Overview
Pasireotide (brand: Signifor) is an FDA-approved cyclic hexapeptide somatostatin analog with a unique multi-receptor binding profile. It is the first pituitary-directed therapy approved for Cushing's disease and also approved for acromegaly (Signifor LAR). Its higher binding affinity for SSTR1, 3, and 5 distinguishes it from octreotide and lanreotide.
Mechanism of action
Pasireotide activates somatostatin receptors SSTR1, 2, 3, and 5, with particularly high affinity for SSTR5, which is overexpressed in corticotroph adenoma cells in Cushing's disease. SSTR5 engagement suppresses ACTH secretion from pituitary adenomas, reducing cortisol production. In acromegaly, combined SSTR2/5 activity more comprehensively inhibits GH secretion than SSTR2-selective agents. Compared to octreotide, pasireotide has 40-fold greater binding affinity for SSTR5.
Dosing protocols
| Purpose | Route | Dosage | Frequency | Notes |
|---|---|---|---|---|
| Cushing's disease | subcutaneous | 600–900 mcg | twice daily | Start at 600 mcg SC BID; increase to 900 mcg BID if UFC not normalized after 2 months |
| acromegaly (LAR formulation) | intramuscular | 40–60 mg | every 4 weeks | Signifor LAR formulation; dose based on GH/IGF-1 response |
Dosing information is for educational purposes only. Consult a qualified healthcare professional before using any peptide.
Research summary
The PASPORT phase III trial demonstrated pasireotide normalized urinary free cortisol (UFC) in ~25% of Cushing's disease patients at 6 months, with sustained response at 24 months. FDA approval for Cushing's disease was granted December 2012. Signifor LAR was approved for acromegaly in 2014. Major limitation: hyperglycemia occurs in 60–80% of patients, requiring glucose-lowering medication. Ongoing research explores its role in ACTH-secreting tumors and combination regimens.
Side effects
Side effects vary by individual. This is not an exhaustive list. Report unusual symptoms to a healthcare professional.
Common stacks
Peptides commonly paired with Pasireotide for synergistic effects.
Legal status
FDA-approved (NDA 203255, December 2012) for Cushing's disease and acromegaly. Available as Signifor (SC, twice daily) for Cushing's and Signifor LAR (IM, monthly) for acromegaly. Prescription-only.
Where to get it
Prescription required
Pasireotide is a prescription medication. Consult your healthcare provider or a licensed telehealth platform for access.