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Ref Type | Journal Article | ||||||||||||
PMID | (21306821) | ||||||||||||
Authors | Nam HJ, Kim HP, Yoon YK, Hur HS, Song SH, Kim MS, Lee GS, Han SW, Im SA, Kim TY, Oh DY, Bang YJ | ||||||||||||
Title | Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer. | ||||||||||||
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Abstract Text | 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. |
Molecular Profile | Treatment Approach |
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Gene Name | Source | Synonyms | Protein Domains | Gene Description | Gene Role |
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Therapy Name | Drugs | Efficacy Evidence | Clinical Trials |
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Poziotinib | Poziotinib | 0 | 7 |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
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Poziotinib | HM781-36B|NOV120101 | EGFR Inhibitor (Pan) 61 HER inhibitor (Pan) 6 | Poziotinib (HM781-36B) is a pan-ErbB inhibitor that inhibits EGFR, ERBB2 (HER2) and ERBB4 (HER4), thereby reducing proliferation of tumor cells that overexpress these receptors (PMID: 21306821, PMID: 31588020). |
Gene | Variant | Impact | Protein Effect | Variant Description | Associated with drug Resistance |
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Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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