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Updated: Jul 18, 2026

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Sunitinib malate
Hassane Izzedine1, Irina Buhaescu, Olivier Rixe
1Department of Nephrology, Pitie-Salpetriere Hospital 83, Blvd de l'Hôpital, 75013 Paris, France. hassan.izzedine@psl.ap-hop-paris.fr
Abstract:
Recently, there has been a growing interest in understanding the role of receptor tyrosine kinases (RTK), such as vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), stem cell factor receptor (KIT), and fms-like tyrosine kinase 3 (FLT3), in promoting tumor angiogenesis, tumor growth and metastasis. Sunitinib (sunitinib malate; SU11248; SUTENT; Pfizer Inc, New York, NY, USA) is a novel, orally bio-available, oxindole, multi-targeted tyrosine kinase inhibitor with high binding affinity for VEGFR and PDGFR which has shown anti-tumor and anti-angiogenic activities. This drug recently received approval from the US Food and Administration (FDA) in two indications simultaneously: advanced renal cell carcinoma (adRCC) and gastrointestinal stromal tumors (GIST), in patients who are resistant or intolerant to the treatment with imatinib. The present article reviews the recent pharmacologic and clinical data related to the use of this new promising drug in the field of oncology.
Insights
Sunitinib, a multi-targeted tyrosine kinase inhibitor, shows anti-tumor and anti-angiogenic effects. It is approved for advanced renal cell carcinoma and gastrointestinal stromal tumors resistant to imatinib.
Area of Science:
- Oncology
- Pharmacology
Background:
- Receptor tyrosine kinases (RTKs) like VEGFR, PDGFR, KIT, and FLT3 play key roles in tumor angiogenesis, growth, and metastasis.
- Understanding RTK roles is crucial for developing targeted cancer therapies.
Purpose of the Study:
- To review pharmacologic and clinical data of sunitinib, a novel multi-targeted tyrosine kinase inhibitor.
- To highlight sunitinib's efficacy in oncology.
Main Methods:
- Review of recent pharmacologic and clinical data.
- Focus on sunitinib's binding affinity for VEGFR and PDGFR.
Main Results:
- Sunitinib exhibits anti-tumor and anti-angiogenic activities.
- Sunitinib received FDA approval for advanced renal cell carcinoma (adRCC) and gastrointestinal stromal tumors (GIST) in imatinib-resistant patients.
Conclusions:
- Sunitinib is a promising oral, multi-targeted tyrosine kinase inhibitor for specific cancer indications.
- The drug offers a new therapeutic option for patients with advanced RCC and GIST.
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