Degarelix

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Degarelix
Clinical data
Trade namesFirmagon, others
Other namesFE-200486
AHFS/Drugs.comMonograph
MedlinePlusa609022
License data
Pregnancy
category
GnRH antagonist; Antigonadotropin
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)[2]
  • US: ℞-only[3]
  • EU: Rx-only[4]
  • In general: ℞ (Prescription only)
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Degarelix, sold under the brand name Firmagon among others, is a

hormonal therapy used in the treatment of prostate cancer.[3][5]

tumours and therefore reducing circulating testosterone to very low (castration) levels is often the treatment goal in the management of advanced prostate cancer. Degarelix has an immediate onset of action, binding to gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland and blocking their interaction with GnRH. This induces a fast and profound reduction in luteinizing hormone (LH), follicle-stimulating hormone (FSH) and in turn, testosterone suppression.[6]

Medical uses

The GnRH antagonist degarelix, through its ability to reduce serum testosterone, is used to treat hormone-sensitive prostate cancer.[7]

Side effects

Degarelix is commonly associated with hormonal side effects such as

subcutaneous injection), degarelix is also associated with injection-site reactions such as injection-site pain, erythema or swelling. Injection-site reactions are usually mild or moderate in intensity and occur predominantly after the first dose, decreasing in frequency thereafter.[7] Less common: Anemia. Diarrhea, nausea. Hyperhidrosis including night sweats, rash. Gynecomastia, testicular atrophy, erectile dysfunction. Increased transaminases. Musculoskeletal pain and discomfort. Dizziness, headache. Insomnia. Weight gain. Chills, fever, fatigue, flu-like illness.[10]

Pharmacology

GnRH agonist leuprorelin (7.5 mg/month).[11]

GnRH antagonists (

testes and subsequently reduces the size and growth of the prostate cancer. This in turn results in a reduction in prostate-specific antigen (PSA) levels in the patient's blood. Measuring PSA levels helps to monitor how patients with prostate cancer are responding to treatment.[medical citation needed
]

Unlike GnRH agonists, which cause an initial stimulation of the

urethral obstruction, and spinal cord compression. Drug agencies have issued boxed warnings regarding this phenomenon in the prescribing information for GnRH agonists. As testosterone surge does not occur with GnRH antagonists, there is no need for patients to receive an antiandrogen as flare protection during prostate cancer treatment. GnRH agonists also induce an increase in testosterone levels after each reinjection of the drug – a phenomenon that does not occur with GnRH antagonists such as degarelix.[medical citation needed
]

GnRH antagonists have an immediate onset of action leading to a fast and profound suppression of testosterone and are therefore especially valuable in the treatment of patients with prostate cancer where fast control of disease is needed.[medical citation needed]

History

In December 2008, the US Food and Drug Administration (FDA) approved degarelix for the treatment of people with advanced prostate cancer.[13][14] It was subsequently approved by the European Commission at the recommendation of the European Medicines Agency (EMA) in February 2009, for use in adult males with advanced, hormone-dependent prostate cancer.[4] Ferring Pharmaceuticals markets the drug under the name Firmagon.[4]

Research

Degarelix is studied for use as a chemical castration agent on men with pedophilia in Sweden.[15] A study demonstrated a reduced the risk score for committing child sexual abuse in men with pedophilic disorder two weeks after initial injection.[16]

See also

References

  1. ^ a b "Degarelix (Firmagon) Use During Pregnancy". Drugs.com. 3 February 2020. Archived from the original on 26 February 2020. Retrieved 25 February 2020.
  2. ^ "Firmagon 120mg Injection - Summary of Product Characteristics (SmPC)". (emc). 15 January 2020. Archived from the original on 26 February 2020. Retrieved 25 February 2020.
  3. ^ a b "Firmagon- degarelix kit". DailyMed. 18 September 2019. Archived from the original on 12 August 2020. Retrieved 26 February 2020.
  4. ^ a b c "Firmagon EPAR". European Medicines Agency (EMA). 10 January 2020. Archived from the original on 26 February 2020. Retrieved 25 February 2020.
  5. ^ "Degarelix Acetate Monograph for Professionals". Drugs.com. 7 October 2019. Archived from the original on 26 February 2020. Retrieved 25 February 2020.
  6. S2CID 2892725
    .
  7. ^
    PMID 28480768
    .
  8. PMID 18801505
    .
  9. PMID 18538469
    .
  10. ^ "Firmagon "Ferring Pharmaceuticals A/S" - Felleskatalogen". www.felleskatalogen.no. Archived from the original on 28 November 2020. Retrieved 5 May 2020.
  11. S2CID 8280692
    .
  12. PMID 18407326
    .
  13. ^ "Drug Approval Package: Degarelix NDA #022201". U.S. Food and Drug Administration (FDA). Archived from the original on 9 August 2020. Retrieved 29 September 2020.
  14. ^ "FDA Approves Ferring Pharmaceuticals' Degarelix (Generic Name) for Treatment of Advanced Prostate Cancer" (Press release). Ferring Pharmaceuticals. 24 December 2008. Archived from the original on 8 June 2011. Retrieved 25 February 2020 – via PR Newswire.
  15. ^ "Pedofiler ska stoppas – med kemisk kastrering". Expressen. Archived from the original on 26 February 2021. Retrieved 4 August 2016.
  16. PMID 32347899
    .
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