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Ganirelix 250 mcg, molecular formula, C80H113ClN18O13, CAS 129311-55-3, It is a synthetic peptide with high antagonistic activity against naturally occurring normegon-releasing hormone (LHRH). By replacing the amino acids at positions 1, 2, 3, 6, 8, and 10 of natural LHRH, the following peptide molecular formula is formed.
This substance is a "stabilizer" for antagonist regimens and is often used in anti caking regimens in vitro. Women under the anti ovulation medication regimen start using ovulation inducing drugs during their menstrual period, and to avoid premature ovulation before the completion of ovulation induction, they will be added during this period to prevent premature luteinizing homone (LH) peaks and thus prevent ovulation.
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Ganirelix COA
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| Certificate of Analysis | ||
| Compound name | Ganirelix | |
| Grade | Pharmaceutical grade | |
| CAS No. | 129311-55-3 | |
| Quantity | 60g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090056 | |
| 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% | 0.32% |
| Loss on drying | ≤1.0% | 0.14% |
| 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% | 99.90% |
| Single impurity | <0.8% | 0.27% |
| Total microbial count | ≤750cfu/g | 319 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 220ppm |
| Storage | Store in a sealed, dark, and dry place below2-8°C | |
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Ganirelix 250 mcg is a synthetic peptide that belongs to the normegon-releasing homone (LHRH) antagonist class and has high antagonistic activity against naturally occurring LHRH. Its mechanism of action mainly revolves around the regulation of the hypothalamic pituitary gonadal axis, as follows:
Competitive blockade of LHRH receptor
The core mechanism of action is its ability to competitively block LHRH receptors on pituitary normegon cells. Under normal physiological conditions, LHRH secreted by the hypothalamus is released in a pulsed manner, which can stimulate the synthesis and secretion of follicle stimulating homone (FSH) and luteinizing homone (ICSH) in the anterior pituitary gland. FSH and ICSH play a crucial role in the female reproductive cycle, with FSH primarily promoting the development and maturation of follicles, while ICSH plays an important role in ovulation.
By binding to the LHRH receptor, the stimulating effect of endogenous LHRH on the pituitary gland is prevented. Due to its high affinity for LHRH receptors, it can effectively occupy receptor sites, thereby reducing or blocking the binding of LHRH to receptors. This competitive blocking effect inhibits the synthesis and secretion of FSH and ICSH in the anterior pituitary gland, thereby regulating gonadal function.
Inhibit the secretion of FSH and ICSH
Inhibition of FSH secretion: It can inhibit the synthesis and secretion of FSH in the anterior pituitary gland. In assisted reproductive technology, controlled ovarian stimulation (COS) protocols typically require the use of exogenous FSH to stimulate the development of multiple follicles. However, excessive FSH levels may lead to adverse reactions such as ovarian hyperstimulation syndrome (OHSS). By inhibiting the secretion of FSH, it helps to control the development speed of follicles and reduce the risk of OHSS. At the same time, it can ensure that follicles develop synchronously in a suitable hormonal environment, improving the chances of obtaining high-quality eggs.
Inhibition of ICSH secretion: The inhibition of ICSH secretion in the pituitary gland is stronger than that of FSH. The appearance of ICSH peak during the female reproductive cycle is a key signal for ovulation. However, in assisted reproductive technology, premature ICSH peaks may lead to premature luteinization and ovulation of follicles, thereby affecting the quantity and quality of eggs obtained. By inhibiting ICSH secretion, premature ICSH peak can be effectively prevented, ensuring that follicles mature and ovulate at the appropriate time.
Rapid and reversible inhibition of normegon secretion
The effect produced is rapid and reversible. After injection of acetic acid ganciclovir, it can rapidly bind to pituitary LHRH receptors and inhibit the secretion of FSH and ICSH. This inhibitory effect can quickly recover after discontinuation of the medication. Research has shown that within 48 hours after discontinuation, the levels of ICSH and FSH in the pituitary gland can be fully restored. This rapid and reversible action characteristic gives it a unique advantage in assisted reproductive technology, allowing for flexible adjustment of homone levels according to treatment needs.
Simulating homone regulation under natural physiological conditions
While regulating homone levels, it can also simulate the homone regulation mode under natural physiological conditions. During a normal menstrual cycle, the pulsatile release of LHRH causes periodic changes in the secretion of FSH and ICSH. By competitively blocking the LHRH receptor, although the secretion of FSH and LH was inhibited, its mode of action did not completely break this periodic change.
In assisted reproductive technology, doctors can adjust the dosage and timing of medication according to the specific situation of the patient to simulate the homone regulation mode under natural physiological conditions, thereby optimizing the development of follicles and ovulation process.
Regulation of gonadal function
By regulating the function of the hypothalamic pituitary gonadal axis, the levels of gonadal homones are restored to normal range. In assisted reproductive technology, a controlled ovarian stimulation regimen may lead to abnormally elevated levels of normegons, increasing the risk of adverse reactions such as OHSS. Acetic acid ganrelic helps control gonadal homone levels and reduce the occurrence of adverse reactions by inhibiting the secretion of FSH and ICSH. At the same time, ganirelix 250 mcg can also improve the responsiveness of the ovaries to normegons and increase the success rate of assisted reproductive therapy.
