Epirubicin: a review of the pharmacology, clinical activity, and adverse effects of an adriamycin analogue

J Clin Oncol. 1986 Mar;4(3):425-39. doi: 10.1200/JCO.1986.4.3.425.


Epirubicin (4'-epidoxorubicin) is an antineoplastic agent derived from doxorubicin. The compounds differ in the configuration of the hydroxyl group at the 4' position. Epirubicin, like doxorubicin, exerts its antitumor effects by interference with the synthesis and function of DNA and is most active during the S phase of the cell cycle. Epirubicin is administered by intravenous (IV) injection. It is metabolized by the liver and primarily eliminated in the bile. About 10% of the drug is eliminated in the urine. Dosage adjustments are recommended for patients with liver metastases or elevated liver function tests. The elimination half-life of epirubicin is 30 to 40 hours. Clinical studies indicate activity in breast cancer, non-Hodgkin's lymphomas, ovarian cancer, soft-tissue sarcomas, and pancreatic cancer. There is also evidence of activity against gastric cancer, small-cell lung cancer, and acute leukemia. Epirubicin has limited activity as a single agent against head and neck tumors or non-small-cell lung cancer, but may be beneficial in combination with other agents. The overall activity of epirubicin appears to be comparable with that of doxorubicin. However, more studies are needed to define its role in combination chemotherapeutic regimens. The acute dose-limiting toxicity of epirubicin is myelosuppression. Nausea, vomiting, and alopecia are also common. Epirubicin may cause transient cardiac arrhythmias and alterations of the electrocardiogram. Chronic therapy is limited, but available data indicate that epirubicin can be administered in higher cumulative doses than doxorubicin before cardiotoxicity limits further therapy.

Publication types

  • Review

MeSH terms

  • Bone Marrow / drug effects
  • Breast Neoplasms / drug therapy
  • Carcinoma, Renal Cell / drug therapy
  • Carcinoma, Small Cell / drug therapy
  • Colonic Neoplasms / drug therapy
  • Doxorubicin / adverse effects
  • Doxorubicin / metabolism
  • Doxorubicin / pharmacology
  • Doxorubicin / therapeutic use*
  • Drug Administration Schedule
  • Drug Evaluation
  • Epirubicin
  • Female
  • Head and Neck Neoplasms / drug therapy
  • Heart / drug effects
  • Humans
  • Kidney Neoplasms / drug therapy
  • Kinetics
  • Leukemia / drug therapy
  • Liver Neoplasms / drug therapy
  • Lung Neoplasms / drug therapy
  • Lymphoma / drug therapy
  • Male
  • Melanoma / drug therapy
  • Neoplasms / drug therapy*
  • Ovarian Neoplasms / drug therapy
  • Pancreatic Neoplasms / drug therapy
  • Rectal Neoplasms / drug therapy
  • Soft Tissue Neoplasms / drug therapy
  • Stomach Neoplasms / drug therapy
  • Urinary Bladder Neoplasms / drug therapy


  • Epirubicin
  • Doxorubicin