Delving into the Latest Updates on Ersteq Co., Ltd. with Synapse

概览

疾病领域	数量

内分泌与代谢疾病	1
肿瘤	1

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

MTTP(微粒体甘油三酯转运蛋白复合体)	1

关联

1

项与 Ersteq Co., Ltd. 相关的药物

Lomitapide Mesylate

甲磺酸洛美他派

靶点

MTTP

作用机制

MTTP抑制剂

在研机构

Amryt Pharma Holdings Ltd. [+4]

原研机构

Bristol Myers Squibb Co.

在研适应症

II a型高脂蛋白血症 [+2]

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

美国

首次获批日期2012-12-21

100 项与 Ersteq Co., Ltd. 相关的临床结果

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0 项与 Ersteq Co., Ltd. 相关的专利（医药）

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1

项与 Ersteq Co., Ltd. 相关的文献（医药）

Cell Death & Disease

Lomitapide, a cholesterol-lowering drug, is an anticancer agent that induces autophagic cell death via inhibiting mTOR

Article

作者: Lee, Eunbeol ; Yoo, Eun-Seon ; Oh, Byung-Chul ; Lee, Seulgi ; Lee, Boah ; Park, Seung Ju ; Kim, Seyun ; Lee, Jinwook ; Chung, Won-Suk ; Sohn, Jong-Woo

AbstractAutophagy is a biological process that maintains cellular homeostasis and regulates the internal cellular environment. Hyperactivating autophagy to trigger cell death has been a suggested therapeutic strategy for cancer treatment. Mechanistic target of rapamycin (mTOR) is a crucial protein kinase that regulates autophagy; therefore, using a structure-based virtual screen analysis, we identified lomitapide, a cholesterol-lowering drug, as a potential mTOR complex 1 (mTORC1) inhibitor. Our results showed that lomitapide directly inhibits mTORC1 in vitro and induces autophagy-dependent cancer cell death by decreasing mTOR signaling, thereby inhibiting the downstream events associated with increased LC3 conversion in various cancer cells (e.g., HCT116 colorectal cancer cells) and tumor xenografts. Lomitapide also significantly suppresses the growth and viability along with elevated autophagy in patient-derived colorectal cancer organoids. Furthermore, a combination of lomitapide and immune checkpoint blocking antibodies synergistically inhibits tumor growth in murine MC38 or B16-F10 preclinical syngeneic tumor models. These results elucidate the direct, tumor-relevant immune-potentiating benefits of mTORC1 inhibition by lomitapide, which complement the current immune checkpoint blockade. This study highlights the potential repurposing of lomitapide as a new therapeutic option for cancer treatment.

100 项与 Ersteq Co., Ltd. 相关的药物交易

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100 项与 Ersteq Co., Ltd. 相关的转化医学

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