Ganirelix (acetate)
(Synonyms: 加尼瑞克,Ganirest) 目录号 : GC43736
A GNRHR antagonist
Cas No.:129311-55-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ganirelix is a gonadotropin-releasing hormone receptor (GNRHR) antagonist (IC50 = 3.6 nM; pA2 = 9.3). It induces a concentration-dependent increase in histamine release from rat peritoneal mast cells in vitro (EC50 = 11 μg/ml). In vivo, ganirelix (2 mg/kg, s.c.) decreases plasma testosterone in intact male rats for the first 7 days post-administration. Ganirelix (125 μg per day for 30 days) decreases the surface area of endometriotic lesions and serum progesterone levels in female baboons. Formulations containing ganirelix have been used to prevent premature ovulation in women undergoing in vitro fertilization.
| Cas No. | 129311-55-3 | SDF | |
| 别名 | 加尼瑞克,Ganirest | ||
| 分子式 | C80H113ClN18O13•2C2H4O2 | 分子量 | 1690.4 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 0.25 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.5916 mL | 2.9579 mL | 5.9158 mL |
| 5 mM | 0.1183 mL | 0.5916 mL | 1.1832 mL |
| 10 mM | 0.0592 mL | 0.2958 mL | 0.5916 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Medroxyprogesterone acetate versus Ganirelix in oocyte donation: a randomized controlled trial
Hum Reprod 2019 May 1;34(5):872-880.PMID:30927417DOI:10.1093/humrep/dez034.
Study question: Is oral medroxiprogesterone acetate (MPA) non-inferior compared to Ganirelix with respect to the number of mature oocytes (MII) retrieved at ovum pick-up (OPU) in oocyte donation cycles? Summary answer: MPA is comparable to Ganirelix in terms of number of MII retrieved at OPU in oocyte donation cycles. What is known already: Oral treatment with MPA inhibits the pituitary LH surge during ovarian stimulation in infertile patients. Because of its negative effect on the endometrium, MPA suppression is combined with freeze-all. Published reports indicate that both the number of MII retrieved and pregnancy rates from these oocytes are comparable to short protocol of GnRH agonists during IVF cycles with freeze-all. MPA might allow for more comfortable and cost-effective ovarian stimulation. Study design, size, duration: Randomized clinical trial, open-label, single center, to assess the non-inferiority of MPA (10 mg/day) versus Ganirelix (0.25 mg/day) from Day 7, in ovarian stimulation cycles triggered with triptoreline acetate. Trigger criterion was ≥3 follicles of diameter >18 mm. Participants/materials, setting, methods: Overall, 252 oocyte donors were selected (eligible), 216 were randomized and 173 reached OPU: 86 under MPA and 87 under Ganirelix. The main outcome was the number of MII retrieved at OPU. Secondary outcomes were embryological laboratory outcomes and reproductive outcomes in recipients. The study was powered to test that the lower limit of the 95% confidence interval of the difference in retrieved MII between groups will be above the non-inferiority limit of -3. Differences were tested using a two-sided Student's t-test or a Pearson's Chi2 test, as appropriate. Main results and the role of chance: All participants were in their first cycle of oocyte donation. On average, donors were 24 (SD 4.5) years old and with a BMI of 23 (SD 2.9) kg/m2. Duration of stimulation was similar in both groups (11.2 days), as well as the total gonadotropin dose up to trigger (2162 IU in MPA and 2163 IU in Ganirelix). The number of MII retrieved was no different: 15.1 (SD 8.3) with MPA and 14.6 (SD 7.0), 95% CI of the difference -2.78, -1.83 excluding the pre-defined non-inferiority limit (-3). Recipients and embryo transfer (ET) characteristics were also similar between groups. The average age of recipients was 42 (SD 4.8) years and the BMI was 24 (SD 4.4) kg/m2. The mean number of MII assigned to each recipients was 6.7 (SD 1.2) in MPA and 6.6 (SD 1.2) in Ganirelix (P = 0.58). MII were fertilized with partner sperm in 84% cycles overall and fertilization rate was 76% in MPA versus 74% in Ganirelix (P = 0.34). Overall, there was 54% of double ET and 46% of single ET, with 40% of ETs were performed in D5. In spite of similar recipients and cycle characteristics, reproductive