Incyte’s novel oral cancer compound enters clinic

The phase I trial is a double-blind, placebo-controlled, single rising dose study designed to assess the safety and pharmacokinetics of INCB7839 in healthy volunteers. A phase I multiple dose study in healthy volunteers is expected to begin in April.

INCB7839 is a sheddase inhibitor. Sheddase is an enzymatic activity attributed to the ADAM (a disintegrin and metalloprotease) family of proteins that has been shown to play a role in controlling the growth and spread of certain cancers that are regulated by members of the human epidermal growth factor receptor (HER) family of receptor tyrosine kinases.

Increased activity of these receptors, which include HER-1, HER-2, HER-3 and HER-4, contributes to the development and progression of many types of cancers, including breast, colon, non-small cell lung, and head and neck cancer.

Upregulation of HER family members has been observed in numerous cancers and is now considered to be a validated target for therapeutic intervention. Several approved drugs target these pathways including the antibodies directed against HER-1 (Erbitux) and HER-2 (Herceptin), and the small molecule inhibitor of the HER-1 tyrosine kinase (Tarceva).

“Several approved drugs that target the HER family have demonstrated the therapeutic value of blocking these pathways,” commented Dr Paul Friedman, president and CEO of Incyte. “Our oral sheddase inhibitor, which targets these pathways at multiple points and acts more broadly than existing therapies, has shown excellent single agent activity in a number of preclinical models and has markedly improved the effectiveness of a variety of anticancer agents without causing incremental toxicity in these models.”