Drug intelligence / Profile preview

idarubicin + amifostine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

Idarubicin is an anthracycline antineoplastic agent used primarily in the treatment of acute myeloid leukemia (AML), often in combination with other chemotherapy drugs. It works by intercalating into DNA and inhibiting topoisomerase II, thereby disrupting DNA replication and transcription, which leads to cell death[1][2][4]. Amifostine is a cytoprotective agent (formerly known as WR-2721) developed to selectively protect normal tissues from the toxic effects of chemotherapy and radiation. It is a prodrug that is dephosphorylated by alkaline phosphatase in normal tissues to its active thiol metabolite, which acts as a free radical scavenger and hydrogen donor, protecting cells from DNA damage caused by cytotoxic agents[3][5][6]. Amifostine is FDA-approved for reducing cumulative renal toxicity associated with cisplatin therapy and for decreasing radiation-induced xerostomia but has also been studied for broader protective effects against various chemotherapeutic toxicities[5][6]. The combination of idarubicin + amifostine may be used when cytoprotection during anthracycline-based chemotherapy regimens is desired.

02

Targets

TOP2A (DNA topoisomerase II)

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