Shanghai, China, Thursday, November 1, 2012: Hutchison MediPharma Limited (“HMP”) announced that it has initiated the first-in-human Phase I clinical trial of Theliatinib (HMPL-309). This is the fourth oncology compound from the internal discovery programs of HMP to enter into clinical development in China. Theliatinib is a novel, orally active small molecule inhibitor targeting the wild type epidermal growth factor receptor (“EGFR”) or resistant EGFR tumors. The first patient was dosed on October 30, 2012.
The primary objectives of the Phase I study are to evaluate its safety and tolerability in patients with advanced solid tumors and to determine its maximum tolerated dose. This study will also evaluate its preliminary efficacy against non-small cell lung cancer (“NSCLC”), determine the pharmacokinetics of Theliatinib under single dose and repeat doses and explore the relationship between the Theliatinib’s activity and certain biomarkers.
In pre-clinical studies, Theliatinib demonstrated strong anti-tumor activity against EGFR wild type tumors at doses that are expected to be well tolerated. Theliatinib was also found to have good pharmacokinetic properties and a favorable safety profile. These studies also exhibited good tissue distribution and stronger anti-tumor activity in EGFR wild type and EGFR resistant tumors, compared with first generation small molecule EGFR inhibitors. “If these attributes are also demonstrated in clinical studies, we believe that Theliatinib could become an important therapy in this area,” said Christian Hogg, Chief Executive Officer.
About epidermal growth factor receptor (“EGFR”) and non-small cell lung cancer (“NSCLC”)
EGFR is a protein that is a cell-surface receptor for epidermal growth factors. Activation of EGFR can lead to a series of downstream signaling activities that mediate tumor cell proliferation and the suppression of cell death. Small molecule tyrosine kinase inhibitors of EGFR block these signals, limiting tumor cell growth and survival.
The estimated incidence of lung cancer worldwide was over 1.6 million in 2008, with over 520,000 cases in China. Lung cancer is the most common cancer both worldwide and in China.
Gefitinib (Iressa™) and erlotinib (Tarceva™), first generation small molecule EGFR inhibitors, are used to treat NSCLC, particularly in patients with EGFR sensitive mutations. Worldwide sales of Tarceva™ alone reached approximately US$1.4 billion in 2011. However, EGFR mutations generally occur in 10-30% of NSCLC patients, with the range differing slightly by region. Currently available EGFR inhibitors have been shown to be less effective in treating patients carrying the wild type EGFR compared to treating patients harboring EGFR activating mutations. Pre-clinical studies suggest that Theliatinib has potential in the treatment of NSCLC patients with wild type EGFR or resistance to gefitinib or erlotinib.
HMP is a novel drug R&D company focusing on discovering, developing and commercializing innovative therapeutics in oncology and autoimmune diseases. With a team of around 200 scientists and staff, its pipeline is comprised of novel oral compounds for cancer and inflammation in development in North America, Europe, Australia and Greater China.