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Ganirelix | CAS No: 124904-93-4 | GMP-certified suppliers
A medication that inhibits premature luteinizing hormone surges during controlled ovarian hyperstimulation in assisted reproduction protocols to improve fertility treatment outcomes.
Therapeutic categories
Primary indications
- Ganirelix is indicated for the inhibition of premature luteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation for assisted reproduction techniques (ART)
- [L43040, L43045]
Product Snapshot
- Ganirelix is a parenteral injectable peptide formulation administered via subcutaneous injection
- It is utilized primarily to inhibit premature luteinizing hormone surges during controlled ovarian hyperstimulation in assisted reproduction procedures
- The product is approved for use in major regulatory markets including the US, EU, and Canada
Clinical Overview
Mechanistically, ganirelix exerts its effects by competitively binding to GnRH receptors in the anterior pituitary gland. By blocking these receptors, it prevents the endogenous GnRH-mediated secretion of pituitary gonadotropins, primarily LH and to a lesser extent follicle-stimulating hormone (FSH). This rapid and reversible suppression of gonadotropin release avoids the initial stimulatory flare effect typically observed with GnRH agonists. The inhibition of premature LH surges is critical during ovarian stimulation to promote optimal follicular maturation and to prevent untimely ovulation and elevated progesterone levels that could adversely affect treatment outcomes.
Pharmacodynamically, ganirelix administration at a typical therapeutic dose of 0.25 mg results in significant reductions from baseline serum concentrations of LH (approximately 74%), FSH (32%), and estradiol (25%) by the end of treatment. The median duration of ganirelix therapy in clinical protocols is about five days, with hormone levels returning to baseline within two days post-treatment cessation.
From an absorption, distribution, metabolism, and excretion (ADME) perspective, ganirelix’s peptidic nature suggests rapid systemic availability following parenteral administration, with a clearance profile consistent with peptidic APIs; detailed pharmacokinetic parameters should be referenced from product-specific technical data.
Safety considerations include its reversible endocrine suppression without the hypoestrogenic side effects or prolonged down-regulation seen with GnRH agonists. However, as with all peptide hormone antagonists, careful patient monitoring is essential to mitigate potential adverse effects related to hormonal manipulation.
Ganirelix has been approved since 1999, with several branded preparations available globally under regulated conditions for use in ART protocols. Drug regulatory approvals emphasize strict adherence to manufacturing and quality standards due to its peptide structure and biological activity.
For API procurement, sourcing ganirelix requires stringent quality assurance measures including verification of peptide sequence integrity, potency, purity, and compliance with relevant pharmacopeial standards. Suppliers should provide comprehensive documentation on manufacturing processes, analytical methods, stability data, and compliance with Good Manufacturing Practice (GMP) to ensure consistent supply suitable for clinical and commercial development.
Identification & chemistry
| Generic name | Ganirelix |
|---|---|
| Molecule type | Small molecule |
| CAS | 124904-93-4 |
| UNII | IX503L9WN0 |
| DrugBank ID | DB06785 |
Pharmacology
| Summary | Ganirelix is a gonadotropin-releasing hormone (GnRH) receptor antagonist that competitively inhibits GnRH receptor signaling in the anterior pituitary. This action rapidly and reversibly suppresses the secretion of luteinizing hormone (LH) and, to a lesser extent, follicle-stimulating hormone (FSH), preventing premature LH surges during controlled ovarian hyperstimulation. By modulating the hypothalamic-pituitary-gonadal axis, ganirelix facilitates synchronized follicular development in assisted reproductive technologies. |
|---|---|
| Mechanism of action | Gonadotropin-releasing hormone (GnRH) is a hypothalamus-derived releasing hormone responsible for the synthesis and release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary. At midcycle, a large increase in GnRH release results in an LH surge, which leads to several physiologic actions such as ovulation, resumption of meiosis in the oocyte, and luteinization. Luteinization results in a rise in serum progesterone with an accompanying decrease in estradiol levels. Controlled ovarian hyperstimulation (COH) is performed in conjunction with other interventions like in vitro fertilization (IVF) during assisted reproductive technology (ART). COH is beneficial as it allows the scheduling of IVF treatments. During this intervention, inhibiting premature surges of LH is important because premature elevated LH levels can hinder effective multiple follicular maturation and can lead to an undesirable increase in progesterone levels. Ganirelix aims to suppress premature LH surges by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathways. Ganirelix-induced suppression of gonadotropin secretion is rapid and reversible. The suppression of pituitary LH secretion by ganirelix is more pronounced than that of FSH. An initial release of endogenous gonadotropins has not been detected with ganirelix, which is consistent with an antagonist effect. |
