Pasireotide
Also known as: Pasireotide acetate, pasireotide diaspartate, Signifor, Signifor LAR, SOM230
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Summary
Pasireotide is a synthetic analogue of somatostatin that binds multiple somatostatin receptor subtypes. It is approved as a prescription medication for the treatment of Cushing's disease when surgery is not curative or feasible, and is being investigated for refractory dumping syndrome. The drug is administered by injection and works by suppressing hormone secretion from pituitary and gastrointestinal sources.
Mechanism of Action
Pasireotide acts as a broad‑spectrum somatostatin receptor ligand, displaying high affinity for SSTR1, SSTR2, SSTR3 and especially SSTR5. Binding to these G‑protein‑coupled receptors inhibits adenylate cyclase, reduces intracellular cAMP, and suppresses calcium‑dependent exocytosis of hormones such as ACTH, GH, insulin and glucagon. In corticotroph adenomas, this leads to decreased ACTH release and downstream cortisol production; in the gut, it slows intestinal motility and hormone secretion that contribute to dumping symptoms.
What the Research Shows
A 2015 Endocrine Reviews article described pasireotide as one of the few pituitary‑directed agents capable of inducing remission in a consistent subgroup of patients with Cushing's disease, leading to its regulatory approval for this indication. A 2017 JAMA review highlighted pasireotide among medical options for ACTH‑secreting pituitary adenomas when surgery fails. A 2025 review of dumping syndrome identified pasireotide as a broad‑spectrum somatostatin analogue under evaluation for refractory cases, noting limited early data. A 2025 structural review discussed pasireotide’s interaction with the conserved Trp‑Lys motif in the receptor binding pocket, linking its pharmacology to clinical effects. Together, these sources portray pasireotide as an approved therapy for Cushing's disease with emerging investigational use in dumping syndrome.
Reported Benefits
In patients with Cushing's disease who cannot undergo or have failed surgery, pasireotide can lower ACTH and cortisol levels, improving metabolic complications and quality of life. Clinical experience shows disease remission in a subset of treated individuals. Preliminary reports suggest it may alleviate severe hypoglycaemia and gastrointestinal symptoms in refractory dumping syndrome, offering a pharmacologic option when dietary measures are insufficient.
Limitations of the Evidence
Response rates in Cushing's disease are variable, and many patients require adjunctive therapies. Evidence for dumping syndrome is limited to early, non‑randomised investigations, and the drug is not yet approved for this use. High acquisition cost and the need for injectable administration restrict accessibility. Long‑acting formulations may not be suitable for all patients, and comparative data with other somatostatin analogues are sparse.
Safety Considerations
The most frequent adverse effect reported is hyperglycaemia, sometimes necessitating antidiabetic medication. Other concerns include gastrointestinal disturbances (diarrhoea, abdominal pain), gallstone formation, and injection‑site reactions. Monitoring of blood glucose, liver function and gallbladder status is advised. Caution is warranted in patients with pre‑existing diabetes or severe hepatic impairment.
How It Is Administered
Pasireotide is supplied as a short‑acting formulation for subcutaneous injection and as a long‑acting depot (LAR) for intramuscular injection, typically administered once weekly or once monthly, respectively. Dosing is individualized based on clinical response and tolerability, and the drug is provided in sterile, pre‑filled syringes or vials.
Routes of Administration
Goals & Uses
- Control hypercortisolismCushing's DiseaseHigh
- Reduction of GH and IGF-1 levelsHormonal ControlHigh
- Management of neuroendocrine tumorsOncologyModerate
- Normalize IGF‑1 and GH levelsAcromegalyHigh
- Treatment of Cushing's diseaseEndocrine DisorderHigh
- Treatment of acromegalyEndocrine DisorderHigh
- Reduction of ACTH secretionHormonal ControlHigh
Contraindications
- Severe hepatic impairment (Child-Pugh C)HepaticHigh
- Severe hepatic impairmentOrganModerateLiver function concerns
- Significant bradycardia or conduction abnormalitiesCardiacModerate
- Hypersensitivity to pasireotide or excipientsAllergyHigh
- Uncontrolled Diabetes MellitusMetabolic / EndocrineModerate
Adverse Effects
- HyperglycemiaMetabolicCommonAbnormally high blood glucose
- Injection site reactionsLocalCommon
- CholelithiasisHepatobiliaryCommon
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- Hyperglycemia / diabetes mellitusMetabolicCommon
- Gallbladder diseaseHepatobiliaryUncommonGallstones, cholecystitis, or biliary complications
- Adrenal insufficiencyEndocrineUncommon
- QT prolongationCardiovascularUncommonExtended QT interval on ECG
- DiarrheaGastrointestinalCommonLoose or frequent stools
Drug Interactions
- Antidiabetic agentsModerate
- CyclosporineModerate
- QT-prolonging drugs (e.g., antiarrhythmics, fluoroquinolones)Moderate
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin)Moderate
- Bromocriptine / dopamine agonistsLow
- Insulin or oral hypoglycemicsModerate
Population Constraints
- Moderate hepatic impairment (Child-Pugh B)HepaticRelative
- PregnancyReproductive SafetyRelative
- Patients with diabetes or pre-diabetesMetabolicRelative
- Pediatric patientsAgeAbsolute
- LactationReproductiveRelative
Regulatory Status
- European UnionApprovedApproved: Cushing's disease, AcromegalySame indications as US.
