Epirubicin (epirubicin HCl)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Epirubicin, the 4'-epimer of doxorubicin, is an anthracycline glycoside antineoplastic antibiotic.

Epirubicin, the 4'-epimer of doxorubicin, is an anthracycline glycoside antineoplastic antibiotic that is a semisynthetic derivative of daunorubicin. The spacial orientation of the hydroxyl group at carbon 4' of the sugar moiety results in epirubicin being a weaker base and more lipophilic than doxorubicin, which may result in an improved therapeutic index for epirubicin; however, substantial differences in the types of biochemical interactions involved in the mechanism(s) of action and toxicity of the epimeric analogs do not appear to exist. As a result, the spectrum of pharmacologic, antineoplastic, and toxic effects of the drugs arequalitatively identical, but at equimolar doses, epirubicin appears to be less toxic with regard to both general toxicity and cardiotoxicity.

The spacial orientation of the hydroxyl group also allows glucuronide conjugation of epirubicin, which is unique among currently available anthracyclines, and may be responsible for the relatively high plasma clearance and faster elimination of the drug.

Epirubicin exhibits pharmacologic actions similar to those of daunorubicin and doxorubicin. The precise and/or principal mechanism(s) of antineoplastic action of anthracyclines is not fully understood. Experimental evidence indicates that epirubicin, like other anthracyclines, forms a complex with DNA by intercalation between base pairs, causing inhibition of DNA synthesis and DNA-dependent RNA synthesis by the resulting template disordering and steric obstruction.

Protein synthesis also is inhibited. Such intercalation triggers DNA cleavage by topoisomerase II, resulting in cytocidal activity. DNA helicase also is inhibited, resulting in interference with replication and transcription; epirubicin also generates cytotoxic free radicals.

For additional information, see Pharmacology in Doxorubicin 10:00. Because of the shared mechanisms between doxorubicin and epirubicin, the drugs appear to exhibit a similar spectrum of activity against a wide variety of solid tumors and hematologic malignancies, and complete cross-resistance between the 2 anthracyclines has been documented in vitro.

Epirubicin undergoes extensive hepatic metabolism, and is eliminated principally by metabolism and biliary excretion; urinary excretion is only a minor elimination pathway.

USES: Epirubicin is used to treat breast cancer. It belongs to a class of drugs known as anthracyclines and works by slowing or stopping the growth of cancer cells.

Generic name: epirubicin HCl
Pronunciation: (epp-ih-REWB-ih-sin)

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Epirubicin:

  • Locally Advanced Breast Carcinoma

Dosing

To obtain optimum therapeutic results with minimum adverse effects, dosage of epirubicin hydrochloride must be based on the clinical, cardiac, hepatic, renal, and hematologic response and tolerance of the patient and on other chemotherapy or irradiation being used.

Drug interactions

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Contraindications

Known hypersensitivity to epirubicin, other anthracyclines, anthracenediones, or any ingredient in the formulation.

Baseline neutrophil count less than 1500/mm3; severe myocardial or hepatic impairment or recent myocardial infarction; previous anthracycline therapy up to the maximum cumulative dose.

Adverse reactions

Epirubicin hydrochloride is a toxic drug with a low therapeutic index. A therapeutic response is not likely to occur without some evidence of toxicity. The major toxic effects of the drug are on the normal, rapidly proliferating tissues, particularly those of the bone marrow, GI and oral mucosa, and hair follicles. Alopecia, nausea/vomiting, myelosuppression (leukopenia, neutropenia, anemia, thrombocytopenia), amenorrhea, mucositis, lethargy, hot flushes (flashes), diarrhea, infection, local effects (e.g., venous irritation), conjunctivitis/keratitis, rash/pruritus, skin and nail changes (e.g., hyperpigmentation) , fever, and anorexia occur commonly. Urticaria, photosensitivity, and anaphylaxis (including shock) also have occurred.

Precautions

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ICD codes

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Formulary status

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Last reviewed · Source: First Databank (FDB) drug data