Epirubicin
(Synonyms: 表柔比星; 4'-Epidoxorubicin) 目录号 : GC35997
An anthracycline antitumor antibiotic
Cas No.:56420-45-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Epirubicin is a stereoisomer of the antitumor anthracycline doxorubicin that undergoes β-
1.Arcamone, F.Properties of antitumor anthracyclines and new developments in their application: Cain memorial award lectureCancer Res.45(12 Pt 1)5995-5999(1985) 2.Yao, X., Hosenpud, J., Chitambar, C.R., et al.A phase II study of concurrent docetaxel, epirubicin and cyclophospha-mide as a neoadjuvant chemotherapy regimen in patients with locally advanced breast cancerJ. Cancer3145-151(2012)
| Cas No. | 56420-45-2 | SDF | |
| 别名 | 表柔比星; 4'-Epidoxorubicin | ||
| Canonical SMILES | O=C(C1=C2C(O)=C3[C@@H](O[C@@]4([H])C[C@H](N)[C@@H](O)[C@H](C)O4)C[C@@](C(CO)=O)(O)CC3=C1O)C5=CC=CC(OC)=C5C2=O | ||
| 分子式 | C27H29NO11 | 分子量 | 543.52 |
| 溶解度 | Soluble in DMSO | 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 | 1.8399 mL | 9.1993 mL | 18.3986 mL |
| 5 mM | 0.368 mL | 1.8399 mL | 3.6797 mL |
| 10 mM | 0.184 mL | 0.9199 mL | 1.8399 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。
Epirubicin: is it like doxorubicin in breast cancer? A clinical review
Breast 2012 Apr;21(2):142-9.PMID:22260846DOI:10.1016/j.breast.2011.12.012.
Anthracyclines are among the most effective chemotherapy treatments available for various types of cancer. The anthracyclines commonly used in treatment of breast cancer are either Epirubicin or doxorubicin. Epirubicin is an epimer of doxorubicin with important role in the chemotherapy treatment of both early and metastatic breast cancer. The efficacy of Epirubicin is similar to doxorubicin while Epirubicin has a different toxicity profile particularly in regard to cardiotoxicity. Epirubicin has been incorporated into most of the anthracycline containing chemotherapy combinations in well-conducted clinical trials involving large numbers of patients. It has also been investigated in studies involving the administration of Epirubicin in dose-dense chemotherapy schedules. Short term follow up of dose-dense clinical trials demonstrated safety comparable to that of doxorubicin. This review summarizes published clinical trials investigating Epirubicin in the treatment of early and advanced breast cancer.
[Epirubicin (4'-epi-adriamycin]
Gan To Kagaku Ryoho 1990 Jan;17(1):151-9.PMID:2404456doi
Epirubicin (trade name: Falmorubicin) is a stereoisomer, in which the hydroxyl group of doxorubicin is inverted at position 4', and has the similar mechanism of action as that of doxorubicin; namely, this new anthracycline anticancer agent for injection shows a wide antitumor spectrum and strong antitumor activity via the inhibition of DNA and RNA synthesis. In non-clinical experiments, the effect of Epirubicin on transplantable murine tumors was similar or superior to that of doxorubicin in rats and mice. As for pharmacodynamics, this drug was found to rapidly penetrate into the tissue from the blood, and to remain there for a long period of time. This drug has been widely used abroad for the treatment of various solid cancers, such as breast cancer, and tumors of hematopoietic organs, such as malignant lymphoma. In Japan, it was proved clinically that the drug was effective on a wide range of tumors, including acute leukemia, malignant lymphoma, breast cancer, ovarian cancer, gastric cancer, hepatic cancer and ureteral epithelioma(bladder cancer, renal cancer and ureteral cancer). In a comparative study of chronic cardiotoxicity, it was noted that Epirubicin produced less damage to the myocardium than doxorubicin when every morphological change was examined as an indicator. Electrocardiographic and histopathological findings also disclosed that Epirubicin exhibited a smaller effect on the myocardium than that of doxorubicin. In conclusion, Epirubicin is a new antitumor agent having an antitumor effect similar or superior to that of doxorubicin with the various toxicities, including cardiotoxicity, which are reduced in this drug in comparison to those of doxorubicin.
