1. Tumor hypoxia is associated with
aggressive phenotypes, notably influencing angiogenesis, metastasis, and response
to therapy. Therefore, the ability to identify hypoxia could allow stratification
for optimized therapy.
2. MRI methods have been developed
to quantify pO2, and hence tumor hypoxia, or provide pertinent surrogate
biomarkers.
3. This presentation will consider
opportunities and applications in the context of competing technologies.
4. Virtues and shortcomings of diverse techniques
will be considered in terms of ease of implementation, nature of observations
(spatial resolution, precision, dynamics, and need for exogenous reporter
agents) and validity and robustness of measurements.
5. Examples will be drawn from
pre-clinical studies of mice and rats, focusing on our own experience. I will indicate
potential for translation to man.
There
is increasing evidence for the importance of tumor oxygenation in development,
progression, and response to therapy. Consequently, many techniques have been
developed to assess tumor oxygenation, as reviewed extensively (1-3). Methods may provide
a qualitative impression of oxygenation status or rigorous quantitation.
Techniques vary in spatial and temporal resolution and the ability to assess
dynamic changes. Some exploit endogenous molecules or physical characteristics,
while many apply reporter molecules to interrogate oxygen tension (pO
).
This tutorial will focus on magnetic resonance approaches, but place them in
the context of competing modalities.
It
has long been appreciated that hypoxic tumor cells are relatively resistant to
radiotherapy (4). A threefold increase in radio resistance may
occur when cells are irradiated under hypoxic conditions compared with pO
> 15 Torr for a single radiation dose. However, modeling indicates that the
proportion of cells in the range 0 - 20 Torr may be most significant in terms
of surviving a course of fractionated radiotherapy (5). Recently, there is much evidence that hypoxia
is associated with a more aggressive phenotype. Notably, low pO
measurements
in tumors using electrodes at many disease sites in patients have been associated
with poor prognosis (6, 7). Electrode
measurements are highly invasive, sample limited regions and are generally not suitable
for evaluating dynamic response to interventions. Several nuclear medicine
reporters have been used with PET (
F-misonidazole), but these introduce the expense and technical
challenges associated with radioactivity. Immunohistochemistry (IHC), based on
biopsies has also been used to stratify patients for modified radiotherapy
paradigms (ARCON), but it is invasive and precludes repeat measurements from
individual areas (8). Thus, we actively search for non-invasive
procedures allowing repeat measurements representing the whole tumor.
may be
measured directly using physical interactions between oxygen and reporter
molecules. The most popular quantitative approach has exploited the
oxygen-dependent
F NMR spin lattice relaxation rate (R1=1/T1)
of perfluorocarbons (PFCs) (9). A linear
dependence R
is observed due to the ideal gas-liquid
interaction of paramagnetic molecular oxygen (O
) dissolving in PFC.
PFCs essentially act as molecular amplifiers, since the solubility of
oxygen is greater than in water, but thermodynamics require that the pO
in the PFC rapidly equilibrates with the surrounding medium. Importantly, ions
do not enter the hydrophobic PFC phase, and thus, do not affect the bulk
relaxation. Early studies focused on perfluorotributylamine (PFTB) and
perfluorooctylbromide (PFOB) (10) and these were
widely exploited for spectroscopy. However, multiple resonances can lead to
chemical shift artifacts in images, requiring more sophisticated imaging
approaches, which often sacrifice signal. Therefore, perfluoro-15-crown-5-ether
(15C5) and hexafluorobenzene (HFB), are preferable since each exhibits a single
F resonance, hence maximizing SNR (9).
PFCs are extremely hydrophobic, but may
be formulated as biocompatible emulsions for IV administration. Shortly after
administration, PFC in the blood provides measurements of vascular pO
(11), but clearance
occurs within 1 to 2 days leading to extensive accumulation in the liver,
spleen, and bone marrow, providing unique insight into these organs (12).
Limited material does accumulate in other organs and oximetry has been reported
with respect to myocardial ischemia (13). Accumulation in
tumors occurs predominantly in regions of greater perfusion, often tumor
periphery, potentially biasing measurements (14). Some PFCs show extended
tissue retention allowing chronic studies during tumor development; progressive
tumor hypoxiation has been observed over extended periods of many days (14, 15).
It has been shown that stem cells may be loaded in vitro with PFC allowing subsequent cell tracking
with the potential for local
oximetry (16).
Direct
intratumoral (IT) injection of neat PFC allows any region of interest to be
interrogated immediately and avoids reticuloendothelial uptake and bias towards
well perfused tumor regions. A fine gauge needle ensures minimal tissue damage
and provides measurements closely analogous to electrodes or fiber optic probes
(17). We favor hexafluorobenzene (HFB) as a
pO
, yet is minimally
responsive to temperature (18). Typically 50 – 100 µl are introduced across the tumor to ensure
that multiple regions are sampled. Recognizing that tumors are heterogeneous
and that pO
may fluctuate, we developed an imaging procedure [FREDOM (Fluorocarbon
Relaxometry using Echo planar imaging for Dynamic Oxygen Mapping)],
which allows repeated quantitative measurements of regional pO
(typically,
50-150 voxels with 1.25 mm in plane resolution) simultaneously in 6.5 mins with
a precision of 1-3 Torr, when pO
is in the range 0-15 Torr (17). It should be noted that pO
may be presented at Torr, which is equivalent to mmHg, or sometimes as %atmosphere,
where 760 Torr = 1 atm. At 37
reaches 12 s under anoxic conditions.
