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Updated: Jan 4, 2026

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Application effect of apatinib in patients with failure of standard treatment for advanced malignant tumours
Guohui Liu1, Chunbo Wang1, Yunlong He1
1Department of Radiation Oncology, The Harbin Medical University Cancer Hospital, Harbin, 150040, China.
Background:
In recent years, targeted therapy has received widespread attention. Among these therapies, anti-angiogenic targeted drugs have become one of the hotspots of research. Apatinib is a novel oral small molecule anti-angiogenic agent that has been clinically tested in a variety of solid tumours. The aim of this study was to investigate the efficacy of apatinib in patients with advanced malignant tumours and failure of standard therapy.
Methods:
We collected 41 patients with advanced malignant tumours in our department; all tumours were pathologically confirmed as malignant. All patients received apatinib after failure of standard therapy: 500 mg/dose, one dose/d, orally 30 min after a meal, until progressive disease or intolerable adverse reactions occurred. When there was a second- or third-degree adverse reaction associated with apatinib during treatment, apatinib treatment could be suspended or reduced to 250 mg/dose. Clinical efficacy and progression-free survival were assessed according to RECIST1.1, and adverse reactions were observed.
Results:
Efficacy assessment was available for 31 patients with a median progression-free survival time of 2.66 months; the objective response rate and disease control rates were 16.1 and 64.5%, respectively. The disease control rates of the patients with lower Eastern Cooperative Oncology Group scores (1-2 points) and with fewer metastatic sites (< 3 sites) were higher than those of the patients with higher scores (3 points) and with more metastatic sites (≥3 sites), respectively (all P < 0.05). The most common adverse reactions were hypertension, neutropenia and hand-foot syndrome.
Conclusion:
For patients with advanced malignant tumours with failure of standard therapy, administration of apatinib can still result in good efficacy. The efficacy of apatinib is better in patients with a higher performance status and lower degree of tumour progression.
Insights
Apatinib shows efficacy in advanced cancers after standard therapy failure. It is more effective in patients with better performance status and less tumor spread, with common side effects including hypertension and neutropenia.
Area of Science:
- Oncology
- Pharmacology
- Clinical Medicine
Background:
- Targeted therapy, particularly anti-angiogenic drugs, is a significant research focus.
- Apatinib is an oral small molecule anti-angiogenic agent evaluated in various solid tumors.
Purpose of the Study:
- To assess the efficacy of apatinib in patients with advanced malignant tumors who have not responded to standard therapies.
- To identify patient subgroups who may benefit most from apatinib treatment.
Main Methods:
- A cohort of 41 patients with advanced malignant tumors received apatinib (500 mg/day orally) after standard therapy failure.
- Efficacy was evaluated using RECIST 1.1 criteria, and adverse reactions were monitored.
- Dosage adjustments were permitted for severe adverse events.
Main Results:
- Median progression-free survival was 2.66 months in 31 assessable patients.
- Objective response rate was 16.1%, and disease control rate was 64.5%.
- Higher disease control rates were observed in patients with better Eastern Cooperative Oncology Group scores (1-2) and fewer metastatic sites (<3).
Conclusions:
- Apatinib demonstrates clinical efficacy in advanced malignant tumors refractory to standard treatments.
- Patient performance status and tumor burden influence apatinib's effectiveness.
- Hypertension, neutropenia, and hand-foot syndrome were the most frequent adverse events.
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