Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer

作者：Nam Hyun Jin; Kim Hwang Phill; Yoon Young Kwang; Hur Hyung Seok; Song Sang Hyun; Kim Maeng Sup; Lee Gwan Sun; Han Sae Won; Im Seock Ah; Kim Tae You; Oh Do Youn; Bang Yung Jue^*

来源：Cancer Letters, 2011, 302(2): 155-165.

DOI：10.1016/j.canlet.2011.01.010

• HM781-36B
• Pan-HER inhibitor
• Gastric cancer
• Antitumor activity
• Chemotherapeutic agents

Trastuzumab, a HER2 directed treatment has shown clinical benefit in HER2 amplified gastric cancer. This study demonstrated the potent antitumor activity of HM781-36B, a quinazoline-based irreversible pan-HER inhibitor, in HER2 amplified gastric cancer cells (SNU216 and N87) in vitro and in vivo. HM781-36B inhibited phosphorylation of HER family and downstream signaling molecules, and induced apoptosis and G1 arrest. Furthermore, HM781-36B exerted synergistic effects with chemotherapeutic agents in both HER2 amplified and HER2 non-amplified gastric cancer cells. Therefore, HM781-36B may be useful for the treatment of HER2 amplified gastric cancer alone or in combination with chemotherapeutic agents.

• 出版日期2011-3-28