Tumour targeting with radiometals for diagnosis and therapy

Abstract

Use of radiometals in nuclear oncology is a rapidly growing field and encompasses a broad spectrum of radiotracers for imaging via PET (positron emission tomography) or SPECT (single-photon emission computed tomography) and therapy via α, β(-), or Auger electron emission. This feature article opens with a brief introduction to the imaging and therapy modalities exploited in nuclear medicine, followed by a discussion of the multi-component strategy used in radiopharmaceutical development, known as the bifunctional chelate (BFC) method. The modular assembly is dissected into its individual components and each is discussed separately. The concepts and knowledge unique to metal-based designs are outlined, giving insight into how these radiopharmaceuticals are evaluated for use in vivo. Imaging nuclides (64)Cu, (68)Ga, (86)Y, (89)Zr, and (111)In, and therapeutic nuclides (90)Y, (177)Lu, (225)Ac, (213)Bi, (188)Re, and (212)Pb will be the focus herein. Finally, key examples have been extracted from the literature to give the reader a sense of breadth of the field.

Production of 177Lu for Targeted Radionuclide Therapy: Available Options

“…Over the last several years, the 177 Lu radionuclide has attracted considerable attention and exhibited great promise in the research, commercial and clinical communities for use in a variety of therapeutic procedures [1][2][3][4][5][6][7][8]. Despite being a late entrant, 177 Lu has not only consolidated its potential, but also established a strong foothold at the forefront of TRT.…”

“…The in vivo applications of key 177 Lu radiopharmaceuticals for a variety of therapeutic procedures include peptide receptor radionuclide therapy [11][12][13][14][15][16][17][18][19][20][21][22][23][24][25][26], bone pain palliation [27][28][29][30][31][32][33], radiation synovectomy [34][35][36][37][38][39] and radioimmonutherapy [40][41][42][43][44][45][46]. There is a steadily expanding list of 177 Lu-labeled radiopharmaceuticals that is currently being evaluated at the preclinical research or at product development stages; these may potentially be used in vivo in humans for evaluation for radionuclide therapy [1][2][3]. A summary of key 177 Lu-labeled radiopharmaceuticals currently used in TRT is depicted in Table 1.…”

Complexos derivados do fragmento <i>fac</i>-[M(CO)₃L] (M = Re e Tc) com ligantes multidentados como novos agentes para radioterapia e radiodiagnóstico

“…The lipophilic character of the complex was confirmed by the determination of the partition coefficient. In addition, In vitro biolgical tests of captation and influx were performed on B16F10 cells (murine melanoma Devido a capacidade de gerar imagens assim como monitorar a progressão do câncer de maneira não-invasiva, na medicina nuclear são utilizadas principalmente duas técnicas para a aquisição de imagem: a SPECT e a PET [14].…”

“…Em ambas as técnicas, o radionuclídeo é administrado no paciente, no qual a parte radioativa está ligada a um fragmento que o direcionará ao local do tumor [14]. O uso clínico da SPECT e PET depende de vários fatores, como o custo, a sensibilidade e resolução da técnica e da disponibilidade do radionuclídeo [14].…”

“…O uso clínico da SPECT e PET depende de vários fatores, como o custo, a sensibilidade e resolução da técnica e da disponibilidade do radionuclídeo [14]. Para essas técnicas, é desejável que o radionuclídeo possua algumas características, dentre as quais podemos citar:…”