Degarelix Injection is a synthetic linear decapeptide amide composed of 10 amino acid residues, but 7 of them have been modified with non natural amino acids. These modifications give it essential structural differences from natural GnRH (decapeptide), and it is precisely these differences that endow it with unique pharmacological properties. Its amino acid sequence (from N-terminus to C-terminus) is as follows: D-2-naphthylalanine (D-2-Nal), D-4-chlorophenylalanine (D-4-Cl Phe), D-3-palmitoylserine (D-3-Pal), serine (Ser), 4-aminophenylalanine derivative (4-Aph (Hor)), D-4-aminophenylalanine derivative (D-4-Aph (Cbm)), leucine (Leu), isoleucine derivative (Ilys), proline (Pro), D-Ala-NH ₂.
Our Products Description






Degarelix COA
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| Certificate of Analysis | ||
| Compound name | Degarelix | |
| Grade | Pharmaceutical grade | |
| CAS No. | 214766-78-6 | |
| Quantity | 50g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090051 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure | ![]() |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.58% |
| Loss on drying | ≤1.0% | 0.47% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.98% |
| Single impurity | <0.8% | 0.57% |
| Total microbial count | ≤750cfu/g | 140 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 400ppm |
| Storage | Store in a sealed, dark, and dry place below -20°C | |
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| Chemical Formula: | C82H103ClN18O16 |
| Exact Mass: | 1630.75 |
| Molecular Weight: | 1632.29 |
| m/z: | 1630.75 (100.0%), 1631.75 (88.7%), 1632.76 (38.8%), 1632.75 (32.0%), 1633.75 (28.3%), 1634.75 (12.4%), 1633.76 (10.4%), 1631.75 (6.6%), 1632.75 (5.9%), 1635.76 (3.6%), 1632.75 (3.3%), 1633.76 (2.9%), 1633.75 (2.6%), 1633.74 (2.1%), 1634.76 (2.0%), 1634.75 (1.9%), 1634.76 (1.3%), 1631.76 (1.1%), 1634.75 (1.1%), 1632.76 (1.0%) |
| Elemental Analysis: | C, 60.34; H, 6.36; Cl, 2.17; N, 15.45; O, 15.68 |

Degarelix Injection is a third-generation long-acting gonadotropin-releasing hormone (GnRH) receptor antagonist, primarily used for androgen deprivation therapy (ADT) in advanced hormone dependent prostate cancer. With its characteristics of no testosterone rebound, 3-day rapid castration, and long-term stable maintenance, it has become the first-line drug of choice for ADT.
First-line androgen deprivation therapy for advanced hormone dependent prostate cancer

The core use of Degarelix is for adult male patients with advanced hormone dependent prostate cancer who require androgen deprivation therapy (ADT). It is currently the only approved long-acting GnRH antagonist that directly competes to block pituitary GnRH receptors, rapidly, stably, and long-term inhibiting testosterone to castration levels (≤ 0.5ng/ml), fundamentally blocking the driving effect of androgens on prostate cancer cells, achieving the core treatment goals of inhibiting tumor proliferation, reducing tumor volume, alleviating clinical symptoms, and prolonging survival. As a revolutionary ADT drug, the basic use value of degarelix is focused on three core advantages, completely solving the fatal defects of traditional GnRH agonists (leuprorelin, goserelin):
Rapid castration, reaching the standard within 3 days: Within 3 days after medication, 96% of patients' testosterone levels drop to castration levels (≤ 0.5ng/ml), and 100% reach the standard within 1 month, while traditional agonists only reach 80% after 2-4 weeks. This can quickly control tumor progression, alleviate clinical symptoms, and seize opportunities for subsequent treatment.

Reference Information Sources
- FDA. 2008. Firmagon (Degarelix Acetate) Approval Letter
- EMA. 2023. Degarelix Summary of Product Characteristics
- China National Medical Products Administration two thousand and ten Approval Document for Injection of Acetic Acid Degarelix
- Chinese Anti Cancer Association Urology Male Reproductive Tumor Professional Committee two thousand and twenty-five Guidelines for Androgen Deprivation Treatment of Prostate Cancer
- Macarius Health. 2026. Degarelix Clinical Utility
Accurate application of prostate cancer in different stages

Metastatic castration sensitive prostate cancer (mHSPC): first-line preferred ADT
MHSCP is a type of prostate cancer that is initially diagnosed with distant metastasis (bone, lymph node, visceral metastasis), has no inhibition of testosterone, and is sensitive to ADT. It accounts for 70% of advanced prostate cancer and is the most important and core application scenario of Degarelix Injection.
Rapid control of tumor progression: 3-day testosterone castration rapidly inhibits tumor cell proliferation and prevents the spread of metastases;
Deep reduction of PSA: PSA decreased by 50% in 2 weeks and 90% in 3 months, significantly better than traditional agonists (70% decrease in 3 months);
Extended survival: The ATHENA Phase III trial confirmed that the progression free survival (PFS) of Degarelix reached 65% at 2 years, significantly higher than the 52% of Leuprorelin, and the overall survival (OS) was extended by 8.2 months;
Reduce the risk of CRPC conversion: Long term stable testosterone without fluctuations reduces androgen receptor (AR) amplification/mutation, resulting in a 30% decrease in CRPC conversion rate.
As the first-line ADT drug for mHSCP, degarelix can be used as a monotherapy or in combination with new endocrine drugs and chemotherapy. It is the basic medication for the full management of mHSCP and is suitable for all newly diagnosed mHSCP patients, especially for those with high tumor burden and rapid progression risk.


