Raptamer-Drug Conjugates as Molecularly Targeted Cancer Therapeutics 

A. COF-01 as a Validated Target in Patient-Derived Tumors

COF-01 has been identified as upregulated in patient-derived tumor samples from non-small cell lung cancer (NSCLC) and head and neck (H&N) cancer. This discovery was based on DIA-label free quantitative proteomic analysis of a large collection of low passage Patient-derived Xenograft (PDX) models, many of which came from patients who had progressed on standard of care (SoC) therapy. Immunohistochemistry (IHC) validation confirmed COF-01 overexpression, particularly in high unmet medical need populations.

B. Targeted Cancer Therapy: Antibody-Drug Conjugates (ADCs)
Antibody-drug conjugates (ADCs) are a promising class of cancer therapeutics that combine targeted antibodies with potent drug payloads to selectively kill tumor cells. ADCs aim to minimize damage to healthy cells, offering a more targeted treatment approach than traditional chemotherapy. However, developing effective ADCs remains challenging, and new strategies are needed to improve their efficacy and overcome current limitations.

C. Raptamer-Drug Conjugates: A Novel Strategy for COF-01 Targeting
We have developed next-generation ssDNA aptamers, or "Raptamers," using a proprietary bead-based oligonucleotide library technology. These Raptamers exhibit enhanced binding affinity and specificity for tumor antigens like COF-01. Our bead-based selection process is efficient, identifying high-affinity Raptamers in just 1-2 weeks. Raptamer-drug conjugates (RapDCs) using these aptamers have shown promising results in inducing targeted cell death in COF-01-positive cancer cells in vitro.