Promestriene
(Synonyms: 普罗雌烯) 目录号 : GC39502
A synthetic estrogen
Cas No.:39219-28-8
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
Promestriene is a synthetic estrogen and derivative of estradiol .1 Topical application of a gel containing promestriene (1%) reduces vaginal atrophy and decreases in endometrial and myometrial wall thickness in ovariectomized rats.2 Formulations containing promestriene have been used in the treatment of vaginal atrophy.
1.Del Pup, L., Di Francia, R., Cavaliere, C., et al.Promestriene, a specific topic estrogen. Review of 40 years of vaginal atrophy treatment: Is it safe even in cancer patients?Anticancer Drugs24(10)989-998(2013) 2.López-Belmonte, J., Nieto, C., Estevez, J., et al.Comparative uterine effects on ovariectomized rats after repeated treatment with different vaginal estrogen formulationsMaturitas72(4)353-358(2012)
| Cas No. | 39219-28-8 | SDF | |
| 别名 | 普罗雌烯 | ||
| Canonical SMILES | C[C@@]12[C@@H](OC)CC[C@@]1([H])[C@]3([H])CCC4=C(C=CC(OCCC)=C4)[C@@]3([H])CC2 | ||
| 分子式 | C22H32O2 | 分子量 | 328.49 |
| 溶解度 | DMSO: 20 mg/mL (60.88 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 | 3.0442 mL | 15.2212 mL | 30.4423 mL |
| 5 mM | 0.6088 mL | 3.0442 mL | 6.0885 mL |
| 10 mM | 0.3044 mL | 1.5221 mL | 3.0442 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。
Promestriene, a specific topic estrogen. Review of 40 years of vaginal atrophy treatment: is it safe even in cancer patients?
Anticancer Drugs 2013 Nov;24(10):989-98.PMID:24080714DOI:10.1097/CAD.0b013e328365288e.
Urogenital symptoms resulting from estrogen deficiency are common problems that impair quality of life and sexuality. Potentially, one out of three postmenopausal women could benefit from a vaginal estrogen therapy, but the fear of systemic absorption limits its use. Promestriene used vaginally to relieve vaginal atrophy is a locally effective estrogen that has not shown systemic estrogenic effects. Thus, it could be a first-line option for those who necessitate a minimal or ideally no vaginal absorption, particularly in symptomatic cancer patients. There are little data available in the literature, mostly consisting of small, open-label, short duration studies, and few randomized-controlled studies. After a long-term market experience (almost 40 years), in 34 countries, and millions of pieces prescribed, the side effects were very rarely reported in pharmacovigilance data, whereas the effectiveness to relieve atrophy was good. To further improve Promestriene safety, especially in estrogen-sensitive cancer patients, a very low dose is used from the beginning, starting from half or less of the usual dose, and then gradually increased till the minimum effective dose, which could further reduce its already minimal vaginal absorption.
Effects of oxytocin versus Promestriene on genitourinary syndrome: a pilot, prospective, randomized, double-blind study
Clinics (Sao Paulo) 2022 Oct 1;77:100116.PMID:36194923DOI:10.1016/j.clinsp.2022.100116.
Objectives: In this pilot, prospective, randomized, double-blind study, the authors compared the efficacy of oxytocin with Promestriene in improving vaginal atrophy of Genitourinary Syndrome of Menopause (GSM). Methods: A total of 51 postmenopausal women with symptoms of GSM were evaluated. They were randomized into two groups: oxytocin (25 patients) and Promestriene (26 patients) and were evaluated before and after 90 days of treatment; the evaluation was based on the domains of the Female Sexual Function Index (FSFI) (lubrication, satisfaction, and pain during sexual intercourse), clinical visual examination, and vaginal wall thickness. Results: After the use of the medications, both groups showed significant improvement in the three evaluated FSFI domains (p < 0.05) and there was no significant difference between the groups (p > 0.05). On clinical examination, the medications improved all the evaluated parameters but without statistical significance (p > 0.05). The evaluation of the thickness of the vaginal epithelium showed that both treatments led to increase in the vaginal epithelium (p < 0.05); however, the efficacy of Promestriene was higher than that of oxytocin (p < 0.05). Conclusions: Both medications were effective, however, studies with larger samples and longer follow-ups are needed to confirm the clinical applicability.
Efficacy of low-dose vaginal 17β-estradiol versus vaginal Promestriene for vulvovaginal atrophy
Climacteric 2022 Aug;25(4):383-387.PMID:34813408DOI:10.1080/13697137.2021.1998436.
