Pasireotide
Also known as: Signifor, Signifor LAR, SOM230
A multi-receptor somatostatin analog FDA-approved as Signifor for Cushing's disease and Signifor LAR for acromegaly. Prescription medication.
Last updated
Mechanism of Action
Pasireotide is a cyclohexapeptide somatostatin analog that binds four of the five somatostatin receptor subtypes, with especially high affinity for subtype 5. Corticotroph pituitary adenomas in Cushing's disease express subtype 5 heavily, so pasireotide suppresses ACTH secretion and lowers cortisol. It also inhibits growth hormone secretion in acromegaly. Its subtype 5 activity reduces insulin and incretin secretion, which explains its high rate of hyperglycemia.
- Half-life
- ~12 hours (subcutaneous); long-acting release given monthly
- Administration Routes
- Subcutaneous, Intramuscular
- Research Status
- Clinical
Reported Benefits
- Approved for Cushing's disease when pituitary surgery is not an option or has not been curative
- Lowers urinary free cortisol in Cushing's disease trials
- Approved (LAR) for acromegaly inadequately controlled by or unsuitable for surgery
- Superior to octreotide LAR for biochemical control in a head-to-head acromegaly trial
Potential Side Effects
- Hyperglycemia and diabetes (very common)
- Diarrhea, nausea and abdominal pain
- Gallstones
- Hypocortisolism
- Bradycardia and QT prolongation; liver test elevations
Common Dosing
Available as a twice-daily subcutaneous injection for Cushing's disease and a monthly intramuscular long-acting release form for acromegaly and Cushing's disease, with glucose, liver tests and ECG monitored during treatment. Dosing is set and supervised by the prescribing clinician.
The dosing information above is aggregated from research literature and anecdotal community reports for educational purposes only. It is not a recommendation, prescription, or medical advice. Peptides are sold as research chemicals only and are not intended for human use.
Contraindications
- Avoid in severe hepatic impairment (Child-Pugh C)
- Use with caution with poorly controlled diabetes
- Use with caution with QT prolongation risk or bradycardia
No documented stacking partners for Pasireotide yet.
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A 12-month phase 3 study of pasireotide in Cushing's disease
2012
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Pasireotide versus continued treatment with octreotide or lanreotide in patients with inadequately controlled acromegaly (PAOLA): a randomised, phase 3 trial
2014
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Efficacy and safety of once-monthly pasireotide in Cushing's disease: a 12 month clinical trial
2018