Angiopoietin-1 and Angiopoietin-2 Inhibitors: Clinical Development

  • Jessica Gillen
  • Debra Richardson
  • Kathleen MooreEmail author
Evolving Therapies (RM Bukowski, Section Editor)
Part of the following topical collections:
  1. Topical Collection on Evolving Therapies


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.


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.


Tie2 inhibition Angiopoietin inhibition Angiogenesis Anti-angiogenic therapy 


Compliance with Ethical Standards

Conflict of Interest

Jessica Gillen declares that she has no conflict of interest.

Debra Richardson has received compensation from Genentech and Ipsen for participation on advisory boards, and has served on steering committees for and received travel grants from Tesaro and Karyopharm Therapeutics.

Kathleen Moore has received research funding for investigator-initiated trials from ImmunoGen, Genentech/Roche, PTC Therapeutics, and Eli Lilly; has received compensation for participation on advisory boards from Clovis, AstraZeneca, Tesaro, ImmunoGen, Genentech/Roche, VBL Therapeutics, Janssen, Aravive, OncoMed, Samumed, and Merck; has received compensation for sales force training from Pfizer; and served as an unbranded speaker for AstraZeneca for DNA damage response.

Human and Animal Rights and Informed Consent

This article does not contain any studies with human or animal subjects performed by any of the authors.


Papers of particular interest, published recently, have been highlighted as: • Of importance

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  • Jessica Gillen
    • 1
  • Debra Richardson
    • 1
  • Kathleen Moore
    • 1
    Email author
  1. 1.The University of Oklahoma Stephenson Cancer CenterOklahoma CityUSA

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