Drug intelligence / Profile preview

mebrofenin

Development stage
Approved
Lead developer
Bracco Diagnostics
Modality
Alpha Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

Mebrofenin is a synthetic iminodiacetic acid (IDA) derivative used as a chelating agent for the radiopharmaceutical technetium Tc 99m. The resulting compound, technetium Tc 99m mebrofenin, is a diagnostic radiopharmaceutical administered intravenously to evaluate hepatobiliary function. After injection, it is rapidly taken up by hepatocytes in the liver and excreted into the bile ducts and gallbladder. Its mechanism relies on high hepatic extraction efficiency and fast biliary excretion, enabling imaging of the liver, gallbladder, and bile ducts using gamma cameras that detect gamma rays emitted by technetium-99m decay. Mebrofenin uptake occurs via Organic Anion Transporting Polypeptide 1B1 (OATP1B1) and Organic Anion Transporting Polypeptide 1B3 (OATP1B3) transporters in hepatocytes; excretion into bile canaliculi involves Multidrug Resistance-Associated Protein 2 (MRP2). It has no known pharmacologic action at recommended doses but serves as an essential tool for non-invasive assessment of liver function and biliary patency[1][5][6][7][8].

Brand names
Choletec
Other names
technetium tc 99m mebrofenintechnetium-99m mebrofenintechnetium99m mebrofenintechnetium 99m mebrofeninTc-99m mebrofeninTc99m mebrofeninTc 99m mebrofenin
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)MRP2 (Canalicular multispecific organic anion transporter 1)SLCO1B3 (Organic anion transporting polypeptide 1B3)

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