Adult: In patients for whom surgery is not an option or has not been curative, or who are inadequately controlled with another somatostatin analogue: As pasireotide pamoate or embonate: Initially, 40 mg every 4 weeks via deep IM inj; may increase to a Max of 60 mg every 4 weeks after 3 months of initial dosing, if necessary. Dose titration or reduction may be required according to individual safety, tolerability, and response (refer to detailed product guidelines).
Intramuscular Cushing's disease
Adult: In patients for whom surgery is not an option or has failed: As pasireotide pamoate: Initially, 10 mg every 4 weeks via deep IM inj. Dose may be titrated every 2-4 months up to Max of 40 mg every 4 weeks. Dose titration, reduction or discontinuation may be required according to individual safety, tolerability, and response (refer to detailed product guidelines).
Subcutaneous Cushing's disease
Adult: In patients for whom surgery is not an option or has failed: As pasireotide diaspartate: Initially, 0.6 mg bid via SC inj for 2 months; may increase to 0.9 mg bid if necessary. Consider treatment discontinuation if there is no response after 2 months. Dose titration, reduction or discontinuation may be required according to individual safety, tolerability, and response (refer to detailed product guidelines).
Hepatic Impairment
Intramuscular: Cushing's disease:
Moderate (Child-Pugh class B): Initially, 10 mg every 4 weeks via deep IM inj. Max recommended dose: 20 mg every 4 weeks. Severe (Child-Pugh class C): Contraindicated.
Acromegaly:
Moderate (Child-Pugh class B): Initially, 20 mg every 4 weeks via deep IM inj. Max recommended dose: 40 mg every 4 weeks. Severe (Child-Pugh class C): Contraindicated.
Subcutaneous: Cushing's disease:
Moderate (Child-Pugh class B): 0.3 mg bid via SC inj. Max recommended dose: 0.6 mg bid. Severe (Child-Pugh class C): Contraindicated.
Reconstitution
IM: Allow to stand at room temperature for at least 30 minutes (Max: 24 hours at room temperature) prior to reconstitution. Add the diluent provided to a vial labelled as containing 10, 20, 40, or 60 mg to provide a solution containing 5, 10, 20, or 30 mg/mL, respectively. Shake moderately in a horizontal direction for at least 30 seconds until a uniform suspension is formed; repeat for another 30 seconds if still incompletely suspended.
Contraindications
Severe hepatic impairment (Child-Pugh class C). Contraindications may vary among countries and individual products (refer to specific product guidelines).
Special Precautions
Patient with pre-existing cardiac disease; risk factors for bradycardia (e.g. high-grade heart block, history of significant bradycardia or acute MI, sustained ventricular tachycardia, ventricular fibrillation, receiving drugs known to cause bradycardia); risk factors for QT prolongation (e.g. congenital long QT syndrome, recent MI, CHF, unstable angina, hypokalaemia, hypomagnesaemia, receiving drugs known to cause QT prolongation); diabetes mellitus, predisposition to hyperglycaemia (e.g. acute illness, infection, alcohol abuse, pancreatic disorders such as pancreatic malignancy, pancreatic surgery). Patients who have undergone transsphenoidal surgery and pituitary irradiation. Moderate hepatic (Child-Pugh class B) and severe renal (including ESRD) impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Bradycardia, QT prolongation; cholelithiasis, cholecystitis, cholangitis, pancreatitis; elevations of liver enzymes; hyperglycaemia, ketoacidosis; hypocortisolism (particularly in patients with Cushing's disease), slight decrease in thyroid function, pituitary hormone deficiency; malabsorption of dietary fats. Endocrine disorders: Adrenal insufficiency, hypoglycaemia. Gastrointestinal disorders: Diarrhoea, abdominal pain, abdominal distension, nausea, vomiting, steatorrhoea, discoloured faeces. General disorders and administration site conditions: Inj site reaction, fatigue. Investigations: Increased HbA1c, GGT, ALT, AST, lipase, and amylase; prolonged prothrombin time. Metabolism and nutrition disorders: Decreased appetite, impaired glucose tolerance. Musculoskeletal and connective tissue disorders: Myalgia, arthralgia. Nervous system disorders: Headache, dizziness. Skin and subcutaneous tissue disorders: Alopecia, pruritus. Vascular disorders: Hypotension.
This drug may cause fatigue and dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Correct hypokalaemia and/or hypomagnesaemia prior to initiation of treatment. Perform ECG at baseline and as clinically indicated; ultrasonic examination of the gallbladder before treatment and every 6-12 months during therapy. Monitor fasting blood glucose and HbA1c prior to initiation, then weekly for the 1st 2-3 months, and periodically thereafter; re-evaluate fasting blood glucose 4 weeks and HbA1c 3 months after discontinuation. Monitor serum potassium and magnesium levels, pituitary function (e.g. TSH, free thyroxine, growth hormone [GH], insulin-like growth factor 1 [IGF-1]), gonadal function, and adrenal function prior to therapy and periodically during treatment; LFTs before treatment, regularly during the 1st 3 months of therapy and as clinically indicated; heart rate (particularly in patients with cardiac disease and/or risk factor for bradycardia). For the treatment of acromegaly: Monitor serum GH and IGF-1 levels at 3 months (before dose adjustment) and as clinically indicated. For the treatment of Cushing's disease: Monitor 24-hour urinary free cortisol at 4 months (before dose adjustment) and as clinically indicated. Assess for signs and symptoms of cholelithiasis, gallbladder problems, adrenal insufficiency, hypokalaemia, hypomagnesaemia, severe metabolic acidosis, hyperglycaemia, hypocortisolism; new or worsening symptoms for possible exocrine insufficiency.
