Micromolecule lung cancer targeted radioactive therapeutic agent and preparation method thereof

Abstract

The invention discloses a micromolecule lung cancer targeted radioactive therapeutic agent. Isotope 131I is marked with eight-peptide molecules with XGXG structures, wherein G shows L glycine, and X shows optional one of 20 amino acids. The invention further discloses a preparation method of the micromolecule lung cancer targeted radioactive therapeutic agent. The micromolecule lung cancer targeted radioactive therapeutic agent has good stability and biological distribution characteristics, can obviously suppress growth of tumour in a human lung cancer nude mouse animal model body, does not have obvious toxic and side effects to vitals such as livers, kidneys, lungs, hearts and the like, is applicable to targeted therapy for patients suffering from non-small cell lung cancer (squamous carcinoma and glandular cancer), and has an important clinical application value in the aspect of molecule targeted treatment for lung cancer.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a small-molecule lung cancer targeted radiotherapy agent and a preparation method thereof. Background technique [0002] According to the latest survey data released by the National Anti-Cancer Association, lung cancer has become the cancer with the highest mortality rate among Chinese people, especially urban residents, seriously endangering the health and lives of Chinese people. The main reason for the poor clinical prognosis of lung cancer is that about 80% of lung cancer patients are diagnosed at an advanced stage and have lost the best opportunity for surgical treatment. It is easy to produce drug resistance, and chemotherapy is more harmful to human health as a whole. Patients with advanced lung cancer often give up treatment because they cannot tolerate the pain of chemotherapy; radiotherapy is currently mainly used as a palliative treatment for lung cance...

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Problems solved by technology

[0005] 131 I-chTNT (Wemeisheng) is the world's first radioimmunotherapy agent for solid tumors. It was officially launched in my country in January 2007 and became the third global radioimmunotherapy agent after Zevalin and Bexxar. It is a radioimmunotherapy agent for solid tumors such as brain tumors. Clinical trials have shown that patients with advanced lung cancer received Weimeisheng injections, and the total effective rate was 33%. However, Weimeisheng still has obvious defects, because Weimeisheng is a human-mouse chimeric Anti-, containing certain mouse-derived ingredients, there is a potential risk of allergies. At the same time, there are also macromolecular antibodies that are easily recognized and phagocytized by the reticuloendothelial system and easily cause non-specific aggregation. Restrictions and other difficult problems have affected its curative effect

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