Approved & therapeutic
Pasireotide
Signifor, Signifor LAR
Pasireotide is a somatostatin analogue with a broader receptor binding profile than octreotide or lanreotide, approved for Cushing's disease in patients for whom pituitary surgery is not an option or has not been curative, and — as a long-acting formulation — for acromegaly.
Also known as: Signifor, Signifor LAR, SOM230
- Status
- Pasireotide is approved by the U.S. FDA and has official prescribing information.
- Evidence
- Approved labeling. Official prescribing information exists, based on clinical trials in people.
- Half-life
- Approximately 12 hours for the immediate-release subcutaneous formulation.
- How it's taken
- Subcutaneous injection twice daily, or long-acting intramuscular injection every 4 weeks
- Mechanism
- Other
- Pathways
- GH axis
How Pasireotide works
Pasireotide binds four of the five somatostatin receptor subtypes, with markedly higher affinity for SSTR5 than octreotide. Corticotroph adenomas in Cushing's disease express SSTR5 densely, which is the rationale for its activity there: receptor binding suppresses ACTH secretion and consequently cortisol production.
What research has looked at
- In Cushing's disease it reduces urinary free cortisol; the pivotal trial's primary endpoint was normalisation of urinary free cortisol without dose increase at six months.
- It is one of the few medical options directed at the pituitary source of Cushing's disease rather than at adrenal steroidogenesis.
- The long-acting intramuscular formulation is approved for acromegaly in patients inadequately controlled on other somatostatin analogues, reflecting its different receptor profile.
Evidence level: Approved labeling. Official prescribing information exists, based on clinical trials in people. These are areas studied or reported, not promised effects.
Reported side effects and risks
- Hyperglycemia is the defining risk and is more frequent and more severe than with other somatostatin analogues — a consequence of strong SSTR5-mediated suppression of insulin secretion. Glucose monitoring before and during treatment is required, and new-onset diabetes is common.
- Bradycardia and QT prolongation; an ECG before and during therapy is recommended.
- Cholelithiasis, as with the somatostatin analogue class.
- Elevated liver enzymes have been reported.
- Hypocortisolism can occur if cortisol is over-suppressed, requiring dose reduction or glucocorticoid replacement.
- Diarrhea, nausea, abdominal pain, fatigue and headache are frequent.
Sources
- FDA approved-drug listing for pasireotide · U.S. Food & Drug Administration
- DailyMed prescribing information for pasireotide · NIH · DailyMed
- PubMed research on pasireotide Cushing disease · NIH · National Library of Medicine
- DrugBank record for pasireotide · DrugBank
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Related compounds
Pasireotide FAQ
What is Pasireotide?
Pasireotide is a somatostatin analogue with a broader receptor binding profile than octreotide or lanreotide, approved for Cushing's disease in patients for whom pituitary surgery is not an option or has not been curative, and — as a long-acting formulation — for acromegaly.
How does Pasireotide work?
Pasireotide binds four of the five somatostatin receptor subtypes, with markedly higher affinity for SSTR5 than octreotide. Corticotroph adenomas in Cushing's disease express SSTR5 densely, which is the rationale for its activity there: receptor binding suppresses ACTH secretion and consequently cortisol production.
Is Pasireotide FDA approved?
Yes. Pasireotide is approved by the U.S. FDA and has official prescribing information. Evidence level: approved labeling. Official prescribing information exists, based on clinical trials in people.
What is the half-life of Pasireotide?
Reported half-life: Approximately 12 hours for the immediate-release subcutaneous formulation.
How is Pasireotide taken?
Subcutaneous injection twice daily, or long-acting intramuscular injection every 4 weeks.
What side effects have been reported with Pasireotide?
Reported in the sources: Hyperglycemia is the defining risk and is more frequent and more severe than with other somatostatin analogues — a consequence of strong SSTR5-mediated suppression of insulin secretion. Glucose monitoring before and during treatment is required, and new-onset diabetes is common; Bradycardia and QT prolongation; an ECG before and during therapy is recommended; Cholelithiasis, as with the somatostatin analogue class; Elevated liver enzymes have been reported; Hypocortisolism can occur if cortisol is over-suppressed, requiring dose reduction or glucocorticoid replacement; Diarrhea, nausea, abdominal pain, fatigue and headache are frequent.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.