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Radionuclides

Lutetium-177

SpectronRx and its partner Global Morpho Pharma understand current reactor and future accelerator production associated with GMP Lu 177 nca. Our success will ensure your sustained growth, availability and future clinical expansion of GMP Lu 177 nca-labeled radiotheranostics.


Lu 177 is a reactor-produced radionuclide that can be obtained via two different routes, one based on irradiation of natural Lutetium-176 [natLu or 176Lu(n,γ)177Lu], the direct route, the other on Ytterbium-176 [176Yb(n,γ)177Yb→177Lu], the indirect route (half-life of the intermediate 177Yb: 1.9h). The two different routes correspond to two different qualities of lutetium. The indirect route provides high specific activity 177Lu (also called nca – non-carrier added) which will allow the manufacturing of higher quality and even carrier-free radiolabeled drugs. The direct route does not allow separation of 177Lu from 176Lu and the use of this radionuclide can have some limitations (e.g., antibody labeling).



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Actinium-225

Actinium 225 is a radioactive element with a half-life of 9.91 days emitting alpha particles with emissions at 5,830 keV and 5,792 keV. It decays first into Francium 221, then successively in Astatine-217, Bismuth 213, Thallium 209 and Lead 209 before leading to the stable Bismuth 209. Actinium 225 is the parent radionuclide of Bismuth 213 in the 225Ac/213Bi generator. Its maximum specific activity is 58,000 Ci/g.


There are six ways possible to produce Ac 225:


1)… Ac 225 has historically been produced at an annual volume of between 600 and 800 mCi through the natural decay of Thorium-229 (half-life 7,340 years).


2)… The neutron irradiation of Ra 226 is another production route but leads to a mixture of Th 229 (half-life 7,340 years) and Th 228 (half-life 1.9 years).


3)… Cyclotron production is possible by irradiating Ra 226 targets via [226Ra(p,2n)225Ac] at about 15 MeV, but is cumbersome.


4)… Another method starts from Thorium-232 [232Th(p,x)225Ac] but needs at least 100 MeV accelerators which are currently only available at BNL (USA), LANL (USA) or INR (Russia).


5)… The use of linear accelerators is presently under final stage evaluation and Ac 225 production needs accelerator produced 15 MeV deuterium beams and is based on the route [226Ra(d,3n)225Ac].


6)… The most recent technology is based on the use of Rhodotron, an electron accelerator that generates gamma and X rays close to the target which can transform Ra 226 in Ac 225 through the reaction [226Ra(γ,n)225Ac]. It has a potential to generate as much Ac 225 as a linear accelerator. The first prototype is under construction.


SpectronRx and their partner GLOBAL MORPHO PHARMA understand all current and future production associated with Ac 225. Our combined success will ensure sustained growth and future expansion of Ac 225-labeled radiopharmaceuticals for the benefit of the cancer patient.

Iodine-131

“Radioactive iodine has been, in various forms, the mainstay of Nuclear Medicine. Iodine-123 is the most widely used iodine isotope for single photon imaging. Iodine-125 continues to be used in diverse applications from in vitro radio-assay to in vivo estimation of various pathophysiologic correlates. Iodine-131 (131I), useful for imaging as well as therapy, has contributed more than any other radionuclide to the growth and sustenance of Nuclear Medicine”


The use of all members of this Iodine group (I-123, I-124, I-131) for molecular imaging of biochemical and physiological processes in vivo will continue to evolve into an important diagnostic tool in modern nuclear medicine and medical research. Positron emission tomography (PET) is currently the most sophisticated molecular imaging methodology.


There are numerous advantages of I-124 with a longer half-life (4.2 days) Moderate (23%) PET (511kev) and gamma ray abundance (90%). Making it ideal for both imaging, monoclonal antibody labeling and therapeutic applications.

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Yttrium-90

Yttrium-90, a radioactive isotope, is used in treatments for various cancers and is used in precision medical needles to sever pain-transmitting nerves in the spinal cord.


Yttrium oxide is the most important compound of yttrium. It is used to make the high-temperature superconductor YBCO (yttrium barium copper oxide). This substance becomes superconducting at -178 oC (meaning that it can be kept in a superconducting state using liquid nitrogen, rather than more expensive and more difficult to handle liquid helium).


Yttrium oxide is also used to make yttrium iron garnets (Y3 Fe5O12) which are very effective microwave filters, blocking some microwave frequencies, while allowing others through in communication devices such as satellites.


Yttrium doped with europium is used to produce phosphors, which provide the red color in color television tubes.

Copper-67

Copper comprises two stable isotopes, 63Cu and 65Cu, and 3 secondary radioisotopes for molecular imaging applications with Cu64 the most popular in research and clinical use. Copper is also used in targeted radiation therapy using 67Cu.


The bio- chemical compounding flexibility of copper allows for a wide variety of chelators, joining systems that can potentially be linked to peptides and other biologically relevant small molecules, antibodies, and proteins. The 12.7-hours half-life of Cu-64 provides the flexibility to image both smaller molecules and larger, slower clearing proteins and nanoparticles.

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Other diagnostic isotopes:

Zirconium-89

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Antibody based PET imaging (Immuno-PET) is showing increasing importance in the visualization of molecular heterogeneity of tumors and associated lesions. Zr-89 has the ideal physical and chemical properties for a variety of conjugation strategies. When compared to I-124 our shipping and shielding requirements will be less. This isotope is produced at our South Bend facility.

Gallium-68

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Gallium 68 (68Ga) is a generator-produced or cyclotron-produced radionuclide for PET imaging with a half-life of 67.7 min. The β+ is emitted at 1,899 keV (88%, average energy 500 keV), followed by annihilation producing two gamma rays at 511 keV. The decay product is the stable 68Zn (100%). Contrary to 18F which can be linked to organic molecules via a covalent bond, 68Ga is a metal and needs a chelating moiety to be attached to the vector.

Fluorine-18

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Accurate diagnosis and staging are essential for the optimal management of cancer patients. The profile of 18F (short half-life, low energy) makes it ideal for imaging. 18F can be bound covalently to any organic molecule and some new chemical procedures have been developed to allow a very fast coupling chemistry with high yields, or to improve large molecule and antibody labeling (aluminum fluorine complexes) or even to perform this chemistry in aqueous media. 

Targeted therapies with leutetium:

Movie on the application of radiolabeled peptides for targeted therapy; 177Lu-DOTA-octreotate emits gamma and beta particle radiation, the peptide molecules bind somatostatin receptors on tumor cells and can be applied for both tumor imaging and radionuclide therapy.

Actinium-225 in Medicine:

How Does Targeted Alpha Therapy Work?