title: Novel prodrugs for targeting diagnostic and therapeutic radionuclides to solid tumors.
abstract: Most cancer therapeutics (chemo, radiation, antibody-based, anti-angiogenic) are at best partially and/or temporarily effective. In general, the causes for failure can be summarized as: (i) poor diffusion and/or nonuniform distribution of drug/prodrug molecules in solid tumors; (ii) high drug concentration and retention in normal tissues (leading to side effects); (iii) requirement for plasma-membrane permeability and/or internalization of drug/prodrug molecules; (iv) low uptake of drug by tumor; (v) lack of retention of drug within tumor (most have gradient-driven reversible binding); and (vi) multidrug resistance. We are developing an innovative technology that aims to surmount these problems by actively concentrating and permanently entrapping radioimaging and radiotherapeutic prodrugs specifically within solid tumors. The approach will enable noninvasive sensing (imaging) and effective therapy of solid tumors, allowing tumor detection, diagnosis, and treatment to be closely coupled (personalized medicine).
authors.affiliation: Department of Radiology, Harvard Medical School, Armenise Building, Room D2-137, 200 Longwood Avenue, Boston, Massachusetts 02115, USA. amin_kassis@hms.harvard.edu
authors.forename: Amin I
authors.initials: AI
authors.lastname: Kassis
authors.forename: Houari
authors.initials: H
authors.lastname: Korideck
authors.forename: Ketai
authors.initials: K
authors.lastname: Wang
authors.forename: Pavel
authors.initials: P
authors.lastname: Pospisil
authors.forename: S James
authors.initials: SJ
authors.lastname: Adelstein
mesh_terms: D000818:Animals; D016503:Drug Delivery Systems; D006801:Humans; D009369:Neoplasms / Q000000981:diagnostic imaging*; D011355:Prodrugs / Q000008:administration & dosage* / Q000737:chemistry; D011868:Radioisotopes / Q000737:chemistry / Q000627:therapeutic use*; D011877:Radionuclide Imaging
chemical_list: D011355:Prodrugs; D011868:Radioisotopes