- Molecular NameAnagrelide
- SynonymAnagrelide HCL; Anagrelide Hydrochloride; BL-4162A
- Weight256.092
- Drugbank_IDDB00261
- ACS_NO68475-42-3
- Show 2D model
- LogP (experiment)2.333
- LogP (predicted, AB/LogP v2.0)1.84
- pkaN/A
- LogD (pH=7, predicted)1.83
- Solubility (experiment)Very slightly soluble
- LogS (predicted, ACD/Labs)(ph=7)-3.3
- LogSw (predicted, AB/LogsW2.0)0.01
- Sw (mg/ml) (predicted, ACD/Labs)0.13
- No.of HBond Donors1
- No.of HBond Acceptors4
- No.of Rotatable Bonds0
- TPSA44.7
- StatusFDA approved
- AdministrationN/A
- PharmacologyA drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia). It also has been used in the treatment of chronic myeloid leukemia.
- Absorption_value70.0
- Absorption (description)Anagrelide is rapidly absorbed after oral administration (minimum 75%) and is extensively metabolised.
- Caco_2N/A
- Bioavailability75.0
- Protein bindingN/A
- Volume of distribution (VD)12 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- Metabollsmtensive, with 1% recovered unchanged in the urine. Metabolized primarily in the liver by cytochrome P450 1A2 (CYP1A2).
- Half life1.3 h (fasting state); 1.8 h (dose administered with food)
- ExcretionIt is excreted mainly in urine (70 to 75% over 5 days) and in faeces (10%). Less than 1% of the dose is excreted unchanged. It is extensively distributed.
- Urinary ExcretionN/A
- Clerance9 L/h.
- ToxicityCardiac and CNS toxicity can be expected with overdose. It may also cause fetotoxicity and renal failure. Doses greater than 5 mg daily can lead to hypotension.
- LD50 (rat)N/A
- LD50 (mouse)N/A