Drug intelligence / Profile preview

99mTc-HYNIC-Tyr3-octreotide

Development stage
Unknown
Lead developer
National Centre for Nuclear Research
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration
Intravenous
01

Overview

99mTc-HYNIC-Tyr3-octreotide is a radiopharmaceutical imaging agent used for the detection and staging of tumors that overexpress somatostatin receptors (SSTRs). It consists of the somatostatin analog [Tyr3]octreotide (TOC) conjugated to the bifunctional chelator hydrazinonicotinamide (HYNIC). The complex is typically stabilized with co-ligands such as ethylenediamine-N,N'-diacetic acid (EDDA) or tricine and labeled with the gamma-emitting radioisotope technetium-99m. The drug acts as a high-affinity agonist for somatostatin receptor subtype 2 (SSTR2), which is frequently overexpressed in neuroendocrine tumors (NETs) and other malignancies like hepatocellular carcinoma. Following intravenous administration, the agent localizes to receptor-positive tissues, allowing for high-resolution visualization via Single Photon Emission Computed Tomography (SPECT) or SPECT/CT. It is favored over older agents like 111In-pentetreotide due to its superior image quality, lower radiation burden, and more efficient clinical workflow.

Brand names
Tektrotyd
Other names
99mTc-HYNIC-octreotide99mTc-labeled [Tyr3]octreotideTechnetium Tc 99m EDDA/HYNIC-Tyr3-octreotide99mTc-EDDA/HYNIC-Tyr3-octreotide
02

Targets

SSTR5 (Somatostatin receptor 5)SSTR3 (Somatostatin receptor 3)SSTR2 (Somatostatin receptor type 2)

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