Delving into the Latest Updates on DX1002 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CDH5 x Tubulin

Action

inhibitors

Mechanism

CDH5 inhibitors(Cadherin 5 inhibitors), Tubulin inhibitors

Therapeutic Areas

NeoplasmsDigestive System Disorders

Active Indication

Advanced gastric carcinomaAdvanced Hepatocellular Carcinoma

Inactive Indication

Advanced Malignant Solid NeoplasmEsophageal Carcinoma

Originator Organization

Guangzhou Anhao Pharmaceutical Technology Co., Ltd.

Active Organization

Guangzhou Anhao Pharmaceutical Technology Co., Ltd.

Dongguan Daxin Biotechnology Co., Ltd.

Inactive Organization-

License Organization-

Drug Highest PhasePhase 1/2

First Approval Date-

RegulationSpecial Review Project (China)

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Structure/Sequence

Molecular FormulaC23H31NO7

InChIKeyJIDZCGNIYVEJGD-FTPOTTDRSA-N

CAS Registry1927914-79-1

Non-Randomized, Open-Label, One-Armed, Competitive Enrollment, Multicenter Phase Ib/IIa Clinical Study to Evaluate Efficacy and PD/PK Characteristics of DX1002 Tablet in Patients with Advanced Hepatocellular Carcinoma /Gastric Cancer - Phase Ib/IIa Clinical Study for DX1002 Table as Treatment of Advance Hepatocellular Carcinoma / Gastric Cancer

Start Date15 Apr 2021

Sponsor / Collaborator

Sun Yat-Sen University Cancer Center

CTR20200996

/ RecruitingPhase 1/2

评估DX1002片在晚期肝细胞癌/胃癌病人中的有效性、药代/药效动力学特征、安全性的非随机、开放、单臂、中心化竞争入组、多中心Ⅰb/Ⅱa期临床试验

[Translation] A non-randomized, open, single-arm, centralized competitive enrollment, multicenter Phase Ib/IIa clinical trial to evaluate the efficacy, pharmacokinetic/pharmacodynamic characteristics, and safety of DX1002 tablets in patients with advanced hepatocellular carcinoma/gastric cancer

1.主要目的：评价DX1002在中国晚期肝细胞癌/胃癌病人中的有效性，为下一步临床研究提供参考。 2.次要目的：进一步评价DX1002给药后在中国晚期肝细胞癌/胃癌病人中的药代/药效动力学特征。评价用药前后受试者生活质量的变化情况。进一步评价DX1002给药后在中国晚期肝细胞癌/胃癌病人中的安全性和耐受性。 3.探索性目的：（仅探索阶段）观察用药前后肿瘤靶病灶内部坏死情况。观察用药前后肿瘤靶病灶内部血供变化情况。

[Translation]

1. Primary purpose: To evaluate the effectiveness of DX1002 in Chinese patients with advanced hepatocellular carcinoma/gastric cancer, and provide reference for the next clinical study. 2. Secondary purpose: To further evaluate the pharmacokinetic/pharmacodynamic characteristics of DX1002 in Chinese patients with advanced hepatocellular carcinoma/gastric cancer after administration. To evaluate the changes in the quality of life of the subjects before and after administration. To further evaluate the safety and tolerability of DX1002 in Chinese patients with advanced hepatocellular carcinoma/gastric cancer after administration. 3. Exploratory purpose: (Exploratory stage only) To observe the internal necrosis of the tumor target lesions before and after administration. To observe the changes in the blood supply of the tumor target lesions before and after administration.

Start Date15 Apr 2021

Sponsor / Collaborator

Guangzhou Anhao Pharmaceutical Technology Co., Ltd.

