Pasireotide

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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
Legal status
  • Prescription only
Routes Subcutaneous
Identifiers
CAS number 396091-73-9 YesY
ATC code H01CB05
PubChem CID 9941444
UNII 98H1T17066 YesY
KEGG D10147 N
ChEBI CHEBI:72312 N
Synonyms SOM230
Chemical data
Formula C58H66N10O9 
Mol. mass 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 et al. Therapeutics and Clinical Risk Management 2010;6:505-516
  4. ^ 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
  5. ^ 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
  6. ^ EMEA Approval for Pasireotide
  7. ^ "FDA Approves Pasireotide for Cushing's Disease".