Goserelin acetate
(Synonyms: 醋酸戈舍瑞林; ICI-118630 acetate) 目录号 : GC36180
A synthetic GNRH agonist
Cas No.:145781-92-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Goserelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 1.6 nM, in CHO cells expressing the human receptor).1 It binds to mouse pituitary αT3-1 cells and human placenta (Kds = 2 and 580 nM, respectively) and increases intracellular calcium in αT3-1 cells.2 Goserelin induces testosterone production in vitro within 4 h in rat Leydig cells (ED50 = 83 nM) but decreases testosterone plasma level in vivo in rats over a period of 2 to 24 weeks.3,4 It inhibits tumor growth in a DU145 human prostate carcinoma mouse xenograft model when administered at a dose of 100 μg per day.5 Formulations containing goserelin have been used in the treatment of hormone-dependent breast and prostate cancers, as well as endometriosis and uterine fibroids.
1.Nederpelt, I., Georgi, V., Schiele, F., et al.Characterization of 12 GnRH peptide agonists - a kinetic perspectiveBr. J. Pharmacol.173(1)128-141(2016) 2.Chatzaki, E., Bax, C.M., Eidne, K.A., et al.The expression of gonadotropin-releasing hormone and its receptor in endometrial cancer, and its relevance as an autocrine growth factorCancer Res.56(9)2059-2065(1996) 3.Sullivan, M.H., and Cooke, B.A.The role of calcium in luteinizing hormone-releasing hormone agonist (ICI 118630)-stimulated steroidogenesis in rat Leydig cellsBiochem. J.218(2)621-624(1984) 4.Ward, J.A., Furr, B.J., Valcaccia, B., et al.Prolonged suppression of rat testis function by a depot formulation of Zoladex, a GnRH agonistJ. Androl.10(6)478-486(1989) 5.Dondi, D., Moretti, R.M., Montagnani, M.M., et al.Growth-inhibitory effects of luteinizing hormone-releasing hormone (LHRH) agonists on xenografts of the DU 145 human androgen-independent prostate cancer cell line in nude miceInt. J. Cancer76(4)506-511(1998)
| Cas No. | 145781-92-6 | SDF | |
| 别名 | 醋酸戈舍瑞林; ICI-118630 acetate | ||
| Canonical SMILES | O=C(N[C@H](C(N[C@@H](CC1=CC=C(O)C=C1)C(N[C@H](COC(C)(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N2CCC[C@H]2C(NNC(N)=O)=O)=O)=O)=O)=O)=O)CO)[C@@H](NC([C@H](CC3=CN=CN3)NC([C@@H](N4)CCC4=O)=O)=O)CC5=CNC6=C5C=CC=C6.CC(O)=O | ||
| 分子式 | C61H88N18O16 | 分子量 | 1329.46 |
| 溶解度 | DMSO: ≥ 28 mg/mL (21.06 mM) | 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 | 0.7522 mL | 3.7609 mL | 7.5219 mL |
| 5 mM | 0.1504 mL | 0.7522 mL | 1.5044 mL |
| 10 mM | 0.0752 mL | 0.3761 mL | 0.7522 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。
Goserelin acetate implant: a depot luteinizing hormone-releasing hormone analog for advanced prostate cancer
DICP 1991 Jul-Aug;25(7-8):796-804.PMID:1835221DOI:10.1177/106002809102500716.
Goserelin acetate implant is a newly approved depot formulation of a luteinizing hormone-releasing hormone (LHRH) agonist indicated for palliation of advanced prostate cancer. LHRH superagonists suppress gonadotropin release from the pituitary gland by causing down-regulation of receptors. The sustained-release dosage form contains Goserelin acetate dispersed in a biodegradable copolymer matrix and is designed to release active drug over 28 days. Pharmacokinetic studies have demonstrated that, despite nonzero order release of goserelin from the matrix, Goserelin acetate implant maintains serum concentrations of testosterone in the range normally found in castrated men (less than 2 nmol/L) throughout the recommended 28-day dosing interval. Response rates similar to those for orchiectomy and estrogen administration have been demonstrated. Combination therapy with either diethylstilbestrol or flutamide has produced favorable results, although the major advantage appears to be a reduction in the tumor flare seen during the first week of LHRH agonist therapy rather than an increase in response rate or survival. Adverse effects are similar to other LHRH agonists and include tumor flare during the first week of therapy, decreased libido, decreased erectile potency, hot flashes, and gynecomastia. In combination with flutamide, additional adverse effects include diarrhea, nausea, vomiting, and elevated hepatic aminotransferases, all of which can be attributed to flutamide administration. Local reactions are minimal; however, some patients require a local anesthetic before Goserelin acetate implant injection. The recommended dose is 3.6 mg administered subcutaneously into the upper abdominal wall every 28 days. The average wholesale cost is approximately +320 per month. Formulary addition is recommended.
Goserelin acetate in combination with radiotherapy for prostate cancer
Expert Opin Pharmacother 2007 Feb;8(2):257-64.PMID:17257094DOI:10.1517/14656566.8.2.257.