Objective: Vulvovaginal atrophy is frequent, can be bothersome and can impair quality of life in postmenopausal women. The main objective of this prospective, randomized study was to compare the acceptability of low-dose vaginal 17β-estradiol (estradiol) tablets and vaginal Promestriene cream in postmenopausal women with moderate-to-severe symptomatic vulvovaginal atrophy. Methods: Overall, 120 patients were randomized to receive estradiol or Promestriene (n = 60 per group). Acceptability was assessed with a specific questionnaire. Symptom intensity, the Vaginal Health Index (VHI), vaginal pH and the Vaginal Maturation Index were also evaluated. Results: Acceptability was higher for estradiol tablets. Compared to Promestriene cream, hygiene and ease of use were greater after 4 weeks (p = 0.011 and p = 0.001, respectively) and after 12 weeks (p = 0.009 and p = 0.011, respectively). Reduction of symptom intensity was greater with estradiol. Both treatments improved the VHI and decreased vaginal pH. However, superficial cell percentages increased significantly (p < 0.001) with estradiol but not with Promestriene (p = 0.241), with a statistically significant difference between means (p = 0.004). Conclusion: Our results support the use of vaginal low-dose estradiol tablets as compared to vaginal Promestriene cream for the management of moderate-to-severe symptomatic vulvovaginal atrophy in postmenopausal women. Clinicaltrials.gov identifier: NCT04232813.
Urogenital disorders associated with oestrogen deficiency: the role of Promestriene as topical oestrogen therapy
Gynecol Endocrinol 2010 Sep;26(9):644-51.PMID:20374067DOI:10.3109/09513591003767948.
Urogenital disorders associated with oestrogen deficiency affect many women throughout menopausal transition. Symptoms such as vaginal dryness, burning, pruritus, dyspareunia, urinary tract urgency/frequency and incontinence have a significant impact on the individual's quality of life. For younger and healthy menopausal women, systemic oestrogen replacement may improve both vasomotor and urogenital symptoms and will be the treatment of choice. However, a proportion of women on systemic therapy still experience symptoms associated with urogenital atrophy, and patients with oestrogen-dependent cancers may be at risk from systemic oestrogen replacement. For women with mainly urogenital symptoms, local oestrogen is a logical choice and it is often more effective than systemic hormone replacement therapy. Generally speaking, there are no contraindications to local therapy. In terms of which topical preparation to use, a wide range of products are available. Promestriene is an analogue of oestradiol which is minimally absorbed and it has been shown to be effective in reversing atrophic changes caused by oestrogen deficiency in women undergoing natural or surgically induced menopause. Given the absence of systemic activity, Promestriene may be a good choice in women requiring purely locally oestrogen, and those who have survived, or who are at risk of breast cancer and who have severe vulvo-vaginal symptoms.
Fractional CO2 laser versus Promestriene and lubricant in genitourinary syndrome of menopause: a randomized clinical trial
Menopause 2019 Aug;26(8):833-840.PMID:31246661DOI:10.1097/GME.0000000000001333.
Objective: The aim of this study was to compare the effects of fractional CO2 laser therapy, Promestriene, and vaginal lubricants on genitourinary syndrome treatment and sexual function in postmenopausal women. Methods: We performed a randomized clinical trial including 72 postmenopausal women over the age of 50 years. The women were randomized into three intervention groups to receive one of the following treatments: three sessions of intravaginal fractional CO2 laser therapy; 10 mg of intravaginal Promestriene cream 3 times a week; and vaginal lubricant application alone. Vaginal maturation, Vaginal Health Index (VHI) score, and Female Sexual Function Index (FSFI) were evaluated at baseline and after 14 weeks of therapy. Results: We observed an improvement in the vaginal elasticity, volume, moisture, and pH in the CO2 laser and Promestriene groups. The VHI score at 14 weeks was higher in the CO2 laser group (mean score 18.68) than in the Promestriene (15.11) and lubricant (10.44) groups (P < 0.001). Regarding vaginal maturation, basal cells were reduced and superficial cells were increased after treatment. This improvement was more significant in the CO2 laser group (P <0.001). The FSFI score only showed improvement in the desire and lubrication domains in the CO2 laser group. There were no differences in total FSFI score among the three treatment groups. There were no adverse effects associated with any of the treatments. Conclusions: The use of fractional CO2 laser therapy to treat genitourinary syndrome resulted in better short-term effects than those of Promestriene or lubricant with respect to improving the vaginal health in postmenopausal women.