Approved & therapeutic
Degarelix
Firmagon
Degarelix is a GnRH receptor antagonist for advanced prostate cancer. Unlike GnRH agonists it blocks the receptor directly, so it suppresses testosterone without the initial testosterone surge.
Also known as: FE200486
- Status
- Degarelix is approved by the U.S. FDA and has official prescribing information.
- Evidence
- Approved labeling. Official prescribing information exists, based on clinical trials in people.
- Half-life
- Approximately 53 days after subcutaneous administration, reflecting depot formation at the injection site.
- How it's taken
- Subcutaneous injection into the abdominal region
- Mechanism
- Reproductive axis (GnRH / kisspeptin / oxytocin)
- Pathways
- GnRH, Androgen
How Degarelix works
Degarelix binds pituitary GnRH receptors competitively and reversibly, blocking the receptor rather than first stimulating it. LH and FSH fall within hours and testosterone reaches castrate levels within about three days, with no flare and therefore no need for antiandrogen cover during initiation.
What research has looked at
- No testosterone flare, which removes the risk of transient disease worsening at initiation — the principal clinical argument for antagonists over agonists.
- Castrate testosterone levels are typically reached within three days of the loading dose, faster than with agonists.
- Some evidence suggests a lower cardiovascular event rate than agonists in men with pre-existing cardiovascular disease, though this remains debated.
Evidence level: Approved labeling. Official prescribing information exists, based on clinical trials in people. These are areas studied or reported, not promised effects.
Reported side effects and risks
- Injection-site reactions are common and more prominent than with agonist depots — pain, erythema, swelling and induration, mostly with the loading dose.
- Hot flashes, weight gain, increased transaminases and fatigue.
- QT prolongation has been reported with androgen deprivation therapy generally.
- Decreased bone mineral density with prolonged use.
- Monthly dosing is required, with no longer-interval depot available in the US.
Sources
- FDA approved-drug listing for degarelix · U.S. Food & Drug Administration
- DailyMed prescribing information for degarelix · NIH · DailyMed
- PubMed research on degarelix GnRH antagonist testosterone · NIH · National Library of Medicine
- DrugBank record for degarelix · DrugBank
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Related compounds
Degarelix FAQ
What is Degarelix?
Degarelix is a GnRH receptor antagonist for advanced prostate cancer. Unlike GnRH agonists it blocks the receptor directly, so it suppresses testosterone without the initial testosterone surge.
How does Degarelix work?
Degarelix binds pituitary GnRH receptors competitively and reversibly, blocking the receptor rather than first stimulating it. LH and FSH fall within hours and testosterone reaches castrate levels within about three days, with no flare and therefore no need for antiandrogen cover during initiation.
Is Degarelix FDA approved?
Yes. Degarelix is approved by the U.S. FDA and has official prescribing information. Evidence level: approved labeling. Official prescribing information exists, based on clinical trials in people.
What is the half-life of Degarelix?
Reported half-life: Approximately 53 days after subcutaneous administration, reflecting depot formation at the injection site.
How is Degarelix taken?
Subcutaneous injection into the abdominal region.
What side effects have been reported with Degarelix?
Reported in the sources: Injection-site reactions are common and more prominent than with agonist depots — pain, erythema, swelling and induration, mostly with the loading dose; Hot flashes, weight gain, increased transaminases and fatigue; QT prolongation has been reported with androgen deprivation therapy generally; Decreased bone mineral density with prolonged use; Monthly dosing is required, with no longer-interval depot available in the US.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.