Pasireotide

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Pasireotide
Pasireotide.svg
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
  • (Prescription only)
Subcutaneous
Identifiers
396091-73-9 YesY
H01CB05
PubChem CID 9941444
DrugBank DB06663 N
UNII 98H1T17066 YesY
KEGG D10147 N
ChEBI CHEBI:72312 N
Synonyms SOM230
Chemical data
Formula C58H66N10O9
1107.26 g/mol
 N (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[edit]

  1. ^ Signifor® (pasireotide) Official Website for healthcare professionals outside the US http://www.signifor.com/
  2. ^ "Novartis drug Signifor® approved in the EU as the first medication to treat patients with Cushing's disease". Retrieved 2012-07-08. 
  3. ^ Mancini, Tatiana; Porcelli, Teresa; Giustina, Andrea (2010). "Treatment of Cushing disease: overview and recent findings". Therapeutics and Clinical Risk Management 6: 505–16. doi:10.2147/TCRM.S12952 (inactive 2015-02-01). PMC 2963160. PMID 21063461. 
  4. ^ Colao et al. (2011). "Pasireotide (SOM230) demonstrates efficacy in patients with Cushing's disease: results from a large, randomized-dose, double-blind, Phase III study". Endocrine Abstracts 26: 265. 
  5. ^ Boscaro M, Ludlam WH, Atkinson B et al. (January 2009). "Treatment of pituitary-dependent Cushing's disease with the multireceptor ligand somatostatin analog pasireotide (SOM230): a multicenter, phase II trial". The Journal of Clinical Endocrinology and Metabolism 94 (1): 115–22. doi:10.1210/jc.2008-1008. PMID 18957506. 
  6. ^ EMEA Approval for Pasireotide
  7. ^ "FDA Approves Pasireotide for Cushing's Disease".