Drug Interactions
Increased risk of QT prolongation with QT-prolonging agents such class Ia antiarrhythmics (e.g. quinidine, procainamide, disopyramide), class III antiarrhythmics (e.g. amiodarone, dronedarone, dofetilide, ibutilide), certain antibacterials (IV erythromycin, pentamidine inj, clarithromycin, moxifloxacin), certain antipsychotics (e.g. chlorpromazine, thioridazine, fluphenazine, pimozide, haloperidol, tiapride, amisulpride, sertindole, methadone), certain antihistamines (e.g. terfenadine, astemizole, mizolastine), antimalarials (e.g. chloroquine, halofantrine, lumefantrine), certain antifungals (e.g. ketoconazole). Increased risk of bradycardia with bradycardic agents such as β-blockers (e.g. metoprolol, carteolol, propranolol, sotalol), acetylcholinesterase inhibitors (e.g. rivastigmine, physostigmine), certain antiarrhythmics, and certain calcium channel blockers (e.g. verapamil, diltiazem, bepridil). May decrease the serum concentration of ciclosporin. May increase serum concentrations of bromocriptine.
Action
Description: Overview: Pasireotide is a cyclohexapeptide somatostatin analogue. Mechanism of Action: Pasireotide inhibits various endocrine, neuroendocrine, and exocrine functions. In Cushing's disease, it binds with high affinity to somatostatin receptor subtypes sst1, sst2, and sst3, with the greatest affinity for sst5. In acromegaly, pasireotide binds to somatostatin receptor subtypes sst2 and sst5. Pharmacodynamics: Somatostatin receptors are widely expressed in various tissues, particularly in neuroendocrine tumours associated with excessive hormone secretion, such as ACTH in Cushing's disease and growth hormone (GH) in acromegaly. In vitro studies demonstrate that corticotroph tumour cells from patients with Cushing's disease express high levels of sst5. The activation of sst5 receptors leads to the inhibition of ACTH secretion and subsequent reduction in cortisol secretion, which helps normalise the mean urinary free cortisol levels. In acromegaly, pasireotide binds to other somatostatin receptors, resulting in suppression of GH secretion. In vivo, it reduces GH and insulin-like growth factor 1 (IGF-1) levels.
Pasireotide-induced hyperglycaemia is attributed to reduced insulin secretion and reduced levels of incretin hormones (e.g. glucagon-like peptide-1, glucose-dependent insulinotropic polypeptide). It appears to moderately inhibit glucagon secretion while peripheral and hepatic insulin sensitivity are unaffected. In addition, pasireotide has been shown to cause a prolongation of the QT interval and a dose-dependent reduction in heart rate. Pharmacokinetics: Absorption: Rapidly absorbed. Time to peak plasma concentration: Within 15-30 minutes. Distribution: Mostly distributed in the plasma. Volume of distribution: >100 L. Plasma protein binding: Approx 88%. Excretion: Mainly via faeces (approx 40-56%, as unchanged drug); urine (approx 6-10%, as unchanged drug). Elimination half-life: Approx 12 hours.
Chemical Structure
Pasireotide Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 9941444, Pasireotide. https://pubchem.ncbi.nlm.nih.gov/compound/Pasireotide. Accessed Sept. 30, 2025.
Storage
Parenteral: Solution for SC inj: Store between 15-30°C. Protect from light. Powder for suspension for IM inj: Store between 2-8°C. Do not freeze.
H01CB05 - pasireotide ; Belongs to the class of antigrowth hormone. Used in hypothalamic hormone preparations.
References
Brayfield A, Cadart C (eds). Pasireotide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/09/2025.Joint Formulary Committee. Pasireotide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/09/2025.Pasireotide. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 08/09/2025.Pasireotide. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 08/09/2025.Pasireotide. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 08/09/2025.Signifor (Recordati Rare Diseases, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 08/09/2025.Signifor 0.3 mg Solution for Injection (Recordati Rare Diseases). MHRA. https://products.mhra.gov.uk. Accessed 08/09/2025.Signifor 20 mg Powder and Solvent for Suspension for Injection (Recordati Rare Diseases). MHRA. https://products.mhra.gov.uk. Accessed 08/09/2025.Signifor LAR (FTA Healthcare Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 08/09/2025.Signifor LAR (Recordati Rare Diseases, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 08/09/2025.
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