Autoradioluminography, a powerful and reliable tool for drug development: Accelera's experience. (4th September 2019)

• Record Type: Journal Article
• Authors: Marzorati, Simona; Messina, Monica; Ghiglieri, Alberto
• Other Names: Elbert Tomas guestEditor.; Lawrie Kenneth guestEditor.
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 62:Number 11(2019)
• Page Start: 776
• Page End: 784
• Publication Date: 2019-09-04
• Subjects: absorption -- metabolism -- ADME studies -- autoradioluminography -- biodistribution studies -- carbon 14 -- radiolabelling; Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3790
• Languages: English
• ISSNs: 0362-4803

Abstract

Abstract: A deeper understanding of the pharmacokinetic and pharmacodynamic properties of a drug candidate is a pivotal component of drug discovery and development. Autoradiography is an excellent technique allowing exploiting the advantages of the use of radioisotopes in the drug disscovery field. The introduction of phosphor imaging technology has revolutionized the handling of drug distribution studies providing high‐resolution images. Specifically, quantitative whole‐body autoradioluminography is employed for preclinical study where the aim is to obtain information about the route of elimination and tissue distribution of a drug candidate. Autoradioluminography is also the technique of choice pursued to deal with all the issue that it is possible to encounter in all stage of drug development (ie, site‐specific drug localization and retention, drug‐drug interactions, penetration into specific target, specific tissue binding, crossing of brain blood barrier, and placental transfer). The purpose of this review is to give a picture of how autoradiography is employed in our laboratory as a key tool for advances in the assessment of the drug disposition and to validate new experimental models. Abstract : Radiolabelled compounds have consistently proved to be the most efficient tool for determining the absorption, distribution, metabolism and excretion (ADME) of chemical entities. Autoradiography is an excellent technique allowing exploiting the advantages of the use of radioisotopes in the drug discovery field. The purpose of this review is to analysis how autoradiography is employed in preclinical studies and specifically in our laboratory as a key tool in the assessment of the drug disposition and to validate new experimental models.