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Methods of synthesis and use of radiolabelled platinum chemotherapeutic agents
| Details |
Inventors: Smith, Suzanne V.;
Assignee: Australian Nuclear Science & Technology Organisation (New South Wales, AU)
Primary Examiner: Jones; Dameron L.
Assistant Examiner:
Attorney, Agent or Firm: Banner & Witcoff, Ltd.
There is provided a method of synthesis of a radiolabelled platinum chemotherapeutic agent comprising the steps of: converting a metal halide to a radiolabelled platinum halide wherein the radiolabel is a radioisotope of Pt; and synthesizing the radiolabelled platinum chemotherapeutic agent from the radiolabelled platinum halide. |
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DETAILED DESCRIPTION OF THE INVENTION Usually, in the method of synthesis of the radiolabelled platinum chemotherapeutic agent the step of converting the metal halide into a radiolabelled platinum halide is carried out in a nuclear reactor or a cyclotron.
Typically this conversion step is carried out by irradiation with neutrons in a nuclear reactor.
The radiolabelled platinum halide may be a Pt(II) halide or a Pt(IV) halide.
More typically, the present invention involves irradiating a Pt(II) halide, even more typically PtCl.
sub.
2, with neutrons in a nuclear reactor.
Alternatively, the metal halide may be the halide of a metal such as gold, iridium, etc.
which can be converted into platinum by bombardment with protons, deuterons, alpha particles or other species in a cyclotron.
In a typical embodiment, the radiolabelled platinum halide is a Pt(II) halide which is converted to cisplatin or carboplatin.
The platinum radioisotope in the synthetic method of the first or second embodiments is typically selected from the group consisting of .
sup.
195mPt, .
sup.
197mPt, .
sup.
197Pt, .
sup.
191Pt, .
sup.
193mPt and mixtures thereof.
Still more typically, the radioisotope is .
sup.
195mPt or .
sup.
193mPt.
Yet still more typically, the radioisotope is .
sup.
195mPt.
The radioisotopes of platinum may be prepared by methods which are generally known in the art.
For example, radioactive halides of platinum which incorporate .
sup.
193mPt, .
sup.
195mPt or .
sup.
197Pt may be prepared by irradiating a halide of .
sup.
192Pt, .
sup.
194Pt and .
sup.
196Pt, respectively (in oxidation state II or IV) with neutrons in a nuclear reactor.
It will appreciated that the irradiation time to achieve a predetermined specific activity will be dependent on the nuclear reactor flux.
Those versed in the art will readily determine the appropriate irradiation time for a given facility's flux.
It will be appreciated that when the platinum chemotherapeutic agent is a Pt(IV) species, the method of the present invention will usually include the steps of converting a metal halide to a radiolabelled Pt(IV) halide and synthesising the radiolabelled platinum chemotherapeutic agent from the radio label led Pt(IV) halide
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Gene Therapy 
