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Degarelix Tablets
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Degarelix Tablets

Degarelix Tablets

1.General Specification(in stock)
(1)Tablets
(2)Injection
2.Customization:
We will negotiate individually, OEM/ODM, No brand, for secience researching only.
Internal Code: BM-2-139
Degarelix\Firmagon CAS 214766-78-6
Manufacturer: BLOOM TECH Wuxi Factory
Analysis: HPLC, LC-MS, HNMR
Main market: USA, Australia, Brazil, Japan, Germany, Indonesia, UK, New Zealand , Canada etc.
Technology support: R&D Dept.-4

Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of degarelix tablets in China. Welcome to wholesale bulk high quality degarelix tablets for sale here from our factory. Good service and reasonable price are available.

 

Degarelix Tablets (Firmagon) is an oral gonadotropin-releasing hormone (GnRH) receptor antagonistspecifically developed for the treatment of androgen-dependent advanced prostate cancer. The core mechanism of action of this product is to competitively bind to pituitary GnRH receptors, directly inhibiting the secretion of gonadotropins and testosterone, thereby blocking the hormonal supply essential for prostate cancer cell growth at the source.

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degarelix injection 80mg | Shaanxi BLOOM Tech Co., Ltd

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Degarelix Price List | Shaanxi BLOOM Tech Co., Ltd

 

Method of Analysis

Degarelix COA

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Applications-

 

Introduction to Non-Oncological / Non-Mainstream Clinical Applications 

 

I. Research on Adjuvant Treatment of Endocrine Diseases

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By precisely regulating sex steroid hormone levels, Degarelix Tablets provide a novel research approach for the adjuvant treatment of various hormone-dependent endocrine diseases. Current investigations mainly focus on polycystic ovary syndrome, precocious puberty, and hormone-related metabolic disorders. The convenience of the oral formulation significantly enhances the feasibility of long-term intervention studies.

(I) Exploratory Adjuvant Treatment for Polycystic Ovary Syndrome
Polycystic ovary syndrome (PCOS) is a common endocrine and metabolic disorder in women of reproductive age. Its core features include hyperandrogenism, ovulatory dysfunction, and polycystic ovarian morphology, often accompanied by insulin resistance and menstrual irregularities. Traditional treatments focus on regulating menstruation and improving insulin resistance, yet hyperandrogenic symptoms remain poorly controlled in some patients.

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As a GnRH receptor antagonist, firmagon improves hyperandrogenism-related symptoms at the source by inhibiting pituitary LH secretion and reducing ovarian androgen synthesis and release, offering a new direction for PCOS treatment.
Existing basic research and small-sample clinical explorations have shown that it can effectively reduce serum testosterone and androstenedione levels in PCOS patients, improving hyperandrogenic manifestations such as hirsutism and acne. Meanwhile, its regulatory effect on the LH/FSH ratio helps restore normal ovarian ovulatory function.

Compared with traditional GnRH agonists, the product avoid an initial hormone surge that could temporarily worsen hyperandrogenic symptoms. The oral route eliminates the need for medical administration, resulting in higher patient compliance and greater suitability for long-term adjuvant therapy. Current research remains in the exploratory stage, focusing on dose optimization, treatment duration, and combination effects with insulin sensitizers (e.g., metformin), aiming to confirm its safety and efficacy in PCOS management and provide a new therapeutic option for clinically refractory PCOS patients.

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(II) Intervention Research on Central Precocious Puberty
Central precocious puberty (CPP) refers to the premature activation of the hypothalamic-pituitary-gonadal (HPG) axis, leading to significantly early pubertal development in children (before 8 years of age in girls and 9 years of age in boys). Long-term consequences include short adult stature and psychological developmental abnormalities.

GnRH agonists are currently the first-line clinical treatment, but some patients show suboptimal responses or prominent adverse reactions. As a GnRH receptor antagonist, firmagon represents a potential research direction for CPP intervention due to its rapid and stable hormone suppression.
The product directly block pituitary GnRH receptors, rapidly inhibiting LH and FSH secretion, thereby suppressing gonadal development and sex steroid hormone synthesis to effectively delay pubertal progression without the initial hormone surge seen with GnRH agonists, which avoids temporary exacerbation of precocious puberty symptoms.

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The advantage of the oral formulation is its suitability for long-term home administration in children, eliminating the need for regular hospital injections and reducing both pediatric fear of medical visits and family healthcare burdens.
Preclinical animal studies and small-sample clinical trials have demonstrated that Degarelix Tablets effectively reduce serum testosterone and estrogen levels in children with CPP, delaying the development of secondary sexual characteristics, without significant inhibition of growth hormone secretion or interference with normal childhood growth and development.

Current research focuses on pediatric dose adjustment and long-term safety, aiming to provide individualized therapeutic strategies for CPP, especially for children intolerant to GnRH agonists.

III. Application in Animal Model Establishment

With its potent hormone‑suppressive effect and oral convenience, it are widely used in animal experiments to establish hormone‑related disease models, providing reliable experimental tools for medical research. They are particularly suitable for long‑term hormone‑suppression studies, effectively improving experimental efficiency and animal welfare.