Metastatic Castration Resistant Prostate Cancer (mCRPC): Maintaining Castration Basis+Combined Enhancement
MCRPC is a prostate cancer that maintains testosterone levels (≤ 0.5ng/ml) after ADT treatment, but still progresses (PSA elevation, increased/new metastases). The prognosis is extremely poor, with a median survival of only 12-18 months.
Maintaining the foundation of castration: All subsequent treatments of mCRPC (abiraterone, enzalutamide, docetaxel) must be based on continuous castration with testosterone, and long-term stable maintenance of testosterone castration with digareol is necessary to avoid AR reactivation and drug resistance caused by testosterone fluctuations;
Combination therapy enhances efficacy: When combined with new endocrine drugs and chemotherapy, it improves anti-tumor efficacy and prolongs survival.
Degarelix Injection is an essential medication for the full maintenance treatment of mCRPC and cannot be replaced. Clinical data shows that when combined with abiraterone and prednisone, the PSA response rate is 85%, significantly higher than that of monotherapy at 60%, and OS is prolonged by 5.6 months; Combined with enzalutamide, OS was prolonged by 6.3 months, bringing significant survival benefits to mCRPC patients.


Locally advanced prostate cancer (LAPC): neoadjuvant+adjuvant ADT to improve cure rate
LAPC is a stage T3-T4 prostate cancer with no distant metastasis, large tumor volume, and difficult to completely remove by surgery. The 5-year survival rate is only 40-50%. The use of ticagrelor for neoadjuvant ADT (before radical treatment) and adjuvant ADT (after radical treatment) is a key link in the comprehensive treatment of LAPC. Core objectives: Reduce tumor volume, lower clinical staging, minimize lymph node metastasis, lower surgical difficulty, and improve radical resection rate;
Application value: Degarelix rapidly reduces tumor volume by 50% within 2 months, significantly better than the 30% reduction of traditional agonists, creating optimal conditions for curative surgery/radiotherapy, especially suitable for high-risk patients with tumor volume>50cm ³ and T4 stage invasion of surrounding tissues.
Core objectives: eliminate small residual lesions, reduce the risk of recurrence, and prolong disease-free survival (DFS);
Application value: Degarelix has long-term stable castration, with a 5-year DFS of 75%, significantly higher than the 60% of traditional agonists, and a 40% reduction in recurrence rate. It is suitable for all high-risk LAPC patients (Gleason ≥ 8, PSA ≥ 20ng/ml, T3-T4 stage).
Biochemical recurrence of prostate cancer (BCR): salvage ADT, delaying metastasis
BCR is a prostate cancer with no clinically visible metastases after radical surgery/radiotherapy, but with a sustained increase in PSA levels (≥ 0.2ng/ml), with a 5-year metastasis rate of 30-50%. Degarelix is the preferred intervention for salvage ADT in BCR patients.
Rapid inhibition of PSA: PSA decreases by 80% within one month, preventing sustained increase in PSA;
Delaying distant metastasis: Long term control of tumor activity, reducing the risk of bone and lymph node metastasis;
Extended metastasis free survival: The 5-year metastasis free survival rate is 65%, significantly better than traditional agonists.
Suitable for all prostate cancer patients who experience biochemical recurrence after radical treatment, especially for high-risk populations with PSA doubling time<6 months, Gleason ≥ 7 points, and PSA>1ng/ml at the time of recurrence. It can effectively delay disease progression and avoid early metastasis.

Reference Information Sources
- Chinese Anti Cancer Association Urology Male Reproductive Tumor Professional Committee two thousand and twenty-five Prostate Cancer Diagnosis and Treatment Guidelines
- NCCN Guidelines. 2025. Prostate Cancer
- EAU Guidelines. 2025. Prostate Cancer
- PMC. 2025. Degarelix for Metastatic Prostate Cancer: A Systematic Review
- PubMed. 2025. Neoadjuvant and Adjuvant Degarelix for Localized Prostate Cancer
Frequently Asked Questions
Which metabolic pathway does it take in the human body?
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Degarelix mainly undergoes limited hydrolysis in the body through peptidases in the liver and bile, without relying on the CYP450 enzyme system. Pharmacokinetic studies have shown that drugs are rapidly absorbed after subcutaneous injection (peak blood drug value 1-2 hours) and mainly exist in the form of the original drug in plasma and urine. In rats and dogs, approximately 40-50% are excreted through feces and 40-50% through urine; Monkeys mainly rely on feces (50%) and urine as a supplement (22%). In vitro studies have confirmed that Degarek is not a substrate for CYP450 enzymes and does not significantly inhibit CYP1A2, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A4/5, therefore the risk of drug interactions is low.
Why is the half-life of Degarelix three times different in different in vitro models?
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The degradation ability of different metabolic enzyme systems (pancreatic mixed enzyme vs liver homogenate) towards decapeptides varies.
A study published in 2025 compared the in vitro stability of various synthetic peptides and found that Degarelix has a half-life of 84 minutes in pancreatic mixase. But in other studies, it has shown significantly higher stability in plasma and liver microsomes. Uncommon mechanism: Degarelix degradation mainly involves aminopeptidase, serine protease, and trypsin, rather than universal peptidases. The difference in enzyme spectrum composition of in vitro models will directly affect the measured half-life.
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