outcomes were unexpectedly lower with MPA. Biochemical pregnancy rate was 44 versus 57% (P = 0.023); clinical pregnancy rate 31 versus 46% (P = 0.006); ongoing pregnancy rate 27 versus 40%, (P = 0.015) and live birth rate 22 versus 31%, (P = 0.10). Limitations, reasons for caution: Although oocyte recipient and ET characteristics are similar among groups, this RCT has been designed under a hypothesis of non-inferiority in the number of MII obtained and recipients were not randomized; therefore, the reproductive outcomes in recipients should be evaluated with extreme caution. Wider implication of the findings: Ovarian stimulation using MPA for prevention of LH surge yields comparable number of MII oocytes compared to Ganirelix in oocyte donation cycles. The unexpected finding in reproductive outcomes should be further investigated. Study funding/competing interest(s): None to report. Trial registration number: EudraCT number: 2015-004328-73; ClinicalTrials.gov Identifier: NCT02796105. Trial registration date: 29 September 2015 (EudraCT); 9 June 2016 (ClinicalTrials.gov). Date of first patient’s enrollment: The date of enrollment of the first participant was 07 July 2016, and the last participant last visit in the study was on 10 July 2017.
Efficacy and safety of Ganirelix acetate versus leuprolide acetate in women undergoing controlled ovarian hyperstimulation
Fertil Steril 2001 Jan;75(1):38-45.PMID:11163814DOI:10.1016/s0015-0282(00)01638-1.
Objective: To assess the efficacy, safety, and local tolerance of Ganirelix acetate for the inhibition of premature luteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation (COH). Design: Phase III, multicenter, open-label randomized trial. Setting: In vitro fertilization (IVF) centers in North America. Patient(s): Healthy female partners (n = 313) in subfertile couples for whom COH and IVF or intracytoplasmic sperm injection were indicated. Intervention(s): Patients were randomized to receive one COH cycle with Ganirelix or the reference treatment, a long protocol of leuprolide acetate in conjunction with follitropin-beta for injection. Outcome measure(s): Number of oocytes retrieved, pregnancy rates, endocrine variables, and safety variables. Result(s): The mean number of oocytes retrieved per attempt was 11.6 in the Ganirelix group and 14.1 in the leuprolide group. Fertilization rates were 62.4% and 61.9% in the Ganirelix and leuprolide groups, respectively, and implantation rates were 21.1% and 26.1%. Clinical and ongoing pregnancy rates per attempt were 35.4% and 30.8% in the Ganirelix group and 38.4% and 36.4% in the leuprolide acetate group. Fewer moderate and severe injection site reactions were reported with Ganirelix (11.9% and 0.6%) than with leuprolide (24.4% and 1.1%). Conclusion(s): Ganirelix is effective, safe, and well tolerated. Compared with leuprolide acetate, Ganirelix therapy has a shorter duration and fewer injections but produces a similar pregnancy rate.
Ganirelix
Drugs 2000 Jan;59(1):107-11; discussion 112-3.PMID:10718102DOI:10.2165/00003495-200059010-00007.
Ganirelix is a synthetic third generation gonadotropin-releasing hormone (GnRH) antagonist that is administered via the subcutaneous route. The drug competitively blocks GnRH receptors in the anterior pituitary gland, preventing endogenous GnRH from inducing luteinising hormone (LH) and follicle stimulating hormone release. Ganirelix effectively inhibited LH surges during controlled ovarian stimulation in a large, multicentre clinical trial in women undergoing in vitro fertilisation. A vital pregnancy rate per embryo transfer of 40.3% was achieved at weeks 5 to 6 after treatment with the 0.25 mg/day dosage. Subcutaneous Ganirelix has been generally well tolerated in clinical trials. The most common adverse events were local injection site events, asthenia, nausea, malaise, headache and fatigue.
A Prospective Randomised Comparative Clinical Trial Study of Luteal PhaseLetrozole versus Ganirelix acetate Administration to Prevent Severity of Early Onset OHSS in ARTs
Int J Fertil Steril 2021 Oct;15(4):263-268.PMID:34913294DOI:10.22074/IJFS.2021.139562.1042.