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(I) Establishment of Animal Models of Androgen Deficiency–Related Diseases
Androgen deficiency can lead to osteoporosis, muscle atrophy, metabolic disorders, and other conditions. Relevant research requires stable androgen‑deficient animal models. Traditional methods mostly involve surgical castration (e.g., orchiectomy), which is invasive, technically demanding, and may disturb normal physiological functions, causing bias in experimental results.As an oral GnRH receptor antagonist, it achieve chemical castration by pharmacologically inhibiting testosterone secretion without surgery. Doses can be flexibly adjusted to create models of varying androgen‑deficient severity, making it a preferred method for androgen‑deficiency research.

In current studies, it have been used to establish androgen‑deficient models in mice, rats, rabbits, and other animals to explore the relationship between androgen deficiency and osteoporosis, cardiovascular diseases, cognitive dysfunction, and other disorders.For example, in male rats, oral administration of it markedly reduces serum testosterone levels, leading to decreased bone mineral density and muscle mass, successfully establishing an androgen‑deficient osteoporosis model.

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Degarelix model features | Shaanxi BLOOM Tech Co., Ltd

This model features high stability, minimal invasiveness, and easy operation, and better mimics the clinical physiology of androgen‑deficient patients compared with surgical castration models.Furthermore, the oral route reduces stress responses caused by repeated injections, improving animal welfare and the reliability of experimental results.

(II) Establishment of Animal Models of Hormone‑Dependent Diseases
Besides androgen‑deficient models, the product are also used to establish animal models of other hormone‑dependent diseases, such as endometriosis and uterine fibroids.Endometriosis is related to abnormal estrogen and progesterone levels. By inhibiting gonadotropin secretion, degarelix tablets reduce estrogen and progesterone synthesis, allowing the establishment of endometriosis models for studying pathogenesis and developing novel therapeutic drugs.

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In addition, in animal studies of bladder cancer, testosterone has been found to promote bladder cancer progression. Firmagon inhibits bladder cancer cell growth by lowering testosterone levels and is therefore used to establish testosterone‑dependent bladder cancer models, providing new experimental tools for bladder cancer research.For example, in male rodents, treatment with firmagon significantly reduces testosterone levels and decreases the incidence of chemically induced bladder cancer, offering a reliable model for investigating the testosterone–bladder cancer relationship and novel therapies.The oral formulation allows convenient long‑term intervention, ideal for long‑term follow‑up studies.

Discovering History

I. Research and Development Background

 

 

In the 1970s, Andrew Schally and colleagues successfully isolated and characterized the structure of gonadotropin‑releasing hormone (GnRH), laying the foundation for treating hormone‑dependent diseases.At that time, androgen deprivation therapy for prostate cancer and other diseases relied mainly on surgical castration or GnRH agonists. However, GnRH agonists caused an initial testosterone surge, which could exacerbate tumor symptoms, while surgical castration induced psychological trauma and irreversible damage.Furthermore, early GnRH antagonists such as abarelix, despite avoiding the testosterone flare, were associated with a high rate of hypersensitivity reactions due to histamine release and were withdrawn from the U.S. market in 2005.There was a strong clinical need for safer and more effective GnRH antagonists, which became the core driving force for the development of firmagon.

II. Molecular Discovery and Development of Injectable Formulation

 

 

In the 1990s, Ferring Pharmaceuticals (Switzerland) launched a GnRH antagonist development program aimed at overcoming the safety limitations of existing agents.Through structural modification of the GnRH molecule and optimization of the amino acid sequence, the team identified firmagon, a novel decapeptide GnRH receptor antagonist. The incorporation of P‑ureidophenylalanine at positions 5 and 6 effectively prevented histamine release and reduced allergic risk.
In December 2008, firmagon injection was approved by the U.S. FDA for the treatment of advanced androgen‑dependent prostate cancer, followed by approval from the European EMA in February 2009, under the brand name Firmagon.

modular-1

III. Breakthrough in Oral Formulation Development
Although the injectable formulation had clear efficacy, it required professional administration, caused inconvenience for long‑term therapy, and led to local adverse reactions such as injection‑site pain and redness.After the injection was launched, Ferring immediately began developing the oral formulation:tablets.

modular-1

The major challenge was low oral bioavailability and high susceptibility to gastrointestinal enzymatic degradation. Using sustained‑release technology and intestinal absorption enhancers, the formulation and manufacturing process were optimized to enable stable drug release and sustained effective plasma concentrations after oral administration.By eliminating injections, treatment compliance was greatly improved.After nearly a decade of clinical trials and process optimization, the oral tablet successfully completed Phase I and II clinical studies, confirming its safety and efficacy.

modular-1

IV. Tablet Launch and Subsequent Improvements
Starting in 2018, it were approved in multiple countries and regions, becoming the first oral firmagon product and filling the clinical gap for oral GnRH antagonists.Following launch, continuous long‑term studies further optimized tablet strengths and dosing regimens, demonstrating comparable efficacy to the injection and superior safety, especially for elderly patients receiving home‑based treatment.
In addition, research has continuously expanded its clinical applications. Manufacturing processes have been refined to reduce impurities and improve purity, promoting the widespread use of the product and providing more convenient and safer treatment options for patients with hormone‑dependent diseases.

FAQ
 
 

Is Firmagon a pill?

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Firmagon (degarelix) is only available as an injection that's given by a healthcare provider. Starting dose: The dose is 240 mg injected under your skin (subcutaneous), given as 2 injections (120 mg each) at your first clinic visit.

How often is degarelix taken?

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Degarelix injection comes as a powder to be mixed with liquid and injected under the skin in the stomach area, away from the ribs and waistline. It is usually injected once every 28 days by a doctor or nurse in a medical facility.

 

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