Drug intelligence / Profile preview

iodine-124 metaiodobenzylguanidine

Development stage
Phase 2
Lead developer
Memorial Sloan Kettering Cancer Center
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Iodine-124 metaiodobenzylguanidine (124I-MIBG) is a positron-emitting radiopharmaceutical designed for high-resolution Positron Emission Tomography (PET) imaging of neuroendocrine tumors. As a structural analog of the neurotransmitter norepinephrine and the antihypertensive drug guanethidine, it acts as a substrate for the norepinephrine transporter (NET/uptake-1). It is selectively taken up by cells of sympathomedullary and neuroectodermal origin—such as neuroblastoma, pheochromocytoma, and paraganglioma—where it is sequestered in neurosecretory storage granules. While 123I-MIBG is commonly used for SPECT imaging, the 124I isotope allows for the superior spatial resolution and quantitative accuracy of PET/CT. This is particularly valuable for lesion detection, staging, and performing patient-specific internal dosimetry for those scheduled to undergo radionuclide therapy with 131I-MIBG (e.g., Azedra).

Other names
124I-meta-iodobenzylguanidineiodine I 124 metaiodobenzylguanidineI124-MIBGI-124-MIBGI 124-MIBG
02

Targets

NET (Norepinephrine Transporter)VMAT2 (Vesicular monoamine transporter 2)VMAT1 (Vesicular monoamine transporter type 1)

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