Idarubicin Hydrochloride is the hydrochloride salt of idarubicin, a semisynthetic anthracycline antineoplastic antibiotic and analogue of daunorubicin. The molecule of Idarubicin Hydrochloride features a tetracyclic anthraquinone chromophore with a daunosamine sugar moiety attached via glycosidic linkage.
Idarubicin Hydrochloride is a potent anthracycline antineoplastic antibiotic approved for the treatment of acute myelogenous leukemia (AML) and pediatric acute lymphocytic leukemia (ALL) . As a topoisomerase II inhibitor, Idarubicin Hydrochloride intercalates into DNA and inhibits DNA replication, ultimately interfering with RNA and protein synthesis . The high lipophilicity of Idarubicin Hydrochloride allows it to penetrate cell membranes more efficiently than other anthracycline compounds . Idarubicin Hydrochloride is rapidly metabolized to its 13-dihydro derivative (idarubicinol), which is more stable than the parent compound and contributes to its clinical activity . The compound is a substrate for CYP2D6 and CYP2C9 and induces apoptosis through enhanced expression of Fas and caspase-3/caspase-7 .
Idarubicin Hydrochloride is an antimitotic and cytotoxic agent. It is used as first-line treatment for adult acute non-lymphocytic leukemia (ANLL), as well as for induction remission therapy in relapsed and refractory patients. As a second-line treatment drug, it is used for acute lymphocytic leukemia (ALL in adults and children.
Untoward Effect
Myelosuppression and cardiotoxicity; fatal infections; reversible alopecia; gastrointestinal reactions such as nausea, vomiting, mucositis, especially oral mucositis, esophagitis, diarrhea, fever, chills, rash; elevated liver enzymes and bilirubin; urine turns red 1 to 2 days after administration of idarubicin hydrochloride
Bioactivity
Idarubicin hydrochloride (4-demethoxydaunorubicin, NSC256439, 4-DMDR) is the hydrochloride salt form of idarubicin, an anthracycline antibiotic. It inhibits DNA topoisomerase II (topo II) in MCF-7 cells, with an IC50 of 3.3 ng/mL in cell-free assays. Idarubicin can induce mTOR-dependent cytotoxic autophagy.
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