Romosozumab

Romosozumab
Monoclonal antibody
TypeWhole antibody
SourceHumanized (from mouse)
TargetSclerostin
Names
Trade namesEvenity
Other namesAMG 785, romosozumab-aqqg
Clinical data
Main usesOsteoporosis[1]
Side effectsHeadache, joint pain, allergic reaction[2]
Pregnancy
category
  • AU: B3
  • US: N (Not classified yet)
Typical dose210 mg[1]
External links
AHFS/Drugs.comMonograph
MedlinePlusa619026
Legal
License data
Legal status
  • AU: S4 (Prescription only)
  • US: ℞-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Chemical and physical data
FormulaC6452H9926N1714O2040S54
Molar mass145877.58 g·mol−1

Romosozumab, sold under the brand name Evenity, is a medication used to treat osteoporosis.[1] It decreases the risk of fractures of the spine.[1] It is used by injection under the skin.[1]

Common side effect include headache, joint pain, and allergic reactions.[2] It may increase the risk of heart attacks and strokes and do so more than other similar agents.[3][4] Other side effects may include low calcium.[1] It is a monoclonal antibody that attaching to and blocks sclerostin.[1] This increases bone formation and reduces bone breakdown.[1]

Romosozumab was approved for medical use in the United States and Europe in 2019.[1][3] In the United States it costs about $2,050 a month as of 2021.[5] This amount in the United Kingdom costs the NHS about £430 and 680 CAD in Canada.[2][4]

Medical uses

Romosozumab is used for osteoporosis to decrease the risk of fractures.[6] Two trials found that it reduced the rate of vertebral fracture. In one, there was a 73% lower risk of vertebral fracture after one year, and the benefit was maintained after a second year of taking denosumab. In the other, one year of romosozumab followed by one year of alendronate had a 50% vertebral fracture reduction compared to two years of alendronate.[6]

Dosage

It is used at a dose of 210 mg once a month for up to a year.[1]

Side effects

Common side effects include headache, joint pain, and pain at the site of injection.[7] It may increase the risk of heart attacks, strokes, and deaths from cardiovascular disease.[7] The risk of heart problems is 0.8% over 2.7 years compared to 0.3% with the alternative alendronate.[4]

Mechanism of action

Mechanism of romosozumab[8]

Romosozumab inhibits sclerostin from inhibiting bone formation which it usually does via binding to LDL receptor-related proteins 5/6 of osteoblasts. As a consequence, Romosozumab permits Wnt signaling in osteoblasts which promotes bone formation [8]

Chemistry

Romosozumab is a biologic drug classified as a humanized monoclonal antibody with a large molecular weight of approximately 145.8 kDa and a complex chemical formula C6452​H9926​N1714​O2040​S54​. This drug is made using recombinant DNA technology in Chinese Hamster Ovary cells and comes as a clear to light yellow solution with a pH of 5.2. Its chemical feature is its strong binding to the protein sclerostin, effectively inhibiting sclerostins function as a negative regulator of bone formation[9][10][8]

History

Romosozumab was approved for medical use in Japan in January 2019,[6] the United States in April 2019[6] and the European Union in December 2019.[11] It was originally discovered by Chiroscience,[12] which was acquired by Celltech (now owned by UCB).[13] Celltech entered in a partnership with Amgen in 2002 for the product's development.[14]

The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[15]

References

  1. ↑ 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 "Evenity". Archived from the original on 7 January 2021. Retrieved 18 October 2021. Archived 7 January 2021 at the Wayback Machine
  2. ↑ 2.0 2.1 2.2 BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 776. ISBN 978-0-85711-369-6.
  3. ↑ 3.0 3.1 "Romosozumab-aqqg Monograph for Professionals". Drugs.com. Archived from the original on 15 June 2021. Retrieved 18 October 2021.
  4. ↑ 4.0 4.1 4.2 Piotrowski, Steven. "#378 Tony Romo-sozumab: Winning touchdown in osteoporosis or interception for the loss? – CFPCLearn". Archived from the original on 10 December 2024. Retrieved 26 November 2024.
  5. ↑ "Evenity Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 19 April 2021. Retrieved 18 October 2021. Archived 19 April 2021 at the Wayback Machine
  6. ↑ 6.0 6.1 6.2 6.3 Kaplon H, Muralidharan M, Schneider Z, Reichert JM (2020). "Antibodies to watch in 2020". mAbs. 12 (1): 1703531. doi:10.1080/19420862.2019.1703531. PMC 6973335. PMID 31847708.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  7. ↑ 7.0 7.1 "FDA approves new treatment for osteoporosis in postmenopausal women at high risk of fracture". U.S. Food and Drug Administration (FDA) (Press release). 9 April 2019. Archived from the original on 2 May 2019. Retrieved 12 April 2019.
  8. ↑ 8.0 8.1 8.2 Lim, Sian Yik; Bolster, Marcy B. (13 April 2017). "Profile of romosozumab and its potential in the management of osteoporosis". Drug Design, Development and Therapy. 11: 1221–1231. doi:10.2147/DDDT.S127568. Archived from the original on 28 September 2022. Retrieved 13 February 2024.{{cite journal}}: CS1 maint: unflagged free DOI (link) Archived 28 September 2022 at the Wayback Machine
  9. ↑ "Romosozumab". go.drugbank.com. Archived from the original on 1 October 2025. Retrieved 6 October 2025.
  10. ↑ "Romosozumab". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases. 2012. Archived from the original on 4 February 2025. Retrieved 6 October 2025.
  11. ↑ Victoria Rees (13 December 2019). "EC approves treatment for severe osteoporosis postmenopausal women". European Pharmaceutical Review. Archived from the original on 28 February 2020. Retrieved 27 February 2020. Archived 28 February 2020 at the Wayback Machine
  12. ↑ Quested T (7 June 2015). "Cream of life science entrepreneurs' first venture was selling doughnuts". Business Weekly. Cambridge, England: Q Communications. Archived from the original on 24 December 2018. Retrieved 24 December 2018. Archived 24 December 2018 at the Wayback Machine
  13. ↑ Winkler DG, Sutherland MK, Geoghegan JC, Yu C, Hayes T, Skonier JE, et al. (December 2003). "Osteocyte control of bone formation via sclerostin, a novel BMP antagonist". The EMBO Journal. 22 (23): 6267–6276. doi:10.1093/emboj/cdg599. PMC 291840. PMID 14633986.
  14. ↑ "Celltech group Interim Report 2002" (PDF). Celltech Group plc. Archived (PDF) from the original on 19 February 2019. Retrieved 24 July 2021. Archived 19 February 2019 at the Wayback Machine
  15. ↑ "New Drug Therapy Approvals 2019". U.S. Food and Drug Administration. 31 December 2019. Archived from the original on 16 September 2020. Retrieved 15 September 2020. Archived 16 September 2020 at the Wayback Machine

External links

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