- Molecular NameIdarubicin
- SynonymIdarubicin Hcl; Idarubicin Hydrochloride; Idarubicina [INN-Spanish]; Idarubicine [INN-French]; Idarubicinum [INN-Latin]
- Weight497.5
- Drugbank_IDDB01177
- ACS_NO58957-92-9
- Show 3D model
- LogP (experiment)0.803
- LogP (predicted, AB/LogP v2.0)1.22
- pkaN/A
- LogD (pH=7, predicted)0.11
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-4.48
- LogSw (predicted, AB/LogsW2.0)0.14
- Sw (mg/ml) (predicted, ACD/Labs)0.01
- No.of HBond Donors6
- No.of HBond Acceptors10
- No.of Rotatable Bonds3
- TPSA176.61
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn anthracycline antileukemic drug that is currently combined with cytosine arabinoside as a first line treatment of acute myeloid leukemia. It belongs to the family of drugs called antitumor antibiotics.
- Absorption_valueN/A
- Absorption (description)After intravenous administration, idarubicin is rapidly distributed into body tissues and extensively tissue bound. After oral administration, idarubicin is rapidly absorbed.
- Caco_2N/A
- Bioavailability28.0
- Protein binding97.0
- Volume of distribution (VD)24.7 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmIt is mostly metabolised in the liver, by aldoketoreductase, which reduces the ketone function at the C13 position to idarubicinol (1,3-dihydroidarubicin), the principal metabolite.
- Half life15.2 h (idarubicin); 41 h (idarubicinol)
- ExcretionThe unchanged drug and metabolite are excreted mainly in bile but also in urine. Oral bioavailability is between 24 and 39% after oral administration.
- Urinary Excretion<5
- Clerance29 ml/min/kg
- ToxicityAcute/high doses of idarubicin (> 600 mg/m2) can lead to myocardial toxicity, with potentially fatal congestive heart failure (CHF), life-threatening arrhythmias and serious gastro-intestinal events, for example, bleeding and preforations.
- LD50 (rat)N/A
- LD50 (mouse)N/A