Source of information:
39 Health Network: Provides information on the pharmacological effects, clinical applications, and interactions with other drugs of acetic acid garenicol.
Spring Rain Doctor: This article introduces the application of acetic acid ganrelic in assisted reproductive technology, including its role in preventing premature ICSH peak and optimizing follicular development.
National Health Network: Detailed description of the mechanism of action of acetic acid ganrelic, including competitive blockade of LHRH receptors, inhibition of FSH and ICSH secretion, and other aspects.
Baidu Baike: provides a detailed introduction to acetic acid ganrelic, including its chemical structure, pharmacological effects, clinical applications, and other information.
Pharmacological action
The pulsatile release of LHRH can stimulate the synthesis and secretion of ICSH and FSH. The ICSH pulse frequency during the mid to late follicular phase is approximately once per hour. These pulses are reflected in the instantaneous increase of serum ICSH. In the middle of menstruation, the massive release of LHRH causes a surge in ICSH. The surge of ICSH during the mid menstrual period can cause several physiological reactions, including ovulation, restoration of oocyte meiosis, and corpus luteum formation. Luteal formation causes an increase in serum progesterone levels and a decrease in estradiol levels.
Ganirelix 250 mcg is a LHRH antagonist that competitively blocks the LHRH receptor on pituitary gonadotropic cells and subsequent transduction pathways. It produces a rapid and reversible inhibitory effect on the secretion of normegons. The inhibitory effect of acetic acid on ICSH secretion in the pituitary gland is stronger than its inhibitory effect on FSH. Acetic acid induced ganciclovir cannot induce the initial release of endogenous normegons, which is consistent with its antagonistic effect. Within 48 hours after discontinuing the use of acetic acid and ganciclovir, the levels of ICSH and FSH in the pituitary gland can be fully restored.
Toxicological study
Genetic toxicity: The results of the acetic acid ganirek Ames test and CHO cell chromosome aberration test were both negative.
Reproductive toxicity: Pregnant rats and rabbits were treated with acetic acid ganrelic starting from day 7 at doses of 10 and 30ug/kg/day (approximately 0.4-3.2 times the human dose based on body surface area), resulting in an increased incidence of nest absorption and no fetal abnormalities observed. During pregnancy and lactation, female rats were treated with acetic acid ganciclovir, and no treatment-related changes in fertility, physical fitness, or behavior were observed in the offspring.
The anti gonadotropic effect of acetic acid injection can cause changes in homone levels, leading to embryo absorption and fetal loss. Pregnant women are prohibited from using acetic acid injection.
pharmacokinetics
After a single subcutaneous administration of 0.25mg ganirix to female volunteers abroad, the blood drug concentration reached its peak concentration (Cmax) within 1-2 hours (tmax), which was approximately 15ng/ml. The elimination half-life (t ݤ) is about 13 hours, and the clearance rate is about 2.4l/h. Excreted through feces (about 75%) and urine (about 22%). The bioavailability of this product after subcutaneous administration is approximately 91%.
In female volunteers abroad, the pharmacokinetic parameters of this product after multiple subcutaneous administrations (once daily injection) were similar to those after a single subcutaneous administration. Within 2-3 days after multiple doses of 0.25mg/day, the blood drug concentration reaches a steady state level of approximately 0.6ng/ml.
Pharmacokinetic analysis of foreign trials shows an inverse relationship between body weight and blood drug concentration of this product.
The main circulating component in plasma is Ganerik. Ganerik is also the main compound found in urine, while feces only contain metabolites. The metabolite is a small peptide fragment formed by the enzymatic hydrolysis of ganirek at its restriction site. The metabolic models of this product in humans and animals are similar.
About 1 hour after a single subcutaneous administration of 0.25mg of Ganirek to healthy Chinese female volunteers, the average blood concentration was 7.88ng/mL. The estimated average elimination half-life time, body weight standardized clearance rate, and body weight standardized distribution volume are 12.1 hours, 80 mL/h/kg, and 1.4 L/kg, respectively.
FAQ
How many days do you take ganirelix?
It is administered as a subcutaneous injection, typically into the abdomen or thigh. It is usually given once daily during the middle to late stage of the ovarian stimulation phase of an IVF cycle. This will be around day 5 or 6 of stimulation and continuing until the day of the trigger injection.
What is the purpose of ganirelix in IVF?
GANIRELIX (ga ni REL iks) prevents premature ovulation in people trying to get pregnant. It works by blocking the release of a hormone that triggers ovulation. This prevents eggs from being released too early, before they are mature.
Does ganirelix stop ovulation?
It is a type of medicine called a normegon-releasing hormone (LHRH) antagonist. It blocks a specific hormone, called luteinizing hormone (LH), from being produced. ICSH tells the body to ovulate, so when gairelix blocks LH, it prevents ovulation.
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