Source: FDA label
| Molecular formula | C58H66N10O9 |
|---|---|
| Molecular weight | 1047.2 g/mol |
| Registered trials | 87 |
| PubChem CID | 9941444 |
| Drug class | Somatostatin Analog [EPC] |
| Brand names | Signifor |
Mechanism of Action
12.1 Mechanism of Action SIGNIFOR is an injectable cyclohexapeptide somatostatin analogue. Pasireotide exerts its pharmacological activity via binding to somatostatin receptors (SSTRs). Five human somatostatin receptor subtypes are known: SSTR 1, 2, 3, 4, and 5. These receptor subtypes are expressed in different tissues under normal physiological conditions. Corticotroph tumor cells from Cushing's disease patients frequently over-express SSTR5 whereas the other receptor subtypes are often not ex
Key takeaways
- Pasireotide is approved under the brand name Signifor for a specific pituitary condition called Cushing's disease.
- It works by binding to somatostatin receptors, particularly the subtype often overexpressed in Cushing's disease tumor cells.
- More than 85 clinical trials have studied pasireotide, including dedicated work on managing its glucose-related side effects.
- The most frequently reported adverse events involve blood sugar changes, followed by gastrointestinal and general symptoms.
- No boxed warning appears on the current label.
What Pasireotide Is
Pasireotide is an injectable cyclohexapeptide classified as a somatostatin analog. It acts by binding to somatostatin receptors, of which five subtypes exist across body tissues. Corticotroph tumor cells in Cushing's disease frequently overexpress one particular subtype, SSTR5, while other receptor types are typically less present. By engaging these receptors, pasireotide can influence hormone signaling tied to the disease process.
What Pasireotide Is Approved For
Signifor is indicated for adult patients with Cushing's disease when pituitary surgery is not a viable option or has not resolved the condition. This is the sole approved use described on the label. The label does not carry a boxed warning.
What The Evidence Shows
Pasireotide has been studied across 87 registered clinical trials. One completed Phase 4 study examined ongoing access to pasireotide for patients already benefiting from it in prior Novartis-sponsored research. Another completed Phase 4 trial focused specifically on managing pasireotide-induced hyperglycemia in patients with Cushing's disease or acromegaly, reflecting the drug's known effect on blood sugar regulation.
Reported Side Effects
FAERS reports for pasireotide are dominated by metabolic effects: increased blood glucose (257 reports), hyperglycemia (243), and diabetes mellitus (242) appear most frequently. Gastrointestinal and general symptoms follow, including nausea (224), diarrhea (206), fatigue (199), and headache (172). These figures represent counts of submitted reports, not confirmed incidence or proven causation. The pattern is consistent with the drug's known influence on glucose metabolism through its receptor activity.
FAQ
What is pasireotide used for?
Pasireotide, sold as Signifor, is approved to treat adult patients with Cushing's disease. It is specifically indicated for those who cannot have pituitary surgery or whose surgery did not cure the condition.
How does pasireotide work?
Pasireotide is a somatostatin analog that binds to somatostatin receptors found on certain cells. In Cushing's disease, the responsible tumor cells often overexpress one particular receptor subtype, SSTR5, which pasireotide targets.
What are the most commonly reported side effects of pasireotide?
The most frequently reported issues involve elevated blood sugar, including increased blood glucose, hyperglycemia, and diabetes mellitus. Gastrointestinal symptoms like nausea and diarrhea, along with fatigue and headache, are also commonly reported. These are report counts from a safety database, not confirmed rates of occurrence.
Does pasireotide carry a boxed warning?
No, the current label for Signifor does not include a boxed warning.
Has pasireotide's effect on blood sugar been studied further?
Yes, a completed Phase 4 clinical trial specifically examined how to manage pasireotide-induced hyperglycemia in patients with Cushing's disease or acromegaly. This reflects the drug's recognized impact on glucose metabolism.
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Content is editorial information, not medical advice. Talk to your doctor before any treatment decision.
Sources: DailyMed label (Signifor) ClinicalTrials.gov FDA FAERS PubChem
Updated 2026-08-03