title: Transport processes of radiopharmaceuticals and -modulators.
abstract: Radiotherapy and radiology have been indispensable components in cancer care for many years. The detection limit of small tumor foci as well as the development of radio-resistance and severe side effects towards normal tissues led to the development of strategies to improve radio-diagnostic and -therapeutic approaches by pharmaceuticals. The term "radiopharmaceutical" has been used for drugs labeled with radioactive tracers for therapy or diagnosis. In addition, drugs have been described to sensitize tumor cells to radiotherapy (radiosensitizers) or to protect normal tissues from detrimental effects of radiation (radioprotectors). The present review summarizes recent concepts on the transport of radiopharmaceuticals, radiosensitizers, and radioprotectors in cells and tissues, e.g. by ATP-binding cassette transporters such as P-glycoprotein. Strengths and weaknesses of current strategies to improve transport-based processes are discussed.
authors.affiliation: Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, Johannes Gutenberg-University, Mainz, Germany. efferth@uni-mainz.de
authors.forename: Thomas
authors.initials: T
authors.lastname: Efferth
authors.forename: Peter
authors.initials: P
authors.lastname: Langguth
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D000818:Animals; D001692:Biological Transport; D059248:Chemoradiotherapy / Q000379:methods; D019788:Fluorodeoxyglucose F18 / Q000493:pharmacokinetics; D005786:Gene Expression Regulation; D006801:Humans; D009369:Neoplasms / Q000000981:diagnostic imaging / Q000532:radiotherapy; D009683:Nuclear Medicine / Q000379:methods; D011838:Radiation-Sensitizing Agents / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics*; D011878:Radiotherapy / Q000379:methods; D017382:Reactive Oxygen Species; D017256:Technetium Tc 99m Sestamibi / Q000493:pharmacokinetics
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D011838:Radiation-Sensitizing Agents; D019275:Radiopharmaceuticals; D017382:Reactive Oxygen Species; D019788:Fluorodeoxyglucose F18; D017256:Technetium Tc 99m Sestamibi