Modulation of the multidrug resistance P-glycoprotein: Detection with technetium-99m-sestamibi in vivo

Journal Article · Sat Mar 01 04:00:00 EST 1997 · Journal of Nuclear Medicine

OSTI ID:466384

Luker, G D; Fracasso, P M; Dobkin, J; Piwnica-Worms, D ^[1]

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1. Washington Univ. School of Medicine, St. Louis, MO (United States)

Overexpression of the multidrug resistance (MDR1) P-glycoprotein (Pgp) has been documented in nearly all forms of human cancers and increased levels of Pgp in some tumors correlate with poor response to treatment. Technetium-99m-sestamibi has recently been validated as a Pgp transport substrate. Pgp is also normally expressed along the biliary canalicular surface of hepatocytes and the luminal side of proximal tubule cells in the kidney, while not expressed in heart. Focused on these organs with known Pgp status, we present the findings on {sup 99m}Tc-sestamibi showed normal, prompt clearance of the radiotracer from the liver and kidneys relative to the heart. After administration of the Pgp modulator, {sup 99m}Tc-sestamibi was selectively retained in the liver and kidneys. Hepatobiliary and renal clearance of {sup 99m}Tc-sestamibi are Pgp-mediated, and inhibition of Pgp transport in these organs can be successfully imaged using {sup 99m}Tc-sestamibi in patients. Similar results might be expected with this and related radiopharmaceuticals for functional imaging of Pgp transport and modulation in tumors. 34 refs., 2 figs.

• OSTI ID: 466384
• Journal Information: Journal of Nuclear Medicine, Journal Name: Journal of Nuclear Medicine Journal Issue: 3 Vol. 38; ISSN 0161-5505; ISSN JNMEAQ
• Country of Publication: United States
• Language: English

Related Subjects

55 BIOLOGY AND MEDICINE
BASIC STUDIES
BIOLOGICAL ACCUMULATION
CHEMOTHERAPY
DIAGNOSTIC TECHNIQUES
GLYCOPROTEINS
HEART
KIDNEYS
LIVER
MEMBRANE TRANSPORT
NEOPLASMS
PATIENTS
RADIOPHARMACEUTICALS
RENAL CLEARANCE
SCINTISCANNING
TECHNETIUM 99
TRACER TECHNIQUES