Signifor LAR

Signifor LAR Uses, Dosage, Side Effects, Food Interaction and all others data.

Signifor LAR is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor, which is used in the treatment of Cushing's disease.

Signifor® is an analogue of somatostatin that promotes reduced levels of cortisol secretion in Cushing's disease patients.

Trade Name Signifor LAR
Availability Prescription only
Generic Pasireotide
Pasireotide Other Names Pasireotida, Pasiréotide, Pasireotide, Pasireotidum
Related Drugs dexamethasone, Decadron, cyproheptadine, octreotide, bromocriptine, mifepristone, Sandostatin, lanreotide, Somatuline Depot
Weight 10mg, 20mg, 30mg, 40mg, 60mg, 0.3mg/ml, 0.6mg/ml, 0.9mg/ml,
Type Intramuscular Powder For Injection, Extended Release, Subcutaneous Solution, Injection
Formula C58H66N10O9
Weight Average: 1047.2062
Monoisotopic: 1046.50142376
Protein binding

Plasma protein binding is 88%.

Groups Approved
Therapeutic Class
Manufacturer
Available Country Canada, United States,
Last Updated: September 19, 2023 at 7:00 am
Signifor LAR
Signifor LAR

Uses

Signifor LAR is a somatostatin analog used in the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery is not appropriate.

For the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery has not been curative or is not an option.

Signifor LAR is also used to associated treatment for these conditions: Acromegaly, Cushing's Disease

How Signifor LAR works

Signifor LAR activates a broad spectrum of somatostatin receptors, exhbiting a much higher binding affinity for somatostatin receptors 1, 3, and 5 than octreotide in vitro, as well as a comparable binding affinity for somatostatin receptor 2. The binding and activation of the somatostatin receptors causes inhibition of ACTH secretion and results in reduced cortisol secretion in Cushing's disease patients. Also this agent is more potent than somatostatin in inhibiting the release of human growth hormone (HGH), glucagon, and insulin.

Toxicity

The most common toxic effects observed are hyperglycemia, cholelithiasis, diarrhea, nausea, headache, abdominal pain, fatigue, and diabetes mellitus.

Food Interaction

No interactions found.

Volume of Distribution

Signifor LAR is widely distributed and has a volume of distribution of >100L.

Elimination Route

The peak plasma concentration of pasireotide occurs in 0.25-0.5 hours. After administration of single and multiple doses, there is dose-proportionoal increases in Cmax and AUC.

Half Life

The half-life is 12 hours.

Clearance

The clearance in healthy patient is ~7.6 L/h and in Cushing’s disease patients is ~3.8 L/h.

Elimination Route

Signifor LAR is eliminated mostly by hepatic clearance (biliary excretion)(about 48%) with some minor renal clearance (about 7.63%).

Innovators Monograph

You find simplified version here Signifor LAR

*** Taking medicines without doctor's advice can cause long-term problems.
Share