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Pasireotide: quick citable summary
Pasireotide is listed by PeptaHub as a other peptide with a prescription legal-status classification. The page summarizes mechanism, research context, common routes, safety notes, and references for writers and AI answer engines.
PeptaHub. “Pasireotide: Mechanism, Research Context, Safety.” peptahub.com, 2026. https://peptahub.com/peptides/pasireotide. Licensed CC BY 4.0.
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What is Pasireotide?
Pasireotide (Signifor) is an FDA-approved cyclic hexapeptide somatostatin analog with uniquely broad receptor binding (SSTR1, 2, 3, 5). It is the first pituitary-directed therapy for Cushing's disease and is also approved for acromegaly, though hyperglycemia affects 60-80% of patients.
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.
Reported study ranges
| Purpose | Route | Reported range | Frequency | Notes |
|---|---|---|---|---|
| Cushing's disease | subcutaneous | 300–900 mcg | twice daily | FDA label range 0.3–0.9 mg SC twice daily; recommended initial dose 0.6 or 0.9 mg BID, then titrated to response and tolerability (reductions of 0.3 mg per injection to manage adverse reactions) |
| acromegaly (LAR formulation) | intramuscular | 40–60 mg | every 4 weeks | Signifor LAR formulation; dose based on GH/IGF-1 response |
Reported ranges are for research context only. Consult a qualified healthcare professional before using any peptide.
Convert Pasireotide research-range units
Need to convert mg to mcg, dose volume, or U-100 syringe units? The Pasireotide dose calculator is preloaded with these ranges, or use the general dose unit converter.
Research summary
The pivotal 12-month Phase 3 trial (Pasireotide B2305 study; Colao et al., NEJM 2012) randomized 162 Cushing's disease patients to 600 or 900 mcg twice daily. The primary endpoint — urinary free cortisol (UFC) normalization at 6 months without a dose increase — was met by 12 of 82 patients (15%) in the 600-mcg group and 21 of 80 patients (26%) in the 900-mcg group; median UFC fell about 50% by month 2. FDA approval for Cushing's disease was granted December 2012. Signifor LAR was approved for acromegaly in 2014 and for Cushing's disease in 2018. Major limitation: hyperglycemia-related adverse events affected 118 of 162 patients (about 73%) in that trial, and 74 of 162 (about 46%) required glucose-lowering medication. Ongoing research explores its role in ACTH-secreting tumors and combination regimens.[1][2][3][4]
Evidence grading
Each claimed benefit is graded by the strength of available evidence. Grades reflect study quality, not effect size.
Strong = multiple RCTs · Moderate = limited trials or observational · Preliminary = animal or in vitro only · Insufficient = anecdotal or no published data
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. Available as Signifor (SC, twice daily) for Cushing's disease and Signifor LAR (IM, monthly), which is approved for acromegaly (2014) and Cushing's disease (2018). Prescription-only. Label lists no contraindications; key warnings include hypocortisolism, hyperglycemia and diabetes, bradycardia and QT prolongation, and liver test elevations.
Sourcing & access
Prescription required
Pasireotide is an FDA-approved prescription medication available through licensed healthcare providers, pharmacies, and label-appropriate access programs; compounded access depends on current FDA shortage status and compounding rules.
Frequently asked questions
Pasireotide (Signifor) is FDA-approved for two indications: Cushing's disease since December 2012 and acromegaly (Signifor LAR, monthly IM) since 2014. It is the first pituitary-directed medical therapy specifically approved for Cushing's disease, addressing the underlying corticotroph adenoma rather than just downstream cortisol effects, and provides a non-surgical option for patients whose adenomas can't be fully resected.
Pasireotide activates somatostatin receptors SSTR1, 2, 3, and 5, with 40-fold greater affinity for SSTR5 than octreotide. SSTR5 is overexpressed in corticotroph adenomas in Cushing's disease, and its engagement suppresses ACTH secretion, reducing cortisol production.
The major limitation is hyperglycemia and diabetes, which affected about 73% of patients in the pivotal Cushing's trial and often requires glucose-lowering medication. The FDA label also warns about hypocortisolism (adrenal insufficiency), liver test elevations, bradycardia and QT prolongation, cholelithiasis, and monitoring for pituitary hormone deficiency. The label lists no contraindications. Other side effects include diarrhea, abdominal pain, and nausea.
Pasireotide has a much broader somatostatin receptor binding profile, with particularly high affinity for SSTR5 (40-fold greater than octreotide). This makes it effective for Cushing's disease where SSTR5 is the dominant receptor on corticotroph tumors, while octreotide primarily targets SSTR2.
The pivotal 12-month Phase 3 trial (the Pasireotide B2305 study, Colao et al., NEJM 2012) randomized 162 Cushing's disease patients to 600 or 900 mcg twice daily. Urinary free cortisol normalized without a dose increase at 6 months in 15% of the 600-mcg group and 26% of the 900-mcg group, and median UFC fell about 50% by month 2. This supported FDA approval as the first medical therapy targeting the pituitary cause of Cushing's disease.
Research references
- Pasireotide versus octreotide in acromegaly: a head-to-head superiority studyPubMed
- A 12-month phase 3 study of pasireotide in Cushing's diseasePubMed
- Pasireotide for the treatment of Cushing's diseasePubMed
- Treatment of pituitary-dependent Cushing's disease with the multireceptor ligand somatostatin analog pasireotide (SOM230): a multicenter, phase II trialPubMed