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Drug intelligence / Profile preview
225Ac-BPR603303 is a novel peptide-based somatostatin receptor subtype 2 (SSTR2) antagonist-based alpha-emitting radiopharmaceutical. Developed by Chengdu Brilliant Pharmaceutical, it is designed to target SSTR2-positive neuroendocrine malignancies, particularly neuroendocrine-derived small cell lung cancer (SCLC). Unlike traditional agonist-based radiopharmaceuticals that rely on receptor internalization, SSTR2 antagonists bind to more receptor sites and demonstrate higher tumor uptake and better image contrast. Preclinical studies have shown that 225Ac-BPR603303 significantly inhibits tumor growth and prolongs survival in SCLC xenograft models with high SSTR2 expression, demonstrating potent and durable antitumor efficacy.
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