Degarelix
Degarelix is an FDA-approved GnRH receptor antagonist. Degarelix binds GnRH receptors on pituitary gonadotrophs competitively and reversibly, immediately blocking the receptor rather than first overstimulating it. Luteinising hormone and follicle-stimulating hormone fall within hours and testosterone follows, avoiding the testosterone flare and the tumour-symptom worsening that can accompany initiation of a GnRH agonist.
For research use only.
Key Facts
- CAS
- 214766-78-6
- Molecular Weight (MW)
- 1632.3 g/mol
- Half-life
- —
- FDA status
- Approved
- Administration Route
- subcutaneous
- Frequency
- —
- Last updated
- Aug 30, 2026
- Reviewed
- Aug 30, 2026
Research summary
Gonadotropin-releasing hormone receptor antagonist approved for advanced hormone-sensitive prostate cancer. Unlike GnRH agonists it lowers testosterone without an initial surge.
Peptide Library's Degarelix profile summarises 5 cited studies listed in the Science section, the compound's regulatory status, and research-protocol parameters reported for it. It is a research reference, not medical advice.
Protocol
- Dosage Range
- —
- Frequency
- —
- Cycle
- —
- Administration Route
- subcutaneous
- Reconstitution Guide
- —
Not yet checked against primary sources
These figures are compiled from earlier reference material. They have not been verified against FDA labelling, registered trials or published literature, no citation is attached to them, and none of them is a recommended dose. Degarelix is queued for dosage evidence review.
Compare reported doses across the whole librarySequence & molecular data
| Molecular formula | C82H103ClN18O16 |
|---|---|
| Molecular weight | 1632.3 g/mol |
| CAS number | 214766-78-6 |
| PubChem CID | 16136245 |
| FDA UNII | SX0XJI3A11 |
| ChEMBL | CHEMBL415606 |
| DrugBank | DB06699 |
Identifiers link to the public PubChem, FDA Substance Registration (UNII), ChEMBL and DrugBank records for the same entity.
Science
Mechanism of Action
Degarelix binds GnRH receptors on pituitary gonadotrophs competitively and reversibly, immediately blocking the receptor rather than first overstimulating it. Luteinising hormone and follicle-stimulating hormone fall within hours and testosterone follows, avoiding the testosterone flare and the tumour-symptom worsening that can accompany initiation of a GnRH agonist.
Studies
- Cambridge Neoadjuvant Cancer of the Prostate (CANCAP03): A Window Study into the Effects of Olaparib ± Degarelix in Primary Prostate Cancer
- ARNEO: A Randomized Phase II Trial of Neoadjuvant Degarelix with or Without Apalutamide Prior to Radical Prostatectomy for High-risk Prostate Cancer
- Cardiovascular Safety of Degarelix Versus Leuprolide in Patients With Prostate Cancer: The Primary Results of the PRONOUNCE Randomized Trial
- The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer
- Relationship between [(18)F]PSMA-1007 PET parameters and biochemical recurrence-free survival in high-risk prostate cancer patients receiving neoadjuvant hormonal treatment
Regulatory & research status
Degarelix is an FDA-approved product for specific labelled indications. Approval does not extend to the research contexts described on this page, and approved products are prescription medicines.
| FDA status | Approved |
|---|---|
| Research status | Approved product (see FDA status) |
| Availability | Prescription-Only |
| WADA (sport) | Unknown / Not Listed |
| Library classification | FDA-Approved |
Benefits
—
Potential Side Effects
No side effects listed yet for this entry.
Storage & stability
Lyophilized (freeze-dried) peptide powder is far more stable than the reconstituted solution. Keep sealed vials cold, dry and away from light; long-term storage is typically frozen, with short-term refrigeration for vials in use.
Once reconstituted in bacteriostatic water, keep the solution refrigerated, avoid repeated freeze–thaw cycles and agitation, and label the vial with the reconstitution date and concentration. Discard any solution that turns cloudy or shows particulates.
Degradation rates differ by sequence: peptides containing methionine, cysteine, asparagine or glutamine are more prone to oxidation and deamidation, so shelf life after reconstitution is compound-specific rather than universal.
Read the full guide: how to store peptides before and after reconstitution →
Source: Manning MC, Chou DK, Murphy BM, Payne RW, Katayama DS. Stability of protein pharmaceuticals: an update. Pharm Res. 2010;27(4):544–575. (PMID 20143256). General guidance for research handling; not product-specific instructions.
Degarelix: frequently asked questions
What is Degarelix?
Gonadotropin-releasing hormone receptor antagonist approved for advanced hormone-sensitive prostate cancer. Unlike GnRH agonists it lowers testosterone without an initial surge.
How does Degarelix work?
Degarelix binds GnRH receptors on pituitary gonadotrophs competitively and reversibly, immediately blocking the receptor rather than first overstimulating it. Luteinising hormone and follicle-stimulating hormone fall within hours and testosterone follows, avoiding the testosterone flare and the tumour-symptom worsening that can accompany initiation of a GnRH agonist.
Is Degarelix FDA approved?
Yes. Degarelix is approved by the FDA, and approved products are prescription medicines. Approval is always for specific indications studied in clinical trials, so an approved status does not mean the compound is approved for every use it is discussed for. Research-chemical material sold under the same name is not the approved product.
What peptides are similar to Degarelix?
Compounds most often compared with Degarelix include Cetrorelix, Ganirelix, Leuprolide and Gonadorelin. They are grouped by shared mechanism or research area rather than by equivalence, and their regulatory status and evidence base differ.
References
- Cambridge Neoadjuvant Cancer of the Prostate (CANCAP03): A Window Study into the Effects of Olaparib ± Degarelix in Primary Prostate Cancer — Clin Cancer Res, 2025External reference
- ARNEO: A Randomized Phase II Trial of Neoadjuvant Degarelix with or Without Apalutamide Prior to Radical Prostatectomy for High-risk Prostate Cancer — Eur Urol, 2023External reference
- Cardiovascular Safety of Degarelix Versus Leuprolide in Patients With Prostate Cancer: The Primary Results of the PRONOUNCE Randomized Trial — Circulation, 2021External reference
- The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer — BJU Int, 2008External reference
- Relationship between [(18)F]PSMA-1007 PET parameters and biochemical recurrence-free survival in high-risk prostate cancer patients receiving neoadjuvant hormonal treatment — Eur J Nucl Med Mol Imaging, 2026External reference
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Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Aug 30, 2026 · Version 1
This Degarelix profile is compiled from published literature (5 cited studies linked above), public regulatory records and chemical registries. It describes what research reports; it is not medical advice, and nothing here is a dosing recommendation for humans. Peptide Library does not sell peptides. Editorial policy · How profiles are compiled · Report an error
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