Epirubicin: A Review of its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Use in Cancer Chemotherapy
Abstract
Epirubicin is the 4' epimer of the anthracycline antibiotic doxorubicin, and has been used alone or in combination with other cytotoxic agents in the treatment of a variety of malignancies. Comparative and noncomparative clinical trials have demonstrated that regimens containing conventional doses of epirubicin achieved equivalent objective response rates and overall median survival as similar doxorubicin-containing regimens in the treatment of advanced and early breast cancer, non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), non-Hodgkin's lymphoma, ovarian cancer, gastric cancer and nonresectable primary hepatocellular carcinoma. Recently, dose-intensive regimens of epirubicin have achieved high response rates in a number of malignancies including early and advanced breast cancer and lung cancer. The major acute dose-limiting toxicity of anthracyclines is myelosuppression. In vitro and clinical studies have shown that, at equimolar doses, epirubicin is less myelotoxic than doxorubicin. The lower haematological toxicity of epirubicin, as well as the recent introduction of supportive measures such as colony-stimulating factors, has allowed dose-intensification of epirubicin-containing regimens, which is particularly significant because of the definite dose-response relationship of anthracyclines. Cardiotoxicity, which is manifested clinically as irreversible congestive heart failure and/or cardiomyopathy, is the most important chronic cumulative dose-limiting toxicity of anthracyclines. Epirubicin has a lower propensity to produce cardiotoxic effects than doxorubicin, and its recommended maximum cumulative dose is almost double that of doxorubicin, thus allowing for more treatment cycles and/or higher doses of epirubicin. In summary, dose-intensive epirubicin-containing regimens, which are feasible due to its lower myelosuppression and cardiotoxicity, have produced high response rates in early breast cancer, a potentially curable malignancy, as well as advanced breast, and lung cancers. Furthermore, there is evidence to suggest that improved response rates can improve quality of life in some clinical settings, but whether this leads to prolonged survival has not yet been determined. Recently implemented supportive measures such as colony-stimulating factors, prophylactic antimicrobials and peripheral blood stem cell support may help achieve other potential advantages of dose-intensive epirubicin-containing regimens such as reductions in morbidity and length of hospital admissions.
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Doxorubicin affects both DNA and RNA synthesis.
“Doxorubicin that has a broad spectrum of activity both in experimental tumor models and in human malignancy, affects both DNA and RNA synthesis [22].”
From Chemotherapeutic treatment efficacy and sensitivity are increased by adjuvant alternating electric fields (TTFields) (2009) · cites this paper as [22]
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Kashima, H., Momose, F., Umehara, H., Miyoshi, N., Ogo, N., Muraoka, D., Shiku, H., Harada, N., & Asai, A. (2016) · PLoS ONE · doi:10.1371/journal.pone.0156643 · Cited by 22 · see citing works
Evangelatov, A., Skrobanska, R., Mladenov, N., Petkova, M., Yordanov, G. G., & Pankov, R. G. (2014) · Drug Delivery · doi:10.3109/10717544.2014.962117 · Cited by 22 · see citing works
- Authors
- Plosker, G. L., & Faulds, D.
- Venue
- Drugs
- Published
- 1993-05
- Volume
- 45
- Issue
- 5
- Pages
- 788-856
- ISSN
- 0012-6667 (ISSN-L)
- OpenAlex
- W1993672158
- Cited by
- 223
- References
- 429
- Citations by year
- 2026: 6 · 2025: 9 · 2024: 13 · 2023: 8 · 2022: 14 · 2021: 10 · 2020: 5 · 2019: 4 · 2018: 1 · 2017: 10 · 2016: 7 · 2015: 5 · 2014: 7 · 2013: 10 · 2012: 4
- FWCI
- 3.62
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drugs (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Cardiology and Cardiovascular Medicine › Chemotherapy-induced cardiotoxicity and mitigation
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Cancer therapeutics and mechanisms
- Health Sciences › Medicine › Oncology › Cancer Treatment and Pharmacology
- Keywords
- epirubicin, anthracyclines, doxorubicin, dose-intensive chemotherapy, myelosuppression, cardiotoxicity, breast cancer, non-small cell lung cancer, small cell lung cancer, non-Hodgkin lymphoma, ovarian cancer, gastric cancer, hepatocellular carcinoma, colony-stimulating factors, hematopoietic growth factors
- MeSH terms
- Clinical Trials as Topic, Female, Humans, Male, Neoplasms, Epirubicin
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