Quick answer: what is Pasireotide?
Pasireotide is a second-generation somatostatin analog that binds a broader set of somatostatin receptors than octreotide or lanreotide.
Quick facts
- Class
- Multi-receptor somatostatin analog
- Brand names
- Signifor, Signifor LAR
- Approved for
- Cushing's disease; acromegaly
- Key distinction
- Binds SSTR1,2,3,5 — broader than octreotide/lanreotide
- Status
- FDA-approved, prescription-only
- Targets
- Somatostatin receptors SSTR1, 2, 3, 5
- Key use
- Cushing's disease (rare among drugs)
- Signature risk
- Hyperglycemia / new diabetes
Key takeaways
- That wider binding lets it treat Cushing's disease, where it lowers ACTH and cortisol, as well as acromegaly.
- Its defining drawback is a strong tendency to raise blood sugar, so glucose monitoring is essential.
- It is FDA-approved and prescription-only, used for difficult pituitary conditions.
Overview
Pasireotide is a second-generation somatostatin analog designed to bind a wider range of somatostatin receptor subtypes than octreotide or lanreotide. That broader binding — particularly a strong affinity for SSTR5 — lets it work where the older analogs fall short, most notably in Cushing's disease.[1]
It is a specialist drug for difficult pituitary conditions, and its use is shaped by a distinctive side effect: a marked tendency to raise blood sugar.[2]
How it works
Where octreotide targets mainly SSTR2, pasireotide activates SSTR1, 2, 3, and especially SSTR5. In Cushing's disease, the ACTH-secreting pituitary tumors express abundant SSTR5, so pasireotide can suppress the excess ACTH — and therefore cortisol — that older analogs do not reach.[1] In acromegaly it suppresses growth hormone through the same broad receptor engagement.[3]
Clinical uses & evidence
Cushing's disease
Pasireotide is one of the few medical therapies that directly targets the pituitary source of Cushing's disease, lowering cortisol in a meaningful fraction of patients for whom surgery has failed or is not an option.[1]
Acromegaly
In acromegaly it can control growth hormone and IGF-1 in some patients who do not respond adequately to first-generation analogs.[3][4]
Forms & how it's given
Pasireotide is available as a twice-daily subcutaneous injection and as a long-acting monthly depot, chosen and titrated by an endocrinologist. Because of its effect on glucose, blood-sugar monitoring is an essential part of treatment. It is prescription-only; we do not provide dosing instructions.
Safety & legal status
The signature safety concern is hyperglycemia: pasireotide suppresses insulin and incretin hormones more than other analogs, and many patients develop high blood sugar or diabetes requiring treatment.[2] It shares the gallstone and gastrointestinal risks of the class. It is an FDA-approved, prescription-only medicine used under close specialist monitoring.
Frequently asked questions
What is pasireotide used for?
Pasireotide is used for Cushing's disease — where its strong SSTR5 binding suppresses the excess ACTH driving cortisol — and for acromegaly not adequately controlled by first-generation somatostatin analogs. It is a specialist medicine for these pituitary conditions.
How is pasireotide different from octreotide?
Octreotide mainly targets one somatostatin receptor subtype (SSTR2), while pasireotide binds four (SSTR1, 2, 3, and especially 5). That broader reach lets pasireotide work in Cushing's disease, but it also drives a much higher risk of raised blood sugar.
Why does pasireotide raise blood sugar?
Pasireotide suppresses insulin and the incretin hormones more strongly than other somatostatin analogs, so many patients develop hyperglycemia or diabetes during treatment. Blood-sugar monitoring and management are a routine part of using it.
Is pasireotide FDA-approved?
Yes. Pasireotide (Signifor, Signifor LAR) is an FDA-approved, prescription-only medicine used under close specialist monitoring, particularly because of its effect on blood glucose.
References
Each source links to its original record — peer-reviewed studies, regulator pages, or reference texts, labelled by type. We summarize findings neutrally; a citation is a reference, not an endorsement, and not a claim that its authors reviewed this page.
- Pivonello R, De Leo M, Cozzolino A, et al. The Treatment of Cushing's Disease. Endocr Rev. 2015. Peer-reviewed study
- Witek P, Bolanowski M, Krętowski A, et al. Pasireotide-induced hyperglycemia in Cushing's disease and Acromegaly: A clinical perspective and algorithms proposal. Front Endocrinol (Lausanne). 2024. Peer-reviewed study
- McKeage K. Pasireotide in Acromegaly: A Review. Drugs. 2015. Peer-reviewed study
- Colao A, Grasso LFS, Giustina A, et al. Acromegaly. Nat Rev Dis Primers. 2019. Peer-reviewed study