Molecular Targeting Technologies, Inc. (MTTI) has released preclinical research findings for their proprietary 225Ac-EBTATE targeting SSTR2-positive neuroendocrine tumors (NET) in the European Journal of Nuclear Medicine. The study, titled "Long-acting 225Ac-EBTATE demonstrates high efficacy against somatostatin receptor-2-positive neuroendocrine tumors," is available online (https://rdcu.be/d2lCG).
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Professor Humphrey Fonge from Université de Laval and the lead author stated, "With only 40% of the dose used for 225Ac-DOTATATE, 225Ac-EBTATE has shown superior anti-tumor effects in Small Cell lung cancer (SCLC) and Pan-neuroendocrine tumor (NET) models, achieving complete tumor remissions. At a therapeutic dose of 2x 34 kBq, 225Ac-EBTATE exhibited general safety over 28 days based on blood biochemistry analysis, CBC, and histopathological examination of major organs and tissues. Our results indicate that 225Ac-EBTATE is effective against human small-cell lung cancer (SCLC), with an 80% complete remission rate and 100% survival in preclinical models."
MTTI has secured commercial use rights for the patented Evans blue (EB) technology from the National Institute of Biomedical Imaging and Bioengineering (NIBIB), a division of the National Institutes of Health (NIH). This technology forms the foundation for a best-in-class, new generation of targeted radiopharmaceuticals (TRP). EB's binding to serum albumin prolongs in vivo circulatory half-life and tumor residence time, enhancing tumor uptake by up to 30-fold and allowing for effective treatment with significantly lower radiopharmaceutical activity and fewer dosing cycles compared to the current standard of care. Our 3-year follow-up of 177Lu-EBTATE in patients* (N=30) with metastatic neuroendocrine tumors showed good safety with no nephro- or hepatoxicity and an 86% disease control rate using only 40% of the administered dose of 177Lu-DOTATATE.
Dr. Jean-Mathieu Beauregard, MD, Associate Professor in the Department of Radiology at Université Laval, expressed, "I am optimistic about the positive outcomes of 225Ac-EBTATE in preclinical studies for treating small cell lung cancer and Pan-neuroendocrine tumor (NET). I am eager to collaborate with MTTI and Professor Fonge to transition these findings into clinical practice."
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According to the data provided by the Synapse Chemical, As of December 12, 2024, there are 67 investigational drugs for the SSTR2 target, including 108 indications, 78 R&D institutions involved, with related clinical trials reaching 281, and as many as 2437 patents.
225Ac-EBTATE is a therapeutic radiopharmaceutical drug designed to target SSTR2, primarily focused on treating neoplasms and respiratory diseases, with a specific indication for small cell lung cancer. The drug is currently in the preclinical stage and is developed by Molecular Targeting Technologies, Inc.