Metastron (89SrCl2) is a
radiopharmaceutical currently used for bone pain palliation in
several countries since the long half-life of 89Sr
(50.5 days) favors wider distribution than other radioisotopes
approved for this application, which have shorter half-lives.
Strontium-89 is not ideal for bone pain palliation due to its
high energy β− particle emission [Eβ(max)=1.49
MeV] and is also difficult to produce in large quantities. A
170Tm [T1/2=128.4 days, Eβ(max)=968
keV, Eγ=84 keV (3.26%)]-based
radiopharmaceutical for bone pain palliation could offer
significant advantages over that of 89Sr. The present
study constitutes the first report of the preparation of a
170Tm-based agent, 170Tm-ethylenediaminetetramethylene
phosphonic acid (EDTMP), and its preliminary biological
evaluation in animal models.
Methods: 170Tm was produced
by thermal neutron bombardment on natural Tm2O3
target for a period of 60 days at a flux of 6×1013
neutrons/cm2.s. 170Tm-EDTMP complex was
prepared at room temperature. Biodistribution and scintigraphic
imaging studies with 170Tm-EDTMP complex were
performed in normal Wistar rats. Preliminary dosimetric
estimation was made using the data to adjudge the suitability of
170Tm-EDTMP for bone pain palliation.
Results: 170Tm was produced
with a specific activity of 6.36 GBq/mg and radionuclidic purity
of 100%. The 170Tm-EDTMP was prepared with high
radiochemical purity (>99%)
and the complex exhibited satisfactory in vitro stability.
Biodistribution and imaging studies showed good skeletal
accumulation (50–55% of the injected activity) with
insignificant uptake in any other vital organ/tissue. Activity
was observed to be retained in skeleton until 60 days
post-injection demonstrating that 170Tm-EDTMP
exhibits good bone-seeking properties with long retention. It is
predicted that a dose of ~0.5
μGy/MBq is accrued to red bone marrow and 4.3 Gy/MBq is
delivered to the skeleton.
Conclusion: 170Tm-EDTMP
shows promising biodistribution features, encouraging dosimetric
values and warrants further investigation in order to develop it
as a bone pain palliative radiopharmaceutical. Despite the
relatively long half-life (128.4 days) of 170Tm,
170Tm-EDTMP could be explored as a cost-effective
alternative to 89SrCl2.
|