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Updated: Apr 11, 2026

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Apatinib: a promising oral antiangiogenic agent in the treatment of multiple solid tumors
A J Scott1, W A Messersmith1, A Jimeno2
1Division of Hematology and Oncology, University of Colorado Cancer Center, Aurora, Colorado, USA.
Abstract:
Aberrant proangiogenic pathways have long been implicated in tumorigenesis and metastasis. Antiangiogenic therapies have shown efficacy in the treatment of a variety of solid tumors including lung, breast, colon, glioblastomas, and other solid tumor types. Apatinib, a small-molecule inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2), is an orally bioavailable agent currently being studied in multiple tumor types. Apatinib has shown a survival benefit in gastric cancer in a phase III trial and non-small cell lung cancer in a phase II trial. With a favorable side effect profile and improved outcomes, apatinib has demonstrated a substantial potential to augment therapeutic options in a variety of tumor types.
Insights
Apatinib, a VEGFR-2 inhibitor, shows promise in treating various solid tumors by targeting proangiogenic pathways. This oral medication offers a survival benefit and a favorable side effect profile, expanding cancer treatment options.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Aberrant proangiogenic pathways are key drivers of tumor growth and metastasis.
- Antiangiogenic therapies targeting these pathways have demonstrated clinical efficacy in diverse solid tumors.
- Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2) is a critical mediator of angiogenesis.
Purpose of the Study:
- To evaluate the therapeutic potential of apatinib, a small-molecule VEGFR-2 inhibitor.
- To assess the efficacy and safety of apatinib in various solid tumor types.
- To determine if apatinib can improve outcomes in patients with advanced cancers.
Main Methods:
- Apatinib, an orally bioavailable small-molecule inhibitor, was investigated.
- Clinical trials were conducted across multiple tumor types, including gastric and non-small cell lung cancer.
- Efficacy, survival benefit, and side effect profiles were assessed.
Main Results:
- Apatinib demonstrated a survival benefit in gastric cancer (Phase III) and non-small cell lung cancer (Phase II).
- The agent is orally bioavailable, offering a convenient administration route.
- Apatinib exhibited a favorable side effect profile compared to other antiangiogenic agents.
Conclusions:
- Apatinib represents a promising therapeutic option for a range of solid tumors.
- Its efficacy in inhibiting VEGFR-2-mediated angiogenesis contributes to improved patient outcomes.
- Apatinib has the potential to augment current treatment strategies in oncology.
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