Drug intelligence / Profile preview

pentetreotide

Development stage
Phase 2
Lead developer
Novartis
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration
Intravenous
01

Overview

Pentetreotide is a synthetic peptide and DTPA conjugate of octreotide, which is a long-acting analog of the human hormone somatostatin. It is primarily used as a radiopharmaceutical diagnostic agent in nuclear medicine, most commonly labeled with Indium-111 (In-111) for imaging. The compound binds with high affinity to somatostatin receptors—especially subtypes 2 and 5—on the surface of neuroendocrine tumor cells. After intravenous administration, indium In‑111 pentetreotide localizes in tissues rich in somatostatin receptors, enabling visualization by gamma camera scintigraphy (Octreoscan). Its main clinical use is for detecting and localizing neuroendocrine tumors such as gastroenteropancreatic neuroendocrine tumors (GEP-NETs), carcinoid tumors, pituitary tumors, and for identifying ectopic ACTH-producing tumors responsible for Cushing’s syndrome. Pentetreotide has also been studied in the diagnosis of Cushing's syndrome[1][2][6].

Brand names
Octreoscan
Other names
pentetreotidaindium In-111 pentetreotide
02

Targets

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

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