Abstract
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.
Highlights
A growing interest in the development of theranostics and “personalised medicine” highlights the utility of dual-functional theranostic compounds, which combine diagnostic and therapeutic modalities within the same agent, for the treatment of neoplastic conditions
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)
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 tumours
Summary
A growing interest in the development of theranostics and “personalised medicine” highlights the utility of dual-functional theranostic compounds, which combine diagnostic and therapeutic modalities within the same agent, for the treatment of neoplastic conditions. 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.
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