Chemical: Drug
idarubicin

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.


1. FDA Label for idarubicin

Full label available at DailyMed

Genes and/or phenotypes found in this label

  • Leukemia
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Leukemia, Myeloid
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Leukemia, Myeloid, Acute
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Leukemia, Nonlymphocytic, Acute
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Neoplasms
    • Warnings section, Adverse reactions section, Precautions section
    • source: PHONT

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for idarubicin

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA
rs1045642 NC_000007.13:g.87138645A>G, NC_000007.14:g.87509329A>G, NG_011513.1:g.208920T>C, NM_000927.4:c.3435T>C, NP_000918.2:p.Ile1145=, rs10239679, rs11568726, rs117328163, rs17210003, rs2229108, rs386513066, rs60023214, rs9690664
A > G
SNP
I1145I
No VIP available CA VA
rs11231825 NC_000011.10:g.64592802T>C, NC_000011.9:g.64360274T>C, NG_008110.1:g.6993T>C, NM_001276326.1:c.426T>C, NM_001276327.1:c.426T>C, NM_144585.3:c.426T>C, NM_153378.2:c.-83T>C, NP_001263255.1:p.His142=, NP_001263256.1:p.His142=, NP_653186.2:p.His142=, XM_005273740.1:c.426T>C, XM_005273741.1:c.426T>C, XM_005273742.1:c.426T>C, XM_005273743.1:c.426T>C, XM_005273744.1:c.426T>C, XM_005273745.1:c.426T>C, XM_005273746.1:c.426T>C, XM_005273747.1:c.-764T>C, XM_006718430.2:c.426T>C, XM_006718431.2:c.321T>C, XP_005273797.1:p.His142=, XP_005273798.1:p.His142=, XP_005273799.1:p.His142=, XP_005273800.1:p.His142=, XP_005273801.1:p.His142=, XP_005273802.1:p.His142=, XP_005273803.1:p.His142=, XP_006718493.1:p.His142=, XP_006718494.1:p.His107=, rs17846504, rs17859573, rs60376821
T > C
SNP
H142H
No VIP available No Clinical Annotations available VA
rs1826909 NC_000004.11:g.100217743C>T, NC_000004.12:g.99296586C>T, NR_037884.1:n.4161-3713C>T, rs17512416, rs4525982, rs61683245
C > T
SNP
rs2032582 NC_000007.13:g.87160618A>C, NC_000007.13:g.87160618A>T, NC_000007.14:g.87531302A>C, NC_000007.14:g.87531302A>T, NG_011513.1:g.186947T>A, NG_011513.1:g.186947T>G, NM_000927.4:c.2677T>A, NM_000927.4:c.2677T>G, NP_000918.2:p.Ser893Ala, NP_000918.2:p.Ser893Thr, rs10228331, rs2229106, rs386553610, rs57135550, rs9641018
A > C
SNP
S893A
No VIP available CA VA
rs2070673 NC_000010.10:g.135340567A>T, NC_000010.11:g.133527063A>T, NG_008383.1:g.4701A>T, NM_000773.3:c.-333A>T, XM_005252665.1:c.21+190A>T
A > T
SNP
No VIP available CA VA
rs2302948 NC_000019.10:g.48592808C>T, NC_000019.9:g.49096065C>T, NG_029063.1:g.45637C>T, NM_004605.2:c.592C>T, NM_177973.1:c.637C>T, NP_004596.2:p.Leu198=, NP_814444.1:p.Leu213=, XM_005259182.1:c.205C>T, XM_005259182.2:c.205C>T, XP_005259239.1:p.Leu69=, rs59383755
C > T
SNP
L198L
No VIP available CA VA
rs2306744 NC_000004.11:g.71859352C>T, NC_000004.12:g.70993635C>T, NG_023303.1:g.5088C>T, NM_000788.2:c.-201C>T
C > T
SNP
No VIP available CA VA
rs2515641 NC_000010.10:g.135351362T>C, NC_000010.11:g.133537858C>T, NG_008383.1:g.15496C=, NG_008383.1:g.15496C>T, NM_000773.3:c.1263C=, NM_000773.3:c.1263C>T, NP_000764.1:p.Phe421=, XM_005252665.1:c.1323T>C, XP_005252722.1:p.Phe441=, rs17012766, rs60244712
T > C
SNP
F421F
No VIP available CA VA
rs3750117 NC_000007.13:g.33060946A>G, NC_000007.14:g.33021334A>G, NG_015800.1:g.46464T>C, NM_001002009.2:c.276T>C, NM_001002010.2:c.393T>C, NM_001166118.2:c.240T>C, NM_016489.12:c.276T>C, NP_001002009.1:p.Tyr92=, NP_001002010.1:p.Tyr131=, NP_001159590.1:p.Tyr80=, NP_057573.2:p.Tyr92=, XM_011515409.1:c.240T>C, XP_011513711.1:p.Tyr80=, rs11547832, rs17851350, rs57965368
A > G
SNP
Y92Y
No VIP available CA VA
rs4149056 NC_000012.11:g.21331549T>C, NC_000012.12:g.21178615T>C, NG_011745.1:g.52422T>C, NM_006446.4:c.521T>C, NP_006437.3:p.Val174Ala, rs52816141, rs60037639
T > C
SNP
V174A
No VIP available No Clinical Annotations available VA
rs6811453 NC_000004.11:g.100194977G>A, NC_000004.12:g.99273820G>A, NR_037884.1:n.3790-12975G>A, XR_244675.1:n.691-305G>A
G > A
SNP
No VIP available CA VA
rs80143932 NC_000004.11:g.71859193C>G, NC_000004.12:g.70993476C>G, NG_023303.1:g.4929C>G, NM_000788.2:c.-360C>G
C > G
C > T
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • Idarubicin Hcl
  • Idarubicin Hydrochloride
  • Idarubicina [INN-Spanish]
  • Idarubicine [INN-French]
  • Idarubicinum [INN-Latin]
Trade Names
  • Idamycin
  • Idamycin PFS
  • Idarubicin Aglycone
  • Idarubicin HCl PFS
Brand Mixture Names

PharmGKB Accession Id

PA449961

Type(s):

Drug

Description

An orally administered anthracycline antineoplastic. The compound has shown activity against breast cancer, lymphomas and leukemias, together with the potential for reduced cardiac toxicity.

