Angiopoietin-1 and Angiopoietin-2 Inhibitors: Clinical Development

Jessica Gillen, Debra Richardson, Kathleen Moore

Research output: Contribution to journalReview articlepeer-review

21 Scopus citations


Purpose of Review: The purpose of this review is to discuss the current understanding of the Tie2-angiopoietin system and its role in tumor growth and metastasis. This review also focuses on preclinical and clinical data published to date that have evaluated Tie2-angiopoietin inhibition. Recent Findings: Tie2 inhibition has shown significant promise in preclinical models, notable for decreased tumor burden and fewer sites of metastatic disease across various malignancies. However, data from human clinical trials have shown more mixed results. Trebananib, rebastanib, and MEDI3617 are the three Tie2-angiopoietin inhibitors that have been most widely evaluated in phase I and II trials. Further investigation into these therapies is ongoing. Summary: The Tie2-angiopoietin pathway continues to show promise in preclinical and some clinical trials, including studies on recurrent or metastatic breast and renal cell carcinomas. Further evaluation of these therapies, however, is warranted to better understand their optimal clinical utility.

Original languageEnglish (US)
Article number22
JournalCurrent oncology reports
Issue number3
StatePublished - Mar 1 2019
Externally publishedYes


  • Angiogenesis
  • Angiopoietin inhibition
  • Anti-angiogenic therapy
  • Tie2 inhibition

ASJC Scopus subject areas

  • Oncology


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