WXFL10030390(WXFL10030390) - 药物靶点：PI3Ks x mTOR_在研适应症：STK11突变肿瘤，子宫颈腺癌，子宫内膜癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

WX 390、WX-390、WXFL 10030390

+ [1]

靶点

PI3Ks x mTOR

作用方式

抑制剂

作用机制

PI3K family 抑制剂(Phosphatidylinositol 3-kinase family inhibitors)、mTOR抑制剂(丝氨酸/苏氨酸蛋白激酶mTOR抑制剂)

治疗领域

肿瘤内分泌与代谢疾病泌尿生殖系统疾病+ [4]

在研适应症

STK11突变肿瘤子宫颈腺癌子宫内膜癌+ [6]

非在研适应症

晚期癌症

原研机构

辰欣药业股份有限公司

在研机构

辰欣药业股份有限公司

上海嘉坦医药科技有限公司上海交通大学医学院

非在研机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)临床2期

特殊审评特殊审批 (中国)

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关联

10

项与 WXFL10030390 相关的临床试验

NCT06124963

/ Recruiting临床2期

A Phase II Study to Evaluate the Safety, Tolerability and Preliminary Efficacy of WX390 Combined With Toripalimab in Patients With Advanced Gastric-type Endocervical Adenocarcinoma With STK11 Mutations

The goal of this clinical trial is to evaluate the safety and preliminary efficacy of WX390 combined with Toripalimab in patients with advanced Gastric-type Endocervical Adenocarcinoma with STK11 mutations. The main questions it aims to answer are:
* Pharmacokinetic (PK) characteristics of WX390 combined with Toripalimab treatment.
* Safety and preliminary in combined therapy. Participants will be treated with WX390 orally and Toripalimab intravenously, and follow the efficacy and safety evaluation according to the protocol.

开始日期2023-08-25

申办/合作机构

上海嘉坦医药科技有限公司

NCT06117566

/ Recruiting临床1/2期

A Phase Ib/IIa Study to Evaluate the Safety and Preliminary Efficacy of WX390 Combined With Toripalimab in Patients With Advanced Solid Tumors

The goal of this clinical trial is to evaluate the safety and preliminary efficacy of WX390 combined with Toripalimab in patients with advanced solid tumors. The main questions it aims to answer are:
* the maximum tolerated dose (MTD) and dose-limiting toxicity (DLT) of WX390;
* safety and preliminary in combined therapy. Participants will be treated with WX390 orally and Toripalimab intravenously, and follow the efficacy and safety evaluation according to the protocol.

开始日期2022-11-18

申办/合作机构

上海嘉坦医药科技有限公司

CTR20222481

/ Recruiting临床1/2期

评估WXFL10030390片联合特瑞普利单抗在晚期实体瘤、淋巴瘤患者中安全性、耐受性和初步疗效的临床试验

评价WXFL10030390片联合特瑞普利单抗治疗晚期实体瘤的剂量限制性毒性（DLT），确定联合治疗中WXFL10030390片最大耐受剂量（MTD）和 II 期推荐剂量（RP2D）

开始日期2022-10-28

申办/合作机构

上海嘉坦医药科技有限公司

100 项与 WXFL10030390 相关的临床结果

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100 项与 WXFL10030390 相关的转化医学

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100 项与 WXFL10030390 相关的专利（医药）

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2

项与 WXFL10030390 相关的文献（医药）

2025-12-01·CANCER CHEMOTHERAPY AND PHARMACOLOGY

Targeting on the PI3K/mTOR: a potential treatment strategy for clear cell ovarian carcinoma

Article

作者: Kang, Yu ; Chai, Ranran ; Xu, Jing ; Jin, Guanqin ; Zheng, Kewei ; Gao, Yi ; Cao, Rui

PURPOSE:

Ovarian clear cell carcinoma is a highly malignant gynecological tumor characterized by a high rate of chemotherapy resistance and poor prognosis. The PI3K/AKT/mTOR pathway is well-known to be closely related to the progression of various malignancies, and recent studies have indicated that this pathway may play a critical role in the progression and worsening of OCCC.

METHODS:

In this study, we investigated the combined effects of WX390, a dual inhibitor of PI3K/mTOR, and cisplatin on OCCC through both in vitro and in vivo experiments to further elucidate their therapeutic effects.

RESULTS:

WX390 significantly inhibited the proliferation of human OCCC cell lines ES2 and OVISE, while promoting apoptosis. Furthermore, the combination of WX390 with CDDP exhibited a synergistic effect, markedly increasing the sensitivity of OCCC cells to chemotherapeutic agents and significantly suppressing tumor growth in PDX models. Western blot and RNA-seq analyses revealed that WX390 robustly inhibited the PI3K/AKT/mTOR pathway, interrupt autophagy, altered cell cycle dynamics, and induced apoptosis.

CONCLUSION:

This study comprehensively assessed the efficacy of WX390 across multiple models of OCCC, laying a solid foundation for the development of new therapeutic strategies for this challenging malignancy.

