05 Nov 2012, BioSpectrum Bureau , BioSpectrum
Singapore: Hutchison MediPharma (HMP) 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 that has entered 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 Dr Christian Hogg, CEO, HMP.