title: A chemical model suggesting the maximum radiolabeled somatostatin analogue tumor uptake, in the presence of unlabeled somatostatin.
abstract: Somatostatin analogues (SSA), both radiolabeled and unlabeled play an important role in the management of carcinoid tumors. They are often administered in parallel, the unlabeled analogue for treating the carcinoid tumors' symptoms and the radiolabeled one for imaging tumors foci. There is a debate about when is the optimum time for a somatostatin receptor scintigraphy during treatment. Opinions are divided, with some authors suggesting stopping SSA treatment, while others do not. Our aim was to try to explore pharmacokinetics behind the radiolabeled peptide administration in the presence of circulating in blood unlabeled SSA, by using a model of "law of mass". Applying the pharmacokinetic data from the manufacturers' Prescription Information Sheet in a formula describing competitive binding, led to a reduced uptake for the radiolabeled peptide in the presence of the unlabeled peptide, in comparison with standalone radiolabeled peptide administration, regardless of the total number of available receptors. We provide data that unlabeled somatostatin should be withdrawn for no less than 14 days before the labeled SSA is administered, because biotherapy agents interfere with both diagnostic and therepeutic nuclear medicine procedures. Further research is needed to reach secure conclusions on patient medication management before diagnostic scans or therapeutic administrations in nuclear medicine. In conclusion, by waiting at least 6 half-lives (14 days), after the unlabeled SSA administration, the radiolabeled receptor uptake increased two-fold to three-fold, as compared to simultaneous administration of radiolabeled and unlabeled peptides depending on which SSA was used.
authors.affiliation: Nuclear Medicine Department, Theagenio Cancer Hospital, Al. Symeonidi 2, Thessaloniki, Greece. kalathas@dr.com.
authors.forename: Theodoros
authors.initials: T
authors.lastname: Kalathas
authors.forename: Maria
authors.initials: M
authors.lastname: Kotzasarlidou
authors.forename: Elissavet
authors.initials: E
authors.lastname: Molyvda-Athanasopoulou
authors.forename: Thalia
authors.initials: T
authors.lastname: Kalatha
authors.forename: Vaggelis
authors.initials: V
authors.lastname: Boultoukas
authors.forename: Anna
authors.initials: A
authors.lastname: Gotzamani-Psarrakou
mesh_terms: D000818:Animals; D002276:Carcinoid Tumor / Q000737:chemistry / Q000188:drug therapy / Q000378:metabolism*; D003198:Computer Simulation; D006801:Humans; D007553:Isotope Labeling; D008657:Metabolic Clearance Rate / Q000187:drug effects*; D008954:Models, Biological; D008956:Models, Chemical; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000493:pharmacokinetics*; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics* / Q000627:therapeutic use
chemical_list: D019275:Radiopharmaceuticals; D013004:Somatostatin