2024-08-01·iScience

PIK3CA mutations enhance the adipogenesis of ADSCs in facial infiltrating lipomatosis through TRPV1

Article

作者: Qiu, Yajing ; Lin, Xiaoxi ; Li, Yongguo ; Chen, Hongrui ; Gao, Wei ; Ye, Wei ; Sun, Bin ; Hua, Chen ; Song, Haoliang ; Wei, Wei

Facial infiltrating lipomatosis (FIL) is a congenital disorder. The pathogenesis of FIL is associated with PIK3CA mutations, but the underlying mechanisms remain undetermined. We found that the adipose tissue in FIL demonstrated adipocytes hypertrophy and increased lipid accumulation. All adipose-derived mesenchymal stem cells from FIL (FIL-ADSCs) harbored PIK3CA mutations. Moreover, FIL-ADSCs exhibited a greater capacity for adipogenesis. Knockdown of PIK3CA resulted in a reduction in the adipogenic potential of FIL-ADSCs. Furthermore, WX390, a dual-target PI3K/mTOR inhibitor, was found to impede PIK3CA-mediated adipogenesis both in vivo and in vitro. RNA sequencing (RNA-seq) revealed that the expression of transient receptor potential vanilloid subtype 1 (TRPV1) was upregulated after PI3K pathway inhibition, and overexpression or activation of TRPV1 both inhibited adipogenesis. Our study showed that PIK3CA mutations promoted adipogenesis in FIL-ADSCs and this effect was achieved by suppressing TPRV1. Pathogenesis experiments suggested that WX390 may serve as an agent for the treatment of FIL.

100 项与 WXFL10030390 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
STK11突变肿瘤	临床2期	中国	上海嘉坦医药科技有限公司	2023-08-25
子宫颈腺癌	临床2期	中国	上海嘉坦医药科技有限公司	2023-08-01
淋巴瘤	临床2期	中国	上海嘉坦医药科技有限公司	2022-10-28
晚期恶性实体瘤	临床2期	中国	辰欣药业股份有限公司	2021-06-03
PIK3CA阳性实体瘤	临床2期	中国	上海嘉坦医药科技有限公司	2021-06-03
子宫内膜癌	临床2期	中国	辰欣药业股份有限公司	2021-04-19
卵巢癌	临床2期	中国	辰欣药业股份有限公司	2021-04-19
晚期癌症	临床1期	中国	上海嘉坦医药科技有限公司	2018-10-25
PIK3CA突变/HR阳性/HER2阴性乳腺癌	临床申请批准	中国	上海嘉坦医药科技有限公司	2023-03-17
脂肪瘤样病	临床前	中国	上海交通大学医学院	2024-08-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT06117540 (ESMO2024) 人工标引	临床2期	肿瘤 ARID1A Mutation \| PIK3CA Mutation	17	WX390	鑰遞製鑰製壓遞繭廠壓(壓製窪觸築構網遞艱鏇) = 獵網鹽憲繭鏇壓鹹艱範壓築齋繭襯顧獵簾醖廠 (製鑰構顧積衊餘製願鬱 ) 更多	积极	2024-09-14
NCT06117540 (ESMO2024) 人工标引	临床2期	肿瘤 ARID1A Mutation \| PIK3CA Mutation	17	WX390bo	鑰遞製鑰製壓遞繭廠壓(壓製窪觸築構網遞艱鏇) = 窪艱構構淵壓蓋製蓋鑰壓築齋繭襯顧獵簾醖廠 (製鑰構顧積衊餘製願鬱 ) 更多	积极	2024-09-14
NCT06117566 (ESMO2024) 人工标引	临床1/2期	晚期宫颈癌二线	24	WX390 + Toripalimab	網願夢衊糧憲鬱夢範衊(網憲艱膚艱製鹹構壓蓋) = 鏇願膚齋願糧夢鹽壓壓繭網廠糧積淵膚淵膚遞 (窪願鹽獵選築齋糧蓋餘 ) 更多	积极	2024-09-14
NCT06117566 (ESMO2024) 人工标引	临床1/2期	头颈部鳞状细胞癌	65	WX390aToripalimab	顧蓋積蓋鹹範醖獵鏇築(構膚網壓遞餘憲夢蓋獵) = 鏇鏇顧廠觸構衊願選蓋蓋醖膚觸網願艱壓醖淵 (壓構餘鑰淵鏇獵獵鹹壓 ) 更多	积极	2024-09-14
NCT06117566 (ESMO2024) 人工标引	临床1/2期	头颈部鳞状细胞癌	65	WX390Toripalimab	窪觸糧顧憲糧蓋願窪鹽(糧鏇夢窪鏇鬱鹹範憲艱) = 鏇襯窪構網壓醖觸構獵襯選製顧鬱築膚鹹繭廠 (醖餘繭淵範餘願衊衊窪 ) 更多	积极	2024-09-14
NCT06117566 (Phase Ib study of a high potent PI3K-mTOR dual inhibitor WX390 combined with toripalimab in patients with advanced solid tumors, ASCO2024)	临床1期	实体瘤 Treg	18	WX390 0.7 mg	齋製構壓鑰網鬱糧遞遞(廠夢遞鹹鏇製遞廠餘膚) = 顧網襯鏇膚艱夢簾衊選築鏇膚鹹襯襯獵襯鑰遞 (製淵鏇壓淵廠廠構鹽簾, 2.53 ~ 6.37)	积极	2024-05-24
NCT03730142 (ASCO 12021 \| ASCO 22021) 人工标引	临床1期	实体瘤 \| 淋巴瘤	25	WX390	衊壓遞築鹽夢淵選鏇膚(願鏇衊願壓廠選遞壓襯) = 鹽衊範淵鏇齋廠遞網網遞網壓餘鑰選醖積構範 (醖鹽網鹽網顧遞獵願衊 ) 更多	积极	2021-05-20