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First-in-human phase 1 study of an orally bioavailable vascular-disrupting agent DX1002 in patients with advanced
Xiao-Li Wei1, Hao-Xiang Wu2, Dan-Yun Ruan2
1Department of Medical Oncology, Sun Yat-sen University Cancer Center, State Key Laboratory of Oncology in South China, Guangdong Provincial Clinical Research Center for Cancer, Sun Yat-sen University, Guangzhou 510060, P.R. China.
Abstract:
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).
Insights
DX1002, an oral vascular-disrupting agent, shows preliminary anti-tumor efficacy in solid tumors. The phase 1 trial determined a safe dosage and observed stable disease in most patients, indicating potential for cancer treatment.
Area of Science:
- Oncology
- Pharmacology
- Clinical Trials
Background:
- DX1002 is an oral vascular-disrupting agent with preclinical efficacy in destroying tumor vasculature and causing necrosis.
- Preclinical studies demonstrated significant tumor destruction and necrosis in various animal models.
Purpose of the Study:
- To evaluate the safety, tolerability, and preliminary efficacy of DX1002 in patients with solid tumors.
- To determine the maximum tolerated dose (MTD) and recommended Phase 2 dose (RP2D) of DX1002.
Main Methods:
- A Phase 1 clinical trial involving 17 patients with solid tumors receiving escalating doses of DX1002 (50-1,100 mg).
- Assessment of treatment-related adverse events, maximum tolerated dose, recommended Phase 2 dose, and anti-tumor response.
- Utilized contrast-enhanced ultrasound to observe changes in tumor blood perfusion.
Main Results:
- The maximum tolerated dose and recommended Phase 2 dose were established at 600 mg once daily.
- Common adverse events included nausea (23.5%), vomiting (17.6%), and fatigue (11.8%).
- Twelve out of 17 patients achieved stable disease, with one non-small cell lung cancer patient maintaining it for 6.5 months. Median time to progression was 2.70 months.
Conclusions:
- DX1002 is well-tolerated in patients with solid tumors at the recommended Phase 2 dose.
- Preliminary anti-tumor efficacy was observed, including stable disease in a majority of patients.
- Further investigation in Phase 2 trials is warranted to confirm the efficacy of DX1002.
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