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QuickView for Anagrelide (compound)
PubChem
| Name: | anagrelide |
|---|---|
| PubChem Compound ID: | 2182 |
| Molecular formula: | C10H7Cl2N3O |
| Molecular weight: | 256.088 g/mol |
| Synonyms: |
Imidazo(2,1-b)quinazolin-2(3H)-one, 6,7-dichloro-1,5-dihydro-; Anagrelidum [INN-Latin]; BRN 0619582; 6,7-Dichlor-1,5-dihydroimidazo(2,1-b)chinazolin-2(3H)-on; Anagrelide [INN:BAN]; Anagrelida; 68475-42-3; BL 416201; 6,7-Dichloro-1,5-dihydroimidazo(2,1-b)quinazolin-2(3H)-one; Anagrelida [INN-Spanish].
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DrugBank
Identification
| Name: | anagrelide |
|---|---|
| Name (isomeric): | DB00261 |
| Drug Type: | small molecule |
| Synonyms: |
Anagrelide HCL; BL-4162A; Anagrelide Hydrochloride
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| Brand: | Agrylin, Xagrid |
| Category: | Fibrinolytic Agents, Platelet Aggregation Inhibitors, Antithrombotic Agents |
| CAS number: | 68475-42-3 |
Pharmacology
| Indication: | For the treatment of patients with thrombocythemia, secondary to myeloproliferative disorders, to reduce the elevated platelet count and the risk of thrombosis and to ameliorate associated symptoms including thrombo-hemorrhagic events. |
|---|---|
| Pharmacology: | Anagrelide is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia). It works by inhibiting the maturation of megakaryocytes into platelets. The exact mechanism of action is unclear, although it is known to be a potent (IC50 = 36nM) inhibitor of phosphodiesterase-III. |
| Mechanism of Action: |
The mechanism by which anagrelide reduces blood platelet count is still under investigation. Studies in patients support a hypothesis of dose-related reduction in platelet production resulting from a decrease in megakaryocyte hypermaturation. In blood withdrawn from normal volunteers treated with anagrelide, a disruption was found in the postmitoti...
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| Biotransformation: | Extensive, with < 1% recovered unchanged in the urine. Metabolized primarily in the liver by cytochrome P450 1A2 (CYP1A2). Recently, it was found that anagrelide is bio-transformed in humans into two major metabolites (6,7-dichloro-3-hydroxy-1,5 dihydro-imidazo[2,1-b]quinazolin-2-one (BCH24426) and 2-amino-5,6-dichloro-3,4,-dihydroquinazoline (RL603). Whether these metabolites have biological activities that may underlie the mode of action of the parent drug is presently unclear. |
| Half Life: | At fasting and at a dose of 0.5 mg of anagrelide, the plasma half-life is 1.3 hours. |
| Toxicity: | There are no reports of overdosage with anagrelide, however thrombocytopenia, which can potentially cause bleeding, is expected from overdosage. Single oral doses of anagrelide at 2,500, 1,500 and 200 mg/kg in mice, rats and monkeys, respectively, were not lethal. Symptoms of acute toxicity were: decreased motor activity in mice and rats and softened stools and decreased appetite in monkeys. |
| Affected organisms: | Humans and other mammals |
Interactions
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Targets
Enzymes
