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Fujifilm Validates Novel Peptide-Oligonucleotide Conjugates for Targeted Cancer Cell Delivery

• Fujifilm has successfully validated peptide-oligonucleotide conjugates that selectively target cancer cells, utilizing cyclic peptides from their proprietary library containing trillions of variants.

• The company developed a cyclic peptide that binds strongly to integrins overexpressed on cancer cell surfaces with a low dissociation constant of 1.6 nM, enabling higher cellular uptake compared to non-conjugated oligonucleotides.

• This breakthrough addresses delivery challenges in oligonucleotide-based therapies and will be presented at TIDES USA 2025 in San Diego, highlighting Fujifilm's expansion of global drug discovery services for peptide therapeutics.

FUJIFILM Corporation has successfully validated the cancer cell-targeting potential of its peptide-oligonucleotide conjugates, the company announced on May 19, 2025. The breakthrough combines oligonucleotides with cyclic peptides developed from Fujifilm's proprietary peptide library, which contains trillions of variants. The research findings will be presented at TIDES USA, an exhibition taking place from May 19 to 22, 2025, in San Diego (poster number: 35).

Novel Approach to Targeted Cancer Therapy

Cyclic peptides, including those containing unnatural amino acids, have emerged as a promising new modality in drug discovery. These peptides offer unique advantages including high binding affinity and specificity, improved tissue permeability, and synthetic versatility. The peptide-oligonucleotide conjugation approach specifically addresses delivery challenges that have historically limited oligonucleotide-based therapies by leveraging the excellent delivery properties of peptides.
Dr. Hiroshi Nakamura, Senior Vice President of Fujifilm's Pharmaceutical Research Division, explained, "Oligonucleotide therapeutics have tremendous potential, but their clinical utility has been limited by delivery challenges. Our approach combines the targeting precision of cyclic peptides with the therapeutic potential of oligonucleotides, potentially opening new avenues for cancer treatment."

Breakthrough in Cancer Cell Targeting

Fujifilm's research team has achieved significant progress by leveraging its large peptide library constructed with mRNA display technology and structural optimization techniques. The company has developed a proprietary cyclic peptide that binds strongly to integrins—proteins that are frequently overexpressed on the surface of cancer cells—with a remarkably low dissociation constant (KD) of 1.6 nM, indicating extremely high binding affinity.
Using advanced chemical modification methods, Fujifilm researchers successfully synthesized the peptide-oligonucleotide conjugate at high yield. Laboratory testing demonstrated that the uptake of these peptide-oligonucleotide conjugates by cancer cells is significantly higher compared to the uptake of non-conjugated oligonucleotides. This confirms the conjugate's ability to selectively accumulate in cancer cells, a critical factor for developing effective targeted therapies.

Expanding Global Drug Discovery Services

This breakthrough comes as Fujifilm expands its drug discovery services for peptide therapeutics globally. The company now provides a comprehensive range of contract research services focusing on peptide discovery, high-throughput screening, and structural optimization.
"Our one-stop comprehensive service includes peptide chemical synthesis and target protein expression and purification to meet diverse research demands," said Teiichi Goto, President of FUJIFILM Corporation. "We're committed to driving research and development that fosters technological innovation in the healthcare field."

Future Implications for Cancer Treatment

The successful validation of these peptide-oligonucleotide conjugates represents a significant step forward in addressing one of the major challenges in oligonucleotide therapeutics: targeted delivery to specific cell types. By enabling more precise delivery to cancer cells, this technology could potentially reduce off-target effects while enhancing therapeutic efficacy.
Fujifilm is leveraging the ability of cyclic peptides to regulate cellular functions and their specific molecular recognition capabilities to contribute to the advancement of pharmaceutical development of peptide therapeutics. The company's continued investment in this area underscores the growing importance of peptide-based approaches in modern drug discovery and development.
Industry analysts suggest that this technology could have applications beyond cancer treatment, potentially extending to other diseases where targeted cellular delivery would improve therapeutic outcomes. The presentation at TIDES USA 2025 is expected to generate significant interest from pharmaceutical companies and research institutions working in the oligonucleotide therapeutics space.
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