Lutetium 177 dotatate (Lutathera) has become a major advancement for patients with advanced neuroendocrine tumors, helping control disease for longer periods.

Lymphomas and blood cancers
Radio-immunotherapy using Iodine 131 or Yttrium 90 targets cancerous B cells with remarkable precision.

These treatments are often used when other therapies are no longer effective, giving patients new options when they are most needed[3].

How Doctors Select Patients

Not every tumor will respond to a radiopharmaceutical. The cancer must express the molecular target that the drug is designed to bind to. Oncologists use special imaging scans to confirm this. These scans show exactly where the radiopharmaceutical binds, helping predict how well the therapy will work.

Other factors that guide eligibility include:

• Stage and extent of the disease;
• Bone marrow and kidney health;
• Previous treatments;
• Rate of disease progression.

This careful assessment ensures that patients receive the treatment that best fits their individual cancer biology[1].

Why These Treatments Matter

Radiopharmaceuticals offer many meaningful advantages:

• They focus on cancer cells while limiting harm to healthy tissues.
• They involve fewer severe side effects than many traditional treatments.
• They can improve mobility and quality of life in advanced disease

For patients, this often translates to more time, more comfort, and more control during their treatment journey.

The next generation of radiopharmaceuticals could extend this approach to many more cancers and offer treatment options where none exist today.

At Helix BioPharma, we are exploring how these advances can be applied to some of the most difficult solid tumors. Our discovery-stage radiopharmaceutical program for pancreatic cancer uses a targeted approach that pairs a radioisotope with targeting molecules designed to guide it directly to CEACAM6-expressing cancer cells. This work builds on our long-standing expertise in CEACAM6 biology and represents an example of how we continue to innovate from strength, by combining the long-established power of nuclear medicine with advanced targeting moieties to deliver radiation precisely to hard-to-treat tumors. It’s a natural evolution of our science and a step toward more precise, adaptable therapies for malignancies that have seen little therapeutic progress for years.

References:

1. Khalaji A, Rostampour M, Riahi F, Rafieezadeh D, Dormiani Tabatabaei SA, Fesharaki S, Tooyserkani SH. The use of radiopharmaceuticals in targeted cancer therapy: a narrative review. Int J Physiol Pathophysiol Pharmacol. 2025 Apr 25;17(2):37-44. doi: 10.62347/LQYR3145. PMID: 40401116; PMCID: PMC12089840.

2. Ferreira CA, Potluri HK, Mahmoudian M, Massey CF, Grudzinski JJ, Carston AM, Clemons NB, Idrissou MB, Thickens AS, Rosenkrans ZT, Choi C, Kerr CP, Pinchuk AN, Kwon O, Jeffery JJ, Bednarz BP, Morris ZS, Weichert JP, McNeel DG, Hernandez R. Immunomodulatory effects of alpha vs beta radiopharmaceutical therapy in murine prostate cancer. Front Immunol. 2025 May 22;16:1563387. doi: 10.3389/fimmu.2025.1563387. PMID: 40475779; PMCID: PMC12137342.

3. https://www.mayoclinic.org/tests-procedures/radiopharmaceutic/about/pac-20587480

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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Tumor Defense Breaker™, L-DOS47


L‑DOS47 is a first‑in‑class, clinical-stage antibody‑enzyme conjugate designed to deliver a game-changing assist to anti-cancer immunity and today’s leading cancer immunotherapies for the treatment of prevalent, hard-to-treat solid tumors. The compound precisely targets CEACAM6, a cell-surface protein overexpressed in non‑small cell lung cancer (NSCLC) and other aggressive tumors, where it delivers an enzymatic payload that raises the extracellular pH of the acidic tumor microenvironment (TME). By neutralizing tumor acidity, L-DOS47 restores immune cell infiltration and activity, helps turn immunologically “cold” tumors “hot”, and enhances the therapeutic reach of immune checkpoint inhibitors. With patented composition-of-matter coverage through 2036 and demonstrated synergy with PD-1 inhibitor, pembrolizumab, L-DOS47 is poised to significantly increase the efficacy of immune checkpoint blockade and unlock broader and more durable responses in NSCLC and other aggressive solid tumors.

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LEUMUNA™


LEUMUNA™ is an oral immune checkpoint modulator designed to activate the donor immune system to recognize and fight relapsing leukemia in patients who have undergone allogeneic stem cell transplantation (allo-SCT). Although a life-saving procedure, up to 30% of patients who undergo allo-SCT see their cancer return, facing a median survival of just four months. LEUMUNA aims to offer these patients a new lease on life, by activating an immune cascade and inciting graft-versus-leukemia (GvL) effect, potentially offering long-term remission. Backed by strong preclinical data and a promising safety record from trials with its precursor compound, ulodesine, LEUMUNA offers a patient‑friendly, oral approach to a difficult-to-treat condition, with patent protection through 2041 and an Orphan Drug Designation granted by the US FDA.

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GEMCEDA™


GEMCEDA is a first-in-class oral prodrug of gemcitabine that opens up the possibility for convenient at-home administration, metronomic dosing and seamless integration into combination regimens with immune checkpoint inhibitors. To date, gemcitabine is only administered intravenously because oral forms have shown poor bioavailability of about 10%. GEMCEDA was developed as a prodrug to enable new uses of gemcitabine by combining it with cedazuridine, an enzyme inhibitor that helps boost its bioavailability to 90%. This remarkable innovation allows for greater flexibility in dosing schedules, fewer clinic visits, and a better quality of life, while achieving bioavailability on par with intravenous gemcitabine. Supported by a well‑established safety profile, scalable manufacturing, and patent coverage to 2043, GEMCEDA reimagines how chemotherapy can fit into patients’ lives.

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