Positron emission tomography (PET) and macromolecular delivery in vivo

Positron emission tomography (PET) examinations with F-18-fluorodeoxyglucose (FDG) provide detailed information about the glucose-like metabolism in tissue. It is generally accepted that FDG reflects the viability of tumour cells. The kinetics of FDG is modulated by several genes, besides the glucose transporters and hexokinases. Additional specific information can be obtained non-invasively by using other tracers specific for cell membrane receptors. PET studies with radiolabelled peptides have emerged as a new diagnostic tool for imaging of certain tumour entities, like neuroendocrine tumours (NETs) and gastrointestinal stromal tumours (GISTs). This application is based on certain properties of these tumours, like the overexpression of somatostatin receptors, which can be visualised by somatostatin analogues, like 1,4,7,10-tetraazacyclododecane-N, N', N'', N'''-tetraacetic-acid-D: -Phe1-Tyr3 octreotide (DOTATOC) in NET. The overexpression of gastrin-releasing peptide (GRP) receptors can be visualised in GIST by using bombesin analogues. These peptides can be labelled by (68)Ga, which is a generator product and therefore more cost-effective than cyclotron products. (68)Ga-DOTATOC is a peptide that binds primarily to somatostatin receptor subtype 2 (SSTR2). PET studies with (68)Ga-DOTATOC are performed in patients with NET and some other tumours. (68)Ga-BZH3 ((68)Ga-Bombesin) is a peptide that binds to at least three bombesin receptor subtypes: the BB1 (also known as neuromedin B), the BB2 (also known as GRP), and the BB3 (bombesin receptor subtype 3). This bombesin analogue, (68)Ga-BZH3, is used in patients with GIST.