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Drug platforms

Transglutaminase (TGM)-mediated synthesis of antibody-drug conjugates (ADCs)

In vitro and rodent studies suggest conjugating chemotherapeutics to engineered glutamine residues could improve the in vivo pharmacokinetics of ADCs. mAbs against three common tumor targets were engineered with recognition sites for Streptoverticillium mobaraense tgm and conjugated to a tubulin inhibitor. In mouse and rat tumor models, the best of these glutamine-conjugated ADCs had similar potency but better stability and pharmacokinetics compared with conventional cysteine-conjugated ADCs. Next steps could include optimizing the engineered conjugation target sites for therapeutic mAbs.

SciBX 6(12); doi:10.1038/scibx.2013.300
Published online March 28, 2013

Patent pending; licensing status undisclosed

Strop, P. et al. Chem. Biol.; published online Feb. 21, 2013;
Contact: Arvind Rajpa, Rinat-Pfizer, South San Francisco, Calif.
Contact: Pavel Strop, same affiliation as above