Background: Ovarian hyperstimulation syndrome (OHSS) is the most notable complication in ovulation induction for assisted reproductive techniques (ARTs) like in vitro fertilization (IVF) and intracytoplasmic sperm injection (ICSI). Hence, we decided to evaluate the effect of the aromatase inhibitor, letrozole, versus gonadotrophin-releasing hormone (GnRH)-antagonist (Ganirelix acetate) on prevention of severity of OHSS and reduction in serum estradiol (E2) levels when administered during the luteal phase after oocyte retrieval in IVF/ICSI cycles. Materials and methods: In this prospective single-centred, randomized, parallel-arm study, 122 patients were randomized to receive oral letrozole (n=61, 2.5 mg twice daily) or Ganirelix acetate (n=61, 0.25 mg subcutaneously daily) from the day of egg retrieval for the next 7 days. Incidence and severity of early OHSS were the primary endpoints assessed by the signs, symptoms, and laboratory findings of OHSS (e.g., serum E2 levels). The secondary endpoints were patient satisfaction and the additional cost of therapy to prevent the severity of OHSS. Results: Letrozole group had lower incidence of OHSS (13.1%) compared to 19.6% in Ganirelix acetate group (P=0.32). Serum E2 levels on post-pick up days 5 and 7 were significantly lower in the letrozole group when compared to the Ganirelix acetate group (P=0.001). The majority of the patients in both groups had no major complications. No significant difference was found between the study groups with respect to the incidence of OHSS (P=0.33). The additional cost per IVF cycle for prevention of severity of early-onset OHSS in the letrozole group was 5.32 USD compared to 267.26 USD in the Ganirelix acetate group, which was almost fifty times costlier. Conclusion: Letrozole and Ganirelix acetate have the same efficiency for the overall prevention of OHSS, whereas letrozole was more effective in preventing moderate OHSS. Letrozole had better patient satisfaction and is cheaper compared to GnRH antagonists (Registration number: CTRI/2020/10/028674).
Efficacy and safety of newly developed Ganirelix acetate in infertile women for assisted reproductive technology: a prospective, randomised, controlled study
J Obstet Gynaecol 2022 Aug;42(6):2197-2202.PMID:35254199DOI:10.1080/01443615.2022.2036955.
This study aimed to investigate the efficacy of Ganilever pre-filled syringe (PFS), a newly developed Ganirelix acetate, for the inhibition of premature luteinising hormone (LH) surge in in vitro fertilisation (IVF). A prospective randomised controlled study was conducted (NCT03051087). A total of 236 women (Ganilever group: 114, Orgalutran group: 122) were finally analysed. The patients with LH of >10 mIU/mL on the day of human chorionic gonadotropin (hCG) injection were 0 (0.0%) and 3 (2.5%) in the Ganilever and Orgalutran groups, respectively (p= .25). The number of retrieved oocytes from two groups did not show any significant difference (12.0 ± 6.4 vs. 11.8 ± 6.3, p= .73). Furthermore, the two groups did not show significant differences in the number of good-quality oocytes and embryo, and the rate of fertilisation. Similar safety profiles were also observed. In conclusion, Ganilever PFS showed comparable IVF outcomes and safety profile in IVF, as compared to the Orgalutran. Impact StatementWhat is already known on this subject? Premature LH surge during controlled ovarian stimulation results in the induction of luteinisation of the immature follicles. Thus, gonadotrophin-releasing hormone (GnRH) antagonist protocol was suggested as an option for suppression of premature LH surge. Currently, one of GnRH antagonists being widely used is Ganirelix acetate (Orgalutran®; Organon, Oss, The Netherlands). Ganilever pre-filled syringe (PFS) is a newly developed GnRH antagonist containing Ganirelix acetate as an active ingredient.What do the results of this study add? Our study demonstrated that Ganilever PFS showed comparable IVF outcomes and patient safety profile in infertile women undergoing in IVF-ET, as compared to the Orgalutran.What are the implications of these findings for clinical practice and/or further research? The results of our study will provide another available GnRH antagonist to be used in patients with IVF.