Linifanib

Current status and future potential in cancer therapy

Caterina Aversa, Francesco Leone, Giorgia Zucchini, Guido Serini, Elena Geuna, Andrea Milani, Donatella Valdembri, Rossella Martinello, Filippo Montemurro

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Angiogenesis is one of the major mechanisms controlling tumor proliferation and metastatic spreading. Targeting of pro-angiogenic factors and their downstream effectors represents an appealing therapeutic option in the treatment of different cancer types. Linifanib (ABT-869) is a novel tyrosine-kinase inhibitor (TKI) inhibitor and its anti-angiogenic activity has been explored in numerous clinical trials. Here, we review preclinical development of linifanib focusing on its pharmacodynamic and pharmacokinetic characteristics and briefly summarize its evaluation in clinical trials. Linifanib selectively targets VEGFR and PDGFR and has low off-target inhibitory activity. Preclinical and early-phase trials have been showing promising efficacy results However, although signals of anti-tumor activity have been proven in some malignancies, linifanib late-phase development has been facing some challenges due to limited efficacy and increased toxicities. New strategies aimed at finding biomarkers of response and minimizing toxicities are needed to allow the further development of a promising compound.

Original languageEnglish
Pages (from-to)677-687
Number of pages11
JournalExpert Review of Anticancer Therapy
Volume15
Issue number6
DOIs
Publication statusPublished - Jun 1 2015

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N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N1-(2-fluoro-5-methylphenyl)urea
Neoplasms
Clinical Trials
Therapeutics
Angiogenesis Inducing Agents
Protein-Tyrosine Kinases
Pharmacokinetics
Biomarkers

Keywords

  • ABT-869
  • angiogenesis
  • chemotherapy
  • Linifanib
  • PDGF
  • VEGF

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Oncology
  • Medicine(all)

Cite this

Linifanib : Current status and future potential in cancer therapy. / Aversa, Caterina; Leone, Francesco; Zucchini, Giorgia; Serini, Guido; Geuna, Elena; Milani, Andrea; Valdembri, Donatella; Martinello, Rossella; Montemurro, Filippo.

In: Expert Review of Anticancer Therapy, Vol. 15, No. 6, 01.06.2015, p. 677-687.

Research output: Contribution to journalArticle

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