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Wikipedia

Pegvisomant

February 13, 2024

Pegvisomant, sold under the brand name Somavert, is a growth hormone receptor antagonist used in the treatment of acromegaly.[1][2][3] It is primarily used if the pituitary gland tumor causing the acromegaly cannot be controlled with surgery or radiation, and the use of somatostatin analogues is unsuccessful, but is also effective as a monotherapy.[4] It is delivered as a powder that is mixed with water and injected under the skin.[5]

Pegvisomant
Clinical data
Trade namesSomavert
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: B3
Routes of
administration		Subcutaneous
ATC code
Legal status
Legal status
Identifiers
CAS Number
  • 218620-50-9 Y
IUPHAR/BPS
  • 7485
DrugBank
  • DB00082 N
ChemSpider
  • none
UNII
  • N824AOU5XV
KEGG
  • D05394 Y
ChEMBL
  • ChEMBL1201515 N
Chemical and physical data
FormulaC990H1532N262O300S7
Molar mass22129.10 g·mol−1
 NY (what is this?)  (verify)

Medical uses edit

Pegvisomant is indicated for the treatment of adults with acromegaly.[1][2]

Side effects edit

Side effects of pegvisomant include reactions at the injection site, swelling of the limbs, chest pain, hypoglycemia, nausea and hepatitis.[6]

Discovery edit

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.[7]

Structure edit

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.[5] 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.[5]

Mechanism of action edit

Pegvisomant blocks the action of growth hormone on the growth hormone receptor to reduce the production of IGF-1.[8][9] IGF-1 is responsible for most of the symptoms of acromegaly, and the normalization of its levels can control the symptoms.[10]

Long-term treatment studies with pegvisomant as a monotherapy have shown it to be safe,[4] and effective.[11]

Research edit

Some studies show the potential of using pegvisomant as an anti-tumor treatment for certain types of cancers.[12][13]

References edit

  1. ^ a b c "Somavert- pegvisomant kit". DailyMed. 18 November 2021. Retrieved 18 May 2022.
  2. ^ a b c "Somavert EPAR". European Medicines Agency. 17 September 2018. Retrieved 18 May 2022.
  3. ^ Schreiber I, Buchfelder M, Droste M, Forssmann K, Mann K, Saller B, Strasburger CJ (January 2007). "Treatment of acromegaly with the GH receptor antagonist pegvisomant in clinical practice: safety and efficacy evaluation from the German Pegvisomant Observational Study". European Journal of Endocrinology. 156 (1): 75–82. doi:10.1530/eje.1.02312. PMID 17218728. S2CID 12121175.
  4. ^ a b 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.
  5. ^ a b c (PDF) (Report). European Medicines Agency. 2004. Archived from the original (PDF) on 18 June 2018. Retrieved 17 February 2011.
  6. ^ 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.
  7. ^ . Ohio University. 15 February 2011. Archived from the original on 22 November 2016. Retrieved 21 November 2016.
  8. ^ 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.
  9. ^ 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.
  10. ^ (PDF) (Report). Canadian Agency for Drugs and Technologies in Health. 2 August 2006. Archived from the original (PDF) on 28 June 2021. Retrieved 22 December 2014.
  11. ^ 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.
  12. ^ 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.
  13. ^ 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.

External links edit

  • "Pegvisomant". Drug Information Portal. U.S. National Library of Medicine.

February 13, 2024
pegvisomant, sold, under, brand, name, somavert, growth, hormone, receptor, antagonist, used, treatment, acromegaly, primarily, used, pituitary, gland, tumor, causing, acromegaly, cannot, controlled, with, surgery, radiation, somatostatin, analogues, unsuccess. Pegvisomant sold under the brand name Somavert is a growth hormone receptor antagonist used in the treatment of acromegaly 1 2 3 It is primarily used if the pituitary gland tumor causing the acromegaly cannot be controlled with surgery or radiation and the use of somatostatin analogues is unsuccessful but is also effective as a monotherapy 4 It is delivered as a powder that is mixed with water and injected under the skin 5 PegvisomantClinical dataTrade namesSomavertAHFS Drugs comMonographLicense dataEU EMA by INN US DailyMed PegvisomantPregnancycategoryAU B3Routes ofadministrationSubcutaneousATC codeH01AX01 WHO Legal statusLegal statusAU S4 Prescription only US only 1 EU Rx only 2 IdentifiersCAS Number218620 50 9 YIUPHAR BPS7485DrugBankDB00082 NChemSpidernoneUNIIN824AOU5XVKEGGD05394 YChEMBLChEMBL1201515 NChemical and physical dataFormulaC 990H 1532N 262O 300S 7Molar mass22129 10 g mol 1 N Y what is this verify Contents 1 Medical uses 2 Side effects 3 Discovery 4 Structure 5 Mechanism of action 6 Research 7 References 8 External linksMedical uses editPegvisomant is indicated for the treatment of adults with acromegaly 1 2 Side effects editSide effects of pegvisomant include reactions at the injection site swelling of the limbs chest pain hypoglycemia nausea and hepatitis 6 Discovery editPegvisomant 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 7 Structure editPegvisomant 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 5 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 5 Mechanism of action editPegvisomant blocks the action of growth hormone on the growth hormone receptor to reduce the production of IGF 1 8 9 IGF 1 is responsible for most of the symptoms of acromegaly and the normalization of its levels can control the symptoms 10 Long term treatment studies with pegvisomant as a monotherapy have shown it to be safe 4 and effective 11 Research editSome studies show the potential of using pegvisomant as an anti tumor treatment for certain types of cancers 12 13 References edit a b c Somavert pegvisomant kit DailyMed 18 November 2021 Retrieved 18 May 2022 a b c Somavert EPAR European Medicines Agency 17 September 2018 Retrieved 18 May 2022 Schreiber I Buchfelder M Droste M Forssmann K Mann K Saller B Strasburger CJ January 2007 Treatment of acromegaly with the GH receptor antagonist pegvisomant in clinical practice safety and efficacy evaluation from the German Pegvisomant Observational Study European Journal of Endocrinology 156 1 75 82 doi 10 1530 eje 1 02312 PMID 17218728 S2CID 12121175 a b 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 a b c Scientific Discussion of Somavert PDF Report European Medicines Agency 2004 Archived from the original PDF on 18 June 2018 Retrieved 17 February 2011 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 Ohio University inventors to receive up to 52 million from drug license transactions Ohio University 15 February 2011 Archived from the original on 22 November 2016 Retrieved 21 November 2016 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 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 CEDAC Final REcommendation on Reconsideration and Reasons for Recommendation Pegvisomant Somavert Pfizer Canada Inc PDF Report Canadian Agency for Drugs and Technologies in Health 2 August 2006 Archived from the original PDF on 28 June 2021 Retrieved 22 December 2014 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 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 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 External links edit Pegvisomant Drug Information Portal U S National Library of Medicine Portal nbsp Medicine Retrieved from https en wikipedia org w index php title Pegvisomant amp oldid 1192897406, wikipedia, wiki, book, books, library,

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