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Pharmacokinetics of Technetium-99m-MAG₃ in Humans

Department of Nuclear Medicine, University of Heidelberg, Department of Nuclear Medicine, University of Münster, Departments of Urology and Physiology, University of Heidelberg
Department of Biostatistics, German Cancer Research Center, Heidelberg, West Germany

Correspondence: For reprints contact: Bernd Bubeck, MD, BSc, Dept. of Nuclear Medicine, University of Heidelberg, Im Neuenheimer Feld 400, D-6900 Heidelberg, West Germany.

ABSTRACT

Technetium-99m-mercaptoacetylglycylglycylglycine (^99mTc-MAG₃) is introduced to replace o-iodohippurate (OIH) for renal function studies. For interpretation of clinical findings, extensive pharmacokinetic studies were performed on patients. These showed that ^99mTc-MAG₃, compared with OIH, has a higher plasma-protein binding, an essentially higher intravascular concentration, a smaller volume of distribution and, with practically identical biologic half-lives, a correspondingly lower clearance. Simultaneous steady-state measurements resulted in a 1.5-fold higher clearance of OIH than of ^99mTc-MAG₃ (n = 124). Competitive inhibition of the tubular transport system by p-aminohippurate (PAH) (20 patients) revealed a distinctly higher suppression of the ^99mTc-MAG₃ clearance than of OIH which indicates a lower affinity of the ^99mTc complex to the tubular cell. The plasma extraction efficiencies of both agents, measured during surgery (n = 5), did not indicate an extrarenal elimination of ^99mTc-MAG₃. This new radiopharmaceutical is a pragmatic alternative to OIH and offers advantages not only for scintigraphic imaging but is also suited for quantitative renal function studies.

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