DESIGN, SYNTHESIS, AND PRECLINICAL EVALUATION OF RADIOACTIVE ACIDIC PEPTIDE CONJUGATES FOR THE TREATMENT OF BONE CANCERS

Breast and prostate cancers frequently metastasize to bone, with approximately 50% of patients with advanced breast cancer and 70-80% of those with advanced prostate cancer developing bone metastasis^1-4. Once cancer cells invade osseous tissues, the prognosis for both cancers declines drastically. Despite the severity of the condition, there is currently no cure for bone metastasis, and existing treatments primarily focus on managing skeletal-related events (Skeletal related events) or alleviating bone damage caused by tumor growth. These therapies, however, do not address the underlying tumor burden within the bones, highlighting the critical need for the development of new, targeted therapeutics.

To address this unmet need, our project aimed to design, synthesize, and evaluate novel bone-targeting radiotherapeutic agents that are tailored to treat bone metastasis. These agents were specifically developed to localize to bone lesions and deliver targeted radiation to metastatic tumor cells, thereby potentially improving patient outcomes. We conducted thorough preclinical assessments to evaluate both the therapeutic efficacy and safety profile of these agents, focusing on their ability to selectively target bone tumors while minimizing off-target effects on healthy tissues.

Our findings demonstrate the potential of these bone-targeting radiotherapeutics not only to reduce tumor burden in bone but also to offer a more effective therapeutic approach for managing metastatic cancer. These agents may represent a significant step forward in addressing the poor prognosis associated with bone metastasis in patients with advanced breast and prostate cancers, offering new hope for improved survival and quality of life.