Pharmaceuticals—Special Issue on Radiopharmaceutical Chemistry between Imaging and Endoradiotherapy

Abstract

The fields of molecular biology, immunology and genetics have generated many important developments that advance the understanding of the induction and progression of oncological, cardiological and neurological diseases as well as the identification of disease-associated molecules and drugs that specifically target diseased cells during therapy. These insights have triggered the development of targeted radiopharmaceuticals which open up a new dimension of radiopharmaceutical sciences in nuclear medicine. Radiopharmaceuticals, also called radiotracers, are radiolabelled molecules, bearing a “radioactive lantern”, and used as molecular probes to address clinically relevant biological targets such as receptors, enzymes, transport systems and others. Positron emission tomography (PET) and single photon emission computed tomography (SPECT) realised in the en-vogue hybrid technologies PET/CT, SPECT/CT and PET/MRI represent the state-of-the-art diagnostic imaging technologies in nuclear medicine which are used to follow the trace of the administered radiopharmaceutical noninvasively thereby in vivo visualising and assessing biological processes at the subcellular and molecular level in a highly sensitive manner. In this connexion novel radiopharmaceuticals for the noninvasive molecular imaging of early disease states and monitoring of treatment responses in vivo by means of PET/CT, SPECT/CT and PET/MRI are indispensable prerequisites to further advance and strengthen the unique competence of radiopharmaceutical sciences. In the era of personalised medicine the diagnostic potential of radiopharmaceuticals is directly linked to a subsequent individual therapeutic approach called endoradiotherapy. Depending on the “radioactive lantern” (gamma or particle emitter) used for radiolabelling of the respective tracer molecule, the field of Radiopharmaceutical Chemistry can contribute to the set-up of an “in vivo theranostic” approach especially in tumour patients by offering tailor-made (radio)chemical entities labelled either with a diagnostic or a therapeutic radionuclide. [...]

Environmental Effect of Potential Radiopharmaceuticals Residuals

“…Table 1 Factor loadings (the highest loadings are marked by bold) mind that BIOWIN 1 and BIOWIN 2 describe biodegradation under aerobic conditions it is very logical to expect that compounds with low accumulation ability will stay principally into water phase where aerobic biodegradation is the most probable. This is the probable reason in PCA BIOWIN 1 and BIOWIN 2 to form separate group PC2 which describe very well molecules in C1 (see Table A1 in supplementary 1, 2,4,5,17,22,19,18,20,16,21) object cluster (Fig. 2).…”

“…The majority of currently available RP are composed of three main components: a targeting biomolecule (bio-vector), the bifunctional agent (conjugation, pharmacokinetic), and the radioisotope (therapy or diagnostic) [15,16]. Carrying out environmental impact studies using existing models [17,18] will provide reliable data about environmental behaviour of the radionuclides without information for the effect of their non-radioactive part.…”

Labeling of Anti-SAS1B with Zirconium-89 as a Novel Immune-PET Probe for Uterine Cancer Imaging

“…PET imaging depends on radionuclide decay by positron emission [5]. Radionuclides are chemically attached to molecular ligands designed to trace biochemical phenomena in vivo, such as the expression of surface antigen on cancer cells [6] [7]. Uterine cancers are considered aggressive cancers [8] and frequently have a terminal prognosis because of the lack of early diagnosis and effective treatment options [9].…”

Σύνθεση Και Ραδιοφαρμακολογική Αξιολόγηση Πολύτροπων Απεικονιστικών Παραγώγων Δεξτράνης Για Εντοπισμό Του Φρουρού Λεμφαδένα

“…Αρχικά, θα παρασκευαστούν με κλασική οργανική σύνθεση οι κατάλληλοι υποκαταστάτες, οι οποίοι θα χαρακτηριστούν με 1 Η NMR. Για τα σύμπλοκα του 99m Tc, θα συντεθούν οι τριδραστικοί υποκαταστάτες DCM (Dextran-S-Cysteine-Mannose), όπου DCM είναι παράγωγο μαννοζυλιωμένης δεξτράνης διαφορετικού μοριακού βάρους κάθε φορά, το οποίο κυμαίνεται από 10-500 kDa, και φέρει το τριδραστικό σύστημα ατόμων δοτών SNO (παράγωγο S-κυστεΐνης), για συναρμογή με τον πυρήνα fac-[ 99m Τc(CO)3] + .…”

“…Over the last decade, research on developing new radiopharmaceuticals has focused on the selective binding of a radiolabeled biomolecule to a receptor. Specifically, the biomolecule acts as a vector that transports the radionuclide to the tissue overexpressing the receptor to enable imaging and diagnosis with a SPECT or PET camera or with radiotherapy [1]. Among the SPECT isotopes currently in use, technetium-99m ( 99m Tc) remains the radionuclide of choice, having excellent physicochemical properties, easy access through generators, and low cost compared with radionuclides, the production of which requires a cyclotron ( 18 F, 123 I, 111 In, 11 C, 13 N, 15 O) [2].…”