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Updated: Mar 18, 2026

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Apatinib for the treatment of gastric cancer
Giandomenico Roviello1,2, Andrea Ravelli3, Anna Ida Fiaschi4
1a Department of Molecular and Translational Medicine , University of Brescia , Brescia , Italy.
Introduction:
Apatinib, a small-molecule inhibitor of vascular endothelial growth factor receptor 2, has demonstrated encouraging anti-cancer activity in gastric cancer within both in vitro and in vivo models.
Areas Covered:
Apatinib's efficacy, tolerability and safety have been evaluated in one Phase II and one Phase III study in metastatic/advanced gastric cancer. In this review, we focus on the mechanism of action of apatinib, its pharmacokinetic profile and its clinical activity in the treatment of advanced/metastatic gastric cancer. Expert commentary: Unfortunately, as yet, there is no definitive biomarker data for apatinib in gastric cancer.
Insights
Apatinib shows promise as a targeted therapy for advanced gastric cancer by inhibiting VEGFR2. Further research is needed to identify predictive biomarkers for patient selection.
Area of Science:
- Oncology
- Pharmacology
Background:
- Apatinib is a novel small-molecule inhibitor targeting vascular endothelial growth factor receptor 2 (VEGFR2).
- Preclinical studies indicate significant anti-cancer effects of apatinib in gastric cancer models.
Purpose of the Study:
- To review the mechanism of action, pharmacokinetics, and clinical efficacy of apatinib in advanced/metastatic gastric cancer.
- To highlight the current limitations regarding predictive biomarker data for apatinib in this patient population.
Main Methods:
- Review of Phase II and Phase III clinical trial data for apatinib in metastatic/advanced gastric cancer.
- Analysis of preclinical in vitro and in vivo study findings.
Main Results:
- Apatinib demonstrates encouraging anti-cancer activity in gastric cancer.
- Clinical evaluations in Phase II and III studies support its use in advanced/metastatic settings.
Conclusions:
- Apatinib is a potential therapeutic option for advanced/metastatic gastric cancer.
- The lack of definitive predictive biomarkers remains a significant challenge for personalized treatment strategies.
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