Product Information
Registration Status: ActiveEBERUBI INJECTION 2MG/ML is approved to be sold in Singapore with effective from 2008-07-25. It is marketed by NOVARTIS (SINGAPORE) PTE LTD, with the registration number of SIN13500P.
This product contains Epirubicin 2mg/ml in the form of INFUSION, SOLUTION CONCENTRATE. It is approved for INTRAVENOUS, INTRAVESICAL use.
This product is manufactured by Ebewe Pharma Ges.m.b.H. Nfg.KG in AUSTRIA.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
An anthracycline which is the 4'-epi-isomer of doxorubicin. The compound exerts its antitumor effects by interference with the synthesis and function of DNA. [PubChem]
Indication
For use as a component of adjuvant therapy in patients with evidence of axillary node tumor involvement following resection of primary breast cancer.
Mechanism of Action
Epirubicin has antimitotic and cytotoxic activity. It inhibits nucleic acid (DNA and RNA) and protein synthesis through a number of proposed mechanisms of action: Epirubicin forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes. It also interferes with DNA replication and transcription by inhibiting DNA helicase activity.
Pharmacokinetics
- Absorption
- 100%
- Distribution
- * 21 ± 2 L/kg [60 mg/m2 Dose] * 27 ± 11 L/kg [75 mg/m2 Dose] * 23 ± 7 L/kg [120 mg/m2 Dose] * 21 ± 7 L/kg [150 mg/m2 Dose]
- Metabolism
- Extensively and rapidly metabolized in the liver. Epirubicin is also metabolized by other organs and cells, including red blood cells. The four main metabolic routes are: (1) reduction of the C-13 keto-group with the formation of the 13(S)-dihydro derivative, epirubicinol; (2) conjugation of both the unchanged drug and epirubicinol with glucuronic acid; (3) loss of the amino sugar moiety through a hydrolytic process with the formation of the doxorubicin and doxorubicinol aglycones; and (4) loss of the amino sugar moiety through a redox process with the formation of the 7-deoxy-doxorubicin aglycone and 7-deoxy-doxorubicinol aglycone. Epirubicinol exhibits in vitro cytoxic activity (~10% that of epirubicin), but it is unlikely to reach sufficient concentrations in vivo to produce cytotoxic effects.
- Elimination
Clearance
* 65 +/- 8 L/hour [Patients1 with Solid Tumors Receiving Intravenous Epirubicin 60 mg/m2] * 83 +/- 14 L/hour [Patients1 with Solid Tumors Receiving Intravenous Epirubicin 75 mg/m2] * 65 +/- 13 L/hour [Patients1 with Solid Tumors Receiving Intravenous Epirubicin 120 mg/m2] * 69 +/- 13 L/hour [Patients1 with Solid Tumors Receiving Intravenous Epirubicin 150 mg/m2]
Toxicity
bone marrow aplasia, grade 4 mucositis, and gastrointestinal bleeding
Active Ingredient/Synonyms
4'-Epiadriamycin | Epiadriamycin | Epirubicin | Epirubicina | Epirubicine | Epirubicinum | Pidorubicina | Pidorubicine | Pidorubicinum | Epirubicin |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.