Related Experiment Video

Updated: Apr 27, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
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Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells

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Aurora kinase inhibitor patents and agents in clinical testing: an update (2011 - 2013)

Chun Hei Antonio Cheung1, Sailu Sarvagalla, Jane Ying-Chieh Lee

  • 1National Cheng Kung University, College of Medicine, Department of Pharmacology , Tainan, Taiwan , Republic of China.

Expert Opinion on Therapeutic Patents
|June 27, 2014
PubMed
Abstract

Insights

Small-molecule inhibitors targeting Aurora kinases (A, B, and C) show promise for cancer treatment but face toxicity challenges. Selective Aurora A inhibitors or supportive therapies may overcome neutropenia, potentially leading to market approval.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Development

Background:

  • Aurora kinases (A, B, C) are serine/threonine kinases crucial for cell division.
  • Overexpression of Aurora kinases is linked to various human cancers.
  • Small-molecule inhibitors of Aurora kinases are investigated as potential cancer therapeutics.

Purpose of the Study:

  • To update the literature and patent information on Aurora kinase inhibitors in clinical trials.
  • To review inhibitors and patents filed between 2011 and 2013.

Main Methods:

  • Literature and patent searches were conducted using databases like Pubmed, Scopus, Scifinder, USPTO, EPO, and clinicaltrials.gov.
  • Focus on clinical trials and patents for Aurora kinase inhibitors from 2011-2013.

Main Results:

  • Both selective and pan-selective Aurora kinase inhibitors demonstrate preclinical and clinical effectiveness.
  • No Aurora kinase inhibitor has received FDA approval for clinical use to date.
  • Neutropenia is a significant dose-limiting toxicity observed with these inhibitors.

Conclusions:

  • Selective Aurora A inhibitors may mitigate Aurora B-mediated neutropenia.
  • Adjunctive therapies, such as granulocyte stimulating factor, could address neutropenia.
  • Overcoming toxicity is crucial for the market approval of Aurora kinase inhibitors.
Keywords:
AMG 900 and KW-2449AT-9283AZD1152Aurora kinase inhibitorCYC116ENMD-2076GSK1070916MLN8054MLN8237PF-3814735PHA739358R763SNS-314VX-680/MK0457VX-689/MK-5108

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