Epitinib (HMPL-813)

Key Features

  • Phase I trial started in late 2011 in China
  • MOA: potent inhibitor targeting EGFR and shows high selectivity to EGFR
  • Demonstrated efficacy and safety profile in vitro and in vivo
  • Unique pharmacokinetic (PK) / pharmacodynamic (PD) relationship due to a favorable and broad drug distribution profile in different tissues
  • Strong IP protection in chemical compounds and medical use

Epitinib (HMPL-813) is a novel small molecule compound that targets Epidermal Growth Factor Receptor (EGFR). EGFR is a clinically validated target for a variety of cancers, and commercially available orally active small molecule EGFR inhibitors such as IressaTM (gefitinib) and TarcevaTM (erlotinib) have met with success, especially in lung cancer. Epitinib’s competitive profile includes its unique PK characteristics with low toxicity and higher potency compared with existing treatments such as TarcevaTM. HMP has global rights to Epitinib.

In Vitro,epitinib is a potent EGFR kinase inhibitor with good kinase selectivity. It reduced survival of EGFR high expression tumor cells by inhibiting EGFR signaling pathway and induced cell cycle arrest and apoptosis. In Vivo, epitinib demonstrated a broad anti-tumor spectrum via oral dosing in multiple xenographs such as non-small cell lung carcinoma HCC827, human epidermoid cancer A-431, nasopharyngeal cancer Fadu and some brain tumors.

Non-clinical safety studies have indicated that epitinib is generally well tolerated in animals.

About the Epidermal Growth Factor Receptor in Cancer Tumors
Mutations involving EGFR could lead to its constant activation which could result in uncontrolled cell division – a predisposition for cancer. Consequently, some mutations of EGFR have been identified in several types of cancer, and it is the target of an expanding class of anticancer therapies.

Commercial anticancer therapeutics directed against EGFR include for example IressaTM (gefitinib) and TarcevaTM (erlotinib) for lung cancer. Recent data suggest that a subset of lung cancer patients with specific mutation EGFR responds particularly well to IressaTM/TarcevaTM treatment, notably Asian female non-smokers. The findings are fueling the sales growth of these products in Asian countries; Japan and China in particular. It is estimated by Datamonitor that the overall market worldwide of anti-EGFR agents will be over 8 billion in 2016.

Related Links