To avoid excessive experimental acquisition time we favor pulse burst
saturation recovery (PBSR) echo planar imaging (EPI) relaxometry. Traditional T
measurement sequences acquire data with delays in monotonic order, whereas we
alternate longer and shorter delays to minimize any systematic errors, which
would be introduced, if the signal amplitude varies during the measurement
(
Alternated Relaxation Delays with Variable Acquisitions to Reduce
Clearance effects) (17). Gallez
maps within
90 s based on a Look-Locker (SNAP-IR) approach (19) allowing spontaneous
fluctuations in tumor oxygenation to be observed (20).
The
most powerful aspect of
is the
ability to follow the fate of individual tissue regions of interest (voxels)
with respect to interventions (
.,
Fig. 1). Most extensive investigations have focused on the response to
respiratory challenge, often comparing the effects of oxygen (O
)
versus carbogen (CB) gas breathing (2, 21-23). Most significantly, it has been shown that the
ability to modulate pO
correlated with tumor growth delay accompanying single high dose
irradiation (24, 25). Other studies have examined
response to vascular disrupting agents (VDAs) such as Combretastatin
(CA4P) and OXi8007 revealing rapid hypoxiation of rat breast tumors (26, 27). Arsenic trioxide (ATO) has been described as a
VDA (28), but Diepart
. unexpectedly found increased pO
within 30-90
minutes (depending on tumor type) of a relatively low dose (5 mg/kg) and
demonstrated that this followed mitochondrial impairment (29). We believe that quantitative PFC oximetry
provides a valuable pre-clinical tool and may serve as a benchmark to calibrate
non-invasive observations such as BOLD and
(a multi-parametric MR based
technique) described below. We recognize that
F remains quite
esoteric on clinical scanners and thus proton MRI methods are preferable.
F MRI oximetry the proton analog of HFB, hexamethyldisiloxane
(HMDSO), has been used for
H MRI oximetry. Like HFB, HMDSO is
highly hydrophobic giving high gas solubility, and hence strong R
. Symmetry provides a single proton
resonance (δ = 0 ppm), which is well removed from water and fat allowing
dynamic maps of tumor oxygenation to be achieved with respect to hyperoxic gas
breathing challenge using
(Proton Imaging of Siloxanes to map Tissue
Oxygenation Levels) (30).
., percentage measurements < 5 Torr). Hypoxia may also be
assessed directly by analysis with PET and IHC approaches based on
nitroimidazole trapping. Several
., hexafluoromisonidazole
(CCI-103F), EF5, NLTQ-1,
SR-4554, and Ro 07-0741). Variants have also been generated
as
H MR reporters both for spectroscopy (31) and imaging (32). Indeed the retention of GdDO3NI matched the pattern of
oxygenation expected in Dunning prostate R3327-AT1 tumors based on extensive
previous
F oximetry imaging (32). Assessment of hypoxia is
predicated on uptake and trapping of the reporter, assessed as the relative
signal at various times (retention index) or based on the relative signals from
tumor and surrounding control tissues. Weak
F signals generally
restrict measurements to a global value across the whole tumor. Trapping may
also depend on expression of nitroreductases and be influenced by glutathione (33). Likewise, tumor perfusion
may influence access of the agents to tumor tissue, particularly poorly
perfused regions, which are expected to be hypoxic. Indeed, uptake of hypoxia reporters
following administration of vascular disrupting agents, did not match hypoxia, presumably
because access was hindered to the very regions which became hypoxic (34)
Imaging per se is non-invasive and it would be
particularly attractive to develop oximetry methods based on properties of
endogenous molecules, rather than requiring administration of reporter agents.
Lactate concentration has been associated with hypoxia as consistent with impaired
oxidative phosphorylation and accelerated glycolysis, though many factors may influence
this phenotype (35).
Beyond pre-clinical investigations, it is noteworthy that BOLD, TOLD,
and MOBILE MRI have been successfully applied in studies of normal human
volunteers and patients enrolled in trials with respect to cancer in various
disease sites including
breast, cervix, prostate and brain (46, 53, 55-62). It remains to be seen which parameter is most useful in
identifying patients to characterize tumors for optimal therapy. Quantitative
F
oximetry is a valuable pre-clinical tool and continues to serve as a validation
for less invasive approaches, but is likely impractical in man due to the
sparse availability of clinical 19F MRI and need for approval of
contrast agents. BOLD and TOLD are being evaluated in patients. The enhanced
oxygen sensitivity of
are
very promising though their general applicability remains to be evaluated. Today,
there are many therapeutic options, but prognostic imaging with respect to
hypoxia remains a work-in progress. The radiation oncology community recognizes
the need to routinely measure tumor oxygenation, as part of precision medicine;
ultimately, MR oximetry methods should provide evidence based choice of therapy
including radiation dose painting, heavy ion beam or application of hypoxic
cell selective cytotoxins.
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