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Development of PDT/PET theranostics: synthesis and biological evaluation of an ¹⁸F-radiolabeled water soluble porphyrin

Entract, Guy M.; Bryden, Francesca; Domarkas, Juozas; Savoie, Huguette; Allott, Louis; Archibald, Stephen J.; Cawthorne, Chris; Boyle, Ross W.


Guy M. Entract

Francesca Bryden

Juozas Domarkas

Huguette Savoie

Louis Allott

Chris Cawthorne


Synthesis of the first water-soluble porphyrin radiolabeled with fluorine-18 is described: a new molecular theranostic agent which integrates the therapeutic selectivity of photodynamic therapy (PDT) with the imaging efficacy of positron emission tomography (PET). Generation of the theranostic was carried out through the conjugation of a cationic water-soluble porphyrin bearing an azide functionality to a fluorine-18 radiolabeled prosthetic bearing an alkyne functionality through click conjugation, with excellent yields obtained in both cold and hot synthesis. Biological evaluation of the synthesized structures shows the first example of an 18 F-radiolabeled porphyrin retaining photocytotoxicity following radiolabeling and demonstrable conjugate uptake and potential application as a radiotracer in vivo. The promising results gained from biological evaluation demonstrate the potential of this structure as a clinically relevant theranostic agent, offering exciting possibilities for the simultaneous imaging and photodynamic treatment of tumors.


Entract, G. M., Bryden, F., Domarkas, J., Savoie, H., Allott, L., Archibald, S. J., …Boyle, R. W. (2015). Development of PDT/PET theranostics: synthesis and biological evaluation of an ¹⁸F-radiolabeled water soluble porphyrin. Molecular pharmaceutics, 12(12), 4414-4423.

Journal Article Type Article
Acceptance Date Nov 11, 2015
Online Publication Date Nov 11, 2015
Publication Date Dec 7, 2015
Deposit Date Dec 17, 2015
Publicly Available Date Dec 17, 2015
Journal Molecular pharmaceutics
Print ISSN 1543-8384
Electronic ISSN 1543-8392
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 12
Issue 12
Pages 4414-4423
Keywords Flourine-18, PET imaging, Photodynamic therapy, Porphyrins, Theranostics
Public URL
Publisher URL
Additional Information This document is the Accepted Manuscript version of a Published Work that appeared in final form in Molecular pharmaceutics, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see


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