[+1]

CTR20180958

/ CompletedPhase 1

DX1002片治疗晚期实体瘤患者的安全性与耐受性Ⅰ期剂量递增试验

[Translation] Phase I dose-escalation trial of the safety and tolerability of DX1002 tablets in patients with advanced solid tumors

1)评价DX1002片的安全性和耐受性；2)确定DX1002片的最大耐受剂量和/或者Ⅱ期推荐剂量；3)观察DX1002片的药代动力学特征。 4)初步评价DX1002片的抗肿瘤疗效；5)探索DX1002片造成的血流变化情况与PK及疗效的相关性。

[Translation]

1) Evaluate the safety and tolerability of DX1002 tablets; 2) Determine the maximum tolerated dose and/or Phase II recommended dose of DX1002 tablets; 3) Observe the pharmacokinetic characteristics of DX1002 tablets. 4) Preliminary evaluation of the anti-tumor efficacy of DX1002 tablets; 5) Explore the correlation between the blood flow changes caused by DX1002 tablets and PK and efficacy.

Start Date30 Oct 2018

Sponsor / Collaborator

Guangzhou Anhao Pharmaceutical Technology Co., Ltd.

[+1]

100 Clinical Results associated with DX1002

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100 Translational Medicine associated with DX1002

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100 Patents (Medical) associated with DX1002

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1

Literatures (Medical) associated with DX1002

01 Feb 2025·Cell Reports Medicine

First-in-human phase 1 study of an orally bioavailable vascular-disrupting agent DX1002 in patients with advanced solid tumors

Article

Author: Ma, Yu-Xiang ; Wu, Hao-Xiang ; Yong, Zhi-Quan ; Wei, Xiao-Li ; Yang, Yun-Peng ; Chen, Bao-Lin ; Zhao, Hong-Yun ; Xu, Li ; Ruan, Dan-Yun ; Wang, Zhi-Qiang ; Wang, Feng ; Xu, Rui-Hua ; Li, Yu-Hong ; Tang, Liang-Wei

DX1002 is an oral vascular-disrupting agent and exhibits promising results in preclinical studies, leading to tumor vasculature destruction and xenografted tumor necrosis in various animal models. In the phase 1 trial, 17 patients with solid tumors receive DX1002 ranging from 50 to 1,100 mg. The maximum tolerated dose and recommended phase 2 dose of DX1002 are determined as 600 mg once daily. The most common treatment-related adverse events are nausea (23.5%), vomiting (17.6%), and fatigue (11.8%). All patients are evaluable for anti-tumor response, 12 of which achieve stable disease as best response. One patient with non-small cell lung cancer achieves a stable disease duration of 6.5 months. The median time to progression (TTP) is 2.70 months (95% confidence interval [CI], 0.90-4.60). Interestingly, reduced blood perfusion is observed by contrast-enhanced ultrasound in a patient with colon cancer. In conclusion, DX1002 is well tolerated and exhibits preliminary anti-tumor efficacy in patients with solid tumors. This study was registered at chictr.org.cn (ChiCTR2400080298).

100 Deals associated with DX1002

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Advanced gastric carcinoma	Phase 2	China	Guangzhou Anhao Pharmaceutical Technology Co., Ltd.	15 Apr 2021
Advanced gastric carcinoma	Phase 2	China	Dongguan Daxin Biotechnology Co., Ltd.	15 Apr 2021
Advanced Hepatocellular Carcinoma	Phase 2	China	Guangzhou Anhao Pharmaceutical Technology Co., Ltd.	15 Apr 2021
Advanced Hepatocellular Carcinoma	Phase 2	China	Dongguan Daxin Biotechnology Co., Ltd.	15 Apr 2021
Esophageal Carcinoma	Preclinical	China	Guangzhou Anhao Pharmaceutical Technology Co., Ltd.	12 Jan 2021
Esophageal Carcinoma	Preclinical	China	Dongguan Daxin Biotechnology Co., Ltd.	12 Jan 2021
Advanced Malignant Solid Neoplasm	Preclinical	China	Guangzhou Anhao Pharmaceutical Technology Co., Ltd.	30 Oct 2018
Advanced Malignant Solid Neoplasm	Preclinical	China	Dongguan Daxin Biotechnology Co., Ltd.	30 Oct 2018

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ChiCTR2400080298 (NEWS) Manual	Phase 1	Advanced Malignant Solid Neoplasm	17	DX1002	(urynebwsuz) = evcgntpexp gptyojawdo (nzcywusqii ) View more	Positive	21 Feb 2025