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Degarelix | CAS No: 214766-78-6 | GMP-certified suppliers
A medication that treats advanced hormone-dependent and high-risk localized prostate cancer by providing sustained androgen deprivation therapy to inhibit tumor growth.
Therapeutic categories
Primary indications
- In Canada and the US, degarelix is indicated for the treatment of advanced prostate cancer in patients requiring androgen deprivation therapy
- In the EU, it is more specifically indicated for the treatment of adult male patients with advanced hormone-dependent prostate cancer, and for treatment of high-risk localized and locally advanced hormone-dependent prostate cancer, in combination with radiotherapy or as a neo-adjuvant prior to radiotherapy
Product Snapshot
- Degarelix is a subcutaneous injectable peptide formulated as a lyophilized powder for solution
- It is primarily used for androgen deprivation therapy in advanced hormone-dependent prostate cancer
- Degarelix is approved for use in the US, Canada, and the EU
Clinical Overview
Pharmacodynamically, degarelix acts as a gonadotropin-releasing hormone (GnRH) receptor antagonist. By competitively binding to GnRH receptors in the pituitary gland, degarelix inhibits the receptor’s interaction with endogenous GnRH. This blockade leads to a concentration-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release. The subsequent reduction in LH levels results in decreased testosterone synthesis by the testes, which is therapeutically relevant because testosterone promotes prostate cancer cell growth.
The mechanism of action of degarelix thus involves direct antagonism at the pituitary GnRH receptor, differentiating it from GnRH agonists that initially stimulate hormone release before downregulation. This antagonism leads to rapid and sustained suppression of testosterone without the initial surge in hormone levels seen with agonists, potentially reducing tumor flare risk.
Key pharmacokinetic parameters specific to degarelix’s absorption, distribution, metabolism, and excretion (ADME) are not detailed herein; however, as a peptide compound, it is administered parenterally to maintain bioavailability. Safety considerations include vigilance for potential QTc interval prolongation. This effect warrants ECG monitoring in susceptible patients and consideration during polypharmacy.
Notable marketed formulations include the FDA-approved injectable formulations used in clinical oncology practice since 2008. For API sourcing, ensuring peptide synthesis purity and compliance with relevant pharmacopeial standards is critical given the complexity of unnatural amino acid incorporation and structural fidelity. Quality control should emphasize characterization of peptide sequence, stereochemistry, and absence of impurities to meet stringent regulatory and therapeutic requirements.
Identification & chemistry
| Generic name | Degarelix |
|---|---|
| Molecule type | Small molecule |
| CAS | 214766-78-6 |
| UNII | SX0XJI3A11 |
| DrugBank ID | DB06699 |
Pharmacology
| Summary | Degarelix is a GnRH receptor antagonist that inhibits the binding of endogenous gonadotropin-releasing hormone to its pituitary receptors, resulting in decreased secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This suppression reduces testosterone production by the testes, which is essential for the growth and progression of hormone-dependent prostate cancer. The drug’s primary pharmacodynamic effect is a concentration-dependent decrease in gonadotropin and androgen levels. |
|---|---|
| Mechanism of action | Degarelix competitively inhibits GnRH receptors in the pituitary gland, preventing the release of luteinizing hormone (LH) and follicle stimulating hormone. Reduced LH suppresses testosterone release, which slows the growth and reduces the size of prostate cancers. |
| Pharmacodynamics | Degarelix is a synthetic derivative of GnRH decapeptide, the ligand of the GnRH receptor. Gonadotropin and androgen production result from the binding of endogenous GnRH to the GnRH receptor. Degarelix antagonizes the GnRH receptor which in turn blocks the release of LH and FSH from the pituitary. LF and FSH decreases in a concentration-dependent manner. The reduction in LH leads to a decrease in testosterone release from the testes. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gonadotropin-releasing hormone receptor | Humans | antagonist |
ADME / PK
| Absorption | Degarelix forms a depot at the site of injection after subcutaneous administration from which the drug slowly released into circulation. After a single bolus dose of 2mg/kg, peak plasma concentrations of degarelix occured within 6 hours at a concentration of 330 ng/mL. Ki = 0.082 ng/mL and 93% of receptors were fully suppressed; MRT = 4.5 days. |
|---|---|
| Half-life | Terminal half-life: 41.5 - 70.2 days; Absorption half-life: 32.9 hours; Half-life from injection site: 1.17 days. |
| Protein binding | 90% of the drug is bound to plasma proteins. |
| Metabolism | 70% - 80% of degarelix is subject to peptide hydrolysis during its passage through the hepatobiliary system and then fecally eliminated. No active or inactive metabolites or involvement of CYP450 isozymes. |
| Route of elimination | Fecal (70% to 80%) and renal (20%-30% of unchanged drug) |
| Volume of distribution | Central compartment: 8.88 - 11.4 L; Peripheral compartment: 40.9 L |
| Clearance | Following subcutaneous administration of degarelix to prostate cancer patients the clearance is approximately 9 L/hr. |
Formulation & handling
- Degarelix is a small molecule peptide administered exclusively via subcutaneous injection as a lyophilized powder or solution requiring reconstitution. Its low water solubility necessitates formulation strategies to ensure adequate dissolution and stability in injectable preparations. Given its peptide nature, handling under controlled temperature and protection from enzymatic degradation is critical to maintain potency.
