HMPL-813 is a novel small molecule compound that targets Epidermal Growth Factor Receptor (EGFR). Orally active small molecule kinase inhibitors, such as Iressa (gifitinib) and Tarceva (erlotinib), have met with success. For instance, the annual sales for Tarceva are expected to top $1 billion in 2008. Recent data suggested that a small subset of lung cancer patients responded particularly well to Iressa/Tarceva treatment. These patients are Asian female non-smokers with abnormal Ras kinase activation. These findings are fueling the sales growth of these products in Asian countries, Japan and China in particular. Therefore, EGFR is a clinically validated target for a variety of cancers and with promising growth potential particularly in Asian countries such as China. Hutchison MediPharma has global rights to HMPL-813.

Key Features

• IND filled with SFDA estimated at 1Q2010
• MOA: Potent inhibitor targeting EGFR and high selectivity to EGFR
• Demonstrated efficacy and safety profile in vitro and in vivo
• Strong IP protection in chemical compounds and medical use

• Narrow kinase spectrum and low toxicity
• Higher potency compared to Tarceva  
• Low costs of goods. Imported drugs of targeted therapies such as Tarceva and Iressa are very expensive. HMPL-813 is planned to be marketed in China for cancer patients.
• Demonstrated excellent pharmacokinetic properties in all preclinical species
• Strong IP position and protection

• In Vitro: HMPL-813 is a potent EGFR kinase inhibitor with good kinase selectivity. It can block survival of EGFR high expression tumor cells by inhibiting EGFR and AKT cell proliferation pathway and inducing cell cycle arrest and apoptosis. HMPL-813 is not a cytotoxic agent based on MTT assay data.
• In Vivo: HMPL-813 demonstrated broad spectrum anti-tumor activity via oral dosing in multiple xerographs such as A-431、Bcap-37 and Fadu.