Pharmacokinetics of indium-111 BLEDTA in man
111In-BLEDTA is a bleomycin-containing radiopharmaceutical that has proven useful as a tumor imaging agent. Whole blood distribution and pharmacokinetic parameters were studied in nine cancer patients, and the results compared with previously reported studies using 57Co-bleomycin. In eight patients studied by bolus intravenous injection, 111In-BLEDTA had a beta half-life (t1/2 beta) of 1.3 hours, a terminal-phase half-life (t1/2) of 11.7 hours, a volume of distribution (Vd gamma) of 57.5L/m2, a total body clearance rate (C1b) of 52.8 ml/min/m2, a renal clearance rate (C1r) of 23.3 ml/min/m2, and a 24-hour urinary excretion of 38.1% total administered dose. 111In-BLEDTA and 57Co-bleomycin have similar C1bs but differing Vds. Polymorphonuclear cell uptake of 111In-BLEDTA may explain its shorter t1/2 beta and t1/2, as well as its lower C1r and 24-hour urinary excretion. While the biologic characteristics of 111In-BLEDTA contribute to a greater background activity than is observed in scans with 57Co-bleomycin, its superior physical properties render it clinically more desirable as a tumor-imaging radiopharmaceutical.
- Research Organization:
- Division of Diagnostic Radiology, Stanford University School of Medicine, California
- OSTI ID:
- 6442913
- Journal Information:
- Invest. Radiol.; (United States), Journal Name: Invest. Radiol.; (United States) Vol. 19:3; ISSN INVRA
- Country of Publication:
- United States
- Language:
- English
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62 RADIOLOGY AND NUCLEAR MEDICINE
ANTI-INFECTIVE AGENTS
ANTIBIOTICS
ANTIMITOTIC DRUGS
ANTINEOPLASTIC DRUGS
BETA DECAY RADIOISOTOPES
BLEOMYCIN
CLEARANCE
DAYS LIVING RADIOISOTOPES
DIAGNOSTIC USES
DISEASES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EXCRETION
INDIUM 111
INDIUM ISOTOPES
INTERMEDIATE MASS NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MINUTES LIVING RADIOISOTOPES
NEOPLASMS
NUCLEI
ODD-EVEN NUCLEI
RADIOISOTOPES
RADIOPHARMACEUTICALS
RENAL CLEARANCE
UPTAKE
USES