Pasireotide

Pasireotide
Names
Trade namesSignifor, Signifor LAR
Other namesSOM230
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
Drug classSomatostatin analog[1]
Main usesCushing's disease, acromegaly[1]
Side effectsHigh blood sugar, diarrhea, abdominal pain, nausea, gallstones, injection site reactions, tiredness[2]
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Pregnancy
category
  • AU: B3
  • US: N (Not classified yet)
    Routes of
    use    		Subcutaneous injection, intramuscular injection
    External links
    AHFS/Drugs.comMonograph
    Legal
    License data
    Legal status
    • UK: POM (Prescription only)
    • US: ℞-only
    • EU: Rx-only
    • In general: ℞ (Prescription only)
    Chemical and physical data
    FormulaC58H66N10O9
    Molar mass1047.227 g·mol−1
    3D model (JSmol)
    SMILES
    • C1[C@H](CN2[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C2=O)CC3=CC=CC=C3)CC4=CC=C(C=C4)OCC5=CC=CC=C5)CCCCN)CC6=CNC7=CC=CC=C76)C8=CC=CC=C8)OC(=O)NCCN
    InChI
    • InChI=1S/C58H66N10O9/c59-27-13-12-22-46-52(69)64-47(30-38-23-25-42(26-24-38)76-36-39-16-6-2-7-17-39)53(70)66-49(31-37-14-4-1-5-15-37)57(74)68-35-43(77-58(75)61-29-28-60)33-50(68)55(72)67-51(40-18-8-3-9-19-40)56(73)65-48(54(71)63-46)32-41-34-62-45-21-11-10-20-44(41)45/h1-11,14-21,23-26,34,43,46-51,62H,12-13,22,27-33,35-36,59-60H2,(H,61,75)(H,63,71)(H,64,69)(H,65,73)(H,66,70)(H,67,72)/t43-,46+,47+,48-,49+,50+,51+/m1/s1 ☒N
    • Key:VMZMNAABQBOLAK-DBILLSOUSA-N ☒N

    Pasireotide, sold under the brand name Signifor, is a medication used to treat Cushing's disease and acromegaly.[1] It is used in Cushing's disease when surgery is not effective, and in acromegaly when neither surgery nor another somatostatin is effective.[1] It is given by injection under the skin or into a muscle.[1]

    Common side effects include high blood sugar, diarrhea, abdominal pain, nausea, gallstones, injection site reactions, and tiredness.[2] Other side effects may include low cortisol, slow heart rate, and liver problems.[3] It is a somatostatin analog which blocks the release of growth hormone and cortisol.[2]

    Pasireotide was approved in Europe and the United States in 2012.[2][3] In the United Kingdom it costs the NHS about £2,300 to £3,200 a month as of 2021.[1] In the United States this amount costs about 15,300 USD.[4]

    Medical uses

    It is used in people who fail or are ineligible for surgical therapy.[5][6][7] A long-acting formulation is used for acromegaly.[8] [2][9]

    Dosage

    For Cushing's it is used at a dose of 600 mcg injected under the skin twice per day; which may be increased to 900 mcg twice per day.[1] A long acting formulation into a muscle every 4 weeks at a dose of 10 to 40 mg may also be used.[1]

    For acromegaly injections of 40 to 60 mg into a muscle every 4 weeks may be used.[1]

    History

    It is an orphan drug approved in the United States[10] and the European Union.[2][11]

    References

    1. 1 2 3 4 5 6 7 8 9 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 995. ISBN 978-0857114105.
    2. 1 2 3 4 5 6 "Signifor EPAR". European Medicines Agency (EMA). Archived from the original on 12 November 2020. Retrieved 13 May 2020. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
    3. 1 2 "Pasireotide Monograph for Professionals". Drugs.com. Archived from the original on 21 August 2021. Retrieved 26 October 2021.
    4. ↑ "Signifor Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 26 October 2021.
    5. ↑ "Pasireotide Orphan Drug Designation and Approval". U.S. Food and Drug Administration (FDA). 24 December 1999. Archived from the original on 21 August 2021. Retrieved 13 May 2020.
    6. ↑ "EU/3/09/671". European Medicines Agency. 17 September 2018. Archived from the original on 8 January 2021. Retrieved 13 May 2020. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
    7. ↑ Mancini T, Porcelli T, Giustina A (October 2010). "Treatment of Cushing disease: overview and recent findings". Therapeutics and Clinical Risk Management. 6: 505–16. doi:10.2147/TCRM.S12952. PMC 2963160. PMID 21063461.
    8. ↑ "Signifor LAR (pasireotide) for injectable suspension". U.S. Food and Drug Administration (FDA). 1 March 2016. Archived from the original on 31 October 2020. Retrieved 13 May 2020.
    9. ↑ Tucker ME (17 December 2014). "FDA Approves Pasireotide for Treating Acromegaly". Medscape. Archived from the original on 27 August 2015. Retrieved 2 August 2015.
    10. ↑ "Drug Approval Package: Signifor (pasireotide) Injection NDA #200677". U.S. Food and Drug Administration (FDA). 24 December 1999. Archived from the original on 9 April 2021. Retrieved 13 May 2020.
    11. ↑ "Summary of Product Characteristics: Signifor" (PDF). European Medicines Agency. Archived (PDF) from the original on 2018-06-14. Retrieved 2021-08-24.
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