Pasireotide
Also known as: Pasireotide acetate, pasireotide diaspartate, Signifor, Signifor LAR, SOM230
Source Pasireotide at Peptiology
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Summary
Pasireotide is a synthetic cyclic peptide somatostatin analogue used primarily for the treatment of Cushing's disease and acromegaly. It is administered by injection and reduces hormone hypersecretion via multi‑receptor somatostatin activation.
Mechanism of Action
Binds somatostatin receptor subtypes 1, 2, 3 and 5 with high affinity, inhibiting secretion of ACTH, GH and other hormones.
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
No sources recorded yet.
Frequently Asked Questions
What is Pasireotide?
Pasireotide is a synthetic cyclic peptide somatostatin analogue used primarily for the treatment of Cushing's disease and acromegaly. It is administered by injection and reduces hormone hypersecretion via multi‑receptor somatostatin activation.
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.