5-(/sup 125/I)-iododeoxyuridine and the Auger effect: biological consequences and implications for therapy

Journal Article · Sun Jan 01 04:00:00 EST 1978 · Pathobiol. Annu.; (United States)

OSTI ID:5100136

Bloomer, W D; Adelstein, S J

The development of a strategy for the treatment of cancer with internally administered radionuclides has two overriding constraints. The first is a biological one requiring the radiopharmaceutical to be incorporated preferentially within tumor cells or tumor cell targets in high enough concentration to be effective yet without causing irreparable damage to surrounding or critical normal tissues. The second is a physical one requiring the radionuclide to deposit its energy within a volume approximately that of the tumor cell or, if possible, confined to the radiosensitive targets of the tumor cell. Conceptually, as we shall explain below, this can be achieved by using the Auger effect from radionuclides decaying by electron capture. In many ways the physical and biological requisites for such an internally administered radiopharmaceutical are met by the thymidine analog 5-(/sup 125/I)-iododeoxyuridine (/sup 125/IUdR), in which the 5-methyl group of thymidine is replaced by /sup 125/I. This substitution produces a compound which behaves remarkably like thymidine because both the methyl group and iodine have similar van der Waal's radii. As a result, the radioiodine deposits its energy within the sensitive structures of the cell. Consideration in this report will be limited to the biologic consequences and implications for therapy of /sup 125/IUdR incorporated into DNA.

• Research Organization: Harvard Medical School, Boston, MA
• OSTI ID: 5100136
• Journal Information: Pathobiol. Annu.; (United States), Journal Name: Pathobiol. Annu.; (United States) Vol. 8; ISSN PBANB
• Country of Publication: United States
• Language: English

Related Subjects

550603 -- Medicine-- External Radiation in Therapy-- (1980-)
550604* -- Medicine-- Unsealed Radionuclides in Therapy-- (1980-)
560161 -- Radionuclide Effects
Kinetics
& Toxicology-- Man
62 RADIOLOGY AND NUCLEAR MEDICINE
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMAL CELLS
ANTIMETABOLITES
ANTIMITOTIC DRUGS
AUGER EFFECT
AZINES
BETA DECAY RADIOISOTOPES
BIOLOGICAL EFFECTS
BIOLOGICAL LOCALIZATION
BIOLOGICAL RADIATION EFFECTS
CHEMICAL PREPARATION
DATA
DAYS LIVING RADIOISOTOPES
DNA
DOSE-RESPONSE RELATIONSHIPS
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EXPERIMENTAL DATA
HETEROCYCLIC COMPOUNDS
HYDROXY COMPOUNDS
INFORMATION
INTERMEDIATE MASS NUCLEI
INTERNAL IRRADIATION
IODINE 125
IODINE ISOTOPES
IODODEOXYURIDINE
IODOURACILS
IRRADIATION
ISOTOPES
MEDICINE
NUCLEAR MEDICINE
NUCLEI
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANIC IODINE COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PYRIMIDINES
RADIATION EFFECTS
RADIOISOTOPES
RADIOLOGY
RADIONUCLIDE KINETICS
RADIOSENSITIVITY
RADIOTHERAPY
RIBOSIDES
SURVIVAL CURVES
SYNTHESIS
THERAPY
THYMIDINE
TUMOR CELLS
URACILS