Radiolabeled Antibodies for Cancer Imaging and Therapy

Abstract

Radiolabeled antibodies were studied first for tumor detection by single-photon imaging, but FDG PET stopped these developments. In the meantime, radiolabeled antibodies were shown to be effective in the treatment of lymphoma. Radiolabeling techniques are well established and radiolabeled antibodies are a clinical and commercial reality that deserves further studies to advance their application in earlier phase of the diseases and to test combination and adjuvant therapies including radiolabeled antibodies in hematological diseases. In solid tumors, more resistant to radiations and less accessible to large molecules such as antibodies, clinical efficacy remains limited. However, radiolabeled antibodies used in minimal or small-size metastatic disease have shown promising clinical efficacy. In the adjuvant setting, ongoing clinical trials show impressive increase in survival in otherwise unmanageable tumors. New technologies are being developed over the years: recombinant antibodies and pretargeting approaches have shown potential in increasing the therapeutic index of radiolabeled antibodies. In several cases, clinical trials have confirmed preclinical studies. Finally, new radionuclides, such as lutetium-177, with better physical properties will further improve the safety of radioimmunotherapy. Alpha particle and Auger electron emitters offer the theoretical possibility to kill isolated tumor cells and microscopic clusters of tumor cells, opening the perspective of killing the last tumor cell, which is the ultimate challenge in cancer therapy. Preliminary preclinical and preliminary clinical results confirm the feasibility of this approach.

Radretumab Radioimmunotherapy in Patients with Brain Metastasis: A 124I-L19SIP Dosimetric PET Study

“…43). We have recently reported the development of the fully human radiolabeled antibody product 124 I-L19-SIP, which is ideally suited for immuno-PET imaging and dosimetric calculations before therapeutic intervention with 131 I-L19SIP RIT (33).…”

Biotinylated and Chelated Poly-L-Lysine as Effector for Pretargeting in Cancer Therapy and Imaging

“…Thereby, the therapeutic/diagnostic window could be improved. 3 GBq/µmol was achieved with the largest amount of DOTA attached to the effector when labelling with 213 Kidney uptake was reduced to approximately 1/4 when changing the molecular size of the effector from 14 kDa to 19 kDa. Consequently, the absorbed dose was reduced to 1/5 using the larger effector.…”

“…RIT has shown high potential as an adjuvant treatment in many types of malignancies [1][2][3]. However, a limitation of treatments with radiolabeled antibodies is that they typically require several hours after intravenous (i. v.) injection to localise the tumour cells.…”

Olfactory receptor 51E1 protein as a potential novel tissue biomarker for small intestine neuroendocrine carcinomas

“…These novel findings support OR51E1 as a potential clinical tissue biomarker for a subpopulation of SI-NECs. Indeed, OR51E1 may be developed as a target for novel diagnostics such as immuno-positron-emission tomography (26) and radioimmunotherapy (27) and/or novel potential therapeutics. We also plan to investigate OR51E1 function in both EC cells and SI-NECs in the near future.…”