Anagrelide
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| Systematic (IUPAC) name | |
|---|---|
| 6,7-dichloro-1,5-dihydroimidazo (2,1-b)quinazolin-2(3H)-one |
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| Identifiers | |
| CAS number | 68475-42-3 |
| ATC code | L01XX35 |
| PubChem | 2182 |
| DrugBank | APRD00798 |
| ChemSpider | 2097 |
| Chemical data | |
| Formula | C10H7Cl2N3O |
| Mol. mass | 256.088 g/mol |
| SMILES | eMolecules & PubChem |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 1.3 hours |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status |
℞ Prescription only |
| Routes | Oral |
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Anagrelide (Agrylin/Xagrid, Shire) is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia). It also has been used in the treatment of chronic myeloid leukemia. [1]
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[edit] Mechanism
It works by inhibiting the maturation of platelets from megakaryocytes.[2] The exact mechanism of action is unclear, although it is known to be a phosphodiesterase inhibitor.[3] It is a potent (IC50 = 36nM) inhibitor of phosphodiesterase-II.[citation needed]
[edit] Uses
According to a 2005 Medical Research Council randomized trial, the combination of hydroxyurea with aspirin is superior to the combination of anagrelide and aspirin for the initial management of ET. The hydroxyurea arm had a lower likelihood of myelofibrosis, arterial thrombosis, and bleeding, but it had a slightly higher rate of venous thrombosis.[4]
[edit] Side-effects
Common side effects are headache, diarrhea, unusual weakness/fatigue, hair loss, nausea and dizziness.
Less common side effects include: congestive heart failure, myocardial infarction, cardiomyopathy, cardiomegaly, complete heart block, atrial fibrillation, cerebrovascular accident, pericarditis, pulmonary infiltrates, pulmonary fibrosis, pulmonary hypertension, pancreatitis, gastric/duodenal ulceration, renal impairment/failure and seizure.
[edit] References
- ^ Voglová J, Maisnar V, Beránek M, Chrobák L (2006). "[Combination of imatinib and anagrelide in treatment of chronic myeloid leukemia in blastic phase]" (in Czech). Vnitr̆ní lékar̆ství 52 (9): 819–22. PMID 17091608.
- ^ Petrides PE (2006). "Anagrelide: what was new in 2004 and 2005?". Semin. Thromb. Hemost. 32 (4 Pt 2): 399–408. doi:. PMID 16810615.
- ^ PMID 3027338
- ^ Harrison CN, Campbell PJ, Buck G, Wheatley K, East CL, Bareford D, Wilkins BS, van der Walt JD, Reilly JT, Grigg AP, Revell P, Woodcock BE, Green AR; United Kingdom Medical Research Council Primary Thrombocythemia 1 Study. Hydroxyurea compared with anagrelide in high-risk essential thrombocythemia. N Engl J Med 2005;353:33-45. PMID 16000354.
[edit] External links
- Shire Pharmaceuticals Agrylin/Xagrid website for international visitors
- Shire Pharmaceuticals Xagrid website for UK visitors
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