Drug intelligence / Profile preview

SMTR-002

Development stage
Preclinical
Lead developer
Grafton Therapeutics
Modality
Peptides
01

Overview

SMTR-002 (also known as B0012387) is a next-generation, dual-subtype somatostatin receptor ligand (SRL) designed and synthesized by Grafton Therapeutics. It is an octapeptide containing novel halogenated amino acids that exhibits equal and sub-nanomolar binding affinities for both somatostatin receptor subtype 2 (SSTR2) and subtype 5 (SSTR5). In preclinical models of neuroendocrine tumors (NETs) and pituitary tumors, SMTR-002 has demonstrated potent anti-secretory and anti-proliferative effects, outperforming standard-of-care agents like octreotide and pasireotide. It is being developed for the treatment of SSTR2/SSTR5-expressing tumors, including pancreatic neuroendocrine tumors (panNETs) and pituitary adenomas, and is also being explored as a radiopharmaceutical platform for targeted radionuclide therapy.

02

Targets

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

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