The¹⁸⁸Re radioisotope represents a useful radioisotope for the preparation of radiopharmaceuticals for therapeutic applications, particularly because of its favorable nuclear properties. The nuclide decay pattern is through the emission of a principle beta particle having 2.12 MeV maximum energy, which is enough to penetrate and destroy abnormal tissues, and principle gamma rays (Eγ=155 keV), which can efficiently be used for imaging and calculations of radiation dose.¹⁸⁸Re may be conveniently produced by¹⁸⁸W/¹⁸⁸Re generator systems. The challenges related to the double neutron capture reaction route to provide only modest yield of the parent¹⁸⁸W radionuclide indeed have been one of the major issues about the use of¹⁸⁸Re in nuclear medicine. Since the specific activity of¹⁸⁸W used in the generator is relatively low (<185 GBq/g), the elutedRe188O4-can have a low radioactive concentration, often ineffective for radiopharmaceutical preparation. However, several efficient postelution concentration techniques have been developed, which yield clinically usefulRe188O4-solutions. This review summarizes the technologies developed for the preparation of¹⁸⁸W/¹⁸⁸Re generators, postelution concentration of the¹⁸⁸Re perrhenate eluate, and a brief discussion of new chemical strategies available for the very high yield preparation of¹⁸⁸Re radiopharmaceuticals.

The widespread availability of novel radioactive isotopes showing nuclear characteristics suitable for diagnostic and therapeutic applications in nuclear medicine (NM) has experienced a great development in the last years, particularly as a result of key advancements of cyclotron-based radioisotope production technologies. At Legnaro National Laboratories of the National Institute of Nuclear Physics (LNL-INFN), Italy, a 70-MeV high current cyclotron has been recently installed. This cyclotron will be dedicated not only to pursuing fundamental nuclear physics studies, but also to research related to other scientific fields with an emphasis on medical applications. LARAMED project was established a few years ago at LNL-INFN as a new research line aimed at exploiting the scientific power of nuclear physics for developing innovative applications to medicine. The goal of this program is to elect LNL as a worldwide recognized hub for the development of production methods of novel medical radionuclides, still unavailable for the scientific and clinical community. Although the research facility is yet to become fully operative, the LARAMED team has already started working on the cyclotron production of conventional medical radionuclides, such as Tc-99m, and on emerging radionuclides of high potential medical interest, such as Cu-67, Sc-47, and Mn-52.

The synthesis of a Zn(II)–phthalocyanine derivative bearing four ¹⁰B-enriched o-carboranyl units (¹⁰B-ZnB₄Pc) and its natural isotopic abundance analogue (ZnB₄Pc) in the peripheral positions of the tetraazaisoindole macrocycle is presented. The photophysical properties of ZnB₄Pc, as tested against model biological systems, were found to be similar with those typical of other photodynamically active porphyrin-type photosensitisers, including a singlet oxygen quantum yield of 0.67. The carboranyl-carrying phthalocyanine was efficiently accumulated by B16F1 melanotic melanoma cells in vitro, appeared to be partitioned in at least some subcellular organelles and, upon red light irradiation, induced extensive cell mortality. Moreover, ZnB₄Pc, once i.v.-injected to C57BL/6 mice bearing a subcutaneously transplanted pigmented melanoma, photosensitised an important tumour response, provided that the irradiation at 600–700 nm was performed 3 h after the phthalocyanine administration, when appreciable concentrations of ZnB₄Pc were still present in the serum. Analogously, irradiation of the ¹⁰B-ZnB₄Pc-loaded pigmented melanoma with thermal neutrons 24 h after injection led to a 4 day delay in tumour growth as compared with control untreated mice. These results open the possibility to use one chemical compound as both a photosensitising and a radiosensitising agent for the treatment of tumours by the combined application of photodynamic therapy and boron neutron capture therapy.