title: Biokinetics of indium-111-bleomycin complex in head and neck cancer--implementations for radiochemotherapy.
abstract: Bleomycin (BLM) has been used successfully for treatment of head and neck cancer. Combining radionuclide therapy with chemotherapy is a fascinating possibility. We have studied the biokinetics of BLM labeled with indium-111 (In-111). A complex formed at low pH had an activity of 100 MBq/mg BLM. This substance was intravenously injected into 10 head and neck cancer patients in escalating doses of 75, 175, and 375 MBq. Scintigraphic data from these patients were compared with tissue samples obtained at surgery. The activity distribution and penetration into tumor tissue was not affected by increasing the injected activity. In-111-BLMC uptake was directly proportional to Ki-67/MIB-1 activity and number of mitoses in tumor tissue. Based on the biokinetics, dosimetric calculations for In-111 and In-114m have been performed. S values for realistic geometry (a phantom designed from Patient CT) have been calculated. In-114m could deliver a 4-fold absorbed radiation dose into the tumor compared with In-111. We think that In-111-BLMC could be used for radiochemotherapy in head and neck cancer or adjuvant Auger-electron therapy using In-114m combined with BLM. Further studies on cellular dosimetry should be undertaken.
authors.affiliation: Department of Clinical Chemistry, University Central Hospital of Helsinki, Finland.
authors.forename: K J
authors.initials: KJ
authors.lastname: Kairemo
authors.forename: H A
authors.initials: HA
authors.lastname: Ramsay
authors.forename: T K
authors.initials: TK
authors.lastname: Paavonen
authors.forename: H A
authors.initials: HA
authors.lastname: Jääskelä-Saari
authors.forename: M
authors.initials: M
authors.lastname: Tagesson
authors.forename: K
authors.initials: K
authors.lastname: Ljunggren
authors.forename: S E
authors.initials: SE
authors.lastname: Strand
mesh_terms: D000328:Adult; D000368:Aged; D000970:Antineoplastic Agents / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001761:Bleomycin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy / Q000378:metabolism* / Q000532:radiotherapy; D002455:Cell Division / Q000187:drug effects / Q000528:radiation effects; D003131:Combined Modality Therapy; D005260:Female; D006207:Half-Life; D006258:Head and Neck Neoplasms / Q000188:drug therapy / Q000378:metabolism* / Q000532:radiotherapy; D006801:Humans; D007205:Indium Radioisotopes / Q000493:pharmacokinetics* / Q000627:therapeutic use; D007668:Kidney / Q000378:metabolism; D008297:Male; D008875:Middle Aged; D009010:Monte Carlo Method; D009942:Organometallic Compounds / Q000493:pharmacokinetics* / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D007205:Indium Radioisotopes; D009942:Organometallic Compounds; C047120:indium-bleomycin; D001761:Bleomycin