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

  • Cancer Lett. 2011 Mar 28;302(2):155-65. doi: 10.1016/j.canlet.2011.01.010.
Hyun-Jin Nam  1 ,  Hwang-Phill Kim ,  Young-Kwang Yoon ,  Hyung-Seok Hur ,  Sang-Hyun Song ,  Maeng-Sup Kim ,  Gwan-Sun Lee ,  Sae-Won Han ,  Seock-Ah Im ,  Tae-You Kim ,  Do-Youn Oh ,  Yung-Jue Bang
Affiliations
  • 1. Cancer Research Institute, Seoul National University College of Medicine, Seoul, Republic of Korea.
PMID: 21306821 DOI: 10.1016/j.canlet.2011.01.010
Abstract

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.

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