- Molecular NameCladribine
- Synonym2-CdA; 2-Chloro-2'-deoxy-beta-adenosine; 2-Chloro-2'-deoxyadenosine; 2-Chlorodeoxyadenosine; Chlorodeoxyadenosine; cladribine
- Weight297.742
- Drugbank_IDDB00242
- ACS_NO4291-63-8
- Show 2D model
- LogP (experiment)0.03
- LogP (predicted, AB/LogP v2.0)1.4
- pkaN/A
- LogD (pH=7, predicted)1.4
- Solubility (experiment)Slightly soluble
- LogS (predicted, ACD/Labs)(ph=7)-2.63
- LogSw (predicted, AB/LogsW2.0)0.96
- Sw (mg/ml) (predicted, ACD/Labs)0.69
- No.of HBond Donors3
- No.of HBond Acceptors6
- No.of Rotatable Bonds3
- TPSA82.53
- StatusFDA approved
- AdministrationN/A
- PharmacologyA drug used to treat hairy cell leukemia (leukemic reticuloendotheliosis) and multiple sclerosis.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability43.0
- Protein binding20.0
- Volume of distribution (VD)9.2 to 12.7 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmCladribine is extensively distributed after intravenous administration and undergoes metabolism in cells containing deoxycytidine kinase activity to form 2-chloro-2′-deoxyadenosine-5′-triphosphate. Other metabolites include, 5′-monophosphate and 2-chloroadenine (CAde), the major metabolite identified in plasma.
- Half life3~22 h
- ExcretionAbout 21 to 32% of an intravenous dose is excreted unchanged in urine within 24 h with 1.5% as CAde. After oral administration, 25% of the dose is excreted in urine with 3.8% the metabolite, CAde.
- Urinary ExcretionN/A
- ClerancePlasma clearance, approx. 26 to 45 L/h/m2; mean, 1.44 L/h/kg.
- ToxicityCladribine has considerable bone marrow toxicity (haemopoietic stem cell toxicity). In a phase I study, patients were administered with doses >0.26 mg/kg daily for 10 to 14 days. Both renal and central nervous system toxicity was observed, with some patients requiring haemodialysis due to severity of toxicity. Toxicity was not observed with doses of 0.9 mg/kg daily for 7 days. [E. Beutler,Lancet,1992, 340, 952–956].
- LD50 (rat)N/A
- LD50 (mouse)N/A