Source: Drug Bank

Indication

For the treatment of acute myeloid leukemia (AML) in adults. This includes French-American-British (FAB) classifications M1 through M7.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

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.

Source: Drug Bank

Pharmacology

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.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Protein Binding

97%

Source: Drug Bank

Half-Life

22 hours

Source: Drug Bank

Route of Elimination

The drug is eliminated predominately by biliary and to a lesser extent by renal excretion, mostly in the form of idarubicinol.

Source: Drug Bank

Chemical Properties

Chemical Formula

C26H27NO9

Source: Drug Bank

Isomeric SMILES

C[C@H]1[C@H]([C@H](C[C@@H](O1)O[C@H]2C[C@@](CC3=C2C(=C4C(=C3O)C(=O)C5=CC=CC=C5C4=O)O)(C(=O)C)O)N)O

Source: Drug Bank

C[C@@H]1O[C@H](C[C@H](N)[C@@H]1O)O[C@H]1C[C@@](O)(CC2=C1C(O)=C1C(=O)C3=C(C=CC=C3)C(=O)C1=C2O)C(C)=O

Source: Drug Bank

Canonical SMILES

C[C@@H]1O[C@H]

Source: Drug Bank

Average Molecular Weight

497.4939

Source: Drug Bank

Monoisotopic Molecular Weight

497.168581467

Source: Drug Bank

SMILES

C[C@@H]1O[C@H](C[C@H](N)[C@@H]1O)O[C@H]1C[C@@](O)(CC2=C1C(O)=C1C(=O)C3=CC=CC=C3C(=O)C1=C2O)C(C)=O

Source: Drug Bank

InChI String

InChI=1S/C26H27NO9/c1-10-21(29)15(27)7-17(35-10)36-16-9-26(34,11(2)28)8-14-18(16)25(33)20-19(24(14)32)22(30)12-5-3-4-6-13(12)23(20)31/h3-6,10,15-17,21,29,32-34H,7-9,27H2,1-2H3/t10-,15-,16-,17-,21+,26-/m0/s1

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
TOP2A (source: Drug Bank)

Drug Interactions

Interaction Description
trastuzumab - idarubicin Trastuzumab may increase the cardiotoxicity of Idarubicin. Signs and symptoms of cardiac dysfunction should be monitored for frequently. Increased risk of heart failure. Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to idarubicin: 13

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenomics and the treatment of acute myeloid leukemia. Pharmacogenomics. 2016. Megías-Vericat Juan Eduardo, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Influence of ABCB1 polymorphisms upon the effectiveness of standard treatment for acute myeloid leukemia: A systematic review and meta-analysis of observational studies. The pharmacogenomics journal. 2015. Megías-Vericat J E, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Association of ABCB1 polymorphisms with prognostic outcomes of anthracycline and cytarabine in Chinese patients with acute myeloid leukemia. European journal of clinical pharmacology. 2015. He Hui, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
NT5C3 polymorphisms and outcome of first induction chemotherapy in acute myeloid leukemia. Pharmacogenetics and genomics. 2014. Cheong Hyun Sub, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Idarubicin is superior to daunorubicin in remission induction of de novo acute myeloid leukemia patients with high MDR1 expression. Pharmacogenomics. 2013. Shi Pengcheng, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Profiling of drug-metabolizing enzymes/transporters in CD33+ acute myeloid leukemia patients treated with Gemtuzumab-Ozogamicin and Fludarabine, Cytarabine and Idarubicin. The pharmacogenomics journal. 2012. Iacobucci I, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Anthracycline-Related Cardiomyopathy After Childhood Cancer: Role of Polymorphisms in Carbonyl Reductase Genes--A report From the Children's Oncology Group. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2011. Blanco Javier G, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenomic characterization of US FDA-approved cytotoxic drugs. Pharmacogenomics. 2011. Peters Eric J, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Association of ABCB1 polymorphisms with survival and in vitro cytotoxicty in de novo acute myeloid leukemia with normal karyotype. The pharmacogenomics journal. 2010. Gréen H, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Multidrug resistance-1 gene polymorphisms associated with treatment outcomes in de novo acute myeloid leukemia. International journal of cancer. Journal international du cancer. 2006. Kim Dong Hwan, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association between single nucleotide polymorphisms in deoxycytidine kinase and treatment response among acute myeloid leukaemia patients. Pharmacogenetics. 2004. Shi Jing-Yi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
New oral drugs in older patients: a review of idarubicin in elderly patients. Critical reviews in oncology/hematology. 2004. Crivellari Diana, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Role of MRP1 in multidrug resistance in acute myeloid leukemia. Leukemia : official journal of the Leukemia Society of America, Leukemia Research Fund, U.K. 1999. Legrand O, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0013-2526-86
DrugBank:
DB01177
ChEBI:
42068
PubChem Compound:
42890
PubChem Substance:
183368
46506973
Drugs Product Database (DPD):
2065630
ChemSpider:
39117
Therapeutic Targets Database:
DAP000050

Clinical Trials

These are trials that mention idarubicin and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.