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Figure 9.9 [68Ga]Ga-PSMA-11 PET images at baseline (left) and three months after [
treatment of eight patients. Any disease with SUVmax >3 is shown in red. PSA values are given below each
scan. SNMMI Image of the Year 2018. Source:SNMMI.
177
Lu]Lu-PSMA-617
The clinical demand for PSMA-targeted tracers is high, and 68Ga derivatives are desirable because of the accessibility of the generator-produced isotope and the potential for
production in existing radiopharmacies, especially with the development of a single-vial
room temperature kit. However, development in technology is moving rapidly, with other
68
Ga and 18F derivatives (and even radiohybrids) being developed simultaneously which
are likely to be viable alternatives to those presented here[128–130, 155–157].
99m
Tc d eriv-
atives, although inferior, are still likely to be used in lower/middle income countries that
have limited isotope and PET scanner access[158–160].
68
Ga radiopharmaceuticals have driven PET imaging forward and paved the way to exploit
the huge potential of RLT. The longstanding promise of more personalized treatments
and treatment stratication based on molecular imaging is now being realized. The pio-
neering path has been trodden by imaging NETs with targeting of SSTRs, demonstrating
that accessible and routine imaging is possible, with the appetite for the new generation
Chapter 9: Labeling withGallium-68 315
of PSMA-targeted agents even greater. The development of further applications of 68Ga
radiopharmaceuticals is a highly active and fast-paced area, with many in clinical trials and
most accompanied by a
likely see a signicant increase in global use, utilizing a wider range of radiopharmaceuticals that are produced by simplied methods, mirroring technetium-99m.
177
Lu therapeutic sister product. The future of clinical 68Ga will
The half-life of 68Ga generally means radiopharmaceuticals must be produced on-site (and
often for a single patient). However, the advent of simple kit radiolabeling, cyclotronproduced isotope, and a tracer with sucient clinical demand makes it viable for distribution. A central location in a large metropolitan area could easily be used to serve multiple
local hospitals. However, the dosimetry concerns for high-energy positron emitters
are signicantly exacerbated by increased activities resulting from cyclotron-produced
activity, and this has to be taken into account to reduce operator doses when carrying out
kit-based radiosyntheses. Once some of the key issues around kits have been resolved
and optimal usage patterns established with regulators (combined with competition
driving cost-eectiveness), the various models will be established for dierent types of
centers. This will likely encompass centers that use solid targets for distribution, those
that use solution targets for on-site supply of a range of gallium (and other) PET tracers,
and dedicated gallium-68 radiopharmacies using generators. In all of these models, there
is still a drive for better understanding of chelator use both for tracer design and to opti-
mize labeling chemistry.
A xed library of chelators are likely to be used in the future (particularly if the chelator is not subject to intellectual property). The relationship between linkers, chelator
properties, and peptide will be used to predict and select combinations for optimal bio-
distribution[161, 162]. The baseline understanding of the key chemical parameters and
limitations on reactivity has been rapidly developed in recent years to give specic radio-
chemical knowledge for gallium-68 complex formation. Once this picture is complete, the
development of the next-generation tracers will be streamlined.
There are still signicant opportunities for new technologies in both the simplication
of new tracer development and the optimization of chemical labeling protocols. Microuidic / lab-on-a-chip technology is ideal for radiochemical applications as chemical
eciency of the reaction is increased (mainly due to the high surface area of the chan-
nels), which can allow reactions to be driven to completion with lower amounts of
316 Handbook of Radiopharmaceuticals
precursor, reduce labeling times, and/or reduce the temperature required[16, 163].
There has been a growing body of research applying this to radiometal reactions[16,
164, 165]. Multi-step processes can be incorporated into microuidic chips; and, perhaps
most importantly for
68
Ga tracers, there is the potential to miniaturize quality-control
processes to also automate and reduce infrastructure requirements for this step. Disposable single-use devices can be developed from plastics and provide a good t with more
stringent regulatory requirements. Microuidic chips have been developed to optimize
key chemical processes such as click chemistry reactions with chelators[166]. Other innovative ways to increase chemical eciency include emulsion-based labeling, which relies
on the concentration of the reagents and orientation of substrates at the micellar surface
to improve yields and reaction rates[167]. Specic chemical reactions and novel tracers
are also being developed that improve currently used protocols and extend the use of
gallium-68 to new applications.
There has been an increase in interest in imaging with antibody-based radioimmunotherapeutic agents, which are usually radiolabeled using isotopes with a longer half-life,
particularly
89
Zr. The rise of 68Ga use clinically may provide a more readily available
source of isotope for PET antibody imaging by exploiting pre-targeted biorthogonal in
vivo click to circumvent the disparity between their respective physical and biological
half-lives[168]. The concept of a radiohybrid, introduced by Wester and coworkers, is
an innovative way of maintaining identical properties with dierent isotope use. They
have produced a molecular structure to target PSMA that incorporates both uorine
and gallium atoms, where the tracer can be labeled with either uorine-18 or gallium-68
(with the other element present in its stable form)[156, 169]. This concept is likely to be
extended and could improve consistency in the interpretation of PET scans with dierent
isotopes. It also links well to opportunities in the use of therapeutic isotopes.
There is a desire for radioisotope therapies utilizing the same peptide precursor as 68Ga
for imaging (including dosimetry planning), switching, for example, to
(e.g. NETSPOT and LUTATHERA); however, this approach is not currently compatible
with the move toward single-vial room temperature
consideration, and there are opposing viewpoints. If
68
Ga kits. This point needs careful
68
Ga imaging is used for staging,
target identication, and therapy monitoring, then an alternate agent can be used for
therapy. There is interest in using
68
Ga agents to calculate personalized
etry, although the disparity in half-lives makes it inherently challenging, and as yet, the
clinical benet of this process is not well established (and the cost may be prohibitive
for routine use). A key issue is the assumption that
68
Ga and
177
Lu radiolabeled versions
of the same precursor have the same biodistribution and uptake in tumors, which is
unveried[170, 171], and these parameters may not be suciently similar for accurate
personalized dosimetry. If personalized dosimetry is important for successful (and even
curative) RLT, as has been suggested recently[172, 173], and the related
available or suitable, the
68
Ga radiopharmaceutical used for imaging could be selected
177
Lu for therapy
177
Lu lesion dosim-
68
Ga agent is not
Chapter 9: Labeling withGallium-68 317
on cost, production simplicity, and imaging characteristics. This could potentially be followed by (or used simultaneously with) low-dose
177
Lu SPECT imaging for accurate dosimetry calculations prior to RLT. It is also worth noting that, whilst the main current interest
is in the theranostic pairing of
advantageous, with
225
Ac being the current leading candidate[174–176].
68
Ga with
177
Lu, the use of alpha-emitting isotopes may be
The authors would like to thank representatives of the following companies for their
engagement during the writing of this chapter: Eckert and Ziegler (Germany), IRE ELiT
(Belgium), iThemba Labs (South Africa), Imaging Equipment Ltd. (UK), Telix Pharmaceuticals (Australia), Isotopia (Israel), Theragnostics (UK), and Curium Pharma (France). Other
companies were approached for comment. The authors would also like to thank Stefano
Boschi (University of Bologna, Italy) for his valuable and interesting conversations.
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Chapter 9: Labeling withGallium-68 323
