pasireotide pamoate: clinical use

Prescribing considerations

• Establish glycaemic status and optimise poorly controlled diabetes before treatment.
• Assess cardiovascular history, QT-risk factors and medicines that slow heart rate or prolong QT.
• Use caution in severe renal impairment or end-stage renal disease because unbound exposure may increase.
• Clinical benefit and biochemical response should be reviewed periodically; excessive hormonal suppression may require treatment modification.
• Safety and efficacy have not been established in people younger than 18 years.

Contraindications and cautions

• Hypersensitivity to pasireotide or an excipient.
• Severe hepatic impairment.

Monitoring

• Fasting plasma glucose, HbA1c and symptoms of hyperglycaemia or ketoacidosis.
• Liver function before and during treatment.
• ECG, heart rate, potassium and magnesium where indicated.
• Cortisol and symptoms of adrenal insufficiency in Cushing’s disease.
• Growth hormone and IGF-1 in acromegaly.
• Gallbladder ultrasound and symptoms of biliary disease.
• Other pituitary function, including thyroid function, as clinically appropriate.
• Coagulation parameters when relevant anticoagulants are used.

Clinical pharmacology

An injectable cyclohexapeptide somatostatin analogue with broad receptor binding and particularly high affinity for somatostatin receptor subtype 5. The pamoate product uses biodegradable microspheres for prolonged intramuscular release and is eliminated mainly through hepatic and biliary pathways.

Formulation and product differences

• The pamoate formulation is a powder and solvent reconstituted as a long-acting intramuscular microsphere suspension.
• It differs from pasireotide diaspartate solution for subcutaneous injection; the formulations should not be treated as directly interchangeable.
• The suspension must be prepared immediately before administration and given by a trained healthcare professional.

Injection

Route: Parenteral

Strengths: 10 mg, 20 mg, 30 mg, 40 mg, 60 mg