Brivanib Alaninate for Cancer

Expert Opin Investig Drugs. 2011 Apr;20(4):577-86. doi: 10.1517/13543784.2011.565329. Epub 2011 Mar 11.

Abstract

Introduction: Angiogenesis inhibition represents a rational therapeutic strategy in the management of solid tumors. Brivanib is a dual tyrosine kinase inhibitor with selectivity against VEFGR-2 and FGFR.

Areas covered: This review provides an updated summary of preclinical and clinical experience with brivanib in cancer. Data presented in abstract form from international conferences or journal articles found with a PubMed search of published literature up to December 2010 are described in this review.

Expert opinion: Brivanib appears tolerable and exhibits favorable pharmacokinetic and pharmacodynamic profiles with evidence of target inhibition in surrogate tissues. Clinical and pharmacodynamic data support an oral once daily administration at 800 mg. Brivanib shows promising activity as single agent in hepatocellular carcinoma and in combination with cetuximab in colorectal cancer. Further evaluations with cytotoxic chemotherapy and in other solid tumors are currently ongoing.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Alanine / analogs & derivatives*
  • Alanine / pharmacology
  • Alanine / therapeutic use
  • Angiogenesis Inhibitors / pharmacology
  • Angiogenesis Inhibitors / therapeutic use
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use*
  • Clinical Trials as Topic
  • Drug Screening Assays, Antitumor
  • Humans
  • Neoplasms / drug therapy*
  • Pyrroles / pharmacology*
  • Pyrroles / therapeutic use*
  • Receptor, Fibroblast Growth Factor, Type 1 / antagonists & inhibitors
  • Triazines / pharmacology*
  • Triazines / therapeutic use*
  • Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors

Substances

  • Angiogenesis Inhibitors
  • Antineoplastic Agents
  • Pyrroles
  • Triazines
  • brivanib
  • Receptor, Fibroblast Growth Factor, Type 1
  • Vascular Endothelial Growth Factor Receptor-2
  • Alanine