氯硝柳胺纳米晶潜在的治疗胃肠间质瘤的研究进展

Research progress on the potential of Niclosamide Nanocrystals in the treatment of gastrointestinal stromal tumor

胃肠间质瘤是最常见的间叶源性肿瘤,手术切除是治疗局限性胃肠间质瘤的主要方法。目前针对胃肠间质瘤的病理性突变,临床上研发了数代酪氨酸激酶抑制剂,均取得一定的成效。然而,酪氨酸激酶抑制剂用药2~3年后,常常会产生耐药性,导致治疗失败。近年来,氯硝柳胺作为一种抗肿瘤活性的药物出现在公众视野,由于其溶解度差等原因,晶体制剂则应运而生,更好地发挥了抗肿瘤特性。文章结合目前的实验基础及相关机制,探讨在酪氨酸激酶抑制剂耐药的胃肠间质瘤中联合给药的可能性,以期开发胃肠间质瘤的新治疗方案。

Gastrointestinal stromal tumor is the most common mesenchymal tumor,and surgical resection is the main method to treat localized gastrointestinal stromal tumor.Currently,several generations of tyrosine kinase inhibitors have been clinically developed to target the pathological mutations of gastrointestinal stromal tumors,all of which have achieved certain results.However,resistance to tyrosine kinase inhibitors often develops after 2-3 years of treatment,leading to treatment failure.In recent years,niclosamide has appeared in the public eye as a drug with anti-tumor activity.Due to its poor solubility and other reasons,crystal preparations have emerged to better exert its anti-tumor properties.This article combines the current experimental basis and related mechanisms to explore the possibility of combined administration in gastrointestinal stromal tumors resistant to tyrosine kinase inhibitors,with a view to developing new treatment options for gastrointestinal stromal tumors.