Product Information
Registration Status: ActiveSIGNIFOR SOLUTION FOR INJECTION 0.3mg/ML is approved to be sold in Singapore with effective from 2013-12-13. It is marketed by NOVARTIS (SINGAPORE) PTE LTD, with the registration number of SIN14457P.
This product contains Pasireotide 0.3mg in the form of INJECTION, SOLUTION. It is approved for SUBCUTANEOUS use.
This product is manufactured by Novartis Pharma Stein AG in SWITZERLAND.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Pasireotide 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.
Indication
For the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery has not been curative or is not an option.
Mechanism of Action
Pasireotide 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.
Pharmacokinetics
- Absorption
- 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.
- Distribution
- Pasireotide is widely distributed and has a volume of distribution of >100L.
- Metabolism
- Metabolism is minimal.
- Elimination
Clearance
The clearance in healthy patient is ~7.6 L/h and in Cushing’s disease patients is ~3.8 L/h.
Toxicity
The most common toxic effects observed are hyperglycemia, cholelithiasis, diarrhea, nausea, headache, abdominal pain, fatigue, and diabetes mellitus.
Active Ingredient/Synonyms
cyclo((4R)-4-(2-aminoethylcarbamoyloxy)-L-prolyl-L-phenylglycyl-D-tryptophyl-L-lysyl-4-O-benzyl-L-tyrosyl-L- phenylalanyl-) | Pasireotida | Pasiréotide | Pasireotidum | Pasireotide |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.