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Anthracyclines and anthracenedionesIn useDerivative of an earlier drug

Idarubicin

Also known as Idamycin, 4-demethoxydaunorubicin

A synthetic analogue of daunorubicin that lacks the methoxy group at position 4, given by injection. The US label lists treatment of acute myeloid leukaemia in adults as part of combination chemotherapy.

From discovery to approval

  1. 1976 · Earliest report found

    A 1976 paper by Arcamone and colleagues in Cancer Treatment Reports described the chemical synthesis of four daunorubicin derivatives lacking the methoxyl group at position C-4. 4-Demethoxydaunorubicin was effective against mouse leukaemias at doses four to eight times lower than daunorubicin.[2][3][4][5][1]

  2. 1990-09-27 · FDA regular

    Idarubicin hydrochloride for injection (Idamycin), NDA 050661, original approval, classed as a new molecular entity with priority review and orphan status in the Drugs@FDA history. The original label and letter are not available there, so the indication at approval is not stated here; the current label lists acute myeloid leukaemia in adults. The type regular is an inference: no accelerated-approval wording was found.[6]

How it works

A DNA-intercalating analogue of daunorubicin that inhibits nucleic acid synthesis and interacts with topoisomerase II. According to the label, the missing methoxy group at position 4 makes the molecule highly lipophilic, which increases the rate of cellular uptake compared with other anthracyclines.[1]

Where it came from and why

Arcamone's 1984 review says the importance of adriamycin led to a programme from 1972 to develop second-generation anthracyclines, which discovered epirubicin, 4-demethoxydaunorubicin (idarubicin) and esorubicin. A 1986 overview describes idarubicin as active by the oral as well as the intravenous route.

Cancers

  • Acute myeloid leukaemia

    The 2022 US label lists idarubicin, with other approved antileukaemic drugs, for acute myeloid leukaemia in adults, including FAB classifications M1 through M7; the 2026 label lists it for adults with AML as a component of combination chemotherapy.[1]

  • Acute myeloid leukaemia, comparison with daunorubicin

    In a single-institution randomised trial of 130 adults aged 16 to 60, complete remission occurred in 48 of 60 patients (80%) given idarubicin with cytarabine and 35 of 60 (58%) given daunorubicin with cytarabine (P = .005).[5]

  • Acute myeloid leukaemia, multicentre comparison

    A 32-site randomised study of 214 untreated adults compared cytarabine plus idarubicin 13 mg/m2 or daunorubicin 45 mg/m2 daily for 3 days and reported complete remission rates of 70% and 59% (P = .08).[7]

Family and partners

Derived from: Daunorubicin

Worth knowing

  • In the single-institution trial overall survival was 19.5 months with idarubicin and cytarabine and 13.5 months with daunorubicin and cytarabine (P = .025) at a median follow-up of 2.5 years.[5]
  • In the 214-patient multicentre trial median survival was 12.9 months after idarubicin and 8.7 months after daunorubicin (P = .038), and the authors concluded that idarubicin plus cytarabine was superior for induction at the doses and schedule used.[7]
  • A 1986 overview reports that oral idarubicin had antitumour activity in breast cancer and as a single agent in adult leukaemias, and describes the drug as active by both oral and intravenous routes.[4]
  • The 2026 US label states that the incidence of drug-induced congestive heart failure is increased at cumulative idarubicin doses exceeding 90 mg/m2 in adults.[8]

On this site

References

  1. U.S. Food and Drug Administration. Idamycin PFS (idarubicin hydrochloride injection): prescribing information (NDA 050661 supplement 017, revised April 2022). Source
  2. Arcamone F, Bernardi L, Giardino P, Patelli B, Marco A, Casazza AM, et al. Synthesis and antitumor activity of 4-demethoxydaunorubicin, 4-demethoxy-7,9-diepidaunorubicin, and their beta anomers. Cancer Treat Rep. 1976;60(7):829-34. PubMed
  3. Arcamone F. [Adriamycin and its analogs]. Tumori. 1984;70(2):113-9. PubMedDOI
  4. Ganzina F, Pacciarini MA, Di Pietro N. Idarubicin (4-demethoxydaunorubicin). A preliminary overview of preclinical and clinical studies. Invest New Drugs. 1986;4(1):85-105. PubMedDOI
  5. Berman E, Heller G, Santorsa J, McKenzie S, Gee T, Kempin S, et al. Results of a randomized trial comparing idarubicin and cytosine arabinoside with daunorubicin and cytosine arabinoside in adult patients with newly diagnosed acute myelogenous leukemia. Blood. 1991;77(8):1666-74. PubMed
  6. U.S. Food and Drug Administration. Drugs@FDA: Approval date(s) and history, letters, labels, reviews for NDA 050661 (Idamycin, idarubicin hydrochloride). Page read 2026-10-29. Source
  7. Wiernik PH, Banks PL, Case DC Jr, Arlin ZA, Periman PO, Todd MB, et al. Cytarabine plus idarubicin or daunorubicin as induction and consolidation therapy for previously untreated adult patients with acute myeloid leukemia. Blood. 1992;79(2):313-9. PubMed
  8. Pfizer Laboratories Div Pfizer Inc. Idamycin PFS (idarubicin hydrochloride) injection: prescribing information. DailyMed, set ID 0a5a6d93-cc1e-4d7f-8da1-446c134503b3, published 17 April 2026. Source
  9. U.S. Food and Drug Administration. Drugs@FDA: Approval date(s) and history, letters, labels, reviews for NDA 050734 (Idamycin PFS, idarubicin hydrochloride). Page read 2026-10-29. Source