AC480 (formerly BMS-599626) is a small molecule kinase inhibitor that selectively inhibits the HER family of receptors, HER1, HER2, and HER4. Ambit licensed worldwide rights to AC480 from Bristol-Myers Squibb (BMS) in October 2007, and is developing both an oral and an intravenous (IV) formulation of AC480.
Role of HER receptors in oncology. Excessive HER signaling has been associated with the development of a wide variety of solid tumor types, including those found in lung, breast, colorectal, head, neck and brain cancers. As key signaling proteins involved in the regulation of cell growth, the HER family of receptors is believed to play a key role in the development and malignancy of these tumors. Currently marketed HER inhibitors inhibit only one or two of the HER family members and a drug that inhibits all of the HER receptors could be effective in more cancer types.