ADMET-Absorption, Distribution, Metabolism, Excretion, and Toxicity

StatusFDA approved
AdministrationExclusively intravenous. Causes severe necrosis if administered intramuscularly or subcutaneously
PharmacologyA chemotherapy of the anthracycline family that is given as a treatment for some types of cancer. It is most commonly used to treat specific types of leukaemia (acute myeloid leukemia and acute lymphocytic leukemia). It was initially isolated from Streptomyces peucetius.

Absorption_valueN/A
Absorption (description)Conventional formulations of daunorubicin are rapidly distributed into body tissues following intravenous administration, particularly liver, lungs, kidneys, spleen and heart. It does not cross the blood–brain barrier.
Caco_2N/A
BioavailabilityN/A

Protein binding97.0
Volume of distribution (VD)Approx. 1000 L; 1055 L or 619 L/m2 (80 mg/m2); 897 L or 511 L/m2 (120 mg/m2).
Blood/Plasma Partitioning ratio (D_blood)N/A

ExcretionExcreted in bile (about 40%) and urine as the unchanged drug and metabolites. The major metabolite, daunorubicinol, has antineoplastic activity. A liposomal formulation of daunorubicin is also available that differs in its pharmacokinetic characteristics. Following intravenous administration it remains largely confined within the vascular fluid volume and therefore plasma clearance is higher. The values below apply to the conventional formulation.
Urinary ExcretionN/A
Clerance230 mL/min

ToxicityCardiotoxicity, both acute and chronic, is the main major dose-limiting adverse effect. It is more likely to occur if the total cumulative dose exceeds 550 mg/m2 in adults or 300 mg/m2 in children.
LD50 (rat)LD50=13 mg/kg (rat, IV)
LD50 (mouse)LD50=20 mg/kg (mice, IV);