Pegvisomant

Pegvisomant
Names
Trade namesSomavert
Clinical data
Drug classGrowth hormone receptor blocker[1]
Main usesAcromegaly[2]
Side effectsHeadache, diarrhea, joint pain[3]
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
    Routes of
    use    		Subcutaneous[2]
    External links
    AHFS/Drugs.comMonograph
    US NLMPegvisomant
    Legal
    License data
    Legal status
    • AU: S4 (Prescription only)
    • US: ℞-only
    • EU: Rx-only
    Chemical and physical data
    FormulaC990H1532N262O300S7
    Molar mass22 129 g·mol−1 (unpegylated)

    Pegvisomant, sold under the brand name Somavert, is a medication used to treat acromegaly.[2] It maybe used when the condition is not controlled by surgery, radiation therapy and somatostatins.[3] It is given by injection under the skin.[2]

    Most side effects are mild to moderate.[3] Common side effects include headache, diarrhea, and joint pain.[3] Other side effects may include liver problems and low blood sugar.[2] While there is no evidence of harm in pregnancy, such use has not been well studied.[4] It is a growth hormone receptor blocker.[1]

    Pegvisomant was approved for medical use in Europe in 2002 and the United States in 2003.[2][3] In the United Kingdom it costs the NHS about £1,500 a month at 10 mg per day as of 2021.[1] This amount in the United States is about 7,500 USD.[5]

    Medical use

    Long-term treatment studies with pegvisomant as a monotherapy have shown it to be safe,[6] and to date it is the most effective treatment of acromegaly as both a monotherapy and in combination with somatostatin analogues.[7]

    Dosage

    It is started at a dose of 80 mg, 10 mg per day is than given which may be increased up to 30 mg per day.[1]

    Side effects

    Side effects of pegvisomant include reactions at the injection site, swelling of the limbs, chest pain, hypoglycemia, nausea and hepatitis.[8][9]

    Mechanism of action

    Pegvisomant blocks the action of growth hormone on the growth hormone receptor to reduce the production of IGF-1.[10][11] IGF-1 is responsible for most of the symptoms of acromegaly, and the normalization of its levels can control the symptoms.[12]

    Structure

    Pegvisomant is a protein containing 191 amino acid residues to which several polyethylene glycol polymers have been covalently bound in order to slow clearance from the blood.[13] The protein is a modified version of human growth hormone designed to bind to and block the growth hormone receptor. It is manufactured using genetically modified E. coli bacteria.[13]

    History

    Pegvisomant was discovered at Ohio University in 1987 by Distinguished Professor John Kopchick and graduate student Wen Chen at the Edison Biotechnology Institute. After completing clinical trials, it was approved for the treatment of acromegaly by the FDA in 2003 and marketed by Pfizer.[14]

    Research

    It is also being studied as an anti-tumor treatment for certain types of cancers, in combination with other treatments.[15][16]

    See also

    References

    1. 1 2 3 4 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 788. ISBN 978-0857114105.
    2. 1 2 3 4 5 6 "Pegvisomant Monograph for Professionals". Drugs.com. Archived from the original on 27 June 2021. Retrieved 27 October 2021.
    3. 1 2 3 4 5 "Somavert". Archived from the original on 27 February 2021. Retrieved 27 October 2021.
    4. ↑ "Pegvisomant (Somavert) Use During Pregnancy". Drugs.com. Archived from the original on 30 November 2020. Retrieved 27 October 2021.
    5. ↑ "Somavert Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 22 April 2021. Retrieved 27 October 2021.
    6. ↑ Freda PU, Gordon MB, Kelepouris N, Jonsson P, Koltowska-Haggstrom M, van der Lely AJ (March 2015). "Long-term treatment with pegvisomant as monotherapy in patients with acromegaly: experience from ACROSTUDY". Endocrine Practice. 21 (3): 264–74. doi:10.4158/EP14330.OR. PMC 4618502. PMID 25370326.
    7. ↑ Neggers SJ, Muhammad A, van der Lely AJ (2015). "Pegvisomant Treatment in Acromegaly". Neuroendocrinology. 103 (1): 59–65. doi:10.1159/000381644. PMID 25792221. S2CID 19588354.
    8. ↑ Feenstra J, van Aken MO, de Herder WW, Feelders RA, van der Lely AJ (June 2006). "Drug-induced hepatitis in an acromegalic patient during combined treatment with pegvisomant and octreotide long-acting repeatable attributed to the use of pegvisomant". European Journal of Endocrinology. 154 (6): 805–6. doi:10.1530/eje.1.02160. PMID 16728538.
    9. ↑ Moore DJ, Adi Y, Connock MJ, Bayliss S (October 2009). "Clinical effectiveness and cost-effectiveness of pegvisomant for the treatment of acromegaly: a systematic review and economic evaluation". BMC Endocrine Disorders. 9: 20. doi:10.1186/1472-6823-9-20. PMC 2768727. PMID 19814797.
    10. ↑ Kopchick JJ (April 2003). "Discovery and mechanism of action of pegvisomant". European Journal of Endocrinology. 148 Suppl 2: S21-5. doi:10.1530/eje.0.148s021. PMID 12670297.
    11. ↑ Berryman DE, Palmer AJ, Gosney ES, Swaminathan S, DeSantis D, Kopchick JJ (2007). "Discovery and uses of pegvisomant: a growth hormone antagonist". Endokrynologia Polska. 58 (4): 322–9. PMID 18058724.
    12. ↑ CEDAC Final REcommendation on Reconsideration and Reasons for Recommendation: Pegvisomant (Somavert - Pfizer Canada Inc.) (PDF) (Report). Canadian Agency for Drugs and Technologies in Health. August 2, 2006. Archived (PDF) from the original on June 28, 2021. Retrieved June 21, 2021.
    13. 1 2 Scientific Discussion of Somavert (PDF) (Report). European Medicines Agency. 2004. Archived (PDF) from the original on 2018-06-18. Retrieved 2021-06-21.
    14. ↑ "Ohio University, inventors to receive up to $52 million from drug license transactions". Ohio University. Feb 15, 2011. Archived from the original on November 22, 2016. Retrieved June 21, 2021.
    15. ↑ Evans A, Jamieson SM, Liu DX, Wilson WR, Perry JK (August 2016). "Growth hormone receptor antagonism suppresses tumour regrowth after radiotherapy in an endometrial cancer xenograft model". Cancer Letters. 379 (1): 117–23. doi:10.1016/j.canlet.2016.05.031. PMID 27241667.
    16. ↑ Divisova J, Kuiatse I, Lazard Z, Weiss H, Vreeland F, Hadsell DL, et al. (August 2006). "The growth hormone receptor antagonist pegvisomant blocks both mammary gland development and MCF-7 breast cancer xenograft growth". Breast Cancer Research and Treatment. 98 (3): 315–27. doi:10.1007/s10549-006-9168-1. PMID 16541323. S2CID 6234700.
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