FDA Approved Growth Hormone Axis

Octreotide

also known as: Sandostatin, Bynfezia, Mycapssa

The first-generation somatostatin analog (FDA-approved as Sandostatin, 1988) — the pharmacological counterweight to growth-hormone excess. Used for acromegaly, carcinoid syndrome, and VIPoma; now available in injectable, LAR-depot, and oral (Mycapssa, 2020) formulations.

A synthetic cyclic octapeptide analog of somatostatin, developed by Sandoz (now Novartis) and FDA-approved in 1988 as Sandostatin, with preferential binding to somatostatin receptor subtypes 2 and 5; the standard-of-care medical therapy for acromegaly and for hormonal symptom control in carcinoid syndrome and VIPoma, and an important reference compound in the growth-hormone-axis encyclopedia.

Mechanism of action

Binds somatostatin receptor subtypes SSTR2 (high affinity) and SSTR5 (moderate affinity) on pituitary somatotrophs, carcinoid tumor cells, and VIPoma cells, inhibiting adenylyl cyclase, suppressing hormone secretion, and reducing tumor growth signaling. In acromegaly this reduces growth hormone and IGF-1; in carcinoid it reduces serotonin and flushing/diarrhea symptoms.

Primary uses

Acromegaly (adjunct or primary medical therapy)
Carcinoid syndrome (flushing and diarrhea)
VIPoma (watery diarrhea)
Variceal bleeding (off-label hemostatic use)

Typical dosing

50–500 mcg TID (SC); 10–30 mg monthly (LAR); 40–80 mg/day (oral) varies by formulation varies (subcutaneous, intramuscular depot, or oral)

Oral Mycapssa offers a non-injectable option for stable acromegaly patients previously controlled on injectable somatostatin analogs.

Regulatory status

FDA-approved as Sandostatin (1988, SC injection), Sandostatin LAR Depot (1998, monthly IM depot), Mycapssa (2020, delayed-release oral capsule — the first approved oral somatostatin analog), and Bynfezia autoinjector. Multiple generics available.

References

[fda-pi] Sandostatin LAR Depot (octreotide acetate) Prescribing Information. Novartis.
[fda-pi] Mycapssa (octreotide) Prescribing Information. Amryt Pharma / Chiesi.
[pubmed] Colao A, et al. "Systematic review and meta-analysis of the efficacy and safety of octreotide and lanreotide in acromegaly." J Clin Endocrinol Metab, 2016;101:1-13.

Related peptides

Lanreotide

The second-generation somatostatin analog (FDA-approved as Somatuline Depot, 2007 for acromegaly; 2014 for GEP-NETs; 2017 for carcinoid) — monthly deep-SC prefilled syringe. Functionally equivalent to octreotide LAR for most indications.

Somatropin (HGH)

FDA-approved recombinant human growth hormone — the direct hormone replacement, with multiple clinical indications, prescription-only status, and specific federal criminal provisions against off-label distribution.

Tesamorelin

An FDA-approved GHRH analog for reducing excess visceral fat in HIV-associated lipodystrophy.

Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.