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Drug intelligence / Profile preview
99mTc exendin (9-39) + Tyr3-octreotide
- Development stage
- Preclinical
- Lead developer
- Instituto Nacional de Investigaciones Nucleares
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Gamma Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
99mTc exendin (9-39) + Tyr3-octreotide is an investigational, dual-targeting radiopharmaceutical imaging agent developed by the Instituto Nacional de Investigaciones Nucleares (ININ) in Mexico. It is formulated as a single freeze-dried kit containing two technetium-99m (99mTc) labeled peptides: Lys27(99mTc-EDDA/HYNIC)-exendin(9-39), a glucagon-like peptide 1 receptor (GLP-1R) antagonist, and 99mTc-EDDA/HYNIC-Tyr3-octreotide, a somatostatin receptor type 2 (SSTR2) agonist. This combination is designed for single-photon emission computed tomography (SPECT) imaging to localize insulinomas and gastrinomas. Benign insulinomas typically express high densities of GLP-1R and low levels of SSTR2, whereas malignant insulinomas and their metastases show the opposite pattern. By simultaneously targeting both receptors, this hybrid imaging agent provides superior sensitivity and specificity for detecting both benign and malignant insulinomas compared to single-receptor tracers.
- Other names
- 99mTc-EDDA/HYNIC-exendin(9-39)/99mTc-EDDA/HYNIC-Tyr3-octreotide99mTc-HYNIC-exendin(9-39)-OCT99mTc-exendin(9-39)/Tyr3-octreotide99mTc-exendin(9-39)/octreotideLys27(99mTc-EDDA/HYNIC)-exendin(9-39)/99mTc-EDDA/HYNIC-Tyr3-octreotide
02
Targets
GLP1R (GLP-1R)SSTR2 (Somatostatin receptor type 2)
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