Pasireotide
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|---|---|
| Systematic (IUPAC) name | |
| [(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3-benzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-15-phenyl-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate | |
| Clinical data | |
| Trade names | Signifor |
| Licence data | EMA:Link |
| Legal status | ℞ Prescription only |
| Routes | Subcutaneous |
| Identifiers | |
| CAS number | 396091-73-9  |
| ATC code | H01CB05 |
| PubChem | CID 9941444 |
| UNII | 98H1T17066 |
| KEGG | D10147  |
| ChEBI | CHEBI:72312 |
| Synonyms | SOM230 |
| Chemical data | |
| Formula | C58H66N10O9 |
| Mol. mass | 1107.26 g/mol |
| (what is this?) (verify) | |
Pasireotide (SOM230, trade name Signifor[1]) is an orphan drug approved in the U.S. and Europe for the treatment of Cushing's disease in patients who fail or are ineligible for surgical therapy.[2][3] It was developed by Novartis. Pasireotide is a somatostatin analog which has a 40-fold increased affinity to somatostatin receptor 5 than other somatostatin analogs.
The drug showed therapeutical potential in a recent study (PASPORT-CUSHINGS B2305) where 162 patients were treated with either 2x 600 µg or 2x 900 µg pasireotide s.c. daily.[4] The effectiveness of the treatment was checked by the UFC-value (urinary free cortisol) after six months of treatment. The mean reduction of UFC after six months was 47.9%, which also lead to amelioration of clinical symptoms such as blood pressure, cholesterol value, and weight loss.[5]
Pasireotide was approved by the EMEA in October 2009[6] and by the FDA in December 2012.[7]
References
- ↑ Signifor® (pasireotide) Official Website for healthcare professionals outside the US http://www.signifor.com/
- ↑ "Novartis drug Signifor® approved in the EU as the first medication to treat patients with Cushing's disease". Retrieved 2012-07-08.
- ↑ Mancini et al. Therapeutics and Clinical Risk Management 2010;6:505-516
- ↑ Colao et al. Pasireotide (SOM230) provides clinical benefit in patients with Cushing’s disease: results from a large, 12-month, randomized-dose, double-blind, Phase III study, Abstract OC1.7. European Neuroendocrine Association (ENEA) 14th Congress, 2010:62-63
- ↑ U.S. National Library of Medicine: Treatment of pituitary-dependent Cushing's disease with the multireceptor ligand somatostatin analog pasireotide (SOM230): a multicenter, phase II trial. http://www.ncbi.nlm.nih.gov/pubmed/18957506?dopt=Abstract
- ↑ EMEA Approval for Pasireotide
- ↑ "FDA Approves Pasireotide for Cushing's Disease".
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