Peptide reference
Octreotide
Sandostatin ·Sandostatin LAR Depot ·Mycapssa ·SMS 201-995
What cited sources report about octreotide
Octreotide is a synthetic 8-amino-acid cyclic analog of the natural 14-residue hormone somatostatin. The molecule retains the canonical somatostatin pharmacophore (Phe-Trp-Lys-Thr) but incorporates D-amino acid substitutions and a single intramolecular disulfide bond that confer resistance to proteolysis and a circulating half-life of approximately 1.5 hours after subcutaneous administration. Octreotide preferentially binds somatostatin receptor subtypes SSTR2 and SSTR5 and inhibits the secretion of growth hormone, glucagon, insulin, and a wide range of gastrointestinal peptide hormones. The drug is marketed as Sandostatin (immediate-release subcutaneous), Sandostatin LAR Depot (once-monthly intramuscular microspheres), and Mycapssa (oral capsule, approved 2020). Octreotide was first FDA-approved in October 1988 and is approved in all major international jurisdictions; it has not been nominated to the FDA Pharmacy Compounding Advisory Committee. The summaries below report what individual cited sources state.
FDA Drug Label — Sandostatin
The DailyMed structured product label for Sandostatin (Novartis) lists three approved indications: reduction of blood levels of growth hormone (GH) and insulin-like growth factor-1 (IGF-1) in patients with acromegaly who have had inadequate response to surgery, irradiation, or bromocriptine; symptomatic treatment of severe diarrhea and flushing in metastatic carcinoid tumors; and treatment of profuse watery diarrhea associated with VIP-secreting tumors (VIPomas). The label specifies that clinical studies did not demonstrate improvements in tumor size or growth rate.
To reduce blood levels of growth hormone (GH) and insulin growth factor-1 (IGF-1)
Yuen and Samson (2022) — Endocrine Practice
A 2022 review surveyed the oral octreotide capsule (OOC, marketed as Mycapssa) formulation for acromegaly, focused on patients previously controlled on injectable somatostatin receptor ligands. The authors examined the CHIASMA OPTIMAL and MPOWERED phase III trials supporting the FDA approval and reviewed practical considerations including assessment of biochemical response, drug interactions, dosing titration, and monitoring.
OOCs are an effective treatment option for patients with acromegaly who previously responded to injectable SRLs, with the benefits of avoiding injection-related side effects.
Yang and Keating (2010) — Drugs
A 2010 Adis review surveyed the published evidence base for Sandostatin LAR Depot, the once-monthly intramuscular microsphere formulation of octreotide approved for acromegaly. The authors reported that octreotide LAR was associated with reductions in growth hormone and IGF-1 in patients with acromegaly and described tumor shrinkage in a subset of treated patients, while emphasizing that the immediate-release subcutaneous product remains useful for initial titration.
PubChem CID 448601 — National Center for Biotechnology Information
The PubChem compound record for octreotide lists molecular formula C49H66N10O10S2, consistent with an 8-amino-acid cyclic somatostatin analog with a single intramolecular disulfide bond. The record aggregates synonyms (including the development code SMS 201-995) and links to the underlying chemical and pharmacological literature.
Coverage notes
Octreotide was the first somatostatin analog approved for human use and remains the most widely prescribed product in the class; lanreotide (Somatuline Depot, Ipsen) and pasireotide (Signifor / Signifor LAR, Recordati) are subsequent somatostatin analogs targeting overlapping but distinct receptor profiles. The same molecule, radiolabelled with indium-111 (Octreoscan) or gallium-68 (NETSPOT, somakit-TATE) or paired with lutetium-177 (Lutathera), underpins a separate class of peptide-receptor radionuclide therapies and diagnostics for somatostatin-receptor-expressing neuroendocrine tumors; those products are distinct from the labels cited on this page.