Development of radioimmunoconjugate for diagnosis and management of head-and-neck subclinical cancer and colorectal carcinoma

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Brazilian Journal of Pharmaceutical Sciences
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Scientific innovations in diagnostic methods are important drivers of cancer control and prevention. Noninvasive imaging of the epidermal growth factor receptor (EGFR) in head-and-neck squamous, cell carcinoma and colorectal cancer could be valuable to select patients for EGFR-targeted therapy, as well as to monitor the efficacy and occurrence of resistance to immunotherapy. In order to develop the first Brazilian radioimmunoconjugate for diagnosis, Cetuximab has been conjugated to p-SCN-Bn-DTPA chelator and radiolabeled with Indium-111. The conjugation methodology was optimized using different mAb:DTPA molar ratios, time was then reduced for immunoconjugate preparation, besides the protein recovery’ percentage increased after purification (m = 83.8 ± 0.91 %). The stability of Cetuximab-DTPA at – 20 oC was evaluated for six months, and its integrity was greater than 90% (m =93.9 ± 1.5%, N = 24). The radioimmunoconjugate with specific activity of 185 MBq/mg showed radiochemical purity above 95% (m=96.8 ± 1.31 %, N = 15). We conclude that the radioimmunoconjugate 111In-DTPA-cetuximab is stable and may be applied to the diagnosis of EGFR-positive tumors.

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BENEDETTO, RAQUEL; MASSICANO, ADRIANA V.F.; SILVA, JEFFERSON J.; BOAS, CRISTIAN A.W.V.; MENGATTI, JAIR; ARAUJO, ELAINE B. de. Development of radioimmunoconjugate for diagnosis and management of head-and-neck subclinical cancer and colorectal carcinoma. Brazilian Journal of Pharmaceutical Sciences, v. 53, n. 4, p. 1-10, 2018. DOI: 10.1590/s2175-97902017000417039. Disponível em: http://repositorio.ipen.br/handle/123456789/28929. Acesso em: 30 Dec 2025.
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