Ganirelix
ganirelix
CAS: 123246-29-7
Molecular Formula: C80H113ClN18O13
Ganirelix - Names and Identifiers
Ganirelix - Physico-chemical Properties
| Molecular Formula | C80H113ClN18O13 |
| Molar Mass | 1570.34 |
Ganirelix - Reference Information
| Overview | Ganiric is a synthetic decapeptide compound, its acetate, Ganiric acetate (Ganirelix Acetate) is a gonadotropin-releasing hormone (GnRH) receptor antagonist. The amino acid sequence is: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-Tyr-D-Homo Arg(9,10-Et2)-Leu-L-Homo Arg(9,10-Et2)-Pro- D-Ala-NH2. Clinically, it is mainly used in women receiving assisted reproductive technology-controlled ovarian stimulation programs to prevent premature luteinizing hormone peaks and treat fertility disorders caused by this reason. The drug has the characteristics of few adverse reactions, high pregnancy rate, and short treatment cycle. It has obvious advantages compared with similar drugs in clinical practice. It has been listed in many countries and approved to be listed in China in June 2013. |
| brief introduction | active ingredient is: ganiric acetate active ingredient ganiric (INN) is a synthetic decapeptide with high antagonistic activity to naturally generated gonadotropin releasing hormone (GnRH). It is formed by replacing amino acids at sites 1, 2, 3, 6, 8, and 10 of the natural GnRH. Chemical name: N-acetyl -3-(2-naphthalene)-D-alanyl -4-chloro-D-phenylalanyl -3-(3-pyridine)-D-alanyl-L-serinyl-L-tyrosyl-N6-[bis (ethylamine) methylene]-D-lysyl-L-leucyl-N6-[bis (ethylamine) methylene]-L-lysyl-L-prolyl-D-alanyamide acetate Molecular formula: c80H113N18O13Cl. 2CH3COOH Molecular weight: 1690.42 Chemical structural formula: Figure 1 shows the molecular structural formula of Ganirick acetate. the other components of this product are: glacial acetic acid, mannitol, water for injection, sodium hydroxide and acetic acid to adjust the pH value. |
| Pharmacological effects | The pulsed release of gonadotropin-releasing hormone (GnRH) can stimulate the synthesis and secretion of LH and FSH. The frequency of LH pulses in the middle and late follicular phase is about 1 time per hour. These pulses are reflected in the transient rise of serum LH. In the middle of menstruation, the massive release of GnRH causes LH to surge. The LH surge in mid-menstrual period can cause several physiological reactions, including ovulation, oocyte meiosis recovery and corpus luteum formation. Luteal formation causes serum progesterone levels to rise and estradiol levels to fall. GnRH acetate is a GnRH antagonist, which can competitively block GnRH receptors on pituitary gonadotropins and subsequent transduction pathways. It produces a rapid, reversible inhibition of gonadotropin secretion. The inhibitory effect of ganiric acetate on pituitary LH secretion is stronger than that of FSH. Ganiric acetate did not cause the first release of endogenous gonadotropins, which was consistent with antagonistic effects. The pituitary LH and FSH levels were completely restored within 48 hours after the withdrawal of ganilic acetate. |
| toxicological study | genotoxicity: the results of ganiric acid Ames test and CHO cell chromosome aberration test were negative. Reproductive toxicity: pregnant rats and rabbits were given ganilic acetate at a dose of 10,30ug/kg/day (calculated by body surface area, about 0.4-3.2 times the human dose) from the 7th day. It was seen that the incidence of fossa absorption increased and no fetal abnormality was found. The female rats were given ganilic acetate during pregnancy and lactation, and no drug-related fertility, physical and behavioral changes were seen in the offspring. The anti-gonadotropin effect of Ganilek acetate injection can cause changes in hormone levels, leading to embryo absorption and fetal loss. Pregnant women are prohibited from using Ganirick Acetate Injection. |
| pharmacokinetics | after a single subcutaneous administration of 0.25 mg canilic to foreign female volunteers, the blood concentration reached a peak concentration (Cmax) within 1-2 hours (Tmax), which was about 15ng/ml. The elimination half-life (t½) is about 13 hours and the clearance rate is about 2.4l/h. It is excreted through feces (about 75%) and urine (about 22%). The bioavailability of this product after subcutaneous administration is about 91%. In foreign female volunteers, the pharmacokinetic parameters of this product after multiple subcutaneous administration (once daily injection) are similar to those after a single subcutaneous administration. Within 2-3 days after multiple administration of 0.25 mg/day, the blood concentration reached a steady-state level of about 0.6 ng/ml. The pharmacokinetic analysis of foreign trials shows that the body weight is inversely proportional to the blood drug concentration of this product. The main circulating component in the plasma of the metabolic model is Garniric. Canilic is also the main compound found in urine, and only metabolites are contained in feces. The metabolite is a small peptide fragment formed by enzymatic hydrolysis at its restriction site. The metabolic model of this product in humans and animals is similar. Chinese data The average blood concentration was 7.88 ng/mL about 1 hour after a single subcutaneous administration of 0.25 mg canilic to healthy Chinese female volunteers. The average elimination half-life time, the clearance rate after weight standardization and the distribution volume after weight standardization are estimated to be 12.1 h, 80 mL/h/kg and 1.4 L/kg respectively. |
| References | [1] Yang Guiying, Li Yingchun, Wang Hua, Zhang Xiquan, Feng Jun. Preparation and Process Optimization of Garniric Acetate [J]. Chinese Journal of Pharmaceutical Industry, 2016,47(08):967-972. [2] Garniric Acetate Injection. Medication reference. |
Last Update：2024-04-09 20:48:19
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CAS: 123246-29-7
Tel: 18301782025
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CAS: 123246-29-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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