| Pharmacodynamics | Ganirelix modulates the hypothalamic-pituitary-gonadal axis by causing a rapid, profound, reversible suppression of endogenous gonadotropins. During controlled ovarian stimulation, it suppresses luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion from the pituitary gland. Unlike GnRH agonists that causes an initial increase in gonadotropin levels, ganirelix does not cause this effect before premature LH surge inhibition. Ganirelix is also not associated with hypo‐estrogenic side effects, flare‐up, and a long down‐regulation period induced by GnRH agonists. In patients undergoing controlled ovarian stimulation, the median duration of ganirelix treatment was five days. In one study, multiple-dose administration of 0.25 mg ganirelix decreased serum LH, FSH and estradiol (E2) concentrations from baseline by 74, 32, and 25% after the last dose, respectively. Serum hormone levels returned to pre-treatment levels within two days after the last injection.[L43040, L43045] |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gonadotropin-releasing hormone receptor | Humans | antagonist |
ADME / PK
| Absorption | Ganirelix is rapidly absorbed following subcutaneous administration with a mean absolute bioavailability of approximately 91%. It has a T<sub>max</sub> ranging from one to two hours.[L43040, L43045] Ganirelix reaches steady-state serum concentrations after three days of administration. |
|---|---|
| Half-life | The elimination half-life (t½) following subcutaneous administration of a single 250-mcg dose is approximately 13 hours.[L43040, L43045] |
| Protein binding | _In vitro_ protein binding to human plasma is 81.9%. |
| Metabolism | The metabolites are small peptide fragments formed by enzymatic hydrolysis of ganirelix at restricted sites. The 1–4 peptide and 1–6 peptide of ganirelix are the primary metabolites observed in the feces. |
| Route of elimination | Following single-dose intravenous administration of radiolabeled ganirelix to healthy female volunteers, Ganirelix is the major compound present in the plasma (50–70% of total radioactivity in the plasma) up to 4 hours and urine (17.1–18.4% of administered dose) up to 24 hours. Ganirelix is not found in the feces. On average, 97.2% of the total radiolabeled ganirelix dose is recovered in the feces and urine (75.1% and 22.1%, respectively) over 288 h following intravenous single dose administration of 1 mg [<sup>14</sup>C]-ganirelix. Urinary excretion is virtually complete in 24 h, whereas fecal excretion starts to plateau 192 h after dosing. |
| Volume of distribution | The mean (SD) volume of distribution of ganirelix in healthy females following subcutaneous administration of a single 250-mcg dose is 43.7 (11.4) L. |
| Clearance | Clearance following subcutaneous administration of a single 250-mcg dose is approximately 2.4 L/h. |
Formulation & handling
- Ganirelix is a polypeptide small molecule administered via subcutaneous or parenteral injection, not suitable for oral use.
- Its low water solubility and peptide nature require careful formulation to maintain stability in injectable solutions.
- Handling should minimize exposure to conditions that could degrade peptide structure, such as extreme pH or temperature variations.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's key patents expired in the United States in 2015 and 2018, with established market presence in the US, EU, and Canada. This indicates the API is in a mature phase with available generic alternatives in these regions. |
|---|
| Markets | US, EU, Canada |
|---|
Supply Chain
| Supply chain summary | Ganirelix is supplied by multiple originator companies with branded products available across the US, EU, and Canadian markets. The presence of several patents filed between 2015 and 2018 indicates protection of formulations in the United States, but given typical patent life spans, the molecule may be approaching or has recently entered a phase allowing generic competition. This suggests a supply landscape with both established branded options and emerging generic manufacturers. |
|---|
Safety
| Toxicity | LD<sub>50</sub> in rats was 40 mg/kg following subcutaneous administration. There have been no reports of overdosage with ganirelix in humans. Clinical studies with subcutaneous administration of ganirelix at single doses up to 12 mg did not show systemic adverse reactions. In acute toxicity studies in rats and monkeys, non-specific toxic symptoms such as hypotension and bradycardia were only observed after intravenous administration of ganirelix over 1 and 3 mg/kg, respectively. As there is no known antidote for ganirelix, the drug should be discontinued in case of an overdose. |
|---|
- Acute toxicity studies reported an LD₅₀ of 40 mg/kg in rats following subcutaneous administration
- Non-specific toxic effects such as hypotension and bradycardia were observed at intravenous doses exceeding 1 mg/kg in rats and 3 mg/kg in monkeys
- No specific antidote is available
Ganirelix 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.
Ganirelix (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.
Ganirelix API manufacturers & distributors
Compare qualified Ganirelix API suppliers worldwide. We currently have 6 companies offering Ganirelix API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| BCN Peptides | Producer | Spain | Spain | CoA, USDMF | 13 products |
| Hybio Pharmaceutical | Producer | China | China | CoA, JDMF, USDMF | 8 products |
| Hybio Pharmaceutical Co L... | Producer | China | China | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, MSDS, USDMF | 34 products |
| Sekisui Medical | Producer | Japan | Japan | CoA, JDMF | 11 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, MSDS, USDMF | 762 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
When sending a request, specify which Ganirelix API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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