Delving into the Latest Updates on WXFL10030390 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

WX 390, WX-390, WXFL 10030390

+ [1]

Target

PI3Ks x mTOR

Action

inhibitors

Mechanism

PI3K family inhibitors(Phosphatidylinositol 3-kinase family inhibitors), mTOR inhibitors(Serine/threonine-protein kinase mTOR inhibitors)

Therapeutic Areas

NeoplasmsEndocrinology and Metabolic DiseaseUrogenital Diseases+ [4]

Active Indication

STK11-mutant cancerUterine Cervix AdenocarcinomaEndometrial Carcinoma+ [6]

Inactive Indication

Advanced cancer

Originator Organization

Cisen Pharmaceutical Ltd.

Active Organization

Cisen Pharmaceutical Ltd.

Shanghai Jiadan Pharmaceutical Technology Co., Ltd.Shanghai Jiao Tong University School of Medicine

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

RegulationSpecial Review Project (China)

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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.

Start Date25 Aug 2023

Sponsor / Collaborator

Shanghai Jiadan Pharmaceutical Technology Co., Ltd.

NCT06117566

/ RecruitingPhase 1/2

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.

Start Date18 Nov 2022

Sponsor / Collaborator

Shanghai Jiadan Pharmaceutical Technology Co., Ltd.

CTR20222481

/ RecruitingPhase 1/2

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

[Translation] A clinical trial to evaluate the safety, tolerability and preliminary efficacy of WXFL10030390 tablets combined with toripalimab in patients with advanced solid tumors and lymphomas

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）

[Translation]

To evaluate the dose-limiting toxicity (DLT) of WXFL10030390 tablets combined with toripalimab in the treatment of advanced solid tumors, and to determine the maximum tolerated dose (MTD) and phase II recommended dose (RP2D) of WXFL10030390 tablets in combination therapy

Start Date28 Oct 2022

Sponsor / Collaborator

Shanghai Jiadan Pharmaceutical Technology Co., Ltd.

100 Clinical Results associated with WXFL10030390

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100 Translational Medicine associated with WXFL10030390

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100 Patents (Medical) associated with WXFL10030390

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2

Literatures (Medical) associated with WXFL10030390

01 Dec 2025·CANCER CHEMOTHERAPY AND PHARMACOLOGY

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

Article

Author: Kang, Yu ; Chai, Ranran ; Xu, Jing ; Gao, Yi ; Zheng, Kewei ; Jin, Guanqin ; 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.

01 Aug 2024·iScience

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

Article

Author: Gao, Wei ; Chen, Hongrui ; Qiu, Yajing ; Lin, Xiaoxi ; Li, Yongguo ; 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 Deals associated with WXFL10030390

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
STK11-mutant cancer	Phase 2	China	Shanghai Jiadan Pharmaceutical Technology Co., Ltd.	25 Aug 2023
Uterine Cervix Adenocarcinoma	Phase 2	China	Shanghai Jiadan Pharmaceutical Technology Co., Ltd.	01 Aug 2023
Lymphoma	Phase 2	China	Shanghai Jiadan Pharmaceutical Technology Co., Ltd.	28 Oct 2022
Advanced Malignant Solid Neoplasm	Phase 2	China	Cisen Pharmaceutical Ltd.	03 Jun 2021
PIK3CA positive Solid Tumors	Phase 2	China	Shanghai Jiadan Pharmaceutical Technology Co., Ltd.	03 Jun 2021
Endometrial Carcinoma	Phase 2	China	Cisen Pharmaceutical Ltd.	19 Apr 2021
Ovarian Cancer	Phase 2	China	Cisen Pharmaceutical Ltd.	19 Apr 2021
Advanced cancer	Phase 1	China	Shanghai Jiadan Pharmaceutical Technology Co., Ltd.	25 Oct 2018
PIK3CA mutation/HR-positive/HER2-negative Breast Cancer	IND Approval	China	Shanghai Jiadan Pharmaceutical Technology Co., Ltd.	17 Mar 2023
Lipomatosis	Preclinical	China	Shanghai Jiao Tong University School of Medicine	01 Aug 2024

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT06117566 (ESMO2024) Manual	Phase 1/2	Advanced Cervical Carcinoma Second line	24	WX390 + Toripalimab	xmhaukykod(ofcqcndsji) = jdlgfofwls luaoksuxbh (dmiuevvyhj ) View more	Positive	14 Sep 2024
NCT06117540 (ESMO2024) Manual	Phase 2	Neoplasms ARID1A Mutation \| PIK3CA Mutation	17	WX390	lomtiudndi(eflsdxobrx) = jzfloncvne ogfeubivxd (wnanqmanty ) View more	Positive	14 Sep 2024
NCT06117540 (ESMO2024) Manual	Phase 2	Neoplasms ARID1A Mutation \| PIK3CA Mutation	17	WX390bo	lomtiudndi(eflsdxobrx) = gueqrwuhsy ogfeubivxd (wnanqmanty ) View more	Positive	14 Sep 2024
NCT06117566 (ESMO2024) Manual	Phase 1/2	Squamous Cell Carcinoma of Head and Neck	65	WX390aToripalimab	guplfirhxa(orznizbqci) = bxatfoampb talimfpfxd (xnzlstwcas ) View more	Positive	14 Sep 2024
NCT06117566 (ESMO2024) Manual	Phase 1/2	Squamous Cell Carcinoma of Head and Neck	65	WX390Toripalimab	inbjlmvspj(zvejfnvphk) = wrrndtuluj lherwtgiqy (wjgbsrlqiw ) View more	Positive	14 Sep 2024
NCT06117566 (Phase Ib study of a high potent PI3K-mTOR dual inhibitor WX390 combined with toripalimab in patients with advanced solid tumors, ASCO2024)	Phase 1	Solid tumor Treg	18	WX390 0.7 mg	apeddonqvw(qpdfqruqxc) = jkesgierbl rfgbeecnlo (hamlyjmygc, 2.53 - 6.37)	Positive	24 May 2024
NCT03730142 (ASCO 12021 \| ASCO 22021) Manual	Phase 1	Solid tumor \| Lymphoma	25	WX390	jkrfzattrs(fjylwmsvci) = fcejdegifv kyzyrlqogy (xaveqchhby ) View more	Positive	20 May 2021