Initiation of fruquintinib Phase II study in colorectal cancer

Shanghai: Friday, April 4, 2014: HMP today announces that it has initiated a Phase II clinical trial in colorectal cancer (“CRC”) patients in China for fruquintinib (HMPL-013), its investigational small molecule agent that selectively inhibits vascular endothelial growth factor receptors (“VEGFR”). Preparations and patient screening began earlier this year, with the first patient dosed on 2 April 2014.

This randomised, double-blind, placebo-controlled, multi-centre, proof-of-concept Phase II study is targeted at treating patients with locally advanced or metastatic colorectal cancer, who have failed at least 2 prior systemic antineoplastic therapies, including fluoropyrimidine, oxaliplatin and irinotecan. Patients will be randomised to receive either fruquintinib plus best supportive care (“BSC”) or placebo plus BSC at a 2:1 ratio. The primary endpoint is progression free survival, with secondary endpoints including disease control rate, overall response rate, overall survival and safety. Approximately 70 patients are expected to be enrolled, with top-line results expected in 2015.

Fruquintinib is designed to selectively inhibit VEGF receptors, namely VEGFR1, VEGFR2, and VEGFR3. In the first-in-human Phase I clinical trial 40 patients were treated with fruquintinib. Detailed results of the Phase I clinical trial are available at http://chi-med.com/eng/irinfo/presentations.htm, and were presented at the annual meeting of the American Association for Cancer Research in April 2013. Based on the Phase I data in CRC, a Phase Ib study was initiated which treated a further 62 CRC patients. Data from this trial are expected to be released in the near future.

In October 2013, HMP entered into a licensing, co-development and commercialisation agreement in China with Eli Lilly and Company for fruquintinib.

About vascular endothelial growth factor (“VEGF”) and colorectal cancer in China
At an advanced stage, tumours secrete large amounts of VEGF, a protein ligand, to stimulate formation of excessive vasculature (angiogenesis) around the tumour in order to provide greater blood flow, oxygen, and nutrients to the tumour. VEGF and VEGF receptors (“VEGFRs”) play a pivotal role in tumour-related angiogenesis, and inhibition of the VEGF/VEGFR pathway therefore represents an exciting therapeutic strategy in blocking the development of new blood vessels essential for tumour to grow and invade.

Colorectal cancer is the third most commonly diagnosed cancer in China, with 10.2% incidence in 2012. An estimated 390,000 cases of colorectal cancer were diagnosed in China. It is the fifth most common cause of cancer death after lung, liver, stomach and oesophagus cancer.

To date, several anti-VEGF/VEGFR agents have shown clinical efficacy against a number of tumour types. Given the scale and growth in the China oncology market, the market for VEGF/VEGFR inhibitors in China is expected to develop quickly in the next few years.
About HMP
HMP is a novel drug R&D company focusing on discovering, developing and commercialising 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. For more information, please visit: www.hmplglobal.com.