title: Aurora kinase inhibitor patents and agents in clinical testing: an update (2011 - 2013).
abstract: BACKGROUND
  Aurora kinase A, B and C, members of serine/threonine kinase family, are key regulators of mitosis. As Aurora kinases are overexpressed in many of the human cancers, small-molecule inhibitors of Aurora kinase have emerged as a possible treatment option for cancer.
  
  
  METHODS
  In 2009 and 2011, the literature pertaining to Aurora kinase inhibitors and their patents was reviewed. Here, the aim is to update the information for Aurora kinase inhibitors in clinical trials and the patents filed between the years 2011 and 2013. Pubmed, Scopus®, Scifinder®, USPTO, EPO and www.clinicaltrials.gov databases were used for searching the literature and patents for Aurora kinase inhibitors.
  
  
  CONCLUSIONS
  Even though both Aurora sub-type selective as well as pan-selective inhibitors show preclinical and clinical efficacy, so far no Aurora kinase inhibitor has been approved for clinical use. Particularly, dose-limiting toxicity (neutropenia) is a key issue that needs to be addressed. Preliminary evidence suggests that the use of selective Aurora A inhibitors could avoid Aurora B-mediated neutropenia in clinical settings. Also, use of adjunctive agents such as granulocyte stimulating factor to overcome neutropenia associated with Aurora B inhibition could be an answer to overcome the toxicity and bring Aurora inhibitors to market in the future.
authors: National Cheng Kung University, College of Medicine, Department of Pharmacology , Tainan, Taiwan , Republic of China.
authors: Chun Hei Antonio
authors: CH
authors: Cheung
authors: Sailu
authors: S
authors: Sarvagalla
authors: Jane Ying-Chieh
authors: JY
authors: Lee
authors: Yi-Chun
authors: YC
authors: Huang
authors: Mohane Selvaraj
authors: MS
authors: Coumar
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D064127:Aurora Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D002986:Clinical Trials as Topic; D015195:Drug Design; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D064127:Aurora Kinases
keywords: AMG 900 and KW-2449; AT-9283; AZD1152; Aurora kinase inhibitor; CYC116; ENMD-2076; GSK1070916; MLN8054; MLN8237; PF-3814735; PHA739358; R763; SNS-314; VX-680/MK0457; VX-689/MK-5108