- United StatesApprovedApproved: Cushing's disease, AcromegalySubcutaneous and long‑acting intramuscular formulations.
- United KingdomApprovedApproved: Cushing's disease, Acromegaly
Approved by FDA (2012) for Cushing's disease and later for acromegaly; also approved in the EU and UK. Available as subcutaneous solution (Signifor) and long‑acting intramuscular depot (Signifor LAR).
Evidence & Sources
- Journal ArticleModerateTack J, et al.2025-01-01T00:00:00.000000Z
- Journal ArticleModeratePivonello R, et al.2015-01-01T00:00:00.000000Z
- Journal ArticleModerateMolitch ME2017-01-01T00:00:00.000000Z
- Journal ArticleModerateZhang B, Xue L, Wu ZB2025-01-01T00:00:00.000000Z
Frequently Asked Questions
What condition is pasireotide officially approved to treat?
Pasireotide is approved as a prescription medication for Cushing's disease when pituitary surgery has failed or is not an option, providing a medical alternative to control excess cortisol.
How does pasireotide differ from older somatostatin analogues?
Unlike octreotide and lanreotide, pasireotide binds with high affinity to a broader range of somatostatin receptors, especially SSTR5, which enhances its ability to suppress ACTH secretion from corticotroph tumors.
Why can pasireotide cause high blood sugar?
By inhibiting insulin and incretin secretion through somatostatin receptors in the pancreas and gut, pasireotide can reduce glucose uptake and raise blood glucose levels, sometimes requiring additional diabetes treatment.
Is pasireotide used for dumping syndrome?
Current literature lists pasireotide as an investigational therapy for refractory dumping syndrome; it is not yet approved for this indication and evidence remains limited to early studies.
What are the common ways the drug is given?
Pasireotide is administered by injection: a short‑acting version subcutaneously, usually weekly, and a long‑acting depot intramuscularly, typically once a month.
What is Pasireotide?
Pasireotide is a synthetic analogue of somatostatin that binds multiple somatostatin receptor subtypes. It is approved as a prescription medication for the treatment of Cushing's disease when surgery is not curative or feasible, and is being investigated for refractory dumping syndrome. The drug is administered by injection and works by suppressing hormone secretion from pituitary and gastrointestinal sources.
What is Pasireotide used for?
Pasireotide is educationally associated with: Control hypercortisolism, Reduction of GH and IGF-1 levels, Management of neuroendocrine tumors, Normalize IGF‑1 and GH levels, Treatment of Cushing's disease, Treatment of acromegaly, Reduction of ACTH secretion. Educational only — not medical advice.
How is Pasireotide administered?
Recorded routes of administration: Intramuscular, Subcutaneous.
What are the potential side effects of Pasireotide?
Reported adverse effects include: Hyperglycemia, Injection site reactions, Cholelithiasis, Nausea, Hyperglycemia / diabetes mellitus, Gallbladder disease, Adrenal insufficiency, QT prolongation, Diarrhea. This list is not exhaustive — consult a qualified clinician.
Who should avoid Pasireotide?
Recorded contraindications: Severe hepatic impairment (Child-Pugh C), Severe hepatic impairment, Significant bradycardia or conduction abnormalities, Hypersensitivity to pasireotide or excipients, Uncontrolled Diabetes Mellitus. Consult a qualified clinician before use.