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Bicyclic peptides conjugated to an albumin-binding peptide to extend serum half-life

A study in mice suggests conjugating bicyclic peptides to an albumin-binding peptide could increase therapeutic duration. In mice, a bicyclic peptide targeting urokinase-type plasminogen activator (PLAU; uPA) conjugated to an albumin-binding peptide had an elimination half-life of about 24 hours, which was 50-fold longer than that of the parent molecule. The conjugated compound and parent molecule had similar levels of activity. Next steps include testing the conjugated bicyclic peptide in a mouse model of cancer and applying the conjugation strategy to additional bicyclic peptides.

SciBX 5(45); doi:10.1038/scibx.2012.1191
Published online Nov. 15, 2012

Bicyclic peptide technology is patented; licensed to Bicycle Therapeutics Ltd.

Angelini, A. et al. J. Med. Chem.; published online Oct. 22, 2012;
doi:10.1021/jm301276e
Contact: Christian Heinis, Swiss Federal Institute of Technology Lausanne, Lausanne, Switzerland
e-mail:

christian.heinis@epfl.ch