Indication |
For the treatment of acute myeloid leukemia (AML) in adults. This
includes French-American-British (FAB) classifications M1 through M7. |
Pharmacodynamics |
Idarubicin is an antineoplastic in the anthracycline class.
General properties of drugs in this class include: interaction with DNA
in a variety of different ways including intercalation (squeezing
between the base pairs), DNA strand breakage and inhibition with the
enzyme topoisomerase II. Most of these compounds have been isolated from
natural sources and antibiotics. However, they lack the specificity of
the antimicrobial antibiotics and thus produce significant toxicity. The
anthracyclines are among the most important antitumor drugs available.
Doxorubicin is widely used for the treatment of several solid tumors
while daunorubicin and idarubicin are used exclusively for the treatment
of leukemia. Idarubicin may also inhibit polymerase activity, affect
regulation of gene expression, and produce free radical damage to DNA.
Idarubicin possesses an antitumor effect against a wide spectrum of
tumors, either grafted or spontaneous. The anthracyclines are cell
cycle-nonspecific. |
Mechanism of action |
Idarubicin has antimitotic and cytotoxic activity through a number
of proposed mechanisms of action: Idarubicin 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. |
Absorption |
Not Available |
Volume of distribution |
Not Available |
Protein binding |
97% |
Metabolism |
Not Available |
Route of elimination |
The drug is eliminated predominately by biliary and to a lesser extent by renal excretion, mostly in the form of idarubicinol. |
Half life |
22 hours |
Clearance |
Not Available |
Toxicity |
Not Available |