HMPL-012
Sulfatinib (HMPL-012) is a novel small molecule compound that targets tumor angiogenic blood vessels crucial for tumor growth and invasion/metastasis. The unique kinase profile provides a promising compound opportunity and strong differentiation against existing products on the market such as Sutent and Nexavar as well as compounds currently in the clinical development for cancer. Hutchison MediPharma has global rights to Sulfatinib.
Key Features
- Obtained Clinical Trial Approval (CTA) by the SFDA on Mar, 2010
- MOA: Potent inhibitor targeting tumor angiogenic blood vessels, tumor growth and invasion/metastasis
- Demonstrated efficacy and safety profile in vitro and in vivo
- Strong IP protection in chemical compounds and medical use
Mechanism of Action (MOA)
Inhibit all three forms of VEGF receptors (VEGFR-1,2,3) and FGF receptor (FGFR-1)
Competitive Advantages
- Narrow kinase spectrum and low toxicity
- Better safety profile than Sutent after consecutive dosing
- Low costs of goods. Imported drugs of targeted therapies such as Sutent and Nevavar are very expensive. Sulfatinib is planned to be marketed in China for cancer patients
- Sulfatinib differentiates from other VEGFR inhibitors in clinical development in China, by inhibiting all three forms of VEGFRs
- Strong IP position and protection
Preclinical Studies
a) Efficacy
- In Vitro: Sulfatinib inhibited VEGF-induced KDR phosphorylation and activation of downstream singal transduction pathways, thus inhibited VEGF-dependent HUVEC invasion
- In Vivo: Sulfatinib demonstrated broad spectrum anti-tumor activity via oral dosing in multiple xerographs such as BGC-823、HT-29、H-460 and Caki-1
b) Safety
- Non-clinical safety studies carried out by Hutchison MediPharma have indicated that Sulfatinib is generally well tolerated in animals. Sulfatinib is neither mutagenic nor teratogenic.
Clinical Plans
- Conduct Phase I clinical trial in patients with solid tumors in China estimated at 1Q2010
- Conduct Phase II (POC) clinical trial in patients with three types of solid tumors (hepatic carcinoma, gastric carcinoma and renal carcinoma) in China
Manufacturing
Kilogram quantities of API and drug product have been manufactured under cGMP for the human clinical studies.
Intellectual Property
Hutchison MediPharma filed patent applications both in US and China in 2007 and PCT application in 2008. The applications claimed the chemical compounds and their medical use.
Hutchison MediPharma filed patent applications both in US and China in 2007 and PCT application in 2008. The applications claimed the chemical compounds and their medical use.
Potential Market of VEGFR Inhibitors
Vascular Endothelial Growth Factor (VEGF) is an important signaling protein involved in both vasculogenesis and angiogenesis. Vascular Endothelial Growth Factor Receptor (VEGFR) tyrosine kinase inhibitor is being developed for the treatment of cancer and acts as an angiogenesis inhibitor.
Two small molecule VEGFR inhibitors have been launched and indication expansion caused their substantial sales growth in seven major markets from $206 million in 2006 to $685 million in 2008. Datamonitor forecasts the small molecule VEGFR inhibitors will reach to $5.4 billion in 2016.
The current marketed VEGFR inhibitors are quite expensive and have unfavorable side effect profiles. There is a strong market need for a safe oral drug which is effective and convenient. Sulfatinib is currently the most promising oral drug candidate in clinical development. Once approved in US and other major markets, Sulfatinib could make the annual sales of $500-$800 million dollars.