Epirubicin in combination with the taxanes
Semin Oncol 2001 Aug;28(4 Suppl 12):41-50.PMID:11552229doi
The anthracyclines, and doxorubicin in particular, have been the most widely used drugs for advanced and metastatic breast cancer. Epirubicin shares the same spectrum of antitumor activity as doxorubicin, however, a therapeutic advantage of Epirubicin is the higher cumulative dose at which the anthracycline-induced cardiotoxicity becomes clinically evident. The taxanes have quickly been established as important chemotherapeutic agents in the armamentarium of drugs to treat breast cancer. Evaluation of the combination of anthracyclines with the taxanes was a logical research step with the aim to improve overall outcome and, potentially, survival of breast cancer patients. The findings of a high rate of cardiotoxicity from the initial phase II trials of combination doxorubicin/paclitaxel led investigators to alter the anthracycline and the taxane component of the combination by substitution with Epirubicin and/or docetaxel, respectively. Results of phase I and II clinical trials with Epirubicin plus a taxane shows a high level of antitumor activity, with the absence of significant cardiac toxicity and limited severity of other nonhematologic toxicities, thus making the Epirubicin and taxane combinations highly attractive. Additional studies in metastatic breast cancer patients, for whom prolonged administration with an anthracycline is of potential clinical benefit, are underway. Evaluation of Epirubicin and taxane combinations in the adjuvant setting are warranted and ongoing where prevention of cardiotoxicity is as important as efficacy.
Epirubicin-induced Kounis syndrome
BMC Cardiovasc Disord 2021 Mar 12;21(1):133.PMID:33711934DOI:10.1186/s12872-021-01936-4.
Background: Kounis syndrome is an acute coronary syndrome that appears in the setting of anaphylactic reaction or hypersensitivity. Many drugs and environmental exposures have been identified as potential offenders, and diagnosis and treatment can be challenging. Case presentation: A 62-year-old man with recurrent bladder cancer underwent an intra-iliac artery Epirubicin injection. After the injection, he developed chest pain and a systemic allergic reaction, with electrocardiographic alterations and elevated troponin-I levels. Emergent coronary angiography showed right coronary artery spasm and no stenosis of the other coronary arteries. This reaction was considered compatible with an allergic coronary vasospasm. A diagnosis of Kounis syndrome was made. Conclusions: Kounis syndrome is common, but a prompt diagnosis is often not possible. This case is the first to suggest that an intraarterial Epirubicin injection could potentially be one of its triggers. All physicians should be aware of the pathophysiology of this condition to better recognize it and start appropriate treatment; this will prevent aggravation of the vasospastic cardiac attacks and yield a better outcome.
Epirubicin: a review of its intravesical use in superficial bladder cancer
Drugs Aging 1999 Oct;15(4):307-33.PMID:10582777DOI:10.2165/00002512-199915040-00006.
The anthracycline Epirubicin has been investigated for intravesical use in patients with superficial bladder cancer. In multicentre, randomised trials, prophylaxis with intravesical Epirubicin 30 to 80 mg after transurethral resection (TUR) was more effective than no prophylaxis in the prevention of disease recurrence. Intravesical prophylaxis with Epirubicin was as effective as that with equivalent dosages of doxorubicin after TUR. Data are conflicting concerning the relative efficacy of intravesical Epirubicin and bacillus Calmette-Guerin (BCG) in patients at intermediate risk of recurrence after TUR, but Epirubicin was less effective than BCG in those at high risk. The efficacy and tolerability of prophylaxis with Epirubicin relative to that with mitomycin is not yet established. The efficacy of Epirubicin as prophylaxis after TUR in combination with BCG or interferon-alpha-2b, or as treatment in patients with superficial bladder cancer has been evaluated in small, noncomparative trials, but requires clarification. Adverse events associated with intravesical Epirubicin were generally mild and transient. The most common adverse events were localised to the bladder (cystitis, haematuria and urinary tract infection). Systemic adverse events (cardiac, haematological or related to hypersensitivity) were not reported in many trials of intravesical Epirubicin, and when reported generally occurred in < or =5% of patients who received the drug. Intravesical Epirubicin was generally tolerated as well as intravesical doxorubicin and was associated with a lower incidence of mild chemical cystitis in 1 clinical trial. The incidence of adverse events associated with intravesical Epirubicin was markedly lower than that associated with intravesical BCG. Conclusions: Intravesical Epirubicin has shown efficacy in preventing disease recurrence after TUR of superficial bladder cancer. In comparison with equivalent dosages of doxorubicin, the efficacy of Epirubicin for this indication is generally similar, and the tolerability profile may be more favourable. Epirubicin is less effective than BCG as intravesical prophylaxis in patients at high risk of recurrence after TUR; the relative efficacy of Epirubicin and BCG after TUR in patients at intermediate risk is not yet clear. Intravesical Epirubicin is generally tolerated better than BCG. Intravesical Epirubicin may be used as prophylaxis after TUR in patients who are at low or intermediate risk of recurrence of superficial bladder cancer.