Regulatory status
| Lifecycle | The API has patent protection in Canada that expired in 2018 and in the United States with key expirations between 2021 and 2032, indicating a staggered patent lifecycle. It is currently marketed in the US, Canada, and the EU, reflecting varying levels of market maturity across these regions. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Degarelix is produced by a limited number of originator companies, with branded products primarily marketed under the name Firmagon across the US, Canada, and EU. Multiple patents protect the product, with key US patents extending into the early 2030s, indicating active patent protection and limited presence of generic competition in major markets. |
|---|
Safety
| Toxicity | The most commonly observed adverse reactions (> 10%) during degarelix therapy included injection site reactions (e.g., pain, erythema, swelling, or induration), hot flashes, increased weight, and increases in serum levels of transaminases and gamma-glutamyltransferase (GGT). |
|---|
- May cause localized injection site reactions including pain, erythema, swelling, and induration
- Potential for systemic effects such as elevated serum transaminases and gamma-glutamyltransferase levels
- Handling precautions advised due to possible induction of hot flashes and weight increase in exposed individuals
Degarelix is a type of Gonadotrophic
Gonadotrophic is a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that plays a crucial role in reproductive health. It includes a group of naturally occurring hormones known as gonadotropins, which are produced by the pituitary gland. These hormones, namely follicle-stimulating hormone (FSH) and luteinizing hormone (LH), regulate the reproductive processes in both males and females.
Gonadotrophic APIs are commonly used in various medical applications, particularly in the field of assisted reproductive technology (ART) and fertility treatments. They stimulate the development of ovarian follicles in females, promoting ovulation and enhancing the chances of successful conception. In males, these APIs stimulate the production of sperm cells and support the production of testosterone.
The pharmaceutical industry produces gonadotrophic APIs through advanced biotechnology techniques, such as recombinant DNA technology. This process involves the use of genetically engineered cells, typically from Chinese hamster ovary (CHO) cells, to produce highly pure and bioactive forms of FSH and LH.
Gonadotrophic APIs are typically formulated into injectable preparations, ensuring their efficient delivery and absorption into the bloodstream. These formulations are administered under the guidance of healthcare professionals and require precise dosing to achieve optimal therapeutic outcomes.
Overall, gonadotrophic APIs have revolutionized the field of reproductive medicine, providing effective solutions for infertility and hormonal imbalances. Their usage has helped countless individuals and couples to overcome fertility challenges and realize their dreams of starting a family.
Degarelix (Gonadotrophic), classified under Hormonal Agents
Hormonal agents are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the medical field. These substances play a crucial role in regulating and modulating hormonal functions within the body. Hormonal agents are designed to mimic or manipulate the effects of naturally occurring hormones, allowing healthcare professionals to treat various endocrine disorders and hormonal imbalances.
Hormonal agents are commonly employed in the treatment of conditions such as hypothyroidism, hyperthyroidism, diabetes, and hormonal cancers. These APIs work by interacting with specific hormone receptors, either by stimulating or inhibiting their activity, to restore the balance of hormones in the body. They can be administered orally, intravenously, or through other routes depending on the specific medication and patient needs.
Pharmaceutical companies employ rigorous manufacturing processes and quality control measures to ensure the purity, potency, and safety of hormonal agent APIs. These APIs are synthesized using chemical or biotechnological methods, often starting from natural hormone sources or through recombinant DNA technology. Stringent regulatory guidelines are in place to guarantee the efficacy and safety of hormonal agent APIs, ensuring that patients receive high-quality medications.
As the demand for hormone-related therapies continues to grow, ongoing research and development efforts focus on enhancing the effectiveness and reducing the side effects of hormonal agent APIs. This includes the exploration of novel delivery systems, advanced formulations, and targeted drug delivery methods. By continuously advancing our understanding and capabilities in hormonal agents, the medical community can improve patient outcomes and quality of life for individuals with hormonal disorders.
Degarelix API manufacturers & distributors
Compare qualified Degarelix API suppliers worldwide. We currently have 7 companies offering Degarelix API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, USDMF | 229 products |
| Hainan Shuangcheng | Producer | China | China | CoA | 11 products |
| Hybio Pharmaceutical Co L... | Producer | China | China | BSE/TSE, CoA, GMP, MSDS, USDMF | 34 products |
| Polypeptide Labs | Producer | Sweden | Sweden | CoA, GMP | 21 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF | 144 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, USDMF | 757 products |
| Suzhou Tianma Pharma Grou... | Producer | China | China | BSE/TSE, CoA, EDMF/ASMF, GMP, JDMF, KDMF, MSDS, USDMF | 25 products |
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