PeptideHormone

Octreotide

A long-acting somatostatin analog used to suppress GH and other hormones.

AnalogEstablishedBased on SomatostatinCompare lineage

Identity

Class
Somatostatin analog (cyclic octapeptide)
Source
Synthetic analog of somatostatin
Receptor
Somatostatin receptors (SSTR2 and SSTR5 preferential)

Key properties

Molecular weight
~1,019.2 Da
Half-life (native)
~1.5 h (subcutaneous; LAR depot ~monthly)
Model dosing

Approximate values for the native hormone. Engineered analogs are often deliberately larger and far longer-acting.

Mechanism

Octreotide reproduces somatostatin's inhibitory action but with a far longer half-life than the native peptide's ~2 minutes. By preferentially engaging SSTR2/SSTR5 it suppresses growth hormone and several gut hormones, which is why it is used in acromegaly and neuroendocrine tumors.

Reference notes

  • Native somatostatin is too short-lived to be a practical drug; octreotide solves the half-life problem.
  • It is receptor-subtype-selective (SSTR2/5), unlike native somatostatin's broad SSTR coverage.
  • Long-acting (LAR) depot formulations act over roughly a month.

Selected literature

Curated peer-reviewed reviews, sourced from PubMed. Selected for relevance, not exhaustive — open any entry on PubMed for the full record and its primary citations.

  1. 1.Octreotide and Octreotide-derived delivery systems · Journal of drug targeting, 2023 · PMID 37211679
  2. 2.Somatostatin Analogs in Clinical Practice: a Review · International journal of molecular sciences, 2020 · PMID 32121432