Regulatory status

Status at a glance

503A compounding status

Not nominated

We found no pending nomination for the 503A bulks list. Unless the substance has another legal pathway (for example, a USP monograph or use in an FDA-approved drug), 503A pharmacies generally may not compound with it.

Status recorded · FDA source document

Also known as
Signifor
FDA approval
An FDA-approved product contains this peptide
503B outsourcing
Not determined
Anti-doping (WADA)
Not on the WADA Prohibited List
DEA schedule
Not a controlled substance

About peptide status

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Status as of

Key takeaway

Pasireotide (sold as Signifor and Signifor LAR) is a somatostatin analog that binds a broader set of somatostatin receptors than older drugs in its class, which makes it useful in Cushing's disease as well as acromegaly. In a 12-month phase 3 trial in Cushing's disease it reduced urinary free cortisol and normalized it in some patients. It has been FDA-approved in the U.S. since 2012, and its most notable side effect is high blood sugar.

At a glance

What it is
A multireceptor-targeted somatostatin analog peptide
Approved for
Cushing's disease and acromegaly
Key fact
In a 12-month phase 3 trial it normalized urinary free cortisol in a subset of Cushing's disease patients
Route
Subcutaneous twice daily (Signifor) or monthly intramuscular depot (Signifor LAR)
Evidence strength
FDA approved

Summary

Pasireotide (Signifor) is an FDA-approved somatostatin analog for Cushing's disease and acromegaly. Learn how it works and why it raises blood sugar.

What is pasireotide?

Pasireotide, sold as Signifor (twice-daily injection) and Signifor LAR (monthly depot), is a synthetic cyclohexapeptide analog of somatostatin. What sets it apart from octreotide and lanreotide is its broader receptor profile: it binds four of the five somatostatin receptor subtypes, with especially high affinity for subtype 5. That breadth lets it act on tumors that older analogs reach poorly. It was developed under the code SOM230 and approved in the United States in 2012.

How does pasireotide work?

Pasireotide binds multiple somatostatin receptor subtypes, most importantly subtype 5, which is highly expressed on the corticotroph tumors that cause Cushing's disease. Activating those receptors suppresses the tumor's secretion of adrenocorticotropic hormone (ACTH), which in turn lowers cortisol production by the adrenal glands. In acromegaly, the same broad receptor activation suppresses growth hormone and insulin-like growth factor 1.

This receptor breadth is the reason pasireotide is used when other somatostatin analogs are inadequate. In a 12-month phase 3 trial in Cushing's disease, pasireotide reduced and in some patients normalized urinary free cortisol, with a greater effect at the higher dose. A notable trade-off is that pasireotide raises blood glucose more than other somatostatin analogs, because its receptor activity reduces insulin secretion.

Is it FDA-approved?

Editor’s note

Status: Yes. Pasireotide was approved by the FDA in stages: Year | Product | Approved for 2012 | Signifor | Cushing's disease when surgery is not an option or has not worked 2014 | Signifor LAR (long-acting) | Acromegaly Later | Signifor LAR (long-acting) | Cushing's disease

Category: FDA-approved · Primary body area: Hormones & metabolism

Yes. Pasireotide was approved by the FDA in stages:

Study findings for Pasireotide
Year Product Approved for
2012SigniforCushing's disease when surgery is not an option or has not worked
2014Signifor LAR (long-acting)Acromegaly
LaterSignifor LAR (long-acting)Cushing's disease

What is pasireotide prescribed for?

Pasireotide is prescribed for Cushing's disease in adults for whom pituitary surgery is not curative or not possible, and for acromegaly inadequately controlled by surgery or other therapy.

What are the side effects?

According to the prescribing information, common side effects include:

  • High blood sugar and new-onset diabetes, which can be pronounced
  • Diarrhea and nausea
  • Gallstones
  • Headache, abdominal pain, and fatigue

More serious considerations include:

  • Significant hyperglycemia requiring glucose monitoring and treatment
  • Slowed heart rate and QT-interval prolongation
  • Elevated liver enzymes and low cortisol if suppression is excessive

Sources: FDA prescribing information for Signifor and Signifor LAR; the phase 3 Cushing's disease trial (Colao et al., New England Journal of Medicine, 2012, DOI: 10.1056/NEJMoa1105743), indexed on PubMed. This document is educational and does not constitute medical advice.

Registered human trials

0 registered human trials on ClinicalTrials.gov that we reviewed

Sources

  1. [1]
  2. [2]

    approved (PDF)

    Primary recordatirarediseases.com

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