Bicycle Therapeutics Reveals First Human Imaging Data and Leadership Strategy for Next-Gen Radiopharmaceuticals at EANM 2024

Bicycle Therapeutics plc, a pioneering pharmaceutical firm utilizing its unique bicyclic peptide technology, has unveiled promising human imaging data that suggest MT1-MMP could serve as a novel target for cancer treatment. These findings also highlight the efficacy of Bicycle Radionuclide Conjugates (BRC®) for use in radiopharmaceutical applications. The data were presented at the European Association of Nuclear Medicine (EANM) 2024 Congress in Hamburg, Germany, alongside preclinical evidence showing optimized BRC radioisotope delivery.

CEO Kevin Lee, Ph.D., emphasized that since the company's inception, Bicycle Therapeutics has aimed to leverage its platform to make significant impacts in patient care. The company has developed a diverse pipeline of oncology treatments, including targeted drug conjugates, immuno-oncology agents, and now radiopharmaceuticals. The data presented at EANM underscore the potential of BRCs to deliver various isotopes to new cancer targets, potentially broadening the use of radiopharmaceuticals for both diagnosis and treatment.

Bicycle Therapeutics is focusing on innovative targets and employing a variety of isotopes in its radiopharmaceutical development strategy. The company has chosen tumor antigen EphA2 as its second BRC target and has signed a letter of intent with isotope technology leader Eckert & Ziegler. This agreement aims to supply a range of radioisotopes and develop BRC molecules. By working with industry and academic leaders, Bicycle Therapeutics aims to be at the forefront of next-generation radiopharmaceutical therapies.

Bicycle molecules are well-suited for radioisotope delivery due to their low molecular weight, high selectivity, and affinity for their targets, as well as their rapid systemic clearance. Michael Skynner, Ph.D., Bicycle Therapeutics' chief technology officer, noted that the data presented at EANM demonstrate the platform's capability to identify high-quality binders to key cancer targets. The ability to optimize biodistribution properties, significantly reducing kidney retention while ensuring selective tumor uptake, positions BRCs as a potentially superior approach for targeted radionuclide therapy.

MT1-MMP is being pursued as the initial target for radiopharmaceutical development due to its expression in multiple solid tumors, including non-small cell lung cancer, esophageal cancer, and triple-negative breast cancer. The German Cancer Consortium (DKTK) presented initial human imaging data for a BRC targeting MT1-MMP during an oral session at EANM. The study involved a 65-year-old male with advanced pulmonary adenocarcinoma. Using fluorine-18-labelled FDG-PET/CT imaging followed by MT1-MMP PET/CT imaging, the scans showed tracer uptake in the primary lung tumor, lymph node, and bone metastases, consistent with FDG imaging. The MT1-MMP BRC tracer demonstrated renal excretion with minimal uptake in other organs, showing clear imaging contrast early on.

An e-poster presentation by Bicycle Therapeutics shared preclinical data illustrating the suitability of Bicycle molecules for delivering indium to tumors due to their specific properties, including high tumor uptake and rapid renal elimination. The data also showed optimized biodistribution to maintain high tumor retention while reducing kidney uptake. This builds on existing preclinical data suggesting Bicycle molecules can effectively deliver various radioisotopes like lutetium and lead to tumors.

In summary, the findings presented at EANM validate the potential of MT1-MMP as a novel cancer treatment target, demonstrate the translatability of BRC preclinical data, and highlight the promise of Bicycle molecules for targeted radionuclide therapy.