Somatostatin analog approved for Cushing's disease and acromegaly when surgery is not possible or has not cured.
Regulatory status
Approved (FDA / EMA)
Family
Somatostatin analog (multireceptor)
Scientific evidence
High
Number of findings
3
Where it acts
Hormones and metabolism · Brain and sleep
Also known as
pasireotide, Signifor, Signifor LAR, SOM230
Regulatory status
FDA (US): Approved (2012, Signifor) for Cushing's disease; Signifor LAR approved in 2014 for acromegaly and in 2020 for Cushing's disease.
EMA (EU): Approved (2012, Signifor) for Cushing's disease; expanded in 2014 to acromegaly (LAR formulation).
Dose
Cushing's: 0.6 or 0.9 mg subcutaneously twice a day (Signifor label; phase 3 trial). Acromegaly: Signifor LAR 40 mg intramuscularly every 4 weeks, adjustable up to 60 mg (FDA/EMA label).
Safety
Hyperglycemia is very common (more than 7 in 10 patients in the Cushing's trial) and often forces the start of antidiabetic drugs; glucose should be monitored before and during treatment. Others: diarrhea, nausea, abdominal pain, gallstones, bradycardia and QT prolongation, adrenal insufficiency from excess effect. Only with a prescription and endocrinology follow-up.
Interactions
Caution with drugs that prolong the QT interval or lower heart rate; may require adjusting insulin and antidiabetic drugs; may reduce absorption of cyclosporine.
Effect by goal · level of evidence
Cortisol control in Cushing's disease
reducesHighRCT (AA)in people
~15–26% normalize cortisol
12-month phase 3 trial with 162 adults: at 6 months, urinary free cortisol normalized in 12/82 patients on 0.6 mg and 21/80 on 0.9 mg twice daily. Levels fell in most patients even if they did not normalize.
12-month trial with 358 treatment-naive patients: biochemical control in 31.3% with pasireotide LAR 40 mg versus 19.2% with octreotide LAR 20 mg. Hyperglycemia in 57.3% versus 21.7%.
It mimics somatostatin, a hormone that slows the secretion of other hormones. Unlike octreotide, it binds strongly to the SST5 receptor, which is abundant in pituitary tumors that produce ACTH. This reduces the production of ACTH (and therefore cortisol) and of growth hormone. It also suppresses insulin and incretins, which explains why glucose rises.
What the evidence says
In people
Cortisol control in Cushing's disease. 12-month phase 3 trial with 162 adults: at 6 months, urinary free cortisol normalized in 12/82 patients with 0.6 mg and 21/80 with 0.9 mg twice daily. Levels fell in most even if they did not normalize. PubMed 22397653
Hyperglycemia as an adverse effect. In the same trial, 118 of 162 patients had hyperglycemia-related effects and 74 needed to start glucose medication. PubMed 22397653
Acromegaly: better control than octreotide. 12-month trial with 358 previously untreated patients: biochemical control in 31.3% with pasireotide LAR 40 mg versus 19.2% with octreotide LAR 20 mg. Hyperglycemia in 57.3% versus 21.7%. PubMed 24423324