Idarubicin
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| Other names | 9-acetyl-7-(4-amino-5-hydroxy-6-methyl-tetrahydropyran-2-yl)oxy-6,9,11-trihydroxy-7,8,9,10-tetrahydrotetracene-5,12-dione |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a691004 |
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| Pharmacokinetic data | |
| Protein binding | 97% |
| Elimination half-life | 22 hours |
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| Chemical and physical data | |
| Formula | C26H27NO9 |
| Molar mass | 497.494 g/mol g·mol−1 |
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Idarubicin /ˌaɪdəˈruːb[invalid input: 'ɨ']sɪn/ or 4-demethoxydaunorubicin is an anthracycline antileukemic drug. It inserts itself into DNA and prevents DNA from unwinding by interfering with the enzyme topoisomerase II. It is an analog of daunorubicin, but the absence of a methoxy group increases its fat solubility and cellular uptake.[1] Similar to other anthracyclines, it also induces histone eviction from chromatin.[2]
It belongs to the family of drugs called antitumor antibiotics.
It is currently combined with cytosine arabinoside as a first line treatment of acute myeloid leukemia.
It is distributed under the trade names Zavedos (UK) and Idamycin (USA).
References
- ^ Package insert
- ^ Pang B, Qiao X, Janssen L, Velds A, Groothuis T, Kerkhoven R, Nieuwland M, Ovaa H, Rottenberg S, van Tellingen O, Janssen J, Huijgens P, Zwart W, Neefjes J (2013). "Drug-induced histone eviction from open chromatin contributes to the chemotherapeutic effects of doxorubicin". Nature Communications. 4: 1908. doi:10.1038/ncomms2921. PMID 23715267.
{{cite journal}}: CS1 maint: multiple names: authors list (link)
External links
- Idarubicin bound to proteins in the PDB
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