Idarubicin Hydrochloride 57852-57-0
Idarubicin Hydrochloride is an anthracycline antibiotic with antineoplastic actions similar to those of doxorubicin. Idarubicin is used as the hydrochloride, alone or with other drugs, for the induction of remission in patients with acute myeloid leukaemias. Idarubicin Hydrochloride differs from doxorubicin in that it lacks a methoxy group at the 4-position of the D-ring on the aglycone. This deletion increases the lipophilicity of Idarubicin Hydrochloride compared with doxorubicin and may increase DNA binding. Idarubicin Hydrochloride is also used as a second-line treatment in acute lymphoblastic leukaemia, and advanced breast cancer. Idarubicin Hydrochloride has been tried in multiple myeloma and non-Hodgkin's lymphoma. Idarubicin Hydrochloride is indicated for use in combination with cytarabine (Ara-C) for induction therapy of acute myelogenous leukemia (AML).
Idarubicin Hydrochloride's innovator is Pfizer-Global and appears world-wide under the brand name Idamycin Pfs.
The mechanism of action of Idarubicin Hydrochloride is similar to that of other anthracycline antineoplastics. Idarubicin Hydrochloride complexes with DNA by intercalating between DNA base pairs, causing the helix to change shape. This simple act of changing the conformation of DNA can interfere with strand elongation by inhibiting DNA polymerase and inhibit protein synthesis due to effects on RNA polymerase. Idarubicin Hydrochloride inhibits the uptake of thymidine into cancer cells and normal fibroblasts at lower concentrations than other anthracyclines. As with other anthracylines, Idarubicin Hydrochloride inbibits topoisomerase II, an enzyme responsible for repairing faulty sections of DNA, causing double-strand DNA breaks. This occurs most commonly in the G2-phase of the cell cycle, although, in general, Idarubicin Hydrochloride is considered non-cell cycle specific.
Idarubicin Hydrochloride and its metabolite seem to be less susceptible to multiple drug resistance (MDR, P-gp) than daunorubicin and its metabolites. Studies have shown that cyclosporine and other modulators of MDR may increase the cytotoxicity of the alcohol metabolite of Idarubicin Hydrochloride.
Idarubicin Hydrochloride appears in the following formulation and dosage:
Intravenous Powder for solution: 5 mg, 10 mg and 20 mg
Intravenous Solution: 1 mg/ml
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|---|---|
| Idarubicin Hydrochloride CAS number: | 57852-57-0 |
| ATC code: | L01DB06 |
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| DrugBank: | |
| Formula: | C26H27NO9, HCl |
| Molecular mass: | 534.0 g/mol |
| Idarubicin Hydrochloride Assay/Purity: | Typically NLT 98% |
