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Strategies for TGF-beta modulation: a review of recent patents
Dominique Bonafoux1, Wen-Cherng Lee
1Abbott Laboratories, Medicinal Chemistry, Worcester, Massachusetts 01605-2323, USA. dominique.bonafoux@abbott.com
Background:
TGF-beta has been identified as a key factor in the progression of various diseases, in particular cancer and fibrosis. The signaling of TGF-beta can be modulated through three distinct strategies: using antisense nucleotides that block TGF-beta mRNA (trabedersen (AP 12009)), using monoclonal antibodies to block TGF-beta isoforms (lerdelimumab, metelimumab) or using small molecule inhibitors of the TGF-beta receptor 1 (TGF-betaR1 or ALK-5).
Objective:
This review focuses on small molecules and summarizes the most recent TGF-betaR1 inhibitors reported in the patent literature.
Methods:
We searched and analyzed the patent literature claiming chemical matter for TGF-betaR1 inhibition from the 1(st) of January 2005 to the 1(st) of January 2009.
Results/Conclusions:
The inhibition of TGF-beta has recently been clinically validated with antisense nucleotide trabedersen. Small molecules inhibitors of TGF-betaR1 that are now in Phase I clinical trials and in preclinical stage are, therefore, of high interest and could provide a more versatile route to TGF-beta modulation through oral dosing while maintaining the same therapeutic benefits.
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