Pasireotide
Somatostatin analogues
Somatostatin analogues
A somatostatin analogue that reaches more receptor types, including SSTR5. It lowers ACTH and cortisol in Cushing's disease, and GH in acromegaly.
Quick facts
- Group
- Somatostatin analogues
- Target
- Somatostatin receptors, highest affinity for SSTR5
- Used for
- Cushing's disease
- Key effects
- Hyperglycaemia and diabetes · Diarrhoea · Headache
- Monitor
- Fasting glucose and HbA1c before · Cortisol · ECG
- ATC
- H01CB05
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows pasireotide itself bound to the human SSTR5 receptor with its Gi protein (cryo-EM).
Pasireotide binds four of the five somatostatin receptor types (1, 2, 3 and 5), with its highest affinity for SSTR5, which corticotroph adenomas express. Through these Gi-coupled receptors it inhibits ACTH secretion, so cortisol falls in Cushing's disease, and it inhibits growth hormone secretion in acromegaly. It also lowers insulin and the incretins GLP-1 and GIP, so blood glucose usually rises.
- Pasireotide binds SSTR5 (and SSTR1, 2, 3)
- Corticotroph ACTH and somatotroph GH secretion fall
- Cortisol and IGF-1 decrease
- Insulin and incretins fall, so glucose rises
Indications
- Cushing's disease in adults who cannot have pituitary surgery or were not cured by it Cushing syndrome →
- Acromegaly when surgery is not an option or has not worked (long-acting form) Acromegaly and gigantism →
Adverse effects
Common
- Hyperglycaemia and diabetes, common and often needing treatment
- Diarrhoea, nausea, abdominal pain
- Injection-site reactions
- Headache, tiredness and hair loss
Contraindications
- Hypersensitivity to pasireotide
- Caution: uncontrolled diabetes, recent heart attack, heart failure, long QT, uncorrected low potassium or magnesium
Key interactions
- Insulin and oral antidiabetic drugs
- Hyperglycaemia often needs new or intensified treatment
- Other drugs that prolong the QT interval or slow the heart
- Additive QT prolongation and bradycardia
What is monitored
- Fasting glucose and HbA1c before and during treatment
- Cortisol (Cushing's) or GH and IGF-1 (acromegaly)
- ECG, potassium and magnesium
- Liver tests and gallbladder symptoms
Administration and safety
- Two forms that are not interchangeable: subcutaneous solution and intramuscular long-acting suspension
- The subcutaneous form may be given at home after training; the intramuscular form is given into the buttock by a health professional
- Look-alike risk with octreotide and lanreotide: confirm the drug and form
Pregnancy and breastfeeding
Information in pregnancy is limited. As cortisol falls, fertility may recover and unplanned pregnancy becomes possible.
Nursing care
- Check glucose regularly and teach the signs of high blood sugar
- Teach the signs of low cortisol: tiredness, weakness, nausea, dizziness
- Check heart rate and ECG results
- Advise reliable contraception if pregnancy is not wanted, since fertility may improve
Pharmacokinetics
- Absorption
- Short-acting solution given subcutaneously; long-acting suspension given intramuscularly
Test yourself
Think of the answer, then tap the question to see it.
Why does pasireotide work in Cushing's disease when octreotide usually does not?
Corticotroph adenomas express mainly SSTR5, and pasireotide has its highest affinity for SSTR5.
Why does pasireotide often cause hyperglycaemia?
It suppresses insulin and the incretins GLP-1 and GIP, so glucose tolerance worsens more than with other analogues.
Which hormone deficiency can pasireotide cause in Cushing's disease?
Hypocortisolism (adrenal insufficiency) from excessive ACTH suppression.
Connections
← Back to the class: Somatostatin analogues
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Pasireotide Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.