astatine and menadiol

From the results of the alpha-particle track autoradiography, the alkaline phosphatase studies, the biodistribution investigations and the therapeutic experiments with the transplanted Franks and Hemmings (1978) adenocarcinoma of the rectum in mice, an important finding is the striking selectivity of the uptake of the compound 6-211 At-astato-2-methyl-1, 4-naphthoquinol bis (diphosphate salt), after intraperitoneal injection into the tumour cell nuclei and in many cases into the nuclei of tumour stem cells, together with negligible uptake into normal colon and narrow. The compound, 6-211 At-astato-2-methyl-1, 4-naphthoquinol bis (diphosphate salt) has been found to cure about two-thirds of the transplanted adenocarcinoma of the rectum in mice after a single intra-peritoneal injection of 3-4 microCi. This approach can be regarded as a form of metabolically-directed drug targetting on to a tumour product which is an enzyme, an alkaline phosphatase isozyme, present in the cells of some tumours. The compound is being studied further from the point of view of possible human therapeutic applications.

Topics: Alkaline Phosphatase; Animals; Astatine; Bromine; Energy Transfer; Injections, Intraperitoneal; Mice; Mice, Inbred C57BL; Neoplasms; Phosphorylation; Radioisotopes; Vitamin K

This report was prepared at the request of the International Atomic Energy Agency and presented at an Advisory Group Meeting on "Applications of Recent Radiobiological Research in Radiotherapy" held in Vienna, Austria, from 24-28 September 1979. Based on the recommendations of the Advisory Group, the I.A.E.A. has decided to initiate a coordinated international research programme entitled "Exploration of the Possibility of high LET RAdiation for Nonconventional Radiotherapy in Cancers". This programme will explore possible applications of corpuscular radiations (neutrons, protons, accelerated heavy ions, negative pi-mesons, thermal and epithermal neutrons) in cancer therapy. In addition, the programme will include research on in situ radiotherapy with unsealed radionuclides and thermal neutron capture. For further information on the programme, please contact Dr T. IWASAKI, Section of Radiation Biology, Division of Life Sciences, International Atomic Energy Agency, Wagramerstrasse 5, P. O. Box 100, A-1400 Vienna, Austria.

Topics: Animals; Antibodies, Neoplasm; Astatine; Cricetinae; Gallium Radioisotopes; Humans; Idoxuridine; Iodine Radioisotopes; Liposomes; Mice; Neoplasms; Radioisotopes; Tamoxifen; Tritium; Vitamin K