Pasireotide is a synthetic cyclohexapeptide somatostatin analog (MW ~1164.7 g/mol) with a unique broad somatostatin receptor binding profile, exhibiting high affinity for SSTR1, SSTR2, SSTR3, and SSTR5 (40-fold higher SSTR5 affinity than octreotide). It is FDA-approved for Cushing disease (Signifor SC, 2012) and acromegaly in patients inadequately controlled on first-generation somatostatin analogs (Signifor LAR, 2014). Pasireotide is the first pituitary-directed medical therapy approved specifically for Cushing disease.
Category: Endocrine / Somatostatin Analog. Evidence rating: A (strong human clinical data).
Clinical status: FDA-approved (Signifor SC for Cushing disease, 2012; Signifor LAR for acromegaly, 2014)
Pasireotide binds to somatostatin receptor subtypes 1, 2, 3, and 5, with particularly high affinity for SSTR5. In corticotroph adenomas of Cushing disease, SSTR5 is the predominantly expressed subtype, explaining why pasireotide is effective where octreotide and lanreotide (primarily SSTR2…
Safety considerations: Hyperglycemia is the most significant adverse effect: occurs in 57-73% of patients; frank diabetes in approximately 40% of previously normoglycemic patients; GI effects: diarrhea (58%), nausea (52%), abdominal pain (24%); Cholelithiasis (30-50% with long-term use).
Reviewed by the PeptideAtlas Editorial Team.
| Molecular weight | ~1164.7 g/mol |
|---|---|
| CAS number | 396091-73-9 |
| Half-life | ~12 hours (SC formulation); ~16-19 days effective duration (LAR) |
| Bioavailability | >90% subcutaneous |
| Production method | synthetic |
| Anti-doping status | not-listed |
| US regulatory status | FDA-approved. Signifor (SC) approved December 2012 for Cushing disease. Signifor LAR (IM) approved December 2014 for acromegaly. |
Related peptides: Octreotide, Lanreotide, Somatostatin.
Corticotroph adenomas predominantly express somatostatin receptor subtype 5 (SSTR5), not SSTR2. Pasireotide has 40-fold higher affinity for SSTR5 compared to octreotide, allowing it to suppress ACTH secretion from these tumors. Octreotide and lanreotide primarily target SSTR2 and have minimal effect on corticotroph adenomas.
Pasireotide inhibits insulin secretion and GLP-1 through its broad SSTR binding profile, particularly SSTR5 expressed on pancreatic beta cells. This suppresses glucose-stimulated insulin secretion more profoundly than octreotide or lanreotide. Approximately 57-73% of patients develop hyperglycemia, often requiring antidiabetic therapy.
No. Pasireotide LAR is approved for acromegaly patients who have had an inadequate response to surgery and/or other somatostatin analogs (octreotide LAR or lanreotide Autogel). Due to its high rate of hyperglycemia, it is reserved for second-line use.
Coverage on this site: Peptide Targeting Agents for In Vivo Tumor Imaging: A Practical Primer, Peptide-Receptor Systems for Tumor Imaging: A Field Guide, Representative Peptides for In Vivo Tumor Imaging, Macrocyclic Peptide Drugs: Structures, Pipelines and Oral Prospects.