Improvements in longer-term survival rates have been demonstrated for locally advanced prostate cancer patients treated with adjuvant androgen deprivation therapy (ADT), and in subsets of men with clinically localized disease treated with ADT combined with external-beam radiotherapy (RT). In these studies, ADT was administered in the form of surgery (orchiectomy) or with a class of drugs called luteinizing hormone-releasing hormone agonists. Goserelin acetate is a member of this class, and 10 of 11 major Phase III trials demonstrating better outcomes with ADT and RT used Goserelin acetate. The reduction in deaths from prostate cancer noted in the mid-1990s may largely be due to the early use of these agents in men with intermediate-to-high-risk disease.
Goserelin acetate Loaded Poloxamer Hydrogel in PLGA Microspheres: Core-Shell Di-Depot Intramuscular Sustained Release Delivery System
Mol Pharm 2019 Aug 5;16(8):3502-3513.PMID:31251642DOI:10.1021/acs.molpharmaceut.9b00344.
This study aimed to prepare and optimize Goserelin acetate (GOS) loaded hydrogel poly(d,l-lactic acid-co-glycolic acid) (PLGA) microsphere that is suitable for long-acting clinical treatment, investigate its structure, and regulate the initial release manner. Here, the PLGA microsphere containing Poloxamer hydrogel loaded with ∼15% (w/w) GOS was prepared by double-emulsion-solvent evaporation method and evaluated in terms of microscopic structure, physicochemical properties, and release manner in vitro and in vivo. Raman volume imaging and scanning electron microscopy studies revealed a core-shell Di-Depot structure of the microsphere, in which multi-GOS-loaded hydrogel depots were distributed in the core region. Under the interaction of hydrogel and PLGA depots, high encapsulation efficiency (94.16%) and low burst release (less than 2%) were achieved, along with the accompanying prolonged administration interval (49 days); an enhanced relative bioavailability 9.36-fold higher than that of Zoladex implant was also observed. Also, by addition of 1-5% acetic acid, the lag time was shortened to 6 days. The strategy for regulating the initial release provides new insights for manipulating the release behavior of the PLGA microspheres. The desirable property of the Poloxamer hydrogel PLGA microsphere indicated its promising application in controlled release drug delivery system.
Zoladex (Goserelin acetate) and the anemic patient: results of a multicenter fibroid study
Fertil Steril 1996 Aug;66(2):223-9.PMID:8690106doi
Objective: To compare the effects of Goserelin acetate treatment with or without iron with iron alone. Design: Multinational, multicenter, prospective, randomized, double-blind study. Patients: Premenopausal women with menorrhagia or metrorrhagia and anemia associated with uterine leiomyomata awaiting hysterectomy. Intervention: Patients were randomized to one of three 12-week treatment groups namely Goserelin acetate 3.6 mg once monthly plus placebo iron; 3.6 mg Goserelin acetate once monthly plus 600 mg/d iron; or sham injection once monthly plus 600 mg/d iron. Main outcome measure: Preoperative hemoglobin concentration; preoperative uterine and fibroid volumes and operative blood loss. Results: Considering the entry and preoperative hemoglobin concentrations, there was a difference in least square means of just over 1 g/dL between the Goserelin acetate plus iron and iron only groups and 2.6 g/dL between the Goserelin acetate plus iron and Goserelin acetate only group. These differences were both statistically significant. Uterine and fibroid volumes were decreased in the goserelin acetate-treated patients by between 37% and 40% and 44% and 47%, respectively, compared with 7% decreases for both in the iron only group. The differences in absolute changes were statistically significant for both the goserelin acetate-treated groups versus the iron-treated group. The least square geometric mean operative blood loss was greatest in the iron only group. Conclusion: In the patient with uterine leiomyomata and anemia, Goserelin acetate in combination with iron therapy has shown significant advantages over the iron alone in restoring hematologic normality, decreasing uterine and fibroid volumes, and reducing operative blood loss.
Goserelin acetate to avoid hysterectomy in pre-menopausal women with fibroids requiring surgery
Eur J Obstet Gynecol Reprod Biol 1999 Nov;87(1):31-3.PMID:10579613DOI:10.1016/s0301-2115(99)00089-5.
Objective: To obtain information on the efficacy of repeated short cycles of GNRH agonist treatment in order to avoid hysterectomy in near-menopausal women with symptomatic fibroids. Study design: 72 pre-menopausal women (mean age 50 years) with one or more uterine fibroids >10 cm in diameter, symptomatic menorrhagia lasting three months or more and haemoglobin=9 g/dl entered the study. The patients were randomized with ratio of approximately 1:4 to: (a) immediate surgery; or (b) treatment with Goserelin acetate. Patients randomized to Goserelin acetate received a first cycle of 3.6 mg depot once every 28 days for four months. They were followed-up for three years. If menorrhagia was observed during the follow-up the woman was given Goserelin acetate 3.6 mg depot for another three months. In case of further menorrhagia, a third cycle of Goserelin acetate 3.6 mg depot for three months was given. After the third cycle of therapy if there was still menorrhagia, the patient underwent hysterectomy plus bilateral oophorectomy. Results: A total of 13 women were assigned to the immediate surgery group and 59 to goserelin. Three years after trial entry a total of 23 women allocated to Goserelin acetate treatment had undergone hysterectomy. Conclusion: This study suggests that GNRH agonists are efficacious for avoiding hysterectomy in women near menopause with uterine fibroids.